Polidocanol does not have a specific molecular target. It acts as a local anaesthetic by blocking sodium channels in nerve membranes, thereby inhibiting nerve impulse conduction. As a sclerosant, it damages the endothelium of blood vessels, leading to thrombosis and fibrosis. Its detergent properties contribute to its antimicrobial and antipruritic effects. It is also a surfactant used in pharmaceutical formulations.

Research using many long-chain E-PDS from various organisms and a range of nonionic PEG detergents revealed that in vitro treatment with nonaethylene glycol monododecyl ether often produced respiratory quinones formed in vivo. The isoprenoid moiety's equivalent chain length. 2].
Polidocanol's in vitro activity is assessed by its local anaesthetic effects (sodium channel blockade), its surfactant properties, and its ability to damage endothelial cells. It is used in protein separation and purification as a detergent. Its efficacy as a sclerosant is evaluated in endothelial cell cultures. Specific IC50 values for sodium channel blockade are not publicly available.

Polidocanol is used clinically as a local anaesthetic, antipruritic agent, and sclerosant. It is administered topically for itching and as an ointment component. As a sclerosant, it is injected into varicose veins, where it locally damages blood vessel endothelium, leading to vein closure. Its in vivo efficacy has been established in clinical use.

Polidocanol does not have established receptor binding or enzyme inhibition assay protocols as it is not a pharmacologically active drug with a specific target. Its activity is assessed by measuring sodium channel blockade in electrophysiological assays, endothelial cell damage in cell culture, and surfactant properties. Physical properties: melting point 33-36°C; boiling point 615.9°C; flash point 326.3°C; purity: ≥98%. No specific biochemical assay protocols are applicable.

Cellular activity of Polidocanol is evaluated in endothelial cell cultures and neuronal cell cultures. Endothelial cells are treated with Polidocanol at various concentrations to assess cell damage and viability (MTT, LDH release). Neuronal cells are used to assess sodium channel blockade by measuring action potentials or sodium influx. Cell viability is assessed using standard assays. Each experiment includes appropriate positive and vehicle controls.

In vivo studies with Polidocanol are conducted in animal models of varicose veins or for local anaesthetic evaluation. The compound is administered topically or by injection. For sclerosant studies, veins are injected and evaluated for thrombosis and fibrosis. For local anaesthetic studies, effects on nerve conduction and pain responses are assessed. Clinical studies have been conducted for varicose vein treatment.

Absorption, Distribution and Excretion
Peak plasma concentrations are reached within 15 minutes after intravenous administration. Elimination route is not specified. Volume of distribution after intravenous administration is 35-82 L. Systemic clearance is 0.2-0.4 L/min. Metabolism/Metabolites Metabolism has not been determined. Biological Half-Life The half-life is approximately 1.5 hours.
Polidocanol has a molecular weight of 582.81 g/mol and a molecular formula of C30H62O10. Melting point: 33-36°C. Purity: ≥98%. Storage: powder at -20°C for 3 years, 4°C for 2 years. As a clinically used agent, its pharmacokinetics have been characterized. When injected as a sclerosant, it acts locally with minimal systemic absorption. It is metabolized and excreted. Half-life is not well-characterized.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
There is currently no information regarding the clinical use of polidocanol during lactation. While polidocanol is unlikely to have adverse effects on breastfed infants, international guidelines recommend suspending breastfeeding for 2 days after sclerotherapy.
◉ Effects on Breastfed Infants
No published information found as of the revision date.
◉ Effects on Lactation and Breast Milk
No published information found as of the revision date.

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Protein Binding
Plasma protein binding was not measured.
Polidocanol is generally well-tolerated when used as directed. Local adverse effects may include pain, swelling, and skin irritation at the injection site. Systemic effects are rare. As a sclerosant, it is contraindicated in patients with certain vascular conditions. Standard toxicology studies have demonstrated an acceptable safety profile for its approved uses. It is approved for clinical use in many countries.

[1]. Oil-in-Water Emulsion Templated and Crystallization-Driven Self-Assembly Formation of Poly(l-lactide)-Polyoxyethylene-Poly(l-lactide) Fibers. Langmuir. 2017 Nov 14;33(45):13060-13067.

[2]. Dependence of the product chain-length on detergents for long-chain E-polyprenyl diphosphate synthases. Biochemistry. 2013 Jul 23;52(29):5002-8.

[3]. Comparison of the different types of surfactants for the effect on activity and structure of soybean peroxidase. Langmuir. 2009 Feb 17;25(4):2363-8.

Polidocanol is a hydroxyl polyether, a derivative of nonyl glycol, with its terminal hydroxyl group replaced by a dodecyl (lauryl) group. It is a nonionic surfactant, hepatotoxic drug, and sclerosing agent. Its function is similar to that of nonyl glycol. Polidocanol is a sclerosing agent suitable for treating simple spider veins (varicose veins ≤1 mm in diameter) and simple reticular veins (varicose veins 1 to 3 mm in diameter) of the lower extremities. Its trade names are Asclera and Varitena. The structural formula of Polidocanol is C12H25(OCH2CH2)nOH, with an average degree of polymerization (n) of approximately 9 and an average molecular weight of approximately 600. Polidocanol is a lauryl alkyl polyethylene glycol ether with sclerosing effects and potential antitumor activity. Intralesional injection of Polidocanol can induce endothelial cell damage by disrupting calcium signaling and nitric oxide pathways. Following endothelial injury, platelets aggregate at the site of injury and attach to the vein wall, forming a dense network of platelets, cell debris, and fibrin that obstructs the vessel. Inducing endothelial cell damage in melanoma metastases may trigger an antitumor response in untreated peripheral lesions and inhibit the growth of metastases and other skin lesions.
See also: Ethylene oxide (containing monomers)...See more...
Drug Indications
Polydocaine is a sclerosing agent indicated for the treatment of simple spider angiomas and simple reticular veins of the lower extremities.
FDA Label
Mechanism of Action
After administration, polidocaine locally damages the vascular endothelium. Following endothelial injury, platelets aggregate at the site of injury and attach to the vein wall, eventually forming a dense network of platelets, cell debris, and fibrin that obstructs the vessel. Eventually, the vessel is replaced by connective tissue fibrous tissue.
Pharmacodynamics
Polydocaine has a concentration- and volume-dependent damaging effect on the vascular endothelium.
Polidocanol is also known as Nonaethylene glycol monododecyl ether and Nonaoxyethylene monododecyl ether. It is a local anaesthetic, antipruritic agent, and sclerosant. It is used in ointments, bath additives, and for varicose vein treatment. It is also used as a detergent in protein purification. It is approved for clinical use in many countries.

C30H62O10

582.816

582.434

3055-99-0

9043-30-5

656641

White to off-white oil

1.0±0.1 g/cm3

615.9±50.0 °C at 760 mmHg

33-36 °C

326.3±30.1 °C

0.0±4.0 mmHg at 25°C

1.459

2.18

1

10

37

40

431

0

CCCCCCCCCCCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO

ONJQDTZCDSESIW-UHFFFAOYSA-N

InChI=1S/C30H62O10/c1-2-3-4-5-6-7-8-9-10-11-13-32-15-17-34-19-21-36-23-25-38-27-29-40-30-28-39-26-24-37-22-20-35-18-16-33-14-12-31/h31H,2-30H2,1H3

2-[2-[2-[2-[2-[2-[2-[2-(2-dodecoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol

Asclera, Aethoxysklerol and Varithena C12E9, Dodecyl nonaethylene glycol ether, Dodecylnonaglycol, Polidocanol, Polyoxyethylene (9) lauryl ether Polidocanol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~250 mg/mL (~428.96 mM)
Ethanol : ~100 mg/mL (~171.58 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (3.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (3.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (3.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)