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

Active substanceIsoniazid + EthambutolIsoniazid + Ethambutol

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Protubetam®

pills inwards

FARMASINTEZ, JSC (Irkutsk) Russia

Phthisoetham®

pills inwards

AKRIKHIN HFK, JSC Russia

Dosage form: & nbsppills

Composition:

One tablet contains:

active substances: isoniazid in terms of 100% substance 150.0 mg, ethambutol hydrochloride in terms of 100% substance 400.0 mg;

Excipients: calcium hydrophosphate dihydrate 45.00 mg, povidone (type K 25) 30.93 mg, crospovidone (type B) 13.49 mg, magnesium stearate 10.40 mg, tropeolin dye O 0.18 mg.

Description:

Tablets from light yellow to yellow with dark and light yellow impregnations and possible white spots, flat-cylindrical, with a facet and a risk.

Pharmacotherapeutic group:Anti-tuberculosis drug combined

ATX: & nbsp

J.04.A.M.03 Isoniazid in combination with ethambutol

Pharmacodynamics:

Isoniazid is a specific anti-tuberculosis drug that has a pronounced bactericidal effect, mainly in relation to rapidly proliferating populations of mycobacterium tuberculosis. Isoniazid suppresses the synthesis of mycolic acid, which is necessary for the formation of the cell wall of mycobacteria.

Ethambutol is a synthetic drug that has a bacteriostatic effect, disrupting the synthesis of RNA in mycobacteria. It has activity only in relation to rapidly proliferating populations of mycobacteria.Besides, ethambutol prevents the emergence of strains resistant to isoniazid and rifampicin.

Pharmacokinetics:

Isoniazid quickly absorbed after ingestion, but with the simultaneous intake of the drug with food, its absorption and bioavailability are reduced. After a single oral intake of 300 mg of isoniazid, the maximum plasma concentrations are noted after 1-2 hours.

Connection with plasma proteins - up to 10%. Isoniazid well penetrates into various tissues and body fluids, including bones and spinal fluid. Isoniazid acetylated and hydrolyzed in the liver. Acetylation is the main pathway of isoniazid metabolism. The rate of acetylation depends on the individual characteristics of the patient. The half-life (T_1/2) is 0.5-1.6 hours "fast acetylators") or 2-5 hours "slow acetylators.") If liver function is impaired (T_1/2) isoniazid is lengthened. Metabolites of isoniazid do not have antimicrobial activity.

Within 24 hours with urine, 75-95% of the administered dose in the form of metabolites (N-acetyl isosine, etc.). Part of isoniazid is excreted unchanged in urine: up to 12% with rapid acetylation and up to 27% with slow acetylation.With severe renal failure in patients with slow acetylation, cumulation of the drug is possible.

Ethambutol: bioavailability after oral administration is 75-80%. After a single administration of ethambutol in a dose of 25 mg / kg body weight, maximum plasma concentrations are noted after 2-4 hours.

Etambutol well penetrates into various tissues and body fluids, except for cerebrospinal fluid. When tuberculous meningitis 10-50% of the drug penetrates through the soft medulla.

Communication with plasma proteins is 20-30%. (T_1/2) is 3-4 hours, with renal failure - increases to 8 hours. Ethambutol undergoes biotransformation in the liver; up to 15% drug is converted into inactive metabolites. Ethambutol is excreted from the body through the kidneys (up to 80%) and the gastrointestinal tract (up to 20%).

Indications:

Treatment of tuberculosis caused by sensitive mycobacteria to isoniazid and ethambutol (all forms and localizations).

Contraindications:

Phthisotam® is contraindicated in children under 12 years of age, patients with hypersensitivity to isoniazid and ethambutol, epilepsy and other diseases,accompanied by a tendency to convulsions, uncontrolled arterial hypertension, severe coronary insufficiency, cirrhosis of the liver, acute hepatitis, myxedema, with optic neuritis, cataract, diabetic retinopathy, bronchial asthma, psoriasis, hyperuricemia, acute gout, gastric ulcer, pregnancy, lactation.

Carefully:

With caution, prescribe the drug to people with chronic kidney failure.

Phthisotam® can have a hepatotoxic effect, so it should be used with caution in patients with impaired hepatic function, in persons with chronic alcoholism, as well as in patients with hypotrophy.

Pregnancy and lactation:

During pregnancy, Ftyzoetam® is administered only on strict indications.

Isoniazid and ethambutol excreted in breast milk. Women who take Phthisoeth® should not breast-feed.

Dosing and Administration:

The drug Ftizoetham ® is applied inside, after a meal, once a day.

Dosage of phthisoetham® is carried out by isoniazid: 5-10 mg / kg of patient weight. The drug is used daily in the intensive care period (3-4 months), in the subsequent time - every other day.

The total course dose of Phthisoetham® for each patient is individual and depends on the nature of the disease, the effectiveness of the treatment and the tolerability.

Side effects:

Isoniazid

From the hepatobiliary system: there may be a violation of liver function, especially in patients with hypotrophy or previous liver diseases, as well as in the elderly.

From the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain.

From the nervous system: headache, dizziness, rarely - irritability, euphoria, insomnia, psychosis. Sometimes the development of peripheral neuropathy is possible, especially in elderly patients, pregnant women, patients with hypotrophy, patients with diabetes mellitus, as well as in patients with chronic liver diseases, including alcoholic etiology. For the prevention of peripheral neuropathy it is recommended to take pyridoxine. Seizures can occur in patients with epilepsy.

From the cardiovascular system: palpitation, angina, increased blood pressure.

Allergic reactions: skin rash, itching.

Other: very rarely - gynecomastia, menorrhagia.

Ethambutol

From the digestive system: decreased appetite, nausea, vomiting, gastralgia, increased activity of "liver" transaminases.

From the nervous system: weakness, headache, dizziness, confusion, disorientation, hallucinations, paresis, peripheral neuritis (tingling in the limbs, numbness, itching).

From the sense organs: optic neuritis (decreased visual acuity, color blindness, scotoma).

Allergic reactions: dermatitis, itching, arthralgia, fever, anaphylaxis.

Other: hyperuricemia.

Overdose:

Overdose Symptoms: nausea, vomiting, abdominal pain, jaundice, increased liver enzymes, acute pulmonary edema, impaired consciousness, coma, convulsions, respiratory failure, hyperglycemia, metabolic ketoacidosis.

Treatment: gastric lavage with the introduction of activated carbon, forced diuresis, general measures to maintain vital functions, hemodialysis.

Interaction:

Isoniazid

Isoniazid slows the metabolism of certain medicines, including phenytoin, carbamazepine, valproat.At a simultaneous appointment with isoniazid dose of these drugs is recommended to reduce.

It is necessary to avoid the simultaneous use of isoniazid and disulfiram, since this can lead to mental disorders. The mechanism of this interaction is not established.

Isoniazid increases the serum concentrations of carbamazepine and phenytoin, reduces the concentration of ketoconazole and cyclosporine in the blood.

Antacids reduce the absorption of isoniazid.

Reduces the effectiveness of oral contraceptives, glipizide, tolbutamide, theophylline, tolazomide, vitamin B₁ enhances the side effects of phenytoin; suppresses the excretion of triazolam, enhances the excretion of vitamin B₁ reduces the content of zinc ions in the blood, increases their excretion.

Drinking alcohol with isoniazid therapy can increase the risk of hepatitis.

Ethambutol

Simultaneous administration of ethambutol and drugs that have a neurotoxic effect may increase the likelihood of developing the optic nerve and peripheral neuritis.

Special instructions:

During treatment with the drug, patients should refrain from drinking alcohol.

For the prevention and treatment of peripheral neuropathy, which can develop against the background of isoniazid therapy, additional administration of pyridoxine (vitamin B₆).

In some cases, especially in patients with a history of gout, it is recommended to periodically monitor the level of uric acid in the serum.

Etambutol can have a negative effect on vision. Vision usually normalizes after the timely abolition of ethambutol. In rare cases, the normalization of vision can occur within a year or more. It is necessary to check the visual acuity of each eye individually and both eyes together; visual acuity is checked before treatment and periodically during treatment. With any change in visual acuity, patients should immediately consult a doctor. If there is a decrease in visual acuity, ethambutol cancel.

Patients with renal insufficiency may need a reduction in the dose of ethambutol.

It is recommended to monitor ALT levels and ACT in the plasma and monthly assess liver function. Isoniazid should be abolished only in cases where the levels of transaminases are more than 3 times higher than the upper limit of the norm,as often there is an asymptomatic transient increase in the level of hepatic enzymes, which does not require discontinuation of the drug. When developing acute or chronic hepatitis isoniazid it is necessary to cancel, in the latter case, it is impossible to resume isoniazid therapy.

When taken in high doses, it is possible to develop adverse reactions from the nervous system (peripheral neuropathy), which affects the ability to drive and work with complex equipment.

Form release / dosage:

Tablets, 150 mg + 400 mg.

Packaging:

For 50 or 100 tablets in a jar of polypropylene or in a jar of polyethylene.

10 tablets per contour cell pack.

Each jar or 5 or 10 contour squares, together with the instruction for use, is placed in a pack of cardboard.

For 500 or 1000 tablets per package of polyethylene film unstabilized; The plastic bag together with the instruction for use is placed in a container made of polypropylene or in a container made of polyethylene (for inpatient).

For 25 cans of 100 tablets or 100 contour packs with an equal number of instructions for use are placed in a box of cardboard (for inpatient).

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000102

Date of registration:12.04.2010 / 18.10.2016

Expiration Date:Unlimited

The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia

Manufacturer: & nbsp

AKRIKHIN HFK, JSC Russia

Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia

Information update date: & nbsp09.01.2017

Illustrated instructions

Instructions

Phthisoetham® (Phtizoethamum®)