Angiotensin II Receptor Blocker Olmesartan medoxomil (prodrug) is rapidly and completely converted to olmesartan after oral doses. By blocking the effects of angiotensin II, olmesartan decreases systemic vascular resistance without a marked change in heart rate.
藥動學
Absorption 1. Absolute bioavailability: approximately 26%. 2. Time to peak: 1 ~ 2 hours. 3. Food does not affect the bioavailability of olmesartan. Distribution Protein binding: 99%. Metobolism Olmesartan does not undergo further metabolism by the liver. Excretion 1. 35-50% of the administered dose is eliminated in urine, and the remainder is eliminated in the feces via biliary excretion. 2. Elimination half-life (terminal): 13 hrs
禁忌症
1. Hypersensitive to olmesartan or any component of this product 2. Bilateral renal artery stenosis 3. Pregnancy
懷孕分類
Drugs that act on the renin-angiotensin system can cause injury and death to the developing fetus. When pregnancy is detected, discontinue as soon as possible.
哺乳分類
Due to the potential for serious adverse reactions in the breastfeeding infant, the manufacturer recommends a decision be made whether to discontinue breastfeeding or to discontinue the drug, considering the importance of treatment to the mother.
副作用
Dizziness, headache, hyperglycemia and hypertriglyceridemia, back pain, CPK increased, influenza-like symptoms, hyperkalemia (In high risk patients, including renal dysfunction, diabetes mellitus, concomitant use of potassium-sparing diuretics, potassium supplements and/or potassium containing salts, should monitor potassium closely
劑量和給藥方法
Adults: Initial 20 mg orally once daily; after 2 weeks of therapy, the dose may be increased to 40 mg. Doses above 40 mg do not appear to have greater effect. Elder: Refer to adult. Twice-daily dosing offers no advantage over the same total dose given once daily.
小兒調整劑量
Adolescents >16 years: Initial 20 mg once daily; if initial response is inadequate, may be increased to 40 mg once daily after 2 weeks Children and Adolescents 6 to 16 years: 1. 20 to <35 kg: 10 mg once daily; if initial response inadequate after 2 weeks, dose may be increased; maximum: 20 mg/day 2. 35 kg: 20 mg once daily; if initial response inadequate after 2 weeks, dose may be increased; maximum: 40 mg/day Children 1 to 5 years and >5 kg: Limited data available Children under 1 year: Not recommended.
腎功能調整劑量
1. CrCl >40 mL/minute: No dosage adjustment necessary. 2. CrCl <40 mL/minute: No initial dosage adjustment necessary. AUC is increased 3-fold in patients with CrCl <20 mL/minute and a maximum dose of 20 mg/day has been recommended for these patients.
肝功能調整劑量
1. Mild impairment: No dosage adjustment necessary. 2. Moderate to severe: No initial dosage adjustment necessary. Total drug exposure increased ~60% in moderate impairment.