Metronidazole, gel 1% 30 g

Metronidazole is a nitroimidazole derivative. It has antimicrobial and antiprotozoal activity against Gram-negative aerobic and anaerobic microorganisms and protozoa. Metronidazole is especially effective against papulopustular inflammatory elements of rosacea when applied topically. The mechanism of action seems to include an anti-inflammatory effect as well.

Pharmacokinetics

The maximum plasma concentration of metronidazole when 1 g of gel is applied externally to the facial skin averages 32.9 ng/ml (range 14.8-54.4 ng/ml) and is reached after 6-24 hours. Maximum plasma concentration of metronidazole in external use does not exceed 0.5% of the average maximum plasma concentration of metronidazole after oral use of 250 mg of metronidazole in tablet form. When administered externally, the concentration of metronidazole in the gel application site is significantly higher than in blood plasma. Binding to plasma proteins is insignificant. The lowest concentration of metronidazole is determined in adipose tissue. It is excreted by the kidneys unchanged and as metabolites.

Indications

Rosacea treatment.

Active ingredient

Metronidazole

Composition

Active ingredient: metronidazole – 1.0 g.

Auxiliary substances: propylene glycol – 5,0 g, carbomer – 1,0 g, sodium hydroxide – 0,127 g, edetate disodium – 0,05 g, propylparahydroxybenzoate – 0,04 g, methylparahydroxybenzoate – 0,032 g, purified water – up to 100,0 g.

How to take, the dosage

For external use only.

Adults. The gel is applied thinly to previously cleansed affected areas of the skin twice a day, morning and evening, avoiding contact with the eyes, lips and nasal mucous membranes. Before applying the gel the affected area of the skin should be washed with warm water or mild detergent, which does not cause skin irritation. After applying the gel it is possible to use cosmetics which do not have comedogenic and astringent properties.

The average duration of treatment is 3-4 months. However, if there are clear signs of effectiveness of therapy, the attending physician may consider continuing treatment for an additional 3-4 months, depending on the severity of the patient’s condition. If there is no obvious clinical improvement, treatment should be discontinued.

In elderly patients, there is no need to adjust the dose.

Metronidazole Gel is not recommended for use in children under 18 years of age due to the lack of data on the safety and effectiveness of metronidazole in patients in this age group.

If there is no improvement or if new symptoms develop after treatment, you should talk to your doctor. Use only according to the route of administration and in the dose indicated in the instructions for use.

Interaction

In the application of the gel no cases of interaction with other medicinal products have been registered. Interaction with systemic drugs is unlikely due to the low absorption of metronidazole when used topically.

The warning about caution when using metronidazole concomitantly with warfarin or other indirect anticoagulants due to possible prolongation of the prothrombin time only applies to metronidazole when taken orally.

If you are using the above medications, or any other medications (including over-the-counter medications), please consult your physician before using Metronidazole Gel.

Special Instructions

Avoid getting the gel in the eyes and on the mucous membranes. If accidental contact occurs, rinse thoroughly with warm water.

If signs of skin irritation occur as a result of using the product, reduce the frequency of application, temporarily suspend or discontinue use, and consult a physician.

Exposure to ultraviolet (UV) radiation (direct sunlight, tanning beds, sunlamps) should be avoided during treatment. Metronidazole is converted to an inactive metabolite when exposed to UV light, so its activity is significantly reduced.

Metronidazole is a nitroimidazole derivative and should be used with caution in patients with a history of blood disorders.

Avoid excessive and prolonged use of the drug.

The drug contains propylene glycol, which may cause skin irritation.

With methyl parahydroxybenzoate and propyl parahydroxybenzoate in the formula, there is a risk of allergic reactions.

Influence on driving and operating ability

The drug has no effect on driving and operating ability (based on the pharmacodynamic profile and clinical experience of use).

Synopsis

Transparent or nearly transparent, colorless or slightly yellowish gel.

Contraindications

Hypersensitivity to metronidazole and other components of the drug. Childhood under 18 years of age.

Side effects

Classification of adverse reactions to the body and systems by frequency of occurrence: Very common (≥ 1/10), common (≥ 1/100, < 1/10), infrequent (≥ 1/1000, < 1/100), rare (≥ 1/10000, < 1/1000), very rare (< 1/10000), including individual reports, frequency unknown (frequency cannot be estimated from available data).

Skin and subcutaneous tissue disorders

Often: dry skin, erythema, itching, skin discomfort (burning sensation of skin, sore skin/tingling), skin irritation, increased manifestation of rosacea.

Frequency unknown: contact dermatitis, skin flaking, facial swelling.

Nervous system disorders

Infrequent: hypoesthesia, paresthesia, dysgeusia (“metallic” taste in the mouth).

Gastrointestinal tract disorders

Infrequent: nausea.

If you experience or worsen the side effects listed in the instructions, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

To date, there have been no reports of overdose when using the drug externally. When using the drug in accordance with the instructions for use, overdose is unlikely.

Pregnancy use

Pregnancy. There are no data on clinical experience of external use of metronidazole in pregnant women. When administered orally, metronidazole penetrates the placental barrier and rapidly enters the fetal bloodstream. After oral administration of metronidazole to rats and mice no signs of fetal toxicity were observed.
However, because reproductive toxicity studies in animals do not always predict response in humans, and because oral administration of metronidazole to rodents has demonstrated its carcinogenic properties, Metronidazole Gel in pregnancy is used only if the anticipated benefit to the mother exceeds the potential risk to the fetus after consultation with a physician. If you are pregnant, or anticipate that you might be pregnant, or are planning a pregnancy, you should consult your physician.

Breastfeeding period. After oral administration, metronidazole penetrates into breast milk in concentrations similar to those found in plasma. Although plasma concentrations of metronidazole are significantly lower in breastfeeding women after external administration than after oral administration, the decision to stop breastfeeding or to discontinue use of the drug should be made based on an assessment of the importance of the drug to the mother and the risk to the baby after consultation with a physician.

Similarities

Flagil, Metrogil, Trichopol, Metronidazole, Rosamet, Metronidazole-Acos, Metronidazole Renewal