Instructions for Ornidazole-Astrapharm capsules 500 mg blister No. 10
Composition
active ingredient: ornidazole;
1 capsule contains 500 mg of ornidazole in terms of 100% substance;
excipients: potato starch, magnesium stearate;
capsule shell composition: gelatin, titanium dioxide (E 171), indigo carmine blue 2 (E 132), azorubine (E 122).
Dosage form
Capsules.
Main physical and chemical properties: hard gelatin capsules No. 0, cylindrical in shape with hemispherical ends, white body, blue cap. Capsule contents: pale yellow crystalline powder.
Pharmacotherapeutic group
Agents used in the treatment of amebiasis and other protozoal infections. Nitroimidazole derivatives. Ornidazole. ATC code P01A B03.
Pharmacological properties
Pharmacodynamics.
Ornidazole is an antiprotozoal and antibacterial agent, a 5-nitroimidazole derivative. It is active against Trichomonas vaginalis, Entamoeba histolytica, Giardiasis lamliasis (Giardia intestinalis), as well as some anaerobic bacteria, such as Bacteroides, Clostridium spp., Fusobacterium spp. and anaerobic cocci.
By the mechanism of action, ornidazole is a DNA-tropic drug with selective activity against microorganisms that have enzyme systems capable of reducing the nitro group and catalyzing the interaction of ferridoxine group proteins with nitro compounds. After the drug penetrates the microbial cell, its mechanism of action is due to the reduction of the nitro group under the influence of nitroreductases of the microorganism and the activity of the already reduced nitroimidazole. The reduction products form complexes with DNA, causing its degradation, disrupting the processes of DNA replication and transcription. In addition, the products of the drug's metabolism have cytotoxic properties and disrupt the processes of cellular respiration of microorganisms.
Pharmacokinetics.
Absorption: After oral administration, ornidazole is rapidly absorbed from the gastrointestinal tract. On average, absorption is 90%. Maximum plasma concentration is reached within 3 hours.
Distribution: The binding of ornidazole to plasma proteins is approximately 13%. The active substance penetrates into the cerebrospinal fluid, other body fluids and tissues.
The concentration of ornidazole in blood plasma is in the range of 6-36 mg/l, i.e. at a level considered optimal for various indications for the use of the drug. After repeated administration in doses of 500 mg and 1000 mg to healthy volunteers every 12 hours, the cumulation coefficient is 1.5-2.5.
Metabolism: Ornidazole is metabolized in the liver to form mainly 2-hydroxymethyl and α-hydroxymethyl metabolites. Both metabolites are less active against Trichomonas vaginalis and anaerobic bacteria than unchanged ornidazole.
Elimination: The elimination half-life is approximately 13 hours. After a single dose, 85% of the dose is excreted within the first 5 days, mainly as metabolites. About 4% of the dose is excreted unchanged by the kidneys.
Features of pharmacokinetics in disorders of organ and system function.
Liver: the half-life of the active substance in liver cirrhosis increases to 22 hours, clearance decreases (from 35 to 51 ml/min) compared to that in healthy volunteers.
Kidneys: the pharmacokinetics of ornidazole do not change in renal function, so the dose does not need to be changed.
Ornidazole is removed by hemodialysis. Before starting hemodialysis, an additional 500 mg of ornidazole should be administered if the daily dose is 2 g per day, or an additional 250 mg of ornidazole if the daily dose is 1 g per day.
Children (including neonates): The pharmacokinetics of ornidazole in children (including neonates) are similar to those in adults.
Indication
Trichomoniasis (urinary tract infections in women and men caused by Trichomonas vaginalis).
Amebiasis (all intestinal infections caused by Entamoeba histolytica, including amoebic dysentery, all extraintestinal forms of amebiasis, especially amoebic liver abscess).
Giardiasis.
Contraindication
Hypersensitivity to ornidazole or other components of the drug or to other nitroimidazole derivatives. Central nervous system damage (epilepsy, brain damage, multiple sclerosis); pathological blood lesions or other hematological abnormalities.
Interaction with other medicinal products and other types of interactions
You should not drink alcohol during the course of treatment for at least 3 days after stopping the drug.
Ornidazole enhances the effect of oral coumarin anticoagulants, which requires appropriate correction of their dosage.
Concomitant use of phenobarbital and other enzyme inducers reduces the circulation period of ornidazole in the blood serum, while enzyme inhibitors (e.g. cimetidine) increase it.
Ornidazole prolongs the muscle relaxant effect of vecuronium bromide.
Application features
When using high doses of the drug and in case of continuation of treatment for more than 10 days, clinical and laboratory monitoring is recommended.
Aggravation of central or peripheral nervous system disorders may occur during treatment. In case of peripheral neuropathy, impaired coordination of movements (ataxia), dizziness or confusion, the drug should be discontinued.
Exacerbation of candidiasis is possible, which will require appropriate treatment.
In the case of hemodialysis, it is necessary to take into account the reduction in the half-life and prescribe additional doses of the drug before or after hemodialysis.
Lithium and electrolyte concentrations, as well as creatinine levels, should be monitored during lithium therapy.
The effect of other medicines may be enhanced or weakened during treatment with the drug.
Use with caution in patients with impaired liver function.
Use during pregnancy or breastfeeding
In the experiment, ornidazole does not show teratogenic or toxic effects on the fetus. Since controlled studies in pregnant women have not been conducted, the drug should be prescribed in early pregnancy or during breastfeeding only if there are absolute indications, when the possible benefits of using the drug for the mother outweigh the potential risk to the fetus/child.
Ability to influence reaction speed when driving vehicles or other mechanisms
When using ornidazole, such manifestations as drowsiness, rigidity, dizziness, tremor, convulsions, impaired coordination, temporary loss of consciousness are possible. The possibility of such manifestations must be taken into account for patients who drive vehicles or work with other mechanisms.
Method of administration and doses
Ornidazole should always be taken orally after meals.
Patients with renal insufficiency: No dose adjustment is required in patients with impaired renal function.
Patients with hepatic impairment: The dosing interval should be doubled for patients with severe hepatic impairment.
Elderly patients: There are no clinical data on the use in elderly patients.
Trichomoniasis: 500 mg capsules are used in single-dose or 5-day therapy regimens.
Taking ornidazole can cause reactions such as redness, numbness, fever, nausea and vomiting, as well as possible hypotension and tinnitus. Alcohol should not be consumed for at least 3 days after taking the drug.
Table 1
| Duration of treatment | Daily dose (capsule, weighing 500 mg) |
| Single therapeutic dose | 3 capsules taken in the evening |
| 5-day therapy | 1 capsule in the morning, 1 capsule in the evening |
To eliminate the possibility of re-infection, the sexual partner must undergo the same course of treatment.
The single daily dose for children is 25 mg/kg.
Amebiasis
Possible treatment regimens:
3-day course of treatment for patients with amoebic dysentery;
5-10-day course of treatment for all forms of amebiasis.
Table 2
Recommended dosage regimen of the drug
| Duration of treatment | Daily dose |
Adults and children weighing more than 35 kg (500 mg capsule) | Children with body weight up to 35 kg |
| 3-day course of treatment | 3 capsules per dose in the evening. With a body weight of over 60 kg: 4 capsules (2 capsules in the morning and 2 capsules in the evening) | 40 mg/kg body weight single dose 35 kg – 3 capsules per dose 25 kg – 2 capsules per dose 13 kg – 1 capsule per dose |
| 5-10-day course of treatment | 2 capsules (1 capsule in the morning and 1 capsule in the evening) | 25 mg/kg body weight single dose 35 kg – 2 capsules per dose 20 kg – 1 capsule per dose |
Giardiasis
Table 3
Recommended dosage regimen of the drug
| Duration of treatment | Daily dose |
| Adults and children weighing more than 35 kg | Children with body weight up to 35 kg |
| 1-2-day course of treatment | 3 capsules per dose in the evening | 40 mg/kg single dose |
Children.
The drug is used in children according to the dosage recommendations specified in the section "Method of administration and dosage".
Overdose
In case of overdose, the symptoms mentioned in the "Adverse reactions" section may occur, but in a more pronounced form.
Treatment is symptomatic. Specific antidote is unknown. In case of convulsions, intravenous diazepam is recommended.
Side effects
Infections and infestations: exacerbation of candidiasis.
From the blood system: manifestations of effects on the bone marrow, leukopenia, neutropenia.
Nervous system: drowsiness, headache, dizziness, tremor, rigidity, impaired coordination, ataxia, convulsions, increased fatigue, spatial disorientation, temporary loss of consciousness, confusion, agitation and peripheral neuropathy.
On the part of the digestive tract: taste disturbance, metallic taste in the mouth, coated tongue, nausea, vomiting, diarrhea, epigastric pain, dry mouth, loss of appetite.
Immune system disorders: hypersensitivity reactions, including anaphylactic shock, angioedema.
Skin and subcutaneous tissue disorders: skin rash, urticaria, skin hyperemia, itching.
General disorders: increased body temperature; chills; general weakness; shortness of breath; darkening of urine; cardiovascular disorders, including decreased blood pressure.
Expiration date
3 years.
Storage conditions
Store in a dry place, protected from light, at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 capsules in a blister; 1 blister in a box.
Leave category. By prescription.
Vacation category
According to the recipe.
Producer
"ASTRAPHARM" LLC.
Location of the manufacturer and address of its operations.
Ukraine, 08132, Kyiv-Svyatoshynskyi district, Vyshneve, Kyivska st., 6.
