Amlodipine Besylate Tablets

Pharmacological actionAmlodipine besylate is a dihydropyridine calcium antagonist (calcium ion antagonist or slow channel blocker). The contraction of myocardial and smooth muscle depends on the entry of extracellular calcium ions into cells through specific ion channels. This product selectively inhibits the transmembrane entry of calcium ions into smooth muscle cells and myocardial cells, and has a greater effect on smooth muscle than on myocardium. Its interaction with calcium channels is determined by the progressive rate of its binding and dissociation with receptor sites, so the pharmacological effect is gradually produced. This product is a peripheral artery dilator that acts directly on vascular smooth muscle, reduces peripheral vascular resistance, and thus lowers blood pressure. At therapeutic doses, negative inotropic effects can be observed in in vitro experiments, but not in whole animal experiments. This product does not affect plasma calcium concentration. 15 randomized double-blind, placebo-controlled clinical trials have confirmed the antihypertensive effect of this product. Patients with mild to moderate hypertension take the drug once a day, which can reduce supine and standing blood pressure for 24 hours, and long-term use does not cause significant changes in heart rate or plasma catecholamines. The antihypertensive effect is stable. The antihypertensive effect is related to the dose, and the extent 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 on people with normal blood pressure after taking the medicine. The effect of this product in reducing diastolic blood pressure is similar in the elderly and young people, and the effect of reducing systolic blood pressure is stronger in the elderly. The exact mechanism of this product in relieving angina pectoris is still unclear, but it may be that during exercise, this product reduces cardiac work and heart rate and blood pressure product by reducing peripheral resistance (afterload), reducing myocardial oxygen demand, and treating exertional angina pectoris; by inhibiting the contraction of coronary arteries and arterioles caused by calcium ions, adrenaline, 5-hydroxytryptamine and thromboxane A2, it restores blood supply to the ischemic area to treat spontaneous angina pectoris. Five of the eight clinical trials showed that this product significantly prolonged the time of exercise-induced exertional angina pectoris; some studies showed that this product prolonged the time of ST segment decline by 1mm and reduced the frequency of angina pectoris. This effect is sustained and does not significantly affect blood pressure and heart rate. A clinical trial in 50 patients with spontaneous angina pectoris showed that this product can reduce 4 angina attacks per week (placebo reduces 1 per week). After taking this product, patients with normal cardiac function measured hemodynamics at rest and under 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 ?-blockers. In a placebo-controlled study, 697 patients with heart failure of heart function class II/III (NYHA) did not show signs of worsening heart failure in exercise tolerance tests, NYHA classification, symptoms and left ventricular ejection fraction after 8-12 weeks of medication. (Another placebo-controlled long-term survival trial, 1153 patients with heart failure of grade III/IV were randomly given this product or placebo on the basis of conventional treatment. The results showed that the mortality and cardiac morbidity of all causes were 39% in the amlodipine group and 42% in the placebo group.) This product does not affect the function of the sinus node and atrioventricular conduction. No abnormal electrocardiogram was found in patients with hypertension or angina pectoris when this product was used in combination with β-blockers. This product does not change the electrocardiogram of patients with angina pectoris and does not aggravate atrioventricular conduction block. After taking this product, hypertensive patients with normal renal function decreased renal vascular resistance, increased glomerular filtration rate and renal blood flow, but the filtration fraction or urine protein remained unchanged. Toxic effects Carcinogenicity, mutagenesis and teratogenesis Rats and mice were fed amlodipine for two years at doses of 0.5, 1.25 and 2.5 mg/kg per day, and no carcinogenicity was confirmed. The highest dose has reached the maximum tolerated dose of mice, but not rats (calculated based on the clinical maximum recommended dose of 10 mg mg/m2). Neither the gene nor the chromosome level revealed drug-related mutagenicity. Male rats were given amlodipine 64 days before mating and female rats were given amlodipine 14 days before mating, daily at 10 mg/kg (8 times the maximum recommended human dose), which did not affect reproductive capacity. Pregnant rats and rabbits were given amlodipine 10 mg/kg (8 times and 23 times the maximum recommended human dose) during the period of major organ formation, and no teratogenicity and other embryotoxicity were found. However, rats were given 10 mg/kg of amlodipine starting 14 days before mating and throughout the mating period and pregnancy, resulting in a significant reduction in the size of the pups (about 50%), a significant increase in the number of intrauterine deaths (about 5 times), and a prolonged pregnancy and delivery time. Toxicity mice and rats were given a single dose of amlodipine up to 40 mg/kg and 100 mg/kg, respectively, which can cause death. A single dose of 4 mg/kg or higher in dogs will cause significant peripheral vasodilation and hypotension.

The main ingredient of this product is amlodipine besylate, and its chemical name is: 3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate.

This product is white tablets.

(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).

The usual starting oral dose is 5 mg, once a day, and the maximum dose is no more than 10 mg, once a day. Thin people, those with weak constitutions, elderly patients, or those with impaired liver function should start taking the drug from 2.5 mg, once a day; those who take other antihypertensive drugs in combination should also start taking the drug from this dose. The dosage is 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, under the premise of clinical guarantee, the adjustment speed can be accelerated. The recommended dose for the treatment of angina pectoris is 5-10 mg, and the elderly patients or those with impaired liver function need to reduce the dose.

This product is well tolerated within the dose range of 10 mg/day, and most adverse reactions are mild to moderate. Only 1.5% of patients discontinued this product due to adverse reactions, which was not significantly different from placebo (about 1%). The most common adverse reactions were headache and edema. The dose-related adverse reactions with an incidence of 1% are as follows: edema, dizziness, flushing, and palpitations. The dose relationship is unclear, but the adverse reactions with an incidence of more than 1.0% are as follows: headache, fatigue, nausea, abdominal pain, and drowsiness. Among the above adverse reactions, the incidence of edema, flushing, palpitations, and drowsiness in women is higher than that in men. The following adverse events occurred at an incidence of ?1% but 0.1%, and the causal relationship with the drug was 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, postural hypotension, and vasculitis; Central and peripheral nervous system: hypoesthesia, peripheral neuropathy, paresthesia, tremor, vertigo; Gastrointestinal: anorexia, constipation, dyspepsia, dysphagia, diarrhea, flatulence, Pancreatitis, vomiting, gingival hyperplasia; musculoskeletal system: arthralgia, arthritis, muscle cramps, myalgia; mental: 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, urination disorder, 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 0.1%: heart failure, irregular pulse, extrasystoles, skin discoloration, urticaria, dry skin, dermatitis, hair loss, muscle weakness, twitching, ataxia, hypertonia, migraine, cold and wet skin, apathy, agitation, amnesia, gastritis, increased appetite, loose stools, cough, rhinitis, dysuria, polyuria, parosmia, taste inversion, visual accommodation disorders, dry eyes. Other occasional reactions such as myocardial infarction and angina pectoris cannot be distinguished as drug effects or disease states. Routine laboratory test items did not change significantly, and no significant changes were found in blood potassium, blood sugar, triglycerides, total cholesterol, high-density lipoprotein (HDL), uric acid, blood urea nitrogen or creatinine. After the drug was launched, there were occasional reports of male breast development in the drug population, but the causal relationship with the drug was unclear; in some cases, jaundice and elevated liver enzymes (often accompanied by cholestasis and hepatitis) were more severe and required hospitalization.

Allergic to dihydropyridine calcium antagonists.

Precautions for children: The safety and effectiveness for children have not been determined. Precautions for pregnancy and lactation: There is a lack of research data on the use of this drug in pregnant women, but according to the results of animal tests, this product can only be used in pregnant women when it is absolutely necessary. It is not yet known whether this product can be secreted through breast milk. Lactating women who take this drug should stop breastfeeding. Precautions for the elderly: Clinical studies have not confirmed that the elderly react to this drug differently from young people, but considering that the elderly often have decreased liver, kidney and heart function, and are accompanied by other diseases and corresponding drug treatments, the lower limit of the dosage range is generally used for initial medication. The clearance rate of this product is reduced in the elderly, and the drug-time curve (AUC) increases by about 40% to 60%, so a lower initial dose is also required.

⑴Cimetidine, grapefruit juice, acidogens: The pharmacokinetics of this product are not changed when used together. ⑵Atorvastatin, digoxin, ethanol: This product does not affect their pharmacokinetics. ⑶Sildenafil: A single dose of sildenafil (Viagra?) in patients with primary hypertension has no effect on the pharmacokinetics of this product. The two drugs produce an independent antihypertensive effect when used together. ⑷Warfarin: This product does not change the prothrombin action time of warfarin. ⑸Digoxin, phenytoin and warfarin: The combination with this product has no effect on the plasma protein binding rate. ⑹Anesthetics: Inhaled hydrocarbons combined with this product can cause hypotension. ⑺Nonsteroidal anti-inflammatory drugs: Indomethacin in particular can weaken the antihypertensive effect of this product. ⑻?-Blockers: The combination with this product is well tolerated, but it can cause excessive hypotension and rarely aggravate heart failure. ⑼Estrogen: The combination can cause fluid retention and increase blood pressure. ⑽ Sulfinpyrazone: Co-administration may increase the protein binding rate of this product and produce changes in blood drug concentration. ⑾ Lithium: Co-administration may cause neurotoxicity, nausea, vomiting, diarrhea, ataxia, tremor and/or numbness, so caution is required. ⑿ Sympathomimetic amines: May weaken the antihypertensive effect of this product. ⒀ Sublingual nitroglycerin and long-acting nitrate preparations: Co-administration with this product may enhance the anti-anginal effect. Although no rebound effect has been reported, the dosage should be gradually reduced under the guidance of a doctor when the drug is discontinued. ⒁ Thiazide diuretics, ACEI, digoxin, warfarin, antibiotics and oral hypoglycemic drugs: Can be safely used with this product.

Keep in a light-proof and sealed place

10 mg

24 months.

Viatris Pharmaceuticals (DALIAN) Co., Ltd.

• Founded in:

  1989-10-07

• Address:

  No. 22 Daqing Road, Dalian Economic and Technological Development Zone, Liaoning Province

• Tax NO.:

  912102006048147187

• Registered Funds:

  $80.4 million

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