Pharmacology (Dr.

Biag)
Antifungals

22-23 January 2008

MYCOTIC INFECTIONS Histoplasma capsulatum – may present as pulmo

Four General Types lesion
Cutaneous Sporotrichosis – cutaneous erythematous nodules &
Subcutaneous papules
Can be superficial but may not be in the skin Side Effects:
Superficial Amphothericin B
Systemic* “Shake & Bake”
Fever Chills Headache Anemia
*Can be life threatening Malaise Nausea Hypotension Tachycardia
*usually occur in immunocompromised Ms & jt pain Anaphylaxis K+ & Mg++
*renal toxicity monitor BUN and creatinine
Candida Albicans *neurotoxicity: seizures & paresthesias

Due to antibiotic therapy, antineoplastics, or Flucytosine

immunosuppresants (steroids)
May result in overgrowth & systemic infections aka 5-fluorocytosine  5 – fluorouracil (antimetabolite)
Opportunistic organism, may multiply in number because Taken up by fungal cells & interferes with DNA synthesis
of the decline in the normal flora Result: fungal cell death
Alone or in combination with amphotericin B for serious
In the mouth: systemic infections caused by susceptible strains of
Oral candidiasis or thrush Cryptococcus & candida species
New born infants & immunocompromised patients
have increased frequency of oral thrush Side Effects:
Nausea, vomiting, anorexia
Vaginal Cadidiasis Confusion, hallucination, headache, sedation
“yeast infections” Agranulocytosis (dec WBC)
Pregnancy, DM, OCP Elevated BUN & creatinine
May occur to both male and females (urethritis and Elevated transaminases
balanitis)
Ketoconazole & Fluconazole
Antiviral Agents
Broken Down into 4 major grps based on their chem’l Interferes with synthesis of ergosterol
structures Increase in cell permeability & ultimately inhibition of
(1) Polyenes: amphoterincin B , nystatin fungal cell growth
(2) Flucytosine
(3) Imidazoles: ketoconazole, miconazole, clotrimazole, Side Effects (Ketoconazole)
fluconazole Rash (if topical), anaphylaxis
(4) Griseofulvin N & V, liver cirrhosis
Gynecomastia, uterine bleeding, loss of libido,
impotence, oligospermia, hair loss
Polyenes: Amphotericin B & Nystatin Acute hypoaldosteronism, renal hypofunction

Binds to sterols in cell membrane lining Side Effects (Fluconazole)

Allowing K+ & Mg2+ to leak out, altering fungal cell Headache
metabolism Nausea and vomiting
Result: fungal cell death Abdominal pain
Diarrhea
Uses: Increase AST in Px w/ cryptococcal meningitis & AIDS
IV: fatal systemic mycotic infections rash
Aspergillus fumigatum
– growth is concentric with radiation Miconazole
– misdiagnosed as TB (SSX: chronic productive
cough, low to moderate fever, inhibit uptake of components essential for cell
immunocompromised patient, hemoptysis) reproduction & growth as well as cell wall structures,
Blastomycosis – ulcers, when scraped (+) yeasts thus promoting cell death of fungi
Coccidiomycosis, paracoccidiodomycosis – San
Side Effects:
Joaquin fever dw (accdg to Fars)
Vulvovaginal burning when used as ointment, cream
Crytococcosis – (CT scan of brain) lesion at basal
and vaginal suppository
ganglia, occipital lobe, L. temporal lobe; & meningitis
Itching

malta & MR + Farsi 1 of 2

 Pharmacology – Antifungals by Dra Biag Page 2 of 2

Irritation
Maceration
Allergic contact dermatitis

Clotrimazole

Canesten: ointment, vaginal suppository

Altering fungal cell membrane permeability
Permeating loss of P cmpds, K & other essential
intracellular constituents w/ consequent loss of ability to
replicate

Side Effects:
Abnormal liver function tests
Stinging, erythema, edema
Cystitis, urethritis
Vaginal soreness during intercourse

Griseofulvin

Disrupts cell division

Result: inhibited fungal mitosis (reproduction)
Deposits in keratin precursor cells & has special affinity
for diseased tissue. It is tightly bound to new keratin of
skin, hair, & nails, w/c becomes highly resistant to fungal
invasion

Side Effects:
Rash, urticaria
Headache
Nausea/Vomiting & anorexia
Leukopenia
Nephrotoxicity
Hepatotoxicity
Overgrowth of nonsusceptible organisms (Candida)