26. Lıpıd formulations of amphotericin B
(ABLC; Abelcet®)
(ABCD; Amphocil® or Amphotec®)
(L-AMB; Ambisome®)
Amphotericin B Lipid Complex(ABLC)
Amphotericin B Colloidal Dispersion(ABCD)
Liposomal Amphotericin B
31. • Systemic mycotic infections
• invasive aspergillosis
• Rapidly progressive Blastomycosis &
Coccidiomycosis
• Mucormycosis.
• Disseminated rapidly progressing
Histoplasmosis
• Cryptococcus neoformans-intra
thecal
•Given as IV
Available as 50mg vial – suspended in 10 ml water and then diluted
with 500 ml glucose
Uses
32. Liposomes in the therapy of infectious
diseases and cancer 1989: 105
Release from
macrophage
Macrophage
Release in blood
compartment
Endocytosis
Liposome Lysosome
Fusion
Liposome
degradation
Endocytic
vesicle
Reserve drugs
for resistant
kala azar
55. Itraconazole
Broad spectrum of activity
also against aspergillus
Does not inhibit steroid
hormone synthesis and no
serious hepatoxicity
56. Pharmacokinetics of itraconazole
Absorption enhanced by food & gastric acidity
Accumulates in vaginal mucosa, skin, nails
CNS penetration is poor
Metabolized in liver
57. Uses of itraconazole
DOC for paracoccidomycosis &
chromoblastomycosis ,
histoplasmosis & blastomycosis
Also used in oesophageal,
oropharyngeal vaginal candidiasis
Dermatophytosis
Onychomycosis
Aspergillosis
60. Uses of voriconazole
DOC for invasive aspergillosis
Most useful for esophageal
candidiasis
First line for moulds like
fusarium
Resistant candida infections
61. Adverse effects of voriconazole
Adverse events:
Transient visual changes like
blurred vision , altered color
perception & photophobia
Prolongation of QT
70. 5 flucytosine
Narrow spectrum
Prodrug, pyrimidine analog
Adverse events:
Bone marrow toxicity , Alopecia,
rarely hepatitis
Uses: in combination with AMB in
cryptococcal meningitis
76. Uses:
Systemically only for dermatophytosis,
ineffective topically
Duration of treatment depends on site,
thickness of keratin and turnover of
keratin.
Treatment must be continued till infected
tissue is completely replaced by normal
skin,hair, nail.
Dose: 125-250 mg QID
77. Duration of treatment
• Body skin = 3 weeks
• Palm, soles = 4- 6 weeks
• Finger nails = 4- 6months
• Toe nails = 8 – 12 months
81. Caspofungin
FDA approved in 2001
Dose – single loading dose 70mg
followed by daily dose of 50mg iv
over 1 hr
Use
Invasive forms of candidosis
Candidemia
Invasive aspergillosis
82. Micafungin
FDA- approved in 2005
Candida esophagitis- 150 mg/day
Candidemia -100mg/day
Prophylaxis of fungal infections in
those receiving stem cell
transplant- 50mg/day
D/I
Micafungin -↑ the levels of
nifedipine,cyclosporine and sirolimus
84. Adverse Effects
Flushing , phlebitis-Anidulafungin
Increase in liver enz.
GI disturbances Caspofungin
85. Topical agents used in dermatophytosis
Tolnaftate:
Tinea infections.
Not effective in hyperkeratinized lesions
Salicylic acid aids its effect by keratolysis
87. Topical agents used in dermatophytosis
Undecylenic acid: 5% (Tineafax)
Generally combined with zinc (20%)
used in tinea cruris and nappy rash
Sodium thiosulfate: (Karpin lotion)
Reducing agent known as hypo
Effective in pitryasis versicolor only
20 % solution for 3-4 weeks
88. Topical agents used in dermatophytosis
Benzoic acid:
Used in combination with salicylic acid
Whitfields ointment: ( benzoic acid 6% +
salicyclic acid 3 %)
Salicyclic acid due to its keratolytic action
helps to remove infected tissue &
promotes penetration of benzoic acid in
fungal infected lesion
Adverse events: irritation & burning
sensation
(Ring cutter ointment)
89. Topical agents used in dermatophytosis
Haloprogin
Dermatophytosis
Mainly-T.pedis
91. Spectrum of action
Nystatin: Candidiasis only
Griseofulvin: Dermatophytosis only
Terbinafine : Dermatophytosis &
candidiasis
Caspofungin: Aspergillosis & candidiasis
92. Important characteristics
• Broad spectrum: AMB, KTZ, FLU, ITR
• Nephrotoxic/ Anemia: AMB
• Leucopenia: 5 FC
• GIT upset: All
• Over all toxicity: highest for AMB
lowest for fluconazole, itraconazole