Interventions for Tuberculosis Control and Elimination 2002

Rifapentine
Rifapentine (cyclopentyl rifamycin SV) is a semisynthetic derivative of
rifampicin, synthesized at the Lepetit laboratories in Italy. Its properties
were first described in a publication in 1981. 1097
Rifapentine is comparable in its spectrum of activity to that of
rifampicin. 1098,1099 It is active in the experimental mouse model both against
latent infection with M. tuberculosis 1100 and clinical active disease. 1101
Rifapentine is an RNA synthesis inhibitor like rifampicin. 1099
The most conspicuous property of rifapentine is shown in a comparison
of its pharmacokinetics with rifampicin. The serum elimination halflife
is much longer in rifapentine 176 than rifampicin (figure 91). 181 The
serum elimination half-life tβ 1/2 is 14 to 18 hours, 1102,1103 and is similar in
adults and adolescents. 1104 Intrapulmonary concentrations of rifapentine are
below those in serum. 1105 In contrast to rifampicin, higher peak levels are
achieved following food intake than after fasting. 1102 Pharmacokinetics are
not influenced by HIV status. 1102 A key issue that needs to be addressed
is its high degree of plasma binding, which might require higher dosages
than used so far.
The usual dosage is currently 600 mg twice-weekly. 1099 However,
higher doses are now being studied.
����� ������������� ������
��
��
��
�
�
�
�
�
� � � � � �� �� �� �� �� �� ��
160
����������
���� ����
�����������
Figure 91. Comparative pharmacokinetics of rifampicin and rifapentine.
Reproduced from 181,1102 by the permission of the publisher ASM Press.