Minoleksin, capsules 100 mg 20 pcs

Pharmacological group: Antibiotic – tetracycline.

ATX code: J01AA08

Pharmacological properties

Pharmacodynamics

Semisynthetic antibiotic from the group of tetracyclines. It has bacteriostatic effect on the cells of sensitive strains of microorganisms due to reversible inhibition of protein synthesis at the level of 30S ribosome subunits. It has a wide spectrum of antibacterial activity.

Sensitivity of microorganisms:

Aerobic Gram-positive:

Some of the microorganisms listed below have shown resistance to minocycline, so laboratory sensitivity testing is recommended before use. Antibiotics of the tetracycline group are not recommended for the treatment of streptococcal and staphylococcal infections unless the sensitivity of the microorganisms to minocycline has been shown.

Aerobic Gram-negative:

Minocycline sensitivity studies are highly recommended for the microorganisms listed below:

• Acinetobacter species
• Enterobacter aerogenes<
• Escherichia coli
• Haemophilus influenzae
• Neisseria gonorrhoeae*
• Neisseria meningitidis *
• Shigella species

Advanced:

• Actinomyces species
• Borrelia recurrentis

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• Chlamydia psittaci
• Chlamydia trachomatis
• Clostridium species<
• Entamoeba species
• Fusobacterium nucleatum subspecies fusiforme
• Mycobacterium marinum
• Mycoplasma pneumoniae
• Propionibacterium acnesPropionibacterium acnes
• Rickettsiae
• Treponema pallidum subspecies pallidum
• Treponema pallidum subspecies pertenue
• Ureaplasma urealyticum

Pharmacokinetics

Eating has no significant effect on the degree of absorption of minocycline. Minocycline has a high degree of lipid solubility and low affinity for Ca2+ binding. It is rapidly absorbed from the digestive tract in proportion to the dose taken. Maximum plasma concentration of minocycline (Cmax) after oral administration of 200 mg is 3.5 mg/l and is reached (tmax) after 2-4 hours. Binding to blood proteins is 75%, the effect of various diseases on this parameter has not been studied.

The volume of distribution is 0.7 l/kg. Minocycline penetrates into organs and tissues very well: 30-45 minutes after oral administration it is found in therapeutic concentrations in kidneys, spleen, eye tissues, pleural and ascitic fluid, synovial exudate, exudate of maxillary and frontal sinuses, gingival sulcus fluid. It penetrates well into cerebrospinal fluid (20 – 25% of the level determined in plasma). Passes through the placenta, penetrates into the mother’s milk.

In repeated administration the drug may cumulate. It accumulates in the reticulo-endothelial system and bone tissue. In bones and teeth it forms insoluble complexes with Ca2+ . It undergoes intestinal-hepatic recirculation, 30-60% of taken dose is excreted with intestinal contents; 30% is excreted by kidneys during 72 hours (among them 20-30% – unchanged), in severe chronic renal failure – only 1-5%. Half-life (T1/2) of minocycline is about 16 hours.

Indications

Minoleksin is used to treat the following diseases, provided the pathogens are sensitive:

Active ingredient

Composition

How to take, the dosage

Ingestion, after meals. It is recommended to drink plenty of fluids (milk is possible) to reduce the risk of irritation and esophageal ulceration.

The starting dose of Minolecsin® is 200 mg (2 100 mg capsules or 4 50 mg capsules) and 100 mg (1 100 mg capsule or 2 50 mg capsules) every 12 hours (twice daily) thereafter.

The maximum daily dose should not exceed 400 mg.

Infections of the urogenital system and anogenital area caused by chlamydia and ureaplasmas: 100 mg (1 100 mg capsule or 2 50 mg capsules) every 12 hours for 7-10 days.

Inflammatory diseases of the pelvic organs in women in the acute stage: 100 mg (1 100 mg capsule or 2 50 mg capsules) every 12 hours, sometimes in combination with cephalosporins.

Primary syphilis in patients with hypersensitivity to penicillins: 100 mg (1 100 mg capsule or 2 50 mg capsules) twice daily for 10-15 days.

Gonorrhea: 100 mg (1 100 mg capsule or 2 50 mg capsules) twice daily for 4-5 days, or once 300 mg.

Uncomplicated gonococcal infections (excluding urethritis and anorectal infections) in men: initial dose is 200 mg (2 100 mg capsules or 4 50 mg capsules), maintenance dose is 100 mg (1 100 mg capsule or 2 50 mg capsules) every 12 hours for at least 4 days, followed by microbiological evaluation of recovery 2-3 days after discontinuation of the drug.

Uncomplicated gonococcal urethritis in men: 100 mg (1 100 mg capsule or 2 50 mg capsules) every 12 hours for 5 days.

Acne: 50 mg (1 50 mg capsule) daily, for a long course of 6-12 weeks.

An increase in plasma urea levels may be observed during drug administration due to the anti-anabolic effect inherent in the drugs of tetracycline group. In patients with normal renal function, this does not require withdrawal of the drug. In patients with significant renal dysfunction, azotemia, hyperphosphatemia and acidosis may occur. In this situation it is necessary to control plasma urea and creatinine levels, and maximum daily dose of minocycline should not exceed 200 mg.

The pharmacokinetics of minocycline in patients with renal impairment (creatinine clearance less than 80 ml/min) have not been sufficiently studied to conclude whether a dose adjustment is necessary at this time.

The drug should be used with caution in liver function disorders. In children over 8 years of age in infections caused by minocycline-sensitive pathogens: the initial dose is 4 mg/kg, then 2 mg/kg every 12 hours.

Interaction

The drugs of the tetracycline group reduce the prothrombin activity of blood plasma, which may necessitate reduction of anticoagulant doses in patients on anticoagulant therapy.

In connection with the fact that bacteriostatic drugs affect the bactericidal effect of penicillins, concomitant administration of drugs of penicillin and tetracyclines groups should be avoided.

The absorption of tetracyclines is impaired when taken simultaneously with antacids containing aluminum, calcium, magnesium or iron-containing drugs, which may reduce the effectiveness of antibiotic therapy.

There have been cases of terminal renal toxicity with concomitant use of methoxyfuran and tetracyclines.

The simultaneous use of tetracycline antibiotics and oral contraceptives may decrease the effectiveness of contraception.

The use of isotretinoin immediately before, at the same time, and immediately after taking minocycline should be avoided because both drugs can cause a benign increase in intracranial pressure.

The simultaneous use of tetracyclines with ergot alkaloids and their derivatives increases the risk of ergotism.

Special Instructions

In long-term use of minocycline, peripheral blood cell composition should be regularly monitored, functional hepatic tests should be performed, serum concentrations of nitrogen and urea should be determined.

If contraceptive drugs with estrogens are used during therapy with minocycline, additional contraceptives or combinations of them should be used.

Possible false elevation of catecholamines in the urine when they are determined by fluorescent method.

When examining a thyroid biopsy in patients who have received long-term tetracyclines, the possibility of dark brown staining of the tissue in microslides should be considered.

With the drug and 2-3 weeks after discontinuation of treatment the development of diarrhea caused by Clostridium dificile (pseudomembranous colitis) is possible. In mild cases, treatment withdrawal and use of ion exchange resins (colestiramine, colestipol) is sufficient; in severe cases, reimbursement of fluid, electrolytes and protein loss, prescription of vancomycin, bacitracin or metronidazole is indicated. Do not use drugs that inhibit intestinal peristalsis.

In order to avoid the development of resistance, minocycline should be used only in accordance with the results of the sensitivity study of pathogenic microorganisms. If a sensitivity study of microorganisms is not possible, the epidemiology and sensitivity profile of microorganisms in a particular region should be taken into account.

In the case of venereal diseases, if concomitant syphilis is suspected, dark-field microscopy studies should be performed before starting treatment. Serological serum diagnosis is recommended at least once every four months.

Periodic laboratory diagnosis of bodily functions, including hematopoietic and renal functions, as well as liver status, is necessary.

Algorithms of action if some side effects occur:

If superinfection develops, minocycline should be discontinued and adequate therapy administered.

In case of increased intracranial pressure, minocycline should be discontinued.

Diarrhea is a common disorder associated with taking antibiotics. If diarrhea occurs during treatment with minocycline, a doctor should be seen urgently.

Tetracycline antibiotics cause increased sensitivity to direct sunlight and ultraviolet radiation. If erythema occurs, the antibiotic should be stopped.

Impact on driving and operating machinery:
Caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and rapid psychomotor reactions due to the fact that minocycline has a side effect such as dizziness (see section “Side effects”).

Contraindications

With caution: hepatic and renal dysfunction, concomitant use with hepatotoxic drugs.

Side effects

Digestive system disorders: anorexia, nausea, vomiting, diarrhea, dyspepsia, stomatitis, glossitis, dysphagia, dental enamel hypoplasia, enterocolitis, pseudomembranous colitis, pancreatitis, inflammatory
lesions (including fungal) in the oral cavity and anogenital area.including fungal) in the oral cavity and anogenital area, hyperbilirubinemia, cholestasis, increased liver enzymes, liver failure, including terminal, hepatitis, including autoimmune.

Urogenital system disorders: candidiasis vulvovaginitis, interstitial nephritis, dose-dependent increase in plasma urea.

Skin disorders: alopecia, erythema nodosum, nail pigmentation, skin itching, toxic epidermal necrosis, vasculitis, maculopapular and erythematous rash, Stevens-Johnson syndrome, exfoliative dermatitis, balanitis.

Respiratory tract disorders: dyspnea, bronchospasm, exacerbation of asthma, pneumonia.

Muscular system disorders: arthralgia, arthritis, restriction of joint mobility and swelling, discoloration of bone tissue, muscle pain (myalgia).

Allergic reactions: urticaria, angioneurotic edema, polyarthralgia, anaphylactic reactions (including shock), anaphylactoid purpura (Schoenlein Henoch purpura), pericarditis, exacerbations of systemic lupus erythematosus, lung infiltration accompanied by eosinophilia.

Hematopoietic organs: agranulocytosis, hemolytic anemia, tr6mbocytopenia, leukopenia, neutrocytopenia, pancytopenia, eosinopenia, eosiophilia.

Central nervous system disorders: convulsions, dizziness, numbness (including limbs), lethargy, vertigo, increased intracranial pressure in adults, headache.

Sensory organs: tinnitus and hearing disorders.

Metabolic disorders: Thyroid: single case of malignant neoplasm, discoloration (based on the results of patho-morphological studies), functional disorders.

Others: discoloration of the oral cavity (tongue, gums, palate), discoloration of tooth enamel, fever, discoloration of secretions (e.g., sweat).

Overdose

Symptoms: Dizziness, nausea and vomiting are the most common.

Treatment: A selective antidote for minocycline is currently unknown. In case of overdose, discontinue the drug, provide symptomatic treatment and supportive therapy. Hemo- and peritoneal dialysis eliminate minocycline in small amounts.