delavirdine

Action and Spectrum

Actions and Spectrum: 

A drug called delavirdine is used to treat HIV infection. As a non-nucleoside reverse transcriptase inhibitor (NNRTI), it prevents the reverse transcriptase enzyme, which the virus needs to reproduce, from doing its job. 

A variety of HIV-1 strains, even those that are resistant to other NNRTIs like nevirapine and efavirenz, are inhibited from replicating when treated with delavirdine. 

Drug Interaction

Adverse Reaction

Frequency Defined  

>10%  

Rashes (19.5%) 

Grade 1 rash (16.7%) 

Grade 2 rash (14.3%) 

Nausea (20.3%) 

Headache (16.8%) 

Asthenia/fatigue (16%) 

Depressive symptoms (12.6%) 

Post marketing reports 

Hemolytic anemia 

Acute renal failure 

Rhabdomyolysis 

Hepatic failure  

1-10% 

Grade 3 rash (vesiculation, moist desquamation, ulceration) 

Generalized abdominal pain 

Increased amylase 

Vomiting 

Fever 

Upper respiratory infection 

Sinusitis 

Bronchitis 

Cough 

Influenza syndrome 

localized pain 

Anxiety 

Insomnia 

Decreased neutrophils  

Decreased hemoglobin  

Prolonged prothrombin time  

Increased activated partial thromboplastin 

Increased ALT  

Increased AST 

Increased bilirubin 

Hyperglycemia or hypoglycemia 

Black Box Warning

Black Box Warning 

delavirdine carries a black box warning from the U.S. Food and Drug Administration (FDA) owing to the possibility of significant and even fatal adverse effects. 

The following hepatotoxicity is listed in the delavirdine black box warning: Hepatitis, increased liver enzyme levels, and liver failure have all been linked to delavirdine’s liver damage. When using delavirdine, patients should be continuously watched for any indications of liver disease. 

delavirdine has been linked to a severe, potentially fatal skin rash. When using delavirdine, patients who have a rash should visit a doctor right once. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Those who have a known hypersensitivity or allergy to delavirdine or any of its ingredients shouldn’t use it. 
• Rifampicin, carbamazepine, phenobarbital, St. John’s wort, and other medications that strongly activate or inhibit the cytochrome P450 3A enzyme system should not be taken together with delavirdine. 

Caution  

• Several other medicines, including prescription and non-prescription drugs, dietary supplements, and herbal therapies, may interact with delavirdine. 
• delavirdine may harm the liver, thus patients who already have liver disease or are taking other drugs that harm the liver need to be constantly watched. 
• A severe skin rash from delavirdine has the potential to be fatal. People should consult a doctor right away if they develop a rash. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category
 

Pharmacology

Pharmacology 

delavirdine is extensively metabolized in the liver, predominantly by the cytochrome P450 (CYP) enzyme system and is strongly protein-bound (98%) to protein. Its strong CYP3A4 and CYP2D6 enzyme inhibitory properties can cause important drug interactions with other drugs that are metabolized via these pathways. 

Pharmacodynamics 

The HIV reverse transcriptase enzyme, which is necessary for viral replication, is inhibited by delavirdine, which is connected to its pharmacodynamics. delavirdine is a member of the group of drugs known as non-nucleoside reverse transcriptase inhibitors (NNRTIs), which stop the activity of the reverse transcriptase enzyme by binding to a particular location on the enzyme. 

Pharmacokinetics  

Absorption   

delavirdine is efficiently absorbed when taken orally, and within 2-4 hours after dosage, peak plasma concentrations are reached. delavirdine’s bioavailability can be increased by eating, especially high-fat meals. 

Distribution 

delavirdine is extensively distributed throughout tissues, including the lungs, liver, and lymphoid tissue, and it is strongly protein-bound (98%). It has a distribution volume of around 0.6 L/kg. 

Metabolism 

delavirdine’s main metabolite, hydroxylated and effective against HIV. delavirdine’s own metabolism is inhibited, which leads to higher plasma concentrations with repeated doses. 

Elimination and excretion 

Less than 5% of delavirdine is excreted in the urine, with the majority of its elimination occurring in the feces. delavirdine has an elimination half-life of around 5-7 hours. 

Adminstartion

Administration:  

Usually, delavirdine is used orally, either with or without meals. It is crucial to adhere to your healthcare provider’s dose and timing recommendations. To keep medication levels in the body constant throughout the day, delavirdine should be given at regular intervals. 

delavirdine should not be skipped or stopped abruptly without first talking to your doctor, since doing so might result in the emergence of HIV strains that are resistant to the medication. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: delavirdine 

Why do we use delavirdine? 

Antiretroviral drug delavirdine is used to treat HIV-1 infections.  

delavirdine is used with other antiretroviral drugs to treat HIV infection. delavirdine can lower the level of HIV in the blood and prevent the spread of the illness by inhibiting the reverse transcriptase enzyme’s activity. 

delavirdine may be used to stop mother-to-child HIV transmission.