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Pharmacology of Opioid analgesics- MORPHINE 2020

This interesting ppt is about the Pharmacology of morphine and acute morphine poisoning dealt with illustrative pictures, diagrams to facilitate learning for medical/paramedical students....

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Pharmacology of Opioid analgesics- MORPHINE 2020

  1. 1. * *Most important symptom that brings the patient to the doctor *Demands immediate relief
  2. 2. * *Unpleasant subjective sensation *Warning signal *Indicates impairment of structural and functional integrity of body
  3. 3. * *Somatic pain *Visceral pain *Referred pain
  4. 4. * *Drug which relieves pain without loss of consciousness *Afford symptomatic relief without affecting the cause
  5. 5. * *OPIOID Morphine type *NON-OPIOID Aspirin type
  6. 6. * *Classes: *Opioid. *Agonist. *Antagonist. *Agonist-antagonist. *Non-opioids. *Salicylates. *NSAIDs. *Adjuncts.
  7. 7. DR. V. SATHYANARAYANAN M.B.B.S.,M.D., ACME., PROFESSOR OF PHARMACOLOGY, SRM MCH & RC *OPIOID ANALGESICS - I
  8. 8. * *Dark brown gummy exudate *Obtained from poppy capsule ( papaver somniferum ) *Opos – juice *In use since 4000 BC *Opium smoking popular by 18th century *Used for medicinal and recreational purposes
  9. 9. * *Serturner --- isolated a pure opium alkaloid ( 1801) *Named it as -------- MORPHINE *By 19th century ----- pure alkaloids available for therapeutic use
  10. 10. * *Drugs with morphine-like actions *Also known as Narcotic analgesics
  11. 11. * *Peptides released in the body in response to pain *These Act on the opioid receptors *ENKEPHALINS - act on delta receptors *ENDORPHINS – act on mu receptors *DYNORPHINS - act on kappa receptors
  12. 12. Actions at Opioid Receptors Drugs Mu Kappa Pure Agonists -morphine, codeine, meperidine (Demerol®), fentanyl (Sublimaze®), remifentanil (Ultiva®), propoxyphene (Darvon®), hydrocodone (Vicodin®), oxycodone (Percocet®) Agonist Agonist Agonist-Antagonist -nalbuphine (Nubaine®), butorphanol (Stadol®) Antagonist Agonist Pure Antagonist -naloxone (Narcan®) Antagonist Antagonist
  13. 13. * *PROTOTYPE *Most important alkaloid of opium *GOLD STANDARD
  14. 14. *
  15. 15. * *Act on opioid receptors ------ *Mu – 1,2 *Kappa – 1, 2, 3 *Delta – 1,2 * all are G-protein coupled receptors *Open K channels and close voltage gated Ca channels  reduces neuronal excitability, inhibit the release of pain neurotransmitters
  16. 16. Actions of Opioid Receptors Response Mu Kappa Analgesia   Respiratory Depression  Sedation   Euphoria  Physical Dependence   GI motility  
  17. 17. *
  18. 18. * ANALGESIA *Dull aching visceral pain is relieved better than somatic pain *Raises pain threshold *Also alters emotional reaction to pain
  19. 19. * *EUPHORIA - feeling of well being, * “HIGH ”, * Colourful daydreams *SEDATION – drowsiness, * inability to concentrate * feeling of detachment and indifference *HYPNOSIS - sleep
  20. 20. * *Respiratory depression - depresses respiratory centre - decreases rate, rhythm, tidal volume *Depresses cough centre *Nausea, vomiting – stimulation of CTZ *Pupils – miosis *Stimulates vagal centre – bradycardia *Body temperature falls slightly
  21. 21. * HYPOTENSION BY *Peripheral vasodilatation *Inhibition of baroreceptor reflexes *Higher doses – histamine release, depression of vasomotor centre
  22. 22. *GIT *Decreased gastric motility  increased gastric emptying time  decreases absorption of drugs *Increased oesophageal reflux *Decreased intestinal motility, secretions *Increased tone of sphincters, spasm of intestine *All actions result in MARKED CONSTIPATION
  23. 23. * *Spasm of sphincter of Oddi - increased intrabiliary pressure  biliary colic *Increases tone, amplitude of ureter may worsen ureteric colic *Increases tone of external sphincter of bladder, inhibits urinary voiding reflex  URINARY RETENTION *BRONCHOCONSTRICTION
  24. 24. * *Decrease renal plasma flow  depress renal function *Anti-diuretic action
  25. 25. * *Inhibit the release of GRH, CRF  DECREASES BLOOD LEVELS OF *FSH *LH *ACTH *Betaendorphins
  26. 26. * *Flushing of face, *Pruritus *Complex immuno modulatory properties
  27. 27. * *Analgesia *Respiratory depression *Constipation *Urinary retention *Cough suppression *Emesis *Increased ICP *Indirect through CO2 retention *Euphoria/Dysphoria *Sedation *Miosis *Pupil constriction * Preload & afterload *Watch for hypotension!
  28. 28. * *Develops On repeated administration for * sedation, * analgesia, * euphoria, * respiratory depression *Cross tolerance also seen *NO TOLERANCE FOR constipation and miosis
  29. 29. * *Drug of addiction *Produce both PSYCHOLOGICAL and PHYSICAL DEPENDENCE *Sudden stoppage  cause withdrawal symptoms  known as COLD TURKEY *Babies born to addicted mothers  also be DEPENDENT
  30. 30. *
  31. 31. * *Orally  absorption slow and incomplete *Bioavailability 20 – 40% *SUBCUTANEOUSLY  * onset of action - 15-20 mins * peak effect - 1 hour * duration of action- 3-5 hours *METABOLISM  By glucuronide conjugation * EXCRETION  through kidneys *Undergoes enterohepatic circulation
  32. 32. * *10 – 50 mg oral, *10 – 15 mg SC/IM injection *2 – 6 mg IV inj *2 - 3 mg epidural inj *10, 30, 40, 100 mg continuous release tablets *Also given as rectal suppositories, transdermal patches
  33. 33. *
  34. 34. * *Sedation, mental clouding *Nausea, vomiting, dizziness *Respiratory depression *Constipation *Urinary retention *Hypotension *Dysphoria *Allergic reactions  skin rash, pruritus, rarely anaphylaxis ( after IV injection ) *DRUG DEPENDENCE
  35. 35. * *Given to pregnant mother in labour  cause APNOEA IN THE NEW BORN *Reversed by inj. Naloxone in the umbilical cord
  36. 36. *
  37. 37. * *Potentiates CNS depressants & *enhances the effects of 1. alcohol 2. Sedative-hypnotics like diazepam 3. Antipsychotics 4. antidepressants 5. Antihistamines *With MAO inhibitors  hyperpyrexia, coma, hypertension
  38. 38. * *Extremes of age *With other CNS depressants
  39. 39. * *HEAD INJURY  increases the intracranial tension * respiratory depression * interfere with assessment & prognosis *UNDIAGNOSED ACUTE ABDOMEN *HYPOVOLAEMIC SHOCK *RESPIRATORY INSUFFICIENCY, COPD *BRONCHIAL ASTHMA
  40. 40. *
  41. 41. * AS AN ANALGESIC *Excellent for severe pain in Acute MI Fractures Burns Pulmonary embolism Terminal stages of cancer Acute pericarditis Postoperative pain
  42. 42. * * AS AN ANALGESIC morphine + atropine  Biliary colic Epidural analgesia Patient Controlled Analgesia
  43. 43. * * As Pre-anaesthetic medication ( reduce anxiety, pain, dose of anaesthetic, smoothen induction ) *Acute left ventricular failure/ Acute pulmonary edema *Special anaesthesia *Relieves anxiety in threatened abortion
  44. 44. * *LETHAL DOSE – 250 MG ( in non-addicts ) *Pin point pupils *Respiratory depression with shallow breathing *Hypotension *Shock *Cyanosis *Hypothermia, flaccidity *Stupor, coma, death
  45. 45. * *Positive pressure respiration *Maintenance of BP *Gastric lavage with KMnO4 *Specific antidote  NALOXONE 0.4 – 0.8 MG IV, repeated every 10 – 15 min
  46. 46. * *Morphine is the prototype of opioid analgesics *It is Very useful in severe visceral pain, Though it has many side effects *It acts on opioid receptors *Long term use cause tolerance and dependence *Naloxone is the specific antidote for morphine poisoning *Respiratory depression and hypotension has to be watched for during morphine use
  47. 47. *
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This interesting ppt is about the Pharmacology of morphine and acute morphine poisoning dealt with illustrative pictures, diagrams to facilitate learning for medical/paramedical students....

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