Urseptia, 200 mg capsules 20 pcs

Pharmacotherapeutic group: ‑quinolone antimicrobial agent.‑

ATX code: J01MB04

Pharmacological properties Pharmacodynamics

It belongs to the group of quinolone drugs and is used in the treatment of urinary tract infections caused by pathogens sensitive to pipemic acid.

Pipemic acid inhibits bacterial DNA-topoisomerase II, which leads to disintegration of the bacterial DNA. This action is more pronounced against microorganisms that are in the phase of proliferation. High concentrations of pipemidic acid inhibit both RNA synthesis and bacterial protein synthesis.

The drug has a bactericidal effect on most gram-negative aerobic microorganisms (Proteus vulgaris, Proteus mirabilis, Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, Neisseria spp. etc.).

The percentage of emergence of resistance ranges from 10% (Escherichia coli, Staphylococcus aureus) to 62% (Pseudomonas aeruginosa). Gram-positive microorganisms are resistant to pipemic acid. It is not active against anaerobes.

Pipemic acid produces high concentrations in urine; activity increases with alkalinization of urine.

Pharmacokinetics

After oral administration it is quickly absorbed, bioavailability is 30-60%. After oral administration at a dose of 400 mg, maximum concentration of pipemidic acid (3.5 µg/ml) is reached after 70-80 minutes.

The binding to plasma proteins is approximately 30% and depends on the serum concentration of pipemic acid.

High concentrations of pipemidic acid are produced in the kidneys, urine and prostate fluid. Pipemidic acid, like other quinolone compounds, penetrates through the placenta and in trace amounts into the mother’s milk. Pipemidic acid is mostly excreted from the body through kidneys in unchanged form. Daily urine contains 50-85% of the administered dose of the drug. Excretion of pipedic acid directly depends on creatinine clearance. Half-life of the drug in normal renal function is 2 hours 15 minutes, and total clearance is 6.3 ml/min. In patients with impaired renal function, slightly higher concentrations of pipemidic acid in plasma are observed than in healthy volunteers. The plasma elimination half-life is slightly prolonged and is 5.7-16 hours.

Indications

Acute and chronic infectious and inflammatory diseases of the urinary tract caused by pipemic acid-sensitive microorganisms, including: pyelonephritis, cystitis, prostatitis.

Active ingredient

Pipemic acid

How to take, the dosage

Orally.

The average daily dose is 800 mg divided into 2 doses, i.e. 400 mg (2 capsules) every 12 hours, morning and evening before meals with water.

The course of treatment is on average 10 days. If necessary, the course of treatment may be prolonged, depending on the course of the disease, but no more than 4 weeks.

The treatment of cystitis in women lasts 3 days. In patients with severe renal insufficiency (CKR > 10 and < 30 ml/min) the dose should be reduced. In elderly patients with normal renal function and in patients with mild to moderate hepatic impairment, no dose adjustment is required.

The patient is advised to drink plenty of fluids during therapy.

Interaction

Pipemic acid causes inhibition of P450 enzyme, due to which metabolism of theophylline and caffeine slows down when concomitant use with pipemic acid. Half-life of theophylline is increased with concomitant use of pipemic acid, its concentration in blood serum is increased by 40-80%. It is necessary to monitor the concentration of theophylline in blood plasma during the use of pipedic acid. Against the background of use of pipedic acid as well as other quinolone antibiotics an increase of caffeine concentration in blood serum (2-4 times) is noted.

Antacids and sucralfate significantly slow absorption of pipemic acid. The interval between the intake of these drugs should be at least 2-3 hours. At the same time, a similar effect was not observed with concomitant use of cimetidine and ranitidine.

Pipemic acid may increase the anticoagulant effect of warfarin when taken simultaneously. Concomitant use with nonsteroidal anti-inflammatory drugs may cause seizures.

When combined administration with aminoglycosides synergism with respect to the bactericidal effect is observed.

Special Instructions

Side effects are in most cases mild and transient, usually not requiring withdrawal of the drug. If allergic reactions to the drug occur, its use should be discontinued.

At the time of treatment, ultraviolet irradiation should be avoided because of the high risk of photosensitization. Patients with glucose-6-phosphate dehydrogenase deficiency may develop hemolytic anemia.

When using the drug for a long time the general blood parameters should be watched, liver and kidney functions should be determined and microflora sensitivity to the drug should be determined repeatedly.

In the course of treatment, the amount of fluid intake should be increased (with controlled diuresis).

Prescribe with caution to patients over 70 years of age (because of increased incidence of side effects in the elderly) and patients with impaired renal function (CK > 10 and < 30 ml/min) (contraindicated in oliguria and anuria, CK < 10 ml/min), dose adjustment and regular patient monitoring is required.

Patients with a history of cerebral circulation disorders (including cerebral hemorrhage, cerebral vasospasm) and seizures should be cautioned when prescribing the drug.

False positive reactions to urine glucose may be noted when using Benedict’s reagent or Felling’s solution. Enzymatic reactions with glucose oxidase are recommended.

Impact on the ability to drive vehicles, mechanisms

Patient should refrain during treatment from engaging in potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Synopsis

Solid gelatin capsules № 1 with a white body and a green cap. The contents of the capsules – powder from white with a yellowish tinge to light yellow, powder clumping is allowed.

Contraindications

– hypersensitivity to pipemic acid or any of the ingredients of the drug;

– severe hepatic impairment (including cirrhosis);

– severe renal impairment (creatinine clearance (CK) < 10 ml/min;

– central nervous system disorders (epilepsy and other neurological conditions with reduced seizure threshold);

– porphyria;

– lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

– history of allergic reactions to quinolones;

– pregnancy and the period of breastfeeding;

– childhood under 18 years of age (period of skeletal formation and growth).

With caution

– patients with renal insufficiency (CK > 10 and < 30 ml/min);

– Older age (over 70 years);

– Cerebral circulation disorder;

– Glucose-6-phosphate dehydrogenase deficiency.

Side effects

Digestive system disorders: nausea, vomiting, diarrhea, pseudomembranous colitis, gastralgia, anorexia, heartburn, abdominal bloating or abdominal pain, constipation.

Nervous system disorders: visual impairment, vertigo, headache, agitation, depression, confusion, hallucinations, tremor, prolonged convulsions associated with cerebral edema, sleep disorders, sensory disturbances.

Skin disorders: itching, rash, photosensitization with erythema, toxic epidermal necrolysis.

Laboratory measures: hemolytic anemia (in patients with glucose-6-phosphate dehydrogenase deficiency), eosinophilia, reversible thrombocytopenia (in elderly patients and in patients with renal failure).

Others: superinfections, acute arthropathy, tendinitis.

Overdose

There are no reports of fatal or life-threatening side effects due to drug overdose. There is no specific antidote.

Symptoms: nausea, vomiting, dizziness, headache, confusion, tremors, seizures.

Treatment: gastric lavage after recent intake (less than 4 hours), intake of activated charcoal, forced diuresis, hemodialysis; if there are side effects on the nervous system (including epileptic seizures) symptomatic therapy (diazepam) is prescribed.

In case of overdose the patient should be under medical supervision.

Pregnancy use

The use of the drug is contraindicated in pregnancy.

Pipemic acid is excreted with breast milk, therefore, if the drug is prescribed during lactation, breastfeeding should be stopped.