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An analysis of the results of the treatment of yaws with a single injection of procaine penicillin with 2% aluminium monostearate.

An extensive yaws eradication campaign has been in operation in Haiti since 1950; this paper deals with material from a special clinic set up at Bainet to evaluate the results of single injections of procaine penicillin with 2% aluminium monostearate (PAM) in various dosages. Treatment results in 862 patients with darkfield-positive secondary yaws and given 600 000 units of PAM are analysed according to age and sex; according to whether the patients lapsed from observation for relatively long periods during the first post-treatment year; and, since an unsatisfactory PAM preparation was used early in the campaign, according to the preparation received. Analyses are also made of results in patients with primary yaws receiving 600 000 units of PAM and in patients with secondary yaws receiving 300 000 units or 150 000 units.It is concluded that a schedule of 600 000 units in a single injection is the treatment method of choice for mass campaigns against yaws, being highly satisfactory in both the primary and secondary stages of disease, provided the PAM preparation conforms to certain minimum standards. The authors also point out that the criteria for the re-treatment of yaws patients after penicillin therapy must be different from those ordinarily adopted with syphilis patients.

Haiti↗

Substance P, bethanechol, 4-aminopyridine, and potassium antagonize the depressing effects of low-frequency stimulation, tetrodotoxin, procaine, and of magnesium on the field-stimulated guinea-pig vas deferens.

The twitch-response enhancing potencies of (the agonists) substance P, bethanechol, 4-aminopyridine and of potassium chloride were compared in the field-stimulated guinea-pig vas deferens. The agonists were tested after the twitching activity of the isolated organ had been reduced to an equal extent by (the antagonists) tetrodotoxin, procaine, magnesium chloride, and by decreased stimulation frequency. Further experiments were performed in the functionally denervated organ. The potencies differed with the type of antagonism of the twitch-response. This pointed at different modes of action and/or sites of mechanism of the response-enhancing compounds. The pharmacological nature of agonists and antagonists as well as the results in the denervated organ indirectly suggested a predominantly neuronal point of mechanism of the agonists. This was most obvious for substance P.

4-Aminopyridine↗

Cholinergic mechanism of sodium nicotinate-induced contractions in rat and guinea-pig descending colon.

In segments of rat descending colon 34.5 microM Na-nicotinate-induced rhythmic contractions that were late in onset, long lasting and reversible. The Na-nicotinate contractile effect was unaffected by 100 microM hexamethonium, whereas it was rapidly blocked by 30 nM scopolamine and inhibited by treating the samples with 20 microM hemicholinium-3, or 40 microM tetrodotoxin or 60 microM procaine, by incubation at 20 degrees C for 60 min or by removing CaCl2 from the incubation medium. In segments of rat descending colon exogenous acetylcholine induced an initial peak in developed tension followed by long lasting rhythmic contractions. Low indomethacin concentrations (from 3 to 60 microM) suppressed both Na-nicotinate and acetylcholine-initiated rhythmic contractile activity while a higher indomethacin concentration (0.6 mM) was required to abolish the acetylcholine-evoked first major contraction. Also in segments of guinea-pig descending colon 34.5 microM Na-nicotinate induced a contractile effect that was abolished by 30 nM scopolamine and almost completely absent in tissue samples treated with 20 microM hemicholinium-3 or exposed to low temperature. The data presented indicate that in segments of rat descending colon Na-nicotinate contractile activity is triggered by acetylcholine release from postganglionic nerve endings and that this cholinergic, calcium-dependent action appears to be modulated by a contemporary release of prostaglandin-like material. In addition, indication is given that this indirect mechanism can be responsible of the Na-nicotinate contractile action at the intestinal level in different animal species.

Acetylcholine↗

The role of Ca2+ in the protoveratrine-induced release of gamma-aminobutyrate from rat brain slices.

1. Protoveratrine A increased the release of gamma-amino[3H]butyrate from small slices of rat cerebral cortex. This effect increased with increasing protoveratrine concentration, reaching a maximum at 100 microM. 2. Removal of Ca2+ from the superfusing medium did not change the increase in release due to 10 microM-protoveratrine; however, the Ca2+ antagonists, compound D-600, La3+, Mn2+, Mg2+ and also high Ca2+ concentration inhibited the effect of the alkaloid, as did procaine. 3. Protoveratrine A increased the uptake of 22Na+ into the slices with a similar dose-response curve to that found for gamma-aminobutyrate release. For the most part, the substances that inhibited protoveratrine-stimulated gamma-aminobutyrate release also inhibited 22Na+ uptake, although the correlation was not perfect. 4. Although extracellular Ca2+ is not required for protoveratrine-induced gamma-aminobutyrate release, an increase in Na+ influx that is susceptible to inhibition by some Ca2+ antagonists does appear to be associated with this phenomenon. However, the possibility remains that changes in the free intracellular Ca2+ concentration may be important for transmitter release induced by depolarizing veratrum alkaloids.

Animals↗

Preiminary investigation of the pharmacology of the human internal anal sphincter.

The smooth muscle from the human internal anal sphincter has been investigated pharmacologically in vitro. The upper and lower parts of the sphincter responded to catecholamines in a similar manner. Noradrenaline caused contraction which could be antagonized by phenoxybenzamine. After phenoxybenzamine, noradrenaline caused relaxation which could be blocked by pronethalol. Isoprenaline caused relaxation which could be specifically prevented by pronethalol. Adrenaline was variable in its effect: low concentrations caused relaxation and high concentrations caused contraction. It is suggested that the anal smooth muscle contains alpha-adrenergic receptors subserving contraction and beta-receptors subserving relaxation. The lower part of the sphincter was generally insensitive to acetylcholine and nicotine whereas the upper part of the sphincter contracted with acetylcholine and regularly relaxed with nicotine. The nicotine response was antagonized by hexamethonium, procaine, and pronethalol. It is suggested that nicotine stimulated some part of the nervous mechanism in the upper part of the sphincter and that a catecholamine was the mediator of the inhibitory response.

Acetylcholine↗

[Qualitative and quantitative determination of procaine-, lidocaine- and tetracaine hydrochloride in drugs by means of capillary isotachophoresis].

The author describes a method for the qualitative and quantitative simultaneous determination of procaine-, lidocaine- and tetracaine hydrochloride in drugs. These active principles are separated by isotachophoresis on the basis of differences in their net mobilities. It took 12 min per sample to perform this analytical technique and the rate of recovery has a mean value of 99.7%. Acids, vitamins and nonionized organic compounds present in the drugs do no interfere with the isotachophoretic separation.

Anesthetics, Local↗