Product Overview
[Drug Name]
Generic Name: Amlodipine Besylate Tablets
Trade Name: YiTong Amlodipine Besylate Tablets 5mg*24 Tablets
Pinyin Full Code: YiTong BenHuangSuanAnLvDiPingPian 5mg*24 Tablets
[Main Ingredient]
The main ingredient of this product is amlodipine besylate.
[Properties]
This product is a white or off-white tablet.
[Indications/Main Functions]
1. Hypertension: This product is indicated for the treatment of hypertension. It can be used alone or in combination with other antihypertensive drugs. Hypertension control is part of a comprehensive cardiovascular risk management strategy that 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 in blood pressure 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. For patients with severe hypertension, even a slight reduction in blood pressure can provide significant clinical benefits. In adults with hypertension, lowering blood pressure generally reduces the risk of cardiovascular events, primarily stroke and myocardial infarction. 2. Coronary Artery Disease (CAD) - Chronic Stable Angina: This product is indicated for the symptomatic treatment of chronic stable angina. It can be used alone or in combination with other anti-anginal medications. Vasospastic Angina (Prinzmetal's or Variant Angina): This product is indicated for the treatment of confirmed or suspected vasospastic angina. It can be used alone or in combination with other anti-anginal medications. For patients with angiographically confirmed CAD, an ejection fraction ≥40%, and no heart failure, this product can reduce the risk of hospitalization for angina and the need for coronary revascularization.
[Specifications]
5mg*24 tablets
[Dosage and Administration]
The typical starting dose for 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 with an incidence greater than 1% were as follows: edema, dizziness, flushing, and palpitations. Adverse reactions with unclear dose relationships but an incidence greater than 1.0% were as follows: headache, fatigue, nausea, abdominal pain, and somnolence. Among these adverse reactions, edema, flushing, 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, asthenia, 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, orthostatic hypotension, and vasculitis; Central and Peripheral Nervous System: hypoesthesia, peripheral neuropathy, paresthesia, tremor, vertigo; Gastrointestinal: anorexia, constipation, dyspepsia, dysphagia, diarrhea, flatulence, pancreatitis, vomiting 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 nitrogen, or creatinine. Post-marketing, there have been occasional reports of gynecomastia in patients taking the drug, but a causal relationship to the drug 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 allergic to dihydropyridine calcium channel blockers or any of its ingredients.
[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, particularly 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 amlodipine's vasodilatory effect develops gradually, rare cases of acute hypotension have been reported following its use. However, caution should be exercised when using amlodipine in combination with other peripheral vasodilators in patients with severe aortic stenosis. 3. Use in Patients with Heart Failure: Calcium channel blockers should be used with caution in patients with congestive heart failure. In a long-term, placebo-controlled study (PRAISE-2) in patients with non-ischemic heart failure (NYHA class II-IV), although the incidence of heart failure exacerbations was not significantly different compared with placebo, there was an increase in reports of pulmonary edema associated with amlodipine. 4. Use in Patients with Impaired Hepatic Function: As with all other calcitonin antagonists, the half-life of amlodipine is prolonged in patients with impaired hepatic function, but a recommended dose has not yet been established. Therefore, caution should be exercised when using this product. 5. Use in Patients with Renal Failure: Changes in amlodipine plasma concentrations are not correlated with the degree of renal impairment; therefore, a normal dose can be used. This product cannot be dialyzed. Please read the package insert carefully and use as directed by your doctor.
[Pediatric Use]
The recommended dose of this product for children aged 6 to 17 years with hypertension is 2.5 mg to 5 mg once daily. No studies have been conducted in pediatric patients using doses exceeding 5 mg daily.
[Elderly Use]
There are currently no clinical studies to determine whether elderly patients (over 65 years) respond differently to this product than younger patients. Other clinical studies have not demonstrated differences in responses between elderly and younger patients. Generally speaking, given that elderly patients often have decreased liver, kidney, or heart function, as well as a greater likelihood of concurrent illnesses or concomitant medication use, dose selection for elderly patients requires caution. Generally, a low dose within the recommended starting dose range is recommended. 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]
Amlodipine 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 demonstrate that amlodipine binds to both dihydropyridine and non-dihydropyridine binding sites. Cardiac and vascular smooth muscle contraction relies on the entry of extracellular calcium ions into the cell through ion channels. Amlodipine selectively inhibits transmembrane calcium transport, with a stronger effect on vascular smooth muscle cells than on myocardial cells. Negative inotropic effects have been observed in vitro, but these effects have not been observed in live animals at clinically effective doses. Amlodipine does not affect serum calcium concentrations. Within the physiological pH range, amlodipine is an ionized complex (pKa = 8.6), achieving its gradual onset of action through slow binding and dissociation at the calcium channel receptor binding site.
