Drug information of Delavirdine

Delavirdine

Drug group:

A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.

Mechanism of effect

Delavirdine binds directly to viral reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by disrupting the enzyme's catalytic site.

Pharmacodynamic

The activity of Delavirdine does not compete with template or nucleoside triphosphates. HIV-2 RT and eukaryotic DNA polymerases (such as human DNA polymerases alpha, beta, or sigma) are not inhibited by Delavirdine.

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%)

Dosage

Adult

HIV-1 Infection

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

Pediatric

HIV-1 Infection

<16 years

  • Safety and efficacy not established

>16 years

  • 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

Drug contraindications

Hypersensitivity

Interactions

Sodium bicarbonate , Lansoprazole , Midazolam , fentanyl , Axitinib , Mefloquine , brigatinib , nasal Mometasone , Efavirenz , Copanlisib , Simeprevir , Etravirine , Dabrafenib , Acalabrutinib , Cabazitaxel , Maraviroc , Halofantrine , Alprazolam , Erythromycin , Everolimus , Irinotecan , Budesonide , Primidone , silodosin , Venetoclax , bosutinib , tolvaptan , levomethadyl acetate , neratinib , eszopiclone , lurasidone , gilteritinib , glasdegib , Ceritinib , Eliglustat , Ruxolitinib , conivaptan , Cabozantinib , Cariprazine , Cobimetinib , Temsirolimus , Naloxegol , ELBASVIR/GRAZOPREVIR , encorafenib , midostaurin , elagolix , ivosidenib , Sonidegib , Crizotinib , Ibrutinib , Isavuconazonium , Iloperidone , Pimavanserin , trabectedine , Duvelisib , Terfenadine , Fesoterodine , Alfuzosin , Pazopanib , Palbociclib , Butorphanol , Ivacaftor , Triazolam , Lumefantrine / artemether , Darifenacin , red yeast rice , Fostamatinib , Panobinostat , Ribociclib , Ticagrelor , Guanfacine , Hydrocodone , Fosphenytoin , Fosamprenavir , Ivabradine , Mifepristone , Tofacitinib , Alfentanil , Osimertinib , Lomitapide , dronedarone , eletriptan , mitotane , valbenazine , Amprenavir , Rifabutin , Ranolazine , astemizole , Quetiapine , Toremifene , Oxycodone , Solifenacin , Enzalutamide , Daclatasvir , eplerenone , ergotamine , ergonovine , Nimodipine , Vinblastin , Vincristin , Vinorelbine , Carbamazepine , Colchicine , Phenytoin , Loratadin , Lovastatin , Methylergonovin , Methylprednisolone , Nilotinib , Sildenafil , Cilostazol , Simvastatin , Cyclosporine , Fluticasone , Phenobarbital , Docetaxel , Disopyramide , Rifampin , Citalopram , Sirolimus , Cisapride , Paclitaxel , Pimozide , Tamsulosin , Triamcinolone , Thioridazine , Deflazacort , Aluminium Mg , Ixazomib , Tasimelteon , Dexlansoprazole , Apalutamide , Flibanserin , Avanafil , Lopinavir and Ritonavir , Larotrectinib , rilpivirine , Brexpiprazole , Gefitinib , Dasatinib , voxelotor , Capmatinib

Alerts

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

Black Box Warnings

Indicated for use only in combination with appropriate antiretroviral drugs

Resistant virus emerges rapidly when delavirdine is administered as monotherapy

Points of recommendation

  • Tell all of your health care providers that you take delavirdine. This includes your doctors, nurses, pharmacists, and dentists.
  • Changes in your immune system can happen when you start taking drugs to treat HIV. If you have an infection that you did not know you had, it may show up when you take delavirdine. Tell your doctor right away if you have any new signs after you start delavirdine, even after taking it for several months. This includes signs of infection like fever, sore throat, weakness, cough, or shortness of breath.
  • This medicine interacts with many other drugs. The chance of delavirdine's side effects may be raised or how well delavirdine works may be lowered. The chance of the other drugs' side effects may also be raised. This may include very bad, life-threatening, or deadly side effects. Check with your doctor and pharmacist to make sure that it is safe for you to take delavirdine with all of your other drugs (prescription or OTC, natural products, vitamins).
  • Do not run out of delavirdine.
  • Have blood work checked as you have been told by the doctor. Talk with the doctor.
  • This medicine is not a cure for HIV. Stay under the care of your doctor.
  • This medicine does not stop the spread of diseases like HIV or hepatitis that are passed through blood or having sex. Do not have any kind of sex without using a latex or polyurethane condom. Do not share needles or other things like toothbrushes or razors. Talk with your doctor.
  • Do not take more than what your doctor told you to take. Taking more than you are told may raise your chance of very bad side effects.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using delavirdine while you are pregnant.

All products:

  • Take with or without food.
  • Keep taking delavirdine as you have been told by your doctor or other health care provider, even if you feel well.
  • It is important that you do not miss or skip a dose of delavirdine during treatment.
  • If you have low stomach acid levels, take delavirdine with an acidic drink like orange or cranberry juice.
  • Do not take didanosine within 1 hour of delavirdine.
  • Do not take antacids within 1 hour of delavirdine.

100 mg tablet:

  • You may put the tablets in at least 3 ounces of water then let it sit for a few minutes. Mix until the tablets dissolve and drink. Rinse glass with more water and drink.

200 mg tablet:

  • Swallow whole. Do not chew, break, or crush.
  • Take a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.
  • If you miss taking delavirdine for a few days in a row, call your doctor before you start taking it again.

Pregnancy level

Group c - Not adequate studies in pregnant women


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