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

Composition:1 ml of the solution contains the active substance: tramadol hydrochloride - 50 mg; auxiliary substances: sodium acetate -1 mg; water for injection - up to 1 ml.

Description:

Colorless transparent liquid.

Pharmacotherapeutic group:An analgesic with a mixed mechanism of action.

ATX: & nbsp

N.02.A.X.02 Tramadol

Pharmacodynamics:Tramadol is a cyclohexanol derivative with opiate agonist properties. Refers to analgesics of the central action. Has a weak affinity for opiate receptors without preferential selectivity to individual receptor populations. It has analgesic, antitussive and sedative effects. The activity of tramadol is 1/10 - 1/6 of the morphine activity. Unlike morphine tramadol in therapeutic doses does not inhibit breathing, does not suppress the motility of the gastrointestinal tract and does not affect cardiovascular activity.

Pharmacokinetics:Binding to plasma proteins is about 20%. Penetrates through the placental barrier (concentration in the blood of the umbilical vein is 80% of the concentration in the blood of the mother). Biotransformation is carried out in the liver by demethylation and conjugation with the formation of 11 metabolites (1 of them is active). It is excreted mainly by the kidneys (90%) and the intestines (about 10%). If the liver and kidney function is impaired (creatinine clearance less than 80 ml / min), the secretion slows down.

Indications:

- acute and chronic pain syndrome of strong and moderate intensity of various genes (malignant tumors, traumas, severe neuralgia, acute myocardial infarction, etc.);

- painful diagnostic and therapeutic manipulations.

Contraindications:

- hypersensitivity to any component of the drug;

- acute alcohol poisoning; analgesics, sleeping pills and psychopharmacological agents;

- treatment with monoamine oxidase inhibitors (MAO) and within 14 days after the end of this treatment;

- as a substitution therapy for drug addiction;

- children under 1 year.

Carefully:

- opioid addiction (dependence on opioids);

- disorders of unclear genesis;

- conditions accompanied by respiratory depression, craniocerebral trauma, as well as in conditions accompanied by increased intracranial pressure, if the patient is not on artificial ventilation of the lungs;

- epilepsy or penchant for convulsive seizures. In patients with epilepsy or prone to the occurrence of convulsive seizures, the drug is used only in exceptional cases;

- patients with hypersensitivity to opioids,

- at patients on a background of pains in an abdominal cavity of an obscure genesis ("an acute stomach").

Pregnancy and lactation:

Tramadol penetrates the placental barrier. In small amounts (0.1% of the concentration in the blood plasma) enters the mother's milk.In this regard, therapy during pregnancy should be limited to individual single doses. Long-term use during pregnancy should be avoided because of the risk of developing addiction in the fetus and the possibility of a withdrawal syndrome in the neonatal period.

The use of tramadol immediately before or during labor does not affect the contractile function of the uterus. In these cases, the newborn can observe a change in the frequency of respiratory movements, which is insignificant for clinical practice.

The use of tramadol directly in the lactation period in the form of single doses does not require the interruption of breastfeeding.

Dosing and Administration:Intravenous, intramuscular and subcutaneous. When administered intravenously tramadol injected slowly (not more than 1 ml of solution per minute), which corresponds to 50 mg of tramadol. To dilute the drug can use water for injection, saline and 5% solution of dextrose.

Dilute Tramadol water to obtain a final concentration

1 ml of the drug contains 50 mg of tramadol

volume of preparation (ml)	volume of water for injection (ml)	the concentration obtained (mg / ml)
1	1	25
1	2	16,7
1	3	12,5
1	4	10
1	5	8,3
1	6	7,1
1	7	6,3
1	8	5,6
1	9	5

2 ml of the drug contains 100 mg of tramadol

volume of preparation (ml	volume of water for injection (ml)	the concentration obtained (mg / ml)
2	2	25
2	4	16,7
2	6	12,5
2	8	10
2	10	8,3
2	12	7,1
2	14	6,3
2	16	5,6
2	18	5

The recommended doses are indicative. In practice, it is necessary to choose the minimum analgesic effective doses. The duration of treatment with the drug is determined individually. Do not use longer than the term justified from a therapeutic point of view.

Adults and adolescents with 14 years of age: single dose of 50-100 mg, it is possible to re-administer the drug after 4-6 hours. The maximum daily dose is 400 mg.

Children from 1 to 14 years: a single dose of 1-2 mg / kg of body weight, the maximum daily dose of 8 mg / kg. Patients with impaired renal and / or liver function:

In patients with impaired renal and / or liver function, it is difficult to remove tramadol from the body. In the case of treatment of acute pain syndromes in such patients, when a rare or single administration of tramadol is required, no special dosage adjustment is required. However, in the case of chronic pain treatment, it is necessary to remember the danger of cumulation of the drug in the body, so it is advisable to increase the intervals between its individual methods. The drug should be administered with caution to patients with impaired renal function (50-100 mg 2 times a day),as well as individuals with cirrhosis of the liver (in this group of patients, the half-life of tramadol is almost 3-fold increased).

Patients of senile age

In patients of senile age (over 75 years), the excretion of tramadol is slowed from the body, even when there are no clinical manifestations of renal and / or liver dysfunction. In these patients, it is also necessary to increase the intervals between individual doses of the drug. It is recommended not to exceed the daily dose of 300 mg.

Side effects:

From the cardiovascular system: tachycardia, lowering blood pressure (right up to the orthostatic collapse), syncopal states.

From the gastrointestinal tract: nausea, vomiting, dry mouth, abdominal pain, anorexia, flatulence, constipation.

From the nervous system: weakness, increased fatigue, inhibition, paradoxical stimulation of the central nervous system (nervousness, agitation, emotional lability), confusion, instability of gait, violation of coordination of movements.

From the digestive side system: diarrhea, difficulty in swallowing. From the side urinary system: retention of urine.

On the part of organs feelings: impaired vision, taste.

Allergic reactions: skin reactions (itching, exanthema) until anaphylactic shock. Psychic sphere: anxiety, impaired coordination, euphoria or depression, miosis, sleep disorders, cognitive impairment, paresthesia, tremor, amnesia, convulsions, hallucinations, respiratory depression, sedation of varying severity, dizziness, headache, increased muscle tone.

Other: increased sweating, dyspnea, violation of the menstrual cycle. With long-term use - drug dependence, with a sharp cancellation - withdrawal syndrome. It was reported that the course of bronchial asthma worsening, however, there was no evidence of a negative effect of tramadol on the course of asthma.

Overdose:

Symptoms: miosis or mydriasis, vomiting, tachycardia, increased blood pressure, collapse, depression, up to coma, respiratory depression (up to apnea). Treatment: ensuring airway patency (intubation), maintaining breathing and cardiovascular system.

Antidote for oppression of the respiratory center is naloxoneRepeated dosesthe duration of its action is shorter than that of tramadol. To stop the seizure syndrome, benzodiazepines are used.

Interaction:

With the simultaneous use of tramadol and:

- drugs that depress the central nervous system, especially antidepressants, as well as alcohol, the side effects of tramadol are increased with respect to the central nervous system;

- drugs that can provoke convulsive seizures or enhance convulsive readiness (eg, antipsychotics and antidepressants), in very rare cases, you can observe epileptic seizures. The risk of seizures is increased with high doses of tramadol;

- carbamazepine decreases and the analgesic effect of tramadol is reduced;

- quinidine increases the plasma concentration of tramadol;

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

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

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

MAO inhibitors, furazolidone, procarbazine increase the risk of convulsions (decrease convulsive threshold).

Pharmaceutically incompatible with solutions of diclofenac, indomethacin, phenylbutazone, diazepam, flunitrazepam, nitroglycerin.

Special instructions:During the treatment it is necessary to exclude the use of alcohol and refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection 50 mg / ml.

Packaging:

Ampoules of 1ml or 2ml. For 10 ampoules together with a knife ampulnym or scarifier ampoule and instructions for use in a cardboard bundle. 5 ampoules per 1 ml or 2 ml in a contour cell package.

1 or 2 contour mesh packages together with a knife ampoule or scarifier ampoule and instructions for use are placed in a pack of cardboard.

Storage conditions:It refers to the list of No. 1 potent BACO substances. In a dry, dark place at a temperature of 15 to 25 ° C. Keep out of the reach of children.

Shelf life:

5 years. Do not use at the end of the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001820 / 01

Date of registration:18.07.2008

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)