Product Name: Tramadol
Generic Name: Tramadol
Common Brands: Ultram
Pharmaceutical Categories: Pain Relief, Muscle Relaxants
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Here is an additional general information about this medication active ingredient tramadol:
Tramadol is an opioid analgesic, a derivative of cyclohexanol. It is non-selective agonist of mu-, delta- and kappa-receptors in the CNS. Tramadol is a racemate (+) and (-) of isomers (50% / 50%) which in various ways are involved in analgesic effects. The isomer (+) is a pure agonist opioid receptors, it has low tropism and has a pronounced selectivity for different subtypes of receptors. The isomer (-) inhibiting neuronal capture of noradrenaline activates the descending noradrenergic influence. Thats why it is broken transmission of pain impulses in the gelatinous substance of spinal cord.
Tramadol causes sedation. At therapeutic doses this medication almost not get respiratory depression. Tramadol has also an antitussive effect.
After oral administration Tramadol quickly and almost completely absorbed from the gastrointestinal tract (90%). Cmax in plasma obtained in 2 h after taking this medication. Bioavailability in single dose is 68% and increases with repeated use.
Plasma protein binding is 20%. Tramadol is widely distributed in tissues. Vd after oral administration and intravenous injection is 306 l and 203 l respectively. This drug crosses the placental barrier in a concentration equal to the concentration of the active substance in the plasma. 0.1% is excreted in breast milk.
Tramadol metabolised by demethylation and conjugation to 11 metabolites, of which only 1 is active.
This medicine excreted by the kidneys - 90% and through the intestines - 10%.
Why is Tramadol prescribed?
Moderate and severe pain of various origins (including malignant tumors, acute myocardial infarction, disease, trauma). Conducting painful diagnostic or therapeutic procedures.
Dosage and administration
A single oral dose for adults and children over 14 years is 50 mg, rectally - 100 mg, IV slowly or IM - 50-100 mg. If for parenteral injection efficiency is not enough, it is possible oral taking in a dose of 50 mg after 20-30 minutes.
For children aged 1 to 14 years set the dose rate of 1-2 mg / kg.
The duration of treatment is determined individually.
The maximum dose for adults and children over 14 years regardless of method of administration is 400 mg / day.
Tramadol side effects
CNS: dizziness, weakness, drowsiness, confusion, and in some cases - seizures and convulsions of cerebral origin (for IV uses in high doses or with concomitant administration of neuroleptics).
Cardio-vascular system: tachycardia, orthostatic hypotension, collapse.
Digestive system: dry mouth, nausea, vomiting.
Metabolism: increased sweating.
Musculoskeletal system: miosis.
acute intoxication with alcohol and drugs, providing a depressing effect on the CNS
children up to age 1 year
hypersensitivity to Tramadol
Using during pregnancy and breastfeeding
During pregnancy patients should avoid prolonged use of Tramadol because the risk of addiction in the fetus and the occurrence of withdrawal in the neonatal period.
If necessary using in lactation (breastfeeding) should be aware that tramadol in small amounts excreted in breast milk. In the case of long-term treatment can not been excluded the possibility of drug dependence.
Tramadol is not recommended for treatment of withdrawal syndrome drugs.
Patients need to avoid combination with MAO inhibitors.
During the period of treatment with Tramadol you should avoid to take alcohol.
Tramadol in the form of long-acting formulations should not be used in children under the age of 14 years.
During the period of tramadol using is not recommended to engage in activities that require special attention, speed of psychomotor reactions.
With caution Tramadol should be used in convulsions of central genesis of drug dependence, confusion, patients with impaired renal function and liver, as well as increased sensitivity to other opioid receptor agonists.
Tramadol should not be used beyond the period justified from a therapeutic point of view.
Tramadol drug interactions
Simultaneous administration of Tramadol with:
drugs providing a depressing effect on the CNS or with ethanol may increase the CNS depressant effects of tramadol;
MAO inhibitors are likely development of serotonin syndrome;
serotonin reuptake inhibitors, tricyclic antidepressants, antipsychotics, other means of reducing the threshold of convulsive readiness, increases the risk of seizures;
warfarin and phenprocoumon increase anticoagulant effect;
carbamazepine reduced the concentration of tramadol in plasma and its analgesic effect;
paroxetine describes cases of serotonin syndrome, seizures;
sertraline, fluoxetine describes cases of serotonin syndrome;
opioid analgesics is likely to reduce the analgesic action. Prolonged use of opioid analgesics or barbiturates stimulates the development of cross-tolerance;
naloxone activates respiration, eliminating analgesia after opioid analgesics.
Tramadol in case of emergency / overdose
Symptoms: respiratory depression, until apnea, seizures, Pupillary, anuria, coma.
Treatment: IV injection of naloxone (a specific antagonist), gastric lavage, maintenance of vital functions.