Author(s): Kumudini Pawar, Aakanksha Kumbhar, Prerana Gherade, Sandhyarani Sonkamble

Email(s): gheradebp099@gmail.com

DOI: 10.52711/2321-5836.2024.00030   

Address: Kumudini Pawar, Aakanksha Kumbhar, Prerana Gherade*, Sandhyarani Sonkamble
Department of Quality Assurance, Abhinav Education Society’s College of Pharmacy, (B. Pharm) Narhe, Pune 411041, Maharashtra, India.
*Corresponding Author

Published In:   Volume - 16,      Issue - 3,     Year - 2024


ABSTRACT:
Efavirenz is an antiretroviral medicine generally used to treat HIV infection. As a non-nucleoside reverse transcriptase inhibitor (NNRTI), it inhibits the replication of the contagion. Efavirenz is well absorbed when taken orally, reaching peak tube attention within 3-5 hours. Its long elimination half-life of 52-76 hours allows for formerly diurnal dosing and improves patient compliance. Efavirenz is primarily metabolized in the liver by cytochrome P450 enzymes, particularly CYP2B6 and CYP3A4, and undergoes expansive hepatic metabolism to form inactive metabolites. The medicine is substantially excreted in the feces, with a small quantum excreted in the urine. Efavirenz may interact with other medicines and substances due to its influence on the exertion of CYP3A4 and its metabolism through CYP2B6. Medicine-medicine relations should be precisely considered to avoid compromising the efficacity and safety of co-administered medicines. There are certain contraindications to the use of Efavirenz. People with known acuity to the medicine or its factors shouldn’t take Efavirenz. Efavirenz isn’t recommended for pregnant women due to the increased threat of fetal neural tube blights. Effective contraception is essential for women of travail eventually taking Efavirenz. In conclusion, Efavirenz is a precious formerly-diurnal dosing antiretroviral medicine that supports patient compliance.


Cite this article:
Kumudini Pawar, Aakanksha Kumbhar, Prerana Gherade, Sandhyarani Sonkamble. Unlocking The Secrets of Efavirenz: A Comprehensive Drug Information Resource. Research Journal of Pharmacology and Pharmacodynamics.2024;16(3):175-0. doi: 10.52711/2321-5836.2024.00030

Cite(Electronic):
Kumudini Pawar, Aakanksha Kumbhar, Prerana Gherade, Sandhyarani Sonkamble. Unlocking The Secrets of Efavirenz: A Comprehensive Drug Information Resource. Research Journal of Pharmacology and Pharmacodynamics.2024;16(3):175-0. doi: 10.52711/2321-5836.2024.00030   Available on: https://rjppd.org/AbstractView.aspx?PID=2024-16-3-7


REFERENCES:
1.    Vrouenraets, S. M. E., Wit, F. W., van Tongeren, J., and Lange, J. M. A. Efavirenz: a review. Expert Opinion on Pharmacotherapy. 2007; 8(6): 851–871. https://doi.org/10.1517/14656566.8.6.851
2.    Sustiva, C., and Mg, 100. Reverse Transcriptase Inhibitor (NNRTI). Yahoo.com. Retrieved March 28, 2024
3.    Pg, Y., and Sm, H. Treatment for adult HIV infection: 2004 recommendations of the International AIDS Society-USA Panel. JAMA. 2004; 292(2): 251–265.
4.    van Leth, F., Phanuphak, P., Stroes, E., Gazzard, B., Cahn, P., Raffi, F., Wood, R., Bloch, M., Katlama, C., Kastelein, J. J. P., Schechter, M., Murphy, R. L., Horban, A., Hall, D. B., Lange, J. M. A., and Reiss, P. Nevirapine and efavirenz elicit different changes in lipid profiles in antiretroviral-therapy-naive patients infected with HIV-1. PLoS Medicine. 2004; 1(1): e19. https://doi.org/10.1371/journal.pmed.0010019
5.    Young, S. D., Britcher, S. F., Tran, L. O., Payne, L. S., Lumma, W. C., Lyle, T. A., Huff, J. R., Anderson, P. S., Olsen, D. B., and Carroll, S. S. L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrobial Agents and Chemotherapy. 1995; 39(12): 2602–2605. https://doi.org/10.1128/aac.39.12.2602
6.    Pauwels, R. New non-nucleoside reverse transcriptase inhibitors (NNRTIs) in development for the treatment of HIV infections. Current Opinion in Pharmacology. 2004; 4(5): 437–446. https://doi.org/10.1016/j.coph.2004.07.005
7.    Gallant, J. E., DeJesus, E., Arribas, J. R., Pozniak, A. L., Gazzard, B., Campo, R. E., Lu, B., McColl, D., Chuck, S., Enejosa, J., Toole, J. J., and Cheng, A. K. Tenofovir DF, emtricitabine, and efavirenz vs. Zidovudine, lamivudine, and efavirenz for HIV. The New England Journal of Medicine. 2006; 354(3): 251–260. https://doi.org/10.1056/nejmoa051871
8.    HIV/AIDS Treatment Guidelines.  Hiv.gov. Retrieved March 28, 2024, from https://clinicalinfo.hiv.gov/en/guidelines
9.    Mannheimer, S., Friedland, G., Matts, J., Child, C., Chesney, M., and Terry Beirn Community Programs for Clinical Research on AIDS. The consistency of adherence to antiretroviral therapy predicts biologic outcomes for human immunodeficiency virus–infected persons in clinical trials. Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America. 2002; 34(8): 1115–1121. https://doi.org/10.1086/339074
10.    Wu, K., Koethe, J., Hulgan, T., Brown, T., Bares, S. H., Tassiopoulos, K., Lake, J. E., Leonard, M., Samuels, D. C., Erlandson, K., and Haas, D. W. Pharmacogenetics of weight gain following switch from efavirenz- to integrase inhibitor-containing regimens. Pharmacogenetics and Genomics. 2024; 34(2): 25–32. https://doi.org/10.1097/FPC.0000000000000515
11.    Plöger, G. F., Abrahamsson, B., Cristofoletti, R., Groot, D. W., Langguth, P., Mehta, M. U., Parr, A., Polli, J. E., Shah, V. P., Tajiri, T., and Dressman, J. B. Biowaiver monographs for immediate release solid oral dosage forms: Proguanil hydrochloride. Journal of Pharmaceutical Sciences. 2018;107(7): 1761–1772. https://doi.org/10.1016/j.xphs.2018.03.009
12.    Rabel, S. R., Maurin, M. B., Rowe, S. M., and Hussain, M. Determination of the pKaand pH-solubility behavior of an ionizable cyclic carbamate, (S)-6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one (DMP 266). Pharmaceutical Development and Technology. 1996; 1(1): 91–95. https://doi.org/10.3109/10837459609031422
13.    Cristofoletti, R., Nair, A., Abrahamsson, B., Groot, D. W., Kopp, S., Langguth, P., Polli, J. E., Shah, V. P., and Dressman, J. B.  Biowaiver monographs for immediate release solid oral dosage forms: Efavirenz. Journal of Pharmaceutical Sciences. 2013; 102(2): 318–329. https://doi.org/10.1002/jps.23380
14.    Reddy, Y. S., Gotzkowsky, S. K., Eron, J. J., Kim, J. Y., Fiske, W. D., Fiscus, S. A., Petch, L., Cohen, M. S., and Kashuba, A. D. M. Pharmacokinetic and pharmacodynamic investigation of efavirenz in the semen and blood of human immunodeficiency virus type 1–infected men. The Journal of Infectious Diseases. 2002; 186(9): 1339–1343. https://doi.org/10.1086/344311
15.    Ghosn, J., Chaix, M.-L., Peytavin, G., Rey, E., Bresson, J.-L., Goujard, C., Katlama, C., Viard, J.-P., Tréluyer, J.-M., andRouzioux, C. Penetration of enfuvirtide, tenofovir, efavirenz, and protease inhibitors in the genital tract of HIV-1-infected men. AIDS (London, England).  2004; 18(14): 1958–1961. https://doi.org/10.1097/00002030-200409240-00014
16.    Adkins, J. C., and Noble, S. (). Efavirenz. Drugs, 56(6), 1055–1064. https://doi.org/10.2165/00003495-199856060-00014
17.    Dieterich, D. T., Robinson, P. A., Love, J., and Stern, J. O. Drug-induced liver injury associated with the use of nonnucleoside reverse-transcriptase inhibitors. Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America, 2004; 38(Supplement 2): S80–S89. https://doi.org/10.1086/381450
18.    Bautista, E. S. Various synthetic pathways towards Efavirenz and its analogs; The replacement of the side chain. Southeastern University. 2023
19.    Frutos, R. P., Wei, X., Patel, N. D., Tampone, T. G., Mulder, J. A., Busacca, C. A., and Senanayake, C. H. One-pot synthesis of 2,5-disubstituted pyrimidines from nitriles. The Journal of Organic Chemistry. 2013; 78(11): 5800–5803. https://doi.org/10.1021/jo400720p
20.    Schneider, M., Buzdin, A., Weber, A., Clavien, P.-A., and Borger, P. Combination of antiretroviral drugs zidovudine and efavirenz impairs tumor growths in a mouse model of cancer. Viruses.  2021; 13(12): 2396. https://doi.org/10.3390/v13122396
21.    Hecht, M., Erber, S., Harrer, T., Klinker, H., Roth, T., Parsch, H., Fiebig, N., Fietkau, R., and Distel, L. V. Efavirenz has the highest anti-proliferative effect of non-nucleoside reverse transcriptase inhibitors against pancreatic cancer cells. PloS One, 2015; 10(6): e0130277. https://doi.org/10.1371/journal.pone.0130277
22.    Schneider, M., Buzdin, A., Weber, A., Clavien, P.-A., and Borger, P. Combination of antiretroviral drugs zidovudine and efavirenz impairs tumor growths in a mouse model of cancer. Viruses, 2021; 13(12): 2396. https://doi.org/10.3390/v13122396
23.    Hecht, M., Harrer, T., Korber, V., Sarpong, E., Moser, F., Fiebig, N., Schwegler, M., Sturzl, M., Fietkau, R., and Distel, L.Cytotoxic effect of Efavirenz in BxPC 3 pancreatic cancer cells is based on oxidative stress and is synergistic with ionizing radiation. Oncology Letters. 2017. https://doi.org/10.3892/ol.2017.7523
24.    Houede, N., Pulido, M., Mourey, L., Joly, F., Ferrero, J.-M., Bellera, C., Priou, F., Lalet, C., Laroche-Clary, A., Raffin, M. C., Ichas, F., Puech, A., and Piazza, P. V. A phase II trial evaluating the efficacy and safety of efavirenz in metastatic castration-resistant prostate cancer. The Oncologist. 2014; 19(12): 1227–1228. https://doi.org/10.1634/theoncologist.2014-0345
25.    Marima, R., Hull, R., Dlamini, Z., and Penny, C. Efavirenz and lopinavir/ritonavir alter cell cycle regulation in lung cancer. Frontiers in Oncology. 2020; 10. https://doi.org/10.3389/fonc.2020.01693
26.    Han, M., Wang, S., Yang, N., Wang, X., Zhao, W., Saed, H. S., Daubon, T., Huang, B., Chen, A., Li, G., Miletic, H., Thorsen, F., Bjerkvig, R., Li, X., and Wang, J. Therapeutic implications of altered cholesterol homeostasis mediated by loss of CYP46A1 in human glioblastoma. EMBO Molecular Medicine. 2020; 12(1): https://doi.org/10.15252/emmm.201910924
27.    Brüning, A., Jückstock, J., Kost, B., Tsikouras, P., Weissenbacher, T., Mahner, S., and Mylonas, I. Induction of DNA damage and apoptosis in human leukemia cells by efavirenz. Oncology Reports. 2017; 37(1): 617–621. https://doi.org/10.3892/or.2016.5243
28.    Ali, T., Hannaoui, S., Nemani, S., Tahir, W., Zemlyankina, I., Cherry, P., Shim, S. Y., Sim, V., Schaetzl, H. M., andGilch, S. Oral administration of repurposed drug targeting Cyp46A1 increases survival times of prion infected mice. Acta Neuropathologica Communications. 2021; 9(1): https://doi.org/10.1186/s40478-021-01162-1
29.    Pereira, M., and Vale, N. Evolution of antiretroviral drug rilpivirine and approach to oncology. International Journal of Molecular Sciences. 2023; 24(3): 2890. https://doi.org/10.3390/ijms24032890
30.    Sustiva Prescribing Information. Bristol Myers Squibb Company Sustiva Prescribing Information. Bristol Myers Squibb Company
31.    Fda.gov. Retrieved March 28, 2024, from https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/091471Orig1s000lbl.pdf
32.    Pricing for 18 Efavirenz brands. Medindia. Retrieved March 28, 2024, from https://www.medindia.net/drug-price/efavirenz.html
33.    Patents and licences on antiretrovirals - A snapshot. HIV/AIDS Data Hub for the Asia Pacific. Retrieved March 28, 2024, from https://www.aidsdatahub.org/resource/unitaid-patents-licences-antiretrovirals-snapshot
34.    Gosavi, S., Joshi, P., Bhogate, V., Gawade, S., Sangelkar, P., andKanekar, S. Comparative study on treatment of rheumatoid arthritis. Asian Journal of Pharmacy and Technology. 2021; 11(1): 5–12. https://doi.org/10.5958/2231-5713.2021.00002.7
35.    Maurya, A., Verma, S. C., Gupta, V., and Shankar, M. B. Angelica archangelica L.-A Phytochemical and Pharmacological Review. Asian Journal of Research in Chemistry. 2017; 10(6): 852. https://doi.org/10.5958/0974-4150.2017.00142.0
36.    Rajaram, C. U. Review of Captopril Drug Formulation, Mechanism of action, Dosage, Use and Adverse drug reactions. Research Journal of Pharmaceutical Dosage Forms and Technology. 2021; 157–160. https://doi.org/10.52711/0975-4377.2021.00028
37.    Jaitak, D., Nacchammai, K., Pavithra, K., Nair, K. G. S., and Kumar, S. S. Polymeric nanoparticles for Anti-cancer treatment-A review of its mechanisms. Research Journal of Pharmacy and Technology. 2021; 14(3): 1747–1754. https://doi.org/10.5958/0974-360x.2021.00311.5
38.    Kumar, M. P. S., and Nandhini, T. Mechanism of action of Bone Morphogenic Protein 3 in the maintenance of Tissue Homeostasis. Research Journal of Pharmacy and Technology, 2018; 11(3): 1270. https://doi.org/10.5958/0974-360x.2018.00236.6
39.    Kumar, U., Narang, R., Nayak, S. K., Singh, S. K., and Gupta, V. Benzimidazole: Structure activity relationship and mechanism of action as antimicrobial agent. Research Journal of Pharmacy and Technology. 2017; 10(7):  2400. https://doi.org/10.5958/0974-360x.2017.00425.5
40.    Maria, J. D., and Aanandhi, M. V. An Overview on Antibiotic use and resistance. Research Journal of Pharmacy and Technology, 2017; 10(8): 2793. https://doi.org/10.5958/0974-360x.2017.00494.2
41.    Mukhopadhyay, N., Sampath, V., Pai, S., Babu, U. V., and Lobo, R. Antiarthritic medicinal plants: A review. Research Journal of Pharmacy and Technology. 2019; 12(1): 375. https://doi.org/10.5958/0974-360x.2019.00068.4
42.    Nisha, and Rao, P. B. Trigonella foenum-graecum: A Common Indian Spice with Medicinal Properties. Research Journal of Pharmacy and Technology. 2016; 9(2): 173. https://doi.org/10.5958/0974-360x.2016.00031.7
43.    Rathod, C. P., andGhante, M. H. Pharmacological importance of Saracaasoca: A review. Research Journal of Pharmacognosy and Phytochemistry. 2021: 131–135. https://doi.org/10.52711/0975-4385.2021.00022
44.    Vijayalakshmi, S., Raj, D., Bennet, R., Arun, K., and Arun, A. Value added jam from wine sediments and augments income for the fruit processing industry. Research Journal of Pharmacy and Technology. 2017; 10(11): 3753. https://doi.org/10.5958/0974-360x.2017.00681.3
45.    Yadollahpour, A., and Rashidi, S. Electromagnetic fields for the treatment of osteoarthritis: A review of potential clinical applications. Research Journal of Pharmacy and Technology, 2017; 10(2): 641. https://doi.org/10.5958/0974-360x.2017.00122.6


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