Identification
- Brand Names
- Phazyme
- Generic Name
- Dimethicone 410
- DrugBank Accession Number
- DB14005
- Background
Dimethicone is a silicone-based polymer used as a moisturizer in different skin OTC products.1 It is formed by repeated polymeric units of -(CH3)2SiO- with a terminal trimethyl siloxy unit.10 It is currently recognized by the FDA as a skin protectant OTC ingredient for human use in a concentration of 1-30%.5 The name dimethicone has a lot of nomenclature inconsistencies as it is used to refer to common names, generic names, trade names or even for the listing of mixtures. It is reported that the term dimethicone includes the notation of polydimethylsiloxane and trimethylsiloxy-terminated fluids between 20-30,000 cSt (viscosity).6
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- Not Available
Pharmacology
- Indication
Dimethicone is approved as a transdermal drug delivery system. Dimethicone 410 is part of the simethicone element in Dow Corning Q7-2242 LVA which is an antifoam.6,7 Some OTC's containing dimethicone are used to relieve the discomfort of infant gas caused by air swallowing or certain formulas or food,8 to prevent and help rash, to protect and relieve chapped or cracked skin9 and as an anti-lice agent.10
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination for symptomatic treatment of Chapped skin Combination Product in combination with: Triamcinolone (DB00620) •••••••••••• Used in combination for symptomatic treatment of Chapped skin Combination Product in combination with: Petrolatum (DB11058) ••• ••• Used in combination for prophylaxis of Diaper rash Combination Product in combination with: Triamcinolone (DB00620) •••••••••••• Used in combination for symptomatic treatment of Diaper rash Combination Product in combination with: Zinc oxide (DB09321) ••• ••• Used in combination for prophylaxis of Diaper rash Combination Product in combination with: Zinc oxide (DB09321) ••• ••• - Contraindications & Blackbox Warnings
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The activity of dimethicone as an anti-flatulent agent prevents the formation of mucus surrounding the gas pockets in the gastrointestinal tract. This allows the formation of big gas bubbles that can be expelled easily. Dimethicone is usually combined with an antacid to confirm the elimination of trapped gas. This particular combination is usually known as simethicone.3
The use of dimethicone 410 as an emollient and occlusive agent for the treatment of dry skin conditions has shown to prevent transepidermal water loss which translates into moisturizing of the dry or chapped skin.11 The effect of dimethicone also reduce flaking and acts as a lubricant which translates into the look of soft, smooth and flexible nature of healthy and young-looking skin.4
The use of dimethicone 410 as an anti-lice medication has been reported to effectively cause a lice mortality between 98-100% but the ovicidal effect seems to be limited.10
- Mechanism of action
Dimethicone, as well as all silicone derivatives, is considered as an occlusive and emollient agent. All occlusive agents act physically blocking transepidermal water loss by the formation of a hydrophobic film on the skin surface and within the superficial interstitium between corneocytes. Simethicone is often combined in drug products with petrolatum, which makes it greasy. The emollient characteristic of dimethicone is performed by filling the space between skin flakes which smooths the skin.2
For its use as an anti-flatulent agent, dimethicone 410 acts as an antifoaming agent and it works by reducing the surface tension of gas bubbles. This causes the combination of the bubbles to form larger bubbles in the stomach which can pass easily by means of belching.3
The use of dimethicone 410 in anti-lice medication has not been fully elucidated but it seems to be related to the disruption of the water balance mechanism in the lice which leads to the rupture of the gut.10
- Absorption
The use of dimethicone in skin moisturizers or anti-lice products have proven a very low absorption rate. Studies have indicated that approximately 0.5% of the dose applied to the skin could be considered as bioavailable. When given orally, as it is administered in anti-gas medications, dimethicone 410 is not absorbed or absorbed in very minimal quantities that account only for 0.001-0.2% of the administered dose. Therefore, a minimal to absent dimethicone form can be detected outside of the GI tract.10
- Volume of distribution
As dimethicone is pharmacologically inert and it is not absorbed, pharmacokinetic studies regarding the volume of distribution are not relevant.
- Protein binding
Dimethicone 410 does not bind to plasma proteins as it is not absorbed.
- Metabolism
Dimethicone 410 is not metabolized and it is excreted unchanged.10
- Route of elimination
In preclinical trials of skin preparations, dimethicone 410 was collected in trace levels in feces, expired air and subcutaneous swabs. When given orally, the entire dose of dimethicone can be found unchanged in feces and the recovery can account for even 99.6-99.8% of the administered dose. The limited absorbed dose can be found in urine as unchanged dimethicone.10
- Half-life
As dimethicone is pharmacologically inert and it is not absorbed, pharmacokinetic studies regarding its half-life are not relevant.
- Clearance
A very minimal amount of dimethicone is excreted unchanged in urine.10
- Adverse Effects
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The reported LD50 in preclinical rat studies after oral administration of dimethicones is 4070 mg/Kg.MSDS Long-term use of dimethicone in skin products may cause skin irritation and impaired cell development. Under the FDA, dimethicone is considered as a safe substance for human use.5
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- No interactions found.
Products
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Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Gas Relief Ultra Strength Capsule, liquid filled 180 mg/1 Oral Humanwell PuraCap Pharmaceutical (Wuhan), Ltd. 2013-04-15 Not applicable US 
Infants Relief Non-Staining Formula Liquid 20 mg/0.3mL Oral CVS Health 2012-02-03 Not applicable US Phazyme Capsule, gelatin coated 180 mg/1 Oral Preferred Pharmaceuticals, Inc. 2014-02-03 2019-02-14 US Phazyme Capsule, gelatin coated 180 mg/1 Oral Glaxo Smith Kline Consumer Heathcare Lp 2011-05-04 2015-09-30 US Phazyme Capsule, gelatin coated 180 mg/1 Oral Preferreed Pharmaceuticals Inc. 2011-05-04 2015-09-30 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image FIRST Mouthwash BLM Dimethicone 410 (0.315 g/236mL) + Aluminum hydroxide (3.15 g/236mL) + Diphenhydramine hydrochloride (.2 g/.2g) + Lidocaine hydrochloride (1.6 g/1.6g) + Magnesium hydroxide (3.15 g/236mL) Kit Oral CutisPharma, Inc. 2004-11-01 Not applicable US
Categories
- Drug Categories
- Not Available
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
- Head lice
Chemical Identifiers
- UNII
- TYU5GP6XGE
- CAS number
- 9006-65-9
References
- General References
- Ihde ES, Boscamp JR, Loh JM, Rosen L: Safety and efficacy of a 100% dimethicone pediculocide in school-age children. BMC Pediatr. 2015 Jun 20;15:70. doi: 10.1186/s12887-015-0381-0. [Article]
- Chularojanamontri L, Tuchinda P, Kulthanan K, Pongparit K: Moisturizers for Acne: What are their Constituents? J Clin Aesthet Dermatol. 2014 May;7(5):36-44. [Article]
- Washington N. (1961). Antacids and anti-reflux agents. CRC Press .
- Schueller R. and Romanowski P. (1999). Conditioning Agents for Hair and Skin. Marcel Dekker.
- FDA Code of Federal Regulations [Link]
- FDA Reports [Link]
- Dow corning monograph [Link]
- Dailymed [Link]
- Dailymed [Link]
- Public Assessment Report, Dimethicone [Link]
- Public Assesment report, Silicone [Link]
- External Links
- Not Available
- MSDS
- Download (41.6 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Completed Supportive Care Head And Neck Cancer / Mucositis / Radiation-Induced Disorder 1 Not Available Completed Other Bubbles in Colon at Time of Colonoscopy 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Kit Oral Capsule, liquid filled Oral 180 mg/1 Liquid Oral 20 mg/0.3mL Capsule, gelatin coated Oral 180 mg/1 - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source boiling point (°C) >65ºC as a silicone fluid 'MSDS' water solubility Insoluble 'MSDS' - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Drug created at April 06, 2018 16:29 / Updated at September 28, 2021 21:54