Universal reference book for medicines
Product name: LOXIDONE PLUS (LOKSIDONE PLUS)

Active substance: pyridoxine, terizidone

Type: Anti-TB drug

Manufacturer: FARMASINTEZ (Russia)
Composition, form of production and packaging
Capsules
number 1, hard gelatin, capsule body white, cap capsule yellow.

1 caps.

terizidone 150 mg

pyridoxine hydrochloride 10 mg

Excipients: lactose 5 mg, silicon colloidal dioxide (aerosil) 4 mg, talc 5 mg.

The composition of the capsules: purified water 14-15 mg, sodium lauryl sulfate 0.24 mg, methyl parahydroxybenzoate 0.8 mg, propyl parahydroxybenzoate 0.2 mg, titanium dioxide 1.1252 mg -2.05 mg, quinoline yellow 0.0562 mg, gelatin up to 100 mg.

10 pieces.
- packings of cellular contour (1) - packs cardboard.
10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (3) - packs cardboard.
30 pcs.
- polymer cans (1) - packs of cardboard.
60 pcs.
- polymer cans (1) - packs of cardboard.
100 pieces.
- polymer cans (1) - packs of cardboard.
120 pcs.
- polymer cans (1) - packs of cardboard.
Capsules number 0, hard gelatinous, capsule body green, cap capsule blue.

1 caps.

terizidone 250 mg

pyridoxine hydrochloride 10 mg

Excipients: lactose 15 mg, silicon dioxide colloid (aerosil) 6.7 mg, talc 8.3 mg.

The composition of the capsules: purified water 14-15 mg, sodium lauryl sulfate 0.24 mg, methyl parahydroxybenzoate 0.8 mg, propyl parahydroxybenzoate 0.2 mg, indigocarmine 0.15 mg, quinoline yellow 0.2656 mg, titanium dioxide 1.1252 mg -2.6256 mg, gelatin up to 100 mg.

10 pieces.
- packings of cellular contour (1) - packs cardboard.
10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (3) - packs cardboard.
30 pcs.
- polymer cans (1) - packs of cardboard.
60 pcs.
- polymer cans (1) - packs of cardboard.
100 pieces.
- polymer cans (1) - packs of cardboard.
120 pcs.
- polymer cans (1) - packs of cardboard.
Capsules №00, hard gelatin, capsule body white, cap capsule red.

1 caps.

terizidone 300 mg

pyridoxine hydrochloride 10 mg

Excipients: lactose 20 mg, silicon dioxide colloid (aerosil) 8 mg, talc 10 mg.

The composition of the capsules: water purified 14-15 mg, sodium lauryl sulfate 0.24 mg, methyl parahydroxybenzoate 0.8 mg, propyl parahydroxybenzoate 0.2 mg, dye azorubin 0.7501 mg, titanium dioxide 0.375 mg - 2.05 mg, gelatin up to 100 mg.

10 pieces.
- packings of cellular contour (1) - packs cardboard.
10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (3) - packs cardboard.
30 pcs.
- polymer cans (1) - packs of cardboard.
60 pcs.
- polymer cans (1) - packs of cardboard.
100 pieces.
- polymer cans (1) - packs of cardboard.
120 pcs.
- polymer cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

Terizidone

Terizidone is a broad-spectrum antibiotic, is a derivative of D-cycloserine.
Terizidone competitively blocks enzymes that incorporate alanine into alanyl-alanine dipeptide, the main component of the mycobacterium wall. Does not have cross-resistance with other anti-TB drugs. Terizidone has antibacterial activity against mycobacteria tuberculosis and bacteria that cause urinary tract infections including strains of bacteria that become resistant to other antibiotics. The minimum inhibitory concentration of terisidone for sensitive strains is 4-250 mg / l, including 10-40 mg / L for mycobacterium tuberculosis, 8-32 mg / L for staphylococci, and 50-250 for gram-negative bacteria mg / l. The following bacteria are sensitive to terizidone: Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium, and Staphylococcus aureus, Staphylococcus epidermidis. To this preparation are also sensitive Enterococcus faecalis, Escherichia coli, Citrobacter, Enterobacter, Morganella morganii, Klebsiella pneumoniae, Pseuclomonas aeruginosa.
Pyridoxine

Pyridoxine acts as a coenzyme, participating in biochemical reactions, including the metabolism of amino acids and glycogen, in the synthesis of nucleic acids, hemoglobin, sphingomyelin and other sphingolipids, in the synthesis of the mediator serotonin, dopamine, norephedrine and gamma-aminobutyric acid.
Pyridoxine has an antineurotoxic effect. The use of pyridoxine reduces the side effects of the central nervous system.
PHARMACOKINETICS

Terizidone

Terizidone is absorbed from the gastrointestinal tract (GIT) quickly and almost completely - by 70-90%.
The intake does not affect the suction speed. After oral administration of 250 mg of terizidone, the maximum concentration in the blood plasma ( Cmax ) is about 6.5 μg / ml, the time to reach the maximum concentration (TC max ) is 2-4 hours. Widely distributed in tissues and body fluids, for example in the lungs, bile, penetrates into ascitic, pleural and synovial fluid, lymph, and saliva. Very well penetrates into the cerebrospinal fluid (concentration in the cerebrospinal fluid reaches 80-100% concentration in the blood serum), a higher concentration is noted in patients with inflammation of the meninges. When administered with terizidone at a dose of 250 mg, the high concentrations of the drug are found in the blood and urine, which makes it possible to use it for the treatment of urinary tract infections, incl. chronic forms.
Kidney excretion occurs slowly and evenly, the half-life period (T 1/2 ) is 24 hours. Slowed excretion of the drug by the kidneys results in a level of concentration of terisidone in the urine maintained for 12 hours, 60-70% of the drug is excreted unchanged by glomerular filtering.
A small amount is excreted by the intestine. The value of the elimination constant is -0.0262 h- 1 . A small amount of terizidone is metabolized, which causes a low / weak toxic effect on the kidneys. With renal failure, the period of the half-lead is prolonged to 72 hours.
Pyridoxine

Absorbed rapidly throughout the small intestine, a larger amount is absorbed in the jejunum.
Metabolised in the liver with the formation of pharmacologically active metabolites (pyridoxal phosphate and pyridoxamine phosphate). Pyridoxal phosphate binds to plasma proteins by 90%. It penetrates well into all tissues; accumulates mainly in the liver, less - in the muscles and central nervous system. Penetrates through the placenta, is secreted with breast milk. T 1/2 is 15-20 days. It is excreted by the kidneys, as well as by hemodialysis.
INDICATIONS

- tuberculosis of various forms and localizations in the complex therapy of drug-resistant forms of tuberculosis.

DOSING MODE

Inside, regardless of food intake (dose indicated by terizidon): adults and children over 14 years of age and body weight less than 60 kg - 300 mg twice a day (600 mg / day);
with a body weight of 60-80 kg - 300 mg three times a day (900 mg / day).
Adults with a body weight of more than 80 kg - 600 mg twice a day (1200 mg / day).

If the kidney function is violated (CC less than 30 ml / min), the dose of the drug and the frequency of administration are reduced: 250 mg once a day daily or 500 mg 3 times a week (for example, Monday, Wednesday, Friday).
When the creatinine concentration is more than 2 mg / dl, the drug is contraindicated.
The duration of treatment is 3-4 months.

The drug does not have the features of the action at the first reception or upon its cancellation.

Under no circumstances should you prematurely discontinue or temporarily discontinue a course of treatment started or take the medication irregularly.

If you miss a dose, you need to take the next dose of the drug at the set time, do not take a double dose.

SIDE EFFECT

To estimate the incidence of undesired reactions, the following grades are used: very often (> 1/10), often (> 1/100, <1/10), infrequently (> 1/1000, <1/100), rarely (> 1 / 10000, <1/1000), very rarely (<1/10000, including reports of single cases).

From the side of the central nervous system: rarely - headache, dizziness, increased excitability, tremor, insomnia, a feeling of intoxication;
very rarely - convulsions (including epileptic), dysarthria, mental disorders, such as mania or depression.
From the digestive tract: rarely - pain in the abdomen, flatulence and diarrhea.

Other: very rarely - allergic reactions, skin rash.

Due to the presence of pyridoxine (in addition): hypersecretion of hydrochloric acid, numbness and the appearance of pressure in the limbs (simtom "stocking" and "gloves"), reducing lactation.

CONTRAINDICATIONS

- hypersensitivity to terizidone or cycloserine, pyridoxine, as well as to any other component of the drug;

- organic diseases of the central nervous system, atherosclerosis of the brain;

- epilepsy, epileptic seizures (including in the anamnesis);

- disorders of the psyche (anxiety, psychosis, depression, including in the anamnesis);

- severe renal failure (creatinine concentration> 2 mg / dL);

- Alcoholism;

- children's age till 14 years;

- pregnancy, lactation period;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

Carefully

Elderly age, ischemic heart disease, impaired liver function, impaired renal function (QC less than 30 ml / min), chronic heart failure, peptic ulcer of the stomach and duodenum.

PREGNANCY AND LACTATION

The use of the drug during pregnancy is contraindicated.

The concentrations of terisidone in human milk are close to those in blood plasma.
In the case of the drug during lactation it is necessary to stop breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be given to patients with impaired renal function (QC less than 30 ml / min). When the creatinine concentration is more than 2 mg / dl, the drug is contraindicated.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution should prescribe the drug to patients with impaired liver function


APPLICATION FOR CHILDREN

Contraindicated in children under 14 years.

APPLICATION IN ELDERLY PATIENTS

Caution should be given to elderly patients.

SPECIAL INSTRUCTIONS

The use of the drug against the background of alcohol is associated with an increased incidence of side effects, up to the development of seizures, so during the intake of the drug should avoid alcohol.

The use of the drug simultaneously with cycloserine is prohibited because of a possible overdose.

Terizidone can cause a deficiency of cyanocobalamin and / or folic acid, in these cases it is necessary to conduct an appropriate examination and treatment of the patient.

It is recommended to take together with glutamic acid in a dose of 500 mg 3 times a day.

When treating the drug should be monitored monthly blood and urine tests, liver function indicators (ALT activity, AST, bilirubin concentration in blood plasma).

It is necessary to monitor the patient's condition: medical personnel monitoring patients in the hospital, as well as members of the family of outpatients taking terizidone, should be informed of the possibility of developing unwanted reactions from the nervous system and are instructed to immediately inform the attending physician when depression or changes in the behavior of the patient.

With severe liver damage, pyridoxine in high doses can cause deterioration of its function.

When determining urobilinogen with Erlich reagent, pyridoxine can distort results.

Impact on the ability to drive vehicles and mechanisms

During the period of treatment, it is necessary to refrain from driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

OVERDOSE

Symptoms: There is no evidence of an overdose of the drug.

In case of an overdose, it is possible to increase neurotoxicity (including epileptiform seizures), gastrointestinal dysfunction.

Treatment: symptomatic, activated charcoal.
For the prevention of neurotoxic action, it is possible to administer pyridoxine, anticonvulsant and sedative drugs.Hemodialysis is effective.
DRUG INTERACTION

Terizidone

Ethanol increases the risk of adverse reactions, incl.
epileptic seizures.
When used simultaneously with ethionamide, there is an increased risk of side effects from the CNS (especially seizures).

With simultaneous use with fentoyinom increase in the concentration of phenytoin in the blood plasma.

Simultaneous use with isoniazid increases the incidence of dizziness, drowsiness.

With simultaneous application with cycloserine, an overdose of the drug is possible.

Pyridoxine

Strengthens the action of diuretics;
weaken the pharmacological effects of levodopa.
Isoniazid, penicillamine, cycloserine and estrogen-containing oral contraceptives weaken the effect of pyridoxine.

The drug is combined with cardiac glycosides (pyridoxine promotes increase of contractile proteins in the myocardium), with glutamic acid and potassium and magnesium asparaginate.

TERMS OF RELEASE FROM PHARMACY

It is released on prescription.

TERMS AND CONDITIONS OF STORAGE

In the original packaging of the manufacturer at a temperature of no higher than 25 ° C.
Keep out of the reach of children. Shelf life - 2 years.
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