Drugs MVST IB - part 1

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Can you name the drugs from MVST IB - part 1?

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DescriptionDrug nameUse
Tricyclic antidepressant - blocks NET
Progestagen receptor agonist
Medium 'reversible' anticholinesterase - binds to esteratic site and carbamoylates ACh
Double chain recombinant human tissue plasminogen activator
Tyrosine kinase inhibitor
Nitrovasodilator - produces NO
A1 receptor antagonist - non-selective phosphodiesterase inhibitor
Binds to plasminogen activator, increasing generation of plasmin
ACE inhibitor - prodrug, must be metabolised in liver
Very potent alpha-2 agonist
Blocks transporter carrying ACh into storage vesicles
Indirectly acting sympathomimetic amine - converted to octopamine by DBH - found in various foodstuffs
Mineralocorticoid receptor agonist
Irreversible alpha-adrenoceptor antagonist - blocks Uptake 2 (and Uptake 1 at 10x higher concs)
Phosphodiesterase III inhibitor - inodilator
Selective antagonist for M1 muscarinic receptors
Irreversibly alkylates muscarinic receptor
Binds to SNAREs involved in membrane fusion, preventing ACh release
ADP-ribosylates alpha-i - prevents activation of Gi in response to stimulation
Class IC antidysrhythmic
Cholinergic agonist - not selective between nicotinic/muscarinic receptors
Causes development of new blood vessels
Muscarinic receptor antagonist - very long duration of action
Non-selective alpha-adrenoceptor antagonist
Slightly selective alpha-2 agonist (also alpha-1 actions) - omitting dose can lead to rebound hypertension
Irreversible anticholinesterase - organophosphorus agent
Blocks transport of adenosine into cells - phosphodiesterase type V inhibitor
Osmotic diuretic - filtered at glomerulus, not reabsorbed
Orally-acting hypoglycaemic agent - sulphonylurea
Combined alpha- and beta-adrenoceptor antagonist
Local anaesthetic - slow onset/offset - use dependence at low rates of stimulation - class IA antidysrhythmic
Selective alpha-1 antagonist (slight effect on alpha-2)
Non-peptide angiotensin II antagonist - acts on AT1 receptors
PPAR-gamma agonist
Non-selective, reversible MAO inhibitor
Competitively inhibits plasminogen activation - inhibits severe bleeding from excessive clot lysis
Non-specific endothelin receptor antagonist
Depolarising blocker selective for NMJ nicotinic receptor - very short duration of action, broken down by BuChe - deficiency in enzyme activity can lead to prolonged action
Partial agonist at alpha-adrenoceptors - 5-HT agonist
NOS inhibitor - not very selective for different forms
Selective inhibitor of phosphodiesterase type V (selectively breaks down cGMP)
K channel opener - also hirsutism effects
ACE inhibitor
Mineralocorticoid receptor antagonist - potassium-sparing diuretic
Non-selective phosphodiesterase inhibitor
Glucocorticoid receptor antagonist
Non-selective agonist for muscarnic receptors
ADP-ribosylates alpha-s - inhibits GTPase activity - sustained activation of adenylyl cyclase
Co-released with NA or ACh - acts on purinoceptors (P2 > P1)
Depolarising blocker selective for ganglion nicotinic receptor
Tricyclic antidepressant - blocks NET
Glucocorticoid receptor agonist
DescriptionDrug nameUse
Selective MAO-B inhibitor
Immunosuppressant drug with antiproliferative effects
Beta-1 agonist - weak beta-2 agonist
Irreversible anticholinesterase - activated by replacement of sulphur atom with oxygen, deoxified by plasma carboxylesterases
Selective inhibitor of NOS in neurons
NSAID used to prevent thrombosis
Cardiac glycoside - inhibits Na/K-ATPase
Uncompetitive inhibitor of phosphatase acting on IP1 --> inositol
Calcium channel blocker - phenylalkylamine - class IV antidysrhythmic
Calcium sensitiser - increases cardiac Ca2+ binding efficiency to troponin - inhibits phosphodiesterase III
Beta-adrenoceptor agonist
Nitrovasodilator - produces NO - taken sublingually
Selective beta-2 agonist (slight effect on beta-1)
Naturally occurring anticoagulant produced by basophils/mast cells - exposes active site of antithrombin III
Converted to alpha-methylNA - released as false transmitter - more potent at alpha-2, less potent at alpha-1
SSRI - blocks 5-HT transporter in Uptake 1
Class III antidysrhythmic - prolongs AP and refractory period
Nitrovasodilator - produces NO - metabolised in liver to active drug
Calcium channel antagonist - dihydropyridine - affects L-type but not T-type channels
Selective non-depolarising neuromuscular blocking agent at NMJ - long action, not hydrolysed
Selective alpha-1 agonist (some action on beta-1)
Binds to synaptobrevin to prevent vesicle release from inhibitory interneuron synapses with motor neurons
Loop diuretic - blocks Na/K/2Cl transport in thick ascending limb
Illegal drug - blocks NET
Competitive antagonist for ganglionic nicotinic receptor - inactive at NMJ
Non-selective beta-adrenoceptor antagonist
Potassium-sparing diuretic - blocks apical Na+ channels in late distal tubule
Irreversible antagonist at nicotinic NMJ receptors (no effect on ganglionic receptors)
Selective alpha-2 antagonist (slight effect on alpha-1)
Cholinergic agonist - +-isomer hydrolysed by AChE
Binds very tightly to VMAT-2, preventing loading of catecholamines into vesicles
Blocks release of neurotransmitter via phospholipase A2 - localises to membrane by K channel binding moiety
Acts on imidazoline receptors
Blocks uptake of choline into neurons
Nicotinic receptor antagonist - relatively non-selective between NMJ and ganglion at clinical doses
K channel opener
Inhibits platelet activation by inhibiting binding of ADP to its receptor on platelets
Alpha-2 antagonist (some effect on alpha-1)
Estrogen receptor antagonist
Selective non-depolarising neuromuscular blocker at NMJ - ester, broken down by spontaneous hydrolysis and plasma esterases
Local anaesthetic (ester, weak base) - broken down by BuChE
Anion exchange resin - prevents reuptake of bile acids from intestine
Inhibits clotting by inhibiting synthesis of factors II, VII, IX, IX and regulatory proteins C, S, Z
Mild partial beta-1 agonist
Quaternary local anaesthetic analogue - only effective if perfused inside cells
Thiazide diuretic - blocks Na/Cl transport in early distal tubule
Blocks If current in SA node
Arteriolar vasodilator - unknown mechanism
Non-selective phosphodiesterase inhibitor
Interferes with normal function of microtubule growth
Angiotensin II partial agonist
Orally-acting hypoglycaemic agent - sulphonylurea
DescriptionDrug nameUse
Reversible anticholinesterase - ionic interaction
Phosphodiesterase III inhibitor - inodilator
Inodilator used to treat canine dilated cardiomyopathy - calcium sensitiser
Potassium-sparing diuretic - blocks apical Na+ channels in late distal tubule
K channel opener - also NO donor
Lowers VLDL (and LDL) by stimulating lipoprotein lipase - may activate PPARs
Selective MAO-A inhibitor
COMT inhibitor
Used experimentally to inhibit dopamine beta-hydroxylase - also inhibits aldehyde dehyddrogenase
Estrogen receptor agonist
Beta-1 antagonist used in heart failure
Selective beta-1 antagonist (slight effect on beta-2)
Inhibits DOPA decarboxylase in periphery
K channel opener
Inhibits HMG-CoA reductase - also many pleiotropic effects
Intracellular tetravalent polyamine - helps produce inward rectification of K+ channels
Selective alpha-2 agonist
Selective antagonist for M3 muscarinic receptor
Calcium channel blocker - benzothiazepine
Involved with providing new blood flow to ischaemic tissues
Binds to neurexins, causing massive ACh release from nerve terminals
Monoclonal antibody against glycoprotein IIb/IIIa receptor - prevents platelet aggregation - also binds to vitronectin receptor
Regulates expression of multiple angiogenic genes
Plasminogen + anisoylated streptokinase
Muscarinic receptor agonist
Competitive antagonist for ganglionic nicotinic receptors - inactive at NMJ
Blocks Na channels from exterior - no use-dependence
Indirectly-acting sympathomimetic amine - weak inhibitor of MAO
Non-selective agonist for muscarinic receptors
Non-peptide inhibitor of glycoprotein IIb/IIIa receptor
Local anaesthetic - uncharged
Cyclic heptapeptide inhibitor of glycoprotein IIb/IIIa receptor
Potent, irreversible inhibitor of iNOS in activated macrophages
Progestagen receptor antagonist
Direct acting vasodilator - metabolised to NO or cyanide
Inhibits liver triglyceride production and VLDL secretion - increases levels of tissue plasminogen activator
Acts on imidazoline receptors
alpha-1 antagonist most commonly used
Depolarising blocker at NMJ
Use-dependent block of ganglionic transmission
Reverse inhibition of AChE by organophosphorus agents
Competitively inhibits plasminogen activation - inhibits severe bleeding from excessive clot lysis
Blocks release of NA evoked by APs (repeated low doses/aftermath of large dose) - indirect sympathomimetic actions (large doses)
Calcium channel agonist - dihydropyridine
Local anaesthetic - weak base - use-dependence and voltage-dependence
Competitive inhibitor of tyrosine hydroxylase
Single chain recombinant human tissue plasminogen activator
Inhibits intestinal absorption of cholesterol - circulates enterohepatically
Beta-1 antagonist used in heart failure
Selective beta-2 antagonist (slight effect on beta-1)
Experimental cardiac glycoside
Carbonic anhydrase inhibitor

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