Delaviridine
Mechanism :
Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1. Delavirdine binds directly to reverse transcriptase (RT) and blocks RNA-dependent and DNA-dependent DNA polymerase activities. Delavirdine does not compete with template: primer or deoxynucleoside triphosphates. HIV-2 RT and human cellular DNA polymerases a, g, or d are not inhibited by delavirdine.
Indication :
Contraindications :
Contraindicated in patients with known hypersensitivity to any of its ingredients. Coadministration is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events.
Dosing :
Under 16 years:
Safety and efficacy not established.
>16 years:
400 mg PO three times daily.
Adverse Effect :
Abdominal cramps, abdominal distention, edema, redistribution/accumulation of body fat, cardiomyopathy, hypertension, migraine, pallor, anorexia, bloody stool, colitis, gingivitis, gum hemorrhage, alcohol intolerance, increased amylase, bilirubinemia, hyperglycemia, hyperkalemia, hypertriglyceridemia, hyperuricemia, hypocalcemia, hyponatremia, hypophosphatemia, increased AST, increased gamma glutamyl transpeptidase, increased lipase, increased serum alkaline phosphatase, increased serum creatinine, angioedema, dermal leukocytoclastic vasculitis, dermatitis.
Interaction :
CYP isoforms: Delavirdine is an inhibitor of CYP3A isoform and other CYP isoforms to a lesser extent including CYP2C9, CYP2D6, and CYP2C19. Coadministration of drugs primarily metabolized by CYP3A (e.g., HMG-CoA reductase inhibitors, and sildenafil) may result in increased plasma concentrations of the coadministered drug that could increase or prolong both its therapeutic or adverse effects.
Hepatic Dose :
Delavirdine is primarily metabolized by the liver, use with caution.