Terbest 250mg tab (Systopic) once daily
Little or no nephrotoxicity. Oral preps. Fungistatic. Inhibit ergosterol syntheis in fungal cell wall.
Canditral 100mg Cap (Glenmark)
Forcan, AF-150mg, 400mg (Systopic).
Both oral & IV.
Long half life.
Good penetration in occular & CSF.
Not effective against Aspergillosis, mucormycosis.
Less effective against C. glabarata, C. krusei.
Preffered Rx in candidemia with 400mg/d.
1st line Rx in Coccidioidomycosis, Cryptococcosis, Histoplasmosis.
Prophylaxis of candidiasis in immunocompromised people.
Side Effects: Rash, headache, dizziness, nausea, vomiting, abdominal pain, diarrhea, elevated liver enzymes, anorexia, fatigue, constipation. Oliguria, hypokalaemia, paraesthesia, seizures, alopecia, Stevens Johnson syndrome, thrombocytopenia, other blood dyscrasias, serious hepatotoxicity including hepatic failure, anaphylactic reaction, QTc prolongation.
Secreted in milk.
Pregnancy Category-C (at 150mg/d) and category-D (400-800mg/d).
Inhibitor of the human cytochrome P450 system.
VFEND-50 & 200mg Tab(Pfizer); Voritro Inj 200mg (Lupin).
1st lineRx in invasive aspergillosis.
Also used in Candidemia (nonneutropenics) and disseminated candidiasis in skin, abdomen, kidney, bladder wall, and wounds.
Esophageal candidiasis.
Emperical Rx: unresolved fever despite broad-spectrum antibiotic therapy who are at risk for breakthrough fungal infections.
Side Effects: Transient visual disturbances, fever, rash, vomiting, nausea, diarrhea, headache, peripheral edema, abdominal pain, and respiratory disorder, phototoxicity, LFT.
Visual disturbance (30%) : approx 1.5 hr after administration, and last approximately 30 minutes. They may go away after continued use. There is no damage to the eye or long-term effect on vision. However, patients taking voriconazole should be advised against driving at night.
Precautions: Being metabolized by hepatic cytochrome P450, voriconazole interacts with some drugs. Contraindicated with some drugs (such as rifampin, rifabutin) and dose adjustments and monitoring when coadministered with others (including cyclosporine, omeprazole, and phenytoin).
Metabolized by the liver, the dose should be halved in patients with mild to moderate hepatic impairment.
Generally no dose adjustment for renal impairment. But avoid IV administration in patients with moderate to severe renal impairment (creatinine clearance below50 mL/min).
Pregnancy Category D.
Safety & effectiveness in patients below 12 years has not been established.
Noxafil (posaconazole) by MSD 100 mg delayed-release tablets and oral suspension. Loading dose of 300 mg B.D. on the first day, followed by 300 mg O.D. from 2nd day of therapy. Injection: 300mg. Oral suspension: 40mg/ml.
Prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk.
Rx of oropharyngeal candidiasis.
Side effects: Diarrhea, nausea, fever, vomiting, headache, coughing, and hypokalemia. Elevations in LFT. Should be avoided in patients with moderate or severe renal impairment. QTc Prolongation.
Inhibits cell wall synthesis, like Penicillin for bacteria. It is fungicidal for yeast but fungistatic for molds. Drug of choice for Candidiasis (yeast), esp. Azole resistant Candidiasis. Emperical Rx of febrile neutropenia. 2nd line drug for Aspergillosis (mold). Low activity against: Histoplasmosis & Blastomycosis. Available as :
Cancidas-MSD, Caspogin-Cipla, Casporan-Ranbaxy.
Low oral bioavailability, so IV.
Long half-life.
Low toxicity. 3% histamine release, 3% phlebitis, 2% NV.
Not a inducer, inhibitor or substrate for CYP.
Renal failure & Dialysis: No interference.
Better or as effective as AmB & Fluconazole.
Category-C
Reduce dose in Liver disease
Decreased occular penetration.
Loading dose of 70mg IV over 1 HR, fol by followed by 50mg IV O.D. Duration: 14 days after last +ve culture. Prolonged duration in neutropenia, use at least 7 days after neutropenia improves. Esophageal: 7-10 days, with no loading dose. Oral dose as suppressive Rx.
Aspergillosis: 2nd line after Voriconazole, AmB or Itraconazole.
Dose with Rifampicin is 70mg/d.
Caspofungin in Liver disease:
Amphotericin-B. Broadest spectrum antifungal. Fungicidal. No oral prep. Significant nephrotoxicity. Original AmB is colloidal deoxicholate.
Now lipid formulations: