Co-trimoxazole [Sulfamethoxazole + Trimethoprim]

When ATH:
J01EE01

Pharmacological action.
Antibacterial, broad antibacterial spectrum, bactericide, protivoprotozoynymi.

Application.

Respiratory Tract Infections: bronchitis (sharp and chronic, relapse prevention), bronchiectasis, empyema, lung abscess, pneumonia (Treatment and Prevention), incl. caused Pneumocystis carinii AIDS patients; urinary tract: uretrit, cystitis, pyelitis, pyelonephritis, prostatitis, epididymitis; urogenital: gonorrhea, chancroid, lymphogranuloma venereum, inguinal pellets; GI: bacterial diarrhea, dysenteries, cholera (in a combination therapy), typhoid and paratyphoid (incl. bacteriocarrier), cholecystitis, kholangit, gastroenteritis, caused by strains enterotoksichnymi E.coli; skin and soft tissue: acne, furunculosis, pyoderma, mug, wound infections, soft tissue abscesses; ENT: otitis media, sinusitis, laringit; Surgical; septicemia, meningitis, osteomyelitis (acute and chronic), encephalopyosis, ostrıy brucellosis, South American blastomycosis, malaria (Plasmodium falciparum), Toxoplasmosis and pertussis (in the complex therapy).

Contraindications.

Hypersensitivity (incl. to sulfonamides or trimethoprim), liver or kidney failure, B12-defitsitnaya anemia, agranulocytosis, leukopenia, deficiency of glucose-6-fosfatdegidrogenazы, pregnancy, lactation, childhood (to 2 months — for oral, to 6 for injecting), hyperbilirubinemia in children.

Side effects.

From the digestive tract: dyspepsia, nausea, vomiting, anorexia, rarely, cholestatic and necrotic hepatitis, increase in transaminases and bilirubin, pseudomembranous enterocolitis, pancreatitis, stomatitis, glossitis.

From the side of hematopoiesis: agranulocytosis, aplasticheskaya anemia, thrombocytopenia, gemoliticheskaya anemia, megaloblasticheskaya anemia, gipoprotrombinemii, metgemoglobinemiâ, eozinofilija.

From the urinary system: kristallurija, renal failure, interstitial nephritis, increase in plasma creatinine, toksicheskaya nephropathy oligouriey and anuriey.

Allergic reactions: hives, rash, toxic epidermal necrolysis (Lyell's syndrome), Syndrome Stevens - Johnson, allergic myocarditis, erythema multiforme, exfoliative dermatitis, angioedema, itch, redness of the sclera, fever.

Other: hyperkalemia, giponatriemiya, aseptic meningitis, peripheral neuritis, headache, depression, artralgii, mialgii, weakness, photosensitivity.

Cooperation.

NSAIDs, antidiabetic drugs (sulfonylureas), difenin, indirect anticoagulants, thiazide diuretics, barbiturates enhance therapeutic (and by) effects (displaced from binding with plasma proteins and increased blood concentration), anestein novocaine-reduced (tk. as a result of their hydrolysis is formed PABA). Geksametilentetramin (urotropyn), ascorbic acid increases crystalluria (cause acidification of urine).

Increases effect of phenytoin, difenina, varfarina. Reduces the reliability of oral contraceptives (It inhibits the intestinal microflora and reduce enterohepatic circulation hormonal compounds). Pirimetamin (more 25 mg / Sun) It increases the likelihood of megaloblastic anemia.

Overdose.

Symptoms: anorexia, nausea, vomiting, weakness, stomach ache, headache, drowsiness, hematuria and crystalluria.

Treatment: gastric lavage, IV fluids, correction of electrolyte disturbances. If necessary, Hepatology.

For chronic overdosage is characterized by bone marrow suppression (pancytopenia). Treatment and prevention: appointment of folic acid (5-15 mg daily).

Dosing and Administration.

Inside, / m, / drip. 2 once a day (through 12 no). Single dose: adults and children over 12 years - 960 mg; children 2-6 months-on 120 mg (or 2,5 ml Pediatric suspension), 6 Months - 5 years - 240 mg (or 5 ml Pediatric suspension), 6-12 Years - 480 mg (or 10 ml Pediatric suspension).

Treatment of acute infections continued until the disappearance of clinical symptoms and in the subsequent 2 day, the average duration is not less than 5 days; duration of the course with urinary tract infections, exacerbation of chronic bronchitis, acute otitis media, chancroid, pahovom limfogranulematose — 10-14 days; shigellosis, diarrhea of travelers — 5 days; uncomplicated lower urinary tract infections is 1-3 days; acute brucelleze is 3-4 weeks; bruchnom tife and paratife is 1-3 months; Chronic prostatitis- 3 Months. Parenteral (in severe infections): adults and children over 12 years - 3 ml / m 2 once a day; children 6-12 years - 1,5 ml / m 2 once a day, or/drip in 10-20 ml 250 ml 0,9% sodium chloride solution or 5% glucose solution 2 once a day, children 6-12 years - 18 mg (15 mg sulfametoksazola and 3 mg trimethoprim) on 1 kg body weight 2 once a day. The average duration is 5 days, then oral.

To prevent a recurrence of chronic infections of the urinary system without bacteriuria: adults and children over 12 years - 480 mg 1 once a day at night, Children up to 12 years - 2 mg/kg body weight per day and trimethoprim 10 mg/kg/day sulfamethoxazole, duration: 3-12 months.

In the treatment of pneumonia, caused by Pneumocystis carinii, use higher doses: 15-20 mg/kg trimetoprima and 75-100 mg/kg/day sulfamethoxazole 4 admission, for 14-21 days orally or parenterally. To prevent Pneumocystis pneumonia is normal dose over a period of a possible relapse.

Neoslojnennaya gonorrhoea is on 480 mg 2 once a day, 2 day, or for the first reception is 2,4 g (5 Table.) and by 8 h more 2,4 g, or a single 3,84 g (8 Table.).

With gonococcal infection of the nasopharynx is on 960 mg 3 times / day for 7 days.

In malaria, caused Plasmodium falciparum, appoint 1,92 g (4 Table.) 2 times / day for 2 days.

Precautions.

Patients with impaired kidney with Cl creatinine 15-25 mL/min inside appointed medium doses during the 3 days, further - 50% of the average daily dose; When the values Cl creatinine less than 15 mL/min using (1/2 medium dose) Only against the background of hemodialysis. For parenteral administration in patients with renal insufficiency should determine the concentration of sulfamethoxazole in blood plasma every 2-3 days samples, taken before the next administration (at concentrations above 150 ug/mL treatment stops before reaching the level of 120 ug / ml).

The caution used in a possible deficiency of folic acid (incl. in elderly, patients with chronic alcoholism, malabsorption syndrome — in these cases, with reduced body weight shown folate supplementation), allergic history, asthma, human liver and thyroid.

When the rash, Cough, arthralgia etc.. symptoms reception should be stopped immediately. Long-term appointment carried out at regular monitoring of peripheral blood cell, the functional state of the liver and kidneys. To prevent crystalluria recommended rich alkaline water (2-3 Liters per day).

Avoid excessive sun and UV radiation. The risk of side effects is significantly higher in patients with AIDS. Co-administration of folic acid HIV-infected patients increases the likelihood of developing resistance to sulfonamides strains Pneumocystis carinii.

Not recommended for tonsillitis and pharyngitis, caused by beta-hemolytic streptococcus group A because of widespread resistance strains.

Cooperation

Active substanceDescription of interaction
AzathioprineFMR. Against the background of co-trimoxazole may be exacerbated leukopenia, especially in patients with kidney transplant.
AzithromycinFMR. The combined application stacks effect.
AmantadinFKV. FMR. Against the background of co-trimoxazole, competing for renal secretion, slows down, level increases in the tissue and increases the risk of toxic effects; described the case of acute psychosis in 84-year-old patient, arising after combined destination.
Vitamin CFKV. FMR. Acidifying the urine and increases crystalluria.
BenzokainFMR: antagonizm. Weakens effect (formed by hydrolysis of PABA).
WarfarinFMR: synergism. Against the background of co-trimoxazole enhanced effect.
ProkaynFMR: antagonizm. Weakens effect (formed by hydrolysis of PABA).
RifampicinFKV. On the background of co-trimoxazole increases blood levels.
PhenytoinFKV. FMR. It displaces due to plasma proteins and increases the concentration in the blood, enhancing therapeutic and side effects. Against the background of co-trimoxazole increases antiepileptic activity.

Back to top button