Instructions for use Metronidazole(tablets, suppositories, gel, solution)

Update: February 2019 Metronidazole is a popular drug with
multiple pharmacological effects, often prescribed in
complex treatment of various pathologies. Received in 1960 and
actively used in medicine today.

It is a highly active drug, has
trichomonacid, antibacterial, antimicrobial,
antiprotozoan, anti-ulcer and anti-alcohol actions.
The drug is active against a wide range of microorganisms and
the simplest. Available in various dosage forms for
systemic, intravaginal and topical use and different
high penetrating power in biological tissues. Increases
the sensitivity of neoplasms to radiation has
disulfiram-like action (during reception
sensitization to alcohol) and activates reparative processes in
the body.

Клинико-фармакологическая группа: Противопротозойное
drug with antibacterial activity.

Composition, physico-chemical properties, price

Выпускается в форме таблеток, раствора (atводится внутривенно),
vaginal suppositories and gel for external and intravaginal
application.

Main substance and auxiliary components Physicochemical properties Packaging
Pills

Metronidazole – 250 or 500 mg in 1 tablet

Potato starch, stearic acid, talc

Pills плоскоцилиндри­ческой формы, белые либо с
yellowish-greenish tinged with chamfer and risky

10, 20, 30 pieces in a cellular package, 1-5, 10 blisters in
carton box

Метронидазол таблетки

Цена: № 24: 80-90 rub.

Solution

Metronidazole – 5 mg in 1 ml, 500 mg in 1 bottle

Sodium chloride, dihydrophosphate sodium dihydrate, water for
injections

Solution прозрачный, светло-желтого цвета, имеет зеленоватый
shade

On 100 ml in bottles from polyethylene, in a pack cardboard

Метронидазол раствор

Price: 100 ml: 25-45 rubles.

Candles

Metronidazole – 125, 250 or 500 mg

Polyethylene oxide, suppository fat, polyethylene oxide

Yellowish or white suppositories
torpedo

On 5 suppositories in a polyethylene strip, in packs
cardboard

Метронидазол свечи

Цена: № 10 по 500 мг: 180-250 руб.

Gel метрони­дазол 1 % (atагинальный и для наружного
application)

Metronidazole – 1 gr. 100 gr. gel

Propylene glycol, propyl parahydroxybenzoate, carbomer disodium
edetate, sodium hydroxide, purified water

Colorless, yellowish or yellow-green gel

30 gr. в алюминиевой тубе, в carton box. With applicator
for intra vaginal insertion

Метронидазол гель

Цена: 60-80 rubles.

pharmachologic effect

The active ingredient is a derivative of 5-nitroimidazole.
Therapeutic effects are based on the biochemical reaction
recovery of the 5-nitro group by intracellular transport proteins
микроорганизмов (анаэробных) и the simplest. In restored form
5-nitro group reacts with the DNA of microorganisms and
stops the synthesis of nucleic acids, which becomes the cause
their doom.

Effective against Gardnerella vaginalis, Lamblia spp.,
Entamoeba histolytica, Trichomonas vaginalis, Bacteroides spp. (at
including ovatus thetaiotaomicron, fragilis, distasonis, vulgatus),
Veillonella spp., Giardia intestinalis, Fusobacterium spp.,
Prevotella (bivia, buccae, disiens). Acts on some
Gram-positive microorganisms: Clostridium spp.,
Peptostreptococcus spp., Eubacter spp., Peptococcus spp.

In combination with amoxicillin has a detrimental effect on
Helicobacter pylori

The drug is insensitive aerobes and facultative anaerobes,
however, in the presence of mixed flora (represented by aerobes and
anaerobes) metronidazole works simultaneously with antibiotics,
effective against conventional aerobes, enhancing their action.

Pharmacodynamics and pharmacokinetics

It is fully and fairly rapidly absorbed by oral administration.
admission (bioavailability is 80%). Maximum level
blood concentrations are determined 1-3 hours after ingestion.
the range of 6-40 µg / ml (depending on the dose). Slightly
binds to plasma proteins, only 10–20%. Effectively
penetrates the body fluids and tissues, creates sufficient
bactericidal levels in seminal fluid, vaginal fluid and
saliva. Penetrates the body’s physiological barriers
(placental and hematoencephalic), as well as in breast milk.
Trichomonacid action, which kills up to 99% of sensitive
protozoa, observed at plasma concentrations of metronidazole
2.5 µg / ml, which lasts for 24 hours

Up to 30-60% of the main substance is metabolized by the reaction
hydroxylation, side chain oxidation and compounds with
glucuronic acid to form metabolites (inactive and
one active – 2-hydroxymetronidazole). The main metabolite is also
characterized by antimicrobial and antiprotozoal
action.

The half-life of the normal functioning of the liver in
the average is 8 hours, but can range from 6 to 12 hours. When
the presence of alcoholic liver damage is displayed longer, about 18
h. Newborns who were born at 28-30 week, displayed
after 75 hours, for births of 32-35 weeks – after 35 hours, and for
full-term babies hatch after 25 hours. Up to 80% is excreted
by the kidneys (20% is excreted unchanged), and about 15%
excreted by the intestines.

Metronidazole itself and its metabolites are removed from the blood at
hemodialysis is very fast, and the half-life in this case
reduced to 2.6 hours. In patients with renal dysfunction after
re-use possible cumulation of the active substance
in serum, so people with severe renal
failure should reduce the frequency of admission.

Indications for use

Tablets and solution

  • Protozoal infections: intestinal amebiasis (amoebic dysentery),
    amebiasis extraintestinal, liver abscess amebic, trichomoniasis (including
    vaginitis and urethritis caused by trichomonads), balantidiasis,
    giardiasis, giardiasis.
  • Infections that are caused by anaerobic bacteria of the genus
    Bacteroides spp .: CNS infections (including meningitis and abscesses
    brain), bones and joints, bacterial endocarditis, abscess and
    empyema of the lungs, pneumonia, sepsis.
  • Infections that are caused by the bacteria Peptostreptococcus spp.,
    Clostridium spp., Peptococcus niger: organ infections,
    localized in the pelvis (ovarian abscesses and fallopian tubes,
    endometritis, infectious lesions of the vaginal fornix), infectious
    processes of the abdominal cavity (liver abscesses, peritonitis).
  • Pseudomembranous colitis, which is associated with the use of
    antibiotics.
  • Gastritis or duodenal ulcer caused by Helicobacter
    pylori
  • Prevention of postoperative complications after intervention
    on the near-rectal zone, colon, upenectomy, after
    gynecological operations.
  • Radiotherapy of patients with tumors. In this case
    metronidazole is prescribed as a radiosensitizing drug and in
    cases where tumor resistance is associated with hypoxia in
    his cages.
  • Ulcerative stomatitis.
  • Alcoholism (currently rarely used
    in the pharmaceutical market more modern drugs).

Candles

As a drug of additional therapy to systemic medicinal
for the treatment of bacterial vaginitis and urogenital
trichomoniasis in women who are caused by sensitive to
metronidazole by microorganisms.

Gel

– vaginal:

  • Urogenital trichomoniasis;
  • Vaginitis nonspecific of various etiologies (with confirmation
    nature of the disease in the laboratory).

– outdoor:

  • Rosacea and acne vulgaris rash.
  • Eczema, including seborrheic, seborrheic dermatitis.
  • Trophic ulcers on the lower limbs that have developed on
    background varicose veins and diabetes.
  • Slow-healing wounds and bedsores.
  • Cracks of the anus, hemorrhoids.

Contraindications

The instructions for use of metronidazole are as follows.
contraindications:

  •  hypersensitivity to any component of the drug, in
    including and other nitroimidazole derivatives;
  • leukopenia (at the time of treatment or in history);
  • lesions of the central nervous system (organic), including epilepsy;
  • liver failure if treatment is required in
    large doses;
  • 1 trimester of pregnancy;
  • children up to 12 months;
  • lactation.

special instructions

Can metronidazole be used in 2-3 trimester of pregnancy? Have this
groups of patients the drug should be used strictly according to
prescribed by a doctor and under his control.

Care should also be taken when treating with metronidazole.
Patients with liver and kidney failure.

With severe liver dysfunction (with creatinine clearance less
10 ml / min) the prescribed daily dose is halved (with
intravenous daily should not be administered more than 1000
mg).

Dosage

The instructions for the tablets metronidazole indicated that the drug
take after or during a meal, without chewing, drinking water.

For the treatment of trichomoniasis is assigned

  • at a dose of 250 mg twice a day. 10 days;
  • or 400 mg twice daily., 5-8 days.
  • in the treatment of women should be prescribed an additional drug and
    vaginal suppositories.
  • alternative therapeutic regimen: 2 gr. once as
    the patient and his sexual partner.

The course of treatment with metronidazole can be repeated. Also permissible
take the drug in high doses up to 0.75-1 g. / day. Between
courses need to take a break for 3-4 weeks and be sure
control to conduct laboratory studies.

Treatment of trichomoniasis in children

In the age group of 2-5 years – 250 mg / day;

In the age group of 5-10 years: 250-375 mg / day;

Children 10-12 years: 500 mg / day.

How to take metronidazole to children: the daily dose is divided into
two doses with an equal period of time. The course of treatment – 10
days

For the treatment of giardiasis

Children up to 12 months. – 125 mg / day, 2-4 years – 250 mg / day, 5-8
years – at 375 mg / day, older than 8 years and adults – at 500 mg / day. (at
two receptions). Курс лечения – 5-8 days

Для лечения бессимптомного амебиаза у взрослых сут.
the dose is 1-1,5 gr. The dose is divided into 2-3 doses and treated in
течение 5-7 days

Для лечения амебиаза хронического сут. dose is 1.5
group, which is also divided into 3 doses and treated for 5-10 days
contract.

Для терапии амебной дизентерии острой принимают в сут.
dose 2.25 g., Which is divided into 3 doses and treated to
cessation of symptoms.

Для лечения амебного абсцесса печени назначается в
maximum day. dose 2,5 гр. on one or two or three doses, spend
treatment for 3-5 days, along with antibacterial drugs
and other methods of treatment. Children 1-3 years old appoint 1/4 adult
doses for children 3-7 years old – 1/3 of the adult dose, and for patients in
age group 7-10 years – 1/2 adult dose.

Для лечения язвенного стоматита назначается по 500 мг
twice a day, lasting 3-5 days (for children not
apply).

Для терапии псевдомембранозного колита принимают по 500
mg three or four times a day.

Для эрадикации бактерии Helicobacter pylory принимают
500 mg three times a day for 7 days, along with other
etiological agents.

При лечении анаэробных инфекций суточная максимальная
the dose is 1.5-2 grams. (divided into 2-3 doses).

Для терапии гиардиазиса: по 15 мг/кг/сут., разделив
dose of 3 doses. Лечение проводят 5 days

При балантидиазе: назначается по 750 мг препарата
трехкратно в сутки в течение 5-6 days

Для предупреждения инфекционных осложнений за 3-4 дня
before the operation, 750-1500 mg / day is prescribed, dividing the dose by 3
reception. The second scheme – the first day after the intervention
once 1 gr. 1-2 days after surgery, nominated for 750
mg / day in a week.

Для лечения алкоголизма в хронической форме: по 500
mg / day for 6 months.

Solution

Intravenous administration of the drug is advisable in case of severe
the course of infection and the impossibility of internal administration of the drug.
You can not mix with other drugs in one dropper.

  • Children from 12 years and adult patients a single dose is
    500 mg. Enter continuously (jet or drip) with speed
    administering 5 ml per minute. The daily maximum dose is 4 grams.
    Between введениями соблюдают восьмичасовой интервал. Duration
    treatment is prescribed individually. Further, after improvement
    condition, it is advisable to switch to other forms of the drug.
  • Children under 12 years old: prescribed at 7.5 mg / kg, dividing the dose by 3
    administration at a rate of 5 ml / min.
  • To prevent anaerobic infection before operative
    intervention on and organs localized in the pelvis or on
    urinary tract children from the age of 12 and adults are prescribed in the form
    infusions in the dosage of 500-1500 mg, which is administered on the day of surgery and
    after the intervention (the next day) every 8 hours. Then proceed
    for supportive treatment with oral forms of the drug.
  • As a radiosensitizing drug metronidazole
    administered by drip, before the start of irradiation, the dose is calculated
    individually: 160 mg / kg. The drug is administered before each session.
    облучения, 7-14 days With further irradiation, metronidazole is no longer
    apply.
  • For cancer of the body or cervix, at least skin cancer drug
    used for local applications (3 g. of the drug is dissolved in
    dimethyl sulfoxide (10% solution), cotton swabs are moistened in it,
    which apply for 1,5-2 h before irradiation. With weak regression
    Tumor procedures with the drug carried out during the course of irradiation.
    With a pronounced positive dynamics and cleansing of the tumor from necrosis
    the drug is used only during the first 14 days of treatment.

Candles метранидазол

Apply intravaginally, at night, 1 suppository (500 mg) per
день 10 дней contract. If necessary, after a month of treatment should
repeat. In gynecology, candle-shaped metoronidazole is most often
used in complex treatment, combining with drugs
system action.

Gel

Вводят интравагинально в рекомендуемой dose 5 гр. (which is equal to
one full applicator), twice a day, in the evening and in the morning, 5
дней contract.

Topically gel applied to cleansed skin or mucous membranes
in a thin layer, twice a day, in the morning and in the evening. Clinical
the effect develops after 3 weeks of treatment, the average course of therapy
is 1-4 months. The drug leaves no marks on the skin and
clothes, can be used and under cosmetics.

Side effects

Oral administration of metronidazole and intravenous administration
possible side effects of the drug:

Органы пищеварения: глоссит, стоматит, сухость во рту,
loose stools, anorexia, nausea, vomiting, constipation, intestinal
colic, taste of metal in the mouth, pancreatitis.

ЦНС: нарушение координации, неясное сознания,
dizziness, headache of varying severity,
ataxia, depression, irritability, irritability,
insomnia, weakness, hallucinations, convulsions, neuropathy
peripheral.

Мочеполовая система: цистит, диз- и полиурия,
urinary incontinence, candidiasis, change in urine color on
brown-red color.

Гепатобилиарная система: холестаз, желтуха, повышение
liver enzyme levels.

Аллергические реакции: сыпь, крапивница, лихорадка,
skin redness, nasal congestion, arthralgia.

Прочие: лейкопения, агранулоцитоз и нейтропения в
blood flattening of the T wave on the ECG.

Local reactions:

  • with injection of the drug at the site of reference is possible
    the development of thrombophlebitis, which is manifested by pain, swelling and
    hyperemia of the skin;
  • during treatment intravaginal forms may cause burning
    or irritation of the skin of the penis at the partner; speeded up
    urination, burning, itching, redness of the vaginal mucosa,
    vulvitis in a patient. After completion of the course of treatment is possible
    the development of vaginal candidiasis;
  • during treatment гелем для местного применения, помимо описанных
    allergic reactions, may develop burning and dry skin and
    lacrimation, if the gel is applied to the skin near the eyes.

Drug interactions

Can be taken with broad spectrum antibiotics (for example,
penicillin, cephalosporins).

  • In combination with indirect anticoagulants leads to an increase in
    period of formation of prothrombin.
  • In combination with disulfiram may develop neurological
    symptoms, so a break of 14 days should be observed between
    drug treatment.
  • Causes intolerance to ethanol, similar to disulfiram.
  • Joint treatment with cimetidine leads to inhibition
    metabolism of metronidazole, which leads to an increase in its
    serum concentration and, accordingly, increase the risk
    formation of side effects.
  • With simultaneous use with phenytoin and phenobarbital
    possible acceleration of elimination of metronidazole. This leads to
    lowering its concentration in the blood plasma.
  • In the appointment with lithium preparations may increase
    plasma lithium concentrations with signs of development
    intoxication.
  • Sulfonamides increase antimicrobial effect
    metronidazole.

Should not be taken simultaneously with non-depolarizing
muscle relaxants.

Analogs

Pills Klion 60-80 rubles.
Trichopol pills for internal use 80-90 rub.
Trichopol vaginal tablets 320-370 rubles
Flagil 120-130 rub.
Gel Metrogyl gel for external use 180-200 rubles
Metrogil vaginal gel 160-180 rubles
Rozamet cream 190-200 rub.
Solution для injections Metrogil 100 ml 28-30 rub.
Candles Flagil суппозитории 800-900 rub.

Автор: врач-гигиенист, эпидемиолог

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