III. Definitions

  1. Retinoids
    1. Retinoids are Vitamin A derived compounds
    2. Retinoic Acid occurs naturally in humans and is involved in cell development and growth (esp. Embryo)

IV. Mechanism

  1. Comedolytic
  2. Antiinflammatory activity
  3. Decreases sebum production
  4. Lowers cohesiveness of follicular epithelial cells
    1. Decreases micro-comedo formation
  5. Increases follicular cell turnover and normalizes epithelial cell Desquamation
    1. Results in extrusion of existing comedones

V. Medications: Topical Tretinoin

  1. Standard preparations
    1. Retin A Cream 0.025% 0.05% 0.1%
      1. Cream 0.025% is as effective and less irritating than .05-.1%
      2. Lower concentration simply takes a little longer for improvement
    2. Retin A Gel 0.01%, 0.025% 0.005%
    3. Retin A Lotion 0.05% (Avoid - VERY irritating)
      1. Altreno (0.05% lotion)
        1. Released in 2019 as "hydrating" with Collagen and hyaluronic acid
        2. Contains fish Proteins (risk of Allergic Reaction)
        3. Expensive ($120/45 grams) and unlikely to be covered by insurance
        4. No evidence of benefit over generic options (e.g. Tretinoin, Adapalene)
        5. (2019) Presc Lett 26(3): 16
  2. Less irritating agents
    1. Retin-A Micro (Tretinoin gel microsphere)
    2. Avita (Tretinoin 0.025%)
  3. Combination agents
    1. Tretinoin 0.025% and Clindamycin 1.2% gel (Veltin, Ziana)
    2. Tretinoin 0.1% and Benzoyl Peroxide 3% cream (Twyneo)
      1. Formulated to prevent Benzoyl Peroxide from breaking down Tretinoin
      2. Applied once daily
      3. Available as a 30 g pump at $425 in 2022 (more than 10 fold the cost of the generic ingredients)
      4. (2022) Med Lett Drugs Ther 64(1650): 75 [PubMed]

VI. Medications: Other Retinoids

  1. Topical Retinoids
    1. Adapalene (Differin)
      1. Also available as combination with Benzoyl Peroxide (Epiduo)
    2. Tazarotene (Tazorac)
      1. More effective than either Adapalene or Tretinoin, but also more irritating
  2. Systemic Retinoids
    1. Isotretinoin (Accutane)
      1. Indicated in Severe Acne Vulgaris Management (Cystic Acne) and treatment resistant Acne Vulgaris
    2. Systemic Tretinoin (Vesanoid)
      1. Indicated in Acute Promyelocytic Leukemia
    3. Bexarotene (Targretin)
      1. Cutaneous T-Cell Lymphoma (refractory)

VII. Dosing: Directions for use

  1. Apply one dot (split-pea size) per one triangle of face (forehead, right malar, left malar)
    1. Typically applied at night to reduce daytime photosensitivity and irritation
  2. Initially apply only for a few hours
    1. Slowly increase length of treatment
    2. Titrate up to overnight application as tolerated
  3. Often used with Topical Antibiotics at spaced intervals (e.g. Benzoyl Peroxide, Clindamycin)
    1. Clindamycin also reduces irritating effect of Tretinoin
    2. Example schedule
      1. Morning: Clindamycin or Benzoyl Peroxide applied
      2. Evening: Tretinoin applied
  4. Avoid use at same time as Benzoyl Peroxide (aside from microspore Tretinoin preparation)
    1. Tretinoin when combined with benyzoyl peroxide, results in oxidation and Tretinoin degradation

VIII. Adverse Effects

  1. Scaling
  2. Skin dryness
  3. Local irritation, erythema or inflammation
    1. Creams irritate less than lotions
    2. Irritation can be reduced by adding Hydrocortisone
      1. 1 part Retin A 0.025%, 1 part Hydrocortisone 1%
  4. Local skin Sensation of burning or stinging
  5. Local Pruritus
  6. Photosensitivity
  7. Initially exacerbates inflammatory lesions

IX. Safety

  1. Pregnancy Category C

X. Efficacy

  1. Most potent Comedolytic
  2. Good results in 75% of patients in 3 months

Images: Related links to external sites (from Bing)

Related Studies

Cost: Medications

tretinoin (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
TRETINOIN 0.01% GEL Generic $3.53 per gram
TRETINOIN 0.025% CREAM Generic $1.24 per gram
TRETINOIN 0.025% GEL Generic $3.48 per gram
TRETINOIN 0.05% CREAM Generic $1.87 per gram
TRETINOIN 0.05% GEL Generic $4.26 per gram
TRETINOIN 0.1% CREAM Generic $2.53 per gram
TRETINOIN GEL MICRO 0.04% TUBE Generic $7.32 per gram
TRETINOIN GEL MICRO 0.1% TUBE Generic $8.85 per gram
retin-a (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
RETIN-A 0.01% GEL Generic $2.55 per gram
RETIN-A 0.025% CREAM Generic $1.24 per gram
RETIN-A 0.025% GEL Generic $3.25 per gram
RETIN-A 0.05% CREAM Generic $1.87 per gram
RETIN-A 0.1% CREAM Generic $2.62 per gram
altreno (on 8/17/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
ALTRENO 0.05% LOTION $2.45 per gram

Ontology: Retinoids (C0035339)

Definition (NCI_CRCH) Class of compounds consisting of four isoprenoid units joined in a head-to-tail manner and customarily containing five conjugated double bonds.
Definition (NCI_NCI-GLOSS) A nutrient that the body needs in small amounts to function and stay healthy. Retinoic acid is made in the body from vitamin A and helps cells to grow and develop, especially in the embryo. A form of retinoic acid made in the laboratory is put on the skin to treat conditions such as acne and is taken by mouth to treat acute promyelocytic leukemia (a fast-growing cancer in which there are too many immature blood-forming cells in the blood and bone marrow). Retinoic acid is being studied in the prevention and treatment of other types of cancer.
Definition (NCI) A group of agents that includes retinol (Vitamin A) and related compounds with potential antineoplastic and/or chemopreventive activities. A retinoic acid agent binds to and/or activates specific nuclear retinoic acid receptors (RARs) and retinoid X receptors (RXRs), thereby modulating transcription of genes responsible for cell differentiation and proliferation. A retinoic acid agent may exhibit immunomodulatory and anti-inflammatory properties and may inhibit ornithine decarboxylase, resulting in a decrease in polyamine synthesis and keratinization. (NCI04)
Definition (MSH) A group of tetraterpenes, with four terpene units joined head-to-tail. Biologically active members of this class are used clinically in the treatment of severe cystic ACNE; PSORIASIS; and other disorders of keratinization.
Definition (CSP) retinol and its derivatives; C(20) polyunsaturated, cyclic, lipid soluble alcohol; deficiency results in night blindness and certain epithelial disorders.
Concepts Pharmacologic Substance (T121) , Biologically Active Substance (T123) , Organic Chemical (T109)
MSH D012176
SnomedCT 116085009, 372579009
Swedish Retinoider
Czech retinoidy
Finnish Retinoidit
Russian RETINOIDY, РЕТИНОИДЫ
English retinoids (medication), retinoids, Retinoids, Retinoids [Chemical/Ingredient], retinoid, RA - Retinoic acid product, Retinoid product, Retinoid (product), Retinoid (substance), Retinoid, Retinoic Acid Agent, Retinoic Acid and Derivatives, Retinoic Acids, Dermatological Retinoids
Japanese レチノイド
Croatian Not Translated[Retinoids]
Polish Retinoidy
Norwegian Not Translated[Retinoids]
Portuguese Retinoides
Spanish retinoide (producto), retinoide (sustancia), retinoide, Retinoides
French Rétinoïdes
German Retinoide
Italian Retinoidi

Ontology: Tretinoin (C0040845)

Definition (CHV) a drug used to treat acne
Definition (CHV) a drug used to treat acne
Definition (CHV) a drug used to treat acne
Definition (CHV) a drug used to treat acne
Definition (CHV) a drug used to treat acne
Definition (NCI_NCI-GLOSS) A nutrient that that body needs in small amounts to function and stay healthy. All-trans retinoic acid is made in the body from vitamin A and helps cells to grow and develop, especially in the embryo. A form of all-trans retinoic acid made in the laboratory is put on the skin to treat conditions such as acne and is taken by mouth to treat acute promyelocytic leukemia (a fast-growing cancer in which there are too many immature blood-forming cells in the blood and bone marrow). All-trans retinoic acid is being studied in the prevention and treatment of other types of cancer.
Definition (NCI) A naturally-occurring acid of retinol. Tretinoin binds to and activates retinoic acid receptors (RARs), thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, and inhibition of tumorigenesis. This agent also inhibits telomerase, resulting in telomere shortening and eventual apoptosis of some tumor cell types. The oral form of tretinoin has teratogenic and embryotoxic properties.
Definition (NCI_CRCH) Retinoid with a carboxylic acid group.
Definition (MSH) An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).
Definition (PDQ) A naturally-occurring acid of retinol. Tretinoin binds to and activates retinoic acid receptors (RARs), thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, and inhibition of tumorigenesis. This agent also inhibits telomerase, resulting in telomere shortening and eventual apoptosis of some tumor cell types. The oral form of tretinoin has teratogenic and embryotoxic properties. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41258&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41258&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C900" NCI Thesaurus)
Concepts Vitamin (T127) , Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D014212
SnomedCT 332319008, 327389004, 387305002, 54972005
English Acid, Retinoic, Acid, trans-Retinoic, Acid, Vitamin A, Retinoic Acid, trans Retinoic Acid, trans-Retinoic Acid, Vitamin A Acid, Acid, all-trans-Retinoic, all trans Retinoic Acid, all-trans-Retinoic Acid, (All-E)-3,7-Dimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraenoic Acid, tretinoin, All-trans Vitamin A Acid, Trans Vitamin A Acid, All-trans Retinoic Acid, Trans Retinoic Acid, Tretinoinum, beta-Retinoic Acid, Tretinoin [cytostatic], Tretinoin [skin], tretinoin (medication), retinoids tretinoin, TRETINOIN, Tretinoin [Chemical/Ingredient], all trans retinoic acid, all-trans-retinoic acid, vitamin a acid, Tretinoin [skin] (product), Tretinoin [cytostatic] (product), trans-Retinoic acid, all trans-Retinoic acid, vitamin A acid, Vitamin A acid, all-trans-, all-trans-Vitamin A acid, ATRA, retinoic acid, all-trans-Retinoic acid, all-trans retinoic acid, 3,7-dimethyl-9-(2,6,6-trimethylcyclohexen-1-yl)-2,4,6,8-nonatetraenoic acid, 2,4,6,8-Nonatetraenoic acid, 3, 7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-, (all-E)-, Retinoic acid, Vitamin A acid, Tretinoin (product), Tretinoin (substance), TRA, Tretinoin [cytostatic] (substance), Tretinoin [skin] (substance), Tretinoin
German Trans-Retinsäure, All-trans-Retinsäure, Tretinoin, Retinsäure, Vitamin-A-Säure
Swedish Tretinoin
Czech tretinoin, kyselina retinová
Finnish Tretinoiini
Russian TRETINOIN, RETINOEVAIA KISLOTA, VITAMIN A-KISLOTA, ВИТАМИН A-КИСЛОТА, РЕТИНОЕВАЯ КИСЛОТА, ТРЕТИНОИН
Japanese トレチノイン, ベサノイド, ビタミンA酸, レチノイン酸
French Vitamine A acide, Acide tout trans rétinoïque, Acide rétinoïque tout trans, Trétinoïne
Italian Acido trans-retinoico, Acido tutto-trans-retinoico, Acido retinoico, Tretinoina
Croatian TRETINOIN
Polish Kwas retynowy, Tretynoina
Portuguese Ácido Retinoico, Ácido da Vitamina A, Tretinoína
Spanish tretinoína (citostático), tretinoína (citostático) (producto), tretinoína (uso dermatológico), tretinoína (uso dermatológico) (producto), tretinoína (piel) (producto), tretinoína (piel), tretinoína (producto), tretinoína (sustancia), tretinoína, ácido de vitamina A, ácido retinoico, Tretinoina, Ácido Retinoico, Ácido de Vitamina A

Ontology: Retin-A (C0593762)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D014212
English Retin A, retin-a, retin a, retin, a retin, Retin-A-Micro, Retin-A
German Retin-A