COMPOSITIONS :
Amlodipine Besilate Tablet 5 mg, each tablet contains : Amlodipine besilate equivalent to Amlodipine 5 mg.
DESCRIPTIONS :
Amlodipine Besilate containing Amlodipine besilate (equivalent to Amlodipine) as active ingredient is available in tablet 5 mg and 10 mg.
INDICATIONS :
- The first line treatment of hypertension and can be used as the sole agent to control blood pressure in the majority of patients. Patients not adequately controlled on a single antihypertensive agent (other than Amlodipine) may benefit from the addition of Amlodipine, which has been used in combination with a Thiazide diuretic, β-adrenoceptor blocking agent or an angiotensin-converting enzyme inhibitor.
- The first line treatment of myocardial ischemia, whether due to fixed obstruction (stable angina) and/or vasospasm/vasoconstriction (Prinzmetals or variant angina) of coronary vasculature. Amlodipine may be used where the clinical presentation suggest a possible vasospastic/vasoconstrictive component but where vasospastic/vasoconstrictive has not been confirmed. Amlodipine may be used alone, as monotherapy or in combination with other antiangina drugs in patients with angina that is refractory to Nitrates and/or adequate doses of β-blockers.
DOSAGE AND ADMINISTRATIONS :
- For hypertension : The usual initial dose is 5 mg Amlodipine once daily which may be increased to a maximum dose of 10 mg, depending on the individual patients response and severity. Small, fragile, or elderly individuals or patients with hepatic insufficiency may be started on 2.5 mg once daily and this dose may be used when adding Amlodipine to other antihypertensive therapy.
- Majority of hypertensive patients with 5 mg/day the dose may not necessarily be increased. For those who need higher dose, Amlodipine can be increased to 7.5 mg/day with maximum dose of 10 mg/day.
- The recommended dose for chronic stable or vasospastic angina is 5 – 10 mg, with the lower dose suggested in the elderly and in patients with hepatic insufficiency.
- No dose adjustment of Amlodipine is required upon concomitant administration of Thiazide diuretics, β-blockers and angiotensin-converting enzyme inhibitors.
- Use in children : No experience is available on use of Amlodipine in children.
OVERDOSAGE :
In humans, experience with intentional overdosage is limited. Gastric lavage may be worthwhile in some cases. Available data suggests that gross overdosage could result in excessive peripheral vasodilation with subsequent marked and probably prolonged systemic hypotension.
Clinically significant hypotension due to Amlodipine overdosage calls for active cardiovascular support including frequent monitoring of cardiac and respiratory function, elevation of extremities and attention to circulating fluid volume and urine output. A vasoconstrictor may be helpful in restoring vascular tone and blood pressure, provided that there is no contraindication to its use. Intravenous Calcium gluconate may be beneficial in reversing the effects of calcium-channel blockade. Since Amlodipine is highly protein-bound, dialysis is not likely to be of benefit.
CONTRAINDICATION :
Amlodipine is contraindicated in patients with a known hypersensitivity to Dihydropyridines.
WARNINGS AND PRECAUTIONS :
- Usage in patients with impaired hepatic function : As with all Calcium antagonists, Amlodipine half-life is prolonged in patients with impaired liver function and dosage recommendations have not been established. The drug should therefore be administered with caution in these patients.
- Usage in renal failure : Amlodipine is extensively metabolized to inactive metabolites with 10% excreted as unchanged drug in the urine. Changes in Amlodipine plasma concentrations are not correlated with degree of renal impairment. Amlodipine may be use in such patients at normal doses. Amlodipine is not dialyzable.
- Usage in the elderly : The time to reach peak plasma concentrations of Amlodipine is similar in elderly and younger subjects. Amlodipine clearance tends to be decrease with resulting increases in AUC and elimination half-life in elderly patients. Amlodipine used at similar doses in elderly or younger patients, is equally well tolerated. Therefore, normal dosage regimens are recommended.
- Usage in pregnant and lactating women : Safety of Amlodipine in human pregnancy or lactation has not been established. Amlodipine does not demonstrate toxicity in animal reproductive studies other than to delay parturition and prolong labor in rats at a dose level fifty times the maximum recommended dose in humans. Accordingly, use in pregnancy is only recommended when there is no safer alternative and when the disease itself carries greater risk for the mother and fetus.
- Effects on ability to drive and use machines : Not applicable.
DRUG INTERACTIONS :
- Amlodipine has been safely administered with Thiazide diuretics, β-blockers, angiotensin-converting enzyme inhibitors, long-acting Nitrates, sublingual Nitroglycerine, NSAIDs, antibiotics and oral hypoglycemic drugs.
- Studies have indicated that the co-administration of Amlodipine with Digoxin did not change serum Digoxin levels or Digoxin renal clearance in normal volunteers and that co-administration of Cimetidine did not alter the pharmacokinetics of Amlodipine.
- In vitro data from studies with human-plasma indicate that Amlodipine has no effect on protein binding of the drugs tested (Digoxin, Phenytoin, Warfarin or Indomethacin).
- Giving Amlodipine with grapefruit or grapefruit juice is not recommended because it resulted in an increase in the blood pressure lowering effect.
- In healthy male volunteers, the co-administration of Amlodipine does not significantly alter the effect of Warfarin on prothrombin response time.
ADVERSE REACTIONS :
- Amlodipine is well tolerated.
- The most commonly observed side effects in patients with hypertension or angina were : Headache, edema, fatigue, somnolence, nausea, abdominal pain, flushing, palpitations and dizziness.
- Less commonly side effects observed include : Pruritus, rash, dyspnea, asthenia, muscle cramps, dyspepsia, gingival hyperplasia and rarely erythema multiforme.
- As with other calcium channel blockers, the following adverse events have been rarely reported and cannot be distinguished from the natural history of the underlying disease : Myocardial infarction arrhythmias (including ventricular tachycardia and atrial fibrillation) and chest pain.
- No pattern of clinically significant laboratory test abnormalities related to Amlodipine has been observed.
PRESENTATIONS :
Amlodipine Besilate Tablet 5 mg Box, 10 blisters @ 10 tablets Reg. No. GKL0702339410A1
STORAGE :
STORE BELOW 30ºC
ON MEDICAL PRESCRIPTION ONLY
Manufactured by :
BERNOFARM
Sidoarjo – Indonesia
