Antifungal Drugs
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Transcript of 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.
THANK YOU FOR LISTENING- GROUP 7
The End