What Are Nonnucleoside Reverse Transcriptase Inhibitors?

Non-nucleoside reverse transcriptase inhibitors belong to non-nucleoside reverse transcriptase inhibitors and are mostly used in combination therapy. Half-life: 2-11 hours; CSF to serum concentration ratio is 0.20.

Non-nucleoside reverse transcriptase inhibitors belong to non-nucleoside reverse transcriptase inhibitors and are mostly used in combination therapy. Half-life: 2-11 hours; CSF to serum concentration ratio is 0.20.

NNRTIs (non-nucleoside reverse transcriptase inhibitors): Different from nucleoside reverse transcriptase inhibitors, the English name is non-nucleoside reverse transcriptase inhibitors. It is a class of small drug molecules that work by binding to a hydrophobic binding pocket near the HIV reverse transcriptase polymerization site. Different from nucleoside reverse transcriptase inhibitors on the substrate binding site of reverse transcriptase. There are currently five non-nucleoside reverse transcriptase inhibitors approved by the FDA, nevirapine, delavirdine, efavirenz, etravirin and ribavirin. Among them, nevirapine and delavirdine belong to the first generation of NNRTIS, and efavirenz are the second generation inhibitors. Both types of inhibitors have been used for more than ten years and have produced stable drug-resistant virus strains. Etravirin and ribavirin belong to the third generation of non-nucleoside reverse transcriptase inhibitors, and currently occupy an important position in clinical treatment. ^[1]

The basic information of the first generation NNRTIS is introduced as follows:

1 Non-nucleoside reverse transcriptase inhibitors Nevirapine

Registered Name:

Viramune

chemical name:

6H-Dipyrido [3,2-b: 2 ", 3'-e] [1,4] diazepin-6-one, 11-cyclopropyl-5, 11-dihydro-4-methyl-3.

Drug effect:

Nevirapine does not need to adjust the dose when combined with ZDV, ddI, ddC and ritonavir, and the combination with indinavir will reduce the effect of indinavir. Nevirapine cannot be combined with ketoconazole. Combination with cimetidine or macrolides (CYP3A family cytochrome P450 isoenzyme inhibitors) will increase the plasma drug concentration of nevirapine. Therefore, nevirapine and CYP3A-dependent When combining drugs, attention should be paid to the monitoring of drug efficacy.

Contraindications:

Patients who are allergic to the drug ingredients are contraindicated. After treatment with this drug, severe skin reactions have occurred, including Stevens-Johnson syndrome. Fever due to rash, blisters, conjunctivitis, and muscle and joint pain should be discontinued.

Dosage and usage:

200 mg orally once daily for 14 days, then 200 mg orally twice daily.

side effect:

Rash, Sjogren's syndrome, fever, nausea, headache, diarrhea, anorexia, lethargy.

2 Non-nucleoside reverse transcriptase inhibitors 2. Delavirdine

Registered Name:

Resciptor

chemical name:

6H-Dipyrido [3,2-b: 2 ', 3'-e [1,4] diazepin-6-one, 11-cyclopropyl-5, 11-dillydro-4-metllyl-1- [3- (Isopropylamino) -2-Pyridyl] -4-[(5-metllane-sulfon-amidoindol-2-y1) carbonyl] piperazine monometh-anesulfonate

Drug dosage form:

Tablets 100mg.

Dosage and usage:

400mg orally three times daily.

3 Non-nucleoside reverse transcriptase inhibitors 3. Efevirenz (Efeveren)

Registered Name:

Stocrin

chemical name:

(S) -6-chloro-4- (cyclopropylethynyl) -1.4-hydro-4- (trifluoromethyl) -2H-3,1-oxazepine-2-one.

Drug dosage form:

Tablets 600mg.

Dosage and usage:

600 mg orally once a night.

4 Non-nucleoside reverse transcriptase inhibitors 4. Etravirine

Registered Name:

Intelence

chemical name:

4-[[6-amino-5-bromo-2-[(4-cyanophenyl) amino] -4-pyrimidinyl] oxy] -3,5dimethylbenzonitrile

Drug dosage form:

Tablets 100mg or 200mg

Dosage and usage:

200mg twice daily.

5 Non-nucleoside reverse transcriptase inhibitors 5. Ripivirine

Registered Name:

Edurant

chemical name:

4-{[4-({4-[( E ) -2-cyanovinyl] -2,6-dimethylphenyl} amino) pyrimidin-2-yl] amino} benzonitrile

Drug dosage form:

Tablets 25mg.

Dosage and usage:

25mg orally once daily.