Treatment of gonorrhoea by one oral dose of ampicillin and probenecid combined.

Abstract

It has been shown by sensitivity testing in vitro that the effect of ampicillin on most gonococcal strains is somewhat weaker than that of penicillin G, but the effect on strains less sensitive is better with ampicillin than with penicillin G. Reyn and Bentzon (1968), in support of this, found that the 50 per cent. inhibitory concentrations for the naturally-occurring more sensitive strains were about twice as high with ampicillin as with sodium penicillin G, whereas an opposite tendency was observed in the less sensitive strains.As the great majority of relapses after treatment with penicillin occur in patients infected with gonococci with reduced sensitivity to penicillin, it is therefore possible that ampicillin could be an effective remedy in the treatment of gonorrhoea. This has proved to be the case. Willcox (1963) found a failure rate of 11 9 per cent. in male patients with uncomplicated gonorrhoea treated with a single oral dose of 0 5 g. ampicillin, which proved comparable to the results achieved with single injections of aqueous procaine penicillin. Willcox (1964) ampicillin combined with one simultaneous injection of 600,000 units procaine penicillin the relapse frequency was 3 per cent., whereas 500 patients *Received for publication February 18, 1969. treated with procaine penicillin only showed a relapse rate 11-6 per cent.Probenecid, which impedes the excretion of penicillin from the body and thus causes a higher serum concentration and a longer duration of penicillinaemia, was given, together with an intramuscular injection of sodium penicillin G, to gonorrhoea patients by Jensen, Kvorning, and Norredam (1963) Roholt (1965), can give an initial penicillinaemia of up to 200 units/ml., and after 8 hours, an average concentration of 5 units/ml. Of the 832 patients treated, there were only eight who relapsed; all had had sexual intercourse after the first treatment and all were cured after a repetition of the treatment. It is therefore highly probable that these cases were not relapses but re-infections and that the cure rate was 100 per cent.We have not been able to find any publication describing the use of an oral dose of ampicillin and probenecid combined in the treatment of gonorrhoea. The object of this paper is to show the results of such treatment. Material and Methods

Sensitivity to ampicillin, penicillin, and tetracyline of gonococci in Rotterdam.

“…The percentage of strains relatively resistant to penicillin has not changed appreciably in recent years among the civilian population. In general, the percentages among seafaring personnel are more difficult to interpret as these patients form a less Our percentages of relatively resistant MC and FC strains are very similar to those found by Lynn, Nicol, Ridley, Rimmer, Symonds, and Warren, (1970) and Leigh, Le Franc, and Turnbull (1969) in London, and by Gundersen, 0degaard, and Gjessing (1969) in Norway, viz. 35, 39, and 34-5 per cent.…”

Comparative Therapeutic and Pharmacological Evaluation of Amoxicillin and Ampicillin Plus Probenecid for the Treatment of Gonorrhea

“…Ampicillin and amoxicillin had comparable activity in vitro. The most sensitive strains of N. gonorrheae were often inhibited by slightly lower concentrations of penicillin G than of ampicillin (or amoxicillin), whereas relatively resistant strains were slightly more sensitive to ampicillin or amoxicillin than to penicillin G. The relatively greater activity of ampicillin against penicillin-resistant strains has been noted previously by others (8), and amoxicillin appears to be similar in this respect. Carbenicillin was the least effective drug in vitro, with 21% of the N. gonorrhoeae strains not inhibited by 0.5 ,ug of antibiotic per ml.…”

“…However, 29% of men with gonorrhea acquired in the Philippines were not cured with 3.5 g of ampicillin (10), and approximately 20% of Swedish men and women infected with strains of N. gonorrhoeae resistant to 0.1 ,ug of ampicillin per ml were not cured with a single 2.0-g oral dose of ampicillin (5). The use of 1.0 g of probenecid with 2.0 to 3.5 g of ampicillin has consistently resulted in cure rates greater than 95% (5,(8)(9)(10)14) in both men and women. The U.S. Public Health Service currently recommends 1.0 g of probenecid plus 3.5 g of ampicillin orally for the treatment of uncomplicated gonorrhea, although the efficacy of lower doses of ampicillin given with probenecid has not been studied in this country.…”

Antibiotic Disk Susceptibility Tests with Neisseria gonorrhoeae

“…As discussed in a review by Sparling (24), many studies have shown that high doses of penicillin or ampicillin, combined with probenecid, will produce high cure rates despite the frequent appearance of gonococcal isolates resistant to 0.5 ,ug of penicillin (8,9,11,12,15) (19,24). It is not known whether gonococcal isolates resistant to 2.7 ,ug of ampicillin per ml would yield a significant number of failures after treatment by the USPHS-recommended 3.5 g of ampicillin plus probenecid.…”