Jiahuangsuan Anlüdiping Pian
Amlodipine Mesylate Tablets
Brand Name: Xinluoping
The active ingredient of this product is amlodipine mesylate, It is used for Hypertension treatment.
Drug interactions: It has been reported in the literature that amlodipine is safe in combination with following medications: thiazide diuretics, beta blockers, angiotensin converting enzyme inhibitors, long-acting nitrates, sublingual nitroglycerin, non-steroidal anti-inflammatory drugs, antibiotics and oral hypoglycemic drugs.
Overdosage: Severe overdose of amlodipine may lead to excessive peripheral vasodilation, followed by significant and persistent systemic hypotension. Bradycardia can also occur, Ⅱ or III atrioventricular block is rare, and cardiac arrest may occur to a few patients. Gastric lavage can be used for overdose of amlodipine. When significant hypotension occurs, aggressive cardiovascular support is required, including cardiac and pulmonary function monitoring, limb elevation, attention to circulation volume and urine volume. In the absence of contraindications, vasoconstrictors may also be used. Atropine or calcium gluconate may be given for bradycardia or atrioventricular block. Dialysis treatment is ineffective in relieving drug overdose.
Pharmacology：This product is a calcium influx blocker that selectively inhibits myocardial and vascular smooth muscle, with greater effect on the latter. It causes the dilation of peripheral arterioles; thus reducing the afterload. It has a negative inotropic effect in vivo , but has no effect on sinoatrial node and atrioventricular node in human.
Pharmacokinetics: Amlodipine is absorbed slowly and completely after oral administration and it is not affected by food intake. The maximum plasma concentration is reached at 6 to 12 hours after single dose, steady state is reached at 7 to 8 days after multiple doses , the bioavailability (F) is 62% to 80%, apparent volume of distribution (Vd) is 21 L/kg, plasma protein binding rate is 97.5%, and elimination phase half-life (t1/2β) is 35 to 50 hours. It is metabolized extensively into inactive metabolites in the liver, and more than 90% of metabolites and about 5% of unchanged drug are excreted in the urine.
Dosage and administration: Oral. The initial dose is 5mg (1 tablet) once daily, which can be increased to a maximum of 10 mg (2 tablets) once daily according to the patient's clinical response..
Adverse reactions: This product is well tolerated by patients. A small number of patients have mild adverse reactions such as redness, headache and edema during medication, and a very small number of patients have other mild side effects such as palpitation, fatigue, dizziness, pruritus, rash and insomnia. Rare adverse reactions of Amlodipine Mesylate have also been reported in the literature as nausea, abdominal pain, dyspnea, muscle cramps and indigestion. No abnormal laboratory test parameters related to this product have been found.
Contraindications: It is contraindicated in patients allergic to dihydropyridine calcium antagonists.
Warnings and Precautions :(1) The half-life of amlodipine is prolonged when liver function is impaired, but the corresponding recommended dose has not been established. Thus, patients with impaired liver function should use this product carefully.
(2) Amlodipine is extensively metabolized to inactive metabolites, and only about 5% of the drug is excreted unchanged in the urine, There was no relationship between the change of plasma concentration and the severity of renal impairment.. Therefore, patients with renal failure may receive normal doses. This product is not dialyzed.
Pregnancy and Nursing Mothers: In the animal experiments, when rats received the dose which was 50 times the maximum recommended dose in human, amlodipine did not show any reproductive toxicity except the delayed parturition and delayed parturition, However, the safety profile in human pregnancy or lactation has not been established. Therefore, this product is recommended only when there is no other substitute medicine with better safety profile and when the mother and child face the severer condition.
Pediatric use: No clinical data on pediatric use.
Geriatric use: Elderly people can use normal dose, but it is recommended to receive small dose for initial use and then gradually increase the dose.
Reference specification: WS1-（X-262）-2004Z-2017
Approval No. : SFDA Approval No. H20000708
Marketing Authorization Holder:Company Name: Kunming Sinoway Pharmaceutical Co.Ltd..