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Identification
- Summary
Triamcinolone is a glucocorticoid used to treat a wide variety of inflammatory conditions of organ systems and tissues.
- Brand Names
- Allernaze, Aristocort, Aristocort R, Juulissa Pharmapak, Kenalog, Kourzeq, Marcaine, Nasacort, Oracort, Oralone, Pediaderm Ta, Triaderm, Trianex, Triderm, Triesence, Triloan Suik, Tritocin, Viaderm Kc, Xipere, Zilretta
- Generic Name
- Triamcinolone
- DrugBank Accession Number
- DB00620
- Background
Triamcinolone is a corticosteroid used to treat various inflammatory conditions in the body from allergic rhinitis to acute exacerbations of multiple sclerosis.13 Triamcinolone can be used as a one time adjunct treatment of osteoarthritic knee pain,16 or first line as a topical treatment of corticosteroid responsive dermatoses.11 Triamcinolone is more commonly seen in the forms triamcinolone hexacetonide, triamcinolone acetonide, and triamcinolone diacetate.10,11,12,13,14,15,16
Triamcinolone was granted FDA approval on 3 December 1957.9 In October 2021, a suspension of triamcinolone acetonide was approved for suprachoroidal injection - the first suprachoroidal injection to receive FDA approval19 - for the treatment of patients with macular edema associated with uveitis.18
- Type
- Small Molecule
- Groups
- Approved, Vet approved
- Structure
Structure for Triamcinolone (DB00620)
- Weight
- Average: 394.4339
Monoisotopic: 394.179166801 - Chemical Formula
- C21H27FO6
- Synonyms
- 11β,16α,17α,21-tetrahydroxy-9α-fluoro-1,4-pregnadiene-3,20-dione
- 9-fluoro-11β,16α,17,21-tetrahydroxypregna-1,4-diene-3,20-dione
- 9α-fluoro-11β,16α,17,21-tetrahydroxypregna-1,4-diene-3,20-dione
- 9α-fluoro-11β,16α,17α,21-tetrahydroxypregna-1,4-diene-3,20-dione
- 9α-fluoro-16α-hydroxyprednisolone
- Fluoxyprednisolone
- Tiamcinolonum
- Triamcinolona
- Triamcinolone
- Triamcinolonum
Pharmacology
- Indication
Triamcinolone hexacetonide injections are indicated for intralesional administration in alopecia areata, discoid lupus erythematosus, keloids, and necrobiosis lipoidica diabeticorum.10 This formulation can also be used for localized hypertrophic infiltrated inflammatory lesions of granuloma annulare, lichen planus, lichen simplex chronicus, and psoriatic plaques.10
Triamcinolone acetonide spray and cream are indicated for the treatment of inflammatory and pruritic manifestations of corticosteroid responsive dermatoses.11,14 A triamcinolone acetonide 10mg/mL or 40mg/mL injection is indicated intra-articularly for acute gouty arthritis, acute and subacute bursitis, acute nonspecific tenosynovitis, epicondylitis, rheumatoid arthritis, and synovitis of osteoarthritis.12,13 The same 10mg/mL injection is indicated by the intralesional route for the treatment of alopecia areata, discoid lupus erythematosus, keloids, necrobiosis lipoidica diabeticorum, and tumors of an aponeurosis or tendon.12 This formulation can also be used for localized hypertrophic infiltrated inflammatory lesions of granuloma annulare, lichen planus, lichen simplex chronicus, and psoriatic plaques.12 The 40mg/mL injection is indicated intramuscularly for controlling severe allergic conditions such as asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity, perennial or seasonal allergic rhinitis, serum sickness, and transfusion reactions; treatment of bullous dermatitis herpetiformis, exfoliative erythroderma, mycosis fungoides, pemphigus, Stevens-Johnson syndrome, congenital adrenal hyperplasia, hypercalcemia in cancer, nonsuppurative thyroiditis, autoimmune hemolytic anemia, Diamond-Blackfan anemia, pure red cell aplasia, secondary thrombocytopenia, trichinosis, tuberculous meningitis, acute exacerbations of multiple sclerosis or cerebral edema, sympathetic ophthalmia, temporal arteritis, uveitis, ocular inflammation, berylliosis, idiopathic eosinophilic pneumonias, symptomatic sarcoidosis, dermatomyositis, polymyositis, and systemic lupus erythematosus; adjunct treatment of adrenocortical insufficiency, regional enteritis, ulcerative colitis, fulminating or disseminated pulmonary tuberculosis, acute gouty arthritis, acute rheumatic carditis, ankylosing spondylitis, psoriatic arthritis, rheumatoid arthritis; palliative management of leukemia and lymphoma; induction of diuresis or remission of proteinuria in idiopathic nephrotic syndrome or lupus erythematosus.13 A triamcinolone intravitreal injection is indicated for the treatment of sympathetic ophthalmia, temporal arteritis, uveitis, and ocular inflammatory conditions.15 The intravitreal injection is also used for visualization during vitrectomy.15 An extended release suspension is indicated intra-articularly for management of pain in osteoarthritis of the knee.16
A triamcinolone acetonide suspension for injection into the suprachoroidal space is indicated for the treatment of macular edema associated with uveitis.18
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Acne Combination Product in combination with: Kanamycin (DB01172) •••••••••••• •••••••• Treatment of Acne vulgaris ••• ••••• ••••••••• Adjunct therapy in management of Acute gouty arthritis •••••••••••• ••••••••• Symptomatic treatment of Acute gouty arthritis •••••••••••• ••••••••• Used in combination to treat Allergic contact dermatitis Combination Product in combination with: Salicylic acid (DB00936) •••••••••••• •••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Triamcinolone is a corticosteroid with anti-inflammatory properties.8 These properties are used to treat inflammation in conditions that affect various organs and tissues.15 Triamcinolone should not be administered as an epidural injection.10,12,13,15,16
- Mechanism of action
Corticosteroids like triamcinolone inhibit phospholipase A2 on cell membranes, preventing the breakdown of lysosomal membranes of leukocytes, which in turn prevent the formation of arachidonic acid, which decrease expression of cyclooxygenase and lipoxygenase, inhibiting synthesis of prostaglandins and leukotrienes.8 Anti-inflammatory activity occurs via reversal of vascular dilation and reducing permeability, which prevents macrophage and leukocyte migration.8 Triamcinolone also inhibits nuclear factor kappa-B, which decreases the production of pro-inflammatory signals such as interleukin-6, interleukin-8, and monocyte chemoattractant protein-1.8
Target Actions Organism AGlucocorticoid receptor agonistHumans - Absorption
A 16mg oral dose of triamcinolone reaches a Cmax of 5.23±0.84ng/mL with a Tmax of 2.24±0.78h and an AUC of 36.0±6.2ng*h/mL.4
A 2mg intravenous dose of triamcinolone acetonide has an AUC of 57.7ng*h/mL.3 The bioavailability of 800µg of inhaled triamcinolone acetonide is 25%, with 10.4% coming from pulmonary absorption and the rest being accounted for by deposition on the oral mucosa and other underlying factors.2 An inhaled dose of triamcinolone acetonide reaches a Cmax of 0.92ng/mL with a Tmax of 1.74h and an AUC of 5.12ng*h/mL.2 The fraction of an inhaled dose that is actually absorbed via the pulmonary route reaches a Cmax of 0.55ng/mL with a Tmax of 0.66h and an AUC of 2.15ng*h/mL.2
A 16mg oral dose of triamcinolone diacetate reaches a Cmax of 5.33±1.55ng/mL with a Tmax of 1.86±0.47h and an AUC of 32.7±9.9ng*h/mL.4
- Volume of distribution
The apparent volume of distribution of triamcinolone is 115.2±10L.4 The mean apparent volume of distribution of triamcinolone acetonide is 1.96L/kg.2 The apparent volume of distribution of triamcinolone diacetate is 119.7±33.14L.4
- Protein binding
Triamcinolone is mostly bound to corticosteroid-binding globulin or serum albumin.5 Triamcinolone acetonide is approximately 68% protein bound in plasma.7
- Metabolism
The major metabolite of triamcinolone is 6-beta-hydroxy-triamcinolone.1 Data regarding the metabolism of triamcinolone is not readily available.10,11,12,13,14,15,16,17
Hover over products below to view reaction partners
- Route of elimination
Approximately 20% of a dose of triamcinolone is recovered in the urine as the unchanged drug, 25% is recovered as 6-beta-hydroxy-triamcinolone, and 5% is recovered as unidentified metabolites.1
- Half-life
The half life of triamcinolone is 2.7h.4 The mean terminal elimination half life following an inhaled dose of triamcinolone acetonide is 2.4h.2 The half life of triamcinolone diacetate is 2.8h.4
- Clearance
The clearance of triamcinolone is 28.6±5.6L/h.4 The mean total body clearance of triamcinolone acetonide is 0.57L/h.2 The clearance of triamcinolone diacetate is 34.4±10.6L/h.4
- Adverse Effects
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The subcutaneous LD50 of triamcinolone acetonide in rats is 13,100µg/kg and in mice is 132mg/kg.17 The oral LD50 in rats is 1451mg/kg and in mice is 2168mg/kg.[LD50] The intraperitoneal LD50 in mice is 105mg/kg.[LD50]
Patients experiencing an overdose may develop Cushing's syndrome.6 This overdose may be treated with supportive therapy and mifepristone for its antiglucocorticoid activity.6
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Triamcinolone can be increased when it is combined with Abametapir. Abatacept The metabolism of Triamcinolone can be increased when combined with Abatacept. Abciximab The therapeutic efficacy of Abciximab can be decreased when used in combination with Triamcinolone. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Triamcinolone. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Triamcinolone. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Triamcinolone acetonide F446C597KA 76-25-5 YNDXUCZADRHECN-JNQJZLCISA-N Triamcinolone diacetate A73MM2Q32P 67-78-7 XGMPVBXKDAHORN-RBWIMXSLSA-N Triamcinolone hexacetonide I7GT1U99Y9 5611-51-8 TZIZWYVVGLXXFV-FLRHRWPCSA-N - Product Images
- International/Other Brands
- Delphicort / Flutex / Kenacort / Omcilon-A / Oracort / Tri-Nasal / Triacet / Triacort / Triaderm / Tricortone / Trilone / Tristoject
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image AllerNaze Spray, metered 0.5 mg/1mL Nasal Lupin Pharmaceuticals 2011-02-01 Not applicable US 
Aristocort Injection, suspension 40 mg/1mL Intra-articular; Intralesional; Intramuscular; Intrasynovial; Parenteral Sandoz 1961-09-05 1961-09-05 US Aristocort Injection, suspension 40 mg/1mL Intra-articular; Intralesional; Intramuscular; Intrasynovial; Parenteral Physicians Total Care, Inc. 1961-09-05 2005-07-28 US Aristocort - Syr Orl 0.4mg/ml Syrup .4 mg / mL Oral Glades, Division Of Stiefel Canada Inc. 1996-10-10 1997-08-05 Canada 
Aristocort - Tab 4mg Tablet 4 mg Oral Glades, Division Of Stiefel Canada Inc. 1998-05-11 2004-01-27 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-triamcinolone AQ Spray, metered 55 mcg / act Nasal Apotex Corporation 2016-06-15 Not applicable Canada DermacinRx Silazone Pak Cream; Kit 1 mg/1g Topical PureTek Corporation 2015-12-10 2018-08-15 US DermacinRx Trizapak Kit 1 mg/1g Topical Pure Tek Corporation 2016-08-02 2017-08-17 US Dermasorb TA Complete Kit Kit 1 mg/1g Topical Crown Laboratories 2013-11-14 2019-08-30 US Dermazone Cream; Kit 1 mg/1g Topical Shoreline Pharmaceuticals, Inc. 2016-04-20 2018-08-15 US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image 24 Hour Nasal Allergy Spray, metered 55 ug/1 Nasal Meijer Distribution Inc 2017-01-18 Not applicable US 24 Hour Nasal Allergy Spray, metered 55 ug/1 Nasal Kroger Company 2016-04-10 Not applicable US Allergy Nasal Spray, metered 55 ug/1 Nasal Walgreen Company 2016-04-10 Not applicable US Basic Care Nasal Allergy Spray, metered 55 ug/1 Nasal L. Perrigo Company 2018-04-25 Not applicable US Basic Care Nasal Allergy Spray, metered 55 ug/1 Nasal Amazon.com Services LLC 2021-07-26 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image AECORAS OINTMENT Triamcinolone acetonide (0.1 %) + Econazole nitrate (1 %) Ointment Topical DUOPHARMA (M) SDN. BHD. 2020-09-08 2022-02-08 Malaysia 
AFTOJEL % 0,1 + %3 JEL (5 G) Triamcinolone acetonide (1 mg/g) + Diclofenac sodium (30 mg/g) Gel Topical ORVA İLAÇ SAN. VE TİC. A.Ş. 2008-04-30 Not applicable Turkey 
Aristoform R Crm 0.1% Triamcinolone acetonide (1 mg / g) + Clioquinol (30 mg / g) Cream Topical Lederle Cyanamid Canada Inc. 1966-12-31 1997-01-29 Canada Aureocort 1 mg/g + 30 mg/g Salbe Triamcinolone acetonide (1 mg/g) + Chlortetracycline hydrochloride (30 mg/g) Ointment Topical Dermapharm Gmb H 1966-09-28 Not applicable Austria 
Bt Triamcinolone acetonide (40 mg/1mL) + Bupivacaine hydrochloride (5 mg/1mL) + Isopropyl alcohol (0.7 mL/1) + Povidone-iodine (0.10 g/1) Cloth; Injection, solution; Kit; Solution Epidural; Infiltration; Intra-articular; Intramuscular; Topical Sa3, Llc 2015-07-01 2017-12-01 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image BLT-25 Kit Triamcinolone acetonide (40 mg/1mL) + Bupivacaine hydrochloride (2.5 mg/1mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL) Kit Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Perineural; Topical Asclemed Usa, Inc. 2024-09-11 Not applicable US Bupivilog Kit Triamcinolone acetonide (40 mg/1mL) + Bupivacaine hydrochloride (5 mg/1mL) + Povidone-iodine (10 mg/1mL) Kit Epidural; Intra-articular; Intramuscular; Topical Asclemed Usa, Inc. 2014-02-04 Not applicable US Bupivilog Kit Triamcinolone acetonide (40 mg/1mL) + Bupivacaine hydrochloride (5 mg/1mL) + Povidone-iodine (10 mg/1mL) Kit Epidural; Intra-articular; Intramuscular; Topical Advanced Rx Pharmacy of Tennessee, LLC 2023-07-31 Not applicable US Calcipotriene 0.005% / Triamcinolone Acetonide 0.1% Triamcinolone acetonide (0.1 g/100g) + Calcipotriol (0.005 g/100g) Ointment Topical Sincerus Florida, LLC 2019-05-11 Not applicable US Ellzia Pak Triamcinolone acetonide (1 mg/1g) + Dimethicone (50 mg/1mL) Kit Topical PureTek Corporation 2016-12-29 Not applicable US
Categories
- ATC Codes
- D07AB09 — Triamcinolone
- D07AB — Corticosteroids, moderately potent (group II)
- D07A — CORTICOSTEROIDS, PLAIN
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- R01AD — Corticosteroids
- R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- R03BA — Glucocorticoids
- R03B — OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- D07BB — Corticosteroids, moderately potent, combinations with antiseptics
- D07B — CORTICOSTEROIDS, COMBINATIONS WITH ANTISEPTICS
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- A01AC — Corticosteroids for local oral treatment
- A01A — STOMATOLOGICAL PREPARATIONS
- A01 — STOMATOLOGICAL PREPARATIONS
- A — ALIMENTARY TRACT AND METABOLISM
- H02AB — Glucocorticoids
- H02A — CORTICOSTEROIDS FOR SYSTEMIC USE, PLAIN
- H02 — CORTICOSTEROIDS FOR SYSTEMIC USE
- H — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
- D07CB — Corticosteroids, moderately potent, combinations with antibiotics
- D07C — CORTICOSTEROIDS, COMBINATIONS WITH ANTIBIOTICS
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- S01BA — Corticosteroids, plain
- S01B — ANTIINFLAMMATORY AGENTS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- D07XB — Corticosteroids, moderately potent, other combinations
- D07X — CORTICOSTEROIDS, OTHER COMBINATIONS
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- S02CA — Corticosteroids and antiinfectives in combination
- S02C — CORTICOSTEROIDS AND ANTIINFECTIVES IN COMBINATION
- S02 — OTOLOGICALS
- S — SENSORY ORGANS
- Drug Categories
- Adrenal Cortex Hormones
- Adrenals
- Agents Causing Muscle Toxicity
- Agents to Treat Airway Disease
- Alimentary Tract and Metabolism
- Anti-Inflammatory Agents
- Corticosteroid Hormone Receptor Agonists
- Corticosteroids
- Corticosteroids for Local Oral Treatment
- Corticosteroids for Systemic Use
- Corticosteroids for Systemic Use, Plain
- Corticosteroids, Dermatological Preparations
- Corticosteroids, Moderately Potent (Group II)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inducers
- Cytochrome P-450 CYP3A5 Inducers (strength unknown)
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Inducers
- Cytochrome P-450 CYP3A7 Inducers (strength unknown)
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Dermatologicals
- Drugs for Obstructive Airway Diseases
- Enzyme Inhibitors
- Fused-Ring Compounds
- Glucocorticoids
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hyperglycemia-Associated Agents
- Immunologic Factors
- Immunosuppressive Agents
- Nasal Preparations
- Ophthalmologicals
- Pregnadienes
- Pregnanes
- Protein-Lysine 6-Oxidase, antagonists & inhibitors
- Sensory Organs
- Steroids
- Steroids, Fluorinated
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- Thyroxine-binding globulin inhibitors
- Vasoprotectives
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Hydroxysteroids
- Direct Parent
- 21-hydroxysteroids
- Alternative Parents
- Gluco/mineralocorticoids, progestogins and derivatives / 20-oxosteroids / 11-beta-hydroxysteroids / 16-alpha-hydroxysteroids / 17-hydroxysteroids / Halogenated steroids / 3-oxo delta-1,4-steroids / Delta-1,4-steroids / Tertiary alcohols / Alpha-hydroxy ketones show 10 more
- Substituents
- 11-beta-hydroxysteroid / 11-hydroxysteroid / 16-alpha-hydroxysteroid / 16-hydroxysteroid / 17-hydroxysteroid / 20-oxosteroid / 21-hydroxysteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / 9-halo-steroid show 26 more
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- 11beta-hydroxy steroid, 17alpha-hydroxy steroid, glucocorticoid, 3-oxo Delta(4)-steroid, 20-oxo steroid, fluorinated steroid, 16alpha-hydroxy steroid, 21-hydroxy steroid, C21-steroid hormone (CHEBI:9667)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 1ZK20VI6TY
- CAS number
- 124-94-7
- InChI Key
- GFNANZIMVAIWHM-OBYCQNJPSA-N
- InChI
- InChI=1S/C21H27FO6/c1-18-6-5-12(24)7-11(18)3-4-13-14-8-15(25)21(28,17(27)10-23)19(14,2)9-16(26)20(13,18)22/h5-7,13-16,23,25-26,28H,3-4,8-10H2,1-2H3/t13-,14-,15+,16-,18-,19-,20-,21-/m0/s1
- IUPAC Name
- (1S,2R,3aS,3bS,9aS,9bR,10S,11aS)-9b-fluoro-1,2,10-trihydroxy-1-(2-hydroxyacetyl)-9a,11a-dimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one
- SMILES
- [H][C@@]12C[C@@H](O)[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
References
- Synthesis Reference
Abu Alam, "Triamcinolone formulations and methods for their preparation and use." U.S. Patent US20040186084, issued September 23, 2004.
US20040186084- General References
- FLORINI JR, SMITH LL, BUYSKE DA: Metabolic fate of a synthetic corticosteroid (triamcinolone) in the dog. J Biol Chem. 1961 Apr;236:1038-42. [Article]
- Argenti D, Shah B, Heald D: A pharmacokinetic study to evaluate the absolute bioavailability of triamcinolone acetonide following inhalation administration. J Clin Pharmacol. 1999 Jul;39(7):695-702. doi: 10.1177/00912709922008335. [Article]
- Derendorf H, Hochhaus G, Rohatagi S, Mollmann H, Barth J, Sourgens H, Erdmann M: Pharmacokinetics of triamcinolone acetonide after intravenous, oral, and inhaled administration. J Clin Pharmacol. 1995 Mar;35(3):302-5. doi: 10.1002/j.1552-4604.1995.tb04064.x. [Article]
- Hochhaus G, Portner M, Barth J, Mollmann H, Rohdewald P: Oral bioavailability of triamcinolone tablets and a triamcinolone diacetate suspension. Pharm Res. 1990 May;7(5):558-60. doi: 10.1023/a:1015889305157. [Article]
- FLORINI JR, BUYSKE DA: Plasma protein binding of triamcinolone-H3 and hydrocortisone-4-C14. J Biol Chem. 1961 Jan;236:247-51. [Article]
- Schweitzer DH, Le-Brun PP, Krishnaswami S, Derendorf H: Clinical and pharmacological aspects of accidental triamcinolone acetonide overdosage: a case study. Neth J Med. 2000 Jan;56(1):12-6. [Article]
- Argenti D, Jensen BK, Hensel R, Bordeaux K, Schleimer R, Bickel C, Heald D: A mass balance study to evaluate the biotransformation and excretion of [14C]-triamcinolone acetonide following oral administration. J Clin Pharmacol. 2000 Jul;40(7):770-80. doi: 10.1177/00912700022009413. [Article]
- Sidhu G, Preuss CV: Triamcinolone . [Article]
- FDA Approved Drug Products: Aristocort Triamcinolone Oral Tablets (Discontinued) [Link]
- FDA Approved Drug Products: Triamcinolone Hexacetonide Injection [Link]
- FDA Approved Drug Products: Triamcinolone Acetonide Topical Spray [Link]
- FDA Approved Drug Products: Triamcinolone Acetonide 10mg/mL Injection [Link]
- FDA Approved Drug Products: Triamcinolone Acetonide 40mg/mL Injection [Link]
- FDA Approved Drug Products: Triamcinolone Acetonide Topical Cream [Link]
- FDA Approved Drug Products: Triamcinolone Acetonide Intravitreal Injection [Link]
- FDA Approved Drug Products: Triamcinolone Acetonide Intraarticular Extended Release Suspension [Link]
- Cayman Chemicals: Triamcinolone Acetonide MSDS [Link]
- FDA Approved Drug Products: Xipere (triamcinolone acetonide) suspension for suprachoroidal injection [Link]
- PR Newswire: Bausch + Lomb and Clearside Biomedical Announce FDA Approval of XIPERE™ (triamcinolone acetonide injectable suspension) for Suprachoroidal Use for the Treatment of Macular Edema Associated with Uveitis [Link]
- External Links
- Human Metabolome Database
- HMDB0014758
- KEGG Drug
- D00385
- PubChem Compound
- 31307
- PubChem Substance
- 46507950
- ChemSpider
- 29046
- BindingDB
- 41132
- 10759
- ChEBI
- 9667
- ChEMBL
- CHEMBL1451
- ZINC
- ZINC000003882036
- Therapeutic Targets Database
- DAP000417
- PharmGKB
- PA451749
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Triamcinolone
- FDA label
- Download (150 KB)
- MSDS
- Download (72.6 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Prevention Oral Lichen Planus 1 somestatus stop reason just information to hide Not Available Completed Not Available Anterior Uveitis (AU) / Panuveitis / Posterior Uveitis / Uveitis / Uveitis, Intermediate 1 somestatus stop reason just information to hide Not Available Completed Not Available Asthma / Severe Persistent Asthma 1 somestatus stop reason just information to hide Not Available Completed Not Available Atopic Dermatitis 1 somestatus stop reason just information to hide Not Available Completed Not Available Diabetes / Osteoarthritis of the Knee 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Astellas pharma us inc
- Bristol myers squibb co
- Barr laboratories inc
- Impax laboratories inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Mylan pharmaceuticals inc
- Purepac pharmaceutical co
- Roxane laboratories inc
- Sandoz inc
- Teva pharmaceuticals usa inc
- Watson laboratories inc
- Abbott laboratories
- Sanofi aventis us llc
- Ivax pharmaceuticals inc
- Apothecon inc div bristol myers squibb
- Solvay pharmaceuticals
- Actavis mid atlantic llc
- Alpharma us pharmaceuticals division
- Altana inc
- Ambix laboratories div organics corp america
- G and w laboratories inc
- Morton grove pharmaceuticals inc
- Perrigo new york inc
- Pharmaderm div altana inc
- Pharmafair inc
- Taro pharmaceuticals inc
- Taro pharmaceuticals usa inc
- Topiderm inc
- Vintage pharmaceuticals llc
- Del ray laboratories inc
- Savage laboratories inc div altana inc
- Parnell pharmaceuticals inc
- Sandoz canada inc
- Allergan inc
- Alcon inc
- Bristol myers squibb co pharmaceutical research institute
- Wockhardt eu operations (swiss) ag
- Carolina medical products co
- Lyne laboratories inc
- Lupin atlantis holding sa switzerland
- Ranbaxy laboratories inc
- Akorn inc
- Packagers
- AAIPharma Inc.
- Abbott Laboratories Ltd.
- Actavis Group
- Advanced Pharmaceutical Services Inc.
- Aidarex Pharmacuticals LLC
- Alcon Laboratories
- Armstrong Pharmaceuticals Inc.
- A-S Medication Solutions LLC
- Blansett Pharmacal Co. Inc.
- Bristol-Myers Squibb Co.
- C.O. Truxton Inc.
- Carlisle Laboratories Inc.
- Carolina Medical Products Co.
- Clint Pharmaceutical Inc.
- Crown Laboratories Inc.
- Darby Dental Supply Co. Inc.
- Del Ray Dermatology
- Dept Health Central Pharmacy
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- E. Fougera and Co.
- E.R. Squibb and Sons LLC
- G & W Labs
- Generics Puerto Rico Inc.
- Genesis Pharmaceutical Inc.
- Goldline Laboratories Inc.
- Group Health Cooperative
- H.J. Harkins Co. Inc.
- Hl Moore Drug Exchange
- Ide Interstate
- Innoviant Pharmacy Inc.
- Inyx Usa Ltd.
- Keene Pharmaceuticals Inc.
- Lake Erie Medical and Surgical Supply
- Major Pharmaceuticals
- Martica Enterprises Inc.
- Martin Surgical Supply
- Medisca Inc.
- Medvantx Inc.
- Mericon
- Merit Pharmaceuticals
- National Pharmaceuticals
- Nycomed Inc.
- Paddock Labs
- Palmetto Pharmaceuticals Inc.
- Parnell Pharmaceuticals Inc.
- Perrigo Co.
- Pharmedix
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Primedics Laboratories
- Princeton Pharmaceutical Products Inc.
- Qualitest
- Ranbaxy Laboratories
- Rebel Distributors Corp.
- Robar Inc.
- San Jose Surgical Supply Inc.
- Sandoz
- Sanofi-Aventis Inc.
- Savage Labs
- Stat Rx Usa
- Suppositoria Laboratories Inc.
- Taro Pharmaceuticals USA
- Topiderm Inc.
- Vintage Pharmaceuticals Inc.
- Watson Pharmaceuticals
- Wockhardt Ltd.
- X-Gen Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet Oral 0025 MG Tablet, multilayer Buccal 25 mcg Spray, metered Nasal 0.5 mg/1mL Injection Injection, suspension Intra-articular; Intralesional; Intramuscular; Intrasynovial; Parenteral 40 mg/1mL Syrup Oral .4 mg / mL Cream Topical 0.5 % w/w Cream Topical 5 mg / g Cream Topical .025 % Cream Topical .25 mg / g Liquid Intra-articular; Intramuscular; Intrasynovial 40 mg / mL Liquid Intra-articular; Intradermal; Intramuscular 25 mg / mL Cream Topical 0.1 % w/w Ointment Topical 0.1 % w/w Cream Topical 1 mg / g Ointment Topical .1 % Syrup Oral 2 mg / 5 mL Tablet Oral 2 mg Injection, suspension Intra-articular; Parenteral 20 mg/1mL Injection, suspension Intralesional; Parenteral 5 mg/1mL Suspension Intra-articular 20 mg / mL Injection, suspension Intra-articular 20 mg/ml Injection, suspension Intra-articular 5 mg/ml Kit Intra-articular; Intramuscular 40 mg/1mL Cream Aerosol, metered Respiratory (inhalation) 200 mcg / act Aerosol, metered Respiratory (inhalation) 75 ug/1 Cream 0.100 g Kit Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Perineural; Topical Cloth; injection, solution; kit; solution Epidural; Infiltration; Intra-articular; Intramuscular; Topical Kit Epidural; Intra-articular; Intramuscular; Topical Injection, solution; injection, suspension; kit Epidural; Intra-articular; Intracaudal; Intramuscular; Intravenous; Perineural; Topical Suspension Intra-articular; Intramuscular 40 mg Cream; injection, suspension; kit Intra-articular; Intramuscular; Topical Kit Topical 1 mg/1g Capsule Oral Cream Topical 10 mg/g Injection 10 mg/ml Injection 40 mg/ml Injection, solution Injection, suspension Intra-articular 40 mg/2mL Emulsion Topical Kit Infiltration; Intra-articular; Intramuscular; Respiratory (inhalation); Topical Suspension Intra-articular 20 mg Inhalant; injection, solution; injection, suspension; kit; solution Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Perineural; Respiratory (inhalation); Topical Kit Intra-articular; Intralesional Kit Intra-articular; Intramuscular Paste Oral 0.1 % Injection, solution Intra-articular; Intradermal 40 mg/mL Injection, suspension Intra-articular; Intramuscular 40 mg Injection, suspension Parenteral 40 MG/ML Suspension Intra-articular; Intradermal 10 mg Ointment Injection Intra-articular; Intramuscular 40 mg Ointment Oral 0.1 % Aerosol, spray Topical 0.147 mg/1g Lotion Topical 0.25 mg/1mL Ointment Topical 5 mg/1g Paste, dentifrice Dental 1 mg/1g Paste Dental 1 mg / g Ointment Topical 1 mg / g Injection, suspension Intra-articular; Intralesional 10 mg/1mL Suspension Intra-articular; Intrabursal; Intradermal; Intrasynovial 10 mg / mL Injection, suspension Intra-articular; Intramuscular 40 mg/1mL Injection, suspension Intramuscular 40 mg/1mL Suspension Intra-articular; Intramuscular 40 mg / mL Injection, suspension Intra-articular; Intramuscular 80 mg/1mL Paste Oral 1 mg/g Suspension Ophthalmic 2.00 mg Cream Topical 1 mg/g Tablet Oral Paste Dental Kit Epidural; Infiltration; Intra-articular; Intramuscular; Topical Kit Epidural; Infiltration; Intra-articular; Intramuscular Injection, solution; injection, suspension; kit; solution; swab Epidural; Infiltration; Intra-articular; Intramuscular; Intrathecal; Intravascular; Intravenous; Perineural; Topical Liquid Buccal Spray Nasal 0.055 % Implant Subcutaneous Aerosol, metered Nasal 100 mcg / dose Aerosol, metered Nasal 55 ug/1 Spray Nasal 0.055 mg Spray, suspension Nasal 55 MCG Spray Nasal 55 UG Spray, metered Nasal 55 mcg / act Suspension Nasal 56.100 mg Spray Nasal 55 microgram Spray Nasal 55 mcg Spray, metered Nasal 55 mcg / dose Spray, metered Nasal 55 mcg Cream Topical Ointment Topical Injection, solution; injection, suspension; kit Infiltration; Intra-articular; Intramuscular; Perineural; Topical Paste Dental 0.1 % Paste Submucosal 3 % w/w Lotion Topical 0.5 % w/v Ointment Buccal 1 mg/1g Paste Submucosal 1 mg/g Ointment Auricular (otic) Paste Submucosal 0.1 % w/w Injection, suspension; kit; solution Intra-articular; Intramuscular; Topical Injection, solution; injection, suspension; kit; solution Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Intravenous; Perineural; Topical Gel Topical Cream Cutaneous Kit Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Perineural; Respiratory (inhalation); Topical Cloth; injection, solution; injection, suspension; kit Infiltration; Intra-articular; Intramuscular; Topical Kit Infiltration; Soft tissue; Topical Kit Topical Lotion Oral Injection, solution Intra-articular; Intramuscular 40 mg/1mL Suspension Intramuscular 40 mg / mL Injection Intra-articular; Intramuscular 40 mg/ml Injection Intradermal; Intramuscular 10 mg/ml Kit; ointment Topical 1 mg/1g Cream; kit Topical 1 mg/1g Injection Intramuscular 40 mg Paste 1 MG/G Injection, suspension Injection, solution Intravenous 200 mg/5ml Injection, solution Intravenous 40 mg/ml Injection, solution Intravenous 80 mg/2ml Injection, suspension Intravitreal 80 MG/ML Injection, suspension Parenteral 40 MG/1ML Cream Topical 0.1 % Ointment Topical 0.25 mg / g Ointment Topical 0.1 % Cream; kit Topical Ointment 0.1 % Suspension Intra-articular 50 mg Cream Topical 0.1 mg/.1g Cream Topical 0.25 mg/1g Cream Topical 0.25 mg/1 Cream Topical 1 mg/1 Cream Topical 1 mg/1g Cream Topical 5 mg/1 Cream Topical 5 mg/1g Injection Intra-articular; Intrabursal; Intradermal; Intralesional 10 MG/ML Injection, suspension Intra-articular; Intrabursal; Intradermal; Intralesional 10 mg/1mL Injection, suspension Intra-articular; Intramuscular 200 mg/5mL Injection, suspension Intra-articular; Intramuscular 400 mg/10mL Injection, suspension Intra-articular; Intramuscular; Soft tissue 40 mg/1mL Lotion Topical 1 mg/1mL Ointment Topical .5 mg/1g Ointment Topical 0.1 mg/0.100g Ointment Topical 0.25 mg/1g Ointment Topical 1 mg/1g Paste Dental 1 mg/1g Paste Topical 1 mg/1g Spray Topical 0.147 mg/1g Spray, metered Nasal 55 ug/1 Suspension Intra-arterial; Intramuscular 40 mg/1mL Cream 1 mg/g Injection Intramuscular 40 mg/ml Ointment Topical .5 mg/1 Suspension Intra-articular; Intrabursal; Intramuscular 40 mg / mL Suspension Intralesional 40 mg / mL Suspension Intra-articular; Intradermal; Intralesional; Intramuscular 40 mg / mL Injection, suspension 40 mg/1ml Injection, suspension Ophthalmic Suspension Ophthalmic Solution Oral 0.2 % Emulsion Topical 0.1 % Injection, suspension Parenteral 80 MG/2ML Ointment Topical 0.5 mg/1g Injection, suspension Intramuscular 40 mg/mL Cream Topical Injection, solution 40 mg/mL Injection, suspension Ophthalmic 40 mg/1mL Suspension Intravitreal 40 mg / mL Injection; injection, suspension 10 mg/ml Ointment 1 mg Suspension Intra-articular; Intradermal 50 mg Suspension Intra-articular; Intrasynovial; Periarticular 20 mg / mL Injection, suspension Parenteral 20 mg/ml Injection, suspension Intra-articular; Intramuscular; Intravitreal 8 mg/0.1mL Tablet Oral 16 MG Tablet Oral 8 MG Cream Cutaneous 1 mg/g Ointment Oral 1 mg/g Ointment Cutaneous 1 mg/g Solution Topical Injection Parenteral 40 mg Injection Parenteral 80 mg Ointment 1 mg/g Cream Topical 0.25 mg/g Ointment 0.25 mg/g Injection, solution Intramuscular 10 mg/mL Injection, solution Intramuscular 40 mg/mL Kit Intra-articular 32 mg/1 Suspension 10 mg/1ml Suspension 40 mg/1ml Cream 0.02 %w/w Lotion Topical 0.1 %w/w Solution; spray Nasal 55 mcg/1dose Gel Oral 0.1 %w/w Cream 0.5 %w/w Tablet Oral 4 mg Cream 0.1 %w/w Ointment Topical 0.1 %w/w Paste Oral 0.1 %w/w - Prices
Unit description Cost Unit Triesence 40 mg/ml vial 148.8USD ml Kenalog Aerosol 63 gm Can 118.99USD can Nasacort AQ 55 mcg/act Aerosol (Nasal Spray) 118.74USD inhaler Triamcinolone Acetonide 0.1% Paste 5 gm Tube 71.7USD tube Kenalog 0.5% Cream 20 gm Tube 54.99USD tube Kenalog 0.1% Lotion 60ml Bottle 51.99USD bottle Kenalog 0.025% Lotion 60ml Bottle 46.99USD bottle Triamcinolone Acetonide 0.025% Lotion 60ml Bottle 40.99USD bottle Triamcinolone diacetate powder 26.01USD g Triamcinolone powder 20.29USD g Kenalog 0.1% Cream 15 gm Tube 18.99USD tube Triamcinolone Acetonide 0.1% Ointment 80 gm Tube 18.99USD tube Triamcinolone Acetonide 0.5% Ointment 15 gm Tube 14.99USD tube Aristospan 20 mg/ml vial 14.19USD ml Oralone 0.1% paste 13.57USD g Triamcinolone Acetonide 0.025% Cream 80 gm Tube 12.99USD tube Triamcinolone Acetonide 0.1% Cream 80 gm Tube 12.99USD tube Triamcinolone Acetonide 0.5% Cream 15 gm Tube 12.99USD tube Triamcinolone Acetonide 0.025% Cream 15 gm Tube 11.99USD tube Triamcinolone Acetonide 0.025% Ointment 80 gm Tube 11.99USD tube Triamcinolone Acetonide 0.1% Cream 15 gm Tube 11.99USD tube Triamcinolone Acetonide 0.1% Ointment 15 gm Tube 11.99USD tube Kenalog-40 40 mg/ml vial 8.99USD ml Triamcinolone acet 40 mg/ml sus 8.42USD ml Kenalog-40 40 mg/ml 7.53USD ml Nasacort aq nasal spray 6.99USD g Triamcinolone 0.1% paste 6.4USD g Triamcinolone Acetonide 40 mg/ml 6.29USD ml Triamcinolone Acetonide Usp 40 mg/ml 5.76USD ml Aristospan 5 mg/ml vial 3.54USD ml Kenalog-10 10 mg/ml 3.24USD ml Triamcinolone Acetonide 10 mg/ml 2.71USD ml Kenalog-10 10 mg/ml vial 2.32USD ml Triamcinolone acet 10 mg/ml sus 2.18USD ml Aristocort C 0.5 % Cream 1.3USD g Oracort 0.1 % Paste 1.19USD g Triderm 0.1% cream 0.47USD g Triamcinolone 0.5% cream 0.22USD g Aristocort R 0.1 % Cream 0.15USD g Aristocort R 0.1 % Ointment 0.15USD g Triamcinolone Acetonide 0.1% Cream 0.07USD gm Triaderm Regular 0.1 % Cream 0.07USD g Triamcinolone 0.025% cream 0.06USD g Triamcinolone Acetonide 0.1% Ointment 0.05USD gm DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2268927 No 2003-09-23 2017-07-02 Canada US5976573 No 1999-11-02 2016-07-03 US US6143329 No 2000-11-07 2016-07-03 US US7977045 No 2011-07-12 2016-07-03 US US6395294 No 2002-05-28 2020-01-13 US US8211880 No 2012-07-03 2029-03-10 US US8128960 No 2012-03-06 2029-12-17 US US8828440 No 2014-09-09 2031-08-04 US US9555048 No 2017-01-31 2031-08-04 US US8636713 No 2014-01-28 2027-05-02 US US9636332 No 2017-05-02 2033-11-08 US US9937075 No 2018-04-10 2034-05-02 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 270 Chemspider - Predicted Properties
Property Value Source Water Solubility 0.847 mg/mL ALOGPS logP 0.84 ALOGPS logP 0.24 Chemaxon logS -2.7 ALOGPS pKa (Strongest Acidic) 11.75 Chemaxon pKa (Strongest Basic) -3.3 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 115.06 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 99.38 m3·mol-1 Chemaxon Polarizability 39.8 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9823 Blood Brain Barrier + 0.9528 Caco-2 permeable + 0.7397 P-glycoprotein substrate Substrate 0.8204 P-glycoprotein inhibitor I Non-inhibitor 0.8759 P-glycoprotein inhibitor II Non-inhibitor 0.9725 Renal organic cation transporter Non-inhibitor 0.8178 CYP450 2C9 substrate Non-substrate 0.8858 CYP450 2D6 substrate Non-substrate 0.9006 CYP450 3A4 substrate Substrate 0.7049 CYP450 1A2 substrate Non-inhibitor 0.9144 CYP450 2C9 inhibitor Non-inhibitor 0.8939 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.911 CYP450 3A4 inhibitor Non-inhibitor 0.9007 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.942 Ames test Non AMES toxic 0.8858 Carcinogenicity Non-carcinogens 0.9521 Biodegradation Not ready biodegradable 0.9952 Rat acute toxicity 2.3369 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9562 hERG inhibition (predictor II) Inhibitor 0.6125
Spectra
- Mass Spec (NIST)
- Download (9.24 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 197.9275218 predictedDarkChem Lite v0.1.0 [M-H]- 196.2095218 predictedDarkChem Lite v0.1.0 [M-H]- 191.57143 predictedDeepCCS 1.0 (2019) [M+H]+ 198.8500218 predictedDarkChem Lite v0.1.0 [M+H]+ 196.4032218 predictedDarkChem Lite v0.1.0 [M+H]+ 193.46683 predictedDeepCCS 1.0 (2019) [M+Na]+ 197.6947218 predictedDarkChem Lite v0.1.0 [M+Na]+ 196.6655218 predictedDarkChem Lite v0.1.0 [M+Na]+ 199.33134 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Receptor for glucocorticoids (GC) (PubMed:27120390, PubMed:37478846). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors (PubMed:28139699). Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Involved in chromatin remodeling (PubMed:9590696). Plays a role in rapid mRNA degradation by binding to the 5' UTR of target mRNAs and interacting with PNRC2 in a ligand-dependent manner which recruits the RNA helicase UPF1 and the mRNA-decapping enzyme DCP1A, leading to RNA decay (PubMed:25775514). Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth (By similarity)
- Specific Function
- core promoter sequence-specific DNA binding
- Gene Name
- NR3C1
- Uniprot ID
- P04150
- Uniprot Name
- Glucocorticoid receptor
- Molecular Weight
- 85658.57 Da
References
- Nehme A, Lobenhofer EK, Stamer WD, Edelman JL: Glucocorticoids with different chemical structures but similar glucocorticoid receptor potency regulate subsets of common and unique genes in human trabecular meshwork cells. BMC Med Genomics. 2009 Sep 10;2:58. doi: 10.1186/1755-8794-2-58. [Article]
- Issar M, Sahasranaman S, Buchwald P, Hochhaus G: Differences in the glucocorticoid to progesterone receptor selectivity of inhaled glucocorticoids. Eur Respir J. 2006 Mar;27(3):511-6. [Article]
- Shahin V, Ludwig Y, Schafer C, Nikova D, Oberleithner H: Glucocorticoids remodel nuclear envelope structure and permeability. J Cell Sci. 2005 Jul 1;118(Pt 13):2881-9. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Dort K, Padia S, Wispelwey B, Moore CC: Adrenal suppression due to an interaction between ritonavir and injected triamcinolone: a case report. AIDS Res Ther. 2009 Jun 8;6:10. doi: 10.1186/1742-6405-6-10. [Article]
- Hagan JB, Erickson D, Singh RJ: Triamcinolone acetonide induced secondary adrenal insufficiency related to impaired CYP3A4 metabolism by coadministration of nefazodone. Pain Med. 2010 Jul;11(7):1132-5. doi: 10.1111/j.1526-4637.2010.00852.x. Epub 2010 Apr 29. [Article]
- Litt J. (2016). Litt's Drug eruption & reaction manual (22nd ed.). CRC Press LLc.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Dual cyclooxygenase and peroxidase in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate ((5Z,8Z,11Z,14Z)-eicosatetraenoate, AA, C20:4(n-6)), with a particular role in the inflammatory response (PubMed:11939906, PubMed:16373578, PubMed:19540099, PubMed:22942274, PubMed:26859324, PubMed:27226593, PubMed:7592599, PubMed:7947975, PubMed:9261177). The cyclooxygenase activity oxygenates AA to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide prostaglandin H2 (PGH2), the precursor of all 2-series prostaglandins and thromboxanes (PubMed:16373578, PubMed:22942274, PubMed:26859324, PubMed:27226593, PubMed:7592599, PubMed:7947975, PubMed:9261177). This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins. The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons (PubMed:16373578, PubMed:22942274, PubMed:26859324, PubMed:27226593, PubMed:7592599, PubMed:7947975, PubMed:9261177). Similarly catalyzes successive cyclooxygenation and peroxidation of dihomo-gamma-linoleate (DGLA, C20:3(n-6)) and eicosapentaenoate (EPA, C20:5(n-3)) to corresponding PGH1 and PGH3, the precursors of 1- and 3-series prostaglandins (PubMed:11939906, PubMed:19540099). In an alternative pathway of prostanoid biosynthesis, converts 2-arachidonoyl lysophopholipids to prostanoid lysophopholipids, which are then hydrolyzed by intracellular phospholipases to release free prostanoids (PubMed:27642067). Metabolizes 2-arachidonoyl glycerol yielding the glyceryl ester of PGH2, a process that can contribute to pain response (PubMed:22942274). Generates lipid mediators from n-3 and n-6 polyunsaturated fatty acids (PUFAs) via a lipoxygenase-type mechanism. Oxygenates PUFAs to hydroperoxy compounds and then reduces them to corresponding alcohols (PubMed:11034610, PubMed:11192938, PubMed:9048568, PubMed:9261177). Plays a role in the generation of resolution phase interaction products (resolvins) during both sterile and infectious inflammation (PubMed:12391014). Metabolizes docosahexaenoate (DHA, C22:6(n-3)) to 17R-HDHA, a precursor of the D-series resolvins (RvDs) (PubMed:12391014). As a component of the biosynthetic pathway of E-series resolvins (RvEs), converts eicosapentaenoate (EPA, C20:5(n-3)) primarily to 18S-HEPE that is further metabolized by ALOX5 and LTA4H to generate 18S-RvE1 and 18S-RvE2 (PubMed:21206090). In vascular endothelial cells, converts docosapentaenoate (DPA, C22:5(n-3)) to 13R-HDPA, a precursor for 13-series resolvins (RvTs) shown to activate macrophage phagocytosis during bacterial infection (PubMed:26236990). In activated leukocytes, contributes to oxygenation of hydroxyeicosatetraenoates (HETE) to diHETES (5,15-diHETE and 5,11-diHETE) (PubMed:22068350, PubMed:26282205). Can also use linoleate (LA, (9Z,12Z)-octadecadienoate, C18:2(n-6)) as substrate and produce hydroxyoctadecadienoates (HODEs) in a regio- and stereospecific manner, being (9R)-HODE ((9R)-hydroxy-(10E,12Z)-octadecadienoate) and (13S)-HODE ((13S)-hydroxy-(9Z,11E)-octadecadienoate) its major products (By similarity). During neuroinflammation, plays a role in neuronal secretion of specialized preresolving mediators (SPMs) 15R-lipoxin A4 that regulates phagocytic microglia (By similarity)
- Specific Function
- enzyme binding
- Gene Name
- PTGS2
- Uniprot ID
- P35354
- Uniprot Name
- Prostaglandin G/H synthase 2
- Molecular Weight
- 68995.625 Da
References
- Schaefer EC, Stewart AA, Durgam SS, Byron CR, Stewart MC: Effects of sodium hyaluronate and triamcinolone acetonide on glucosaminoglycan metabolism in equine articular chondrocytes treated with interleukin-1. Am J Vet Res. 2009 Dec;70(12):1494-501. doi: 10.2460/ajvr.70.12.1494. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters
- Specific Function
- acetylcholinesterase activity
- Gene Name
- BCHE
- Uniprot ID
- P06276
- Uniprot Name
- Cholinesterase
- Molecular Weight
- 68417.575 Da
References
- Ehrich M, Jortner BS, Gross WB: Types of adrenocorticoids and their effect on organophosphorus-induced delayed neuropathy in chickens. Toxicol Appl Pharmacol. 1988 Feb;92(2):214-23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione (PubMed:2732228). Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine (PubMed:2732228)
- Specific Function
- aromatase activity
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [Article]
- Moore CD, Roberts JK, Orton CR, Murai T, Fidler TP, Reilly CA, Ward RM, Yost GS: Metabolic pathways of inhaled glucocorticoids by the CYP3A enzymes. Drug Metab Dispos. 2013 Feb;41(2):379-89. doi: 10.1124/dmd.112.046318. Epub 2012 Nov 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins during embryogenesis (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes 3beta-hydroxyandrost-5-en-17-one (dehydroepiandrosterone, DHEA), a precursor in the biosynthesis of androgen and estrogen steroid hormones (PubMed:17178770, PubMed:9555064). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1), particularly D-ring hydroxylated estrone at the C16-alpha position (PubMed:12865317, PubMed:14559847). Mainly hydroxylates all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in atRA clearance during fetal development (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics including anticonvulsants (PubMed:9555064)
- Specific Function
- all-trans retinoic acid 18-hydroxylase activity
- Gene Name
- CYP3A7
- Uniprot ID
- P24462
- Uniprot Name
- Cytochrome P450 3A7
- Molecular Weight
- 57469.95 Da
References
- Moore CD, Roberts JK, Orton CR, Murai T, Fidler TP, Reilly CA, Ward RM, Yost GS: Metabolic pathways of inhaled glucocorticoids by the CYP3A enzymes. Drug Metab Dispos. 2013 Feb;41(2):379-89. doi: 10.1124/dmd.112.046318. Epub 2012 Nov 9. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species
- Specific Function
- serine-type endopeptidase inhibitor activity
- Gene Name
- SERPINA6
- Uniprot ID
- P08185
- Uniprot Name
- Corticosteroid-binding globulin
- Molecular Weight
- 45140.49 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Groyer A, Le Bouc Y, Joab I, Radanyi C, Renoir JM, Robel P, Baulieu EE: Chick oviduct glucocorticosteroid receptor. Specific binding of the synthetic steroid RU 486 and immunological studies with antibodies to chick oviduct progesterone receptor. Eur J Biochem. 1985 Jun 3;149(2):445-51. [Article]
- Svec F, Harrison RW: Conditions affecting AtT-20 cell glucocorticoid uptake. Steroids. 1981 Feb;37(2):143-56. [Article]
- Eisen HJ: An antiserum to the rat liver glucocorticoid receptor. Proc Natl Acad Sci U S A. 1980 Jul;77(7):3893-7. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
- Specific Function
- antioxidant activity
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Albumin
- Molecular Weight
- 69365.94 Da
References
- FLORINI JR, BUYSKE DA: Plasma protein binding of triamcinolone-H3 and hydrocortisone-4-C14. J Biol Chem. 1961 Jan;236:247-51. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 07, 2024 17:55