antifungal drugs

Antifungal Drugs

Group 7Sison, Josef F.

Songco, Marjorie Ann R.Tagupa, Gerald Bong G.

Tamayo, Rose MayTaotao, Krisha Anne C.

Tulagan, Precious

Antifungal Drugs

• Also called antimycotic drugs

• Used to treat two types of fungal infection:– Superficial fungal infections

• (skin or mucous membrane)

– Systemic fungal infectons• (lungs or central nervous system)

Antifungal Drugs

• Groups:– Polyenes,including amphotericin B and

nystatin– Imidazoles, which include ketoconazole,

miconazole, clotrimazole and others– The antimetabolic antifungal flucytosine– Antiprotozoal agents

Polyenes

1.Amphotericin B

2.Nystatin (Mycostatin)

Amphotericin B

• Available Forms:– Lozenges: 10mg– Oral Suspension: 100mg/mL– Powder for injection: 50mg– Tablets: 100mg

Amphotericin B

• Route and Test dose:– A: IV: 0.25-1.0 mg in 20ml of D5W infused

over 20-30 min– A: IV: 0.25-1.0 mg/kg/d in D5W or 1.5 mg/kg

q.o.d .; max: 1.5 mg/kg/d– C: IV: Same as adults, expect dilution and

infuse time differ

Amphotericin B

• Uses:– For treatment of a variety of systemic fungal

(mycotic) infections, such as aspergillosis, blastomycosis, coccidioidomycosis. Nephrotoxicity may occur when given in high doses. Hypokalemia might occur.

• Consideration:– Pregnancy category: B; PB: 95%; t 1/2 : 24 h

Amphotericin B

• Indications:– Systemic fungal inferctions

(hystoplasmosis,coccidioidomycosis,blastomycosis,cryptococcosis,disseminated candidiasis,aspergillosis,phycomycosis,zygomycosis), meningitis

– Infection of the G.I tract caused by Candida albicans– Oral and perioral candidal infections

Amphotericin B

• Contraindications:– Contraindicated in patients hypersensitive to

drug

Amphotericin B

• Side Effects:– CNS: headache, peripheral neuropathy,

transcient vertigo, malaise, seizures– CV: hypotension, arrhytmias, asystole,

hypertension, tachycardia, flushing, phlebitis, thrombophlebitis

Amphotericin B

• Side Effects:– EENT: hearing loss, innitus, blurred vision,

diplopia– GI: anorexia, nausea, vomiting, dyspepsia,

diarrhea, epigastric pain, crumping, melena, steatorrhea, hemorrhagic gastroenteritis

Amphotericin B

• Side Effects:– GU: abnormal renal function with hypokalemia,

azotemia hypostenuria, renal tubular acidosis, nephrocalcinosis, permanent renal impairment; anuria; oliguria

– HEMATOLOGIC: normochronic anemia, normocytic anemia, thrombocytopenia, leukopenia, agrunulocytes, eosinophilia, leukocytosis

Amphotericin B

• Side Effects:– HEPATIC: hepatitis, undice, acute liver failure– METABOLIC: weight loss, hypokalemia,

hypoglycaemia, hyperglycemia, hyperuricemia, hypomagnesemia

Amphotericin B

• Side Effects:– MUSCULOSKELETAL:arthalgia,myalgia– RESPIRATORY:dyspnea,tachypnea,broncho

spasm,wheezing– SKIN: maculopopular rash,pruritus

Amphotericin B

• Nursing Resposibilities:– Use cautiously in patients with impaired renal function– Because of drug dangerous drug effect,it’s used

primarily for treatment of patients with progressive and potentially fatal fungal infections

– Infusion-related reactions,including fever,shaking chills,hyporension,anorexia,nausea,vomiting,headache,dyspnea and tachypnea,may occur 1-3 hoursafter starting infusion

Amphotericin B

• Nursing Responsibilities:– Monitor fluid intake and output; report change in urine

appearance or volume.– Hydration before infusion may reduce risk of

neprotoxicity– Monitor potassium levels closely and report signs of

hypokalemia– Drug is potentially ototoxic. Report evidenced of

hearing loss,tinnitus, vertigo or unsteady gait

Nystatin (Mycostatin)

• Drug class: – Antifungal– Trade name: Mycostatin, Nadostine, Nyaderm– Pregnancy Category: C

• Drug-lab-food Interaction:– No significant interactions known

Nystatin (Mycostatin)

• Available Forms:– Lozenges:200,000 units– Oral suspension:100,000 units/mL– Powder: 50,150, or 500 million units; 1,2 0r 5

billions units– Tablets: 500,000 units– Vaginal Suppositories: 100,000 units

Nystatin (Mycostatin)

• Dosage:– A: Topical use as directed – Intestinal infection:– A: PO: 500,000 – 1,000,000 U t.i.d or q8h– Oral candidiasis:– A:PO: 400,000 – 600,000 U q6-q8h– Neonate (<7 d): PO: 100,000 U q.i.d.– C: PO:250,000 – 500,000 U q.i.d.

Nystatin (Mycostatin)

• Indications:– Intestinal Candidiasis– Oral Candidiasis (thush)– vaginal Candidiasis

• Contraindication:– Hypersensitivity– Vag: Pregnancy

Nystatin (Mycostatin)

• Pharmacokinetics:– Absorption: PO: poorly absorbed– Distribution: PB: UK– Metabolism t ½ : UK– Excretion: in feces unchanged

Nystatin (Mycostatin)

• Pharmacodynamics:– Vag:

• Peak: UK• Duration: 6-12 h

– PO: • Onset: Rapid• Peak: UK• Duration: 6 – 12h

Nystatin (Mycostatin)

• Therapeutic Effects/Uses:– To treat Candida infections– Mode of Action: Increase Permeability of the fungal cell

membrane• Side Effects:

– PO: Anorexia, nausea, vomiting, diarrhea (large doses), stomach cramps, rash

– Vag: Rash, burning sensation– GI: transcient nausea, vomiting, diarrhea

• Adverse Reaction: – None known

Nystatin (Mycostatin)

• Nursing Interventions:– Nystatin isn’t effective against systemic

infections– Vaginal tablets can be used by pregnant

patients up to 6 weeks before term to treat maternal infection that may caused oral candidiasis in neonates

Nystatin (Mycostatin)

• Nursing Interventions:– For treatment of oral candidiasis: After the mouth is

clean of food debris, have patient hold suspension in mouth for several minutes,before swallowing. When treating infanmts,swab medications on oral mucosa. Prescriber may instruct immunosuppresed patients to suck on vaginal tablets (100,000 units) because this provides prolonged contact with oral mucosa

Immidazoles

Fluconazole (Diflucan)Itraconazale (Sporanox)

Ketoconazole ( Sporanox)Miconazole nitrate ( Monistat, Micatin)

Fluconazole (Diflucan)

• Available Forms:– Injection: 200mg/mL,400 mg/200 mL– Powder for oral suspension: 10mg/mL,

40mg/mL– Tablets: 50mg,100mg150mg,200 mg

Fluconazole (Diflucan)

• Route and Dose:– A: PO/IV: 200mg x 1 d; maint: 100mg/d for 2 wk– C: PO/IV: 3-6 mg/kg/d

• Uses and Considerations:– For a variety of fungal infections. Highly selective

inhibitor of fungal cytochrome P- 450. Used to treat cryptococcal meningitis in AIDS clients and oropharyngeal and systemic candidiasis. Pregnancy category: C; PB: 12%; t ½: 20-50h

Fluconazole (Diflucan)

• Indications:– Oropharyngeal Candidiasis– Esophageal Candidiasis– Vulvovaginal Candidiasis– Systemic Candidiasis– Cryptoccal meningitis– Prevention of candidiasis in bone marrow transplant– Suppression of relapse of cryptococcal meningitis in

patients with AIDS

Fluconazole (Diflucan)

• Contraindication:– Contraindicated in patients hypersensitive to

drug. Don’t use in breast-feeding patients

Fluconazole (Diflucan)

• Side Effects:– CNS; headache,dizziness– GI: nausea,vomiting,abdominal

pain,diarrhea,dyspepsia,taste perversion– HEMATOLOGIC: leukopnea,

thrombocytopenia– SKIN: Rash

Fluconazole (Diflucan)

• Nursing Interventions:– Use cautiously in patients hypersensitive to

other antifungal azole compounds; no data exist regarding cross-sensitivity

– Serious hepatoxicity has occurred in patients with underlying medical conditions

– Periodically monitor liver function during prolonged therapy

Fluconazole (Diflucan)

• Nursing Interventions:– If patients develop mild rash, monitor him

closely. – Discontinue drug if lesions progress,and notify

prescriber.– Risk of adverse reactions appears to be

greater in HIV-infected patients

Itraconazale (Sporanox)

• Available Forms:– Capsules: 100mg– Injection:10mg/mL– Oral Solution: 10mg/mL

Itraconazale (Sporanox)

• Route and Dose:– A: PO: Loading dose: 200mg q8h x 3 d; maint:

200mg/d; max: 400 mg/d in two divided doses.

•  Uses and Considerations:– Effective against various systemic fungal

infections, particularly blastomycosis and histoplasmosis. Pregnancy category: C; PB: 99%- t1/2:21-42h.

Itraconazale (Sporanox)

• Indications:– Pulmonary and extrapulmonary

blastomycosis,nonmeningeal histoplasmosis– Aspergillosis– Onychomycosis of the toenail– Onychomycosis of the fingernail– Oropharyngeal Candidiasis– Oropharyngeal Candidiasis in patients unresponsive

to fluconazole tablets– Esophageal Candidiasis

Itraconazale (Sporanox)

• Contraindications:– Contraindicated in patients hypersensitive to

drugs or receiving oral triazolam or midazolam, in those with ventricular dysfunction or a history of heart failure and in those who are breast-feeding.

Itraconazale (Sporanox)

• Side Effects:– CNS:

headache,dizziness,somnolence,fatigue,malaise– CV: hypertension,edema– GI:nausea, vomiting, diarrhea, abdominal pain,

anorexia– GU: albuminuria, impotence– HEPATIC: impaired hepatic function– METABOLIC: hypokalemia– SKIN: rash,pruritus

Itraconazale (Sporanox)

• Nursing Intervention:– Use cautiously in patients with hypochlorhydria; they

may not absorb drud readily– Because hypochlorhydria can accopmpany HIV

infection, use cautiously in HIV-infected patients– Use cautiously in patients receiving other highly

bound drugs because drug and its metabolites are bound to plasma proteins

Itraconazale (Sporanox)

• Nursing Interventions:– Confirm the diagnosis of onychomycosis

before starting therapy by having nail specimens undergo appropriate laboratory testing

– Perform baseline liver function tests and monitor results periodically

Ketoconazole (Sporanox)

• Available Form:– Oral Suspension: 100mg/ml– Tablets: 200mg

Ketoconazole (Sporanox)

• Route and Dose:– A:PO:200-400mg/d as a single dose– C: > 20 y: PO: 3.3-6.6 mg/kg/d as single dose– C: < 20kg: PO: 50mg/d

•  Uses and Considerations:– For infections by Candida spp. , histoplasmosis,

blacstomycosis, and others Treatment could last 1-6 months for systemic infections. Take with food to avoid GI discomfort. Pregnancy category: C; PB: 95%; t 1/2 : 2-8h

Ketoconazole (Sporanox)

• Indications:– Systemic Candidiasis, Chronic

mucocandidiasis, oral candidiasis, candiduri, coccidiodomycosis, blastomycosis, histoplasmosis, chromomycosis and paracoccidioidomycosis; severe cutaneous dermatophyte infections resistant to therapy with topical or oral griseofulvin

Ketoconazole (Sporanox)

• Contraindications:– Contraindicated in patients hypersensitive to

drug

Ketoconazole (Sporanox)

• Side Effects:– CNS: headache, nervousness, dizziness,

somnolence, suicidal tendencies, severe depression

– EENT: photophobia– GI: nausea, vomiting, abdominal pain,

diarrhea

Ketoconazole (Sporanox)

• Side Effects:– GU: Impotence– HEMATOLOGIC: thrombocytopenia,

haemolytic anemia, leukopenia– HEPATIC: fatal hepatoxicity– METABOLIC: hyperlipidemia– SKIN: pruritus

Ketoconazole (Sporanox)

• Nursing Interventions:– Use cautiously in patients with hepatic

disease and in those who are taking other hepetotoxic drugs

– Because potential for serious hepatoxicity, don’t use ketoconazole for less serious conditions, such as fungal infections of skin or nails

Ketoconazole (Sporanox)

• Nursing Interventions:– Monitor patients for signs and symptoms of

hepatoxicity including elevated liver enzyme levels, nausea that doesn’t subside and unusual fatigue,jaundice,dark urine,or pale stool

– Doses up to 800 mg/day can be used to treat fungal meningitis and intracerebral fungal lesions.

Miconazole nitrate (Monistat, Micatin)

• Available Forms:– Cream: 2%– Powder: 2%– Spray: 2%– Topical Ointment: 2%– Topical Solution: 2%– Vaginal– Cream: 2%– Vaginal Suppositories: 100mg,200mg

Miconazole nitrate (Monistat, Micatin)

• Route and Dose:– A: IV: 200-3600 mg/d in D5W in three divided

doses; infuse IV over 30-60 min– C: IV: 20-40mg/kg/d in divided doses; max:

15mgkg per inf– A: Supp: 100mg vag h.s. for 7 d – Available: Vaginal cream 2% lotion

Miconazole nitrate (Monistat, Micatin)

• Uses and Considerations:– For fungal meningitis and fungal bladder

infections. Also for vaginal fungal infections. Pregnancy category: B; PB: 92%; t1/2 2-24h

Miconazole nitrate (Monistat, Micatin)

• Indications:– tinea corporis,tinea crusis,tinea pedis;

cutaneous candidiasis; common dermatophyte infections

– tinea versicolor– Vulvovaginal candidiasis

Miconazole nitrate (Monistat, Micatin)

• Contraindications:– Contraindicated in patients hypersensitive to

drug or its components

Miconazole nitrate (Monistat, Micatin)

• Side Effects:– CNS: headache– GU: pelvic cramps, vulvovaginal burning,

pruritus, and irritation with vaginal cream– SKIN: irritationb, burning, maceration, allergic

contact dermatitis

Miconazole nitrate (Monistat, Micatin)

• Nursing Intervntions:– Use together (within 72 hours) of intravaginal

forms and certain latex products, such as condoms or vaginal contraceptive diaphragms,isn’t recommended because of possible interaction

– Don’t use occlusive dressings– Lotion should be used in intertriginous areas

Antimetabolites

Flucytonsine (Ancobon)

Flucytonsine (Ancobon)

• Available Forms:– Capsules: 250mg, 500mg – Indications Flucytonsine (Ancobon)

Flucytonsine (Ancobon)

• Route and Dose:– A: PO: 50-150mg/kg/d in four divided doses.– C:>50kg:PO: 50-150mg/kg/d in 4 divided doses.– C: < 50kg :PO: 1.5-4.5 g/m2 /d in four divided doses.– C: < 50: PO:1.5-4.5 g/m2 /d in four divided doses.– Neonate: PO: 50-100mg/kg/d in 1-2 divided doses.

Flucytonsine (Ancobon)

• Uses and Contraindication:– Use with amphotericin B may increase

therapeutic action as well as toxicity. Fungal resistance occurs if the drug is given alone. Pregnancy category: C: PB: UK; t 1/2 : 3-6h

Flucytonsine (Ancobon)

• Indications:– Severe fungal infections caused by

susceptible strains of Candida species, including septicaemia, endocarditis, urinary tract, and pulmonary infections, and of Cryptococcus species,including meningitis,pulmonary infections, and urinary tract infections

Flucytonsine (Ancobon)

• Contraindications:– Contraindicated in patients hypersensitive to

drug

Flucytonsine (Ancobon)

• Side Effects:– CNS: headache, vertigo, sedation, fatigue,

weakness, confusion, hallucinations, psychosis, ataxia, hearing loss, paresthesia, parkinsonism, peripheral neuropathy

– CV: cardiac arrest, chest pain

Flucytonsine (Ancobon)

• Side Effects:– GI: nausea, vomiting, diarrhea, abdominal pain, dry

mouth, duodenal ulcer,hemorrhage,ulcerative colitis, anorexia

– GU: azotemia, crystalluria, renal failure– HEMATOLOGIC HEMATOLOGIC: anemia,

leukopenia, bone marrow suppression, thrombocytopenia, eosinophilia, agranulocytosis, aplastic anemia

Flucytonsine (Ancobon)

• Side Effects:– HEPATIC: jaundice– METABOLIC: hypoglycaemia, hypokalemia – RESPIRATORY: respiratory arrest, dyspnea– SKIN: occasional rash, pruritus, urticaria,

photosensitivity

Flucytonsine (Ancobon)

• Nursing Interventions:– Use with extreme caution in patients with hepatic or

renal function or bone marrow suppression– Administer capsules over 15 minutes to reduce

reduce adverse GI reactions– Monitor blood, liver, and renal function studies

frequently during therapy; obtain susceptibility test weekly to monitor drug resistance

Flucytonsine (Ancobon)

• Nursing Interventions:– If possible, regularly perform blood level

assays of drug, to maintain flucytosine at therapeutic level of 40 to 60 mcg/mL. Blood levels above 100 mcg/mL may be toxic.

– Monitor fluid intake and output; report marked changes

Antiprotozoal

Atovaquone (Mepron)

Atovaquone (Mepron)

• Available Forms:– Suspension: 750 mg/5 mL

• Route and Dose:– A: PO: 750mg b.i.d. with food x 21d

Atovaquone (Mepron)

• Uses And Contraindication:– For treatment of mid to moderate

Pneumocystis carinii pneumonia. Pregnancy category: C; PB: t ½: 2-3d

Atovaquone (Mepron)

• Indications:– Acute, mild to moderate Pneumocystis carinii

pneumonia in patients who can’t tolerate co-trimoxazole

• Contraindications:– Contraindicated in patients hypersensitive to

drug

Atovaquone (Mepron)

• Side Effects:– CNS: headache, insomia, asthenia, anxiety,

dizziness– CV: hypotension– EENT: sinusitis, rhinitis– GI: nausea, diarrhea, vomiting, constipation,

abdominal pain, anorexia, dyspepsia, oral candidiasis, taste perversion

Atovaquone (Mepron)

• Side Effects:– HEMATOLOGIC: anemia, neutropenia– METABOLIC: hypoglycaemia, hyponatremia– RESPIRATORY: cough– SKIN: fever, pain

Atovaquone (Mepron)

• Nursing Interventions:– Drug has appeared in breast milk. Use cautiously in

breast-feeding patients.– Because drug is bound to plasma protein, use

cautiously with other highly protein-bound drugs, and assess patient for toxicity when used together

– Alert: Because of risk of concurrent pulmonary infections, monitor patient closely during therapy.

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