bethanechol

Summary

Summary: A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.

Top Publications

  1. Law N, Bharucha A, Undale A, Zinsmeister A. Cholinergic stimulation enhances colonic motor activity, transit, and sensation in humans. Am J Physiol Gastrointest Liver Physiol. 2001;281:G1228-37 pubmed
    ..We investigated the dose-response profile for the colonic sensorimotor effects of neostigmine and bethanechol, a direct muscarinic M(2)/M(3) agonist in humans...
  2. Zagorodnyuk V, Kyloh M, BROOKES S, Nicholas S, Spencer N. Firing patterns and functional roles of different classes of spinal afferents in rectal nerves during colonic migrating motor complexes in mouse colon. Am J Physiol Gastrointest Liver Physiol. 2012;303:G404-11 pubmed publisher
    ..afferents were never activated during spontaneous CMMC contractions or tonic contractions induced by bethanechol (100 ?M)...
  3. Hindley R, Brierly R, Thomas P. Prostaglandin E2 and bethanechol in combination for treating detrusor underactivity. BJU Int. 2004;93:89-92 pubmed
    ..randomized double-blind study, that the combination of intravesical prostaglandin E2 (PGE2) and oral bethanechol chloride (BC) are additive or synergistic in improving bladder emptying, as they have been used alone for ..
  4. Liu L, Rittenhouse A. Pharmacological discrimination between muscarinic receptor signal transduction cascades with bethanechol chloride. Br J Pharmacol. 2003;138:1259-70 pubmed
    ..We have characterized the inhibitory effects of two muscarinic agonists, oxotremorine-M (Oxo-M) and bethanechol chloride (BeCh), on Ca(2+) currents in neonatal rat superior cervical ganglion neurons. 2...
  5. Buranakarl C, Kijtawornrat A, Angkanaporn K, Komolvanich S, Bovee K. Effects of bethanechol on canine urinary bladder smooth muscle function. Res Vet Sci. 2001;71:175-81 pubmed
    We studied whether the effects of bethanechol are mediated via a muscarinic receptor, the role of extracellular calcium on bladder contraction, and down-regulation of bladder contraction by bethanechol after activation with potassium ..
  6. Allen L, Erickson M. Stability of bethanechol chloride, pyrazinamide, quinidine sulfate, rifampin, and tetracycline hydrochloride in extemporaneously compounded oral liquids. Am J Health Syst Pharm. 1998;55:1804-9 pubmed
    ..b>Bethanechol chloride 5 mg/mL, pyrazinamide 10 mg/mL, quinidine sulfate 10 mg/mL, rifampin 25 mg/mL, and tetracycline ..
  7. Prado W, Dias T. Postoperative analgesia induced by intrathecal neostigmine or bethanechol in rats. Clin Exp Pharmacol Physiol. 2009;36:648-54 pubmed publisher
    ..2. In the present study, a model of postoperative pain was used to determine the antinociceptive effects of bethanechol (a muscarinic agonist) and neostigmine administered intrathecally 2, 24 or 48 h after a plantar incision in a ..
  8. Al Izki S, Pryce G, Giovannoni G, Baker D. Evaluating potential therapies for bladder dysfunction in a mouse model of multiple sclerosis with high-resolution ultrasonography. Mult Scler. 2009;15:795-801 pubmed publisher
    ..Such signs can develop in animal models of MS. Current assessments of bladder properties in animal models are generally invasive, electrophysiological techniques...
  9. Holzer Petsche U. Modulation of gastric contractions in response to tachykinins and bethanechol by extrinsic nerves. Br J Pharmacol. 1991;103:1958-62 pubmed
    ..3. The order of potency in inducing gastric contractions was NKA greater than SP greater than bethanechol. SP-methylester was markedly less effective than SP and its effects did not fit sigmoid dose-response curves (..

More Information

Publications62

  1. Manchana T, Prasartsakulchai C. Bethanechol chloride for the prevention of bladder dysfunction after radical hysterectomy in gynecologic cancer patients: a randomized controlled trial study. Int J Gynecol Cancer. 2011;21:730-6 pubmed publisher
    b>Bethanechol chloride is considered as a treatment in patients with high postvoid residual urine (PVR)...
  2. Satoh Y, Ishikawa K, Oomori Y, Takeda S, Ono K. Bethanechol and a G-protein activator, NaF/AlCl3, induce secretory response in Paneth cells of mouse intestine. Cell Tissue Res. 1992;269:213-20 pubmed
    ..intra-arterial perfusion with Hanks' balanced salt solution containing a cholinergic muscarinic secretagogue (bethanechol), a neuroblocking agent (tetrodotoxin), or a G-protein activator (NAF/AlCl3)...
  3. Hasebe K, Horie S, Noji T, Watanabe K, Yano S. Stimulatory effects of endogenous and exogenous nitric oxide on gastric acid secretion in anesthetized rats. Nitric Oxide. 2005;13:264-71 pubmed
    ..The acid secretory response to the muscarinic receptor agonist bethanechol (2 mg/kg, s.c.), the cholecystokinin(2) receptor agonist pentagastrin (20 microg/kg, s.c...
  4. Struhal W, Hödl S, Mazhar S, Ransmayr G. Acute pandysautonomia--restitutio ad integrum by high prednisolone therapy. Wien Klin Wochenschr. 2011;123:508-11 pubmed publisher
    ..Further tests failed to find a cause of acute neuropathy especially where there was no evidence for paraneoplastic or infectious etiology. The patient was treated with high dose intravenous prednisolone and completely recovered...
  5. Kitada S, Wein A, Kato K, Levin R. Effect of acute complete obstruction on the rabbit urinary bladder. J Urol. 1989;141:166-9 pubmed
    ..time course of the effect of complete obstruction of the rabbit urinary bladder on the contractile response to bethanechol and field stimulation and on the muscarinic receptor density...
  6. Mantle M, Thakore E, Mathison R, Davison J. Intestinal mucin secretion in streptozotocin-diabetic rats: lack of response to cholinergic stimulation and cholera toxin. Dig Dis Sci. 1991;36:1574-81 pubmed
    ..The cholinergic agonist bethanechol caused a dose-dependent and atropine-sensitive increase in mucin secretion from the normal intestine but had no ..
  7. Chancellor M, Kaplan S, Blaivas J. The cholinergic and purinergic components of detrusor contractility in a whole rabbit bladder model. J Urol. 1992;148:906-9 pubmed
    Whole rabbit bladders were suspended in a bath chamber and stimulated with ATP, bethanechol, electrical field stimulation, and bethanechol + ATP...
  8. Boyle P, Liggett S, Shah S, Cryer P. Direct muscarinic cholinergic inhibition of hepatic glucose production in humans. J Clin Invest. 1988;82:445-9 pubmed
    ..nervous system in human glucoregulatory physiology, responses to the muscarinic cholinergic agonist bethanechol (5.0 mg s.c.) and antagonist atropine (1.0 mg i.v.) were measured in normal humans...
  9. Pomeranz I, Davison J, Shaffer E. Effect of chlorpromazine (CPZ) on cholecystokinin-induced gallbladder contraction: the role of calcium. Isr J Med Sci. 1988;24:275-81 pubmed
    ..Guinea pig gallbladders were mounted in an organ bath and auxotonic contractions induced by bethanechol, KCl and the octapeptide of cholecystokinin (CCK)...
  10. Garrick T, Mulvihill S, Buack S, Maeda Hagiwara M, Tache Y. Intracerebroventricular pressure inhibits gastric antral and duodenal contractility but not acid secretion in conscious rabbits. Gastroenterology. 1988;95:26-31 pubmed
    ..Intravenous bolus injection of bethanechol reversed the suppression of gastric antral contractility induced by increased intracranial pressure...
  11. Bertiger G, Ouyang A, Reynolds J, Cohen S. Evidence for a direct and indirect action of leucine enkephalin at the feline ileocecal sphincter. Life Sci. 1988;42:1697-703 pubmed
    ..Thus both an indirect and direct opiate action at the ICS was demonstrated...
  12. Knight K, Kawabata H, Coe S, Martin T, Angus J, O Brien B. The salvage of rabbit ischaemic epigastric free flaps using the vasodilator calcitonin gene-related peptide. Br J Plast Surg. 1990;43:447-51 pubmed
    ..vasodilators, calcitonin gene-related peptide (CGRP) and carbamyl beta-methylcholine chloride (MCh, bethanechol chloride, the stable acetylcholine analogue) to improve flap viability...
  13. Flowe K, Lally K, Mulholland M. Galanin inhibits rat pancreatic amylase release via cholinergic suppression. Peptides. 1992;13:487-92 pubmed
    ..3.1 +/- 0.1 times basal) and cholecystokinin octapeptide (21.5 +/- 0.6 vs. 16.8 +/- 0.5), while not inhibiting bethanechol-stimulated secretion...
  14. Zderic S, Duckett J, Wein A, Snyder H, Levin R. Development factors in the contractile response of the rabbit bladder to both autonomic and non-autonomic agents. Pharmacology. 1990;41:119-23 pubmed
    ..However, the response of all age groups to bethanechol was approximately the same, and the response to KCl was only 40% greater in the 1-day-old bladders as compared ..
  15. Katsuragi T, Tokunaga T, Usune S, Furukawa T. A possible coupling of postjunctional ATP release and transmitters' receptor stimulation in smooth muscles. Life Sci. 1990;46:1301-7 pubmed
    ..In ileal longitudinal muscles, amounts of net ATP release by ACh and bethanechol (1-10 microM) were much larger (about 10 fold) than that by other drugs, e.g...
  16. Dolezal V, Tucek S. The effects of brucine and alcuronium on the inhibition of [3H]acetylcholine release from rat striatum by muscarinic receptor agonists. Br J Pharmacol. 1998;124:1213-8 pubmed
    ..2. The evoked release of [3H]ACh was inhibited by all agonists tested (i.e., furmethide, oxotremorine-M, bethanechol and oxotremorine). 3...
  17. Deng X, Wood P, Eagon P, Whitcomb D. Rapid adaptation of pancreatic exocrine function to short-term alcohol feeding in rats. Pancreatology. 2005;5:183-95 pubmed
    ..However, the origin, nature and timing of hyperstimulation/hypersecretion are unknown...
  18. Shibata C, Funayama Y, Fukushima K, Ueno T, Nagao M, Naito H, et al. Effect of ileo-jejunal transposition on ileal longitudinal smooth muscle contractility in vitro in rats. J Gastrointest Surg. 2004;8:1083-9 pubmed
    ..25 +/- 0.02 g/min per mg tissue, p < 0.05). The motor response to cholinergic agonist bethanechol in the IJT group was greater than in the control group above 10(-6) M dosage...
  19. Madeiro A, Rufino A, Sartori M, Baracat E, Lima G, Girao M. The effects of bethanechol and cisapride on urodynamic parameters in patients undergoing radical hysterectomy for cervical cancer. A randomized, double-blind, placebo-controlled study. Int Urogynecol J Pelvic Floor Dysfunct. 2006;17:248-52 pubmed
    To evaluate the effects of bethanechol and cisapride on urodynamic parameters in patients undergoing radical hysterectomy for cervical cancer...
  20. Fong J, Hong S, Wang F. Somatostatin inhibits pepsinogen secretion via a cyclic AMP-independent pathway. Regul Pept. 1991;32:351-60 pubmed
    ..The pepsinogen secretion in response to bethanechol was inhibited by somatostatin in a noncompetitive fashion...
  21. Sevy N, Snape W. Sources of calcium for contraction of distal circular muscle or taenia coli in the rabbit. Am J Physiol. 1988;254:G808-13 pubmed
    ..proximal taenia coli and distal circular muscle from the rabbit to determine if the source of Ca2+ required for bethanechol stimulation of contraction was similar after permeabilizing the tissues with saponin...
  22. Bengtsson M, Mäkelä K, Sjöblom M, Uotila S, Akerman K, Herzig K, et al. Food-induced expression of orexin receptors in rat duodenal mucosa regulates the bicarbonate secretory response to orexin-A. Am J Physiol Gastrointest Liver Physiol. 2007;293:G501-9 pubmed
    ..abolished the orexin-induced secretory response but did not affect secretion induced by the muscarinic agonist bethanechol. Atropine, in contrast, inhibited bethanechol but not orexin-induced secretion...
  23. Harrington K, Bomzon A, Sharkey K, Davison J, Shaffer E. Differential sensitivities of the sphincter of Oddi and gallbladder to cholecystokinin in the guinea pig: their role in transsphincteric bile flow. Can J Physiol Pharmacol. 1992;70:1336-41 pubmed
    ..01). Conversely, the sphincter was more sensitive to bethanechol than was the gallbladder...
  24. Knopman D. The necessity of human trials of putative therapies for Alzheimer's disease. Neurobiol Aging. 1989;10:633-4; discussion 648-50 pubmed
    ..Scientific rationale and likelihood of success should be major considerations. Novel approaches of delivering drugs to the central nervous system should not be discouraged so long as complication rates can be shown to be low...
  25. Herman J, Bass P. Pharmacologic characterization of the changes in cholinergic sensitivity of rat jejunal circular muscle after myenteric plexus ablation. J Pharmacol Exp Ther. 1990;252:135-9 pubmed
    ..The in vitro isometric responses of naive and myenterically denervated (MD) rat jejunal circular muscle to bethanechol and carbachol, alone and in the presence and absence of neuronal antagonists (hexamethonium bromide, ..
  26. Nowak T, Harrington B, Kalbfleisch J. Adaptation of cholinergic enteric neuromuscular transmission in diabetic rat small intestine. Diabetes. 1990;39:891-7 pubmed
    ..studies of intestinal muscle after 3 mo of untreated diabetes showed normal tension development to both bethanechol chloride and physostigmine...
  27. Cook D, Wegman E, Ishikawa T, Poronnik P, Allen D, Young J. Tetraethylammonium blocks muscarinically evoked secretion in the sheep parotid gland by a mechanism additional to its blockade of BK channels. Pflugers Arch. 1992;420:167-71 pubmed
    ..3-10 mmol/l TEA inhibited the increase in intracellular free Ca2+ induced by 5.0 mumol/l bethanechol or by 0.1 mumol/l acetylcholine...
  28. Katsuragi T, Tokunaga T, Ogawa S, Soejima O, Sato C, Furukawa T. Existence of ATP-evoked ATP release system in smooth muscles. J Pharmacol Exp Ther. 1991;259:513-8 pubmed
    ..By contrast, ATP release and contractile response to norepinephrine in the vas deferens and those to bethanechol in the ileum were virtually unaffected by this antagonist...
  29. Shi M, Jones A, Niedringhaus M, Pearson R, Biehl A, Ferreira M, et al. Glucose acts in the CNS to regulate gastric motility during hypoglycemia. Am J Physiol Regul Integr Comp Physiol. 2003;285:R1192-202 pubmed
    ..infusion was tested on gastric contractions that were 1) spontaneously occurring, 2) evoked by iv administered bethanechol in vagotomized animals, and 3) evoked by the TRH analog RX77368, microinjected into the dorsal motor nucleus of ..
  30. Behar J, Biancani P. Pathogenesis of simultaneous esophageal contractions in patients with motility disorders. Gastroenterology. 1993;105:111-8 pubmed
    ..Simultaneous and spontaneous contractions are frequently recorded in patients with esophageal motility disorders. The aim was to investigate the pathogenesis of swallow-induced simultaneous and spontaneous contractions...
  31. Yin J, Chen J. Electroacupuncture improves rectal distension-induced delay in solid gastric emptying in dogs. Am J Physiol Regul Integr Comp Physiol. 2011;301:R465-72 pubmed publisher
    ..b>Bethanechol and atropine were used to qualitatively validate the method...
  32. Parkman H, Reynolds J. Somatostatin selectively inhibits excitatory contractile pathways of the feline lower esophageal sphincter. Regul Pept. 1990;27:325-34 pubmed
    ..0 +/- 0.6 mmHg, P less than 0.001). We have previously shown that bombesin (BN) but not substance P (SP) or bethanechol contracts the LES via tetrodotoxin-sensitive pathways. BN at the D50 (5...
  33. Dieckgraefe B, Seetharam B, Alpers D. Developmental regulation of rat intrinsic factor mRNA. Am J Physiol. 1988;254:G913-9 pubmed
    ..These results show that developmental expression of IF activity in rat is closely related to the expression of its mRNA and that corticosteroids play an important role in such an expression...
  34. Penn R, Martin E, Wilson R, Fox J, Savoy S. Intraventricular bethanechol infusion for Alzheimer's disease: results of double-blind and escalating-dose trials. Neurology. 1988;38:219-22 pubmed
    Ten patients with biopsy-proven Alzheimer's disease (AD) received low-dose (0.35 mg/d) intraventricular bethanechol, a muscarinic agonist, and saline placebo in a 24-week double-blind crossover design...
  35. Keating M, Duckett J, Snyder H, Wein A, Potter L, Levin R. Ontogeny of bladder function in the rabbit. J Urol. 1990;144:766-9 pubmed
    ..weeks of age; 2) the ability to empty is similar for all ages; 3) pressure responsiveness to field stimulation, bethanechol, and ATP is greater at one day? of age, intermediate at one week of age, and similar for the other age groups; ..
  36. Lloyd K, Raybould H, Tache Y, Walsh J. Role of gastrin, histamine, and acetylcholine in the gastric phase of acid secretion in anesthetized rats. Am J Physiol. 1992;262:G747-55 pubmed
    ..Approximately 30% of acid output was due to other unidentified mechanisms, such as chemical secretagogues, a direct effect of amino acids, or novel peptides...
  37. Wong K, Tzeng S. Norepinephrine-induced contractile responses in isolated rat aortae from different duration of diabetes. Artery. 1992;19:1-13 pubmed
    ..Moreover, the bethanechol-induced relaxation of 12-week diabetic aortae preconstricted with norepinephrine was also significantly ..
  38. Mochida S, Kobayashi H. A novel muscarinic receptor antagonist AF-DX 116 differentially blocks slow inhibitory and slow excitatory postsynaptic potentials in the rabbit sympathetic ganglia. Life Sci. 1988;42:2195-201 pubmed
    ..AF-DX 116 was thus shown to be an useful tool for discriminating the M2-type muscarinic responses from those of M1-type in the nervous system...
  39. Kushiku K, Araki Y, Furukawa T, Iwasa T, Inoue N, Miyamoto E. Increment of calmodulin in proportion to enhancement of non-nicotinic responses after preganglionic stimulation of the dog cardiac sympathetic ganglia. J Pharmacol Exp Ther. 1988;245:311-8 pubmed
    ..After the stimulation, positive chronotropic responses to bethanechol (2.5, 5 and 10 micrograms), but not those to dimethylphenylpiperazinium (2...
  40. De Dios I, Arranz A, Lopez M. Exocrine pancreatic response to secretin and bethanechol in rabbits under hypothermia. Rev Esp Fisiol. 1987;43:329-34 pubmed
    The effect of the administration of secretin and bethanechol on exocrine pancreatic secretion was studied in rabbits subjected to temperature changes; these involved a drop from 38 degrees C +/- 1 to 28 degrees C +/- 1 (hypothermia) and ..
  41. Leuchter A, Read S, Shapira J, Walter D, Smith C. Stable bimodal response to cholinomimetic drugs in Alzheimer's disease. Brain mapping correlates. Neuropsychopharmacology. 1991;4:165-73 pubmed
    ..studying the stability of intersubject variability in patients with Alzheimer's disease (AD) who were receiving bethanechol through intracerebroventricular (ICV) shunts...
  42. Blanco Molina A, Lopez Miranda J, Nicolás Puiggarí M, Torre Cisneros J, Lopez Segura F, Perez Jimenez F. Evidence of a direct TRH effect on the rat exocrine pancreas. Rev Esp Fisiol. 1991;47:173-9 pubmed
    ..inhibitory effect when TRH was used alone, although the hormone did blunt the secretion elicited by CCK8 and bethanechol from isolated lobules and dissociated acini...
  43. O Rourke M, Reidelberger R, Solomon T. Effects of atropine on pancreatic response to bethanechol, cholecystokinin, and food intake in rats. Am J Physiol. 1991;261:G735-41 pubmed
    ..The maximal response to bethanechol (4 mg.kg-1.h-1) was similar to cholecystokinin (CCK)-8-induced maximal secretion. Atropine (25-200 micrograms...
  44. Mabe A, Hoover D. Structural and functional cardiac cholinergic deficits in adult neurturin knockout mice. Cardiovasc Res. 2009;82:93-9 pubmed publisher
    ..This study used nrtn knockout (KO) and wild-type (WT) mice to determine the effect of nrtn deletion on cardiac cholinergic innervation and function in the adult heart...
  45. Hyun K, Shin H, Kim D. Malakoplakia in a healthy young female patient. Korean J Intern Med. 2013;28:475-80 pubmed publisher
    ..We treated the patient with ciprofloxacin, the cholinergic agonist bethanechol, and a multivitamin for 6 months...
  46. Varma A, Smigiel J, Eck N, Brooks S. Bethanechol for buprenorphine-related urinary hesitancy: a case series. J Addict Med. 2011;5:227-8 pubmed publisher
    ..Reported are the 2 cases of men older than 50 years who experienced disabling urinary hesitancy with buprenorphine and naloxone combination (suboxone) and were successfully treated with bethanechol, a cholinergic medication.
  47. Tan H, Collewijn H. Muscarinic nature of cholinergic receptors in the cerebellar flocculus involved in the enhancement of the rabbit's optokinetic response. Brain Res. 1992;591:337-40 pubmed
    ..We conclude that muscarinic receptors are involved in the positive modulatory action of the cholinergic system in the cerebellar flocculus...
  48. Silva J, Pinto R, Carvallho T, Coelho A, Avelino A, Dinis P, et al. Mechanisms of prostate atrophy after glandular botulinum neurotoxin type a injection: an experimental study in the rat. Eur Urol. 2009;56:134-40 pubmed publisher
    ..Previous studies in humans, dogs, and rats have shown that intraprostatic injection of botulinum neurotoxin type A (BoNTA) reduces gland size...
  49. Gareau M, Jury J, Perdue M. Neonatal maternal separation of rat pups results in abnormal cholinergic regulation of epithelial permeability. Am J Physiol Gastrointest Liver Physiol. 2007;293:G198-203 pubmed
    ..Our study provides evidence that MS stimulates synthesis of acetylcholine, which, together with released CRF, creates a condition conducive to the development of epithelial barrier defects...
  50. Sidi A, Dykstra D, Peng W. Bethanechol supersensitivity test, rhabdosphincter electromyography and bulbocavernosus reflex latency in the diagnosis of neuropathic detrusor areflexia. J Urol. 1988;140:335-7 pubmed
    A total of 57 patients with neuropathic or nonneuropathic detrusor areflexia was studied with the bethanechol supersensitivity test, electromyography of the urethral rhabdosphincter and bulbocavernosus reflex latency...
  51. Kuvshinoff B, Brodish R, James L, McFadden D, Fink A. Somatostatin inhibits secretin-induced canine pancreatic response via a cholinergic mechanism. Gastroenterology. 1993;105:539-47 pubmed
    ..The present study examined the influence of extrapancreatic nerves and intrapancreatic cholinergic activity on somatostatin-induced inhibition of pancreatic exocrine secretion in conscious dogs...
  52. McCallum R. Pharmacologic modulation of motility. Yale J Biol Med. 1999;72:173-80 pubmed
    ..The multifactorial aspects of GERD are addressed and the potential for tailoring medical therapy also emphasized...
  53. Singh J, Cohen S, Mehendiratta V, Mendoza F, Jimenez S, DiMarino A, et al. Effects of scleroderma antibodies and pooled human immunoglobulin on anal sphincter and colonic smooth muscle function. Gastroenterology. 2012;143:1308-1318 pubmed publisher
    ..We also examined the effects of SScIgGs on M(3)-R activation by bethanechol (BeCh), M(3)-R occupancy, and receptor binding using immunofluorescence, immunoblot, and enzyme-linked ..