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all-trans retinoic acid; tretinoin (Retin-A, Renova, Avita, Altreno, ATRA)

Topical agent: Tradename: Retin-A, Avita. Systemic agent: ATRA. Indications: 1) acne vulgaris 2) palliative care for skin aging a) improve signs of photodamage (dermatoheliosis) b) most effective on non-sun-exposed areas [5] 3) treatment of promyelocytic leukemia -> alone or in combination with anthracyclines 4) verruca plana 5) lamellar ichthyosis 6) Darier-White disease Contraindications: - prevention of non-melanoma skin cancers [8] - pregnancy category D (oral) [4] - pregnancy category C (topical) [4]* * ref [4] adds that anticipated benefit should clearly outweigh any potential risk & that most dermatologists avoid using topical retinoids during pregnancy Dosage: - topical: apply QHS. Packaging: 1) Retin-A for acne a) cream 0.025%, 0.05%, 0.1% (20 g, 45 g) b) gel 0.01%, 0.025% (15 g, 45 g) c) liquid 0.05% (28 mL) 2) Renova for wrinkles - cream 0.05% 3) Avita 0.025% gel or cream 4) Altreno (lotion 0.05%) [9] Adverse effects: 1) not common (1-10%) - edema, excessive dryness, erythema, scaling of skin, hyperpigmentation, hypopigmentation, stinging, blistering, photosensitivity 2) other - local inflammation - teratogenic - avoid during pregnancy & nursing - topical use associated with increased risk of mortality in elderly [7] - all-trans-retinoic acid-induced differentiation syndrome [4] - neutrophilic dermatosis - pyoderma gangrenosum, Sweet syndrome [4] Mechanism of action: 1) inhibition of keratinization 2) sloughing of horny cells 3) may enhance repair of UV damage 4) promotes cellular differentiation 5) thickens epidermis & rete ridges

General

antineoplastic agent (chemotherapeutic agent) retinoic acid

Properties

MISC-INFO: pregnancy-category D safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Medical Knowledge Self Assessment Program (MKSAP) 11, 16, 17. American College of Physicians, Philadelphia 1998, 2012, 2015.
  5. UCLA Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 12-15, 2001
  6. Department of Veterans Affairs, VA National Formulary
  7. Weinstock MA et al Topical tretinoin therapy and all-cause mortality. Arch Dermatol 2009 Jan; 145:18. PMID: 19153339 - Schilling LM and Dellavalle RP Dealing with unanticipated mortality in a large randomized clinical trial of topical tretinoin. Arch Dermatol 2009 Jan; 145:76 PMID: 19153348
  8. Weinstock MA et al. Tretinoin and the prevention of keratinocyte carcinoma (basal and squamous cell carcinoma of the skin): A Veterans Affairs randomized chemoprevention trial. J Invest Dermatol 2012 Jun; 132:1583 PMID: 22318383
  9. Brooks M FDA Clears First Tretinoin Lotion for Acne (Altreno) Medscape - Aug 27, 2018. https://www.medscape.com/viewarticle/901240

Substructures

isoprene

Component-of

all trans retinoic acid/clindamycin all trans retinoic acid/clindamycin/phosphate all trans retinoic acid/fluocinolone/hydroquinone all trans retinoic acid/fluticasone/hydroquinone all trans retinoic acid/mequinol benzoyl peroxide/tretinoin (Benzashave) mequinol/tretinoin (Solage)