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COMPARISON CHART

DRUG NAME Terbinafine Amphoteracin B Nystatin

Pharmacokinetic Activei Activei Activei


(Active or
Prodrug)
Terbinafine is hypothesized to Amphotericin B is fungistatic or Nystatin exerts its
act by inhibiting squalene fungicidal depending on the antifungal activity by
monooxygenase, thus blocking concentration obtained in body binding to sterols in
Mechansim the biosynthesis of ergosterol, fluids and the susceptibility of the fungal cell
Of action an essential component of the fungus. The drug acts by membrane. The drug
fungal cell membranes. This binding to sterols (ergosterol) in is not active against
inhibition also results in an the cell membrane of susceptible organisms (e.g.,
accumulation of squalene, fungi. This creates a bacteria) that do not
which is a substrate catalyzed to transmembrane channel, and the contain sterols in
2,3-oxydo squalene by squalene resultant change in membrane their cell membrane.
monooxygenase. The resultant permeability allowing leakage of As a result of this
high concentration of squalene intracellular components. binding, the
and decreased amount of Ergosterol, the principal sterol in membrane is no
ergosterol are both thought to the fungal cytoplasmic longer able to
contribute to terbinafine's membrane, is the target site of function as a
antifungal activity.ii action of amphotericin B and the selective barrier, and
azoles. Amphotericin B, a potassium and other
polyene, binds irreversibly to cellular constituents
ergosterol, resulting in disruption are lost.iii
of membrane integrity and
ultimately cell death.ii
Solubility Slightly soluble in wateriv Insoluble in waterv Soluble in wateriii
(Lipid or Water)
Protein Binding >99%vi 90%vi Not availablevi
Absorption Absortpion >70% Poor PO
Bioavailabiliy: Bioavailability 100% for absorptionvi
40%(adults);36-64%
intravenous infusion.vii
Peak plasma time :1-2hr Onset: symptom
Peak plasma relief for oral
concentration(250-mg dose): candidiasis 24-72hr
1mcg/mlvi
Distribution Predominantly distributed Lipid complex show Not availablevi
to sebum and skinvi lower kidney cons than
conventionalvi
Metabolism Metabolized in liver by Exclusively through Not availableii
several CYP450 enzyme; renalii
first pass effect (40%)vi
Half Life 36hr(drug released very Elimination half Not availablevi
slowly from skin and life:15days
adipose tissues)vi Half life,Plasma:24hrvi

Active Metabolite Inactive metabolitevi Not availablevi


Hypersensitivity and Hypersensistive people Hypersensitive
Contraindication chronic liver disease should avoid this and also patient its
avoid in nursing contraindicated
females.viii
Anti-fungal Candidiasis,Cutaneous Coccidioidomycosis Oral Candidiasis
spectrum Onychomycosis,Pityriasis Histoplasmosis,Infections, Mucocutaneousvii
versicolor,Sporotrichosis Fungal Invasive
Tinea Capitis,Tinea Aspergillosis
Corporis,Tinea Cruris Invasive Fungal Infections
i
Tinea Pedis. Leishmaniasis Meningitis,
Cryptococcal Meningitis,
Fungal Mucocutaneous
Leishmaniasis,Penicillium
marneffei infection
Visceral Leishmaniasis
Candidal cystitis
Disseminated
Cryptococcosis
Fungal endophthalmitis
Fungal osteoarticular
infections
Ocular aspergillosis
Refractory aspergillosis
Severe
Coccidioidomycosis
Severe Fungal infection
caused by Conidiobolus
spp.
Severe Fungal infection
caused by sporotrichosis
spp.
Severe Histoplasmosis
Severe Mucocutaneous
leishmaniasis
Severe North American
blastomycosis
Severe Systemic
candidiasisii
Usual Adult Dose for Usual Adult Dose for Ocular Fungal
Onychomycosis - Fingernail Infection
Tablets: 250 mg orally once a day 5 to 10 micrograms INTRAVITREALLY
Dosage Schedule Duration of therapy Fingernail -Use with systemic voriconazole.
onychomycosis: 6 weeks Usual Adult Dose for
-Toenail onychomycosis: 12 weeks AspergillosisInvasive ESPECIALLY IF
DOSE EXCEEDS 1.5 MG/KG**
Usual Adult Dose for Test dose: 1 mg in 20 mL dextrose,
Onychomycosis - Toenail slow IV over 20 to 30 minutes, with
Tablets: 250 mg orally once a day monitoring for 2 to 4 hours
afterward.
Duration of therapy: Initial dose (patients with good
-Fingernail onychomycosis: 6 cardio-renal function and well
weeks tolerated test dose): 0.25 mg/kg
-Toenail onychomycosis: 12 weeks slow IV daily
Usual Adult Dose for Tinea Capitis Initial dose (severe and rapidly
Oral granules: 250 mg orally once a progressive infection): 0.3 mg/kg
day for 6 weeks slow IV daily
Usual Adult Dose for Tinea Initial dose (patients with impaired
Corporis: cardio-renal function OR severe
reaction to test dose): use smaller
-Tablets: 250 mg orally once a day doses (e.g. 5 to 10 mg)
for 2 to 4 weeks -Gradually increase dose by 5 to 10
mg/day to a final daily dose of 0.5 to
0.7 mg/kg IV once a day depending
on cardio-renal status.
Maximum dose: 1.5 mg/kg total
Duration of therapy: Up to 11
months
Usual Adult Dose for Candidemia
Candida chorioretinitis without
vitreous and with macular
involvement: 5 to 10 mcg/0.1 mL
sterile water by INTRAVITREAL
injection
-For use with concomitant
antifungal treatment (oral or IV)
Central nervous system candidiasis
in patients in whom a ventricular
device cannot be removed: 0.01 to
0.5 mg in 2 mL of 5% dextrose
administered THROUGH THE DEVICE
into the ventricle
Administration
Guidelines

i
https://www.drugbank.ca/salts/DBSALT000470M
ii
https://www.drugbank.ca/drugs/DB00857
iii
https://pubchem.ncbi.nlm.nih.gov/compound/nystatin#section=Mechanism-of-Action
iv
https://pubchem.ncbi.nlm.nih.gov/compound/terbinafine#section=physical and chemical properties
v
Good man Gillman book
vi
Medscape.com
vii
https://www.drugbank.ca/drugs/DB00681
viii
https://www.drugs.com/pro/amphotericin-b.html

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