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بسماللهالرحمنالرحيم صدق   الله   العظيم ( قَالُواْ سُبْحَانَكَ لاَ عِلْمَ لَنَا إِلاَّ مَا عَلَّمْتَنَا  إِنَّكَ أَنتَ الْعَلِيمُ الْحَكِيمُ )
Mansoura University Faculty of Medicine
Analgesic Drugs
Drugs which relieve pain be central action .  Certain drugs can relieve specific types of pain (not proper analgesic drugs) e.g., atropine in colics.  Peripheral analgesic include :  physical protectives, local and surface anaesthetics , obtundants , astringents and counterirritants
Central Analgesics include:    No drug dependence     No euphoria or drowsiness.     Subcortical on thalamus     Relieve low intensity pain, e.g., headache , neuralgia, myalgia  Analgesic antipyretics     Addictive     Produce euphoria and stupor     Act cortical and subcortical .     Can relieve any type (except itching ).  Opioid (narcotic ) analgesic
Opioid analgesics
Opioid actions CNS: analgesia  Respiratory and cough centre: depression Vomiting centre: Nausea  Higher centres: Euphoria & dysphoria  Bowel: relax.  Uses: relief of pain ( ischemic-post operative- palliative  Dirrhea  (codeine)
Contraindications :
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Preparations  : Morphine HCI or ulphate 10-15 mg S.C., I.M. or I.V.  Adverse effects:  Respiratory depression, nausea , dizziness, mental clouding, dysphoria , pruritus, constipation , increased biliary pressure, urine retention and hypotension.
Non steroidal anti-inflammatory drugs (NSAIDs)
Non steroidal anti-inflammatory drugs (NSAIDs)
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],Usese of NSAIDS
Pyrazolone derivatives  : rarely used due to bone marrow depression  Adverse effects : GIT upset, salt and water retention, oedema, h7ypertension , bone marrow depression, liver and renal toxicity, skin rash, and bronchospasm.  Indole derivatives  : is potent  Adverse effects:   GIT disturbances , frontal headache , vertigo, confusion, psychosis , blood dyscrasias , liver and kidney toxicity, kin rash and asthma.  Classification Of NSAIDS
Sulindac : it is prodrug which is converted into active metabolite and ahs kess gastric irritation.  Anthranilic acid derivatives : fenamates  Central analgesic action (which is specific with mefenamic acid .  Propionic acid derivatives (IBUPROFEN  : Most safe  Oxicams  : Piroxicam (Feldene). It has enterohepatic cycle, so has long plasma half life
Side Effects  of Salicylate :
Gastric irritation , increased occult blood in stools.  Hypersensitivity reaction: asthma, rash, ……  Idiosyncracy: In patient: with G-6-PD deficiency  ->haemolytic  anaemia  Prolonged use may lead to hypoprothrombinaemia.
Chronic use -> Salicylism: Headache , mental confusion, vertigo, ringing in ears (tinnitus), Sweating , nausea, vomiting.  Acute salicylate poisoning : Restlessness, tremors , convulsions vomiting , dehydration, ↓ B.P., metabolic acidosis (in children), respiratory alkalosis (in adults), hyperglycemia , hyperpyrexia.
1-  Epigastric distress, naused and v0omiting ( # PGS in GIT)  2-  CVS & M.I.: with Cox-2 inhibitors (rofecoxib ) 3-  Coagulation disorders (reversible ) 4-  Renal toxicity (# Pgs).  5-  Hypersensitivity  N.B.  Newer NSAIDS have lower incidence of gastric distribution but higher incidence of renal damage   adverse effects of NSAIDs
Kinetics  Major    Minor  Conjugate with Toxic metabolite glucuronic and  (N-acetyle Benzo quinone  acid sulphate  which is detoxificated  by glutathione  acetaminophen (paracetamol )
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],acetaminophen (paracetamol )
THANK YOU
بحمد  تم

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Analgesics

  • 1.  
  • 2. بسماللهالرحمنالرحيم صدق الله العظيم ( قَالُواْ سُبْحَانَكَ لاَ عِلْمَ لَنَا إِلاَّ مَا عَلَّمْتَنَا إِنَّكَ أَنتَ الْعَلِيمُ الْحَكِيمُ )
  • 5. Drugs which relieve pain be central action . Certain drugs can relieve specific types of pain (not proper analgesic drugs) e.g., atropine in colics. Peripheral analgesic include : physical protectives, local and surface anaesthetics , obtundants , astringents and counterirritants
  • 6. Central Analgesics include:  No drug dependence  No euphoria or drowsiness.  Subcortical on thalamus  Relieve low intensity pain, e.g., headache , neuralgia, myalgia Analgesic antipyretics  Addictive  Produce euphoria and stupor  Act cortical and subcortical .  Can relieve any type (except itching ). Opioid (narcotic ) analgesic
  • 8. Opioid actions CNS: analgesia Respiratory and cough centre: depression Vomiting centre: Nausea Higher centres: Euphoria & dysphoria Bowel: relax. Uses: relief of pain ( ischemic-post operative- palliative Dirrhea (codeine)
  • 10.
  • 11. Preparations : Morphine HCI or ulphate 10-15 mg S.C., I.M. or I.V. Adverse effects: Respiratory depression, nausea , dizziness, mental clouding, dysphoria , pruritus, constipation , increased biliary pressure, urine retention and hypotension.
  • 14.
  • 15. Pyrazolone derivatives : rarely used due to bone marrow depression Adverse effects : GIT upset, salt and water retention, oedema, h7ypertension , bone marrow depression, liver and renal toxicity, skin rash, and bronchospasm. Indole derivatives : is potent Adverse effects: GIT disturbances , frontal headache , vertigo, confusion, psychosis , blood dyscrasias , liver and kidney toxicity, kin rash and asthma. Classification Of NSAIDS
  • 16. Sulindac : it is prodrug which is converted into active metabolite and ahs kess gastric irritation. Anthranilic acid derivatives : fenamates Central analgesic action (which is specific with mefenamic acid . Propionic acid derivatives (IBUPROFEN : Most safe Oxicams : Piroxicam (Feldene). It has enterohepatic cycle, so has long plasma half life
  • 17. Side Effects of Salicylate :
  • 18. Gastric irritation , increased occult blood in stools. Hypersensitivity reaction: asthma, rash, …… Idiosyncracy: In patient: with G-6-PD deficiency ->haemolytic anaemia Prolonged use may lead to hypoprothrombinaemia.
  • 19. Chronic use -> Salicylism: Headache , mental confusion, vertigo, ringing in ears (tinnitus), Sweating , nausea, vomiting. Acute salicylate poisoning : Restlessness, tremors , convulsions vomiting , dehydration, ↓ B.P., metabolic acidosis (in children), respiratory alkalosis (in adults), hyperglycemia , hyperpyrexia.
  • 20. 1- Epigastric distress, naused and v0omiting ( # PGS in GIT) 2- CVS & M.I.: with Cox-2 inhibitors (rofecoxib ) 3- Coagulation disorders (reversible ) 4- Renal toxicity (# Pgs). 5- Hypersensitivity N.B. Newer NSAIDS have lower incidence of gastric distribution but higher incidence of renal damage adverse effects of NSAIDs
  • 21. Kinetics Major Minor Conjugate with Toxic metabolite glucuronic and (N-acetyle Benzo quinone acid sulphate which is detoxificated by glutathione acetaminophen (paracetamol )
  • 22.