Product Overview
[Drug Name]
Generic Name: Amlodipine Besylate Tablets
Trade Name: Bilodipine
English Name: Amlodipine Besylate Tablets
Chinese Pinyin: Benhuɑnɡsuɑn Anlüdipinɡ Pian
[Ingredients]
The chemical name of this product is: 3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate. Molecular formula: C20H25ClN2O5C6H6O3S, molecular weight: 567.1.
[Properties]
This product is a white tablet.
[Indications]
Hypertension and angina pectoris.
[Dosage and Administration]
The usual starting oral dose is 5 mg once daily, with a maximum of 10 mg once daily. For thin patients, those with frail constitutions, elderly patients, or those with impaired liver function, the dosage should be started at 2.5 mg once daily. Patients taking other antihypertensive medications should also start at this dose. The dosage should be adjusted based on individual needs, and the adjustment period should be at least 7-14 days to allow the physician to fully assess the patient's response to the dose. However, more rapid adjustment can be performed if clinically warranted. The recommended dose for treating angina pectoris is 5-10 mg; elderly patients or those with impaired liver function may require a reduced dose.
[Adverse Reactions]
This product is well tolerated within the 10 mg/day dose range, with most adverse reactions being mild to moderate. Discontinuation rates due to adverse reactions were only 1.5%, which was 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, flushing, and palpitations. Adverse reactions with unclear dose relationships but occurring in more than 1.0% of patients were as follows: headache, fatigue, nausea, abdominal pain, and somnolence. Among the above adverse reactions, edema, flushing, palpitations and drowsiness occur more frequently in women than in men. The incidence of the following adverse events is less than 1% but 0.1%, and the causal relationship with the drug is unclear: General: allergic reaction, weakness, back pain, hot flashes, discomfort, 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: decreased sensation, peripheral neuropathy, paresthesia, tremor, dizziness; Gastrointestinal: anorexia, constipation, dyspepsia, dysphagia, diarrhea, flatulence, Pancreatitis, vomiting, gingival hyperplasia; musculoskeletal system: arthralgia, arthritis, muscle cramps, myalgia; psychiatric: sexual dysfunction, insomnia, tension, depression, nightmares, anxiety, depersonalization; skin and appendages: angioedema, erythema, pruritus, rash, maculopapular rash; special senses: visual abnormalities, conjunctivitis, diplopia, eye pain, tinnitus; urinary system: frequent urination, dysuria, nocturia; autonomic nervous system: dry mouth, night sweats; metabolism and nutrition: hyperglycemia, thirst; hematopoietic system: leukopenia, purpura, thrombocytopenia. The incidence of the following adverse events is less than 0.1%: heart failure, irregular pulse, extrasystoles, skin discoloration, urticaria, dry skin, dermatitis, alopecia, muscle weakness, twitching, 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]
Allergic to dihydropyridine calcium channel blockers.
[Precautions]
1. Angina and/or Myocardial Infarction: Rare. Patients with severe obstructive coronary artery disease may experience an increase in the frequency, duration, and/or severity of angina attacks, or the development of acute myocardial infarction, when initiating or increasing the dose of calcium channel blockers. The mechanism is unknown. 2. Hypotension: Due to the gradual onset of vasodilatory effects, acute hypotension is generally uncommon with oral administration. However, caution is advised when using this drug in combination with other peripheral vasodilators, especially in patients with severe aortic stenosis. 3. Patients with Heart Failure: Calcium channel blockers should be used with caution in patients with heart failure. 4. Patients with Hepatic Insufficiency: This drug should be used with caution in patients with severe hepatic insufficiency. 5. Patients with Renal Failure: The starting dose can be maintained in patients with renal failure. 6. Discontinuation of β-blockers: This drug does not protect against rebound symptoms associated with abrupt discontinuation of β-blockers. Therefore, a gradual dose reduction is still necessary when discontinuing β-blockers. 7. This drug can be safely used in patients with obstructive pulmonary disease, well-compensated heart failure, peripheral vascular disease, diabetes, and lipid disorders.
[Use in Special Populations]
Precautions for Pediatric Use: Safety and efficacy in children have not been established.
Precautions for Pregnancy and Lactation: Research data on its use in pregnant women are lacking, but based on animal studies, this drug should be used in pregnant women only when absolutely necessary. It is unknown whether this drug is excreted in breast milk; lactating women taking this drug should discontinue breastfeeding.
Precautions for Elderly Use: Clinical studies have not demonstrated a difference in the response of the elderly compared to younger adults to this drug. However, given that the elderly often have impaired liver, kidney, and heart function, as well as other medical conditions and medications, the lower end of the initial dose range is generally used. Elderly individuals experience decreased clearance of this drug, with an increase in the area under the curve (AUC) of approximately 40% to 60%, necessitating a lower initial dose.
[Drug Interactions]
1. Cimetidine, grapefruit juice, and acidogens: Coadministration does not alter the pharmacokinetics of this drug. 2. Atorvastatin, digoxin, and ethanol: This drug does not affect their pharmacokinetics. 3. Sildenafil: Single-dose sildenafil has no effect on the pharmacokinetics of this drug in patients with essential hypertension. The two drugs produce an independent antihypertensive effect when taken together. 4. Warfarin: This drug does not alter the prothrombin effect of warfarin.
[Pharmacological Action]
Amlodipine besylate is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker). Cardiac and smooth muscle contraction depends on the entry of extracellular calcium ions into cells through specific ion channels. This drug selectively inhibits the transmembrane entry of calcium ions into smooth muscle cells and cardiomyocytes, resulting in a greater effect on smooth muscle than on cardiac muscle. Its interaction with calcium channels is determined by the progressive rate of binding and dissociation between it and its receptor sites, resulting in a gradual onset of pharmacological action. This drug is a peripheral arterial dilator that acts directly on vascular smooth muscle, reducing peripheral vascular resistance and thereby lowering blood pressure. At therapeutic doses, negative inotropic effects have been observed in vitro but not in whole animal studies. This product does not affect plasma calcium concentration. Fifteen randomized, double-blind, placebo-controlled clinical trials have confirmed its antihypertensive effects. A once-daily dose in patients with mild to moderate hypertension can lower supine and standing blood pressure for 24 hours. Long-term use does not cause significant changes in heart rate or plasma catecholamines. The antihypertensive effect is stable. The antihypertensive effect is dose-related, and the magnitude of the reduction is related to pre-treatment blood pressure. The efficacy is greater in patients with moderate hypertension (diastolic blood pressure 105-114 mmHg) than in those with mild hypertension (diastolic blood pressure 90-104 mmHg). There is no significant effect in patients with normal blood pressure. This product has a similar diastolic blood pressure-lowering effect in older and younger adults, but a stronger systolic blood pressure-lowering effect in older adults. The precise mechanism by which this drug relieves angina is unclear, but it may treat exertional angina by reducing peripheral resistance (afterload), thereby reducing cardiac work and the heart rate-blood pressure product, and thus lowering myocardial oxygen demand. It also treats spontaneous angina by inhibiting calcium, epinephrine, 5-hydroxytryptamine, and thromboxane A2-induced coronary artery and arteriolar constriction, thereby restoring blood supply to the ischemic area. Five of eight clinical trials demonstrated that this drug significantly prolonged the duration of exercise-induced exertional angina. Some studies also showed that this drug prolonged the time to a 1mm ST-segment depression and reduced the frequency of angina attacks. This effect was sustained and did not significantly affect blood pressure or heart rate. In a clinical trial of 50 patients with spontaneous angina, this drug reduced angina attacks by four per week (compared to one per week with placebo). In patients with normal cardiac function, resting and exercise hemodynamics were assessed after taking this drug, and cardiac ejection fraction increased, but there was no significant effect on dP/dt or left ventricular end-diastolic pressure/volume. At therapeutic doses, amlodipine does not cause negative inotropic effects when used alone or in combination with beta-blockers. In a placebo-controlled study, 697 patients with NYHA class II/III heart failure showed no worsening of heart failure after 8 to 12 weeks of treatment, including exercise tolerance testing, NYHA class, symptoms, and left ventricular ejection fraction. (In another placebo-controlled long-term survival trial, 1,153 patients with class III/IV heart failure were randomized to receive amlodipine or placebo in addition to conventional treatment. The results showed that all-cause mortality and cardiac morbidity were 39% in the amlodipine group and 42% in the placebo group.) Amlodipine does not affect sinus node function or atrioventricular conduction. No electrocardiographic abnormalities were observed when amlodipine was used in combination with beta-blockers in patients with hypertension or angina. Amlodipine does not alter the electrocardiogram in patients with angina and does not worsen atrioventricular block. In hypertensive patients with normal renal function, this medication reduces renal vascular resistance, increases glomerular filtration rate (GFR) and renal blood flow, but does not affect filtration fraction or urine protein.
[Storage] Store in a sealed, light-proof container.
[Packaging] 7*5mg tablets
[Expiry Date] 36 months.
[Approval Number] National Medicine Standard H20057316
[Manufacturer] Guangdong PID Pharmaceutical Co., Ltd.
