Pharmacodynamics sustanon 250 cycle – represents allylamine, which has broad spectrum of activity against fungi which cause diseases of the skin, hair and nails, including dermatophytes such as Trichophyton (eg T.rubrum, T.mentagrophytes, T.tonsurans, T.verrucosum , T.violaceum), Microsporum (eg, .M. Canis), Epidermophyton floccosum , fungi and yeast genus Candida (e.g., Candida albicans) and Pityrosporum. At low concentrations of sustanon 250 cycle has fungicidal activity against dermatophytes, molds and certain dimorphic fungi. Activity against yeast fungi, depending on their type, may be a fungicidal or fungistatic.
sustanon 250 cycle specifically inhibits early step in the biosynthesis of sterols fungal cell. This leads to a deficiency of ergosterol and intracellular accumulation of squalene, which causes death of fungal cells. sustanon 250 cycle action effected by inhibition of the enzyme squalene epoxidase in the cell membrane of the fungus. This enzyme does not belong to the cytochrome P450 system. sustanon 250 cycle has no influence on the metabolism of hormones or other drugs.
When assigning Binafina inside the skin, hair and nails are drug concentration providing fungicidal activity.
After receiving a single oral dose of sustanon 250 cycle 250 mg maximum plasma concentration of the drug achieved in 2 h and was 0.97 g / ml. Poluabsorbtsii period is 0.8 hours; and poluraspredeleniya period – 4.6 hours. Not required correction doses when taken with food. sustanon 250 cycle largely bound to plasma proteins (99%), rapidly penetrates into the dermal layer of the skin, and concentrates in the lipophilic stratum corneum. sustanon 250 cycle is also penetrates the sebum, which results in a high concentration in the hair follicles, the hair and the skin rich in sebaceous glands. We also show that sustanon 250 cycle penetrates the nail plate in the first few weeks after beginning therapy.
sustanon 250 cycle is metabolised rapidly and substantially, with the participation of at least seven isoenzymes of cytochrome P450, with the main role is played isoenzymes CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C19. The resulting biotransformation sustanon 250 cycle metabolites formed without having antifungal activity and can be output primarily with urine. Terminal half-life of the drug 17 hours. Any evidence of drug accumulation in the body is not there. There were no changes Binafina equilibrium plasma concentration, depending on age, but in patients with impaired renal or hepatic function may be slowed rate of excretion of the drug, resulting in higher concentrations of sustanon 250 cycle in plasma. In pharmacokinetic studies, single dose Binafina in patients with concomitant diseases of the liver was shown the possibility of reducing the clearance of the drug by 50%.
Indications for use
onychomycosis caused by fungi dermatophytes;
fungal infections of the skin – treatment of dermatomycoses torso, legs, feet, and yeast infections of the skin caused by fungi of the genus Candida (e.g., Candida albicans) – in cases where localization, the severity or incidence of infection determine the feasibility of oral therapy.
Note: Unlike Binafina topical Binafin pills are not effective in pityriasis versicolor.
: Hypersensitivity to sustanon 250 cycle or any other component, which is a part Binafina.
If during treatment Binafinom patient observed phenomena, suggesting liver dysfunction, such as unexplained persistent nausea, vomiting, lack of appetite, fatigue, jaundice, pain in the right upper quadrant, dark urine or discolored feces, in this case, you should confirm the hepatic origin these symptoms (determination of serum concentrations of ALT, ACT) and cancel the treatment Binafinom. Patients should be warned of the need to consult a doctor in case of he-like symptoms.
As prospective clinical study on a course of Binafina in patients with underlying chronic or active liver disease has not carried out his assignment to this category of patients is not recommended.
Patients with impaired function renal (creatinine clearance less than 50 mL / min or serum creatinine 300 umol / l) should receive half the normal dose.
In in vitro studies, it was found that sustanon 250 cycle inhibits metabolism mediated by the enzyme cytochrome 2D6 (CYP2D6). It is therefore necessary to carry out continuous monitoring of patients receiving simultaneously with Binafinom treatment with drugs predominantly metabolized with the participation of the enzyme, such as tricyclic antidepressants, beta-blockers, selective serotonin reuptake inhibitors and inhibitors of monoamine oxidase type B, in case the drug is used at the same time It has a small range of therapeutic concentrations.
Effects on ability to drive and use machines
The data on the effect of Binafina on ability to drive and work with no mechanisms.
Use during pregnancy and lactation
As clinical experience with Binafina in pregnant women is very limited, the drug should not be used during pregnancy unless the potential therapeutic effect does not exceed the potential risks of therapy.sustanon 250 cycle is excreted in breast milk, therefore women receiving Binafin inside, should not breastfeed.
The interaction with other drugs
Studies conducted in vitro in healthy volunteers show that sustanon 250 cycle has little capacity to inhibit or enhance the clearance of most drugs that are metabolized by the participation of cytochrome P450 (eg, cyclosporine, terfenadine, tolbutamide, triazolam or oral contraceptives ).
The in vitro studies, however it was found that sustanon 250 cycle inhibits CYP2D6-mediated metabolism. These obtained in in vitro experiments, the data may be clinically important for those drugs that preferentially metabolized by this enzyme, such as tricyclic antidepressants, beta-blockers, selective serotonin reuptake inhibitor, and inhibitors of monoamine oxidase type B – in the event that used simultaneously formulation has a small range of therapeutic concentrations. In patients simultaneously taking oral contraceptives Binafin and, in some cases marked irregularity of the menstrual cycle, although the incidence of these disorders remains within the values were observed in patients who use only oral contraceptives. On the other hand, the overall clearance of sustanon 250 cycle may be accelerated by drugs which accelerate metabolism (such as rafampitsin) can be slowed down and drugs that inhibit cytochrome P450 (such as cimetidine). In cases where it is necessary the simultaneous use of these drugs may require doses Binafina adequate correction.
Dosage and administration:
The duration of treatment depends on the indication and the severity of the disease.
Data on the use of the drug in children under 2 years old (body weight which is usually less than 12 kg) – are absent.
The preparation is administered once daily.
Single dose depends on the body weight and is for children weighing less than 20 kg – 62.5 mg (1/4 250 mg tablet or half a tablet of 125 mg); from 20 kg to 40 kg -125 mg (1 tablet of 125 mg, or 1.2 mg tablet, 250); 40 kg -250 mg (1 tablet of 250 mg).
Adults usually prescribed Binafin 1 table. (250 mg) once daily.
Recommended duration of treatment:
Tinea pedis (interdigital, plantar or by type of socks): 2-6 weeks;
Ringworm of the body, legs – 2-4 weeks;
. Skin candidiasis – 2-4 weeks
The complete disappearance of the manifestations of infection and related complaints it can only come a few weeks after mycological cure.
Infections hair and scalp
Recommended duration of treatment:
Mycosis of the scalp: 4 weeks
fungal infections of the scalp mostly seen in children.
duration of effective treatment for most patients Binafinom from 2 to 6 weeks. In onychomycosis brushes in most cases enough to 6 weeks of treatment. In onychomycosis stop in most cases enough to 12 weeks of treatment. Some patients who have a decreased rate of nail growth, may require longer treatment. The optimal clinical effect is seen some months after mycological cure and cessation of therapy.This is determined by the period of time that is required for regrowth of healthy nail.
Use in the elderly
There is no evidence to suggest that elderly patients require a dosage adjustment or change that they have observed side effects that differ from those of younger patients. In the case of use in this age group of the drug in tablets should consider the possibility of concomitant abnormal liver or renal function.
Use in children
In children older than 2 years Binafina tolerability of oral good.
Binafin generally well tolerated. Side effects usually are mild or moderate and transient in nature are. In most cases (with a frequency of 1 to 10%) had symptoms of gastro-intestinal tract (feeling of fullness, loss of appetite, dyspepsia, nausea, mild abdominal pain, diarrhea), not heavy skin reactions (rash, urticaria), muscular -skeletnye reactions (arthralgia, myalgia). With a frequency of 0.1 to 1% mouthfeel violations occur, including loss (recovery occurs within several weeks after cessation of treatment); Occasionally a frequency between 0.01, 1% in relation to the treatment reported Binafinom hepatobiliary disorders (primarily associated with cholestasis, including cases of liver failure). There are reports of liver failure cases, some of which resulted in death or liver transplantation, but in most cases the patients had serious comorbidities and communication of cases of liver failure using Binafina was regarded as doubtful.
There are reports of very rare (with a frequency of less than 0 , 01%) encountered serious skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis, anaphylactoid reactions). If progressive skin rash develops, treatment should be discontinued Binafinom. There are also reports of very rare hematological disorders such as neutropenia, agranulocytosis, thrombocytopenia. There have been reports of rare cases of hair loss, although a causal link with the administration of the drug has not been established.
There have been reports of several cases Binafina overdose (dose taken was 5 g), in which the observed headache, nausea, epigastric pain and dizziness.
Recommended in case of overdose, treatment includes measures to eliminate the drug, primarily by the appointment of activated carbon , gastric lavage, and, where appropriate, use of symptomatic maintenance therapy.