Secnidazole

Pharmacological properties

Pharmacodynamics

Mechanism of action. Secnidazole is an antiprotozoal agent of the nitroimidazole group with antibacterial effect. Secnidazole is characterized by a bactericidal (against gram-positive and gram-negative anaerobic bacteria) and amoebicidal (intra- and external intestinal) effect. Secnidazole is especially active against Trichomonas vaginalis, Entamoeba histolytica, Giardia lamblia. Penetrating into the cell of the microorganism, secnidazole is activated as a result of the restoration of the 5-nitro group, due to which it interacts with cellular DNA. There is a violation of its spiral structure and destruction of filaments, inhibition of nucleotide synthesis and cell death.

Pharmacokinetics

Absorption. After oral administration, secnidazole is rapidly and completely absorbed in the digestive tract. Bioavailability is almost 100%. After oral administration of a single dose of 2 g of C_max secnidazole in blood plasma is reached after 3 hours

Distribution. The binding of secnidazole to plasma proteins is approximately 15%. Secnidazole passes through the BBB and into breast milk.

Metabolism. Secnidazole is metabolized in the liver.

T_½ secnidazole is approximately 25 hours. Secnidazole is excreted mainly in the urine. Excretion is slow: 16% of the administered dose of secnidazole is excreted within 72 hours, and 50% within 120 hours.

Indications

• Trichomonas urethritis and vaginitis (caused by trichomonas vaginalis); bacterial vaginosis; intestinal amoebiasis (caused by entamoeba histolytica); liver amoebiasis (caused by entamoeba histolytica); giardiasis (caused by giardia lamblia).

Application

Samitol should be used orally immediately before meals with a small amount of water.

Doses for adults

Urogenital trichomoniasis, bacterial vaginosis: 4 tablets of 500 mg are used in one dose 1 time per day or in two doses per day with an interval of 12 hours (total - 2 g).

Acute intestinal amoebiasis and giardiasis: 4 tablets of 500 mg are used in one dose 1 time per day or in two doses per day with an interval of 12 hours (total - 2 g).

Chronic carriage of cysts or amoebas: 3 tablets of 500 mg should be used in one dose or in several doses for 3 days.

Liver amoebiasis: 3 tablets of 500 mg should be used in one dose or in several doses for 5 days.

Doses for children *

At the discretion of the doctor, from 25 to 30 mg / kg / day. The duration of treatment depends on the indications and is similar to that for adults.

* This dosage form is intended for use by children with a body weight of 20 kg.

Doses for patients with renal or hepatic impairment

For patients with renal or hepatic insufficiency, recommendations for dose adjustment depend on those recommended for nitro-5-imidazole derivatives in general.

Renal failure of moderate to severe degree: usually dose adjustment is not required, especially with short-term treatment.

Severe liver failure: a reduction in the daily dose is necessary depending on the condition of the patient.

Contraindications

• Hypersensitivity to secnidazole or other components of the drug or to other nitroimidazole derivatives; organic diseases of the central nervous system; i trimester of pregnancy; blood dysrasia, including a history.

Side effects

On the part of the immune system: hypersensitivity reactions, including hyperemia (erythema), rash, urticaria, angioedema, bronchospasm, fever and anaphylactic reactions.

On the part of the blood and lymphatic system: moderate reversible leukopenia, reversible neutropenia, agranulocytosis, thrombocytopenia.

From the cardiovascular system: palpitations.

From the digestive system: pain in the epigastrium and / or abdomen, nausea, vomiting, diarrhea, constipation, glossitis, stomatitis, taste disturbance (metallic taste in the mouth), anorexia.

On the part of the liver and biliary tract: hepatitis.

From the nervous system: headache, cramps, dizziness, loss of consciousness, paresthesia, neuropathy (sensory peripheral and sensory-motor polyneuritis), encephalopathy * (state of confusion), cerebellar syndrome * (ataxia, dysarthria, impaired coordination of movements, nystagmus, tremor).

From the side of the psyche: psychosis, confusion, hallucinations.

General disorders: weakness.

Note: * after discontinuation of treatment, the symptoms disappear.

special instructions

Alcohol. during the use of the drug and for 72 hours after the completion of its use, alcohol is contraindicated in order to prevent the occurrence of adverse reactions similar to those observed with the use of disulfiram (redness of the skin, colicky abdominal pain, vomiting and tachycardia).

Long reception. If it is necessary to use secnidazole for a long period, compared with the recommended, patients need to monitor the blood picture (in particular, the number of leukocytes). It is also recommended that a doctor observe because of the risk of adverse reactions from the central nervous system and peripheral nervous system (paresthesia, ataxia, dizziness, convulsive seizures).

Hepatic encephalopathy. Secnidazole should be prescribed with caution to patients with hepatic encephalopathy. Therapy should be discontinued in case of impaired coordination of movements, dizziness or blurred consciousness.

Sexual relations. You should refrain from sexual intercourse during treatment with secnidazole.

Use during pregnancy and lactation. Do not use during pregnancy and lactation.

Children. The drug is approved for use in children in accordance with the dosage recommendations specified in the APPLICATION section, taking into account the possibility of using this dosage form in children weighing 20 kg.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Secnidazole does not affect the reaction rate when driving vehicles or working with other mechanisms.

Interactions

Disulfiram: concomitant use with secnidazole can cause paranoid reactions and psychoses.

Alcohol: combination with alcohol causes symptoms of a disulfiram-like reaction (abdominal cramps, nausea, vomiting, headache, flushing of the face), delirious attacks and dizziness are possible.

Anticoagulants: secnidazole with simultaneous use enhances the effect of indirect anticoagulants (coumarin and indandion derivatives), the risk of bleeding increases. Monitoring of prothrombin time and dose adjustment if necessary are necessary.

Lithium preparations: with simultaneous use with secnidazole, the concentration of lithium in the blood plasma increases.

Cyclosporine: risk of elevated plasma cyclosporine levels. It is necessary to monitor the level of cyclosporine and creatinine in the case of the combined use of secnidazole with cyclosporine.

Non-depolarizing muscle relaxants (vecuronium bromide): not recommended for combination with secnidazole.

Amoxicillin: with simultaneous use with secnidazole, activity against Helicobacter pylori increases (amoxicillin inhibits the development of resistance).

5-Fluorouracil: when combined with secnidazole, the clearance of 5-fluorouracil decreases, which causes an increase in its toxicity.

Overdose

Symptoms: it is possible to increase adverse reactions, in particular from the nervous system.

Treatment: there is no specific antidote. If necessary, carry out symptomatic therapy or hemodialysis.

Storage conditions

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