テルビナフィン 化学特性,用途語,生産方法
外観
白色～うすい黄色粉末～結晶
効能
抗真菌薬, エルゴステロール合成阻害薬
使用
Terbinafine (Lamisil) is a second-generation allylamine that is related to naftifine; however, it is 10 to 100 times more potent in vitro. It is fungicidal, whereas griseofulvin, ketoconazole, itraconazole, and other azole derivatives are all fungistatic. Because it is fungicidal, duration of therapy is shorter, and relapse rates are less than with other oral or topical therapies. Terbinafine acts by inhibiting squalene epoxidase and thereby decreasing synthesis of ergosterol, an essential component of fungal cell membranes. It is highly lipophilic and concentrates in the stratum corneum, sebum, and hair follicles. Slightly better cure rates are attained with b.i.d. than with daily dosing.
適応症
Terbinafine (Lamisil) is a second-generation allylamine that is related to
naftifine; however, it is 10 to 100 times more potent in vitro. It is fungicidal,
whereas griseofulvin, ketoconazole, itraconazole, and other azole derivatives
are all fungistatic. Because it is fungicidal, duration of therapy is shorter, and
relapse rates are less than with other oral or topical therapies.
Terbinafine acts by inhibiting squalene epoxidase and thereby decreasing
synthesis of ergosterol, an essential component of fungal cell membranes.
It is highly lipophilic and concentrates in the stratum corneum, sebum, and
hair follicles. Slightly better cure rates are attained with b.i.d. than with daily
dosing.
定義
ChEBI: A tertiary amine that is N-methyl-1-naphthalenemethylamine in which the amino hydrogen is replaced by a 3-(tertbutylethynyl)allyl group. An antifungal agent administered orally (generally as the hydrochloride salt) for the t
eatment of skin and nail infections.
抗菌性
Terbinafine is active against a wide range of pathogenic fungi,
including dermatophytes (Epidermophyton, Microsporum and
Trichophyton spp.), various Candida spp., Aspergillus spp.,
some dimorphic fungi (Blastomyces dermatitidis, Histoplasma
capsulatum and Sporothrix schenckii) and many dematiaceous
fungi.
獲得抵抗性
Resistance has not been reported.
応用例（製薬）
A synthetic allylamine available as the hydrochloride for oral
and topical administration.
薬物動態学
Oral absorption: 70–80%
C
max 250 mg oral: c. 1 mg/L after 2 h
Plasma half-life: c. 17 h
Volume of distribution: 1000 L
Plasma protein binding: >99%
Blood concentrations increase in proportion to dosage. It is
lipophilic and is rapidly and extensively distributed to body
tissues. It reaches the stratum corneum by diffusion through
the dermis and epidermis, and secretion in sebum. Diffusion
from the nail bed is the major factor in its rapid penetration
of nails. It is metabolized by the liver and the inactive metabolites
are mostly excreted in the urine. The elimination half-life
is prolonged in patients with hepatic or renal impairment.
臨床応用
Terbinafine hydrochloride can be used in Tinea pedis, tinea corporis, tinea cruris, tinea capitis, Onychomycosis caused by dermatophytes.
副作用
These include abdominal discomfort, loss of appetite,
nausea, diarrhea, headache, impairment of taste, rash
and urticaria. Serious skin reactions, including Stevens–
Johnson syndrome, and rare hepatotoxic reactions, including
jaundice, cholestasis and hepatitis, are occasionally
encountered.
テルビナフィン 上流と下流の製品情報
原材料
準備製品