Doxycycline Solution pills dispersible 100 mg, 10 pcs.

Composition

Per tablet:Active ingredient: doxycycline monohydrate – 104.00 mg, in terms of doxycycline-100.00 mg. Auxiliary substances: lactose monohydrate (milk sugar) – 140.80 mg; microcrystalline cellulose – 96.00 mg; low – grade hyprolose – 29.25 mg; sodium saccharinate – 10.00 mg; hypromellose – 5.85 mg; magnesium stearate – 3.12 mg; colloidal silicon dioxide – 0.98 mg

. Pharmacological action

Pharmacotherapy group: antibiotic-Tetracycline code ATX: J01AA02 Pharmacological action action

Pharmacodynamics

A broad-spectrum antibiotic from the tetracycline group. It acts bacteriostatically, suppresses protein synthesis in the microbial cell by interacting with the 30S subunit of ribosomes. It is active against many gram-positive and Gram-negative microorganisms: Streptococcus spp., Treponema spp., Staphylococcus spp., Klebsiella spp., Enterobacter spp. (including E. aerugenes), Neisseria gonorrhoeae. Neisseria meningitidis, Haemophilus influenzae, Chlamydia spp., Mycoplasma spp., Ureaplasma urealyticum, Listeria monocytogenes, Rickettsia spp, Typhus exanthematicus, Escherichia coli, Shigella spp., Campylobacter fetus, Vibrio cholerae, Yersinia spp. (including Yersinia pestis), Brucella spp., Francisella tularensis, Bacillus anthracis, Bartonella bacilliformis, Pasteurella multocida, Borrelia recurrentis, Clostridium spp. (except Clostridium difficile), Actinomyces spp., Fusobacterium fusiforme, Calymmatobacterium granulomatosis, Propionibacterium acnes, some of the protozoa (Entamoeba spp., Plasmodium falciparum).

As a rule, it does not act on Acinetobacter spp., Proteus spp., Pseudomonas spp., Serratia spp., Providencia spp., Enterococcus spp.

It is necessary to take into account the possibility of acquired resistance to doxycycline in a number of pathogens, which is often cross-linked within the group (i. e., strains resistant to doxycycline will simultaneously be resistant to the entire group of tetracyclines).

Pharmacokinetics

Suction

Absorption is fast and high (about 100%). Food intake does not significantly affect the absorption of the drug.

The maximum concentration of doxycycline in the blood plasma (2.6-3 mcg/ml) is reached 2 hours after taking 200 mg; after 24 hours, the concentration of the Active ingredient in the blood plasma decreases to 1.5 mcg / ml.

After taking 200 mg on the first day of treatment and 100 mg per day on subsequent days, the concentration of doxycycline in blood plasma is 1.5-3 mcg / ml.

Distribution

Doxycycline reversibly binds to plasma proteins (80-90%), penetrates well into organs and tissues, poorly – into the cerebrospinal fluid (10-20% of the concentration in blood plasma), but the concentration of doxycycline in the cerebrospinal fluid increases with inflammation of the cerebrospinal membrane.

The volume of distribution is 1.58 l / kg. In 30-45 minutes after oral administration, doxycycline is detected in therapeutic concentrations in the liver, kidneys, lungs, spleen, bones, teeth, prostate gland, eye tissues, pleural and ascitic fluids, bile, synovial exudate, maxillary and frontal sinus exudate, and gingival sulcus fluid.

With normal liver function, the concentration of doxycycline in bile is 5-10 times higher than in plasma.

In saliva,5-27% of the concentration of doxycycline in blood plasma is determined.

Doxycycline penetrates the placental barrier and is secreted in small amounts into breast milk. It accumulates in dentin and bone tissue.

Metabolism

A small part of doxycycline is metabolized.

Deduction

The half-life after a single oral dose is 16-18 hours, after repeated doses – 22-23 hours. Approximately 40% of the administered doxycycline is excreted by the kidneys and 20-40% is excreted by the intestines as inactive forms (chelates).

Pharmacokinetics in special clinical cases

The half-life of doxycycline in patients with impaired renal function does not change, because its intestinal excretion increases. Hemodialysis and peritoneal dialysis do not affect the concentration of doxycycline in blood plasma.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to doxycycline:

• respiratory tract infections, including pharyngitis, acute bronchitis, exacerbation of chronic obstructive pulmonary disease, bronchitis, bronchopneumonia, lobar pneumonia, community-acquired pneumonia, lung abscess, empyema;
• infections of the upper respiratory tract, including otitis media, sinusitis, tonsillitis;
• infections of the genitourinary system: cystitis, pyelonephritis, bacterial prostatitis, urethritis, urethrocystitis, urogenital mycoplasmosis, acute orchiepididymitis; endometritis, endocervicitis and oophoritis in a combination therapy; including sexually transmitted infections: genital chlamydia, syphilis in patients with intolerance to penicillins, uncomplicated gonorrhea (as an alternative therapy), inguinal granuloma, lymphogranuloma venereum,
• an infection of the gastrointestinal tract and biliary tract diseases (cholera, yersiniosis, cholecystitis, cholangitis, gastroenterocolitis, bacillary and amoebic dysentery, diarrhea “travelers”);
• infections of skin and soft tissue (including wound infection after an animal bite), severe acne (as part of combination therapy);
• other diseases: yaws, legionellosis, chlamydia various locations (including prostatitis and proctitis), rickettsiosis, a fever, Rocky mountain spotted fever, fever (including typhus, tick), Lyme disease (I. – the erythema migrans), tularemia, anthrax, actinomycosis, malaria and communicable diseases of the eye, in a combination therapy – trachoma; leptospirosis, psittacosis, ornithosis, anthrax (including pneumonic form), bartonellosis, granulocyte herlihys; whooping cough, brucellosis, osteomyelitis; septicemia, subacute bacterial endocarditis, peritonitis;
• prevention of postoperative septic complications; malaria due to Plasmodium falciparum in short-term travel (less than 4 months). in the area where the prevalent strains resistant to chloroquine and/or pyrimethamine-sulfadoxine.

Use during pregnancy and lactation

Doxycycline penetrates the blood-placental barrier. Tetracyclines have an adverse effect on the fetus (slowing down osteogenesis) and on the formation of tooth enamel (irreversible discoloration, hypoplasia). Because of this, as well as the increased risk of liver damage in the mother, tetracyclines are not used during pregnancy, except in cases where the drug is the only means for the treatment or prevention of particularly dangerous and severe infections (Rocky Mountain spotted fever, inhalation exposure to Bacillus anthracis, etc. ). Before prescribing doxycycline to women of childbearing age, the presence of pregnancy should be previously excluded. Doxycycline passes into breast milk. Due to the adverse effect on the fetus, doxycycline, like other tetracyclines, is not used during breastfeeding. If the administration of tetracyclines is necessary, breast-feeding is discontinued.

Contraindications

• hypersensitivity to doxycycline, other tetracyclines or other components of the drug;
• pregnancy; breast-feeding;
• children under 8 years of age;
• severe liver and/or kidney function disorders;
• porphyria;
• lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Side effects

From the gastrointestinal tract: anorexia, nausea, vomiting, dysphagia, diarrhea, anal pruritus, esophagitis, esophageal ulcer, dark staining of the tongue. With long-term therapy, there may be a deficiency of B vitamins due to the suppression of the growth of vitamin B-producing bacteria in the normal intestinal microflora. Allergic reactions: exacerbation of systemic lupus erythematosus, a syndrome similar to serum sickness, erythema multiforme, low blood pressure, tachycardia, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms (DRESS-syndrome). From the side of the skin: urticaria, photosensitivity, angioedema, anaphylactic reactions, maculopapular and erythematous rash, exfoliative dermatitis, Schonlein-Henoch purpura, photonicholysis. From the cardiovascular system: pericarditis. From the liver: liver damage, sometimes associated with pancreatitis (with prolonged use of the drug or in patients with renal or hepatic insufficiency), cholestasis. From the side of the kidneys: an increase in the concentration of residual urea nitrogen due to the antianabolic effect of the drug, aggravation of azotemia in patients with renal insufficiency. The use of products containing citric acid, while taking doxycycline, can cause symptoms similar to Fanconi syndrome: albuminuria, glucosuria, hypophosphatemia, hypokalemia) and renal tubular acidosis. From the hematopoietic system: hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia, decreased prothrombin activity. Nervous system disorders: benign increase in intracranial pressure (anorexia, vomiting, headache, tinnitus, tremor, edema of the optic nerve), vestibular disorders (dizziness or instability), hallucinations, blurred vision, scotoma, double vision. From the thyroid gland: in patients who have been treated with tetracycline antibiotics for a long time, reversible dark brown staining of thyroid tissue is possible, in most cases not accompanied by a violation of its function.From the side of teeth and bones: doxycycline slows down osteogenesis, disrupts the normal development of teeth in children (the color of teeth irreversibly changes, enamel hypoplasia develops). From the musculoskeletal system: arthralgia, myalgia. Other services: candidiasis, glossitis, staphylococcal enterocolitis, pseudomembranous colitis, anogenital candidiasis, stomatitis, vaginitis.

Interaction

Antacids containing aluminum, magnesium, calcium, iron preparations, sodium bicarbonate, magnesium-containing laxatives reduce the absorption of doxycycline, so their use should be separated by an interval of 3 hours. Due to the suppression of intestinal microflora by doxycycline, the prothrombin index decreases, which requires dose adjustment of indirect anticoagulants. When doxycycline is combined with bactericidal antibiotics that disrupt cell wall synthesis (penicillins, cephalosporins), the effectiveness of the latter decreases. Doxycycline reduces the reliability of contraception and increases the frequency of acyclic bleeding when taking estrogen-containing hormonal contraceptives. Ethanol, barbiturates, rifampicin, carbamazepine, phenytoin, etc. stimulators of microsomal oxidation, accelerating the metabolism of doxycycline, reduce its concentration in blood plasma. Simultaneous use of doxycycline and retinol increases intracranial pressure.

How to take, course of administration and dosage

Inside. Tablets are dissolved in a small amount of water (about 20 ml) to form a suspension, tablets can also be swallowed whole, divided into parts or chewed with water. Preferably taken with a meal. Take tablets sitting or standing, which reduces the likelihood of developing esophagitis or esophageal ulcers. The drug should not be taken immediately before bedtime. Usually, the duration of treatment is 5-10 days. Adults and children over 8 years of age with a body weight of more than 50 kg receive 200 mg in 1-2 doses on the first day of treatment, then 100 mg daily. In cases of severe infections, the drug is prescribed at a dose of 200 mg daily for the entire course of treatment. For children aged 8-12 years with a body weight of less than 50 kg, the average daily dose is 4 mg / kg on the first day, then 2 mg / kg per day (in 1-2 doses). In cases of severe infection, the drug is used at a dose of 4 mg/kg daily for the entire course of treatment. Dosage features for certain diseasesin case of infection caused by S. pyogenes, the drug is taken for at least 10 days. Uncomplicated gonorrhea (with the exception of anorectal infections in men):Adults – 100 mg 2 times a day until complete cure (on average for 7 days), or for one day 600 mg – 300 mg in 2 doses (the second reception 1 hour after the first) is prescribed. For primary syphilis-100 mg 2 times a day for 14 days, for secondary syphilis-100 mg 2 times a day for 28 days. For uncomplicated urogenital infections caused by Chlamydia trachomatis, cervicitis, non-gonococcal urethritis caused by Ureaplasma urealiticum-100 mg 2 times a day for 7 days. For acne – 100 mg 1 time a day, the course of treatment is 6-12 weeks. Malaria (prevention): 100 mg once a day 1-2 days before the trip, then daily during the trip and for 4 weeks after returning; children over 8 years – 2 mg / kg once a day. Travelers ‘ diarrhea (prevention) – 200 mg on the first day of the trip in 1 or 2 doses, then 100 mg once a day during the entire stay in the region (no more than 3 weeks). Treatment of leptospirosis – 100 mg orally 2 times a day for 7 days; prevention of leptospirosis-200 mg once a week during your stay in a poor area and 200 mg at the end of the trip. In order to prevent infections during medical abortion – 100 mg 1 hour before and 200 mg after the intervention. The maximum daily dose for adults is up to 300 mg / day or up to 600 mg / day for 5 days for severe gonococcal infections. For children over 8 years of age with a body weight of more than 50 kg – up to 200 mg, for children 8-12 years of age with a body weight of less than 50 kg-4 mg / kg daily during the entire treatment. In the presence of renal insufficiency (creatinine clearance less than 60 ml/min) and / or hepatic insufficiency, a reduction in the daily dose of doxycycline is required, since it gradually accumulates in the body (risk of hepatotoxic effects).

Overdose

Symptoms: Increased dose-dependent adverse reactions caused by liver damage – vomiting, fever, jaundice, azotemia, increased transaminase activity, increased prothrombin time. Treatment Immediately after taking large doses, gastric lavage, heavy drinking, and, if necessary, inducing vomiting are recommended. Take activated charcoal and osmotic laxatives. Hemodialysis and peritoneal dialysis are not recommended due to low efficacy.

Special instructions

There is a possibility of cross-resistance and hypersensitivity with other tetracycline drugs.

Tetracyclines may increase prothrombin time, and the use of tetracyclines in patients with coagulopathy should be carefully monitored.

The antianabolic effect of tetracyclines can lead to an increase in the concentration of residual urea nitrogen in the blood. As a rule, this is not significant for patients with normal renal function. However, patients with renal insufficiency may experience an increase in azotemia.

The use of tetracyclines in patients with impaired renal function requires medical supervision.

With prolonged use of the drug, periodic monitoring of laboratory parameters of blood, liver and kidney function is required.

Due to the possible development of photodermatitis, it is necessary to limit sun exposure during treatment and for 4-5 days after it.

When using the drug, both against the background of taking it, and 2-3 weeks after stopping treatment, diarrhea caused by Clostridium difficile may develop. In mild cases, it is sufficient to cancel treatment and use ion exchange resins (colestyramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin, metronidazole is indicated. Do not use medications that inhibit intestinal motility.

Prolonged use of the drug can cause dysbiosis and, as a result, the development of hypovitaminosis (especially B vitamins).

To prevent dyspeptic symptoms, it is recommended to take the drug with meals.

To avoid the development of esophagitis or esophageal ulcers, it is necessary to take the drug with plenty of water and avoid using it immediately before bedtime.

Influence on the ability to drive vehicles and mechanisms

The effect on the ability to drive vehicles, machines and mechanisms is unknown.

In case of dizziness, blurred vision or double vision, driving vehicles or mechanisms is not recommended (see “Side effects”).

Storage conditions

At a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date.

Active ingredient

Doxycycline

Conditions of release from pharmacies

By prescription

Dosage form

tablets soluble

Weight

Weight: 12 gr.