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Product Name
:
TERBINA (cream)
Chemical Name
:
Terbinafine (HCl)
Therapeutic Category
:
Antifungal drugs & Antiviral drugs
Pharmacologic Category
:
Antifungal Agent, Oral
Pharmaceutical Form
:
Cream
Composition
:
Terbinafine (HCl) 1 g/100 g
Dosing
 
Dosing: Adult
Superficial mycoses (onychomycosis): Oral:
Fingernail: 250 mg daily for up to 6 weeks; may be given in 2 divided doses
Toenail: 250 mg daily for 12 weeks; may be given in 2 divided doses
Systemic mycosis (unlabeled use): Oral: 250-500 mg/day for up to 16 months

Dosing: Pediatric

Tinea capitis: Oral: Granules: Children ≥4 years:
<25 kg: 125 mg once daily for 6 weeks
25-35 kg: 187.5 mg once daily for 6 weeks
>35 kg: 250 mg once daily for 6 weeks
Onychomycosis (unlabeled use): Oral: Tablet: Children:
10-20 kg: 62.5 mg once daily for 6 weeks (fingernails) or 12 weeks (toenails)
20-40 kg: 125 mg once daily for 6 weeks (fingernails) or 12 weeks (toenails)
>40 kg: 250 mg once daily for 6 weeks (fingernails) or 12 weeks (toenails)

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

Clcr <50 mL/minute: Oral administration is not recommended; clearance is decreased by ~50%.

Dosing: Hepatic Impairment

Hepatic cirrhosis: Oral administration is not recommended; clearance is decreased by ~50%.
Use
 
Active against most strains of Trichophyton mentagrophytes, Trichophyton rubrum; may be effective for infections of Microsporum gypseum and M. nanum, Trichophyton verrucosum, Epidermophyton floccosum, Candida albicans, and Scopulariopsis brevicaulis
Onychomycosis of the toenail or fingernail due to susceptible dermatophytes; treatment of tinea capitis
Adverse Reactions
 
Adverse events listed for tablets unless otherwise specified. Granules were studied in patients 4-12 years of age.
>10%: Central nervous system: Headache (13%; granules 7%)
1% to 10%:
Central nervous system: Fever (granules 7%)
Dermatologic: Rash (6%; granules 2%), pruritus (3%; granules 1%), urticaria (1%)
Gastrointestinal: Diarrhea (6%; granules 3%), vomiting (granules 5%), dyspepsia (4%), nausea (3%; granules 2%), taste disturbance (3%), abdominal pain (2%; granules 2% to 4%), toothache (granules 1%)
Hepatic: Liver enzyme abnormalities (3%)
Respiratory: Nasopharyngitis (granules 10%), cough (granules 6%), nasal congestion (granules 2%), pharyngeal pain (granules 2%), rhinorrhea (granules 2%)
<1%, postmarketing, and/or case reports: Acute pancreatitis, anemia, angioedema, agranulocytosis, allergic reactions, alopecia, anaphylaxis, appetite decreased, arthralgia, dizziness, fatigue, generalized exanthematous pustulosis (acute), hepatic failure, malaise, myalgia, neutropenia (severe), ocular lens and retina changes, precipitation/exacerbation of cutaneous and systemic lupus erythematosus, pancytopenia, psoriasiform eruption, psoriasis exacerbation, rhabdomyolysis, Stevens-Johnson syndrome, thrombocytopenia, toxic epidermal necrolysis, visual field acuity decreased, visual field defects, vomiting
Contraindications
 
Hypersensitivity to terbinafine or any component of the formulation
Warnings / Precautions Drug
 
Concerns related to adverse effects:
• Allylamine antifungal hypersensitivity: Use caution in patients sensitive to allylamine antifungals (eg, naftifine, butenafine); cross sensitivity to terbinafine may exist
• Dermatologic effects: Although rare, Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported; discontinue therapy if progressive skin rash occurs.
• Hematologic effects: Although rare, pancytopenia and neutropenia have been reported; discontinuation of therapy may be required. Monitor CBCs in patients with pre-existing immunosuppression if use to continue >6 weeks.
• Hepatic failure: Rare cases of hepatic failure (including fatal cases) have been reported; not recommended for use in patients with active or chronic liver disease. Discontinue if symptoms or signs of hepatobiliary dysfunction or cholestatic hepatitis develop.
• Ocular effects: Although rare, changes in the ocular lens and retina have been reported; discontinuation of therapy may be required.
Disease-related concerns:
• Hepatic cirrhosis: Not recommended in patients with hepatic cirrhosis; clearance is reduced by approximately 50%.
• Lupus: Precipitation or exacerbation of cutaneous or systemic lupus erythematosus has been observed; discontinue if signs and/or symptoms develop.
• Renal dysfunction: Not recommended in patients with renal dysfunction (Clcr ≤50 mL/minute); clearance is reduced by approximately 50%.
Metabolism/Transport Effects
Substrate (minor) of 1A2, 2C9, 2C19, 3A4; Inhibits CYP2D6 (strong); Induces CYP3A4 (weak)
Interactions
 
Atomoxetine: CYP2D6 Inhibitors (Strong) may increase the serum concentration of Atomoxetine. Management: Initiate atomoxetine at a reduced dose (adult doses -- patients up to 70kg: 0.5mg/kg/day; patients 70kg or more: 40mg/day) in patients receiving a strong CYP2D6 inhibitor. Risk D: Consider therapy modification
Codeine: CYP2D6 Inhibitors (Strong) may diminish the therapeutic effect of Codeine. These CYP2D6 inhibitors may prevent the metabolic conversion of codeine to its active metabolite morphine. Risk D: Consider therapy modification
Conivaptan: May increase the serum concentration of CYP3A4 Substrates (Low risk). Risk C: Monitor therapy
CycloSPORINE: Terbinafine (Systemic) may decrease the serum concentration of CycloSPORINE. Risk C: Monitor therapy
CYP2D6 Substrates: CYP2D6 Inhibitors (Strong) may decrease the metabolism of CYP2D6 Substrates. Exceptions: Tamoxifen. Risk D: Consider therapy modification
Cyproterone: May decrease the serum concentration of CYP1A2 Substrates. Risk C: Monitor therapy
Fesoterodine: CYP2D6 Inhibitors may increase serum concentrations of the active metabolite(s) of Fesoterodine. Risk C: Monitor therapy
Iloperidone: CYP2D6 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolite P88 may be increased. CYP2D6 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolite P95 may be decreased. CYP2D6 Inhibitors (Strong) may increase the serum concentration of Iloperidone. Management: Reduce iloperidone dose by half when administered with a strong CYP2D6 inhibitor. Risk D: Consider therapy modification
Nebivolol: CYP2D6 Inhibitors (Strong) may increase the serum concentration of Nebivolol. Risk C: Monitor therapy
Rifamycin Derivatives: May increase the metabolism of Terbinafine (Systemic). Risk D: Consider therapy modification
Saccharomyces boulardii: Antifungal Agents may diminish the therapeutic effect of Saccharomyces boulardii. Risk D: Consider therapy modification
Saxagliptin: CYP3A4 Inducers may decrease the serum concentration of Saxagliptin. Risk C: Monitor therapy
Tamoxifen: CYP2D6 Inhibitors (Strong) may decrease the metabolism of Tamoxifen. Specifically, strong CYP2D6 inhibitors may decrease the formation of highly potent active metabolites. Risk X: Avoid combination
Tetrabenazine: CYP2D6 Inhibitors (Strong) may increase the serum concentration of Tetrabenazine. Specifically, concentrations of the active alpha- and beta-dihydrotetrabenazine metabolites may be increased. Management: Tetrabenazine adult dose should be reduced by 50% when starting a strong CYP2D6 inhibitor. Maximum tetrabenazine adult dose is 50 mg/day when used with a strong CYP2D6 inhibitor. Risk D: Consider therapy modification
Thioridazine: CYP2D6 Inhibitors may decrease the metabolism of Thioridazine. Risk X: Avoid combination
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
TraMADol: CYP2D6 Inhibitors (Strong) may diminish the therapeutic effect of TraMADol. These CYP2D6 inhibitors may prevent the metabolic conversion of tramadol to its active metabolite that accounts for much of its opioid-like effects. Risk C: Monitor therapy
Tricyclic Antidepressants: Terbinafine (Systemic) may decrease the metabolism of Tricyclic Antidepressants. Risk D: Consider therapy modification
Pregnancy
 
B
Pregnancy Implications
Adverse events were not observed in animal reproduction studies. Avoid use in pregnancy since treatment of onychomycosis is postponable.
Lactation
 
Enters breast milk/not recommended
Breast-Feeding Considerations
Terbinafine is found in breast milk following oral administration. The milk/plasma ratio is 7:1.
Monitoring Parameters
 
AST/ALT prior to initiation, repeat if used >6 weeks; CBC
Mechanism of Action
 
Synthetic allylamine derivative which inhibits squalene epoxidase, a key enzyme in sterol biosynthesis in fungi. This results in a deficiency in ergosterol within the fungal cell wall and results in fungal cell death.
Pharmacodynamics / Kinetics
 
Absorption: Children and Adults: >70%
Distribution: Vd: 1000 L; distributed to sebum and skin predominantly
Protein binding: Children and Adults: Plasma: >99%
Metabolism: Hepatic; no active metabolites; first-pass effect; little effect on CYP
Bioavailability: 40%; Children 36% to 64%
Half-life elimination: Terminal half-life: 200-400 hours; very slow release of drug from skin and adipose tissues occurs; effective half-life: ~36 hours; Children 27-31 hours
Time to peak, plasma: Children and Adults: 1-2 hours
Excretion: Urine (70% to 75%; Children 70%)
 
   
 
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