**Acknowledgements**

ANTITUBERCULOUS DRUGS

Rare adverse reactions. To be avoided in pregnancy. Interferes with antiacids

Clarithromycin interfers with PIs and efavirenz; azithromicin does not display these

hepatotoxicity; indicated in patients with acute

Hypersensitivity reactions. Can be used with the

Hepatotoxicity (requires monitoring of hepatic enzymes). Rash. Prolonged QT interval. PIs are not recommended with rifampicin. Adjust the dose of PIs when combined with rifabutin

Hepatotoxicity. Hypersensitivity reactions. Fewer interactions with RIF; nevirapine does not affect the levels of RIF; efavirenz or nevirapine-based regimen are preffered when using associated therapy with RIF; etravirine not recommended with RIF. Adjust the doses in the combination of

Allergic reactions. Digestive reactions. Hepatotoxicity. Neurotoxicity. Teratogenic

Neuropsy-chic reactions. Rash. Not recommended with efavirenz. No

hepatitis in combination with other

Hepatotoxicity. Rash. Caution and dose adjustment is necessary when MVC is used in combination with CYP3A inducers agents (such

Hypersensitivity reactions. Rifampin and rifabutin can significantly reduce the

nonhepatotoxic drugs.

as EFV or rifampin).

concentration of RAL.

EFV and rifabutin /rifampicine

Hepatitis. Neuropathy (only stavudine, didanosine). Optic neuritis (didanosine)

rifamycins

interferences.

effects

Drug Pharmacologic aspects Drug interactions/Adverse reactions

Belongs to fluorochinolones class. Bactericidal. Active on rapidly multiplying bacilli. Acts on nontuberculous mycobacteria. Good CSF penetrations. except for

nontuberculous mycobacteria. High intracellular levels Do not cross the blood brain barrier.

Bacteriostatic/bactericidal (dose depending). Effect on extra/intra cellular bacilli. Good CSF penetration (equal to those in serum).Active on resistant

Bactericidal/bacteriostatic (dose depending). Effect on intra and extracellular bacilli, including resistant

Belongs to the entry inhibitor class (chemokine receptor antagonist); it blocks HIV entry into the host

Belongs to the entry inhibitor class. It is not affected

RAL entry; meningeal inflammation enhances drug

Interfere with the protease enzyme that HIV uses to

NNRTI bind to revers transcriptase, interfering with its ability to convert the HIV RNA into HIV DNA The NNRTIs are also substrates of CYP3A4 and can act

NNRTIs are related with an increased risk of resistance if the therapeutic regimen is not respected.

Interfere with reverse transcription and conversion of HIV RNA to HIV-DNA. Do not use the CYP metabolic pathway. No significant interaction with rifampicin or

\*\*\*very good ability to cross the blood-brain barrier; \*\* moderate ability to cross the blood-brain barrier; \* low

**Table 3.** The most important antituberculous and antiretroviral drugs used in the treatment of CNS tuberculosis

mycobacteria. Good CSF penetration

Substrate of CYP3A enzymes.

produce infectious viral particles. PI are CYP P450 inducer and substrate

as an inducer/inhibitor or mixt

by the CYP enzymes

Integrase inhibitor: RAL\*\* HIV-1 integrase inhibitor. Blood-brain-barrier restrict

ciprofloxacin

316 Tuberculosis - Current Issues in Diagnosis and Management

mycobacteria.

cell.

entry.

rifabutin

Azithromycin Clarithromycin Belongs to macrolides class. Bacteriostatic. Active on

Ofloxacin\*\*

Ciprofloxacin \*

Ethionamide\*\*\* (second-line drug)

Cycloserine\*\*\* (second-line drug)

(MVC) \*\*

(EFV) \*

CCR5 antagonist: maraviroc

Fusion inhibitor: enfuvirtide

Protease inhibitors (PI): SQV\*;ATV\*\*\*;DRV\*;FPV\*\*\*; AMP \*\*\*; IDV\*\*\*; LPV\*\*\*; NFV\*;RTV\*; TPV\*

Non-nucleoside reverse transcriptase inhibitors (NNRTI): EFV\*\*;NVP\*\*\* ETV; DVR\*\*\*

Nucleos(t)ide reverse transcriptase inhibitors (NRTI): ZDV\*\*\*; 3TC\*\* ABC \*\*\*; d4T \*\* ddI\* ; FTC\*\*TDF\*; ZAL\*

[113-118]

ability to cross the blood-brain barrier

Levofloxacin\*\* Moxifloxacin\*\*

The authors wish to express special thanks to professor Ionescu Virgil for the MRI reproduc‐ tions and their interpretation.
