Tramadol+Paracetamol
( 37.5mg/325mg Tablet)
Availability
100’s
Therapeutic Class
Analgesics (Opioid) / Supportive Care Therapy
Mode of Actions
Description: Tramadol is a centrally acting opioid analgesic, which binds to mu-opioid receptors and weakly inhibits the reuptake of norepinephrine and serotonin. Paracetamol, a para-aminophenol derivative, has analgesic, antipyretic and weak anti-inflammatory activity. Together, tramadol and paracetamol has faster onset of action compared to tramadol alone and longer duration of action compared to paracetamol alone.
Duration: 5 hr.
Pharmacokinetics:
Absorption: Readily absorbed from GI tract. Tramadol: Bioavailability: Approx 70-75% (oral); 100% (IM). Paracetamol: Time to peak plasma concentration: 10-60 min.
Distribution: Widely distributed, crosses the placenta and distributesd into the breast milk. Plasma protein binding: Approx 20% (tramadol); negligible (paracetamol).
Metabolism: Tramadol: Undergoes N- and O-demethylation by CYP3A4 and CYP2D6 isoenzymes and by glucuronidation and sulfation. Paracetamol: Hepatic via glucuronic and sulfuric acid conjugation.
Excretion: Tramadol: Via urine as metabolites. Elimination half-life: Approx 6 hr.
Paracetamol: Via urine as glucuronide and sulfate conjugates; <5% as unchanged drug Elimination half-life: Approx 1-3 hr.
Indication
For management of moderate to severe pain.
Dosage
Adult & childn >16 yr 1-2 tab 4-6 hrly. Max: 8 tab/day.
Contradiction
Acute intoxication w/ alcohol, hypnotics, narcotics, centrally acting analgesic, opioids or psychotropic.
Special Precaution
Contains tartrazine that may cause allergic reactions.
Drug Interaction
Increased risk of seizures and serotonin syndrome w/ SSRIs, SNRIs, TCAs, and 5-HT agonists (e.g. sumatriptan). Increased CNS depression w/ barbiturates, benzodiazepines, other anxiolytics, hypnotics, sedative antidepressants, sedative antihistamines, neuroleptics, centrally acting antihypertensive drugs, thalidomide and baclofen. Decreased analgesic efficacy w/ ondansetron.
Increased INR w/ warfarin.
Potentially Fatal: May enhance serotonergic, neuro excitatory and/or seizure-potentiating effect of MAOIs.
