Paracetamol + Tramadol (Paracetamolum + Tramadolum)

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

Opioid non-narcotic analgesics and opioid antagonists

Included in the formulation
  • Zaldiar
    pills inwards 
    Grünenthal GmbH     Germany
  • Rutram®
    pills inwards 
    BALTIMOR FK, LLC     Russia
  • TRAMACETTE
    capsules inwards 
    K.O. Ромфарм Компани С.Р.Л.     Romania
    • АТХ:

    N.02.A.X   Other opioids

    N.02.A.X.52   Tramadol in combination with other drugs

    Pharmacodynamics:

    Combined drug. Paracetamol accelerates the onset of analgesic effect, tramadol - prolongs it.

    Paracetamol

    Has antipyretic, analgesic and anti-inflammatory effect. Inhibits cyclooxygenase, mainly in the central nervous system, affects the centers of pain and thermoregulation. It does not have a negative effect on water-salt metabolism and mucous membranes of the gastrointestinal tract, and therefore has little effect on the synthesis of prostaglandins in peripheral tissues.

    Tramadol

    Non-selective agonist of 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:

    Paracetamol

    After oral administration, it is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 20-30 minutes. The connection with plasma proteins is 15%. Penetrates through the blood-brain barrier, enters the breast milk.

    Metabolism in the liver by glucuronation and sulfation (80%) with the formation of inactive metabolites, about 17% is hydroxylated to active metabolites, which are subsequently deactivated after conjugation with sulfates and glutathione. With a lack of glutathione, these metabolites block the enzyme systems of the liver, causing necrosis of hepatocytes.

    Half-life is 2-3 hours. Elimination by the kidneys, about 3% unchanged.

    Tramadol

    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 elimination 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.

    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 1-2 tablets with pain, interval in the reception at least 6 hours.

    The highest daily dose: 8 tablets (2.6 paracetamol and 300 mg of tramadol).

    The highest single dose: 2 tablets.

    Side effects:

    Central and peripheral nervous system: dizziness, headache, inhibition, nervousness, euphoria, hallucinations, tremors, muscle spasms, cognitive impairment, unsteadiness of gait, paresthesia, visual impairment and taste.

    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:

    Paracetamol

    Diarrhea, anorexia - with acute overdose (develops 6-14 hours after exceeding the dose), with chronic (develops 2-4 days after exceeding the dose) - hypocoagulation, DIC syndrome, cerebral edema, rarely - fulminant renal failure due to tubular necrosis .

    Tramadol

    Myos, collapse, coma, cramps, apnea.

    Necrosis of liver cells, due to the formation of a toxic metabolite of acetaminophen - N-acetyl-p-benzoquinonimine.

    Treatment: application of donators SH-groups, precursors of the synthesis of glutathione-methionine and N-acetylcysteine ​​for 12 hours after an overdose.

    Introduction of naloxone, diazepam.

    Interaction:

    Paracetamol

    Strengthens the effect of indirect coagulants and toxicity of chloramphenicol.

    The intake of ethanol in the treatment of the drug leads to the development of acute pancreatitis.

    Simultaneous use with stimulators of microsomal oxidation in the liver - barbiturates, rifampicin, ethanol, phenylbutazone, phenothionine, increases the toxicity of paracetamol.

    Reduces the risk of hepatotoxic effects of microsomal oxidation inhibitors (cimetidine).

    Tramadol

    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) increase the side effects of tramadol.

    Special instructions:

    Monitoring of glucose and uric acid in the plasma, the composition of peripheral blood, the functional state of the liver.

    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.

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