Canrenone
Canrenone, sold under the brand names Contaren, Luvion, Phanurane, and Spiroletan, is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone which is used as a diuretic in Europe, including in Italy and Belgium. It is also an important active metabolite of spironolactone, and partially accounts for its therapeutic effects.Canrenone is mainly used as a diuretic.
Canrenone has been found to be effective in the treatment of hirsutism in women.Pharmacology
Pharmacodynamics
Canrenone is reportedly more potent as an antimineralocorticoid relative to spironolactone, but is considerably less potent and effective as an antiandrogen. Similarly to spironolactone, canrenone inhibits steroidogenic enzymes such as 11β-hydroxylase, cholesterol side-chain cleavage enzyme, 17α-hydroxylase, 17,20-lyase, and 21-hydroxylase, but once again, is comparatively less potent in doing so.Pharmacokinetics
The elimination half-life of canrenone is about 16.5 hours.Canrenone is an active metabolite of spironolactone, canrenoic acid, and potassium canrenoate, and is considered to be partially responsible for their effects. It has been found to account for approximately 10 to 25% of the potassium-sparing effect of spironolactone, whereas another metabolite, 7α-thiomethylspironolactone, accounts for around 80% of the potassium-sparing effect of the drug.History
Canrenone was described and characterized in 1959. It was introduced for medical use, in the form of potassium canrenoate, by 1968.Canrenone is the and of the drug.Brand names
Canrenone has been marketed under the brand names Contaren, Luvion, Phanurane, and Spiroletan, among others.Availability
Canrenone appears to remain available only in Italy, although potassium canrenoate remains marketed in various other countries as well.
