Metronidazole

Pharmacological properties

metronidazole is a synthetic antibacterial and antiprotozoal agent of the nitroimidazole group. efloran is active against trichomonas vaginalis, entamoeba histolytica and giardia lamblia, as well as anaerobic gram-negative and gram-positive bacteria (different types of clostridium, eubacterium, peptococcus, peptostreptococcus and other anaerobic bacteria sensitive to metronidazole).

Metronidazole penetrates the bacterial cell, its nitro group is reduced to hydroxylamine and interacts with the DNA of the microbial cell, which leads to inhibition or death of the DNA of the microorganism.

Pharmacokinetics The maximum concentration in blood plasma is almost the same after iv administration or oral administration; bioavailability is 90-100%. After 4–6 hours, the concentration of metronidazole in tissues and body fluids reaches 80–90% of its concentration in blood plasma. An insignificant part of metronidazole binds to blood plasma proteins - not more than 20%. T_½ active substance is 8 hours. It penetrates well into all tissues, organs and body fluids.

Metronidazole is converted in the liver to oxide metabolites, which are mainly excreted in the urine as glucuronides.

The presystemic metabolism of the active substance is negligible. Metabolism is slowed down in patients with liver diseases. In patients with renal failure, metabolites can accumulate.

Unmetabolized metronidazole is excreted mainly in urine. From 6 to 15% of the administered dose is excreted in the feces. Metronidazole and its metabolites are rapidly removed during hemodialysis.

Indications

• treatment and prevention of bacterial infections caused by susceptible microorganisms (various types of bacteroides spp., Fusobacteria spp., Clostridium spp., Eubacterium spp., Gardnerella vaginalis, as well as anaerobic cocci, trichomonas, entamoeba histolytica, giardia lamblia,)

• prevention of postoperative anaerobic infections caused by various types of Bacteroides spp. and Streptococci;

• treatment of septicemia, bacteremia, peritonitis, brain abscess, necrotic pneumonia, osteomyelitis, postpartum sepsis, pelvic abscess and postoperative wound infection;

• urogenital trichomoniasis in women (trichomonas vaginitis) and men;

• non-specific vaginitis;

• all forms of amoebiasis;

• giardiasis;

• ulcers of the lower extremities and pressure sores caused by anaerobic microorganisms;

• acute dental infections (acute pericoronitis, acute apical infection).

Application

Orally

The tablets are swallowed without chewing, washed down with water, during or after a meal. Treatment lasts for 7 days. If necessary, and given the type of infection, the duration of treatment can be increased, depending on the indications.

Prevention of anaerobic infections (especially during surgical interventions on the digestive tract and during gynecological operations)

Treatment usually begins with iv administration. At the earliest opportunity, you should switch to treatment in tablet form.

The adult dose is 400 mg every 8 hours.

Treatment for anaerobic infections

The adult dose is 800 mg every 8 hours.

Protozoal and other infections

Amoebiasis

In children, the drug is used in proportionally lower doses in liquid dosage forms.

Elderly patients. In elderly patients, the pharmacokinetics of metronidazole may change, therefore, control of plasma levels of metronidazole may be necessary.

Parenteral

Before use, it is necessary to make skin tests for tolerance to the drug.

Therapy usually begins with a slow intravenous injection (average infusion rate is 5 ml / min). At the earliest opportunity, you should switch to treatment with pills.

Prevention of postoperative anaerobic infections: abdominal (especially large intestine) and gynecological

The adult dose is 500 mg every 8 hours iv slowly. At the first opportunity, it is necessary to switch to treatment with tablets - 200 or 400 mg every 8 hours. If necessary, and taking into account the type of infection, treatment can be longer, depending on the indications.

The dose for children under the age of 12 years is 7.5 mg / kg body weight (1.5 ml / kg) every 8 hours iv slowly.

With the development of postoperative infection, therapy should be continued for at least 7 days.

Treatment for anaerobic infections

The adult dose is 500 mg every 8 hours iv slowly.

For children under the age of 12 years, the dose is 7.5 mg / kg body weight by slow iv infusion according to the same scheme as for adults. Treatment lasts for 7 days.

Contraindications

• Hypersensitivity to metronidazole or other drugs with a similar chemical structure (nitroimidazole), as well as to other components of the drug;

• I trimester of pregnancy - for the drug in the form of tablets;

• period of pregnancy - for the drug in the form of a solution for infusion;

• lactation period.