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TRAMASPEN™
SCHEDULING STATUS:
S5
PROPRIETARY NAME
(and dosage form):
TRAMASPEN™
100 mg/2 mL (injection)
COMPOSITION:
Each 2 mL ampoule contains: 100 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 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.
Tramado
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