Clotrimazole is a broad-spectrum antimycotic or antifungal agent. The antimycotic properties of clotrimazole were discovered in the late 1960s. The drug belongs to the category of imidazole azole antifungals. It is available in a variety of dosage forms, including creams, ointments, tablets, and slow-dissolving capsules.
Clotrimazole may be used to treat anemia
In addition to its antifungal activity, clotrimazole has become a drug of interest for the treatment of a number of other diseases, such as sickle cell disease, malaria and some types of cancer. This drug's minimal side effects and uncomplicated metabolic profile have led to its widespread use for the treatment of fungal outbreaks, such as vaginal infections caused by yeast spores (candida vulvitis or thrush), as well as athlete's foot.
Use of the drug
Clotrimazole cream is prescribed for the topical treatment of the following skin infections:
- Tinea pedis, tinea cruris and tinea corporis caused by Trichophyton rubrum, Trichophyton mentagrophytes, Floccosum Epidermophyton;
- Candidiasis caused by Candida albicans;
- Herpes zoster caused by Malassezia furfur;
- Diaper rash infected with Candida Albicans;
In some drugs, clotrimazole can be combined with betamethasone dipropionate and corticosteroids.
The oral formulation is indicated as a prophylactic drug to reduce the incidence of oral and pharyngeal candidiasis in immunocompromised patients receiving chemotherapy, radiation therapy, or steroid therapy used to treat leukemia, cancer, or kidney transplantation. The drug is not indicated for the treatment of any systemic mycoses.
Pharmacological properties of the drug Clotrimazole
Clotrimazole belongs to the group of imidazole antifungal drugs. The antimycotic effect is due to a disruption in the composition of the fungal cell membrane, a change in its permeability and subsequent cell lysis. Has a wide spectrum of action. Effective against dermatophytes and yeast fungi. In addition, it has an antimicrobial effect against gram-positive (staphylococci and streptococci) and gram-negative bacteria ( Bacteroides spp. , Gardnerella vaginalis ), as well as against Trichomonas vaginalis , Malassezia furfur , Corynebacterium minutissimum. Dosage forms of clotrimazole do not have a resorptive effect. When administered intravaginally, approximately 5–10% of clotrimazole is absorbed. The fungicidal concentration in the vagina remains for 3 days after application. The absorbed substance is metabolized in the liver and excreted in the bile.
pharmachologic effect
Clotrimazole is a broad-spectrum antifungal agent that inhibits the growth of pathogenic yeasts by altering the permeability of cell membranes. The action of clotrimazole is fungistatic at concentrations of the drug up to 20 μg/ml and can be fungicidal in vitro against Candida albicans and other species of the genus Candida at higher concentrations. Unfortunately, resistance to clotrimazole, which was rare in the past, is now common among various patient groups.
The drug Clotrimazole fights fungus well
Clotrimazole is generally considered a fungistatic rather than a fungicidal drug, although this difference is not absolute as clotrimazole exhibits fungicidal properties at higher concentrations.
The action of the drug is based primarily on damage to the permeability barrier in the cell membrane of fungi. Clotrimazole inhibits the biosynthesis of ergosterol, an essential component of fungal cell membranes. If ergosterol synthesis is either completely or partially inhibited, the cell is no longer able to create an intact and functional cell membrane. Since ergosterol directly stimulates the growth of fungal cells in a hormone-like manner, the rapid onset of the above processes results in dose-dependent inhibition of fungal growth.
Although there is a decrease in ergosterol, due to the inhibition of lanosterol 14-demethylase (also known as CYP51), which is believed to be responsible for the antifungal properties of clotrimazole, this drug also exhibits other pharmacological effects. These include inhibition of sarcoplasmic reticulum Ca2+ -ATPase, intracellular calcium depletion, and blockade of calcium-gated potassium channels and voltage-gated calcium channels. The action of clotrimazole on these complexes explains other effects of this drug that differ from its antifungal activity.
Clotrimazole-Akrikhin vaginal tablets 100 mg 6 pcs
Registration Certificate Holder
Chemical and pharmaceutical plant AKRIKHIN (Russia)
Dosage form
Medicine - Clotrimazole-Akrikhin
Description
Vaginal tablets
white or almost white, oval, biconvex.
1 tab.
clotrimazole 100 mg
Excipients
: lactose (milk sugar), potato starch, microcrystalline cellulose, citric acid, magnesium stearate.
6 pcs. — cellular contour packages (1) — cardboard packs.
Indications
Genital infections caused by yeast-like fungi of the genus Candida (vulvovaginal candidiasis); sanitation of the birth canal before childbirth.
Contraindications for use
Hypersensitivity to clotrimazole; I trimester of pregnancy, menstruation period.
pharmachologic effect
Broad-spectrum antifungal agent for vaginal use. The action of clotrimazole is associated with a disruption in the synthesis of ergosterol, which is part of the cell membrane of fungi, which changes the permeability of the cytoplasmic membrane and causes subsequent cell lysis. In small concentrations it has a fungistatic effect, in large concentrations it has a fungicidal effect, and not only on proliferating cells. At fungicidal concentrations, it interacts with mitochondrial and peroxidase enzymes, resulting in an increase in the concentration of hydrogen peroxide to a toxic level, which also contributes to the destruction of fungal cells.
Clotrimazole exhibits fungicidal and fungistatic activity against dermatomycetes (Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis), yeast-like and mold fungi (Candida spp., including Candida albicans; Torulopsis glabrata, genus Rhodotorula, Pityrosporum orbiculare). Active against the causative agent of pityriasis versicolor - Pityrosporum orbiculare (Malassezia furfur). Effective against gram-positive bacteria - the causative agent of erythrasma Corynebacterium minutissimum, as well as Staphylococcus spp., Streptococcus spp., gram-negative bacteria - Bacteroides, Gardnerella vaginalis. In high concentrations it is active against Trichomonas vaginalis.
Has no effect on lactobacilli. Primary resistant variants of sensitive fungi are very rare; the development of secondary resistance in sensitive fungi is also observed in exceptional cases under therapeutic conditions.
Drug interactions
When used simultaneously with amphotericin B and nystatin, the activity of clotrimazole is reduced.
The simultaneous use of intravaginal clotrimazole and tacrolimus, sirolimus orally can lead to an increase in the concentration of the latter in the blood plasma, therefore patients should be monitored for the development of symptoms of overdose, if necessary, measuring plasma concentrations.
Dosage regimen
The dose, method and regimen of use are determined individually, depending on the indications, the age of the patient and the dosage form used.
When applied topically, the recommended duration of therapy is 6 days.
The compliance of the indications and the dosage form used should be strictly observed.
Side effect
From the immune system:
allergic reactions, incl. urticaria, shortness of breath, arterial hypotension, fainting.
From the digestive system:
frequency unknown - abdominal pain.
From the urinary system:
frequency unknown - frequent urination, intercurrent cystitis.
From the reproductive system:
frequency unknown - itching, burning, hyperemia and swelling of the vaginal mucosa, ulceration of the vaginal mucosa, rash, pain in the pelvic area, burning sensation in the penis of the sexual partner, pain during sexual intercourse.
Other:
frequency unknown - headache.
special instructions
If allergic reactions or irritation occur at the site of application, treatment is stopped.
To prevent reinfection, hygiene rules should be observed.
It is not recommended to apply clotrimazole to the skin in the eye area.
If clinical signs of infection persist after completion of treatment, repeat microbiological testing should be performed to confirm the diagnosis.
To prevent infection/reinfection with genital infections, simultaneous treatment of sexual partners is necessary. During the treatment period it is recommended to abstain from sexual intercourse.
When using dosage forms intended for local intravaginal use, it is recommended to use reliable contraception. The risk of condom or diaphragm rupture increases when used concomitantly with clotrimazole.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - With caution. Restrictions when breastfeeding - Contraindicated.
Use is contraindicated in the first trimester of pregnancy. Use in the II-III trimesters of pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.
If it is necessary to use it during lactation, the issue of stopping breastfeeding should be decided.
Use for liver dysfunction
Restrictions for liver dysfunction - With caution.
In patients with liver failure, the functional state of the liver should be periodically monitored.
Use in children
Restrictions for children - With caution. Can be used in children according to indications, in doses and dosage forms recommended according to age. It is necessary to strictly follow the instructions in the instructions for clotrimazole preparations for the use of specific dosage forms of clotrimazole in children of different ages and for contraindications for specific age groups in this category of patients.
Overdose
Symptoms of overdose include erythema, tingling, blistering, peeling, swelling, itching, urticaria, burning and general skin irritation, and cramps. As with all topical medications, skin sensitization may occur.
Clotrimazole does not pose a risk of acute toxicity as it is unlikely to occur after a single vaginal or cutaneous application. Overdose when applied is possible over a large area under conditions favorable for absorption, or accidental oral administration. There is no specific antidote.
Peculiarities
Clotrimazole should not be used during the first trimester of pregnancy unless the doctor considers its use necessary for the patient's health. The drug should not be used during menstrual periods in the treatment of candidiasis vulvitis (thrush). If breastfeeding, clotrimazole can be used only as prescribed by your doctor.
The drug weakens the effect of nystatin, natamycin, amphotericin B when used simultaneously. The cream is not used to treat nails or fungal diseases of the head.
For external use, Clotrimazole cream is rubbed into the affected areas of the skin. Do not apply the product to the area around the eyes.
Clotrimazole is not prescribed to infants and premature infants
To treat candidiasis vulvitis, the capsule is inserted into the vulva, and the perineal area and mucous tissues are treated with cream. During treatment of candidal vulvitis, unprotected sex should be avoided so as not to infect the partner. If infection does occur, treatment should also be carried out by the partner. When carrying out therapy with the drug, tampons, spermicides and other vaginal products should not be used.
Clotrimazole
Read the instructions for use carefully before you start using the drug. Save the instructions, you may need them again. If you have any questions, consult your doctor. The medicine you are using is intended for you personally and should not be given to others as it may cause harm even if you have the same symptoms as you.
If allergic reactions or irritation occur at the injection site, treatment should be discontinued.
The drug should not be used during menstruation; it is advisable to start treatment after menstruation.
In case of simultaneous infection of the labia and adjacent areas (candidal vulvitis), additional local treatment with the drug clotrimazole in the dosage form of a cream, ointment, or gel should be carried out.
During pregnancy, treatment with vaginal tablets is carried out without an applicator.
To prevent infection, simultaneous treatment of sexual partners is necessary. During the treatment period it is necessary to abstain from sexual intercourse. To prevent reinfection, hygiene rules should be observed.
If clinical signs of infection persist after completion of treatment, a repeat microbiological examination should be performed to clarify the diagnosis.
It is not recommended to use the drug if the following phenomena are observed:
- Irregular bleeding from the genital tract, ulceration of the mucous membrane of the vulva and/or vagina, pain, irritation, swelling, rash, burning, itching, discomfort in the vagina;
- Vaginal discharge with an unpleasant odor;
- Fever (temperature 38° or higher) or chills;
- Nausea, vomiting, diarrhea;
- Lower abdominal pain;
- Backache.
Before vaginal tablets are completely dissolved, normal humidity of the vaginal mucosa is required, otherwise undissolved parts of the tablet may crumble and come out. With vaginal dryness, women may notice the passage of undissolved pieces of pills. To prevent this, you should insert the tablet as deep into the vagina as possible before going to bed.
You should not use tampons, douche, use spermicides or other drugs for intravaginal use during treatment with this drug.
During treatment, it is recommended to use contraception. The risk of condom or diaphragm rupture increases when used simultaneously with the drug. It is necessary to use reliable methods of contraception.
Application and dosage
Clotrimazole in cream form is available in 20 gram tubes. 1 gram of the drug contains 20 mg of active substance.
The drug is rubbed into the affected areas of the skin in a thin layer 2-3 times a day.
The duration of the course of therapy is:
- dermatomycosis - 3-4 weeks;
- erythrasma - 2-4 weeks;
- lichen versicolor - 1-3 weeks;
- candidal vulvitis and candidal balanitis - 1-2 weeks.
To consolidate the positive results of treatment and prevent re-development of the disease, the course can be continued for 2 weeks after the symptoms of the disease disappear.
If the patient's condition does not improve after 4 weeks of using the drug, you should consult a doctor.
If you have hypersensitivity to the drug, allergic reactions, headaches, or other side effects, you should consult a doctor. When prescribing a course of treatment, the patient must report a history of sexually transmitted diseases, allergic reactions, if the patient’s temperature is above 38C.
