INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo AMLODAC 5 TABLETS
AMLODAC 10 TABLETS

SCHEDULING STATUS:
S3

PROPRIETARY NAME
(and dosage form):

AMLODAC 5 TABLETS
AMLODAC 10 TABLETS

COMPOSITION:
Each tablet contains amlodipine besylate equivalent to 5 mg or 10 mg
amlodipine.

PHARMACOLOGICAL CLASSIFICATION:
A 7.1 Vasodilators, hypotensive medicines.

PHARMACOLOGICAL ACTION:
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 arteriolar 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:
AMLODAC 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
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 AMLODAC therapy at a lower dose.
Use in Renal Failure
Although AMLODAC 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 AMLODAC is significantly prolonged in patients with impaired hepatic function. AMLODAC should therefore be administered at lower doses in these patients.
Use in Children
Safety and efficacy have not been established.
Use in Heart Failure
An increased incidence of pulmonary oedema has been reported. AMLODAC may have a negative inotropic effect. AUC of AMLODAC 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 AMLODAC 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 AMLODAC to thiazide diuretics, beta-blockers, or angiotensionconverting 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, hypaesthesia/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 AMLODAC 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 AMLODAC 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:
AMLODAC 5 TABLETS
: A brown, round, biconvex, film coated tablet with breakline on one side and plain on other side.
AMLODAC 10 TABLETS: A white, round, biconvex, film coated tablet with breakline on one side and plain on other side.

PRESENTATION:
AMLODAC 5 TABLETS
: PVC/Aluminium foil blister strips containing 10 tablets. 3 or 10 blister strips are packed in an outer carton.
AMLODAC 10 TABLETS: PVC/Aluminium foil blister strips containing 10 tablets. 3 or 10 blister strips are packed in an outer carton.

STORAGE INSTRUCTIONS:
Store in a cool (below 25ºC), dry place. Protect from light.
Do not remove blisters from outer carton until required for use.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER:
AMLODAC 5 TABLETS
: A39/7.1/0532
AMLODAC 10 TABLETS: A39/7.1/0533

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION:
Zydus Healthcare SA (Pty) Ltd
Adrina Building, First Floor
32-34 Klinkenberg Street
Van Der Hoff Park
Potchefstroom 2531

DATE OF PUBLICATION OF THE PACKAGE INSERT:
24 June 2005

JETA18BSAAA

New addition to this site: January 2008
Source: Pharmaceutical Industry

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