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ANTICHOLINERGICS

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ANTICHOLINERGICS

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ANTICHOLINERGICS

  1. 1. Dr Anu Chandran FINAL YEAR PG DEPARTMENT OF PHARMACOLOGY
  2. 2.  Cholinergic receptors Receptor ? Cholinoreceptor Nicotinic receptor Muscarinic receptor
  3. 3.  Classification
  4. 4. 1. Anti muscarinic 2. Anti nicotinic
  5. 5.  1.NATURAL ALKALOIDS  Atropine  Hyoscine 1.ANTI MUSCARINIC DRUGS
  6. 6.  Atropine Scopolamine Atropine prototype drug Source---Atropa belladona (deadly night shade) Datura stramonium NATURAL ALKALOIDS
  7. 7. GUESS? BELLADONNAATROPOS History Linnaeus – Atropa belladona
  8. 8.  NATURAL ALKALOIDS Atropa belladona Hyocyamus niger Solanaceae family
  9. 9.  ACTIONS CNS Overall stimulant action. low doses restricted entry into the brain. High dose .- •stimulates many medullary centers vagal, respiratory & vasоmotor.
  10. 10. •Antimotion sickness property : ↓vestib excitation •suppresses tremor & rigidity in parkinsonism. •High doses cause cortical excitation, restlessness, disorientation, hallucinations & delirium followed by resp depression & coma.
  11. 11.  CVS Heart SA node-Block M2-Tachycardia AV node-↓refractoryperiod↑conduction PR interval shortened Blood vessel No consistent effect Cutaneous Vasodiln--Atropine flush
  12. 12.  EYE Mydriasis Dryness ↑IOT Abolition of light reflex Photophobia Blurring of near vision
  13. 13.  SMOOTH MUSCLE Relaxant GIT ↓ tone ,amplitude of peristaltic contraction-Constipation Mild antispasmodic-Gallbladder, bileduct Urinary tract ↓Tone , amplitude of contractions of ureter,bladder—Urinary retention
  14. 14.  Smooth muscle--- Respiratory  Broncho dilation,decrease in airway resistance Depress mucociliary clearance
  15. 15.  GLANDS Decrease secretions Salivary Sweat Bronchial Lacrimal Gastric
  16. 16. Comparison- Atropine Hyoscine Source Atropa belladona Datura stromonium Hyoscyamus niger Ester of tropic acid Tropine scopine Duration long short CNS Excitation Depression
  17. 17.  Atropine (pk)  Duration of action - to 8 hours except in the eyes (72 hours or longer)  Dose -0.5 mg to 1 mg  Metabolism -40% liver,  Excretion -60% un changed in the urineJune 16 23Dr. Med. Khaled Radaideh
  18. 18.  USES OF ATROPINE Counteract brady cardia& partial heart block Myocardial infarction Digitalis toxicity Secific antidote in anticholineesterase poisoning,early mushroom poisoning Atropine 2mg i/v every 10 min till signs of atropinisation appear
  19. 19.  USES-ATROPINE -- Mydriatic Preanaesthetic medication
  20. 20.  CONTRA INDICATIONS Narrow Iridocorneal angle ppt Acute Congestive Glaucoma Elderly males with Prostatic Hypertrophy Urinary retention may occur
  21. 21.  Belladona poisoning Consumption of seeds& berries Children more susceptible Drug overdose
  22. 22. Gen.exmn-dry mouth,hot flushed skin Eyes- dilated pupil,photophobia,blurring near vision CVS tachycardia,hypotension,weak pulse GIT decreased bowel sounds,constipation UT difficuilty in micturition CNS psycotic behaviour,ataxia,delirium,visual hallucn,respdepression,covulsion,coma Dry as bone,blind as bat ,red as beet,mad as hatter BELLADONA POISONING
  23. 23.   Homatropine  Atropine Methonitrate  Hyoscine Butylbromide  Ipratropium Br  Tiotropium Br 2.SEMISYNTHETIC
  24. 24.   Mydratics Anti sec – antispasmodics Vasicoselective Antiparkinsonian 3.SYNTHETIC
  25. 25.  ANTISPASMODIC  Intestinalcolic,Renalcolic,biliarycolic,  Abdominal cramps in dysentry,diarrhoea dysmenorrhoea  Dicyclomine  Propantheline  Oxyphenonium  Pipenzolate  Hyoscine butyl bromide
  26. 26. SYNTHETIC Antispasmodics Quaternary compds Propantheline Oxyphenonium Clidinium Pipenzolate Glycopyrrolate Tertiary compds Dicyclomine Valethamate Pirenzepine Vasicoselective Oxybutynin Flavoxate Tolterodine Antiparkinsonian Benzhexol Procyclidine Biperidin Mydratics Tropicamide Cyclopentolate
  27. 27.  COPD &ASTHMA Ipratropium,Tiotropium  Broncho dilation(additive with adrenergics) No impairment of muco ciliary clearance Acute attack of asthma –Ipratropium nebulised with salbutamol
  28. 28.  ANTISECRETORY Atropine,Hyoscine,Glycopyrrolate Preanasthetic medication  ↓ salivary,tracheobronchial secretions  prevent laryngospasm  Vasovagal attacks in anasthesia ↓ Peptic ulcer  ↓ gastric secretion  Atropine,Pirenzepine
  29. 29.  VASICOSELECTIVE Oxybutynin,Tolterodine,Darifenacin Trospium,Flavoxate  Relax smooth muscle of ureters &bladder  Improve bladder capacity,↓involuntary voiding Decrease pain USE Neurogenic bladder Detrusor instability,urinary incompetence Nocturnal enuresis
  30. 30.  ANTISPASMODIC Intestinalcolic,Renalcolic,biliarycolic, Abdominal cramps in dysentry,diarrhoea dysmenorrhoea  Dicyclomine  Propantheline  Oxyphenonium  Pipenzolate  Hyoscine butyl bromide
  31. 31.  Ganglion blockers NMJ BLOCKERS ANTINICOTINIC DRUG
  32. 32.  Hexamethonium (3,5,6 MP) pentolinium Mecamylamine Pempidine Trimethaphan( monosulphan ) Ganglion blockers
  33. 33.  SLOW IV Ultra short acting Uses a. hypertension (dissecting aortic aneurysm) b. hypertensive emergency c. Autonomic hyperreflexia d. Acute pulmonary oedema CI a. Asthma TRIMETHAPHAN
  34. 34.  Non depolarising Tubocurarine Pancuronium Pipecuronium Vecuronium Atracurium Mivacurium NMJ BLOCKERS
  35. 35.  Suxamethonium decamethonium Depolarizing blockers
  36. 36.  Opening Na channel Phase 1 - rapid ,depolarization, gradual repolarization Phase 2 – desensitization of receptors to acetyl choline, full repolarization Depolarizing blockers
  37. 37. Skeletal muscles - muscle weekness ,flaccid paralysis Cvs – BP falls ( sch variable) CNS – do not cross BBB Histamine release Autonomic ganglion – some blockage GIT – paralytic ileus Actions
  38. 38.  IV Metabolized in liver Excreted kidney Sch - pseudocholinesterase PK
  39. 39.  General anesthesia Assisted ventilation Tetanus Status epilepticus Uses
  40. 40.  THANK YOU
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ANTICHOLINERGICS

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