The non-nucleoside reverse transcriptase inhibitors have direct effects on the HIV virus activities within the cell. The non-nucleoside reverse transcriptase inhibitors available include delavirdine (Rescriptor), efavirenz (Sustiva), and nevirapine (Viramune).
The non-nucleoside reverse transcriptase inhibitors bind directly to HIV reverse transcriptase, blocking both RNA and DNA-dependent DNA polymerase activities. They prevent the transfer of information that would allow the virus to carry on the formation of viral DNA. As a result, the virus is unable to take over the cell and reproduce. These antiviral agents are indicated for the treatment of patients with documented AIDS or ARC who have decreased numbers of T cells and evidence of increased opportunistic infections in combination with other antiviral drugs.
Delavirdine is rapidly absorbed from the GI tract, with peak levels occurring within 1 hour. Delavirdine is extensively metabolized by the cytochrome P450 system in the liver and is excreted through the urine.
地拉韦啶经胃肠道迅速吸收，1小时内达峰。地拉韦啶在肝内被细胞色素P450广泛代谢，经尿排出。
Efavirenz is absorbed rapidly from the GI tract, reaching peak levels in 3 to 5 hours. Efavirenz is metabolized in the liver by the cytochrome P450 system and is excreted in the urine and feces with a half-life of 52 to 76 hours.
Nevirapine is recommended for use in adults and children older than 2 months. After rapid GI absorption with a peak effect occurring at 4 hours, nevirapine is metabolized by the cytochrome P450 system in the liver. Excretion is through the urine with a half-life of 45 hours.
奈韦拉平推荐用于成人及2个月以上儿童。经胃肠道迅速吸收、4小时达峰后，奈拉韦平在肝被细胞色素P450代谢。经尿排出，半衰期45小时。
Contraindications and Cautions
禁忌症和注意事项
There are no adequate studies of non-nucleoside reverse transcriptase inhibitors in pregnancy, so use should be limited to situations in which the benefits clearly outweigh any risks. It is suggested that women not breast-feed if they are infected with HIV. Safety for the use of delavirdine in children has not been established.
Video Non-Nucleosides Reverse transcriptase Inhibitors
Test 1. A young adult female patient who is human immunodeficiency virus (HIV)-positive has a new prescription for efavirenz (Sustiva). Which information is most important to include in the medication teaching plan?
A. Driving is allowed when starting this medication.
B. Report any bizarre dreams to the health care provider.
C. Continue to use contraception while on this medication.
D. Take this medication in the morning on an empty stomach.
2. Which patient exposure by the nurse is most likely to require postexposure prophylaxis when the patient's human immunodeficiency virus (HIV) status is unknown?
A. Needle stick with a needle and syringe used to draw blood
B. Splash into the eyes when emptying a bedpan containing stool
C. Contamination of open skin lesions with patient vaginal secretions
D. Needle stick injury with a suture needle during a surgical procedure
本期ISPN Review答案： 1. C. Continue to use contraception while on this medication.
Efavirenz can cause fetal anomalies and should not be used in patients who may be pregnant. The drug should not be used during pregnancy because large doses could cause fetal anomalies. Once-a-day doses should be taken at bedtime (at least initially) to help patients cope with the side effects that include dizziness and confusion. Patients should be cautioned about driving when starting this drug. Patients should be informed that many people who use the drug have reported vivid and sometimes bizarre dreams
2. A. Needle stick with a needle and syringe used to draw blood.
Puncture wounds are the most common means for workplace transmission of blood-borne diseases, and a needle with a hollow bore that had been contaminated with the patient's blood would be a high-risk situation. The other situations described would be much less likely to result in transmission of the virus.
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