TRAMINO tablets combine two analgesics, Tramadol 37.5 mg and acetaminophen 325 mg. Tramadol is an opioid analgesics where as acetaminophen is a non-opioid analgesic and antipyretic. This combination medication is used to manage moderate to moderately severe pain in adults. It decreases pain by working on the central nervous system. Acetaminophen is a less potent pain reliever that increases the effects of Tramadol. When used together, the combination provides better pain relief than either medicine used alone.

Pharmacodynamic

Tramadol is a centrally acting synthetic opioid analgesic showing dual mode of action which possesses both opioid agonist activity and activates the spinal pain inhibitory system. Tramadol is µ opioid agonist. Tramadol alleviates the pain by binding with the µ receptor resulting a complex series of neuronal interactions and finally raising the threshold of the pain. The parent compound tramadol and its active metabolite O-desmethyl tramadol (ODT) both exhibits analgesic effect. The active metabolite ODT exhibits 300 fold greater affinity to µ receptor than parent compound.

Tramadol also possess spinal pain inhibitory system. It exerts the analgesic activity via pain descending inhibitory system, which involved the nor-epinephrine and serotonin. Activation of the inhibitory neurons relates to release of nor-epinephrine and serotonin, thus increasing the concentration of these neurotransmitters in the synaptic cleft due to which the transmission of the pain message is stopped.

Paracetamol blocks the cyclo-oxygenase in the brain and hence blocks the formation and release of prostaglandins (PG) in the central nervous system. It further inhibits the action of endogenous pyrogens on the heat regulating centers in the brain and hence shows antipyretic action.

Pharmacokinetics

Absorption: Tramadol is rapidly and almost completely absorbed after oral administration. After repeated administration, the bioavailability is increased and reaches approximately 90%. The oral absorption of paracetamol is rapid and nearly complete and takes place mainly in the small intestine. Peak plasma concentration of paracetamol is reached in one hour and is not modified by concomitant administration of Tramadol.

When administered with food, the peak plasma concentrations, and the extents of absorption, of tramadol and acetaminophen are not affected. So TRAMINO can be taken independent of meal time.

Distribution: Tramadol has a high tissue affinity. The binding of tramadol to human plasma proteins is approximately 20%. Acetaminophen appears to be widely distributed throughout most body tissues except fat. A relative small portion (~20%) of acetaminophen is bound to plasma protein.

Metabolism: Following oral administration, tramadol is extensively metabolized. Approximately 30% of the dose is excreted in the urine as unchanged drug, whereas 60% of the dose is excreted as metabolites. Acetaminophen is primarily metabolized in the liver through glucuronidation and sulfation.

Elimination: Tramadol and the metabolites are eliminated primarily by the kidneys. The half-life of acetaminophen is about 2 to 3 hours in adults. It is somewhat shorter in children and somewhat longer in neonates and in cirrhotic patients. Less than 9% of acetaminophen is excreted unchanged in the urine.

Indication

For symptomatic treatment of moderate to severe pain

• Cancer pain
• Dental pain
• Post operative pain
• Orthopedic pain
• Neuralgia

Dosage

An initial dose of 1-2 tablets of TRAMINO is recommended. Additional doses can be taken as needed, not exceeding 8 tablets per day. The dosing interval should not be less than six hours. TRAMINO should not be administered for longer that needed.

Contraindications

• Hypersensitivity to Tramadol, Acetaminophen, other opioid analgesic
• Patient intoxicated with alcohol
• In patients with liver disease

Special precautions

Use in caution with medications such as tranquilizers, hypnotics, serotonergic drugs such as SSRIs, MAOIs, triptans, linezolid, lithium, Carbamazepine.

Alcohol should be avoided while taking Tramino.

Should be advised for caution while driving or operating machinery.

Pregnancy Category

Category C

Adverse effects

Abdominal pain, constipation, diarrhea, dry mouth, nausea, vomiting, dizziness, somnolence, anorexia, insomnia, increased sweating has been reported.