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Terbinafine, an antifungal, inhibits biosynthesis of ergosterol, an essential component of fungal cell membrane, via inhibition of squalene epoxidase enzyme. This results in fungal cell death primarily due to the increased membrane permeability mediated by the accumulation of high concentrations of squalene but not due to ergosterol deficiency.
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TERBINAFINE HCl TABLET
BIBEK SINGH MAHATM. PHARM.
Dermatophytes• Dermatophytes (name based on the Greek for 'skin
plants') are a common label for a group of three types of fungus that commonly causes skin disease in animals and humans.
• These anamorphic (asexual or imperfect fungi) genera are: Microsporum, Epidermophyton and Trichophyton. There are about 40 species in these three genera.
TERBINAFINE HCl Tablet TERBINAFINE HCl® contains Terbinafine
hydrochloride. It is a synthetic antifungal and highly
lipophilic in nature. It tends to accumulate in skin, nails and fatty
tissues. Terbinafine is mainly effective on
the dermatophytes group of fungi.
TERBINAFINE HCl Tablet
Terbinafine hydrochloride
FDA approval• On September 28, 2007, the FDA stated that
terbinafine hydrochloride is a new treatment approved for use by children age 4 and up.
• The antifungal can be used to treat ringworm of the scalp, Tinea capitis.
FDA approval treatment
• TERBINAFINE HCl® 250 mg Tablets are often prescribed for the treatment of onychomycosis of the toenail or fingernail due to the dermatophyte Tinea unguium.
• Fungal nail infections are located deep under the nail in the cuticle to which topically applied treatments are unable to penetrate in sufficient amounts.
FDA approval treatment• TERBINAFINE HCl® 250 mg Tablets are used
for the treatment of fungal infections of:1.The groin area. 2.The skin (ringworm). 3.Toe and finger nails (yellow, opaque and
thickened nails). 4.The feet (athlete’s foot).
Pharmacokinetics• Following oral administration, Terbinafine is well
absorbed (>70%) and the bioavailability of Terbinafine tablets as a result of first-pass metabolism is approximately 40%.
• Peak plasma concentrations appear within 2 hours after a single 250 mg dose; the AUC (area under the curve) is approximately 4.56 μg.h/mL.
• An increase in the AUC of Terbinafine of less than 20% is observed when Terbinafine tablets are administered with food.
Pharmacokinetics• In plasma, Terbinafine is >99% bound to plasma
proteins and there are no specific binding sites. Terbinafine is distributed to the sebum and skin.
• The increase in plasma AUC is consistent with an effective half-life of ~36 hours. A terminal half-life of 200-400 hours may represent the slow elimination of Terbinafine from tissues such as skin and adipose.
Mechanism of action• Terbinafine, an antifungal, inhibits biosynthesis of
ergosterol, an essential component of fungal cell membrane, via inhibition of squalene epoxidase enzyme.
• This results in fungal cell death primarily due to the increased membrane permeability mediated by the accumulation of high concentrations of squalene but not due to ergosterol deficiency.
Mechanism of action
• Depending on the concentration of the drug and the fungal species, Test in vitro, Terbinafine may be fungicidal.
Mechanism of action
• Depending on the concentration of the drug and the fungal species, Test in vitro, Terbinafine may be fungicidal.
Therapeutic window of antifungal agents
ergosterol
nucleic acid synthesis
glucan synthesis
chitin synthesis
nucleic acid synthesis
cholesterol
protein synthesis protein synthesis
mannan synthesis
huma fungus
Dosage and Administration• Adults (including the elderly): Duration of
treatment depends on the type of fungal infection and the severity of the infection.
• Fungal infection of the groin area, skin and feet:
TERBINAFINE HCl® 250 mg Tablets, once a day for 2-4 weeks. Some cases of athlete’s foot may require treatment for up to 6 weeks.
• Complete healing of the infection may not occur until several weeks after completing the course of treatment.
Dosage and Administration Fungal infection of the nails:- Fingernails: TERBINAFINE HCl® 250 mg Tablets once a day
for 6 weeks. Toenails: TERBINAFINE HCl® 250 mg Tablets , once a day
for 12 weeks. Some cases may require treatment for up to 6 months.
Complete healing of the infection may not occur until several weeks after completing the course of treatment.
A healthy nail may take several months to grow back.
Onychomycosis• Onychomycosis is defined as the fungal infection of
the nail.• It is the most common disease of the nails and can
constitute to about a half of all nail abnormalities. • Onychomycosis can affect either the toenails or the
fingernails. However, it is particularly common in toenails.
• Approximately 6-8% of the adult population has onychomycosis.
Onychomycosis• Onychomycosis is defined as the fungal infection of
the nail.• It is the most common disease of the nails and can
constitute to about a half of all nail abnormalities. • Onychomycosis can affect either the toenails or the
fingernails. However, it is particularly common in toenails.
• Approximately 6-8% of the adult population has onychomycosis.
Dosage and AdministrationOnychomycosis
Dosage and Administration
Tinea pedis, tinea corporis
Adverse Effect:• Common: Headache, feeling of fullness, loss of
appetite, indigestion, feeling sick, mild stomach pain, diarrhoea
• Uncommon: Taste disturbances and loss of taste sense.
• Rare : ‘Pins and needles’ or tingling, reduced sense of touch, dizziness, a feeling of general discomfort and illness, tiredness, joint pain (arthralgia), muscle pain (myalgia).
• Skin Reactions: If progressive skin rash occurs, treatment should be discontinued.
Use in Specific Populations:• Pregnancy Category B: Terbinafine not to be initiated
during pregnancy.• Nursing Mothers: After oral administration,
Terbinafine is present in breast milk of nursing mothers.
• The ratio of Terbinafine in milk to plasma is 7:1. Treatment with Terbinafine is not recommended in nursing mothers.
• Pediatric Use: The safety and efficacy of Terbinafine tablets have not been established in pediatric patients.
TERBINAFINE HCl CREAMTerbinafine Hydrochloride 1% w/w.
TERBINAFINE HCl Cream• TERBINAFINE HCl®, as a 1% cream is used for superficial
skin infections such as jock itch (Tinea cruris), athlete's foot (Tinea pedis) and other types of ringworm (Tinea corporis).
• Studies have shown that TERBINAFINE HCl® cream works in about half the time required by other antifungal.
• Terbinafine Hydrochloride 1% cream is presented in aluminium tubes with polyethylene caps in packs of 10g.
TERBINAFINE HCl Cream• TERBINAFINE HCl® Cream is also used to treat yeast
infections of the skin. • Yeasts are another type of fungus, a common example
being Candida albicans.
• TERBINAFINE HCl Cream is also useful in treating Pityriasis versicolor, a superficial fungus infection of the skin.
• Terbinafine, the active ingredient in TERBINAFINE HCl® Cream, works by killing dermatophytes and by killing or stopping the growth of yeasts.
TERBINAFINE HCl Cream• INDICATIONS
• Fungal infections of the skin caused by Trichophyton (e.g. T. Rubrum, T.Mentagrophytes, T. Verrucosum, T. Violaceum), Microsporum canis and Epidermophyton floccosum.
• Yeast infections of the skin, principally those caused by the genus Candida (eg. C. albicans).
• Pityriasis (tinea) versicolor due to Pityrosporum orbiculare (also known as Malassezia furfur).
TERBINAFINE HCl Cream• DOSAGE AND DIRECTIONS • TERBINAFINE HCl®, Cream is usually applied once or twice
daily. • It is important to clean and thoroughly dry the affected
areas before applying TERBINAFINE HCl®, Cream.• Apply the cream to the affected skin and surrounding area
in a thin layer and rub it in lightly.• If you need to apply the cream between your toes, fingers
or buttocks, under a breast or armpit, or in the groin region, the area may be covered with a gauze after applying the cream.
• This is particularly useful at bedtime.
TERBINAFINE HCl Cream
Tinea pedis (athlete's foot) 1 week
Tinea corporis/cruris (ringworm, jock itch)
1 week
Cutaneous candidiasis 1 week
Pityriasis versicolor 2 weeks
How long to use TERBINAFINE HCl® Cream
CLINICAL PHARMACOLOGY • Pharmacokinetics
• This is a locally acting locally applied preparation with minimal systemic absorption (<5%). Therefore, systemic pharmacokinetics is not relevant.
• Pharmacodynamics• The pharmacodynamic effects of terbinafine have
been well established both as a topical agent and for systemic administration in the indications sought.
Important safety information:• Terbinafine Cream is for external use only. Do not
get it into eyes, nose, or mouth.
• Do not use Terbinafine Cream on the nails or scalp. • Do not use it for vaginal yeast infections.
• Do not use more than the recommended dose.
• Terbinafine Cream should not be used in CHILDREN younger than 12 years old, safety and effectiveness in these children have not been confirmed.
Possible side effects of Terbinafine Cream:
• Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); skin irritation
Additional informations• What are the symptoms and signs of athlete's foot?• Most individuals with athlete's foot have no
symptoms at all and do not even know they have an infection.
• Many may think they simply have dry skin on the soles of their feet.
• Common symptoms of athlete's foot typically include various degrees of itching and burning.
• The skin may frequently peel, and in particularly severe cases, there may be some cracking, pain, and bleeding as well.
• Rarely, athlete's foot can blister (called bullous tinea pedis).
Additional informations
Additional informations
Additional informations
Eczematous Skin Lesions in an Infant
Cutaneous cadidyasis
Jock itch
Ring worm
Additional informations
•Pityriasis versicolor is a common skin complaint in which flaky discoloured patches appear mainly on the chest and back. •It is sometimes called tinea versicolor, refer to infection with a dermatophyte fungus.
References