Tramadol Hydrochloride (6263-c)
Tramadol Hydrochloride (BANM, USAN, rlNNAM).
CG-315; U-26225A. (±)-trans-2-Dimethylaminomethly -I-(3-methoxyphenyl) cyclohexanol hydrochloride.
C6H25NO2, HCL = 299.8.
CAS–27203-92-5 (Tramadol); 22204-88-2 (Tramadol hydrochloride); 36282-47-0 (Tramadol hydrochloride).
Incompatibilities.
An injection of Tramadol hydrochloride 50 mg per mL is reported to be incompatible with injection of diazepam, diclofenac sodium, indomethacin, midazolam, and piroxicam if mixed in the same syringe.
Uses and Administration
Tramadol Hydrochloride is an opioid analgesic (p.68). It also has noradrenergic and serotonergic properties that may contribute to its analgesic activity. Tramadol is used for moderate to sever pain.
Tramadol Hydrochloride is given by mouth, intravenously, or rectally as a suppository. The intramuscular route has also been used. It may also be given by infusion or as part of a patient controlled analgesia system. Usual doses by mouth are 50 to 100 mg every 4 to 6 hours. Tramadol hydrochloride may also be given orally as a modified-release preparation once or twice daily. The total daily dosage by mouth should not exceed 400 mg.
A dose of 50 to 100 mg may be given every 4 to 6 hours by intravenous injection over 2 to 3 minute, or by intravenous infusion. For the treatment of postoperative pain, the initial dose is 100 mg followed by 50 mg every 10 to 20 minutes if necessary to a total maximum (including the initial dose) of 250 mg in the first hour. Thereafter doses are 50 to100 mg every 4 to 6 hours up to a total daily dose of 600 mg.
Rectal dose by suppository are 100 mg up to 4 times daily. The dosage interval should be increased to 12 hours in patients with a creatinine clearance less then 30 mL per minute; in the USA the manufactures suggest that the maximum dose by mouth should not be exceed 200 mg daily in these patients.Tramadol should not be given to patients with more sever renal impairment (creative clearance less than 10 mL per minute).A dosage interval of 12 hours is also recommended in sever hepatic impairment.
Pharmacokinetics
Tramadol is readily absorbed following oral administration but is subject to first –pass metabolism. Tramadol is metabolized by N-and O-demethylation and glucuronidation sulfation in the liver. The metabolite O-desmethyltramadol is pharmacologically active.Tramadol excreted mainly in the urine predominantly as metabolites. Tramadol is widely distributed, crosses the placenta , and appears in small amount in breast milk. The elimination half-life following oral administration is about 6 hours.
Adverse effect and treatment
As for Opioid Analgesics in general, p.67.
Tramadol may produce fewer typical opioid adverse affects such as respectively depression and constipation.
In addition to hypotension hypertension has occasionally occurred. Anaphylaxis hallucination, and confusion heave also been reported.
Respiratory depression has been reported after Tramadol infusion anesthesia, although in a postoperative study Tramadol had no significant respiratory depressant effect when equianalgesic dose of morphine, pentazocine, pethidine, piritramide , and Tramadol were compared.
Precautions
As for opioid Analgesics in general,
Tramodol should be used with caution in patients with renal or liver impairment and should avoid if renal impairment is sever. Removed by haemodialysis is reported to be very slow. Tramadol should be used with care in patient with a history of epilepsy or those susceptible to seizures. See also effects on the CNS under Adverse Effect above.
Interactions
For interaction associated with opioid analgesics, see p.68.Carbamazepine is reported to diminish the analgesic activity of Tramadol by reducing serum concentrations.
The risk of seizures is increased if Tramadol is administered concomitantly with other drugs that heave the potential to lower the seizure threshold. See also under Effects on the CNS under Adverse Effects, above
Tramodal inhibits reuptake of noradrenaline and serotonin enhance serotonin release and there is the possibility that it may interact with other drugs that enhance monoaminergic neurotransmission including lithium , tricycles antidepressants, and selective serotonin reuptake inhibitors; it should not given to patients receiving MAOIs or within14 days of their discontinuation.
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