Product Overview
[Drug name]
Generic name: Amlodipine Besylate Tablets
Trade name: Jingxin
English name: Amlodipine Besylate Tablets
Chinese Pinyin: Amlodipine Besylate Tablets
[Ingredients]
The main ingredient of this product is amlodipine.
[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).
[Usage and Dosage]
The usual oral starting 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 of the drug 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 5-10 mg, and the dose needs to be reduced for elderly patients or those with impaired liver function.
[Adverse Reactions]
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 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: hypoesthesia, peripheral neuropathy, paresthesia, tremor, vertigo; 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, 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%: asthenia, irregular pulse, extrasystoles, skin discoloration, urticaria, dry skin, dermatitis, alopecia, muscle weakness, twitches, 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. There were no significant changes in routine laboratory tests, and no significant changes were found in serum 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-using 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.
[Contraindications] Allergic to dihydropyridine calcium antagonists.
[Precautions]
1. Patients with severe obstructive coronary artery disease will experience an increase in the frequency and severity of angina attacks, or develop acute myocardial infarction when they start treatment with calcium channel antagonists or increase the dosage. The mechanism is unknown;
2. Since this product gradually produces a vasodilatory effect, oral administration generally rarely causes acute hypotension. However, caution is still required when this product is used in combination with other peripheral vasodilators, especially for patients with severe aortic stenosis; 3. Calcium channel blockers should be used with caution in patients with heart failure; 4. This product should be used with caution in patients with severe liver dysfunction; 5. The starting dose of patients with renal failure can remain unchanged; 6. This product has no protective effect on rebound symptoms caused by sudden discontinuation of blockers. Therefore, discontinuation of blockers still requires gradual reduction; 7. This product can be used safely in patients with obstructive pulmonary disease, well-compensated heart failure, peripheral vascular disease, diabetes and lipid abnormalities.
[Medication for special populations]
Precautions for children: The safety and effectiveness of children have not yet been determined.
Precautions for pregnancy and lactation: There is a lack of corresponding research data on the use of drugs in pregnant women, but according to the results of animal tests, this product can only be used in pregnant women when it is very necessary. It is not known whether this product can be secreted through breast milk, and lactating women who take the drug should stop breastfeeding.
Precautions for the elderly: Clinical studies have not confirmed that the elderly react differently to the drug than the young, 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 the 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%, and a lower initial dose is also required.
[Drug Interactions]
Cimetidine, grapefruit juice, acidogens: The pharmacokinetics of this product are not changed when used in combination. Atorvastatin, digoxin, ethanol: This product does not affect their pharmacokinetics. Sildenafil: 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 in combination. Warfarin: This product does not change the prothrombin action time of warfarin. Digoxin, phenytoin and warfarin: There is no effect on the plasma protein binding rate when used in combination with this product. 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: This product is well tolerated when used in combination, but 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: The combination can cause neurotoxicity, nausea, vomiting, diarrhea, ataxia, tremor and/or numbness, so be cautious. Sympathomimetic amines: The antihypertensive effect of this product can be weakened. Sublingual nitroglycerin and long-acting nitrate preparations: The combination with this product can 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. Thiazide diuretics, ACEI, digoxin, warfarin, antibiotics and oral hypoglycemic drugs: They can be safely used in combination with this product.
[Pharmacological action]
Pharmacological action Amlodipine besylate is a dihydropyridine calcium antagonist (calcium ion antagonist or slow channel blocker). The contraction of myocardial and smooth muscles 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 action 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
[Storage] Store in a dark and sealed place.
[Specification] 5mg (in terms of amlodipine)
[Packaging specification] 5mg
[Expiration date] 24 months
[Approval number] National Medicine Standard H20103356
[Manufacturer] Company name: Zhejiang Jingxin Pharmaceutical Co., Ltd.
