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Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy
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Drugs in endodontics /certified fixed orthodontic courses by Indian dental academy

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The Indian Dental Academy is the Leader in continuing dental education , training dentists in all aspects of dentistry and offering a wide range of dental certified courses in different formats.

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  • 1. Drugs in endodontics and operative dentistry www.indiandentalacademy.com
  • 2. INDIAN DENTAL ACADEMY Leader in continuing dental education www.indiandentalacademy.com www.indiandentalacademy.com
  • 3. CONTENTS  INTRODUCTION  DEFINITIONS  PHARMACODYNAMICS  PHARMACOKINETICS  DRUG NOMENCLATURE  ROUTES OF DRUG ADMINISTRATION www.indiandentalacademy.com
  • 4. ABSORPTION KINETICS OF ELIMINATION FACTORS MODIFYING DRUG ACTION DRUGS IN ENDODONTICS - ANTIANXIETY DRUGS - ANALGESICS * Opioid Analgesics * Non Opioid Analgesics -ANTIBIOTICS IN ENDODONTICS - LOCAL ANAESTHETICS DRUGS IN OPERATIVE DENTISTRY - ANTI SIALOGOUGES - STYPTICS - DESENSITIZING AGENTS  www.indiandentalacademy.com
  • 5. Introduction www.indiandentalacademy.com
  • 6. What is Pharmacology? - the study of how drugs effect a biological system What is a drug? - any chemical agent which effects any biological process WHO 1966, “Drug is any substance or product that is used or intended to be used to modify or explore physiological systems or pathological states for the benefit of the recipient” www.indiandentalacademy.com
  • 7. What is Pharmacology ? The study of how drugs effect biological systems Pharmacokinetics What the body does to drug Pharmacodynamics What the drug does to body Pharmacology Pharmacotherapeutics The study of the use of drugs Pharmacocognosy Identifying crude materials as drugs Toxicology www.indiandentalacademy.com
  • 8. Pharmacodynamics What the drug does to the body Physiological and biochemical effects of drug and their mechanism of action at organ system or subcellular or macromolecular level Ex- adrenaline-adrenoreceptors- G-protein mediated cell membrane bound adenyl cyclase-intracellular 3,5 AMP-cardiac stimulation-hepatic glycogenolysishyperglycemia  www.indiandentalacademy.com
  • 9. Pharmacodynamics Dose response curve…... www.indiandentalacademy.com
  • 10. Pharmacokinetics What the body does to the drug  Movement of the drug in and alteration of the drug by the body; includes absorption, distribution, binding or localization or storage, biotransformation and excretion of the drug.  Pharmacodynamic agents  Chemotherapeutic agents www.indiandentalacademy.com
  • 11. Pharmacokinetics What the body does to the drug t1/2 (Half-Life) - the time required for the plasma concentration of a drug to be reduced by 50% ED50 (effective dose) - The dose of a drug that is effective for 50% of the population exposed to the drug LD50 (lethal dose) - the dose at which death occurs in 50% of subjects www.indiandentalacademy.com
  • 12. Drug Nomenclature *Chemical name- propranolol 1-(isopropylamino)-3-(1-naphthyloxy) propranolol *Nonproprietary name competent scientific body- USAN, BAN Ex-Meperidine (USA) & Pethidine( UK, India) *Proprietary name ( Brand name) accepted by manufacturer & is his property or trademark Ex- Atenolol ALTOL, ATECOR, BETACARD, ATEN, ATCARDIL, ATEN, LONOL, TENOLOL, TENORMIN www.indiandentalacademy.com
  • 13. Routes of Drug Administration I) LOCAL ROUTES 1) Topical 2) Deeper tissues 3) Arterial supply II) SYSTEMIC ROUTES 1) Oral 2) Sublingual or buccal 3) Rectal 4) Cutaneous 5) Inhalation 6) Nasal 7) Parenteral - subcutaneous - Intramascular - intravenous - intradermal injection www.indiandentalacademy.com
  • 14. Oral absorption (enteral route) Advantages 1) safe, convenient, economical 2)Self medication 3)drug withdrawl Disadvantages 1)Slow onset 2) Bitter taste 3) Nausea and vomitting 4) Inactivated by gastric enzymes 5) Not possible in unconscious patient Enteric coated pills and tablets- cellulose acetate or gluten cant destoy by acid juice of stomach, alkaline intestinal juice removes the coatings www.indiandentalacademy.com
  • 15. Parenteral route Routes of administration other than oral route termed as parenteral Advantages 1)Absorption rapid & quick 2) Accurate dose can be given 3) Drug enters in active form to circulation 4) Useful in emergency 5) Useful in unconscious patient Disadvantages 1) pain on injection 2) abscess and inflammation at the site of injection 3) sterile procedure required for injection 4) expensive 5) self medication is not possible  www.indiandentalacademy.com
  • 16. Anti anxiety drugs  Anxiety- it is an emotional state, unpleasant in nature, associated with uneasiness, discomfort and concern or fear about some defined or undefined future threat. www.indiandentalacademy.com
  • 17.  Antianxiety- these are ill defined group of mild CNS depressants which are aimed to control the symptoms of anxiety, produce a restful state of mind without interfering with normal mental or physical functions.  Sedatives- the drug that subdues the excitement and calms the subject without inducing sleep though drowsiness may be produced  Hypnotic- a drug that induces and or maintains sleep similar to normal arousable sleep www.indiandentalacademy.com
  • 18. Oral benzodiazepines  Classification- www.indiandentalacademy.com
  • 19. Pharmacological actions  Preparation-1960  Pharmacodynamics- 1) 2) 3) 4) 5) 6) Antianxiety Sedative-hypnotic Anticonvulsant Amnesic Skeletal muscle relaxant Induce anterograde amnesia Mechanism of action-facilitates inhibitory action of gamma aminobutyric acid (GABA) www.indiandentalacademy.com
  • 20.    With short half lives- 10-20 hrs (Triazolam at 2.6 to 4 hrs) With long half lives (lorazepam 10-20 hrs) 50 hrs or more to eliminate Bzd biotransformed in the liver to active metabolite have the potential for a long duration of action ADVERSE REACTIONSse Few n mild Excessive CNS depression Drowsiness Somnolence Decreased motor coordination, Impaired intellectual functions other are - CNS depressant synergism - Release of anxiety bound hostility - acute overdosage - excerberation of porphyria  www.indiandentalacademy.com
  • 21. PSYCHIC AND PHYSICAL DEPENDENCE - Tremor, anorexia, sweating, agitation, and insomnia - Tachycardia, hypertension, visual, tactile, auditory or gustatory hallucinations - paresthesias, photophobia, Abdominal muscular pain depersonization and psychosis BENZODIAZEPINE WIHDRAWL 1) Drug taken longer then 4 months 2) Higher doses have been used 3) Drug stopped suddenly 4) Short acting BZD has been used DRUG INTERACTIONS Cimetidine, Ranitidine, increase blood levels of triazolam and midazolam possibly decreasing their liver metabolism rates All CNS depressants are synergistic with BZD for respiratory depression CONTRAINDICATIONS 1) Allergic patients 2) Narrow angle glaucoma 3) Porphyrism THERAPEUTIC USES www.indiandentalacademy.com
  • 22. Non benzodiazepine anxiolytic  - BUSPIRONE Devoid of hypnotic, anticonvulsant, or muscle relaxant properties. not involve GABA ergic neurons Equieffective to diazepam Not effect automobile driving performace Adverse effects Dizzinesss Headache Insomnia GIT upset www.indiandentalacademy.com
  • 23. Benzodiazepine antagonists Flumazenil -competetive antagonist of BZD receptor used to reverse BZD induced CNS depression -commonly given IV also well absorbed orally -Eliminaion half life is 1 hr i.e. less than midazolam and less than diazepam or its metabolite- Rebound CNS depression  ADVERSE EFFECTS -Nausea and vomitting -physical abstinence syndrome Dose- 0.2 mg IV followed by 0.1 to 0.2 mgmin until patient awakens for BZD overdose antagonism www.indiandentalacademy.com
  • 24. Pharmacology of pain Two components of pain -Pain perception, and Pain reaction Pain perception is the reasonably objective component of the pain phenomenon  Pain reaction is the emotional response to the percieved injury and its painful manifestation www.indiandentalacademy.com
  • 25.  Analgesics-relieve pain without loss of consciouness Opiates-products obtained from opium poppy Opioid analgesics- naturally occuring, semisynthetic and synthetic drugs which have a morphine like action i.e relief of pain and depression of CNS Narcotic analgesics-old term for opioid analgesics www.indiandentalacademy.com
  • 26. OPIUM  Dried latex from the seed capsules of certain types of poppy (Papaver somniferum).  Psychological have been recognized for over 6000 years.  Name derived from the Greek name for juice.  First undisputed reference to “poppy juice” dates to Greek medicine, 300 B.C.  In the 18th century, the drinking of “Laudanum” was socially acceptable in Europe, particularly among the artistic in-crowd.  Mid-19th century, the use of pure alkaloids began to prevail over the use of the cruder opium. www.indiandentalacademy.com
  • 27. Classification 1.Natural opium alkaloids - Morphine, Codeine 2.Semisynthetic opiates - Diacetylmorphine(Heroin), Pholcodeine many others like- Hydromorphone, Oxymorphone, Hydrocodeine, Oxycodone, are not used in India 3. Synthetic opioids- Pethidine, Fentanyl, Methadone, Dextroprpxyphene, Tramadol, Ethoheptazine www.indiandentalacademy.com
  • 28. Morphine *Source- natural opium alkaloid milky exudate of unripe capsules of poppy plant, papaver somniferum a) Phenanthrene group- Morphine, Codeine and Thebaine. b) Benzylisoquinoline group- Papaverine, Noscapine, Narcine www.indiandentalacademy.com
  • 29. Pharmacological actions  1) Analgesia- visceral, pain of trauma - elevates pain threshold - alters emotional reaction to pain - produce sleep which also elevates threshold 2) CNS- euphoria- dysphoria- sleep 3) Respiration- depression 4) Pupil- miosis 5) Emetic action- stimulates and inhibits 6) Antitussive effect-suppress 7) ADH secretion-decrease urinary output 8) GIT- decreases peristalitic propulsive movement-spasm-increases water absorption- dry feces- constipation 9) Biliary tract- spasm of sphincter of oddi-increase intrabiliary pressure 10) Other smooth musclesIncreases tone of detrusor muscle, vesicle spehincter contracted increases tone of ureter and decreases its peristalisis constriction of bronchi www.indiandentalacademy.com
  • 30. 11) CVS- hypotension at toxic dose Absorption, fate and excretionPreparation and dose 1. tincture opium – 0.3 to 2 ml by mouth 2. morphine sulphate3. morphine hydrochloride 8 to 20 mg by mouth or by injection Adverse reactions 1.Dysphoria, mental clouding 2.Nausea, vomiting, rashes 3. Tremor, delirium, and skin rashes 4. acute morphine poisoning- resp. depression, pin point pupil, cyanosis, reduced body temp, hypotension, shock and coma 5. Depression of foetal respiration 6. Tolerance and drug dpendenance Therapeutic uses 1.analgesic 2. sedation and slep 3. pre-anaesthetic medication 4. acute LVF 5. Diarrhoeae www.indiandentalacademy.com 6. As antitussive
  • 31. Other opioid analgesics *Codeine: phenanthrene alkaloid, antitussive - less potent to morphine - spasmogenic effect, nausea,vomitting, miosis, addiction are less *Papaverine: benzylisoquinoline alkaloid - predominant relaxant on smooth muscles *Noscapine: benzylisoquinoline, antitussive *Heroin (DiacetylMorphine); semisynthetic, more potent than morphine because it produce euphoria, capable of producing severe addiction *Apomorphine: semisynthetic, emetic *pethidine; synthetic -analgesic - spasmogenic on smooth muscle, and sphincter - nausea and vomitting - sedation and euphoria - respiratry depression does not produce miosis and antitussive effect as is produced by morphine Adverse reactions; 1. local irritation on parenteral administration 2. dry mouth, nausea,and vomitting www.indiandentalacademy.com
  • 32. 3. Euphoria, dysphoria, and vomitting 4. depression of foetal respiration 5. resp. depression, coma,convulsion 6. addiction and tolerance Preparation and dose 1.pethindine hydrochloride tablets- 25 to 100 mg 2. pethidine hydrochloride injection- 25 to 100 mg by sc, im, and 25 to 50 mg by iv Methadone synthetic, analgesic, resp depressant, emetic, antitussive, constipating and biliary action similar to morphine - used in opioid dependence mechanism www.indiandentalacademy.com
  • 33. OPIOID RECEPTORS  inhibition of neurotransmission via presynaptic and postsynaptic actions  coupled to guanine nucleotide-binding regulatory proteins (Gproteins) www.indiandentalacademy.com
  • 34. Narcotic Analgesics in Dentistry  opioids used in dentistry are primarily those used for oral administration such as codeine, hydrocodone, oxycodone, and pentazocine.  employed exclusively for pain relief  opioid drugs are NOT anti-inflammatory and much of the pain produced by dental procedures is due to inflammation. Therefore, antiinflammatory drugs such as aspirin, ibuprofen, etc. should be used first to relieve pain - then move to opioids if pain relief is not sufficient.  combinations of opioids such as codeine and aspirin or acetaminophen are commonly employed e.g Oxycodone (related to codeine - but 6-fold more potent) (Percocet -- contains acetaminophen) (Percodan www.indiandentalacademy.com -- contains ASA)   
  • 35. Comments related to use of narcotic analgesics in dentistry  DRUG INTERACTIONS  other CNS depressants will increase the degree of respiratory depression with opioids  opioids and phenothiazines produce at least additive CNS depression. This combination may also increase orthostatic hypotension, as can opioids and tricyclic antidepressants.  respiratory acidosis caused by large doses of opioid agonists may increase entry of local anaesthetics into the CNS  well documented interaction between meperidine and MAO inhibitors severe and immediate reactions - include excitation, rigidity, hypertension, and sometimes death. www.indiandentalacademy.com
  • 36. CLASSIFICATION (Acc. to Tripathi) A. Analgesic and antiinflammatory : Salicylates Aspirin, Salicylamide, Benorylate, Diflunisal Pyrazolone derivatives Phenylbutazone, oxyphenbutazone Indole derivatives Indomethacin, sulindac Propionic acid derivatives Ibuprofen,Naproxen, Ketoprofen, Fenoprofen, Flurbiprofen. Anthranilic acid derivative Mephenamic acid Aryl-acetic acid derivatives Diclofenac, Tolmetin Oxicam derivatives Piroxicam, Tenoxicam, Meloxicam. Pyrrolo-pyrrole derivative Ketorolac. Sulfonanilide derivative NImesulide Alkanones www.indiandentalacademy.com Nabumetone
  • 37. B. Analgesic but poor antiinflammatory: Paraaminophenol derivative Paracetamol (Acetaminophen) Pyrazolone derivatives Metamizol (Dipyrone), propiphenazone Benzoxazocine derivative Nefopam Acc. to Goodman and Gillman A. Non selective Cox inhibitor Salicylic acid derivatives Aspirin, sodium salicylate, choline magnesium trisalicylate, salsalate, diflunisal, salfasalazine, olsalazine. Para amino derivatives Acetaminophen Indole & indene acetic acid Indomethacin, sulindac Heteroaryl acetic acid Tolmetin, diclofenac, www.indiandentalacademy.com ketorolac.
  • 38. Aryl propionic acid Ibuprofen, naproxen, flurbiprofen, ketoprofen, fenoprofen, oxaproxin. Anthranilic acid (fenamates) Enolic acid Mefenamic acid, meclofenamic acid Oxicams (piroxicam, Meloxicam) Alkanones Nabumetone. B. Selective cox-2 inhibitor Diaryl substituted furanones Diaryl substituted Pyrazoles Indole acetic acid Sulfonanilides Rofecoxib Celecoxib Etodolac Nimesulide www.indiandentalacademy.com
  • 39. MECHANISM OF ACTION Odontogenic pain Noxious stimuli Disease process + Surgical intervention Acute pain Tissue destruction or injury Cellular destruction Release / synthesis of histamine / prostaglandin / bradykinin + Peripheral nociceptor / free nerve endings PAIN www.indiandentalacademy.com
  • 40. Beneficial actions due to PG Synthesis inhibition  Analgesia  Antipyresis  Antiinflammatory  Antithrombotic  Closure of ductus arteriosus Shared toxicities due to PG synthesis inhibition  Gastric mucosal damage  Bleeding  Limitation of renal blood flow  Delay / prolongation of labour  Asthma & anaphylactoid reactions www.indiandentalacademy.com
  • 41. COMMON PROPERTIES OF ALL NSAIDS Analgesia Anaphylactoid reactions Antipyresis Antiinflammatory Renal effects Dysmenorrhoea Gastric mucosal damage Parturition Ductus arteriosus closure www.indiandentalacademy.com Antiplatelet aggregatory
  • 42. SALICYLATES Aspirin (prototype) Pharmacological actions • Analgesic (0.3-1.5 g/day) • Antipyretic • Respiration • GIT • Antiinflammatory (3-6 g/day or 100mg/kg/day) • Immunological effect • Uricosuric effect • CVS • Blood • Endocrines  <2g/day  • Metabolic effect 2-5 g/day • Local actions  > 5g/day www.indiandentalacademy.com
  • 43. Pharmacokinetics  80% bound to plasma proteins.  Volume distribution 0.17 L/kg.  Plasma t ½ = 15-20 min.  Release salicylic acid (t ½) = 3-5 hrs.  Antiinflammatory doses (t ½) = 8-12 hrs. (30 hrs in poisoning) www.indiandentalacademy.com
  • 44. Adverse effects Salicylism : dizziness, tinnitus, vertigo, reversible impairment of hearing & vision, excitement & mental confusion, hyperventilation & electrolyte imbalance. www.indiandentalacademy.com Acute salicylate poisoning : fatal dose-15-30g , > 50 mg/dl.
  • 45. Contraindications :  Sensitivity, peptic ulcers, bleeding tendency, chicken pox or influenza.  Chronic liver disease  Diabetics, low cardiac reserve or frank CHF, juvenile rheumatoid arthritis. Precautions :  Stopped 1 week before elective surgery.  During pregnancy  Avoided by breast feeding mothers.  G-6-PD deficient individuals www.indiandentalacademy.com
  • 46. Interactions :  Warfarin, naproxen, sulfonylureas, phenytoin and methotrexate.  Oral anticoagulants.  Uric acid  Probenecid  Methotrexate.  Furosemide and thiazides  Spironolactone. www.indiandentalacademy.com  Protein bound iodine levels.
  • 47. Uses : Patent ductus arteriosus Analgesic Pregnancy induced hypertension and preeclampsia Antipyretic Acute rheumatic fever (4-6 g) Postmyocardial infarction & poststroke patients Delay labour Rheumatoid arthritis (3-5 g) Osteoarthritis www.indiandentalacademy.com * Aspirin, dispirin, colosprin
  • 48. PYRAZOLONES Phenylbutazone Pharmacokinetics  98% bound to plasma proteins.  Plasma t ½ = 60 hrs.  Dose 100-200 mg BD/TDS Adverse effects  Bone marrow depression  Agranulocytosis  Stevens-Johnson syndrome www.indiandentalacademy.com
  • 49. PYRAZOLONES Phenylbutazone Pharmacokinetics  98% bound to plasma proteins.  Plasma t ½ = 60 hrs.  Dose 100-200 mg BD/TDS Adverse effects  Bone marrow depression  Agranulocytosis  Stevens-Johnson syndrome www.indiandentalacademy.com
  • 50. Interactions :  Sulfonamides, tolbutamide, imipramine & methotrexate warfarin,  Anticoagulants  Phenytoin & tolbutamide P L Uses : Rheumatic fever Severe cases Acute gout Ankylosing spondylitis Zolandin www.indiandentalacademy.com Rheumatoid arthritis
  • 51. Sioril, phenabid  Oxyphenbutazone  Metamizol (Dipyrone) : 0.5-1.5 g Analgin, novalgin  Propiphenazone : 300-600 mg TDS Saridon, anafebrin INDOLE DERIVATIVES Indomethacin Pharmacokinetics  90% bound to plasma proteins.  Plasma t ½ = 2-5 hrs.  Dose 25-50mg BD/QID www.indiandentalacademy.com
  • 52. Adverse effects Interactions :  Furosemide  Thiazides, furosemide, β blockers, ACE inhibitors  Warfarin www.indiandentalacademy.com
  • 53. Uses : P L Psoriatic arthritis Rheumatoid arthritis Ankylosing spondylitis Acute gout Malignancy asso. fever Acu. Exa. destructive arthropathies Patent ductus arteriosus closure (0.1/0.2 mg/kg/12 hrly Indicin, indocap www.indiandentalacademy.com
  • 54. PROPIONIC ACID DERIVATIVES Pharmacokinetics  90-99% bound to plasma proteins. Drug Plasma t ½ Ibuprofen Naproxen 2 hr 12-16 hr Ketoprofen Fenoprofen 2-3 hr 2-4 hr Dosage 400-800 mg TDS Brufen, emflam 250 mg BD/TDS Xenobid, naxid 100 mg BD/TDS Ketofen 300-600 mg TDS Arflur www.indiandentalacademy.com Flurbiprofen 4-6 hr 50 mg BD/QID Flurofen
  • 55. Adverse effects Interactions :  Anticoagulants  Furosemide, thiazides & β blockers www.indiandentalacademy.com
  • 56. Uses : Antipyretic Analgesic Dysmenorrhoea ANTHRANILIC ACID DERIVATIVE (Fenamate) Mephenamic acid Pharmacokinetics  Highly bound to plasma proteins.  Plasma t ½ = 2-4 hrs  250-500 mg TDS www.indiandentalacademy.com
  • 57. Adverse effects L Uses : Osteoarthritis Analgesic Rheumatoid arthritis Dysmenorrhoea www.indiandentalacademy.com Medol, meftal, ponstan
  • 58. ARYL-ACETIC ACID DERIVATIVES Diclofenac sodium : Pharmacokinetics  99% bound to plasma proteins.  Plasma t ½ = 2 hrs  50 mg TDS/BD, 75 mg i.m. Adverse effects www.indiandentalacademy.com
  • 59. Uses : Ankylosing spondylitis Osteoarthritis Rheumatoid arthritis Bursitis Dysmenorrhoea Post-traumatic / post-op inflammatory condition Voveran, diclonac, movonac Tolmetin : 400-600 mg TDS www.indiandentalacademy.com
  • 60. OXICAM DERIVATIVES Piroxicam Pharmacokinetics  99% bound to plasma proteins.  Plasma t ½ = 2 days  20 mg BD / 20 mg OD Adverse effects www.indiandentalacademy.com
  • 61. Uses : P L Ankylosing spondylitis Osteoarthritis Rheumatoid arthritis Dysmenorrhoea Dentistry Acute gout Episiotomy Musculoskeletal injuries Dolonex, pirox, piricam, toldin Tenoxicam : 20 mg OD Meloxicam : 7.5-15 mg/day (rheumatoid & osteo-arthritis) www.indiandentalacademy.com www.indiandentalacademy.com Melflam, Meloxi
  • 62. PYRROLO-PYRROLE DERIVATIVE Ketorolac : Pharmacokinetics  Highly bound to plasma proteins.  Plasma t ½ = 5-7 hrs  10-20 mg / 6 hrly (orally) Adverse effects www.indiandentalacademy.com
  • 63. Uses : Renal colic Bony metastasis Migraine Post-op / acute musculoskeletal pain (15-30 mg i.m. / 4-6 hrs Ketorol, torolac SULFONANILIDE DERIVATIVE Nimesulide : Pharmacokinetics  99% bound to plasma proteins.  Plasma t ½ = 2-5 hrs  100 mg BD www.indiandentalacademy.com
  • 64. Adverse effects Uses : Sports injuries Dental surgery ENT disorders Bursitis Low backache Dysmenorrhoea Post-op www.indiandentalacademy.com pain/osteoarthritis Nimulid, nimodol
  • 65. PARA-AMINO PHENOL DERIVATIVES • Phenacetin 1887 • Paracetamol (acetaminophen) 1950 Actions Pharmacokinetics  1/3 bound to plasma proteins.  Plasma t ½ = 2-3 hrs  3-5 hrs (orally)  0.5-1g TDS  Infants - 50 mg  Children 1-3 yrs- 80-160 mg 4-8 yrs 240-320 mg www.indiandentalacademy.com 9-12 yrs 300-600 mg
  • 66. Adverse effects Analgesic nephropathy Acute paracetamol poisoning  150 mg/kg  Fatality > 250 mg/kg  Early manifestations / 12-18 hrs / 2 days www.indiandentalacademy.com
  • 67.  Mechanism of toxicity  Treatment – • Gastric lavage • N-acetylcysteine 150 mg/kg / i.v./ 15 min / 20 hrs • 75 mg/kg / orally / 4-6 hrs / 2-3 days Uses : ‘Over the counter’ analgesic Antipyretic Dysmenorrhoea Musculoskeletal pain Crocin, metacin, paracin www.indiandentalacademy.com
  • 68. BENZOXAZOCINE DERIVATIVE Nefopam 30-60 mg TDS oral 20 mg i.m. 6 hrly Nefomax CHOICE OF NSAIDS • Mild to moderate pain – paracetamol, ibuprofen • Acute musculoskeletal, osteoarthritic, injury associated inflammation – ibuprofen, diclofenac, piroxicam • Post-op / acute / short lasting painful condition – ketorolac, nefopam www.indiandentalacademy.com
  • 69. • Exacerbation of rheumatoid arthritis, ankylosing spondylitis, acute gout, acute rheumatic fever – aspirin, indomethacin, naproxen, piroxicam • Asthma or anaphylactoid reactions to aspirin – nimesulide www.indiandentalacademy.com
  • 70. Analgesics after certain endodontic procedures www.indiandentalacademy.com
  • 71. PAIN MANAGEMENT STRATEGY D 3 iagnosis efinitive Rx rugs Definitive treatment : Drug : •Pulpotomy, pulpectomy •Pretreat with NSAIDs •Extraction •Prescribe by clock •Incision & drainage •Long acting LA •Flexible prescription plan www.indiandentalacademy.com
  • 72. Flexible analgesic prescription plan Mild pain Aspirin like drugs indicated Ibuprofen 200 mg Moderate pain NSAIDs (alone max.effective dose) OR NSAID + acetaminophen Aspirin like drugs contra indicated Acetaminophen 600-1000mg Acetaminophen 600-1000 mg + codine 60 mg Ibuprofen 400 mg/4 hrly and equivalent of acetaminophen 600 mg / codine 60 mg 4 hrly Severe pain NSAID (max. dose) & Acetaminophen 1000 mg with acetaminophen / oxycodone equivalent of oxycodone 10 www.indiandentalacademy.com 10 mg combination mg
  • 73. ADVANCES Selective cox-2 inhibitors : Celecoxib, rofecoxib, valdecoxib, etoricoxib, meloxicam, diisopropyl flurophosphate. Action Celecoxib P© L© Use-osteoarthritis, rheumatoid arthritis Dose – 200 mg / day OD or 100 mg BD. Commercial names – Celebrex, Celib, Celfast, Celact etc. Banned – July 2001 Rofecoxib P© L© Dose – 12.5 mg OD (max. dose 25 mg) Commercial name – Vioxx, Dolib MD, Roff, Rofaday www.indiandentalacademy.com Banned – September 2004
  • 74. Valdecoxib Dose – 10-20 mg OD Commercial name – Valed, Valus, Vorth, Bextra Banned –7 April 2005. Other drugs banned by FDA  Benoxaprofen  Phynylbutazone  Oxyphenbutazone  Saprofen  Piroxicam www.indiandentalacademy.com
  • 75. ANTIBIOTICS www.indiandentalacademy.com
  • 76. Antimicrobial agent : substances that will suppress the growth / multiplication of microorganisms. antimicrobial agents may be antibacterial, antiviral / antifungal. Antibacterial agent : substances that destroy or suppress the growth / multiplication of bacteria. They are classified as antibiotic or synthetic agents. Antibiotic agent : against life (greek-anti means against and biosis means life). Chemical substances produced by microorganisms that have the capacity in dilute solutions, to produce antimicrobial action. www.indiandentalacademy.com
  • 77. Principles of appropriate antibiotic use : 1. Presence of infection : If a patient has infection. • Local signs and symptoms • Systemic signs and symptoms • Other disease conditions having some of the same signs and symptoms. 2. State of host defenses : • Final outcome of a bacterial insult. • It is important to understand that infections are ultimately cured by the host, NOT by antibiotics. • Antibiotics can only help • Control of infection www.indiandentalacademy.com
  • 78. 3. Surgical Drainage and incision : •Treatment of deep tissue infections – surgical drainage •If unreleased – vascularity of the tissue and prevents host defense substance for getting to the area. •Odontogenic infection 4. The decision to use antibiotic therapy : •Intact host defenses may not require antibiotic therapy. •Severe conditions can be treated. •In all instances of infection. www.indiandentalacademy.com
  • 79. PRINCIPLES FOR CHOOSING THE APPROPRIATE ANTIBIOTIC 1) Identification of the causative organism : Isolated from pus, blood or tissue. Situations in which cultures should be done are a) The patient has received treatment for 3 days without improvement. b) Infection is a postoperative wound infection. c) Recurrent infection d) Actinomycosis is suspected www.indiandentalacademy.com e) Osteomyelitis is present
  • 80. 2. Determination of antibiotic sensitivity : Not responded to initial antibiotic therapy. Antibiotic sensitivity can be done by 2 methods : 1) Disc –diffusion method (Kibby-Bauer) 2) Agar-or broth dilution tests www.indiandentalacademy.com
  • 81. 3. Use of specific, Narrow spectrum antibiotic : Narrowest antibacterial spectrum should be chosen. Penicillin, a cephalosporin and a tetracycline. Penicillin should be used There are 2 reasons for this : i) Specific narrow-spectrum antibiotics frequently are more effective against specific groups of susceptible microorganisms than are broad-spectrum agents. ii) Narrow spectrum antibiotics produce less alteration of the normal microflora, thereby reducing the incidence of superinfection. www.indiandentalacademy.com
  • 82. 4. Use of a least toxic antibiotic : • Antibiotics are utilized to kill living bacteria, also kill or injure human cells. • Antibiotics can be highly toxic. • Odontogenic infections sensitive chloramphenicol. www.indiandentalacademy.com to penicillin and
  • 83. 5. Use of a bactericidal rather than a bacteriostatic drug : • Bacteriostatic drugs exert their influence by inhibiting growth and reproduction of the bacteria, usually by inhibiting protein synthesis. Growth is slowed, the host defenses can now cure the infection. The advantages of bactericidal drugs are : a) Less reliance on host resistance. b) Antibiotic itself kills the bacteria. c) Works faster than bacteriostatic drugs d) There is greater flexibility with dosage intervals. e) To kill all pathogens. 6. Use of the antibiotic with a proven history of success : • • Penicillin has a proven track recorded. www.indiandentalacademy.com
  • 84. Choice of newer drug should be made only when : • Effective against bacteria, against which no other AMA is effective. • More active at lower concentration • Less toxic / less severe side effects • Less expensive. Because : • The drug fails to reach it’s target. • The drug is inactivated • The target is altered (Davies 1994; Nikaido, 1994: Spratt, 1994) 7. Cost of the antibiotic : • It is difficult to place a price tag on health. • Surgeon should consider the cost of the antibiotic. • Parenteral antibiotics given in the hospital cost more. www.indiandentalacademy.com
  • 85. PRINCIPLES OF ANTIBIOTIC ADMINISTRATION 1) Proper dose : • Peak concentration should be 3 to 4 times. Eg : cephalexin vs penicillinase 2) Proper time interval : • Plasma half-life • Dosage interval therapeutic use is 4 times • At 5 times 95% of the drug has been excreted. Eg : Cefazolin www.indiandentalacademy.com
  • 86. 3) Proper route of administration : • Parentral administration will produce the necessary serum level of antibiotics. • Oral route also results in the most variable absorption. • For maximum absorption is taken in fasting stage. 4) Consistency in regard to route of administration : • When treating a serious, established infections, parenteral antibiotic therapy is frequently the method of choice. • Discontinue the parenteral route immediately and start the oral route. • Important to maintain peak blood levels. • Antibiotic has been given for 5 or 6 days. • Switching from the parenteral to the oral route on the 2 nd or 3rd www.indiandentalacademy.com day of antibiotic therapy, recurrence of the infection is more likely.
  • 87. 5) Combination antibiotic therapy : The rationale for the use of 2 or more drugs together is to minimize • the emergence of antibiotic resistant microorganisms • to increase the certainty of a successful clinical outcome • to treat mixed bacterial infections • to prevent suprainfection • to treat severe infections of unknown etiology • www.indiandentalacademy.com to decrease toxicity without decreasing efficacy
  • 88. Examples : 1) Isoniazid + ethambutol + streptomycin in treatment of tuberculosis. With one exception, combinations of antibiotics are not used in the dental office. The exception is use of penicillin G + streptomycin before dental procedures in patients at high risk of developing bacterial endocarditis. Rules : 1) 2 bactericidal drugs produce, supraadditive effects, not antagonism. 2) The combination of a bacteriostatic and a bactericidal drug generally results in diminished effects. www.indiandentalacademy.com 3) 2 bacteriostatic drugs are never inhibitory.
  • 89. Results : 1) Indifference when the effect is equal to the single most active drug or equal to the arithematic sum of the two use is not justified. 2) Antagonism : when the combined drug effect is less than the algebric sum of the effects on the individual drugs in the mixture. Bactericidal drugs require dividing organisms without an intact cell wall ; bacteriostatic drugs inhibit cell replication. The end result is that there are less number of bacteria available for bactericidal drug. 3) Synergism : ability of two antibiotics acting together to markedly increases the rate of bactericidal action compared to either drug alone. www.indiandentalacademy.com
  • 90. Disadvantages : i) Adds nothing to therapeutic efficacy and may even reduce it (antagonism). ii) Increase antibiotic toxicity and allergy. iii) Increase the likelihood of superinfection iv) Discourages specific etiologic diagnosis and promote false security. v) Encourage inadequate doses, particularly with fixed dose combination therapy. vi) Increased cost vii) Emergence of resistant bacterial strains viii)Increase the environmental spread of antibiotic resistant www.indiandentalacademy.com bacteria.
  • 91. MONITORING THE PATIENT 1. Response to treatment : • Noticeable response first 24 to 48 hours. • If the end of the 3rd day, no improvement is noted, the patient must be carefully reevaluated. Several questions should be considered : a) Have the route of administration and the dose of the antibiotic been adequate ? b) Is the patient taking the antibiotic as prescribed ? c) Have the physician’s orders on the chart been understood and carried out ? d) Was the initial choice of the antibiotic correct ? many of times, the combination of SURGICAL and NATURAL www.indiandentalacademy.com HOST DEFENSES has resulted in resolution of the infection.
  • 92. CAUSES OF FAILURE IN TREATMENT OF INFECTION : • Inadequate surgical treatment • Depressed host defenses • Presence of foreign body • Antibiotic problems - Drug not reaching infection - Dose not adequate - Wrong bacterial diagnosis - Wrong antibiotic www.indiandentalacademy.com
  • 93. 2. Development of adverse reactions : • Adverse reactions occur all too commonly. • 15 to 20 percent of hospitalized patients receiving antibiotics experience and adverse reactions. • Hypersensitivity (type I) reactions occur with all antibiotics – penicillins and cephalosporins • Less severe reactions – edema, urticaria and itching are delayed reactions. • Anaphylactic reactions is not difficult, but treatment must be rapid and intense. • Treatment is to discontinue the causative antibiotic, restore fluid and electrolyte balance. • The usual choice is oral vancomycin, but metronidazole may www.indiandentalacademy.com be used also.
  • 94. 3. Superinfection and recurrent infection : • During treatment normal host bacteria that are susceptible to the drugs are eliminated. • In the normal state, these bacteria live in peaceful coexistence with the host and by their physical presence prevent bacteria capable of producing disease from growing in large numbers. • The normal flora acts as a defense mechanisms, but when the indigenous flora is altered, the pathogenic bacteria resistant to an antibiotic may cause a secondary infection, or SUPERINFECTION. • Example is of CANDIDIASIS with the use of PENICILLIN, which eliminates the gram-positive cocci (seen after long term www.indiandentalacademy.com high dose penicillin therapy).
  • 95. PROPHYLACTIC ANTIBIOTICS Advantages : • Prevention of infection • Decreased patient morbidity • Decreased patient mortality • Decreased hospital stay • Decreased medical costs • Decreased total antibiotic usage • Decreased number of resistant bacteria www.indiandentalacademy.com
  • 96. Disadvantages : 1) No reduction of infection, despite prophylaxis 2) Development of increased number of resistant bacteria 3) Delayed onset of infection 4) Adverse effect on surgical technique Note : Effective is a short-term administration of a narrowspectrum antibiotic. www.indiandentalacademy.com
  • 97. Principles for the use of prophylactic antibiotics : 1) Operative procedure must have a risk of significant bacterial contamination and a high incidence of infection. 2) The organism most likely to cause the infection must be known. 3) The antibiotic susceptibility of the causative organism must be known. 4) To be effective and to minimize adverse effects, the antibiotic must be in the tissue at the time of contamination (operation), and it must be continued for no more than 4 hours after cessation of contamination. 5) The drugs must be given in dosages sufficient to reach 4 times or MIC of thewww.indiandentalacademy.com causative organisms.
  • 98. CLASSIFICATION OF ANTIMICROBIAL DRUGS A) Mechanism of action : 1. Inhibit cell wall synthesis • Penicillins • Cephalosporins • Vancomycin • Bacitracin 2. Cause leakage from cell membranes • Polypeptides – Polymyxins, colistin, Bacitracin • Polyenes – Amphotericin B, Nystatin www.indiandentalacademy.com
  • 99. 3. Inhibit protein synthesis • Tetracyclines • Chloramphenicol • Erthromycin, • Clindamycin • Linezolid 3. Cause misreading of m-RNA code and affect permeability • Aminoglycosides o Streptomycin o Gentamicin www.indiandentalacademy.com
  • 100. 5. Inhibit DNA gyrase • Fluoroquinolones – Ciprofloxacin 5. Interfere with DNA function • Rifampin • Metronidozole 5. Interfere with DNA synthesis • Idoxuridine • Acyclovir • Zidovudine 5. Interfere with intermediary metabolism Sulfonamides Sulfones PAS www.indiandentalacademy.com Ethambutol
  • 101. B) Chemical structure 1. Sulfonamides and related drugs • Sulfadiazine and others • Sulfones – Dapsone (DDS), Paraaminosalicylic acid (PAS). 2. Diaminopyrimidines • Trimethoprim • Pyrimethamine 3. Quinolones • Nalidixic acid • Norfloxacin • www.indiandentalacademy.com Ciprofloxacin etc
  • 102. 4. β-lactam antibiotics • Penicillins • Cephalosporins • Monobactams • Carbapenems 4. Tetracyclines • Oxytetracycline • Doxycycline etc 4. Nitrobenzene derivative • Chloramphenicol www.indiandentalacademy.com
  • 103. 7. Aminoglycosides • Streptomycin • Gentamicin • Neomycin etc 7. Macrolide antibiotics • Erythromycin • Roxithromycin • Azithromycin etc 7. Polypeptide antibiotics • Polymyxin-B • Colistin • Bacitracin • Tyrothricin www.indiandentalacademy.com
  • 104. 10. Glycopeptides • Vancomycin • Teicoplanin 10. Oxazolidinone • Linezolid 10. Nitrofuran derivatives • Nitrofurantoin • Furazolidone 10. Nitroimidozoles • Metronidozole • Tinidazole www.indiandentalacademy.com
  • 105. 14. Nicotinic acid derivatives • Isoniazid • Pyrazinamide • Ethionamide 14. Polyene antibiotics • Nystatin • Amphotericin-B • Hamycin 14. Azole derivatives • Miconazole • Clotrimazole • Ketoconazole • fluconazole www.indiandentalacademy.com
  • 106. 17. Others • Rifampin • Lincomycin • Clindamycin • Spectinomycin • Sod. fusidate • Cycloserine • Viomycin • Ethambutol • Thiacetazone • Clofazimine • Griseofulvin www.indiandentalacademy.com
  • 107. C) Type of organisms against which primarily active 1. Antibacterial • Penicillins • Aminoglycosides • Erythromycin etc 2. Antifungal • Griseofulvin • Amphotericin B • Ketoconazole 3. Antiviral • Idoxuridine • Acyclovir • Amantadine • Zidovudine etc www.indiandentalacademy.com
  • 108. 4. Antiprotozoal • Chloroquine • Pyrimethamine • Metronidazole • Diloxanide etc 4. Anthelmintic • Mebendazole • Pyrantel • Niclosamide • Diethyl carbamazine etc www.indiandentalacademy.com
  • 109. D) Spectrum of activity 1. Narrow spectrum • Penicillin G • Streptomycin • Erythromycin 2. Broad spectrum • Tetracyclines • Chloramphenicol www.indiandentalacademy.com
  • 110. E) Type of action 1. Primarily bacteriostatic 2. Primarily bactericidal • Sulfonamides • Penicillins • Tetracyclines • Aminoglycosides • Chloramphenicol • Polypeptides • Erythromycin • Rifampin • Ethambutol • Cotrimoxazole • Cephalosporins • Vancomycin • Nalidixic acid • Ciprofloxacin www.indiandentalacademy.com
  • 111. F) Antibiotics are obtained from 1. Fungi 3. Actinomycetes • Pencillin • Aminoglycosides • Cephalosporin • Tetracyclines • Griseofulvin • Chloramphenicol • Macrolides • Polyenes 2. Bacteria • Polymyxin B • Colistin • Bacitracin • Tyrothricin • Aztreonam www.indiandentalacademy.com
  • 112. Misconception about antibiotics        Improper choice- drug, dosage, duration of therapy Ignorance of Microbial biology Antibiotics- “safe & do no harm” Antibiotics prophylaxis commonly successful To mask poor surgical procedure “ I don’t know what else to do syndrome” Malpractice negligence suit www.indiandentalacademy.com
  • 113. Myths in antibiotic theapy        I. Antibiotic cure patients II. Antibiotics are substitute for surgical drainage III. The most important decision is which antibiotic use IV. Antibiotic therapy is a science and not an art V. Culture and sensitivity are required VI. Antibiotics increase host defence to infection VII. Multiple antibiotics are superior to a single antibiotic www.indiandentalacademy.com
  • 114.       VIII. Antibiotic prophylaxis is usually effective IX. Bactericidal agents are always superior to bacteriostatic agent X. Antimicrobial are effective in chronic infectious diseases XI. Antibiotics are safe and nontoxic XII. Antibiotic dosage are established for most infections XIII. Infection require a complete course of therapy www.indiandentalacademy.com
  • 115. BETA LACTAM ANTIBIOTICS Pencillins Most important antibiotics first extracted from the mould PENICILLIUM NOTATUM First used in 1941 clinically and was a miracle drug with a least toxic effect. www.indiandentalacademy.com
  • 116. CLASSIFICATION OF PENICILLINS 1. Natural penicillin • Penicillin G (benzyle penicillin) • Procaine penicillin G • Benzathine penicillin G 2. Acid resistant penicillin • Phenoxymethyl penicillin (pencillin V) • Phenoxyethylpenicillin (phenethecillin) 3. Penicillianse – resistant penicillins • Acid labile – methecillin, nafcillin, cloxacillin, dicloxacillin • Acid resistant – flucloxacillin www.indiandentalacademy.com
  • 117. 4. Penicillins effective against gram positive and some gramnegative organisms • Ampecillin • Ampoxycillin • Talampicillin 4. Extended spectrum penicillins • Carboxypenicillins – carbenicillin, ticarcillin • Ureidopencillins – piperacillin, mezlocillin • Amidino pencillins – mecillinam, pivmecillinam 4. Penicillins with betalactamase inhibitors • Amoxycillin – clavulanic acid (Augmentin) • www.indiandentalacademy.com Ticarcillin – clavulanic acid (Timentin)
  • 118. BENZYL PENICILLIN (PENCILLIN G) • PnG is a narrow spectrum antibiotic; activity is limited primarily to gram positive bacteria • Is available in the form of water soluble sodium and potassium salts • This salts in a dry state are stable at room temperature for years. The aqueous solution however requires refrigeration and deteriorates considerably with in 72 hours. Antibactrial activity • Most potent AMA, inhibits the growth of susceptible organism. • Mainly gram +ve, gram –ve cocci and some gram +ve bacilli with exception of enterococci. • Cocci – Highly sensitive – Streptococci, Pneumococci, Staph. aureus, N. gonorrhoeae, N. meningitis • Bacilli – B. anthracis, Corynebacterium diphtheriae, clostridium tetany and spirocheteswww.indiandentalacademy.com • Actinomyces israelii is moderately sensitive
  • 119. Mechanism of action : • Bactericidal drug effective mainly against multiplying organisms. • Pencilline requires cell wall that contains peptidoglycans. • Peptidoglycan is heteropolymeric component of cell wall provides rigid mechanical, crosslinked lattice like structure. • Penicillin binding to this proteins are bacterial enzymes on the cell wall are responsible for synthesis and cross linkage of peptidoglycans in the cell wall. • Penicillins bind to these proteins and inactivate them, thereby preventing the synthesis and cross linkage. • This weakens bacterial cell wall and makes organism vulnerable to damage. • As the cell wall synthesis occurs during the growth phase the antibiotic is more www.indiandentalacademy.com actively multiplying effective against organisms.
  • 120. www.indiandentalacademy.com
  • 121. Absorption fate and excretion : • About 1/3 of drug is activated on oral administration. • Absorbed from the duodenum. • Because of the inadequate absorption the oral dose should be 4/5 times larger than the intramuscular dose. • As food interferes with its absorption PnG should be given orally atleast 30 min after food or 2 to 3 hours before food. • B. Pencillin in aqucous solution is rapidly absorbed after SC or IM administration. • Peak plasma level of 8 to 10 units per ml is reached with in 15 to 30 min and drug disappears from plasma with in 3-6 hours. www.indiandentalacademy.com
  • 122. • Widely distributed in the body and significant amounts appear in liver, bile, kidney, jointfluid and interstine. • PnG is excreted mainly by the kidney but in small part in the bile and other routes. • 50% drug is eliminated in urine with in first hour. Preparation and dose : • PnG inj 0.5-5 MU i.m or i.v 6-12 hours • Procaine pencillin inj 0.5, 1 MU dry powder in vial • Penidure 0.6, 1.2, 2.4 MU as dry powder in vial • Fortifide PP inj 3+1 lac U vial www.indiandentalacademy.com
  • 123. ADVERSE REACTIONS : a) Miscellaneous reactions : • Nausea and vomiting on oral PnG • Sterile inflammatory reaction at the site of IM inj. • Prolonged IV administration may cause thrombophlebitis • Accidental IV administration of procaine PP cause anxiety, mental disturbances paraesthesia and convulsions a) Intolerance : • Major problem with PnG includes anaphylactic and allergic reactions www.indiandentalacademy.com idiosyncratic,
  • 124. c) Other allergic reactions are • Skin rashes • Serum sickness • Renal disturbance • Hemolytic disturbance • Anaphylaxis • Jarisch herxheimer reaction • Super infection • Hyperkalemia • Acute non allergic reaction www.indiandentalacademy.com
  • 125. Uses : PnG is the drug of choice for infections 1. Streptococcal infections 2. Pneumococcal infections 3. Meningococcal infections 4. Gonorrhoea 5. Syphilis 6. Diphtheria 7. Tetanus and gas gangrene 8. Prophylactic uses www.indiandentalacademy.com
  • 126. SEMI SYNTHETIC PENCILLINS The major drawbacks of benzyl pencillin are : 1. Inactivation by the gastric hydrochloric acid 2. Short duration of action 3. Poor penetration into CSF 4. Activity mainly against gram +ve organism 5. Possibility of anaphylaxis Attempts therefore have been made to synthesize pencillin free from such drawbacks. P.chrysogenum produces natural penicillins which produce the 6 amino-penicillanic acid (6-APA) nucleus. The attachment of side chains are inhibited and instead various organic radicals can be substituted. www.indiandentalacademy.com Thus a variety of semisynthetic resins are produced.
  • 127. I) Acid resistant pencillins : 1. Potassium phenoxymethyl penicillin (penicillin V) • Similar antibacterial spectrum like benzylpenicillin. • More active against resistant staphylococci • Less inactivated by the gastric acid. • Plasma levels achieved is 2 to 5 times higher than benzylpenicillin. • 50-70% is bond to plasma proteins. • 25% of drug is eliminated in urine • Available as 60 & 125 mg tablets. • Administered in the dose of 250 –500 mg at 4-8 hours intervals, atleast 30 min before food. • This can be used in less serious infections (pneumocci www.indiandentalacademy.com and streptococci).
  • 128. Dose : infants 60 mg, children 125-250 mg given 6 hourly CRYSTAPEN-V, KAYPEN, PENIVORAL 65, 130, 125, 250 mg tablets 125 mg/5 ml dry ser 2. Potassium phenoxyethyl penicillin and 3. Azidocillin Both have similar properties to penicillin V and no difference in the antibacterial effect www.indiandentalacademy.com
  • 129. II) Pencillinase resistant pencillins : 1. Methicillin 1. Effective in staphylococci 2. It is given IM or IV (slow) in the dose of 1 gm every 4-6 hours. 3. Haematuria, albuminuria and reversible interstitial nephritis are the special adverse effect of methicillin. 2. Cloxacillin 1. Weaker antibacterial activity. 2. Distrubuted thro out the body, but highest s concentration in kidney and liver. 30% excreted in urine. 3. Oral dose for adults 2-4 gm divided into 4 portions children 50-100mg/kg/day. 4. IM adults 2-12 gm/day, children 100-300 mg/kg/day every 4-6 hours. www.indiandentalacademy.com BIOCLOX, KLOX, CLOCILIN 0.25, 0.5 gm cap, 0.5 gm/vial.
  • 130. Oxacillin, Dicloxacillin, Flucloxacillin are other isoxazolyl penicillins, similar to cloxacillin, but not marketed in India. Nafcillin : More active than methicillin and cloxacillin but less active than PnG 80% of drug bonds with plasma proteins excreted by liver in patients with renal failure. Dose is similar to cloxacillin. www.indiandentalacademy.com
  • 131. III) Extended spectrum pencillins : 1. Amino pencillins 1. Ampicillin – • Antibacterial activity is similar to that of PnG that is more effective than PnG against a variety of gram-ve bacteria • Drug is effective against H.influenzae strep.viridans, N.gonorrhea, Salmonella, shigellae, Klebsilla and enterococci. Absorption, fate and excretion : • Oral absorption is incomplete but adequate • Food interferes with absorption • Partly excreted in bile and partly by kidney www.indiandentalacademy.com
  • 132. Dose : 0.5-2 gm oral/IM or IV depending on severity of infection every 6 hours Children : 25-50 mg/kg/day AMPILIN, ROSCILLIAN, BIOCILIN – 250, 500 mg cap 100mg/ml ped drops, 250 mg/ml dry syr, 1 gm/vial inj. USES : • Urinary tract infections • Respiratory tract infections • Meningitis • Gonorrhoea • Typhoid fever • Bacillary dysentry • Septicaemias • www.indiandentalacademy.com
  • 133. Adverse effects : • Diarrhoea is frequent • Skin rashes is more common • Unabsorbed drug irritates lower interstines • Patient with history of hypersensitivity to PnG should not be given ampicillin. www.indiandentalacademy.com
  • 134. AMOXYCILLIN : • This is a semisynthetic penicillin • (amino-p-hydroxy-benzylpencillin) • Antibacterial spectrum is similar to ampicillin but less effective than ampicillin for shigellosis. • Oral absorption is better; food does not interfere; higher and more sustained blood levels are produced. • It is less protein bond and urinary excretion is higher than that of ampicillin. • Incidence of diarrhoea is less www.indiandentalacademy.com
  • 135. Dose : 0.25-1 g TDS oral; AMOXYLIN, NOVAMOX, SYNAMOX, MOX, AMOXIL 250, 500 mg cap, 125 mg/5ml dry syr, 500 mg/vial inj. USES : • Typhoid • Bronchitis • Urinary infection • SBE • Gonorrhoea www.indiandentalacademy.com
  • 136. Carboxy penciillins : The Carboxypenicillins, the Ureidopenicillins and the Amidino penicillins are considered extended spectrum penicillins, because they inhibit a wide variety of aerobic gram-ve bacilli They are ineffective against most strains of staph. Aureus They have following properties : 1. Highly active against anaerobes 2. Most useful in infections caused by other gram-ve rods 3. Act synergistically with amino particularly enterobacteriacea. glycoside antibiotics, 4. Much less active than penicillin G against gram+ve organisms 5. The CNS penetration is about 10% of their serum levels and hence not recommended for the treatment of meningeal www.indiandentalacademy.com infections.
  • 137. CARBENICILLIN • Has similar spectrum as other penicillin • Weaker antibacterial activity than ampicillin • Active against –pseudomonas, proteus • < Salmonella , E coli Enterobacter • Inactive against – klebsiella and gram –ve cocci • Acid labile and has to be given by parenteral route only • Peak plasma level is 2hours and excreted in urine www.indiandentalacademy.com
  • 138. Dose : 1-2g im/iv 4-6hours Adverse effects : • Cause congestive heart failure • Bleeding disorders-impaired platelet function Uses : • Pseudomonas ,burns, UTI and septicemia • PYOPEN,CARBELIN 1g,5g per vial www.indiandentalacademy.com
  • 139. UREIDOPENICILLINS –PIPERACILLIN ( PIPRIL) AMIDINOCILLIN – MECILLINAM Has similar indications of carbenicillin www.indiandentalacademy.com
  • 140. BETA LACTAMASE INHIBITORS •CLAVULANIC ACID •Obtained from STREPTOMYCES CLAVULIGERUS •Betalactam ring – no antibacterial activity •Suicide inhibitor –inactivated after binding to enzyme •Permeates the outer layers of cell wall of gram-ve bacteria www.indiandentalacademy.com
  • 141. Pharmacokinetics : • Oral absorption- rapid • Bioavailability-60% • Distribution similar that of amoxicillin • Excretion-tubular secretion Uses : • Amoxicillin+clavulanic acid (augmentin) • Ticarcillin+clavulanic acid (timentin) • Staph aureus,H influenza, gonorrhoea and E coli www.indiandentalacademy.com
  • 142. Adverse effects : • Poor g.i. tolerance • Hepatotoxicity AUGMENTIN, AMONATE, ENHANCIN • 250+125mg tab 1-2tab TDS • 250+50mg vial im/iv 6-8 hourly www.indiandentalacademy.com
  • 143. SULBACTAM • Semisnythetic betalactamase inhibitor • Related chemically in activity to clavulanic acid • Progressive inhibitor ,highly active against betalactamase • 2-3 times < potent • Oral absorption- inconsistent,preferably im/iv • Sulbactam+ ampicillin=Dicapen • SULBACIN, AMPITUM • 1g+ 0.5g per vial im/iv 6-8hourly www.indiandentalacademy.com
  • 144. Adverse effects : • Pain-thrombophebitis • Rashes and diarrhoea Uses : • Mixed aerobic-anaerobic infections • Gonorrhoea • Skin/soft tissue infections www.indiandentalacademy.com
  • 145. CEPHALOSPORINS Cephalosporium acremonium was the first source. They contain 7 amino cephalosporonic acid nucleus. Structurally they contain betalactam and didhydro thiazine rings. Mechanism of action : Act by inhibiting bacterial cell was synthesis and are bactericidal. New derivatives are much more resistant than the older cephalosporins www.indiandentalacademy.com
  • 146. Classification Classified according to its antibacterial activity. First generation cephalosporin •Good activity against gram +ve bacteria. (except enterococci). •Most oral cavity anaerobes are sensitive. Parental Oral CEPHALOTHIN CEPHALEXIN CEFAZOLIN CEPHRADINE CEFADROXIL www.indiandentalacademy.com
  • 147. Cephalaxin and Cephadroxil : •Useful in treating community acquired, respiratory and urinary tract infections and in surgical prophylaxis. •Not choice for systemic infections. Cefazolin : •For antimicrobial prophylaxis in most surgical procedures. •Given only IM / IV. •Dose: Oral 0.25 - 1g 6-8 hrly Children : 25-100mg/kg/day IM – 0.25g 8 hrly (mild cases) 1g 6 hrly (severe cases). Drops – cephaxin 125mg/5ml syrup. 100mg /ml ped. drops. SPORIDEX, DROXYL CEPHAXIN, CEPHACILLIN, www.indiandentalacademy.com CEFADROX,
  • 148. Second generation cephalosporins : Increased activity against gram –ve organism. More active against anaerobes. Parenteral Oral CEFUROXIME CEFACLOR CEFOXITIN CEFUROXIME AXETIL Cefaclor and cefuroxime axetil retains significant by oral route. More active against H. influenzae, E coli. Dose : 250mg, 125mg, 125mg/5ml syr. and 50 mg /ml ped. drops. KEFLOR, CEFTUM, CEFOGEN, FUROXIL. www.indiandentalacademy.com
  • 149. Third generation cephalosporin : •They highly augmented against gram –ve enterobacter and pseudomonas. •Highly resistant to β-lactamase from gram –ve bacteria. •Less active on gram +ve cocci Parenteral Oral CEFOTAXIME CEFIXIME CEFTIZOXIME CEFDINIR CEFTRIAXONE CEFTIBUTEN CEFTAZIDIME CEFOPERAZONE Dose : 100, 200 mg tab/cap. 100mg/5ml syr., 50mg/ml susp. CESPAN, CEFOPROX, www.indiandentalacademy.com PROCADAX, CEPODEM, ORFIX.
  • 150. Fourth generation cephalosporins : Developed in 1990 similar to that of 3rd generation. Highly resistant to β-lactamases. Active against many bacteria resistant to earlier drugs. It has high potency and extended spectrum. Effective in many serious infections. Parenteral CEFEPINE, CEFPIROME USES : Serious and resistant hospital acquired infections. Septicaemia, Lower respiratory tract infection. Dose : 1-2g IM / IV 12 hrly. www.indiandentalacademy.com CEFROM, CEFORTH – 1g inj.
  • 151. Guiding principle for the use of cephalosporins : •Cephalosporins are expensive and should not be used where an equally effective, alternative antibiotic is available. •None of them is effective against infections by enterococci. •None of them is agent of choice of anaerobic infections. •Except for cefotaxine, ceftriazone, the CNS penetration of cephalosporins is poor. General features of cephalosporins •Most of them given by oral route •IM can cause pain so IV is given. •Mainly excreted by kidney. •Dosage is altered in patients with renal insufficiency. •Most cephalosporins penetrate CSF so useful for the treatment of www.indiandentalacademy.com meningitis.
  • 152. Adverse reactions : • Local reactions – thrombophlebitis (IV) • Allergy – skin rashes • Super infection • Nephrotoxicity • CNS toxicity • Blood toxicity • Intolerance to alcohol • Cross reactivity with penicillin cause pain www.indiandentalacademy.com (IM) and cause
  • 153. Uses : • Alternatives to pencicillins. • RTI, UTI and soft tissue infection • Penicillinase producing staph infection. • Septicaemias. • Surgical prophylaxis • Meningitis, gonorrhoea • Typhoid • Mixed aerobic and anaerobic infections • Infection by odd organism or hospital infections • Prophylactic treatment in neutropenic patients. www.indiandentalacademy.com
  • 154. MACROLIDES They are called macrolides because they contain a many membered lactone ring to which are attached one or more deoxy sugars. Clarithromycin differs from erythromycin only by methylation of the hydroxyl group at the 6 position, and Azithromycin by the addition of a methyl substituted nitrogen atom into the lactone ring. www.indiandentalacademy.com
  • 155. Antibacterial activity :  Narrow spectrum antibiotic  Bacteriostatic but bactericidal at higher conc  Effective against penicillin resistant staphylococci  Active against gram+ve cocci and bacilli Pharmacokinetics :  Erythromycin base - acid labile  Given with enteric coated - incomplete absorption  Its acid stable esters are better absorbed  Widely distributed in body  Metabolised in liver www.indiandentalacademy.com  Excreted through kidney and bile
  • 156. Dose :  Adults 250 - 500mg 6hrly  Children 30 – 60mg/kg/day  Erythromycin base - ERYSAFE 250 mg tab  EROMED - 333mg tab, 125/5ml susp  Erythromycin stearate  ERYTHROCIN – 250,500mg tab 100mg/5ml susp 100mg/ml ped drops www.indiandentalacademy.com
  • 157. Adverse effects :  GIT – epigastric pain  On high doses – hearing impairment  Hypersensitivity reactions – rare Uses :  Substitute for penicillin  Whooping cough  Chancroid  Penicillin resistant infections www.indiandentalacademy.com
  • 158. ROXITHROMYCIN  Semisynthetic - long acting stable macrolide  Antibacterial spectrum similar to erythromycin Dose - 150-300mg BD  Children - 2.5-5mg/kg BD  ROXID, ROXIBID 150,300mg tab  50mg kid tab,150 mg tab www.indiandentalacademy.com
  • 159. AZITHROMYCIN  This differs chemically from other macrolide group in that lactone ring contains nitrogen atom  More active than erythromycin  Less active against gram +ve organisms Pharmacokinetics :  Rapidly absorbed and distributed through out the body  Drug is highly concentrated in cells  Excreted unchanged – bile www.indiandentalacademy.com
  • 160. Uses :  Chlamydial infection  Respiratory infection  Strep and Staph skin and soft tissue infections Doses :  500mg once daily for 3days  Children above 6months 10mg/kg  AZITHRAL 250,500mg 250mg/5ml syr  AZIWIN 100,250,500mg tab 200mg/5ml liq  AZITHRAL 500mgwww.indiandentalacademy.com inj
  • 161. CLINDAMYCIN  It is lincosamide antibiotic having similar action (macrolide 50s)  Semisynthetic derivative of Lincomycin  Bacteriostatic – low conc  Bacteriocidal – high conc  Most active Actinomyces against gram+ve cocci,  Highly active against – anaerobes (B fragilis) Pharmacokinetics :  Oral absorption – good  Distribution – skeletal and soft tissues  Excreted in urine www.indiandentalacademy.com C.diphtheriae,
  • 162. Adverse effects :  Rashes  Urticaria  Abdominal pain  Superinfection  Enterocolitis  Diarrhoea Uses :  Anaerobic and mixed infections Doses : 150-300 mg QID oral ; 200-600mg I.v. 8 hourly DALCAP, CLINCIN, DALCIN, 150, 300 mg cap, 300mg/2ml and 600 mg/4ml inj.www.indiandentalacademy.com
  • 163. TETRACYCLINES  Tetracyclines are napthacene derivatives.  The napthacene nucleus is made up by fusion of 4 partially unsaturated cyclohexane radicals and hence the name tetracyclines.  Tetracyclines are bacteriostatic. www.indiandentalacademy.com
  • 164. On the basis of chronology of development, convenience of description, divided into 3 groups. Group I Group II Tetracycline Demeclocyline Oxytetracycline Methacycline Group III Doxycycline Minocycline Mechanism of action : Tetracyclines are thought to inhibit bacterial protein synthesis by binding to the 30 S bacterial ribosome and preventing the access of aminoacyl tRNA to the acceptor (A) www.indiandentalacademy.com sites on the mRNA ribosome complex.
  • 165. www.indiandentalacademy.com
  • 166. Antimicrobial activity :  Gram+ve and –ve cocci are sensitive  Gram+ve bacilli are inhibited  Entero bactereae are highly resistant  Spirochetes and Borrelia are quite sensitive  All rickettsiae and chlamydiae are highly sensitive Pharmacokinetics :  Incompletely absorbed from GIT  Absorption is impaired by iron or zinc salts[due to chelation of cations]  They cross the placenta and enter fetal circulation and amniotic fluid  Widely distributed in liver ,bone marrow and spleen  They accumulate in dentine and enamel of unerupted teeth  Primarily excreted inwww.indiandentalacademy.com urine through kidney
  • 167. Adverse effects :  GIT-epigastric burning, nausea, vomiting,diarrhoea  Hepatoxicity  Renal toxicity  Effects on teeth-Orthophosphate complex  Thrombophlebitis  Hypersensitivity Reactions  Superinfection  Antianabolic effect www.indiandentalacademy.com
  • 168. Dose :  Tetracycline – 1-2g per day in adults  Children over 8yrs -25 to 50mg /kg daily in 2 to4 divided doses  Doxycyline – 100mg,12hrs first day followed by 100mg once a day  Children over 8yrs – 4-5mg /kg/day divided into 2 equal doses during first 24hrs  TERRAMYCIN, RESTECLIN-250,500mg in10ml vial inj www.indiandentalacademy.com  DOXT, NOVADOX, TETRADOX-100mg cap. cap,50mg/ml
  • 169. Precaution :  Not to be used in pregnancy, lactation and in children  Avoided in patients on diuretics  Used cautiously in renal and hepatic insufficiency  Beyond expiry date should not be used  Do not mix injectable Tc with Pn- inactivation occurs Uses :  Mixed infections  Venereal diseases  Atypical Pneumonia, Cholera, Brucellosis, Plague,Rickettsial infections  Alternate to Pn/Ap, Ciprofloxacin,Azithromycin  Other situations –UTI,amoebiasis, chronic lung disease www.indiandentalacademy.com
  • 170. QUINOLONES  These are entirely synthetic antimicrobials having a quinolone structure that are active primarily against gram – ve bacteria.  These are quinolone antimicrobials having one or more fluorine substitutions. www.indiandentalacademy.com
  • 171. Mechanism of action :  The FQs inhibit the enzyme bacterial DNA gyrase, which nicks double stranded DNA.  The DNA gyrase consists of two A and two B subunits; A subunit carries out nicking of DNA, B subunit introduces –ve supercoils and then a subunit reseals the strands. First generation FQs : Norfloxacin Ofloxacin Ciprofloxacin Pefloxacin Second generation FQs : Lomefloxacin Levofloxacin Sparfloxacin Gatifloxacin Moxifloxacin www.indiandentalacademy.com
  • 172. CIPROFLOXACIN First generation FQ active against a broad range of bacteria especially gram –ve aerobic bacilli. Highly susceptible : E coli, shigella, N meningitis, K pneumoniae, Proteus, H influenza, Enterobacter, V. cholerae, S. typhi, N gonorrhoea. Moderately susceptible : Staph aureus, brucella, M. tuberculosis www.indiandentalacademy.com
  • 173. Microbiological features :  Rapid bactericidal activity and high potency.  Relatively long post antibiotic effect on enterobacteriaceae pseudomonas and staph.  Low frequency of mutational resistance.  Low protective intestinal streptococci and anaerobes are spared.  Active against many β lactam and amino glycoside resistant bacteria.  Less active at acidic pH. Phramocokinetics :  Rapidly absorbed on oral, food delays absorption.  High tissue penetration, concentration in lung sputum, muscle, bone. www.indiandentalacademy.com  Excreted primarily in urine.
  • 174. Adverse effect :  GIT – Nausea, vomiting, bad taste, anorexia, diarrhoea is infrequent.  CNS- Dizziness, headache, restlessness, anxiety, insomnia and seizures are rare.  Skin/hypersensitivity – rashes, pruritis, urticaria.  Tendonitis and tendon rupture Uses :  UTI  Typhoid  Gonorrhoea  Bone, soft tissue, wound infection.  Chancroid  RTI  Bacterial gastroenteritis  Tuberculosis  Meningitis  Gr-ve septicaemias  Prophylaxis  Conjunctivitis www.indiandentalacademy.com
  • 175. CIFRAN, CIPLOX, CIPROBID, CIPROLET 250, 500,750 mg tab, 200mg/100 ml IV infusion 3mg/ml eye drops. NORFLOXACIN  It is less potent than cipro  It attains lower concentration in tissues.  It is metabolized as well as excreted unchanged in urine. USES :  UTI and Genital infections.  Bacterial diarrhoea.  (not recommended for respiratory / any other systemic infection).  NORBACTIN, NORFLOX, UROFLOX www.indiandentalacademy.com  200, 400, 800 mg tab, 3mg/ml eyedrops.
  • 176. OFLOXACIN Intermediate between Cirpro and Nor in activity against Gr-ve bacteria  More potent for Gr +ve organisms  Good activity against chlamydia, alternative drug for nonspecific urethritis and atypical pneumonia.  Inhibits M tuberculosis.  Highly active against M. leprae.  Used in multidrug regimens.  Relatively lipid soluble  Oral bioavailability is high.  Food does not interfere. www.indiandentalacademy.com  Excreted largely unchanged in urine(dose reduced in renal failure)
  • 177. Uses :  Chronic bronchitis, respiratory/ENT infection.  Gonorrhoea  Nongonococcal urethritis.  ZENFLOX, OFLOX  100, 200, 400 mg tab, 200 mg/100IV infusion 5mg/5ml susp. www.indiandentalacademy.com
  • 178. LEVOFLOXACIN  It is levoisomer of ofloxacin having improved activity against strep pneumoniae and some other gram +ve and –ve bacteria.  Anaerobes are moderately susceptible.  Oral bioavailability is nearly 100%  Excreted unchanged and single daily dose is sufficient www.indiandentalacademy.com
  • 179.  Oral and IV doses are similar.  Theophylline, Warfarin, Cyclosporine has been found to remain unchanged during levofloxacin treatment. The primary indication of this is  Community acquired pneumonia  Chronic bronchitis  Sinusitis,  Pyelonephritis and  Soft/skin tissue infection as well.  TAVANIC, GIEVO, 500mg tab, 500 mg/100 ml inj. www.indiandentalacademy.com
  • 180. GATIFLOXACIN Another 2nd generation FQ has excellent activity against strep. Pneumonia and many atypical respiratory pathogens including chlamydia pneumonia and other anaerobes. Uses :  Community acquired pneumonia  Chronic bronchitis.  Upper/lower RTI  UTI and gonorrhoea.  T1/2 is 8 hr www.indiandentalacademy.com
  • 181. Adverse effect :  Tachycardia  CNS effects and swelling over face are other side effects.  It is contraindicated in hypokalemia and other drugs than can prolong QT. Dose :  400 mg on 1 day followed by 200-400 mg OD.  MYGAT, GATIQIN, GAITY  200, 400 mg tab, 400 mg/200 ml inj www.indiandentalacademy.com
  • 182. MOXIFLOXACIN :  It is long acting 2nd generation FQ having high activity against strep pneumonia, other Gr +ve bacteria  Primarily used for pneumonias, bronchitis, sinusitis, and otitis media Side effects : similar to other FQ  CI in patients predisposed to seizures.  MOXIF 400 mg tab,  Dose – 400 mg OD www.indiandentalacademy.com
  • 183. ANTIAMOEBIC AND OTHER ANTIPROTOZOAL DRUGS METRONIDAZOLE :  It is the prototype nitroimidazole and found to be highly active amoebicide. Antiprotozoal activity :  Broad spectrum cidal activity against protozoa and anaerobic bacteria such as B fragilis, Fusobacterium.  Metronidazole is microorganisms. selectively toxic to anaerobic  Metronidazole has been found to inhibit cell mediated www.indiandentalacademy.com immunity and cause radiosensitization.
  • 184. Pharmacokinetics :  Completely absorbed from the small intestine.  Widely distributed in the body  It is metabolized in liver primarily by oxidation and glucuronide conjugation, and  Excreted in urine. Adverse effects : Side effects relatively frequent but mostly not serious,  Anorexia, nausea, metallic taste and abdominal cramps are the most common. www.indiandentalacademy.com
  • 185.  Looseness of stool is occasional,  Headache, glossitis, dryness of mouth, dizziness, rashes and transient neutropenia.  Prolonged administration may cause peripheral neuropathy and CNS effects  Seizures have followed by high doses.  Thrombophebitis of injected vein. Contraindications :  In neurological disease, blood dyscrasias, first trimester of pregnancy, chronic alcoholism. www.indiandentalacademy.com
  • 186. Uses :  Amoebiasis  Giardiasis  Trichomonas vaginitis.  Anaerobic bacterial infections  Pseudomembranous enterocolits.  Ulcerative gingivitis  Helicobacter pylori gastritis/peptic ulcer  Guinea worm infestation.  FLAGYL, METROGYL, METRON, ALDEZOLE 200, 400 mg tab, 200 mg/5ml susp. www.indiandentalacademy.com
  • 187. TINIDAZOLE  It is an equally efficacious congener of metronidazole, similar to it in every way except.  Metabolism is slower.  Incidence of side effects is lower.  Metallic taste, nausea, rashes  TINIBA, TRIDAZOLE, 300, 500, 1000 mg tab, 800 mg/400 ml I.V. www.indiandentalacademy.com
  • 188. Role of antibiotics in endodontics (jr of Dent 26 (2001) 539-48) I ENDODONTICS AND THERAPEUTIC ANTIBIOTICS 1) Adjunct to operative treatment 2) Contingency treatment 3) Antibiotics at Obturation 4) Antibiotics for perio-endo lesion 5) which antibiotic II TOPICAL ANTIBIOTICS AND ENDODONTICS 1) Pulpitis 2) Pulp capping 3) Root canal therapy 4) Flare- ups 5) Perio endo lesion 6) Tooth avulsion www.indiandentalacademy.com III ANTIBIOTIC PROPHYLAXIS AND ENDODONTICS
  • 189. What are local anesthetics?  Local anesthetic: are agents which block conduction impulses in nerves. When applied locally, they produce loss of sensation in the desired area. www.indiandentalacademy.com
  • 190. Classification INJECTABLE Low potency, short duration Procaine Chloroprocaine Intermediate potency and duration Lidocaine (Lignocaine) Prilocaine High potency, long duration Tetracaine Bupivacaine Ropivacaine Dibucaine  SURFACE ANAESTHETIC Soluble Cocaine Lidocaine Tetracine Insoluble Benzocaine Butylaminobenzoate Oxyethazine www.indiandentalacademy.com
  • 191. History       Coca leaves from the genus Erythroxylum Erythroxylum contains high concentration of alkaloid up to 0.7-1.8% Alkaloid has natural nitrogen bases found in the coca leaves, also known as cocaine Genus Erythroxylum discovered in South America, Venezuela, Bolivia, and Peru since pre-Columbian periods Earliest cultivation and use of the coca leaf went back to about 700 BC in Bolivia and Andes regions New discoveries showed humans used coca more than 5,000 years ago in Ecuador www.indiandentalacademy.com
  • 192. History (cont.)     Spanish conquistadors and explorers witnessed the consumption of coca in South America Spaniards, such as Alfred Buhler, hypothesized a tribe in the Negro River area called Arhuaco was the original discoverers of the properties and functions of the drugs. In 1571, Pedro Pizarro, a conquistador of Inca, observed nobles and high rank officials of the Inca empire consumed the coca plant. After the fall of the Inca empire, coca consumption spread widely to the population www.indiandentalacademy.com
  • 193. Cocaine Addiction      More physicians began to do research of cocaine in the clinic trials. The physician Sigmund Freud used the stimulant effect of cocaine to treat the morphine addiction in patients An ophthalmologist Carl Koller realized the importance of the alkaloid’s anesthetic effect on mucous membranes In 1884, he used the first local anesthetic on a patient with glaucoma Freud, Halsted, and Koller became addicted to the drug through self-experimentation www.indiandentalacademy.com
  • 194. Side Effects of Cocaine and Solutions Minor:  Addiction  Intoxication Severe:  Death Solutions:  Used nitrous oxide gases and ether for minor surgery in dentistry  Give a low concentration of cocaine; it slows down the release of the drug into the bloodstream causing little side effects www.indiandentalacademy.com
  • 195. Procaine replaced cocaine   In 1898, Professor Heinrich Braun introduced procaine as the first derivative of cocaine, also known as the first synthetic local anesthetic drug Trade name is Novocaine® Novocaine Problems Took too long to set (i.e. to produce the desired anesthetic result)  Wore off too quickly, not nearly as potent as cocaine  Classified as an ester; esters have high potential to cause allergic reactions  Caused high conc. of adrenaline resulted in increasing heart rate, make people feel nervous Most dentists preferred not to used any local anesthetic at all that time; they used nitrous oxide gas. Today, procaine is not even available for dental procedures.  www.indiandentalacademy.com
  • 196. Lidocaine       In 1940, the first modern local anesthetic agent was lidocaine, trade name Xylocaine® It developed as a derivative of xylidine Lidocaine relieves pain during the dental surgeries Belongs to the amide class, cause little allergenic reaction; it’s hypoallergenic Sets on quickly and produces a desired anesthesia effect for several hours It’s accepted broadly as the local anesthetic in United States today www.indiandentalacademy.com
  • 197. Differences of Esters and Amides All local anesthetics are weak bases. Chemical structure of local anesthetics have an amine group on one end connect to an aromatic ring on the other and an amine group on the right side. The amine end is hydrophilic (soluble in water), and the aromatic end is lipophilic (soluble in lipids)  Two classes of local anesthetics are amino amides and amino esters. Amides: Esters: --Amide link b/t intermediate --Ester link b/t intermediate chain and chain and aromatic ring aromatic ring --Metabolized in liver and very --Metabolized in plasma through soluble in the solution pseudocholinesterases and not stable in the solution --Cause allergic reactions  www.indiandentalacademy.com
  • 198. Structures of Amides and Esters    The amine end is hydrophilic (soluble in water), anesthetic molecule dissolve in water in which it is delivered from the dentist’s syringe into the patient’s tissue. It’s also responsible for the solution to remain on either side of the nerve membrane. The aromatic end is lipophilic (soluble in lipids). Because nerve cell is made of lipid bilayer it is possible for anesthetic molecule to penetrate through the nerve membrane. The trick the anesthetic molecule must play is getting from one side of the membrane to the other. www.indiandentalacademy.com
  • 199. Mechanism      The mechanism of local anesthetics connects with the ion channels, nerve, and depolarization. Local anesthetics block the conduction in peripheral nerves that inhibited the nerve to excited and created anesthesia. The anesthetic is a reversible reaction. It binds and activates the sodium channels. The sodium influx through these channels and depolarizes the nerve cell membranes. It also created high impulses along the way. As a result, the nerve loses depolarization and the capacity to create the impulse, the patient loses sensation in the area supplied by the nerve. www.indiandentalacademy.com
  • 200. Factors Affect the Reaction of Local Anesthetics Lipid solubility     All local anesthetics have weak bases. Increasing the lipid solubility leads to faster nerve penetration, block sodium channels, and speed up the onset of action. The more tightly local anesthetics bind to the protein, the longer the duration of onset action. Local anesthetics have two forms, ionized and nonionized. The nonionized form can cross the nerve membranes and block the sodium channels. So, the more nonionized presented, the faster the onset action. pH influence  Usually at range 7.6 – 8.9  Decrease in pH shifts equilibrium toward the ionized form, delaying the onset action.  Lower pH, solution more acidic, gives slower onset of action www.indiandentalacademy.com
  • 201. Factors Affect the Reaction of Local Anesthetics (cont.) Vasodilation  Vasoconstrictor is a substance used to keep the anesthetic solution in place at a longer period and prolongs the action of the drug  vasoconstrictor delays the absorption which slows down the absorption into the bloodstream  Lower vasodilator activity of a local anesthetic leads to a slower absorption and longer duration of action  Vasoconstrictor used the naturally hormone called epinephrine (adrenaline). Epinephrine decreases vasodilator. Side effects of epinephrine  Epinephrine circulates the heart, causes the heart beat stronger and faster, and makes people feel nervous. www.indiandentalacademy.com
  • 202. Toxicity Toxicity is the peak circulation levels of local anesthetics  Levels of local anesthetic concentration administered to patients are varied according to age, weight, and health.  Maximum dose for an individual is usually between 70mg to 500mg  The amount of dose also varied based on the type of solution used and the presence of vasoconstrictor Example: ---For adult whose weight is 150lbs and up, maximum dose Articaine and lidocaine is about 500mg ---For children, the dosage reduced to about 1/3 to ½ depending on their weight. The doses are not considered lethal.  Some common toxic effects: --light headedness ---shivering or twitching --hypotension (low blood pressure) --numbness www.indiandentalacademy.com --seizures
  • 203. Factors of circulation levels      Factors of circulation levels are the rates of absorption, distribution, and metabolism. Absorption depends on the speed of administration and levels of the doses. Distribution allows absorption to occur in three phases. First, the drug occurs at highly vascular tissues in the lungs and kidneys. Then it appears less in vascular muscle and fat. Then the drug is metabolized. Metabolism involves in the chemical structure based on two classes, amide and ester as discussed earlier. Decreasing the potential toxicity resulted in rapid metabolism. www.indiandentalacademy.com
  • 204. Three special drugs used in dental anesthesia  Bupivicaine (Marcaine® --Produce very long acting anesthetic effect to delay the post operative pain from the surgery for as long as possible --0.5% solution with vasoconstrictor --toxicity showed by the pKa is very basic --Onset time is longer than other drugs b/c most of the radicals (about 80%) bind to sodium channel proteins effectively --most toxic local anesthetic drug  Prilocaine (Citanest®) --Identical pKa and same conc. with lidocaine --Almost same duration as lidocaine --Less toxic in higher doses than lidocaine b/c small vasodilatory activity  Articaine (Septocaine®) --newest local anesthetic drug approved by FDA in 2000 --Same pKa and toxicity as lidocaine, but its half life is less than about ¼ of lidocaine --Used with vasoconstrictor. --Enters blood barrier smoothly --The drug is widely used in most nations today www.indiandentalacademy.com
  • 205. Conclusion Anesthetic pKa Onset Duration (with Epinephrine) in minutes Max Dose (with Epinephrine) Procaine 9.1 Slow 45 - 90 8mg/kg – 10mg/kg Lidocaine 7.9 Rapid 120 - 240 4.5mg/kg – 7mg/kg Bupivacaine 8.1 Slow 4 hours – 8 hours 2.5mg/kg – 3mg/kg Prilocaine 7.9 Medium 90 - 360 5mg/kg – 7.5mg/kg Articaine 7.8 Rapid 140 - 270 4.0mg/kg – 7mg/kg www.indiandentalacademy.com
  • 206. Antimuscarinic drugs  Natural alkaloids (and derivatives)    Synthetic quaternary ammonium drugs     Atropine (Sal-Tropine) Scopolamine (Scopace, Transderm-Scop) Glycopyrrolate (Robinul) Propantheline (Pro-Banthine) Ipratropium (Atrovent) Other synthetic drugs   Benztropine (Cogentin) Tolterodine (Detrol) www.indiandentalacademy.com
  • 207. Pharmacologic effects: atropine as a prototype Dose (mg) Effects 0.5 Slight cardiac slowing; some dryness of mouth; inhibition of sweating 1.0 Dryness of mouth; thirst, mild tachycardia; mild pupillary dilation 2.0 Tachycardia; palpitation; marked dryness of mouth; dilated pupils; some blurring of vision 5.0 All above more marked; difficulty in speaking, swallowing; headache; fatigue; dry, hot skin; urinary, GI inhibition 10+ All above more marked; ataxia; www.indiandentalacademy.com excitement; delirium; coma
  • 208. Therapeutic uses Antisialogogues for dentistry Drug Dose (mg) Atropine sulfate 0.4-1.2 (Sal-Tropine) Scopolamine HBr 0.4-0.8 (Scopace) Glycopyrrolate 1-2 (Robinul) Propantheline Br 7.5-30 (Pro-Banthine) www.indiandentalacademy.com Onset time 0.5-1 hr 0.5-1 hr 0.5-0.75 hr 0.5-0.75 hr
  • 209. Therapeutic uses (cont.)          Bradycardia: atropine Ocular examination: topical antimuscarinics Bronchial asthma: ipratropium aerosol GI hyperactivity: numerous antimuscarinics Hyperactive urinary bladder: tolterodine Meniere’s disease: scopolamine Motion sickness: scopolamine Parkinson’s disease: benztropine, others Anticholinesterase poisoning: atropine www.indiandentalacademy.com
  • 210. Clinical considerations  Contraindications/precautions     Angle-closure glaucoma Obstructive or paralytic GI or GU disease Myasthenia gravis Common adverse effects      Xerostomia Hyperthermia in children Tachycardia with atropine Sedation/confusion with scopolamine Mydriasis, cycloplegia www.indiandentalacademy.com
  • 211. Hemostatic Agents  Local measures  Dressings - Dentoalveolar surgery: pressure with sterile cotton gauze > soft tissue bleeding: clamping with hemostats, ligation, electrocautery, or application of microfibrillar collagen or collagen sheets > bleeding from bone structure: a collagen plug or gelatin sponge may be inserted within the extraction socket www.indiandentalacademy.com
  • 212. Hemostatic Agents (con’t)  Clotting factors - topically applied thrombin, NOT INTRAVENOUSLY (Severe thrombosis and death may occur). - fibrin glue  Astringents and styptics: Used in our restorative clinic for bleeding control prior to impressions and placements of subgingival restorations. Mechanism of action: denatures blood and tissue proteins, which then agglutinate and form plugs that occlude the capillary orifices. -Nephrostat-active ingredient is 25% aluminum chloride -Viscostat-active ingredient is 20% ferric sulfate www.indiandentalacademy.com
  • 213. Hemostatic agents (cont’d)  • Vasoconstrictor - epinephrine (epinephrine solution and dry cotton pellets impregnated with racemic epinephrine are available for topical application) - tetrahydrozoline (0.5%) and oxymetazoline (0.5%) Systemic measures  Platelet disorders (patients with a platelet count of less than 50,000/mm3 are at risk for surgical or other trauma) - platelet transfusion - aspirin therapy precaution: pts. On aspirin therapy should consult with their physician regarding reducing or discontinuing use 4-7 days prior to surgery. www.indiandentalacademy.com
  • 214. Desensitizing agents         Fluorides Silver nitrate Strontium chloride Formalin Sodium monoflurophosphate Sodium silicofluoride Calcium hypophosphate Corticosteroids www.indiandentalacademy.com
  • 215.           Calcium hydroxide Zinc chloride Sodium sulphate + barium chloride Sodium carbonate + calcium chloride Sodium fluoride & Iontophoresis Sodium citrate Potassium nitrate Stannous fluoride Potassium oxalate Glutaraldehyde www.indiandentalacademy.com
  • 216. CONCLUSION www.indiandentalacademy.com
  • 217. Thank you www.indiandentalacademy.com Leader in continuing dental education

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