Drugs that penetrate the brain
Treating HIV in the brain can be a challenge, since many antiretroviral drugs cannot cross the blood-brain barrier. Further, studies seem to suggest that the amount of a specific drug that reaches the brain can vary from person to person.
Among the nucleoside reverse transcriptase inhibitors (NRTIs), AZT (zidovudine, Retrovir), 3TC (lamivudine, Epivir), d4T (stavudine, Zerit) and abacavir (Ziagen) have been shown to penetrate the blood-brain barrier. The nucleotide reverse transcriptase inhibitor tenofovir (Viread) does not enter the central nervous system. The non-nucleoside reverse transcriptase inhibitors (NNRTIs) nevirapine (Viramune) and efavirenz (Sustiva / Stocrin) also reach the central nervous system.
Protease inhibitors penetrate the brain to varying degrees, with amprenavir (Agenerase), fosamprenavir (Telzir), indinavir (Crixivan), atazanavir and lopinavir/ritonavir (Kaletra) reaching the highest levels [1] [2]. T-20 (enfuvirtide, Fuzeon) does not seem to enter the brain. The ability of the newest anti-HIV drugs to penetrate the blood-brain barrier has not yet been extensively studied in humans.
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