Pharmacodynamics and pharmacokinetics
The effect of the drug is due to the complex effect on the vaginal microflora of its constituent components.
Miconazole is an antifungal agent that destroys dermatophytes and yeasts , but does not disturb the pH or destroy healthy microflora in the vagina. The substance directly affects the synthesis of lipid components in the fungal membrane, thereby destroying it. It does not penetrate into the blood and is not found in the kidneys and products of the excretory organs; 90% remains in the vagina. The maximum concentration is after 8 hours.
Metronidazole is an antibiotic . It inhibits the process of RNA and DNA of destructive bacteria by restoring the 5-nitro group by transport proteins inside the cell. After entering the vagina, it penetrates into the blood. Its maximum concentration in the blood (half of the administered dose) can be detected after 9 hours.
Vaginal tablets Klion-D 100 (Klion-D 100)
Instructions for medical use of the drug
Description of pharmacological action
The mechanism of action of metronidazole is the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group interacts with the DNA of the cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of microorganisms. Metronidazole is a broad-spectrum antimicrobial and antiprotozoal agent. Active against Trichomonas vaginalis, Giardia intestinalis, Entamoeba histolytica, Lamblia intestinalis as well as against obligate anaerobes (spore-forming and non-spore-forming) - Bacteroides spp. (Bacteroides fragilis, Bacteroides ovatus, Bacteroides distasonis, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Clostridium spp., Peptostreptococcus spp., sensitive strains of Eubacterium. Aerobic microorganisms and facultative anaerobes are not sensitive to metronidazole. Miconazole has antifungal activity against common dermatophytes, yeasts and various other fungi and antibacterial activity against certain gram-positive bacteria. 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. Quickly relieves itching that often accompanies infections caused by yeast and dermatophytes. Does not change the composition of the microflora and pH of the vagina.
Indications for use
Trichomonas, candidal and nonspecific vaginitis (local treatment).
Release form
vaginal tablets; contour packaging without cells 10, cardboard pack 1; vaginal tablets 100 mg + 100 mg; strip 10, cardboard pack 1; vaginal tablets 100 mg + 100 mg; strip 10, box 100; Composition Vaginal tablets 1 table. metronidazole 100 mg miconazole nitrate 100 mg excipients: sodium lauryl sulfate; colloidal silicon dioxide; magnesium stearate; povidone; sodium bicarbonate; tartaric acid; sodium carboxymethyl starch (type A); crospovidone; hypromelose; lactose monohydrate in contour-free packaging 10 pcs.; in a cardboard pack 1 package.
Pharmacodynamics
The mechanism of action of metronidazole is the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group interacts with the DNA of the cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of microorganisms. Metronidazole is a broad-spectrum antimicrobial and antiprotozoal agent. Active against Trichomonas vaginalis, Giardia intestinalis, Entamoeba histolytica, Lamblia intestinalis as well as against obligate anaerobes (spore-forming and non-spore-forming) - Bacteroides spp. (Bacteroides fragilis, Bacteroides ovatus, Bacteroides distasonis, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Clostridium spp., Peptostreptococcus spp., sensitive strains of Eubacterium. Aerobic microorganisms and facultative anaerobes are not sensitive to metronidazole. Miconazole has antifungal activity against common dermatophytes, yeasts and various other fungi and antibacterial activity against certain gram-positive bacteria. 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. Quickly relieves itching that often accompanies infections caused by yeast and dermatophytes. Does not change the composition of the microflora and pH of the vagina.
Pharmacokinetics
Metronidazole. When administered intravaginally, it is absorbed into the systemic circulation. Cmax in the blood is determined after 6–12 hours and is approximately 50% of the Cmax that is achieved (after 1–3 hours) after a single dose of metronidazole orally. Miconazole. Systemic absorption of miconazole nitrate after intravaginal use is limited. 8 hours after application of the drug, 90% of miconazole is still present in the vagina. Unchanged miconazole is not detectable in either plasma or urine.
Use during pregnancy
Contraindicated during pregnancy. Breastfeeding should be stopped during treatment.
Contraindications for use
- hypersensitivity to the components of the drug (including other nitroimidazole derivatives); - blood diseases, leukopenia (including history); — impaired coordination of movements, organic lesions of the central nervous system (including epilepsy); - liver failure (in case of prescribing large doses); - pregnancy; - period of breastfeeding. With caution: - diabetes mellitus; - microcirculation disturbance.
Side effects
Local: itching, burning, pain and irritation in the vagina; thick, white, mucous vaginal discharge without odor or with a faint odor, frequent urination; a burning sensation or irritation of the penis in a sexual partner. From the gastrointestinal tract: nausea, changes in taste, “metallic” taste and dry mouth, loss of appetite, cramping pain in the abdominal cavity; vomiting, constipation or diarrhea. Allergic reactions: urticaria, itching of the skin, rash. From the nervous system: headache, dizziness. Other: leukopenia or leukocytosis. In rare cases, urine is colored red-brown (due to the presence of a water-soluble pigment formed as a result of the metabolism of metronidazole).
Directions for use and doses
Intravaginally (deeply), after moistening the tablet with water. Trichomonas vaginitis - 1 table. per day for 10 days in combination with oral metronidazole. Nonspecific vaginitis or candidal vaginitis - 1 table. 2 times a day for 10 days, if necessary in combination with oral metronidazole. Treatment with metronidazole should not last more than 10 days and be repeated more than 2-3 times a year.
Interactions with other drugs
Like disulfiram, it causes ethanol intolerance. Concomitant use with disulfiram can lead to the development of various mental disorders and depression of consciousness. Strengthens the effect of indirect anticoagulants (warfarin, etc.), which leads to an increase in the time of prothrombin formation. It is not recommended to combine with non-depolarizing muscle relaxants (vecuronium bromide). Co-administration with barbiturates may accelerate the elimination of metronidazole, resulting in a decrease in its effect. Cimetidine inhibits the metabolism of metronidazole, which may lead to an increase in its concentration in the blood serum and an increased risk of side effects. When taken simultaneously with lithium preparations, the concentration of the latter in plasma may increase.
Special instructions for use
Simultaneous treatment of the sexual partner is recommended, regardless of whether he has manifestations of the disease. During the treatment period you should abstain from sexual intercourse. If there are indications in the anamnesis of changes in the composition of peripheral blood, as well as when using the drug in high doses and/or with its long-term use, monitoring of a general blood test is necessary. Metronidazole can immobilize treponemes, leading to a false-positive Nelson test. Use with caution while working for drivers of vehicles and people whose profession is associated with increased concentration of attention (dizziness associated with taking the drug may occur).
Storage conditions
List B.: In a dry place, protected from light, at a temperature of 15–30 °C.
Best before date
60 months
ATX classification:
G Genitourinary system and sex hormones
G01 Antiseptics and antimicrobials for the treatment of gynecological diseases
G01A Antiseptics and antimicrobials for the treatment of gynecological diseases (excluding combinations with corticosteroids)
G01AF Imidazole derivatives
G01AF20 Combinations of imidazole derivatives
Interaction
The medicine is not combined with ethanol, disulfiram , non-depolarizing muscle relaxants, cimetidine, and lithium preparations .
When taking indirect anticoagulants , it is worth additionally monitoring the prothrombin index .
The effectiveness of metronidazole is reduced when combined with phenobarbital and phenytoin .
Analogs
Level 4 ATX code matches:
Gainomax
Sertaconazole
Ornisis
Metrogil Plus
Livarol
Flagyl
Ginofort
Zalain
Ketoconazole
Candide B6
Candide
Gyno-Travogen Ovulum
Kanizon
Metromicon-Neo
Lomexin
Neo-Penotran
Gyno-Pevaril
Ginesol
Antifungol
Analogs of suppositories are: Metromicon-Neo, Ginalgin, Clomezol, Neo-Penotran Forte, Clevazol, Pulsitex, Candibene, Ketodin, Candide, Ketonazole, Livarol, Metronidazole, Clotrimazole, Trichopolum, Econazole.
What is the difference between Klion and Klion-D 100?
Klion tablets contain metronidazole and have a wider range of applications. Usually, to combat trichomoniasis, oral intake of tablets alone is not enough, for which Klion-D 100 suppositories are prescribed.
Reviews about Klion-D 100
Reviews on forums: Overall good. Many people used Klion-D 100 for thrush and were satisfied with the result. Some women complain of severe side effects. The drug is quite effective not only against thrush, but also against other types of vaginitis .
Reviews during pregnancy: Despite the fact that the use of the product during pregnancy is not recommended, women are often prescribed suppositories. Reviews of Klion-D 100 suppositories were divided; some women tolerated the medication well and it did not affect their children in any way. Many experienced severe burning, itching, abdominal pain and voluntarily stopped taking the drug.
Klion
Orally and parenterally.
Orally, during or after meals (or with milk), without chewing.
For trichomoniasis - 250 mg 2 times a day for 10 days or 400 mg 2 times a day for 5-8 days. Women must additionally be prescribed vaginal suppositories or vaginal tablets with metronidazole. If necessary, you can repeat the course of treatment with Klion or increase the dose to 0.75-1 g/day. Between courses you should take a break of 3-4 weeks with repeated control laboratory tests. An alternative treatment regimen is to prescribe 2 g once to the patient and his sexual partner.
Children 2-5 years old - 250 mg/day; 5-10 years - 250-375 mg/day, over 10 years - 500 mg/day. The daily dose should be divided into 2 doses. The course of treatment is 10 days.
For giardiasis - 500 mg 2 times a day for 5-7 days.
Children under 1 year old - 125 mg/day, 2-4 years old - 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.
For giardiasis - 15 mg/kg/day in 3 divided doses for 5 days.
Adults: for asymptomatic amebiasis (if a cyst is detected), the daily dose is 1-1.5 g (500 mg 2-3 times a day) for 5-7 days.
For chronic amebiasis, the daily dose is 1.5 g in 3 divided doses for 5-10 days, for acute amoebic dysentery - 2.25 g in 3 divided doses until the symptoms stop.
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 adult dose, 3-7 years old - 1/3 adult dose, 7-10 years old - 1/2 adult dose.
For balantidiasis - 750 mg 3 times a day for 5-6 days.
For ulcerative stomatitis, adults are prescribed 500 mg 2 times a day for 3-5 days; In this case, the drug is not indicated for children.
For pseudomembranous colitis - 500 mg 3-4 times a day.
For eradication of Helicobacter pylori - 500 mg 3 times a day for 7 days (as part of combination therapy, for example in combination with amoxicillin 2.25 g/day).
When treating 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 (not more than) months.
To prevent infectious complications - 750-1500 mg/day in 3 doses 3-4 days before surgery or 1 g once on the first day after surgery. 1-2 days after surgery (when oral administration is already allowed) - 750 mg/day for 7 days.
In case of severe renal dysfunction (creatinine clearance less than 10 ml/min), the daily dose should be reduced by 2 times.
Suspension for oral administration. Anaerobic bacterial infections: children - 7 mg/kg every 8 hours, course of treatment - 7-10 days; Giardiasis: children 2-5 years old - 200 mg/day, 5-10 years old - 300 mg/day, 10-15 years old - 400 mg/day. The duration of treatment for giardiasis is 5 days. The course of treatment can be repeated after 10-15 days
Parenterally. For adults and children over 12 years of age, an initial dose of 0.5-1 g IV drip (infusion duration is 30-40 minutes), and then every 8 hours, 500 mg at a rate of 5 ml/min. If well tolerated, after the first 2-3 infusions they switch to jet administration. The course of treatment is 7 days. If necessary, intravenous administration is continued for a longer time. The maximum daily dose is 4 g. According to indications, switch to maintenance oral administration at a dose of 400 mg 3 times a day. Children under 12 years of age are prescribed according to the same regimen in a single dose of 7.5 mg/kg.
For purulent-septic diseases, 1 course of treatment is usually carried out.
For preventive purposes, adults and children over 12 years of age are prescribed 0.5-1 g intravenously on the eve of surgery, on the day of surgery and the next day - 1.5 g / day (500 mg every 8 hours). After 1-2 days, they switch to maintenance therapy orally. For patients with chronic renal failure and creatinine clearance less than 30 ml/min and/or liver failure, the maximum daily dose is no more than 1 g, the frequency of administration is 2 times a day.
As a radiosensitizing drug, it is administered intravenously at a rate of 160 mg/kg or 4-6 g/sq.m of body surface 0.5-1 hour before the start of irradiation. Apply before each irradiation session for 1-2 weeks. During the remaining period of radiation treatment, therapy with Klion is not carried out. The maximum single dose should not exceed 10 g, course dose - 60 g. To relieve intoxication caused by radiation, drip administration of a 5% dextrose solution, Hemodez or 0.9% NaCl solution is used.
For cervical and uterine cancer, skin cancer, they are used in the form of local applications (3 g dissolved in a 10% DMSO solution), moisten tampons, which are used topically, 1.5-2 hours before irradiation). In case of poor tumor regression, applications are carried out throughout the entire course of radiation therapy. If there is a positive dynamics of tumor clearance from necrosis - during the first 2 weeks of treatment.
Price Klion-D 100 (where to buy)
On average, the price of Klion-D 100 suppositories in Ukraine is 100 UAH for 10 vaginal tablets.
How much does it cost to buy medicine in Kyiv? About 120 UAH for 10 pieces.
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
Pharmacy24
- Klion-D 100 N10 tablets VAT "Gedeon Richter", Ugorshchina
201 UAH. order
PaniPharmacy
- Klion-D 100 tablets Klion D tab. vag. No. 10 Hungary, Gedeon Richter
212 UAH order
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Instructions for use KLION tablets
- 1. Basic therapy:
- 500 mg/day (1 tablet in the morning and evening) for 10 days (for women, simultaneous use of vaginal tablets Klion-D 100 is necessary, 1 tablet at night (the tablets are inserted deep into the vagina, pre-moistened with water). To prevent reinfection it is necessary to treat the sexual partner with the same dose of Klion. If necessary, treatment can be repeated. Between courses it is recommended to observe a 3-4 week break with repeated laboratory tests.
- single dose of 2 g (8 tablets) in the evening, before bedtime. The patient and sexual partner are treated simultaneously.
2. Pulse therapy:
For gardnerellosis
the drug is prescribed 500 mg 2 times a day (2 tablets 2 times a day) daily for 7 days, or a single dose of 2 g (8 tablets). If necessary, this dose can be repeated after a one-day break.
When treating giardiasis,
adults and children over 12 years of age
are prescribed 250 mg 3 times a day (1 tablet 3 times a day) for 5 days.
Children aged 8 years
- 500 mg/day in 2 doses (1 tablet 2 times/day),
aged 5 to 8 years
- 375 mg/day (1.5 tablets/day),
aged 2 to 4 years
- 250 mg/day (1 tablet/day),
for children under 1 year of age,
a dose of 125 mg/day (1/2 tablet/day) is prescribed. The duration of treatment is 5 days. The drug is taken after meals.
For amebiasis and acute amoebic dysentery,
adults
are prescribed a dose of 500-750 mg/day,
children under 12 years of age
- 50 mg/kg/day. Frequency of administration: 3 times/day. The duration of treatment is 5-10 days.
For amoebic liver abscess,
adults
are prescribed a dose of 500-750 mg/day, frequency of use - 3 times/day, duration of treatment - 5-10 days;
children aged 7 to 10 years
should be prescribed 1/2 the dose for adults,
from 3 to 7 years old
- 1/3 dose for adults,
from 1 to 3 years old
- 1/4 dose for adults,
children aged up to 1 year
- less than 1/4 of the dose for adults, which should be reduced according to age.
For ulcerative stomatitis
in adults
- 500 mg/day in 2 divided doses (1 tablet 2 times/day) for 3-5 days. In severe cases, Klion can be used on the ulcer as a compress for 20 minutes.
For children
The drug is not indicated for the treatment of ulcerative stomatitis.
To prevent postoperative complications,
adults
are prescribed 500 mg every 8 hours 24 hours before surgery, or prescribed at an initial dose of 1 g 1 time.
After surgery - 500 mg 3 times a day for 7 days. For children under 12 years of age,
the drug is prescribed at a dose of 3.5-7.5 mg/kg according to the same regimen.
When treating infections caused by anaerobic microorganisms,
for
adults and children over 12 years of age,
the dose of Klion is set individually, depending on the patient’s age, location and severity of the disease. The average dose (for a body weight of about 70 kg) is 500 mg 3 times a day. If necessary, the initial dose can be increased to 15 mg/kg (about 1 g per 70 kg of body weight). In especially severe cases, the dose can be increased, but the total dose should not exceed 4 g/day.
For children under 12 years of age
the average dose is 7.5 mg/kg.
Renal dysfunction
does not have a significant effect on the pharmacokinetic parameters of the drug; no change in dosage regimen is required.
However, during hemodialysis, additional use of the drug (orally or intravenously as an infusion) may be required due to a decrease in T1/2 of metronidazole. In patients not on hemodialysis, with CC less than 10 ml/min,
metronidazole metabolites may accumulate. In this case, hemodialysis is recommended; peritoneal dialysis is ineffective.
Metronidazole and its metabolites are well excreted by hemodialysis
. Because during hemodialysis, T1/2 of metronidazole decreases significantly (up to approximately 3 hours); in some cases, additional use of the drug (orally or intravenously as an infusion) may be required.
For severe liver diseases
the metabolism of metronidazole slows down, so the active substance and its metabolites can accumulate in the blood plasma. In these cases, adjustment of the dosage regimen is required depending on the severity of liver damage.
In elderly patients
The pharmacokinetics of metronidazole may change, so treatment is recommended to be carried out under the control of metronidazole levels in the blood plasma.