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

Tramadol is an opioid synthetic analgesic with central action and action on the spinal cord (contributes to the discovery of K- and Ca2 + -channels, causes hyperpolarization of membranes and inhibits pain impulses), enhances the action of sedative drugs. Activates opiate receptors (mu, delta, kappa) on the pre- and postsynaptic membranes of the afferent fibers of the nociceptive system in the brain and gastrointestinal tract.

The analgesic effect is due to a decrease in nociceptive activity and an increase in the antinociceptive systems of the body.

In therapeutic doses, it does not significantly affect haemodynamics and breathing, does not change the pressure in the pulmonary artery, slightly slows the intestinal motility, does not cause constipation. Has some antitussive and sedative effect. Oppresses the respiratory center, excites the start zone of the vomiting center, the nucleus of the oculomotor nerve.

With prolonged use, the development of tolerance is possible.

Analgesic effect develops 15-30 minutes after ingestion and continues until

6 hours

Pharmacokinetics:

Absorption - 90%; bioavailability - 68% (increases with repeated use).

Time to reach the maximum concentration after ingestion - 2 h. Ml metabolite - 3 h.

Penetrates through the blood-brain barrier and placenta, 0.1% excreted in breast milk. The volume of distribution is 306 liters. Connection with plasma proteins - 20%.

In the liver, it is metabolized by N- and O-dimethylation followed by conjugation with glucuronic acid. 11 metabolites have been identified, of which mono-O-dimethyltrimadol (Ml) has pharmacological activity. The half-life in the second phase is -6h (tramadol), 7.9 h (M1); in patients older than 75 years - 7.4 h (tramadol); with cirrhosis of the liver -13.3 ± 4.9 h (tramadol), 18.5 ± 9.4 (Ml), in severe cases - 22.3 and 36 hours, respectively; with chronic renal failure (creatinine clearance less than 5 ml / min) - 11 +/- 3.2 h (tramadol), 16.9 ± 3 h (Ml), in severe cases - 19.5 h and 43.2 h, respectively.

It is excreted by the kidneys (25-35% unchanged), the average cumulative index of renal excretion is 94%.

About 7% is excreted by hemodialysis.

Indications:

Pain syndrome (strong and moderate intensity, including inflammatory, traumatic, vascular origin).

Anesthesia in the conduct of painful diagnostic or therapeutic measures.

Contraindications:Hypersensitivity; poisoning with alcohol, hypnotic drugs, narcotic analgesics and other psychoactive drugs; severe hepatic and / or renal insufficiency (creatinine clearance less than 10 ml / min); pregnancy and lactation period (the application is possible only according to vital indications and should be limited only to one-time administration); children's age (up to 14 years), administration of MAO inhibitors.

Carefully:With caution should take the drug to people with drug dependence on opioids; patients with impaired renal and hepatic function, with craniocerebral trauma, increased intracranial pressure, epileptic syndrome (cerebral genesis); in a state accompanied by respiratory depression or severe oppression of the central nervous system.

Dosing and Administration:

The drug is used according to the doctor's prescription, the dosage regimen is selected individually, depending on the severity of the pain syndrome of the patient's sensitivity.Duration of treatment is determined individually, do not prescribe the drug beyond the term justified from a therapeutic point of view.

In the absence of other prescriptions, the drug should be administered in the following dosages: inside for single use for adults and children older than 14 years - 50 mg with a small amount of fluid, after 30-60 minutes you can repeat the dose at the same dose, but not more than 8 doses per day . The maximum daily dose is 400 mg.

Individuals who are elderly (75 years and older) and patients with renal insufficiency need an individual dosage. When the creatinine clearance is less than 30 ml / min and in patients with liver failure 12 h interval between taking the next doses of the drug is needed.

Side effects:

From the side of the nervous system: increased sweating, dizziness, headache, weakness, fatigue, inhibition, paradoxical stimulation of the central nervous system (nervousness, agitation, anxiety, tremor, muscle spasms, euphoria, emotional lability, hallucinations), drowsiness, sleep disturbance, confusion, violation of coordination of movements, convulsions of the central genesis, depression, amnesia, cognitive impairment, paresthesia.

On the part of the digestive system: dry mouth, nausea, vomiting, flatulence, abdominal pain, constipation or diarrhea, difficulty in swallowing.

From the cardiovascular system: the manifestation of vasodilation - tachycardia, orthostatic hypotension, fainting, collapse.

Allergic reactions: hives, itching, exanthema, bullous rash.

From the urinary system: difficulty urinating, dysuria, urinary retention.

From the senses: a violation of sight, taste.

From the respiratory system: dyspnoea.

Other: violation of the menstrual cycle. With prolonged use - drug dependence. With a sharp cancellation, the "cancellation" syndrome.

Overdose:

Symptoms: miosis, vomiting, collapse, coma, convulsions, respiratory center depression, apnea.

Treatment: maintenance of patency of respiratory ways, maintenance of breath and activity of cardiovascular system. Opiate-like effects can be stopped with naloxone, convulsions with benzodiazepine.

Interaction:

Strengthens the effect of drugs that depress the central nervous system, and the standard.

Inductors of microsomal oxidation (incl. carbamazepine, barbiturates) reduce the severity of the analgesic effect and the duration of the action.

Long-term use of opioid analgesics or barbiturates stimulates the development of cross tolerance.

Anxiolytics increase the severity of the analgesic effect; The duration of anesthesia increases with combination with barbiturates.

Naloxone activates breathing, eliminating analgesia after the use of opioid analgesics.

MAO inhibitors, furazolidone, procarbazine, antipsychotic drugs (neuroleptics) increase the risk of seizures (reduction of the convulsive threshold).

Quinidine increases the plasma concentration of tramadol and reduces the M1 metabolite due to competitive inhibition of the CYP2D6 isoenzyme.

Special instructions:

Do not apply for the treatment of withdrawal syndrome.

Do not use at the same time ethanol.

In the case of a single dose, there is no need to interrupt breastfeeding.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of 100 mg.

Packaging:

For 10 tablets in a contour mesh package or 20 tablets in a can of lightproof glass. 2 contour mesh packages or each jar along with the instructions for use are placed in a pack of cardboard.

Storage conditions:

List of potent substances.

In the dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:5 years. Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001820 / 02

Date of registration:22.10.2008

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp19.09.2015

Illustrated instructions

Instructions

Tramadol (Tramadol)