Tecnazol - instructions for use, doses, side effects, contraindications

Itraconazole pellets 460 mg: active substance: itraconazole 100 mg; Excipients: hypromellose (hydroxypropylmethylcellulose), macrogol (polyethylene glycol), neutral micropellets (sucrose, corn starch).

Hard gelatine capsules: gelatin, titanium dioxide E 171, dye azorubin H122, dye patented blue VE 131, dye caramel E 150.

Description:

Hard gelatin capsules without odor; cap capsule - matte, pink; the body of the capsule is transparent, brown in color.

Contents of capsules - spherical white or almost white micropellets.

Pharmacotherapeutic group:antifungal agent

ATX: & nbsp

J.02.A.C.02 Itraconazole

Pharmacodynamics:

Synthetic antifungal agent of a wide spectrum of action. The triazole derivative. Suppresses the synthesis of ergosterol cell membrane of fungi.

Active against dermatophytes (Trichophyton spp., Microsporum spp., Epidermophyton floccosum), yeast fungi Candida spp. (including Candida albicans, Candida parapsilosis), molds (Cryptococcus neoformans, Aspergillus spp., Trichosporon spp., Geotrichum spp., Penicillium mameffei, Pseudallescheria boydii, Histoplasma spp., Coccidioides immitis, Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecaea spp., Cladosporium spp., Blastomyces dermatitis), Malassezia spp.

Some strains can be resistant: Candida glabrata, Candida krusei, Candida tropicalis, Absidia spp., Fusarium spp., Mucor spp., Rhizomucor spp., Rhizopus spp., Scedosporium proliferous, Scopulariopsis spp.

The effectiveness of treatment is estimated after 2-4 weeks after discontinuation of therapy (with mycosis), after 6-9 months - with onychomycosis (as the nails change).

Pharmacokinetics:

It is absorbed from the digestive tract quite full. Taking itraconazole in capsules immediately after meals increases bioavailability. Receiving it in the form of a solution on an empty stomach leads to a higher rate of achievement C_mOh and greater Css compared with the reception after meals (by 25%).

TS_mOh when taking capsules - about 3-4 hours, Css when taking 100 mg of the drug once a day - 0.4 μg / ml; when administered 200 mg once a day - 1.1 μg / ml, 200 mg twice a day - 2 μg / ml.

TS_mOh when taking the solution - about 2 hours when taken on an empty stomach and 5 hours after eating.

Time of approach Css in plasma with prolonged use - 1-2 weeks. The connection with plasma proteins is 99.8%.

It penetrates well into tissues and organs (including the mucous membrane of the vagina), is contained in the secretion of sebaceous and sweat glands. The concentration of itraconazole in the lungs, kidneys, liver, bones, stomach, spleen, skeletal muscles at 2-3 times its concentration at plasma; at tissues containing keratin, - 4 times.

The therapeutic concentration of itraconazole in the skin persists for 2-4 weeks after the cessation of 4 weeks of treatment.

Therapeutic concentration in the nail keratin is achieved 1 week after the start of treatment and is maintained for 6 months after the completion of 3 months of treatment.

Low concentrations are determined in the sebaceous and sweat glands of the skin.

Metabolized in the liver with the formation of active metabolites, incl. hydroxyitraconazole. Is an inhibitor of isoenzymes CYP3A4, CYP3A5 and CYP3A7.

Excretion from plasma - two-phase: by kidneys for 1 week (35% in the form of metabolites,0,03% - unchanged) and through the intestine (3-18% unchanged). T_1/2 - 1-1,5 days. It is not removed during dialysis.

Indications:

- Vulvovaginal candidiasis;

- dermatomycosis;

- colored lichen;

Candidiasis of the oral mucosa;

- dermatomycosis;

- onychomycosis caused by dermatophytes or yeast-like fungi;

- Systemic mycoses: systemic aspergillosis or candidosis, cryptococcosis (including cryptococcal meningitis) in immunocompromised individuals and cryptococcosis of the CNS, regardless of the immune status if the first line is ineffective;

- Histoplasmosis;

- blastomycosis;

- sporotrichosis;

- Paracoccidioidosis;

- Other rare systemic and tropical mycoses.

Contraindications:

- Hypersensitivity;

- CHF, incl. in the anamnesis (except for therapy of life-threatening conditions);

- simultaneous reception of isoenzyme substrates CYP3A4, extending the interval QT (astemizole, bepridil, cisapride, dofetilide, levacetylmetadol, misolastine, pimozide, quinidine, sertindole, terfenadine); inhibitors of HMG-CoA reductase metabolized by isoenzyme CYP3A4 (lovastatin, simvastatin); simultaneous oral administration of triazolam and midazolam,alkaloids of ergot (dihydroergotamine ergometrine, ergotamine, methylergotamine), nisoldipine, eletriptan;

- Pregnancy, lactation.

Carefully:

- Renal / hepatic insufficiency;

- peripheral neuropathy;

- Risk factors for CHF (CHD, damage to the heart valves, severe lung diseases, including COPD, conditions accompanied by edematous syndrome);

- Hearing impairment;

- Simultaneous reception of BCCC;

- Children's and the elderly.

Dosing and Administration:

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

With vulvovaginal candidiasis - 200 mg twice a day for 1 day or 200 mg once a day for 3 days;

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

lesions of high-keratinized skin areas (dermatophytosis of feet and brushes) - 200 mg twice a day for 7 days or 100 mg once a day for 30 days;

with pityriasis - 200 mg once daily for 7 days;

at a candidiasis of a mucous membrane of an oral cavity - 100 mg once a day for 15 days (in some cases in immunocompromised individuals, the bioavailability of itraconazole may decrease, which sometimes requires a dose doubling);

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

with onychomycosis - 200 mg once a day for 3 months or 200 mg 2 times a day for 1 week per course. When the nails are injured on the legs (regardless of the presence of nail lesions on the hands), 3 courses are conducted at intervals of 3 weeks. When the nails are damaged only on the hands, 2 courses are conducted at intervals of 3 weeks.

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

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

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

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

When cryptococcal meningitis - 200 mg twice a day for 2-12 months.

Treatment histoplasmosis begin with 200 mg once a day, a maintenance dose of 200 mg twice a day for 8 months.

With blastomycosis - 100 mg once a day, maintaining a dose of 200 mg twice a day for 6 months.

With sporotrichosis - 100 mg once a day for 3 months.

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

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

Children appoint if the expected benefit exceeds the potential risk.

Side effects:

Very often more than 1/10, often more than 1/100 and less than 1/10, infrequently more than 1/1000 and less than 1/100, rarely more than 1/10000 and less than 1/1000, very rarely, including single messages - less than 1/10000.

On the part of the organs of hematopoiesis: infrequently - leukopenia, neutropenia, thrombocytopenia.

Allergic reactions: frequency unknown - serum sickness, angioedema, anaphylactic and anaphylactoid reactions, hypersensitivity.

From the side of metabolism: infrequently - hypokalemia; frequency is unknown - hypertriglyceridemia.

From the nervous system: often - headache; infrequently - peripheral neuropathy, dizziness; frequency unknown - paresthesia, hypoesthesia.

From the sense organs: infrequently - impaired vision, including vagueness and diplopia; frequency unknown - tinnitus, transient or permanent deafness.

On the part of the CAS: frequency unknown - congestive heart failure.

From the respiratory system: frequency unknown - pulmonary edema.

From the digestive system: often - abdominal pain, vomiting, nausea, diarrhea, a violation of taste perception, increased activity of "liver" enzymes; infrequently - dyspepsia, constipation, hepatitis, hyperbilirubinemia; frequency unknown - hepatotoxicity, acute hepatic insufficiency.

From the skin: often - a rash; infrequently itching; frequency unknown - toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis, leukoclastic vasculitis, hives, alopecia, photosensitivity.

From the side of the musculoskeletal system: the frequency is unknown - myalgia, arthralgia.

From the genitourinary system: the frequency is unknown - pollakiuria, urinary incontinence, menstrual irregularities, erectile dysfunction.

Other: infrequently - swelling.

Overdose:

No data available. During the first hour, wash the stomach and, if necessary, assign Activated carbon, symptomatic treatment.

Itraconazole is not excreted by hemodialysis. There is no specific antidote.

Interaction:

Drugs that reduce the acidity of gastric juice, violate the absorption of itraconazole.

Inductors of isoenzyme CYP3A4 (including, rifampicin, rifabutin, phenytoin) reduce the bioavailability of itraconazole, and inhibitors of isoenzyme CYP3A4 (including, ritonavir, indinavir, clarithromycin, erythromycin) increase it.

Itraconazole enhances the effect (including side-effect) of drugs metabolized by isoenzyme CYP3A4.

Particular care should be taken with simultaneous use of indirect anticoagulants, HIV protease inhibitors, certain antitumor drugs (busulfan, docetaxel, trimetrexate, vinca alkaloids), BCCI metabolized by isoenzyme CYP3A4 (dihydropyridines, verapamil), some immunosuppressants (ciclosporin, tacrolimus, sirolimus), some GCS (budesonide, dexamethasone, fluticasone, methylprednisolone), digoxin (due to inhibition of P-glycoprotein), others (cilostazol, disopyramide, carbamazepine, buspirone, alfentanil, alprazolam, brotisolam, midazolam (w / w), rifabutin, ebastine, repaglinide, fentanyl, halofantrine, reboxetine, loperamide).

Special instructions:

Simultaneous treatment of sexual partners and personal hygiene are necessary to prevent reinfection. During treatment it is recommended to abstain from sexual intercourse.

If signs of infection persist after treatment is complete, a second microbiological study should be conducted to confirm the diagnosis.

The effectiveness of itraconazole for the treatment of fungal infections in severe neutropenia is unknown, so in such cases the drug should be used only if the first line of therapy is ineffective.

If there are risk factors for CHF (CHD, damage to the heart valves, severe lung diseases, including COPD, conditions accompanied by edematous syndrome) during treatment with itraconazole therapy should be canceled.

When taking itraconazole, some patients experienced transient and permanent deafness.

Effect on the ability to drive transp. cf. and fur:

Not observed.

Form release / dosage:

Capsules, 100 mg.

Packaging:

For 4 or 15 capsules in a blister of polyvinylchloride film and aluminum foil.

1 blister for 4 or 15 capsules, or 2 blisters of 15 capsules together with instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002406/10

Date of registration:24.03.2010

The owner of the registration certificate:Nobel Ilach Sanayi Ve Tidjaret A.Sh.Nobel Ilach Sanayi Ve Tidjaret A.Sh. Turkey

Manufacturer: & nbsp

NOBEL ILAC SANAYII VE TICARET, A.S. Turkey

Representation: & nbspNobel Ilach Sanayi Ve Tidjaret A.Sh.Nobel Ilach Sanayi Ve Tidjaret A.Sh.Russia

Information update date: & nbsp05.11.2015

Illustrated instructions

Instructions

Tecnazol (Teknazol)