Tramadol – 37.5 mg
Paracetamol – 325 mg
Each box contain 10 Blister strips of 10 tablets
Tramadol is centrally acting analgesic. The chemical name for tramadol is (±) cis-2-[(dimethylamino) methyl]-1-(3methoxyphenyl) cyclohexanol hydrochloride. Tramadol is white in color with crystalline powder. The drug is soluble in water and ethanol. It acts in brain through which it causes relieve in pain.
It is also known as acetaminophen and is widely used as over the counter analgesic and anti-pyretic. It is a mild analgesic which causes relief in mild headaches and other aches and pains. In combination with other drugs like opioid analgesic, paracetamol is used in the management of post surgical pain and severe pain.
- Moderate to severe pain
- Post operative pain
- Pain occurring in fibroyalgia
- Potent analgesic
- Acute pain
Mechanism of action
It involves inhibition of reuptake of norepinephrine and serotonin. It acts as µ-opioid receptor agonist which enhances the serotonin release. Tramadol produces inhibitory action on 5-HT2c receptor. This blockage of 5-HT2c receptor causes lowering of seizer’s threshold. The active metabolite present in tramadol is O-desmethyltramadol, which is a high affinity ligand of the δ- and κ-opioid receptors.
It inhibits the synthesis of prostaglandin synthesis by competing with arachidonic acid for the active site of COX.
The mean absolute bioavailability of tramadol is about 75%. This concentration reaches in 2-3hrs. Both the enantiomers of tramadol produce dose dependent response. High plasma concentration achieves in two days. Co-administration of food with drug does not affect the rate of absorption.
The volume of distribution of tramadol was 2.6 L/Kg in men and 2.9 L/Kg. 205 of tramadol binds to plasma protein. Saturation of the drug occurs when the administration of the drug is more than the safe dose. The drug is metabolized by enzymes CYP2D6 and CYP3A4 present in liver.
Tramadol metabolites are eliminated through kidneys. The plasma half life of the drug is 6.3±1.4 hrs. On multiple use of the drug the plasma half life of tramadol increases.
It has rapid and complete absorption
The protein binding of the drug is about 25%, it undergoes glucuronidation in liver.
About 80% of acetaminophen is excreted in the urine after conjugation and about 3% of the drug is excreted unchanged.
- Patients with hypersensitivity to tramadol
- Any allergy with opioids
- Contraindicated in acute intoxication with alcohol, hypnotics, narcotics, centrally acting analgesics.
- CNS and respiratory depression in patients.
- Hepatic and renal impairment
- Complicated acute abdominal conditions
- Renal disease
- Hepatic disease
- Prolong half life can cause difficulty in achieving steady state of drug in body.
- Prolong use is makes it carcinogen.