ITRACONAZOLE or TEKNAZOLE – which is better, what is the difference, reviews 2020

Medicinal substance

The drug itself and any analogue of Itracanozole belongs to the class of antifungal triazoles. This artificially synthesized drug prevents the synthesis of ergosterol, which is necessary for the normal functioning of fungi. The drug "Itraconazole" suppresses the development of dermagophytes, Candida yeast fungi, molds and other pathogens. Some strains of microorganisms are resistant to the action of this product.

The drug "Itraconazole" is available in tablets, capsules, in the form of a solution (liquid), and ointment. There is far more than one analogue of Itraconazole on sale. Such drugs are available in different dosage forms.

Any analogue of Itraconazole and, in fact, this drug itself is most often used for the treatment of fungal infections of the respiratory system, in particular the lungs. These medications are also used to treat patients whose throat, oral cavity or esophagus are affected by fungi. Very often this infection affects human nails. In this case, another dosage form of the drug “Itraconazole” is used - an ointment for external use, which effectively fights fungal infections on the nails or skin. It is also prescribed for psoriasis.

Side effects

The drug is used to fight fungal infections; once it enters the body, it quickly accumulates in the blood and is transported through the bloodstream to the affected area.
Once in a fungal cell, it disrupts its structure and functioning by blocking cytochrome P450, which is necessary for cell growth and development. Active regarding:

• dermatophytes (Trichophyton, Trichophyton tonsurans, Trichophyton verrucosum, Trichophyton rubrum, Microsporum, Microsporum canis, Epidermophyton floccosum);
• yeast-like fungi Candida (Pityrosporum orbiculare, Trichosporon Beigellii, Candida albicans, Candida glabrata, Cryptococcus neoformans, Candida krusei, Blastomyces dermatitidis);
• molds (Cryptococcus neoformans, Aspergillus, Blastomyces dermatitidis Histoplasma, Sporothrix schenckii, Paracoccidioides brasiliensis, Fonsecaea, Cladosporium,).

• headache;
• dizziness;
• drowsiness;
• fast fatiguability;
• allergic reactions: pinpoint pink rash on the skin, itching, swelling of soft tissues;
• increased blood pressure;
• nausea;
• vomit;
• stomach ache;
• sudden weight loss;
• hepatitis – inflammation of the liver with the development of liver failure;
• constipation;
• swelling of the soft tissues of the face and lower extremities;
• darkening of urine;
• alopecia areata (baldness);
• pulmonary edema;
• impotence;

Methods of administration for pulmonary infections

For the treatment of fungal infections of the respiratory tract, Itraconazole tablets or capsules are prescribed. Analogs are cheaper, but they may have a more distant effect in time, so the disease is more difficult to defeat in the shortest possible time. Tablets or capsules are taken 1-2 times a day, during or immediately after meals. It usually takes at least 3 months to cure a fungal lung infection. In some cases, the doctor may prescribe the following course of therapy: 3 tablets per day for 3 days, and then 3 months, 1-2 tablets per day.

Pharmacokinetics

Absorbed from the gastrointestinal tract quite completely. Taking itraconazole capsules immediately after meals increases bioavailability. Taking it in the form of a solution on an empty stomach leads to a higher rate of reaching Cmax and a higher Css value compared to taking it after a meal (by 25%). TCmax when taking capsules is about 3-4 hours. Css when taking 100 mg of the drug once a day is 0.4 mcg/ml; when taking 200 mg once a day - 1.1 mcg/ml, 200 mg twice a day - 2 mcg/ml. TCmax when taking the solution is about 2 hours when taken on an empty stomach and 5 hours after meals. The time for the onset of Css in plasma with long-term use is 1-2 weeks. Bonding with plasma proteins is 99.8%. Penetrates well into tissues and organs (including the vaginal mucosa), and is contained in the secretions of the sebaceous and sweat glands. The concentration of itraconazole in the lungs, kidneys, liver, bones, stomach, spleen, and skeletal muscles is 2-3 times higher than its concentration in plasma; in tissues containing keratin - 4 times. The therapeutic concentration of itraconazole in the skin remains for 2-4 weeks after cessation of the 4-week course of treatment. Therapeutic concentration in nail keratin is achieved 1 week after the start of treatment and remains for 6 months after completion of 3 months of treatment. Low concentrations are detected in the sebaceous and sweat glands of the skin. Metabolized in the liver to form active metabolites, including hydroxyitraconazole. It is an inhibitor of the isoenzymes CYP3A4, CYP3A5 and CYP3A7. Excretion from plasma is two-phase: by the kidneys within 1 week (35% in the form of metabolites, 0.03% unchanged) and through the intestines (3-18% unchanged). T

1/2 - 1-1.5 days. It is not removed during dialysis. When administered intravaginally, an effective local concentration of itraconazole is created. Systemic absorption is minimal.

Taking the drug for nail infections

The drug “Itraconazole” is a tablet that is also prescribed for the treatment of fungal nail infections. For complete cure, it is taken once a day for 12 weeks. The oral solution Itraconazole is more effective. It is taken for 1-4 weeks 1-2 times a day. At the same time, for faster absorption, the medicine is taken on an empty stomach. Only the attending physician can choose the most optimal regimen for taking the drug or prescribe an analogue of Itraconazole, who will take into account the severity of the disease and the general condition of the patient. In particularly advanced cases, another form of the drug “Itraconazole” is used to treat fungal nail infections - an ointment that is applied to the affected areas 1-2 times a day.

Itraconazole

Inside, immediately after eating, the capsules are swallowed whole.

For vulvovaginal candidiasis - 200 mg of the drug 2 times a day for 1 day or 200 mg 1 time a day for 3 days;

for dermatomycosis - 200 mg once a day for 7 days or 100 mg once a day for 15 days;

lesions of highly keratinized skin areas (dermatophytosis of the feet and hands) - 200 mg 2 times a day for 7 days or 100 mg 1 time a day for 30 days;

for pityriasis versicolor - 200 mg once a day for 7 days;

for candidiasis of the oral mucosa - 100 mg 1 time per day for 15 days (in some cases, in immunocompromised individuals, the bioavailability of the drug may decrease, which sometimes requires doubling the dose);

for keratomycosis - 200 mg once a day for 21 days (the duration of treatment depends on the clinical response);

for onychomycosis - 200 mg of the drug once a day for 3 months or 200 mg 2 times a day for 1 week per course. If the toenails are affected (regardless of the presence of damage to the fingernails), 3 courses are given with an interval of 3 weeks. If nails are affected only on the hands, 2 courses are given with an interval of 3 weeks.

Elimination of the drug from the skin and nails is slow; the optimal clinical response for dermatomycosis is achieved 2-4 months after completion of treatment, for onychomycosis - 6-9 months.

For systemic aspergillosis - 200 mg/day for 2-5 months; with progression and dissemination of the disease, the dose is increased to 200 mg 2 times a day.

For systemic candidiasis - 100-200 mg once a day for 3 weeks - 7 months; with progression and dissemination of the disease, the dose is increased to 200 mg 2 times a day.

For systemic cryptococcosis without signs of meningitis - 200 mg once a day for 2-12 months. For cryptococcal meningitis - 200 mg 2 times a day for 2-12 months.

Treatment of histoplasmosis begins with 200 mg once a day, the maintenance dose is 200 mg 2 times a day for 8 months.

For blastomycosis - 100 mg 1 time per day, maintenance dose - 200 mg 2 times per day for 6 months.

For sporotrichosis - 100 mg of the drug once a day for 3 months.

For paracoccidioidosis - 100 mg once a day for 6 months;

For chromomycosis - 100-200 mg once a day for 6 months.

Oral solution: orally, at least 1 hour before meals. When treating candidiasis of the oral mucosa or esophagus, the solution should be kept in the mouth for 20 seconds and then swallowed (you should not rinse your mouth with other liquids after taking the drug).

Treatment of candidiasis of the oral mucosa or esophagus - 100 mg 2 times a day or 200 mg 1 time a day for 7 days; if ineffective, treatment is extended for another 7 days.

Treatment of candidiasis of the oral mucosa or esophagus resistant to fluconazole - 100-200 mg 2 times a day for 14 days; if ineffective, treatment is extended for another 14 days. The maximum course of treatment at a dose of 400 mg/day if there is no improvement is 14 days.

Prevention of fungal infections with the drug - 5 mg/kg/day in 2 doses. Treatment begins simultaneously with the start of cytostatic therapy or 1 week before transplantation. Fungal infections occur when the number of neutrophils decreases to less than 100 cells/ml; treatment is continued until the number of neutrophils is restored (more than 1000 cells/ml).

Children are prescribed if the expected benefit outweighs the potential risk.

special instructions

The drug "Itraconazole" and analogues of this medicine should be taken in accordance with the instructions and recommendations of the attending physician. In smaller or larger doses they may be ineffective or may harm the patient's health.

Itraconazole capsules, cheap or expensive analogues, are taken as follows: capsules and tablets are swallowed whole. However, they should not be chewed or crushed. If the level of acidity in the stomach decreases, caused, for example, by cystic fibrosis, this should be reported to your doctor.

In some cases, the regimen for taking this drug may be changed. Most often this happens when the patient takes the following drugs during therapy: Famotidine, Nizatidine, Esomeprazole, Cimetidine, Omeprazole, Ranitidine, Lansoprazole, Pantoprazole, " Rabeprazole."

Contraindications

In some cases, Itraconazole is contraindicated for patients. The instructions for similar drugs often prohibit the use of such antifungal drugs if you are allergic to their components. That is why, when prescribing therapy using these drugs, the attending physician must know exactly whether the patient has an allergic reaction to the substances included in their composition.

The medication should not be taken by pregnant and lactating women. To prevent possible pregnancy during treatment, it is necessary to use effective contraception. This drug should be prescribed to elderly patients with caution. Taking it in childhood is possible only if the benefit outweighs the potential risk. The drug is not recommended for patients with heart failure, ischemia, severe lung diseases, or renal failure.

Itraconazole and drug analogues should not be taken in double doses in case of possible missed doses of the medication. It is best to forget about the missed dose and continue to follow the dosage regimen. An overdose of this drug or its analogues should not be allowed, as this can lead to very serious health complications.

Interaction with other drugs

Before taking Itraconazole, the attending physician should be aware of what medications the patient took before. This is especially true for the use of drugs such as Efavirenz, Everolimus, Sildenafil, Aliskiren, Rifabutin, Apixaban, Nevirapine, Dasatinib, Ibrutinib, Salmeterol, " Darifenacin", "Nilotinib", "Carbazepine", "Sunitinib", "Colchicine", "Rivaroxaban", "Phenobarbital", "Tamsulosin", "Isoniazid", "Phenytoin", "Vardenafil", "Rifampicin", "Nevirapine" , "Temsirolimus".

In addition to the above medications, before using Itraconazole, you should inform your doctor about taking the following medications:

• anticoagulants;

• antibiotics;

• HIV protease inhibitors;

• vitamins;

• food additives (dietary supplements).

When using Itraconazole and antacid drugs simultaneously, the latter are taken 1 hour before or a couple of hours after taking the antifungal medication.

Itraconazole capsules

The accepted pharmacological classification classifies Itraconazole as a broad-spectrum antifungal drug. The medication contains the active substance itraconazole in micropellets. Due to its constituent components, the medicine stops the production of vital substances for the fungal pathogen, which leads to cell death.

Composition of Itraconazole

The active substance of the drug is itraconazole at a concentration of 100 mg per capsule. Hard gelatin capsules of an opaque pink color with a blue cap contain spherical microgranules of a white-cream hue inside. Check out the detailed composition of the drug:

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Pharmacodynamics and pharmacokinetics

A synthetic antifungal agent acts on many pathogens. The active substance is a triazole derivative that inhibits the production of ergosterol in the fungal cell membrane. The drug destroys dermatophytes, yeast, and mold fungi. The effectiveness of treatment can be assessed a month after the start of treatment for mycotic skin diseases, and after 6-9 months for nail lesions.

Itraconazole is absorbed in the stomach and intestines, and its bioavailability increases with food intake. When using the solution on an empty stomach, the rate at which the maximum concentration is achieved becomes faster. The capsules begin to act four hours after administration, the active substance binds to plasma proteins by 99%. The drug penetrates into tissues, organs, vaginal mucosa, and the secretions of the sebaceous and sweat glands.

Clinical concentration of the drug in the skin is achieved a week after the first day of treatment with Itraconazole and lasts for 30 days after completion of the monthly course, in nail keratin - a week after and lasts for six months after completion of the three-month course. Metabolism of Itraconazole occurs in the liver, the metabolites are isoenzyme inhibitors. The drug is excreted from the plasma by the kidneys within a week and by the intestines in two days; it is not removed by dialysis.

Indications for use

According to the instructions, the indications for the use of the drug are the following conditions:

• vulvovaginal candidiasis;
• dermatomycosis;
• pityriasis versicolor;
• candidiasis of the oral mucosa;
• keratomycosis, onychomycosis (nail fungus);
• systemic mycoses of the skin – aspergillosis, candidiasis, cryptococcosis, cryptococcal meningitis;
• histoplasmosis, blastomycosis, sporotrichosis, paracoccidioidosis.

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Side effects

The drug Itraconazole sometimes causes dizziness and blurred vision in the form of double vision. While taking this medicine, you should not drive a car or operate any machinery. The most commonly reported side effects when taking it include bloating, increased gas formation, diarrhea, constipation, heartburn, and an unpleasant taste in the mouth; increased sweating, dizziness, headache, bleeding and sore gums, muscle pain, decreased muscle tone, runny nose, fever, joint pain, depression, decreased libido, hair loss.

The following side effects are considered particularly dangerous to the patient’s health: double vision, nausea, vomiting, abdominal pain, heart failure, hepatitis, involuntary urination, anaphylactic and allergic reactions, dark urine, ringing in the ears, hearing loss, loss of appetite, excessive fatigue , yellowing of the skin and eyes, numbness and tingling of soft tissues and skin, photophobia, skin rash, itching, hoarseness, pulmonary edema, menstrual irregularities, swelling in the face, throat, hands, ankles. If any of the above symptoms occur, you should immediately inform your doctor.

Overdose of itraconazole

If the prescribed dose of the drug is exceeded or self-treatment is started, symptoms of overdose may develop, these include:

• drowsiness;
• disturbance of consciousness;
• vomiting;
• stomach ache;
• the appearance of peripheral edema, mainly in the face and lower extremities;

If these symptoms are detected, it is necessary to discontinue the drug, rinse the stomach with cold, clean water, and take activated carbon tablets at the rate of 1 tablet per 10 kg of body weight. There is no specific antidote to the drug.

How to choose an analogue of Itraconazole

Every year, more and more people are faced with the problem of fungal diseases. At the same time, many patients decide that it is not necessary to purchase Itraconazole for their treatment. Analogues are cheaper, so they are often preferred. In fact, the choice of this drug or its analogues should be decided only by the attending physician. In some particularly severe cases, complete recovery of the patient is achieved exclusively by Itraconazole. Analogues are cheap, but not all of them are as effective as this drug.

What can replace Itraconazole? Ointment and analogues of this drug in other dosage forms are widely available in pharmacies. Structural analogues include the following medications produced in capsule feeds: “Irunin”, “Intramykol”, “Itrazol”, “Mikonihol”, “Kanditral”, “Kanazol”, “Teknazol”, “Orungal”, “Rumikoz”, “Orungamin” ", "Orunit".

The following drugs are analogues of Itraconazole in terms of therapeutic effect:

• capsules: “Diflucan”, “Diflazon”, “Itrazol”, “Orungal”, “Rumikoz”, “Flucostat”, “Fluconazole”, “Fungolon”;
• tablets: Atifin, Binafin, Ketoconazole, Fungoterbin, Exifin, Nizoral;
• ointments, creams, gels: “Akriderm”, “Lamisil Dermagel”, “Terbizil”, “Exifin”, “Mikomax”, “Mikozoral”, “Triderm”, “Fungotherbin”, “Ketoconazole”, “Kanizon”, “Lamitel” , “Candide”, “Amiclone”, “Zalain”, “Kanizon”, “Atifin”, “Clotrimazole”, “Lamisil”, “Ifenek”, “Lamitel”, “Terbix”, “Imidil”;
• suppositories, vaginal tablets: “Zalain”, “Candide”, “Kanizon”, “Mikogal”, “Imidil”.

Reviews

What is the opinion of people who have taken the drug Itraconazole? Analogs, reviews of which often have a negative connotation, and this drug itself often do not bring the expected results from therapy. Moreover, the presence of a huge number of contraindications and side effects makes these medications quite dangerous for the health of many patients. Moreover, the risk of unpleasant consequences from the use of Itraconazole and its analogues increases significantly if the instructions of the attending physician are not followed or self-medication.

Very often there are negative reviews about the drug “Itraconazole” (suppositories). Analogues of this drug are also often perceived with caution by patients. This is due to the fact that in some cases, therapy for fungal diseases with suppositories must be supplemented by taking Itraconazole or its analogues orally.

Itraconazole caps 100 mg No. 14

1. Medicines that affect the absorption of itraconazole.

Medicines that reduce gastric acidity reduce the absorption of itraconazole, which is associated with the solubility of the capsule shells.

2. Medicines that affect the metabolism of itraconazole.

Itraconazole is mainly metabolized by the CYP3A4 isoenzyme. The interaction of itraconazole with rifampicin, rifabutin and phenytoin, which are powerful inducers of the CYP3A4 isoenzyme, was studied. The study found that in these cases, the bioavailability of itraconazole and hydroxyitraconazole is significantly reduced, which leads to a significant decrease in the effectiveness of the drug. The simultaneous use of itraconazole with these drugs, which are potential inducers of microsomal liver enzymes, is not recommended. Interaction studies with other inducers of liver microsomal enzymes, such as carbamazepine, phenobarbital and isoniazid, have not been conducted, however, similar results can be expected.

Potent CYP3A4 inhibitors such as ritonavir, indinavir, clarithromycin and erythromycin may increase the bioavailability of itraconazole.

3. The effect of itraconazole on the metabolism of other drugs.

Itraconazole may inhibit the metabolism of drugs metabolized by CYP3A4. The result of this may be an increase or prolongation of their action, including side effects. Before starting to take concomitant medications, you should consult with your doctor about the metabolic pathways of this drug indicated in the instructions for medical use. After discontinuation of treatment, plasma concentrations of itraconazole decrease gradually depending on the dose and duration of treatment (see Pharmacokinetics

). This must be taken into account when discussing the migratory effect of itraconazole on concomitant medications.

Examples of such drugs are:

Drugs that should not be given concomitantly with itraconazole:

• Terfenadine, astemizole, mizolastine, cisapride, dofetilide, quinidine, pimozide, levacetylmethadol, sertindole - concomitant use of these drugs with itraconazole may cause increased plasma concentrations of these substances and increase the risk of QT prolongation and, in rare cases, torsade de pointes. des pointes),
• HMG-CoA reductase inhibitors metabolized by the CYP3A4 isoenzyme, such as simvastatin and lovastatin,
• Midazolam for oral administration and triazolam,
• Ergot alkaloids such as dihydroergotamine, ergometrine, ergotamine and methylergometrine,
• Slow calcium channel blockers - In addition to the possible pharmacokinetic interaction associated with the common pathway of metabolism involving the CYP3A4 isoenzyme, slow calcium channel blockers may have a negative inotropic effect, which is enhanced when taken concomitantly with itraconazole.

Drugs, when prescribed, it is necessary to monitor their plasma concentrations, effects, and side effects.

When co-administered with itraconazole, the dose of these drugs should be reduced, if necessary.

• Indirect anticoagulants;
• HIV protease inhibitors such as ritonavir, indinavir, saquinavir;
• Some anticancer drugs such as rose vinca alkaloids, busulfan, docetaxel, trimetrexate;
• Blockers of “slow” calcium channels metabolized by the CYP3A4 isoenzyme, such as verapamil and dihydropyridine derivatives;
• Some immunosuppressive drugs: cyclosporine, tacrolimus, sirolimus (also known as rapamycin);
• Some HMG-CoA reductase inhibitors metabolized by the CYP3A4 isoenzyme, such as atorvastatin;
• Some glucocorticosteroids such as budesonide, dexamethasone and methylprednisolone;
• Other drugs: digoxin, carbamazepine, buspirone alfentanil, alprazolam, brotizolam, intravenous midazolam, rifabutin, ebastine, reboxetine, cilostazol, disopyramide, eletriptan, halofantrine, repaglinide.

No interaction was found between itraconazole and zidovudine and fluvastatin.

There was no effect of itraconazole on the metabolism of ethinyl estradiol and norethisterone.

4. Effect on plasma protein binding.

In vitro studies have demonstrated that there is no interaction between itraconazole and drugs such as imipramine, propranolol, diazepam, cimetidine, indomethacin, tolbutamide and sulfamethazine when bound to plasma proteins.