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ANTIFUNGAL AGENTS презентация
Содержание
- 1. ANTIFUNGAL AGENTS
- 2. Fungi Very large and diverse group of
- 3. FUNGAL INFECTIONS Yeast infections Candida species Cryptococcus
- 4. Infection disease caused by fungi called mycoses
- 5. Antifungal agents Drugs used to treat
- 6. Antifungal agents Polyene antibiotics Nystatin Amphotericin
- 7. Mechanism of action
- 8. Amphotericin B Pharmacokinetics is an amphoteric
- 9. Amphotericin B Mechanism of action Binds to
- 10. Amphotericin B A-Aspergillus B-Blastomyces C-Coccoides C-Candida C-Can not cross BBB INTRATHECALLY FLUCONAZOLE
- 11. Amphotericin B Adverse effects “Shake and bake”
- 13. Flucytosine (5-FC) Synthetic
- 14. Ketoconazole Mechanism of action Inhibits an enzyme,
- 15. Ketoconazole Drug interactions Inhibits CYP450 Adverse
- 16. Caspofungin Belongs to Echinocandis Inhibits β(1,3)-D-glucan synthesis
- 17. Terbinafine Oral form is essential for the
- 18. Mechanism of action Terbinafine inhibits squalene epoxidase
- 19. Terbinafine Has fungicidal action, mostly active against
- 20. Griseofulvin Is fungistatic and used for dermatophytosis
Fungi Very large and diverse group of microorganisms Broken down into yeast and molds Yeast is single cell organism, useful for baking and alcohol beverages Molds are multicellular, characterized by long,
Слайд 2Fungi
Very large and diverse group of microorganisms
Broken down into yeast and
molds
Yeast is single cell organism, useful for baking and alcohol beverages
Molds are multicellular, characterized by long, branching filaments called hyphae
Yeast is single cell organism, useful for baking and alcohol beverages
Molds are multicellular, characterized by long, branching filaments called hyphae
Слайд 3FUNGAL INFECTIONS
Yeast infections
Candida species
Cryptococcus neoformats
Moulds (filamentous fungi)
Aspergillus sp.
Dermatophytes
Trichophyton
Microsporum
Слайд 4Infection disease caused by fungi called mycoses
Major Types of Mycoses
superficial
cutaneous
subcutaneous
systemic
opportunistic
Symptoms vary from cosmetic to life threatening
Слайд 5 Antifungal agents
Drugs used to treat fungal infection
Systemic: amphotericin B, fluconazole,
ketoconazole, itraconazole, caspofungin
Topical: terbinafine, clotrimazole, grizeofulvin, nistatin
Topical: terbinafine, clotrimazole, grizeofulvin, nistatin
Слайд 6Antifungal agents
Polyene antibiotics
Nystatin
Amphotericin B
Imidazoles and triazoles* =AZOLES
Ketoconazole Fluconazole *
Clotrimazole Itraconazole*
Mebendazole
Allylamines
Terbinafine
Echinocandins
Caspofungin
Слайд 8Amphotericin B
Pharmacokinetics
is an amphoteric polyene macrolide
is insoluble in water
is poorly
absorbed from the GIT
more than 90% bound by serum proteins
more than 90% bound by serum proteins
Слайд 9Amphotericin B
Mechanism of action
Binds to sterols in the cell membrane lining
Allow
to K+ and Mg2+ to leak out, altering fungal cell metabolism
Result fungal cell death
Result fungal cell death
Слайд 10Amphotericin B
A-Aspergillus
B-Blastomyces
C-Coccoides
C-Candida
C-Can not cross BBB
INTRATHECALLY
FLUCONAZOLE
Слайд 11Amphotericin B
Adverse effects
“Shake and bake” (fever, chills), headache, tachycardia, hypotension, muscle
pain, anemia
Renal toxicity (Mg/K suppl), neural toxicity (seizures, parestesias)
Renal toxicity (Mg/K suppl), neural toxicity (seizures, parestesias)
Слайд 13 Flucytosine (5-FC)
Synthetic pyrimidine, used in combination with
amphotericin B
Amphotericin B increases cell permeability
5-FC forms false nucleotide
Disrupts nucleic acid and protein synthesis
Bone marrow depression, dyspepsia, hepatic dysfunction
Amphotericin B increases cell permeability
5-FC forms false nucleotide
Disrupts nucleic acid and protein synthesis
Bone marrow depression, dyspepsia, hepatic dysfunction
Слайд 14Ketoconazole
Mechanism of action
Inhibits an enzyme, resulting
in cell wall leaking
Blocks demethylation of
lanosterol
to ergosterol
Leads to altered cell membrane (unstable)
Result: fungal cell death
Spectrum
Both topical and oral forms used for wide spectrum mycoses
Leads to altered cell membrane (unstable)
Result: fungal cell death
Spectrum
Both topical and oral forms used for wide spectrum mycoses
Слайд 15Ketoconazole
Drug interactions
Inhibits CYP450
Adverse effects
Alters synthesis of
gonadal and adrenal
steroid
hormones
Allergy
Dyspepsia
Anorexia
Gynecomastia
Impotence
Menstrual irregularities
Allergy
Dyspepsia
Anorexia
Gynecomastia
Impotence
Menstrual irregularities
Слайд 16Caspofungin
Belongs to Echinocandis
Inhibits β(1,3)-D-glucan synthesis destroying cell wall, resulting in lysis
and cell death
Effective mostly against Aspergillus and Candida
Second line drug
Fever, rush, nausea and phlebitis are common adverse reactions
Effective mostly against Aspergillus and Candida
Second line drug
Fever, rush, nausea and phlebitis are common adverse reactions
Слайд 17Terbinafine
Oral form is essential for the treatment of onychomycoses
Cream of solution
useful for skin infection
Слайд 18Mechanism of action
Terbinafine inhibits squalene epoxidase of the fungi, which leads
to decreasing of ergosterol synthesis
Слайд 19Terbinafine
Has fungicidal action, mostly active against Trychophyton
Half life from 200 to
400 hours
Adverse effects
Dyspepsia
Rash
Neutropenia
Hepatotoxicity
Visual disturbances
Adverse effects
Dyspepsia
Rash
Neutropenia
Hepatotoxicity
Visual disturbances
Слайд 20Griseofulvin
Is fungistatic and used for dermatophytosis
Causes disruption of the
mitotic spindle,
inhibiting
mitosis
Induces hepatic CYP450 activity
Unwanted effects
Dyspepsia
Fatigue
Allergy
Induces hepatic CYP450 activity
Unwanted effects
Dyspepsia
Fatigue
Allergy
