Delavirdine mesylate


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Delavirdine mesylate
Delavirdine mesylate (Rescriptor)
Delavirdine mesylate
(deh-lah- VIR-deen)
Pregnancy Category: C Rescriptor (Rx)

Classification: Antiviral drug, nonnucleoside reverse transcriptase inhibitor

See Also: See also Antiviral Drugs.

Action/Kinetics: Non-nucleoside reverse transcriptase inhibitor that binds directly to reverse transcriptase and blocks RNA-dependent and DNA-dependent DNA polymerase activities. Effect is additive if used with other antiviral drugs. Delavirdine may confer cross-resistance to other non-nucleoside reverse transcriptase inhibitors when used alone or in combination. Rapidly absorbed. Peak plasma levels: About 1 hr. Extensively bound to plasma albumin. Converted to inactive metabolites which are excreted in urine and feces. It inhibits its own metabolism.

Uses: Treatment of HIV-1 infections in combination with appropriate antiretroviral agents.

Special Concerns: Use with caution in impaired hepatic function. Safety and efficacy in combination with other antiretroviral drugs have not been determined in HIV-1-infected clients less than 16 years of age.

Side Effects: Body as a whole: Headache, fatigue, asthenia, allergic reaction, chest pain, chills, general or local edema, fever, flu syndrome, lethargy, malaise, neck rigidity, general or local pain, trauma. CV: Bradycardia, migraine, pallor, palpitation, postural hypotension, syncope, tachycardia, vasodilation. CNS: Abnormal coordination, agitation, amnesia, anxiety, change in dreams, cognitive impairment, confusion, decreased libido, depression, disorientation, dizziness, emotional lability, hallucinations, hyperesthesia, hyperreflexia, hypesthesia, impaired coordination, insomnia, mania, nervousness, neuropathy, nightmares, paralysis, paranoia, paresthesia, restlessness, somnolence, tingling, tremor, vertigo, weakness. GI: N&V, diarrhea, anorexia, aphthous stomatitis, bloody stool, colitis, constipation, appetite decreased or increased, diarrhea, duodenitis, dry mouth, diverticulitis, dyspepsia, dysphagia, fecal incontinence, flatulence, enteritis, esophagitis, gastritis, gagging, gastroesophageal reflux, GI bleeding or disorder, gingivitis, gum hemorrhage, increased saliva, increased thirst, mouth ulcer, abdominal cramps/distention/pain, lip edema, hepatitis (nonspecified), pancreatitis, rectal disorder, sialadenitis, stomatitis, tongue edema, ulceration. Dermatologic: Skin rashes, maculopapular rash, pruritus, angioedema, dermal leukocytoblastic vasculitis, dermatitis, desquamation, diaphoresis, dry skin, erythema, erythema multiforme, folliculitis, fungal dermatitis, alopecia, nail disorder, petechial rash, seborrhea, skin disorder, skin nodule, Stevens-Johnson syndrome vesiculobullous rash, sebaceous cyst. GU: Breast enlargement, kidney calculi, epididymitis, hematuria, hemospermia, impotence, kidney pain, metrorrhagia, nocturia, polyuria, proteinuria, vaginal moniliasis. Musculoskeletal: Back pain, neck rigidity, arthritis or arthralgia of single or multiple joints, bone disorder or pain, leg cramps, muscle weakness, myalgia, tendon disorder, tenosynovitis, tetany, muscle cramps. Respiratory: Upper respiratory infection, bronchitis, chest congestion, cough, dyspnea, epistaxis, laryngismus, pharyngitis, rhinitis, sinusitis. Hematologic: Anemia, bruises, ecchymosis, eosinophilia, granulocytosis, neutropenia, pancytopenia, petechiae, purpura, spleen disorder, thrombocytopenia. Ophthalmic: Nystagmus, blepharitis, conjunctivitis, diplopia, dry eyes, photophobia. Miscellaneous: Alcohol intolerance, peripheral edema, weight increase or decrease, taste perversion, tinnitus, ear pain.

Laboratory Test Alterations: ALT, AST, bilirubin, GGT, lipase, serum alkaline phosphatase, serum amylase, serum creatinine phosphatase, serum creatinine. Bilirubinemia, hyperkalemia, hyperuricemia, hypocalcemia, hyponatremia, hypophosphatemia

Drug Interactions: Antacids / Delavirdine absorption; separate doses by 1 hr Anticonvulsants / Delavirdine plasma levels R/T hepatic metabolism Astemizole / Possible serious or life-threatening drug side effects R/T metabolism Benzodiazpines / Possible serious or life-threatening drug side effects R/T metabolism Calcium channel blockers, dihydropyridine-type / Possible serious or life-threatening drug side effects R/T metabolism Cisapride / Possible serious or life-threatening drug side effects R/T metabolism Clarithromycin / Significant in amount absorbed of both drugs; possible serious side effects Dapsone / Possible serious or life-threatening drug side effects of dapsone R/T metabolism Didanosine / Absorption of both drugs; separate administration by at least 1 hr Ergot derivatives / Possible serious or life-threatening drug side effects of ergot R/T metabolism Fluoxetine / Trough levels of delavirdine by 50% Indinavir / Indinavir levels R/T metabolism; possible serious side effects Quinidine / Possible serious or life-threatening drug side effects R/T metabolism Rifabutin, Rifampin / Delavirdine plasma levels R/T hepatic metabolism Saquinavir / Saquinavir levels R/T metabolism; possible serious side effects Terfenadine / Possible serious or life-threatening terfenadine side effects R/T metabolism Warfarin / Possible serious or life-threatening warfarin side effects R/T metabolism

How Supplied: Tablets: 100 mg, 200 mg

Dosage
?Tablets HIV-1 infection.
400 mg t.i.d. in combination with other antiretroviral therapy.