Monograph: |
Adverse Effects and Precautions
As for Losartan Potassium.
Interactions
As for Losartan Potassium.
Pharmacokinetics
Eprosartan is absorbed from the gastrointestinal tract with an absolute oral bioavailability of about 13%. Peak plasma concentrations occur about 1 to 2 hours after an oral dose in the fasted state; administration with food delays absorption but this is not clinically significant. Eprosartan is about 98% bound to plasma proteins. It is excreted in the bile and in the urine, primarily as the unchanged drug; after oral doses approximately 7% of the drug is excreted in the urine, with about 2% as the acyl glucuronide. The terminal elimination half-life is about 5 to 9 hours.
Uses and Administration
Eprosartan is an angiotensin II receptor antagonist with actions similar to those of losartan. It is used in the management of hypertension.
Eprosartan is given by mouth as the mesilate but doses are expressed in terms of the base; eprosartan mesilate 1.2 mg is equivalent to about 1 mg of eprosartan. The onset of antihypertensive effect occurs about 1 to 2 hours after administration and the maximum effect is achieved within 2 to 3 weeks after initiating therapy.
In the management of hypertension, eprosartan is given in an initial dose of 600 mg once daily. A lower initial dose of 300 mg once daily may be used in elderly patients over 75 years and has been recommended in renal or hepatic impairment. The dose should be adjusted according to response; the usual maintenance dose is 400 to 800 mg daily in a single dose or in two divided doses.
Administration in hepatic or renal impairment.
In the UK a lower initial dose of 300 mg daily of eprosartan is recommended in patients with renal impairment (creatinine clearance less than 60 mL/minute) or mild to moderate hepatic impairment; this seems to be due to lack of clinical experience in such patients. In the USA, however, no reduction in the initial dose is considered necessary in hepatic or renal impairment, but a maximum dose of 600 mg daily is recommended for patients with moderate or severe renal impairment.
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