Pharmamax Amlodipine Besylate Tablets

Amlodipine-5

Amlodipine Besylate Tablets USP

Amlodipine-10

Amlodipine Besylate Tablet USP

For the use of a Registered Medical Practitioner, or a Hospital or a Laboratory only.

 

COMPOSITION

Each uncoated tablet contains:

Amlodipine Besylate USP

Eq. to Amlodipine 5mg/10mg

Excipients q.s.

 

PHARMACOLOGICAL ACTION

PHARMAMAX AMLODIPINE is a dihydropyridine calcium channel blocker.

It inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle without affecting serum calcium concentrations. Direct relaxation of vascular smooth muscle forms the basis of the antihypertensive action. In angina pectoris, amlodipine acts as a peripheral arteriolor vasodilator resulting in a reduction in total peripheral resistance (afterload). Myocardial energy and oxygen requirements are reduced. Amlodipine exerts its activity by binding to the dihydropyridine binding sites. It exerts minimal action on cardiac conduction, contraction and heart rate.

 

PHARMACOKINETICS

Complete absorption of amlodipine is slow following oral administration with peak plasma levels being attained after 6 to 12 hours. Amlodipine has a bioavailability of about 64% and a plasma elimination half-life of 35 to 50 hours, allowing for once-daily oral dosing. Steady state plasma concentrations are achieved after 7 to 8 days of consecutive dosing. The volume of distribution is about 20/kg. Metabolism is via the liver and is extensive with less than 10% of amlodipine appearing unchanged in the urine. Metabolites are inactive and primarily (up to 60%) excreted via the kidney.

 

INDICATIONS

PHARMAMAX AMLODIPINE is indicated for the

• Treatment of angina pectoris.

• Treatment of mild to moderate hypertension, alone or in combination with other antihypertensives.

 

CONTRA-INDICATIONS

Hypersensitivity to any of the ingredients.

Hypersensitivity to dihydropyridines.

 

WARNINGS

Use in the Elderly

PHARMAMAX AMLODIPINE clearance is decreased (40-60%) in the elderly, which results in increases of amlodipine concentration in the area under the concentration-time curve (AUC) and elimination half-life. Therefore, elderly patients should start PHARMAMAX AMLODIPINE therapy at a lower dose.

Use in Renal Failure

Although PHARMAMAX AMLODIPINE is excreted primarily via the kidneys, mild renal impairment does not appear to have an effect on the plasma concentrations. Severe renal impairment may however require a dosage reduction. Amlodipine is not dialysable.

Use in impaired Hepatic Function

The half-life of PHARMAMAX AMLODIPINE is significantly prolonged in patients with impaired hepatic function.

PHARMAMAX AMLODIPINE should therefore be administered at lower doses in those patients.

Use in Children

Safety and efficacy hove not been established.

Use in Heart Failure

An increased incidence of pulmonary oedema has been reported. PHARMAMAX AMLODIPINE may have a negative inotropic effect. AUC of PHARMAMAX AMLODIPINE may increase in patients with heart failure.

Porphyria

Safety has not been established.

 

INTERACTIONS

Concurrent administration of sublingual nitroglycerin, long acting nitrates, beta-blockers or other antianginal agents with amlodipine may cause severe hypotension.

 

PREGNANCY AND LACTATION

Safety in pregnancy and lactation has not been established (see CONTRA-INDICATIONS).

 

DOSAGE AND DIRECTIONS FOR USE

Hypertension and Angina Pectoris

Adults

An initial dose of 5 mg PHARMAMAX AMLODIPINE once daily is recommended which may be increased to 10 mg once a day after 10 -14 days of therapy if there is no improvement. No dose reduction is required when adding PHARMAMAX AMLODIPINE to thiazide diuretics, beta-blockers, or angiotension converting enzyme inhibitors.

 

SIDE EFFECTS AND SPECIAL PRECAUTIONS

Side effects

Cardiovascular

Frequent: Peripheral oedema, palpitations.

Less frequent: Hypotension (including orthostatic hypotension), syncope, vasculitis, myocardial infarction, arrhythmia (including ventricular tachycardia and atrial fibrillation), chest pain.

Neurological

Frequent: Dizziness, headache, somnolence.

Less frequent: Hypertonia, hypoesthesia/paraesthesia, peripheral neuropathy, tremor, insomnia, mood changes.

Gastro-Intestinal

Frequent: Nausea, abdominal pain.

Less frequent: Altered bowel habits, vomiting, dyspepsia, gingival hyperplasia, pancreatitis.

Musculoskeletal

Frequent: Fatigue.

Less frequent: Arthralgia, asthenia, back pain, muscle cramps, myalgia.

Autonomic Nervous system

Frequent: Flushing.

Less frequent: Dry mouth, increased sweating.

Hepatobilliary

Less frequent: Hepatitis, jaundice, raised liver enzymes (mostly consistent with cholestasis).

Haematological

Less frequent: Purpura, thrombocytopenia, leucopenia.

Genito-urinary

Less frequent: Increased urinary frequency, impotence.

Body as whole

Less frequent: Pain, weight increase/decrease.

Endocrine

Less frequent: Gynaecomastia.

Metabolic

Less frequent: Hyperglycemia.

Skin and Appendages

Less frequent: Alopecia.

Respiratory

Less frequent: Coughing, dyspnoea.

Vision

Less frequent: Visual disturbances.

Special Senses

Less frequent: Taste perversion, tinnitus.

Hypersensitivity reactions

Less frequent: Allergic reactions with pruritus, rash angioedema and erythema multiforme.

 

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT

There is no documented experience with PHARMAMAX AMLODIPINE overdosage. Gastric lavage may be of benefit. Gross overdosage could result in excessive peripheral vasodilatation, resulting in marked and probably prolonged systemic hypotension. Clinically significant hypotension due to PHARMAMAX AMLODIPINE over- dosage requires active cardiovascular support. Intravenous calcium gluconate may be of benefit in reversing the effects of calcium channel blockade. Since amlodipine is highly protein-bound, dialysis is not likely to be of benefit. Treatment is symptomatic and supportive.

 

IDENTIFICATION

PHARMAMAX AMLODIPINE – 5 TABLETS: An uncoated tablet with breakline on one side and plain on other side.

PHARMAMAX AMLODIPINE -10 TABLETS: An uncoated tablet with breakline on one side and plain on other side.

 

PRESENTATION

PHARMAMAX AMLODIPINE – 5 TABLETS: PVC/Aluminium foil blister strips containing 2 x 14 tablets and 10 x 14 tablets.

PHARMAMAX AMLODIPINE -10 TABLETS: PVC/Aluminium foil blister strips containing 2 x 14 tablets and 10 x 14 tablets.

 

STORAGE INSTRUCTIONS

Keep all medicine out of reach of children.

Store at a temperature not exceeding 30oC in a dry place.

Protect from light.

 

Product License Holder

TICOS LIFESCIENCES LIMITED

1103/A, Synergy Tower,

Ahmedabad – 380 015. INDIA.

 

Manufactured by

Baroque Pharmaceuticals Pvt. Ltd.

192/2 & 3, Sokhada-380 620 (Khambhat)

 

Marketed by

PHARMAMAX NIGERIA LIMITED

A Member of KCH Group

49, Orange Drive, Crown Estate,

Lekki-Epe Expressway, Lagos, Nigeria.