Terbinafine drug data and news

Terbinafine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Terbinafine
Brand Names/Synonyms Bramazil; Lamasil; Lamisil; Lamisil At; Terbina; Terbinafine; Terbinafine Hcl; Terbinafine Hydrochloride; Ternbinafine Hcl
Indication For the treatment of interdigital tinea infections
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Description Not Available
Pharmacology Terbinafine is an allylamine antifungal agent and acts by inhibiting squalene epoxidase, thus blocking the biosynthesis of ergosterol, an essential component of fungal cell membranes. in vitro, mammalian squalene epoxidase is only inhibited at higher (4000 fold) concentrations than is needed for inhibition of the dermatophyte enzyme. Depending on the concentration of the drug and the fungal species test in vitro, Terbinafine may be fungicidal. However, the clinical significance of in vitro data is unknown.
Mechanism Of Action Terbinafine is hypothesized to act by inhibiting squalene epoxidase, thus blocking the biosynthesis of ergosterol, an essential component of fungal cell membranes.
Terbinafine News
(When available)

Fungal prosthetic mitral valve endocarditis caused by ...  May 9, 2006
Calif) identified the organism as S brevicaulis and demonstrated mean inhibitory concentrations of 4 µg/mL to amphotericin B, 1 µg/mL to terbinafine, 8 µg ... - The Journal of Thoracic and Cardiovascular Surgery

(PZ) Novartis Delivers Strong Start to 2006 in First Quarter with ...  Apr 24, 2006
...since the 2005 first quarter included the antibiotics azithromycin (Zithromax(R)) and ceftriaxone (Rocephin(R)) in the US as well as terbinafine (Lamisil) and ... - Houston Chronicle,

Sore Feet a Sure Sign of Aging  Apr 21, 2006
Oral medications for fungal infections, including fungal nails and athlete's foot, are Lamisil (terbinafine) made by Novartis Pharmaceuticals of East Hanover ... - SeniorJournal.com,

Novartis Delivers Strong Start to 2006 in First Quarter with ...  Apr 24, 2006
...since the 2005 first quarter included the antibiotics azithromycin (Zithromax®) and ceftriaxone (Rocephin®) in the US as well as terbinafine (Lamisil) and a ... - PharmaLive.com (press release),

Dosage Forms TABLET; CREAM; SPRAY
Drug_Category Trypanocidal Agents; Antifungals; Allylamines; ATC:D01AE15; ATC:D01BA02
Absorption Readily absorbed from gastrointestinal tract.
Interactions -->Interactions for Terbinafine:

In vitro studies with human liver microsomes showed that terbinafine does not inhibit the metabolism of tolbutamide, ethinylestradiol, ethoxycoumarin, and cyclosporine. In vitro studies have also shown that terbinafine inhibits CYP2D6-mediated metabolism. This may be of clinical relevance for compounds predominantly metabolized by this enzyme, such as tricyclic antidepressants, ß-blockers, selective serotonin reuptake inhibitors (SSRIs), and monoamine oxidase inhibitors (MAO-Is) Type B, if they have a narrow therapeutic window.

In vivo drug-drug interaction studies conducted in normal volunteer subjects showed that terbinafine does not affect the clearance of antipyrine or digoxin. Terbinafine decreases the clearance of caffeine by 19%. Terbinafine increases the clearance of cyclosporine by 15%.

There have been spontaneous reports of increase or decrease in prothrombin times in patients concomitantly taking oral terbinafine and warfarin, however, a causal relationship between LAMISIL® Tablets and these changes has not been established.

Terbinafine clearance is increased 100% by rifampin, a CyP450 enzyme inducer, and decreased 33% by cimetidine, a CyP450 enzyme inhibitor. Terbinafine clearance is unaffected by cyclosporine.

There is no information available from adequate drug-drug interaction studies with the following classes of drugs: oral contraceptives, hormone replacement therapies, hypoglycemics, theophyllines, phenytoins, thiazide diuretics, beta blockers, and calcium channel blockers.

Toxicity Not Available
Organisms Affected Humans and other mammals
Chemical IUPAC Name N,6,6-trimethyl-N-(naphthalen-1-ylmethyl)hept-2-en-4-yn-1-amine
Chemical Formula C21H25N
Molecular Weight 291.43 g/mol
Smiles String CC(C)(C)C#CC=CCN(C)CC1=CC=CC2=CC=CC=C21
Melting Point 195-198 °C
Water Solubility Slightly soluble
State Solid
LogP/Hphobicity 6.466
Isoelectric Point Not Available
Biotransformation Liver
Half Life 36 hours
Protein Binding [%] >99%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Terbinafine.html
http://www.rxlist.com/cgi/generic/terbin.htm
Drug Type Approved Drug
Accession No APRD00508
CAS Registry Number 91161-71-6
KEGG Compound ID C08079
PubChem ID SID:66593
PharmGKB ID PA451614
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2240346

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