Amlodipine Besylate Tablets
Function and Efficacy
Pharmacological action: Amlodipine 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 binding and dissociation between it and 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 concentrations. 15 randomized, double-blind, placebo-controlled trials
Ingredients
Amlodipine besylate. Molecular weight: C20H25ClN2O5·C6H6O3S
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| Amlodipine BesylateIngredients |
Dihydropyridine calcium antagonists selectively inhibit calcium ions from entering smooth muscle cells and myocardial cells across the membrane, and have a greater effect on smooth muscle than on myocardium. They lower blood pressure by reducing peripheral vascular resistance without affecting plasma calcium concentration. More |
111470-99-6 | 81 |
Appearance
This product is white tablets.
Indication
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).
Usage and Dosage
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, weak people, elderly patients or those with impaired liver function start taking the drug from 2.5 mg, once a day; those who take other antihypertensive drugs in combination 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 to 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 to 10 mg, and the elderly patients or those with impaired liver function need to reduce the dose.
Adverse Reactions
Patients tolerate this product well. The more common side effects are headache, edema, fatigue, insomnia, heart and abdominal pain, flushing, palpitations and dizziness; rare side effects are itching, rash, dyspnea, weakness, muscle cramps and indigestion. Similar to other calcium antagonists, there are very few reports of adverse reactions such as myocardial infarction and chest pain, and these adverse reactions cannot be clearly distinguished from the patient's underlying diseases. No abnormal laboratory test parameters related to this product have been found.
Precautions
Allergic to dihydropyridine calcium antagonists.
Special Population Medication
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.
Drug Interactions
Cimetidine, grapefruit juice, acidogens: The pharmacokinetics of this product are not changed when used together. Atorvastatin, digoxin, ethanol: This product does not affect their pharmacokinetics. Sildenafil: A single dose of sildenafil (Viagra) in patients with essential hypertension has no effect on the pharmacokinetics of this product. The two drugs produce an independent antihypertensive effect when used together. Warfarin: This product does not change the prothrombin action time of warfarin. Digoxin, phenytoin and warfarin: The combination with this product has no effect on the plasma protein binding rate. Anesthetics: Inhaled hydrocarbons combined with this product can cause hypotension. Nonsteroidal anti-inflammatory drugs: Indomethacin in particular can weaken the antihypertensive effect of this product. -Blockers: The combination with this product is well tolerated, but it can cause excessive hypotension and rarely aggravate heart failure. Estrogen: The combination can cause fluid retention and increase blood pressure. Sulfinpyrazone: The combination can increase the protein binding rate of this product and produce changes in blood drug concentration. Lithium: Co-administration may cause neurotoxicity, nausea, vomiting, diarrhea, ataxia, tremor and/or numbness, so be cautious. Sympathomimetic amines: May weaken the antihypertensive effect of this product. Sublingual nitroglycerin and long-acting nitrate preparations: Co-administration with this product may enhance the anti-anginal effect. Although rebound effects have not been reported, the dosage should be gradually reduced under the guidance of a doctor when the drug is discontinued. Thiazide diuretics, ACEI, digoxin, warfarin, antibiotics and oral hypoglycemic drugs: Can be safely used with this product.
Storage
Keep in a light-proof and airtight container.
Packaging Specification
5mg (calculated as amlodipine)
Validity Period
24 months.
Manufacturer
Jiangsu Disainuo Pharmaceutical Co., Ltd.
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Founded in:
2006-10-11 -
Address:
No. 3, Kang'an Road, Liyang Economic Development Zone, Jiangsu Province -
Tax NO.:
91320481792322090C -
Registered Funds:
100 million yuan -
Website:
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Email: