Ketokonazol

Кетоконазол Drug photo

The description is actual on 23.04.2016

  • Latin name: Ketoconazole
  • ATH code: G01AF11
  • Active ingredient: Ketokonazol (Ketoconazole)
  • Producer: Ultratech India (India), Piramal Healthcare (India), Aarti Drugs (India), Farmaprim (Republic of Moldova)

Structure

  • Ketokonazol contains in 1 gram of cream 200 mg of the medicinal substance of the same name. Additional substances: labrafit M, emultsir 61, nipagin, a liquid paraffin, water.
  • As a part of one candle Ketokonazol contains 200 mg of the medicinal substance of the same name. Additional substances: glycerides semi-synthetic (before obtaining lump of a candle of 2000 mg), butylhydroxyanisole.
  • One tablet of drug Ketokonazol includes 200 mg of the medicinal substance of the same name. Additional substances: lactose, corn starch, magnesium stearate, silicon dioxide, low-molecular PVP.

Release form

  • Homogeneous white cream with a yellowish shade. 10, 15 or 25 grams of cream in an aluminum tuba, one tuba in a pack from paper.
  • White, cylindrical vaginal candles with a yellowish shade of color, on a section presence of an air core or deepening of a funneled form is allowed. 5 candles in planimetric packaging, 1 packaging cell in a pack from paper.
  • White round tablets with a yellowish shade, with a crosswise notch on one party. 10 tablets in the blister, 1 or 2 blisters in a pack from paper.

Pharmacological action

Anti-fungal, fungicidal, fungistatic, anti-androgenic action.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Ketokonazol is to artificial derivatives of an imidazole. Has fungistatic and fungicidal action. Slows down biosynthesis of ergosterol and breaks normal lipidic structure of a cell wall of mushrooms.

Affects Epidermophyton floccosum, dermatophytes of the sorts Microsporum, Trichophyton, and also mushrooms of the sort Pityrosporum and Candida.

Cream pharmacokinetics

At local use active agent is practically not exposed to system absorption, at long use in blood its contents is not defined.

Pharmacokinetics of candles

Absorption in a system blood stream at intravaginalny use is not enough.

Pharmacokinetics of tablets

Bioavailability of a ketokonazol reaches the greatest values at its use with food. At observance of this condition the maximum content of drug in blood is reached 1-2 hours later. Absorption of active agent is reduced at persons with the reduced acidity of a gastric juice and with an achlorhydria.

Reaction with blood proteins reaches 99%. It is widely distributed in bodies and fabrics, except cerebrospinal fluid. It is metabolized in a liver with allocation of a large number of inactive derivatives. The main ways of biotransformation are the aromatic hydroxylation, splitting and oxidation of piperazinovy and imidazolny rings, oxidizing O-dealkylation. Time of semi-removal makes about 10 hours.

It is allocated generally with bile and with a stake.

Indications to use

Indications to cream use Ketokonazol

Indications to use of candles Ketokonazol

  • Therapy of vaginal recurrent candidiasis, both acute, and chronic character.
  • The prevention of development of fungal infections of a vagina at reduced protective function of an organism and against therapy by the antibacterial agents and other drugs changing normal microflora.

Indications to use of tablets Ketokonazol

  • Therapy and prevention of the mycoses provoked by microorganisms, sensitive to medicine: infectious defeats mucous digestive tract; severe damages of skin, nails and hair (an onychomycosis, a dermatofitiya, multi-colored deprive also others); vaginal recurrent candidiasis of chronic character at inefficiency of topical treatment; system mycoses (parakoktsidiomikoz, candidiasis, koktsidiomikoz, histoplasmosis, zymonematosis).
  • Preventions of fungal infections at the weakened patients, including suffering from an immunodeficiency.

Contraindications

Contraindications to cream use

  • Hypersensitivity to medicine components.
  • Disturbance of integrity of skin in places of intended use of cream.

Contraindications to use of candles

  • First trimester of pregnancy.
  • Hypersensitivity to medicine components.
  • Age less than 12 years.

Candles Ketokonazol with care use during a lactation, in the second and third trimesters of pregnancy and at children 12 years are more senior.

Contraindications to use of tablets

  • Diseases of a liver of acute and chronic character.
  • Pregnancy or lactation.
  • The age is younger than 3 years.
  • Hypersensitivity to medicine components.

Joint reception with the following drugs decaying CYP3A4 isoenzyme (increase in concentration of these drugs in blood which leads to strengthening of medical and side effects and to lengthening of a piece of QT and development of arrhythmias is possible), is prohibited:

  • analgetics (Methadone, Levatsetilmetadol);
  • antiaritmik (Dronedaron, Disopyramidum, Dofetilid, Quinidine);
  • anthelmintic and anti-protozoan means (Galofantrin);
  • antihistaminic drugs (Mizolastin, Astemizol, Terfenadin);
  • means for treatment of migraine (Ergometrine, Ergotamine, Digidroergotamin, Metilergometrin);
  • antineoplastic means (Irinotekan);
  • blockers of channels of calcium (Lerkanidipin, Felodipin, Bepridil, Nisoldipin);
  • antipsychotic and hypnagogues, anxiolytics (Sertindol, Lurazidon, Pimozidum, Midazolam, to Triazoles);
  • hypolipidemic means (Simvastatin, Lovastatin);
  • cardiovascular means (Ranolazin, Ivabradin);
  • immunodepressants (Everolimus);
  • diuretics (Eplerenon);
  • gastrointestinal means (Domperidon, Tsizaprid);
  • other means (Colchicine at therapy of patients with disorders of work of a liver and kidneys).

Side effects

Side effects after cream use

  • The irritation of skin, itch, burning in the place of use, skin rash which disappear right after cream cancellation are possible.

Side effects after use of candles

  • Local reactions: vagina itch, irritation mucous vaginas.
  • Allergic reactions: urticaria, skin rash.

Side effects after use of tablets

  • Reactions from nervous activity: dizziness, drowsiness, paresthesias, headache, excitability, alarm, sleeplessness, weakness, reversible increase in intracranial pressure.
  • Reactions from a metabolism: anorexia, intolerance of alcohol, appetite strengthening, lipidemia.
  • Reactions from digestion: nausea, diarrhea, an abdominal pain, dyspepsia, disturbance of work of a liver, a lock, vomiting, a dysgeusia, dryness in a mouth, change of coloring of language, abdominal distention, toxic hepatitis, jaundice, increase in activity of liver enzymes, cholestatic hepatitis, cirrhosis, gepatonekroz, a liver failure.
  • Reactions from a musculoskeletal system: muscle and joints pains.
  • Reactions from breath: bleeding from a nose.
  • Reactions from skin: dermatitis, alopecia, erythema, itch, xeroderma, rash, inflow, acute exanthematous pustulez generalized type, photosensitization.
  • Reactions from blood circulation: orthostatic hypotension.
  • Reactions from the hormonal sphere: deficit of function of adrenal glands, a gynecomastia, frustration of a menstrual cycle, temporary lowering of content of testosterone in blood is not excluded (this indicator returns to normal within a day after reception).
  • Reactions from datas of laboratory: decrease in quantity thrombocytopenia.
  • Reactions from touch bodies: fear of a sunlight.
  • Reactions from the sexual sphere: azoospermism, erectile dysfunction.
  • Reactions from immunity: urticaria, rash, Quincke's edema, acute anaphylaxis, pseudoanaphylactic shock.
  • Reactions of the general character: peripheral hypostasis, fever, fever.

Application instruction of Ketokonazol (Way and dosage)

Cream Ketokonazol, application instruction

At treatment of a dermatomycosis of skin, an epidermophitia (feet, brushes and inguinal area), a chromophytosis and candidiasis of skin cream with ketokonazoly is applied on struck also by surrounding fabrics of times a day.

At treatment of seborrheal dermatitis ointment is applied on the necessary area to 2 times a day, depending on weight of an illness. The maintenance therapy at this pathology is carried out to two weekly. Treatment is continued within several more days after stopping of symptoms of an illness or fixing of negative takes of mycologic research of skin.

Duration of treatment is determined by the attending physician. The standard duration of treatment by cream at an inguinal epidermophitia makes 15-30 days, at a skin dermatomycosis – 20-30 days, at a chromophytosis – 15-20 days, at an epidermophitia of feet and brushes – 30-45 days, at seborrheal dermatitis – 15-30 days, at skin candidiasis – 15-20 days,

The instruction on candles

Candles it is applied intravaginalno. In advance having exempted a candle from packaging, it is entered into a vagina as it is possible more deeply in horizontal position. Use one candle a day for 3-5 days depending on disease severity.
At treatment of chronic candidiasis treatment is carried out within 10 days with preservation of the specified frequency rate of reception.

Tablets Ketokonazol, application instruction

Tablets Ketokonazol apply orally during reception of food.

To children weighing more than 30 kg and adult 200 mg recommend to take medicine of times a day. Treatment duration at multi-colored herpes makes 10 days, at candidiasis of skin and an oral cavity – 15-20 days, at onychomycoses – from 6 months to one year, at dermatomycoses – till 30 days, at system mycoses – 30-60 days.

If essential positive changes during a disease against drug use (on 200 mg a day) are not observed, then it is authorized to raise a daily dosage to 400 mg.

At treatment of vaginal candidiasis the dosage makes 400 mg a day, and reception duration – 5 days. For the warning of fungal infections to patients of adult age appoint 400 mg of drug a day.

Overdose

Overdose when using cream or candles

As these forms of production of drug do not reach a system blood-groove, emergence of signs of overdose is improbable.

At a proglatyvaniye of cream or candles it is necessary to make a gastric lavage and to begin a symptomatic treatment.

Overdose by tablets

At overdose tablets expected strengthening of by-effects. Overdose treatment: gastric lavage, carrying out symptomatic therapy.

Interaction

At use according to the instruction of a candle and cream (ointment) Ketokonazol are almost not soaked up in a system blood stream and interaction with other drugs it is improbable.

Possible medicinal interactions at reception of tablets

At combined use of Ketokonazol with antacids (blockers of H2-histamine receptors, aluminum hydroxide, inhibitors of the pump of protons) absorption of the first of intestines decreases. At the specified combinations it is necessary to control efficiency of treatment by drug and in case of need to make correction of its doses.

At combined use of Ketokonazol with strong activators of an isoenzyme CYP3A4 (Rifabutin, the Isoniazid, Efavirenz, Rifampicin, Phenytoinum, Carbamazepine, Nevirapin) decrease in bioavailability of the first which is capable to develop into considerable lowering of its efficiency is not excluded. If the specified combinations cannot be avoided, then it is necessary to control efficiency of the described drug and in case of need to raise its dose.

At combined use of Ketokonazol with the substances suppressing CYP3A4 isoenzyme (antiviral and other drugs) increase in bioavailability of a ketokonazol is possible. At the specified combinations it is necessary to control a condition of the patient for the purpose of identification of signs of strengthening of action Ketokonazol and if necessary to lower his dose.

At simultaneous use of a tablet Ketokonazol can block CYP3A4 - the mediated transformation of drugs, and also caused by a P-glycoprotein, transport of substances. It leads to increase of concentration of these drugs in blood that in turn causes strengthening of their medical or side effects.

Simultaneous use with Ketokonazol of the following drugs is not recommended: Fentanyl, Tamsulozin, Rifabutin, Carbamazepine, Rivaroksaban, Dazatinib, Trabektedin, Nilotinib, Salmeterol.

With care it is necessary to apply tablets Ketokonazol with the following means: Buprenorphine, Alfentanil, Oxycodone, coumarins, Saksagliptin, Tsilostazol, Digoxin, Repaglinid, Eletriptan, Praziquantel, Ebastin, Dotsetaksel, Bortezomib, Imatinib, Busulfan, Iksabepilon, Erlotinib, Trimetreksat, Alprazolam, Lapatinib, periwinkle alkaloids, Buspiron, Aripiprazol, Midazolam, Brotiozolam, Haloperidol, Perospiron, Ramelteron, Kvetiapin, Risperidon, Indinavir, Maravirok, Nadololum, Sakvinavir, Aliskiren, Verapamil, Budesonid, Aprepitant, Cyclosporine, Tsiklesonid, Dexamethasone, Methylprednisolonum, Flutikazon, Takrolimus, Sirolimus, Atorvastatin, Temsirolimus, Reboksetin, Imidafenatsin, Fezoterodin, Solifenatsin, Mozavaptan, Sildenafil, Tadalfil, Tolterodin, Tsinakaltset, Alitretinoin, Tolvaptan.

Terms of sale

Medicine is sold according to the recipe.

Storage conditions

To store in the dry dark place, at a temperature of 15-25 degrees Celsius. To protect from children.

Period of validity

Three years.

Special instructions

Cream is not intended for use in ophthalmologic practice, it is also recommended to avoid its hit in eyes.

At cream use directly after prolonged use of outside glucocorticosteroids the irritation of skin for which stopping it is recommended to continue treatment by local glucocorticosteroids in the morning is not excluded, and to apply cream with ketokonazoly in the evening. Within 3 next weeks it is necessary to lower a corticosteroid dose before its full cancellation.

At a fungal infection of pilar part of the head it will be perhaps more preferable to use shampoo with Ketokonazol.

Seldom or never when using candles development of a local allergy of external genitals in the partner is possible.

For lowering of risk of a palindromia when using candles it is recommended to carry out at the same time therapy at the sexual partner.

Use of candles is capable to reduce reliability of barrier contraception.

Use of the tableted forms of drug is inexpedient at treatment of fungal meningitis because ketokonazol badly passes through through a blood-brain barrier.

Because of high risk of development of a hepatotoxic drug tablets should be used only in special cases in the presence of indications and from appointment of the doctor.
Before therapy by tablets it is necessary to estimate the level of work of a liver for the purpose of an exception of diseases, and during therapy it is regularly necessary to exercise control of indicators of blood, a condition of kidneys, adrenal glands and a liver not to miss emergence of signs of a hepatotoxic.

If for treatment of diseases of skin glucocorticosteroids were used, then Ketokonazol in tablets appoint only in 14 days after their full cancellation.

Reception of acid drinks increases absorbability of a ketokonazol.

Drug Ketokonazol does not influence ability to management of motor transport.

Analogs

Ketokonazol's analogs: Dermazol, Ketokonazol of DS, Mikozoral, shampoo Ketokonazol, Mikoket, Ketokonazol-Altfarm, Nizoral, Livarol, Oronazol, Perkhotal, Fungavis, Sebozol, Funginok, Fungistab.

Zdravzona

  • Ketokonazol-DS 200 mg No. 10 tabletkimekophar Chemical-Pharmac.Joint
  • Ketokonazol of 200 mg No. 20 to a tabletkizdorovya firm of Ltd company
  • Ketokonazol-Altfarm of 400 mg No. 5 of a candle vaginalnyealtfarm Ltd company
  • Horsepower anti-dandruff shampoo with ketokonazoly 250mlloshadinaya force
  • Sulsenum Forte shampoo with ketokonazoly against dandruff 150mlmirra Ltd company
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Apteka24

  • Ketokonazol5
  • Ketokonazol cream of 2% 15gfitofarm (Ukraine, Artemovsk)
  • Ketokonazol cream of 2% 25gfitofarm (Ukraine, Artemovsk)
  • Ketokonazol pessaries of 400 mg No. 5farmeks of Groups of Ltd company (Ukraine, Borispol)
  • Ketokonazol pessaries of 400 mg No. 10farmeks of Groups of Ltd company (Ukraine, Borispol)

BIOSPHERE

  • Ketokonazol of 150 ml shampoo neutral
  • Ketokonazol + Zn of 100 ml shamp. against dandruff
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Section: Dermatological Antifungal
in more detail

Education: Graduated from the Vitebsk state medical university majoring in "Surgery". At university headed Council of students' scientific society. Professional development in 2010 - in "Oncology" and in 2011 - in "A mammology, visual forms of oncology".

Experience: Work in an all-medical network 3 years the surgeon (The Vitebsk hospital of an emergency medical service, Lioznensky TsRB) and in combination the regional oncologist and the traumatologist. Work farm the representative within a year in the Rubicon company.

Provided 3 improvement suggestions on the subject "Optimization of an Antibioticotherapia depending on Species Composition of Microflora", 2 works took prizes in a republican competition review of student's scientific works (1 and 3 categories).
PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use Ketokonazol surely consult with the attending physician.