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

Logo TRAMAZAC CAPSULES

SCHEDULING STATUS:
S5

PROPRIETARY NAME
(and dosage form):

TRAMAZAC CAPSULES

COMPOSITION:
Each capsule contains 50 mg
tramadol hydrochloride.

PHARMACOLOGICAL CLASSIFICATION:
A.2.9. Other analgesics

PHARMACOLOGICAL ACTION:
Tramadol hydrochloride is a centrally-acting synthetic opioid analgesic binding to specific opioid receptors. It is a non-selective, pure agonist at mu (µ), delta (
d) and kappa (K) opioid receptors with a higher affinity for the µ receptor. Other mechanisms, which may contribute to its analgesic effect, are inhibition of neuronal re-uptake of noradrenaline and enhancement of serotonin release.
Tramadol hydrochloride does not promote histamine release.
Pharmacokinetics:
Tramadol hydrochloride is readily absorbed following oral administration. Oral bioavailability is approximately 68% after a single dose and increases to 90% at steady state. Onset of action is dose dependent but generally occurs within one hour of dosing, peaking within 2 to 3 hours. Duration of analgesia is about 6 hours. The rate or extent of absorption is not significantly affected by co-administration with food.
The bioavailability of tramadol hydrochloride after intramuscular injection or intravenous administration is the same; the mean peak serum concentration is achieved after 45 minutes. Tramadol hydrochloride is primarily metabolised in the liver (90%) with one of its metabolites, mono-O-desmethyltramadol (M1), being 2 to 4 times as potent as the parent compound.
Tramadol hydrochloride has a linear pharmacokinetic profile within the therapeutic dosage range.
Tramadol hydrochloride and its metabolites are excreted mainly in the urine. The elimination half-life is 5 to 7 hours, but is prolonged in impaired hepatic and renal function.
Tramadol hydrochloride crosses the blood-brain and placental barrier. Small amounts are excreted in breast milk unchanged or as the metabolite M1.

INDICATIONS:
TRAMAZAC CAPSULES
is indicated for the management of moderate to moderately severe pain.

CONTRA-INDICATIONS:
Hypersensitivity to tramadol hydrochloride or opioids.
Acute intoxication with alcohol, hypnotics, analgesic opioids or psychotropic medicines (due to the risk of respiratory depression).
Patients taking monoamine oxidase (MAO) inhibitors or within two weeks of their discontinuation (see INTERACTIONS)
Narcotic withdrawal treatment.
Respiratory depression especially in the presence of cyanosis and excessive bronchial secretions.
Increased intracranial pressure or central nervous depression due to head injury or cerebral disease.
Pregnancy and lactation.

WARNINGS:
Avoid the use of TRAMAZAC CAPSULES in patients with a history of addiction, as physical dependence of the morphine-type may develop. Reinstatement of physical dependence in patients that have previously been dependent may occur with TRAMAZAC CAPSULES.
Use with caution in patients with a history of epilepsy or those susceptible to seizures (e.g. patients taking neuroleptics and other drugs that reduce the seizure threshold).
Use with caution in patients with renal or hepatic impairment and avoid if severe.

INTERACTIONS:
Monoamine oxidase inhibitors (MAOIs):
Because of its inhibitory effect on serotonin uptake, TRAMAZAC CAPSULES should not be used concomitantly with MAOIs or within 14 days after discontinuing such treatment (see CONTRA-INDICATIONS).
Central nervous system (CNS) depression-producing medications, including alcohol and anaesthetics: Caution is recommended because concurrent use may potentiate the CNS depressant effects. The duration of anaesthesia may be prolonged when TRAMAZAC CAPSULES is combined with barbiturates.
Carbamazepine: Serum concentrations of TRAMAZAC CAPSULES are reduced by carbamazepine, resulting in diminished analgesic activity of TRAMAZAC CAPSULES. Inhibitors of CYP3A4 such as ketoconazole and erythromycin may inhibit the metabolism of TRAMAZAC CAPSULES.

PREGNANCY AND LACTATION:
Safety in pregnancy and lactation has not been established (see CONTRA-INDICATIONS)

DOSAGE AND DIRECTIONS FOR USE:
The dosage should be adjusted to the intensity of pain and the individual’s response to the analgesic action of TRAMAZAC CAPSULES. TRAMAZAC CAPSULES should not be used for the treatment of minor pain.
Adults and children over the age of 14 years:
Oral administration:
Initial dose of 50 mg, followed by 100 mg twice daily.
The dose may be increased to 150 mg or 200 mg twice daily.
A total daily dose of more than 400 mg per day must not be exceeded.
Elderly:
The usual doses may be used except in patients 75 years of age and over. A downward adjustment of the dose and/or prolongation of the interval between doses are recommended.
Renal impairment:
The elimination of TRAMAZAC CAPSULES may be prolonged. The usual initial dose should be used, but for patients with creatinine clearance <30 mL/min, the dosage interval should be increased to 12 hours.
Hepatic impairment:
The elimination of TRAMAZAC CAPSULES may be prolonged. The usual initial dose should be used but in severe hepatic impairment, the dosage interval should be increased to 12 hours.

SIDE EFFECTS AND SPECIAL PRECAUTIONS:
Side effects:
Cardiac disorders:
Less frequent: Syncope, bradycardia, tachycardia, cardiovascular collapse.
Vascular disorders:
Less frequent: Flushing, postural hypotension, angioedema.
Nervous system disorders:
Frequent: Fatigue, sedation, drowsiness, dizziness, headache.
Less frequent: Parasthesia, amnesia, confusion, hallucinations, seizures (see WARNINGS), syncope.
Gastrointestinal disorders:
Frequent: Nausea, vomiting, dry mouth, dyspepsia, constipation, diarrhoea, anorexia, abdominal pain.
Renal and urinary disorders:
Less frequent: Urinary retention, urinary frequency.
Hepato-biliary disorders:
Less frequent: Increase in liver enzymes.
Eye disorders:
Less frequent: Blurred vision.
Skin disorders:
Frequent: Sweating (especially when IV administration is too rapid), skin rashes, pruritus.
Less frequent: Vesicles, urticaria, toxic epidermal necrolysis and Stevens-Johnson syndrome have been reported.
Respiratory disorders:
Less frequent: Bronchospasm.
Immune system disorders:
Less frequent: Anaphylaxis, and anaphylactoid reactions. These reactions may occur after the first dose.

Special precautions:
The administration of TRAMAZAC CAPSULES concurrently with other central nervous system medicines is likely to intensify and prolong CNS effects (see INTERACTIONS). Patients should be warned not to operate machinery or drive a car while using TRAMAZAC CAPSULES.
The possibility of respiratory depression cannot be excluded if the recommended dose is exceeded or other centrally depressant medicines are given concomitantly.
TRAMAZAC CAPSULES should not be used for the treatment of minor pain.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Symptoms of overdose:
(See SIDE EFFECTS AND SPECIAL PRECAUTIONS)
Symptoms of overdosage are typical of opioids, and include pinpoint pupils, slow heartbeat, slow or troubled breathing, weakness, seizures, cold, clammy skin.
Treatment of overdose:
Supportive measures such as maintaining the patency of the airway and maintaining cardiovascular function should be instituted. Treatment of restlessness is symptomatic and supportive.
Naloxone should be used to reverse some, but not all, symptoms caused by overdosage with TRAMAZAC CAPSULES. Administration of naloxone should be done with caution because it may precipitate seizures.
Diazepam has been found to be effective in treating convulsions caused by TRAMAZAC CAPSULES toxicity.
Haemodialysis is not recommended in overdose, since it removes less than 7% of the administered dose of TRAMAZAC CAPSULES in a 4-hour dialysis period.

IDENTIFICATION:
Size ‘2’locked hard gelatin capsule with a green cap and green body, containing white off-white powder.

PRESENTATION:
Clear PVC and printed Aluminium foil blister strips containing 10 or 20 capsules packed in an outer carton containing 20, 100 or 140 capsules.

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

REGISTRATION NUMBER:
A39/2.9/0415

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION:
Zydus Healthcare S.A. (Pty) Ltd.
Adrina Building
32-34 Klinkenberg Street
Potchefstroom
2351

DATE OF PUBLICATION OF THE PACKAGE INSERT:
26 October 2005

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

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