New Release: Alpha testing version has been released.

Lauromacrogol

C05B - Antivaricose therapy ATC C05BB02 Small molecule approved 2010 Parenteral

JFDA label: Aethoxysklerol 1%

Mechanism of Action

— Unknown

Indications

Approved

  • Asclera
  • Varicose veins
  • Varithena

Contraindications

Source: Lexicomp

  • Additional contraindications (not in the US labeling): Thrombophilia Absolute
  • Hypersensitivity to polidocanol or any component of the formulation Absolute
  • acute thromboembolic diseases Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Other (7)

Very Common irritation at injection site · local discoloration · local pruritus · Local: Hematoma at injection site · pain at injection site · warm sensation at injection site

Common Local: Venous thrombosis at injection site

Dosing

Source: Lexicomp

Varicose veins: IV: Asclera: Reticular veins (1 to 3 mm diameter): 0.1 to 0.3 mL of 1% solution per injection (maximum: 10 mL per session); may repeat in 7 to 14 days Spider veins (≤1 mm diameter): 0.1 to 0.3 mL of 0.5% solution per injection (maximum: 10 mL per session); may repeat in 7 to 14 days Varithena: Great saphenous veins and accessory saphenous veins: Up to 5 mL of 1% solution per injection (maximum: 5 mL per injection; 15 mL per session); may repeat in ≥5 days
Refer to adult dosing.
There are no dosage adjustments provided in the manufacturer’s labeling.
There are no dosage adjustments provided in the manufacturer’s labeling.

Warnings & Precautions

Source: Lexicomp

Anaphylaxis/hypersensitivity reaction

Severe allergic reactions, including anaphylaxis and fatal anaphylactoid reactions have been reported with polidocanol. More frequent with larger volumes (>3 mL), therefore, dose should be minimized. Observe 10 to 20 minutes following injection to monitor for hypersensitivity/anaphylactic reaction; emergency resuscitation equipment should be available.

Arterial embolism

Stroke, TIA, MI, and impaired cardiac function have been reported with IV solution. May be caused by air embolism, when using polidocanol IV solution foamed with room air, or thromboembolism. Avoid using polidocanol IV solution foamed with room air; safety and efficacy has not been established.

Thromboembolism

Thrombosis and subsequent pulmonary embolism or other thrombotic events can occur. Use with caution in patients with reduced mobility, history of deep vein thrombosis or pulmonary embolism, recent (≤3 months of age) major surgery, or prolonged hospitalization; increased risk for thrombosis. Other warnings/precautions:

Appropriate use

Check for proper needle placement; the smallest effective volume should be used at each injection site. After injection is complete, apply compression with stocking or bandage, and have patient walk for 15 to 20 minutes. Small intravaricose blood clots (thrombi) can develop; may be removed by stab incision and thrombus expression (microthrombectomy).

Tissue ischemia/necrosis

Intra-arterial injection or extravasation can cause severe necrosis, ischemia, or gangrene. Patients with underlying arterial disease, such as marked peripheral arteriosclerosis or thromboangiitis obliterans may be at increased risk for tissue ischemia. Consult a vascular surgeon immediately if intra-arterial injection occurs.

Pregnancy & Lactation

Pregnancy

FDA category C

Adverse events have been observed in animal reproduction studies. Do not use polidocanol during pregnancy.

Lactation

Avoid

It is not known if polidocanol is present in breast milk. Due to the potential for adverse reactions in a breastfed infant, breastfeeding is not recommended by the manufacturer.

Monitoring

Clinical pearlMonitor patient for anaphylactic or allergic reaction for at least 10 to 20 minutes after injection, and for signs/symptoms of DVT or PE.

Chemistry & Properties

2D structure
FormulaC30H62O10
Molecular weight582.8 g/mol
IUPAC name2-[2-[2-[2-[2-[2-[2-[2-(2-dodecoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol
CAS3055-99-0
PubChem CID656641
InChIKeyONJQDTZCDSESIW-UHFFFAOYSA-N
logP3.9 (XLogP 3.9)
Polar surface area103.0 Ų
H-bond acceptors / donors10 / 1
SMILESCCCCCCCCCCCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability10.0%
Half-life0.415 h
Volume of distribution15.573 L/kg
Protein binding99.3%
BBB penetrantNo

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (3)

BrandForm / strengthPackAgentCitizen (JOD)
Aethoxysklerol Ampoule 1 % 5 amp Almutanabbe Drug Store
Aethoxysklerol Ampoule 0.5 % 5 amp Almutanabbe Drug Store
Aethoxysklerol Ampoule 3 % 5 amp Almutanabbe Drug Store