Tramadol: Pharmacology
tramadol: Pharmacology
Metabolism: liver extensively; CYP450: 2B6, 2D6, 3A4 substrate; Info: active metabolite
Excretion: urine (30% unchanged); Half-life: 6.3h (tramadol), 7.4h (metabolite)
Class: Other Analgesics
Mechanism Of Action
exact mechanism of action unknown; binds to mu opioid receptors and weakly inhibits norepinephrine/serotonin reuptake, producing analgesia (central opioid agonist)
tramadol: Safety Monitoring
Pregnancy: C
Lactation: Possibly Unsafe
Monitoring Parameters: Cr at baseline
Avoid Abrupt Cessation: taper dose gradually to D/C (abrupt cessation of tramadol may cause a withdrawal syndrome including anxiety, panic attacks, insomnia, paresthesias, sweating, piloerection, rigors, tremors, pain, nausea, diarrhea, upper respiratory symptoms, and rarely hallucinations)
tramadol: Adverse Reactions
Serious Reactions
- seizures
- respiratory depression
- anaphylaxis
- angioedema
- bronchospasm
- Stevens-Johnson syndrome
- toxic epidermal necrolysis
- hypotension, orthostatic
- serotonin syndrome
- withdrawal if abrupt D/C
- dependency, abuse
Common Reactions
- dizziness
- nausea
- constipation
- headache
- somnolence
- vomiting
- pruritus
- CNS stimulation
- asthenia
- sweating
- dyspepsia
- dry mouth
- diarrhea
tramadol: Contraindications/Cautions
- hypersens. to drug/class/compon.
- opioid anaphylaxis hx
- acute alcohol/drug intoxication
- caution if substance abuse hx
- caution if CNS depressant use
- caution if resp. depressant use
- caution if respiratory depression
- avoid abrupt withdrawal
- caution if seizure hx or risk
- caution if seizure threshold lowered
- caution if alcohol/drug withdrawal
- caution if head injury
- caution if CNS infection/lesion
- caution if incr. ICP
- caution if acute abdomen
- caution if impaired liver fxn
- caution if impaired renal fxn
- caution in elderly pts
- caution in pregnancy
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