Triamcinolone acetonide

Описание

Triamcinolone acetonide is a synthetic corticosteroid. It decreases cytokine levels, the firing rate of sensory neurons, and mechanical hypersensitivity in a rat spinal nerve ligation model when used at a dose of 1.5 mg/kg prior to and following surgery for three days. Triamcinolone acetonide also decreases outflow facility in a mouse model of steroid-induced glaucoma when 20 μl of a 40 mg/ml suspension is administered subconjunctivally. Formulations containing triamcinolone acetonide are used in the treatment of diabetic macular edema.

Химические свойства

White Solid

Определение

ChEBI: A synthetic glucocorticoid that is the 16,17-acetonide of triamcinolone. Used to treat various skin infections.

Показания

Triamcinolone acetonide (Aristocort, Kenalog) is a synthetic fluorinated corticosteroid.

Общее описание

The three main metabolitesof triamcinolone acetonide (Azmacort, Nasacort) are 6β-hydroxytriamcinolone acetonide, 21-carboxytriamcinoloneacetonide, and 6β-hydroxy-21-carboxytriamcinolone acetonide.All are much less active than the parent compound.The 6β-hydroxyl group and the 21-carboxy group are bothstructural features that greatly reduce GC action. The increasedwater solubility of these metabolites also facilitatesmore rapid excretion.

Клиническое использование

Triamcinolone acetonide used topically to treat various skin conditions, to relieve the discomfort of mouth sores, and by injection into joints to treat various joint conditions.Triamcinolone acetonide frequently is used by inhalation for the treatment of lung diseases (e.g., asthma).

Побочные эффекты

The side effects of using Triamcinolone acetonide include:Skin dryness, flaking, crusting, burning, or blistering; Skin irritation; Skin soreness, itching, swelling, scaling, or severe redness; Scaling or redness near mouth; Skin thinning or bruising, especially in skin folds (like between the finger) or on the face (when directed to use it there); New or worsening pimples or acne; Skin burning and itching with tiny red blisters; Skin softening; Itching, pain, or burning sensation in hairy areas, or pus at the root of the hair; Increased hair growth on the legs, arms, back, or forehead; Lightening of skin tone; Red or purple lines on the arms, face, legs, groin, or trunk.

Профиль безопасности

Poison by subcutaneous and intraperitoneal routes. An experimental teratogen. Other experimental reproductive effects. Human mutation data reported. When heated to decomposition it emits acrid smoke and toxic fumes of F-.

Метаболизм

Triamcinolone acetonide frequently is used by inhalation for the treatment of lung diseases (e.g., asthma). After inhalation, triamcinolone acetonide can become systemically available when the inhaled formulation is swallowed and absorbed unchanged from the GI tract, causing undesirable systemic effects. Triamcinolone acetonide that is swallowed is metabolized to 6β-hydroxytriamcinolone acetonide, 21-carboxytriamcinolone acetonide, and 21-carboxy-6β-hydroxytriamcinolone acetonide, all of which are more hydrophilic than their parent drug. Only approximately 1% of the dose was recovered from the urine as triamcinolone acetonide. Triamcinolone is not a major metabolite of triamcinolone acetonide in humans, suggesting that acetonide is resistant to hydrolytic cleavage. Triamcinolone acetonide is approximately eight times more potent than prednisolone.