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

Logo AMLOC 5 mg tablets
AMLOC 10 mg tablets

SCHEDULING STATUS:
S3

PROPRIETARY NAME
(and dosage form):

AMLOC 5 mg tablets
AMLOC 10 mg tablets

COMPOSITION:
Each Amloc 5 mg contains Amlodipine maleate equivalent to 5 mg
amlodipine.
Each Amloc 10 mg contains Amlodipine maleate equivalent to 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 L/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:
Amloc
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 Amloc therapy at a lower dose.
Use in Renal Failure:
Although Amloc is excreted primarily via the kidney, 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 Amloc is significantly prolonged in patients with impaired hepatic function. Amloc should therefore be administered at lower doses in these patients.
Use in Children:
Safety and efficacy has not been established.
Use in Heart Failure:
An increased incidence of pulmonary oedema has been reported. Amloc may have a negative inotropic effect. AUC of Amloc 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 produce additive antihypertensive and antianginal effects. Sublingual nitroglycerin may be used as needed to abort acute angina attacks during amlodipine therapy. Nitrate medication may be used during amlodipine therapy for angina prophylaxis. Amlodipine will not protect against the consequences of abrupt beta-blocker withdrawal; gradual beta-blocker dose reduction is recommended.
Although no “rebound effect”has been reported upon discontinuation of amlodipine, a gradual decrease of dosage with medical practitioner supervision is recommended.

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 Amloc 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 Amloc to thiazide diuretics, beta-blockers, or angiotensin-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/paresthesia, 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 Amloc over-dosage. Gastric lavage may be of benefit. Gross over-dosage could result in excessive peripheral vasodilatation, resulting in marked and probably prolonged systemic hypotension. Clinically significant hypotension due to Amloc 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:
Amloc 5 mg: A white, round, slightly biconvex, bevelled edge tablet scored on one side.
Diameter: 8,0 mm
Amloc 10 mg: A white, round, slightly biconvex, bevelled edge tablet scored on one side.
Diameter: 10,0 mm.

PRESENTATION:
Amloc 5 mg: Opaque PVC/Aluminium foil blisters of 30 tablets.
Amloc 10 mg: Opaque PVC/Aluminium foil blisters of 30 tablets.

STORAGE INSTRUCTIONS:
Store in a cool (below 25°C), dry place. Protect from light.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBERS:
Amloc 5 mg:         38/7.1/0183
Amloc 10 mg:         38/7.1/0147

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION:
Pharma Dynamics (Pty) Ltd.
F02 Grapevine House
Steenberg Office Park
Westlake
7945

DATE OF PUBLICATION OF THE PACKAGE INSERT:
12 August 2004

New addition to this site: April 2006
Source: Pharmaceutical Industry

SAEPI HOME PAGE      TRADE NAME INDEX      GENERIC NAME INDEX      FEEDBACK
Information presented by Malahyde Information Systems © Copyright 1996-2006