Tramadol
Ultram | ConZip
Overview
Tramadol is a centrally acting opioid analgesic with additional serotonin and norepinephrine reuptake inhibition, used for moderate to moderately severe pain.
Indications
- Moderate to moderately severe pain
Contraindications
- Significant respiratory depression
- Acute intoxication with alcohol or CNS depressants
- Children under 12 years
- Concurrent or recent use of monoamine oxidase inhibitors
Classification
Mechanism of Action
Binds weakly to mu-opioid receptors and inhibits reuptake of serotonin and norepinephrine. Its active metabolite O-desmethyltramadol has substantially greater mu-opioid affinity.
Pharmacodynamics
Provides analgesia through combined opioid and monoaminergic mechanisms. Its analgesic efficacy depends in part on CYP2D6-mediated conversion to the active metabolite.
Pharmacokinetics
- Absorption
- Well absorbed orally with high bioavailability.
- Distribution
- Widely distributed with moderate protein binding.
- Metabolism
- Metabolized in the liver by CYP2D6 and CYP3A4 to active and inactive metabolites.
- Excretion
- Excreted mainly in urine as metabolites.
- Half-life
- Approximately 6-7 hours
- Bioavailability
- Approximately 70% (rising with repeated dosing)
- Protein Binding
- Approximately 20%
Dosage
Typical dosage: 50-100 mg every 4-6 hours as needed; maximum 400 mg per day
Available Forms
- Tablet
- Extended-release tablet
- Capsule
Side Effects
Common
- Nausea
- Dizziness
- Constipation
- Headache
- Somnolence
Serious
- Respiratory depression
- Seizures
- Serotonin syndrome
Rare
- Anaphylaxis
Drug Interactions
Combined serotonergic activity increases the risk of serotonin syndrome.
Induces tramadol metabolism, reducing analgesic effect and increasing seizure potential.
Warnings
Tramadol carries risks of addiction, abuse, and misuse; life-threatening respiratory depression; and neonatal opioid withdrawal syndrome with prolonged use in pregnancy. Ultra-rapid CYP2D6 metabolizers and children are at particular risk of respiratory depression. Concomitant use with benzodiazepines or other CNS depressants can be fatal.
Pregnancy
Category C
Toxicity
Overdose can cause CNS and respiratory depression, seizures, and serotonin syndrome.
Overdose
Support ventilation; naloxone can reverse respiratory depression but may increase seizure risk. Manage seizures with benzodiazepines.
References
Looking for patient-friendly information? Visit RemedyDoor for easy-to-read guides about this medication.