Tramadola hydrochloride

General characteristics. Structure:

Active ingredient: tramadol;

1 ml of solution contains 50 mg of a tramadol of a hydrochloride;

excipients: sodium acetate, trihydrate; water for injections.

Pharmacological properties:

Pharmacodynamics. Tramadol – an analgetic of the central action. Has the mixed action mechanism. Is a non-selective agonist of opioid mu - delta and kaparetseptor. Other mechanisms which participate in ensuring analgeziruyushchy action of Tramadol of a hydrochloride is the inhibition of the return capture of noradrenaline in neurons and strengthening of the serotonergic answer.

Opens K+ and ++-channels Sa, causes hyperpolarization of membranes and slows down carrying out painful impulses. The analgetic effect is caused by decrease of the activity nociceptive and strengthening of anti-nociceptive system of an organism. Tramadola a hydrochloride shows antibechic action. At use of therapeutic doses of Tramadol the hydrochloride does not oppress breath and does not influence motility of intestines.

At intravenous administration shows analgeziruyushchy action in 5-10 minutes, works within 3-5 hours.

Pharmacokinetics. Absorption at intramuscular introduction – 100%. Time of achievement of the maximum concentration after intramuscular introduction – 45 minutes. Absolute bioavailability – nearly 70%. Linkng with blood proteins makes 20%. Gets through hematoencephalic and placental barriers. 0,1% of drug get into breast milk. It is metabolized in a liver. An elimination half-life – 6 hours. Tramadol and his metabolites are removed by kidneys (25-35%) in not changed state. About 7% are removed by means of a hemodialysis.

Increase in an elimination half-life at patients is noted 75 years are more senior.

Pharmaceutical characteristics.

Main physical and chemical properties: transparent colourless liquid.

Incompatibility. Tramadol is incompatible with solutions of diclofenac, indometacin, phenylbutazone, diazepam, flunitrazepam, nitroglycerine, midazolam.

Indications to use:

Acute and chronic pain syndrome of moderate and considerable degree of manifestation (before - and postoperative the periods, malignant tumors, injuries, neuralgia). Carrying out painful diagnostic and medical manipulations.

Route of administration and doses:

Drug is used intravenously, intramusculary or subcutaneously.

The dose is established by the doctor individually, proceeding from intensity of a pain syndrome.

To adults and children 14 years are aged more senior enter intravenously (slowly kapelno), intramusculary or subcutaneously 50-100 mg (1-2 ml of solution). In the absence of satisfactory effect in 30-60 minutes возможо additional introduction of 50 mg (1 ml) of drug. Frequency rate of introduction makes 1-4 times a day depending on expressiveness of a pain syndrome and efficiency of therapy. The maximum daily dose – 400 mg.

Children from 1 to 14 years solution for injections can appoint (in exceptional cases) in a single dose 1-2 mg/kg of body weight of the child. The maximum daily dose – 4-8 mg/kg of body weight.

And also elderly (75 years are also more senior) dosing correction is necessary for patients with dysfunctions of livers/kidneys: reduction of a dose and frequency of administration of drug. The highest daily dose for patients is more senior than 75 years should not exceed 300 mg (6 ml of drug).

Treatment duration is defined by drug individually. A hydrochloride it is longer impossible to apply Tramadol than the term justified from the therapeutic point of view.

Features of use:

During Tramadol's treatment by a hydrochloride it is not necessary to take alcohol.

At prolonged use of Tramadol of a hydrochloride can develop accustoming and medicinal dependence.

Tramadol a hydrochloride should not be applied to therapy of a withdrawal of narcotic substances.

It is necessary to be careful at purpose of drug at the confused consciousness, dysfunction of a respiratory center, the increased intracranial pressure, a convulsive syndrome of cerebral genesis, and also to patients with hypersensitivity to opiates.

Ability to influence speed of response at control of motor transport or work with other mechanisms. At use of drug it is necessary to refrain from control of motor transport and work with other mechanisms which requires special attention and bystry mental and motor reactions.

Side effects:

From a nervous system: sweating strengthening, a headache, dizziness, weakness, block, reduction in the rate of reactions, a sleep disorder, a spasm of muscles, euphoria, hallucinations, uneasiness, emotional lability, a depression, amnesia, paresthesias is possible; in some cases – spasms of cerebral genesis (at intravenous administration of high doses or at co-administration of neuroleptics).

From sense bodys: vision disorder, taste.

From digestive tract: nausea, vomiting, dryness in a mouth, a lock, a meteorism, pain in epigastriums, diarrhea, appetite change.

From cardiovascular system: tachycardia, it is rare – a heart consciousness; decrease or increase in arterial pressure up to a collapse (an orthostatic collapse), bradycardia.

Allergic reactions: urticaria, itch, dieback, violent rash, acute anaphylaxis, toxic epidermal necrolysis, Stephens-Johnson's syndrome.

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

From respiratory system: диспноэ.

Others: disturbance of a menstrual cycle.

Interaction with other medicines:

At co-administration of Tramadol of a hydrochloride with drugs which oppress the central nervous system, perhaps mutual strengthening of the central effects, including respiratory depression.

Inductors of a microsomal oxidation (carbamazepine, barbiturates) reduce expressiveness of analgetic effect and duration of action. Prolonged use of opioid analgetics or barbiturates stimulates development of cross tolerance.

Anxiolytics increase expressiveness of analgetic effect, duration of anesthesia increases at a combination with barbiturates. Naloxonum activates breath, stopping an analgesia after use of opiodny analgetics. At use together with MAO inhibitors, furasolidone, Procarbazinum, neuroleptics there is a risk of development of spasms.

Quinidine increases plasma concentration of a tramadol and reduces the maintenance of a metabolite of M1 at the expense of competitive inhibition of CYP2D6 isoenzyme.

At simultaneous use of Tramadol of a hydrochloride and warfarin the risk of emergence of side effects from coagulant system of blood increases. Tramadola a hydrochloride can cause attacks and/or development of potentially life-threatening serotoninovy syndrome at use together with serotonergic drugs.

Contraindications:

Hypersensitivity to active ingredient or to other components of drug. Acute intoxication the alcohol and medicines oppressing the central nervous system (neuroleptics, sedative, antidepressants, anxiolytics, hypnotic drugs). Epilepsy. Simultaneous use of MAO inhibitors. Heavy liver/renal failure. Pregnancy and period of feeding by a breast. Children aged till 1 year.

Overdose:

Symptoms: vomiting, a miosis, circulator disturbances, consciousness oppression (up to a coma), spasms, a depression of a respiratory center to a full apnoea.

Treatment is aimed at providing passability of respiratory tracts, maintenance of breath and function of cardiovascular system.

Antidote at oppression of a respiratory center is Naloxonum, at spasms – benzodiazepine. Tramadol is poorly brought by means of dialysis therefore separate use of a hemodialysis or haemo filtering is not enough.

Use during pregnancy or feeding by a breast.

Tramadol gets through a placental barrier therefore it is not recommended to use drug during pregnancy. If there are indications for performing the anesthetizing therapy during pregnancy, it is necessary to be limited to single application.

A small amount of Tramadol of a hydrochloride gets into breast milk therefore it is not necessary to use drug during the feeding period a breast. At single application feeding by a breast can be not interrupted.

Children.

Drug is not used for treatment of children aged till 1 year. To children 1 years drug are more senior appoint in the presence of direct indications.

Storage conditions:

Period of validity. 3 years. Not to use drug after the termination of the period of validity specified on packaging. To store in protected from light and the place, unavailable to children, at a temperature from 15 ºС to 25 ºС.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in an ampoule. On 10 ampoules enclosed in a pack.