Terbinafin pills 250mg, 30pcs

Composition

Active ingredient:  terbinafine hydrochloride 281.25 mg (corresponding to 250 mg of terbinafine base); Excipients:  colloidal silicon dioxide 3.9 mg, magnesium stearate 3.9 mg, hypromellose 11.7 mg, microcrystalline cellulose 44.4 mg, sodium carboxymethyl starch, type ” A ” 44.85 mg

Pharmacological action

Terbinafine belongs to the group of allylamines, has a wide spectrum of antifungal action. In low concentrations, it has a fungicidal effect on dermatophytes Trychophyton spp. (T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T. violaceum), Microsporum canis, Epidermophyton floccosum, mold fungi (eg. Scopulariopsis brevicaulis), yeast fungi, mainly Candida albicans. For fungi Candida spp. and their mycelial forms have a fungicidal or fungistatic effect, depending on the type of fungus. Terbinafine disrupts the early stage of biosynthesis of the main component of the fungal cell membrane, ergosterol, by inhibiting the squalene oxidase enzyme. When administered orally, it is not effective in the treatment of multicolored lichen caused by Pityrosporum ovale, Pityrosporum orbiculare, Malassezia furfur. Pharmacokinetic Sin oral use, more than 70% is well absorbed, the absolute bioavailability due to the “first pass” effect is about 50%. After a single oral dose of 250 mg, the time to reach the maximum plasma concentration (Cmax) is about 1.5 hours; the maximum concentration (Cmax – is 1.3 mcg / ml. The area under the concentration-time curve (AUC) is 4.56 mcgh/ml, and the AUC increases by 20% when taken concomitantly with food. With prolonged use, Cmax increases by 25%, AUC-by 2.3 times. The effective half-life (T 1/2) is about 30 hours, the terminal T 1/2 is 200-400 hours (indicates long-term elimination from the skin and adipose tissue). The equilibrium concentration (Css) is independent of age. The concentration of terbinafine in plasma does not depend on gender. Binding to plasma proteins is more than 99%. Quickly distributed in the tissues, penetrates the dermal layer of the skin and nail plates. Penetrates the secret of the sebaceous glands, and accumulates in high concentrations in the hair follicles, hair, skin and subcutaneous tissue. Undergoes significant metabolism, the resulting metabolites do not have antifungal activity. 70% are excreted by the kidneys. It does not accumulate in the body. The age of patients does not affect the pharmacokinetics of terbinafine, but elimination may decrease with liver and kidney damage, leading to high concentrations of terbinafine in the blood. It is excreted in breast milk.

Indications

Mycoses of the scalp (trichophytosis, microsporia). – Fungal diseases of the skin and nails (onychomycosis) caused by Trychophyton spp. (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaccum), Microsporum spp. (M. canis, M. gypseum) and Epidermophyton floccosum. – Severe, widespread dermatomycosis of smooth skin of the trunk and limbs, requiring systemic treatment. – Candidiasis of the skin and mucous membranes.

Use during pregnancy and lactation

There are no data on the safety of using terbinafine during pregnancy. Therefore, terbinafine should only be used during pregnancy if the intended benefit to the mother outweighs the possible risk to the fetus. Lactation periodit Erbinafine is excreted in breast milk. Its use during breastfeeding is contraindicated.

Contraindications

• Hypersensitivity to the Active ingredient or to any of the excipients;
• Acute or chronic liver diseases;
• Children under 2 years of age (efficacy and safety have not been established);
• Lactation period.

With caution:  pregnancy; kidney failure; alcoholism, suppression of bone marrow hematopoiesis, tumors, metabolic diseases, occlusive vascular diseases of the extremities.

Side effects

From the digestive tract:  often: feeling of fullness of the stomach, nausea, abdominal pain, diarrhea, decreased appetite; in isolated cases (0.1-1%)-violation of taste sensations, including their loss (recovery occurs within a few weeks after stopping treatment); rarely (0.01 – 0.1%) – hepatotoxic effect (increased activity of “liver” enzymes, liver failure). From the central nervous system:  often: headache, dizziness. From the hematopoietic system:  very rare (From the immune system:  rare: anaphylactoid reactions, including angioedema, exacerbation of systemic lupus erythematosus. Skin and subcutaneous tissue disorders:  often: rash, urticaria; very rare: psoriasis-like skin rashes, exacerbation of psoriasis, Stevens-Johnson syndrome, toxic epidermal necrolysis, hair loss, acute generalized exanthematous pustulosis. Musculoskeletal and connective tissue disorders:  common: arthralgia, myalgia. Common disorders:  very rare: fatigue.

Interaction

Inhibits the CYP2D6 isoenzyme and disrupts the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (for example, desipramine, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmics (flecainide, propafenone), monoamine oxidase B inhibitors (for example, selegiline) and antipsychotics (for example, chlorpromazine, haloperidol) means.

Drugs that are inducers of cytochrome P450 isoenzymes (for example, rifampicin) can accelerate the metabolism and elimination of terbinafine from the body. Drugs that inhibit cytochrome P450 isoenzymes (for example, cimetidine) can slow down the metabolism and elimination of terbinafine from the body. Terbinafine dosage adjustment may be required when these drugs are used concomitantly.

Menstrual disorders may occur when taking terbinafine and oral contraceptives at the same time. Terbinafine reduces the clearance of caffeine by 21% and prolongs its half-life by 31%. It does not affect the clearance of phenazone, digoxin, or warfarin.

When combined with ethanol or drugs that have a hepatotoxic effect, there is a risk of developing drug-induced liver damage.

How to take, course of use and dosage

For adults:

Inside, after eating. The usual dose is 250 mg once a day.

Children over 3 years of age:

With a body weight of 20 to 40 kg-125 mg once a day.

With a body weight of more than 40 kg-250 mg once a day.

The duration of the course of treatment and the dosage regimen are determined individually and depend on the localization of the process and the severity of the disease.

Onychomycosis:  The average duration of therapy is 6-12 weeks. If the nails of the fingers and feet are affected (with the exception of the big toe), or if the patient is young, the duration of treatment may be less than 12 weeks. For a big toe infection, a 3-month course of treatment is usually sufficient.

Some patients who have a reduced rate of nail growth may require a longer treatment period.

Fungal skin infections:  the duration of treatment for interdigital, plantar or “sock” localization of infection is 2-6 weeks; for mycoses of other parts of the body: legs – 2-4 weeks, trunk – 2-4 weeks; for mycoses caused by fungi of the genus Candida – 2-4 weeks; for mycoses of the scalp caused by fungi of the genus Microsporum – more than 4 weeks.

The duration of treatment for mycoses of the scalp is about 4 weeks, if infected with Microsporum canis-it can be longer.

Elderly patients are prescribed the drug in the same doses as adults.

Patients with hepatic or renal insufficiency – 125 mg once a day.

Overdose

Symptoms:  nausea, vomiting, headache, dizziness, pain in the epigastric region, in the lower abdomen, frequent urination. Treatment: gastric lavage followed by the use of activated charcoal and / or symptomatic therapy.

Special instructions

Irregular use or early termination of treatment increases the risk of relapse.

The duration of therapy may also be affected by factors such as the presence of concomitant diseases, the condition of nails with onychomycosis at the beginning of the course of treatment.

If there is no improvement in the condition after 2 weeks of treatment for a skin infection, it is necessary to re-determine the causative agent of the disease and its sensitivity to the drug.

Systemic use in onychomycosis is justified only in the case of total damage to most nails, the presence of pronounced subungual hyperkeratosis, and the ineffectiveness of previous local therapy.

In the treatment of onychomycosis, a laboratory-confirmed clinical response is usually observed several months after mycological treatment and discontinuation of treatment, due to the rate of regrowth of a healthy nail.

Removal of nail plates in the treatment of onychomycosis of the hands for 3 weeks and onychomycosis of the feet for 6 weeks is not required.

In the presence of liver disease, the clearance of terbinafine may be reduced. During treatment, it is necessary to monitor the activity of “hepatic” transaminases in the blood serum.

In rare cases, cholestasis and hepatitis occur after 3 months of treatment. If signs of impaired liver function appear (weakness, persistent nausea, decreased appetite, excessive abdominal pain, jaundice, dark urine or discolored stools), the drug should be discontinued.

Prescribing terbinafine to patients with psoriasis requires caution, because in very rare cases, terbinafine can provoke an exacerbation of psoriasis.

When treating with terbinafine, general hygiene rules should be observed to prevent the possibility of re-infection through underwear and shoes. During the course of treatment (after 2 weeks) and at the end of it, it is necessary to perform antifungal treatment of shoes, socks and stockings.

Influence on the ability to drive motor vehicles and manage mechanisms

There are no data on the effect of Terbinafine on the ability to drive vehicles and mechanisms.

Active ingredient

Terbinafine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Fungus, Scalp Fungus, Skin Fungus, Nail Fungus