Tramadol is a synthetic opioid analgesic that is centrally acting. Tramadol is a serotonin/norepinephrine reuptake inhibitor (SNRI). It is structurally related to morphine and codeine. Tramadol is a lower-risk opioid analgesic for the treatment of moderate to severe pain.
| Parameters | Description |
|---|---|
| Category of Drug | Tramadol is an Opioid Analgesics |
| Mechanism of Action | Tramadol is a selective agonist of mu receptors (1). It preferentially inhibits serotonin reuptake, whereas tramadol mainly inhibits noradrenaline reuptake. The action of these two enantiomers is both complementary and synergistic and results in the analgesic effect. |
| Indications | Tramadol is used for 1. Moderate or severe pain 2. Postoperative pain, 3. In patients contraindicated to NSAIDs. |
| Well Known Pharmaceutical Brands | 1. CONTRAMAL- ABBOTT 2. TRD-CONTIN- MODI MUNDI PHARMA 3. TRAMAZAC- ZYDUS CADILA 4. TRAMASURE- MANKIND 5. DOMADOL- TORRENT  |
| Available dosage forms | 1. TABLETS 2. CAPSULES 3. INJECTION |
| Dose | Adult- Moderate to severe pain: 50 to 100 mg, 4 to 6 hourly (max 400 mg/day) |
| Structure |  |
| Molecular details | Molecular Formula- C16H25NO2 Molecular Weight- 263.37 g/mol |
| IUPAC Name | (1R,2R)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexan-1-ol |
| Pharmacokinetic properties | 1. oral dose of 100mg produces Cmax- 300μg/L with a Tmax-1.6-1.9 hours 2. Vd- 2.6-2.9 L/kg 3. Protein binding-About 20% 4. Approximately 30%- excreted in the urine as unchanged drug, 5. 60% -excreted as metabolites 6. half-life- 5-6 hours |
| Contraindications | 1. Patients with suicidal tendency 2. Raised intracranial pressure 3. Severe renal impairment 4. Acute alcoholism 5. Lactation. |
| Precautions | 1. Renal or hepatic impairment 2. History of epilepsy 3. Inflammatory or obstructive bowel disease 4. Myasthenia gravis 5. Hypothyroidism 6. Adreno-cortical insufficiency 7. Respiratory depression 8. Prostatic hyperplasia 9. pregnancy |
| Adverse Effects | Same as other opioids, however, it has less addictive potential. |
| Pregnancy Category | C |
Refer
Pingback: NSAIDs: Pain Relief, Classification, Uses - PharmaCampus
This is a very interesting article. Please, share more like this!