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

Logo AMLATE 5 (tablets)
AMLATE 10 (tablets)
SCHEDULING STATUS:
S3

PROPRIETARY NAME
(and dosage form):

AMLATE 5 (tablets)
AMLATE 10 (tablets)

COMPOSITION:
AMLATE 5         Each tablet contains amlodipine maleate equivalent to 5 mg amlodipine base.
AMLATE 10         Each tablet contains amlodipine maleate equivalent to 10 mg amlodipine base.

PHARMACOLOGICAL CLASSIFICATION
A7.1 Vasodilators, hypotensive medicines

PHARMACOLOGICAL ACTION
Amlodipine is a dihydropyridine calcium ion 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
AMLATE is indicated for:
• The treatment of angina pectoris
• The treatment of mild-to moderate hypertension, alone or in combination with other antihypertensives

CONTRA-INDICATIONS
Hypersensitivity to any of the ingredients
Hypersensitivity to dihydropyridines
Safety in pregnancy and lactation has not been established

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 startAMLATE therapy at a lower dose.
Use in renal failure
Although amlodipine 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-lifeamlodipine is significantly prolonged in patients with impaired hepatic function. AMLATE 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.
AMLATE may have a negative inotropic effect. AUC of amlodipinemay 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.

DOSAGE AND DIRECTIONS FOR USE
Hypertension and Angina Pectoris
Adults:
An initial dose of 5 mg AMLATE 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 AMLATE 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
Hepatobiliary:
Less Frequent: Hepatitis, jaundice, raised liver enzymes (mostly consistent with cholestasis)
Haematological:
Less Frequent: Purpura, thrombocytopenia, leucopenia
Genitourinary:
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 AMLATE overdosage. Gastric lavage may be of benefit. Gross overdosage could result in excessive peripheral vasodilation, resulting in marked and probably prolonged systemic hypotension.
Clinically significant hypotension due to AMLATE overdosage 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
AMLATE 5: White to off-white, round, biconvex, uncoated tablets with beveled edges, embossed “R”on one side and “177”on the other.
AMLATE 10: White to off-white, oval, flat, uncoated tablets with beveled edges, embossed “R” on one side and “178”on the other.

PRESENTATION
AMLAT 5: 30 tablets packed in aluminium foil blister packs
30 tablets packed in HDPE bottles with child resistant caps and inclusion of a silica gel container
AMLATE 10: 30 tablets packed in aluminium foil blister packs
30 tablets packed in HDPE bottles with child resistant caps and inclusion of a silica gel container

STORAGE INSTRUCTIONS
Store below 25°C. Protect from light. Keep the blisters in the outer carton until required for use.
KEEP OUT OF THE REACH OF CHILDREN

REGISTRATION NUMBER
AMLATE 5:        40/7.1/0312
AMLATE 10:        40/7.1/0313

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION
Dr. Reddy’s Laboratories (Pty) Ltd
3rd Floor TA Bank Building
160 Jan Smuts Avenue
Rosebank
2196

DATE OF PUBLICATION OF THE PACKAGE INSERT
September 2006

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


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