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Antisialogogue Activity of Some Oral Anticholinergic Formulations

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Antisialogogue Activity of Some Oral Anticholinergic Formulations LETTER TO THE EDITOR ANTISIALOGOGUE ACTIVITY OF SOME ORAL ANTICHOLINERGIC FORMULATIONS Sir, ( Received on March 28, 1985 ) Oral anticholinergic agents are commonly prescribed to decrease gastric secre­ tions and to relieve spasmodic pain. Many of them are quaternary ammonium compounds which do not readily cross blood brain barrier, but dry mouth invariably occurs at the doses that suppress gastric acid secretions (4). In India oral anticholinergic preparations are available which contain either single agent or in combination with tranquill'izers. Com­ parative study of the effects of these oral anticholinergics on salivary flow has not been done so far. Aim of this study was to evaluate the effects of few such preparations on salivary f ow in human volunteers. The study was done on 8 healthy male and 2 healthy female nonsmoking, nonalcoholic medical students (20-24 years, 45-48 kg) who had not taken any drugs at least for 2 weeks. After an overnight fast subjects swallowed capsulles with 90 mt water in the morning at 9 A.M. Saliva was collected 60 min later. Capsules were coded as A,B,C,D' and E that contained crushed tablEits of propantheline bromide 15 mg (Pro Banthine. Searle India Ltd.), oxyphenonium bromide 10 mg (Antrenyl. Ciba-Geigy India Ltd.), isopro~ r-amide 10 mg±trifluoperazir,e 2 mg (Stelabid, Eskay Lab. India Ltd), clidinium bromide b mg+chlordiazepoxide 10 mg (Spasril. Montar,i Lab India Ltd) and placebo respectively. Anticholinergics and placebo were given in a double blind fashion to the subjects in such a way that each subject received each preparations and placebo. The time interval between two medications wa~ 7 days. Saliva was collected by asking the subjects to exercise the muscles of cheek and press the tip of tongue on hard palate continuously for. 10 min and spit out the month contents in a dean graduated glass test tubes (1). Table I summarises the results. Only propantheline and oxyphenonium significantly reduced the salivary secretion under the stated experimental conditions. Antisialogogue activity of propantheline was maximum (59.5%) compared to other preparations. Grossman (2) has reported significant reduction of salivary flow by isopropamide 10 mg(Darbid)but our study did not show significant effect on salivary flow by 10 mg isopropamide (Stelabid). Clidinium 5 mg (present in 2 tablets of Spasril) could not inhibit salivary flow significantly in our subjects which supports the finding of Hurwitz et al. (3) who showed weak 182 Letter to the Editor JUly-september 1985 Ind. J. Physio!. Pharmac. TABLE I: Effect ct $'lme oral anticholine~gic preparations on salivary flow rate (SFR) i'l volunteers. Preparation Contents SFR(ml/min. mean±SEM) (mg) n=10 Placebo Anticholinergic P~o Ba'lthine Propanthslir.e brc mide 15 074±0.11 026±011" An renyl Oxypher,oni,' m bromide 10 0.75±0.07 053±002· Stelabid Isopropamide 10+ 076=0.11 o 68±009 Trif!uoparazine 2 '. Spasril Clidinium bromide 5+ 0.70±0.05 061 ± 0.05 Chlordiazepoxide 10 "Highly significant (P<:OOl). ·Significant (P<O 05) : Paired'!' test. artisialogogue activity of clidinium by the same dose. Whereas. Randall et al. (5) have repor­ ted that clindinium inhibited the salliva even more than atropine, which is quite surprising. Propantheline bromide caused dryness of mouth in many as compared to oxyphe­ nonium and other drugs. Few subjects complained of headache with oxyphenonium and some felt dr.owsy with clidinium (Spasril) which might be due to presence of ch lord iazepoxide with it. R. K. SRIVASTAVA. K. N. GARG. K. K. AGARWAL* Department of Pharmacology, Medica/ Co//ege, Rohtak - 124 001 REFERENCES 1. Blum. A.L. and G.M. Makhlouf. Determination of salivary response to mechanical stimulation. Gut, 1'2 : 650-653. 1971. 2. Grossman. M.I. Inhibition of gastric and saliv~ry secretion by Darbid. Gastroenterologv. 35: 312-315.1958. 3. Hurwitz. A.. R.G. Robinson and H.F. Herrin: Oral anti-cholinergics and gastric emptying. Clin. Fharmac. Ther.. 31 : 1E8-174. 1982. 4. Ivey. K.J. Anticholinergics. Do thev work in peptic ulcer? Gastroenterologv. 68 : E4-1G6. 1975. 5. Randall. L.O .• W.M. Benson and P.L. StefkO: Spasmolytic action of bicyclic basic alcohOl esters. J. Pharmac. Exp. Ther .. 104 : 284-290. 1952. ·Depalment of Pharmacology. Maulana Azad Medical College, New Delhi - 110 002.
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