delavirdine (Discontinued)

Brand and Other Names:Rescriptor
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 100mg
  • 200mg

HIV-1 Infection

May 11, 2017: Manufacturer announced delavirdine will be discontinued; supply expected to be depleted by October 2018

400 mg PO q8hr with other antiretrovirals

Solution administration

  • Add 100 mg-tablets (4 tablets totaling 400 mg) in at least 3 oz water; allow to stand for few minutes
  • Do NOT use 200 mg tablets (not well-dispersed in water)
  • Stir slurry until mixed uniformly; consume promptly
  • Rinse glass with water and swallow entire contents of rinse

Administration

Used in combination with at least 2 other antiretroviral agents

Dosage Forms & Strengths

tablet

  • 100mg
  • 200mg

HIV-1 Infection

<16 years

  • Safety and efficacy not established

>16 years

  • May 11, 2017: Manufacturer announced delavirdine will be discontinued; supply expected to be depleted by October 2018
  • 400 mg PO q8hr with other antiretrovirals
  • Solution administration:
  • Add 100 mg-tablets (4 tablets totaling 400 mg) in at least 3 oz water; allow to stand for few minutes
  • Do NOT use 200 mg tablets (not well-dispersed in water)
  • Stir slurry until mixed uniformly; consume promptly
  • Rinse glass with water and swallow entire contents of rinse
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Interactions

Interaction Checker

and delavirdine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Rash (32-35%)

            Headache (19-20%)

            Fever (4-12%)

            Depression (10-15%)

            Nausea (20%)

            Vomiting (3-11%)

            1-10%

            Diarrhea (4-6%)

            Anxiety (6-8%)

            Abdominal pain (4-6%)

            Increased prothrombin time (2%)

            Bronchitis (6-8%)

            Decreased hemoglobin (1-3%)

            Frequency Not Defined

            Adenopathy

            Anorexia

            Chest congestion

            Colitis

            Conjunctivitis

            Gastroenteritis

            Hypertension

            Urinary tract infection

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            Warnings

            Black Box Warnings

            Indicated for use only in combination with appropriate antiretroviral drugs

            Resistant virus emerges rapidly when delavirdine is administered as monotherapy

            Contraindications

            Hypersensitivity

            Coadministration with drugs highly dependent on CYP3A4 for clearance and those for which elevated plasma levels are associated with serious or life-threatening events (eg, dihydroergotamine, ergonovine, ergotamine, methylergonovine, cisapride, pimozide, alprazolam, midazolam, triazolam)

            Coadministration with drugs (eg, CYP inducers) where significant decreases in delavirdine plasma concentrations may occur, which may result in loss of virologic response and possible resistance and cross-resistance to other NNRTIs

            Cautions

            Use only in combination with other antiretroviral drugs - delavirdine alone results in rapid resistance

            Patients with achlorhydria should take with acidic juice

            Avoid antacids 1 hr prior to and after administration

            Discontinue if severe rash or rash with associated mucocutaneous lesions; erythema multiforme and Stevens-Johnson Syndrome

            Avoid St John's wort: may result in loss of virologic response/resistance

            Hepatic impairment

            Rash may occur within 1-3 weeks and lasts < 2 weeks; discontinue treatment and resume after brief interruption

            May cause redistribution of fat (cushingoid appearance)

            Risk of cross resistance to other NNRTI

            Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: Not known whether distributed into milk. Because of both the potential for HIV transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breastfeed.

            Health professionals should contact the antiretroviral pregnancy registry to monitor outcomes of pregnant women exposed to delavirdine or other antiretroviral medications by calling 1-800-258-4263 or going to www.APRegistry.com.

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) of HIV-1

            Directly binds to reverse transcriptase and inhibits RNA- & DNA-dependent DNA polymerase activity

            Pharmacokinetics

            Absorption: Rapid

            Distribution: Low concentration in saliva & semen; CSF 0.4% concurrent plasma concentration

            Protein Bound: ~98%, primarily albumin

            Bioavailability: 85%; ~20% increased with slurry

            Half-life: 5.8 hr (mean)

            Peak Plasma Time: 1 hr

            Metabolism: Hepatic via CYP3A4 & 2D6

            Excretion: Urine (51%, <5% as unchanged drug); feces (44%)

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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.