Co-trimoxazole

General characteristics. Structure:

Active ingredient: 400 mg of sulfamethoxazole, 80 mg of Trimethoprimum.

Excipients: starch corn, sodium starch, Natrium benzoicum, magnesium glikolit stearate, talc.

Co-trimoxazole has bactericidal, bacteriostatic and antiprotozoan action.

Pharmacological properties:

Pharmacodynamics. Bacteriostatic action of sulfamethoxazole is connected with inhibition of process of utilization of PABK and disturbance of synthesis of dihydrofolic acid in bacterial cells. Trimethoprimum inhibits enzyme which participates in utilization of folic acid, turning dihydrofolate into tetrahydrofolate. Thus, 2 consecutive stages of biosynthesis of purines and, therefore, nucleic acids which are necessary for growth and reproduction of bacteria are blocked. High concentration are created in tissues of lungs, kidneys, a prostate, in cerebrospinal fluid, bile, bones.

Co-trimoxazole is active concerning gram-positive microorganisms: cocci – Staphylococcusspp. (including producing a penicillinase), Streptococcusspp., including Streptococcuspneumoniae; bacteria - Corynebacteriumdiphtheriae; gram-negative microorganisms: cocci - Neisseriagonorrhoeae; bacteria - EscherichiacoliShigellaspp. Salmonellaspp. Proteusspp. Klebsiellaspp. Yersiniaspp. VibriocholeraeHaemophilusinfuenzae; anaerobic asporous bacteria - Bacteroidesspp.; concerning Chlamidiaspp.

Are steady against the drug Pseudomonasaeruginosa, Trepoinemaspp., Mycoplasmaspp., Mycobacteriumtuberculosis, and also viruses and mushrooms.

Pharmacokinetics. After intake sulfamethoxazole and Trimethoprimum are quickly soaked up from a GIT. Meal slows down their absorption. Are widely distributed in fabrics and liquids of an organism. Linkng of Trimethoprimum with proteins of plasma – 50%, sulfamethoxazole – 66%. The elimination half-life makes 8,6 – 17 hours, sulfamethoxazole – 9-11 hours. Trimethoprimum is removed with urine, is preferential in not changed look.

Indications to use:

- the infectious and inflammatory diseases caused by microorganisms, sensitive to co-trimoxazole:
- respiratory infections (including acute and chronic bronchitis, pleura empyema, bronchoectatic disease, lung abscess, pneumonia, tonsillitis, pharyngitis);
- infections of urinary tract (including gonococcal urethritis, cystitis, pyelitis, chronic pyelonephritis, prostatitis);
- GIT infections (enteritis, typhoid, paratyphoid, dysentery, cholecystitis, cholangitis);
- infections of skin and soft tissues (pyoderma, furunculosis, wound fever);
septicaemia, brucellosis.

Route of administration and doses:

Appoint inside. To adults and children 12 years are more senior give usually 2 tablets (for adults) 2 times a day (in the morning and in the evening after food); in hard cases appoint 3 tablets 2 times a day; at persistent infections – on 1 tablet 2 times a day. To children from 2 to 5 years usually appoint ½ tablets 2 times a day, from 5 to 12 years – on 1 tablet 2 times a day.

The course of treatment proceeds from 5 to 12-14 days, and at persistent infections it longer also depends on disease.

Features of use:

During therapy it is necessary to consume enough liquid. Drug is appointed with care to patients with possible deficit of folic acid, allergic reactions in the anamnesis, bronchial asthma, abnormal liver functions, kidneys, a thyroid gland. At prolonged use of drug it is necessary to conduct systematically researches of a picture of peripheral blood, a functional condition of a liver and kidneys.

Additional purpose of folic acid is recommended to elderly patients. At disturbances of functions of kidneys the dose should be reduced, and to increase intervals between receptions.

Administration of drug is not recommended to children of early age.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, a glossitis, a diarrhea, stomach pains, lack of appetite, a lozhnodifteriyny inflammation of intestines, increase in content of enzymes (enzymes) in a liver and creatinine in blood serum, an oral cavity inflammation, a language inflammation, a pancreas inflammation, cholestatic hepatitis.

Allergic reactions: allergic myocarditis, fever, medicamentous fever, photosensitization, anaphylactic symptoms, skin rash, Quincke's edema, Stephens-Jones's syndrome, Lyell's disease,

From a hemopoiesis: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastny anemia.

From an urinary system: crystalluria, hamaturia, intersticial nephrite.

Metabolism: hypopotassemia, hyponatremia.

Nervous system: apathy, aseptic meningitis, ataxia, headache, depression, spasm, hallucinations, nervousness, sonitus, inflammation of spinal nerves.

Bodies of incretion: cross allergy, hypoglycemia, increase in a piurez.

Musculoskeletal system: pains of joints, muscular pains.

Respiratory organs: suffocation, cough, infiltrates in lungs.

Others: easing, feeling of fatigue, sleeplessness.

Interaction with other medicines:

Interaction with other medicines

At simultaneous use of co-trimoxazole with anticoagulants of indirect action the effect of the last considerably amplifies because of delay of an inactivation of the last, and also their release from communication with proteins of plasma.

At combinative use with some derivatives of sulphonylurea strengthening of gipoglikemiziruyushchy effect is possible.

Simultaneous use of co-trimoxazole and methotrexate can lead to increase in toxicity of the last (in particular, to emergence of a pancytopenia).

Under the influence of Butadionum, indometacin, Naproxenum, salicylates and some other NPVS strengthening of effect of co-trimoxazole with development of undesirable effects as there is a release of active agents from communication with blood proteins and increase in their concentration is possible.

The concomitant use of diuretics and co-trimoxazole increases probability of development of the thrombocytopenia caused by the last, especially in patients of advanced age. In case of co-administration of Chloridinum with co-trimoxazole antimicrobic action amplifies as Chloridinum slows down formation of the tetrahydrofolic acid necessary for synthesis of nucleic acids and proteins. In turn streptocides slow down formation of dihydrofolic acid, being the predecessor of tetrahydrofolic acid. This combination is widely used at treatment of a toxoplasmosis. Absorption of co-trimoxazole at joint reception with holestiraminy decreases as a result of formation of insoluble complexes that leads to decrease in their concentration in blood.

Contraindications:

The expressed renal failures and a liver, blood diseases, deficit glyukozo-6-fosfatdegidrogenazy, a lactation, hypersensitivity to streptocides and Trimethoprimum.

Streptocides and Trimethoprimum get through a placenta, are emitted with breast milk. Can cause in a fruit and newborn children development of a kernicterus and hemolitic anemia. Besides, the risk of development of fatty infiltration of a liver in pregnant women increases. Therefore use of co-trimoxazole for pregnant women is contraindicated. If necessary to accept drug in the period of a lactation breastfeeding needs to be stopped.

Overdose:

Symptoms: anorexia, nausea, weakness, abdominal pains, headache, drowsiness, hamaturia, crystalluria.

Treatment: plentiful drink, gastric lavage, correction of electrolytic disturbances. If necessary appoint a hemodialysis.

Oppression of marrow is characteristic of chronic overdose (pancytopenia).

Treatment and prevention: purpose of folic acid (5 – 15 mg daily).

Storage conditions:

List B. In the place protected from moisture and light at a temperature not over +25 ºС. Period of validity of 5 years.

Issue conditions:

According to the recipe

Packaging:

On 10 or 20 tablets in banks polymeric. On 10 tablets in a blister strip packaging. One bank or 1 or 2 blister strip packagings together with a leaf insert in secondary packaging.