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Delavirdine

 

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Delavirdine



 
 
Delavirdine (DLV) (brand name Rescriptor) is a non-nucleoside reverse transcriptase inhibitor
Reverse transcriptase inhibitor

Reverse transcriptase inhibitors are a class of antiretroviral drug used to treat HIV infection, tumors, and cancer. RTIs inhibit activity of reverse transcriptase, a viral DNA polymerase enzyme that retroviruses need to reproduce....
 (NNRTI) marketed by Pfizer
Pfizer

Pfizer Incorporated is a major pharmaceutical company, ranking number one in sales in the world. The company is based in New York City, and its research headquarters is in Groton, Connecticut....
. It is used as part of highly active antiretroviral therapy (HAART) for the treatment of human immunodeficiency virus (HIV) type 1. It is presented as the mesylate. The recommended dosage is 400 mg, three times a day.

Although delavirdine was approved by the U.S. Food and Drug Administration
Food and Drug Administration

The U.S. Food and Drug Administration is an Government agency of the United States Department of Health and Human Services and is responsible for regulating and supervising the safety of foods, dietary supplements, Medications, vaccines, Biopharmaceutical, blood transfusion, medical devices, Electromagnetic radiation-emitting devices, veteri...
 in 1997, its efficacy is lower than other NNRTIs, especially efavirenz
Efavirenz

Efavirenz is a non-nucleoside reverse transcriptase inhibitor and is used as part of highly active antiretroviral therapy for the treatment of a human immunodeficiency virus type 1....
, and it also has an inconvenient schedule.






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Delavirdine (DLV) (brand name Rescriptor) is a non-nucleoside reverse transcriptase inhibitor
Reverse transcriptase inhibitor

Reverse transcriptase inhibitors are a class of antiretroviral drug used to treat HIV infection, tumors, and cancer. RTIs inhibit activity of reverse transcriptase, a viral DNA polymerase enzyme that retroviruses need to reproduce....
 (NNRTI) marketed by Pfizer
Pfizer

Pfizer Incorporated is a major pharmaceutical company, ranking number one in sales in the world. The company is based in New York City, and its research headquarters is in Groton, Connecticut....
. It is used as part of highly active antiretroviral therapy (HAART) for the treatment of human immunodeficiency virus (HIV) type 1. It is presented as the mesylate. The recommended dosage is 400 mg, three times a day.

Although delavirdine was approved by the U.S. Food and Drug Administration
Food and Drug Administration

The U.S. Food and Drug Administration is an Government agency of the United States Department of Health and Human Services and is responsible for regulating and supervising the safety of foods, dietary supplements, Medications, vaccines, Biopharmaceutical, blood transfusion, medical devices, Electromagnetic radiation-emitting devices, veteri...
 in 1997, its efficacy is lower than other NNRTIs, especially efavirenz
Efavirenz

Efavirenz is a non-nucleoside reverse transcriptase inhibitor and is used as part of highly active antiretroviral therapy for the treatment of a human immunodeficiency virus type 1....
, and it also has an inconvenient schedule. These factors have led the U.S. DHHS not to recommend its use as part of initial therapy. The risk of cross-resistance across the NNRTI class, as well as its complex set of drug interactions, make the place of delavirdine in second-line and salvage therapy unclear, and it is currently rarely used.

Like ritonavir
Ritonavir

Ritonavir, with trade name Norvir , is an antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS.Ritonavir is frequently prescribed with HAART, not for its antiviral action, but as it inhibits the same host enzyme that metabolizes other protease inhibitors....
, delavirdine is an inhibitor of cytochrome P450 isozyme CYP3A4
CYP3A4

Cytochrome P450 3A4 , a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body....
, and interacts with many medications. It should not be administered with a wide range of drugs, including amprenavir
Amprenavir

Amprenavir is a protease inhibitor used to treat HIV infection. It was approved by the Food and Drug Administration on April 15, 1999, for twice-a-day dosing instead of needing to be taken every eight hours....
, fosamprenavir
Fosamprenavir

Fosamprenavir is a pro-drug of the protease inhibitor and antiretroviral drug amprenavir. The FDA approved it October 20, 2003, while the EMEA approved it on July 12, 2004....
, simvastatin
Simvastatin

Simvastatin , is a hypolipidemic agent belonging to the class of pharmaceuticals called "statins". It is used to control hypercholesterolemia and to prevent cardiovascular disease....
, lovastatin
Lovastatin

Lovastatin is a member of the drug class of statins, used for lowering cholesterol in those with hypercholesterolemia and so preventing cardiovascular disease....
, rifampin, rifabutin
Rifabutin

Rifabutin is a bactericidal antibiotic drug primarily used in the treatment of tuberculosis. The drug is a semi-synthetic derivative of rifamycin S....
, rifapentine
Rifapentine

Rifapentine is an antibiotic drug used in the treatment of tuberculosis....
, St John's wort
St John's wort

St John's wort used alone refers to the species Hypericum perforatum, also known as Tipton's Weed or Klamath weed, but, with qualifiers, is used to refer to any species of the genus Hypericum....
, astemizole
Astemizole

Astemizole is a second generation antihistamine drug which has a long duration of action. Astemizole was discovered by Janssen Pharmaceutica in 1977....
, midazolam
Midazolam

Midazolam, pronounced m?'d?z?l?m is a drug which is a benzodiazepine derivative . It has potent anxiolytic, amnestic, hypnotic, anticonvulsant, skeletal muscle relaxant and sedative properties....
, triazolam
Triazolam

Triazolam is a benzodiazepine derivative drug. It possesses pharmacological properties similar to that of other benzodiazepines, but it is generally only used as a sedative to treat insomnia....
, ergot
Ergot

Ergot refers to a group of fungus of the genus Claviceps . The most prominent member of this group is Claviceps purpurea. This fungus grows on rye and related plants, and can cause ergotism in humans and other mammals consuming seeds contaminated with the fruiting structure of this fungus, called an ergot sclerotium....
 medications, and several medications for acid reflux.

The most common adverse event is moderate to severe rash
Rash

A rash is a change of the skin which affects its color, appearance, or texture. A rash may be localized in one part of the body, or affect all the skin....
, which occurs in up to 20% of patients. Other common adverse events include fatigue
Fatigue (physical)

Fatigue is a weariness caused by exertion. It can describe a range of afflictions, varying from a general state of wikt:lethargy to a specific work-induced burning sensation within one's muscles....
, headache
Headache

In medicine a headache or wiktionary:cephalalgia is a symptom of a number of different conditions of the head and sometimes neck. Some of the causes are benign while others are medical emergencies....
 and nausea
Nausea

Nausea is the sensation of unease and discomfort in the stomach with an urge to vomit....
. Liver toxicity has also been reported.