Crisaborole


Generic Medicine Info
Indications and Dosage
Topical/Cutaneous
Atopic dermatitis
Adult: For the treatment of mild to moderate cases: As 2% ointment: Apply a thin layer to the affected area(s) bid.
Child: ≥3 months Same as adult dose.
Special Precautions
Pregnancy and lactation.
Adverse Reactions
Significant: Hypersensitivity reactions (e.g. contact urticaria).
General disorders and administration site conditions: Application site pain (e.g. mild transient burning or stinging).
Skin and subcutaneous tissue disorders: Allergic contact dermatitis.
Monitoring Parameters
Monitor for signs of hypersensitivity reactions.
Action
Description:
Mechanism of Action: Crisaborole inhibits phosphodiesterase 4 (PDE-4) which causes an increase in intracellular cyclic adenosine monophosphate (cAMP) levels, a modulator of inflammatory responses. Although it acts as an anti-inflammatory agent, the exact mechanism for its effect on the treatment of atopic dermatitis has not been fully elucidated.
Pharmacokinetics:
Absorption: Rapidly absorbed systemically after topical application.
Distribution: Plasma protein binding: 97%.
Metabolism: Metabolised in the liver via hydrolysis into inactive major metabolite, 5-(4-cyanophenoxy)-2-hydroxyl benzylalcohol; this metabolite is metabolised further via oxidation into downstream metabolites, among which includes another major metabolite, 5-(4-cyanophenoxy)-2-hydroxyl benzoic acid.
Excretion: Via urine (as inactive metabolites).
Chemical Structure

Chemical Structure Image
Crisaborole

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 44591583, Crisaborole. https://pubchem.ncbi.nlm.nih.gov/compound/Crisaborole. Accessed Feb. 23, 2021.

Storage
Store between 15-30°C.
MIMS Class
Other Dermatologicals
ATC Classification
D11AH06 - crisaborole ; Belongs to the class of agents for atopic dermatitis, excluding corticosteroids. Used in the treatment of atopic dermatitis.
References
Anon. Crisaborole. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 05/02/2021.

Anon. Crisaborole. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 26/05/2023.

Buckingham R (ed). Crisaborole. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/02/2021.

Crisaborole. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 26/05/2023.

Eucrisa (Pfizer Laboratories Div Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 26/05/2023.

Eucrisa Ointment (Pfizer Labs). U.S. FDA. https://www.fda.gov. Accessed 26/05/2023.

Disclaimer: This information is independently developed by MIMS based on Crisaborole from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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