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PHAR2002 Term 1

PHAR2002 Term 1 Drugs

Excitatory NANC ATP, Substance P
Inhibitory NANC Neurotensin, VIP
Muscarinic ACh receptors are antagonized by ... and produced by ... doses of ACh Atropine, Low
Nicotinic ACh receptors are antagonized by ... and produced by ... doses of ACh Tubocurarine, High
Adrenaline release from Adrenal Medulla blocked by Hexamethonium
Muscarinic Agonists ACh, Methacholine, Carbachol, Pilocarpine
Muscarinic Antagonists Atropine, Hyoscine (Scopolamine), Homatrophine All tertiary bases --> enter brain easily
Ganglion-blocking Drugs Hexamethonium (no longer used, too many side effects), Trimetaphan (controlled hypotension during surgery)
Neuromuscular Blocking Drugs Hemicholinium (inhibits reuptake of ACh), Botulinium toxin (blocks release of ACh at NMJ), Streptomycin (inhibits ACh by blocking Ca entry)
Clinically Useful NM Blocking Agents Pancuronium/Atracurium (competitive blocks, Myastenia Gravis sensitive), Suxamethonium (depolarizing block)
Types of Cholinesterases (ChE) Acetylcholinesterase (ChE), Butyrylcholinesterase
ChE Inhibitors Slow-acting: Erdophonium Medium-Long/Reversible: Neostigmine, Eserine Long/Irreversible: Dyflos, Organophosphates
ChE Reactivators (for Organophosphate poisoning) Pralidoxime
Bile acid binding Resins, Fibrates, Niacin, Inhibitors of Cholesterol from Gut Cholestyramine, Fenofibrate, Nicotinic acid, Ezetimibe
Inflammatory Mediators for Heat/Redness Histamine, NO, Bradykinin
Inflammatory Mediators for Swelling Histamine, PAF, Bradykinin
Inflammatory Mediators for Pain Substance P, Calcitonin-gene related peptide, Bradykinin
Inflammatory Mediators for Loss of Function Lipases, Proteases, Free radicals
Histamine Equation Histidine --(Histidine Carboxylase)--> Histamine
Metabolism of Histamine Oxidation - Diamine oxidase (histaminase) N-methylation - N-methyltransferase Acetylation - Gut flora
Bradykinin Equation Kininogens --> Kallidin --(Aminopeptidase)--> Bradykinin
Platelet-Activating Factor (PAF) Equation Acly-PAF --(PLA2)--> lysoPAF --(Acetylation)-->PAF
Cytokines Interleukins, Tumor necrosis factors, Interferons
H1 Agonist 2-methyl histamine
H1 Antagonist that CROSS BBB Diphenhydramine, Chlopheniramine
H1 Antagonist that DO NOT CROSS BBB Astemizole, Terfenadin, Cetirizine
H2 Agonist 4-methyl histamine, Dimaprit, Impromidine
H2 Antagonist Cimetidine, Ranitidine
Peptic Ulcers: Proton pump inhibitors Omeprazole
Peptic Ulcers: Antacids Aluminum hydroxide, Magnesium bicarbonate
Peptic Ulcers: Coating agents Sucralfate
Peptic Ulcers: Anticholinergic agents Dicyclomine
2 Metabolic Pathways for Arachidonic Acid Arach Acid --(5'-lipoxygenase + FLAP)--> HPETE Arach Acid --(Cyclooxygenase)--> PGG2
Eicosanoid Equation Phospholipid --(Phospholipase A)--> Arachidonate --(Cyclooxygenase)--> Cyclic-endoperoxidases --> PGI2 / TXA2
Anti-inflammatory Drugs Prednisolone, Betamethasone
NSAIDs (COX-1 Non-selective inhibitor) Aspirin, Oxyphenbutazone, Paracetamol, Indomethacin, Meclofenamic acid, Ibuprofen, Naproxen
NSAIDs COX-2 Selective inhibitor Celecoxib
Overdose of Aspirin Forced Alkaline Diuresis
Overdose of Paracetamol Methionine
Overdose of Indomethacin Anti-TNF╬▒
Created by: zccayxc