Product Overview
[Drug Name]
Generic Name: Amifendipine Besylate Tablets
Trade Name: Shan Nuoning Amifendipine Besylate Tablets 5mg*7 Tablets
Pinyin Full Code: ShanNuoNing BenHuangSuanAnLvDiPingPian 5mg*7 Tablets
[Main Ingredient]
The main ingredient of this product is amifendipine besylate.
[Properties]
This product is white or off-white tablets.
[Indications/Main Functions]
1. Hypertension. This product can be used alone or in combination with other antihypertensive drugs. 2. Chronic stable angina and variant angina. This product can be used alone or in combination with other antianginal drugs.
[Specifications]
5mg*7 tablets
[Dosage and Administration]
The usual starting dose for treating hypertension is 5mg once daily, with a maximum dose of 10mg once daily. For patients who are small, frail, elderly, or have hepatic insufficiency, the starting dose is 2.5 mg once daily; this dose can also be used in combination with other antihypertensive medications.
[Adverse Reactions]
This drug is well tolerated within the 10 mg/day dose range, with most adverse reactions being mild to moderate. Discontinuation due to adverse reactions was only 1.5%, not significantly different from placebo (approximately 1%). The most common adverse reactions were headache and edema. Dose-related adverse reactions occurring in >1% of patients were as follows: edema, dizziness, hot flashes, and palpitations. Adverse reactions with unclear dose relationships but occurring in >1% of patients were as follows: headache, fatigue, nausea, abdominal pain, and somnolence. Among these adverse reactions, edema, hot flashes, palpitations, and somnolence were more common in women than in men. What is the incidence of the following adverse events? 1% but >0.1%, causal relationship to drug unclear: General: allergic reaction, weakness, back pain, hot flashes, malaise, pain, stiffness, weight gain; Cardiovascular: arrhythmia (including tachycardia, bradycardia, or atrial fibrillation), chest pain, hypotension, peripheral ischemia, syncope, postural dizziness, postural hypotension, and vasculitis; Central and peripheral nervous system: hypoesthesia, peripheral neuropathy, paresthesia, tremors, vertigo; Gastrointestinal: anorexia, constipation, dyspepsia, dysphagia, diarrhea, flatulence, pancreatitis, Vomiting, gingival hyperplasia; Musculoskeletal system: arthralgia, arthritis, muscle cramps, myalgia; Psychiatric system: sexual dysfunction, insomnia, tension, depression, nightmares, anxiety, depersonalization; Skin and appendages: angioedema, erythema, pruritus, rash, maculopapular rash; Special senses: visual disturbances, conjunctivitis, diplopia, eye pain, tinnitus; Urinary system: frequent urination, dysuria, nocturia; Autonomic nervous system: dry mouth, night sweats; Metabolic and nutritional system: hyperglycemia, thirst; Hematopoietic system: leukopenia, purpura, thrombocytopenia. What is the incidence of the following adverse events? 0.1%: Heart failure, irregular pulse, extrasystoles, skin discoloration, urticaria, dry skin, dermatitis, alopecia, muscle weakness, tremors, ataxia, hypertonia, migraine, cold and clammy skin, apathy, agitation, amnesia, gastritis, increased appetite, loose stools, cough, rhinitis, dysuria, polyuria, parosmia, taste disturbances, visual accommodation disturbances, and xerophthalmia. Other rare reactions, such as myocardial infarction and angina, cannot be distinguished as drug effects or disease states. Routine laboratory tests were unremarkable, with no significant changes in serum potassium, blood glucose, triglycerides, total cholesterol, high-density lipoprotein (HDL), uric acid, blood urea, or creatinine. Post-marketing, there have been occasional reports of gynecomastia in patients taking the drug, but a causal relationship is unclear. In some cases, jaundice and elevated liver enzymes (often associated with cholestasis and hepatitis) have been severe, requiring hospitalization.
[Contraindications]
This product is contraindicated in patients with hypersensitivity to dihydropyridine calcium channel blockers or any of the ingredients in this product.
[Drug Interactions]
This product does not affect the binding of digoxin, phenytoin, warfarin, or indomethacin to plasma proteins.
[Precautions]
1. Warning: A very small number of patients, especially those with severe coronary artery obstructive disease, may experience increased frequency, prolonged duration, and/or worsening of angina pectoris, or acute myocardial infarction, when initiating or increasing the dose of calcium channel blockers. The mechanism of action is currently unknown. 2. Because the vasodilatory effect of ammonia is gradual, rare cases of acute hypotension have been reported following ammonia administration. However, caution should be exercised when using ammonia channel blockers in combination with other peripheral vasodilators in patients with severe aortic stenosis. 3. Use in Patients with Congestive Heart Failure: Calcium channel blockers should be used with caution in patients with congestive heart failure. In patients with non-ischemic heart failure (NYHA) In a long-term, placebo-controlled study (PRAISE-2) conducted at a level II-IV, although the incidence of worsening heart failure was not significantly different from placebo, there was an increase in reports of pulmonary edema associated with amlodipine. 4. Use in patients with impaired liver function: Like all other calcium antagonists, the half-life of amlodipine is prolonged in patients with impaired liver function, but the corresponding recommended dose has not yet been determined. Therefore, this product should be used with caution. 5. Use in patients with renal failure: Changes in the blood concentration of amlodipine are not correlated with the degree of renal impairment. Therefore, a normal dose can be used. This product cannot be dialyzed. Please read the instructions carefully. Use as directed by your doctor.
[Pediatric Use]
The recommended dose of this drug for hypertensive children aged 6 to 17 years is 2.5 mg to 5 mg once daily. No studies have been conducted on pediatric patients using doses exceeding 5 mg daily.
[Elderly Use]
Currently, no clinical studies have determined whether elderly patients (over 65 years) respond differently to this drug than younger patients. Other clinical studies have not found differences in responses between elderly and younger patients. Generally speaking, given that elderly patients are often more likely to have impaired liver, kidney, or heart function, as well as to have concurrent illnesses or to be taking other medications, the elderly are more likely to be treated with this drug. Caution should be exercised in selecting the dose for elderly patients; it is generally advisable to start with a low dose within the dosage range. Elderly patients have decreased clearance of this drug, resulting in an approximately 40-60% increase in the area under the curve (AUC), so a low starting dose is recommended.
[Overdose]
Severe overdose may result in excessive peripheral vasodilation accompanied by significant hypotension and reflex tachycardia.
[Pharmacology and Toxicology]
Amifedipine is a dihydropyridine calcium antagonist (also known as a calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane entry of calcium ions into vascular smooth muscle and myocardium. Experimental data indicate that amifedipine binds to dihydropyridines and non-dihydropyridines at the same site. The contraction of cardiac and vascular smooth muscle depends on the entry of extracellular calcium ions into the cell through ion channels. Amifloxacin selectively inhibits transmembrane calcium transport, with a stronger effect on vascular smooth muscle cells than on cardiac cells. Negative inotropic effects have been observed in vitro, but this effect has not been observed in live animals at clinical therapeutic doses. Amifloxacin does not affect serum calcium concentrations. Within the physiological pH range, amifloxacin is an ionized complex (pKa = 8.6) that achieves its gradual onset of action by slowly binding to and dissociating from calcium channel receptors at their binding sites.
