Treatment of acute gonorrhoea with a single oral dose of rifampicin.

Rifampicin (Rimactane(& (CIBA)) is a semi-synthetic antibiotic (3-(4-methyl-l-piperazinyl-iminomethyl)rifamycin SV), derived from the rifamycins, which are produced by Streptomyces mediterranei. Rifampicin differs from other rifamycins in that it is active when taken by mouth, has a wider spectrum of action, and is eliminated more slowly. It is active against Gram-positive bacteria, particularly streptococci, against Gram-negative bacteria, including gonococci, and against Mycobacterium tuberculosis. Its activity is presumably mediated by the fact that rifampicin, in vitro as well as in vivo, prevents the formation of messenger-RNA, since it inhibits RNA-polymerase by forming a stable complex with it. DNA-polymerase is not affected (Hartmann, Honikel, Knusel, and Nuesch, 1967). Rifampicin does not appear to be toxic to human enzymes (Wehrli, Nuesch, Knusel, and Staehelin, 1968). The most recent experimental studies have shown that rifampicin inhibits the growth of certain poxand adeno-viruses (Heller, Argaman, Levy, and Goldblum, 1969; Subak-Sharpe, Timbury, and Williams, 1969). Furthermore, rifampicin is said to inhibit TRIc-agents (Becker and Zakay-Rones, 1969); but this finding is not of clinical significance as the therapeutic concentrations which are necessary would have a toxic effect on human cells during growth. After administration the maximum serum concentration of rifampicin is reached at 2 hours. With a single oral dose of 900 mg. a concentration of 27-2 jig./ml. is reached after 2 hours, and then falls to 15-44 jig./ml. after 8 hours, 8-33 ,Lg./ml. after 12 hours, and 1-64 jig./ml. after 24 hours. For purposes of comparison it should be mentioned that the minimum inhibitory concentration for gonococci is of the order of 0-02 jig./ml. (Lepetit Pharmaceuticals, 1968). The serum concentration is said to increase more rapidly and to reach a higher level if the preparation is taken on an empty stomach. The