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

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Created May 3, 2010ReportNominate
Tags:description, drug