Drug Receptors and Ion Channels Flashcards
Quinidine
Local anaesthetic
Blocks fast inward sodium current
Class Ia antidysrhythmic
Intermediate rate of association/dissociation
Increases action potential duration
Diltiazem
Non-DHP calcium channel blocker
Vasodilator of coronary and peripheral vessels
Nifedipine
Dihydropyridine calcium channel blocker
Blocks L-type channels in vascular smooth muscle
Used in treatment of hypertension and angina
Increases Mode 0 type behaviour
Verapamil
L-type calcium channel blocker
Class IV antidysrhythmic
Causes vasodilatation
α-Bungarotoxin
Nicotinic antagonist
Competitive irreversible antagonism
Causes paralysis
Spironolactone
Mineralocorticoid/aldosterone antagonist
Potassium-sparing diuretic
Antihypertensive
Tetrodotoxin
Sodium channel blocker
Possesses guanidinium groups
Blocks extracellular pore
Does not show use dependence
Adenosine
Neurotransmitter
Inhibits calcium channels
Increases potassium permeability
Glibenclamide
Sulfonylurea
Binds to inhibitory subunit of ATP-sensitive potassium channels
Stimulates insulin release
d-Tubocurarine
Nicotinic antagonist
Reversible anticholinergic
Causes paralysis
Prednisolone
Synthetic glucocorticoid agonist
Anti-inflammatory
Immunosuppressive
Pertussis toxin
Whooping cough pathogen
Ribosylates Gαi subunit
Les inhibition of adenylyl cyclase
Increased cAMP
Causes insulin release so hypoglycaemia
Benzilylcholine mustard
Muscarinic antagonist
Irreversible anticholinergic
Alkylating agent
Benzocaine
Local anaesthetic
Inhibits voltage-gated sodium channels on axon membrane to stop action potential
Uncharged
Cholera toxin
Ribosylates Gαs subunit
Inhibits GTPase
Increases cAMP
Causes massive water loss in diarrhoea
Tyrphostins
Receptor tyrosine kinase inhibitor
Inhibit phosphorylation
Inhibit EGFR
Used to treat cancer
Tamoxifen
Oestrogen receptor antagonist
Used to treat breast cancer
Norethisterone
Progestogen agonist
Used in oral contraceptive
Minoxidil
Potassium channel opener
Used to promote hair growth
Lidocaine
Local anaesthetic
Blocks fast voltage-gated sodium channels so AP not propagated
Class Ib antidysrhythmic
Very fast association and dissociation
Decreased action potential duration
Binds preferentially to inactivated state of sodium channel
Isoprenaline
β-adrenoceptor agonist
Elevates heart rate
Ethinylestradiol
Oestrogen agonist
Used in oral contraceptive
Atropine
Muscarinic antagonist
Competitive anticholinergic
Inhibits parasympathetic nervous system
Bay K 8644
Calcium channel agonist
Targets L-type dihydropyridine calcium channels