Classifications:
[A]On
the basis of disease:
|
1.Superficial/cutaneous mycoses
|
i)Dermatophytes
ii)Candidiasis
iii)Pityriasis versicolor
|
i)Benzoic acid
·
Ketoconazole(topical).
·
Miconazole.
·
Clotrimazole.
·
Econazole.
·
Oxiconazole.
·
Griseofulvin.
ii)Topical azole ionment
·
Clotrimazole.
·
Econazole.
·
Nystatin.
·
Amphotericin
B.
·
Ketoconazole.
·
Miconazole.
For oral administration:
·
Miconazole.
·
Ketoconazole.
·
Itraconazole.
·
Fluconazole.
iii)Itraconazole,Ketoconazole,
Selenium
sulphate
|
|
2.Subcutaneous mycoses
|
i)Madura foot
ii)Sporothrichosis
|
i)Griseofulvin(if the causative
agent
infection),Ketoconazole.
ii)Itraconazole.
|
|
3.Systemic mycoses
|
i)candidiasis.
ii)Histplasmosis
iii)Crytococcosis
(Meningitis)
|
i)Miconazole i.v,Amphotericin i.v,
Ketokonazole(oral)
ii)Amphotericin I.V.
iii)Amphotericin I.V,
Flucylosine(oral),Fluconazole.
|
[B]On
the basis of site of administration:
|
1.For topical application
|
·
Nystatin.
·
Clotrimazole.
·
Econazole.
·
Amphotericin B.
·
Ketoconazole.
·
Miconazole.
·
Oxiconazole.
|
|
2.For oral administration
|
·
Miconazole.
·
Ketoconazole.
·
Fluconazole.
·
Itracanazole.
·
Flucytosine.
·
Griseofulvin
·
Terbinafine.
|
|
3.For intravenous infusion
|
·
Amphotericin
·
Miconazole
·
Fluconazole
·
Flucytosine
|
(Ref:Katzung-11th,P-836-843)
Classify
antifungal agents according to mechanism of action:
[A]Drugs
that disrupt the fungal cell membrane:
1)
Polyenes-e.g
Amphotericin.
2)
Azole-e.g
Ketoconazole,Fluconazole.
3)
Allylamine-e.g
Terbinafine.
[B]Drugs
that inhibit mitosis:e.g Griseofulvin.
[C]Drugs
that inhibit DNA synthesis:e.g Flucytosine. (Ref:Bennett Brown-10th)
Mechanism
of action of fluconazole:
Antifungal
drugs of azole group(Fluconazole/Miconazole/Ketoconazole)
↓
Inhibition of fungal cytochrome P450 enzyme
↓
Inhibition of synthesis of fungal cell membrane ergosterol
↓
Disruption of fungal cell membrane
(Ref:Katzung-11th,P-839)
Indications
of Griseofulvin/Nystatin/Ketokonazole:
|
Grisefulvin
|
Madura foot
|
|
Nystatin
|
1.Superficial candidiasis of mouth,oesophagus &
intestinal tract.
2.Vaginal candidiasis.
3.Cutaneous candidiasis.
4.Prophylactic use with broad spectrum antibiotics.
|
|
Ketokonazole
|
1.Systemic fungal infection(because it is absorped
from gut) & widely distributed.
2.Superficial mycoses.(Topical use).
3.Advance prostatic cancer(because it impairs
testosterone synthesis)
4.Hyper-adrenal corticocism(because it impairs
testosterone synthesis)
|
Advers
effects of Griseofulvin/Ketokonazole:
|
Griseofulvin
|
1.Sever general weakness.
2.GIT upset.
3.Rash.
|
|
Ketoconazole
|
1.↓Libido in man
2.Gynacomastia.
3.Liver damage.
4.Pruritus.
5.Minor gastrointestinal upset.
6.Hepatitis(uncommon).
|
Difference
between Ketoconazole & Fluconazole:
|
Ketoconazole
|
Fluconazole
|
|
1.They are imidazoles.
|
1.They are Triazoles.
|
|
2.Less selective for fangal cytochorome P450
enzymes.
|
2.More selective/higher specificity.
|
|
3.More side effects.
|
3.Fewer side effects.
|
|
4.Contraindicated in pregnancy(Present in breast
milk)
|
4.Not.
|
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