Lauromacrogol
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
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
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
Adverse events have been observed in animal reproduction studies. Do not use polidocanol during pregnancy.
Lactation
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 pearl | Monitor 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
| Formula | C30H62O10 |
|---|---|
| Molecular weight | 582.8 g/mol |
| IUPAC name | 2-[2-[2-[2-[2-[2-[2-[2-(2-dodecoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol |
| CAS | 3055-99-0 |
| PubChem CID | 656641 |
| InChIKey | ONJQDTZCDSESIW-UHFFFAOYSA-N |
| logP | 3.9 (XLogP 3.9) |
| Polar surface area | 103.0 Ų |
| H-bond acceptors / donors | 10 / 1 |
SMILES
CCCCCCCCCCCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOBiology & Pharmacokinetics
Pharmacokinetics predicted
| Bioavailability | 10.0% |
|---|---|
| Half-life | 0.415 h |
| Volume of distribution | 15.573 L/kg |
| Protein binding | 99.3% |
| BBB penetrant | No |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Registered Products (3)
| Brand | Form / strength | Pack | Agent | Citizen (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 | — |