Crisaborole

Registered South African indications: 

• Atopic dermatitis - mild to moderate

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of its excipients

South African recommendations

Exercise caution in the following patient groups

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly

Hypersensitivity

• Hypersensitivity reactions like contact urticaria have been reported
• Severe pruritus, swelling, and erythema at the application site or a distant site
• Discontinue crisaborole immediately and initiate appropriate therapy if signs and symptoms of hypersensitivity appear

Ability to drive or use machines

• No studies with crisaborole on the effect of the ability to drive or use machines have been performed, therefore crisaborole has no known influence on the ability to drive or use machines

Forms avail. in SA and covered in this monograph: oin

South African registered indications and dosages

Atopic dermatitis - mild to moderate

• Topical (oin): Apply a thin layer, twice daily to the affected areas of skin

Safety and efficacy beyond 12 months of treatment have not been established

Crisaborole is for topical use only and not for ophthalmic, intranasal, oral, or intravaginal use

Paed. forms avail. in SA and covered in this monograph: oin

South African registered indications and dosages

Atopic dermatitis - mild to moderate

Younger than 2 years

• Not established for use

Older than 2 years

• See adult dosage

Safety and efficacy beyond 12 months of treatment have not been established

The safety and efficacy of crisaborole in paediatric patients below the age of 2 years have not been established

Crisaborole is for topical use only and not for ophthalmic, intranasal, oral, or intravaginal use

Pregnancy

South African recommendations

• Caution
• Safe use during pregnancy has not been established. There is no available data with crisaborole in pregnant women to inform the medicine-associated risk for major birth defects and miscarriage. In animal reproduction studies, there were no adverse developmental effects observed with oral administration of crisaborole in pregnant rats and rabbits during organogenesis at doses up to 3 and 2 times, respectively, the maximum recommended human dose (MRHD)

Breastfeeding

South African recommendations

• Caution
• Crisaborole is systemically absorbed following topical application, however it is unknown if crisaborole is excreted in human milk. Safe use during breastfeeding has not been established

Fertility

South African recommendations

• Reproduction studies in male or female rats using oral administration of crisaborole revelated no effects on fertility

South African recommendations

• Caution; no information available
  Pharmacokinetic profiles of crisaborole and its two metabolites have not been assessed in patients with renal impairment

South African recommendations

• Caution; no information available
  Pharmacokinetic profiles of crisaborole and its two metabolites have not been assessed in patients with hepatic impairment

South African recommendations

• Caution; no information available
  Pharmacokinetic profiles of crisaborole and its two metabolites have not been assessed in elderly patients
  Evidence from clinical studies of crisaborole did not include sufficient numbers of patients aged 65 years and over to determine whether they respond differently from younger patients

Skin and Subcutaneous Tissue Disorders

Common

• Atopic dermatitis
• Application site pain
  - Sensations such as burning and stinging
• Application site infection

Less common

• Application site reactions (including contact dermatitis and pruritus)
• Flare of atopic dermatitis

• None known

• Signs of hypersensitivity

Crisaborole is a phosphodiesterase 4 (PDE-4) inhibitor. PDE-4 inhibition results in increased intracellular cyclic adenosine monophosphate (cAMP) levels. While the specific mechanism(s) by which crisaborole exerts its therapeutic action is not well defined, crisaborole reduces the production of some inflammatory cytokines implicated in the pathophysiology of atopic dermatitis.

Ointment (per g) 20mg

• Staquis Ointment (Pfizer Laboratories) originator