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Visko Amlodipine 5

Visko Pharmacy Limited
9/26 Udi Road Asata, Enugu, Enugu State, Nigeria.
Email: nnamdi@viskopharm.org
Tel: 234-80-35085021, 234-70-31601265, 234-80-37430071
Website: http://visko.biz/

Brand Name

Visko Amlodipine 5

Manufacturer

Osho Pharma PVT. Ltd, Plot No.2404, Phase IV, GIDC Vatva, Ahmedabad-382445 (India).

Therapeutic Class

Calcium channel blockers (CCBs)

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Tablets (NRN:A4-3044): Amlodipine 5 mg

Pack size: 1 x 10's.

Pharmacology

Amlodipine is long-acting dihydropyridine derivative calcium channasodilasodilation el blocker.Amlodipine blocks both voltage induced and frequency induced calcium channels in inhibits the calcium influx through slow channels in peripheral and coronary vascular beds, resulting in vasodilation of the peripheral vascular system.

Vasodilation is particularly marked in the arterioles, reducing cardiac afterload and oxygen consumption. The dilated coronary vessels provide increased blood supple in myocardial ischaemia. In addition to its ability to reduce total peripheral resistance,amlodipine reduce myocardial oxygen consumption.With these pharmacological properties, amlodipine is indicatedfor hypertension. Stable and vasospastic angina.

Pharmacokinetic properties

Amlodipine is slowly and completely absorbed after oral administration.Peak plasma concentrations are attained within 6 to 12 hours.Absolute bioavailability has been estimated to be between 64 - 90%.Volume of distribution is approximately 211/kg.Amlodipine is extensively(about 90%)converted to inactive metabolites via hepatic metabolism,10%being excreted unchanged and 60%as metabolites in urine.

The bioavailability of amlodipine is not altered in the presence of food.Amlodipine is 98%bound to plasma proteins.Terminal elimination half-life is about 30 - 50 hours and steady-state plasma concentrations are achieved after 7 - 8 days. Following administration of single dose to patients with hypertension,amlodipine reduce supine and standing blood pressures within 24 hours. Due to gradual effect,hypotension is usually not observed.Antihypertensive effect is maintained for at least 24 daily after once a day administration.

Amlodipine peak plasma concentration is similar in both young and elder patients. In the elderly.amlodipine clearance tends to decrease,resulting in an increase in area under the curve (AUC) and elimination half-life.In patients with congestive heart failure,increasein area under curve (AUC)and elimination half-life were observed as expected.

Indications

Amlodipine is indicated for the treatment of mild to moderate hypertension,either used alone or together with thiazide diuretics, B-blockers or ACE Inhibitos.It is indicated for stable and variant (prinzental)angina. Amlodipine may be used as monotherapy or in combination with other agents for the treatment of angina pectoris.

Contra-indications

Amlodipine is contraindicated in patients with known sensitivity to dihydropyridine derivatives. Do not use in the case of cardiogenic shock and non-stable angina.

Precautions/Warnings

Since the vasodilation induced by amlodipine is gradual in onset, acute hypertension has rarely been reported after oral administration of Amloidpine. Nonetheless, caution should be exercised when administering Amlodipin as with any other peripheral vasodilator particularly in patients with severe aortic stenosis. Amlodipine used in similar doses in both elderly and young patient were equally tolerated. Clinical studies showed that amlodipine has no effect on driving and machinery operation.

Patients with Hepatic Failure

Since Amlodipine is extensively Metabolized by the liver,and as the plasma elimination half-life (t½) of amlodipine is 56 hours in patients with impaired hepatic function,caution should be exercised when administering amlodipine to patients to patients with severe hepatic impairment.

Beta-Blocker Withdrawal

Amlodipine is not a beta-blocker and therefore does not provide any protection againstthe dangers of abrupt beta-blocker withdrawal,this any such withdrawal should be made gradually by reduction of the beta-blocker

Pregnancy and Lactation(Pregnancy Category C)

There are no adequate and well-controlled studies in pregnant woman. Thus, amlodipine should used in these patients only if it is inevitable if the potential benefit justifies the potential risk to the foetus.It is not known whether amlodipine is excreted in human milk. In the absence of this information, it is recommended that nursing be discontinued while amlodipine is administered.

Interactions

No interaction has been observed during administration of amlodipine in conb ination wilth other agents (thiazide diuretics, B-blockers, angiotensin converting enzyme inhibitos, long-acting nitrates, digoxin, cimetidine, non-steroidal anti-inflammatory drugs and antibiotics.)

Co-adminstration of amlodipine with digoxin or cimetidine did not alter the pharmacokinetics of amlodipine. In vitro data in human plasma indicate that amlodipine has no effect on the protein binding of drugs tested (digoxin, phenytoin, warfarin and indomethacin).

Co-administration of amlodipine with warfarin in healthy male volunteers, did not change the warfrin prothrombin response time. Azole antifungals (itaconazole, ketocanole, fluconazole), erythromycin and other cytocrome P450 isoenzyme inhibitors may inhibit amlodipine metobolism. Grapefruit juice increases the concentration of amlodipine at moderate levels. Amlodipine may increase cyclosporin levels. Blood pressure lowering effect of sildenafil potentiate amlodipine effect of sildenafil potiate amlodipine effect.

Rifampin (and other potentiate enzyme inducers) increases amlodipine metabolism. Calcium however, would decrease hypotensive effect of calcium calcium channel blockers like amlodipine.

Effect of Ethanol/Herb/Nutraceuticals: Amlodipine 5 mg.has no significant effect on the pharmacokinetics o ethanol. Hardhay (Hypericum perforatum) may decrease amlodipine levels. Amlodipine should not be used with dong quai, ephedra, yohimbe, gingsen and garlic.

Adverse Effects

The frequency of observed side effects is between 0.1% and 1%.

Possible side effects observed during clincal trials and/or postmarketing phase experience are summarized as follows: Placebo controlled studies have shown that the most common side effects observed: Headache edema, somnolence, nausea, fatigue, abdominal, flushing, palpitations and dizziness. Novapin threapy has not been associated with any significant change in biochemical parameters.

The following events occurred less commonly during post marketing phase: Constipation, artralgia, back pain, dyspepsia, dyspnea, gingival hyerplasia, gynecomastia, hyperglycemia, asthenia, importence, micturition frequency, weight loss, leukopenia, fatigue, deprssion, dry mouth, muscle cramps, myalgia, neuropathy peripheral, pancreatitis, sweating increase, syncope, thrombocytopenia, vasculitis and abnormal vision.

Rarely, allergic reactions such as pruritus,rash,angioedema, erythema multiforme occurs. Seldomly,hepatitis and hepatic enzyme elevations(mostly consistent with cholestasis) were reported. Some severe cases requiring hospitalization have been reported during the use of amlodipine but no direct correlation being established. As with other calcium channel blockers,rarely myocardial infarctio, arrhythmia (including ventricular tachycardia and atrial fibrliation) and chest pain have been reported.

Dosage & Administration

Hypertension: The initial dose is 2.5 mg - 5.0 mg daily,with usual dose being 5 mg once a day a maximum dose of 10 mg daily.

Angina: The usual dose is 5 mg - 10 mg, with lower dose suggested in the elderly and in patients with hepatic insufficiency.

Dialysis: Hemodialysis and peritoneal dialysis dose not increase elimination of amlodipine. No extra dosage regiment is required.

Hepatic insufficiency: 2.5 mg once a daily.

No adequate information is available regarding the overdosage of amlodipine. In some cases gastric lavage may be useful. However, the available date indicate that overdosage of amlodipine may cause excessive peripheral vasodilation and thus long-term hypotension.

In such cases elevate lower extremities and moitor closely the cardiac and respiratory functions togther with circulation fluid volume and urinary output. As amlodipine is highly protein, hemodialysis is not likely to be of any benefit. Intravenous calcium gluconate may help to reverse the effects of calcium blocking.

Geriatric Use: Due to higher incidence of decredsed hepatic, renal or cardiac function in geriatric patient, treatment shart from lowest possible dosage initially.

Elderly patients have decreased clearance for amlodipine.

Storage/Handling Recommendations

Store in a dry place at room temperature below 25oC in its package. Keep out of reach of children.

Review Date

2016-10-28 04:29:41