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Delavirdine

Medically reviewed by Drugs.com. Last updated on Oct 9, 2020.

Pronunciation

(de la VIR deen)

Index Terms

  • DLV
  • U-90152S

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral, as mesylate:

Rescriptor: 100 mg [DSC], 200 mg [DSC]

Brand Names: U.S.

  • Rescriptor [DSC]

Pharmacologic Category

  • Antiretroviral, Reverse Transcriptase Inhibitor, Non-nucleoside (Anti-HIV)

Pharmacology

Delavirdine binds directly to reverse transcriptase, blocking RNA-dependent and DNA-dependent DNA polymerase activities

Absorption

Rapid

Distribution

Low concentration in saliva and semen; CSF 0.4% concurrent plasma concentration

Metabolism

Hepatic via CYP3A4 and 2D6 (Note: May reduce CYP3A activity and inhibit its own metabolism.)

Excretion

Urine (51%, <5% as unchanged drug); feces (44%); nonlinear kinetics exhibited

Time to Peak

Plasma: 1 hour

Half-Life Elimination

5.8 hours (range: 2 to 11 hours)

Protein Binding

~98%, primarily to albumin

Use: Labeled Indications

HIV-1 infection: Treatment of HIV-1 infection in combination with at least two additional antiretroviral agents. Note: Delavirdine is no longer recommended for use in the treatment of HIV (HHS [adult] 2019).

Contraindications

Hypersensitivity to delavirdine or any component of the formulation; concurrent use of alprazolam, astemizole, cisapride, ergot alkaloids, midazolam, pimozide, rifampin, terfenadine, or triazolam

Dosing: Adult

HIV-1 infection (part of combination): Oral: 400 mg 3 times/day. Note: Delavirdine is no longer recommended for use in the treatment of HIV (HHS [adult] 2019).

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

HIV-1 infection (part of combination): Adolescents ≥16 years: Refer to adult dosing.

Extemporaneously Prepared

A dispersion of delavirdine may be made with tablets. Add four 100 mg tablets to at least 3 oz of water; allow to stand for a few minutes and stir until uniform dispersion. Administer immediately. To ensure full dose is administered, rinse glass and drink liquid; also rinse mouth and swallow following ingestion.

Administration

Patients with achlorhydria should take the drug with an acidic beverage; antacids and delavirdine should be separated by 1 hour. A dispersion of delavirdine may be prepared by adding four 100 mg tablets to at least 3 oz of water. Allow to stand for a few minutes and stir until uniform dispersion. Drink immediately. Rinse glass and mouth, then swallow the rinse to ensure total dose administered. The 200 mg tablets should be taken intact.

Dietary Considerations

May be taken without regard to meals.

Storage

Store at 20°C to 25°C (68°F to 77°F). Protect from humidity.

Drug Interactions

Antacids: May decrease the serum concentration of Delavirdine. Management: Separate doses of delavirdine and antacids by at least 1 hour. Monitor for decreased delavirdine therapeutic effects with this combination. Consider therapy modification

Astemizole: Delavirdine may enhance the arrhythmogenic effect of Astemizole. Delavirdine may increase the serum concentration of Astemizole. Avoid combination

CarBAMazepine: May decrease the serum concentration of Delavirdine. Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to concomitant therapy when possible. If concomitant therapy cannot be avoided, monitor for reduced clinical effects of the CYP3A4 substrate. Consider therapy modification

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Dofetilide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide. Monitor therapy

Efavirenz: Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of Efavirenz. Reverse Transcriptase Inhibitors (Non-Nucleoside) may decrease the serum concentration of Efavirenz. Avoid combination

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification

Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Ergonovine: Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of Ergonovine. Specifically, this would be most likely with delavrdine, while other Non-Nucleoside Reverse Transcriptase Inhibitors may be more likely to decrease the concentration of Ergonovine. Avoid combination

Etravirine: Reverse Transcriptase Inhibitors (Non-Nucleoside) may decrease the serum concentration of Etravirine. This has been observed with the NNRTIs efavirenz and nevirapine. Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of Etravirine. This has been observed with delavirdine. Avoid combination

Flibanserin: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin. Monitor therapy

Fosamprenavir: May decrease the serum concentration of Delavirdine. The active metabolite amprenavir is likely responsible for this effect. Delavirdine may increase the serum concentration of Fosamprenavir. Specifically, delavirdine may increase concentrations of the active metabolite amprenavir. Avoid combination

Fosphenytoin: May decrease the serum concentration of Delavirdine. Delavirdine may increase the serum concentration of Fosphenytoin. Avoid combination

Histamine H2 Receptor Antagonists: May decrease the serum concentration of Delavirdine. Avoid combination

Indinavir: Delavirdine may increase the serum concentration of Indinavir. Management: Consider reducing the indinavir dose to 600 mg every 8 hours if coadministered with delavirdine 400 mg three times daily. Consider therapy modification

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Lemborexant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lemborexant. Management: The maximum recommended dosage of lemborexant is 5 mg, no more than once per night, when coadministered with weak CYP3A4 inhibitors. Consider therapy modification

Lomitapide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 30 mg/day. Consider therapy modification

Lopinavir: Delavirdine may increase the serum concentration of Lopinavir. Management: Consider alternatives to this combination. Safe and effective doses for coadministration have not been determined according to lopinavir/ritonavir prescribing information. Consider therapy modification

Maraviroc: Delavirdine may increase the serum concentration of Maraviroc. Monitor therapy

Mitotane: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification

Nelfinavir: May decrease the serum concentration of Delavirdine. Delavirdine may increase the serum concentration of Nelfinavir. Management: Consider alternatives to this combination. Safe and effective doses for coadministration have not been determined according to the nelfinavir prescribing information. Consider therapy modification

NiMODipine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine. Monitor therapy

Orlistat: May decrease the serum concentration of Antiretroviral Agents. Monitor therapy

Phenytoin: May decrease the serum concentration of Delavirdine. Delavirdine may increase the serum concentration of Phenytoin. Avoid combination

Pimozide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide. Avoid combination

Proton Pump Inhibitors: May decrease the serum concentration of Delavirdine. Management: Chronic therapy with proton pump inhibitors (PPIs) should be avoided in patients treated with delavirdine. The clinical significance of short-term PPI therapy with delavirdine is uncertain, but such therapy should be undertaken with caution. Avoid combination

Rifamycin Derivatives: May increase the metabolism of Delavirdine. Delavirdine may increase the serum concentration of Rifamycin Derivatives. Specifically, Rifabutin serum concentration may be increased. Avoid combination

Rilpivirine: Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of Rilpivirine. This mechanism applies to coadministration of delavirdine. Reverse Transcriptase Inhibitors (Non-Nucleoside) may decrease the serum concentration of Rilpivirine. This mechanism applies to coadministration of efavirenz, etravirine, and nevirapine. Avoid combination

Ritonavir: Delavirdine may increase the serum concentration of Ritonavir. Management: Consider alternatives to this combination. Safe and effective doses for coadministration have not been determined according to lopinavir/ritonavir prescribing information. Consider therapy modification

Saquinavir: Delavirdine may increase the serum concentration of Saquinavir. Consider therapy modification

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Simeprevir: Delavirdine may increase the serum concentration of Simeprevir. Avoid combination

St John's Wort: May decrease the serum concentration of Reverse Transcriptase Inhibitors (Non-Nucleoside). Specifically, St. Johns Wort may increase the metabolism of Reverse Transcriptase Inhibitors (Non-Nucleoside). Avoid combination

Tacrolimus (Systemic): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Tacrolimus (Systemic). Monitor therapy

Terfenadine: Delavirdine may enhance the arrhythmogenic effect of Terfenadine. Delavirdine may increase the serum concentration of Terfenadine. Avoid combination

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Triazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Triazolam. Management: Consider triazolam dose reduction in patients receiving concomitant weak CYP3A4 inhibitors. Consider therapy modification

Ubrogepant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Ubrogepant. Management: In patients taking weak CYP3A4 inhibitors, the initial and second dose (given at least 2 hours later if needed) of ubrogepant should be limited to 50 mg. Consider therapy modification

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Frequency not always defined. Frequency of adverse reactions reported from occurrence in clinical trials with delavirdine when used as part of combination antiretroviral therapy.

Cardiovascular: Cardiac arrhythmia, cardiac insufficiency, cardiac rate disturbance, cardiomyopathy, hypersensitivity angiitis, hypertension, orthostatic hypotension, peripheral vascular disease

Central nervous system: Headache (19% to 20%), depression (10% to 15%), anxiety (6% to 8%), cognitive dysfunction, confusion, emotional lability, hallucination, paralysis, vertigo

Dermatologic: Skin rash (16% to 32%), desquamation, erythema multiforme, fungal dermatitis, Stevens-Johnson syndrome

Endocrine & metabolic: Increased serum transaminases (2% to 5%), increased amylase (3%), increased serum bilirubin (2%), hyperglycemia, hyperkalemia, hypertriglyceridemia, hyperuricemia, hypocalcemia, hyponatremia, hypophosphatemia, increased gamma-glutamyl transferase, menstrual disease, redistribution of body fat

Gastrointestinal: Nausea (20% to 25%), vomiting (3% to 11%), abdominal pain (4% to 6%), anorexia, bloody stools, colitis, diarrhea, diverticulitis, fecal incontinence, gastroenteritis, gastrointestinal hemorrhage, gingival hemorrhage, increased serum lipase, pancreatitis, vomiting

Genitourinary: Hematuria, urinary tract infection

Hematologic & oncologic: Decreased hemoglobin (1% to 3%), prolonged prothrombin time (2%), adenopathy, bruise, eosinophilia, granulocytosis, leukopenia, pancytopenia, purpura, spleen disease, thrombocytopenia

Hepatic: Hepatomegaly, increased serum alkaline phosphatase, jaundice

Hypersensitivity: Angioedema, hypersensitivity reaction

Infection: Abscess, candidiasis (oral/vaginal), infection

Neuromuscular & skeletal: Ostealgia, tetany

Ophthalmic: Conjunctivitis

Renal: Increased serum creatinine, nephrolithiasis, renal pain

Respiratory: Bronchitis (6% to 8%), chest congestion, dyspnea, pneumonia

Miscellaneous: Fever (4% to 12%)

<1%, postmarketing and/or case reports: Acute renal failure, hemolytic anemia, hepatic failure, immune reconstitution syndrome, rhabdomyolysis

Warnings/Precautions

Concerns related to adverse effects:

• Fat redistribution: May cause redistribution of fat (eg, buffalo hump, peripheral wasting with increased abdominal girth, cushingoid appearance).

• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.

• Rash: Occurs frequently, may require discontinuation of therapy; usually occurs within 1-3 weeks and lasts <2 weeks. Most patients may resume therapy following a treatment interruption.

Disease-related concerns:

• Hepatic impairment: Use with caution in patients with hepatic impairment.

• HIV: Appropriate use: Due to rapid emergence of resistance, delavirdine should not be used as monotherapy or as a component of an initial antiretroviral regimen; cross-resistance may be conferred to other non-nucleoside reverse transcriptase inhibitors, although potential for cross-resistance with protease inhibitors is low.

• Renal impairment: Use with caution in patients with renal impairment.

Concurrent drug therapy issues:

• High potential for interactions: Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates (see Drug Interactions); consider alternative agents that avoid or lessen the potential for CYP-mediated interactions.

Special populations:

• Pediatric: Safety and efficacy have not been established in children.

Other warnings/precautions:

• Long-term effects: The long-term effects of delavirdine are not known.

Monitoring Parameters

Liver function tests if administered with saquinavir

Reproductive Considerations

Based on the Health and Humans Services (HHS) perinatal HIV guidelines, delavirdine is not one of the recommended antiretroviral agents for use in females who are trying to conceive.

For males and females living with HIV and planning a pregnancy, maximum viral suppression below the limits of detection with antiretroviral therapy (ART), modification of therapy (if needed), optimization of the woman’s health, and a discussion of the potential risks and benefits of ART therapy during pregnancy is recommended prior to conception (HHS [perinatal] 2019).

Pregnancy Considerations

Outcome information specific to delavirdine use in pregnancy is no longer being reviewed and updated in the Health and Humans Services (HHS) perinatal guidelines. Maternal antiretroviral therapy (ART) may be associated with adverse pregnancy outcomes including preterm delivery, stillbirth, low birth weight, and small for gestational age infants. Actual risks may be influenced by maternal factors such as disease severity, gestational age at initiation of therapy, and specific ART regimen, therefore close fetal monitoring is recommended. Because there is clear benefit to appropriate treatment, maternal ART should not be withheld due to concerns for adverse neonatal outcomes. Long-term follow-up is recommended for all infants exposed to antiretroviral medications; children without HIV but who were exposed to ART in utero and develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential mitochondrial dysfunction. Hypersensitivity reactions (including hepatic toxicity and rash) are more common in women on non-nucleoside reverse transcriptase inhibitor therapy; it is not known if pregnancy increases this risk.

Based on the HHS perinatal HIV guidelines, delavirdine is not one of the recommended antiretroviral agents for use during pregnancy.

In general, ART is recommended for all pregnant females living with HIV to keep the viral load below the limit of detection and reduce the risk of perinatal transmission. Therapy should be individualized following a discussion of the potential risks and benefits of treatment during pregnancy. Monitoring of pregnant females is more frequent than in nonpregnant adults. ART should be continued postpartum for all females living with HIV and can be modified after delivery.

Health care providers are encouraged to enroll pregnant females exposed to antiretroviral medications as early in pregnancy as possible in the Antiretroviral Pregnancy Registry (1-800-258-4263 or http://www.APRegistry.com). Health care providers caring for pregnant females living with HIV and their infants may contact the National Perinatal HIV Hotline (888-448-8765) for clinical consultation (HHS [perinatal] 2019).

Patient Education

What is this drug used for?

• It is used to treat HIV infection.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Nausea

• Vomiting

• Diarrhea

• Loss of strength and energy

• Headache

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Infection

• Depression

• Mood changes

• Swelling

• Vision changes

• Eye pain

• Severe eye irritation

• Change in body fat

• Muscle pain

• Joint pain

• Stevens-Johnson syndrome/toxic epidermal necrolysis like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in mouth, throat, nose, or eyes

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

More about delavirdine

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Other brands: Rescriptor

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