Terbofin Plus

Uses

Fluticasone Propionate is used for the relief of inflammatory and pruritic manifestations of corticosteroid-responsive eczema or dermatitis.

Terbinafine cream is used for the treatment of the following dermatological infections: interdigital tinea pedis (Athlete’s foot), tinea cruris (jock itch) or tinea corporis (ring worm) due to susceptible organisms and planter tinea pedis (mocasin type) due to Trichophyton spp.

Terbinafine tablet is used for the treatment of onychomycosis of the toe nail or finger nail due to dermatophytes and also by non-dermatophyte fungi.

Terbofin Plus is also used to associated treatment for these conditions: Asthma, Bronchostenosis, Skin discomfort, Moderate, severe Chronic Obstructive Pulmonary Disease (COPD)Onychomycosis, Pityriasis versicolor, Sporotrichosis, Tinea Capitis, Tinea Corporis, Tinea Cruris, Tinea Pedis, Cutaneous candidiasis, Severe Tinea Corporis, Severe Tinea Cruris, Severe Tinea Pedis

How Terbofin Plus works

Fluticasone furoate and Fluticasone propionate work through an unknown mechanism to affect the action of various cell types and mediators of inflammation. In vitro experiments show Fluticasone furoate activating glucocorticoid receptors, inhibiting nuclear factor kappa b, and inhibiting lung eosinophilia in rats. Fluticasone propionate performs similar activity but is not stated to affect nuclear factor kappa b.

Terbinafine inhibits the enzyme squalene monooxygenase (also called squalene epoxidase), preventing the conversion of squalene to 2,3-oxydosqualene, a step in the synthesis of ergosterol. This inhibition leads to decreased ergosterol, which would normally be incorporated into the cell wall, and accumulation of squalene.

Generation of a large number of squalene containing vesicles in the cytoplasm may leach other lipids away from, and further weaken, the cell wall.

Dosage

Terbofin Plus dosage

Cream: Apply a thin layer of Fluticasone propionate cream to the affected skin areas once daily.

Ointment: Apply a thin layer of Fluticasone propionate Ointment to the affected skin areas twice daily.

Topical application:

Terbinafine cream to affected areas once or twice daily for 1-2 weeks may be adequate for fungal infections of the skin but certain infections may require oral Terbinafine tablet therapy.Usual duration of treatment of Terbinafine cream:

• In Tinea corporis and Tinea cruris: 1-2 weeks.
• In Tinea pedis: 2-4 weeks (One week of treatment will normally suffice if the cream is applied twice daily.).
• In Cutaneous candidiasis: 1-2 weeks
• In Pityriasis (tinea) versicolor: 2 weeks.

To prevent relapses in fungal infection, treatment should be continued for a adequate length of time. To apply Terbinafine cream clean and dry the affected areas thoroughly and apply the cream once or twice a day to the affected skin and surrounding area in a thin layer and rub in lightly. In the case of intertriginous infections the application may be covered with a gauze strip, especially at night.

Oral administration:

Terbinafine tablet is essential for hair or nail infections:

• The usual oral dose: Terbinafine 250 mg daily for 2 to 12 weeks depending upon the infection.
• Finger nail onychomycosis: Terbinafine 250 mg once daily for 6 weeks.
• Toe nail onychomycosis: Terbinafine 250 mg once daily for 12 weeks.

Side Effects

The fluticasone propionate preparations are usually well tolerated; local burning and pruritus have been reported. If signs of hypersensitivity appear, application should be stopped immediately. Prolonged and intensive treatment with potent corticosteroid preparations may cause local atrophic changes in the skin such as thinning, striae, dilatation of the superficial blood vessels, hypertrichosis and hypopigmentation.

Secondary infection, particularly when occlusive dressings are used or when skin folds are involved and allergic contact dermatitis have also been reported with corticosteroid use. Exacerbation of the signs and symptoms of the dermatoses have been reported with corticosteroid use.

Prolonged use of large amounts of corticosteroids, or treatment of extensive areas, can result in sufficient systemic absorption to produce the features of hypercorticism. This effect is more likely to occur in infants and children, and if occlusive dressings are used. In infants, the napkin may act as an occlusive dressing.

Terbinafine Tablet: Abdominal discomfort, anorexia, nausea, diarrhoea, headache, rash and urticaria occasionally with arthralgia or myalgia. Less frequently taste disturbance. Rarely liver toxicity, photosensitivity, serious skin reactions etc.

Terbinafine Cream: Redness, itching, or stinging; rarely allergic reactions.

Toxicity

Fluticasone furoate administered nasally may be associated with adrenal suppression or an increase in QTc interval though the association has not been well demonstrated in studies. Fluticasone furoate requires no dosage adjustment in renal impairment but must be used in caution in hepatic impairment due to the elimination mechanisms. Fluticasone furoate is not associated with carcinogenicity, mutagenicity, or impairment of fertility. There are no well controlled studies in pregnancy or lactation though animal studies have shown teratogenicity and hypoadrenalism in the offspring of treated mothers and other corticosteroids are known to be excreted in breast milk. Generally, there are no reported adverse effects with fluticasone in pregnancy. Pediatric patients should be given the lowest possible dose and monitored for reduction in growth velocity. There is insufficient evidence to determine whether geriatric patients respond differently to other patients. Systemic exposure may be 27-49% higher in Japanese, Korean, and Chinese patients compared to Caucasian patients. Caution should be exercised in these patients and the benefit and risk should be assessed before deciding on a treatment.

Fluticasone propionate's use in specific populations has not been well studied. Fluticasone propionate is not carcinogenic, mutagenic, or clastogenic, nor did it affect fertility in animal studies. Subcutaneous Fluticasone propionate has been shown to produce teratogenic effects in rats though oral administration does not. Generally, there are no reported adverse effects with fluticasone in pregnancy. Fluticasone propionate in human milk may cause growth suppression, effects on endogenous corticosteroid production, or other effects. Pediatric patients treated with Fluticasone propionate ointment experienced adrenal suppression. Geriatric patients treated with Fluticasone propionate did not show any difference in safety or efficacy compared to other patient groups, though older patients may be more sensitive to adverse effects. There is no difference in the clearance of Fluticasone propionate across genders or race. Patients with hepatic impairment should be closely monitored due to the elimination mechanism.

The subcutaneous LD₅₀ in rats and mice is >2g/kg. The TDLO for women is 210mg/kg/6W.

Overdose data with terbinafine is rare, however symptoms are expected to be nausea, vomiting, abdominal pain, dizziness, rash, frequent urination, and headache. Treat overdose with activated charcoal as well as symptomatic and supportive therapy.

Precaution

Fluticasone propionate has a very low propensity for systemic absorption, nevertheless, prolonged application of high doses to large areas of body surface, especially in infants and small children might lead to adrenal suppression. Children may absorb proportionally larger amounts of topical corticosteroids and thus be more susceptible to systemic toxicity.

The face, more than other areas of the body, may exhibit atropic changes after prolonged treatment with potent topical corticosteroids. This must be borne in mind when treating severe eczema.

Appropriate antimicrobial therapy should be used whenever treating inflammatory lesions which have become infected. Any spread of infection requires withdrawal of topical corticosteroid therapy and systemic administration of antimicrobial agents. Bacterial infection is encouraged by the warm, moist conditions induced by occlusive dressing, and so the skin should be cleansed before a fresh dressing is applied.

Terbifine cream is for external use only. Contact with eyes should be avoided.Good general hygiene is necessary in conjunction with the use of Terbinafine in order to prevent reinfection (eg. from underwear, socks,shoes etc).

Terbinafine tablet is not recommended for patients with chronic or active liver disease. Before prescribing terbinafine, pre-existing liver disease should be assessed. Hepatotoxicity may occur in patients with and without pre-existing liver disease. Pretreatment serum transaminase (ALT and AST) tests are advised for all patients before taking terbinafine tablets.

Interaction

In vivo studies have shown that terbinafine is an inhibitor of the CYP450 2D6 isozyme. Drugs predominantly metabolized by the CYP450 2D6 isozyme include the following drug classes: tricyclic antidepressants, selective serotonin reuptake inhibitors, beta-blockers, antiarrhythmics class 1C (e.g., flecainide and propafenone) and monoamine oxidase inhibitors Type B. Co-administration of terbinafine should be done with careful monitoring and may require a reduction in dose of the 2D6-metabolized drug.

Volume of Distribution

608L at steady state for intravenous administration of Fluticasone furoate. Other reports suggest the mean volume of distribution at steady state is 661L. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 704L following intravenous administration.

The volume of distribution of intravenous Fluticasone propionate is 4.2L/kg. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 577L following intravenous administration.

A single 250mg oral dose of terbinafine has a volume of distribution at steady state of 947.5L or 16.6L/kg.

Elimination Route

Oral terbinafine is >70% absorbed but only 40% bioavailable after first pass metabolism, reaching a C_max of 1µg/mL with a T_max of 2 hours an an AUC of 4.56µg*h/mL. Over the course of a week, 1% topical terbinafine's C_max increases from 949-1049ng/cm²

Half Life

15.1 hours for intranasal Fluticasone furoate and 24 hours for the inhaled formulation. A study of 24 healthy Caucasian males showed a half life of 13.6 hours following intravenous administration and 17.3-23.9 hours followed inhalation.

7.8 hours for intravenous Fluticasone propionate. A study of 24 healthy Caucasian males shows a half life of 14.0 hours following intravenous administration and 10.8 hours following inhalation.

Oral terbinafine has an effective half life of approximately 36 hours. However, the terminal half life ranges from 200-400 hours as it distributes into skin and adipose tissue. 1% topical terbinafine's half life increases over the first seven days from approximately 10-40 hours.

Clearance

57.8L/h for Fluticasone furoate. A study of 24 healthy Caucasian males showed a clearance of 71.8L/h following intravenous administration.

1093mL/min for Fluticasone propionate. A study of 24 healthy Caucasian males showed a clearance of 63.9L/h following intravenous administration.

A single 250mg oral dose of terbinafine has a clearance of 76L/h or 1.11L/h/kg.

Elimination Route

Fluticasone furoate is eliminated ≥90% in the feces and 1-2% in the urine.

Fluticasone propionate is mainly eliminated in the feces with

Pregnancy & Breastfeeding use

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