Anye Amlodipine Besilate and Folic Acid Tablets (II)

1. Indications and Usage
Essential Hypertension: Indicated for the treatment of essential hypertension.
Hcy Reduction: Specifically indicated for patients with hypertension accompanied by elevated plasma homocysteine (Hcy) levels, as the combination provides dual benefits of blood pressure control and cardiovascular risk reduction.
2. Dosage and Administration
Recommended Dose: Usually 1 tablet once daily. The initial and maintenance doses vary by specific product specification (e.g., 5.8 mg or 5.4 mg per tablet).
Administration: Swallow the tablet whole with water. It can be taken before or after meals.
Dose Titration: The dose should be adjusted based on individual blood pressure control and tolerance. The adjustment interval should generally be no less than 7 to 14 days. The maximum daily dose is typically limited to two tablets of 5.4 mg strength.
3. Mechanism of Action
Amlodipine Besilate: A long-acting calcium channel blocker that inhibits the influx of extracellular calcium into vascular smooth muscle and cardiac muscle cells. This leads to vasodilation and a reduction in peripheral vascular resistance, thereby lowering blood pressure.
Folic Acid: A vitamin B9 derivative that acts as a cofactor in the methionine cycle. It facilitates the conversion of homocysteine to methionine, effectively lowering plasma homocysteine levels and reducing endothelial damage.
4. Safety and Warnings
Hypotension: Symptomatic hypotension may occur, especially in patients with severe aortic stenosis or severe heart failure.
Ankle Edema: Peripheral edema is a common side effect of calcium channel blocker therapy.
Vitamin B12 Deficiency: In patients with suspected vitamin B12 deficiency or megaloblastic anemia, folic acid supplementation may mask hematologic signs of B12 deficiency, potentially allowing neurological symptoms to progress.
Hepatic Impairment: Amlodipine is extensively metabolized by the liver. Patients with severe hepatic impairment require slower dose titration and close monitoring.
5. Adverse Reactions and Clinical Research
Adverse Reactions: The most common adverse reactions include dizziness, peripheral edema, flushing, palpitations, fatigue, and gastrointestinal disorders.
Clinical Research: Clinical trials have demonstrated that this combination effectively lowers both blood pressure and homocysteine levels, offering superior cardiovascular protection compared to monotherapy in patients with hypertension and hyperhomocysteinemia.
6. Drug Interactions
CYP3A4 Inhibitors: Strong or moderate CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase plasma concentrations of amlodipine, potentially increasing the risk of hypotension and edema.
CYP3A4 Inducers: CYP3A4 inducers (e.g., rifampin, St. John’s Wort) may decrease the efficacy of amlodipine.
Sildenafil: Concomitant use may independently lower blood pressure; blood pressure should be monitored.
Antiepileptics: High-dose folic acid can antagonize the antiepileptic effects of phenobarbital, phenytoin, and primidone.
7. Pharmaceutical Information
Composition: Each tablet contains varying ratios of amlodipine besilate (5 mg) and folic acid (0.8 mg).
Appearance: The tablets are typically pale yellow or yellow, with “5.8” engraved on one side.
Storage: Store at controlled room temperature and protect from moisture.