Name: Amyl Nitrate
Class: Antianginal Agent (Organonitrate)
Mechanism: Converted to NO ® activation of cytosolic guanylate cyclase ® cGMP ® activation of cGMP-dependent protein kinase ® smooth muscle relaxation ® vasodilation. Greater effect in veins & large arteries than in resistance vessels ® ¯¯ preload, ¯ afterload ® ¯ work ® ¯ O2 demand. Inhib. of platelet fxn.
Absorption: Inhalation ® rapid onset.
Dist.:
Metabolism.: Hepatic inactivation via glutathione-organic nitrate reductase.
Excretion, t½: Renal. Short duration of action (3-5 min.).
Toxicity/S.E.s: Orthostatic hypotension, tachycardia, severe throbbing headache, dizziness, flushing, syncope. C/i w/elevated ICP.
Utility: Treat angina. Not suitable for maintenance therapy.
Special Features: