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Tramadol Metabolization

Tramadol is a centrally acting opioid analgesic, pure non-selective agonist of μ, delta and kappa opioid receptors, with higher affinity for μ receptor. It is widely used to treat moderate to intense pain.

CONTRAINDICATIONS

Tramadol is contraindicated in the following situations:

Hypersensitivity to tramadol; acute intoxication or overdose with CNS depressants (alcohol, hypnotics, other opioid analgesics); concomitance with MAOIs or patients who have been treated during the previous 2 weeks; concomitance with linezolid; severe hepatic or renal impairment; epilepsy not adequately controlled with treatment; severe respiratory failure; during lactation if a long-term treatment is necessary (more than 2 or 3 days); for the treatment of opioid withdrawal syndrome.

CAUTIONS

Precautions should be taken when prescribing tramadol in people older than 75 years old.

In patients with moderate renal and hepatic impairment tramadol should be given using prolonged dosing intervals.

Caution should be exercised in people dependent on opioids or with a tendency to abuse.

Caution should be exercised in patients who have suffered head trauma, shock, disturbance of knowledge of unknown origin.

Beware of prescribing codeine in patients with respiratory depression, intracranial hypertension, acute porphyria, alterations of the biliary tract, epileptics or patients tending to seizures.

Caution in patients treated with medications that lower the seizure threshold or metabolized by CYP3A4 or CYP2D6 or treated with CNS depressant medications.

Tramadol has a low dependency potential, but in the long term it can induce tolerance, dependence and withdrawal syndrome.

SIDE EFFECTS

Dizziness, headache, confusion, drowsiness, nausea, vomiting, constipation, dry mouth, sweating, fatigue.

PHARMACOLOGIC INTERACTIONS

The toxicity of tramadol can be enhanced by: central depressants, alcohol, ritonavir.

There is a risk of respiratory depression if it is taken in concomitance with: other morphine derivatives, benzodiazepines, barbiturates.

The effect of tramadol is diminished by: carbamazepine, buprenorphine, nalbuphine, pentazocine.

There is a risk of seizures in concomitance with: SSRIs, serotonin/norepinephrine reuptake inhibitors, tricyclic antidepressants, antipsychotics, and other medications that reduce the seizure threshold, such as bupropion, mirtazapine, tetrahydrocannabinol.

The requirements of tramadol are increased by ondasetron (postoperative pain).

BRAND NAMES

  • Adolonta ®
  • Dolpar ®
  • Gelotradol ®
  • Tioner ®
  • Tradonal ®
  • Zytram ®

Gene or region studied

  • CYP2D6
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