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Doxycycline

Doxycycline
Doxycycline is intended for the treatment of infections caused by susceptible strains of gram-positive and gram-negative microorganisms and some other microorganisms.

Brand: Doxycycline

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: September 2023
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Doxycycline 200 mg
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Product description

Pharmacological action of Doxycycline 

Buy Doxycycline in Canada

Semisynthetic tetracycline, broad-spectrum bacteriostatic antibiotic. Penetrating into the cell, it acts on intracellular pathogens. Suppresses protein synthesis in a microbial cell, disrupts the connection of transport aminoacyl-RNA with the 30S subunit of the ribosomal membrane.

to it Highly sensitive gram-positive microorganisms: Staphylococcus spp. (including Staphylococcus aureus, Staphylococcus epidermidis), Streptococcus spp. (including Streptococcus pneumoniae), Clostridium spp., Listeria spp .; Actinomyces israeli; and gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Klebsiella spp., Escherichia coli, Shigella spp., Enterobacter, Salmonella spp., Bordetella pertussis. Bacteroides spp., Treponema spp. (including strains resistant to other antibiotics, such as modern penicillins and cephalosporins). The most sensitive are Haemophilus influenzae (91-96%) and intracellular pathogens.

Doxycycline is active against most causative agents of dangerous infectious diseases: plague (Yersinia spp.), Tularemia (Francisella tularensis), anthrax microbes (Bacillus anthracis), Legionella (Legionella spp.), Brucella (Brucella spp.), Vibrio cholera cholera cholera , rickettsia (Rickettsia spp.), pathogens of glanders (Actinobacillus mallei), chlamydia (causative agents of ornithosis (Chlamydia psittaci), psittacosis (Rickettsiaformis psittacosi), trachoma (Chlamydia trachomatis; dysentery (Entamoeba histolytica).

It does not act on most strains of Proteus, Pseudomonas aeruginosa and fungi.

To a lesser extent than other tetracycline antibiotics, it inhibits the intestinal flora, differs from them in more complete absorption and longer duration of action. In terms of the degree of antibacterial activity, doxycycline is superior to natural tetracyclines Unlike tetracycline and oxytetracycline ina has a higher therapeutic efficacy, which is manifested in the treatment of 10 times lower doses, and a longer effect. There is cross-resistance to other tetracyclines as well as to penicillins.

Pharmacokinetics

Absorption - fast and high (about 100%). Reception of food does not significantly affect the degree of absorption. It has a high degree of lipid solubility and low affinity for binding calcium ions (Ca2+). After oral administration of 200 mg, the time to reach the maximum concentration in the blood plasma is 2.5 hours, the maximum concentration in the blood plasma is 2.5 μg / ml, 24 hours after administration is 1.25 μg / ml.

The connection with plasma proteins is 80-93%. Penetrates well into organs and tissues; 30-45 minutes after ingestion, it is found in therapeutic concentrations in the liver, kidneys, lungs, spleen, bones, teeth, prostate gland, eye tissues, in pleural and ascitic fluids, bile, synovial exudate, exudate of maxillary and frontal sinuses, in fluid gingival grooves. Poorly penetrates into the cerebrospinal fluid (10-20% of the plasma level). It penetrates the placental barrier, is determined in human milk. The volume of distribution is 0.7 l / kg.

Metabolized in the liver 30-60%. The half-life is 10-16 hours (mostly 12-14 hours, on average 16.3 hours). With repeated administrations, the drug may accumulate. It accumulates in the reticulo-endothelial system and bone tissue. In bones and teeth, forms insoluble complexes with calcium ions (Ca2+). It is excreted in the bile, where it is found in high concentration. Undergoes intestinal-hepatic recirculation, excreted by the intestines (20-60%); 40% of the dose taken is excreted by the kidneys within 72 hours (of which 20-50% - unchanged), with severe chronic renal failure - only 1-5%.

In patients with impaired renal function or azotemia, gastrointestinal secretion is an important route of elimination.

Indications of the drug Doxycycline

Treatment of respiratory tract infection with Doxycycline

  • infectious and inflammatory diseases caused by sensitive microorganisms: respiratory tract infections (pharyngitis, acute and chronic bronchitis, tracheitis, bronchopneumonia, lobar pneumonia, lung abscess, pleural empyema);

  • infections of the ENT organs (otitis media, tonsillitis, sinusitis, etc.);

  • infections of the genitourinary system (cystitis, pyelonephritis, prostatitis, urethritis, urethrocystitis, urogenital mycoplasmosis, endometritis, endocervicitis, acute orchiepididymitis; gonorrhea);

  • infections of the biliary tract and gastrointestinal tract (cholecystitis, cholangitis, gastroenterocolitis, bacterial dysentery, travelers' diarrhea);

  • infections of the skin and soft tissues (phlegmon, abscesses, furunculosis, panaritium, infected burns, wounds, etc.);

  • infectious eye diseases, syphilis, yaws, yersiniosis, legionellosis, rickettsiosis, chlamydia of various localization (including prostatitis and proctitis), Q fever, Rocky Mountain spotted fever, typhus (including rash, tick-borne, recurrent), Lyme disease (I st. - erythema migrans), bacillary and amoebic dysentery, tularemia, cholera, actinomycosis, malaria; as part of combination therapy - leptospirosis, trachoma, psittacosis, psittacosis, granulocytic ehrlichiosis; whooping cough, brucellosis, osteomyelitis; sepsis, subacute septic endocarditis, peritonitis;

  • prevention of postoperative purulent complications; malaria caused by Plasmodium falciparum, during short travel (less than 4 months) in an area where strains resistant to chloroquine and / or pyrimethamine sulfadoxine are common;

  • as a "first" line drug is prescribed to patients under 65 years of age with exacerbation of chronic bronchitis (including against the background of bronchial asthma) without concomitant diseases (these exacerbations are often caused by Haemophilus influenzae). Effective in exacerbation of bronchopulmonary infection (usually staphylococcal etiology) in patients with cystic fibrosis, chlamydial arthritis, granulocytic ehrlichiosis. In elderly patients, it is used to treat acute prostatitis and urinary infections caused by Escherichia coli.

Dosing regimen

Orally, in adults and children over 12 years of age weighing more than 45 kg, the average daily dose is 200 mg on the first day (divided into 2 doses - 100 mg 2 times a day), then 100 mg / day.

For chronic infections of the urinary system - 200 mg / day throughout the entire period of therapy.

In the treatment of gonorrhea, it is prescribed according to one of the following schemes: acute uncomplicated urethritis - a course dose of 500 mg (1 dose - 300 mg, the next 2 - 100 mg at an interval of 6 hours) or 100 mg / day until complete recovery (in women) or 100 mg 2 times a day for 7 days (in men); for complicated forms of gonorrhea, the course dose is 800-900 mg, which is divided into 6-7 doses (300 mg - 1 dose, then with an interval of 6 hours for 5-6 subsequent doses).

In the treatment of syphilis - 300 mg / day for at least 10 days.

For uncomplicated infections of the urethra, cervix and rectum caused by Chlamydia trachomatis, appoint 100 mg 2 times a day for at least 7 days.

Male genital infections - 100 mg 2 times a day for 4 weeks. Treatment of chloroquine-resistant malaria - 200 mg / day for 7 days (in combination with schizontocidal drugs - quinine); malaria prophylaxis -100 mg once a day 1-2 days before the trip, then every day during the trip and for 4 weeks after returning;

Diarrhea of ​​"travelers" (prevention) - 200 mg on the first day of the trip (for 1 dose or 100 mg 2 times a day), 100 mg 1 time 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 a stay in a disadvantaged area and 200 mg at the end of the trip.

Prevention of infections after medical abortion - 100 mg 1 hour before the abortion and 200 mg 30 minutes after.

With acne - 100 mg / day, course - 6-12 weeks.

The maximum daily dose for adults is up to 300 mg / day or up to 600 mg / day for 5 days in severe gonococcal infections.

In the presence of severe hepatic impairment, a decrease in the daily dose of doxycycline is required, since it gradually accumulates in the body (risk of hepatotoxic action).


Application during pregnancy and lactation

The use of the drug during pregnancy is contraindicated, since, penetrating through the placenta, the drug can disrupt the normal development of teeth, inhibit the growth of the bones of the fetal skeleton, and also cause fatty liver infiltration.

The use of doxycycline is contraindicated during lactation. If it is necessary to use the drug, breastfeeding should be discontinued for the period of treatment.

Application for violations of liver function

Contraindicated in severe hepatic failure. In the presence of severe hepatic impairment, a decrease in the daily dose of doxycycline is required, since it gradually accumulates in the body (risk of hepatotoxic action).

Use in children

Contraindicated in children under 12 years of age (the possibility of the formation of insoluble complexes with calcium ions (Ca2+) with deposition in the bone skeleton, enamel and dentin of the teeth); and children over the age of 12 with a body weight of up to 45 kg.

Application is possible in children over 12 years of age weighing more than 45 kg according to the dosage regimen.

Special instructions

To prevent local irritating effects (esophagitis, gastritis, ulceration of the mucous membrane of the gastrointestinal tract), it is recommended to take it in the daytime with a large amount of liquid, food. Due to the possible development of photosensitization, it is necessary to limit insolation during treatment and for 4-5 days after it. With prolonged use, periodic monitoring of liver function and hematopoietic organs is necessary. It can mask the manifestations of syphilis, and therefore, if a mixed infection is possible, a monthly serological test is required for 4 months. All tetracyclines form stable complexes with calcium ions (Ca2+) in any bone-forming tissue. In this regard, reception during the development of teeth can cause long-term staining of teeth in a yellow-gray-brown color, as well as enamel hypoplasia. 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 doxycycline for a long time, dark brown staining of tissue in microspecimens is possible without impairing its function.

In the experiment, it was found that doxycycline can have a toxic effect on fetal development (delayed skeletal development) - it blocks metalloproteases (enzymes that catalyze the degradation of collagen and proteoglycans) in cartilage, leading to a decrease in lesions in deforming osteoarthritis. When the dose is increased above 4 g, the pharmacokinetics of doxycycline does not depend on the dose and the concentration in the blood does not increase.

When using the drug, both while taking it and 2-3 weeks after stopping treatment, diarrhea caused by Clostridium difficile may develop. In mild cases, it is sufficient to discontinue treatment and use ion exchange resins (cholestyramine, colestipol), in severe cases, it is shown that the loss of fluid, electrolytes and protein is replaced, the appointment of vancomycin, bacitracin or metronidazole. Do not use drugs that inhibit intestinal peristalsis.

Influence on the ability to drive vehicles and control mechanisms

Patients should refrain from all types of activities that require increased attention, quick mental and physical.

Overdose

Symptoms: when high doses are administered, especially in patients with impaired liver function, neurotoxic reactions may appear: dizziness, nausea, vomiting, seizures, impaired consciousness due to increased intracranial pressure.

Treatment: drug withdrawal, gastric lavage with activated charcoal, symptomatic therapy, antacids and magnesium sulfate are prescribed orally to prevent the absorption of doxycycline. There is no specific antidote. Hemodialysis and peritoneal dialysis are ineffective.

Drug interactions

Absorption is reduced by antacids containing aluminum (Al3+ ), calcium (Ca2+) and magnesium (Mgsalts2+), iron (Fe) preparations, sodium bicarbonate, laxatives containing magnesium salts (Mg2+), colestyramine and colestipol, so their use should be separated at 3 hour intervals.

Due to the suppression of the intestinal microflora, it reduces the prothrombin index, which requires a dose adjustment of indirect anticoagulants.

When combined with bactericidal antibiotics that disrupt the synthesis of the cell wall (penicillins, cephalosporins), the effectiveness of the latter decreases. Reduces the reliability of contraception and increases the frequency of breakthrough bleeding while taking estrogen-containing oral contraceptives.

Ethanol, barbiturates, rifampicin, carbamazepine, phenytoin, and other stimulants of microsomal oxidation, accelerating the metabolism of doxycycline, reduce its plasma concentration.

With simultaneous use with methoxyflurane, the development of acute renal failure, up to a lethal outcome, is possible.

The simultaneous use of retinol increases intracranial pressure.


Side effect

From the nervous system: a benign increase in intracranial pressure (decreased appetite, vomiting, headache, edema of the optic nerve head), toxic effects on the central nervous system (dizziness or instability),

Metabolic disorders: anorexia.

On the part of the hearing and vestibular apparatus: ringing in the ears.

From the side of the organs of vision: blurred vision, scotoma and diplopia as a result of increased intracranial pressure.

From the digestive system: nausea, constipation or diarrhea, abdominal pain, glossitis, dysphagia, esophagitis (including erosive), gastritis, ulceration of the stomach and 12 duodenal ulcer, pseudomembranous colitis, enterocolitis (due to the proliferation of resistant strains of staphylococcus aureus ).

Allergic reactions: maculopapular rash, pruritus, skin flushing, angioedema, anaphylactoid reactions, medicinal lupus erythematosus, erythematous rash, exfoliative dermatitis, urticaria, anaphylaxis, anaphylactic shock, anaphylactic Stevens-Jones syndrome.

From the side of the cardiovascular system: pericarditis, lowering blood pressure, tachycardia, erythema multiforme.

On the part of the hematopoietic organs: hemolytic anemia, thrombocytopenia, neutropenia, leukopenia, eosinophilia, decreased prothrombin index.

From the hepatobiliary system: liver dysfunction, increased hepatic transaminases, autoimmune hepatitis, cholestasis.

Musculoskeletal apparatus: arthralgia, myalgia.

Dysfunction of the kidneys and urinary tract: an increase in the level of residual urea nitrogen.

Others: photosensitivity, superinfection; persistent discoloration of tooth enamel, inflammation in the anogenital zone. Candidiasis (vaginitis, glossitis, stomatitis, proctitis), dysbiosis, a syndrome similar to serum sickness, toxic epidermal necrolysis.