Fluconazole was developed over 20 years ago, but it is still on the list of the safest and most effective medicines according to the World Health Organization.
Fluconazole is indicated for the prevention and treatment of fungal infections. It is a synthetic drug that disrupts pathogens. Most often it is prescribed as part of the drug therapy of candidiasis, however, it can be used to treat other fungal diseases. Used in pediatric and therapeutic practice. Treatment is carried out under the supervision of a physician.
Composition and form of release
Fluconazole is an active ingredient in various antifungal drugs. The dosage and composition of the auxiliary components depend on the dosage form.
The liquid form of the drug, in addition to the active ingredient, usually contains sorbitol, glycerol and other substances. The standard dosage of antifungal agent in ten milliliters of liquid is 50 milligrams. Variations in composition and purpose are possible.
The special capsule shell, which contains gelatin and titanium dioxide, improves the absorption of the active substance in the desired part of the gastrointestinal tract. Available dosage options are 50, 100, or 150 milligrams.
The tablet form does not differ in its purpose from capsules. The tablet shell protects the active substance and improves the absorption of the drug in the body. Available dosage options are 50, 100, or 150 milligrams.
This dosage form is suitable for intravenous (infusion) administration of the drug. Contains sodium chloride and other substances used to make injection solutions. The dosage depends on the manufacturer, but usually one bottle contains from 50 to 200 milligrams of the active ingredient.
Treatment with intravenous injection is usually carried out in a hospital setting, when oral administration is not effective or impossible.
According to the classification, the active substance is classified as antifungal drugs or antimycotics. The medicinal component is absorbed into the circulatory system through the walls of the gastrointestinal tract and is distributed in the body. The chemical compound penetrates the fungal cells and disrupts the vital activity of the pathogen, due to which the development of the infection stops. Compared to other antimycotics, the agent causes fewer side effects.
- The medicine fights against the causative agents of candidiasis, cryptococcosis, coccidioidomycosis, microsporia, trichophytosis, blastomycosis and histoplasmosis.
- The mechanism of antifungal activity is associated with the suppression of special enzymes required to perform the main functions of the pathogen. Pathogens cannot multiply and grow.
- The drug is highly selective. Unlike many other medicines, the active substance of the medicine does not suppress the action of a person’s own enzymes. Also, the drug does not affect hormonal levels.
- Fluconazole can be used to treat opportunistic diseases of a fungal nature that occur against a background of decreased immunity.
- The action of the drug helps to reduce the risk of developing a fungal infection during treatment with cytotoxic drugs, radiation therapy and immunosuppressants.
It is impossible to completely exclude side effects on the background of drug therapy. In some patients, unwanted reactions are formed due to the effect of the active substance on organs and tissues. A typical side effect is the sensitivity of the immune system to the chemical compounds that make up the drug. To reduce the risk of allergies, you must first study the composition of the product and clarify the anamnesis.
Other unwanted effects:
- Nervous system: cephalalgia, dizziness, fatigue, convulsive reactions.
Digestive system: lack of appetite, disruption of the liver tissue, urge to vomit, discomfort in the abdomen, bloating, increased gas production in the intestines, loose stools, inflammation and necrosis of the liver.
- Immune system: skin rashes, redness of integumentary tissues, Stevens-Johnson syndrome, other erythemal reactions, Lyell’s syndrome, Quincke’s edema, urticaria and other anaphylactoid manifestations.
- Hematopoietic system: a decrease in the level of neutrophils, granulocytes, platelets and leukocytes. Hemorrhage is possible.
- Cardiovascular system: prolongation of the QT interval, impaired contraction of the ventricles of the heart.
- Additionally: impaired renal function, baldness, potassium deficiency, increased cholesterol and triglyceride levels.
Indications for use
The medicine is used to treat fungal infections of the genitourinary system, membranes of the brain, mucous membranes of the gastrointestinal tract and other parts of the body. The specific prescription list depends on the dosage form. The most versatile are oral forms (tablets, capsules and syrup). Infusion is usually used to treat severe infections with other medications.
Cryptococcosis of various organs, including fungal infection of the membranes of the brain, lung tissue and skin. The tool is used in patients with normal immune status and in people suffering from immunodeficiency (against the background of HIV infection, organ transplantation and other conditions). Can be used for prophylactic purposes in patients with reduced immunity.
Candidiasis of the genitourinary system, including fungal invasion of the vaginal mucosa, penis, cervix, and urinary tract. It is also used to reduce the risk of recurrence of these diseases.
Often, such treatment is carried out in patients suffering from cancer. Generalized form of candidiasis, in which the pathogen penetrates into different parts of the body.
Candidiasis of the mucous membranes of the gastrointestinal tract, respiratory system and other organs.
Reducing the risk of infection in people at risk, including patients with HIV infection and cancer.
Other pathologies: fungal infection of the skin, coccidioidomycosis, infection of the nail plate, versicolor versicolor and histoplasmosis.
Assimilation and excretion
A small amount of the active ingredient binds to blood proteins. The chemical compound is well absorbed in the gastrointestinal tract. Up to 90% of the substance is absorbed. The drug passes into major body fluids, including saliva, phlegm, urine, and breast milk. Penetration of the agent into the cerebrospinal fluid is also observed, so it is possible to treat an infectious brain lesion. The drug is excreted mainly by the kidneys.
In some cases, the use of the drug is undesirable due to the high risk of complications. The main contraindication is considered sensitivity to any component of the drug. The doctor must rule out allergies and other reactions in advance. If a patient has been diagnosed with an allergy to azole antimycotics in the past, fluconazole is not prescribed.
Other possible contraindications:
- Patient age up to 4 years for capsules and tablets.
- Carrying a child and the period of breastfeeding.
- Simultaneous reception with other medications that lengthen the QT interval.
- For use with cisapride tablets.
Treatment is carried out with caution in the presence of the following factors: impaired renal function, the appearance of skin reactions, a combination with other antimycotics, alcohol dependence, taking other hepatotoxic medications, disruption of the cardiovascular system or the presence of risk factors for such a condition, childhood, liver dysfunction.
Fluconazole instructions for use
The way of using the drug depends on the dosage form, manufacturer, dosage, patient’s condition and the characteristics of the identified disease. The course of drug therapy can be individualized. Treatment is always prescribed by a doctor after clarifying the patient’s complaints and conducting laboratory tests.
Oral forms of the drug are taken orally, regardless of food intake. Capsules and tablets are taken with water. To use the syrup, you need to use the measuring container, which can be found in the package. It is recommended to rinse the mouth with the liquid for two minutes before swallowing.
All instructions are described for reference purposes. While taking antimycotics, the patient should be guided by the instructions of the attending physician and official instructions.
Application of capsules
- Treatment of cryptococcal infection in patients over fifteen years of age (weighing at least 50 kilograms): the standard regimen on the first day is eight capsules of fifty milligrams. On other days, the dosage can be maintained or reduced to four capsules of fifty milligrams once a day. The duration of therapy is determined by a specialist.
- Prevention of the disease in patients suffering from acquired immunodeficiency syndrome: four capsules (50 mg) per day for a long time.
- Candidal diseases: eight capsules of fifty milligrams on the first day and four capsules with a similar dose on the remaining days.
- Treatment of cryptococcal infection in adults: 400 milligrams on the first day and 200 milligrams per day on the remaining days.
- Reducing the risk of developing the disease in patients with immunodeficiency: two hundred milligrams per day.
- Pathologies caused by Candida: 400 milligrams on the first day and 200 milligrams daily further.
- Inflammation of the mouth and pharynx: fifty to one hundred milligrams per day for one or two weeks.
- Oral candidiasis with mucosal atrophy: fifty milligrams per day with other medications.
- Damage to the vaginal mucosa: a single dose of one hundred and fifty milligrams.
The use of tablets
Drug therapy in adults: fifty to four hundred milligrams per day.
Drug therapy in children: the dose is calculated taking into account 3-12 milligrams per kilogram of body weight per day. Once.
The procedure is carried out using a dropper. The rate of intravenous administration should not exceed two hundred milligrams per hour. The daily dosage is determined by the doctor taking into account the patient’s history. Transfusion therapy kits are used.
In case of impaired renal function, the doctor should adjust the drug intake regimen taking into account the creatinine clearance rate.
There is a long list of drug interactions. The use of fluconazole with other medicines may reduce the effectiveness of therapy, alter the effects of other medicines, or cause complications. It is necessary to inform the doctor about the drugs taken and read the official instructions.
Rarely, during treatment, patients develop serious (including life-threatening) pathologies of the liver tissue. If there is a history of diseases of this organ, the doctor should treat with caution.
In patients with acquired immunodeficiency, skin rashes often appear after taking the drug. If these symptoms occur, you need to see a specialist. Cancellation of the drug may be required.