Baclofenum

General characteristics. Structure:

Active agent: Baclofenum of 10 mg

Other ingredients: lactose, starch corn, gelatin, talc, magnesium stearate, ethyl cellulose.

Active agent: Baclofenum of 25 mg

Other ingredients: lactose, starch corn, gelatin, talc, magnesium stearate, ethyl cellulose.

Pharmacological properties:

Muscle relaxant with the central mechanism of action of group of derivatives of chlorphenyl-butyric acid.
Reduces the raised tone of skeletal muscles caused preferential by damage of a spinal cord. Baclofenum oppresses cutaneous reflexes and a tone of muscles, slightly reduces amplitude of tendon jerks. Pharmacological effect of drug, perhaps, is caused by hyperpolarization of the ascending nerve fibrils and oppression of both monosinaptichesky, and polisinaptichesky reflexes at the level of a spinal cord. Baclofenum does not influence neuromuscular transmission processes. As use of Baclofenum in high doses can cause TsNS function oppression, influence of drug on the centers located supraspinalno is not excluded.
After intake Baclofenum is quickly and completely soaked up in a GIT. Therapeutic concentration makes 80–395 ng/ml. Cmax in a blood plasma (500–600 ng/ml) is reached later 2–3 h after oral administration. Then concentration is maintained at the level of 200 ng/ml during 8 h.
Baclofenum gets into many fabrics, but only its insignificant part passes through GEB. Baclofenum gets through a placental barrier. The minimum quantity of drug gets to breast milk. Baclofenum contacts proteins of a blood plasma approximately for 30%. About 15% of the accepted dose of drug are metabolized in a liver by means of deamination. Т½ makes 2,5–4 h. From 70 to 80% of Baclofenum are removed with urine in not changed look or in the form of metabolites, the rest — with a stake. Drug is almost completely removed from an organism during 72 h after reception.

Indications to use:

The chronic serious spastic condition of skeletal muscles arising owing to multiple sclerosis or a traumatic rupture of a spinal cord.

Route of administration and doses:

Inside (it is better during food).
The recommended doses for adults
Initial dose — 5 mg 3 times a day within 3 days, then for every 4th day of treatment raise a single dose on 5 mg (frequency rate of reception — 3 times a day) to achievement of an optimum dose in 20–25 mg 3 times a day. The recommended scheme of reception:
The 1-3rd day — on 5 mg (1/2 tablets on 10 mg) 3 times a day;
The 4-6th day — on 10 mg (1 tablet) 3 times a day;
The 7-9th day — on 15 mg (1 1/2 tablets on 10 mg) 3 times a day;
The 10-12th day — on 20 mg (2 tablets on 10 mg) 3 times a day.
At most of patients therapeutic effect note after use of drug in a dose 30–75 mg/days.
If necessary the dose can be raised gradually. It is desirable for the patients needing the raised doses (a daily dose of 75-100 mg) to appoint the tablets containing 25 mg of Baclofenum.
The daily dose of drug should not exceed 100 mg. Duration of treatment depends on a clinical condition of the patient. Administration of drug should not be interrupted suddenly as in this case there can be hallucinations and become aggravated spastic states. In need of cancellation of Baclofenum its dose is reduced gradually.
Patients of advanced age should raise a dose of drug with extra care as the risk of emergence of side reactions at them is higher.
The recommended doses for children:
The usual daily dose of drug makes 0,75–2 mg/kg of body weight. Treatment it is necessary to begin 5 mg which is accepted by 2 times a day with a dose. To children aged from 12 months up to 2 years appoint 10–20 mg/days, 2–6 years — 20–30 mg/days, 6–10 years — 30–60 mg/days. For children 10 years the maximum daily dose are more senior makes 2,5 mg/kg of body weight. If necessary it is possible to raise a dose carefully each 3 days to obtaining optimum therapeutic effect.
The recommended doses for patients with an impaired renal function:
To patients with an impaired renal function, and also to the patient who are on a hemodialysis, the dose of drug is reduced to 5 mg/days.

Features of use:

During treatment by Baclofenum the aggravation of psychotic syndromes, schizophrenia, spasms and emergence of a condition of a disorientation in time and space is possible. Such patients need to appoint drug carefully and under careful medical observation.
The dose of drug needs to be reduced gradually during 1–2 weeks as after sudden cancellation of treatment uneasiness and confusion of consciousness, a hallucination, psychosis, a maniacal syndrome, paranoia and convulsions can develop, increase in expressiveness of spastic symptoms is possible.
With care appoint Baclofenum to patients with a renal failure or a liver (the dose is reduced depending on extent of disturbance); to patients of advanced age (there is an increased risk of emergence of undesirable reactions); the patient with epilepsy (also EEG-control as revealed cases of decrease in efficiency of anticonvulsant treatment and change in the chart EEG is necessary careful clinical); to persons who have a maintenance of vertical position of a body balances or increase in motive amplitude depend on a tone of muscles; to the patients receiving anti-hypertensive treatment (possibility of hypotension); the patient with a stroke, disturbance of respiratory function; to patients with the raised bladder sphincter tone (the ischuria is possible).
At treatment by Baclofenum in a blood plasma can raise concentration of ALAT, ShchF or glucose. Constant laboratory control, especially at patients with abnormal liver functions and patients with a diabetes mellitus is recommended.
Baclofenum gets through a placental barrier. Due to the lack of data on use of drug during pregnancy it is necessary to accept Baclofenum only in urgent cases. Before purpose of Baclofenum it is necessary to weigh carefully potential advantage and possible risk both for mother, and for a fruit. Baclofenum is allocated with milk therefore during administration of drug feeding is not recommended by a breast.
At administration of drug can note the symptoms caused by its sedative action and ability to reduce concentration of attention. In this case it is not recommended to manage vehicles or to work with potentially dangerous mechanisms.

Side effects:

Arise after sudden increase in a dose, administration of drug in high doses or at patients of advanced age more often. In most cases after a drug dose decline they weaken and disappear. In case of serious side effects treatment needs to be stopped.
From TsNS: 10–63% — drowsiness; 5–15% — вертиго; 4–12% — nausea; 1–11% — confusion of consciousness; 4–8% — a headache; 2–7% — sleeplessness; 2–4% — weakness and increased fatigue; seldom — euphoria, hypererethism, a depression, hallucinations, paresthesia, pain and weakness in muscles, an ataxy, dryness in a mouth, exhaustion, a tremor, an adynamy, oppression of function of respiratory and cardiovascular system, a disorientation in space, dizziness, vomiting, adaptation disturbance, nightmares, a nystagmus, decrease in a convulsive threshold and development of a convulsive attack (especially at patients with epilepsy).
From cardiovascular system: 0–9% — arterial hypotension; seldom — диспноэ, tachycardia, a stethalgia, a syncope.
From the alimentary system: 2–6% — a lock; seldom — anorexia, a dysgeusia, an abdominal pain, diarrhea, positive takes of the test for existence of the occult blood in Calais.
From urinogenital system: 2–6% — frequent desires to an urination.
Others: vision disorder and taste, rash, itch, ankle hypostasis, excessive sweating, increase in body weight, feeling of a congestion of a nose, change of level of glucose in a blood plasma and other biochemical indicators. At some patients noted an aggravation of spastic states (paradoxical reaction to medicine).

Interaction with other medicines:

At simultaneous use of Baclofenum with the drugs influencing TsNS, and alcohol strengthening of sedative action is possible; with lithium salts — increase in expressiveness of hyperkinetic symptoms; with tricyclic antidepressants — strengthening of action of Baclofenum with considerable decrease in a tone of muscles; with anti-hypertensive drugs — strengthening of hypotensive action (dose adjustment can be required); with drugs which use can lead to a renal failure (for example an ibuprofen) removal of Baclofenum is slowed down and its toxic effects can amplify; with a levodopa, karbidopy — at patients with Parkinson's disease manifestation of confusion of consciousness, hallucinations and a hyperexcitability is possible; with fentanyl — the anesthetizing action of the last is prolonged.

Contraindications:

Hypersensitivity to drug components, a round ulcer.

Overdose:

Acute intoxication Baclofenum can be followed by sleeplessness, a loss of consciousness, a coma, breath disturbance. Also dizziness, hallucinations, uneasiness, accommodation disturbance, loss of a pupillary reflex, a hypomyotonia, clonic spasms, a hyporeflexia or an areflexia, spasms, a peripheral vazodilatation, bradycardia, decrease in body temperature, nausea, vomiting, diarrhea, hypersalivation, increase in the LDG, ALAT and ASAT levels can develop.
Treatment: it is necessary to wash out a stomach and to accept absorbent carbon. If necessary apply salt laxatives. The patients who are in coma before a gastric lavage need to be intubated. Hold events for maintenance of functions of respiratory and cardiovascular systems. There is no specific antidote.
In case of slight intoxication for elimination of the undesirable phenomena from TsNS, especially at sleeplessness and respiratory depression, in/in enter physostigmine. Apply an artificial diuresis to strengthening of removal of Baclofenum from an organism. At spasms it is shown careful in/in administration of diazepam.

Storage conditions:

In the dry, protected from light place at a temperature up to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tab. of 10 mg, No. 50

Tab. of 25 mg, No. 50.