about Fluconazole class, uses, side effects contraindications
Fluconazole
Short Description
Fluconazole is an antifungal medicine that belongs to a class of medicines called triazoles. It works by slowing the growth of the fungi that cause infection.
Category
Chemical class: Triazole derivative
Therapeutic class: Antifungal
Pregnancy category: C
Indications
To treat oral and esophageal candidiasis ORAL SUSPENSION,,
I.V.INJECTION Adults and adolescents. 200 mg on day 1 followed by 100 mg daily for at least 2 (oral) or 3 (esophageal) wk after symptoms resolve. Children.3 mg/kg daily for at least 2 (oral) or 3 (esophageal) wk and then for 2 wk after esophageal symptoms resolve. To treat systemic candidiasis ORAL SUSPENSION,,
I.V.INJECTION Adults and adolescents.400 mg on day 1, followed by 200 mg daily for at least 4 wk and then for additional 2 wk after symptoms resolve. To treat cryptococcal meningitis ORAL SUSPENSION,,
I.V.INJECTION Adults and adolescents.400 mg daily until patient responds to treatment, then 200 to 400 mg daily for 10 to 12 wk after CSF culture is negative. Maintenance: 200 mg daily to suppress relapse. Children.6 to 12 mg/kg daily for 10 to 12 wk after CSF culture is negative. To prevent candidiasis after bone marrow transplantation ORAL SUSPENSION,,
I.V.INJECTION Adults and adolescents.400 mg daily starting several days before procedure if severe neutropenia is expected and continued for 7 days after absolute neutrophil count exceeds 1,000/mm3. To treat vaginal candidiasis , ORAL SUSPENSION,
Adults. 150 mg as a single dose.
DOSAGE ADJUSTMENT Dosage reduced for patients with hepatic or renal impairment. Dosage reduced by 50% for patients with creatinine clearance of 11 to 50 ml/min/ 1.73 m2.
Mechanism of Action
Damages fungal cells by interfering with a cytochrome P-450 enzyme needed to confluconazole 443 E F vert lanosterol to ergosterol, an essential part of the fungal cell membrane. Decreased ergosterol synthesis causes increased cell permeability, which allows cell contents to leak. Fluconazole also may inhibit endogenous respiration, interact with membrane phospholipids, inhibit transformation of yeasts to mycelial forms, inhibit purine uptake, and impair biosynthesis of triglycerides and phospholipids.
Incompatibilities
Don’t add fluconazole to I.V. bag that contains any other drug.
Contraindications
Hypersensitivity to fluconazole or its components
Interactions
astemizole, terfenadine: Increased blood levels of these benzodiazepines (short-acting): Possibly increased benzodiazepine level and psychomotor effects
cimetidine: Decreased fluconazole level cisapride: Possibly increased QT interval, leading to torsades de pointes cyclosporine: Increased cyclosporine level glipizide, glyburide, tolbutamide: Increased risk of hypoglycemia hydrochlorothiazide: Increased fluconazole level from decreased excretion isoniazid,
rifampin: Decreased fluconazole effects nonsedating antihistamines: Increased blood antihistamine level, increased risk of cardiotoxicity oral anticoagulants: Increased anticoagulant effects
phenytoin: Increased phenytoin level
rifabutin: Increased rifabutin level
theophylline: Increased theophylline level zidovudine: Increased zidovudine level
Side Efect
CNS: Chills, dizziness, drowsiness, fever, headache, seizures
CV: Prolonged QT interval, torsades de pointes
GI: Abdominal pain, anorexia, constipation, diarrhea, hepatic failure, nausea, vomiting
HEME: Agranulocytosis, leukopenia, thrombocytopenia
SKIN: Exfoliative dermatitis, photosensitivity, pruritus, rash
Other: Anaphylaxis, angioedema
Cautions
Use fluconazole cautiously in patients with potentially proarrhythmic conditions because drug may prolong the QT interval, which can lead to life-threatening torsades de pointes. Expect to obtain BUN and serum creatinine levels and culture and sensitivity and liver function test results before therapy starts. Refrigerate, but don’t freeze, fluconazole oral suspension. Shake well before administering. Discard I.V. solution that’s cloudy or contains precipitate. Don’t infuse more than 200 mg/hr or add supplemental to infusion. Monitor hepatic and renal function periodically during therapy, and notify prescriber if you detect signs of dysfunction. Assess for rash every 8 hours during therapy, and notify prescriber if rash occurs. If patient receives an oral anticoagulant, monitor coagulation test results and assess patient for bleeding. Monitor patient for symptoms of overdose, such as hallucinations and paranoia. If they occur, provide supportive treatment, gastric lavage, and, possibly, hemodialysis, which can reduce blood fluconazole level by half after about 3 hours. PATIENT SAFTY
Instruct patient to take fluconazole tablets or oral suspension 30 minutes before or 2 hours after meals. Inform her that tablets may be crushed for easier swallowing if needed. Advise patient to complete entire course of therapy, even if she feels better. If patient takes an oral antidiabetic, urge her to monitor blood glucose level often because of increased risk of hypoglycemia. Alert patient that fluconazole may change the taste of food. Encourage patient to notify prescriber immediately about diarrhea, headache, nausea, rash, right-upper-quadrant abdominal pain, yellow skin or whites of eyes, or vomiting. Suggest that breast-feeding patient consult prescriber because breast-feeding may need to be stopped during therapy.
Trade Name & Company Name
effect of Fluconazole in Pregnancy, Fetal Health
and Breast feeding
Pregnancy
. There are no adequate reports or well-controlled studies of fluconazole in pregnant women. It has been used for the treatment of coccidioidomycosis during Pregnancy
and Candida sepsis postpartum. The systemic antifungal drug with which there has been the most experience is amphotericin B. Fetal Health
There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fluconazole crosses the human placenta. Four children are described with a similar and rare pattern of anomalies. The features include brachycephaly, abnormal facies, abnormal calvarial development, cleft palate, femoral bowing, thin ribs and long bones, arthrogryposis and congenital heart disease. Each was associated with chronic, parenteral use in the 1st trimester. Limited duration oral therapy is unlikely to pose a teratogenic risk. Fluconazole does not appear to increase the risks of IUGR or preterm delivery. It has been used for the treatment of congenital candidiasis. Rodent studies conducted at multiples of the MRHD revealed a variety of ossification defects considered consistent with inhibition of estrogen synthesis. There was an increased risk of cleft palate in rats when combined with phenytoin. Similar concerns have been reported in humans. Breastfeeding
There are no adequate reports or well-controlled studies in nursing women. Fluconazole enters human breast milk at concentrations similar to maternal plasma. It is generally recommended that Breastfeeding be avoided. 401
the follwing drugs will increse Fluconazole by inhepiting cyp450
the follwing drugs will decrease Fluconazole by inhancing cyp450
trad drugs based on Fluconazole
| Gen name | Trade name | Catagory name |
| Fluconazole | CANDIVAST 150MG CAP | |
| Fluconazole | CANDIVAST 50MG CAP | |
| Fluconazole | DIFLUCAN 150MG CAPS | |
| Fluconazole | DIFLUCAN 200MG CAPS | |
| Fluconazole | DIFLUCAN 50MG CAPS | |
| Fluconazole | FLUCAND 200MG-100ML INFUSION VIAL | |
| Fluconazole | FUNZOL 150MG CAPSULES | |
| Fluconazole | MYXEN 150MG TABLETS | |
| Fluconazole | MYXEN 50MG TABLETS | |
| Fluconazole | ORAMAX 150MG CAPSULES | |
other drugs from same cataogory
| Gen name | trade name | catogry |