(British Approved Name, rINN)
Pharmacopoeias. In China, Europe, Japan, and US.
European Pharmacopoeia, 6th ed. (Triamcinolone). A white or almost white, crystalline powder. It shows polymorphism. Practically insoluble in water and in dichloromethane slightly soluble in methyl alcohol. Protect from light.
The United States Pharmacopeia 31, 2008 (Triamcinolone). A white or practically white, odourless, crystalline powder. Very slightly soluble in water, in chloroform, and in ether slightly soluble in alcohol and in methyl alcohol.
(British Approved Name Modified, rINNM)
Pharmacopoeias. In China, Europe, Japan, and US. China, also includes Triamcinolone Acetonide Acetate.
European Pharmacopoeia, 6th ed. (Triamcinolone Acetonide). A white or almost white, crystalline powder. It shows polymorphism. Practically insoluble in water sparingly soluble in alcohol. Protect from light.
The United States Pharmacopeia 31, 2008 (Tnamcinolone Acetonide). A white to cream-coloured crystalline powder, having not more than a slight odour. Practically insoluble in water sparingly soluble in dehydrated alcohol, in chloroform, and in methyl alcohol. Store at a temperature of 25°, excursions permitted between 15° and 30°.
Triamcinolone Acetonide Sodium Phosphate
(BANM, US Adopted Name, rINNM)
(British Approved Name Modified, rINNM)
Pharmacopoeias. In US.
The United States Pharmacopeia 31, 2008 (Triamcinolone Diacetate). A fine, white to off-white, crystalline powder, having not more than a slight odour. Practically insoluble in water soluble 1 in 13 of alcohol, 1 in 80 of chloroform, and 1 in 40 of methyl alcohol slightly soluble in ether.
(British Approved Name, US Adopted Name, rINN)
Pharmacopoeias. In Europe and US.
European Pharmacopoeia, 6th ed. (Triamcinolone Hexacetonide). A white or almost white, crystalline powder. Practically insoluble in water sparingly soluble in dehydrated alcohol and in methyl alcohol. Protect from light.
The United States Pharmacopeia 31, 2008 (Triamcinolone Hexacetonide). A white to cream-coloured powder. Practically insoluble in water soluble in chloroform slightly soluble in methyl alcohol.
Adverse Effects, Treatment, Withdrawal, and Precautions
As for corticosteroids in general. High doses of triamcinolone may have a greater tendency to produce proximal myopathy Its effects on sodium and water retention are less than those of prednisolone. When applied topically, particularly to large areas, when the skin is broken, or under occlusive dressings, or when given intranasally, corticosteroids may be absorbed in sufficient amounts to cause systemic effects.
Effects on the eye. For complications and precautions associated with intravitreal use of triamcinolone see under Eye Disorders, below.
Hypersensitivity. Local reactions to topical triamcinolone preparations have been attributed to the content of ethylenedi-amine. However, there have also been reports of anaphylactic shock after intra-articular or intramuscular injection of triamcinolone acetonide.
For a brief outline of the pharmacokinetics of corticosteroids.
Triamcinolone is reported to have a half-life in plasma of about 2 to over 5 hours. It is bound to plasma albumin to a much smaller extent than hydrocortisone. The acetonide, diacetate, and hexacetonide esters of triamcinolone are only very slowly absorbed from injection sites. Triamcinolone crosses the placenta.
Uses and Administration
Triamcinolone is a corticosteroid with mainly glucocorticoid activity 4mg of triamcinolone is equivalent in anti-inflammatory activity to about 5 mg of prednisolone. It is used, either in the form of the free alcohol or in one of the esterified forms, in the treatment of conditions for which corticosteroid therapy is indicated, except adrenocortical insufficiency for which hydrocortisone with supplementary fludrocortisone is preferred.
For oral dosage triamcinolone is used in doses ranging from 4 to 48 mg daily.
For parenteral use the acetonide or diacetate esters are given in doses of about 40 mg by intramuscular injection. They are usually given as suspensions to provide a prolonged systemic effect. A dose of 40 to 100 mg of the acetonide may provide symptomatic control throughout the pollen season for hay fever sufferers (but see Rhinitis, below) for the diacetate, a 40-mg dose is given weekly.
For intra-articular injection triamcinolone acetonide, diacetate, and hexacetonide have all been used. Doses for these esters have typically been in the range of 2.5 to 40 mg, 3 to 48 mg, and 2 to 30 mg respectively, depending upon the size of the joint injected.
For topical application in the treatment of various skin disorders triamcinolone acetonide is used, usually in creams, lotions, or ointments containing 0.1% although concentrations ranging from 0.025 to 0.5% have been employed. Several topical preparations also contain an antimicrobial drug. For recommendations concerning the correct use of corticosteroids on the skin, and a rough guide to the clinical potencies of topical corticosteroids. Triamcinolone esters are also commonly used by intralesional or intradermal injection in the treatment of some inflammatory skin disorders such as keloids. Suggested doses for the various esters have been:
• acetonide: 1 to 3 mg per site with no more than 5 mg injected into any one site or not more than 30 mg in total if several sites of injection are used
• diacetate: a total of 5 mg in divided doses into small lesions or up to a total of 48 mg in divided doses into large lesions with no more than 12.5 mg injected into any one site or 25 mg injected into any one lesion
• hexacetonide: up to 500 micrograms per square inch (about 80 micrograms/cm) of affected skin.
Triamcinolone acetonide is also used by inhalation for the control of asthma in a usual dose of about 150 micrograms by metered-dose inhaler three or four times daily, or 300 micrograms twice daily the dose should not exceed 1200 micrograms daily. Children aged 6 to 12 years may be given 75 or 150 micrograms three or four times daily, or 150 to 300 micrograms twice daily the daily dose should not exceed 900 micrograms.
In the prophylaxis and treatment of allergic rhinitis triamcinolone acetonide may be given by a nasal spray in a usual initial dose of 2 sprays (110 micrograms) into each nostril once daily, reduced to 1 spray (55 micrograms) when control is achieved. Children aged 6 to 12 years may be given 1 spray (55 micrograms) into each nostril once daily in severe symptoms this may be increased to 220 micrograms daily.
A preservative-free suspension of triamcinolone acetonide 40 mg/mL is available for intravitreal injection. A dose of 4 mg is used for the treatment of sympathetic ophthalmia, temporal arteritis, uveitis, and ocular inflammatory conditions that are unresponsive to topical corticosteroids. Further doses may be given as needed during the course of treatment. A dose of 1 to 4 mg may be used for visualisation during vitrectomy. Other esters of triamcinolone that have occasionally been used include the acetonide dipotassium phosphate, acetonide hemisuccinate, aminobenzal benzamidoisobutyrate, and benetonide. Flupamesone (triamcinolone acetonide metembonate) has also been used.
Asthma. Intramuscular triamcinolone acetonide has been reported to be more effective than oral low-dose prednisone in controlling exacerbations in patients with severe, chronic, life-threatening asthma, although this conclusion is controversial. Corticosteroids and beta2-adrenoceptor agonists form the cornerstone of the management of asthma. Inhaled corticosteroids are added to therapy with a short-acting beta2 agonist if symptom relief with the latter is needed more than once daily, although corticosteroids with reduced systemic activity are generally preferred to triamcinolone. Systemic corticosteroids are reserved for the most severe cases, and for the management of acute severe asthma attacks (status asthmaticus).
Chronic obstructive pulmonary disease. For discussion of the value of inhaled corticosteroids in chronic obstructive pulmonary disease, including reference to the use of triamcinolone acetonide.
Eye disorders. Intravitreal injection of triamcinolone acetonide has been tried in the management of eye disorders characterised by oedema and the abnormal proliferation of intra-ocular cells. Promising results have been reported in diabetic macular oedema, cystoid macular oedema, and oedema associated with retinal vein occlusion. It has also been used in agerelated macular degeneration (better results being seen when it is combined with photodynamic therapy), in proliferative diabetic retinopathy, and in the management of some forms of cataract and non-infectious uveitis. Complications of treatment may include raised intra-ocular pressure (IOP) and both infectious and non-infectious endophthalmitis. Patients with a baseline IOP greater than 16 mmHg or receiving a second injection should be carefully monitored, as they may be at greater risk of an increase monitoring should continue beyond 6 months. Dissolved drugs are not retained in the eye for prolonged periods, and early studies and off-label treatment have used injectable suspensions to achieve long-lasting concentrations of triamcinolone in the vitreous body. However, these commercial products were intended for intramuscular and intra-articular use and not licensed for intravitreal injection, and there has been concern about the potential ocular toxicity of their preservative, benzyl alcohol. Various techniques, such as sedimentation, centrifu-gation, and filtration, have been used extemporaneously to reduce the benzyl alcohol content of such products, but the quantity of triamcinolone in the final preparation may be altered depending on the technique used. More recently, a preservative-free product has been licensed in the USA for intravitreal use (Triesence Alcon, USA — see Uses and Administration, above).
Haemangioma. For reference to the use of a mixture of triamcinolone and betamethasone for intralesional injection of haemangioma.
Rhinitis. Triamcinolone is used in the management of allergic rhinitis. However, the use of depot injections of triamcinolone to manage seasonal allergic rhinitis has been deemed unacceptable by some.
British Pharmacopoeia 2008: Triamcinolone Acetonide Injection; Triamcinolone Cream; Triamcinolone Hexacetonide Injection; Triamcinolone Ointment; Triamcinolone Oromucosal Paste; Triamcinolone Tablets
The United States Pharmacopeia 31, 2008: Neomycin Sulfate and Triamcinolone Acetonide Cream; Neomycin Sulfate and Triamcinolone Acetonide Ophthalmic Ointment; Nystatin and Triamcinolone Acetonide Cream; Nystatin and Triamcinolone Acetonide Ointment; Nystatin, Neomycin Sulfate, Gramicidin, and Triamcinolone Acetonide Cream; Nystatin, Neomycin Sulfate, Gramicidin, and Triamcinolone Acetonide Ointment; Triamcinolone Acetonide Cream; Triamcinolone Acetonide Dental Paste; Triamcinolone Acetonide Injectable Suspension; Triamcinolone Acetonide Lotion; Triamcinolone Acetonide Ointment; Triamcinolone Acetonide Topical Aerosol; Triamcinolone Diacetate Injectable Suspension; Triamcinolone Diacetate Syrup; Triamcinolone Hexacetonide Injectable Suspension; Triamcinolone Tablets
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
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