Land: Zuid-Afrika
Taal: Engels
Bron: South African Health Products Regulatory Authority (SAHPRA)
Dr-reddy
TRAMAZAC INJECTION SCHEDULING STATUS: S5 PROPRIETARY NAME (and dosage form): TRAMAZAC INJECTION COMPOSITION: Each 2 mL ampoule contains tramadol hydrochloride 100 mg. 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, delta and kappa opioid receptors with a higher affinity for the mu 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 Lees het volledige document