Tramadol - instructions for use, dose, side effects, contraindications

Complementary binding with opioid μ receptors (weak agonist) and inhibition of reuptake of norepinephrine and serotonin. A mixture of (+) and (-) - enantiomers causes antinociception. (+) - enantiomer - greater affinity for μ-receptors, selective inhibition of reuptake of serotonin.(-) - enantiomer - less affinity for μ-receptors, inhibition of norepinephrine reuptake and stimulation of α2-adrenergic receptors.

Pharmacokinetics:

Absorption ~ 75% (100 mg). The volume of distribution is 2.6 and 2.9 l / kg in men and women, respectively. Connection with plasma proteins - 20%. Biotransformation in the liver (CYP2D6, 3A4) to form an active metabolite of mono-O-desmethyltramadol (M1). The half-life is ~ 6.3 h. Half-life M1 ~ 7.4 hours. Elimination by the kidneys is ~ 30% unchanged, 60% - in the form of metabolites, 7% is excreted in hemodialysis.

Indications:

Moderate and strong pain syndrome of various genesis (including malignant tumors, acute myocardial infarction, neuralgia, trauma). Conducting painful diagnostic or therapeutic procedures.

ICD-10

IX.I20-I25.I21 Acute myocardial infarction

XVIII.R50-R69.R52.0 Acute pain

XVIII.R50-R69.R52.2 Another constant pain

Contraindications:

Hypersensitivity, poisoning with alcohol, hypnotics, narcotic analgesics and other psychoactive drugs, pregnancy, breast-feeding (in case of prolonged use), children's age (up to 1 year - for parenteral administration, up to 14 years for oral administration), MAO inhibitors.

Carefully:

Opioid addiction, impaired consciousness of various genesis, intracranial hypertension, head trauma, epileptic syndrome (cerebral genesis), conditions accompanied by respiratory depression or severe CNS depression.

Pregnancy and lactation:

Adequate and well-controlled studies in humans have not been conducted. In animals, induced embryo- and fetotoxic, but not teratogenic, effects. Do not apply! Penetrates into breast milk in low doses. Do not apply!

Recommendations for FDA - Category C.

Dosing and Administration:

Adults and children over 14 years of age receive a single dose when taken orally - 50 mg, rectally - 100 mg, intravenously slowly or intramuscularly - 50-100 mg. If the effectiveness of parenteral administration is insufficient, then in 20-30 minutes, oral administration in a dose of 50 mg is possible.

Children aged 1 to 14 years of age are given a dose of 1-2 mg / kg.

The duration of treatment is determined individually.

The maximum dose: adults and children over 14 years, regardless of the mode of administration - 400 mg per day.

Side effects:

From the side CNS: dizziness, weakness, drowsiness, confusion; in some cases, seizures of cerebral genesis (with intravenous administration in high doses or with the simultaneous appointment of neuroleptics).

From the side of cardio-vascular system: tachycardia, orthostatic hypotension, collapse.

From the side digestive system: dry mouth, nausea, vomiting.

From the side metabolism: increased sweating.

From the side musculoskeletal system: miosis.

Overdose:

Symptoms acute and chronic overdose: cold sticky sweat, confusion, dizziness, drowsiness, decreased blood pressure, nervousness, fatigue, miosis, bradycardia, severe weakness, slow labored breathing, hypothermia, anxiety, dry mouth, delirious psychosis, intracranial hypertension (up to disorders of cerebral circulation), hallucinations, muscle rigidity, convulsions, in severe cases - loss of consciousness, respiratory arrest, coma.

Treatment: gastric lavage, recovery of respiration and maintenance of cardiac activity and blood pressure; intravenous injection of a specific antagonist opioid analgesics - naloxone in a single dose of 0.2-0.4 mg with repeated administration 2-3 minutes before the total dose of 10 mg; the initial dose of naloxone for children is 0.01 mg / kg. With convulsions - diazepam.

Interaction:

Alcohol, anesthetics, tricyclic antidepressants, other opioid analgesics, phenothiazines, sedative hypnotics, tranquilizers and other drugs that depress the central nervous system - potentiating CNS depression.

Serotonin 5-HT antagonists₃-receptors (ondansetron and others) - a decrease in the effectiveness of tramadol.

Anticoagulants indirect - potentiation of anticoagulant effect.

Diclofenac, indomethacin, phenylbutazone, diazepam, flunitrazepam, nitroglycerine - Pharmaceutical incompatibility with tramadol.

MAO inhibitors, including furazolidone and procarbazine - reduction of the convulsive threshold, occurrence of epileptic seizures.

Carbamazepine - an increase in the metabolism of tramadol and a decrease in its effect, with a daily dose of carbamazepine 800 mg a dose of tramadol can be doubled.

Tricyclic antidepressants, fluoxetine, sertraline - increased risk of epileptic seizures.

Quinidine, propafenone (inhibition of CYP2D6) - an increase in the concentration of tramadol and a decrease in the concentration of the active metabolite.

Special instructions:

Synthetic opioid analgesic, less affinity for opioid receptors - 10 times compared with codeine and 6000 times - as compared with morphine. However, the active metabolite is 2-4 times more active than tramadol.Expression of analgesic action: 5-10 times weaker than morphine.

It is dose-dependent for postoperative pain, 75-150 mg once is comparable in effectiveness with combinations of acetaminophen + propoxyphene and aspirin + codeine, 100 mg are intravenously equal in the analgesic activity of 2.5 grams of metamizole (dipiro) intravenously.

Tramadol is effective in back pain, but the advisability of its use in this condition requires further research.

Instructions

Tramadol (Tramadolum)