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Summary Notes on Dr. Petrianue's lectures Unit 7

Summary Notes on Dr. Petrianue's lectures Unit 7 . R.E.B, 4MedStudents.com, 2003 . Drugs acting on Calcium Channels. Calcium Channel Blockers. L-type Ca channel blocker. NPQR Ca channel blocker. T-type Ca channel blocker. Pimozid Mibefradil Succinimide Antiepliptic drugs Phenytoin.

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Summary Notes on Dr. Petrianue's lectures Unit 7

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  1. Summary Notes on Dr. Petrianue's lectures Unit 7 R.E.B, 4MedStudents.com, 2003

  2. Drugs acting on Calcium Channels Calcium Channel Blockers L-type Ca channel blocker NPQR Ca channel blocker T-type Ca channel blocker • Pimozid • Mibefradil • Succinimide Antiepliptic drugs • Phenytoin • Verapamil • Diltiazem • Nifedipine • Gabapentin

  3. Drugs acting on Sodium Channels Sodium Channel Blockers Local Anesthetics Anti-Arrhythmic Anti-Epileptics • Class I A • Quinidine • Class IB • Lidocaine • Class IC • Flecainide • Ester LA (one i) • Amide LA (two i) • Carbamazepine

  4. Drugs acting on potassium Channels Potassium Channel Blockers Anti-arrhythmic Hypoglycemic • Sotalol • Bretylium • Amiodarone • Difetilide, Ibutilide • Sulfonyl-Urea Agents • Non-Sulfonyl-Urea Agents • Repaglinide Not selective to K Highly selective to K

  5. Drugs acting on potassium Channels Potassium Channel Openers Vascular relaxation Promotes hair growth Lower Blood pressure • Minoxidil

  6. Drugs acting on GABA receptors GABA Agonist Drugs Propafol Benzodiazepine Barbiturates Vagabatrin Tiagabin • BNZ Agonist • Diazepam • Oxazepam • Midazolam • BNZ Antagonist • Flumazenil • Sedative: • Thiopental • Anti-epileptic: • Phenobarbital • Inhibits GABA- transaminase • Inhibits GABA uptake

  7. Drugs acting on Opioid receptors Endogenous opioid agonists Enkephalines Dynorphines Endorphines • Spinal & Supra-spinal analgesics • High affinity to  opioid receptors • Mechanism of action: • They activate K channels leading to hyperpolarization • Supra-spinal analgesics • High affinity to κ opioid receptors • Mechanism of Action: • They block Ca channels to inhibit the release of neurotransmitters • High affinity to δ opioid receptors.

  8. Drugs acting on Opioid receptors Opioid agonists Drugs * Morphine AP=1 Weak acting opioid analgesics, AP<1 Strong acting opioid analgesics, AP>1 • Methadone • Remifentanil (must be given in continues infusion because it has very short half life) • Sulfentanil (Most POTENT analgesic) • Codiene • Tramadol • Pentazocine Act on  opioid receptors Act on κ opioid receptors * Opioid agonists are classified according to their analgesic potency (AP) in comparison to morphine, which has an analgesic potency = 1

  9. Drugs acting on NMDA receptors NMDA Antagonists Memantine Methadone Ketamine NMDA Antagonists (Anti-epileptic drugs) Flabomate Topiramate Lamotrigin Glycine NMDA GABA Glutamate NMDA NMDA GABA

  10. Drugs acting on PPAR PPAR Agonists PPAR-α Agonist PPAR-γ Agonist • e.g Fibrates • The main effect of Fibrates: • Lower Triglycerides • Used to treat hyperlipidemia • e.g -glitazone • The main effect of glitazone: • Increase Insulin sensitivity. • Used to treat Diabetes

  11. Insulin pharmacology Insulin Drugs * Intermediate acting insulin Slow Onset Long Acting insulin (SOLA) Rapid Onset Short Acting insulin (ROSA) • NPH Insulin • Aspart Insulin • Lispro Insulin • Regular Insulin (Only insulin given by IV) • Lente insulin • Ultra-Lente Insulin • Lentus Insulin * Insulin drugs are classifies according to their onset and rapidity of action

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