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

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