Olmesartan Medoxomil Tablets

Under the catalysis of angiotensin converting enzyme (ACE, kinase II), angiotensin I (ATⅠ) is converted into angiotensin II (ATⅡ). Angiotensin II is the main pressor factor of the renin-angiotensin system. Its functions include constricting blood vessels, promoting the synthesis and release of aldosterone, stimulating the heart, and promoting the renal reabsorption of sodium. Olmesartan medoxomil is a prodrug that is absorbed and hydrolyzed into olmesartan through the gastrointestinal tract. Olmesartan is a selective angiotensin II type 1 receptor (AT1) antagonist. It blocks the vasoconstriction effect of angiotensin II by selectively blocking the binding of angiotensin II to the vascular smooth muscle AT1 receptor. Therefore, its action is independent of the ATⅡ synthesis pathway. Olmesartan has an affinity for AT1 that is more than 12,500 times greater than its affinity for AT2. Blocking the renin-angiotensin system (RAS) with ACE inhibitors is a mechanism of action for many drugs used to treat hypertension, but ACE inhibitors also inhibit the degradation of bradykinin, whereas olmesartan medoxomil does not inhibit ACE and therefore does not affect bradykinin. Whether this difference is clinically relevant is unclear. Blockade of angiotensin II receptors inhibits the negative feedback regulation of angiotensin II on renin secretion. However, the resulting increase in plasma renin activity and circulating angiotensin II concentrations does not affect the antihypertensive effect of olmesartan.

Olmesartan medoxomil.

This product is white or off-white tablets.

This product is suitable for the treatment of hypertension.

Dosage should be individualized. As monotherapy in normovolemic patients, the usual recommended starting dose is 20 mg once daily. For patients who still need further blood pressure reduction after 2 weeks of treatment, the dose can be increased to 40 mg. Doses greater than 40 mg have not shown a greater antihypertensive effect. When the daily dose is the same, twice-daily dosing has not shown superiority compared to once-daily dosing. This product can be taken with or without food. This product can be used in combination with other diuretics and can also be used in combination with other antihypertensive drugs. Children: Olmesartan pharmacokinetics have not been studied in people under 18 years of age. Elderly: The maximum plasma concentration of olmesartan is similar in young adults and the elderly (ge; 65 years). Mild accumulation of olmesartan was observed in elderly people with multiple doses; the mean steady-state area under the curve (AUCss) was 33% higher in the elderly, and the corresponding renal clearance (CLR) was reduced by 30%. Hepatic impairment: AUC0rarr;infin; and maximum plasma concentration (Cmax) are increased in patients with moderate hepatic impairment, with AUC increased by approximately 60%. Renal impairment: The area under the drug-time curve (AUC) after multiple doses in patients with severe renal impairment (creatinine clearance less than 20 ml/min) is approximately 3 times that of patients with normal renal function. No studies have been conducted on patients receiving hemodialysis.

The safety of Olmesartan Medoxomil was evaluated in controlled clinical trials of up to 3275 patients, of which approximately 900 patients received at least 6 months of treatment and more than 525 patients received 1 year of treatment. The results showed that Olmesartan Medoxomil was well tolerated, with an adverse event rate similar to that of the placebo group. Adverse events were generally mild and transient, and were not related to dose, age, or racial differences. In placebo-controlled clinical trials, the only adverse event with an incidence greater than 1% and higher than that of the placebo-treated group in patients treated with Olmesartan Medoxomil was dizziness (3% vs 1%); the incidence was similar to that of placebo, and the adverse events greater than 1% were: back pain, bronchitis, increased creatine phosphokinase, diarrhea, headache, hematuria, hyperglycemia, hypertriglyceridemia, pharyngitis, rhinitis, and sinusitis. The incidence of cough was similar in patients in the placebo group (0.7%) and the Olmesartan Medoxomil group (0.9%). The incidence was similar to that of the placebo group, and the adverse events with an incidence rate lower than 1% and greater than 0.5% included chest pain, fatigue, pain, peripheral edema, dizziness, abdominal pain, dyspepsia, gastroenteritis, nausea, tachycardia, hypercholesterolemia, hyperlipidemia, hyperuricemia, joint pain, arthritis, muscle pain, bone pain, rash and facial edema. It is not clear whether the above adverse events are related to this product. Laboratory test results: In clinical controlled trials, changes in clinically significant laboratory parameters were less associated with Olmesartan Medoxomil. Hemoglobin and hematocrit: Occasionally, hemoglobin and hematocrit decreased slightly (decreased by approximately 0.3g/dL and 0.3 volume percentage, respectively). Liver function tests: Occasionally, liver enzymes and/or blood bilirubin increased, but they would return to normal on their own. Past market experience: There are rare reports of rhabdomyolysis caused by angiotensin II receptor antagonists.

This product is contraindicated for use by those who are allergic to its ingredients.

Precautions for children: This experiment has not been conducted and there are no reliable references. Safety and efficacy data for children have not yet been established. Precautions for pregnancy and lactation: When pregnant women use the drug in the middle and late stages of pregnancy, drugs that directly act on the renin-angiotensin system can cause damage to the developing fetus or even death. Once pregnancy is discovered, this product should be discontinued as soon as possible. There is currently no clinical experience with the use of this product by pregnant women. It is not clear whether Olmesartan Medoxomil can be secreted through breast milk, but a small amount is secreted in the milk of lactating rats. Because of the potential adverse effects on nursing newborns, the importance of the drug to the mother must be considered to decide whether to stop breastfeeding or stop the drug. Precautions for the elderly: In clinical trials, no overall differences in the efficacy or safety of this product were observed between elderly patients and young patients, and elderly patients do not need to adjust the dose when taking this product. However, the possibility that some older individual patients are more sensitive cannot be ruled out.

Olmesartan medoxomil is not metabolized by the hepatic cytochrome P450 system and has no effect on P450 enzymes. Therefore, drug interactions related to inhibition, induction or metabolism of these enzymes will not occur. There were no significant drug interactions with the concomitant use of digoxin or warfarin in healthy subjects, and the concomitant use of antacids [Al(OH)3/Mg(OH)2] did not significantly change the bioavailability of Olmesartan medoxomil.

Keep away from light and store in sealed container.

20mg

Tentative 24 months

Beijing Foyou Pharma Co., Ltd.

• Founded in:

  1999-02-03

• Address:

  No. 8 Guangyuan East Street, Tongzhou Industrial Development Zone, Tongzhou District, Beijing

• Tax NO.:

  91110112700216160K

• Registered Funds:

  480 million yuan

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