Full Prescribing Info
Amlodipine besilate.
Each 5- and 10-mg tablet contains amlodipine besilate equivalent to amlodipine 5 and 10 mg, respectively.
Amlodipine besilate is a 1, 4-dihydropyridine derivative, long-acting calcium channel blocking agent which is used in the management of angina pectoris and hypertension.
Pharmacology: Amlodipine besilate belongs to the 3rd generation dihydropyridine calcium-channel blockers. It primarily acts as a vasodilator, affecting slow L-type channels and has a greater selectivity for vascular smooth muscle as compared to the cardiac tissues.
It is a potent vasodilator with actions similar to other dihydropyridines. Only, amlodipine has smooth onset of effects and is longer lasting than other calcium blocking agents. Its actions are also found to be dependent on K+ concentration and thus, its effects are voltage dependent. Amlodipine exerts its peripheral and coronary vasodilating effect by interacting directly with both 1,4-dihydropyridine and diltiazem-binding sites on the calcium channel.
Pharmacokinetics: Amlodipine besilate is well absorbed upon oral administration. It reaches peak plasma concentration (Cmax) after 6-12 hrs. Cmax of the drug is not delayed by food. Its bioavailability is about 60-65%. Amlodipine besilate is reported to be about 97.5% bound to plasma protein with a volume of distribution of 21 L/kg.
Food does not affect the absorption of amlodipine.
It has a prolonged terminal elimination t½ of approximately 35-50 hrs and achieves steady-state plasma concentration after 7-8 days of administration of Amlokard. Amlodipine besilate is mainly metabolized in the liver with its metabolites mostly excreted in the urine together with <10% of unchanged drug.
Amlodipine cannot be removed by dialysis.
Management of angina pectoris, hypertension and Prinzmetal angina.
Dosage/Direction for Use
Hypertension, Stable Angina and Prinzmetal Angina: Adults: 5 mg once a day as monotherapy, may be increased to 10 mg if necessary.
Elderly Patients, Small Frail Individuals and Patients with Hepatic Impairment: Recommended Dose: 2.5 mg once daily.
Studies prove that amlodipine 2.5-5 mg/day was well tolerated by children and adolescents with hypertension providing effective blood pressure control without experiencing significant adverse effects in children. However, it was found that younger children may require higher doses than older children.
Administration: Amlodipine is administered orally as besilate salt and may be given without regard to timing of meals.
Symptoms of overdosage with amlodipine include severe dizziness, fast, irregular or very slow heartbeat and confusion.
A study effecting intentional overdose with amlodipine showed that Amlokard produced prolonged hemodynamic effects which may lead to pulmonary edema. Patients with amlodipine overdose are recommended to be given aggressive decontamination therapy, considering the long elimination t½ and delayed onset of effects of Amlokard. Extended clinical monitoring and supportive care may be required if patients are hemodynamically unstable.
Hypersensitivity to Amlokard and other dihydropyridines and those with severe hypotension, aortic valve stenosis, chronic idiopathic constipation, severe liver impairment and coronary artery disease.
Special Precautions
Patients with Renal Impairment: There is no need to adjust the dose of amlodipine in patients with renal disease since once-daily administration of Amlokard is found to be suitable for all degrees of renal functions.
Patients with Hepatic Impairment: In the presence of hepatic impairment, dosage of amlodipine should be adjusted to 2.5 mg/day.
Use in lactation: There is no available data yet confirming the excretion of amlodipine in breast milk. Caution should be taken when giving Amlokard to lactating mothers.
Use in children: In a study done among hypertensive children with mean age of 12 years, amlodipine was found to effectively lower systolic blood pressure. The safety and efficacy of amlodipine in children <6 years has not yet been established.
Use in the elderly: Amlodipine is well tolerated in elderly hypertensive patients at a dose of 2.5 mg/day.
Use In Pregnancy & Lactation
Use in lactation: There is no available data yet confirming the excretion of amlodipine in breast milk. Caution should be taken when giving Amlokard to lactating mothers.
Adverse Reactions
The most common adverse effects of amlodipine besilate, similar to that of other calcium-channel blockers, are associated with its vasodilating effects are often lessened with continued use of the drug. Among them are flushing, headache disorders, dizziness and peripheral edema, the most common of which are edema and flushing which are due to the vasodilating effect of Amlokard.
Abdominal pain with cramps, fatigue, palpitations, tachycardia and nausea are less frequently experienced with the use of amlodipine.
Other adverse effects associated with the use of Amlokard include increased micturition, eye pain and other visual disturbances, mental or mood changes eg, depression, anxiety or nervousness, decreased sexual ability/desire, constipation and fainting.
At the start of the treatment, a paradoxical increase in ischemic chest pain may be experienced. In some patients, cerebral or myocardial ischemia or transient blindness caused by excessive fall in blood pressure occur. Amlodipine, in 1 study was found to induce gingival overgrowth.
Hypersensitivity reactions to amlodipine may occur leading to rashes, including erythema multiforme, fever and abnormal liver functions eg, cholestasis. Other symptoms of allergic reactions are itching, swelling, severe dizziness and trouble breathing.
Drug Interactions
As with other calcium-channel blockers, amlodipine may enhance the antihypertensive effects of other drugs for hypertension. Combination with β-blockers, however, is said to be well tolerated.
Concomitant use of Amlokard with aldesleukin and antipsychotics that cause hypotension may enhance its antihypertensive effect. Amlodipine also show additive effect when used with diuretics, β-blockers and angiotensin-converting enzyme inhibitors.
In hypertensive patients with diabetes, the use of amlodipine 5 mg/day with quinapril 20 mg/day was found to be more effective in lowering blood pressure than with quinapril 40 g/day alone.
Amlodipine may be used in combination with atorvastatin in the treatment of cardiovascular risk.
Amlodipine, being mainly metabolized in the liver, may cause interaction with other drugs eg, quinidine which has the same metabolic pathway.
The effects of amlodipine may be reduced by rifampicin and enzyme-inducing antiepileptic drugs eg, carbamazepine, phenobarbital and phenytoin. Enzyme inhibitors eg, cimetidine, erythromycin and HIV-protease inhibitors may interfere with the metabolism of amlodipine and other calcium-channel blockers.
In general, the bioavailability of orally administered calcium-channel blockers is significantly increased when taken with grapefruit juice. However, in a study done in 20 normal men, co-administration of grapefruit juice with amlodipine did not change the pharmacokinetic and pharmacodynamic properties of Amlokard. Therefore, in clinical practice, no significant change is expected to be seen in the profile of response of patients taking amlodipine with grapefruit juice.
Store at temperatures not exceeding 30°C.
MIMS Class
Calcium Antagonists / Anti-Anginal Drugs
ATC Classification
C08CA01 - amlodipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
Amlokard tab 10 mg
100's (P2,100/strip, P21/tab)
Amlokard tab 5 mg
100's (P1,300/strip, P13/tab)
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