Docusate

Identification

Name
Docusate
Accession Number
DB11089
Type
Small Molecule
Groups
Approved
Description

Docusate, or dioctyl sulfosuccinate, is a stool softener used for the treatment of constipation and stimulation of bowel movement. It works by increasing the amount of water the stool absorbs in the gut, making the stool softer and easier to pass [3]. Docusate exhibits little intrinsic stimulatory actions at recommended doses [4]. Its sodium salt form dioctyl sodium sulfosuccinate commonly being the active ingredient, docusate can be orally or rectally administered. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. However the effectiveness of docusate in treating constipation remains unclear, as several studies report docusate to be no more effective than placebo for increasing the frequency of stool or stool softening [2]. Additionally, it does not appear to lessen symptoms associated with constipation such as abdominal cramps. Still decussate is available in over-the-counter products as one of common laxatives.

Synonyms
  • Colace
  • D-S-S
  • DIOCTYL CALCIUM SULFOSUCCINATE
  • DIOCTYL SODIUM SULFOSUCCINATE
  • dioctyl sulfosuccinate
  • docusate salts
  • doxinate
External IDs
E480
Product Ingredients
IngredientUNIICASInChI Key
Docusate calcium6K7YS503HC128-49-4DWKPZOZZBLWFJX-UHFFFAOYSA-L
Docusate sodiumNot Available577-11-7APSBXTVYXVQYAB-UHFFFAOYSA-M
Active Moieties
NameKindUNIICASInChI Key
Sodium cationionicLYR4M0NH3717341-25-2FKNQFGJONOIPTF-UHFFFAOYSA-N
Product Images
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Albert DocusateCapsule240 mgOralAventis Pharma Ltd.1991-12-312001-07-20Canada
Alta-docusate SodiumCapsule100 mgOralAltamed PharmaNot applicableNot applicableCanada
Apo-docusate CalciumCapsule240 mgOralApotex Corporation2002-11-25Not applicableCanada
Apo-docusate SodiumCapsule100 mgOralApotex Corporation2002-11-04Not applicableCanada
Basic Care Stool SoftenerCapsule, liquid filled100 mg/1OralL. Perrigo Company2018-03-27Not applicableUs
Calax Cap 240mgCapsule240 mgOralOdan Laboratories Ltd1989-12-312015-06-16Canada
ColaceSolution10 mgOralBoyd Pharmaceuticals Inc.1997-04-01Not applicableCanada
ColaceCapsule, liquid filled50 mg/1OralPurdue Pharmaceutical Products LP1900-01-07Not applicableUs
ColaceCapsule50 mg/1OralCardinal Health2011-06-072013-12-31Us
ColaceCapsule100 mg/1OralPhysicians Total Care, Inc.2011-11-08Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Calcium Docuphen CapDocusate calcium (60 mg) + Phenolphthalein (65 mg)CapsuleOralPharmascience Inc1988-12-311997-10-10Canada
CAREALL Senna-S LaxativeDocusate sodium (50 mg/1) + Sennosides (8.6 mg/1)TabletOralNew World Imports2016-04-18Not applicableUs
ColaceDocusate sodium (50 mg/1) + Sennosides (8.6 mg/1)Tablet, film coatedOralPurdue Pharmaceutical Products LP1957-02-08Not applicableUs
ColaceDocusate sodium (50 mg/1) + Sennosides (8.6 mg/1)Tablet, film coatedOralPurdue Pharmaceutical Products LP1957-02-08Not applicableUs
Colistat PlusDocusate sodium (50 mg/1) + Sennosides (8.6 mg/1)Tablet, film coatedOralAmvilab Llc2015-07-16Not applicableUs
Correctol Laxative TabDocusate sodium (100 mg) + Phenolphthalein (65 mg)TabletOralSchering Plough Healthcare Products Canada, A Division Of Schering Canada Inc.1971-12-311997-08-08Canada
CVS Adult EnemaDocusate sodium (283 mg/4.6g) + Benzocaine (20 mg/4.6g)LiquidRectalSummit Pharmaceuticals2014-09-01Not applicableUs
DocQLaxDocusate sodium (50 mg/1) + Sennosides (8.6 mg/1)Tablet, film coatedOralPar Pharmaceutical2007-07-262020-05-31Us
Docusate Plus SennaDocusate sodium (50 mg/1) + Sennosides A and B (8.6 min/1)Tablet, film coatedOralSafecor Health, LLC2014-09-30Not applicableUs
Docusate Sodium - SennosidesDocusate sodium (50 mg/1) + Sennosides (8.6 mg/1)Tablet, film coatedOralCardinal Health2017-01-27Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
BioFerr 90Docusate sodium (55 mg/1) + Ascorbic acid (138 mg/1) + Cyanocobalamin (16.8 ug/1) + Ferrous gluconate dihydrate (13.2 mg/1) + Folic Acid (1.4 mg/1) + Iron (88.5 mg/1)Tablet, film coatedOralBiocomp Pharma, Inc.2014-07-01Not applicableUs
CitraNatal 90 DHADocusate sodium (50 mg/1) + Ascorbic acid (120 mg/1) + Calcium citrate tetrahydrate (160 mg/1) + Cupric oxide (2 mg/1) + Folic Acid (1 mg/1) + Iron (90 mg/1) + Nicotinamide (20 mg/1) + Potassium triiodide (150 ug/1) + Pyridoxine hydrochloride (20 mg/1) + Riboprine (3.4 mg/1) + Thiamine chloride (3 mg/1) + Vitamin D (400 [iU]/1) + Zinc oxide (25 mg/1) + alpha-Tocopherol acetate (30 [iU]/1)TabletOralMission Pharmacal2010-02-01Not applicableUs
CitraNatal 90 DHADocusate sodium (50 mg/1) + Ascorbic acid (120 mg/1) + Calcium citrate tetrahydrate (159 mg/1) + Cupric oxide (2 mg/1) + Ferrous gluconate dihydrate (5 mg/1) + Folic Acid (1 mg/1) + Iron (85 mg/1) + Nicotinamide (20 mg/1) + Potassium Iodide (150 ug/1) + Pyridoxine hydrochloride (20 mg/1) + Riboflavin (3.4 mg/1) + Thiamine chloride (3 mg/1) + Thiamine mononitrate (4.54 mg/1) + Vitamin D (400 [iU]/1) + Zinc oxide (25 mg/1) + alpha-Tocopherol acetate (30 [iU]/1)TabletOralMission Pharmacal2014-04-11Not applicableUs
CitraNatal AssureDocusate sodium (50 mg/1) + Ascorbic acid (120 mg/1) + Calcium citrate tetrahydrate (124 mg/1) + Cholecalciferol (400 [iU]/1) + Copper (2 mg/1) + Doconexent (300 mg/1) + Folic Acid (1 mg/1) + Icosapent (0.75 mg/1) + Iodine (150 ug/1) + Iron (35 mg/1) + Nicotinamide (20 mg/1) + Pyridoxine hydrochloride (25 mg/1) + Riboflavin (3.4 mg/1) + Thiamine chloride (3 mg/1) + Vitamin E (30 [iU]/1) + Zinc (25 mg/1)KitMission Pharmacal2014-04-30Not applicableUs
CitraNatal AssureDocusate sodium (50 mg/1) + Ascorbic acid (120 mg/1) + Calcium citrate tetrahydrate (125 mg/1) + Cholecalciferol (400 [iU]/1) + Copper (2 mg/1) + Doconexent (300 mg/1) + Folic Acid (1 mg/1) + Icosapent (0.75 mg/1) + Iodine (150 ug/1) + Iron (35 mg/1) + Nicotinamide (20 mg/1) + Pyridoxine hydrochloride (25 mg/1) + Riboflavin (3.4 mg/1) + Thiamine chloride (3 mg/1) + Vitamin E (30 [iU]/1) + Zinc (25 mg/1)KitMission Pharmacal2008-11-19Not applicableUs
CitraNatal BloomDocusate sodium (55 mg/1) + Ascorbic acid (138 mg/1) + Cyanocobalamin (16.8 ug/1) + Ferrous gluconate dihydrate (13.2 mg/1) + Folic Acid (1.4 mg/1) + Iron (88.5 mg/1)Tablet, film coatedOralMission Pharmacal2017-08-01Not applicableUs
CitraNatal BloomDocusate sodium (55 mg/1) + Ascorbic acid (138 mg/1) + Cyanocobalamin (16.8 ug/1) + Ferrous gluconate dihydrate (13.2 mg/1) + Folic Acid (1.4 mg/1) + Iron (88.5 mg/1)Tablet, film coatedOralMission Pharmacal Company2017-08-012017-07-20Us
CitraNatal Bloom DHADocusate sodium (50 mg/1) + Ascorbic acid (120 mg/1) + Crypthecodinium cohnii dha oil (300 mg/300mg) + Cyanocobalamin (12 ug/1) + Ferrous gluconate dihydrate (1.5 mg/1) + Folic Acid (1 mg/1) + Iron (88.5 mg/1)KitOralMission Pharmacal2018-01-18Not applicableUs
CitraNatal DHADocusate sodium (50 mg/1) + Ascorbic acid (120 mg/1) + Calcium citrate tetrahydrate (125 mg/1) + Cupric oxide (2 mg/1) + Folic Acid (1 mg/1) + Iron (27 mg/1) + Nicotinamide (20 mg/1) + Potassium Iodide (150 mg/1) + Pyridoxine hydrochloride (20 mg/1) + Riboflavin (3.4 mg/1) + Thiamine chloride (3 mg/1) + Vitamin D (400 [iU]/1) + Zinc oxide (25 mg/1) + alpha-Tocopherol acetate (30 [iU]/1)TabletOralMission Pharmacal2007-11-20Not applicableUs
CitraNatal DHADocusate sodium (50 mg/1) + Ascorbic acid (120 mg/1) + Calcium citrate tetrahydrate (124 mg/1) + Cupric oxide (2 mg/1) + Doconexent (250 mg/1) + Folic Acid (1 mg/1) + Icosapent (0.625 mg/1) + Iron (27 mg/1) + Nicotinamide (20 mg/1) + Potassium Iodide (150 mg/1) + Pyridoxine hydrochloride (20 mg/1) + Riboflavin (3.4 mg/1) + Thiamine chloride (3 mg/1) + Vitamin D (400 [iU]/1) + Zinc oxide (25 mg/1) + alpha-Tocopherol acetate (30 [iU]/1)KitMission Pharmacal2014-05-22Not applicableUs
Categories
UNII
F05Q2T2JA0
CAS number
577-11-7
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Indicated for the treatment of constipation associated with dry, hard stools and decreased intestinal motility.

Indicated for the prevention of occasional constipation or opioid-induced constipation.

Pharmacodynamics

Docusate sodium is a laxative and an anionic detergent that promotes incorporation of water into stool, resulting in softer fecal mass [3]. The onset of action is 6-72 hours orally and 2 to 15 minutes rectally [3, 4]. The effects of docusate are thought to be exerted locally.

Mechanism of action

The effects of docusate may arise from the direct laxative effects of the molecule on the intestinal mucosa, or the indirect action of local endogenous prostaglandins released from the intestine upon contact with docusate. Docusate may involve multiple mechanisms of action. It stimulates the net secretion of water, sodium, chloride, and potassium and inhibits the net absorption of bicarbonate in the small intestine in vivo. It also induces active electrolyte secretion by increasing mucosal cAMP concentrations, as cAMP inhibits coupled sodium chloride entry and stimulates active chloride secretion in vitro. In vivo, the actions of cAMP are involved in inhibiting bicarbonate absorption in the jejunum. These changes promote the passive secretion of water and potassium. Docusate may partially involve impaired solute absorption such as glucose and bicarbonate by increasing the rate of desquamation of epithelial cells and mucosal cell damage. Mucosal damage may lead to the formation and release of local prostaglandins. Altered mucosal permeability may also be seen with docusate [1].

Absorption

Although docusate is minimally absorbed, small amounts may be absorbed systemically from the duodenum and jejunum following oral administration [3]. As the actions of docusate are mostly local, the pharmacokinetic parameters are not applied.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination

Systemically absorbed docusate undergoes biliary excretion [3].

Half life
Not Available
Clearance
Not Available
Toxicity

Docusate is not known to be carcinogenic or cause reproductive toxicity. It was not mutagenic in the Ames assay [MSDS]. Acute oral LD50 in rat is 1900 mg/kg [MSDS].

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(2-benzhydryloxyethyl)diethyl-methylammonium iodideThe therapeutic efficacy of Docusate can be decreased when used in combination with (2-benzhydryloxyethyl)diethyl-methylammonium iodide.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Docusate.
AclidiniumThe therapeutic efficacy of Docusate can be decreased when used in combination with Aclidinium.
AgmatineThe therapeutic efficacy of Docusate can be decreased when used in combination with Agmatine.
AlfentanilThe therapeutic efficacy of Docusate can be decreased when used in combination with Alfentanil.
AlmasilateThe therapeutic efficacy of Docusate can be decreased when used in combination with Almasilate.
AloglutamolThe therapeutic efficacy of Docusate can be decreased when used in combination with Aloglutamol.
AlphacetylmethadolThe therapeutic efficacy of Docusate can be decreased when used in combination with Alphacetylmethadol.
AlphaprodineThe therapeutic efficacy of Docusate can be decreased when used in combination with Alphaprodine.
Aluminium acetoacetateThe therapeutic efficacy of Docusate can be decreased when used in combination with Aluminium acetoacetate.
Food Interactions
Not Available

References

General References
  1. Moriarty KJ, Kelly MJ, Beetham R, Clark ML: Studies on the mechanism of action of dioctyl sodium sulphosuccinate in the human jejunum. Gut. 1985 Oct;26(10):1008-13. [PubMed:2414161]
  2. Tarumi Y, Wilson MP, Szafran O, Spooner GR: Randomized, double-blind, placebo-controlled trial of oral docusate in the management of constipation in hospice patients. J Pain Symptom Manage. 2013 Jan;45(1):2-13. doi: 10.1016/j.jpainsymman.2012.02.008. Epub 2012 Aug 11. [PubMed:22889861]
  3. Docusate sodium/Senna: Drug Information [Link]
  4. Docusate sodium Drug Summary [Link]
External Links
KEGG Drug
D00305
PubChem Substance
347911112
ChEBI
4674
ChEMBL
CHEMBL1477036
Drugs.com
Drugs.com Drug Page
Wikipedia
Docusate
ATC Codes
A06AG10 — Docusate sodium, incl. combinationsA06AA02 — Docusate sodium
AHFS Codes
  • 56:12.00 — Cathartics and Laxatives
MSDS
Download (129 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentIleus1
1, 2Not Yet RecruitingTreatmentOsteosarcoma in Children / Recurrent Osteosarcoma / Sarcoma, Osteogenic / Sarcomas1
1, 2RecruitingTreatmentMalignant Neoplasm of Pancreas1
2Active Not RecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML) / Myelodysplastic Syndrome1
2CompletedTreatmentAbdominal Pain (AP) / Prophylaxis against postoperative nausea and vomiting1
2RecruitingTreatmentDiabetic Gastroparesis1
2RecruitingTreatmentDisseminated Sclerosis / Incontinence, Fecal / Occasional Constipation1
2, 3CompletedTreatmentOccasional Constipation1
3CompletedTreatmentOccasional Constipation1
4CompletedDiagnosticColonoscopy1
4CompletedTreatmentColorectal Cleansing Prior Operation1
4CompletedTreatmentGeneral Surgery / Ileus / Occasional Constipation1
4RecruitingPreventionOccasional Constipation2
4TerminatedPreventionAnalgesia / Occasional Constipation1
Not AvailableCompletedPreventionFunctional Disorder of Intestine1
Not AvailableCompletedPreventionOccasional Constipation / Palliative Care1
Not AvailableCompletedScreeningColorectal Cancers1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Kit
CapsuleOral50 mg/1
Solution / dropsOral10 mg
SyrupOral20 mg/5mL
CapsuleOral240 mg/1
CapsuleOral100 mg/1
CapsuleOral250 mg/1
Capsule, liquid filledOral100 mg/1
Capsule, liquid filledOral50 mg/1
LiquidOral100 mg/10mL
LiquidOral50 mg/5mL
SolutionOral10 mg
LiquidRectal100 mg/5mL
Tablet, film coatedOral100 mg/1
TabletOral
LiquidRectal283 mg/5mL
LiquidRectal
TabletOral100 mg
Capsule, liquid filledOral250 mg/250mg
Capsule, liquid filledOral250 mg/1
Capsule, gelatin coatedOral100 mg/601
Capsule, liquid filledOral
Tablet, coatedOral
SyrupOral10 mg
LiquidOral50 mg/15mL
CapsuleOral200 mg
SyrupOral4 mg
SyrupOral50 mg
Capsule, gelatin coatedOral
TabletOral100 mg/1
SyrupOral20 mg
KitOral
CapsuleOral
CapsuleOral250 mg
TabletOral160 mg/1
Tablet, film coatedOral
PillOral
LiquidOral10 mg/1mL
SyrupOral60 mg/15mL
LiquidOral20 mg
Capsule, gelatin coatedOral100 mg/1
Capsule, liquid filledOral200 mg/1
Capsule, liquid filledOral240 mg/1
Capsule, gelatin coatedOral240 mg/1
CapsuleOral240 mg
CapsuleOral100 mg
EnemaRectal283 mg/5mL
EnemaRectal
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)153-157MSDS
water solubilitySolubleMSDS
logP3.95MSDS
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Drug created on December 03, 2015 09:51 / Updated on September 18, 2018 23:02