Triamcinolone

Overview

Triamcinolone is a glucocorticoid used to treat certain skin diseases, allergies, and rheumatic disorders among others. It is also used to prevent worsening of asthma and chronic obstructive pulmonary disease (COPD). It can be taken in various ways including by mouth, injection into a muscle, and inhalation.[1] WP

Common side effects with long-term use include osteoporosis, cataracts, thrush, and muscle weakness. Serious side effects may include psychosis, increased risk of infections, adrenal suppression, and bronchospasm. Use in pregnancy is generally safe. It works by decreasing inflammation and immune system activity.[1][2] WP

Triamcinolone was patented in 1956 and came into medical use in 1958. It is available as a generic medication. In 2023, it was the 108th most commonly prescribed medication in the United States, with more than 6 million prescriptions.[3–6] WP

Uses, dosage and effects

Medical uses

Triamcinolone is used to treat various medical conditions, such as eczema, alopecia areata, lichen sclerosus, psoriasis, arthritis, allergies, ulcerative colitis, lupus, sympathetic ophthalmia, temporal arteritis, uveitis, ocular inflammation, keloids, urushiol-induced contact dermatitis, aphthous ulcers (usually as triamcinolone acetonide), central retinal vein occlusion, visualization during vitrectomy and the prevention of asthma attacks.[7][8][9] WP

The derivative triamcinolone acetonide is the active ingredient in various topical skin preparations (cream, lotion, ointment, aerosol spray) designed to treat such skin conditions as rash, inflammation, redness, or intense itching due to eczema and dermatitis.[10][11] WP

Risks and side effects

Contraindications

Contraindications for systemic triamcinolone are similar to those of other corticoids. They include systemic mycoses (fungal infections) and parasitic diseases, as well as eight weeks before and two weeks after application of live vaccines. For long-term treatment, the drug is also contraindicated in people with peptic ulcers, severe osteoporosis, severe myopathy, certain viral infections, glaucoma, and metastasizing tumours.[12] WP

There are no contraindications for use in emergency medicine.[13] WP

Side effects

The side effects of triamcinolone are similar to other corticosteroids. In short-term treatment of up to ten days, it has very few adverse effects; however, sometimes gastrointestinal bleeding is seen, as well as acute infections (mainly viral) and impaired glucose tolerance.[13] WP⚠ Part of this sentence could not be copied from the source. Open the source to read it in full.

Side effects of triamcinolone long-term treatment may include coughing (up to bronchospasms), sinusitis, metabolic syndrome–like symptoms such as high blood sugar and cholesterol, weight gain due to water retention, and electrolyte imbalance, as well as cataract, thrush, osteoporosis, reduced muscle mass, and psychosis. Triamcinolone injections can cause bruising and joint swelling. Symptoms of an allergic reaction include rash, itch, swelling, severe dizziness, trouble breathing, and anaphylaxis.[1][12][14][15] WP

Overdose

No acute overdosing of triamcinolone has been described.[12] WP

Interactions

Interactions

Drug interactions are mainly pharmacodynamic, that is, they result from other drugs either adding to triamcinolone's corticosteroid side effects or working against its desired effects. They include:[12][13] WP

• Atropine and other anticholinergics can substantially increase pressure in the eyes.[12][13] WP
• Antidiabetic drugs can become less effective because triamcinolone causes diabetes-like symptoms.[12][13] WP
• Aspirin and other NSAIDs, as well as anticoagulants such as warfarin, add to the risk of gastrointestinal bleeding.[12][13] WP
• Diuretics that excrete potassium (such as loop diuretics and thiazides) can increase the risk of hypokalemia and thus lead to abnormal heart rhythm.[12][13] WP
• Cardiac glycosides may have more adverse effects due to reduced potassium levels in the blood.[12][13] WP
• The risk for blood count changes is increased when combining triamcinolone with ACE inhibitors.[12][13] WP

Triamcinolone and other drugs can also influence each other's concentrations in the body, amounting to pharmacokinetic interactions such as:[12][13] WP

• Rifampicin, phenytoin, carbamazepine and other inducers of the liver enzyme CYP3A4 speed up metabolization of triamcinolone and can therefore reduce its effectiveness.[16] WP
• Conversely, CYP3A4 inhibitors, such as ketoconazole and itraconazole, can increase its concentrations in the body and the risk for adverse effects.[12][13] WP
• Blood concentrations of ciclosporin can be increased.[12][13] WP

Pharmacology

Mechanism of action

Triamcinolone is a glucocorticoid that is about five times as potent as cortisol but has very few mineralocorticoid effects.[13] WP⚠ Part of this sentence could not be copied from the source. Open the source to read it in full.

Pharmacokinetics

When taken by mouth, the drug's bioavailability is over 90%. It reaches its highest concentrations in the blood plasma after one to two hours and is bound to plasma proteins to about 80%. The biological half-life from the plasma is 200 to 300 minutes; due to stable complexes of triamcinolone and its receptor in the intracellular fluid, the total half-life is significantly longer at about 36 hours.[13][14] WP

A small fraction of the substance is metabolized to 6-hydroxy- and 20-dihydro-triamcinolone; most of it probably undergoes glucuronidation, and a smaller part sulfation. Three-quarters are excreted via the urine, and the rest via the faeces.[12][13] WP

Due to corticoids' mechanism of action, the effects are delayed as compared to plasma concentrations. Depending on the route of administration and the treated condition, the onset of action can be from two hours up to one or two days after application; and the drug can act much longer than its elimination half-life would suggest.[13][14] WP

Legal status

Society and culture

In 2010, Teva and Perrigo launched the first generic inhalable triamcinolone.[17] WP

According to Chang et al. (2014), "Triamcinolone acetonide (TA) is classified as an S9 glucocorticoid in the 2014 Prohibited List published by the World Anti-Doping Agency, which caused it to be prohibited in international athletic competition when administered orally, intravenously, intramuscularly or rectally".[18] WP

Chemistry

Formula

C21H27FO6 PC

CAS number

124-94-7 PC

Molar mass (g/mol)

394.4 PC

IUPAC name (computed by PubChem)

(8S,9R,10S,11S,13S,14S,16R,17S)-9-fluoro-11,16,17-trihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one PC

SMILES

C[C@]12C[C@@H]([C@]3([C@H]([C@@H]1C[C@H]([C@@]2(C(=O)CO)O)O)CCC4=CC(=O)C=C[C@@]43C)F)O PC

InChIKey

GFNANZIMVAIWHM-OBYCQNJPSA-N PC

PubChem CID

31307

IUPAC name

(11β,16α)-9-Fluoro-11,16,17,21-tetrahydroxypregna-1,4-diene-3,20-dione WP

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

User reports

Pop culture

No references added yet.

Sources

1. Other Triamcinolone Monograph for Professionals
2. Other Triamcinolone Use During Pregnancy
3. Other Fischer J, Ganellin CR. Analogue-based Drug Discovery. 2006
4. Other Vallerand AH. Davis's Drug Guide for Nurses. 2018
5. Other Top 300 of 2023
6. Other Triamcinolone Drug Usage Statistics, United States, 2014 - 2023
7. Other Triamcinolone: Uses, Dosage, Side Effects, Warnings
8. Other Azmacort Inhaler: Side Effects, Dosage & Uses
9. Other Alcon Receives FDA Approval of Triesence Injectable Triamcinolone Suspension for Use in Eye Surgery
10. Journal / agency Chong M, Fonacier L. Treatment of Eczema: Corticosteroids and Beyond. Clinical Reviews in Allergy & Immunology. December 2016. doi:10.1007/s12016-015-8486-7 · PMID 25869743
11. Journal / agency Eichenfield LF, Tom WL, Berger TG, Krol A, Paller AS, Schwarzenberger K, Bergman JN, Chamlin SL, Cohen DE, Cooper KD, Cordoro KM, Davis DM, Feldman SR, Hanifin JM, Margolis DJ, Silverman RA, Simpson EL, Williams HC, Elmets CA, Block J, Harrod CG, Smith Begolka W, Sidbury R. Guidelines of care for the management of atopic dermatitis: section 2. Management and treatment of atopic dermatitis with topical therapies. Journal of the American Academy of Dermatology. July 2014. doi:10.1016/j.jaad.2014.03.023 · PMID 24813302 · PMC4326095
12. Other Austria-Codex. 2020
13. Other Arzneistoff-Profile. 2004
14. Other Triamcinolone (systemic). Accessed 19 August 2020 drugs.com PPA triamcinolone-systemic
15. Other Drugs and Treatments – Nasacort AQ Nasl – Patient Handout
16. Journal / agency 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 Metabolism and Disposition. February 2013. doi:10.1124/dmd.112.046318 · PMID 23143891 · PMC3558858
17. Other Perrigo Announces Launch Of Generic Version Of Nasacort AQ. 15 June 2011
18. Journal / agency Chang CW, Huang TY, Tseng YC, Chang-Chien GP, Lin SF, Hsu MC. Positive doping results caused by the single-dose local injection of triamcinolone acetonide. Forensic Science International. November 2014. doi:10.1016/j.forsciint.2014.07.024 · PMID 25126738

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.