Terbinafine Canon

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Terbinafine Canon: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Terbinafine Canon

ATX code: D01AE15; D01BA02

Active ingredient: terbinafine (Terbinafine)

Producer: CJSC "Kanonfarma Production" (Russia); CJSC "Raduga Production" (Russia)

Description and photo update: 2020-06-02

Prices in pharmacies: from 108 rubles.

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Gel for external use 1% Terbinafine Canon

Terbinafine Canon is an antifungal drug of the allylamine group.

Release form and composition

tablets (125 and 250 mg): round, flat-cylindrical, beveled, white with a yellow tinge or white, a dividing line is applied on one side (in blisters: 7 or 10 pcs., in a cardboard box 1, 2, 3 or 4 packs; 14 pcs., In a cardboard box 1 or 2 packs);
gel for external use 1%: a homogeneous mass of white or almost white color (15 g each in aluminum tubes, in a cardboard box 1 tube).

Each pack also contains instructions for the use of Terbinafine Canon.

1 tablet contains:

active substance: terbinafine hydrochloride - 140.7 or 281.4 mg, which is equivalent to 125 and 250 mg of terbinafine, respectively;
auxiliary components: croscarmellose sodium, calcium stearate, hyprolose (hydroxypropyl cellulose), colloidal silicon dioxide, microcrystalline cellulose.

100 g of gel contains:

active substance: terbinafine hydrochloride - 1125 mg, which corresponds to 1000 mg of terbinafine;
auxiliary components: ethanol (ethyl alcohol 96%), benzyl alcohol, isopropyl myristate, butylhydroxytoluene, carbomer (Carbopol Ultrez 10 NF), trolamine (triethanolamine), polysorbate 20, purified water.

Pharmacological properties

Pharmacodynamics

Terbinafine Canon is an antifungal drug. Its active substance, terbinafine, belongs to the group of allylamines and has a wide spectrum of action against fungi that cause diseases of the skin, nails and hair. The mechanism of action of terbinafine is due to its ability to specifically suppress the early stage of sterol synthesis in the fungal cell. This occurs as a result of inhibition of squalene epoxidase, an enzyme in the cell membrane of the fungus that does not belong to the cytochrome P _{450 system}. The death of a fungal cell is associated with the appearance of ergosterol deficiency and intracellular accumulation of squalene.

Dermatophytes are sensitive to terbinafine, including the fungi Trichophyton (T. rubrum, T. verrucosum, T. mentagrophytes, T. Tonsurans, T. violaceum), Epidermophyton floccosum, Microsporum canis, yeast fungi of the genus Pityrosporum and Candida (including C. albicans).

In low concentrations, Terbinafine Canon has a fungicidal effect against dermatophytes, individual dimorphic and mold fungi.

Depending on the type of yeast, it exhibits fungicidal or fungistatic activity.

Oral administration of terbinafine creates concentrations in the skin, nails and hair that provide a fungicidal effect.

Due to the absence of the effect of terbinafine on the cytochrome P _{450 system, the} drug does not affect the metabolism of hormones and other drugs.

Pharmacokinetics

After taking the pill, more than 70% of terbinafine is absorbed inside. The absolute bioavailability is about 50%, it is due to the effect of the first pass or presystemic elimination. The maximum concentration (C _max) of terbinafine in plasma against the background of a single dose of 250 mg is achieved after 1.5 hours and is 0.0013 mg / ml. With the systematic administration of tablets C _max terbinafine increases by about 25%, and AUC (area under the concentration-time curve) - 2.3 times. The effective half-life (T _1/2) is 30 hours.

With simultaneous ingestion of food, the bioavailability of the drug is not significantly impaired (AUC increases by less than 20%), therefore, dose adjustment is not required.

Plasma protein binding - 99%.

It quickly penetrates into the dermal layer of the skin, concentrating in the lipophilic stratum corneum, and into the secretion of the sebaceous glands. It accumulates in high concentrations in the skin, hair and hair follicles rich in sebaceous glands. After several weeks of therapy, it penetrates the nail plate.

Terbinafine is excreted in breast milk.

It is metabolized rapidly, mainly with the participation of cytochrome P ₄₅₀ isoenzymes with the formation of metabolites that do not have antifungal activity. In the biotransformation of terbinafine, isoenzymes such as CYP1A2, CYP3A4, CYP2C9, CYP2C8 and CYP2C19 play a major role.

It is excreted mainly through the kidneys, including in the form of metabolites.

For repeated administration of terbinafine, accompanied by an increase in serum concentration, three-phase elimination with a final T _{1/2 of} about 396 hours is characteristic.

The patient's age does not affect the equilibrium plasma concentration of terbinafine.

In case of impaired renal function with creatinine clearance (CC) less than 50 ml / min and liver disease, terbinafine clearance may decrease by 50%.

When applied topically, absorption is less than 5%, therefore the systemic effect of Terbinafine Canon in the form of a gel is insignificant.

Indications for use

Pills

The use of Terbinafine Canon tablets is indicated for the treatment of mycoses caused by microorganisms sensitive to the drug, such as:

onychomycosis caused by dermatophytes;
mycoses of the scalp;
fungal infections of the skin: dermatomycosis of the trunk, legs, feet, yeast infections of the skin caused by fungi of the genus Candida, in cases where the appropriateness of oral therapy is due to the localization, prevalence and severity of the infection.

Gel for external use

The use of Terbinafine Canon gel is indicated for the prevention and treatment of fungal infections of the skin (mycoses of the feet, inguinal epidermophytosis, fungal lesions of the smooth skin of the body) caused by dermatophytes such as Trichophyton (including T. rubrum, T. mentagrophytes, T. Violaceum, T. verrucosum), Microsporum canis and Epidermophyton floccosum.

In addition, the gel is used to treat pityriasis versicolor caused by Pityrosporum orbiculare (Malassezia furfur).

Contraindications

Absolute contraindications to the use of Terbinafine Canon in both dosage forms are breastfeeding and hypersensitivity to the components of the drug.

In addition, there are additional contraindications for certain forms of Terbinafine Canon.

Pills

Absolute contraindications:

liver disease in a chronic, severe or active form;
impaired renal function (CC less than 50 ml / min or serum creatinine concentration more than 300 μmol / l);
age up to 3 years and the child's body weight is less than 20 kg.

Pills should be taken with caution in patients with impaired liver function, inhibition of bone marrow hematopoiesis, cutaneous lupus erythematosus, systemic lupus erythematosus, psoriasis, during pregnancy.

Gel for external use

The use of Terbinafine Canon is contraindicated in patients under the age of 18 years.

The drug should be applied with caution to areas of the body with impaired skin integrity, during pregnancy.

Terbinafine Canon, instructions for use: method and dosage

Pills

Terbinafine Canon tablets are taken orally with a small amount of water, preferably at the same time, regardless of the meal.

The doctor prescribes the duration of treatment, taking into account the clinical indications and the severity of the course of the disease.

Recommended dosage:

adults and children over 3 years old with a body weight of more than 40 kg: 250 mg once a day;
children over 3 years old with a body weight of 20 to 40 kg: 125 mg once a day.

Recommended duration of treatment for adults:

dermatomycosis of the feet (interdigital, plantar or sock-like): 14–42 days;
dermatomycosis of the legs and trunk, skin candidiasis: 14–28 days;
mycosis of the scalp: 28 days;
onychomycosis of the hands: usually 42 days; in some cases - a longer course of therapy (but not more than 84 days);
onychomycosis of the feet: usually - 84 days, with a reduced rate of nail growth - a longer course of therapy. To assess the clinical effect, a period is required for the regrowth of a healthy nail, therefore, the degree of its optimality can be observed after mycological cure and discontinuation of therapy.

It should be borne in mind that the complete disappearance of the symptoms of infection and related complaints usually occurs some time after mycological cure.

For elderly patients, dose adjustment of Terbinafine Canon is not required in cases where they do not have concomitant hepatic or renal dysfunction.

Gel for external use

Gel Terbinafin Canon is applied externally by applying and lightly rubbing onto previously cleaned and dried affected areas and adjacent tissues. Frequency rate of application - 1 time per day.

When treating infections localized in the gluteal and inguinal folds, under the mammary glands, between the fingers and accompanied by diaper rash, after applying the drug, these areas can be covered with gauze, including at night.

The period of treatment depends on the clinical indication and the severity of the disease.

The recommended duration of the course of therapy for dermatomycosis of the trunk, legs, feet, versicolor lichen is 7 days.

The severity of clinical manifestations usually begins to decrease after several days of gel application. It should be borne in mind that irregularity of procedures or premature termination of treatment may cause recurrence of the infection.

If after 14 days of using the gel there are no signs of positive dynamics or the symptoms are aggravated, you should consult a doctor to clarify the diagnosis.

Elderly patients do not need to adjust the dosage regimen of Terbinafine Canon.

Side effects

In general, the tolerability of Terbinafine Canon is good. Adverse events were mild or moderate and were transient. The side effects listed below were observed in the course of clinical trials / in the post-registration period.

Adverse reactions are classified as follows: very often (≥ 1/10); often (from ≥ 1/100 to <1/10); infrequently (from ≥ 1/1000 to <1/100); rarely (from ≥ 1/10 000 to <1/1000); very rare (<1/10 000, including single messages); the frequency has not been established (it is not possible, based on the available data, to establish the frequency of the development of side effects).

Pills

on the part of the immune system: very rarely - angioedema and other anaphylactoid reactions, exacerbation or appearance of cutaneous and systemic lupus erythematosus; frequency not established - anaphylactic reactions, a syndrome similar to serum sickness;
on the part of the blood and lymphatic system: infrequently - anemia; very rarely - pancytopenia, neutropenia, agranulocytosis, thrombocytopenia;
from the nervous system: very often - headache; often - a transient violation of taste (up to a complete loss of taste), dizziness; infrequently - hypesthesia, paresthesia; very rarely - exhaustion; the frequency is not established - a decrease or loss of smell (including over a long period);
on the part of the psyche: often - depression; infrequently - anxiety;
on the part of the skin and subcutaneous tissues: very often - skin rash, urticaria; infrequently - photosensitivity; very rarely - toxic skin rash, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis, toxic epidermal necrolysis, erythema multiforme, bullous dermatitis, alopecia, exfoliative dermatitis, psoriasis-like rashes, exacerbation of psoriasis; frequency not established - drug rash with eosinophilia and systemic symptoms (fever, rash, edema, swollen lymph nodes);
from the gastrointestinal tract: very often - decreased appetite, nausea, bloating, dyspepsia, diarrhea, abdominal pain of a mild nature; frequency not established - pancreatitis;
from the liver and biliary tract: rarely - hepatobiliary dysfunction (mainly of cholestatic nature), liver failure (more often in patients with serious concomitant systemic diseases; causal relationship has not been established), cholestasis, hepatitis, jaundice, increased liver transaminase activity; very rarely - severe hepatic failure requiring liver transplantation (including deaths);
on the part of the organ of vision: infrequently - visual impairment; frequency has not been established - decreased visual acuity, blurred vision;
from the organ of hearing and labyrinth disorders: infrequently - tinnitus; frequency not established - hearing impairment, hearing loss;
from the musculoskeletal and connective tissue: very often - myalgia, arthralgia; frequency not established - rhabdomyolysis;
from the side of the vessels: the frequency is not established - vasculitis;
general disorders: often - feeling tired; infrequently - an increase in body temperature; frequency not established - flu-like syndrome;
laboratory and instrumental disorders: infrequently - a decrease in body weight (secondary to a violation of taste); the frequency has not been established - an increase in the activity of creatine phosphokinase in the blood serum.

Gel for external use

from the immune system: very rarely - hypersensitivity reactions;
on the part of the organ of vision: rarely - eye irritation;
from the skin and subcutaneous tissues: often - itching, peeling of the skin; infrequently - burning sensation of the skin, crusting, skin damage, skin lesions, erythema, pigmentation disorders; rarely - contact dermatitis, dry skin, eczema; very rarely - rash;
general disorders: infrequently - pain, pain and / or irritation at the site of application; rarely - exacerbation of symptoms.

Overdose

In case of an overdose of terbinafine, nausea, epigastric pain, headache, and dizziness occur. The same symptoms are observed in case of accidental ingestion of the gel.

With external use of Terbinafine Canon, cases of overdose were not recorded, since the absorption of terbinafine when applied topically is less than 5%.

If an overdose is suspected, an immediate gastric lavage is performed, and activated charcoal is prescribed. Shows careful monitoring of the patient's condition, the appointment of symptomatic and supportive therapy.

special instructions

When prescribing Terbinafine Canon in the form of tablets, the doctor should analyze the patient's liver function and inform about the increased risk of a relapse of the disease if the drug is taken irregularly or the treatment is stopped early.

It should be borne in mind that all patients are at risk of hepatotoxicity, including those without prior liver dysfunction. Therefore, 28–42 days after the start of treatment, it is recommended to periodically examine the state of the liver during the entire course of therapy. In case of an increase in the activity of liver transaminases, treatment should be stopped immediately.

Terbinafine Canon is generally well tolerated. The resulting side effects are usually transient and mild to moderate.

Patients should be aware that if persistent nausea, vomiting, loss of appetite, fatigue, pain in the right hypochondrium, jaundice, dark urine or light stool appear against the background of the use of Terbinafine Canon, it is necessary to stop taking the pills and immediately consult a doctor. Such symptoms require a liver function test.

In cases when, against the background of the use of tablets, qualitative or quantitative changes in the blood corpuscles occur, the dose of the drug should be reduced and the cause of the disorders should be established. If necessary, it is possible to consider the issue of drug withdrawal.

Terbinafine Canon in the form of a gel should not be applied to the face and allowed to get into the eyes. If the drug accidentally gets into your eyes, rinse them immediately with running water. In case of persistent irritation, you should consult an ophthalmologist.

There is a risk of developing local allergic reactions (contact dermatitis) or irritation of the mucous membranes and eyes due to the content of butylhydroxytoluene in the gel. In addition, ethanol is present in the gel as an auxiliary component, therefore, when applied to damaged skin areas, care should be taken, since alcohol can cause irritation.

When applying the gel, in rare cases, hypersensitivity reactions in the form of a skin rash may occur, requiring discontinuation of therapy.

It should be borne in mind that against the background of the use of the gel, an aggravation of the course of the fungal infection is possible.

Influence on the ability to drive vehicles and complex mechanisms

In connection with the possible development of an undesirable phenomenon on the part of the nervous system in the form of dizziness, patients during the period of taking the pills are advised to be careful when driving or working with complex mechanisms.

Application during pregnancy and lactation

The appointment of Terbinafine Canon during breastfeeding is contraindicated.

During pregnancy, the use of tablets and gel is allowed only in cases where, in the opinion of the doctor, the expected benefit from therapy to the mother outweighs the potential risk to the fetus.

The results of experimental studies suggest that there is no toxic effect of terbinafine on the fetus and no adverse effects on fertility.

Pediatric use

The use of Terbinafine Canon is contraindicated in the form of tablets under the age of 3 years (with a body weight of less than 20 kg), in the form of a gel - under the age of 18.

With impaired renal function

The use of Terbinafine Canon in the form of tablets is contraindicated for impaired renal function (CC less than 50 ml / min or serum creatinine concentration of more than 300 μmol / l).

For violations of liver function

The use of Terbinafine Canon in the form of tablets is contraindicated for liver diseases in a chronic, severe or active form.

With caution, Terbinafine Canon tablets should be prescribed in the presence of liver dysfunction.

Use in the elderly

When using Terbinafine Canon for the treatment of elderly patients, dose adjustment is not required.

Drug interactions

inducers and inhibitors of cytochrome P ₄₅₀: when terbinafine interacts with drugs that are inducers of metabolism, it is possible to accelerate its plasma clearance, with inhibitors of cytochrome P ₄₅₀ - to slow down its plasma clearance. In this regard, if such a combination is necessary, it is recommended to carry out an appropriate correction of the terbinafine dosage regimen;
cimetidine: helps to reduce the clearance of terbinafine by 33%, increase its concentration in plasma and enhance the effect of the drug;
fluconazole, ketoconazole, amiodarone: against the background of concomitant therapy with these or other agents that inhibit the isoenzymes CYP2C9 and CYP3A4, the exposure of terbinafine increases by about 60%;
rifampicin: combination with rifampicin increases terbinafine clearance by 100%, a decrease in its concentration in plasma leads to a weakening of the drug's effect;
beta-blockers, tricyclic antidepressants, selective serotonin reuptake inhibitors, monoamine oxidase inhibitors (type B), class 1A, 1B and 1C antiarrhythmic drugs: terbinafine inhibits the metabolism of these and other drugs with a small range of therapeutic concentrations, the metabolism of which is mediated mainly by C2D6. Their interaction can be accompanied by clinically significant consequences;
desipramine: reduces its clearance by 82%;
caffeine: the clearance of caffeine (administered intravenously) decreases by 19%;
cyclosporine: increases its clearance by 15%;
oral contraceptives: the combination with oral contraceptives may be accompanied by menstrual irregularities;
phenazone, digoxin: the clearance of these funds is not violated;
fluconazole, zidovudine, theophylline, trimethoprim, sulfamethoxazole: no clinically significant interactions with each of these drugs have been established.

Analogs

Terbinafine Canon analogs are Terbinafine, Terbinafine Sandoz, Terbinafin-Teva, Atifin, Binafin, Lamisil, Lamisil Dermgel, Lamisil Uno, Lamitel, Lamifungin, Mikonorm, Tebikur, Terbized-Ajio, Terbiksonil-Serbikon, Exifin, Fungoterbin, etc.

Terms and conditions of storage

Keep out of the reach of children.

Store at temperatures up to 25 ° C.

Shelf life: tablets - 4 years; gel for external use - 3 years.

Terms of dispensing from pharmacies

The tablets are available with a prescription and the gel without a prescription.

Reviews about Terbinafine Canon

The few reviews about Terbinafine Canon are positive. Patients, pointing out the effectiveness of the drug in the form of tablets, place particular emphasis on the need to take them regularly for a period sufficient to cure fungal infections of the nails of the hands. Otherwise, the likelihood of relapse is inevitable and the resumed course of therapy may be longer.

Price for Terbinafine Canon in pharmacies

The price of Terbinafine Canon in the form of tablets with a dosage of 250 mg per pack containing 10 pcs. Can range from 132 rubles, 14 pcs. - from 199 rubles.

Terbinafine Canon: prices in online pharmacies

Drug name

Price

Pharmacy

Terbinafine Canon 250 mg tablets 10 pcs.

108 RUB

Buy

Terbinafine Canon 250mg tablets 10 pcs.

130 RUB

Buy

Terbinafine Canon gel for external use approx. 1% tube 15g

171 r

Buy

Terbinafine Canon 1% gel for external use 15 g 1 pc.

171 r

Buy

Terbinafine Canon 250 mg tablets 14 pcs.

209 RUB

Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!