octinoxate/bisoctrizole

Action and Spectrum

Actions and Spectrum: 

octinoxate and bisoctrizole are chemical compounds commonly used in sunscreens for UV protection. They belong to a class of compounds known as organic UV filters, which absorb or scatter ultraviolet (UV) radiation to prevent it from penetrating the skin.  

octinoxate: 

Action:  

octinoxate primarily absorbs UVB (shorter wavelength) radiation and converts it into less damaging heat. It is often combined with other sunscreen ingredients to provide broad-spectrum protection. 

UV Protection: octinoxate provides good protection against UVB radiation, which is responsible for causing sunburn and contributing to skin cancer. However, it offers limited protection against UVA radiation, penetrating deeper into the skin and contributing to premature aging and skin cancer. 

bisoctrizole: 

Action:  

bisoctrizole is a newer UV filter that provides broad-spectrum protection by absorbing UVA and UVB radiation. It is also known as Tinosorb M. 

UV Protection: bisoctrizole offers adequate protection against UVA and UVB radiation, making it a valuable ingredient in sunscreens. UVA protection is critical as it helps prevent skin aging and the growth of skin cancer. 

When combined in a sunscreen formulation, octinoxate and bisoctrizole can work synergistically to provide comprehensive protection against a wide range of UV radiation.

Drug Interaction

Adverse Reaction

Frequency not defined 

Hormonal disruption  

Skin rash  

Redness 

Skin irritation 

Skin allergy 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

octinoxate: 

Allergic Reactions: Individuals hypersensitive or allergic to octinoxate or other sunscreen ingredients should avoid using products containing octinoxate to prevent allergic reactions. 

bisoctrizole: 

Allergic Reactions: Like any other cosmetic ingredient, there is a potential for allergic reactions to bisoctrizole. Individuals with a known sensitivity or allergy to bisoctrizole or related compounds should avoid products containing this ingredient. 

Caution 

octinoxate: 

• Photosensitivity: octinoxate can cause photosensitivity in some individuals, potentially leading to increased skin sensitivity to sunlight. This could result in skin irritation or other adverse reactions upon sun exposure. 
• Hormone Disruption: There has been some concern about octinoxate’s potential to act as an endocrine disruptor due to its estrogenic activity. However, the levels used in sunscreen products are generally considered safe, and more research is needed to understand any potential effects fully. 
• Environmental Impact: octinoxate has been found to negatively affect aquatic life and coral reefs when it enters water systems. Be mindful of using sunscreens containing octinoxate when swimming in natural bodies of water. 

bisoctrizole: 

• Photosensitivity: While bisoctrizole is considered safe for use in sunscreens, like any sunscreen ingredient, some individuals can experience photosensitivity or skin irritation. 
• Allergic Reactions: Although less common, some individuals may still develop allergic reactions to bisoctrizole. If you have a history of skin allergies or sensitivities, it’s a good idea to do a patch test before applying sunscreen with bisoctrizole to a larger area. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

octinoxate (Ethylhexyl Methoxycinnamate) and bisoctrizole (Tinosorb M) are organic UV filters used in sunscreens. octinoxate absorbs UVB radiation and converts it into less harmful heat, protecting against sunburn. bisoctrizole, a broad-spectrum filter, absorbs UVA and UVB radiation, preventing skin damage, premature aging, and skin cancer. These compounds form a protective barrier on the skin’s surface, reducing the penetration of UV rays and minimizing their detrimental effects on skin cells and DNA, making them vital components in sun protection formulations. 

Pharmacodynamics: 

Mechanism of action: The mechanism of action for octinoxate and bisoctrizole involves their roles as organic ultraviolet (UV) filters in sunscreen products. These compounds protect the skin from the injurious effects of UV radiation from sun by absorbing or scattering the UV rays.  

octinoxate: octinoxate primarily absorbs UVB (ultraviolet B) radiation, which has shorter wavelengths and is responsible for causing sunburn and contributing to skin cancer. When octinoxate absorbs UVB radiation, it undergoes a photochemical reaction that converts the energy of the UV rays into heat. This heat is then dissipated away from the skin, reducing the potential for UV-induced damage. 

bisoctrizole: bisoctrizole is a broad-spectrum UV filter that absorbs UVA (ultraviolet A) and UVB radiation. It works by absorbing the energy of the UV rays and converting it into less harmful forms of energy, such as heat. bisoctrizole’s unique chemical structure effectively absorbs a wide range of UV wavelengths, making it a valuable component of sunscreens that provide comprehensive protection against UVA and UVB radiation. 

Pharmacokinetics: 

Absorption 

octinoxate is absorbed through the skin and is intended to remain on the skin’s surface, where it can absorb and filter UVB radiation. Some small amounts of octinoxate may be absorbed into the bloodstream, but studies suggest systemic absorption is generally low. 

bisoctrizole is designed to stay on the skin’s surface, absorbing and scattering UVA and UVB radiation. Some absorption through the skin may occur, but systemic absorption is generally considered low. 

Distribution 

Once absorbed into the bloodstream, octinoxate may be distributed throughout the body to some extent, but it is not typically expected to accumulate in tissues. 

bisoctrizole is not expected to accumulate in significant amounts in tissues if absorbed into the bloodstream. 

Metabolism 

octinoxate may undergo metabolism in the liver through hydroxylation and conjugation. The metabolites are then eliminated from the body. 

Information on the metabolism of bisoctrizole is limited, but it is likely to undergo similar processes of metabolism and elimination as other compounds in the body. 

Elimination and Excretion 

Metabolites of octinoxate are excreted from the body, primarily through urine and feces. 

Metabolites of bisoctrizole, if formed, would likely be excreted through urine and feces. 

Adminstartion

Administration: 

octinoxate and bisoctrizole are both organic UV filters commonly found in sunscreen products. They are applied topically to the skin to protect against the harmful effects of sun ultraviolet (UV) radiation.  

octinoxate: 

• octinoxate is available in various sunscreen formulations, including lotions, creams, sprays, and sticks. 
• To use octinoxate-containing sunscreen, follow these general steps: 
• Shake the sunscreen bottle (if applicable) before use. 
• Apply a small amount of sunscreen to all exposed skin areas that will be exposed to the sun. This includes the face, neck, arms, legs, and other exposed areas. 
• Rub the sunscreen into the skin until it is absorbed. 
• Reapply the sunscreen for every two hours or more frequently if you are sweating or swimming. 

bisoctrizole: 

• bisoctrizole is also available in various sunscreen formulations, similar to octinoxate. 
• To use bisoctrizole-containing sunscreen, follow similar steps as outlined for octinoxate: 
• Apply a sufficient amount of sunscreen to cover all exposed skin areas. 
• Gently massage the sunscreen into the skin until it is evenly distributed. 
• Reapply the sunscreen as directed on the product label, typically every two hours or after swimming or sweating. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: octinoxate / bisoctrizole 

Why do we use octinoxate / bisoctrizole? 

octinoxate (Ethylhexyl Methoxycinnamate) and bisoctrizole (Tinosorb M) are organic UV filters used primarily in sunscreen products. Their primary purpose is to protect against the harmful effects of the sun’s ultraviolet (UV) radiation. Here are their primary uses: 

Sunscreen Products: 

• octinoxate: octinoxate is commonly used in sunscreens to absorb and filter UVB radiation. It helps prevent sunburn and is often included in sunscreen formulations to provide broad-spectrum protection. 
• bisoctrizole: bisoctrizole is a newer UV filter offering UVA and UVB protection. It provides broad-spectrum coverage and enhances the effectiveness of sunscreens in preventing skin damage and premature aging caused by UV radiation. 

Both octinoxate and bisoctrizole, when formulated into sunscreen products, help reduce the risk of sunburn, skin aging, and skin cancer by providing a barrier against harmful UV rays.