TAPENTADOL (Tapentadolum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Opioid narcotic analgesics

Included in the formulation
  • Palexia
    pills inwards 
    Grünenthal GmbH     Germany
  • Palexia
    pills inwards 
    Grünenthal GmbH     Germany
    • АТХ:

    N.02.A.X.06   TAPENTADOL

    Pharmacodynamics:

    Tapentadol is a non-selective agonist of the σ- μ and κ receptors of the central nervous system. Opioid analgesic, a cyclohexanol derivative - a racemate of (+) and (-) isomers. The isomer (+) is an opioid receptor agonist that does not have a pronounced selectivity. The isomer (-) inhibits the neuronal seizure of norepinephrine, thereby activating the descending noradrenalinergic effects. Thus, the transmission of pain impulses to the gelatinous substance of the spinal cord is interrupted. It inhibits pain impulses due to the opening of potassium and calcium channels, resulting in the hyperpolarization of postsynaptic membranes.

    Has antitussive effect, does not depress respiration in therapeutic doses.

    Pharmacokinetics:

    After oral administration, up to 90% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2 hours. The connection with plasma proteins is 20%. It spreads in the tissues. It penetrates the placental barrier and enters the breast milk.

    Therapeutic effect develops after the reception.Metabolism in the liver up to 11 metabolites, only one of which has pharmacological activity.

    The half-life is 4.5 hours. Elimination by the kidneys (90%) and with feces (10%).

    Indications:

    It is used to stop the pain syndrome of medium and strong intensity, used in the postoperative period and before carrying out painful diagnostic procedures.

    ICD-10

    XVIII.R50-R69.R52.0   Acute pain

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

    XXI.Z40-Z54.Z51.4   Preparatory procedures for subsequent treatment, not elsewhere classified

    Contraindications:

    Acute intoxication with ethanol, opioids and psychotropic drugs, severe renal and hepatic insufficiency, epilepsy, withdrawal syndrome, individual intolerance, children under 18 years of age.

    Carefully:

    State of shock, craniocerebral trauma, respiratory function disorder, viral hepatitis, alcoholism, drug addiction, deficiency of glucose-6-phosphate dehydrogenase, patients older than 75 years.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside to 50, 75 or 100 mg every 4 to 6 hours.

    The highest daily dose: 700 mg.

    The highest single dose: 100 mg.

    Side effects:

    Central and peripheral nervous system: dizziness, headache, inhibition, nervousness, euphoria, hallucinations, tremor, muscle spasms, cognitive impairment, gait instability, paresthesia, visual and taste disorders.

    Respiratory system: dyspnoea.

    The system of hematopoiesis: Sulfhemoglobinemia, aplastic anemia, pancytopenia.

    The cardiovascular system: tachycardia, orthostatic hypotension, syncope.

    Digestive system: dry mouth, nausea, vomiting, flatulence, constipation, difficulty in swallowing, diarrhea.

    Endocrine system: hypoglycemia.

    Dermatological reactions: hyperhidrosis, bullous rash, toxic epidermal necrolysis (Lyell's syndrome).

    Reproductive system: violation of the menstrual cycle.

    Allergic reactions.

    Overdose:

    Myos, collapse, coma, cramps, apnea.

    Treatment: the administration of naloxone, diazepam.

    Interaction:

    Strengthens the effect of indirect anticoagulants.

    Reduces the analgesic effect when combined with opioid agonist antagonists (buprenorphine, nalboufine, pentazocine) as a result of competing effects on receptors.

    Simultaneous use with drugs that lower the threshold of seizure activity (selective serotonin reuptake inhibitors, antipsychotic antidepressants) increases the risk of developing convulsive syndrome.

    Simultaneous use with other drugs that depress the central nervous system (tranquilizers, sleeping pills, ethanol) increases the side effects of tapentadol.

    Special instructions:

    With prolonged use of the drug, symptoms of drug dependence develop, with sudden discontinuation of reception - withdrawal syndrome.

    During the treatment, alcohol is not allowed.

    During the treatment it is not recommended to drive the car and work with moving mechanisms.

    Instructions
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