TERMYKON – Pills
Active material: Terʙinafin
When ATH: D01BA02
CCF: Antifungal agent
ICD-10 codes (testimony): B35.0, B35.1, B35.2, B35.3, B35.4, B35.6, B36.0, B37.2
When CSF: 08.01.02
Manufacturer: Pharmstandard-Leksredstva JSC (Russia)
Pharmaceutical form, composition and packaging
Pills white or white with a yellowish tint, Valium, a facet and Valium.
| 1 tab. | |
| terbinafine hydrochloride | 281.25 mg, |
| that corresponds to the content of terbinafine | 250 mg |
Excipients: sodium starch glycolate, microcrystalline cellulose, lactose, gipromelloza (hydroxypropyl), magnesium stearate, colloidal silicon dioxide (aэrosyl).
7 PC. – packings Valium planimetric (2) – packs cardboard.
Pharmacological action
Antifungal agent, allilamin. It has a wide range of antifungal activity.
It is active against dermatofitov: Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Trichophyton verrucosum, Trichophyton violet, Microspores dog, Epidermophyton floccosum. At low concentrations it has a fungicidal effect on dermatophyte, molds (incl. Aspergillus, Cladosporium, Scopulariopsis brevicaulis) and certain dimorphic fungi. In yeast fungi of the genus Candida (especially Candida albicans) and filamentous forms, depending on the type of, the drug has fungicidal or fungistatic.
Termykon® violates the early stage of the biosynthesis of the main component of the fungus cell membrane ergosterol by inhibiting the enzyme squalene epoxidase. This leads to a deficiency of ergosterol and to an intracellular accumulation of squalene, causing cell death fungus. Step terbinafine accomplished by inhibition of the enzyme squalene epoxidase, located on the cell membrane of the fungus.
If ingestion is not effective in the treatment of multi-colored lichen, called Pityrosporum orbiculare (Malassezia furfur).
Pharmacokinetics
Absorption
After oral administration, the drug is well absorbed from the gastrointestinal tract. Through 0.8 h absorbed half the dose.
After receiving a single dose 250 mg Cmax Terbinafine blood plasma achieved by 1-2 h and is 0.97 ug / ml. Bioavailability is 80%. Eating does not affect the bioavailability of terbinafine.
Distribution
The binding to plasma proteins – 99%.
Through 4.6 half hours after administration of the dose distributed in the body. The drug is rapidly penetrates the dermal layer of the skin and the nail plate. It penetrates sebum, It accumulates in high concentrations in the hair follicles, hair, skin and subcutaneous tissue. Not accumulates in the body.
Terbinafine is excreted in breast milk.
Metabolism
Biotransformed in the liver with the formation of active metabolites.
Deduction
In the form of metabolites in urine output of about 80% the dose, the rest of the – with feces (22%).
Pharmacokinetics in special clinical situations
Age of patients do not affect the pharmacokinetics of terbinafine, however, removal of the drug may be reduced in patients with lesions of the liver or kidneys, resulting in high concentrations of terbinafine blood.
T1/2 is 16-18 no. T1/2 in the terminal phase – 200-400 no.
Testimony
- Fungal infections of the scalp (ringworm, microsporia);
- Fungal infections of the skin and nails, обусловленные Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Trichophyton verrucosum, Trichophyton violet, Microspores dog, Microsporum gypseum and Epidermophyton floccosum;
- Onychomycosis;
- Heavy common ringworm smooth skin of the trunk and extremities, requiring systemic treatment;
- Candidiasis of the skin and mucous membranes.
Dosage regimen
The duration of treatment and dosage regimen is established individually and depends on the location and severity of the disease.
Inside adult the drug is prescribed for 250 mg 1 time / day (postprandial).
At onixomikoze the duration of treatment is about 6-12 weeks. When onychomycosis of hands and feet (except hallux), or in young patients the duration of treatment may be less than 12 weeks. For infections of the big toe is usually sufficient treatment in 3 of the month. In rare cases, the slow rate of nail growth may require longer treatment – to 6 months or more.
At Tinea pedis (interdigital, Plantar or by type of socks) the duration of treatment ranged from 2 to 6 weeks; at dermatomycotic goleneй – from 2 to 4 weeks; at ringworm of the body – 4 of the week; at candidiasis of the skin and mucous membranes from 2 to 4 weeks.
At mycosis of the scalp, вызванном Microsporum canis the recommended duration of treatment – more 4 weeks.
For children weighing from 20 to 40 kg the drug is prescribed in a dose 125 mg (1/2 tab.) 1 time / day, from weighing more than 40 mg – 250 mg 1 time / day. Duration of treatment fungal infections of the scalp is about 4 weeks. In cases, If the agent is Microsporum canis, treatment may be longer.
Elderly patients drug administered in the same doses, as adults.
At severe renal insufficiency (CC<50 ml / min or serum creatinine content >300 mmol / l), at impaired renal function the dose should be reduced 2 times, to Adult – 125 mg 1 time / day.
Side effect
From the digestive system: dyspepsia, decreased appetite, nausea, diarrhea, feeling of fullness, abdominal pain, dysgeusia, including loss (recovery occurs within a few weeks after cessation of treatment); rarely – hepatobiliary disorders (cholestatic jaundice).
On the part of the musculoskeletal system: arthralgia, myalgia.
From the hematopoietic system: agranulocytosis, thrombocytopenia, neutropenia.
Allergic reactions: hives, rash; rarely – toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions, malignant exudative erythema (Stevens-Johnson syndrome).
Contraindications
- Pregnancy;
- Breastfeeding;
- Children up to age 3 s and children weighing up 20 kg;
- Hypersensitivity to the drug.
FROM caution should use the drug inside with renal and / or hepatic insufficiency, alcoholism, suppression of bone marrow hematopoiesis, tumors, metabolic diseases, occlusive vascular diseases of extremities.
Pregnancy and lactation
Experience with the drug Termikon® during pregnancy is limited, therefore its function during pregnancy is contraindicated.
Terbinafine is excreted in breast milk, so if necessary, the appointment during lactation should decide the issue of termination of breastfeeding.
IN experimental studies teratogenic effects of terbinafine is not revealed. So far no reports of any malformations in the application of terbinafine.
Cautions
It should be taken into account, that the irregular use or early termination of the treatment increases the risk of relapse.
Duration of treatment may be determined by the presence of comorbidities, the state of the nails in the beginning of treatment.
If after 2 weeks of treatment Termikonom® no improvement in the state, must re-determine the causative agent and its sensitivity to the drug.
Systemic application in onychomycosis justified only in the case of total destruction of the majority of nail, availability expressed subungual hyperkeratosis, ineffectiveness of previous local therapy. In the treatment of onychomycosis clinical response is usually seen after a few months after mycological cure and cessation of treatment, due to the speed of regrowth of healthy nails. Removal of the nail plate in the treatment of onychomycosis of brushes for 3 weeks and stop for onychomycosis 6 weeks is not required.
During treatment should monitor the activity of liver transaminases in blood serum. In rare cases, through 3 months of treatment developed cholestasis and hepatitis. If any symptoms of liver dysfunction (weakness, persistent nausea, anorexia, stomach ache, jaundice, dark urine or feces colorless), you need to stop the drug.
Special care should be prescribed to patients with psoriasis, because very rarely terbinafine can cause exacerbation of psoriasis.
When drug treatment should follow the general rules of hygiene to prevent the possibility of re-infection through underwear and footwear. During (through 2 Sun.) and at the end of treatment should be performed antifungal treatment of footwear, socks and stockings.
With the development of allergic reactions the drug should be discontinued.
Use in Pediatrics
Termykon® contraindicated for use in children aged 3 years and children weighing up 20 kg.
Effects on ability to drive vehicles and management mechanisms
Terbinafine does not influence the ability to drive vehicles and work performance, require high concentration and speed of psychomotor reactions.
Overdose
Symptoms: nausea, vomiting, Pain in the lower abdomen and epigastric, dizziness.
Treatment: gastric lavage, followed by the appointment of activated carbon and / or symptomatic therapy.
Drug Interactions
Terbinafine inhibits the CYP2D6 isoenzyme and slows the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake blockers (eg, desipramine, fluvoxamine), beta1-adrenoblokatorы (metoprolol, propranolol), antiarrhythmics (flekainid, propafenone), MAO inhibitors type B (eg, selegiline) and antipsychotics (eg, chlorpromazine, haloperidol).
Inducers of cytochrome P450 isoenzymes (eg, rifampicin) can accelerate the excretion from the body of terbinafine, inhibitors of cytochrome P450 isozymes (eg, cimetidine) can slow it down. While the use of these drugs may require dose adjustment tebinafina.
At the same time taking terbinafine and oral contraceptives may be in breach of the menstrual cycle.
Terbinafine decreases the clearance of caffeine on 20% and increases T1/2 na31%.
Terbinafine does not influence the clearance of antipyrine, digoksina, varfarina.
Ethanol and other hepatotoxic drugs, while the use Termikonom® increase the risk of hepatotoxicity.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children, dark place at a temperature no higher than 25 ° C. Shelf life – 3 year.
