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Details

Stereochemistry ACHIRAL
Molecular Formula C18H13NO8S2.2Na.H2O
Molecular Weight 499.4254
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SODIUM PICOSULFATE

SMILES

c1ccnc(c1)C(c2ccc(cc2)OS(=O)(=O)[O-])c3ccc(cc3)OS(=O)(=O)[O-].[Na+].[Na+].O

InChI

InChIKey=FHYUVJHZGPGDSP-UHFFFAOYSA-L
InChI=1S/C18H15NO8S2.2Na.H2O/c20-28(21,22)26-15-8-4-13(5-9-15)18(17-3-1-2-12-19-17)14-6-10-16(11-7-14)27-29(23,24)25;;;/h1-12,18H,(H,20,21,22)(H,23,24,25);;;1H2/q;2*+1;/p-2

HIDE SMILES / InChI

Molecular Formula Na
Molecular Weight 22.9898
Charge 1
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula HO
Molecular Weight 17.0073
Charge -1
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C18H14NO8S2
Molecular Weight 436.4385
Charge -1
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Picosulfuric acid (as sodium picosulfate) is a contact laxative, which is used in combination with: magnesium oxide, and anhydrous citric acid for cleansing of the colon as a preparation for colonoscopy in adults. Sodium picosulfate is a prodrug. It has no significant direct physiological effect on the intestine. But it is hydrolyzed by colonic bacteria to form an active metabolite: bis-(p-hydroxy-phenyl)-pyridyl-2-methane, BHPM, which acts directly on the colonic mucosa to stimulate colonic peristalsis

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
PREPOPIK

Approved Use

PREPOPIK (sodium picosulfate, magnesium oxide and anhydrous citric acid) for oral solution is indicated for cleansing of the colon as a preparation for colonoscopy in adults.

Launch Date

1.34231045E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
18.1 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DEACETYLBISACODYL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
2.3 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DIHYDROXYDIPHENYL-PYRIDYL METHANE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
21.3 ng/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DEACETYLBISACODYL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
209 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DEACETYLBISACODYL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
275 ng × h/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DEACETYLBISACODYL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7.3 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DEACETYLBISACODYL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
7.4 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DIHYDROXYDIPHENYL-PYRIDYL METHANE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
10 h
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DEACETYLBISACODYL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG


OverviewOther

Drug as perpetrator​
PubMed

PubMed

TitleDatePubMed
Analytical control of a pharmaceutical formulation of sodium picosulfate by capillary zone electrophoresis.
2001 Feb 10
Oral sodium phosphate solution: a review of its use as a colorectal cleanser.
2004
Retrospective study of long-term treatment with sodium picosulfate.
2004 Apr
Is bowel preparation required before cystoplasty in children?
2006 Oct
[Distigmine bromide improves chronic intestinal pseudo-obstruction in a case of MELAS].
2007 Apr
Interaction between Shaoyao-Gancao-Tang and a laxative with respect to alteration of paeoniflorin metabolism by intestinal bacteria in rats.
2007 Aug
Evaluation of 18F-2-deoxy-2-fluoro-glucose positron emission tomography for gastric cancer screening in asymptomatic individuals undergoing endoscopy.
2007 Dec 3
A review of laxative therapies for treatment of chronic constipation in older adults.
2010 Dec
Laxative activities of Mareya micrantha (Benth.) Müll. Arg. (Euphorbiaceae) leaf aqueous extract in rats.
2010 Feb 16
Fixed combination of oxycodone with naloxone: a new way to prevent and treat opioid-induced constipation.
2010 Sep
Patents

Sample Use Guides

PREPOPIK ((sodium picosulfate, magnesium oxide, and anhydrous citric acid), supplied as a powder, must be reconstituted with cold water right before its use. There are two dosing regimens, each requires two separate dosing times: The preferred method is the “Split Dose” method and consists of two separate doses: the first dose during the evening before the colonoscopy and the second dose the next day, during the morning prior to the colonoscopy. The alternative method is the “Day Before” method and consists of two separate doses: the first dose during the afternoon or early evening before the colonoscopy and the second dose 6 hours later during the evening before the colonoscopy). Additional fluids must be consumed after every dose in both dosing regimens. Instruct patients to consume only clear liquids (no solid food or milk) on the day before the colonoscopy up until 2 hours before the time of the colonoscopy. Instruct patients that if they experience severe bloating, distention, or abdominal pain following the first dose, delay the second dose until their symptoms resolve.
Route of Administration: Oral
In Vitro Use Guide
Sodium picosulfate was biotransformed by intestinal flora that produced a novel sulfotransferase (not sulfatase). The biotransformation was activated by adding phenolic compounds such as phenol, acetaminophen and flavonoids. The enzyme activity related to this biotransformation was the highest in the contents of the caecum region of the intestine. The enzyme activity was 3.0 umole/hr/g wet feces in humans and 0.75 in rats (pH 8.0). The optimal pH was 9.0. The sulfotransferase activity was assayed in reaction mixture consisting of 60 uL of 50 mM PNS (occasionally sodium picosulfate), tyramine and 0.2 ml of the enzyme solution. Sulfatase activity was measured under the assay conditions for he sulfotransferase acitivity without the addition of the acceptor tyramine.
Substance Class Chemical
Created
by admin
on Fri Jun 25 20:53:44 UTC 2021
Edited
by admin
on Fri Jun 25 20:53:44 UTC 2021
Record UNII
LR57574HN8
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SODIUM PICOSULFATE
DASH   EP   MART.   ORANGE BOOK   USAN   USP   VANDF   WHO-DD  
USAN  
Official Name English
SODIUM PICOSULFATE HYDRATE [JAN]
Common Name English
SODIUM PICOSULFATE [VANDF]
Common Name English
DA 1773
Code English
DA-1773
Code English
PICO-SALAX
Brand Name English
SODIUM PICOSULFATE [WHO-DD]
Common Name English
GUTTALAX-FHER
Brand Name English
PICOSULFATE SODIUM
Common Name English
SODIUM PICOSULFATE [ORANGE BOOK]
Common Name English
4,4'-(2-PYRIDYLMETHYLENE)DIPHENOL BIS(HYDROGEN SULFATE) DISODIUM SALT MONOHYDRATE
Systematic Name English
SODIUM PICOSULFATE [EP]
Common Name English
LAXOBERAL
Brand Name English
SODIUM PICOSULFATE [MART.]
Common Name English
LA-391
Code English
SODIUM PICOSULFATE [EP MONOGRAPH]
Common Name English
SODIUM PICOSULFATE [USP MONOGRAPH]
Common Name English
LAXOBERON
Brand Name English
SODIUM PICOSULPHATE MONOHYDRATE
Common Name English
SODIUM PICOSULFATE [USAN]
Common Name English
SODIUM PICOSULPHATE
Common Name English
CLENPIQ COMPONENT SODIUM PICOSULFATE
Brand Name English
LA 391
Code English
SODIUM PICOSULFATE COMPONENT OF CLENPIQ
Brand Name English
SODIUM PICOSULFATE HYDRATE
JAN  
Common Name English
NEOPAX
Brand Name English
SODIUM PICOSULFATE MONOHYDRATE
Common Name English
PICOSULFATE SODIUM HYDRATE
Common Name English
PREPOPIK COMPONENT SODIUM PICOSULFATE
Brand Name English
SODIUM PICOSULFATE COMPONENT OF PREPOPIK
Brand Name English
SODIUM PICOSULFATE [USP-RS]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29697
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
WHO-VATC QA06AB58
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
WHO-ATC A06AB08
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
WHO-ATC A06AB58
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
WHO-VATC QA06AB08
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
Code System Code Type Description
DRUG BANK
DBSALT001830
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
FDA UNII
LR57574HN8
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
PUBCHEM
5282431
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
NCI_THESAURUS
C73845
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
USP_CATALOG
1614578
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY USP-RS
EPA CompTox
1307301-38-7
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
WIKIPEDIA
SODIUM PICOSULFATE
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
LACTMED
Sodium Picosulfate
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
EVMPD
SUB10569MIG
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
RXCUI
33688
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY RxNorm
MESH
C005701
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
DRUG CENTRAL
4779
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
EVMPD
SUB30654
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
CAS
1307301-38-7
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
ChEMBL
CHEMBL1741134
Created by admin on Fri Jun 25 20:53:44 UTC 2021 , Edited by admin on Fri Jun 25 20:53:44 UTC 2021
PRIMARY
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BASIS OF STRENGTH->SUBSTANCE
ASSAY (TITRATION)
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IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
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ACTIVE MOIETY