Summary: Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS.

Top Publications

  1. Khan A, Khan M, Subhan F, Gilani A. Antispasmodic, bronchodilator and blood pressure lowering properties of Hypericum oblongifolium--possible mechanism of action. Phytother Res. 2010;24:1027-32 pubmed publisher
    ..These results indicate that Ho.Cr possesses gastrointestinal, respiratory and cardiovascular inhibitory effects, mediated via a Ca(++) antagonist mechanism...
  2. Budriesi R, Ioan P, Micucci M, Micucci E, Limongelli V, Chiarini A. Stop Fitan: antispasmodic effect of natural extract of chestnut wood in guinea pig ileum and proximal colon smooth muscle. J Med Food. 2010;13:1104-10 pubmed publisher
    ..These findings, taken together with the antibacterial, antiviral, and antispasmodic properties of tannins, suggest that the combination of tannins and S. boulardii may be relevant to treat diarrhea by Stop Fitan...
  3. Jabeen Q, Bashir S, Lyoussi B, Gilani A. Coriander fruit exhibits gut modulatory, blood pressure lowering and diuretic activities. J Ethnopharmacol. 2009;122:123-30 pubmed publisher
    ..Diuretic activity adds value to its use in hypertension. ..
  4. Najeeb Ur Rehman -, Mehmood M, Al Rehaily A, Mothana R, Gilani A. Species and tissue-specificity of prokinetic, laxative and spasmodic effects of Fumaria parviflora. BMC Complement Altern Med. 2012;12:16 pubmed publisher
    ..This study was designed to provide pharmacological basis for the medicinal use of Fumaria parviflora in gut motility disorders...
  5. Gilani A, Mandukhail S, Iqbal J, Yasinzai M, Aziz N, Khan A, et al. Antispasmodic and vasodilator activities of Morinda citrifolia root extract are mediated through blockade of voltage dependent calcium channels. BMC Complement Altern Med. 2010;10:2 pubmed publisher
    ..The objective of this study was to explore the possible mode(s) of action for its antispasmodic, vasodilator and cardio-suppressant effects to rationalize its medicinal use in gut and cardiovascular disorders...
  6. Gilani S, Khan A, Gilani A. Pharmacological basis for the medicinal use of Zanthoxylum armatum in gut, airways and cardiovascular disorders. Phytother Res. 2010;24:553-8 pubmed publisher
  7. Ali N, Ali Shah S. Antispasmodic activity of Teucrium stocksianum Boiss. Pak J Pharm Sci. 2011;24:171-4 pubmed
    ..The results confirm the folkloric use of Teucrium stocksianum as antispasmodic possibly through the calcium channel blocking mechanism...
  8. Souza H, De Araújo J, Martins Pinge M, Cozza I, Martins Dias D. Nitric oxide synthesis blockade reduced the baroreflex sensitivity in trained rats. Auton Neurosci. 2009;150:38-44 pubmed publisher
  9. Ali N, Ahmed G, Shah S, Shah I, Ghias M, Khan I. Acute toxicity, brine shrimp cytotoxicity and relaxant activity of fruits of callistemon citrinus curtis. BMC Complement Altern Med. 2011;11:99 pubmed publisher
    ..The crude methanol extract is safe at concentration 250 mg/ml or below and results of brine shrimp cytotoxicity assay imply the plant specie may be a source of cytotoxic agents. ..

More Information


  1. Chaudhary M, Imran I, Bashir S, Mehmood M, Rehman N, Gilani A. Evaluation of gut modulatory and bronchodilator activities of Amaranthus spinosus Linn. BMC Complement Altern Med. 2012;12:166 pubmed publisher
    ..The aqueous-methanolic extract of Amaranthus spinosus (A. spinosus Linn.,) whole plant, was studied for its laxative, spasmolytic and bronchodilator activities to validate some of its medicinal uses...
  2. Coelho L, Serra M, Pires A, Cordeiro R, Rodrigues e Silva P, dos Santos M, et al. 7-Epiclusianone, a tetraprenylated benzophenone, relaxes airway smooth muscle through activation of the nitric oxide-cGMP pathway. J Pharmacol Exp Ther. 2008;327:206-14 pubmed publisher
    ..Furthermore, oral administration of 7-epiclusianone reduces episodes of bronchial obstruction, warranting further research on this compound regarding a putative application in asthma therapy. ..
  3. Ali N, Ahmad B, Shah S. Spasmogenic and spasmolytic activities of Onosma griffithii Vatke. Pak J Pharm Sci. 2011;24:553-8 pubmed
    ..OG is exerted through blocking of calcium channels. However, n-butanolic and aqueous fractions produced spasmogenic effects that require further work for isolation of pharmacologically active substances. ..
  4. Ahmed T, Gilani A. Inhibitory effect of curcuminoids on acetylcholinesterase activity and attenuation of scopolamine-induced amnesia may explain medicinal use of turmeric in Alzheimer's disease. Pharmacol Biochem Behav. 2009;91:554-9 pubmed publisher
    ..Thus curcuminoids mixture might possess better therapeutic profile than curcumin for its medicinal use in AD. ..
  5. Radomirov R, Ivancheva C, Brading A, Itzev D, Rakovska A, Negrev N. Ascending and descending reflex motor activity of recto-anal region-cholinergic and nitrergic implications in a rat model. Brain Res Bull. 2009;79:147-55 pubmed publisher
  6. Gilani A, Shah A, Zubair A, Khalid S, Kiani J, Ahmed A, et al. Chemical composition and mechanisms underlying the spasmolytic and bronchodilatory properties of the essential oil of Nepeta cataria L. J Ethnopharmacol. 2009;121:405-11 pubmed publisher
    ..The study was aimed to investigate the chemical composition and pharmacological basis for traditional use of essential oil of Nepeta cataria L. (Limiaceae) (Nc.Oil) in gastrointestinal and respiratory disorders...
  7. Brandt L, Bjorkman D, Fennerty M, Locke G, Olden K, Peterson W, et al. Systematic review on the management of irritable bowel syndrome in North America. Am J Gastroenterol. 2002;97:S7-26 pubmed
  8. Williams D, Grill H, Cummings D, Kaplan J. Vagotomy dissociates short- and long-term controls of circulating ghrelin. Endocrinology. 2003;144:5184-7 pubmed
    ..The dissociation between nutrient load- and deprivation-related ghrelin responses indicates that the regulation of circulating ghrelin levels involves separate mechanisms operating through anatomically distinct pathways. ..
  9. Lesbros Pantoflickova D, Michetti P, Fried M, Beglinger C, Blum A. Meta-analysis: The treatment of irritable bowel syndrome. Aliment Pharmacol Ther. 2004;20:1253-69 pubmed
    ..Loperamide can be recommended in painless diarrhoea. Evidence is weak to recommend the use of bulking agents in the treatment of irritable bowel syndrome with constipation. ..
  10. Kennedy T, Jones R, Darnley S, Seed P, Wessely S, Chalder T. Cognitive behaviour therapy in addition to antispasmodic treatment for irritable bowel syndrome in primary care: randomised controlled trial. BMJ. 2005;331:435 pubmed
    ..To assess the efficacy of cognitive behaviour therapy delivered in primary care for treating irritable bowel syndrome...
  11. Alberti I, Grenier A, Kraus H, Carrara D. Pharmaceutical development and clinical effectiveness of a novel gel technology for transdermal drug delivery. Expert Opin Drug Deliv. 2005;2:935-50 pubmed
    ..This gel technology has demonstrated to be efficient for many drugs, as shown in the preclinical and clinical pharmacokinetic studies presented in this technology evaluation. ..
  12. Bashir S, Janbaz K, Jabeen Q, Gilani A. Studies on spasmogenic and spasmolytic activities of Calendula officinalis flowers. Phytother Res. 2006;20:906-10 pubmed
  13. Tack J, Fried M, Houghton L, Spicak J, Fisher G. Systematic review: the efficacy of treatments for irritable bowel syndrome--a European perspective. Aliment Pharmacol Ther. 2006;24:183-205 pubmed
  14. Gilani A, Jabeen Q, Ghayur M, Janbaz K, Akhtar M. Studies on the antihypertensive, antispasmodic, bronchodilator and hepatoprotective activities of the Carum copticum seed extract. J Ethnopharmacol. 2005;98:127-35 pubmed
    ..These results indicate the presence of calcium antagonist(s) in Carum copticum seeds and thus provides sound mechanistic basis for some of their folkloric uses. ..
  15. Ghayur M, Gilani A. Species differences in the prokinetic effects of ginger. Int J Food Sci Nutr. 2006;57:65-73 pubmed
  16. Zobrist R, Schmid B, Feick A, Quan D, Sanders S. Pharmacokinetics of the R- and S-enantiomers of oxybutynin and N-desethyloxybutynin following oral and transdermal administration of the racemate in healthy volunteers. Pharm Res. 2001;18:1029-34 pubmed
    ..The differences between R-OXY and R-DEO following the two routes of administration support the potential for comparable clinical efficacy and reduced anticholinergic side-effects with transdermal treatment. ..
  17. Lai H, Yang C, Huang F, Lee Y, Kuo Y, Kuo T. Respiratory-related arterial pressure variability as an indicator of graded blood loss: involvement of the autonomic nervous system. Clin Sci (Lond). 2003;105:491-7 pubmed
    ..We conclude that RAPV is comparable with%SPV as an indicator of graded haemorrhage and that, in anaesthetized and positive pressure ventilated rats, both are dependent on autonomic function, especially beta-adrenoceptors. ..
  18. Choudhury S, Garg S, Singh T, Mishra S. Cellular coupling of potassium channels with beta2 adrenoceptors in mediating myometrial relaxation in buffaloes (Bubalus bubalis). J Vet Pharmacol Ther. 2010;33:22-7 pubmed publisher
    ..Further, our studies also suggest promising therapeutic potential of potassium channel modulators as tocolytics in buffaloes. ..
  19. Vahedi F, Odenstedt J, Hartford M, Gilljam T, Bergfeldt L. Vectorcardiography analysis of the repolarization response to pharmacologically induced autonomic nervous system modulation in healthy subjects. J Appl Physiol (1985). 2012;113:368-76 pubmed publisher
  20. Romanski K. Characteristics of phase 3-like activity and rebound excitation triggered by hexamethonium and atropine administration in the ovine small bowel. Indian J Exp Biol. 2010;48:124-32 pubmed
    ..It is concluded that Hx and atropine evoke phase 3-like activity alternating with RE as the secondary stimulatory response in conscious sheep and both these types of the intestinal motility represent two distinct motility patterns...
  21. Eme J, Rhen T, Tate K, Gruchalla K, Kohl Z, Slay C, et al. Plasticity of cardiovascular function in snapping turtle embryos (Chelydra serpentina): chronic hypoxia alters autonomic regulation and gene expression. Am J Physiol Regul Integr Comp Physiol. 2013;304:R966-79 pubmed publisher
    ..This is the first study to link gene expression with morphological and cardioregulatory plasticity in a developing reptile embryo. ..
  22. Zhang G, Shimokawa S, Mochizuki M, Kumamoto T, Nakanishi W, Watanabe T, et al. Chemical constituents of Aristolochia constricta: antispasmodic effects of its constituents in guinea-pig ileum and isolation of a diterpeno-lignan hybrid. J Nat Prod. 2008;71:1167-72 pubmed publisher
    ..In addition, 9- O-[(-)-kaur-15-en-17-oxyl]cubebin was isolated as a new diterpeno-lignan hybrid, although this constituent did not exhibit antispasmodic activity. ..
  23. Astegiano M, Pellicano R, Sguazzini C, Berrutti M, Simondi D, Reggiani S, et al. 2008 Clinical approach to irritable bowel syndrome. Minerva Gastroenterol Dietol. 2008;54:251-7 pubmed
    ..Soluble fiber represents the first option in subjects with IBS and constipation or mixed IBS. Dietary integrators composed of probiotics and serotonin precursors are a promising therapeutic option. ..
  24. Fardiazar Z, Niknami F, Mashayekhi S, Ghojazadeh M. Hyoscine-N-butylbromide versus atropine as labour accelerant and analgesic: a randomized clinical trial. Pak J Biol Sci. 2013;16:443-5 pubmed
    ..001). Hyoscine appeared to be preferable to atropine specially in reducing the length of first stage of pregnancy. ..
  25. Xu A, Li Y, Zhu L, Tian T, Hao J, Zhao J, et al. Inhibition of endometrial fundocervical wave by phloroglucinol and the outcome of in vitro fertilization. Reprod Biol. 2013;13:88-91 pubmed publisher
    ..We found that phloroglucinol significantly inhibited (P<0.05) peristaltic fundocervical wave, suggesting a feasible way of application of phloroglucinol to suppress endometrial waves during IVF. ..
  26. Yilmaz B, Kart C, Kelekci S, Gokturk U, Sut N, Tarlan N, et al. Meperidine versus valethamate bromide in shortening the duration of active labor. Int J Gynaecol Obstet. 2009;107:126-9 pubmed publisher
    ..6+/-71.9 minutes), or between the valethamate bromide and the placebo group. Meperidine, but not valethamate bromide, significantly shortened the duration of active labor in nulliparous women with a singleton pregnancy at term. ..
  27. Khan A, Ali F, Khan D, Gilani A. Gut modulatory effects of Daphne oleoides are mediated through cholinergic and Ca++ antagonist mechanisms. Pharm Biol. 2011;49:821-5 pubmed publisher
    ..The present study describes the spasmogenic and spasmolytic activities of Daphne oleoides Schreb. (Thymelaeaceae), exploring the possible underlying pharmacological mechanisms...
  28. Leopard D, Fishpool S, Winter S. The management of oesophageal soft food bolus obstruction: a systematic review. Ann R Coll Surg Engl. 2011;93:441-4 pubmed publisher
    ..Until the results from such trials are available, the treatment of OSFBO will remain based on inconsistent clinical judgement. ..
  29. Darvish Damavandi M, Nikfar S, Abdollahi M. A systematic review of efficacy and tolerability of mebeverine in irritable bowel syndrome. World J Gastroenterol. 2010;16:547-53 pubmed
    ..08 (95% CI: 0.87-1.34, P = 0.463) for relief of abdominal pain. Thus, mebeverine is mostly well tolerated with no significant adverse effects; however, its efficacy in global improvement of IBS is not statistically significant. ..
  30. Tytgat G. Hyoscine butylbromide - a review on its parenteral use in acute abdominal spasm and as an aid in abdominal diagnostic and therapeutic procedures. Curr Med Res Opin. 2008;24:3159-73 pubmed
    ..With the generic and trade name of the drug combined with various search terms related to the relevant clinical applications, a thorough literature search was performed in the Medline and EMBASE databases in April 2008...
  31. Dekić M, Radulović N, Stojanović N, Randjelović P, Stojanović Radić Z, Najman S, et al. Spasmolytic, antimicrobial and cytotoxic activities of 5-phenylpentyl isothiocyanate, a new glucosinolate autolysis product from horseradish (Armoracia rusticana P. Gaertn., B. Mey. & Scherb., Brassicaceae). Food Chem. 2017;232:329-339 pubmed publisher
    ..A non-selective antimicrobial activity of all ITCs was revealed in the case of 6 bacterial and 2 fungal strains. ..
  32. Sekhavat L, Karbasi S, Fallah R, Mirowliai M. Effect of hyoscine butylbromide first stage of labour in multiparus women. Afr Health Sci. 2012;12:408-11 pubmed
    ..No serious adverse events were seen in the two groups. Injection of hyoscine in active phase of labor can be effective in shortening of labor without any adverse effect on mother and fetus. ..
  33. Tamai N, Matsuda K, Sumiyama K, Yoshida Y, Tajiri H. Glucagon facilitates colonoscopy and reduces patient discomfort: a randomized double-blind controlled trial with salivary amylase stress analysis. Eur J Gastroenterol Hepatol. 2013;25:575-9 pubmed publisher
    ..These results indicate that intravenous administration of glucagon can reduce patient discomfort and improve scope intubation during screening colonoscopy. ..
  34. Díaz Ferrer J, Parra V, Bendaño T, Montes P, Solorzano P. [Probiotic supplement (Lactobacillus acidophilus and bulgaricus) utility in the treatment of irritable bowel syndrome]. Rev Gastroenterol Peru. 2012;32:387-93 pubmed
    ..There were statistical differences in four variables: abdominal pain, intensity of pain, days of pain and total score at the end of therapy. Probiotics used as supplement are effective in improving symptomatology of IBS. ..
  35. Maser R, Lenhard M, Kolm P, Edwards D. Direct renin inhibition improves parasympathetic function in diabetes. Diabetes Obes Metab. 2013;15:28-34 pubmed publisher
    ..MCR means, baseline vs. follow-up, were 41.8 ± 19.7 vs. 50.8 ± 26.1 (aliskiren) and 38.2 ± 23.6 vs. 37.5 ± 24.1 (placebo). Parasympathetic function (i.e. MCR and E/I ratio) was enhanced by downregulation of the RAAS. ..
  36. Matsumoto F, Watanabe Y, Obi T, Islam M, Yamazaki Himeno E, Shiraishi M, et al. Characterization of 5-hydroxytryptamine-induced contraction and acetylcholine-induced relaxation in isolated chicken basilar artery. Poult Sci. 2012;91:1158-64 pubmed publisher
    ..The 5-HT(1) receptor might play a dominant role in 5-HT-induced contraction. One of the factors involved in ACh-induced relaxation is probably nitric oxide released from endothelial cells...
  37. Brankovic S, Kitic D, Radenkovic M, Veljkovic S, Jankovic T, Savikin K, et al. Spasmolytic activity of the ethanol extract of Sideritis raeseri spp. raeseri Boiss. & Heldr. on the isolated rat ileum contractions. J Med Food. 2011;14:495-8 pubmed publisher
    ..These data indicate that S. raeseri acts as a spasmolytic on intestinal smooth muscle, which justifies its use in gastrointestinal disorders. ..
  38. Nieves Martinez E, Haynes K, Childers S, Sonntag W, Nicolle M. Muscarinic receptor/G-protein coupling is reduced in the dorsomedial striatum of cognitively impaired aged rats. Behav Brain Res. 2012;227:258-64 pubmed publisher
    ..There was no effect of age on striatal [(3)H]AFDX-384 receptor binding. These results suggest that a decrease in M2/M4 muscarinic receptor coupling is involved in the age-associated decline in behavioral flexibility. ..
  39. Sayin H, Chapuis B, Chevalier P, Barrès C, Julien C. Assessment of cardiac autonomic tone in conscious rats. Auton Neurosci. 2016;194:26-31 pubmed publisher
    ..These data seriously question the use of the LF/HF ratio as an index of SVB, and the possibility to reliably estimate vagal and sympathetic tones separately through current pharmacological approaches in conscious rats. ..
  40. Harrison J, Hildreth C, Callahan S, Goodchild A, Phillips J. Cardiovascular autonomic dysfunction in a novel rodent model of polycystic kidney disease. Auton Neurosci. 2010;152:60-6 pubmed publisher
    ..01). Sympathetic baroreflex gain was not altered. This data suggests that sympathetic hyperactivity and reduced vagal function underlies the hypertension and reduced cardiac baroreflex function in the LPK model...
  41. He Y, Gai Y, Wu X, Wan H. Quantitatively analyze composition principle of Ma Huang Tang by structural equation modeling. J Ethnopharmacol. 2012;143:851-8 pubmed publisher
    ..SME can be used to quantitatively analyze the composition principle of Chinese compound prescriptions like MHT, which demystifies the ancient and classical system theory of traditional Chinese medicine from a totally new viewpoint. ..
  42. Mathew P, Bhatia S. Pathogenesis and management of irritable bowel syndrome. Trop Gastroenterol. 2009;30:19-25 pubmed
    ..The treatment of IBS is targeted at the management of constipation, diarrhoea and abdominal pain and includes pharmacotherapy with tegaserod, alosetron and lubiprostone. Cognitive behavioral therapy is very beneficial. ..
  43. Waine E, Stott M. Changing treatments for overactive bladder. Nurs Times. 2008;104:45-8 pubmed
    ..Elizabeth Waine and Mark Stott summarise the symptoms and investigations for overactive bladder and provide an overview of the treatments available. ..
  44. Williamson K, Breed M, Alibertis K, Brady W. The impact of the code drugs: cardioactive medications in cardiac arrest resuscitation. Emerg Med Clin North Am. 2012;30:65-75 pubmed publisher
    ..Although short-term outcomes are improved as a function of these medications, the final outcome has not been altered significantly in most instances. ..
  45. Azam S, Bashir S, Ahmad B. Anti-spasmodic action of crude methanolic extract and a new compound isolated from the aerial parts of Myrsine africana. BMC Complement Altern Med. 2011;11:55 pubmed publisher
    ..africana has antispasmodic action possibly through the calcium channel blocking mechanisms. A new compound Myrsigenin was isolated from the EtOAc fraction of the plant. ..
  46. Khan M, Anisuzzaman A, Semba S, Ma Y, Uwada J, Hayashi H, et al. M1 is a major subtype of muscarinic acetylcholine receptors on mouse colonic epithelial cells. J Gastroenterol. 2013;48:885-96 pubmed publisher
    ..The major M1 subtype was likely to regulate epithelial chloride secretion negatively and was susceptible to inflammation and may be relevant to inflammatory gut dysfunction. ..
  47. Cabitza P, Randelli P. Efficacy and safety of eperisone in patients with low back pain: a double blind randomized study. Eur Rev Med Pharmacol Sci. 2008;12:229-35 pubmed
    ..In conclusions, eperisone represents a valuable and safer alternative to other muscle relaxant agents for treatment of low back pain. ..
  48. Reme S, Stahl D, Kennedy T, Jones R, Darnley S, Chalder T. Mediators of change in cognitive behaviour therapy and mebeverine for irritable bowel syndrome. Psychol Med. 2011;41:2669-79 pubmed publisher
    ..Changes in behaviour and cognitions mediate the change in CBT given to IBS patients. The results strengthen the validity of a theoretical model of CBT by confirming the interaction of cognitive, emotional and behavioural factors in IBS. ..
  49. Joosen M, Smit A, van Helden H. Treatment efficacy in a soman-poisoned guinea pig model: added value of physostigmine?. Arch Toxicol. 2011;85:227-37 pubmed publisher
    ..Administration of physostigmine at that moment showed to be redundant or even harmful. Therefore, treatment of OP poisoning with a carbamate, such as physostigmine, should be carefully re-evaluated...
  50. Janbaz K, Jan A, Qadir M, Gilani A. Spasmolytic, bronchodilator and vasorelaxant activity of methanolic extract of Tephrosia purpurea. Acta Pol Pharm. 2013;70:261-9 pubmed
    ..On the basis of the above-mentioned findings, it can be concluded that the use of Tephrosia purpurea, in gastrointestinal spasm, asthma and hypertension is likely to be mediated through calcium channel blockage...
  51. West P, Horowitz B. Zigadenus poisoning treated with atropine and dopamine. J Med Toxicol. 2009;5:214-7 pubmed
    ..It has been suggested that vasopressors may be an effective therapy for this ingestion. We report the successful use of dopamine as therapy in Zigadenus ingestion...
  52. Wittmann T, Paradowski L, Ducrotte P, Bueno L, Andro Delestrain M. Clinical trial: the efficacy of alverine citrate/simeticone combination on abdominal pain/discomfort in irritable bowel syndrome--a randomized, double-blind, placebo-controlled study. Aliment Pharmacol Ther. 2010;31:615-24 pubmed publisher
    ..0001). Reported adverse events were similar in both groups. Alverine citrate/simeticone combination was significantly more effective than placebo in relieving abdominal pain/discomfort in patients with IBS. ..
  53. Olvey E, Armstrong E, Grizzle A. Contemporary pharmacologic treatments for spasticity of the upper limb after stroke: a systematic review. Clin Ther. 2010;32:2282-303 pubmed publisher
    ..BTX appeared to be an effective and well-tolerated focal treatment for reducing tonicity in patients with upper limb spasticity after stroke, supporting current guideline recommendations. ..