Gensia

GENSIA^®
Tablet

COMPOSITION
GENSIA^® 5
Each tablet contains Amlodipine besylate 7.1 mg equivalent to 5 mg Amlodipine base.
GENSIA^® 10
Each tablet contains Amlodipine besylate 14.2 mg equivalent to 10 mg Amlodipine base.

ACTIONS
Pharmacodynamic Properties
Amlodipine is a calcium ion influx inhibitor (slow channel blocker or calcium ion antagonist) and inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle.
The mechanism of the antihypertensive action of amlodipine is due to a direct relaxant effect on vascular smooth muscle. The precise mechanism by which amlodipine re levels angina has not been fully determined but amlodipine reduces total ischemic burden by the following two actions:

• Amlodipine dilates peripheral arterioles and thus, reduces the total peripheral resistance (afterload) againts which the heart works. Since the heart rate remains stable, this unloading of the heart reduces myocardial energy consumption and oxygen requirements.
• The mechanism of action of amlodipine also probably involves dilatation of the main coronary arteries and coronary arterioles, both in normal and ischemic regions. This dilatation increases myocardial oxygen delivery in patients with coronary artery spasm (Prinzmetal's or variant angina).

In patients with hypertension, once daily dosing provides clinically significant reductions of blood pressure in both the supine and standing positions throughout the 24 hour interval. Due to the slow onset action, acute
hypotension is not a feature of amlodipine administration.
In patients with angina, once daily administration of amlodipine increases total exercise time, time to angina onset; and time to 1 mm ST segment depression, and decreases both angina attack frequency and nitroglycerine tablet consumption.

INDICATIONS
Amlodipine is indicated for:
Treatment of hypertension, it may be used alone or in combination with other antihypertensive agents.
Treatment of chronic stable angina; it may be used alone or in combination with other anginal agents.
Treatment of confirmed or suspected vasospastic (Prinzmental's or variant) angina; it may be used alone or in combination with other antianginal agents.

DOSAGE AND ADMINISTRATION
Posology and Method of Administration
For hypertension 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 patients response and severity.
Small, fragile or elderly individuals, or patients with hepatic insufficiency may be started on 2.5 mg once daily and this dose may be used when adding amlodipine to other antihypertensive therapy.
Majority of hypertensive patients with 5 mg/day the dose may not necessarily be increased. For those who need higherdose, amlodipine can be increased to 7.5 mg/day with maximum dose of 10 mg/day.
The recommended dose for chronic stable or vasospastic angina is 5-10 mg, with the lower dose suggested in the elderly and in patients with hepatic insufficiency.
No dose adjustment of amlodipine is required upon concomitant administration of thiazide diuretics, beta blocker, and angiotensin-converting enzyme inhibitors.

Use in Children
No experience is available on use of amlodipine in children.

OVERDOSAGE
In humans, experience with intentional overdose is limited. Gastric lavage may be worthwhile is some cases. Available data suggest that gross overdosage could result in excessive peripheral vasodilatation with subsequent marked and probably prolonged systemic hypotension. Clinically significant hypotension due to amlodipine overdosage calls for active cardiovascular support including frequent monitoring of cardiac and respiratory function, elevation of extremities, and attention to circulating fluid volume and urine output. A vasoconstrictor may be helpful in restoring vascular tone and blood pressure, provided that there is no contraindication to its use. Intravenous calcium gluconate may be beneficial in reversing the effects of calcium channel blockage. Since amlodipine is highly protein-bound, dialysis is not likely to be of benefit.

CONTRAINDICATIONS
Hypersensitive to this drug.

DRUG INTERACTIONS
Interaction with Other Medicaments and Other Forms of Interaction
Amlodipine has been safely administered with thiazide diuretics, alpha blockers, angiotensin-converting enzyme inhibitors, long-acting nitrates, sublingual nitroglycerine, non steroidal anti-inflammatory drugs, antibiotics, and oral hypoglycemic drugs.

Co-administration of amlodipine with digoxin did not change serum digoxin levels or digoxin renal clearance in normal volunteers, and that co-administration of cimetidine did not alter the pharmacokinetics of amlodipine. Amlodipine has no effect on protein binding of the drugs tested (digoxin, phenytoin, warfarin, or indomethacin).
In healthy male volunteers, the co-administration of amlodipine does not significantly alter the effect of warfarin on prothrombin response time.

Pregnancy and Lactation
Safety of amlodipine in human pregnancy or lactation  has not been established. Amlodipine does not demonstrate toxicity in animal reproductive studies other than to delay parturition and prolong labor in rats at a dose level fifty times the maximum recommended dose in humans. Accordingly, use in pregnancy is only recommended when there is no safer alternative and when the disease itself carries greater risk for the mother and fetus.

Effects on Ability to Drive and Use Machines
Not applicable.

WARNINGS
Special Warning and Special Precaution for Use
Use in Patients with Impaired Hepatic Function
As with all calcium antagonists, amlodipine 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.

Use in Renal Failure
Amlodipine is extensively metabolized to inactive metabolites with 10% excreted as unchanged drug in the urine. Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment. Amlodipine may be used in such patients at normal dose. Amlodipine is not dialyzable.

Use in Patients with Congestive Heart Failure
In general, calcium channel blockers should be used with caution in patients with heart failure. Amlodipine (5-10 mg per day) has been studied in a placebo-controlled trial of 1153 patients with NYHA class II or IV heart failure on stable doses of ACE inhibitor, digoxin and diuretics. Follow-up was at least 6 months, with a mean of about 14 months. There was no overall adverse effect on survival or cardiac morbidity (as defined by life-threatening arrhythmia, acute myocardial infarction, or hospitalization for worsened heart failure). Amlodipine has been compared with placebo in four 8-12 week studies of patients with NYHACIass ll/lll heart failure, involving a total of 697 patients. In these studies, there was no evidence of worsened heart failure based on measures of exercise tolerance, NYHA classification symptoms, or LVEF.

Use in Elderly
The time to reach peak plasma concentrations of amlodipine is similar in elderly and younger subjects. Amlodipine clearance tends to be decreased with resulting increases in AUC and elimination, half-life in elderly patients.
Amlodipine, used at similar doses in elderly or younger patients, is equally well tolerated. Therefore normal dosage regimens are recommended.

ADVERSE REACTIONS
Undesirable Effects
Amlodipine is well tolerated. The most commonly observed side effects were headache, edema, fatigue, somnolence, nausea, abdominal pain, flushing, palpitations, and dizziness.
Less commonly observed side effects in marketing experience include altered bowel habits, arthralgia, asthenia, dyspepsia, dyspnea, gingiva hyperplasia, gynaecomastia, impotence, increased urinary frequency, mood changes, muscle cramps, myalgia pruritus, rash, visual disturbance, and rarely erythema multiforme.
Jaundice and hepatic enzyme elevations have been reported very infrequently (mostly consistent with cholestasis). Some cases severe enough to require hospitalization have been reported in association with use of amlodipine. In many instances, causal association is uncertain.
As with other calcium channel blockers the following adverse events have been rarely reported and cannot be distinguished from the natural history of the
underlying disease: myocardial infarction, arrhythmia (including ventricular tachycardia and atrial fibrillation) and chest pain.

PRESENTATION
GENSIA^®5 : Box, 3 blisters@ 10 tablets (available as 5 mg tablets) Reg.No.DKL0821635210A1
GENSIA^® 10 : Box, 3 blisters @ 10 tablets (available as 10 mg tablets) Reg.No.BKL0821635210B1                    

STORE BELOW 30°C

ON MEDICAL PRESCRIPTION ONLY

HARUS DENGAN RESEP DOKTER

Manufactured by:
PHAROS
Jakarta - Indonesia

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