AmIong-5: Each tablet contains: Amlodipine Besilate BP equivalent to Amlodipine 5mg
Amlong-10: Each tablet contains: Amlodipine Besilate BP equivalent to Amlodipine 10mg
A Long-acting Calcium Channel Blocker.
Amlodipine is a dihydropyridine calcium antagonist that inhibits the transmembrane influx of calcium ions into the vascular smooth muscle and cardiac muscle. The mechanism of the antihypertensive action is due to a direct relaxant effect on vascular smooth muscle. The precise mechanism by which Amlodipine relieves angina may be due to the following two actions:
1. Amlodipine dilates peripheral arterioles and thus reduces the total peripheral resistance against which the heart works. Since there is no associated reflex tachycardia, this unloading of the heart reduces myocardial energy consumption and oxygen requirements and probably accounts for the effectiveness of Amlodipine in myocardial ischaemia.
2. The mechanism of action of Amlodipine probably involves dilation of the main coronary arteries and coronary arterioles, both in normal and ischaemic regions.
After oral administration of the therapeutic doses, Amlodipine is well absorbed with peak blood levels between 6-12 hours post dose. The volume of distribution was approximately 20 liters per kg. The terminal elimination half-life is about 35-50 hours and is consistent with once daily dosing, steady state plasma levels are reached after 7-8 days of consecutive dosing. Amlodipine is extensively metabolised to inactive metabolites with 10% of the parent compound and 60% of metabolites excreted in the urine. Bioavailability following oral administration is approximately 60-65%. Approximately 97.5% of the drug is bound to plasma proteins.
INDICATIONS AND USES
Amlodlpine is indicated in treatment of Hypertension and Myocardial Ischaemia associated with angina pectoris.
Amlodipine is contraindicated in patients with known hypersensitivity to Amlodipine.
SIDE EFFECTS/ADVERSE EFFECTS
The most commonly observed side effects were headache, oedema, fatigue, nausea, flushing and dizziness.
Increased Angina and/or Myocardial infarction: Rarely, patients, particularly those with severe obstructive coronary artery disease, have developed documented increased frequency, duration and/or severity of angina or acute myocardial infarction on starting calcium channel blocker therapy or at the time of dosage increase. The mechanism of this effect has not been elucidated.
Amlodipine has been safely administered with thiazide diuretics, beta-adrenoceptor blocking drugs, angiotensin converting enzyme inhibitor, long acting nitrates, sublingual glyceryl nitrate, non-steroidal anti-inflammatory drugs, antibiotics, and oral hypoglycaemic agents. 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 Digoxin, Phenytoin, Warfarin, or Indomethacin.
USE IN PREGNANCY AND LACTATION
Safety of Amlodipine in human pregnancy and lactation has not been established. Therefore, Amlodipine should not be administered during pregnancy, or lactation, or to women of child bearing potential unless effective contraception is used.
DOSAGE AND ADMINISTRATION
Adults: For both hypertension and angina, the recommended initial dose is 5mg Amlodipine orally once daily which may be increased to a maximum dose of 10mg depending on the individual patient’s response. The dose does not need adjusting when Amlodipine is given concurrently with thiazide diuretics, beta-adrenoreceptor blocking agents or angiotensin-converting enzyme inhibitors. Amlodipine can be administered with or without food.
Use in children: Since there is no clinical experience in patients of less than 18 years, use in children is not currently recommended.
Use in the elderly: Although elderly patients may have higher plasma concentration of Amlodipine than younger patients, the terminal elimination half-lives are similar. Amlodipine is similarly well tolerated in elderly or younger patients. Therefore the normal dosage is recommended.
Use with renal Impairment: Changes in Amlodipine plasma concentration are not correlated with degree of renal impairment, therefore the normal dosage is recommended. Amlodipine is not dialysable.
Use in patients with impaired hepatic function: The half-life of Amlodipine in patients with impaired liver function and dosage recommendation have not been established. Amlodipine should therefore be administered with caution in these patients.
OVERDOSAGE, SYMPTOMS AND ANTIDOTE
There is no documented experience with Amlodipine overdosage. Since Amlodipine absorption is slow, gastric lava-may be worrthwhile in some cases. Available data suggest that gross overdosage would 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 monitoring of cardiac and respiratory function, elevation of extremities, and attention to circulating fluid volume and urine output. A vasoconstrictor agent may be helpful in restoring vascular tone and blood pressure provided that there is no contraindication to its use. Since Amlodipine is highly protein-bound, dialysis is unlikely to be of benefit.
Keep in a cool, dry place. Keep out from the reach of children.
Alu Alu Blister pack of 1 x 10’s, 3 x 10’s and 10 x 10’s.
DATE OF PUBLICATION
MICRO LABS LIMITED
HOSUR-635 126. INDIA.
1, African Church Close, Off Coker Road.
Ilupeju, Lagos, Nigeria.