Drugs that cross the blood-brain barrier


A friend has just been diagnosed with PML. He is starting HIV meds today or tomorrow, and I want to be sure he takes meds that cross the blood-brain barrier. Is this list I found on the web complete?

AZT, d4T, 3TC, abacavir, nevirapine, efavirenz, amprenavir

Should I add fosamprenavir? Any others? I called Gilead to ask about tenofovir and FTC, and they said they didn't know!

Thanks for any help.



Dear Mark-

AZT and d4T do seem to get into the spinal fluid better than other HIV drugs. Nevirapine does fairly well and interestingly, efavirenz has poor penetration into the central nervous system. Protease inhibitors also don't get in well although indinavir better than the others. Tenofovir concentrations in the spinal fluid are low compared to blood plasma.

That said, there are conflicting data regarding the benefit of using HIV drugs that do or don't get into the central nervious system and the course of HIV dementia. I am unaware of studies of spinal fluid concentration of HIV meds and response of PML.

I think a combo of Combivir+Nevirapine+Kaletra would be an aggressive choice that could be started with and possibly reduced to Combivir+Kaletra if toxicity to nevirapine develops or after he improves and has undetectable blood viral load. It may be that any combo that can get the blood viral load down quickly will have the best chance to work.