Pharmacological action

Semi-synthetic antibiotic from the tetracycline group. It has a bacteriostatic effect on cells of sensitive strains of microorganisms due to the reversible inhibition of protein synthesis at the level of the 30S subunits of ribosomes. It has a wide range of antibacterial activity.

The sensitivity of microorganisms:

aerobic Gram positive - some of the microorganisms listed below have shown resistance to minocycline, therefore laboratory sensitivity testing is recommended before use - Bacillus anthracis, Listeria monocytogenes, Staphylococcus aureus, Streptococcus pneumoniae. Antibiotics from the tetracycline group are not recommended for the treatment of streptococcal and staphylococcal infections, unless the susceptibility of microorganisms to minocycline is indicated;
Aerobic Gram negative - Bartonella bacilliformis, species Brucella, Calymmatobacterium granulomatis, Campylobacter fetus, Francisella tularensis, Haemophilus ducrey, Vibrio cholerae, Yersinia pestis.

For the following microorganisms, sensitivity studies to minocycline are strongly recommended: Acinetobacter species, Enterobacter aerogenes, Escherichia coli, Haemophilus influenzae, Klebsiella species, Neisseria gonorrhoeae, Neisseria meningitidis, Shigella species.

Pharmacokinetics

Aspiration

Eating does not significantly affect the degree of absorption of minocycline. Minocycline has a high degree of lipid solubility and a low affinity for binding to Ca2 +. Rapidly absorbed from the digestive tract in proportion to the dose taken. The maximum concentration of minocycline in plasma (Cmax) after oral administration at a dose of 200 mg is 3.5 mg / l and is reached (Tmax) after 2 to 4 hours.

Distribution

The binding to blood proteins is 75%, the effect of various diseases on this parameter has not been studied. Vd is 0.7 L / kg. Minomycin penetrates well into organs and tissues: 30 to 45 minutes after ingestion, it is found in therapeutic concentrations in the kidneys, spleen, eye tissue, pleural and ascites fluids, synovial exudate, exudate from the maxillary and frontal sinuses, and into the gingival sulcus fluid. It penetrates well into the cerebrospinal fluid (20-25% of the level determined in the plasma). Penetrates through the placental barrier, excreted in breast milk.

With repeated injections, the drug can accumulate. It accumulates in the reticuloendothelial system and bone tissue. Forms insoluble complexes with Ca2 + in bones and teeth.

Breeding

It undergoes enterohepatic recirculation, 30 to 60% of the dose taken is excreted with the intestinal contents; 30% are excreted by the kidneys in 72 hours (of which 20-30% - unchanged), with severe chronic renal failure - only 1-5%. The half-life (T1 / 2) of minocycline is approximately 16 hours.

Indications

Minocycline hydrochloride is used to treat the following diseases, provided that the sensitivity of pathogenic microorganisms:

acne;
skin infections;
spotted fever, typhoid fever, typhoid fever, Q fever (coxiellosis), vesicular rickettsial disease and tick-borne fever;
respiratory tract infections;
venereal lymphogranuloma;
ornithosis;
trachoma (infectious keratoconjunctivitis);
conjunctivitis with inclusions (paratrachoma);
non-gonococcal urethritis, infections of the cervical canal and anus in adults;
cyclic fever;
chancroid;
plague;
tularemia;
cholera;
brucellosis;
bartonella;
inguinal granuloma;
syphilis;
gonorrhea;
raspberry (tropical granuloma, non-venereal syphilis);
listeriosis;
anthrax;
Vincent's sore throat;
actinomycosis.

In the case of acute intestinal amebiasis, the use of minocycline in addition to amebicidal drugs is authorized.

In severe acne, minocycline can be used as an adjunct treatment. The use of minocycline is indicated for the asymptomatic carriage of Neisseria meningitidis for the eradication of meningococci from the nasopharynx.

To avoid the development of resistance, the use of minocycline is recommended in accordance with the results of laboratory tests, including serotyping and the determination of the susceptibility of pathogens. For the same reason, the use of minocycline for prophylactic purposes is not recommended in cases of high risk of contracting meningococcal meningitis. Clinical experience has shown the efficacy of minocycline in the treatment of Mycobacterium marinum infections, but these data are currently not supported by controlled clinical trials.

Dosage schedule

The drug is taken orally after a meal. It is recommended to drink the capsules with a sufficient amount of liquid (milk can be) to reduce the risk of irritation and ulceration in the esophagus.

The initial dose of Minolexin® is 200 mg (2 capsules 100 mg or 4 capsules 50 mg), then 100 mg (1 capsule 100 mg or 2 capsules 50 mg) every 12 hours (2 times / day). The maximum daily dose should not exceed 400 mg. Infections of the genitourinary system and the anogenital region caused by chlamydia and ureaplasma: 100 mg (1 capsule of 100 mg or 2 capsules of 50 mg) every 12 hours for 7 to 10 days.

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

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

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

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

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

Acne: 50 mg (1 capsule of 50 mg) per day, with a long course of 6 to 12 weeks.

Against the background of taking the drug, due to the anti-anabolic effect inherent in drugs from the tetracycline group, an increase in the level of urea in the blood plasma can be observed. In patients with normal kidney function, this does not require stopping the drug. In patients with severe renal impairment, development of azotemia, hyperphosphatemia and acidosis may occur. In this situation, it is necessary to control the level of urea and creatinine in the blood plasma, the maximum daily dose of minocycline should not exceed 200 mg. The pharmacokinetics of minocycline in patients with renal impairment (CC less than 80 ml / min) is currently insufficiently studied to conclude that a dose adjustment is necessary.

In case of liver failure, use the drug with caution.

Children over 8 years of age with infections caused by pathogens sensitive to minocycline: the initial dose is 4 mg / kg, then 2 mg / kg every 12 hours.

Side effect

The spectrum of adverse events associated with minocycline administration does not differ from other tetracyclines.

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

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

On the part of the skin: baldness, knotty erythema, nail pigmentation, itching, toxic epidermal necrosis, vasculitis, maculopapular and erythematous rashes, Stevens-Johnson syndrome, exfoliative dermatitis. From the respiratory system: 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 (Shenlein-Genoch violet), pericarditis, exacerbations of systemic lupus, pulmonary infiltration, accompanied by eosinophilia.

From the hemopoietic system: agranulocytosis, hemolytic anemia, thrombocytopenia, leukopenia, neutrocytopenia, pancytopenia, eosinopenia, eosinophilia.

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

Sensory organs: tinnitus and hearing impairment.

In terms of metabolism: a single case of malignant neoplasm of the thyroid gland, discoloration (according to the results of pathomorphological studies), impaired thyroid function.

Other: discoloration of the oral cavity (tongue, gums, palate), discoloration of tooth enamel, fever, staining of secretions (for example, sweat).

Cons-indications

hypersensitivity to minocycline, tetracyclines and other components of the drug;
porphyria;
severe liver failure;
severe renal failure;
leukopenia;
systemic lupus erythematosus;
simultaneous administration of isotretinoin;
pregnancy;
lactation (breastfeeding);
age of children up to 8 years (period of tooth development);
lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

With caution, the drug should be prescribed for liver and kidney failure, the simultaneous use of hepatotoxic drugs.

Pregnancy and breast feeding

During pregnancy, minocycline is only recommended in cases where the expected benefits from its use for the mother outweigh the potential risk to the fetus.

During treatment with minocycline, breastfeeding is stopped.

Use for impaired liver function

With caution, the drug should be prescribed for liver failure. The use of the drug is contraindicated in severe liver failure.

Use in renal failure

With caution, the drug should be prescribed for kidney failure.

The use of the drug is contraindicated in severe renal impairment.

Use in children

The use of the drug is contraindicated in children under 8 years of age (period of dental development).

Special instructions

In case of prolonged use of minocycline, the cellular composition of peripheral blood should be regularly monitored, liver function tests should be performed and serum nitrogen and urea concentrations should be determined.

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

Perhaps a false increase in the level of catecholamines in the urine when determined by the fluorescent method.

When examining a thyroid biopsy sample from patients who have been taking tetracyclines for a long time, the possibility of dark brown tissue staining in micropreparations should be taken into account.

In the context of taking the drug and 2 to 3 weeks after stopping treatment, the development of diarrhea caused by Clostridium dificile (pseudomembranous colitis) is possible. In mild cases, stopping treatment and using ion exchange resins (colestyramine, colestipol) is sufficient, in severe cases, compensating for the loss of fluid, electrolytes and proteins, appointing vancomycin, bacitracin or metronidazole are indicated. Do not use drugs that inhibit bowel motility.

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

In the case of sexually transmitted diseases, in case of suspected syphilis concomitant, it is necessary to carry out a microscopic examination in a dark field before starting treatment. Serological diagnosis of blood serum is recommended at least once in 4 months.

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

Action algorithms in case of side effects:

in case of secondary infection, minocycline should be discontinued and appropriate therapy prescribed;
if the intracranial pressure increases, minocycline should be stopped;
diarrhea is a common disorder associated with taking antibiotics. In case of diarrhea during treatment with minocycline, it is urgent to consult a doctor;
tetracycline antibiotics cause increased sensitivity to direct sunlight and ultraviolet rays. If erythema occurs, stop taking the antibiotic.

Influence on the ability to drive vehicles and control mechanisms

Care should be taken when driving vehicles and other potentially dangerous activities that require increased concentration of attention and the speed of psychomotor reactions, as minocycline has a side effect such as dizziness.

Overdose

Symptoms: dizziness, nausea and vomiting are most commonly seen.

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

Drug interaction

Medicines in the tetracycline group reduce the activity of prothrombin in the blood plasma, which may require a reduction in the doses of anticoagulants in patients receiving anticoagulant therapy.

Since bacteriostatic drugs affect the bactericidal effect of penicillins, the simultaneous administration of penicillin and tetracycline groups should be avoided.

The absorption of tetracyclines is impaired when taken with antacids containing aluminum, calcium, magnesium or medicines containing iron, which can lead to a decrease in the effectiveness of antibiotic therapy.

There have been cases of end-stage renal toxicity while taking methoxyfrurane and drugs from the tetracycline group.

Co-administration of tetracycline antibiotics and oral contraceptives may decrease the effectiveness of contraception.

You should avoid taking isotretinoin immediately before, simultaneously and immediately after taking minocycline, as both drugs can cause a mild increase in intracranial pressure.

Co-administration of drugs from the tetracycline group with ergot alkaloids and their derivatives increases the risk of ergotism.

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