Tramadol

International name: Tramadol.

Pharmacological action of Tramadol

Drug Tramadol – a synthetic analgetic, concerns to group of opioid means, has effect on the central nervous system and a spinal cord, causing hyperpolarization of membranes and slowing down carrying out painful impulses. Gives the powerful analgeziruyushchy effect lasting long time. Activates opiate receptors in a brain and digestive tract. Slows down destruction and stabilizes concentration of catecholamines in the central nervous system.

Drug Tramadol – the selection agonist of a mu - opioid receptors, selectively braking return neyronalny serotonin reuptake and noradrenaline. Analgeziruyushchy action of Tramadol, at identical doses, is 5-10 times weaker, than at morphine.

At observance of the dosage specified in the instruction, Tramadol has no significant effect on breath and a hemodynamics, does not change indicators of pulmonary pressure, does not render the considerable slowing-down effect on an intestines peristaltics.

Has sedative and easy antibechic effect. At long therapy tolerance development is probable. The analgesic effect occurs in 15-30 minutes after the internal use of drug and continues to work till 6 o'clock.

Tramadol's pharmacokinetics

After oral administration, drug approximately for 90% is soaked up by digestive tract. The maximum concentration of Tramadol in a blood plasma is reached in two hours after reception. At a single dose of drug, bioavailability makes 68%, and grows in process of use.

Drug contacts proteins of plasma for 20%. Tramadol can get through a placental barrier, into concentration of similar concentration in plasma. About 11 metabolites from which 1 is active are metabolized. It is brought to 10% through intestines and 90% by kidneys.

Indications to Tramadol's use

Tramadol apply at strong and moderately severe pain of an inflammatory, traumatic and vascular etiology. When holding the diagnostic or therapeutic procedures connected with painful feelings. And also during the post-operational period, and to patients with oncological diseases. At mild pains purpose of drug is not recommended.

Contraindications for Tramadol's use

Tramadol is not recommended for use at:

• hypersensitivity to Tramadol;
• states with oppressed breath or the oppressed central nervous system, because of alcoholic or drug poisoning;
• pregnancies;
• chest feeding (except one-time receptions);
• reception of monoamine oxidase inhibitors;
• heavy renal or liver failure.

Tramadol is not recommended by the instruction to children till 1 year (parenteral administration) and to children up to 14 years (internal acceptance).

It is necessary to apply with care Tramadol to patients with: drug addiction, confusion of consciousness, intracranial hypertensia, craniocereberal injuries, epileptic syndromes (cerebral genesis), pains in an abdominal cavity of not clear origin.

Side effects of Tramadol

On the received comments Tramadol can cause side effects in a look: the increased sweating, dizziness, a headache, weakness, block, paradoxical stimulation of the central nervous system (hallucinations, nervousness, uneasiness, agitation, spasms of muscles, a tremor, euphoria, emotional lability), drowsiness, sleep disorders, confusion of consciousness, lacks of coordination of the movement, spasms, a depression, amnesia, disturbances of cognitive function, instability of gait.

Side effects of Tramadol from the alimentary system can be shown in a look: dryness in a mouth, nausea, a meteorism, an abdominal pain, locks or diarrhea.

From cardiovascular system in a look: tachycardias, orthostatic hypotension, faint, collapse.

From an urinary system: the complicated urination, a dysuria, an ischuria.

Side effects in a look are also possible: allergic reactions, vision disorder, taste, disturbances of a menstrual cycle.

Prolonged use of drug causes dependence. At sharp cancellation, the syndrome of "cancellation" is shown.

Overdose

The comments received about overdose by Tramadol show possible manifestations of the following symptoms: collapse, coma, miosis, apnoea, vomiting, depression of a respiratory center, spasm.

Treatment of overdose is carried out by support of passability of respiratory tracts, and maintenance of activity of cardiovascular system. For stopping of opiatopodobny effects use Naloxonum, at spasms – benzodiazepine.

Dosage and routes of administration

According to the instruction, Tramadol is applied intravenously, intramusculary, subcutaneously, orally and rektalno.

Orally: to adults and children 14 years, single use – one tablet or the capsule of 0,05 g with liquid, or 20 drops of solution for internal reception with liquid or on sugar are more senior. Repeated reception is possible in 30-60 minutes, in the same dosage, no more than 8 times a day.

Rektalno: 0,1 grams to 4 times a day.

Intravenously (slowly), subcutaneously and intramusculary: 0.05-0.1. At insufficient effect further infusion with a speed of 12 mg/h or additional intake. The total dose should not exceed per day 0.4 g.

To children is more senior than one year, only in the form of drops or parenterally, with a dosage of 1-2 mg/kg. A daily dosage to 8 mg/kg.

To elderly people and patients with a renal failure the recipe on Tramadol has to be formed taking into account an individual dosage.

Special instructions

Tramadol it is not necessary to apply to treatment of a syndrome of "cancellation" of drugs. It is not applied along with ethanol. At one-time uses it is admissible not to interrupt chest feeding. During therapy should be careful the persons occupied at potentially dangerous works including driving of motor transport.

Interaction with other drugs

Tramadol is incompatible with solutions of diclofenac, indometacin, diazepam, nitroglycerine, phenylbutazone, flunitrazepam. Strengthens effect of the medicines oppressing the central nervous system and ethanol.

At prolonged use of barbiturates or opioid analgetics there is a development of cross tolerance. At the combined reception of barbiturates with Tramadol responses show strengthening of anesthetic effect.

In combination with monoamine oxidase inhibitors, furasolidone, Procarbazinum and anti-psychotropic drugs there is a decrease in a convulsive threshold and there is a risk of emergence of spasms.

Drug storage

Tramadol is stored by the rules similar to rules of storage of morphine and other narcotic drugs. Issue from drugstores is made only upon presentation of the recipe on Tramadol.