Identification
- Summary
Lactitol is an orally administered osmotic laxative used to treat chronic idiopathic constipation.
- Brand Names
- Pizensy
- Generic Name
- Lactitol
- DrugBank Accession Number
- DB12942
- Background
Lactitol, also known as 4-β-D-galactopyranosyl-D-glucitol, is a sugar alcohol synthesized from lactose.3 It is used in food manufacturing as a nutritive sweetener and is approximately 35% as sweet as table sugar (i.e. sucrose).1 Clinically, lactitol has been investigated for use as an osmotic laxative and, along with other non-absorbable disaccharides such as lactulose, in the treatment of hepatic encephalopathy in patients with cirrhosis.2,3
Pizensy, an oral lactitol powder for solution, was approved by the FDA for use in chronic idiopathic constipation in February 2020.4
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Lactitol (DB12942)
- Weight
- Average: 344.3124
Monoisotopic: 344.13186161 - Chemical Formula
- C12H24O11
- Synonyms
- Lactitol
- Lactitolum
- External IDs
- E-966
- INS NO.966
- INS-966
- NSC-231323
Pharmacology
- Indication
Lactitol is indicated for the treatment of chronic idiopathic constipation in adults.4
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Chronic idiopathic constipation •••••••••••• ••••• ••••••• ••• •••••••• Symptomatic treatment of Constipation •••••••••••• •••••• Treatment of Hepatic encephalopathy (he) •••••••••••• •••••• Symptomatic treatment of Occasional constipation ••• ••• ••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Lactitol helps to facilitate bowel movements by drawing water into the gastrointestinal tract.4 The oral administration of lactitol may reduce the absorption of concomitant medications - other oral medications should be administered at least 2 hours before or 2 hours after lactitol.4
- Mechanism of action
Lactitol is an osmotic laxative - it exerts its pharmacologic effect by creating a hyperosmotic environment within the small intestine. The osmotic effect generated by lactitol draws water into the small intestine, which loosens stools and ultimately facilitates bowel movements.4
- Absorption
In healthy subjects under fed conditions, oral administration of 20 grams of lactitol resulted in a mean Tmax of 3.6 ± 1.2 hours, Cmax of 776 ± 253 ng/mL, and a mean AUC of 6,019 ± 1,771 ng*hr/mL.4
- Volume of distribution
Data regarding the volume of distribution of lactitol are unavailable.
- Protein binding
As it undergoes little-to-no systemic absorption, lactitol is unlikely to be subject to protein binding.4
- Metabolism
As it undergoes little-to-no systemic absorption, lactitol is unlikely to undergo any significant degree of metabolism.4
- Route of elimination
Lactitol is not absorbed in the gastrointestinal tract to any significant extent. The vast majority of an ingested dose is likely degraded into organic acids in the colon and eliminated in the feces.4
- Half-life
The average half-life of orally administered lactitol is 2.4 hours.4
- Clearance
Data regarding the clearance of lactitol are unavailable.
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
The LD50 is 23 g/kg in mice and >30 g/kg in rats.5
Experience with acute overdosage is limited, but is likely to involve significant gastrointestinal upset and diarrhea consistent with the pharmacologic profile of lactitol. Overdosage should be managed with symptomatic and supportive measures, where necessary.4
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcetazolamide The risk or severity of dehydration can be increased when Acetazolamide is combined with Lactitol. Aclidinium The therapeutic efficacy of Lactitol can be decreased when used in combination with Aclidinium. Alfentanil The therapeutic efficacy of Lactitol can be decreased when used in combination with Alfentanil. Alloin The risk or severity of adverse effects can be increased when Lactitol is combined with Alloin. Almasilate The therapeutic efficacy of Lactitol can be decreased when used in combination with Almasilate. - Food Interactions
- Take with food. The manufacturer recommends administration with meals.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Lactitol monohydrate UH2K6W1Y64 81025-04-9 LXMBXZRLTPSWCR-XBLONOLSSA-N - International/Other Brands
- Importal
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Pizensy Powder, for solution 1 g/1g Oral Braintree Laboratories, Inc. 2020-02-12 Not applicable US 
Categories
- ATC Codes
- A06AD12 — Lactitol
- Drug Categories
- Alcohols
- Alimentary Tract and Metabolism
- Carbohydrates
- Compounds used in a research, industrial, or household setting
- Diet, Food, and Nutrition
- Drugs for Constipation
- Flavoring Agents
- Food
- Food Additives
- Food Ingredients
- Gastrointestinal Agents
- Laxatives
- Osmotic Activity
- Osmotic Laxatives
- Pharmaceutic Aids
- Pharmaceutical Preparations
- Stimulation Small Intestine Fluid/Electrolyte Secretion
- Sweetening Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as fatty acyl glycosides of mono- and disaccharides. These are compounds composed of a mono- or disaccharide moiety linked to one hydroxyl group of a fatty alcohol or of a phosphorylated alcohol (phosphoprenols), a hydroxy fatty acid or to one carboxyl group of a fatty acid (ester linkage) or to an amino alcohol.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Fatty Acyls
- Sub Class
- Fatty acyl glycosides
- Direct Parent
- Fatty acyl glycosides of mono- and disaccharides
- Alternative Parents
- Alkyl glycosides / O-glycosyl compounds / Disaccharides / Fatty alcohols / Sugar alcohols / Oxanes / Secondary alcohols / Polyols / Oxacyclic compounds / Acetals show 2 more
- Substituents
- Acetal / Alcohol / Aliphatic heteromonocyclic compound / Alkyl glycoside / Disaccharide / Fatty acyl glycoside of mono- or disaccharide / Fatty alcohol / Glycosyl compound / Hydrocarbon derivative / O-glycosyl compound show 9 more
- Molecular Framework
- Aliphatic heteromonocyclic compounds
- External Descriptors
- disaccharide (CHEBI:75323)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- L2B0WJF7ZY
- CAS number
- 585-86-4
- InChI Key
- VQHSOMBJVWLPSR-JVCRWLNRSA-N
- InChI
- InChI=1S/C12H24O11/c13-1-4(16)7(18)11(5(17)2-14)23-12-10(21)9(20)8(19)6(3-15)22-12/h4-21H,1-3H2/t4-,5+,6+,7+,8-,9-,10+,11+,12-/m0/s1
- IUPAC Name
- (2S,3R,4R,5R)-4-{[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}hexane-1,2,3,5,6-pentol
- SMILES
- OC[C@H](O)[C@@H](O)[C@H](O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O)[C@H](O)CO
References
- Synthesis Reference
冯建鹏, 孙田江, 张玉斌, 张虎跃, 朱年青, 杨俊, 赵文镜, 陆宏国, 霍浩刚, 高力虎. "Preparation of lactitol ." Chinese Patent CN101481395B, issued August 2011.
- General References
- Mooradian AD, Smith M, Tokuda M: The role of artificial and natural sweeteners in reducing the consumption of table sugar: A narrative review. Clin Nutr ESPEN. 2017 Apr;18:1-8. doi: 10.1016/j.clnesp.2017.01.004. Epub 2017 Feb 4. [Article]
- Gluud LL, Vilstrup H, Morgan MY: Non-absorbable disaccharides versus placebo/no intervention and lactulose versus lactitol for the prevention and treatment of hepatic encephalopathy in people with cirrhosis. Cochrane Database Syst Rev. 2016 May 6;(5):CD003044. doi: 10.1002/14651858.CD003044.pub4. [Article]
- Finney M, Smullen J, Foster HA, Brokx S, Storey DM: Effects of low doses of lactitol on faecal microflora, pH, short chain fatty acids and gastrointestinal symptomology. Eur J Nutr. 2007 Sep;46(6):307-14. doi: 10.1007/s00394-007-0666-7. Epub 2007 Jul 11. [Article]
- FDA Approved Drug Products: Pizensy (lactitol) oral solution [Link]
- MOLBASE: Lactitol monohydrate MSDS [Link]
- External Links
- KEGG Drug
- D08266
- PubChem Compound
- 157355
- PubChem Substance
- 347829086
- ChemSpider
- 138481
- BindingDB
- 50240023
- 28395
- ChEBI
- 75323
- ChEMBL
- CHEMBL1661
- ZINC
- ZINC000005225520
- Wikipedia
- Lactitol
- FDA label
- Download (265 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 2 Unknown Status Treatment Bacterial Colonization 1 Not Available Completed Not Available Bladder Dysfunction / Bowel Dysfunction / Fecal Impaction / Lower Urinary Tract Disorder 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Powder Oral 10 g Powder, for solution Oral 1 g/1g Powder, for solution Oral Syrup Oral Tablet, chewable Oral Tablet, soluble Powder, for solution Oral 10 G Powder, for solution Oral 200 G Syrup Oral 66.67 G/100ML - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US10806743 No 2020-10-20 2037-05-12 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 377.0 mg/mL ALOGPS logP -3.2 ALOGPS logP -5.5 Chemaxon logS 0.04 ALOGPS pKa (Strongest Acidic) 12.1 Chemaxon pKa (Strongest Basic) -3 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 11 Chemaxon Hydrogen Donor Count 9 Chemaxon Polar Surface Area 200.53 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 70.82 m3·mol-1 Chemaxon Polarizability 31.98 Å3 Chemaxon Number of Rings 1 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 173.00713 predictedDeepCCS 1.0 (2019) [M+H]+ 175.33714 predictedDeepCCS 1.0 (2019) [M+Na]+ 181.24965 predictedDeepCCS 1.0 (2019)
Drug created at October 21, 2016 01:30 / Updated at January 08, 2021 01:06