Trade Names:Rescriptor- Tablets 100 mg
Inhibits replication of HIV-1 infection by interfering with DNA synthesis.
Rapidly absorbed. T max approximately 1 h. C max approximately 35 mcM. AUC approximately 180 mcM•h.
Approximately 98% protein bound, primarily albumin.
Primarily metabolized by CYP3A and possibly CYP2D6 to several inactive metabolites.
Approximately 44% excreted in feces and approximately 51% in urine (less than 5% as unchanged drug). t ½ is approximately 5.8 h.
Treatment of HIV-1 infection in combination with appropriate antiretroviral agents when therapy is warranted.
PO 400 mg 3 times daily in combination with appropriate antiretroviral therapy.
Store at controlled room temperature in tightly closed container. Protect from high humidity.
Antacids reduce absorption of delavirdine. Separate doses by at least 1 h.Anticonvulsants (eg, carbamazepine, phenobarbital, phenytoin)
Induce hepatic metabolism of delavirdine resulting in decreased plasma concentrations.Benzodiazepines (eg, alprazolam, midazolam, triazolam)
Delavirdine may increase blood levels of these drugs, which may produce extreme sedation and respiratory depression.Cisapride, dapsone, ergot derivatives, quinidine, rifabutin, warfarin
Delavirdine may elevate blood levels of these drugs, which may increase the risk of arrhythmias or other potentially serious adverse reactions.Clarithromycin
Coadministration may increase blood levels of delavirdine or clarithromycin.Didanosine
Separate administration of didanosine and delavirdine by at least 1 h; coadministration results in a 20% reduction in systemic exposure of both drugs.Dihydropyridine calcium channel blockers (eg, nifedipine)
Delavirdine may elevate blood levels, which may increase toxicity.Fluoxetine, ketoconazole
Increased delavirdine plasma concentrations.H 2 antagonists (eg, cimetidine)
Concurrent use may reduce absorption of delavirdine. Chronic use of these drugs with delavirdine is not recommended.Indinavir
Delavirdine inhibits metabolism of indinavir. Consider indinavir dosage reduction if coadministered with delavirdine.Rifabutin, rifampin
Induce hepatic metabolism of delavirdine resulting in decreased plasma concentrations. These agents should not be coadministered with delavirdine.Saquinavir
Delavirdine inhibits metabolism of saquinavir. Monitor hepatocellular enzymes frequently if coadministered.
None well documented.
Fatigue; tachycardia; bradycardia; pallor; palpitation; postural hypotension; syncope; vasodilation.
Lethargy; headache; migraine; abnormal coordination; agitation; amnesia; anxiety; change in dreams; cognitive impairment; confusion; depression; disorientation; dizziness; emotional lability; hallucination; hyperesthesia; impaired concentration; insomnia; manic symptoms; nervousness; neuropathy; nightmares; paranoid symptoms; paresthesia; restlessness; somnolence; tingling; tremor; vertigo.
Rash; pruritus; angioedema; dermal leukocytoblastic vasculitis; dermatitis; desquamation; sweating; dry skin; erythema; erythema multiforme; folliculitis; fungal dermatitis; alopecia; nail disorder; petechial rash; seborrhea; skin nodule; Stevens-Johnson syndrome; urticaria; vesiculobullous rash; bruise; ecchymosis; petechia; purpura.
Nystagmus; blepharitis; conjunctivitis; diplopia; dry eyes; photophobia; tinnitus; ear pain; esophagitis; laryngismus; pharyngitis; sinusitis; rhinitis; epistaxis.
Nausea; diarrhea; vomiting; abdominal cramps; distention; pain; lip edema; anorexia; aphthous stomatitis; bloody stool; colitis; constipation; decreased appetite; diverticulitis; duodenitis; dry mouth; dyspepsia; dysphagia; enteritis; fecal incontinence; flatulence; gagging; gastritis; gastroesophageal reflux; GI bleeding; gingivitis; gum hemorrhage; increased appetite; increased saliva; thirst; mouth ulcer; pancreatitis; rectal disorder; sialadenitis; stomatitis; tongue edema; ulceration; taste perversion.
Decreased libido; breast enlargement; kidney calculi; epididymitis; hematuria; hemospermia; impotence; kidney pain; metrorrhagia; nocturia; polyuria; proteinuria; vaginal moniliasis.
Anemia; eosinophilia; granulocytosis; neutropenia; pancytopenia; prolonged partial thromboplastin; spleen disorder; thrombocytopenia.
Increased ALT; increased AST; hepatitis.
Bilirubinemia; hyperkalemia; hyperuricemia; hypocalcemia; hyponatremia; hypophosphatemia; increased gamma glutamyl transpeptidase, lipase, serum alkaline phosphatase, serum amylase, serum creatinine phosphokinase, or serum creatinine; peripheral edema.
Upper respiratory infection; bronchitis; chest congestion; cough; dyspnea.
Asthenia; back pain; chest pain; flank pain; chills; edema; fever; flu-like syndrome; lethargy; weakness; malaise; neck rigidity; sebaceous and epidermal cysts; muscle cramps; paralysis; weight increase or decrease; arthralgia; arthritis; bone disorder; bone pain; myalgia; tendon disorder; tenosynovitis; tetany.
Category C .
Undetermined. HIV infected mothers should not breast-feed their infants.
Safety and efficacy in children younger than 16 yr of age not established.
Delavirdine is metabolized primarily by the liver. Use with caution in patients with hepatic function impairment.
Rash is the most common adverse reaction and may range from minor to severe.
Resistant virus emerges rapidly when delavirdine is administered as monotherapy. Always use in combination with appropriate antiretroviral therapy.
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