COMPOSITION
AmlowideTM: Each tablet contains Amlodipine Besilate BP equivalent to Amlodipine 5 mg.
PHARMACOLOGICAL INFORMATION
Pharmacological Action
Amlowide is a calcium ion influx inhibitor (slow channel blocker or calcium ion antagonist) and inhibits the transmembrane influx of calcium ions into cardiac and smooth muscle without changing serum calcium concentrations.
Mechanism of Action
The mechanism of the antihypertensive action of Amlowide is due to a direct relaxant effect on vascular smooth muscle. Amlowide dilates peripheral arterioles and thus reduces the total peripheral resistance (afterload) against which the heart works. Unloading of the heart reduces myocardial energy consumption and oxygen requirements.
PHARMACOKINETIC PROPERTIES
Absorption: Peak plasma concentrations of amlodipine reached 6-12 hours after administration of Amlowide; the extent of absorption is 64%-90%.
Distribution: The apparent volume of distribution of amlodipine is about 21 L/kg. Approximately 93% of circulating amlodipine is bound to plasma proteins. Plasma half life of amlodipine is 30-60 hr and time to reach steady state is 7-9 days.
Metabolism: Amlodipine is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine.
Elimination: Elimination of Amlodipine from the plasma is biphasic with a terminal elimination half-life of about 30-50 hours. Approximately 47% of an oral dose is eliminated in the urine and faeces respectively.
CLINICAL INFORMATION
Therapeutic Indications
Hypertension: Amlowide is indicated for the first line treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.
Chronic Stable Angina: Amlowide is indicated for the treatment of stable angina. Amlowide may be used alone or in combination with other antianginal agents.
Vasospastic Angina: Amlowide is indicated for the treatment of confirmed or suspected vasospastic angina. Amlowide may be used as monotherapy or in combination with other antianginal drugs.
Dosage and Administration
Adults: The usual initial antihypertensive oral dose of Amlowide is 5 mg once daily with a maximum dose of 10 mg once daily. Dosage should be adjusted according to each patient's need.
The recommended dose for chronic stable or vasospastic angina is 5-10 mg. Most patients will require 10 mg for adequate effect.
The recommended dose range for patients with coronary artery disease is 5-10 mg once daily. The majority of patients required 10 mg.
No dose adjustment of Amlowide is required during combined administration of thiazide diuretics, beta blockers, or angiotensin converting enzyme inhibitors.
Use in Pregnancy & Lactation
Pregnancy: Amlowide should be used during pregnancy only if the expected benefit outweighs the potential fetal risk.
Lactation: Nursing mothers should not use amlowide. If its use is considered necessary, breast feeding should be stopped.
Dosage in Hepatic Impairment
Since Amlowide is extensively metabolized by the liver, the plasma elimination half-life (t ½) is 56 hours in patients with impaired hepatic function, caution should be exercised when administering Amlowide to patients with severe hepatic impairment.
Dosage in Renal Impairment
The pharmacokinetics of amlodipine is not significantly influenced by renal impairment. Patients with renal failure may therefore receive the usual initial dose.
Side Effects
Overall side effects include fatigue, peripheral edema, nausea, dizziness, flushing, palpitation, hypotension, GI disturbance, drowsiness, headache, weakness, muscle cramps.
Contraindications
Amlowide is contraindicated in patients with known hypersensitivity to amlodipine.
Precautions
Use in patients with congestive heart failure: Although haemodynamic studies and a controlled in class II-III heart failure patients have shown that amlodipine did not lead to clinical deterioration as measured by exercise tolerance, left ventricular ejection fraction and clinical symptomatology. In general, all calcium channel blockers should be used with caution in patients with heart failure.
Drug Interactions
Antiinflammatory drugs, nonsteroidal (NSAIDs), especially indomethacin: NSAIDs may reduce the antihypertensive effects of amlodipine by inhibiting renal prostaglandin synthesis and/or causing sodium and fluid retention.
Hypotension-producing medication: Antihypertensive effect may be potentiated when amlodipine is used concurrently with hypotension producing medication, in this case dosage adjustment may be necessary.
Lithium: Concurrent use with amlodipine potentially may result in neurotoxicity in the form of nausea, vomiting, diarrhoea, ataxia, tremors, and/or tinnitus: caution is recommended.
Sympathomimetics: Concurrent use may reduce antihypertensive effects of amlodipine; the patient should be carefully monitored to confirm that the desired effect is being obtained.
Overdosage
There is no well documented experience with amlodipine overdosage. Gastric lavage may be worthwhile. Available data suggest 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. 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.
PHARMACEUTICAL INFORMATION
Storage Conditions
Store in a cool and dry place away from light. Keep out of reach of children.
Presentation & Packaging
AmlowideTM: Each commercial box contains 50 tablets in Alu-Alu blister pack. |