A Review on Antiretroviral Tablets
DOI:
https://doi.org/10.32628/IJSRST52411252Keywords:
Lamivudine, Dolutegravir, Tenofovir Disoproxil Fumarate, Nucleoside Reverse Transcriptase InhibitorAbstract
The usage of fixed dose combination (FDC) tablets of Lamivudine, Dolutegravir and Tenofovir Disoproxil Fumarate (TDF) is increasing due to increased incidences of HIV/Hepatitis B and HIV/TB co-infections. This is likely to increase the financial crisis due to limited resources for funding procurement of ready-made products from the pharmaceuticals manufacturing leading countries. Therefore, production of local oral tablets containing Lamivudine and TDF FDC is inevitable. Lamivudine 300 mg/TDF 300 mg tablets were developed and optimized by D-optimal mixture design and produced by direct compression technique. The first-ever 2-drug regimen approved for the treatment of HIV-1 infection for treatment-naive people living with HIV (PLWH), consisting of the integrase inhibitor dolutegravir (DTG) and the nucleoside reverse transcriptase inhibitor (NRTI) lamivudine (3TC), is reviewed in this paper. The chemical composition and properties, pharmacokinetic and pharmacodynamics profile, and clinical trial data on efficacy and safety of DTG/3TC are presented. An expert opinion aims to highlight important considerations for the use of DTG/3TC in the context of existing and emerging ARV options.
Downloads
References
Corbett E.L., Watt C.J., Walker N., Maher D., Williams B.G., Raviglione M.C. The growing burden of tuberculosis: global trends and interactions with the HIV epidemic. Arch. Intern. Med. 2003;163(9):1009–1021. [PubMed] [Google Scholar]
Trinh Q.M., Nguyen H.L., Nguyen V.N., Nguyen T.V.A., Sintchenko V., Marais B.J. Tuberculosis and HIV co-infection-focus on the Asia-Pacific region. Int. J. Infect. Dis. 2015:170–178. [PubMed] [Google Scholar]
Klopper M., Warren R.M., Hayes C., van Pittius N.C.G., Streicher E.M., Miller B. Emergence and spread of extensively and totally drug-resistant tuberculosis, South Africa. Emerg. Infect. Dis.2013;19(3):449–455. [PMC free article] [PubMed] [Google Scholar]
Mungrue K., Beharry A., Kalloo J., Mahabir S., Maraj T., Ramoutar R. Trends in HIV/TB coinfection in Trinidad and Tobago for the period 1998-2007. J. Int. Assoc. Physicians AIDS Care (Chic)2009;8(3):170–175. [PubMed] [Google Scholar]
Sharma S.K., Mohan A., Kadhiravan T. HIV-TB co-infection: Epidemiology, diagnosis & management. Indian J. Med. Res. 2005:550–567. [PubMed] [Google Scholar]
Alexander P.E., De P. The emergence of extensively drug-resistant tuberculosis (TB): TB/HIV coinfection, multidrug-resistant TB and the resulting public health threat from extensively drug-resistant TB, globally and in Canada. Can. J. Infect. Dis. Med. Microbiol.2007:289–291. [PMC free article] [PubMed] [Google Scholar]
Chintu C. Tuberculosis and human immunodeficiency virus co-infection in children: management challenges. Paediatr. Respir. Rev.2007:142–147. [PubMed] [Google Scholar]
Shipton L.K., Wester C.W., Stock S., Ndwapi N., Gaolathe T., Thior I. Safety and efficacy of nevirapine- and efavirenz-based antiretroviral treatment in adults treated for TB-HIV co-infection in Botswana. Int. J. Tuberc. Lung Dis. 2009;13(3):360–366. [PMC free article] [PubMed] [Google Scholar]
Manosuthi W., Tantanathip P., Chimsuntorn S., Eampokarap B., Thongyen S., Nilkamhang S. Treatment outcomes of patients co-infected with HIV and tuberculosis who received a nevirapine-based antiretroviral regimen: A four-year prospective study. Int. J. Infect. Dis. 2010;14(11) [PubMed] [Google Scholar]
Cohen K., Meintjes G. Management of individuals requiring antiretroviral therapy and TB treatment. Curr. Opin. HIV AIDS. 2010;5(1):61–69. [PMC free article][PubMed] [Google Scholar]
Uttayamakul S., Likanonsakul S., Manosuthi W., Wichukchinda N., Kalambaheti T., Nakayama E.E. Effects of CYP2B6 G516T polymorphisms on plasma efavirenz and nevirapine levels when co-administered with rifampicin in HIV/TB co-infected Thai adults. AIDS Res. Ther. 2010;7:8. [PMC free article][PubMed] [Google Scholar]
Lehmann C., Wyen C., Fätkenheuer G. Rapid improvement of liver function in a patient with HIV and hepatitis B coinfection treated with lamivudine and tenofovir. Infection. 2006;34(4):234–235. [PubMed] [Google Scholar]
Kumar V.R., Rupa Y., Chaitanya M. Estimation of lamivudine in bulk and formulation by titrimetric and uv-visible spectrophotometry. 2014;4(1):75–79.[Google Scholar]
Grim S.A., Romanelli F. Tenofovir disoproxil fumarate. Ann. Pharmacother. 2003;37(6):849–859.[PubMed] [Google Scholar]
Nyamweru B., Kaale E., Mugoyela V., Chambuso M. Development and validation of an HPTLC-densitometric method for simultaneous analysis of lamivudine, tenofovir disoproxil fumarate, and efavirenz (LTE) in tablets. J. Planar Chromatogr. - Mod. TLC. 2013;26(3):226–231. [Google Scholar]
“Lamivudine” National Center for Biotechnology Information. PubChem Compound Database, U.S. National Library of Medicine. Available from: https://pubchem.ncbi.nlm.nih.gov/compound/Lamivudine Accessed August1, 2019.
PubChem. Lamivudine. [online]. 2019. Available from: https://pubchem.ncbi.nlm.nih.gov/compound/60825#section=Structures Accessed August1, 2019.
Eron JJ, Benoit SL, Jemsek J, et al. Treatment with lamivudine, zidovudine, or both in HIV-positive patients with 200 to 500 CD4+ cells per cubic millimeter. North American HIV working party. N Engl J Med. 1995;333:1662–1669. doi: 10.1056/NEJM199512213332502 [PubMed] [CrossRef] [Google Scholar]
Moore KHP Pharmacokinetics (PK) of lamivudine (3TC) phosphorylation on peripheral blood mammalian cells (PBMC) from HIV-infected patients [abstract]. 12th International Conference on AIDS; June 28–July 3; 1998; Geneva, CH. [Google Scholar]
Perry CM, Faulds D. Lamivudine: a review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy in the management of HIV infection. Drugs. 1997;53(4):657–680. doi: 10.2165/00003495-199753040-00008 [PubMed] [CrossRef] [Google Scholar]
Katlama C, Ingrand D, Loveday C, et al. Safety and efficacy of lamivudine-zidovudine combination therapy in antiretroviral-naive patients: a randomized controlled comparison with zidovudine monotherapy. JAMA. 1996;276(2):118–125.
Wainberg MA. The impact of the M184V substitution on drug resistance and viral fitness. Expert Rev Anti Infect Ther. 2004;2:147–151. [PubMed]
Paredes R, Sagar M, Marconi VC, Hoh R, Martin JN, Parkin NT. In vivo fitness cost of the M184V mutation in multidrug-resistant human immunodeficiency virus type 1 in the absence of lamivudine. J Virol. 2009;83:2038–2043. doi: 10.1128/JVI.02154-08 [PMC free article] [PubMed] [CrossRef].
Anon. Tenofovir Disoproxil Fumarate. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/02/2021.
Buckingham R (ed). Tenofovir Disoproxil Fumarate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/02/2021.
Tenofovir Disoproxil Accordpharma 245 mg Film-coated Tablets (Accord Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 05/02/2021.
Viread Tablet, Coated, Powder (Gilead Sciences, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/02/2021.
“Dolutegravir.” National center for biotechnology information. PubChem Compound Database, U.S. National Library of Medicine. Available from: pubchem.ncbi.nlm.nih.gov/compound/Dolutegravir Accessed August1st, 2019.
PubChem. Dolutegravir. [online]. 2019. Available from: https://pubchem.ncbi.nlm.nih.gov/compound/Dolutegravir-sodium Accessed August1, 2019.
Podany AT, Scarsi KK, Fletcher CV, et al. Comparative clinical pharmaco-kinetics and pharmacodynamics of HIV-1 integrase strand transfer inhibitors. Clin Pharmacokin. 2017;56(1):25–40. doi: 10.1007/s40262-016-0424-1 [PMC free article] [PubMed] [CrossRef] [Google Scholar]
Kandel C, Walmsley S. DTG – a review of the pharmacology, efficacy, and safety in the treatment of HIV. Drug Des Devel Ther. 2015;9:3547–3555. doi: 10.2147/DDDT.S84850 [PMC free article] [PubMed] [CrossRef] [Google Scholar]
Cottrell ML, Hadzic T, Kashuba AD, et al. Clinical pharmacokinetic, pharmacodynamic and drug-interaction profile of the integrase inhibitor dolutegravir. Clin Pharmacokin. 2013;52(11):981–994. doi: 10.1007/s40262-013-0093-2 [PMC free article] [PubMed] [CrossRef] [Google Scholar]
Shah SU, Shah KU, Jan SU, Ahmad K, Rehman A, Hussain A, Khan GM. Formulation and in vitro evaluation of ofloxacin-ethocel controlled release matrix tablets prepared by wet granulation method: Influence of co-excipients on drug release rates. Pak. J. Pharm. Sci. 2011 Jul 1;24(3):255-61.
Gohel MC, Panchal MK. Formulation optimization of diltiazem HCl matrix tablets containing modified guar gum using a central composite design. Pharmacy and pharmacology communications. 1999 May;5(5):331-8.
Downloads
Published
Issue
Section
License
Copyright (c) 2024 International Journal of Scientific Research in Science and Technology
This work is licensed under a Creative Commons Attribution 4.0 International License.