In all measurements, dicyclomine hydrochloride (ip; 8 mg/kg; daily) increased cognitive impairment. Additionally, compared to the dicyclomine hydrochloride-treated NonTg model, the memory impairment in the 3xTg-AD model was more severe. Mice were given dicyclomine hydrochloride (ip; 2.0, 4.0, and 8.0 mg/kg; 7 days). a notable influence on the model association learning (PAL) task's performance. Small results from systemic treatment at lower doses

Animal/Disease Models: C57Bl/6 mice [1]
Doses: 2.0, 4.0, 8.0 mg/kg
Route of Administration: intraperitoneal (ip) injection; behavioral impairment of mice in spatial tasks [3]. Daily; 7-day
Experimental Results: Damage due to factors outside the hippocampus.

Absorption, Distribution and Excretion
The bioavailability of dicyclomine has not been determined, though it is likely well absorbed as the primary route of elimination is in the urine. Dicyclomine has a Tmax of 1-1.5h.
Dicyclomine is 79.5% eliminated in the urine and 8.4% in the feces.
The volume of distribution for a 20mg oral dose is 3.65L/kg.
Data regarding the clearance of dicyclomine is not readily available.

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Metabolism / Metabolites
The metabolism of dicyclomine has not been well researched.

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Biological Half-Life
The mean plasma elimination half life is approximately 1.8 hours.

Hepatotoxicity
Like other anticholinergic agents, dicyclomine has not been linked to episodes of liver enzyme elevations or clinically apparent liver injury. The metabolism of dicyclomine is not well defined but it is likely metabolized by the liver.
References on the safety and potential hepatotoxicity of anticholinergics are given together in the Overview section on Anticholinergic Agents.
Drug Class: Anticholinergic Agents

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Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Dicyclomine has not been well studied during breastfeeding. However, one possible case of apnea has been reported in a breastfed infant that is similar to reactions that have occurred in infants given the drug directly. Dicyclomine should not be used during lactation.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date. The manufacturer reported a breastfed infant who developed apnea during maternal therapy with dicyclomine. Dicyclomine is a possible cause of the reaction.
◉ Effects on Lactation and Breastmilk
Relevant published information in nursing mothers was not found as of the revision date. Anticholinergics can inhibit lactation in animals, apparently by inhibiting growth hormone and oxytocin secretion. Anticholinergic drugs can also reduce serum prolactin in nonnursing women. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

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Protein Binding
Data regarding plasma protein binding of dicyclomine is not readily available.

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Interactions
...ANTICHOLINERGIC AGENTS, SUCH AS...DICYCLOMINE...WOULD BE EXPECTED TO INTERACT WITH DIGOXIN...

[1]. Pharmacological Characterization and Distribution of Muscarinic Receptors in Human Placental Syncytiotrophoblast Brush-Border and Basal Plasma Membranes. Eur J Pharmacol. 1997 Feb 12;320(2-3):209-14.

[2]. M1 Receptors Play a Central Role in Modulating AD-like Pathology in Transgenic Mice. 2006 Mar 2;49(5):671-82.doi: 10.1016/j.neuron.2006.01.020.

[3]. A Computer-Automated Touchscreen Paired-Associates Learning (PAL) Task for Mice: Impairments Following Administration of Scopolamine or Dicyclomine and Improvements Following Donepezil.Psychopharmacology (Berl). 2011 Mar;214(2):537-48.

Dicyclomine is the ester resulting from the formal condensation of 1-cyclohexylcyclohexanecarboxylic acid with 2-(diethylamino)ethanol. An anticholinergic, it is used as the hydrochloride to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome. It has a role as a muscarinic antagonist, an antispasmodic drug and a parasympatholytic. It is a tertiary amine and a carboxylic ester. It is functionally related to a 2-diethylaminoethanol and a 1,1'-bi(cyclohexyl)-1-carboxylic acid.
Dicyclomine is a muscarinic M1, M3, and M2 receptor antagonist as well as a non-competitive inhibitor of histamine and bradykinin used to treat spasms of the intestines seen in functional bowel disorder and irritable bowel syndrome. Though it is commonly prescribed, its recommendation may have been based on a small amount of evidence and so its prescription is becoming less favourable. Dicyclomine was granted FDA approval on 11 May 1950.
Dicyclomine is an Anticholinergic. The mechanism of action of dicyclomine is as a Cholinergic Antagonist.
Dicyclomine is an anticholinergic agent used to treat gastrointestinal conditions such as acid peptic disease and irritable bowel syndrome. Dicyclomine has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.
Dicyclomine is a carboxylic acid derivative and a selective anticholinergic with antispasmodic activity. Dicyclomine blocks acetylcholine from binding to muscarinic receptors on smooth muscle. This agent has a direct relaxing effect on smooth muscle and therefore prevents spasms in the muscles of the gastrointestinal tract, inhibits gastrointestinal propulsive motility, decreases gastric acid secretion and controls excessive pharyngeal, tracheal and bronchial secretion.
A muscarinic antagonist used as an antispasmodic and in urinary incontinence. It has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms.
See also: Dicyclomine Hydrochloride (has salt form).

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Drug Indication
Dicyclomine is indicated for the treatment of functional bowel disorder and irritable bowel syndrome.
FDA Label

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Mechanism of Action
Dicyclomine achieves its action partially through direct antimuscarinic activity of the M1, M3, and M2 receptors; and partially through antagonism of bradykinin and histamine. Dicyclomine non-competitively inhibits the action of bradykinin and histamine, resulting in direct action on the smooth muscle, and decreased strength of contractions seen in spasms of the ileum.
...MAJOR ACTION APPEARS TO BE NONSPECIFIC DIRECT RELAXANT ACTION ON SMOOTH MUSLCE RATHER THAN COMPETITIVE ANTAGONISM OF ACH.

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Therapeutic Uses
Muscarinic Antagonists; Parasympatholytics
...OFTEN CLASSIFIED WITH ANTIMUSCARINIC AGENTS AS "ANTISPASMODICS," DO NOT PROPERLY BELONG TO GROUP OF ANTIMUSCARINIC AGENTS. ...DICYCLOMINE HYDROCHLORIDE, VSP-DECR SPASM OF GI TRACT, BILIARY TRACT, URETER, & UTERUS WITHOUT PRODUCING CHARACTERISTIC ATROPINIC EFFECTS ON SALIVARY, SWEAT, OR GI GLANDS, EYE, CV SYSTEM... /HCL/
IT DECR MOTILITY BUT DOES NOT SUPPRESS GASTRIC SECRETION. IT IS USED IN TREATMENT OF IRRITABLE COLON, SPASTIC CONSTIPATION, MUCOUS COLITIS, SPASTIC COLITIS, PYLOROSPASM, & BILIARY DYSKINESIA. IN TREATMENT OF PEPTIC ULCER IT IS USED TO DELAY GASTRIC EMPTYING. /HYDROCHLORIDE/
ANTICHOLINERGIC /HYDROCHLORIDE/

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Drug Warnings
DICYCLOMINE SHOULD BE USED CAUTIOUSLY IN PT WITH PROSTATIC HYPERTROPHY, BLADDER NECK OBSTRUCTION, PYLORIC OBSTRUCTION, & CARDIOSPASM. EVEN THOUGH IT DOES NOT APPEAR TO RAISE INTRAOCULAR PRESSURE IN NARROW-ANGLE GLAUCOMA, IT IS ADVISABLE TO MONITOR PRESSURE OF SUCH PT.
CLINICAL USE OF.../BENTYL/ HAS BEEN DISAPPOINTING.
A 3-YR-OLD MALE INGESTED APPROX 100 TABLETS OF BENDECTIN & DEVELOPED TONIC-CLONIC SEIZURES FOLLOWED BY CARDIAC ARREST. ANALYSIS YIELDED HIGH LEVELS OF DOXYLAMINE, DICYCLOMINE & PYRIDOXINE. DOXYLAMINE APPEARS TO BE TOXIC CONSTITUENT.

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Pharmacodynamics
Dicyclomine is an anticholinergic drug used to relax the smooth muscles of the intestines. It's duration of action is not especially long as it is usually taken 4 times daily with individual doses of 20-40mg orally or 10-20mg by intramuscular injection. Dicyclomine should not be administered intravenously.

C19H35NO2.HCL

345.94764

345.243

67-92-5

Dicyclomine;77-19-0

3042

White to off-white solid powder

399.8ºC at 760 mmHg

164-166ºC

116.5ºC

5.204

0

3

8

22

326

0

CURUTKGFNZGFSE-UHFFFAOYSA-N

InChI=1S/C19H35NO2/c1-3-20(4-2)15-16-22-18(21)19(13-9-6-10-14-19)17-11-7-5-8-12-17/h17H,3-16H2,1-2H3

2-(diethylamino)ethyl 1-cyclohexylcyclohexane-1-carboxylate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~50 mg/mL (~144.53 mM)
DMSO : ~33.33 mg/mL (~96.34 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (7.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (7.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 50 mg/mL (144.53 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)