Oriprim

Oriprim is an effective medication that combines two different medicinal components in its composition – trimethoprim together with sulfamethoxazole.

The drug has a pronounced bactericidal effect on a large number of gram-negative and -positive bacteria. The principle of the drug's effect is based on the antimicrobial effect of the active element complex, which develops through therapeutic action in 2 phases of 4-folic acid binding.

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Indications Oriprima

It is used in cases of inflammatory and infectious infections that develop under the influence of bacteria sensitive to the drug:

• lesions of the urinary system: active and chronic phases of infection of the urinary tract - chronic stage of bacteriuria, cystitis in the active or chronic stage, prostatitis, pyelonephritis, and urethritis;
• respiratory tract infections: pharyngitis, active or chronic bronchitis, otitis, pneumonia or sinusitis;
• infections affecting the gastrointestinal tract;
• inflammations and infections associated with the epidermis and soft tissues: furunculosis, pyoderma, infected wounds and abscesses;
• active phase of urethritis of gonococcal origin (in women as well as men);
• nocardiosis;
• active phase of brucellosis;
• mycetoma (excluding that caused by true fungi).

Release form

The drug is produced in tablets - 10 pieces inside a blister pack. There are 2 or 10 such packs inside a pack.

Pharmacodynamics

Sulfamethoxazole slows down the penetration of PABA into dihydrofolic acid, while trimethoprim prevents the return of dihydrofolic acid to the state of 4-folic acid. As a result, the complex of active elements blocks 2 consecutive stages of biosynthesis of proteins with nucleic acids, which are extremely important for many microbes.

The drug actively affects a wide range of bacteria, including gram-negative and -positive aerobes, nocardia (actinomycetes), chlamydia, many anaerobes and individual protozoa with mycobacteria.

Among the microbes resistant to the drug are Treponema pallidum, Koch's bacillus, Mycoplasma species and Pseudomonas aeruginosa.

The range of activity against gram-negative microorganisms is Ducray bacillus, Klebsiella oxytoca, Haemophilus parainfluenzae, Enterobacter cloacae, Citrobacter freundii, Serratia marcescens, etc.

Pharmacokinetics

The drug is absorbed at high speed after oral use. High LS is formed inside the prostate, bile, lung tissue, cerebrospinal fluid, bones and kidneys. The introduction of trimethoprim with sulfamethoxazole in a ratio of 5:1 leads to the development of a ratio within 20:1-30:1; the Cmax level is noted after 2 hours. It is at these proportions that the most pronounced synergism of the effect of a relatively large part of bacteria is recorded.

A significant portion of the orally administered trimethoprim is excreted unchanged in the urine, and only 10% is excreted in the form of metabolic elements that have little or no activity.

The urine level after a standard dose exceeds plasma values by approximately 100 times, remaining within these limits for 24 hours.

Sulfamethoxazole is almost completely excreted in urine. Its levels in urine are significantly higher than those in plasma.

Trimethoprim is rapidly distributed within tissues.

Dosing and administration

The dose of Oriprim must be selected individually. The therapeutic cycle lasts at least 5 days or until the symptoms of the disease disappear.

In the active phase of brucellosis and prostatitis, therapy lasts at least 1 month, and actinomycetoma and nocardiosis are treated in long courses.

The medicine should be taken orally after eating.

For adolescents over 12 years of age and adults, the dosage is 0.8 sulfamethoxazole/0.16 g trimethoprim, 2 times a day. The maintenance dose is similar, but it should be taken once a day.

For the age group 5-12 years, the dose is 0.4 g sulfamethoxazole/0.08 g trimethoprim, 2 times a day.

Age category 2-5 years – 0.2 g sulfamethoxazole/0.04 g trimethoprim, 2 times per day.

Use Oriprima during pregnancy

It is prohibited to prescribe Oriprim during pregnancy.

Contraindications

Main contraindications:

• severe sensitivity to the drug components (sulfamethoxazole with trimethoprim);
• severe pathologies affecting the liver parenchyma;
• severe renal dysfunction;
• blood diseases;
• breast-feeding;
• deficiency of the G6PD component.

Side effects Oriprima

When using standard doses of the drug, no complications are observed. Most often, side effects develop that affect the functioning of the gastrointestinal tract, as well as epidermal lesions of allergic origin.

Gastrointestinal disorders include vomiting, diarrhea, glossitis, nausea, stomatitis and pancreatitis, as well as (rarely) pseudomembranous colitis.

Disorders of allergic origin – allergic myocarditis, anaphylactoid symptoms, photosensitivity and hemorrhagic vasculitis.

Common manifestations are lupus erythematosus or nodose panarteritis. Sometimes TEN or erythema is observed.

Due to the presence of sulfamethoxazole in the composition of the drug, there is a risk of pathological changes in blood tests. Among these are purpura, eosinophilia, hemolytic anemia, leuko-, thrombocyto- or neutropenia. Sometimes pernicious anemia, pancytopenia or agranulocytosis appear. At the same time, there is an opinion that disorders of blood function are more likely in elderly people.

Disorders of neurological origin – tinnitus, ataxia, headaches, convulsions, hallucinations, aseptic meningitis and dizziness.

Lesions of the musculoskeletal structure – myalgia or arthralgia.

Urogenital dysfunction – toxic nephrosis, tubulointerstitial nephritis and increased plasma creatinine levels.

Overdose

In acute sulfonamide intoxication, symptoms such as vomiting, headaches, colic, dizziness, nausea, anorexia, loss of consciousness, and drowsiness may develop. There is information about the appearance of crystalluria, hyperthermia, or hematuria.

In case of chronic poisoning, suppression of hematopoietic processes (leukopenia or thrombocytopenia) occurs, as well as other pathological changes in the blood structure associated with a lack of vitamin B9.

Among the standard procedures used in case of overdose are induction of vomiting or gastric lavage, and in addition potentiation of renal excretion through forced diuresis (due to alkalization of urine, excretion of sulfamethoxazole is enhanced). To remove the symptoms of the effect of trimethoprim on the hematopoietic function, use Ca folinate: intramuscular injections of 3-6 mg for 5-7 days. In case of poisoning, it is necessary to monitor blood processes and the biochemical structure of the blood (also for salt indicators).

In the event of jaundice or significant pathological changes in the blood, special therapeutic measures are taken. Peritoneal dialysis procedures will be ineffective, while hemodialysis demonstrates a moderate effect in eliminating sulfamethoxazole with trimethoprim.

Interactions with other drugs

It is prohibited to combine the drug with orally taken antidiabetic drugs, salicylates, thiazide-type diuretics, phenylbutazone, as well as with indirect coagulants, phenytoin and naproxen.

In elderly patients using diuretics (especially thiazides) together with Oriprim, the development of purpura with thrombocytopenia has occasionally been reported.

There is information about the continuation of PV in individuals who combined the drug with warfarin.

Trimethoprim with sulfamethoxazole are able to inhibit intrahepatic metabolic processes of phenytoin. Clinical doses of the drug prolong the half-life of phenytoin by 39% and reduce the rate of metabolic clearance by 27%.

Sulfonamides disrupt the intraplasmic protein synthesis of methotrexate, causing the level of this free component to increase.

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Storage conditions

Oriprim must be stored in a dark place, out of reach of children. Temperature indicators – no higher than 30°C.

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Shelf life

Oriprim can be used within a 4-year period from the date of manufacture of the therapeutic substance.

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Application for children

The drug is not used in premature infants, children under 3 months of age (there is a risk of developing nuclear jaundice). In general, children under 5 years of age are recommended to use the drug suspension.

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Analogues

The analogs of the drug are Baktiseptol, Groseptol, Bikotrim with Baktrim, Brifeseptol and Bel-septol with Biseptol, and in addition to this, Solyuseptol and Bi-sept. Also on the list are Sumetrolim, Bi-tol, Raseptol with Biseptrim, Triseptol and Co-trimoxazole.