Instructions for Orgil film-coated tablets 500 mg No. 10
Composition
active ingredient: ornidazole;
1 tablet contains 500 mg of ornidazole;
excipients: microcrystalline cellulose, corn starch, magnesium stearate, croscarmellose sodium, Opadry 03B53217 orange coating: hypromellose, titanium dioxide (E 171), sunset yellow FCF (E 110), polyethylene glycols.
Dosage form
Film-coated tablets.
Main physicochemical properties: round tablets, coated with an orange shell.
Pharmacotherapeutic group
Agents used in the treatment of amebiasis and other protozoal infections. Nitroimidazole derivatives. Ornidazole. ATX 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, Giardia lamblia (Gardia intestinalis), as well as against 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.
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 use of the drug. After multiple doses of 500 mg and 1000 mg to healthy volunteers every 12 hours, the accumulation 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.
Breeding.
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 certain disorders of the functioning of organs and systems.
Liver dysfunction.
The half-life of the active substance in liver cirrhosis increases to 22 hours, clearance decreases (35 versus 51 ml/minute) compared to healthy volunteers.
Kidney dysfunction.
The pharmacokinetics of Ornidazole does not change in renal impairment, so the dose of the drug 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.
The pharmacokinetics of ornidazole in children (including newborns) 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 the active substance or other components of the drug or to other nitroimidazole derivatives. Patients with central nervous system damage (epilepsy, brain damage, multiple sclerosis); blood dyscrasia or other hematological disorders.
Interaction with other medicinal products and other types of interactions
Although ornidazole (unlike other nitroimidazole derivatives) does not inhibit aldehyde dehydrogenase, alcohol should not be consumed during treatment with Orgil® and for at least 3 days after stopping the drug.
Ornidazole enhances the effect of oral coumarin anticoagulants, which requires appropriate correction of their dosage.
Ornidazole prolongs the muscle relaxant effect of vecuronium bromide.
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.
Lithium.
The concomitant use of ornidazole with lithium preparations should be accompanied by monitoring of the concentration of lithium salts and electrolytes, as well as the level of creatinine in the blood serum (see section "Special warnings and precautions for use").
Application features
When using high doses of the drug and in the case of treatment for more than 10 days, clinical and laboratory monitoring is recommended.
In individuals with a history of blood disorders, monitoring of leukocytes is recommended, especially during repeated courses of treatment.
Aggravation of central or peripheral nervous system disorders may occur during treatment with the drug. In the event of peripheral neuropathy, impaired coordination of movements (ataxia), dizziness or confusion, treatment should be discontinued.
Exacerbation of candidiasis may occur, 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 salt concentrations, creatinine and electrolyte concentrations should be monitored during lithium therapy.
The effect of other medicines may be increased or decreased during treatment with the drug.
Use with caution in patients with impaired liver function.
Excipients.
The drug contains the azo dye sunset yellow FCF, which may cause allergic reactions.
Use during pregnancy or breastfeeding
Animal studies have not revealed any teratogenic or toxic effects of ornidazole on the fetus. Since controlled studies in pregnant women have not been conducted, the drug is contraindicated in the first trimester of pregnancy. The drug should be prescribed in the second and third trimesters 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. If necessary, the use of ornidazole should be discontinued.
Ability to influence reaction speed when driving vehicles or other mechanisms
When using ornidazole, such manifestations as drowsiness, muscle 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
Orgil® should be taken orally after meals, with a small amount of water.
Since taking ornidazole can cause reactions such as redness, numbness, fever, nausea and vomiting, hypotension and tinnitus are also possible. Alcohol should not be consumed for at least 3 days after taking the medicine.
Trichomoniasis
500 mg tablets are used in single- or five-day therapy regimens.
Since taking ornidazole can cause reactions such as redness, numbness, fever, nausea and vomiting, hypotension and tinnitus are also possible. Alcohol should not be consumed for at least 3 days after taking the medicine.
Table 1
| Duration of treatment | Daily dose (tablet, weighing 500 mg) |
| Single therapeutic dose | 3 tablets taken in the evening |
| Five-day therapy | 1 tablet in the morning, 1 tablet 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 tablet) | Children with body weight up to 35 kg |
| 3-day course of treatment | 3 tablets at a time in the evening. With a body weight of more than 60 kg: 4 tablets (2 tablets in the morning and 2 tablets in the evening) | 40 mg/kg body weight single dose |
| 5-10-day course of treatment | 2 tablets (1 tablet in the morning and 1 tablet in the evening) | 25 mg/kg body weight single 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 tablets at a time in the evening | 40 mg/kg, single dose |
Patients with renal insufficiency: No dose adjustment is required for 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.
Children.
Children should use the drug according to the dosage recommendations specified in the "Method of administration and doses" section.
Overdose
In case of overdose, the symptoms mentioned in the section "Adverse reactions" are possible, but in a more pronounced form. Treatment is symptomatic, a specific antidote is unknown. In case of convulsions, intravenous administration of diazepam is recommended.
Side effects
From the blood and lymphatic system: manifestations of effects on the bone marrow, including suppression of bone marrow hematopoiesis, leukopenia, neutropenia.
On the part of the immune system: hypersensitivity reactions, including manifestations of skin allergic reactions, anaphylactic shock, angioedema.
Skin and subcutaneous tissue disorders: skin rash, itching, urticaria, skin hyperemia.
Nervous system: headache, fatigue, agitation, confusion, tremor, rigidity, impaired coordination, ataxia, convulsions, temporary loss of consciousness, signs of sensory or mixed peripheral neuropathy, dizziness, drowsiness, spatial disorientation.
Gastrointestinal: nausea, vomiting, metallic taste in the mouth, coated tongue, dry mouth, changes in taste, diarrhea, epigastric pain, dyspepsia, loss of appetite.
From the hepatobiliary system: jaundice, hepatotoxicity, impaired biochemical indicators of liver function, increased levels of liver enzymes.
General disorders: fever; chills; general weakness; shortness of breath.
Infections and infestations: exacerbation of candidiasis.
Others: darkening of urine color, cardiovascular disorders, including decreased blood pressure.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 tablets in a blister; 1 blister in a cardboard box.
Vacation category
According to the recipe.
Producer
KUSUM HEALTHCARE PVT LTD/KUSUM HEALTHCARE PVT LTD.
Address
Plot No. M-3, Indore Special Economic Zone, Phase-II, Pithampur, Distt. Dhar, Madhya Pradesh, Pin 454774, India/Plot No. M-3, Indore Special Economic Zone, Phase-II, Pithampur, Distt. Dhar, Madhya Pradesh, Pin 454774, India
