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PubMedDate not supplied

Dose effect of dicyclomine on the reduction of peristaltic artifacts on MRI of the abdomen.

BACKGROUND: It has been demonstrated that oral administration of dicyclomine significantly reduces the noise associated with the movement of the gastrointestinal tract in abdominal magnetic resonance (MR) images. Our objective was to determine the efficacy and security of two different doses of oral dicyclomine for the reduction of the gastrointestinal noise in abdominal MR imaging. METHODS: Forty-eight patients with MR imaging of the upper abdomen were enrolled in a prospective, controlled, randomized, and double-blind study. All patients ingested barium of high density (196 g in 130 mL of tap water, 250 w/v) approximately 25 min before the MR examination. Patients were randomly distributed into three groups of 16 patients each: (a) no-drug control group, (b) 20 mg of dicyclomine chlorhydrate, and (c) 80 mg of dicyclomine chlorhydrate. Quantitative image analysis was performed with region-of-interest measurements of the signal intensity in background air posterior and lateral to the patient and in the liver. Adverse effects were counted at 2 h and 1 day after the MR examination. RESULTS: The liver and incoherent noise signal intensities were not statistically different among groups. The control group presented a gastrointestinal noise (mean and SD of the air signal intensity) that was statistically superior to that of the groups with dicyclomine (p = 0.004 and p = 0.004, respectively), although significant differences were not observed between the two dicyclomine groups. Although the differences were not significant, adverse effects were more frequently associated with the higher doses of dicyclomine. All the adverse effects (most frequently, constipation, diarrhea, and abdominal pain) were considered minor and did not require treatment. CONCLUSION: Oral dicyclomine is effective and safe for the reduction of peristaltic artifacts on abdominal MR imaging. The dose of 20 mg presents an efficacy similar to that of 80 mg, with a probably lower incidence of adverse reactions.

Abdomen↗

PubMed2003

Antibacterial potential of an antispasmodic drug dicyclomine hydrochloride.

BACKGROUND & OBJECTIVES: Several compounds are known to possess antimicrobial activity in addition to their predesignated pharmacological actions. In the present study, dicyclomine hydrochloride, an antispasmodic drug, was tested for possible antimicrobial property in vitro and in vivo. METHODS: The minimum inhibitory concentration (MIC) of dicyclomine against the bacteria was determined by agar and broth dilution methods in vitro. The antibacterial activity of dicyclomine was confirmed by animal experiments. Toxicity and protective efficacy of the drug were tested in vivo. RESULTS: Dicyclomine inhibited most of the bacterial isolates tested at 25-100 microg/ml concentration, and a few were sensitive even at a lower concentration (10 microg/ml). Dicyclomine was found to be bacteriostatic in nature against Shigella dysenteriae 7, and bactericidal against S. aureus NCTC 6571, 8530, and 8531. When administered to Swiss white mice at doses of 30 and 60 microg/mouse, dicyclomine protected the animals challenged with 50 MLD of Salmonella typhimurium NCTC 74. INTERPRETATION & CONCLUSION: Dicyclomine showed inhibitory action against several pathogenic bacteria. It also offered significant protection to mice against the bacterial challange. As dicyclomine is in routine therapeutic use, it may be developed as a potent antimicrobial agent in many infections.

Anti-Bacterial Agents↗

PubMed1979

In vitro study of antispasmodic effects of dicyclomine hydrochloride on vesicourethral smooth muscle of guinea pig and rabbit.

Dicyclomine inhibition of acetylcholine-induced and barium chloride-induced isotonic contractions of the smooth muscle from three segments of the lower urinary tract (bladder body, bladder base, and proximal urethra) of the guinea pig and the rabbit was studied in vitro. In the guinea pig dicyclomine caused competitive inhibition of acetylcholine-induced contraction of the bladder body (1 x 10(-7) M to 1 x 10(-5) M) and the bladder base (1 x 10(-6) M, 1 X 10(-5) M) and was less potent than atropine and propantheline. In the rabbit significant blockade of acetylcholine-induced contractions occurred at dicyclomine concentrations of 5 x 10(-6) M to 3 x 10(-5) M in the bladder body and at 1 x 10(-5) M and 3 x 10(-5) M in the bladder base. In both species dicyclomine inhibitory effects were most marked in the bladder body, moderate in the bladder base, and minimal in the proximal urethra. Dicyclomine failed to cause inhibition of the barium chloride-induced contractions in the guinea pig vesicourethral smooth muscle. In rabbits, however, significant antagonism P less than 0.01) of barium chloride-induced muscle contraction was observed with dicyclomine at concentration 1 x 10(-5) M in both bladder body and the bladder base. The clinical implication of such properties of dicyclomine are discussed.

Acetylcholine↗

PubMed1986

Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine.

The selectivity profiles of the muscarinic receptor antagonists dicyclomine and trihexyphenidyl have been examined in binding and functional studies and compared with those of pirenzepine and atropine. Dicyclomine, trihexyphenidyl and pirenzepine demonstrated the highest affinity for the M1 muscarinic receptor subtype as revealed in competition experiments against [3H]-pirenzepine labelling of cortical membranes. Their affinity values lay in a narrow range (3.7-14 nM) approaching that of atropine (1.6 nM). Competition experiments against [3H]-N-methylscopolamine in cardiac and glandular (salivary) membranes revealed differences between the drugs examined. Dicyclomine, trihexyphenidyl and pirenzepine displayed low affinity for the cardiac and intermediate affinity for the glandular receptors. Thus, the drugs appeared to discriminate between the M1 (cortical) and the peripheral muscarinic subtypes (cardiac and glandular). However, atropine displayed similar affinities for either subtype with IC50s varying only slightly (1.6-4.6 nM). The rank order of selectivity was: pirenzepine greater than dicyclomine greater than trihexyphenidyl greater than atropine. Mirroring the binding data, pirenzepine, dicyclomine and trihexyphenidyl showed a tenfold greater ability at inhibiting M1-receptor mediated ganglionic responses (McN A-343 pressor effect in pithed rats and nictitating membrane contraction in cats) than at inhibiting peripheral muscarinic responses in the heart and cardiovascular smooth muscle (vagal bradycardia in rats and cats and vagally-induced vasodilatation in cats). The muscarinic antagonists so far examined can be categorized into two groups. Trihexyphenidyl, dicyclomine and pirenzepine, included in one group, are characterized by a higher affinity for the neuronal (M1) muscarinic receptor, hence they antagonize functional responses mediated by the M1 subtype. Atropine, a member of the other group, shows essentially no selectivity. 6 Differentiation of M1 and peripheral muscarinic receptor subtypes appears to be a property not confined to tricyclics such as pirenzepine but shared by diverse chemical structures. Both trihexyphenidyl and dicyclomine appear to be useful pharmacological tools in the classification of muscarinic receptor subtypes.

(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethy↗

PubMedDate not supplied

Effects of the selective M1 muscarinic receptor antagonist dicyclomine on emotional memory.

The nonselective muscarinic antagonist scopolamine is known to impair the acquisition of some learning tasks such as inhibitory avoidance. There has been recent research into the effects of this drug in contextual fear conditioning and tone fear conditioning paradigms. The purpose of the present study was to assess the role of the selective M1 muscarinic antagonist dicyclomine in these paradigms and in the inhibitory avoidance test. Rats were administered different doses of dicyclomine or saline 30 min before acquisition training. The animals were tested 24 hr later, and it was observed that 16 mg/kg of dicyclomine impaired both contextual fear conditioning and inhibitory avoidance. However, dicyclomine (up to 64 mg/kg) did not affect tone fear conditioning. These results suggest that the selective M1 muscarinic antagonist dicyclomine differentially affects aversively motivated tasks known to be dependent on hippocampal integrity (such as contextual fear conditioning and inhibitory avoidance) but does not affect similar hippocampus-independent tasks.

Acoustic Stimulation↗

PubMed1976

The mechanism of action of dicyclomine hydrochloride on rabbit detrusor muscle and vas deferens.

Dicyclomine inhibited responses of rabbit detrusor muscle to transmural stimulation more than atropine or lidocaine, and also inhibited responses to acetylcholine and to KCl. Responses of rabbit vas deferens to noradrenaline and transmural stimulation were inhibited by dicyclomine. Dicyclomine was as potent a local anesthetic as lidocaine, as determined by the guinea-pig wheal test. 45Ca++ exchange in the rabbit detrusor, measured by the lanthanum methods, was not altered by atropine, lidocaine or dicyclomine. It is concluded that dicyclomine not only acts as an anticholinergic agent but also impairs excitation-contraction coupling and release of transmitter from autonomic nerves.

Acetylcholine↗

PubMed1986

Dicyclomine in the sudden infant death syndrome (SIDS)--a cause of death or an incidental finding?

We report a case of a small infant apparently dying of the Sudden Infant Death Syndrome (SIDS) with a postmortem blood dicyclomine level of 200 ng/mL. Review of the literature and the comparison with blood dicyclomine values from four rabbits given equivalent doses suggests that a blood dicyclomine value of 200 ng/mL probably is in the therapeutic range for infants. Although safely used for years for infantile colic, recently, the administration of dicyclomine has been related to acute episodes of apnea, seizures, and coma. In the absence of those acute reactions, we feel that a 200-ng/mL blood dicyclomine level in a child dying of apparent SIDS should not prevent categorization of the death as SIDS.

Animals↗

PubMed1988

Dicyclomine discriminates between M1- and M2-muscarinic receptors in the guinea-pig ileum.

1. The affinity of the antagonist dicyclomine for subtypes of muscarinic receptors has been assessed in the myenteric plexus-longitudinal muscle preparation of the guinea-pig. 2. Dicyclomine had a high affinity (pA2 9.13) for the neuronal M1-receptor whose activation by pilocarpine causes an increase in acetylcholine release. Dicyclomine had a low affinity for both the prejunctional M2-receptor (pA2 7.61) mediating inhibition of the electrically-evoked acetylcholine release and the postjunctional M2-receptor (pA2 7.21). 3. It is concluded that dicyclomine distinguishes between M1- and M2-muscarinic receptors in functional experiments.

Animals↗

PubMed1985

Effect of dicyclomine on intestinal absorption, disposition and biliary excretion of dexamethasone.

The effect of dicyclomine, a cholinergic blocking agent, on the in situ intestinal absorption, plasma clearance, biliary excretion of dexamethasone was examined in rats. The plasma concentrations and area under the plasma concentration-time curve (AUC) of dexamethasone after both a single and repeated oral coadministration with dexamethasone phosphate (4 mg/kg) and dicyclomine (4 mg/kg) were significantly reduced compared with those after dexamethasone alone, without the alteration of elimination rate. The in situ absorption study also indicated that the absorption of dexamethasone was reduced to about a half after repeated coadministration of the two drugs. The renal plasma flow (RPF) in coadministration group was significantly enhanced compared with that of dexamethasone alone. The biliary excretion of dexamethasone was reduced, in proportion to the plasma concentrations, by dicyclomine. Therefore, dicyclomine should be administered taking much care in the corticosteroid treatment, because of producing the decrease in absorption.

Administration, Oral↗

PubMed1977

Antimuscarinic and noncompetitive antagonist properties of dicyclomine hydrochloride in isolated human and rabbit bladder muscle.

In isolated strips of bladder neck (prostatic capsule) and detrusor of rabbit and man, dicyclomine had minimal effect on the resting tension. Competitive antimuscarinic activity against carbachol could be demonstrated at doses of dicyclomine less than or equal to 1 X 10(-6) M, whereas at higher doses a noncompetitive action against both carbachol and potassium was observed. The ratio of dissociation constants relating to the noncompetitive and competitive actions, respectively, was about 1200, approximately 100 times higher than that previously reported in ileum. Dicyclomine was only about 1/30 as potent as atropine in competitive antimuscarinic activity. Dicyclomine hydrochloride may be useful in the clinical management of "uninhibited bladder."

Animals↗

PubMed1986

Dicyclomine, benzhexol and oxybutynine distinguish between subclasses of muscarinic binding sites.

The interactions of various unlabelled antimuscarinic drugs with the muscarinic receptors in the cerebral cortex, heart and urinary bladder were studied by a receptor binding technique, using (-)[3H]QNB as radioligand. In contrast to the other drugs examined, dicyclomine, benzhexol, oxybutynine and pirenzepine were bound with a significantly higher affinity in the cortex than in the heart and bladder. Furthermore, not only pirenzepine, but also dicyclomine and benzhexol were capable of distinguishing between two populations of muscarinic binding sites in the cortex. The low affinity sites for these drugs in the cortex were characterised by dissociation constants which were similar to those determined in the heart and the bladder, respectively. It was concluded that dicyclomine and benzhexol, like pirenzepine, are selective antagonists at the putative M1-receptor. Oxybutynine exhibited the same affinity profile but the tissue selectivity of this drug was less pronounced.

Animals↗

PubMed1981

Treatment of the irritable bowel syndrome with Bentyl (dicyclomine hydrochloride).

The effectiveness of Bentyl (dicyclomine hydrochloride) 40 mg 4 times daily was evaluated in an ambulatory population with recent irritable bowel syndrome (IBS). During the 2-week double-blind study, the effects of dicyclomine hydrochloride compared to placebo were assesed by: 1) physicians' global evaluation of treatment, 2) patients' self-evaluation of treatment, and 3) patients' evaluation of duration of abdominal pain. It was concluded that over a 2-week period dicyclomine hydrochloride 40 mg 4 times a day is superior to placebo in improving the overall condition of the patient, decreasing abdominal pain, decreasing abdominal tenderness, and improving bowel habits. The majority of adverse effects reported were related to the anti-cholinergic activity of the drug.

Abdomen↗

PubMed1981

Antagonism of calcium-induced contraction in potassium-depolarized rabbit detrusor muscle strips by dicyclomine hydrochloride and rociverine.

The musculotropic action of dicyclomine hydrochloride in bladder muscle has been attributed to its local anesthetic activity. In this study rabbit detrusor strips were depleted of calcium by incubation in Ca2+-free solution containing ethylene glycol bis(beta-aminoethyl ether)-N,N'-tetraacetic acid (EGTA). Contractions elicited by replacement of Ca2+ during depolarization with 80 mM K+ were only slightly affected by atropine or scopolamine but were antagonized in a noncompetitive manner by dicyclomine and rociverine (pD2' = 4.89 and 4.61, respectively). These contractions were also blocked with greater potency by nifedipine (pD2' = 8.50) and with lesser potency by lidocaine (pD2' = 2.52). Procaine was ineffective up to 1 mM. Comparison of the antagonism produced by dicyclomine and rociverine with that produced by nifedipine or lidocaine did not help to define the mechanism of the musculotropic drugs. However, as rociverine is not a local anesthetic and procaine was not effective, it appears that the "local anesthetic" property is not sufficient to explain the action of these musculotropic drugs.

Animals↗

PubMed2004

Experimental analysis of antimicrobial action of dicyclomine hydrochloride.

Dicyclomine hydrochloride is an antispasmodic agent. The MIC of dicyclomine against standard strains of Gram positive and Gram negative bacteria were performed by NCCLS broth dilution technique. These drugs showed a rapid killing action on Gram positive bacteria, Staphylococcus aureus NCTC 6571, 8530 and several other reference strains. The killing effect against Gram negative bacteria, Shigella boydii 8 NCTC 254/66 and Salmonella typhimurium NCTC 74 showed that the drug was bacteriostatic with respect to these strains. High rate of killing was achieved for most strains of Gram positive bacteria within 2 h. When administered to Swiss strain of white mice at doses of 30 and 60 microg/g of mouse, the drug could significantly protect the animals challenged with 50 MLD of Salmonella typhimurium NCTC 74. According to chi2 test, the in vivo data were highly significant (p<0.001). Since dicyclomine showed a remarkable inhibitory action against several pathogenic bacteria, in the course of time, it may be developed as a potent antimicrobial agent for many bacterial infections.

Animals↗

PubMed1975

A comparative study of two dicyclomine preparations in functional bowel disorders.

Using a double-blind crossover technique in patients suffering from maladies associated with gastrointestinal spasm, sustained-release 40 mg dicyclomine hydrochloride tablets (Merbentyl Dospan) have been compared with 20 mg plain dicyclomine hydrochloride tablets (Merbentyl). It has been concluded that these two dicyclomine formulations are equivalent in terms of efficacy and low incidence of side effects.

Adult↗

PubMedDate not supplied

Nuclear magnetic resonance spectroscopic determination of dicyclomine hydrochloride in tablet, capsule, and injection dosage forms.

A rapid and specific nuclear magnetic resonance (NMR) spectroscopic method was developed for determining dicyclomine hydrochloride in tablet, capsule, and injection dosage forms. The method consists of an extraction step with chloroform, evaporation of the solvent, addition of maleic acid as an internal standard, dissolution of the mixture in deuterated chloroform-deuterated acetone (40 + 60), NMR spectral determination, and integration of the peaks of interest. The concentration of dicyclomine hydrochloride in the dosage form was calculated from the integral values for the peaks of the test compound and the internal standard. The average recovery value +/- the standard deviation (n = 5) of dicyclomine hydrochloride added to synthetic samples was 99.7 +/- 0.9% (coefficient of variation 0.9%). The assay values for various commercial tablets, capsules, and injectables analyzed by using the proposed method differed in all cases by less than 1% from those obtained by using the USP XX titrimetric method. There was no interference from stearate, an excipient found in tablets and capsules, or from chloral hydrate, a preservative found in injectables .

Capsules↗

PubMed1988

Facilitatory and inhibitory muscarine receptors on the rat phrenic nerve: effects of pirenzepine and dicyclomine.

Neuronal transmitter stores of the rat phrenic nerve were labelled by an incubation with [3H]choline. Release of [3H]acetylcholine was elicited either by a short (100 pulses, 5 Hz) or by a long (1500 pulses, 5 or 25 Hz) period of electrical nerve stimulation. Pirenzepine and dicyclomine enhanced transmitter release evoked by the short stimulation period. Both antagonists reduced transmitter release evoked by the long stimulation period. Pirenzepine reduced transmitter release at low concentrations (1 nmol/l) whereas a higher concentration was necessary for the enhancing effect; the opposite pattern was found for dicyclomine. A low concentration of oxotremorine (10 nmol/l) enhanced and a high concentration (1 mumol/l) reduced transmitter release evoked by the short stimulation period. Both effects could be prevented by a low concentration of pirenzepine (10 nmol/l). It is concluded that facilitatory and inhibitory muscarine receptors are present on the motor nerve. A short stimulation period activates predominantly the negative muscarinic feedback, whereas during a long period of continuous nerve stimulation the positive muscarinic feedback mechanism is additionally activated. Both the facilitatory and inhibitory receptors might be regarded as M1-receptors but differences in the pharmacological properties between both receptor populations appear possible.

Acetylcholine↗

PubMed2000

Dicyclomine, an M1 muscarinic antagonist, reduces infarct volume in a rat subdural hematoma model.

The rat subdural hematoma (SDH) model produces a zone of ischemic brain damage within the hemisphere beneath the SDH. Previous studies have measured large increases in extracellular acetylcholine during cerebral ischemia in the rat. We examined infarct volume after selectively blocking muscarinic M1 receptors with dicyclomine during SDH. Rats were anesthetized with isoflurane (2%), intubated, and femoral artery and vein cannulated. Autologous blood (0.375 ml) was injected (0.05 ml/min) under the dura of the right parietal cortex. Dicyclomine (5 mg/kg, i.v.) was injected at 5 min after and again at 2 h after completion of the subdural blood infusion. Blood pressure and intracranial pressure (ICP) were continuously measured. At 4 h after SDH rats were euthanized, brains sectioned, and immunoreacted with glia fibrillary acidic protein. Cortical infarct volume was quantified in coronal brain sections at 0.7-mm intervals from +1.0 mm to -3.9 mm relative to bregma. Infarct volume in drug-treated rats (n = 10) 22.1 +/- 6.99 mm3 was significantly smaller (p < 0.02) than vehicle treated rats (n = 10) 56.7 +/- 9.59 mm3. ICP, blood pressure and cerebral perfusion pressure were not significantly different between groups. These data suggest that activation of M1 muscarinic receptors during an ischemic event may contribute to the development of subsequent pathology.

Animals↗