Full Prescribing Info
Amlodipine besilate.
One Stadovas 5 tablet contains 5 mg of amlodipine (as amlodipine besilate).
One Stadovas 10 tablet contains 10 mg of amlodipine (as amlodipine besilate).
Pharmacology: Pharmacodynamics: Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.
Pharmacokinetics: Amlodipine is well absorbed after oral doses with peak blood concentrations occurring after 6 to 12 hours. The bioavailability varies but is usually about 60 to 65%. Amlodipine is reported to be about 97.5% bound to plasma proteins. It has a prolonged terminal elimination half-life of 35 to 50 hours and steady-state plasma concentrations are not achieved until after 7 to 8 days of use. Amlodipine is extensively metabolised in the liver; metabolites are mostly excreted in urine together with less than 10% of a dose as unchanged drug. Amlodipine is not removed by dialysis.
Amlodipine is used alone or in combination with other classes of antihypertensive agents in the management of hypertension.
Amlodipine also is used for the management of Prinzmetal variant angina and chronic stable angina pectoris. The drug has been used alone or in combination with other antianginal agents.
Dosage/Direction for Use
Stadovas is administered orally and may be given without regard to meals.
Dosage: For both hypertension and angina 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 patient's response.
No dose adjustment of amlodipine is required upon concomitant administration of thiazide diuretics, beta-blockers, and angiotensin-converting enzyme inhibitors.
Use in the elderly normal dosage regimens are recommended. Amlodipine, used at similar doses in elderly or younger patients, is equally well tolerated. Use in children safety and effectiveness of amlodipine in children have not been established.
Single oral doses of amlodipine equivalent to 40 mg/kg and 100 mg/kg in mice and rats, respectively, caused deaths. Overdosage might be expected to cause excessive peripheral vasodilation with marked hypotension and possibly a reflex tachycardia.
If massive overdosage occurs, active cardiac and respiratory monitoring should be instituted.
Frequent blood pressure measurements are essential. Should hypotension occur, cardiovascular support including elevation of the extremities and the judicious administration of fluids should be initiated. If hypotension remains unresponsive to these conservative measures, administration of vasopressors (such as phenylephrine) should be considered with attention to circulating volume and urine output. Intravenous calcium gluconate may help to reverse the effects of calcium entry blockade. As amlodipine is highly protein bound, hemodialysis is not likely to be of benefit.
Amlodipine is contraindicated in patients with a known sensitivity to dihydropyridines, amlodipine, or any of the inert ingredients.
Special Precautions
Amlodipine should be used with caution in patients with hypotension, cardiac reserve is poor, heart failure.
The drug should not be used in cardiogenic shock, in patients who have suffered a myocardial infarction in the previous 2 to 4 weeks, or in acute unstable angina, in treatment an anginal attack in chronic stable angina.
In patients with severe aortic stenosis amlodipine may increase the risk of developing heart failure.
Sudden withdrawal of amlodipine might be associated with an exacerbation of angina.
The dose may need to be reduced in patients with hepatic impairment.
Effects on Ability to Drive and Use Machine: Amlodipine can have minor or moderate influence on the ability to drive and use machines. If patients taking amlodipine suffer from dizziness, headache, fatigue or nausea the ability to react may be impaired. Caution is recommended especially at the start of treatment.
Use In Pregnancy & Lactation
No clinical experience with the preparation in pregnancy or lactation. Accordingly, amlodipine should not be administered during pregnancy, or lactation, or to women of childbearing potential unless effective contraception is used.
Adverse Reactions
The most common adverse effects of amlodipine are associated with its vasodilator action and often diminish on continued therapy. They include dizziness, flushing, headache, hypotension, peripheral oedema, tachycardia, and palpitations. Nausea and other gastrointestinal disturbances, increased micturition frequency, lethargy, eye pain, visual disturbances, and mental depression have also occurred. A paradoxical increase in ischaemic chest pain may occur at the start of treatment and in a few patients excessive fall in blood pressure has led to cerebral or myocardial ischaemia or transient blindness.
Drug Interactions
Amlodipine has been safely administered with thiazide diuretics, alpha blockers, beta blockers, angiotensin-converting enzyme inhibitors, long-acting nitrates, sublingual glyceryl trinitrate, non-steroidal anti-inflammatory drugs, antibiotics, and oral hypoglycaemic drugs.
Cimetidine, grapefruit juice, antacid: Co-administration of amlodipine and those had no significant effect on the pharmacokinetics of amlodipine.
Sildenafil: When amlodipine and sildenafil were used in combination, each agent independently exerted its own blood pressure lowering effect.
Atorvastatin: Co-administration amlodipine with 80 mg atorvastatin resulted in no significant change in the steady-state pharmacokinetics parameters of atorvastatin.
Digoxin: Co-administration of amlodipine with digoxin did not change serum digoxin levels or digoxin renal clearance.
Warfarin: Co-administration of amlodipine with warfarin did not change the warfarin prothrombin response time.
Do not store above 30°C. Protect from light.
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.
Stadovas tab 10 mg
Stadovas tab 5 mg
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