Terbinafine

Terbinafine is an antimycotic drug with fungicidal activity. It has an impact on most types of fungi that can infect the human body.

In low concentrations, the drug has a fungicidal effect on the activity of dermatophytes with mold fungi, and in addition, certain types of dimorphic fungi. In relation to yeast fungi, it can have not only fungicidal, but also fungistatic effects.

Indications Terbinafine

All forms of drug release can be used for diseases whose development was caused by the action of mold and yeast-like fungi, and in addition to this dermatophytes.

Tablets are used in pathologies with fungal genesis and trimatophytes type trimatophytes (T. Mentagrophytes, T. Violaceum, as well as red trihofiton, T. Verrucosum and triterophytic trihofiton), fluffy microsporum and flape-like epidermofiton, etc. The drug in pills is used for microsporia, athlete's disease, trichophytosis with onychomycosis and candidiasis.

Tablets are often used in cases of intense and common manifestations. To use pills with a pityriasis form of lichen will be ineffective.

The cream is usually prescribed for fungal pathologies caused by the action of Candida, Trichophyton, Fluffy Microsporum, Flaky Epidermophyte and Pityriasis.

Along with this cream with ointment can be used for epidermal lesions caused by the influence of dermatophytes, candidiasis and herpies.

[1], [2], [3]

Release form

The release of drugs produced in tablets with a volume of 0.25 g; A pack may contain 7 or 10 tablets. In addition, it is implemented in such forms: 1% cream for external treatment, spray and ointment.

[4], [5], [6]

Pharmacodynamics

The drug's drug effect develops through the damaging effects on the walls of fungal cells, and in addition to the specific slowing down of the activity of squalene epoxidase (this enzyme is extremely important for the normal activity of the fungal cell wall).

The effect of terbinafine helps to stop the production of ergosterol, the deficiency of which inside the fungal cell leads to an increase in the volume of squalene. As a result, all enzyme systems are inactivated and the cell dies.

The active ingredient of the drug does not affect the hemoprotein P450 system, therefore it does not affect the metabolic processes of hormones or other drugs.

[7], [8], [9], [10], [11]

Pharmacokinetics

After taking the medication inside, its rapid absorption from the gastrointestinal tract develops. Part of the metabolic processes of drugs occur inside the liver, so the values of its bioavailability are reduced to 40%. The use of food has an insignificant effect on the bioavailability indicators, which is why there is no need for a portion adjustment.

Blood values of Cmax are noted after 120 minutes have passed since the use of 0.25 g of the substance. 99% of the drug is synthesized with intraplasma protein.

Indicators of drugs that are optimal for the development of drug exposure are observed inside the epidermis with the subcutaneous layer, hair and nails.

Inside the body, terbinafine hydrochloride is converted into metabolic elements that do not have an antimycotic effect. Most of them are excreted in the urine. The term half-life is 17 hours.

The medication taken does not accumulate.

If a patient has kidney or liver disease, a slowdown in drug conversion may occur. As a result, its indices inside biological fluids increase and the period of circulation of the substance inside the blood is prolonged.

In the case of using the drug locally, a maximum of 5% of the active element penetrates the blood.

[12], [13], [14], [15], [16],

Dosing and administration

Drug regimens.

The duration of the use of tablets is selected by the attending doctor, taking into account the intensity of the disease. Children should use the medication after eating food, 1 time per day. During the selection of 1-fold dosage should also take into account the weight of the child.

Children weighing less than 20 kg are required to use 62.5 mg of the substance; children whose weight is 20-40 kg - 125 mg each; children whose weight is over 40 kg - 0.25 g. Each

Adults need to apply 0.25 g of the substance 1 time per day or 125 mg 2 times a day.

The duration of the therapeutic cycle is determined by the type of disease. In the case of ringworm, affecting the feet, tablets take 0.5-1.5 months.

In the case of ringworms infecting the trunk, limbs or tibia, as well as epidermal candidiasis, therapy lasts 0.5-1 months.

In the case of infections affecting the scalp, therapy lasts 1 month.

During onychomycosis, treatment should continue within 1.5-3 months. Sometimes, if a patient's nails grow too slowly, therapy may be longer. The therapeutic effect is observed after several months from the end of the treatment cycle.

Methods of using medicinal ointment.

Cream or ointment to treat infected areas 1-2 times per day. Before using the medication, it is necessary to clean and dry the affected epidermis. The treatment is done in a thin layer - in addition to the contaminated places, the substance is applied, rubbing a little, and on the adjacent areas. When diaper rash appears on the background of the infection, after treatment with Terbinafin, these areas can be covered with gauze. It is recommended to do this when applying the medication for the night.

The duration of the therapeutic course depends on the type of the disease.

In the case of ringworm in the trunk, extremities or lower legs, as well as candidiasis affecting the epidermis, the drug is applied in the period of 7-14 days.

During depriving a scaly-like character - 14 days.

With ringworm in the area of the feet - 0.5-1 month.

In the case of nail mycosis, the medication is used for a 3-6 month period.

Typically, clinical symptoms subside after the first few days of drug use. It must be borne in mind that in the event of irregular use or premature discontinuation of treatment, a relapse of infection may occur.

If after 14 days of constant use of the cream, the signs of pathology are not weakened, it is necessary to consult a doctor and verify the diagnosis.

Spray should be applied externally - 1-2 times a day.

[20], [21], [22], [23], [24]

Use Terbinafine during pregnancy

During testing, no active teratogenic activity was detected in the active component of the drug. Use of the drug in pregnant women is allowed only in situations where the likely benefits are more expected than the risks of complications for the fetus.

Because the active substance is excreted with milk, breastfeeding at the time of therapy should be canceled.

Contraindications

The main contraindications of tablets:

• hepatic diseases of an active or chronic nature;
• failure of the kidneys in the chronic stage (CC values below 50 ml per minute);
• hypolactasia, lactase deficiency, and glucose-galactose malabsorption;
• severe intolerance to the components of the drug.

With caution, tablets are used in such conditions:

• CKD (KF indicators over 50 ml per minute when performing Reberg test);
• hematopoietic disorders;
• alcoholism;
• endocrine pathologies;
• psoriasis;
• tumors;
• vascular constriction in the limbs;
• SLE or lupus erythematosus.

During the application of terbinafine, it is necessary to closely monitor the work of the kidneys with the liver. To cancel the pill is necessary for the development of such signs:

• nausea, abdominal pain, loss of appetite;
• feeling weak;
• jaundice or darkening of the color of urine;
• light feces.

Local forms of medication are not prescribed for symptoms of allergies and severe intolerance.

Caution in applying the cream or ointment is required for such disorders:

• tumors;
• failure of the liver or kidneys;
• endocrine pathologies;
• alcoholism;
• disorders of hematopoietic processes;
• narrowing of the vascular lumen.

Side effects Terbinafine

Among the side effects when using pills:

• loss of appetite, weakness and pain in the area of epigastria, diarrhea, taste disorder, nausea;
• cholestasis;
• allergy signs;
• decrease in blood indices of neutrophils with platelets.

After local treatment with an ointment or cream, in the areas of application there may be hyperemia, burning or itching. Occasionally, allergy symptoms may occur.

[17], [18], [19]

Overdose

When poisoning with Terbinafine tablets, the patient may experience rashes, headaches, nausea, dizziness, increased urination, vomiting, and pain in the epigastric zone.

Gastric lavage should be performed and activated charcoal should be given to the patient; symptomatic measures are being taken.

If a patient accidentally takes an oral medicinal cream, he may experience dizziness, nausea, pain in the epigastric region and headaches.

At the same time, symptomatic procedures are performed and activated carbon is prescribed.

[25], [26], [27]

Interactions with other drugs

The use of terbinafine can affect the clearance of drugs whose metabolic processes take place with the help of the hemoprotein P450 system. Among them is cyclosporine with tolbutamide and oral contraception.

The drug increases the plasma values of H2-histamine blockers.

The drug inhibits the excretion of rifampicin, and the latter at the same time doubles the performance of Terbinafine clearance.

Women who use oral contraception may experience irregular menstruation cycles.

The drug slows down the activity of CYP2P6 isoenzyme, which interferes with the exchange of SSRIs, tricyclics with antiarrhythmic drugs, and in addition, β-blockers, antipsychotics and MAOI of type B.

The effect of the drug leads to a 21% decrease in the level of caffeine clearance, while the term of its half-life increases by 31%.

The drug does not affect the performance of clearance of warfarin with digoxin and phenazone.

Combination with drugs with hepatotoxic properties, or ethyl alcohol increases the risk of drug damage to the liver.

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Storage conditions

Terbinafine must be kept in a closed place from small children. Temperature values - not higher than 25 ° C.

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Shelf life

Terbinafine is allowed to apply for a 2-year term since the production of the drug.

Application for children

Drugs tablets are not used in children under the age of 3 with a weight of less than 20 kg. Also, when using them, you should carefully observe the designated portion.

Local forms of medication prescribed for children over 12 years of age.

[30], [31], [32], [33], [34]

Analogs

Analogues of the tablet form of the drug are Exifin, Lamican, Binafin with Onyhon, and in addition Miconorm, Terbizil, Terbinafine hydrochloride, etc.

Analogues of drugs for external processing - Terbinoks, Lamitel with Thermicon, Miconorm with Lamisil Uno, Terbinafin-MFF, Terbizil and so on.

[35], [36]

Reviews

Terbinafine tablets generally get good reviews on the forums. They help to eliminate fungal infections and restore the damaged nail structure.

Comments on ointments and creams are also pretty good. There is a high efficiency (for several weeks of therapy completely eliminate fungi and diaper rash), as well as the relatively low price of medication. Of the benefits and there are rare occurrence of adverse symptoms.

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