Tramadol

General characteristics. Structure:

Active ingredient: 50 mg or 100 mg of a tramadol of a hydrochloride in 1 tablet.

Excipients: sugar milk (lactose), magnesium stearate, potato starch.

Pharmacological properties:

Pharmacodynamics. Tramadol is a cyclohexanol derivative with opiatagonistichesky properties. Treats analgetics of the central action. Has weak affinity to opiate receptors without preferential selectivity to separate populations of receptors. Possesses anesthetic, antibechic and sedative effects. Activity of a tramadol makes 1/10-1/6 part of activity of morphine. Unlike morphine трамадол in therapeutic doses breath does not oppress, does not suppress motility of digestive tract and does not influence srdechno-vascular activity.

Pharmacokinetics. At intake it is quickly soaked up, therapeutic action comes in 15-30 minutes. Therapeutic action remains within 4-8 hours. The maximum concentration in a blood plasma after intake is observed through a 1,5-2chas. Linkng with proteins of a blood plasma about 20%. Gets through a placental barrier (concentration in blood of an umbilical vein makes 80% of concentration in mother's blood).

Biotransformation is carried out in a liver by demethylation and conjugation with formation of 11 metabolites (1 of them – active). It is removed preferential by kidneys (90%) and intestines (about 10%). At disturbance of functions of a liver and kidneys (clearance of creatinine less than 80 ml/min.) removal is slowed down.

Indications to use:

• Acute and chronic pain syndrome of strong and average intensity of various genesis (malignant tumors, injuries, heavy neurology, etc.).
• Painful diagnostic and therapeutic manipulations.

Route of administration and doses:

Inside. The applied dosages depend on degree of manifestation of a pain syndrome and individual sensitivity of the patient. Time of administration of drug does not depend on meal time.

Adults and teenagers since 14 years. The single dose makes 50 mg of a tramadol. In case of insufficiency or in the absence of the anesthetizing action in 30-60 minutes accept 50 mg of a tramadol repeatedly. At pains of strong intensity a single dose of 100 mg of a tramadol. The anesthetizing action usually remains within 4-8 hours. Maximum daily dose of 400 mg.

Patients with a renal failure and/or a liver. At patients with a renal failure and/or a liver removal of a tramadol from an organism is complicated. In case of treatment of acute pain syndromes special change of dosages is not required from such patients when, rare or single purpose of a tramadol is necessary. However in cases of treatment of chronic pains it is necessary to remember danger of cumulation of drug in an organism therefore it is reasonable to increase intervals between its separate receptions. Patients should appoint drug with care with renal failures (50-100 mg 2 times a day), and also to persons with cirrhosis (at this group of sick T 1/2 tramadola increase almost by 3 times).

Patients of senile age. At patients of senile age (75 years are more senior) removal of a tramadol from an organism even when there is no clinical manifestations of a renal failure and/or a liver is slowed down. At these patients it is also necessary to increase intervals between separate administrations of drug. It is recommended not to exceed a daily dose in 300 mg.

Features of use:

Use during pregnancy and during feeding by a breast. Tramadol gets through a placental barrier. In insignificant quantities (0,1% of concentration in a blood plasma) comes to maternal milk. In this regard, therapy during pregnancy has to be limited to separate single doses. Prolonged use during pregnancy should be avoided because of risk of development of accustoming in a fruit and possibility of a withdrawal in the neonatal period. Use of a tramadol just before or during childbirth does not influence sokratitelny function of a uterus. In these cases at the newborn it is possible being observed by change of frequency of respiratory movements which not significantly for clinical practice. Use of a tramadol in the period of a lactation in the form of single doses does not demand feeding interruption by a breast.

The recommended doses are approximate. In practice it is necessary to choose effective doses minimum analgetic.

Treatment duration is defined by drug individually. It is impossible to apply longer than the term justified from the therapeutic point of view. At treatment it is long the remaining pain syndrome reasonablly to do short-term pauses in use of a tramadol again to define a necessary therapeutic dose.

During treatment it is necessary to exclude alcohol intake and to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Cardiovascular system: tachycardia, a lowering of arterial pressure (up to - to an orthostatic collapse), syncopal states.

Digestive tract: nausea, vomiting, dryness in a mouth, abdominal pain, anorexia, a meteorism, a lock.

Nervous system and mental sphere: alarm, a lack of coordination, euphoria or a depression, a miosis, frustration of a dream, the increased nervous irritability, disturbances of cognitive functions, paresthesias, a tremor, amnesia, spasms, hallucinations, respiratory depression, sedation of different degree of manifestation, dizziness, a headache, increase in a muscle tone.

Urinary system: the complicated or speeded up urination.

Others: skin reactions (a dieback, an itch) up to an acute anaphylaxis, Stephen-Johnson's syndrome, the increased perspiration, диспноэ.

At prolonged use - medicinal dependence, at sharp cancellation – a syndrome of "cancellation". It was reported about deterioration in a course of bronchial asthma, however, evidential data on negative influence of a tramadol on the course of asthma were not received.

Interaction with other medicines:

At simultaneous use of a tramadol and:
• the medicines oppressing the central nervous system, especially antidepressants, and also alcohol side effects of a tramadol concerning the central nervous system amplify;
• the medicines capable to provoke convulsive attacks or to increase convulsive readiness (for example, neuroleptics and antidepressants), seldom or never it is possible to observe epileptic seizures. The risk of developing of convulsive attacks increases at use of high doses of a tramadol - over 400 mg a day;
• carbamazepine the analgeziruyushchy effect of a tramadol decreases and reduced;
• quinidine increases plasma concentration of a tramadol;
• barbiturates and tranquilizers strengthening and increase in duration of analgeziruyushchy and sedative action of a tramadol is possible.

Prolonged use of opioid analgetics or barbiturates stimulates development of cross tolerance.

Contraindications:

• Hypersensitivity to any of drug components.
• Acute alcoholic poisonings, analgetics, somnolent and psychopharmacological means.
• Treatment by MAO inhibitors and within 14 days after the end of this treatment.
• Children's age up to 14 years.

Tramadol it is impossible to use as replacement therapy at drug addiction.

With care:

• opioid drug addiction (dependence on opioids);
• disturbances of consciousness of not clear genesis;
• disturbances of a respiratory center and respiratory functions, and also at the states which are followed by increase in intracranial pressure if the patient is not on an artificial respiration;
• brain diseases;
• shock;
• epilepsy or tendency to convulsive attacks. At patients with epilepsy or convulsive attacks, inclined to emergence, drug is used only in exceptional cases;
• patients with hypersensitivity to opioids.

Overdose:

Symptoms: a miosis or a mydriasis, vomiting, tachycardia, increase in arterial pressure, a collapse, consciousness oppression, up to a coma, respiratory depression (up to an apnoea).

Treatment: at intake, first of all, it is necessary to provide release of a stomach from yet not soaked up drug (artificial vomiting, a gastric lavage).

The main urgent actions in more hard cases are ensuring passability of respiratory tracts (intubation), maintenance of breath and cardiovascular system.

Antidote at oppression of a respiratory center is Naloxonum which is entered repeated doses since duration of its action is shorter, than action of a tramadol. Benzodiazepines are applied to stopping of a convulsive syndrome.

Storage conditions:

Not to use after the period of validity specified on packaging. Treats the list of 1 strong substances. In the dry, protected from light place at a temperature not above 25 °C, in places unavailable to children. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 or 20 tablets in a blister strip packaging. 1 or 2 blister strip packagings together with the application instruction place in a pack from a cardboard.