Tramadol. Dosage, Side Effects, Interactions
Tramadol is approved for the treatment of moderate to severe pain. The active ingredient should never be used longer than absolutely necessary to treat pain.
Tramadol is available on US market as film-coated tablets, hard capsules, prolonged-release tablets, prolonged-release capsules, oral solution, solution for injection, effervescent tablet, suppository, oral drops and ampoules. The active ingredient can be administered orally, intravenously, intramuscularly or subcutaneously.
How Tramadol works
Tramadol is a centrally acting opioid analgesic . The active substance binds to μ, δ and κ opioid receptors. Furthermore, the active ingredient inhibits the reuptake of serotonin and norepinephrine. Tramadol has analgesic and antitussive effects, but has no respiratory depressant effect over a wide dose range and does not affect gastrointestinal motility.
More than 90 percent of tramadol is absorbed after oral administration and has an absolute bioavailability of around 70 percent, regardless of food intake. The drug undergoes little first-pass metabolism and is about 20 percent bound to serum proteins. Tramadol crosses the blood-brain barrier and the placenta and is also excreted in breast milk. The elimination half-life is about 6 hours, regardless of the application.
The metabolism of tramadol proceeds via N- and O-demethylation and via conjugation of the O-demethylation products with glucuronic acid. The O-demethyltramadol is a pharmacologically active metabolite, which exceeds the potency of the parent substance by a factor of 2-4.
Inhibition of CYP3A4 and/or CYP2D6 may affect plasma concentrations of tramadol and its active metabolite.
Tramadol is primarily eliminated via the kidneys, so a slight prolongation of the half-life must be expected in the case of disorders of the liver and kidney function.
Dosage of Tramadol
Drugs containing the active ingredient tramadol require a prescription. The dosage of tramadol depends on the severity of the pain and the individual sensitivity of the patient.
For adults and adolescents over 12 years of age, the usual single dose is 50 – 100 mg 3 to 4 times a day, every 4 – 6 hours (except for slow-release preparations!).
Side effects of Tramadol
The most commonly reported side effects (≥10 percent of patients) are nausea and dizziness.
Common (≥1/100 to <1/10) the following side effects may also occur:
- Dry mouth
There are the following interactions when taking tramadol:
- Tramadol must not be used concomitantly with MAO inhibitors
- Simultaneous use of centrally depressant substances
- Simultaneous administration of carbamazepine (enzyme inducer) -> reduction in the serum concentration of tramadol
- Combination of mixed agonists/antagonists (e.g. buprenorphine , nalbuphine , pentazocine ) -> analgesic effect of a pure agonist can be weakened
- Coumarin derivatives (e.g. warfarin ) -> increased INR values and ecchymosis possible
- Serotonin reuptake inhibitors (SSRIs) , serotonin norepinephrine reuptake inhibitors (SNRIs) , tricyclic antidepressants , neuroleptics and other drugs that lower the seizure threshold (such as bupropion , mirtazapine and tetrahydrocannabinol) -> seizures can be triggered
- Serotonin drugs, MAO inhibitors, tricyclic antidepressants, mirtazapine -> risk of serotonin syndrome
- CYP3A4 inhibitors (e.g. ketoconazole , erythromycin ) -> Tramadol metabolism can be inhibited -> However, the clinical significance of this interaction is unknown
- 5-HT3 antagonists ( Ondansetron ) -> increased tramadol requirements in postoperative pain in clinical studies
- Sedatives-> Risk of sedation, respiratory depression, coma and death due to an additive CNS depressant effect is increased
- Known hypersensitivity to tramadol
- Acute intoxication with alcohol, sleeping pills, analgesics , opioids and psychotropic drugs
- Concurrent or up to 14 days in the past use of MAO inhibitors
- Drug substitution
If tramadol needs to be used during pregnancy, it should be limited to single doses. Chronic use should be avoided as tramadol crosses the placenta and withdrawal symptoms in the newborn are possible after birth.
Tramadol should not be used while breastfeeding. However, it is generally not necessary to discontinue breast-feeding after a single dose of tramadol. However, a short-term treatment with paracetamol and/or ibuprofen should be tried first.
Since use of tramadol can cause drowsiness and dizziness, the ability to drive and use machines is impaired under these circumstances. In this case, patients should not drive or use machines.
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