Ornizol®

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT ORNIZOL® (ORNIZOLE®)

Composition:

Active substance: ornidazole;

1 ml of solution contains ornidazole – 5 mg;

Excipients: sodium chloride, water for injections.

Pharmaceutical form. Infusion solution.

Main physicochemical properties: clear colorless or light yellow liquid.

Pharmacotherapeutic group. Antibacterial agents. Imidazole derivatives.

ATC code J01X D03.

Pharmacological properties.

Pharmacodynamics.

The mechanism of action of ornidazole is associated with disruption of DNA structure in susceptible microorganisms. Ornidazole is active against Trichomonas vaginalis, Entamoeba histolytica, Giardia lamblia (Giardia intestinalis), as well as certain anaerobic bacteria such as Bacteroides, Fusobacterium spp.; anaerobic Gram-positive bacteria: Clostridium spp., sensitive strains of Eubacterium spp.; and anaerobic Gram-positive cocci: Peptococcus spp., Peptostreptococcus spp.

It readily penetrates microbial cells and, by binding to DNA, disrupts the replication process.

Pharmacokinetics.

Ornidazole readily crosses the blood-brain barrier and placental barrier, and penetrates into cerebrospinal fluid and bile; it also passes into breast milk. After intravenous administration at a dose of 15 mg/kg, followed by subsequent doses of 7.5 mg per kg of body weight every 6 hours, steady-state concentrations range from 18 to 26 μg/mL. Approximately 30–60% of the drug is metabolized in the body via hydroxylation, oxidation, and glucuronidation.

Excretion. Ornidazole is excreted primarily in the urine (60–80%), of which nearly 20% is unchanged, and 6–15% is excreted in feces.

Clinical characteristics.

Indications.

Parenteral administration of the drug is indicated in cases of acute and severe infection or when oral administration is not feasible, in the following diseases and conditions:

• anaerobic systemic infections caused by microorganisms sensitive to ornidazole: sepsis, meningitis, peritonitis, postoperative wound infections, postpartum sepsis, septic abortion, and endometritis;
• prophylaxis of infections caused by anaerobic bacteria during surgical procedures (particularly surgeries on the colon and rectum), and gynecological operations;
• severe course of amebic dysentery, all extraintestinal forms of amebiasis, giardiasis, hepatic abscess.

Contraindications.

Hypersensitivity to the components of the drug or to other nitroimidazole derivatives. Patients with CNS disorders, epilepsy, multiple sclerosis, chronic alcoholism. Circulatory disorders, pathological blood conditions or other hematological abnormalities.

Interaction with other medicinal products and other types of interactions.

Unlike other nitroimidazole derivatives, ornidazole does not inhibit aldehyde dehydrogenase and therefore is compatible with alcohol. However, ornidazole enhances the effect of oral anticoagulants of the coumarin series (warfarin), requiring appropriate adjustment 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 blood serum, whereas enzyme inhibitors (e.g., cimetidine) increase it.

Special precautions for use.

When recommended doses are exceeded, there is a certain risk of adverse effects in children, patients with liver impairment, and patients who abuse alcohol. When high doses of ornidazole are used or treatment lasts longer than 10 days, clinical and laboratory monitoring is recommended.

In patients with a history of blood disorders, leukocyte monitoring is recommended, especially during repeated treatment courses.

Exacerbation of central or peripheral nervous system disorders may occur during ornidazole therapy. In case of peripheral neuropathy, movement coordination disturbances (ataxia), dizziness, or clouding of consciousness, treatment should be discontinued.

Exacerbation of candidiasis may occur, which will require appropriate treatment.

During hemodialysis, reduced elimination half-life should be taken into account, and additional doses of the drug should be administered before or after hemodialysis.

Serum lithium, creatinine, and electrolyte concentrations should be monitored during concomitant lithium therapy.

The effects of other medicinal products may be enhanced or diminished during treatment with ornidazole.

Use during pregnancy or breastfeeding.

Ornidazol® is contraindicated during the first trimester of pregnancy. In the second and third trimesters, the drug should be prescribed only if strictly indicated. If use is necessary, breastfeeding should be discontinued.

Ability to influence reaction rate when driving or operating machinery.

During ornidazole use, adverse effects such as drowsiness, muscle rigidity, dizziness, tremor, seizures, impaired coordination, and transient loss of consciousness may occur. The possibility of such effects should be considered in patients driving or operating machinery.

Dosage and Administration

The dosage and duration of treatment are determined by a physician depending on the nature of the disease and treatment regimen.

The drug should be administered intravenously over 15–30 minutes.

For anaerobic systemic infections: administer intravenously at a dose of
500–1000 mg as an initial dose, followed by 500 mg every 12 hours or 1000 mg every
24 hours for 5–10 days (stepwise dosing). After the patient's condition has stabilized, switch to oral administration of ornidazole (e.g., 500 mg tablets, 1 tablet every 12 hours).

For children under 12 years of age weighing more than 6 kg, the daily dose should be administered at 20 mg/kg body weight, divided into two infusions over 5–10 days.

For prophylaxis of infections caused by anaerobic bacteria during surgical procedures: in adults and children aged 12 years and older, administer ornidazole at a dose of 500–1000 mg 30 minutes before surgery.

For prophylaxis of mixed infections, ornidazole should be used in combination with aminoglycosides, penicillin, or cephalosporins. The drugs should be administered separately.

Severe amebic dysentery, all extraintestinal forms of amebiasis, giardiasis, hepatic abscess: in adults and children aged 12 years and older, the first dose is
500–1000 mg, followed by 500 mg every 12 hours for 3–6 days.

For children under 12 years of age weighing more than 6 kg, the daily dose should be administered at 20–30 mg/kg body weight, divided into two infusions. The treatment duration is determined by the physician depending on the nature of the disease.

In case of impaired renal function, prolong the interval between doses or reduce the single and daily dose of the drug.

Children.

Ornidazol® should not be administered to children weighing less than 6 kg.

Overdose.

Symptoms: nausea, vomiting, anorexia, possible intensification of symptoms of other adverse reactions.

Treatment: no specific antidote is known; in case of seizures, diazepam should be administered. Symptomatic therapy.

Adverse Reactions.

Blood and lymphatic system disorders: manifestations of bone marrow suppression, moderate leukopenia, neutropenia.

Immune system disorders: hypersensitivity reactions, including anaphylactic shock, angioneurotic edema.

Skin and subcutaneous tissue disorders: skin rashes, urticaria, skin hyperemia, pruritus.

Nervous system disorders: dizziness, somnolence, headache, tremor, muscle rigidity, coordination disturbances, ataxia, seizures, transient loss of consciousness, confusion, signs of sensory or mixed peripheral neuropathy, excitement.

Gastrointestinal disorders: taste disturbances, metallic taste in the mouth, dry mouth, coated tongue, nausea, vomiting, dyspepsia, sensation of heaviness and tenderness in the epigastric area.

Hepatobiliary disorders: hepatotoxicity, changes in liver function tests.

General disorders and administration site conditions: increased body temperature, chills, general weakness, increased fatigue, dyspnea, changes at the injection site, including pain, redness, burning sensation at the injection site.

Other: darkening of urine color, cardiovascular disorders, including arterial hypotension.

Shelf life. 2 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25°C.

Keep out of reach of children.

Incompatibility.

The drug should not be mixed with other injectable solutions during administration.

Packaging.

100 ml in glass bottles with a rubber stopper, sealed with an aluminum cap.

1 bottle per carton.

Prescription status. Prescription only.

Manufacturer.

JSC "Halychpharm".

Manufacturer's location and address of business activity.

79024, Lviv, Opryshkovska St., 6/8, Ukraine.

Marketing Authorization Holder.

JSC "Halychpharm".

Address of Marketing Authorization Holder.

79024, Lviv, Opryshkovska St., 6/8, Ukraine.

INSTRUCTION

for medical use of medicinal product

ORNIZOL

(ORNIZOLE®)

Composition:

Active substance: ornidazole;

1 ml of solution contains ornidazole – 5 mg;

Excipients: sodium chloride, water for injections.

Pharmaceutical form. Infusion solution.

Main physicochemical properties: clear, colorless or pale yellow liquid.

Pharmacotherapeutic group. Antibacterial agents. Imidazole derivatives.

ATC code J01XD03.

Pharmacological properties.

Pharmacodynamics.

The mechanism of action of ornidazole is related to disruption of DNA structure in susceptible microorganisms. Ornidazole is active against Trichomonas vaginalis, Entamoeba histolytica, Giardia lamblia (Giardia intestinalis), and certain anaerobic bacteria such as Bacteroides, Fusobacterium spp.; anaerobic gram-positive bacteria: Clostridium spp., sensitive strains of Eubacterium spp.; anaerobic gram-positive cocci: Peptococcus spp., Peptostreptococcus spp.

Ornidazole easily penetrates microbial cells and, by binding to DNA, disrupts the replication process.

Pharmacokinetics.

Ornidazole readily crosses the blood-brain and placental barriers, enters cerebrospinal fluid and bile, and penetrates into breast milk. After intravenous administration at a dose of 15 mg/kg and subsequent dosing at 7.5 mg per 1 kg body weight every 6 hours, steady-state concentration ranges from 18–26 µg/mL. Approximately 30–60% of the drug is metabolized in the body via hydroxylation, oxidation, and glucuronidation.

Elimination. Ornidazole is excreted predominantly in urine (60–80%), with nearly 20% excreted unchanged and 6–15% excreted in feces.

Clinical characteristics.

Indications.

Parenteral administration of the drug is indicated in cases of acute and severe infection or when oral administration is not feasible, in the following conditions:

• Anaerobic systemic infections caused by microflora sensitive to ornidazole: septicemia, meningitis, peritonitis, postoperative wound infections, postpartum sepsis, septic abortion, and endometritis;
• Prophylaxis of infections caused by anaerobic bacteria during surgical procedures (especially colorectal and rectal surgery), and gynecological operations;
• Severe amoebic dysentery, all extraintestinal forms of amoebiasis, giardiasis, liver abscess.

Contraindications.

Hypersensitivity to the components of the drug or to other nitroimidazole derivatives. Patients with CNS disorders, epilepsy, multiple sclerosis, chronic alcoholism. Circulatory disorders, blood pathology or other hematological abnormalities.

Interaction with other medicinal products and other forms of interaction.

Unlike other nitroimidazole derivatives, ornidazole does not inhibit aldehyde dehydrogenase and is therefore compatible with alcohol. However, ornidazole potentiates the effect of oral anticoagulants of the coumarin group (e.g., warfarin), requiring appropriate dose adjustment.

Ornidazole prolongs the muscle relaxant effect of vecuronium bromide.

Concomitant use of phenobarbital and other enzyme inducers reduces the circulation time of ornidazole in serum, whereas enzyme inhibitors (e.g., cimetidine) increase it.

Special precautions.

Exceeding recommended doses may increase the risk of adverse effects in children, patients with liver impairment, and patients with alcohol abuse. When high doses of ornidazole are used or treatment exceeds 10 days, clinical and laboratory monitoring is recommended.

Patients with a history of blood disorders should be monitored for leukocyte counts, especially during repeated treatment courses.

Exacerbation of central or peripheral nervous system disturbances may occur during treatment with ornidazole. In case of peripheral neuropathy, movement coordination disturbances (ataxia), dizziness, or mental confusion, treatment should be discontinued.

Exacerbation of candidiasis may occur, which may require appropriate treatment.

In patients undergoing hemodialysis, the shortened elimination half-life should be considered, and additional doses of the drug should be administered before or after dialysis.

Serum concentrations of lithium salts, creatinine, and electrolytes should be monitored during concomitant lithium therapy.

The effects of other medicinal products may be enhanced or diminished during treatment with ornidazole.

Use during pregnancy or breastfeeding.

Ornidazole is contraindicated during the first trimester of pregnancy. In the second and third trimesters, it should be used only if absolutely necessary. Breastfeeding should be discontinued if the drug is required.

Ability to affect reaction rate when driving or operating machinery.

Ornidazole may cause symptoms such as somnolence, muscle rigidity, dizziness, tremor, seizures, impaired coordination, and transient loss of consciousness. Patients who drive or operate machinery should be aware of these potential effects.

Method of administration and dosage.

Dosage and duration of treatment are determined by the physician according to the nature of the disease and treatment regimen.

The drug should be administered intravenously over 15–30 minutes.

For anaerobic systemic infections: initial intravenous dose of 500–1000 mg, followed by 500 mg every 12 hours or 1000 mg every 24 hours for 5–10 days (stepwise dosing). After stabilization of the patient's condition, switch to oral ornidazole (e.g., 500 mg tablets, one tablet every 12 hours).

For children under 12 years of age with body weight over 6 kg, the daily dose should be 20 mg/kg, divided into two doses, administered for 5–10 days.

For prophylaxis of anaerobic bacterial infections during surgical procedures: administer 500–1000 mg to adults and children aged 12 years and older, 30 minutes before surgery.

For prophylaxis of mixed infections, ornidazole should be used concomitantly with aminoglycosides, penicillin, or cephalosporins. The drugs should be administered separately.

Severe amoebic dysentery, all extraintestinal forms of amoebiasis, giardiasis, liver abscess: initial dose for adults and children aged 12 years and older is 500–1000 mg, followed by 500 mg every 12 hours for 3–6 days.

For children under 12 years of age with body weight over 6 kg, the daily dose should be 20–30 mg/kg, divided into two doses. The duration of treatment is determined by the physician according to the nature of the disease.

In patients with impaired renal function, the dosing interval should be prolonged or the single and daily dose reduced.

Children.

Ornidazole should not be administered to children with body weight less than 6 kg.

Overdose.

Symptoms: nausea, vomiting, anorexia, possible intensification of other adverse reaction symptoms.

Treatment: no specific antidote is known; in case of seizures, diazepam should be administered. Symptomatic therapy.

Adverse reactions.

Blood and lymphatic system disorders: manifestations of bone marrow suppression, moderate leukopenia, neutropenia.

Immune system disorders: hypersensitivity reactions, including anaphylactic shock, angioedema.

Skin and subcutaneous tissue disorders: skin rash, urticaria, skin hyperemia, pruritus.

Nervous system disorders: dizziness, somnolence, headache, tremor, muscle rigidity, coordination disturbances, ataxia, seizures, transient loss of consciousness, confusion, signs of sensory or mixed peripheral neuropathy, excitement.

Gastrointestinal disorders: taste disturbances, metallic taste in the mouth, dry mouth, coated tongue, nausea, vomiting, dyspepsia, sensation of heaviness and tenderness in the epigastric area.

Hepatobiliary disorders: hepatotoxicity, changes in liver function tests.

General disorders and administration site conditions: increased body temperature, chills, general weakness, increased fatigue, dyspnea, changes at the injection site, including pain, redness, burning sensation at the injection site.

Other: darkening of urine color, cardiovascular disorders, including arterial hypotension.

Shelf life. 2 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25°C.

Keep out of reach of children.

Incompatibility.

The drug should not be mixed with other injectable solutions during administration.

Packaging.

100 ml in glass bottles with a rubber stopper, sealed with an aluminum cap. 1 bottle per carton.

Prescription status. Prescription only.

Manufacturer.

JSC "Halychpharm".

Manufacturer's location and address of business activity.

79024, Lviv, Opryshkovska St., 6/8, Ukraine.

Marketing Authorization Holder.

JSC "Halychpharm".

Address of Marketing Authorization Holder.

79024, Lviv, Opryshkovska St., 6/8, Ukraine.