Twilight Litaka


ECE Pharma
Full Prescribing Info
Amlodipine besilate.
Each 5 mg tab contains: Amlodipine (as Besilate) 5 mg.
Each 10 mg tab contains: Amlodipine (as Besilate) 10 mg.
Amlodipine is a dihydropyridine, a calcium channel blocking agent. Amlodipine Besilate is chemically described as 3-Ethyl-5-methyl(+/-)2-[(2-aminoethoxy)methyl]-4-(o-chlophenyl)-1,4-duhydro-6-methyl-3,5-pyridine dicarboxylate. Slightly soluble in water and sparingly soluble in ethanol.
Pharmacology: Amlodipine is a selective calcium inhibitor through the cellular membrane in the vascular and cardiac smooth muscle. It has a higher effect on the vascular smooth muscle. Amlodipine is a peripheral arterial vasodilator that acts directly on the vascular smooth muscle to cause a reduction of the peripheral vascular resistance and reduction of arterial pressure.
Amlodipine has negative inotropic effects in vivo, but apparently it does not have a significant effect over the sinoatrial nodule (SA) or atrioventricular (AV) in humans.
For the treatment of hypertension and prophylaxis of angina.
Dosage/Direction for Use
Adults: For both hypertension and angina the usual initial dose is 5 mg once daily which may be increased to a maximum dose of 10 mg depending on the individual patient's response.
In hypertensive patients, amlodipine has been used in combination with a thiazide diuretic, alpha blocker, beta blocker, or an angiotensin converting enzyme inhibitor.
For angina, amlodipine may be used as monotherapy or in combination with other anti-anginal medicinal products in patients with angina that is refractory to nitrates and/or to adequate doses of beta blockers.
No dose adjustment of amlodipine is required upon concomitant administration of thiazide diuretics, beta blockers, and angiotensin-converting enzyme inhibitors. Or as prescribed by the physician.
Special populations: Elderly: Amlodipine is used at similar doses in elderly and younger patients. Normal dosage regimens are recommended in the elderly, but increase of the dosage should take place with care.
Hepatic impairment: Dosage recommendations have not been established in patients with mild to moderate hepatic impairment; therefore dose selection should be cautious and should start at the lower end of the dosing range. The pharmacokinetics of amlodipine have not been studied in severe hepatic impairment Amlodipine should be initiated at the lowest dose and titrated slowly in patients with severe hepatic impairment.
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.
Pediatric population: Children and adolescents with hypertension from 6 years to 17 years of age.
The recommended antihypertensive oral dose in pediatric patients ages 6-17 years is 2.5 mg once daily as a starting dose, up-titrated to 5 mg once daily if blood pressure goal is not achieved after 4 weeks. Doses in excess of 5 mg daily have not been studied in pediatric patients.
Administration: Swallow the tablet whole and unchewed, preferably with a glass of water.
Hypersensitivity to dihydropyridine derivatives, amlodipine or any of the excipients; Severe hypotension; Shock (including cardiogenic shock); Obstruction of the outflow tract of the left ventricle (e.g. high grade stenosis); Haemodynamically unstable heart failure after acute myocardial infarction.
Special Precautions
Amlodipine studies have not been made during pregnancy.
It is not known if Amlodipine is distributed into human breast milk.
There exists no available information about the relationship of age to Amlodipine effects in pediatric patients. Safety and efficacy have not been established in children of less than 6 years old.
Recent evidences suggest that discontinuance of antihypertensive therapy prior to surgery may be undesirable. However, anaesthesiologist must be informed of this therapy.
The safety and efficacy of amlodipine in hypertensive crisis has not been established.
Patients with heart failure should be treated with caution. In a long-term, placebo controlled study in patients with severe heart failure (NYHA class III and IV) the reported incidence of pulmonary oedema was higher in the amlodipine treated group than in the placebo group.
Calcium channel blockers, including amlodipine, should be used with caution in patients with congestive heart failure, as they may increase the risk of future cardiovascular events and mortality.
The half-life of amlodipine is prolonged and AUC values are higher in patients with impaired liver function; dosage recommendations have not been established. Amlodipine should therefore be initiated at the lower end of the dosing range and caution should be used, both on initial treatment and when increasing the dose. Slow dose titration and careful monitoring may be required in patients with severe hepatic impairment.
In the elderly increase of the dosage should take place with care.
Amlodipine may be used in renal failure at normal doses. Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment. Amlodipine is not dialyzable.
Adverse Reactions
The most commonly reported adverse reactions during treatment are somnolence, dizziness, headache, palpitations, flushing, abdominal pain, nausea, ankle swelling, oedema and fatigue.
The following undesirable effects have been observed and reported during treatment with amlodipine with the following frequencies: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to ≤1/100); rare (≥1/10,000 to ≤1/1,000); very rare (≥1/10,000).
Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness. (See table.)

Click on icon to see table/diagram/image

Exceptional cases of extrapyramidal syndrome have been reported.
Drug Interactions
The following interactions with other drugs and/or related problems have been selected based on their potential clinical importance: Note: Combinations which contain any of the following medications, depending on the current amount, may also interact with amlodipine.
Anaesthetic, hydrocarbon inhalation (it may produce additional hypotension).
Nonsteroidal anti-inflammatory drugs (NSAlDs), especially indomethacin (NSAIDS may reduce Amlodipine antihypertensive effect); Beta-adrenergic blocking agents; Estrogens; Medications with high plasma protein binding, such as anticonvulsants, hydantoin, anticoagulants deriving from coumarin and indandione, nonsteroidal anti-inflammatory drugs, quinine, salicylates, sulfinpyrazone.
Other medications producing hypotension (antihypertensive effects may be increased); Lithium; Sympathomimetics (may reduce amlodipine antihypertensive effects).
Concomitant use of amlodipine with strong or moderate CYP3A4 inhibitors (protease inhibitors, azole antifungals, macrolides like erythromycin or clarithromycin, verapamil or diltiazem) may give rise to significant increase in amlodipine exposure. The clinical translation of these PK variation may be more pronounced in the elderly.
There is no data available regarding the effect of CYP3A4 inducers on amlodipine. The concomitant use of CYP3A4 inducers (e.g., rifampicin, Hypericum perforatum) may give a lower plasma concentration of amlodipine. Amlodipine should be used with caution together with CYP3A4 inducers.
Administration of amlodipine with grapefruit or grapefruit juice is not recommended as bioavailability may be increased in some patients resulting in increased blood pressure lowering effects.
Dantrolene (infusion): In animals, lethal ventricular fibrillation and cardiovascular collapse are observed in association with hyperkalemia after administration of verapamil and dantrolene IV. Due to risk of hyperkalemia, it is recommended that the co-administration of calcium channel blockers such as amlodipine be avoided in patients susceptible to malignant hyperthermia and in the management of malignant hyperthermia.
The blood pressure lowering effects of amlodipine adds to the blood pressure-lowering effects of the other medicinal products with antihypertensive properties.
In clinical interaction studies, amlodipine did not affect the pharmacokinetics of atorvastatin, digoxin, warfarin or cyclosporin.
Simvastatin: Co-administration of multiple doses of 10 mg of amlodipine with 80 mg simvastatin resulted in a 77% increase in exposure to simvastatin compared to simvastatin alone. Limit the dose of simvastatin in patients on amlodipine to 20 mg daily.
Store at temperatures not exceeding 30°C.
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.
Tab 5 mg x 30's. 10 mg x 30's.
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