Metronidazole - Instructions For Use And Indications

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Metronidazole - Instructions For Use And Indications
Metronidazole - Instructions For Use And Indications

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Video: How and When to use Metronidazole (Flagyl, Metrogel) - Doctor Explains 2023, February
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Metronidazole is an instruction for a broad-spectrum drug that is used in the treatment of various diseases. The drug can be used to treat amoebiasis, trichomoniasis, infections of bones and joints, lower respiratory tract, bacterial septicemia, endocarditis, and a number of other diseases. The release of metronidazole is produced in several dosage forms, which is an undoubted advantage of this drug.

The content of the article:

  • 1 Pharmacodynamics
  • 2 Pharmacokinetics of metronidazole
  • 3 Form of release of metronidazole
  • 4 Indications for the use of metronidazole

    • 4.1 Trichomoniasis with clinical symptoms
    • 4.2 Asymptomatic trichomoniasis
    • 4.3 Treatment of a spouse without clinical manifestations
    • 4.4 Amoebiasis
    • 4.5 Anaerobic bacterial infections
    • 4.6 Metronidazole - instructions. Other indications:
  • 5 Metronidazole - instructions. Side effects
  • 6 Precautions
  • 7 Application during pregnancy and during breastfeeding
  • 8 Special instructions
  • 9 Metronidazole - instructions for dosing regimen
  • 10 Interaction with other medicinal products

Pharmacodynamics

Synthetic antibacterial and antiprotozoal drug of the 5-nitroimidazole group. The drug has an antibacterial, antiprotozoal effect. The mechanism of action consists in the biochemical reduction of the 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa.

What is metronidazole for?
What is metronidazole for?

The reduced 5-nitro group of metronidazole interacts with the DNA of the cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Suppresses the development of protozoa (Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp.), Highly effective against obligate anaerobic bacteria Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (Prevotella bivia, Prevotella and gram-positive microorganisms) Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). The MIC for these strains is 0.125-6.25 μg / ml.

In combination with amoxicillin, it is active against Helicobacter pylori (amoxicillin inhibits the development of resistance to metronidazole). Has no direct effect on aerobes and facultative anaerobes.

In mixed aerobic-anaerobic infections, metronidazole acts synergistically with antibiotics that are effective against pathogenic aerobes. It increases the sensitivity of tumors to radiation, causes disulfiram-like reactions, and stimulates reparative processes.

Pharmacokinetics of metronidazole

What is metronidazole for?
What is metronidazole for?

Metronidazole - instructions for oral administration. The drug is rapidly and almost completely absorbed. Bioavailability is not less than 80%. Possesses high penetrating ability, reaching bactericidal concentrations in most tissues and body fluids, including lungs, kidneys, liver, skin, CSF, brain, bile, saliva, amniotic fluid, abscess cavities, vaginal secretions, semen, breast milk, penetrates the BBB and the placental barrier.

Food intake does not affect the absorption of the drug. The half-life is 8-10 hours, the connection with blood proteins is insignificant and does not exceed 10-20%. Volume of distribution: adults - about 0.55 l / kg, newborns - 0.54-0.81 l / kg. TCmax - 1-3 hours. Communication with plasma proteins - 10-20%.

Good to know! Metronidazole - instructions. The main metabolite (2-oxymetronidazole) also has antiprotozoal and antimicrobial effects. T1 / 2 with normal liver function - 8 hours (from 6 to 12 hours), with alcoholic liver damage - 18 hours (from 10 to 29 hours), in newborns: those born during pregnancy - 28-30 weeks - about 75 hours, 32-35 weeks - 35 hours, 36-40 weeks - 25 hours.

The drug quickly penetrates into tissues (lungs, kidneys, liver, skin, bile, cerebrospinal fluid, saliva, seminal fluid, vaginal secretions), into breast milk and passes through the placental barrier.

Metronidazole is metabolized by hydroxylation, oxidation and glucuronidation. It is excreted by the kidneys 60-80% (20% unchanged), through the intestines - 6-15%.

What is metronidazole for?
What is metronidazole for?

Renal clearance - 10.2 ml / min. In patients with impaired renal function after repeated administration, accumulation of metronidazole in the blood serum may be observed (therefore, in patients with severe renal insufficiency, the frequency of administration should be reduced).

Metronidazole and the main metabolites are quickly removed from the blood during hemodialysis (T1 / 2 is reduced to 2.6 hours). With peritoneal dialysis, it is excreted in small quantities.

Release form of metronidazole

Metronidazole - instructions for external use, cream for external use, vaginal gel, vaginal suppositories, vaginal tablets, powder for preparing a solution for intravenous administration, solution for infusion, suspension for oral administration, tablets, coated tablets.

Indications for the use of metronidazole

In order to avoid the development of resistance of microorganisms, metronidazole should be used only for the treatment of infections caused by metronidazole-susceptible strains (according to microbiological examination of the material or epidemiological data).

Trichomoniasis with clinical symptoms

What is metronidazole for?
What is metronidazole for?

Metronidazole is indicated for the treatment of symptomatic trichomoniasis in women and men if the presence of Trichomonas has been confirmed by appropriate laboratory tests (smear and / or culture).

Asymptomatic trichomoniasis

Metronidazole is indicated for the treatment of women with asymptomatic trichomoniasis (endocervicitis, cervicitis, or cervical erosion). Since there is evidence that the presence of Trichomonas can interfere with the accurate assessment of cytological smears, additional smears should be performed after the parasite is eradicated.

Treatment of a spouse without clinical manifestations

T. vaginalis infection is a sexually transmitted disease. Thus, symptomatic sexual partners should be treated concurrently to prevent re-infection from the partner, even if the pathogen is not isolated.

Metronidazole - instructions. The decision as to whether to treat a clinically non-symptomatic male partner who does not have Trichomonas, or if no analysis has been performed, is individual. In making this decision, it should be noted that there is evidence that a woman can become infected again if her spouse has not been treated.

In addition, since there are significant difficulties in isolating the pathogen in a patient without clinical manifestations, one should not rely on a negative smear and culture result. In any case, in case of re-infection, the spouses should be treated with metronidazole at the same time.

Amebiasis

What is metronidazole for?
What is metronidazole for?

Metronidazole - instructions for the treatment of acute intestinal amebiasis (amoebic dysentery) and liver abscess caused by amoebae. When treating liver abscess caused by amoebae with metronidazole, the need for aspiration or drainage of pus is not excluded.

Anaerobic bacterial infections

Metronidazole is indicated for the treatment of severe infections caused by susceptible anaerobic bacteria. Necessary surgical procedures must be performed in conjunction with metronidazole therapy.

In the case of mixed aerobic and anaerobic infection, appropriate antimicrobial agents should be used in addition to metronidazole. When treating severe anaerobic infections, metronidazole is usually given first.

Intra-abdominal infections, including peritonitis, intra-abdominal abscess, and liver abscess, are caused by Bacteroides including the B. fragilis group (B. fragilis, B. distasonis, B. ovatus, B. thetaiotaomicron, B. vulgatus), Clostridium, Eubacterium, Peptococcusnigercocus Peptost.

Metronidazole - instructions. Other indications:

  • Infections of the skin and cutaneous structures caused by Bacteroides (including group B. Fragilis), Clostridium, Peptococcusniger, Peptostreptococcus and Fusobacterium.
  • Gynecological infections, including endometritis, endomyometritis, tubo-ovarian abscess, and infections after gynecological surgery, caused by Bacteroides (including group B. Fragilis), Clostridium, Peptococcus niger, and Peptostreptococcus.
  • Bacterial septicemia caused by Bacteroides (including group B. Fragilis) and Clostridium.
  • Bone and joint infections caused by Bacteroides species (including group B. Fragilis) as adjunctive therapy.
  • Central nervous system infections, including meningitis and brain abscess, caused by Bacteroides (including group B. Fragilis).
  • Lower respiratory tract infections, including pneumonia, empyema and lung abscess, caused by Bacteroides (including group B. Fragilis).
  • Endocarditis caused by Bacteroides (including B. Fragilis group).

Metronidazole - instructions. Side effects

Possible lack of appetite, nausea, loose stools, discomfort in the supragastric region, abdominal cramps, constipation, intestinal colic, headache, digestive disorders (stomatitis, metallic taste, sensation of unevenness of the tongue, dry mouth, inflammation of the tongue), changes in the blood test (persistent thrombocytopenia, reversible neutropenia), cardiovascular disorders (flattening of the T-wave on the ECG), neurological disorders (aseptic meningitis, seizures, encephalopathy, impaired coordination, optic neuropathy, dizziness, peripheral neuropathy, excitability, confusion, disturbances in consciousness, hallucinations insomnia, irritability, depression), urinary disorders (dyspareunia, urinary disorders, dark urine, cystitis, urinary incontinence, vaginal candidiasis),allergic reactions (redness of the skin, urticaria, joint pain, Stevens-Johnson syndrome, erythematous rash, hot flashes, nasal congestion, toxic epidermal necrolysis), fever, dryness in the vagina, vulva, decreased sex drive, proctitis, dry mouth.

Precautions

Metronidazole - instructions for long-term therapy. It is necessary to control the blood picture. With leukopenia, the possibility of continuing treatment depends on the risk of developing an infectious process. The appearance of ataxia, dizziness and any other deterioration in the neurological status of patients requires discontinuation of treatment.

May immobilize treponemas and lead to false positive Nelson's test. It is recommended to stop breastfeeding during lactation.

Influence on the ability to drive vehicles and other potentially dangerous mechanisms. Dizziness, confusion, hallucinations, or seizures associated with taking this drug may develop, which interferes with operator activity.

Application during pregnancy and during breastfeeding

What is metronidazole for?
What is metronidazole for?

Since metronidazole passes through the placental barrier and its effect on the organogenesis of the human fetus is unknown, it is not recommended to use metronidazole during pregnancy.

Metronidazole passes into breast milk, so its use should be avoided during breastfeeding.

special instructions

During the treatment period, ethanol is contraindicated (a disulfiram-like reaction may develop: spastic abdominal pain, nausea, vomiting, headache, sudden flushing of the face).

In combination with amoxicillin, it is not recommended for use in patients under 18 years of age.

With prolonged therapy, it is necessary to control the blood picture.

What is metronidazole for?
What is metronidazole for?

Metronidazole - instructions for leukopenia, the possibility of continuing treatment depends on the risk of developing an infectious process. The appearance of ataxia, dizziness and any other deterioration in the neurological status of patients requires discontinuation of treatment. May immobilize treponemas and lead to false positive Nelson's test. Stains urine dark.

When treating Trichomonas vaginitis in women and Trichomonas urethritis in men, it is necessary to refrain from sexual activity. Simultaneous treatment of sexual partners is mandatory.

Treatment does not stop during menses. After trichomoniasis therapy, control tests should be performed during three successive cycles before and after menstruation.

After treatment of giardiasis, if symptoms persist, after 3-4 weeks, conduct 3 fecal analyzes at intervals of several days (in some successfully treated patients, lactose intolerance caused by invasion may persist for several weeks or months, resembling the symptoms of giardiasis).

Metronidazole - dosing instructions

Inside, during or after meals, (or with milk), without chewing.

With trichomoniasis - 250 mg 2 times / day for 10 days or 400 mg 2 times / day for 5-8 days. Women need to additionally prescribe Metronidazole in the form of vaginal suppositories or tablets. If necessary, you can repeat the course of treatment or increase the dose to 0.75-1 g / day.

What is metronidazole for?
What is metronidazole for?

Between courses, you should take a break of 3-4 weeks with repeated control laboratory tests. An alternative therapy regimen is the appointment of 2 g once to the patient and his sexual partner. Children 2-5 years old - 250 mg / day; 5-10 years old - 250-375 mg / day, over 10 years old - 500 mg / day. The daily dose should be divided into 2 doses. The course of treatment is 10 days.

With giardiasis - 500 mg 2 times / day for 5-7 days. Children under 1 year old - 125 mg / day, 2-4 years old - but 250 mg / day, 5-8 years old - 375 mg / day, over 8 years old - 500 mg / day (in 2 doses). The course of treatment is 5 days.

With giardiasis - 15 mg / kg / day in 3 divided doses for 5 days.

Adults: with asymptomatic amebiasis (if a cyst is detected), the daily dose is 1-1.5 g (500 mg 2-3 times / day) for 5-7 days.

In chronic amoebiasis, the daily dose is 1.5 g in 3 divided doses for 5-10 days.

In acute amoebic dysentery - 2.25 g in 3 divided doses until symptoms stop.

What is metronidazole for?
What is metronidazole for?

For liver abscess - the maximum daily dose is 2.5 g in 1 or 2-3 doses, for 3-5 days, in combination with antibiotics (tetracyclines) and other methods of therapy. Children 1-3 years old - 1/4 of the adult dose, 3 -7 years old - 1/3 adult dose, 7-10 years old - 1/2 adult dose.

With balantidiasis - 750 mg 3 times / day for 5-6 days.

In case of ulcerative stomatitis, adults are prescribed 500 mg 2 times / day for 3-5 days; in this case, the drug is not indicated for children.

With pseudomembranous colitis - 500 mg 3-4 times / day.

For the eradication of Helicobacter pylory - 500 mg 3 times / day for 7 days (as part of combination therapy, for example, a combination with amoxicillin 2.25 g / day).

Metronidazole - instructions. In the treatment of anaerobic infection, the maximum daily dose is 1.5-2 g. In the treatment of chronic alcoholism, 500 mg / day is prescribed for a period of up to 6 (no more) months.

For the prevention of infectious complications - 750-1500 mg / cyt in 3 doses 3-4 days before the operation, or once 1 g on the 1st day after the operation. 1-2 days after surgery (when oral administration is already allowed) - 750 mg / day for 7 days.

In severe renal impairment (CC less than 10 ml / min), the daily dose should be halved.

Interaction with other medicinal products

It enhances the effect of indirect anticoagulants, which leads to an increase in the time of prothrombin formation (a dose adjustment of anticoagulants is required). The simultaneous administration of drugs that stimulate enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin) can accelerate the excretion of metronidazole, as a result of which its concentration in plasma decreases. Cimetidine inhibits the metabolism of metronidazole, which can lead to an increase in its concentration in the blood serum and an increased risk of side effects.

What is metronidazole for?
What is metronidazole for?

Simultaneous use with disulfiram can lead to the development of various neurological symptoms (the interval between appointments is at least 2 weeks).

When taken simultaneously with lithium preparations, the concentration of the latter in the plasma may increase and the development of symptoms of intoxication (you should stop taking lithium preparations or reduce the dose). It is not recommended to combine with non-depolarizing muscle relaxants (vecuronium bromide).

Sulfonamides enhance the antimicrobial effect of metronidazole. The simultaneous use of alcohol and metronidazole causes disulfiram-like reactions (cramp-like abdominal pain, nausea, vomiting, headache, flushing of the skin).

Metronidazole can affect the determination of biochemical parameters such as aspartate aminotransferase (ACT), alanine aminotransferase (ALT), lactate dehydrogenase (LDH), triglycerides, glucose.

Find out more:

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  • Metronidazole tablets: properties and instructions for use

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