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Tramadol is an opioid agonist, which is used to treat moderate to severe chronic pain. It works in the central nervous system to alleviate pain. It was first authorized by the US FDA in March 1995. It was previously classified as a non-controlled substance, but in 204 it was reclassified to Schedule IV of controlled substances, with prescribing limitations. It is also used to relieve pain following surgery.
BRAND NAMES:
Conzip – It is available in the form of extended-release oral capsules that contain tramadol hydrochloride as the active ingredient present with strengths of 100, 200, and 300 mg.
Ultram – Ultram is available with the composition of two drugs tramadol 37.5 mg and paracetamol 325 mg for oral consumption.
MECHANISM OF ACTION:
Tramadol's mode of action involves selectively binding to specific opiate receptors in the central nervous system due to its opioid properties. The liver enzyme CYP2D6 converts tramadol to its active metabolite, M1, which has a higher affinity for the mu receptor than the inactive form. The M1 metabolite has analgesic effectiveness up to six times stronger than tramadol. It doesn't bind to the mu receptor.
PHARMACOKINETICS:
Absorption: The absolute bioavailability of oral doses is approximately 75%. The maximum peak concentration of tramadol is observed at 2 to 3 hours.
Distribution: The volume of distribution of tramadol in males is 2.6 L/kg and 2.9 L/kg in females.
Metabolism: It is metabolized by CYP2D6 and CYP3A4 enzymes and through conjugation. The primary metabolic involves N- and O-demethylation and glucuronidation or sulfation reactions in the liver.
Excretion: About 30% of the tramadol administered is excreted through urine and 60% is eliminated as metabolites.
PHARMACODYNAMICS:
Tramadol regulates the descending pathways in the central nervous system by binding parent and M1 metabolites to opioid receptors and weakly inhibiting norepinephrine and serotonin reuptake.
DOSAGE AND ADMINISTRATION:
Tramadol is available in extended-release tablets, immediate-release tablets, and solutions. It is available in various dosage forms 100, 200, and 300mg for extended-release tablets., 50 mg for immediate release tablet, and 5 mg/ml of tramadol solution.
• In acute pain treatment the recommended dose is Immediate release tramadol capsules of 50 mg and 100 mg every 4 to 6 hours. The maximum dosage of tramadol recommended per day is 400mg.
• In treating chronic noncancer pain, the recommended dose is tramadol extended-release tablets 100mg once a day. The dose can be titrated up to 150, 200, and 300mg every 5 days.
• In a recent meta-analysis it was revealed that tramadol can be taken 25 to 50 mg before intercourse, and is effective for premature ejaculation.
CONTRAINDICATIONS:
It is contraindicated in patients with hypersensitivity.
DRUG INTERACTIONS:
Tramadol can interact with other drugs, decrease its efficacy, and also cause some severe side effects. Below are the medicines mentioned in which tramadol interacts with
• Antibiotics – Ciprofloxacin, erythromycin
• Antidepressants – Fluoxetine, doxepin
• Blood thinners – Warfarin
• Anti-anxiety drugs – Alprazolam
• Antifungal drugs – Ketoconazole
• Pain killers- pentazocine, buprenorphine, nalbuphine
• Nausea drug – Ondansetron
• Fits drugs – Carbamazepine
• Immuno suppressants – Fingolimod
• Antipsychotics – Droperidol
• HIV/AIDS drugs – Saquinavir.
• Anti cancer drugs – Ceritinib, lapatinib
FOOD INTERACTIONS:
Avoid grapefruits and grape juices.
ADVERSE EFFECTS:
• Breathing problems
• Difficulty in swallowing
• Hives
• Headache
• Dry mouth
• Constipation
• Swollen lymph nodes
• Dizziness
• Stomach cramps
• Flu symptoms
OVERDOSE:
Taking an overdose can cause some toxic effects.
• Altered mental status
• Multiorgan dysfunction
• Cardiopulmonary arrest
• Respiratory depression.
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