(AMLODIPINE 5MG/CAPLET)
COMPOSITION:
Each caplet contains Amlodipine besylate (equivalent to 5mg Amlodipine).
ACTIONS:
Amlodipine in Drulovask®caplets is a dihydropyridine calcium channel blocking agent (slow channel blocker or calcium ion antagonist) and selectively inhibits calcium influx across cell membranes in cardiac and vascular smooth muscle.
The antihypertensive action is due to a relaxant effect on vascular smooth muscle. The antianginal effect is believed to be due to a reduction in the total ischemic burden either by dilating the peripheral arterioles and thus, reducing the total peripheral resistance (after load) against which the heart works or by dilating the main coronary arteries and coronary arterioles there by increasing myocardial oxygen delivery in patients with coronary artery spasm (or prinzmetal’s or variant angina).
INDICATIONS:
Amlodipine is indicated for the treatment of hypertension; it may be used alone or in combination with a thiazide diuretic, alpha blockers,beta adrenoceptor blocking agents, or an angiotensin-converting enzyme inhibitor.
Amlodipine is indicated for the treatment of myocardial ischaemia wether due to fixed obstruction (stable angina) and /or vasospasm /vasoconstriction (prinzmetal’s or variant angina) of coronary vasculature; alone or with angina that is refractory to nitrates and /or beta blockers.
CONTRAINDICATIONS
– Amlodipine is contraindicated in patients with a known sensitivities to dihydropyridines
– Amlodipine should be used with caution in patients with congestive heart failure because of the slight risk for negative inotropic effect.
PREGNANCY AND LACTATION:
Safety of amlodipine in human pregnancy or lactation has not been established. Amlodipine has been shown to prolong the duration of labor in rats. Use in pregnancy only when clearly needed and when the benefits outweigh the potential hazard to the fetus.
WARNINGS / PRECAUTIONS:
As with all calcium antagonists, amlodipine’s 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.
KEEP OUT OF THE REACH OF CHILDREN!
SIDE/ADVERSE EFFECTS
The side effects include headache, oedema, rash, fatigue, nausea, flushing and dizziness.
The following adverse reactions have been reported rarely: pruritus, angioedema, palpitations, dyspnoea, abdominal pain, back pain, dyspepsia, muscle cramps, altered bowel habit, myalgia, peripheral neuropathy, mood changes, dry mouth, increased sweating and visual disturbance.
DRUG INTERACTION
– 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.
– Azole antifungals (itraconazole, ketoconazole, fluconazole), erythromycin and other inhibitors of cytochrome P450 isoenzyme 3A4 may inhibit amlodipine’s metabolism.
Blood pressure lowering effects of sildenafil are additive with amlodipine. Rifampicin (and potentiallyother enzymes inducers) increase metabolism of amlodipine. Calcium may reduce the calcium channel blockers hypotensive effects.
DOSAGES AND ADMINISTRATION
For both hypertension and angina, the usual initial dose is 5mg once daily which may be increased to a maximum dose of 10mg 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 ELDERLY
Dosing should start at the lower end of dosing range due to possible increased incidence of hepatic, renal, or cardiac impairment. Elderly patients also show decreased clearance of amlodipine
USE IN CHILDREN
Safety and efficacy have not been established.
USE IN PATIENTS WITH HEPATIC IMPAIRMENT
As with all calcium antagonists, amlodipine’s half life is prolonged in patients with impaired liver function and dosage recommendations have not been established. The drug should be administered with caution in these patients.
USE IN PATIENTS WITH RENAL IMPAIRMENT
Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment, therefore the normal dosage is recommended.
OVERDOSE
Primary cardiac symptoms of calcium blocker overdose include hypotention and bradycardia. Hypotension is caused by peripheral vasodilation, myocardial depression and bradycardia.
Recommended treatment consists of the following:
-Hypotension–intravenous fluids, intravenous dopamine or dobutamine, calcium gluconate, isoproterenol, metaraminol, or norepinephrine should be used as appropriate.
– Bradycardia – intravenous atropine, isoproterenol, norepinephrine or calcium chloride or use of electronic cardiac pacemalcer as appropriate.
-Patient with suspected calcium channel blocker overdose should be placed on a cardiac monitor. Monitor homodynamic status closely including heart rate, blood pressure, EKG and urinary output.
-Monitor electrolytes, renal function tests and glucose.
-Monitor respiratory function and oxygenation, pulmonary edema may occur.
STORAGE
Store below 300C.
PRESENTATION:
DrulovaskR is available as caplets containing 5mg amlodipine in a blister of 10’s per pack.