Flagil

Flagil contains the active ingredient metronidazole; the drug belongs to the subgroup of nitro-5-imidazoles and has a therapeutic effect on the biochemical reduction of the 5-nitro group of metronidazoles using transport proteins of cells of protozoan bacteria and anaerobes.

After recovery, the specified group, interacting with the DNA of the microbial cells, inhibits the binding of nucleic acids, causing the lysis of the pathogenic bacterium cell. [1]

2-oxymetronidazole (the main metabolic element of metronidazole) also has antiprotozoal and antimicrobial effects. [2]

Indications Flagil

It is used (in tablets) for such diseases:

• protozoal infections (among them the extraintestinal form of amebiasis (also amoebic liver abscess) and its intestinal form, balantidiasis, giardiasis , vaginitis or urethritis of Trichomonas origin, epidermal leishmaniasis and trichomoniasis);
• lesions associated with the influence of bacteroids (this includes infections of bones with joints or the central nervous system ( meningitis or brain abscess), bacterial endocarditis, pulmonary empyema or abscess, pneumonia and sepsis);
• infections arising under the influence of strains of clostridia, peptostreptococci and peptococci (among them, infections affecting the pelvic organs (abscess in the fallopian tubes and ovaries, endometritis and infection of the vaginal vault), and intraperitoneal lesions (peritonitis or liver abscess));
• gastritis or ulcers in the duodenal region associated with the influence of Helicobacter pylori (combined treatment);
• colitis of the pseudomembranous type (associated with taking antibiotics);
• prevention of the development of complications during the postoperative period (especially for operations in the colon area, appendectomy, pararectal procedures and gynecological interventions).

Suppositories are prescribed in such cases:

• local treatment for vaginitis (this includes its Trichomonas and nonspecific forms);
• prevention of the formation of anaerobic infections, possible in the case of operations in the peritoneum and pelvic organs.

Release form

The release of the drug is realized in the form of tablets for oral administration (20 pieces each) and vaginal suppositories (10 pieces each).

Pharmacodynamics

The antiprotozoal and antimicrobial effect of metronidazole develops relative to the majority of pathogenic bacteria, including: Trichomonas, peptostreptococci with dysentery amoeba, peptococci, fusobacteria with intestinal lamblia and clostridia, and in addition to this anaerobic bacteroid strains of the etiologic eutamic type and obligate spore-forming.

Facultative and aerobic strains of anaerobic bacteria are resistant to metronidazole. [3]

Pharmacokinetics

After oral administration, metronidazole is almost completely and at high speed absorbed inside the gastrointestinal tract (approximately 80% in 1 hour). Eating food does not alter drug absorption. The bioavailability level is 100%. After oral administration of 0.5 g of metronidazole, after 1 hour, its plasma index is 10 μg / ml, and after 3 hours - 13.5 μg / ml.

The half-life is within 8-10 hours. Synthesis with whey protein is equal to no more than 10-20% of the applied dosage.

Metronidazole quickly passes into fluids with tissues (among them the kidneys, liver, bile, lungs, skin, vaginal discharge, saliva, cerebrospinal fluid and seminal fluid) and breast milk, and in addition, it overcomes the placenta.

About 30-60% of the drug undergoes changes in metabolic processes, through hydroxylation, oxidation and glucuronidation.

Metronidazole is excreted by 40-70% through the kidneys (35% have an unchanged form).

In the case of kidney disease, with repeated use of metronidazole, its serum accumulation may occur.

With the introduction of the drug into the vagina in a portion of 0.5 g, systemic absorption is about 20%; in this case, intraplasma values are equal to about 12%, compared with the same 1-time portion taken orally.

Less than 20% of the drug undergoes protein synthesis. The term half-life for systemic use and healthy liver function is 8-10 hours.

Dosing and administration

Schemes for the use of tablets.

The tablets are taken orally.

With amoebiasis, adults need to use 1.5 g of the medication per day (divide the portion into 3 uses). The therapy lasts 7 days.

In the case of giardiasis, a child of 6-10 years old should take 375 mg of the substance per day, a child of 10-15 years old - 0.5 g each, and an adult - 0.75-1 g each. Treatment lasts 5 days.

Trichomoniasis (urethritis or vaginitis in a woman and urethritis in a man) requires a 1-time intake of a 2 g portion or a course of treatment - with a daily dosage of 0.5 g (divided into 2 applications) and a duration of therapy of 10 days.

For non-specific vaginitis, 0.5 g of Flagil is used per day (divided by 2 uses); therapy lasts 1 week.

For the treatment of anaerobic infections, 1-1.5 g of the drug must be used per day.

In the case of severe renal dysfunction (CC level below 10 ml per minute), it is required to halve the daily portion.

Schemes for the use of suppositories.

Suppositories should only be used by adult women. The suppository must be injected deep into the vagina.

With Trichomonas vaginitis, you should use 1 suppository (0.5 g) per day, in combination with Flagil tablets. The therapy lasts 10 days.

With a nonspecific form of vaginitis, 1 suppository is used 2 times a day (a portion is 1 g). The treatment lasts 1 week. If necessary, you can also use the oral form of the medication.

It is imperative to carry out the same therapy with the woman's sexual partner, regardless of the presence of visible signs of the disease.

Flagil can be used for a maximum of 10 days; the course can be repeated a maximum of 2-3 times a year.

• Application for children

It is forbidden to use tablets in persons under 6 years of age, and suppositories in patients under 18 years of age.

Use Flagil during pregnancy

Flagil should not be prescribed during breastfeeding and pregnancy.

Contraindications

Among the contraindications for suppositories and tablets:

• having an organic nature of the lesion of the central nervous system;
• blood diseases (among them a history of leukopenia);
• personal intolerance to imidazole;
• failure of the liver (when large portions are used).

Side effects Flagil

Side signs for suppositories and tablets:

• leuko- or neutropenia;
• xerostomia, glossitis, vomiting or nausea, metal taste and impaired appetite, and in addition, diarrhea or constipation, stomatitis, anorexia and epigastric pain;
• polyuria, cystitis, dysuria, urinary incontinence, reddish-brown urine;
• fever, disorder of coordination, headaches, hallucinations, dizziness, confusion, insomnia, convulsions, weakness and polyneuropathy (especially after prolonged use), and besides this, ataxia, severe excitability, depression and irritability;
• epidermal rash or hyperemia, urticaria;
• nasal congestion, candidiasis, pancreatitis, T-wave flattening in ECG readings and arthralgia.
• Negative manifestations of candles:
• burning or irritation in the area of the penis in the patient's sexual partner;;
• increased frequency of urination;
• vulvitis;
• vaginal burning;
• vaginal candidiasis (develops after stopping treatment).

Overdose

When poisoning with metronidazole, vomiting or nausea and ataxia occurs, and besides this, polyneuropathy and convulsions; requires symptomatic actions.

Interactions with other drugs

When used together with drugs containing ethanol, their intolerance develops.

The combination of metronidazole and disulfiram can provoke the development of various neurological symptoms, which is why it is necessary to use these drugs with a minimum of 2 weeks.

The combination with indirect anticoagulants potentiates their activity, which leads to an increase in the PTV level.

The introduction of simultaneously with cyclosporine or lithium agents can cause an increase in their plasma values.

Cimetidine can inhibit the metabolic transformations of metronidazole, as a result of which its serum index may increase and the risk of developing negative signs may increase.

The combination with medications that stimulate liver microsomal enzymes (phenobarbital or phenytoin) can increase the excretion of metronidazole, which reduces its plasma level.

Flagil reduces the clearance of 5-fluorouracil and increases the serum values of busulfan, which increases the toxicity of these drugs.

It is forbidden to combine metronidazole with non-depolarizing muscle relaxants (vecuronium bromide).

Storage conditions

Flagil must be kept at temperatures not exceeding 25 ° C.

Shelf life

Flagyl tablets can be used within a 5-year term from the date of manufacture of the therapeutic product; the shelf life of suppositories is 4 years.

Analogs

The analogs of the drug are the drugs Ginofort, Zalain and Atrikan with Tinidazole, and in addition, Ginalgin, Livarol and Nitazol, Candide and Ketoconazole with Neo-Penotran. Also on the list are Clotrimazole, Candibene, Funginal and Mikogal.

Reviews

Flagil gets quite different reviews. In some comments, the high therapeutic efficacy of the drug is noted, but there are also reports in which patients write about the frequent development of intense side symptoms with its use.

It should be noted that the use of metronidazole often causes various, at times severe, negative manifestations (weakness, fever, dizziness, epigastric pain, vomiting or nausea, urticaria, etc.), but due to the high effectiveness of treatment and the low cost of the drug, they do not prevent him from remaining quite a popular therapy.