Olmesartan Medoxomil
(British Approved Name, US Adopted Name, rINN)
Drug Nomenclature
International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):
Olmesartan Medoxomil
Note. The name olmesartan has been applied to both the base and to the medoxomil ester.
Adverse Effects and Precautions
As for Losartan Potassium.
Interactions
As for Losartan Potassium.
Pharmacokinetics
Olmesartan medoxomil is an ester prodrug that is hy-drolysed during absorption from the gastrointestinal tract to the active form olmesartan. The absolute bioavailability is about 26%. Peak plasma concentrations of olmesartan occur about 1 to 2 hours after oral doses. Olmesartan is at least 99% bound to plasma proteins. It is excreted in the urine and the bile as olmesartan; about 35 to 50% of the absorbed dose is excreted in the urine and the remainder in the bile. The terminal elimination half-life is between 10 and 15 hours.
Uses and Administration
Olmesartan is an angiotensin II receptor antagonist with actions similar to those of losartan. It is used in the management of hypertension. Olmesartan is given orally as the ester prodrug olmesartan medoxomil. After a dose the hypotensive effect lasts for 24 hours. Most of the hypotensive effect is apparent within 2 weeks after starting therapy and is maximal within about 8 weeks.
In hypertension, olmesartan medoxomil is given in a usual dose of 20 mg once daily, although in the UK an initial dose of 10 mg once daily is recommended. The dose may be increased to 40 mg once daily if required. For doses in hepatic or renal impairment, see below.
Administration in hepatic or renal impairment. Olmesartan is excreted in both urine and bile and raised plasma concentrations have been noted in patients with renal or hepatic impairment. In patients with renal impairment, licensed product information in the UK does not recommend the use of olmesartan in severe impairment (creatinine clearance (CC) below 20 mL/minute) since experience is limited, and the maximum dose in mild to moderate impairment (CC 20 to 60 mL/minute) is 20 mg once daily. Similarly, in patients with hepatic impairment, licensed product information in the UK does not recommend the use of olmesartan in severe impairment since there is no experience. Those with moderate hepatic impairment should be given an initial dose of 10 mg once daily and the maximum dose is 20 mg once daily.
Migraine. For reference to the use of angiotensin II receptor antagonists, including olmesartan, in the prophylaxis of migraine, see under Losartan.
Preparations
Single-ingredient Preparations
Argentina: Olmec; Tensonit; Austria: Olmetec; France: Alteis; Olmetec; Germany: Olmetec; Votum; Greece: Olmetec; Ireland: Benetor; Omesar; Japan: Olmetec; Netherlands: Olmes; Olmetec; Portugal: Olmetec; Spain: Ixia; Olmetec; Openvas; United Kingdom: Olmetec; United States: Benicar
Multi-ingredient Preparations
United Kingdom: Olmetec Plus; United States: Benicar HCT
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