Sie sind auf Seite 1von 3

Antifungals

Drug Action Antifungal Spectrum Pharmacokinetics Adverse Effects Other


Amphotericin B -Binds to ergosterol in PM of fungal -DOC: life-threatening -Administered by slow, IV infusion -Fever and chills (1-3 -Polyene macrolide
cells  Forms pores  Disrupt systemic mycoses -Insoluble in water, so injectable hours after IV) antibiotic
membrane function  Electrolytes -FUNGICIDAL OR preparations require addition of -Renal impairment -Used with FLUCYTOSINE
and small molecules leak from cell FUNGISTATIC sodium deoxycholate, forming -Hypotension to reduce dosage of drug
 Cell death -C. albicans soluble colloidal dispersion -Hypokalemia -Dose should be decreased
-H. capsulatum -Intrathecal route used for -Normochromic, by 50% when drug causes
-C. neoformans meningitis normocytic anemia renal dysfunction
-C. immitis -Formulated with variety of -Neurological -Low therapeutic index, so
-Blastomyces artificial lipids which reduce renal problems adult daily dose shouldn’t
dermatitidis and infusion toxicity -Thrombophlebitis exceed 1.5 mg/kg
-Aspergillus -Bound to plasma proteins (can be alleviated w/
-Used against -Low amounts found in CSF, HEPARIN)
Leishmaniasis as well vitreous humour, amniotic fluid
-Does cross placenta
-Sodium loading with infusions of
normal saline can be used to
reduce nephrotoxicity
Flucytosine -Enters fungal cells via cytosine- -w/ AMPHOTERICIN B: -Well absorbed orally -Reversible -Synthetic pyrimidine
specific permease  Converted to systemic mycoses, -Penetrates into CSF neutropenia antimetabolite
false nucleotide  Inhibits meningitis due to C. -Excreted by kidneys -Thrombocytopenia -Resistance occurs due to
thymidylate synthase neoformans, C. albicans -Dose should be adjusted in pts -Bone marrow decreased levels of
-Mononucleotide further -FUNGISTATIC with renal function compromise depression enzymes involved it
converted to trinucleotide  -w/ ITRACONAZOLE: -Reversible hepatic metabolism of drug
Incorporated into fungal RNA Chromoblastomycosis dysfunction
Disrupts nucleic acid and protein -Nausea
synthesis -Vomiting
-Diarrhea
-Severe enterocolitis
Ketoconazole -Inhibit c-14 α-demethylase -Systemic mycoses -Inhibits CYP450 enzymes -Nausea -Potentiates toxicities of:
Blocks demethylation of lanosterol -FUNGISTATIC -Given orally only -Anorexia CYCLOSPORINE,
to ergosterol Disrupts cell -Histoplasma -Requires gastric acid for -Vomiting PHENYTOIN,
membrane structure and function -Blastomyces dissolution and absorbed through -Gynecomastia TOLBUTAMIDE, WARFARIN
 Inhibits fungal cell growth -Candida gastric mucosa -Decreased libido -Shouldn’t be used with
-Inhibits human gonadal and -Coccidioides -Bound to plasma proteins -Impotence AMPHOTERICIN B
PharmaIdea Publications ©
Antifungals

adrenal steroid synthesis  -Metabolism in liver and excreted -Menstrual -Shouldn’t be used in
Decreased testosterone and in bile irregularities pregnancy
cortisol -Frank hepatitis
Fluconazole -Inhibits synthesis of fungal -Prophylactic for -given orally or IV -Nausea -Dose should be reduced
membrane ergosterol reducing fungal -Absorbed really well -Vomiting in pts with renal
infections in recipients -Penetrates CSF well -Rash insufficiency
of BM transplants -Poorly metabolized -Hepatitis -Shouldn’t be used in
-DOC: C. neoformans, -Excreted via kidneys pregnancy
Candidemia, -Inhibits CYP450 enzymes
Coccidioidomycosis
Itraconazole -DOC: Blastomycosis, -Well absorbed orally -Nausea -Synthetic triazole
Sporotrichosis, -Requires acid for dissolution -Vomiting -Should be avoided in
Paracoccidioidomycosis, -Extensively bound to plasma -Rash pregnancy
Histoplasmosis proteins -Hypokalemia -Inhibits metabolism of
-Effective in AIDS- -Extensively metabolized by liver -HTN ANTICOAGULANTS,
associated -Edema STATINS, QUINIDINE
histoplasmosis -Headache
Voriconazole -Invasive aspergillosis -IV or oral administration -Transient visual
-Scedosporium -Metabolized by a variety of disturbance w/in 30
apiospermum CYP450 minutes of dosing
-Fusarium
Posaconazole -Candida and -Oral -Nausea -Contraindicated with:
Aspergillus in -Inhibits CYP3A4 -Vomiting ERGOT ALKALOIDS,
immunocompromised -Should be given with full meal or -Diarrhea PIMOZIDE, QUINIDINE
pts nutrition supplement -Abdominal pain
-Oropharyngeal -Prophylaxis of Candida and -Headache
candidiasis (daily Aspergillus: 3 times daily -HUS, Thrombotic
dosing) thrombocytopenic
-Mucor infections purpura, PE (when
used with
CYCLOSPORINE,
TACROLIMUS)
Caspofungin -Interferes with synthesis of fungal -Aspergillus -highly bound to serum proteins -Fever -Echinocandins
cell wall by inhibiting synthesis of -Candida -1/2 life: 9-11 hours -Rash -Shouldn’t be
β(1,3)-D-Glucan  Lysis and cell -given IV -Nausea coadministered with
PharmaIdea Publications ©
Antifungals

death -Phlebitis CYCLOSPORINE


-Flushing
Micafungin -Candida -IV infusion -Flushing -Echinocandins
Anidulafungin
Terbinafine -Inhibits fungal squalene -DOC: Dermatophytoses -Therapy: 3 months -Diarrhea -Should not be given to
epoxidase  Decreased synthesis (especially -Orally active -Dyspepsia nursing mothers
of ergosterol  Death of fungal onchomycoses) -More than 99% bound to plasma -Nausea -Reduced clearance in pts
cell -FUNGICIDAL proteins -Headache with moderate renal
-C. albicans -Deposited in skin, nails, fat -Rash impairment or hepatic
-Accumulates in breast milk -Taste and visual cirrhosis
-Extensively metabolized disturbances
-Transient increased
in serum liver
enzymes
-Hepatotoxicity
-Neutropenia
Griseofulvin -Accumulates in newly synthesized, -Dermatophytic -Treatment: 6-12 months -Exacerbates -Pts shouldn’t drink
keratin-containing tissue  infections of nails -Ultrafine crystalline preparations intermittent porphyria alcoholic beverages during
Disruption of mitotic spindle and -FUNGISTATIC absorbed from GIT therapy
inhibition of fungal mitosis -Absorption enhanced by high-fat
meals
-Induces CYP450
Nystatin -Similar to AMPHOTERICIN B -Topical treatment of -Oral agent: “swish and swallow” -Nausea -Polyene antibiotic
Candida or “swish and spit” for oral -Vomiting
candidiasis
Miconazole -Topical -Contact dermatitis -Miconazole: potent
Clotrimazole -Vulvar irritation inhibitor of WARFARIN
Butoconazole -Edema metabolism
Terconazole

PharmaIdea Publications ©

Das könnte Ihnen auch gefallen