Pharmacology- anti-fungal drugs.Classification and details on polyenes, echinocandins, griseofulvin, azoles, terbinafine, and topical azoles.
Their uses, side effects, adverse effects are mentioned with the mechanism of action.
7. Adverse effects
Toxicity of 5-FC is lower
than that of AMB
Consists of dose dependent
bone marrow depression
Gastrointestinal disturbances
(enteritis and diarrhoea)
Liver dysfunction- mild and
irreversible
Uses
Not employed as sole
therapy
Rapid development of
resistance limits its utility in
deep mycosis
Used in meningeal,
nonmeningeal
cryptococcosis with AMB
to produce a synergistic
action
8. Mechanism of action
Binds to ergosterol
Pore formation
Cell contents leak out
Death of fungus(fungicidal)
9. Fungicidal drug
Effective against
most of the fungal
infections(broad
spectrum)
But given in very
serious
conditions only
Given Intravenous(5%
dextrose) (not effective
orally)
10. Poorly absorbed orally
(exp: intestinal candidiasis)
Administered I.V. as a suspension
made with help of deoxycholate.
t1/2 = 15 days
60% metabolized in liver
11.
12. • Chills, fever, headache, pain all over, nausea,
dyspnea(release of IL & TNF)
Acute reaction
• Nephrotoxicity:Azotemia
• Hypokalemia, acidosis, anemia
Long term toxicity
• nerve palsies, headache
CNS toxicity
Hepatotoxicity rarely
13. Infusion related reaction (most common)
Nephrotoxicity (renal tubular acidosis with
hypokalemia)
Bone marrow suppression
hypotension
14.
15.
16. Inhibition of Sq.
epoxide
Accumulation
of squalene
• Toxic to
fungal cells
Death of fungal
cells (fungicidal)
Fungicidal drugs
given orally as well as topical preparations
These drugs accumulate in keratin rich areas
17. Nausea, vomiting
Taste disturbances
Rarely hepatic dysfunction
Topical: erythema, itching,
dryness, rashes, urticaria
Uses
Used in fungal infections
(dermatophytosis infection)
Tinea pedis/cruris corporis
• 1% cream twice daily
Onychomycosis, tinea
capitis
• 250mg OD
Less effective in cutaneous
and mucosal candidiasis
19. PK- Fatty foods increase the absorption
• Efficacy of oral contraceptives may be lost
Interaction: It induces CYP450 enzymes and hastens
warfarin metabolism
• DOSE : 125-250 mg QID with meals
DOC- Only for dermatophytosis
Avoided in patient taking disulfiram
S/E- Hepatotoxic, neutropenia