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

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Created May 3, 2010ReportNominate
Tags:description, drug