sol.Reblaks

Indications for use:

Brand name:

Reblaks

INTERNATIONAL NONPROPRIETARY NAME:

Thiocolchicoside

Drug form:

Solution for injections

Description:

Clear yellow colour solution

Composition:

One ampule contains solution for injections (2 ml):

Active substance: thiocolchicoside – 4 mg;

Excipients: sodium chloride, hydrochloric acid, water for injection.

ATC Code: M03BX05

Pharmacotherapeutic group:

Muscle relaxants. Centrally acting agents

Pharmacological properties

Pharmacodynamics:

Reblaks contains thiocolchicoside as an active substance, a semi-synthetic muscle relaxant obtained from natural glycoside colchicoside. Thiocolchicoside exhibits selective affinity to gamma-aminobutyric acid (GABA) and glycine receptors determining drug effect at various levels of nervous system, both with local spasms and spasms of central origin.

Reblaks does not possess similar to curare effect, thus does not induce paralysis and does not affect cardiovascular and respiratory systems.

Pharmacokinetics:

Distribution

After intramuscular administration thiocolchicoside C_max is obtained in 30 min and reached 113 ng/ml for the dose 4 mg and 175 ng/ml for the dose 8 mg. AUC values are 283 and 417 ng.h /ml, respectively. Pharmacologically active metabolite thiocolchicoside SL18.0740 is determined at lower concentrations with C_max 11.7 ng/ml in 5 hours after injection with AUC of 83 ng.h /ml. There are no data on pharmacokinetics of an inactive metabolite SL59.0955 after thiocolchicoside intramuscular administration.

Distribution

The apparent volume of distribution of thiocolchicoside is approximately 42.7 l after intramuscular administration at a dose of 8 mg. There is no data on metabolites distribution after thiocolchicoside intramuscular administration.

Excretion

After thiocolchicoside intramuscular injection T_1/2 is 1.5 hours and plasma clearance is 19.2 l/h.

Indications for use:

Reblaks is used in rheumatology for additional treatment of painful muscle contractures.

Contraindications:

- hypersensitivity to the drug components;

- muscle hypotension;

- mild paralysis;

- children over 16 years;

- pregnancy;

- lactation period;

- women of reproductive age not using contraception.

Dosage and administration:

Reblaks is used intramuscularly. The recommended and maximum dose is 4 mg every 12 hours (i.e., 8 mg per day). The treatment period should not exceed 5 days.

Do not exceed recommended doses and treatment period.

Side effect:

Immune system disorders: hypersensitivity reactions; infrequently: urticaria; rarely: anaphylactic shock after intramuscular administration, Quincke’s edema.

Skin and subcutaneous tissue disorders: infrequently: erythema (at the injection site).

Nervous system disorders: often: drowsiness; very rarely: irritation; unknown frequency: convulsions.

Cardiovascular system disorders: rarely: arterial hypotension; unknown frequency: vasovagal syncope (usually within a few minutes after intramuscular injection).

Gastrointestinal tract disorders: often: diarrhea, gastralgia; infrequently: nausea, vomiting.

Precautionary measures:

Reblaks should be used with caution in case of kidney or liver disorders. Thiocolchicoside can cause seizures in patients with epilepsy or risk of seizures.

In this regard it is necessary to avoid the recommended doses excess and treatment duration.

Effect on ability to drive and use machinery:

During the treatment period, care must be taken when driving vehicles, controlling machinery and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Pregnancy use:

The drug is contraindicated in pregnancy and women of childbearing age who do not use contraception.

Lactation period:

Due to the fact that thiocolchicoside passes into the breast milk its use in lactation period is prohibited.

Fertility:

Thiocolchicoside and its metabolites in different concentrations can cause aneuploidy, which may be a risk factor of fertility decrease in humans.

Pediatric Use:

For safety reasons the drug should not be used in children and adolescents under 16 years.

Overdose:

There is no data on overdose.

Symptoms: may increase side effects.

Treatment: symptomatic therapy.

Interaction with other drugs:

There are no data on drug interactions, but caution is advised when taken concomitantly with other muscle relaxants.

Concomitant use of drugs depressing the central nervous system, including alcohol, antihypertensive drugs, curare-like drugs, can increase muscle relaxation and depression of the central nervous system, as well as hypotension development.

Concomitant use of anticoagulants increases the risk of bleeding.

Interaction with other drugs:

There are no data on drug interactions but caution is advised when taken concomitantly with other muscle relaxants.

Concomitant use with drugs depressing the central nervous system, including alcohol, antihypertensive drugs and curare-like drugs can cause muscle relaxation increase and central nervous system depression as well as hypotension aggravation.

Concomitant use of anticoagulants increases the risk of bleeding.

Storage conditions:

Store in a place protected from sunlight at a temperature not higher than 25°С

Keep out of reach of children!

Shelf-life:

Shelf life is 3 years. Do not use after an expiry date indicated on the pack.

Prescription Status:

By prescription

Packaging

Solution for injection, 2 ml in ampules made of clear glass.

6 ampoules made of clear glass, 2 ml each are placed into a polyvinyl chloride separator.

Manufacturer Information

Foreign production and trade unitary enterprise “Reb-Pharma”, 223216, Republic of Belarus, Minsk region, Chervensky district, Smilovichi, Sadovaya st., 1, tel./fax: (+375) 17 240 26 35,

e-mail: rebpharma@rebpharma.by, http://www.rebpharma.by