Rosamet, cream 1% 25 g

Pharmacodynamics:

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 Rosamet cream is applied externally to the face averages 32.9 ng/ml (range 14.8 – 54.4 ng/ml) and is reached after 6-24 hours. Maximum plasma concentration of metronidazole when administered externally does not exceed 0.5% of the average maximum plasma concentration of metronidazole after oral administration of 250 mg of metronidazole in tablet form.

In external use, the concentration of metronidazole at the site of application of the cream is significantly higher than in plasma. Binding to plasma proteins is insignificant. The lowest concentration of metronidazole is determined in adipose tissue. Excreted by the kidneys unchanged and as metabolites.

Indications

Treatment of inflamed papules, pustules, erythema with rosacea and vulgar acne (acne rozacea, acne vulgaris), balanoposthitis, vulvovaginitis.

Pharmacological effect

Pharmacodynamics:

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

Pharmacokinetics:

The maximum concentration of metronidazole in blood plasma with external use of 1 g of Rosamet cream on the facial skin averages 32.9 ng/ml (range 14.8 – 54.4 ng/ml) and is achieved after 6-24 hours. The maximum concentration of metronidazole in blood plasma when applied externally does not exceed 0.5% of the average maximum concentration of metronidazole in blood plasma after oral administration of 250 mg of metronidazole in tablet form.

When applied externally, the concentration of metronidazole at the site of application of the cream is significantly higher than in the blood plasma. Communication with plasma proteins is insignificant. The lowest concentration of metronidazole is determined in adipose tissue. It is excreted by the kidneys unchanged and in the form of metabolites.

Special instructions

If signs of skin irritation appear due to the use of Rosamet cream, you should reduce the frequency of its application, temporarily suspend or discontinue use of the drug and consult a doctor.
Avoid contact of the cream with the eyes and mucous membranes. In case of accidental contact, rinse thoroughly with warm water.

During treatment, exposure to ultraviolet (UV) radiation (direct sunlight, solarium, sun lamps) should be avoided. Under the influence of UV radiation, metronidazole becomes an inactive metabolite, so its activity is significantly reduced.

Avoid excessive and prolonged use of the drug.

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

This product contains propylene glycol, which may cause skin irritation.

Considering that the drug contains methyl parahydroxybenzoate and propyl parahydroxybenzoate, there is a risk of developing allergic reactions.

Impact on the ability to drive vehicles. Wed and fur.:
The drug does not affect the ability to drive vehicles and machines (based on the pharmacodynamic profile and clinical experience with use).

Active ingredient

Metronidazole

Composition

1 g of cream contains:

active ingredient: metronidazole 10.00 mg;

excipients: glycerol, liquid paraffin, Lanette SX emulsifier [cetostearyl alcohol, sodium lauryl sulfate, purified water], propylene glycol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, purified water.

Pregnancy

Pregnancy
There are no data on clinical experience with topical use of metronidazole in pregnant women. When taken orally, metronidazole penetrates the placental barrier and quickly enters the fetal bloodstream. No signs of fetal toxicity were observed following oral administration of metronidazole to rats or mice. However, because reproductive toxicity studies in animals are not always predictive of response in humans, and because metronidazole has been shown to be carcinogenic when administered orally to rodents, the drug should only be used during pregnancy if the expected benefit to the mother outweighs the potential risk to the fetus, after consultation with a physician. If you are pregnant, or think you might be pregnant, or are planning a pregnancy, you should consult your doctor.

Breastfeeding period

After oral administration, metronidazole passes into breast milk in concentrations similar to those found in blood plasma. Despite the fact that after topical use of metronidazole in breastfeeding women, its plasma concentration is significantly lower than after oral administration, the decision to stop breastfeeding or discontinue use of the drug should be made taking into account the importance of using the drug for the mother and the risk to the child after consultation with a doctor.

Contraindications

Hypersensitivity to metronidazole and other components of the drug.

Children under 18 years of age.

Side Effects

Classification of adverse reactions by organs and systems, indicating the frequency of their occurrence:

Very common (≥1/10)

Often (≥1/100 to <1/10)

Uncommon (≥1/1,000 to <1/100)

Rare (≥1/10,000 to <1/1,000)

Very rare (<1/10,000), including isolated reports

Frequency unknown (frequency cannot be estimated from available data).

Skin and subcutaneous tissue disorders

Common: dry skin, erythema, itching, skin discomfort (skin burning sensation, skin soreness/tingling), skin irritation, increased manifestations of rosacea.

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

Nervous system disorders

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

Gastrointestinal disorders

Uncommon: nausea.

If any of the side effects indicated in the instructions worsen, or any other side effects not listed in the instructions are noted, you should immediately inform your doctor.

Interaction

When using Rosamet cream, no cases of interaction with other drugs have been reported. Interaction with systemic drugs is unlikely due to the low absorption of metronidazole when applied topically.

However, a disulfiram-like reaction has been observed in a small number of patients when metronidazole and ethanol were administered orally at the same time.

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

If you are using the above or other medications (including over-the-counter medications), consult your doctor before using the drug.

Overdose

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

Storage conditions

At a temperature not exceeding 25 °C, out of the reach of children.

Shelf life

2 years. Do not use after expiration date.

Manufacturer

JADRAN-GALENSKI LABORATORY j.s., Croatia