VASPRIM (AMLODIPINE BESILATE )

FORMULATION
Each tablet contains: Amlodipine besilate equivalent to 5 mg amlodipine or amlodipine (as besilate) 5 mg

INDICATIONS
For the first line treatment of hypertension and can be used as the sole agent to control blood pressure ion the majority of patients.patients not adequetely controlled on a single antihypertensive agent may benefit from the addition of amlodopine,which has been used in combination with thiazide diuretic,b-adrenoceptor blocking agent or an angiotensinconverting enzyme inhibitor.Amlodipine is indicated for the first line treatment for myocardial ischemia,whether due to fixed obstruction (stable angina)and/or vasospasm/vasoconstriction(prinzmetal’s or variant angina)Amlodipine may used where the clinical presentation suggest a possible vasospatic/vasocostractive component but where vasospasm/vasoconstriction has not been confirmed.
Administration and Dosage

For both hypertension and angina, the usual initial dose is 5mg amlodipine once daily which may be increased to maximum dose of 10 mg depending on the individual patient’s response.no dose adjustment of amlodipine is required upon concomitant administration of thiazide diuretic, b-blockers and angiotensinconverting inhibitors or as prescribed by a physician.

PHARMACOKINETICS PROPERTIES
ABSORPTION after oral administraton of the therapeutic doses,is well absorbed with pick blood levels between 6-12 hours post dose. Absolute bioavailability has been estimated to be between 64 and 80%. The volume of distribution is approximately 21L/kg. In vitro studies have show that approximately 97.5% of circulating amlodipine is bound to plasma proteins. Absorption of amlodipine is unaffected by compsumption of food.

BIOTRANSFORMATION / ELIMINATION
The terminal plasma elimination half life is about 35-50 hours and is consistent with once daily dosing.steady state plasma levels are reached after 7-8 days of consecutive dosing.Amlodipine is extensively metabolized by the liver to inactive metabolites with 10% of the parent compound and 60% of metabolites are excreted in the urine.

CONTRAINDICATIONS:
patients with known sensitivity to dehydropyridines,amlodipine or other ingredients in the formula.

Special warnings and precautions for use:
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 in extensuvely metabolized to inactive metabolites with 10% excreted as unchange 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 doses. Amlodipine is not dialyzable.

Use in Elderly
To be decreased with resulting increases in AUC and elimination hal-life in elderly patients,the same in patients with congestive heart failure. Amlodipine used at similar doses in elderly or younger patients is equally tolerated. Therefore, normal dosage regimens are recommended.

Use in pregnancy and lactation:
Safety of amlodipine in pregnancy or lactation has not been established accordingly,use in pregnancy is only recommended whwn there is no safe alternative and when the disease itself carriers greater risk for the mother and fetus.

ADVERSE REACTIONS:
The most commonly observed side effects where fatigue, flushing, dizziness, headache. Edema, palpitation, abdominal pain, nausea and somnolence. The less commonly obseved side effects where back pain, alopecia, dry mouth, malaise, muscle cramps, syncope, peripheral neuropathy, hypertonia, tremor, hyperglycemia, gynecomastia, altered bowel habits, dyspepsia, dyspnea, pancreatitis, vomiting, impotence, increase urinary frequency, mood changes, thrombocytopenia, visual disturbances, leucopenia, allegic reaction including pruritis, rash,angioedema, and erythema multiforme.