Macrogol

Source: Wikipedia, the free encyclopedia.
For non-medical uses of this substance, see Polyethylene glycol.

Macrogol
Clinical data
Trade namesMiraLax, ClearLax, Golytely, others
Other namesPolyethylene glycol (PEG), PEG 3350, PEG 4000, PEG 6000
AHFS/Drugs.comProfessional Drug Facts
MedlinePlusa603032
License data
Pregnancy
category
  • AU: B1
Osmotic laxative
ATC code
Legal status
Legal status
  • UK: P (
    Pharmacy medicines
    ) / POM
  • US: ℞-only / OTC
  • Rx-only / OTC
Pharmacokinetic data
BioavailabilityNone
ExcretionFeces (100%)
Identifiers
  • Poly(oxyethylene)
CAS Number
DrugBank
ChemSpider
  • none
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaH–(OCH2CH2)n–OH
 ☒NcheckY (what is this?)  (verify)

Macrogol, also known as

bowels (known as "bowel prep") before a colonoscopy,[1] when the onset of the laxative effect is more rapid, typically within an hour.[5]

Side effects may include

osmotic laxative.[2] It works by increasing the amount of water in the stool.[3]

Macrogol came into use as a

electrolytes.[14] In 2021, the combination with electrolytes was the 295th most commonly prescribed medication in the US, with more than 500,000 prescriptions.[12][15]

Medical uses

A polyethylene glycol (PEG) and electrolytes solution used as a laxative used to cleanse the colon before colonoscopy, lower gastrointestinal series, or colon surgery.

Constipation

Macrogol 4000, pharmaceutical quality

Macrogol 3350, often in combination with electrolytes, is used for short-term relief of constipation as well as for long-term use in constipation of various causes, including in multiple sclerosis and Parkinson's disease patients (an often-overlooked non-motor symptom) as well as constipation caused by pharmaceutical drugs such as opioids and anticholinergics. Whole bowel irrigation with macrogol is part of the bowel preparation before surgery or colonoscopy. Limited data also support its use for the treatment of fecal impaction.[16]

In those with chronic constipation it works better than lactulose.[17]

A 2007 comparison showed that people with constipation had a better response to macrogol than to tegaserod.[18] Popular types include: macrogol 3350,[19] macrogol 4000, and macrogol 6000.[20] The number represents the average molecular mass.[citation needed] Combining different molecular masses provides some control over the consistency.[21]

Excipient

Macrogol is used as an

ointment bases, tablet binders, film coatings, and lubricants.[21]

For example, PEG-2000 is one of the excipients in the Moderna COVID-19 vaccine.[22][23]

PEGylation

Macrogols are also attached to

biopharmaceutical drugs to slow down their degradation in the human body and increase their duration of action, as well as to reduce immunogenicity. This process is called PEGylation.[24][25]

Contraindications

Contraindications for macrogol taken orally as a laxative are

intestinal perforation, bowel obstruction, ileus, inflammatory bowel diseases, and toxic megacolon.[16]

The doses of macrogol as an excipient are too low to have relevant contraindications.[26]

Allergy to macrogol is rare, and usually appears as an allergy to an increasing number of seemingly unrelated products, including cosmetics, drugs that use it as an excipient, and peri-procedural substances such as ultrasound gel.[27]

Adverse effects

Oral macrogol is generally well tolerated. Possible side effects include headache, bloating, nausea,

hyperkalaemia (high blood potassium levels). Hyperkalaemia is not an effect of macrogol itself but of potassium salts which are usually part of macrogol formulations.[16]
With excessive use, it can cause diarrhea.

Interactions

The interaction potential is low. Absorption of other pharmaceutical drugs can be reduced because oral macrogol accelerates intestinal passage, but this is seldom clinically relevant. For

antiepileptic drugs, such a mechanism has been described in rare cases.[16]

Pharmacology

Mechanism of action as a laxative

Macrogol is an osmotically acting laxative; that is, an inert substance that passes through the

gut motility.[16][28][29]

Chemistry

Main article: Polyethylene glycol
For the synthesis of macrogol, see Polyethylene glycol § Production.

Available forms

When sold for gut cleansing (and as a laxative), it is usually in combination with salts such as sodium bicarbonate, sodium chloride and potassium chloride[30] to help mitigate the possibility of electrolyte imbalance and dehydration. Brand names include CosmoCol, Cololyt, Glycoprep, Laxido, MiraLax, Molaxole, Movicol, and Osmolax.

Polyethylene glycol-electrolyte solution is a

indicated for cleansing of the colon in preparation for colonoscopy in adults.[38]

Research

PEGylation

PEGylated to form pegloticase, which improves its solubility at physiological pH, increases serum half-life and reduces immunogenicity without compromising activity. Upper images show the whole tetramer, lower images show one of the lysines that is PEGylated. (PDB: 1uox​ PEG-uricase model from reference[39]
)
Main article: PEGylation

When attached to various biopharmaceutical medications (which are proteins), macrogol results in a slowed clearance of the carried protein from the blood. This makes for a longer-acting medicinal effect and reduces toxicity, and it allows for longer dosing intervals. It also reduces the proteins' immunogenicity. Examples for PEGylated proteins include peginterferon alfa-2a and -2b, which are used to treat hepatitis C, pegfilgrastim, which is used to treat neutropenia, and pegloticase for the treatment of gout.[16]

Nerves and spinal cords

There is evidence demonstrating PEG-induced repair of specific nerve cells in animal models:

  • It has been shown that macrogol can improve healing of spinal injuries in dogs.[40]
  • One of the earlier findings is that macrogol can aid in nerve repair in earthworms.[41]
  • The subcutaneous injection of macrogol 2000 in guinea pigs after spinal cord injury leads to rapid recovery through molecular repair of nerve membranes.[42] The effectiveness of this treatment to prevent paraplegia in humans after an accident is not known yet.
  • Macrogol is being used in the repair of motor neurons damaged in crush or laceration incidents in vivo and in vitro in rats. When coupled with melatonin, 75% of damaged sciatic nerves were rendered viable.[43]

Cancer prevention

  • High-molecular-weight macrogol (e.g., 8000 g/mol) has been shown to be a dietary preventive agent against colorectal cancer in animal models.[44][medical citation needed]
  • The Chemoprevention Database shows macrogol is the most effective known agent for the suppression of chemical carcinogenesis in rats. Cancer prevention applications in humans, however, have not yet been tested in clinical trials.[45]

Other

References

  1. ^
    ISBN 9780857113382
    .
  2. ^ a b "DailyMed - polyethylene glycol 3350 powder, for solution". dailymed.nlm.nih.gov. Archived from the original on 26 April 2021. Retrieved 19 April 2019.
  3. ^ a b "Polyethylene Glycol 3350: MedlinePlus Drug Information". MedlinePlus. Archived from the original on 27 April 2021. Retrieved 19 April 2019.
  4. ^ a b "Macrogol as Excipient". Biesterfeld AG. Retrieved 10 June 2022.
  5. ^ "Package leaflet: Information for the User - Moviprep, powder for oral solution" (PDF). Medicines.org.uk. Retrieved 11 February 2024.
  6. ^ "PEG-3350 and Electrolytes for Oral Solution" (PDF). FDA. Archived (PDF) from the original on 30 August 2017. Retrieved 19 April 2019.
  7. ^ "Polyethylene glycol 3350 Use During Pregnancy". Drugs.com. Archived from the original on 28 April 2021. Retrieved 19 April 2019.
  8. ISBN 9780323401630
    .
  9. ^ "Prescription Polyethylene Glycol 3350; Denial of a Hearing and Order Withdrawing Approval of Abbreviated New Drug Applications". Federal Register. 2 April 2018. Archived from the original on 28 April 2021. Retrieved 19 April 2019.
  10. S2CID 78762418
    .
  11. ^ "Polyethylene glycol 3350 Uses, Side Effects & Warnings". Drugs.com. Archived from the original on 28 April 2021. Retrieved 19 April 2019.
  12. ^ a b "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  13. ^ "Polyethylene Glycol 3350 - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  14. ISBN 9780444537164
    .
  15. ^ "Polyethylene Glycol 3350 With Electrolytes - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  16. ^ a b c d e f Haberfeld, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag.
  17. PMID 20614462
    .
  18. S2CID 32055676
    .
  19. S2CID 42699177
    .
  20. S2CID 36543393
    .
  21. ^ a b Smolinske SC (1992). Handbook of Food, Drug, and Cosmetic Excipients. CRC Press. p. 287.
    ISBN 9780849335853
    .
  22. ^ "Pfizer–BioNTech COVID-19 Vaccine Standing Orders for Administering Vaccine to Persons 12 Years of Age and Older" (PDF). Centers for Disease Control and Prevention (CDC). Archived (PDF) from the original on 2 March 2021. Retrieved 5 March 2021.
  23. ^ "What Ingredients are in the COVID-19 Vaccine?" (PDF). Connecticut Department of Public Health. Archived (PDF) from the original on 7 July 2021. Retrieved 11 July 2021.
  24. PMID 12052707
    .
  25. S2CID 226664780
    .
  26. ^ "Compound Macrogol Oral Powder Sugar Free. - Summary of Product Characteristics (SmPC) - (emc)". www.medicines.org.uk. Archived from the original on 28 August 2021. Retrieved 10 January 2020.
  27. S2CID 1247758
    .
  28. ISBN 978-3-8047-2898-1
    .
  29. PMID 10726227
    .
  30. ^ [eg. Laxido package insert]
  31. ^ Meda Pharmaceuticals (February 2019). "COLYTE- peg-3350 and lectrolytes powder, for solution". dailymed. U.S. National Library of Medicine.
  32. ^ "Golytely- polyethylene glycol 3350, sodium sulfate anhydrous, sodium bicarbonate, sodium chloride, potassium chloride powder, for solution". DailyMed. 28 May 2021. Archived from the original on 31 March 2023. Retrieved 17 June 2023.
  33. ^ "Nulytely- polyethylene glycol 3350, sodium chloride, sodium bicarbonate and potassium chloride powder, for solution". DailyMed. 16 June 2022. Retrieved 17 June 2023.
  34. ^ "Moviprep- polyethylene glycol 3350, sodium sulfate, sodium chloride, potassium chloride, ascorbic acid, sodium ascorbate kit". DailyMed. 15 April 2022. Archived from the original on 3 February 2023. Retrieved 17 June 2023.
  35. ^ "Trilyte (polyethylene glycol 3350, sodium chloride, sodium bicarbonate and potassium chloride for oral solution) with flavor packs Initial U.S. Approval: 1991". DailyMed. Retrieved 17 June 2023.
  36. ^ "Polyethylene Glycol-Electrolyte Solution (Professional Patient Advice)". Drugs.com. 20 February 2020. Archived from the original on 8 June 2020. Retrieved 8 June 2020.
  37. ^ "Search or browse MIMS". mims.co.uk. Archived from the original on 24 April 2023. Retrieved 24 April 2023.
  38. ^ a b "SUFLAVE (polyethylene glycol 3350, sodium sulfate, potassium chloride, magnesium sulfate, and sodium chloride for oral solution)" (PDF). Braintree Laboratories, Inc. U.S. Food and Drug Administration. June 2023.
  39. PMID 17826865
    .
  40. ^ Bowman, Lee (4 December 2004). "Study on dogs yields hope in human paralysis treatment". seattlepi.com. Archived from the original on 22 September 2021. Retrieved 26 June 2016.
  41. PMID 2304913
    .
  42. S2CID 11902183
    .
  43. S2CID 24634247
    .
  44. PMID 10866305
    .
  45. ^ "Chemoprevention of Colorectal Cancer". Chemoprevention Database. Archived from the original on 23 November 2005. Retrieved 30 November 2012 – via Inra.fr.
  46. S2CID 4357934
    .

External links
Retrieved from "https://en.wikipedia.org/w/index.php?title=Macrogol&oldid=1211751967"