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POLIDOCANOL

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Polidocanol skeletal.svg
Molecular Structure of 3055-99-0 (3,6,9,12,15,18,21,24,27-Nonaoxanonatriacontan-1-ol)

POLIDOCANOL

Synonym: Polidocanol; C12E9, Dodecyl nonaethylene glycol ether, Dodecylnonaglycol, Polidocanol, Polyoxyethylene (9) lauryl ether; trade names: Asclera, Aethoxysklerol and Varithena; Laureth-9; Dodecylnonaoxyethylene glycol monoether

IUPAC/Chemical Name: 3,6,9,12,15,18,21,24,27-nonaoxanonatriacontan-1-ol

3055-99-0
Chemical Formula: C30H62O10
Exact Mass: 582.4343Polidocanol 
CAS Registry Number: 9002-92-0 
CAS Name: a-Dodecyl-w-hydroxypoly(oxy-1,2-ethanediyl) 
Additional Names: polyethylene glycol (9) monododecyl ether; dodecyl alcohol polyoxyethylene ether; hydroxypolyethoxydodecane; laureth 9; polyoxyethylene lauryl ether 
Trademarks: Aethoxysklerol (Kreussler); Aetoxisclerol (Dexo); Atlas G-4829 (ICI); Hetoxol L-9 (Heterene Chem.)Line Formula: C12H25(OCH2CH2)nOH 
Literature References: Contains an average of nine ethylene oxide units and has an average mol wt ~600. Prepd by reaction of ethylene oxide and dodecyl alcohol: Pertsemlides, Soehring, Arzneim.-Forsch.10, 990 (1960). Toxicology: H. S. Zipf et al.,ibid.7, 162 (1957). Review of clinical experience: P. M. Goldman, J. Dermatol. Surg. Oncol.15, 204-209 (1989). 
Properties: Sol in water, ethanol, toluene. Miscible with hot mineral, natural and synthetic oils; with fats and fatty alcohols. LD50 in mice (mg/kg): 1170 orally, 125 i.v. (Zipf). 
Toxicity data: LD50 in mice (mg/kg): 1170 orally, 125 i.v. (Zipf) 
Use: Solvent; nonionic emulsifier; pharmaceutic aid (surfactant); spermaticide. 
Therap-Cat: Anesthetic (topical); antipruritic; sclerosing agent. 
Keywords: Anesthetic (Local); Antipruritic; Sclerosing Agent.

EINECS221-284-4
CAS No.3055-99-0Density1.007 g/cm3
PSA103.30000LogP4.04900
Solubility Melting Point33-36 °C
FormulaC30H62O10Boiling Point615.857 °C at 760 mmHg
Molecular Weight582.43Flash Point326.259 °C

Polidocanol is a local anaesthetic and antipruritic component of ointments and bath additives. It relieves itching caused by eczema and dry skin.[1] It has also been used to treat varicose veins,[2] hemangiomas, and vascular malformations.[3] It is formed by the ethoxylation of dodecanol.

Polidocanol is a local anaesthetic and antipruritic component of ointments and bath additives. It relieves itching caused by eczema and dry skin. It is formed by the ethoxylation of dodecanol. The substance is also used as a sclerosant, an irritant injected to treat varicose veins, under the trade names Asclera, Aethoxysklerol and Varithena. Polidocanol causes fibrosis inside varicose veins, occluding the lumen of the vessel, and reducing the appearance of the varicosity. The FDA has approved polidocanol injections for the treatment of small varicose (less than 1 mm in diameter) and reticular veins (1 to 3 mm in diameter). Polidocanol works by damaging the cell lining of blood vessels, causing them to close and eventually be replaced by other types of tissue.

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SYN

 

Yu, Zeqiong; Bo, Shaowei; Wang, Huiyuan; Li, Yu; Yang, Zhigang; Huang, Yongzhuo; Jiang, Zhong-Xing. Application of Monodisperse PEGs in Pharmaceutics: Monodisperse Polidocanols. Molecular Pharmaceutics. Volume 14. Issue 10. Pages 3473-3479. 2017.

SYN 2

Jiang, Zhongxing; Yu, Zeqiong. Process for preparation of monodisperse nona-polyethylene glycol dodecyl alcohol monoether and sulfate. Assignee Wuhan University, Peop. Rep. China. CN 106316802. (2017).

Sclerotherapy

Polidocanol is also used as a sclerosant, an irritant injected to treat varicose veins, under the trade names AscleraAethoxysklerol[4] and Varithena.[5] Polidocanol causes fibrosis inside varicose veins, occluding the lumen of the vessel, and reducing the appearance of the varicosity.

The FDA has approved polidocanol injections for the treatment of small varicose (less than 1 mm in diameter) and reticular veins (1 to 3 mm in diameter). Polidocanol works by damaging the cell lining of blood vessels, causing them to close and eventually be replaced by other types of tissue.[6][7] Polidocanol in the form of Varithena injected in the greater saphenous vein can cause the eruption of varicose and spider veins throughout the lower leg. This procedure should be done with caution and with the knowledge that the appearance of the leg may be forever compromised.

Pure polidocanol for pharmaceutical use

On March 30th,2010 the FDA approved Polidocanol under the trade name Asclera. Polidocanol is a sclerosing agent indicated to treat uncomplicated spider veins (varicose veins ≤1 mm in diameter) and uncomplicated reticular veins (varicose veins 1 to 3 mm in diameter) in the lower extremities. Varicose veins develop when the small valves inside the veins no longer work properly, allowing the blood to flow backwards and then pool in the vein.
When injected intravenously, Polidocanol works by locally damaging the endothelium of the blood vessel, causing platelets to aggregate at the site of damage and attach to the venous wall. Eventually, a dense network of platelets, cellular debris and fibrin occludes the vessel, which is then replaced with connective fibrous tissue. As one would expect for this type of molecule and also the mechanism of action, there is believed to be no specific molecular target for Polidocanol.
Polidocanol is a large ‘small molecule’ drug (Molecular Weight of 583 g.mol-1), with a mean half-life of 1.5 hr. Polidocanol is administrated intravenously and the strength of the solution and the volume injected depend on the size and extent of the varicose veins. Thus, the recommended dosage is 0.1 to 0.3 mL for each injection (Asclera 0.5% for spider veins and Asclera 1% for reticular veins) into each varicose vein, and a maximum recommended volume per treatment session of 10 mL.
Polidocanol’s chemical structure is 2-[2-[2-[2-[2-[2-[2-[2-[2-(dodecyloxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol. It is a non-ionic detergent, similar to polyethylene glycol (PEG) in structure, consisting of two components, a polar hydrophilic (dodecyl alcohol) and an apolar hydrophobic (polyethylene oxide – the part in brackets in the chemical structure) chain.

References

  1. ^ “E45 itch relief cream”. netdoctor.co.uk. Retrieved 2007-07-12.
  2. ^ Star P, Connor DE, Parsi K (April 2018). “Novel developments in foam sclerotherapy: Focus on Varithena® (polidocanol endovenous microfoam) in the management of varicose veins”. Phlebology33 (3): 150–162. doi:10.1177/0268355516687864PMID 28166694.
  3. ^ Gao Z, Zhang Y, Li W, Shi C (January 2018). “Effectiveness and safety of polidocanol for the treatment of hemangiomas and vascular malformations: A meta-analysis”. Dermatologic Therapy31 (1). doi:10.1111/dth.12568PMID 29082587.
  4. ^ Sclerotherapy, Laurence Z Rosenberg, MD, eMedicine.com
  5. ^ “Varithena™ (polidocanol injectable foam) For Intravenous Use. Full Prescribing Information” (PDF). Biocompatibles, Inc. Archived from the original (PDF) on 4 August 2016. Retrieved 1 October 2015.
  6. ^ Facts and Companies: Varicose Vein Treatment Approved
  7. ^ “Asclera Full Prescribing Information in Drug Reference Encyclopedia”. Retrieved 2010-04-11.
Clinical data
Other namesPolydocanolLaureth 9Macrogol lauryl etherLauromacrogolPEG-9 lauryl alcoholPOE-9 lauryl alcoholDodecylpolyethyleneglycoletherHydroxyl polyethoxy dodecaneOxypolyethoxydodecane
AHFS/Drugs.comInternational Drug Names
Pregnancy
category
Topical: allowed
Injection: contraindication in months 1–3 and after week 36
Routes of
administration
topical, subcutaneous injection
ATC codeC05BB02 (WHO)
Legal status
Legal statusOTC (topical),  (injection)
Identifiers
showIUPAC name
CAS Number9002-92-0 
3055-99-0
PubChem CID656641
ChemSpider570993 
UNII0AWH8BFG9A
KEGGD01993 
ChEMBLChEMBL1201751 
ECHA InfoCard100.019.351 
Chemical and physical data
FormulaC30H62O10
Molar mass582.816 g·mol−1
3D model (JSmol)Interactive image
showSMILES
showInChI
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////////POLIDOCANOL, Anesthetic ,  Antipruritic, Sclerosing Agent,

CCCCCCCCCCCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO

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DR ANTHONY CRASTO

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK LIFE SCIENCES LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 30 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 30 PLUS year tenure till date June 2021, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 90 Lakh plus views on dozen plus blogs, 233 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 33 lakh plus views on New Drug Approvals Blog in 233 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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