pharmacology presentation

1. PAIN KILLERS
 SUBJECT- PHARMACOLOGY
 SUBMITTED TO- DR. RAHUL PEDDAWAD
 SUBMISSION DATE- 25/09/2016
 PRESENTED BY- MS. PAYAL BARIYA
F.Y PHARMA MBA
ROLL NO. – MBAPH016001

2. WHAT IS PAIN ? ? ?
 Subjective experience
 Hard to explain
Pain is a direct response to an untoward
event associated with tissue damage such as
 Injury
 Inflammation
 Cancer, etc.

3. TYPES OF PAIN
 ACUTE trauma or injury,
 CHRONIC conditions for which cures were
unknown,
 MALIGNANT processes (cancer)
Based on etiology pain is differentiated into two
types
1) NOCICEPTIVE PAIN
2) NEUROPATHIC PAIN

4. Nociceptive Pain:
• Result of activation of sensory receptors
(nociceptors) by mechanical, chemical, or
thermal stimuli.
• Functional, physiologic or “normal” pain.
Neuropathic Pain:
• Pain resulting from damage to peripheral
nervous or central nervous system tissue or
from altered processing of pain in the
CNS.

5. HOW PAIN IS GENERATED ? ?

6. CONTD……

7. ANALGESIC
DRUGS
PAIN KILLERS
OPIOIDSNSAIDS

8. OPIOIDS - OPIUM
A dark brown, resinous material obtained from poppy plant
(Papaver Somniferum; Family: Papaveraceae)capsule. It
contains two types of alkaloids.
Phenanthrene
derivatives
• Morphine
• Codiene
• Thebaine
Benzoisoquinoloine
derivatives
• Papaverine
• Noscapine

9. CLASSIFICATION OF OPIOIDS
• MORPHINE, CODIENE
NATURAL OPIUM ALKALOIDS
• DIACETYLMORPHINE(HEROIN),
PHOLCODIENE
SEMISYNTHETIC OPIATES
• PETHIDINE, FENTANYL, METHADONE,
DEXTROPROPOXYPHENE, TRAMADOL
SYNTHETIC OPIATES

10. MORPHINE
MORPHINE IS THE PRINCIPLE ALKALOID IN OPIUM
AND WIDELY USED ANALGESIC DRUG.

11. PHARMACOLOGICALACTIONS OF MORPHINE.
 ON CNS
ANALGESIA:
- Strong analgesic
- High doses-severe pain
- Intrathecal injection causes segmental analgesia
SEDATION:
- Drowsiness
- Inability to concentrate
- Extravagant imagination
- Larger doses produce sleep- EEG resembles normal
sleep.

12. PHARMACOLOGICALACTIONS OF MORPHINE (CONTD.)
DEPRESSION
• Respiratory
centre
depression
• Cough centre
• Temperature
regulating
centre
• Vasomotor
centre.
STIMULATION
• Vagal centre
• Hippocampal
cells-
convulsions
(inhibition of
GABA
release).

13. Pharmacological actions of morphine contd.
MOOD EFFECTS:
- Normal person – calming effect, absence of pain
- Dysphoria
- In addicted persons- KICK
- Euphoria
 NEURO-ENDOCRINE:
- Hypothalamic activation is dampened
- Hypothalamic influence on pituitary
- Thus; FSH, LH and ACTH levels are lowered – only short
term- tolerance develops.
- Decrease in levels of sex hormones and corticosteroids, but
no infertility; except in few cases.

14. PHARMACOLOGICALACTIONS OF MORPHINE. (CONTD.)
 CVS:
- Direct effect on heart
- Vasodilation- histamine release, depression of
vasomotor centre.
- Postural hypotension and fainting
- Decreased cardiac output.
 GIT:
- Constipation- reduced spasm of sphincters and GIT
secretions
 ANS:
- Mild hyperglyceamia

15. MORPHINE PHARMACOKINETICS
 ABSORPTION:
- Variable orally, IM or IV
 DISTRIBUTION:
- Widely distributed – liver, kidney, spleen, etc.
- Enters brain slowly
- Crosses placental barrier- dependence in foetus
 METABOLISM:
- In liver by glucoronidation-water soluble metabolites
- Morphine-6-glucoronide –analgesic-renal failure-prolong analgesia
- Morphine-3-glucoronide –no analgesia- neuroexcitatory.
 EXCRETION:
- Action lasts for 4-6 Hrs
- Completely eliminated in 24 Hrs.

16. MORPHINE- ADVERSE EFFECTS
Respiratory depression-Infants and Old
Vomiting
Sedation: Mental clouding
Hypotensive effect
Apnoea: newborn
Urinary retention
Idiosyncrasy and allergy
Acute morphine poisoning
Tolerance and dependence

17. MORPHINE – THERAPEUTIC USES
 ANALGESIC
1. Long bone fracture
2. Myocardial infarction
3. Terminal stages of cancer
4. Burn
5. Postoperative patients
6. Biliary colic and renal colic
7. Obstetric analgesia
8. Segmental analgesia

18. MORPHINE – THERAPEUTIC
USES (CONTD.)
OTHERS
1.Preanaesthetic medication
2.Surgical analgesia
3.Cardiac asthma
4.Diarrhoea

19. PETHIDINE
 MORPHINE Vs PETHIDINE
 1/10th as potent as morphine, but efficacy
is same.
 Same amount of sedation, euphoria and
respiratory depression
 Rapid but short DOA
 No antitussive action
 Safe margin in asthamic conditions
 Better oral absorption

20. PETHIDINE – CONTD.
 PHARMACOKINETICS:
 Well absorbed orally.
 Effect produced within 20 mins
 Parenteral administration- action lasts for 2-3
hrs
 Metabolized in liver-mepiridinic acid and
norpethidine
 Norpethidine accumulates on chronic use
 Excreted In urine

21. PETHIDINE – CONTD.
 ADVERSE EFFECTS:
 Similar to morphine
 Atropine like effects
 Overdose- tremors, mydriasis, convulsion
due to norpethidine accumulation.
 USES:
 Substitute for morphine
 Preanaesthetic medication
 Analgesic during labour- less foetal
respiratory depression.

22. METHADONE
 Chemically dissimilar but pharmacologically similar
 Action is shown orally and parenterally
 DOA same as morphine
 Accumulation – repeated administration
 Highly bound to plasma proteins 80-90%
 Metabolized by liver
 Excreted in urine
 Abuse potential is low
 Substitution therapy – 1:4mg and 1:20mg of Morphine and
Pethidine resp.
 Codiene as a substitute in Methadone addiction.

23. TRAMADOL
Analgesic
Low action
Spinal inhibition of pain
Effective both orally and by IV
Side effects = morphine but less
prominent
Well tolerated and low abuse
potential

24. REFERENCES:
Essentials of Medical
Pharmaccology, KD Tripathi
Rang and Dale’s Pharmacology
Pharmacology, Vidyakumar
Padmaja