Drug Interactions With Receptors And Ion Channels Flashcards
Atropine
From Atropa belladonna, competitive antagonist of mAChR. Parasympatholytic.
Adenosine
Purine nucleoside. Four receptor subtypes, all GPCRs: A1 (Gi/o), 2A (Gs), 2B (Gs) and A3. Promotes sleep, suppresses arousal, vasodilatation.
Bay K 8644
Calcium channel agonist. Research tool. +ve inotropic.
Benzilylcholine choline
Irreversible inhibitor of mAChR. Investigate relationship between receptor occupancy and response.
Benzocaine
Inhibits voltage-dependent sodium channels on nerve. Stops AP. Local anaesthetic.
Alpha-bungarotoxin
Snake venom. Irreversible competitive inhibitor of nAChR at NMJ. Paralysis, respiratory failure and death.
Cholera toxin
Causes CFTR activity. Secretion of ions and water into intestinal lumen. Rapid loss of fluid. Severe dehydration.
Diltiazem
Calcium channel blocker. Potent vasodilator, increase heart blood flow. Negative inotropic effect. Hypertension, angina and arrhythmia.
d-tubocurarine
nAChR antagonist. Skeletal muscle relaxant in anaesthesia.
Ethinylestradiol
Derivative of endogenous oestrogen. Acts on oestrogen receptor. Used in combined pill.
Glibenclamide
Anti diabetic drug. Binds to KATP and activates inhibitory subunit. Caused insulin release via depolarisation
Isoprenaline
Beta 1 and 2 agonist. Positive chromite optic and inotropic effects. Used to treat asthma
Lidocaine/lignocaine
Blocks fast voltage gated sodium channel in cardiomyocytes and neurones. Local anaesthetic.
Minoxidil
Nitric oxide agonist. Vasodilator. Anti hypertensive. Also promotes hair growth - used in androgenic alopecia.
Nicorandil
Stimulates cGMP production. Activates KATP hyper polarising cell and reducing [Ca2+]i. Smooth muscle relaxation and vasodilatation due to nitrate group.
Nifedipine
L-type calcium channel blocker. Antianginal and anti hypertensive. Primary treatment for African American patients.
Norethisterone
Progestogen agonist. Treats PMS, painful/heavy periods.
Pertussis toxin
Causes whooping cough. Bonds to receptor - interferes with cell signalling, causes insulin release and inhibits immune responses. Could treat hypertension, autoimmunity.
Prednisolone
Cortisol derivative irreversibly binds to alpha and beta glucocorticoid receptors. Changes gene transcription. Treats inflammatory and auto-immune conditions.
Quinidine
Blocks fast inward sodium current. Causes increase in AP and QT duration. Used dependent block. Used as an antiarrhythmic.
Spironactone
Antagonist of mineralocorticoid and androgen receptor. Potassium soaring diuretic and antihypertensive.
Tamoxifen
Antagonist to oestrogen receptor. Prodrug metabolised in liver. Used in endocrine therapy for certain breast cancer.
Tetrodotoxin (TTX)
From pufferfish. Binds to VGCC, block AP firing. Toxic - paralysis of voluntary muscles, respiratory failure and loss of vagal regulation of HR.
Tyrphostins
Tyrosine kinase inhibitor (eg inhibit EGFR activity). Anti-cancer drug.
Verapamil
Preferentially block L-type Ca2+ channels in cardiac muscle. Use dependent. Hypertension, angina and antidysrhythmias (class IV).
