Blood-brain barrier properties of human immunodeficiency virus antiretrovirals

Journal of Pharmaceutical Sciences

Volumn 88, Issue 10, 1999, Pages 950-954

  Yazdanian, Mehran ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ABACAVIR; AMPRENAVIR; ANTIRETROVIRUS AGENT; DELAVIRDINE; DIDANOSINE; EFAVIRENZ; INDINAVIR; LAMIVUDINE; NELFINAVIR; NEVIRAPINE; RITONAVIR; SAQUINAVIR; STAVUDINE; ZALCITABINE; ZIDOVUDINE;

BLOOD BRAIN BARRIER; DRUG BLOOD LEVEL; DRUG CEREBROSPINAL FLUID LEVEL; DRUG PENETRATION; DRUG PROTEIN BINDING; DRUG SOLUBILITY; DRUG TRANSPORT; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LIPOPHILICITY; NONHUMAN; PARTITION COEFFICIENT; SHORT SURVEY;

EID: 0032862119     PISSN: 00223549     EISSN: None     Source Type: Journal    
DOI: 10.1021/js990174i     Document Type: Short Survey

References (58)

1. Davis, L. E.; Hjelle, B. L.; Miller, V. E., Palmer, D. L.; Llewellyn, A. L.; Merlin, T. L.; Young, S. A.; Mills, R. G., Wachsman, W.; Wiley: C. A. Early viral brain invasion in iatrogenic human immunodeficiency virus infection. Neurology 1992, 42, 1736-1739.
2. Pang, S.; Koyangi, Y.; Miles, S.; Wiley, C.; Harry, V.; Chen, I. High levels of unintegrated HIV-1 DNA in brain tissue of AIDS dementia patients. Nature 1990, 34, 85-89.
3. Lipton, S. A.; Gendelman, H. E. Dementia associated with the acquired immunodeficiency syndrome. N. Engl. J. Med. 1995, 332, 934-940.
4. Spencer, D. C.; Price, R. W. Human immunodeficiency virus and the central nervous system. Annu. Rec. Microbiol. 1992, 46, 655-693.
5. Hurwitz, A. A.; Berman, J. W.; Lyman, W. D.. The role of the blood brain barrier in HIV infection of the central nervous system. Adv. Neuroimmuno. 1994, 4, 249-256.
6. Moses, A. V.; Nelson, J. A. HIV infection of human brain capillary endothelial cells - implications for AIDS dementia. Adv. Neuroimmun. 1994, 4, 239-247.
7. Power, C.; Kong, P.-A.; Crawford, T. O.; Wesselingh, S.; Glass, J. D.; McArthur. J. C.; Trapp, B. D. Cerebral white matter changes in acquired immunodeficiency syndrome dementia: alterations of the blood-brain barrier. Ann. Neutrol. 1993, 34, 339-350.
8. Lenhardt, T. M.; Wiley: C. A. Absence of humorally mediated damage within the central nervous system of AIDS patients. Neurology 1989, 39, 278-280.
9. Clifford, D. B.; Simpson, D. Targeting HIV therapy for the brain. HIV: Adv. Res. Ther. 1998, 8, 10-17.
10. Audus, K. L.; Borchardt, R. T. Characterization of an in vitro blood-brain barrier model system for studying drug transport and metabolism. Pharm. Res. 1986, 3, 81-87.
11. Glynn, S. L.; Yazdanian, M. In vitro blood-brain barrier permeability of nevirapine compared to other HIV antiretroviral agents. J. Pharm. Sci. 1998, 87, 306-310.
12. th World AIDS Conference, 1998; pp 303-307.
13. Sidtis, J. J.; Gatsonis, C.; Price, R. W.; Singer, E. J.; Collier, A. C.; Richman, D. D.; Hirsch, M. S.; Schaerf, F. W.; Fischl, M. A.; Kieburtz, K.; Simpson, D.; Koch, M. A.; Feinberg, J.; Dafni, U. Zidovudine treatment of the AIDS dementia complex: results of a placebo controlled trial. Ann. Neurol. 1993, 33, 343-349.
14. th World AIDS Conference, Geneva, Switzerland, June 28-July 3, 1998; Abstract 32207.
15. Rollinski, B.; Bogner, J. P.; Sadri, I.; Wintergerst, U.; Goebel, F. D., Absorption and elimination kinetics of zidovudine in the cerebrospinal fluid in HFV-1 infected patients. J. Acquired Immune Defic. Synd. Hum. Retrovirol. 1997, 15, 192-197.
16. Fenstermacher, J. D., Blasberg, R. G., Patlak, C. S. Methods for quantifying the transport of drugs across brain barrier systems. Pharmacol. Ther. 1981, 14, 217-248.
17. Groothuis, D. R.; Levy R. M. The entry of antiviral and antiretroviral drugs into the central nervous system. J. Neurol. Virol. 1997, 3, 387-400.
18. Gisslen, M.; Norkans, G.; Svennerholm, B.; Hagberg, L. The effect on human immunodeficiency virus type 1 RNA levels in cerebrospinal fluid after initiation of zidovudine or didanosine. J. Infect. Dis. 1997, 175, 434-437.
19. Portegis, P.; Enting, R. H.; De Jong, M. D.; Danner, S. A.; Reiss, P.; Goudamit, J.; Lang, J. M. A. AID dementia complex and didanosine, Lancet 1994, 344, 759.
20. Baldeweg, T.; Catalan, J.; Lovett, E.; Gruzelier, J.; Riccio, M., Hawkins, D. Long-term zidovudine reduces neurocognitive deficits in HIV-1 infection. AIDS 1995, 9, 589-596.
21. Portegis, P.; de Gans, J.; Lange, J.; Derix, M. M. A.; Speelman, H.; Bakker, M.; Danner, S. A.; Goudsmit, J. Declining incidence of AIDS dementia complex after introduction of zidovudine treatment. Br. Med. J. 1989, 299, 819-821.
22. Foudraine, N. A.; Hoetelmans, R. M. W.; Lange, J. M. A., de Wolf, J., van Benthem, H. B., Maas, J. J., Keer, I. P. M., Portegies, P. Cerebrospinal fluid HIV-1 RNA and drug concentrations after treatment with lamivudine plum zidovudine or stavudine. Lancet 1998, 351, 1547-1551.
23. Silverstein, H.; Riska, P.; Johnstone, J. N.; Richter, I.; Norris, S.; Hattox, S.; Grob. P. Nevirapine, a Nonnucleoside Reverse Transcriptase Inhibitor, Freely Enters the Brain and crosses the Placental Barrier. XI International Conference on AIDS, Vancouver British Columbia, Canada, July 9, 1996, Abstract 2325.
24. Physicians' Desk Reference, 52 ed., Medical Economic Company: Montvale, NJ; 1998.
25. Davey, R. T.; Chiatt, D. G.; Reed, G. F.; Freimuth, W. W.; Herpin, B. R.; Metcalf, J. A.; Eastman, P. S.; Fallon, J.; Kovacs, J. A.; Polis, M. A.; Wlaker, R. E.; Masur, H.; Boyle, J. Coleman, S.; Cox, S. R.; Wathen, L.; Daenzer, C. L.; Lane, H. C. Randomized, controlled phase I/II trail of combination therapy with delavirdine (U-910152S) and conventional nucleosides in HIV-1 infected patients. Antimicrob. Agents Chemother. 1996, 40, 1657-1664.
26. th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC), Sept. 28-Oct. 1, 1997; Abstract A-12.
27. Ståhle, L.; Guzenda, E.; Ljungdahle-Ståhle, E. Pharmacokinetics and extracellular distribution to blood, brain, and muscle of alovudine (3′-fluorothymidine) and zidovudine in the rat studied by microdialysis. J. Accquired Immune Deffic. Syndr. 1993, 6, 435-439.
28. Ståhle, L.; Martin, C.; Svensson, J. O.; Sonnerborg, A. Indinavir in cerebrospinal fluid of HIV-1 infected patients. Lancet. 1997, 350, 1823.
29. th Conference on Retroviruses and Opportunistic Infections, Jan 31-Feb 4, 1999; Abstract 407.
30. Swindells, S. Therapy of HIV-1 infection: a practical guide for providers. In The Neurology of AIDS; Gendelman, H. E.; Lipton, S. A.; Epstein, L.; Swindells, S., Eds.; Chapman & Hall, New York, 1998; pp 364-376.
31. Invirase, Saquinavir mesylate, Roche Laboratories Inc.; Package Insert.
32. Aweeka, F.; Jayewardene, A.; Staprans, S.; Beltibas, E.; Kearney, B.; Lizak, P.; Novakovic-Agopian, Price, R. W. Failure to detect nelfinavir in the cerebrospinal fluid of HIV-1 infected patients with and without AIDS dementia. J. Accquired Immune Deffic. Syndr. 1999, 20, 39-43.
33. Lin, J. H.; Chiba., M.; Balani, S. K.; Chen, I.; Kwei, G. Y. S.; Vastag, K. J.; Nishime, J. A. Species differences in the pharmacokmetics and metabolism of indinavir, a potent human immunodeficiency virus inhibitor. Drug. Metab. Dispos. 1996, 24, 1111-1120.
34. Scolnick, A. A. Protease inhibitors may reverse AIDS dementia. JAMA 1998, 279, 419.
35. th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC), Sept. 28-Oct. 1, 1997; Abstract LB3.
36. th World AIDS Conference, June 28-July 3, Geneva, Switzerland; Abstract 32197.
37. Shah, M. V.; Audus, K. A.; Borchardt, R. T. The application of bovine brain microvessel endothelial cell monolayers grown onto polycarbonate membranes in vitro to estimate the potential permeability of solutes through the blood-brain barrier. Pharm. Res. 1989, 6, 624-627.
38. Barrand, M. A.; Robertson, K. J.; von Wiekersthal, S. F. Comparisons of P-glycoprotein in isolated rat brain microvessels and in primary cultures of endothelial cells derived from microvasculature of rat brain, epididymal fat pad and from aorta. FEBS Lett. 1995, 374, 179-183.
39. Alsenz, J.; Steffen, H.; Alex, R. Active apical secretory efflux of the HIV protease inhibitors Saquinavir and Ritonavir in Caco-2 cell monolayers. Pharm Res. 1998, 15, 423-428.
40. Kim, R. B.; Fromm, M. F.; Wandel, C.; Leake, B.; Wood, A. J. J.; Roden, D. M.; Wilkinson, G. R. The drug transporter P-glycoprotein limits oral absorption and brain entry pf HIV-1 protease inhibitors. J. Clin. Inves. 1998, 101, 289-294.
41. Anderson, B. D.; Hoesterey, B. L.; Baker, D. C.; Galinsky, R. E. Uptake kinetics of 2′, 3′-dideoxyinosine into brain and cerebrospinal fluid of rats: intravenous infusion studies. J. Pharmacol. Exp. Ther. 1990, 253, 113-118.
42. Galinsky, R. E.; Flaharty, K. K.; Hoesterey, B. L.; Anderson, B. D. Probenicid enhances central nervous system uptake of 2′,3′-dideoxyinosine by inhibiting cerebrospinal fluid efflux. J. Pharmacol. Exp. Ther. 1991, 257, 972-978.
43. Masereeuw, R.; Jaehde, U.; Langemeijer, M. W. E.; de Boer, A. G.; Breimer,. D. D. In vitro and in vivo transport of zidovudine (AZT) across the blood-brain barrier and the effect of transport inhibitors. Pharm. Res. 1994, 11, 324-330.
44. Wang, Y.; Sawchuck, R. J. Zidovudine transport in the rabbit brain during intravenous and intracerebroventricular infusion. J. Pharm. Sci. 1995, 84, 871-876.
45. Wong, S. L.; VanBelle, K.; Sawchuck, R. J. Distributional transport kinetics of zidovudine between plasma and brain extracellular fluid and cerebrospinal fluid in rabbit: investigation of the inhibitory effect of probenicid utilizing micordialysis. J. Pharmacol. Exp. Ther. 1993, 264, 899-909.
46. Takasawa, K.; Terasaki, T.; Suzuki, H.; Sugiyama, Y. In vivo evidence for carrier-mediated efflux transport of 3′-azido-3′-deoxythymidine and 2′,3′-dideoxyinosine across the blood-brain barrier via a probenicid-sensitive transport system. J. Pharmacol. Exp. Ther. 1997, 281, 369-375.
47. Ziagen, abacavir, GlaxoWellcome, Package Insert.
48. a and pH-solubility behavior of an ionizable cyclic carbamate, (S)-6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluromethyl)-2H-3,1- benzoxazin-2-one (DMP266). Pharm. Dev. Technol. 1996, 1, 91-95.
49. Agenerase, Amprenavir, Vertex, Package Insert.
50. Longer, M.; Shetty, B.; Zamansky, I.; Tyle, P. Preformulation studies of a novel HIV protease inhibitor, AG1343. J. Pharm. Sci. 1984, 84, 1090-1093.
51. Dennisen, J. F.; Grabowski, B. A.; Johnson, M. K.; Buko, A. M.; Kempp, D. J., Thomas, S. B., Surber, B. W. Metabolism and disposition of the HIV-1 protease inhibitor ritonavir (ABT-538) in rats, dogs, and humans. Drug Metab. Dispos. 1997, 25, 489-501.
52. Shelton, M, J.; O'Donnell, A. M.; Morse, G. D. Didanosine. Ann. Pharmacother. 1992, 26, 660-670.
53. Ballis, F. M.; Pizzo, P. A.; Butler, K. M.; Hawkins, M. E.; Brouwers, Pim, Husson, R. N.; Jacobson, F.; Blaney, S. M.; Gress, J.; Jarosinski, P.; Polack, D. G. Clinical pharmacology of 2′-3′-didoexyinsoine in human immunodeficiency virus infected children. J. Infect. Dis. 1992, 324, 137-144.
54. Zerit, Stavudine, Bristol Meyers Squibb. Package Insert.
55. Yang, A.; Brundage, R. C.; Barbhaiya, R. H.; Sawchuck, R. J. Microdialysis studies of the distribution of stavudine into the central nervous system in the freely moving rat. Pharm. Res. 1997, 14, 865-872.
56. Terasaki, T.; Pardridge, W. M. Restricted transport of 3′-azido-3′-deoxythymidine and dideoxynucleosides through the blood-brain barrier. J. Infect. Dis. 1988, 158, 630-632.
57. Klecker, R. W.; Collins, J. M.; Yarchoan, R.; Thomas, R.; Jenkins, J. F.; Border, S.; Myers, C. E. Plasma and cerebrospinal fluid pharmacokinetics of 3′-azido-3′-deoxythymidine: A novel pyrimidine analogue with potential applications for the treatment of patients with AIDS and related diseases. Clin. Pharmacol. Ther. 1987, 41, 407-412.
58. Galinsky, R. E.; Hoesterey, B. L.; Anderson, B. D. Brain and cerebrospinal fluid uptake of zidovudine (AZT) in rats after intravenous injection. Life Sci. 1990, 47, 781-788.