Trade Names: Ultram, Ultram ER, ConZip
Drug Class: Opioid analgesic
Preparations: 25-, 50 mg tablet immediate release; 100-, 200-, 300 mg tablet extended release
Dose: Adults: immediate release: 50–100 mg every 4–6 hours (not to exceed 400 mg/day); extended release: 100 mg daily and titrate allowing at least 5 days between dose changes to maximum of 300 mg daily
Indications: Pain not controlled by nonopioid analgesics
Mechanism of Action: Binds to opioid receptors; inhibits uptake of norepinephrine and serotonin
Contraindications: Hypersensitivity to tramadol or opioids, drug abuse, within 14 days of a MAOI, respiratory depression
Precautions: Seizure risk and risk of serotonin syndrome increased in patients also receiving tricyclic anti-depressants and structurally related drugs (cyclobenzaprine, promethazine), MAOIs, SSRIs. Renal and hepatic impairment decreases clearance of tramadol.
Monitoring: Use the lowest dose necessary to control pain. Escalate dose only with uncontrolled pain.
Pregnancy Risk: C
Common: Dizziness, flushing, nausea, constipation, headache, sleepiness, itch
Less common: Agitation, respiratory depression, seizures, dependence, addiction, withdrawal, increased hepatic enzymes, allergy, Stevens-Johnson syndrome
Antidepressants, MAOIs, opioids: Increased seizure risk
Quinidine and other CYP2D6 inhibitors and CYP3A4 inhibitors: Increased tramadol concentrations and side effects
Carbamazepine and CYP450 inducers: Decreased tramadol concentrations
CNS depressants: Increased risk of respiratory and CNS depression
MAOI, linezolid, triptans: Increased risk of serotonin syndrome
Patient Instructions: Drug is addictive and must only be used to control pain. Do not drink alcohol. It may cause drowsiness and impair ability to operate machinery. Increased risk of seizures.
Comments: Efficacy seems similar to that of other weak opioids.
Clinical Pharmacology: Bioavailability 70%; hepatic metabolism by CYP P2D6 to active M1 metabolite and by CYP3A4. Half-life is 6-8 hours.
Adapted from: RheumaKnowledgy