Fulitan Allisartan Isoproxil and Amlodipine Besylate Tablets

1. Indications and Usage
Hypertension: Indicated for the treatment of primary hypertension. This fixed-dose combination is for adult patients whose blood pressure is not adequately controlled by Allisartan Isoproxil or Amlodipine Besylate monotherapy.
2. Dosage and Administration
Recommended Dose: The usual dosage is one tablet taken orally once daily.
Administration: The tablets should be swallowed whole with water and should not be crushed or chewed. The medication should be taken without food to ensure optimal absorption of Allisartan Isoproxil.
Dose Adjustment: Dosage adjustment should generally be based on the individual component requirements, and the maximum recommended daily dose is allisartan isopropil 240 mg and amlodipine besylate 5 mg.
3. Mechanism of Action
AT1 Receptor Antagonism: Allisartan Isoproxil is a prodrug rapidly metabolized into its active form, which selectively blocks the angiotensin II type 1 (AT1) receptor, inhibiting vasoconstriction and aldosterone release.
Calcium Channel Blockade: Amlodipine Besylate inhibits the influx of calcium ions into vascular smooth muscle and cardiac muscle, causing direct vasodilation.
Complementary Effects: The combination provides synergistic blood pressure lowering by targeting two different pathways of the renin-angiotensin-aldosterone system and calcium homeostasis.
4. Safety and Warnings
Pregnancy and Lactation: Contraindicated during the second and third trimesters of pregnancy due to the ARB component. It is also contraindicated during lactation.
Hepatic Impairment: Use with extreme caution in patients with severe hepatic impairment; amlodipine clearance is decreased, and allisartan isoproxil metabolism may be affected.
Hypotension: Symptomatic hypotension may occur, particularly in volume-depleted patients or those with severe heart failure.
Peripheral Edema: Amlodipine is associated with dose-dependent peripheral edema.
5. Adverse Reactions and Clinical Research
Adverse Reactions: Common adverse reactions include peripheral edema, dizziness, flushing, fatigue, headache, palpitations, and gastrointestinal disturbances.
Clinical Research: Clinical trials have demonstrated that the combination therapy provides significantly greater blood pressure reduction compared to monotherapy in patients with inadequate blood pressure control.
6. Drug Interactions
Strong CYP3A4 Inhibitors: Concomitant use with drugs like ketoconazole or ritonavir may significantly increase amlodipine plasma concentrations, increasing the risk of hypotension and edema.
Lithium: Concomitant use with lithium may cause reversible increases in serum lithium levels and toxicity.
NSAIDs: Non-steroidal anti-inflammatory drugs may weaken the antihypertensive effect of the combination.
7. Pharmaceutical Information
Composition: The active ingredients are Allisartan Isoproxil and Amlodipine Besylate.
Appearance: Film-coated tablets, appearing white to off-white when the coating is removed.
Storage: Store in a dry place, protected from light, at controlled room temperature.