Universal reference book for medicines
Product name: LOMECOMB ® (LOMECOMB ® )

Active substance: comb.
drug
Type: Anti-TB drug

Manufacturer: Chemical-Pharmaceutical Plant Akrihin (Russia)

Composition, form of production and packaging
Tablets coated with a
film (film) are light brown or pinkish-brown in color, oval, biconvex;
On a cross-section - from white to white with a creamy or yellowish shade of color.
1 tab.

isoniazid 135 mg

Lomefloxacin hydrochloride 200 mg

pyrazinamide 370 mg

ethambutol hydrochloride 325 mg

pyridoxine hydrochloride 10 mg

Excipients: povidone, polyethylene glycol, sodium croscarmellose, silicon dioxide colloid, magnesium stearate, hypromellose, glycerol, talc, titanium dioxide, iron oxide red oxide, lactose.

500 pcs.
- Polymer containers.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2008.

PHARMACHOLOGIC EFFECT

Lomecomb ® is a combined five-component preparation containing a fixed amount of isoniazid, lomefloxacin hydrochloride, pyrazinamide, ethambutol hydrochloride and pyridoxine hydrochloride.

Isoniazid has a bactericidal effect on the actively dividing cells of Mycobacterium tuberculosis.
The mechanism of its action is the inhibition of the synthesis of mycolic acids, which are a component of the cell wall of mycobacteria. For mycobacteria tuberculosis, the minimum inhibitory concentration of the drug (MIC) is 0.025-0.05 mg / l. Isoniazid has a moderate effect on slow and fast-growing atypical mycobacteria.
Lomefloxacin

Antimicrobial bactericide of broad spectrum of action from the group of fluoroquinolones.
Affects the bacterial enzyme DNA-gyrase, which provides supercoiling, forms a complex with its tetramer (subunit of gyrase A2B2) and disrupts transcription and replication of DNA, leads to the death of the microbial cell. Beta-lactamases, produced by pathogens, do not affect the activity of lomefloxacin. Highly active against Gram-negative aerobic microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter divcrsus, Klebsiella pneumoniae, Enterobacter cloacae, Proteus vulgaris, Salmonella spp., Shigella spp., Moraxella catarrhalis, Morganella morganii, Haemophilus influenzae and parainfluenzae, Legionella pneumophila , Pseudomonas aeruginosa.
Moderately sensitive to the drug Staphylococcus aureus, Staphylococcus epidermidis, Serratia liquifaciens and marcescens, Pseudomonas aeruginosa, Mycobacterium tuberculosis,
Chlamydia trachomatis, Hafnia alvei, Citrobacter freundii, Aeromonas hydrophila, Proteus mirabilis and Proteus stuartii, Providcncia rettgeri and Providencia alcalifaciens, Klebsiella oxytoca, Klebsiella ozaenae , Enterobacter aerogenes, Enterobacter agglomerans. Resistant to the drug Streptococcus spp., Pseudomonas cepacia, Ureaplasma urealyticum, Treponema pallidum, Mycoplasma hominis and anaerobic bacteria.
It acts on both extracellular and intracellularly located Mycobacterium tuberculosis, shortens the time of their isolation from the body, provides a faster resolution of infiltrates.
Most microorganisms act at low concentrations (the concentration necessary to suppress the growth of 90% of the strains, usually not more than 1 μg / ml).Resistance is rare.
Pyrazinamide

The pyrazinamide target is the synthase I gene of mycobacterial fatty acid, which is involved in the biosynthesis of mycolic acid.
Pyrazinamide has a bactericidal effect at acidic pH values. Well penetrates into the tuberculosis foci. Its activity is high in caseous-necrotic processes, caseous lymphadenitis, tuberculosis. To manifest the bactericidal activity of pyrazinamide, the preparation is subjected to enzymatic conversion into the active form - pyrazinic acid. At acidic pH values, the MPC of pyrazinamide in vitro is 20 mg / L. On non-tuberculosis pathogens does not work.
Ethambutol

Etambutol is a bacteriostatic drug that is effective against typical and atypical mycobacteria tuberculosis.
The mechanism of action of the drug is associated with a violation of the synthesis of RNA in bacterial cells, it suppresses the synthesis of the cell wall, blocking the inclusion of mycolic acids in it. Etambutol is active against rapidly and slowly growing atypical mycobacteria. The MIC of ethambutol is 0.78-2.0 mg / l. Ethambutol does not act on nontuberculous pathogenic microorganisms.
Pyridoxine hydrochloride

Vitamin product.
Participates in the metabolism. It is necessary for the normal functioning of the central and peripheral nervous system. Anti-TB drugs cause peripheral polyneuropathy, the occurrence of which can reduce pyridoxine. In this regard, the daily dose of vitamin increases to 60 mg. With the simultaneous administration of pyridoxine inwards with isoniazid, rifampicin, pyrazinamide and ethambutol, there is no interaction of these drugs at the pharmacokinetic and microbiological levels.
PHARMACOKINETICS

Isoniazid

Taking isoniazid in together with the preparations that make up Isocomb ® does not affect the rate of its absorption from the digestive tract.
Penetrates isoniazid in many tissues and fluids, including spinal fluid (CSF). The time to reach the maximum concentration of the drug in the blood is 2 hours, the value of C max is -6.6 mg / l, T 1/2 is 5.8 hours. High C max and T 1/2 is due to the slowing down of isoniazid excretion under the influence of pyrazinamide. Isoniazid practically does not bind to plasma proteins.
Isoniazid up to 80-90% excreted in urine and 10% with feces during the day.
The main products of isoniazid metabolism are N-acetylisoaniazide and isonicotinic acid.
Lomefloxacin

Lomefloxacin intake in conjunction with the preparations that make up Prothiocomb ® does not affect the rate of its absorption from the digestive tract).

Bioavailability of Lomefloxacin is more than 90%.
The drug after ingestion is rapidly absorbed from the digestive tract. C max is 5.1 mg / l, the time to reach C max is 1-1.5 hours. It circulates for a long time in the body: T 1/2 in blood - 8-9 hours. The connection with blood proteins is insignificant - 10%. Well penetrates into various organs and tissues, where concentrations are created, 9-13 times higher than serum. In small amounts, biotransformation is performed in the liver with the formation of 5 metabolites, which have little antimicrobial activity. In 80% is excreted by the kidneys, in 20% - with feces, then with saliva.
Hepatic failure does not affect the biotransformation of lomefloxacin.
A small part of the drug undergoes metabolism with the formation of metabolites. Т 1/2 - 8-9 hours; the average renal clearance is 145 ml / min.
In elderly patients, plasma clearance is reduced by 25%.
With a decrease in the clearance of creatinine (CC) to 10-40 ml / min / 1.73 m2 T 1/2 increases.
The kidneys are secreted 70-80% by tubular secretion (mostly unchanged, 9% in the form of glucuronides, 0.5% in the form of other metabolites)

Pyrazinamide

After taking Isocomb® C max, pyrazinamide in plasma reaches 24.1 mg / L after 3 hours. T 1/2 of the drug is an average of 17 hours. The main active metabolite of pyrazinamide is pyrazinic acid.
Up to 70% metabolites of pyrazinamide are excreted in urine and about 4% - unchanged drug.
Ethambutol

After intake of Isocomb® C max, ethambutol is 6.4-7.6 mg / l.
High C max ethambutol is explained by the slowing of its excretion under the influence of isoniazid. Cmax of the drug in plasma (60%) is achieved after 2 hours. Etambutol is excreted in urine 70% unchanged, in 30% - in the form of aldehyde and carboxyl inactive metabolites. On average, 25% of the drug binds to plasma proteins.
Pyridoxine hydrochloride

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 with plasma proteins binds to 90%. Well penetrate into all tissues; accumulate mainly in the liver, less - in the muscles and the central nervous system. Penetrates through the placenta, is secreted with breast milk. T 1/2 - 15-20 days. It is excreted by the kidneys.
INDICATIONS

- acutely progressive course of tuberculosis;

- tuberculosis with concomitant inflammatory diseases caused by nonspecific pathogenic flora, sensitive to lomefloxacin.

DOSING MODE

Inside, regardless of food intake, 1 time / day, preferably in the first half of the day.
Lomecomb ® is dosed according to lomefloxacin 13.2 mg / kg body weight, but not more than 5 tab. Duration of treatment - 3 months.
With a body weight> 80 kg, isoniazid is additionally prescribed in the evening (total daily dose of isoniazid up to 10 mg / kg).
According to the indications Lomecomb ® is combined with streptomycin (in / m in a dose of 16 mg / kg 1 time / day for 3 months).
SIDE EFFECT

Isoniazid

From the side of the central nervous system and peripheral nervous system: headache, dizziness, rarely unusual fatigability or weakness, irritability, euphoria, insomnia, paresthesia, numbness of limbs, peripheral neuropathy, optic neuritis, polyneuritis, psychosis, mood change, depression.
Seizures can occur in patients with epilepsy.
From the cardiovascular system: palpitation, angina pectoris, increased blood pressure.

On the part of the digestive system: nausea, vomiting, gastralgia, toxic hepatitis.

Allergic reactions: skin rash, itching, hyperthermia, arthralgia.

Other: very rarely - gynecomastia, menorrhagia, tendency to bleeding and hemorrhage.

Lomefloxacin

On the part of the digestive system: nausea, vomiting, dry mouth, stomachalgia, abdominal pain, diarrhea or constipation, flatulence, pseudomembranous enterocolitis, dysphagia, discoloration of the tongue, decreased appetite or bulimia, taste distortion, dysbiosis, increased activity of hepatic transaminases.

From the central nervous system and peripheral nervous system: fatigue, malaise, asthenia, headache, dizziness, fainting, insomnia, hallucinations, convulsions, hyperkinesia, tremor, paresthesia, nervousness, anxiety, depression, agitation.

From the genitourinary system : glomerulonephritis, dysuria, polyuria, anuria, albuminuria, urethral hemorrhages, crystalluria, hematuria, urinary retention, edema;
in women - vaginitis, leukorrhea, intermenstrual bleeding, pain in the perineum, vaginal candidiasis; in men - orchitis, epididymitis.
From the side of metabolism: hypoglycemia, gout.

From the musculoskeletal system: arthralgia, vasculitis, calf muscle cramps, pain in the back and chest.

On the part of the hematopoiesis and hemostasis system: bleeding from the digestive tract, thrombocytopenic purpura, increased fibrinolysis, epistaxis, lymphadenopathy.

On the part of the respiratory system: dyspnoea, respiratory infections, bronchospasm, cough, hypersecretion of phlegm, influenza-like symptoms.

From the senses: visual impairment, pain and noise in the ears, pain in the eyes.

From the cardiovascular system: lowering blood pressure, tachycardia, bradycardia, extrasystole, arrhythmias, progression of heart failure and angina pectoris, pulmonary embolism, myocardiopathy, phlebitis.

Allergic reactions: pruritus, hives, photosensitivity, malignant exudative erythema (Stevens-Johnson syndrome).

Influence on the fetus: the experiment described fetotoxic action (arthropathy).

Other: candidiasis, increased sweating, chills, thirst, superinfection.

Pyrazinamide

On the part of the digestive system: nausea, vomiting, diarrhea, "metallic" taste in the mouth, impaired liver function (decreased appetite, liver tenderness, hepatomegaly, jaundice, yellow atrophy of the liver);
exacerbation of peptic ulcer.
From the side of the central nervous system: dizziness, headache, sleep disturbances, increased excitability, depression;
in some cases - hallucinations, convulsions, confusion.
On the part of the hematopoiesis and hemostasis system: thrombocytopenia, sideroblastic anemia, erythrocyte vacuolization, porphyria, hypercoagulation, splenomegaly.

From the musculoskeletal system: arthralgia, myalgia.

From the side of the urinary system: dysuria, interstitial nephritis.

Allergic reactions: skin rash, hives.

Other: hyperthermia, acne, hyperuricemia, exacerbation of gout, photosensitivity, increased serum iron concentration.

Ethambutol

From the side of the central nervous system, peripheral nervous system and sensory organs: weakness, headache, dizziness, impaired consciousness, disorientation, hallucinations, depression, peripheral neuritis (paresthesia in the extremities, numbness, paresis, itching), optic neuritis (visual acuity, impaired color perception, mainly green and red colors, color blindness, scotoma).

On the part of the digestive system: decreased appetite, nausea, vomiting, gastralgia, impaired liver function - increased activity of hepatic transaminases.

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

Other: hyperuricemia, exacerbation of gout.

Pyridoxine hydrochloride

Allergic reactions, hypersecretion of hydrochloric acid, numbness, the appearance of a feeling of compression in the limbs - a symptom of "stocking" and "gloves", rarely - a skin rash, itching of the skin.

Treatment of patients with a multicomponent drug reduces the medical burden on the patient by 3 times, which contributes to the improvement of drug tolerance.

CONTRAINDICATIONS

hypersensitivity to any component of the drug;

- pregnancy, lactation period;

- Children's age under 18 (the period of formation and growth of the skeleton),

- Stomach ulcer and duodenal ulcer;

- ulcerative colitis;

- Acute hepatitis, cirrhosis of the liver;

- CNS diseases (epilepsy and other diseases with a tendency to convulsive seizures);

- Diseases of the organs of vision (inflammation of the optic nerve, cataracts, diabetic retinopathy, inflammatory diseases of the eyes);

- gout;

- Thrombophlebitis.

PREGNANCY AND LACTATION

The drug is contraindicated during pregnancy and lactation.

APPLICATION FOR CHILDREN

The drug is contraindicated in children and adolescents under 18 years.

DRUG INTERACTION

The use of lomefloxacin together with isoniazid, ethambutol and, especially, pyrazinamide significantly increases antimicrobial activity against sensitive and, in particular, resistant Mycobacterium tuberculosis (MT).
The combined use of Lomecomb® with probenecid slows the excretion of lomefloxacin.
Sucralfate and antacid agents containing magnesium or aluminum form chelate complexes with lomefloxacin.
The use of these drugs should be performed 2 hours before or 2 hours after taking Lomefloxacin.
Admission of Lomecombe ® together with rifampicin leads to a decrease in antimicrobial activity of this combination in relation to MW because of the antagonism existing between lomefloxacin and rifampicin.

Rifampicin induces certain enzymes of the cytochrome P450 system, accelerating the metabolism of prednisolone, phenytoin, quinidine, oral anticoagulants, hormonal contraceptives of antifungals, cimetidine, cyclosporine A.

Isoniazid reduces the association of rifampicin with plasma proteins, pyrazinamide slows the excretion of rifampicin.

PASK (para-aminosalicylic acid) impairs the absorption of rifampicin.

Antacids, opioid analgesics reduce the bioavailability of rifampicin.

Isoniazid

MAO inhibitors increase the risk of side effects from the central nervous system and the cardiovascular system.

Pyridoxine (vitamin B 6 ), glutamic acid reduces the risk of developing side effects of isoniazid.
The combined use of isoniazid and cycloserine increases the risk of developing neurotoxic side effects.
Pyrazinamide

Pyrazinamide increases the concentration of isoniazid and rifampicin in the serum, slowing their excretion.
When taking rifampicin together with pyrazinamide, the risk of developing hepatotoxic reactions increases.
Ethambutol

Aluminum hydroxide reduces the absorption of ethambutol.

The use of ethambutol with aminoglycosides, ciprofloxacin, imipenem, carbamazepine, lithium salts, quinine increases the risk of neurotoxic action of the drug.Etambutol enhances the antimicrobial activity of other antituberculosis drugs.

Pyridoxine hydrochloride

Pyridoxine hydrochloride weakens the action of levodopa when combined.
Pyridoxine hydrochloride reduces the risk of toxic effects of antituberculosis drugs on the central nervous system and peripheral nervous system.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. In a dry, dark place, out of reach of children, at a temperature of no higher than 25 ° C.

Shelf life - 2 years.
Do not use after the expiration date indicated on the package.
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