Composition, form of production and packaging
The vaginal tablets are almost white in color, oval, biconvex, with a pointed end, with an engraving "100" on one side.
1 tab.
metronidazole 100 mg
miconazole nitrate 100 mg
Auxiliary substances: sodium lauryl sulfate - 0.5 mg, silicon colloidal dioxide 7 mg, magnesium stearate 13 mg, povidone 26 mg, sodium hydrogen carbonate 90 mg, tartaric acid 100 mg, sodium carboxymethyl starch (type A) 100 mg, crospovidone - 100 mg, hypromellose - 190 mg, lactose monohydrate - 473.5 mg.
10 pieces. - Strips aluminum (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
Combined preparation with antibacterial, antiprotozoal and antifungal action for intravaginal application.
Metronidazole , a derivative of nitro-5-imidazole. The mechanism of its action is the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The restored 5-nitro group of metronidazole interacts with the DNA of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of microorganisms.
It is active against Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia lamblia, and also with respect to obligate anaerobes Bacteroides spp.(including B. fragilis, B. ovatus, B. distasonis, B. thetaiotaomicron, B. vulgatus), Fusobacterium spp., Veillonella spp., Prevotella spp. (Prevotella bivia, Prevotella buccae, Prevotella disiens) and some Gram-positive microorganisms (Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). The MIC for these strains is 0.125-6.25 Ојg / ml.
Metronidazole is resistant to aerobic microorganisms and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against aerobes.
Miconazole has an antifungal effect against dermatophytes, yeast fungi. When intravaginal application is active mainly in relation to Candida albicans. Miconazole inhibits the biosynthesis of ergosterol in fungi and changes the composition of other lipid components in the membrane, which leads to the death of fungal cells.Miconazole does not change the composition of normal microflora and the pH of the vagina.
PHARMACOKINETICS
With intravaginal application, metronidazole is absorbed into the systemic circulation. The maximum concentration of metronidazole in the blood is determined after 6-12 hours and is approximately 50% of the maximum concentration that
is achieved (in 1-3 hours) after a single dose of metronidazole equivalent dose inside.
Systemic absorption of miconazole after intravaginal application is low.
Metronidazole penetrates into breast milk and most tissues, passes through the blood-brain barrier and the placenta.
Binding to plasma proteins is less than 20%.
Metabolized in the liver by hydroxylation, oxidation and glucuronation. The activity of the main metabolite (2-hydroxymethonidazole) is 30% of the activity of the parent compound.
It is excreted by the kidneys - 60-80% of the dose of the systemic action drug (20% of this quantity in unchanged form).
Metronidazole Metabolite, 2-oxymetronidazole, stains urine in a reddish-brown color, due to the presence of a water-soluble pigment formed as a result of metronidazole metabolism. The intestine is excreted - 6-15% of the dose of the systemic drug.
Rapidly destroyed in the liver.
Histohematetic barriers overcome badly. In 8 hours after application of the preparation, 90% of miconazole is still present in the vagina. Unchanged miconazole is not found in either plasma or urine.
INDICATIONS
- topical treatment of mixed etiologies of vaginitis caused simultaneously by Trichomonas spp. and Candida spp.
DOSING MODE
Intravaginal. 1 vaginal tablet (previously moistened with water) is injected deep into the vagina in the evening before going to bed for 10 days in combination with taking the drug metronidazole inside.
SIDE EFFECT
Local reactions: burning, itching, pain and irritation of the vaginal mucosa; thick, white, mucous discharge from the vagina without smell or with a faint smell; a burning sensation or irritation of the penis in the partner.
On the part of the digestive system: nausea, vomiting, taste changes, metallic taste in the mouth, decreased appetite, abdominal pain, spasmodic, constipation or diarrhea.
From the side of the central nervous system: headache, dizziness.
On the part of the hematopoiesis system: leukopenia or leukocytosis.
Allergic reactions: urticaria, itching of the skin, rash.
From the urinary system: staining the urine in the red-brown color due to the presence of a water-soluble pigment (metronidazole metabolite - 2 oxymetronidazole), formed as a result of metronidazole metabolism.
CONTRAINDICATIONS
- Lakopenia (including in the anamnesis);
- organic lesions of the central nervous system (including epilepsy);
- liver failure;
- Pregnancy (I trimester);
- the period of lactation (breastfeeding);
- children's age till 12 years;
- hypersensitivity to the components of the drug;
- hypersensitivity to other azoles.
With caution should prescribe the drug in diabetes mellitus, violations of microcirculation.
PREGNANCY AND LACTATION
Klion-D 100 is contraindicated for use in the first trimester of pregnancy. The use of the drug in the II and III trimesters is possible only in cases where the intended use for the mother exceeds the potential risk to the fetus.
Metronidazole is excreted in breast milk. During the period of breast-feeding, the use of Clion-D 100 is contraindicated. If it is necessary to use the drug during lactation, breastfeeding should be stopped.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in liver failure (with the appointment of the drug in high doses).
SPECIAL INSTRUCTIONS
During the use of the drug should not drink alcohol (the danger of development of disulfiram-like reactions).
During the period of drug use, it is recommended to abstain from sexual intercourse. Simultaneous treatment of sexual partners is recommended.
Metronidazole can immobilize treponema, which leads to a false positive TPI test (Nelson's test).
Control of laboratory indicators
With the use of Clion-D 100, minor leukopenia can be observed, so it is advisable to monitor the blood picture (the number of white blood cells) at the beginning and at the end of therapy.
Impact on the ability to drive vehicles and manage mechanisms
When there are side effects from the central nervous system, one should refrain from managing motor vehicles and working with potentially dangerous mechanisms.
OVERDOSE
Data on overdose with intravaginal application of metronidazole are not available. However, with simultaneous use with metronidazole inside, systemic effects can develop.
Symptoms of an overdose of metronidazole: nausea, vomiting, abdominal pain, diarrhea, generalized itching, metallic taste in the mouth, motor disorders (ataxia), dizziness, paresthesia, convulsions, peripheral neuropathy, leukopenia, darkening of urine.
Symptoms of an overdose of miconazole are not revealed.
Treatment: with the occasional ingestion of a large number of vaginal Clion-D 100 tablets, if necessary, gastric lavage, the introduction of activated carbon, and hemodialysis may be performed. Metronidazole does not have a specific antidote. Metronidazole and its metabolites are well eliminated in hemodialysis. When any symptoms of an overdose occur, symptomatic and supportive therapy is recommended.
DRUG INTERACTION
Since systemic absorption of miconazole is low, interaction with other drugs is caused by metronidazole.
Metronidazole is compatible with sulfonamides and antibiotics.
With the simultaneous use of alcohol causes reactions like disulfiram (cramping pain in the abdomen, nausea, vomiting, headache, skin hyperemia). It is inadmissible to use together with disulfiram (additive effect, can cause confusion).
The drug is able to enhance the effect of indirect anticoagulants. Prothrombin time can increase, so correction of the dose of indirect anticoagulants is necessary.
It is not recommended to combine the drug with nondepolarizing muscle relaxants (vecuronium bromide).
Inducers of microsomal oxidation enzymes in the liver (eg, phenytoin, phenobarbital) can accelerate the elimination of metronidazole, which leads to a decrease in its concentration in the blood plasma.
Cimetidine inhibits metronidazole metabolism, which can lead to an increase in its serum concentration and an increased risk of side effects.
It is possible to increase the concentration of lithium in blood plasma during the course of treatment with metronidazole, therefore before starting the application of Clion-D 100, it is necessary to reduce the dose of lithium or stop taking it during treatment.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, protected from light at a temperature of no higher than 30 В° C. Shelf life - 5 years.
