Similar drugsTo uncover
Dosage form: & nbspDrops for oral administration.
Composition:

1 ml of drop for oral administration contains:

Active substance:

Tramadol hydrochloride 100.00 mg

Excipients: sucrose, glycerol, propylene glycol, polysorbate-20, potassium sorbate, sodium saccharinate dihydrate, peppermint flavor, anise flavor, purified water.

Description:Transparent colorless or slightly brownish solution with a characteristic smell of mint and anise.
Pharmacotherapeutic group:An analgesic with a mixed mechanism of action.
Pharmacodynamics:
Opioid synthetic analgesic, which has a central effect and action on the spinal cord (contributes to the discovery of potassium and calcium channels, causes hyperpolarization of membranes and inhibits pain impulses), enhances the action of sedative drugs. Activates opioid receptors (mu, delta, kappa) on the pre- and postsynaptic membranes of the afferent fibers of the nociceptive system in the brain and gastrointestinal tract (GI tract). Slows down the destruction of catecholamines, stabilizes their concentration in the central nervous system (CNS).
Tramadol is a racemic mixture of 2 enantiomers - dextrorotatory (+) and levorotatory (-), each of which exhibits a different receptor affinity.
The dextrorotatory enantiomer of tramadol is a selective agonist of mu-opioid receptors, and selectively inhibits the reverse neuronal capture of serotonin, while the levorotatory inhibits the reverse neuronal seizure of norepinephrine. Mono-O-desmethyltramadol (Ml metabolite) also selectively stimulates mu-opioid receptors.
The affinity of tramadol for opioid receptors is ten times weaker than that of codeine, and 6000 times weaker than morphine. Expression of analgesic action is 5-10 times weaker than morphine.
Analgesic effect is due to a decrease in nociceptive activity and an increase in the antinociceptive systems of the body.
Oppresses the respiratory center, excites the start zone of the vomiting center, the nucleus of the oculomotor nerve.

Pharmacokinetics:
Absorption - 90%, with oral bioavailability - 75% (increases with repeated use). Time to reach the maximum concentration (TCmax) after ingestion - 1 h, Ml metabolite - 3 h.
Penetrates through blood-brain and placental barriers, 0.1% of tramadol is excreted in breast milk. The volume of distribution is 306 liters, the connection with plasma proteins is 20%.
In the liver, it is metabolized by N- and O-demethylation followed by conjugation with glucuronic acid.11 metabolites have been identified, of which mono-O-desmethyltramadol (Ml) has pharmacological activity. The half-life (T1 / 2) in the second phase is 6 h (tramadol), 7.9 h (mono-O-desmethyltramadol); 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 hours (mono-O-desmethyltramadol), in severe cases -22.3 hours and 36 hours, respectively; with chronic renal failure (creatinine clearance (CK) less than 5 ml / min) - 11 ± 3.2 h (tramadol), 16.9 ± 3 h (mono-O-desmethyltramadol), 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 of strong and moderate intensity of different etiology (including trauma, postoperative period, pain in cancer patients);

- anesthesia in the conduct of painful diagnostic and therapeutic manipulations.
Contraindications:
-increased sensitivity to tramadol and other analgesics;
-States accompanied by respiratory depression or severe depression of the central nervous system (including poisoning with alcohol, hypnotic drugs,narcotic analgesics and other psychoactive drugs);
-pharmacoresistance epilepsy;
-generous renal and / or hepatic insufficiency (CC less than 10 ml / min);
- The use of tramadol as a drug for the treatment of the syndrome of "withdrawal" of drugs;
-Children under 1 year;
- simultaneous application of monoamine oxidase inhibitors (MAO) and within 14 days after their cancellation;
- suicidal tendencies, propensity to abuse of psychoactive substances;
- pregnancy, lactation period (during pregnancy and during breastfeeding, the application is possible only for life indications);
-Sugarase / isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption.
Carefully:Disturbance of renal function (QC 10-30 ml / min) and / or liver, craniocerebral trauma, disorders of consciousness of various genesis, convulsions, intracranial hypertension, epilepsy, abdominal pain of unclear genesis "acute" abdomen, simultaneous application with selective inhibitors re-uptake of serotonin (some antidepressants and drugs that reduce appetite), tricyclic antidepressants,other tricyclic compounds (for example, trimetasin), antimigrenous drugs (triptans), narcotic analgesics, neuroleptics and other drugs that reduce the threshold of convulsive activity, a propensity for dependence (alcoholism, drug or drug dependence).
Pregnancy and lactation:
Safety of use during pregnancy is not established. High doses can have adverse effects on the fetus and the newborn. The application is possible only under the strictest medical supervision and in individual, exceptional cases, if the potential benefit to the mother justifies the risk to the child.
It should be taken into account that during lactation approximately 0.1% of the dose is secreted into breast milk.
Dosing and Administration:

Inside. The dose depends on the severity of the pain syndrome and the individual sensitivity of the patient. The time of taking the drug does not depend on the time of eating. Adults and adolescents over 12 years of age:

A single dose is 20-40 drops (equivalent to 50 mg) of tramadol. In case of insufficiency or in the absence of an analgesic effect, after 50-60 minutes, 50 mg of tramadol is taken repeatedly.

In severe pain syndrome, a higher single dose of tramadol (100 mg) may be administered as the initial dosage.

The daily dose is up to 160 drops for ingestion Tramadol.

Children 1-12 years old:

As a single dose appoint 1-2 mg of tramadol per 1 kg of body weight. The maximum daily dose for children is 4-8 mg / kg / day.

The table shows typical dosing regimens for different age groups of children (1 drop contains 2.5 mg of tramadol):

Age

Body mass

Number of drops

1 year

10 kg

4-8

3 years

15 kg

6-12

6 years

20 kg

8-16

9 years

30 kg

12-24

12 years

45 kg

18-36

Patients with impaired renal and / or liver function:

In patients with impaired renal and / or liver function tramadol can last longer due to possible lengthening T1/2. For such patients, the doctor may recommend an increase in the interval between taking single doses. With QC less than 30 ml / min and in patients with hepatic insufficiency, an interval of 12 hours between taking the next doses of the drug Tramadol.

The drug should be administered with caution to patients with impaired renal function (50-100 mg twice a day), as well as individuals with cirrhosis (in this group of patients with T1/2 tramadol increases almost 3 times).

Patients older than 75 years

In patients older than 75 years, the excretion of tramadol is slowed from the body, even when there are no clinical manifestations of renal and / or hepatic impairment. These patients also need to increase the interval between taking the drug. Do not exceed the maximum daily dose - not more than 160 drops for oral administration.

Side effects:

Classification of the incidence of adverse events (WHO):

very often> 1/10

often from> 1/100 to <1/10

infrequently from> 1/1000 to <1/100

rarely from> 1/10000 to <1/1000

very rarely from <1/10000, including individual messages.

From the central and peripheral nervous system:

Often: dizziness;

Often: headache;

Infrequently: anxiety, confusion, drowsiness;

Rarely: euphoria, emotional instability, sleep disturbance, nightmares, cognitive disorders, hallucinations, amnesia; disorders of coordination, convulsions, paresthesia, tremor, attention deficit disorder, epileptiform seizures, with prolonged use - the development of drug dependence;

Rarely: panic attacks, ringing in the ears;

From the side of the cardiovascular system:

Rarely: tachycardia, palpitations, cardiovascular collapse, fainting,

orthostatic hypotension, cardiovascular failure;

Rarely: bradycardia, arterial hypertension;

From the respiratory system:

Rarely: shortness of breath, respiratory depression, pulmonary edema;

From the sense organs:

Rarely: decreased visual acuity, sometimes mydriasis, a taste disorder;

From the digestive system:

Often: nausea;

Often: vomiting, constipation or diarrhea, dryness of the oral mucosa;

Infrequently: dyspepsia, abdominal pain, bloating;

Rarely: difficulty in swallowing;

Rarely: increased activity of "liver" transaminases;

From the skin:

Often: sweating;

Infrequently: skin rash, itchy skin;

Rarely: hives;

From the genitourinary system:

Infrequently: urinary retention, increased frequency of urination, menstrual irregularity, signs of menopause;

Rarely: dysuria;

From the musculoskeletal system:

Rarely: muscle weakness;

From the side of metabolism:

Infrequently: anorexia;

Rarely: decreased body weight;

Allergic Reagents:

Rarely: allergic reactions manifested by dyspnea, bronchospasm, wheezing, and also angioedema.

Other: with prolonged use - drug dependence; with a sharp abolition - the "cancellation" syndrome.

Overdose:
Symptoms: impaired consciousness (up to coma), seizures, lowering blood pressure, tachycardia, narrowing or dilating the pupils, respiratory depression.
Treatment: with severe intoxication with loss of consciousness and superficial, mild breathing, it is necessary to introduce antagonists of opioid receptors (naloxone), and with cerebral convulsions - preparations of benzodiazepine series (diazepam), intravenously. Hemodialysis is ineffective. Excretion of tramadol by hemodialysis is about 7%.
Interaction:

Tramadol can not be used concomitantly with MAO inhibitors or within 2 weeks after they are discontinued.

With the simultaneous use of substances acting on the central nervous system (anesthetics, antidepressants, antipsychotics, sedatives, anxiolytics, hypnotics) or with the use of alcohol, there is a possibility of a synergistic effect, manifested by excessive sedation and increased analgesic effect. Tramadol strengthens the action JIC, depressing central nervous system, and ethanol.

Inductors of microsomal oxidation (incl. carbamazepine, barbiturates) reduce the severity of the analgesic effect and the duration of the action. Due to the increased risk of seizures, the simultaneous use of carbamazepine and tramadol is not recommended. 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 AC (antipsychotics) increase the risk of seizures (reduction of the convulsive threshold). Quinidine increases the plasma concentration of tramadol and reduces Ml metabolite due to competitive inhibition of isoenzyme CYP2D6.

Inhibitor inhibitors CYP2D6 (such as fluoxetine, paroxetine and amitriptyline) reduce the metabolism of tramadol.

Selective serotonin reuptake inhibitors (some antidepressants and LC, reducing appetite), tricyclic antidepressants, other tricyclic compounds (for example, promethazine), antimigraine AC (triptans), narcotic analgesics, MAO inhibitors, neuroleptics, etc.C, reducing the threshold of convulsive readiness, increase the risk of seizures.

Selective serotonin reuptake inhibitors, serotonin and noradrenaline reuptake inhibitors, tricyclic antidepressants, MAO inhibitors, antimigraine AC (triptans) and AC, disturbing metabolism of tramadol (inhibitors of isoenzymes CYP2D6 and CYP3A4), when combined with tramadol can cause serotonin syndrome (confusion, agitation, hyperthermia, sweating, ataxia, hyperreflexia, myoclonus, diarrhea). The abolition of serotonergic drugs causes rapid relief of the symptoms of serotonin syndrome.

Caution should be exercised with simultaneous therapy with tramadol and coumarin derivatives (eg, warfarin), since there are reports of an increase in the international normalized ratio (MHO) and the appearance of ecchymoses in some patients.

Pre- or post-operative use of an anti-emetic agent, a 5-HTZ-serotonin receptor antagonist, increases the need for tramadol in patients with postoperative pain syndrome.

Special instructions:Tramadol can be used in patients with hypersensitivity to opioids, but with great caution.
Tramadol should be avoided for those who are addicted to addiction (alcoholism, drug or drug dependence). With the use of tramadol, the risk of suicide increases.
With the development of severe adverse effects should stop taking the drug.
Patients with cramps should remain under close medical supervision during drug treatment and within a few days after discontinuation. Tramadol It is not suitable as a substitute therapy for opioid dependence. In patients with impaired liver function due to reduced hepatic clearance, the concentration of tramadol in the blood serum increases and its T1 / 2 increases. Such patients are recommended smaller doses and / or increased intervals between drug intake Tramadol.
Tramadol can, but with great caution, be used in patients with elevated intracranial pressure and a traumatic brain injury in the anamnesis.
Effect on the ability to drive transp. cf. and fur:A drug Tramadol can cause disturbance of concentration of attention, hallucinations, confusion, dizziness and other side effects, therefore during drug treatment it is necessary to refrain from driving and other potentially dangerous activities requiring high concentration of attention and speed of psychomotor reactions.
Form release / dosage:
Drops for oral administration, 100 mg / ml.
Packaging:
10 ml of the preparation in a bottle of amber glass (type III, Ph.Eur.) With a built-in dropper of low-density polyethylene and a screw cap of polypropylene type "push and open" with control of the first opening.
1 bottle is placed in a pack of cardboard along with instructions for use.
Storage conditions:
At temperatures not higher than 30 ° C, in the original packaging. Keep out of the reach of children.
The drug belongs to the list of No. 1 potent substances of the Standing Committee on Drug Control of the Ministry of Health and Social Development.
Shelf life:Do not use the drug after the expiration date.
Terms of leave from pharmacies:On prescription
Registration number:П N012155 / 03
Date of registration:03.12.2010
The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
Manufacturer: & nbsp
KRKA, d.d. Slovenia
Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
Information update date: & nbsp15.09.2015
Illustrated instructions
    Instructions
    Up