AMLIVE-AT and AMLIVE-ATH

AMLIVE-AT and AMLIVE-ATH TAB

COMPOSITION

AMLIVE-AT TAB

Each tablet contains:

Amlodipine besilate eqv. to Amlodipine                    5 mg

Atenolol IP                                                                 50 mg 

AMLIVE-ATH TAB

Each tablet contains:

Amlodipine besilate eqv. to Amlodipine                    2.5 mg

Atenolol IP                                                                 25 mg             

DESCRIPTION

AMLIVE- AT and AMLIVE-ATH contains combination of Amlodipine belonging to Calcium Channel Blockers and Atenolol belonging to beta-blockers, important groups of drugs for treatment of hypertension. They are efficacious, safe drugs and are well tolerated. Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow calcium channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells.

Atenolol is a cardioselective beta blocker, selective to β₁. It is reported to lack intrinsic sympathomimetics activity and membrane-stabilizing properties and are thus used in hypertension, angina pectoris, cardiac arrhythmia and myocardial infarction as well as in prophylaxis of migraine.

The combination product results in additive anti-hypertensive activity.

PHARMACOLOGY

Pharmacodynamics

Amlodipine: Following administration of therapeutic doses to patients with hypertension, amlodipine produces vasodilation resulting in a reduction of supine and standing blood pressures. These decreases in blood pressure are not accompanied by a significant change in heart rate or plasma catecholamine levels with chronic dosing. Although the acute intravenous administration of amlodipine decreases arterial blood pressure and increases heart rate in hemodynamic studies of patients with chronic stable angina, chronic oral administration of amlodipine in clinical trials did not lead to clinically significant changes in heart rate or blood pressures in normotensive patients with angina.

Atenolol: It acts by blocking the intrinsic sympathomimetics activity of cardioselective β₁, thereby producing vasodilation and decrease in blood pressure.

Pharmacokinetics

Amlodipine: After oral administration of therapeutic doses of amlodipine, absorption produces peak plasma concentrations between 6 and 12 hours. Absolute bioavailability has been estimated to be between 64 and 90%. The bioavailability of amlodipine is not altered by the presence of food. Amlodipine is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine. Ex vivo studies have shown that approximately 93% of the circulating drug is bound to plasma proteins in hypertensive patients. Elimination from the plasma is biphasic with a terminal elimination half-life of about 30-50 hours. Steady-state plasma levels of amlodipine are reached after 7 to 8 days of consecutive daily dosing.

Elderly patients and patients with hepatic insufficiency have decreased clearance of amlodipine with a resulting increase in AUC of approximately 40-60%, and a lower initial dose may be required. A similar increase in AUC was observed in patients with moderate to severe heart failure.

Atenolol: After oral administration, it is incompletely absorbed (about 50%) from the GI tract. Peak plasma concentrations are reached in 2-4 hours. It crosses the placenta and is also found in breast milk. Only small amounts are reported to cross the blood brain barrier. It undergoes little or no hepatic metabolism and is excreted mainly in the urine.

Indications
AMLIVE-AT and AMLIVE-ATH is indicated for hypertension, chronic stable angina and vasospastic angina (Prinzmetal's or variant angina).

DOSAGE AND ADMINISTRATION

Hypertension, Chronic unstable, vasospastic or unstable angina:

AMLIVE-AT: 1 tab OD.

AMLIVE-ATH: 1 tab BD.

CONTRAINDICATIONS

Hypotension, sinus bradycardia, 2^nd and 3^rd degree block, cardiogenic shock, overt congestive failure, hypersensitivity to either component, pregnancy.

WARNING AND PRECAUTIONS

Excessive fall of BP may occur in elderly patients, should be used with caution in patients with COPD, thyrotoxicosis, congestive failure, diabetics tachycardia, lactation.

ADVERSE EFFECTS

Headache, hypotension, dizziness, breathlessness, fatigue, muscle cramps, bradycardia, drowsiness, chest pain, hypersensitivity reactions and rarely impotence.

DRUG INTERACTIONS

• Decreased effect with aluminium and calcium salts, barbiturates, cholestyramine, NSAIDs, ampicillin and rifampin.

STORAGE
Store in a cool and dry place

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Flusing, rare case of hypersensitivity, angioedema, bronchospasm, shortness of breath, hypotension, urticaria are some of the side effect observed

CONTRAINDICATIONS:

VOMICARE is contraindicated for patients known to have hypersensitivity to Ondansetron Hydrochloride.

VOMICARE: SAFETY PROFILE

·         No dosage adjustment is required for VOMICARE taking phenytoin, carbamazepine, Rifamipicin as these drugs hastens the metabolism of other drugs.

• Carcinogenesis, mutagenesis and impairment of fertility:

Carcinogenic effects were not seen in 2-years studies in rats and mice with dose up to 10 and 30 mg/kg/day, respectively. Ondansetron was not mutagenic in standard tests for mutagenicity. Oral administration of ondansetron up to 15 mg/kg/day did not affect he fertility or general reproductive performance of male and female rats.

• Pregnancy: Teratogenicity:

Studies have been performed in pregnant rats and rabbits at daily oral dose up to 15 and 30 mg/kg/day, respectively and have revealed no evidence of impaired fertility or harm to the fetus. There are however, no adequate and well control tests carried out in pregnant women, the drug, should therefore be used in pregnancy only if clearly indicated.

• Nursing Mothers:

Ondansetron is excreted in the breast milk of rats. It is not known whether ondansetron is excreted in human milk, caution should be exercised when ondansetron is administered to a nursing woman.

• Pediartic Use:

Little information is available about dosage in pediatric patients 4 years of age or younger.

• Geriartic Use:

Of the total number of subjects enrolled in the cancer chemotherapy induced and post operative nausea and vomiting clinical trials, no overall differences in the safety and effectiveness were observed in young and geriartic (over 65years) subjects. Dose adjustment in not needed in patients over the age of 65 years.