Product Overview
[Drug Name]
Generic Name: Olmesartan Medoxomil Tablets
Trade Name: Shengyu Olmesartan Medoxomil Tablets 20mg*7 Tablets
Pinyin Full Code: ShengYu AoMeiShaTanZuoPian 20mg*7 Tablets
[Main Ingredients]
The main ingredient of this product is Olmesartan Medoxomil. Chemical Name: 2,3-Dihydroxy-2-butenyl-4-(1-hydroxy-1-methylethyl)-2-propyl-1-[p-(o-1H-tetrazol-5-phenyl)benzyl]imidazole-5-carboxylate, cyclo-2,3-carbonic acid. Molecular Formula: C29H30N6O6. Molecular Weight: 558.59
[Properties]
This product is a film-coated tablet that appears white or off-white after removal of the coating.
[Indications/Main Functions]
This product is indicated for the treatment of hypertension. Hypertension control is part of comprehensive cardiovascular risk management, which may include lipid control, diabetes management, antithrombotic therapy, smoking cessation, physical exercise, and sodium restriction. Increases in either systolic or diastolic blood pressure increase cardiovascular risk. The absolute risk increase per mmHg increase is greater at higher baseline blood pressure levels. The relative magnitude of risk reduction achieved by lowering blood pressure is similar among individuals with varying absolute cardiovascular risk. In patients with severe hypertension, even a small reduction in blood pressure can provide a significant clinical benefit. In adults with hypertension, lowering blood pressure generally reduces the risk of cardiovascular events, primarily stroke and myocardial infarction. However, there is no controlled clinical evidence that this product reduces cardiovascular risk.
[Specifications]
20mg*7 tablets
[Dosage and Administration]
The dosage should be individualized. In normovolemic patients, as monotherapy, the recommended starting dose is 20mg once daily. For patients who require further blood pressure lowering after two weeks of treatment, the dose can be increased to 40mg. Doses greater than 40mg have not demonstrated a greater antihypertensive effect. When the daily dose is the same, twice-daily dosing has not been shown to be superior to once-daily dosing. Olmesartan medoxomil can be taken with or without food. It can be used in combination with other diuretics and other antihypertensive drugs. No dose adjustment is required for elderly patients and patients with moderate to significant hepatic or renal impairment (creatinine clearance <40 mL/minute) (see Special Populations under Pharmacokinetics). Olmesartan medoxomil must be used under close medical supervision in patients with potential volume depletion (e.g., those receiving diuretics, particularly those with renal impairment), and a lower starting dose may be considered.
[Adverse Reactions]
Clinical Trial Experience: The safety of olmesartan medoxomil was evaluated in controlled clinical trials involving up to 3,275 patients, of whom approximately 900 received treatment for at least six months and over 525 received treatment for at least one year. 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 associated with dose, gender, age, or race. In placebo-controlled clinical trials, the only adverse event with an incidence greater than 1% and higher in patients receiving olmesartan medoxomil than in those receiving placebo was dizziness (3% vs. 1%). Adverse events with an incidence greater than 1% and similar to or lower than that of the placebo group included back pain, bronchitis, increased creatine phosphokinase, diarrhea, headache, hematuria, hyperglycemia, hypertriglyceridemia, flu-like symptoms, pharyngitis, rhinitis, and sinusitis. The incidence of cough was similar in patients receiving placebo (0.7%) and olmesartan medoxomil (0.9%). Adverse events with an incidence rate similar to that of the placebo group, less than 1%, and greater than 0.5% included chest pain, fatigue, 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 the use of this product is unknown. Laboratory Test Results: In controlled clinical trials, changes in clinically important laboratory parameters were rarely associated with olmesartan medoxomil. Hemoglobin and hematocrit: Slight decreases in hemoglobin and hematocrit were occasionally observed (mean decreases of approximately 0.3 g/dL and 0.3 volume percent, respectively). Liver Function Tests: Elevated liver enzymes and/or blood bilirubin were occasionally observed, but these elevations resolved spontaneously. Postmarketing Experience: The following adverse reactions have been reported postmarketing. Because these adverse reactions are reported voluntarily from an uncertain number of patients, their incidence and causal relationship to the drug cannot generally be definitively assessed. General: Asthenia, fatigue, drowsiness, malaise, peripheral edema, angioedema, allergic reactions. Gastrointestinal: Abdominal pain, nausea, vomiting, diarrhea, sprue-like enteropathy. Respiratory: Cough. Neurologic: Headache. Metabolic and Nutritional: Hyperkalemia. Musculoskeletal: Rhabdomyolysis, myalgia. Genitourinary: Acute renal failure, increased serum creatinine. Skin and Appendages: Alopecia, pruritus, rash, urticaria. Data from a controlled trial and epidemiological studies suggest that high-dose olmesartan may increase cardiovascular (CV) risk in patients with diabetes, but overall data are inconclusive. The ROADMAP (Olmesartan vs. Diabetes Microalbuminuria Prevention Randomized Trial, n=4447) randomized, placebo-controlled, double-blind study evaluated olmesartan 40 mg/day versus placebo in patients with type 2 diabetes, normoalbuminuria, and at least one other CV risk factor (with or without hypertension). The study achieved its primary endpoint of delaying the onset of microalbuminuria, but olmesartan showed no benefit in reducing glomerular filtration rate (GFR). Results showed that CV mortality (specifically sudden cardiac death, fatal myocardial infarction, fatal stroke, and death requiring revascularization) was higher in the olmesartan group than in the placebo group (15 patients in the olmesartan group vs. 3 patients in the placebo group, HR 4.9, 95% confidence interval [CI] 1.4, 1.7), but the risk of nonfatal myocardial infarction was lower in the olmesartan group (HR 0.64, 95% CI 0.35, 1.18). The epidemiological study included patients aged 65 years and older, with a total exposure of >300,000 patient-years. The subgroup of diabetic patients who received high-dose olmesartan (40 mg/day) for >6 months had a higher risk of death than those receiving other angiotensin receptor blockers (HR 2.0, 95% CI 1.1, 3.8). Conversely, nondiabetic patients receiving high-dose olmesartan had a lower risk of death compared with nondiabetic patients receiving other angiotensin receptor blockers (HR 0.46, 95% CI 0.24, 0.86). No difference was observed between patients receiving low-dose olmesartan and those receiving other angiotensin receptor blockers or those treated for less than 6 months. In summary, these data raise concerns about a potential increase in cardiovascular risk with high-dose olmesartan in patients with diabetes. However, the robustness of these findings is of concern. Of note, large epidemiological studies demonstrating a survival benefit in nondiabetic patients have similarly observed adverse outcomes in patients with diabetes.
[Contraindications]
This product is contraindicated in patients with allergies to its ingredients. This product should not be used in combination with aliskiren in patients with diabetes.
[Precautions]
Fetal toxicity: During the second and third trimesters of pregnancy, the use of drugs that directly act on the renin-angiotensin system can reduce fetal renal function and increase fetal and neonatal morbidity and mortality. The resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformities. Potential neonatal adverse reactions include craniosynostosis, anuria, hypotension, renal failure, and death. Upon detection of pregnancy, this product should be discontinued as soon as possible (see [Use in Pregnant and Lactating Women]). Neonatal morbidity: This product should not be used to treat hypertension in children under one year of age. Drugs that directly act on the renin-angiotensin system can affect immature renal development. Hypotension in patients with volume depletion or hyponatremia: Patients with volume depletion or hyponatremia (e.g., those receiving high-dose diuretics) may experience symptomatic hypotension after the first dose of this product and must be treated under close medical supervision. If hypotension occurs, the patient should be placed supine and normal saline administered intravenously as needed. Treatment with this medication may be continued once blood pressure stabilizes. Renal Impairment: Use of ACE inhibitors and angiotensin receptor blockers in patients whose renal function depends on the activity of the renin-angiotensin-aldosterone system (e.g., patients with severe congestive heart failure) has been associated with oliguria and/or progressive azotemia, acute renal failure, and/or death (rarely). Olmesartan therapy in such patients might be expected to produce similar outcomes. Renal Impairment: Olmesartan blood concentrations are increased in patients with renal impairment compared with those with normal renal function. After multiple doses, the AUC in patients with severe renal impairment (creatinine clearance <20 mL/minute) is approximately three times the normal value. Olmesartan pharmacokinetics have not been studied in patients undergoing hemodialysis. No initial dose adjustment is required in patients with moderate to marked renal impairment (creatinine clearance <40 mL/minute). Hepatic Impairment: Compared with controls, patients with moderate hepatic impairment have observed increases in both AUC and maximum plasma concentration (Cmax), with an approximately 60% increase in AUC. No initial dose adjustment is required in patients with moderate to marked hepatic impairment. Renal Artery Stenosis: ACE inhibitors have been reported to increase serum creatinine or blood urea nitrogen (BUN) in patients with unilateral or bilateral renal artery stenosis. Long-term use of olmesartan medoxomil in such patients is not available, but similar results are possible. Sprue-like Enteropathy: Severe, chronic diarrhea accompanied by significant weight loss has been reported in patients taking olmesartan for months to years. Intestinal biopsies often reveal signs of villous atrophy. If these symptoms occur while taking olmesartan, alternative etiologies should be excluded. If no alternative etiology is found, consider discontinuing this medication. Electrolyte Imbalance: This medication contains olmesartan. Olmesartan inhibits the renin-angiotensin system (RAS). Drugs that inhibit the renin-angiotensin system (RAS) may cause hyperkalemia, and serum electrolytes should be monitored regularly. Like other ACE inhibitors, beta-blockers, and other angiotensin receptor blockers, this medication may have a lesser antihypertensive effect in black patients (who typically have low renin levels).
