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Adapalene topical cream 0.1%; gel 0.1% and 0.3%; lotion 0.1%

Summary about Adapalene topical

Adapalene is a chemically stable, retinoid-like (Vitamin A) compound. Biochemical and pharmacological profile studies have demonstrated that adapalene is a potent modulator of cellular differentiation, keratinization and inflammatory processes all of which represent important features in the pathology of acne vulgaris. Mechanistically, adapalene binds to specific retinoic acid nuclear receptors but, unlike tretinoin, does not bind to the cytosolic receptor protein. Although the exact mode of action of adapalene is unknown, current evidence suggests that topical adapalene normalizes the differentiation of follicular epithelial cells resulting in decreased microcomedone formation. Studies in acne patients provide clinical evidence that topical adapalene is effective in reducing the noninflammatory acne lesions (open and closed comedones). Adapalene inhibits the chemotactic (directional) and chemokinetic (random) responses of human polymorphonuclear leucocytes in in vitro assay models; it also inhibits the metabolism of arachidonic acid, by lipoxidation, to inflammatory mediators. This profile suggests that the cell mediated inflammatory component of acne is modified by adapalene. Studies in human patients provide clinical evidence that topical adapalene is effective in reducing the inflammatory components of acne (i.e., papules and pustules).

 

 

Adapalene is for topical use. It is available on the market in the form of cream, gel and lotion.

 

 

Adapalene topical

Active Ingredient

Adapalene

Administration Route

Topical

Alcohol Warning

Avoid! Adapalene has the potential to induce local irritation in some patients, concomitant use of other potentially irritating topical products (medicated or abrasive soaps and cleansers, soaps and cosmetics that have a strong drying effect and products with high concentrations of alcohol, astringents, spices, or lime) should be approached with caution.

Available Strength

0,1 % and 0,3%

Breastfeeding Warning

Caution is recommended; use considered a low risk to the nursing infant.

Excreted into human milk: Unknown

Excreted into animal milk: Unknown

Comments:

-This drug should be used in areas away from the chest to prevent accidental contact with the infant’s skin.

-Ointments should not be applied to the breast prior to breastfeeding; if necessary, water-miscible cream or gel products may be used, but the products should not be applied to the nipple area.

Risk to the nursing infant is considered low, as only a negligible amount is absorbed after topical application.

Clinical Pharmacology

Pharmacodynamics

Adapalene is a chemically stable retinoid-like compound. Biochemical and pharmacological profile studies have demonstrated that adapalene is a modulator of cellular differentiation, keratinization, and inflammatory processes all of which represent important features in the pathology of acne vulgaris.

Pharmacokinetics 

Onset of action: 8 to 12 weeks

Absorption: Topical: Minimal; only trace amounts have been measured in serum after chronic application

Half-life elimination, terminal: 7 to 51 hours (gel)

Excretion: Bile

Cost

Cream (Adapalene External):

0.1% (per gram): $6.03 – $6.55

Gel (Adapalene External):

0.1% (per gram): $4.37

0.3% (per gram): $6.60 – $6.88

Lotion (Differin External)

0.1% (per mL): $9.86

Dosage Form

Cream, External:

0.1% (2 g, 15 g, 45 g, 60 g) [contains edetate disodium, methylparaben, propylparaben, trolamine (triethanolamine)]

Gel, External:

0.1% (2 g, 15 g, 45 g, 60 g) [contains edetate disodium, methylparaben, propylene glycol]

0.3% (2 g, 60 g) [contains edetate disodium, methylparaben, propylene glycol]

Lotion, External:

0.1% (59 mL) [contains methylparaben, propylene glycol, propylparaben]

Dose Schedule

Acne vulgaris: Topical: Apply once daily in the evening before bedtime. If irritation occurs, may reduce the frequency of application.

Rosacea (off-label use): Topical: 0.1% Gel: Apply to affected area once daily in the evening for up to 12 weeks 

Dosing: Pediatric

Acne vulgaris, treatment: Children ≥7 years and Adolescents: Limited data available in ages <12 years Topical: Apply once daily; cream, gel, or solution should be applied in the evening (at bedtime). Note: During the initial 2 weeks of therapy, it may appear that acne worsens; full effect may take up to 8 to 12 weeks of therapy.

Drug Class

D10AD — Retinoids for topical use in acne

Drug Unit

g/g (%)

Food Warning

No known interactions

Included In
Health Insurance Plan

32% of Medicare Part D and Medicare Advantage plans cover this drug.

Interacting Drugs

Adaplene topical has the potential to induce local irritation in some patients, concomitant use of other potentially irritating topical products (medicated or abrasive soaps and cleansers, soaps and cosmetics that have a strong drying effect, and products with high concentrations of alcohol, astringents, spices, or lime) should be approached with caution. Particular caution should be exercised in using preparations containing sulfur, resorcinol, or salicylic acid in combination with adapalene topical If these preparations have been used, it is advisable not to start therapy with adapalene topical until the effects of such preparations have subsided. No formal drug-drug interaction studies were conducted with adapalene topical.  

Is Available Generically

Yes. 

Is Proprietary

No

Label Details

https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021753s004lbl.pdf 

Legal Status

Legal.

Is not subject to the Controlled Substances Act.

Manufacturer

Galderma Laboratories

Maximum Intake

Once per day. No more than 12 weeks. 

Mechanism of Action

Mechanistically, adapalene binds to specific retinoic acid nuclear receptors (gamma and beta) and retinoid X receptors but does not bind to the cytosolic receptor protein. Although the exact mode of action of adapalene is unknown, it is suggested that topical adapalene may normalize the differentiation of follicular epithelial cells resulting in decreased microcomedone formation.

Non Proprietary Name

Adapalene

Overdosage

If the medication is applied excessively, no more rapid or better results will be obtained and marked redness, scaling, or skin discomfort may occur. Chronic ingestion of the drug may lead to the same side effects as those associated with excessive oral intake of vitamin A.

Pregnancy Category

This drug should be used during pregnancy only if the benefit clearly outweighs the risk to the fetus.

AU TGA pregnancy category: D
US FDA pregnancy category: CAU TGA pregnancy category D: Drugs which have caused, are suspected to have caused or may be expected to cause, an increased incidence of human fetal malformations or irreversible damage. These drugs may also have adverse pharmacological effects. Accompanying texts should be consulted for further details.

US FDA pregnancy category C: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

 

Pregnancy Warning

This drug should be used during pregnancy only if the benefit clearly outweighs the risk to the fetus.

Some experts recommend treatment discontinuation during pregnancy, while other experts recommend avoiding use during the first trimester.

Animal data have revealed evidence of fetal skeletal malformations, including supernumerary ribs, at high topical doses. Teratogenic effects were observed in animal models given large oral doses. There are no controlled data in human pregnancy.

Prescribing Info

https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021753s004lbl.pdf

Prescription Status

Prescription only

Proprietary Name

Differin, Plixda

Related Drugs

Tretinoin, Isotretinoin, Trifarotene, Motretinide

RxCUI

60223

Warning

Concerns related to adverse effects:

• Hypersensitivity reactions: Reactions such as pruritus, face edema, eyelid edema, and swelling have been reported. Discontinue use immediately if allergic or anaphylactoid/anaphylactic reactions occur.

• Photosensitivity: Use is associated with increased susceptibility/sensitivity to UV light; avoid sunlamps or excessive sunlight exposure. Daily sunscreen use and other protective measures are recommended. Patients with sunburn should discontinue use until sunburn has healed.

• Skin irritation: Certain cutaneous signs and symptoms such as erythema, dryness, scaling, stinging/burning, or pruritus may occur during treatment; these are most likely to occur during the first 2 to 4 weeks and will usually lessen with continued use. Treatment can increase skin sensitivity to weather extremes of wind or cold. Concomitant topical medications (eg, medicated or abrasive soaps and cleansers, or cosmetics with a strong drying effect, products with high concentrations of alcohol, astringents, spices or limes) should be avoided due to increased skin irritation. Depending on the severity of irritation, use moisturizer, reduce the frequency of application, or discontinue use.

Other warnings/precautions:

• Appropriate use: For external use only; avoid contact with abraded, broken, eczematous, or sunburned skin, mucous membranes, eyes, lips, and angles of the nose. Wax depilation is not recommended.

Warnings: Additional Pediatric Considerations

May cause mild hyperglycemia; more common in pediatric patients. Some dosage forms may contain propylene glycol; in neonates large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures and respiratory depression; use caution

 

References:

Drugs.com [Internet]. Adapalene Information from Drugs.com; c1996-2019 [Updated: 5 August 2019, Cited: 7 December 2019]. Available from: https://www.drugs.com/mtm/adapalene-topical.html 

Drugbank.ca [Internet]. Adapalene Information from Drugbank.ca; c1996-2019 [Updated: 6 December 2019, Cited: 7 December 2019]. Available from: https://www.drugbank.ca/drugs/DB00210 

Uptodate.com [Internet]. Adapalene Information from Uptodate.com; c1996-2019 [Topic 9621 Version 383.0, Cited: 7 December 2019]. Available from https://www.uptodate.com/contents/adapalene-drug-information#F130542 

Piskin S, Uzunali E. A review of the use of adapalene for the treatment of acne vulgaris. Ther Clin Risk Manag. 2007;3(4):621–624.

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