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

<

• 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

Minolexin is used to treat the following diseases, subject to the sensitivity of pathogenic microorganisms:

Acne
Skin infections
Spotted fever, typhoid fever, typhoid fever, Q fever (coxiellosis), vesicular rickettsiosis and tick fever
Respiratory tract infections
Lymphogranuloma venereum
Psittacosis
Trachoma (infectious keratoconjunctivitis)
Conjunctivitis with inclusions (paratrachoma)
Nongonococcal urethritis, cervical and anal infections in adults
Cyclic fever
Chancroid
Plague
Tularemia
Cholera
Brucellosis
Bartonellosis
Granuloma inguinale
Syphilis
Gonorrhea
Yaws (tropical granuloma, non-venereal syphilis)
Listeriosis
Anthrax
Vincent’s angina
Actinomycosis.

In the case of acute intestinal amebiasis, the use of minocycline as an addition to amoebicidal drugs is allowed.

For severe acne. Minocycline may be used as adjunctive therapy.

Oral administration of minocycline is indicated for asymptomatic carriage of Neisseria mepigitidis for the eradication of meningococci from the nasopharynx.

Pharmacological effect

Pharmacological group:
Antibiotic – tetracycline.

ATX code: J01AA08

Pharmacological properties

Pharmacodynamics

Semi-synthetic antibiotic from the tetracycline group. It has a bacteriostatic effect on cells of sensitive strains of microorganisms due to reversible inhibition of protein synthesis at the level of 30S ribosomal subunits. 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 sensitivity of microorganisms to minocycline is shown.

Bacillus anthracis
Listeria monocytogenes
Staphylococcus aureus
Streptococcus pneumoniae

Aerobic gram-negative:

Bartonella bacilliformis
Brucella species
Calymmatobacterium granulomatis
Campylobacter fetus
Francisella tularensis
Haemophilus ducreyi
Vibrio cholerae
Yersinia pestis

For the following microorganisms, sensitivity testing to minocycline is strongly recommended:

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

Additionally:

Actinomyces species
Borrelia recurrentis
Chlamydia psittaci
Chlamydia trachomatis
Clostridium species
Entamoeba species
Fusobacterium nucleatum subspecies fusiforme
Mycobacterium marinum
Mycoplasma pneumoniae
Propionibacterium acnes
Rickettsiae
Treponema pallidum subspecies pallidum
Treponema pallidum subspecies pertenue
Ureaplasma urealyticum

Pharmacokinetics

Food intake does not have a significant effect on the extent of absorption of minocycline. Minocycline has a high degree of lipid solubility and low affinity for Ca2+ binding. It is quickly absorbed from the digestive tract in proportion to the dose taken. The maximum concentration of minocycline in blood plasma (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 well into organs and tissues: 30 – 45 minutes after oral administration it is found in therapeutic concentrations in the kidneys, spleen, eye tissues, pleural and ascitic fluids, synovial exudate, exudate of the maxillary and frontal sinuses, and in the fluid of the gingival grooves. Penetrates well into the cerebrospinal fluid (20 – 25% of the level determined in plasma). Passes through the placenta and enters breast milk.

With repeated administrations, the drug may accumulate. Accumulates in the reticuloendothelial system and bone tissue. In bones and teeth it forms insoluble complexes with Ca2+. Subject to enterohepatic recirculation, 30-60% of the dose taken is excreted with intestinal contents; 30% is excreted by the kidneys in 72 hours (of which 20-30% is unchanged), in severe chronic renal failure – only 1-5%. The half-life (T1/2) of minocycline is approximately 16 hours.

Special instructions

With long-term use of minocycline, the cellular composition of peripheral blood should be regularly monitored, liver function tests should be performed, and the concentration of nitrogen and urea in the serum should be determined.

When using contraceptives with estrogens, additional contraceptives or a combination of contraceptives should be used during minocycline therapy.

A false increase in the level of catecholamines in urine is possible when they are determined by the fluorescent method.

When examining a biopsy of the thyroid gland in patients who have been receiving tetracyclines for a long time, one should take into account the possibility of dark brown staining of the tissue in micropreparations.

While taking the drug and 2-3 weeks after stopping treatment, diarrhea caused by Clostridium dificile (pseudomembranous colitis) may develop. In mild cases, it is sufficient to discontinue treatment and use ion-exchange resins (colestyramine, colestipol); in severe cases, replacement of loss of fluid, electrolytes and protein, and the appointment of vancomycin, bacitracin or metronidazole are indicated. You should not use medications that inhibit intestinal motility.

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

In the case of sexually transmitted diseases, if concomitant syphilis is suspected, before starting treatment it is necessary to conduct dark-field microscopy studies. Serological diagnostics of blood serum is recommended to be carried out at least once every four months.

Periodic laboratory diagnostics of body functions, including hematopoietic and renal functions, as well as the condition of the liver, are necessary.

Algorithms for action in the event of certain side effects:

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

If intracranial pressure increases, minocycline should be discontinued.

Diarrhea is a common disorder associated with antibiotic use. If diarrhea occurs during treatment with minocycline, you should immediately consult a doctor.

Antibiotics of the tetracycline group cause increased sensitivity to direct sunlight and ultraviolet radiation. If erythema occurs, you should stop taking the antibiotic.

Impact on the ability to drive vehicles and operate machinery:
Caution must be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions, due to the fact that minocycline has a side effect such as dizziness (see section “Side Effects”).

Active ingredient

Minocycline

Composition

Active substance:

minocycline hydrochloride dihydrate (in terms of minocycline) – 100 mg.

Excipients: microcrystalline cellulose (147.0 mg), low molecular weight povidone (17.5 mg), potato starch (14.0 mg), magnesium stearate (3.5 mg), lactose monohydrate (up to 350.0 mg).

Hard gelatin capsules: water (13 – 16%), titanium dioxide (2.0% – 2.1118%), gelatin (up to 100%).

Contraindications

Hypersensitivity to minocycline, tetracyclines and other components of the drug
Porphyria
Severe liver and kidney failure
Leukopenia
Pregnancy
Breast-feeding
Systemic lupus erythematosus
Children under 8 years of age (period of dental development)
Concomitant use with isotretinoin
Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

With caution: impaired liver and kidney function, simultaneous use with hepatotoxic drugs.

Side Effects

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

From the genitourinary system: vulvovaginal candidiasis, interstitial nephritis, dose-dependent increase in urea content in the blood plasma.

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

From the respiratory tract: shortness of breath, bronchospasm, exacerbation of asthma, pneumonia.

From the musculoskeletal system: arthralgia, arthritis, limited mobility and swelling of the joints, discoloration of bone tissue, muscle pain (myalgia).

Allergic reactions: urticaria, angioedema, polyarthralgia, anaphylactic reactions (including shock), anaphylactoid purpura (Henoch Schonlein purpura), pericarditis, exacerbations of systemic lupus, pulmonary infiltration accompanied by eosinophilia.

From the hematopoietic organs: agranulocytosis, hemolytic anemia, thrombocytopenia, leukopenia, neutrocytopenia, pancytopenia, eosinopenia, eosiophilia.

From the central nervous system: convulsions, dizziness, numbness (including limbs), lethargy, vertigo, increased intracranial pressure in adults, headaches.

From the senses: tinnitus and hearing impairment.

Metabolism: Thyroid gland: a single case of malignant neoplasm, discoloration (according to the results of pathomorphological studies), dysfunction.

Other: Change in color of the oral cavity (tongue, gums, palate), change in color of tooth enamel, fever, color of discharge (for example, sweat).

Interaction

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

Due to the fact that bacteriostatic drugs affect the bactericidal effect of penicillins, simultaneous administration of drugs from the penicillin and tetracycline 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 lead to a decrease in the effectiveness of antibiotic therapy.

Cases of terminal renal toxicity have been reported with concomitant use of methoxyfruranium and drugs of the
group
tetracyclines.

Simultaneous use of tetracycline antibiotics and oral contraceptives may lead to a decrease in the effectiveness of contraception.

Avoid taking isotretinoin immediately before, at the same time, or immediately after taking minocycline, since both drugs can cause a benign increase in intracranial pressure.

Concomitant use of drugs from the tetracycline group with ergot alkaloids and their derivatives increases the risk of developing ergotism.

Overdose

Symptoms: dizziness, nausea and vomiting are most common.

Treatment: A selective antidote for minocycline is currently unknown. In case of overdose, it is necessary to stop taking the drug, provide symptomatic treatment and supportive care. Hemo- and peritoneal dialysis remove minocycline in small quantities.

Storage conditions

In a place protected from light and moisture, at a temperature not exceeding 25 °C

Shelf life

2 years

Manufacturer

ABVA RUS, Russia