Product Overview
[Drug Name]
Generic Name: Olmesartan Medoxomil Tablets
Trade Name: Ao Tan
English Name: Olmesartan Medoxomil Tablets
Chinese Pinyin: Aomeishatanzhi Pian
[Ingredients]
Olmesartan Medoxomil.
[Properties]
This product is white or off-white tablets.
[Indications]
This product is indicated for the treatment of hypertension.
[Dosage and Administration]
The dosage should be individualized. As monotherapy in normovolemic patients, the recommended starting dose is 20 mg once daily. For patients who require further blood pressure lowering after two weeks of treatment, the dose can be increased to 40 mg. Doses greater than 40 mg have not demonstrated a greater antihypertensive effect. When the daily dose is the same, twice-daily dosing has not demonstrated 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 other antihypertensive medications. Children: The pharmacokinetics of olmesartan have not been studied in children under 18 years of age. Elderly: Maximum plasma concentrations of olmesartan are similar in young adults and elderly adults (≥65 years). Mild accumulation of olmesartan was observed in elderly patients with multiple doses; the mean steady-state area under the concentration-time curve (AUCss) was 33% higher in elderly patients, corresponding to a 30% decrease in renal clearance (CLR). Hepatic Impairment: Both AUC0° and maximum plasma concentration (Cmax) were increased in patients with moderate hepatic impairment, with AUC increased by approximately 60%. Renal Impairment: The area under the concentration-time curve (AUC) after multiple doses in patients with severe renal impairment (creatinine clearance <20 ml/min) was approximately three times that of subjects with normal renal function. Patients undergoing hemodialysis have not been studied.
[Adverse Reactions]
The safety of olmesartan medoxomil was evaluated in controlled clinical trials involving up to 3275 patients, of whom approximately 900 received treatment for at least 6 months and more than 525 received treatment for 1 year. 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 unrelated to dose, age, and race. 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 receiving Olmesartan medoxomil was dizziness (3% vs 1%); adverse events with an incidence greater than 1% similar to that of placebo included: 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%). Adverse events with an incidence rate similar to that of the placebo group, less than 1% but greater than 0.5%, included chest pain, nausea, pain, peripheral edema, dizziness, abdominal pain, dyspepsia, gastroenteritis, nausea, tachycardia, hypercholesterolemia, hyperlipidemia, hyperuricemia, arthralgia, arthritis, myalgia, bone pain, rash, and facial edema. Whether these adverse events are related to Olmesartan medoxomil is unclear. Laboratory Test Results: In controlled clinical trials, clinically significant changes in laboratory parameters were rarely associated with Olmesartan medoxomil.
[Contraindications]
This product is contraindicated in patients with allergies to its ingredients.
[Precautions]
1. Renal Artery Stenosis: There have been reports that ACE inhibitors may increase serum creatinine or blood urea nitrogen (BUN) in patients with unilateral or bilateral renal artery stenosis. However, there is no experience with long-term use of Olmesartan in such patients, but similar results are possible. 2. Renal Impairment: In patients whose renal function depends on the activity of the renin-angiotensin-aldosterone system (such as those with severe, well-established heart failure), the use of ACE inhibitors and AT1 receptor antagonists may result in oliguria and/or progressive azotocin-induced renal failure and/or death (rarely). Olmesartan medoxomil should be used in such patients. 3. Fetal/Neonatal Morbidity and Mortality: In pregnancy category D (fifth and second trimesters), drugs directly acting on the renin-angiotensin-aldosterone system have been associated with fetal and neonatal harm. Olmesartan should be discontinued as soon as pregnancy is detected. If medication is necessary, pregnant women should be informed of the potential risk to their fetus, and serial ultrasounds should be performed to assess intraamniotic fluid. Infants who have been exposed to angiotensin-receptor antagonists in utero should be closely monitored for hypotension, oliguria, and hyperkalemia, and appropriate treatment should be administered if necessary. 4. Hypovolemia or Hyponatremia: Patients with hypotension due to hypovolemia or hyponatremia (e.g., those receiving high-dose diuretics) may experience symptomatic hypotension after their first dose of Olmesartan. Treatment with this medication must be conducted under close medical supervision. If hypotension occurs, the patient should lie supine.
[Special Population Use]
Precautions for Pediatric Use:
Safety and efficacy data for this medication have not been established in children.
Precautions for Pregnancy and Lactation:
Pregnant and lactating women are contraindicated.
Precautions for the Elderly:
In clinical trials, no overall differences in the efficacy or safety of Olmesartan were observed between elderly and younger patients. Dosage adjustment is not required for elderly patients. However, the possibility of increased sensitivity in some older individuals cannot be ruled out.
[Drug Interactions]
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 are unlikely. Concomitant use of digoxin or warfarin in healthy subjects did not result in significant drug interactions, and concomitant use of antacids [Al(OH)3/Mg(OH)2] did not significantly alter the bioavailability of olmesartan medoxomil.
[Pharmacological Action]
Angiotensin I (ATI) is converted to angiotensin II (ATII) catalyzed by angiotensin-converting enzyme (ACE, kinase II). Angiotensin II is the primary pressor of the renin-angiotensin system, with actions including vasoconstriction, stimulation of aldosterone synthesis and release, cardiac stimulation, and increased renal sodium reabsorption. Olmesartan medoxomil is a prodrug that is absorbed and hydrolyzed to olmesartan via the gastrointestinal tract. Olmesartan is a selective angiotensin II type 1 receptor (AT1) antagonist. It blocks the vasoconstrictive effects of angiotensin II by selectively blocking its binding to the AT1 receptor on vascular smooth muscle, thus acting independently of the ATII synthesis pathway. Olmesartan has an affinity for AT1 that is over 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 antihypertensive drugs. However, ACE inhibitors also inhibit the degradation of bradykinin. Olmesartan medoxomil does not inhibit ACE and therefore does not affect bradykinin. The clinical relevance of this difference 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.
Storage: Store in a sealed container away from light.
Strength: 20 mg
Packaging: 20 mg x 7 tablets
Expiration Date: 36 months
Approval Number: National Medicine Standard H20060371
Manufacturer: Daiichi Sankyo Pharmaceutical (Shanghai) Co., Ltd.
