Product Overview
[Drug Name]
Generic Name: Amlodipine Maleate Tablets
Trade Name: Malaisuan Anlvdiping Pian
English Name: Amlodipine Maleate Tablets
Chinese Pinyin: Malaisuan Anlvdiping Pian
[Main Ingredients]
Amlodipine Maleate.
[Properties]
This product is a white tablet.
[Indications]
(1) Hypertension (used alone or in combination with other drugs) (2) Angina pectoris: especially spontaneous angina pectoris (used alone or in combination with other drugs)
[Dosage and Administration]
The usual oral starting dose is 5 mg once a day, with a maximum of 10 mg once a day. Thin people, weak people, elderly patients or those with impaired liver function should start with 2.5 mg once a day; those who take other antihypertensive drugs should also start with this dose. The dosage should be adjusted according to individual needs, and the adjustment period should be no less than 7-14 days so that the doctor can fully evaluate the patient's response to the dose. However, the adjustment speed can be accelerated under the premise of clinical guarantee. The recommended dose for the treatment of angina pectoris is 5-10 mg. A reduced dose is required for elderly patients or those with impaired liver function.
[Adverse Reactions]
This product 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, hot flashes, 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, hot flashes, palpitations, and somnolence were more common in women than in men. The following adverse events occurred in 1% but >0.1% of patients, and the causal relationship to the drug was unclear: General: allergic reaction, asthenia, back pain, hot flashes, malaise, pain, stiffness, weight gain; Cardiovascular: arrhythmias (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, tremor, and vertigo; Gastrointestinal: anorexia, constipation, dyspepsia, dysphagia, diarrhea, flatulence, pancreatitis, vomiting, and gingival hyperplasia; Musculoskeletal system: arthralgia, arthritis, muscle cramps, and myalgia; Psychiatric: sexual dysfunction, insomnia, tension, depression, nightmares, anxiety, and depersonalization; Skin 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; Metabolism and Nutrition: Hyperglycemia, thirst; Hematopoietic System: Leukopenia, purpura, thrombocytopenia.
The following adverse events occurred in 0.1% of patients: heart failure, irregular pulse, premature contractions, skin discoloration, dry skin with urticaria, 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 pectoris, cannot be distinguished as drug effects or disease states. Routine laboratory tests showed no significant changes, and no meaningful changes were found in serum potassium, blood glucose, total triglycerides, total cholesterol, high-density lipoprotein (HDL), uric acid, blood urea nitrogen, or creatinine. Since the drug's launch, occasional reports of gynecomastia have been reported in patients taking it, but the causal relationship is unclear. In some cases, jaundice and elevated liver enzymes (often accompanied by cholestasis and hepatitis) have been reported, often requiring hospitalization.
[Contraindications]
1. Hypersensitivity to dihydropyridine calcium channel blockers. 2. Severe hypotension; aortic valve stenosis.
[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 vasodilatory effect of this drug, acute hypotension is generally rare with oral administration. However, caution is advised when using this drug in combination with other peripheral vasodilators, especially in patients with severe aortic valve 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 product should be used with caution in patients with severe hepatic insufficiency. 5. Patients with renal failure: The starting dose of patients with renal failure can remain unchanged. 6. Discontinuation of β-blockers: This product has no protective effect on the rebound symptoms caused by sudden discontinuation of β-blockers. Therefore, discontinuation of β-blockers still requires gradual reduction of the dose. 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:
There is a lack of research data on its use in pregnant women, but based on animal studies, this drug should only be used in pregnant women 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 that elderly individuals respond differently to this drug than younger individuals. However, given that elderly individuals 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 approximately 40%-60% increase in the area under the curve (AUC), 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, ethanol: This product does not affect their pharmacokinetics. 3. Sildenafil: A single dose of sildenafil has no effect on the pharmacokinetics of this product in patients with essential hypertension. The two drugs produce an independent antihypertensive effect when used in combination. 4. Warfarin: This product does not change the prothrombin action time of warfarin. 5. Digoxin, phenytoin and warfarin: There is no effect on plasma protein binding when used in combination with this product. 6. Anesthetics: Inhaled hydrocarbons combined with this product can cause hypotension. 7. Non-steroidal anti-inflammatory drugs: Indomethacin in particular can weaken the antihypertensive effect of this product. 8. Beta-blockers: Combination with this product is well tolerated, but can cause excessive hypotension and rarely worsen heart failure. 9. Estrogen: Combination can cause fluid retention and increase blood pressure. 10. Sulfinpyrazone: Combination can increase the protein binding rate of this product and produce changes in blood drug concentration. 11 Lithium: Combined use can cause neurotoxicity, resulting in nausea, vomiting, diarrhea, ataxia, tremor, and/or numbness, so caution is advised. 12 Sympathomimetic amines: May weaken the antihypertensive effect of this product. 13 Sublingual nitroglycerin and long-acting nitrate preparations: Combined use with this product may enhance the anti-anginal effect. Although rebound effects have not been reported, the dose should be gradually reduced under the guidance of a doctor when discontinuing the drug. 14 Thiazide diuretics, ACE inhibitors, digoxin, warfarin, antibiotics, and oral hypoglycemic agents can be safely used with this drug.
[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 through specific ion channels. This drug selectively inhibits the transmembrane entry of calcium ions into smooth muscle cells and cardiomyocytes, with 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 from receptor sites, resulting in a gradual onset of pharmacological action. This drug is a peripheral arterial dilator, acting directly on vascular smooth muscle to reduce peripheral vascular resistance and thereby lower blood pressure. Negative inotropic effects have been observed in vitro at therapeutic doses, but not in whole animal studies. This drug does not affect plasma calcium concentrations. Its antihypertensive activity has been confirmed in 15 randomized, double-blind, placebo-controlled clinical trials. A once-daily dose can lower supine and standing blood pressure in patients with mild to moderate hypertension over a 24-hour period. , long-term use does not cause significant changes in heart rate or plasma catecholamines. The antihypertensive effect is stable, and the difference between peak and trough values is not much. The antihypertensive effect is related to the dose, and the magnitude of blood pressure reduction is related to the blood pressure before treatment. The efficacy of moderate hypertension (diastolic blood pressure 105-114mmHg) is higher than that of mild hypertension (diastolic blood pressure 90-104mmHg), and there is no obvious effect after taking the drug in people with normal blood pressure. The effect of this product in lowering diastolic blood pressure is similar in the elderly and young people, and the effect of lowering systolic blood pressure is stronger in the elderly. This product relieves angina The exact mechanism of pain relief is still unclear, but it is possible that during exercise, this product reduces the work of the heart and the rate-blood-pressure product by reducing peripheral resistance (afterload), thereby reducing myocardial oxygen demand to treat exertional angina pectoris; it also treats spontaneous angina pectoris by inhibiting the contraction of coronary arteries and arterioles caused by calcium ions, adrenaline, 5-hydroxytryptamine, and thromboxane A2, thereby restoring blood supply to the ischemic area. Five of the eight clinical trials showed that this product significantly prolonged the duration of exercise-induced exertional angina pectoris and reduced the frequency of angina attacks. It also did not significantly affect blood Pressure and heart rate. After taking this product, patients with normal cardiac function had their hemodynamics measured at rest and during exercise, and the cardiac ejection fraction increased, but there was no significant effect on dP/dt or left ventricular end-diastolic pressure/volume. At therapeutic doses, this product does not cause negative inotropic effects when used alone or in combination with β-blockers. This product does not affect sinus node function and atrioventricular conduction. After taking this product, hypertensive patients with normal renal function have reduced renal vascular resistance, increased glomerular filtration rate and renal blood flow, but the filtration fraction or urine protein remains unchanged. Carcinogenicity, mutagenesis and teratogenesis Amlodipine was continuously fed to rats and mice at doses of 0.5, 1.25 and 2.5 mg/kg per day for two years without any confirmed carcinogenicity. The highest dose reached the maximum tolerated dose in mice, but not in rats (calculated based on the clinical maximum recommended dose of 10 mg/m2). No drug-related mutagenicity was revealed at the gene and chromosome levels. Amlodipine was given to male rats 64 days before mating and to female rats 14 days before mating, at a dose of 10 mg/kg per day. kg (8 times the maximum recommended human dose), without affecting reproductive capacity. Administration of amlodipine at 10 mg/kg (8 and 23 times the maximum recommended human dose) to pregnant rats and rabbits during the period of major organogenesis revealed no teratogenicity or other embryotoxic effects. However, administration of 10 mg/kg of amlodipine to rats, beginning 14 days before mating and continuing throughout mating and gestation, resulted in a significant reduction in pup size (approximately 50%), a significant increase in intrauterine mortality (approximately 5-fold), and prolonged gestation and delivery. Single doses of amlodipine up to 40 mg/kg and 100 mg/kg, respectively, can cause lethality in mice and rats. Single doses of 4 mg/kg or higher in dogs result in significant peripheral vasodilation and hypotension.
Storage: Store in a dark, airtight container.
Strength: 5 mg
Packaging: 5 mg x 14 s
Expiration Date: 24 months
Approval Number: National Medicine Standard H19990374
Manufacturer: Shaanxi Chaoqun Pharmaceutical Co., Ltd.
