Antifungal drugs are a wide range of both cosmetic and pharmaceutical preparations. And this is not surprising, because diseases provoked by various fungi not only affect the well-being and health of a person, but also adversely affect their appearance and emotional health.
Most often, during the treatment of such ailments, specialists prescribe the drug "Itraconazole". Instructions for use, reviews and analogues of this drug are of interest to many patients.
What is this medicine? What is its spectrum of action? How to use the drug to achieve the desired effect? Instructions for use of Itraconazole and reviews of the medication of doctors and patients will help to find the correct answers to the above questions.
The most important thing is the active substance
According to the instructions for use for the Itraconazole preparation, its main component contributing to recovery is the substance of the same name, which is a powder of light shades. This synthetic component is a triazole derivative. It does not dissolve in water and practically does not dissolve in alcohols, which cannot be said about dichloromethane.
Forms of drug release
According to reviews and instructions, itraconazole as an active substance is available in three forms - capsules, suppositories and ointment.
Due to this diversity, the drug is very popular. We will talk about each form of release separately below. However, first, let's discuss the pharmacological properties of itraconazole. Instructions and reviews of experts will help us determine in which diseases this drug is prescribed.
Effects on the body
Thanks to what the main component of the drug has a beneficial effect on the healing process? The thing is that the substance inhibits a fungal microorganism, namely ergosterol, which is a component of the membrane of a parasitic element and is responsible for the integrity of its structure. Due to the fact that the cell membrane is broken, the fungus dies.
What types of harmful microorganisms do itraconazole target? Annotation to the drug explains that the substance is able to destroy dermatophytes, trichovitis, microspores, as well as mold and yeast fungi (including those from the Candida genus). And yet, not all yeast strains are affected by the substance. Therefore, before starting treatment with itraconazole, it is necessary to take tests and identify the true causative agent of the disease.
Pharmacokinetic properties of the substance
Itraconazole in capsule form is believed to be the most effective treatment. That is why in this section we will focus mainly on the oral administration of the drug.
What happens after ingestion of itraconazole capsules? Instructions for use explain that with prolonged therapy, a substance can accumulate in blood plasma. As soon as the patient stops taking the drug, the main component is completely eliminated from the body within one to two weeks.
The half-life of the substance in the case of a single dose is 24 hours. If we are talking about prolonged use of the drug, then this period can increase to 1.5-2 days.
Itraconazole is absorbed quickly enough. After two to five hours, its maximum amount in plasma is observed. In this case, the bioavailability of the substance is about 50%. This indicator in the maximum value is noted if the capsules are taken orally immediately after a meal.
The binding of itraconazole to plasma proteins is approximately equal to 100%. At the same time, the highest concentration of the substance is observed not in the circulatory system, but in various organs, such as the stomach, lungs, spleen, kidneys, muscles, and even bones. The concentration of itraconazole in cerebrospinal fluid is much lower than in plasma, but this indicator is sufficient to eliminate infectious pathogens in cerebrospinal fluids.
The substance is excreted mainly through the intestines (54%), and only 35% of itraconazole leaves the body through the kidneys. This information is confirmed by the instruction for tablets “Itraconazole”.
With regard to suppositories and ointments, it should be said that their use does not have a strong effect on the human body, since in such circumstances the active substance acts locally. The use of itraconazole in the form of an ointment or suppository practically does not affect its concentration in blood plasma or other vital organs. Nevertheless, doctors often prescribe such drugs for local use in order to enhance the effect of oral therapy. This information is contained in the annotation for Itraconazole suppositories. Instructions for use of the drug will be discussed in detail below.
Capsule Use Conditions
In what cases are Itraconazole tablets prescribed? Instructions for use of capsules provides a detailed list of diseases.
First of all, these are candidiasis on the mucous membrane or skin (including vulvovaginal), mycoses on the epidermis or mucous membrane of the eyes and mouth, pityriasis (or multi-colored) lichen.
Also, the drug can be recommended in case of onychomycosis (in other words, with fungal infections of the nails). Very often, a medication becomes the main method of treatment for various dermatomycoses, histoplasmoses, paracoccidioidoses, sporotrichoses, as well as various lesions caused by cryptococci. In some cases, the drug can be effective in combating pathologies caused by rare, for example, tropical fungi.
Conditions for using the ointment
In what cases is itraconazole ointment prescribed? The instructions for use explain that the drug of this form of release is effective in mild forms of pityriasis versicolor, erythrasma, trichophytosis and dermatomycosis, the manifestations of which are expressed in the affected areas of the epidermis.
Despite the fact that many consider the nail fungus an explicit indication for the use of ointment, an external agent is extremely rarely prescribed by specialists to treat such diseases. Most often, doctors prescribe in such cases capsules with itraconazole or recommend combining oral administration of the active substance with an external agent.
If the ailments have a pronounced neglected form, or the lesion area is too vast, they practice combining ointments and capsules, taking into account the fact that the latter have a stronger effect on the human body.
Conditions for Using Suppositories
In what cases are candles prescribed? Most often, this is one single indication - vaginal candidiasis of a chronic or recurring form.
If the disease is complicated and proceeds in a severe form, then capsules are additionally prescribed to the suppositories.
Dosages and regimens
How to take the active substance depending on the type of ailment? In the beginning, let's discuss the general recommendations for Itraconazole 100 mg capsules. Instructions for use provide a universal treatment regimen, regardless of the age, sex and physical condition of the patient. Therefore, for more accurate information on how to carry out therapy, consult your doctor. He will prescribe the correct treatment, suitable only for you, based on the data of the tests and the accompanying ailments.
With regard to oral administration, it should be clarified that the capsules should be swallowed whole without damaging the protective membrane. An abstract to the medication recommends doing this immediately after eating.
So, here is an approximate dosage regimen with a dosage of 100 mg, depending on the type of ailment:
- With vaginal candidiasis, there are several methods of oral administration. One of them is to use two capsules in the morning and evening for one day. The second method involves a longer course of administration - two capsules once a day for three days. In parallel (or as monotherapy), vaginal suppositories are prescribed one at a time. The duration of such therapy is six days.
- For the treatment of dermatomycosis, capsules are taken orally once a day, in two pieces for a week, or one piece for fifteen days.
- Treatment of dermatophytosis on the feet or hands involves taking two tablets in the morning and evening for a week or one tablet for a month. At the same time, ointment can be used. The duration of the use of an external agent is determined by the attending physician.
- With pityriasis, two capsules of Itraconazole are prescribed once a day. The course of treatment is at least a week.
- Candidiasis of the oral mucosa involves the use of one capsule for oral administration once a day for fifteen days.
- Keratomycosis requires a longer treatment. For three weeks, you need to take two capsules once a day.
- How to get rid of nail fungus? Instructions for use "Itraconazole" recommends using capsules (two twice a day) for three weeks. Then a break of 21 days is taken and the therapy is repeated again. The duration of treatment may be six months or more.
- Long-term therapy is also necessary for systemic aspergillosis. For two to five months, two Itraconazole capsules are prescribed once a day. If necessary, the dosage can be increased.
- The duration of therapy for systemic candidiasis can be either normal (from three weeks) or long (up to seven months). The drug is prescribed one or two capsules once a day. With a more severe course of the disease, the dose can be increased.
- Treatment of systemic cryptococcosis involves oral administration of Itraconazole 200 mg once a day. If the disease is complicated by symptoms of meningitis, then the daily dosage must be doubled. The course of treatment is from two to twelve months.
- With histoplasmosis, treatment is carried out with a minimum dosage of two tablets daily. The duration of therapy is at least eight months.
- Such an ailment as sporotrichosis involves taking the drug for three months. Every day you need to take one capsule.
- The same doctor may prescribe the same treatment regimen for paracoccidioidosis. However, in this case, the duration of the course is increased to six months.
- Exactly the same dosage regimen is recommended for the treatment of chromomycosis. In some cases, a specialist can double the daily dose.
When you can not take medication
Regarding contraindications for Itraconazole, it should be borne in mind that the patient may show individual intolerance to the active substance or other components of the drug. In this case, treatment must be stopped, and the medication replaced.
Another contraindication of the drug is serious cardiac pathology, which may be in the patient's history.
And it is possible, and it is impossible
The conditional contraindications of “Itraconazole” include such diseases of the patient as heart failure, impaired renal or hepatic function, peripheral neuropathies. Also, caution is prescribed for patients after seventy and up to eighteen years of age.
Future and lactating mothers
Also, you can not take the drug to pregnant women in the first trimester and breastfeeding. This is due to the fact that the active substance of the drug has a negative effect on the embryo, provoking anomalies in development.
If “Itraconazole” is prescribed to women of childbearing age, then they should be carefully protected. It is worth remembering contraception methods, even several weeks after the end of itraconazole therapy. If a nursing mother needs to undergo a course of treatment, then the attending physician will recommend that she transfer the baby to artificial feeding.
Negative reactions
How come without side effects? Any antifungal drug has a lot of them and Itraconazole is no exception.
When applying the ointment to the affected area or with the vaginal administration of a suppository, side effects can manifest itself in the form of itching and burning, as well as redness of the skin or mucous membranes.
With oral administration, more serious negative reactions of the body to the active substance of the drug are possible. First of all, the digestive system can declare itself. In this case, side effects will be manifested in disorders of the stool, bouts of nausea, bloating, vomiting, and abdominal pain.
On the part of the nervous system, unpleasant symptoms such as dizziness, decreased attention span, and nervousness can be observed.
Disruptions in the menstrual cycle, loss of sexual interest and the like are also possible.
Possible negative reactions from the cardiovascular system. First of all, it can be the development or progression of heart failure, arrhythmia, increased pressure or other disorders in the work of the heart.
Side effects such as pulmonary edema, hair loss, skin rashes, hives and so on are also possible.
Interaction with other drugs
Itraconazole should be taken with caution in conjunction with other pharmacological agents. For example, you should know that rifampicin and phenytoin-based drugs reduce the concentration of the drug in question in the blood plasma.
Such drugs as m-anticholinergics, antacids and others decrease the absorption of intraconazole.
Joint administration of Itraconazole can provoke the intensity of exposure to substances such as astemizole, triazolam, terfenadine, cisapride, cyclosporine, midazolam, quinidine, vincristine, digoxin, and also increase the effectiveness of indirect anticoagulants and calcium channel blockers.
A bit about the cost of the drug
As many patients say, the price of “Itraconazole” can be called acceptable for most of our compatriots. Depending on the pharmacy chain and the manufacturer, the price of a package of fourteen capsules with a dosage of 100 mg varies between 270 and 380 rubles. On the other hand, if we are talking about long-term treatment for up to six months or more, then the price of the drug may already “bite”.
Reviews about the drug
What do patients taking Itraconazole say? Almost everyone recognizes that the drug is an effective antifungal agent that can overcome candidiasis, lesions on the skin and mucous membranes, nail fungus and much more.
However, not everything is so rosy. Many patients complain of severe side effects that accompany the drug and pass only a few days after the end of therapy. Patients were worried about headaches, mood swings, sadness, depression, abdominal pain, constant nausea, and so on. There are also some complaints that the use of the drug provoked the development of serious pathologies of the liver and kidneys. Moreover, as some patients have noted, they were uncomfortable with the fact that drug therapy can last for months. However, the duration of treatment is most often associated not with the low effectiveness of the medication, but with the peculiarity of the fungal disease itself.
As you can see, not all people are satisfied with the treatment with Itraconazole, even though it helped to defeat the fungus. The reason for this is the long courses of therapy, the considerable cost of the drug (given the duration of administration), many side effects. Therefore, in some cases, patients may ask for the replacement of Itraconazole with analogues. Instructions for using some of them will be discussed in detail below.
Drug Substitutes
Among the analogues of the drug, two broad groups can be distinguished - according to the active substance and the spectrum of action. In the beginning, we will discuss the first type of Itraconazole generics, which include the active substance of the same name.
First of all, “Irunin”. The drug is available in the form of vaginal tablets with a dosage of the main component of two hundred milligrams. Excipients - potato starch, lactose, polyvinylpyrrolidone, magnesium stearate, sodium lauryl sulfate, talc. The indication of the drug is vulvovaginal candidiasis. To treat the disease, it is necessary to introduce suppositories into the vagina. The course of therapy varies from one to two weeks and is prescribed by a doctor. Schedule of admission - one suppository per night. The drug is not recommended in the first trimester of pregnancy and with breastfeeding. A side effect of the medication may be a skin rash, accompanied by itching and burning in the area of the external genitalia. Such unpleasant symptoms often do not require cancellation or dose adjustment.
“Itrazole” - a drug produced in the form of capsules, which include the active substance - itraconazole.The appearance of these pills is remarkable. Inside each capsule are spherical microgranules of yellow hues, which are coated with a hard gelatin shell. Excipients in the composition of the drug are corn starch, titanium dioxide, sucrose, gelatin, hypromellose. The drug is prescribed for dermatomycosis, onychomycosis, fungal keratitis, pityriasis versicolor, candidomycosis. The course of treatment and dosage is similar to Itraconazole.
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“Pimafucin” is an antifungal agent available in the form of ointments, tablets and suppositories. Its active ingredient is natamycin - a macrolide antibiotic belonging to the polyene series. The medication is prescribed for the treatment of ailments provoked by fungal infections. These include candidal vulvovaginitis, intestinal candidiasis, skin lesions of the hands and nails. Suppository treatment lasts about nine days. The drug is injected into the vagina once a day, most often at night. Ointments have been successfully used to treat thrush in both adults and children, and even in newborns. The composition of the drug for external use includes, in addition to natamycin, methyl parahydroxybenzoate, propylene glycol, cetyl ether wax, purified water, propyl parahydroxybenzoate, sodium lauryl sulfate, cetostearyl alcohol and so on. Pimafucin tablets are white pills that contain such additional components as potato starch, magnesium stearate, beeswax, cellulose acetate, sucrose, polyvinylpyrrolidone, methyl parahydroxybenzoate, gum arabic, calcium carbonate and so on. On average, tablets are prescribed one four times a day. The course of admission can vary from two weeks to six months. Children can be prescribed half a tablet of the drug. The regimen is prescribed by the attending physician. Reception of ointment or suppositories “Pimafucin” is best combined with the use of a tablet preparation.
Other common analogues of Itraconazole are D-Panthenol, Effezel Gel, Nezulin, Lamisil, Fluconazole, Fungerbin, Exoderil and other drugs. As you can see, there are a large number of Itraconazole substitutes. They are very different from each other by the form of release, the name of the active substance and the dosage. Therefore, it is clear that only a specialist should prescribe this or that dosage, as well as prescribe the dosage and regimen for taking it, based on the available analyzes, clinical picture and physical characteristics of the patient himself.
We reviewed the instructions for use of Itraconazole. Analogues of the drug and reviews about it were also presented.