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

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Created May 3, 2010ReportNominate
Tags:description, drug