Astocort

Uses

is used for the relief of the inflammatory and pruritic manifestations of corticosteroid responsive dermatoses including atopic dermatitis, contact dermatitis, eczematous dermatitis, neurodermatitis, seborrheic dermatitis, insect bites, lichen simplex chronicus, exfoliative dermatitis, stasis dermatitis, nummular eczema, psoriasis and pruritus ani and vulvae.

Astocort is also used to associated treatment for these conditions: Acne, Acne Vulgaris, Acute Gouty Arthritis, Allergic Contact Dermatitis, Allergic Rhinitis (AR), Allergy Skin, Alopecia Areata (AA), Ankylosing Spondylitis (AS), Asthma, Atopic Dermatitis (AD), Autoimmune Hemolytic Anemia, Berylliosis, Bullous dermatitis herpetiformis, Chapped skin, Chronic Eczema, Chronic Inflammatory Skin Diseases, Congenital Adrenal Hyperplasia (CAH), Congenital Hypoplastic Anemia, Crohn's Disease (CD), Dental Cavity, Dermatitis, Dermatitis, Contact, Dermatitis, Eczematous, Dermatomyositis, Diaper Rash, Discoid Lupus Erythematosus (DLE), Edema of the cerebrum, Epicondylitis, Erythroderma, Fungal infectious disorders of the Beard, Gingivitis, Hemangiomas, Hemorrhoids, Hypercalcemia, Infected Wound, Infections, Fungal, Inflammation of Mouth, Intertrigo, Itching of the Anus, Itching of the External Genitalia, Itching of the Foot, Itching of the genitals, Itching of the hand, Juvenile Idiopathic Arthritis (JIA), Keloid Scars, Leukemias, Lichen Planus (LP), Lichen simplex chronicus, Malignant Lymphomas, Mycosis Fungoides (MF), Mycotic Eczema, Necrobiosis lipoidica diabeticorum, Neurodermatitis, Nummular Dermatitis, Ocular Inflammation, Ophthalmia, Sympathetic, Oral Erosive Lichen Planus, Oral Infection, Otitis Externa, Pemphigus, Pericarditis, Polymyositis, Post-Herpetic Neuralgia (PHN), Primary adrenocortical insufficiency, Proteinuria, Psoriasis Vulgaris (Plaque Psoriasis), Psoriatic Arthritis, Psoriatic plaque, Pure Red Cell Aplasia, Purulent Wounds, Pyoderma caused by susceptible bacteria, Regional Enteritis, Rheumatoid Arthritis, Ringworm Folliculitis, Seborrheic Dermatitis, Seborrheic Dermatitis, Eczematous, Secondary Impetiginization, Secondary adrenocortical insufficiency, Secondary thrombocytopenia, Serum Sickness, Skin Mycoses, Stomatitis, Aphthous, Stomatitis, Denture, Synovitis, Systemic Lupus Erythematosus (SLE), Temporal Arteritis, Tinea Corporis, Transfusion Reactions, Trichinosis, Tuberculosis (TB), Ulcerative Colitis, Urticaria, Uveitis, Acute Bursitis, Acute Multiple sclerosis, Acute Rheumatic heart disease, unspecified, Acute Tenosynovitis, Corticosteroid-responsive dermatoses, Cutaneous candidiasis, Cystic tumour of the ganglia, Exfoliative erythroderma, Granuloma annulare lesions, Idiopathic eosinophilic pneumonias, Non-suppurative Thyroiditis, Oral infections, Oral lesions, Severe Erythema multiforme, Subacute Dermatitis, Eczematous, Symptomatic Sarcoidosis, Ulceration of the mouth, Ulcerative stomatitis

How Astocort works

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. Anti-inflammatory activity occurs via reversal of vascular dilation and reducing permeability, which prevents macrophage and leukocyte migration. Astocort 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.

Dosage

Astocort dosage

A small amount of Astocort is gently rub to the affected area 1-2 times daily. Some cases of eczematised psoriasis may be treated more effectively by the application of Astocort under an occlusive dressing.

Occlusive dressing technique: Gently rub a small amount of Astocort on the lesion until it disappears. Then reapply, leaving a thin coating and cover with a pliable non porous film. For convenience apply Astocort intermittently (12 hour occlusion during the night) followed by reapplication without occlusion, during the day.

Pediatric use: Astocortshould not be used in children under 8 years. Administration of topical corticosteroids to children should be limited to the least amount compatible with an effective therapeutic regimen. Chronic corticosteroid therapy may interfere with the growth and development of children. As children are more likely to get side effects, they should not normally be treated for longer than 5 days.

Side Effects

The following local side effects have been reported with topical corticosteroids, either with or without occlusive dressings: burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis and allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae and miliaria.

Toxicity

The subcutaneous LD₅₀ of triamcinolone acetonide in rats is 13,100µg/kg and in mice is 132mg/kg. 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. This overdose may be treated with supportive therapy and mifepristone for its antiglucocorticoid activity.

Precaution

If reactions or idiosyncrasies are encountered, Astocort Acetonide should be discontinued. The use of topical steroids on infected areas should be attended with caution and careful observation, bearing in mind the potential spreading of infections by anti-inflammatory steroids and the possible advisability of discontinuing steroid therapy and/or initiating antibacterial measures.

Astocort Acetonide should not be used on healthy skin or over large areas of skin and not to be used in the eye as there is potential risk of glaucoma and cataract. When steroids are applied for long periods of time (more than 4 weeks) the occurrence of atrophic striae is likely. Prolonged use on flexures and intertriginous areas is undesirable. Children may absorb proportionately larger amounts of topical corticosteroids and thus may be more susceptible to systemic toxicity. In infants, long term continuous topical steroid therapy should be avoided. Adrenal suppression can occur even without occlusion.

Food Interaction

Astocort Cholesterol interaction

[Moderate] Corticosteroids may elevate serum triglyceride and LDL cholesterol levels if used for longer than brief periods.

Patients with preexisting hyperlipidemia may require closer monitoring during prolonged corticosteroid therapy, and adjustments made accordingly in their lipid-lowering regimen.

Astocort Hypertension interaction

[Moderate] Corticosteroids may cause hypernatremia, hypokalemia, fluid retention, and elevation in blood pressure.

These mineralocorticoid effects are most significant with fludrocortisone, followed by hydrocortisone and cortisone, then by prednisone and prednisolone.

The remaining corticosteroids, betamethasone, dexamethasone, methylprednisolone, and triamcinolone, have little mineralocorticoid activities.

However, large doses of any corticosteroid can demonstrate these effects, particularly if given for longer than brief periods.

Therapy with corticosteroids should be administered cautiously in patients with preexisting fluid retention, hypertension, congestive heart failure, and

Dietary sodium restriction and potassium supplementation may be advisable.

Astocort Drug Interaction

Moderate: aspirin, furosemide, metoprolol, polyethylene glycol 3350Minor: albuterol, albuterolUnknown: diphenhydramine, duloxetine, omega-3 polyunsaturated fatty acids, fluticasone nasal, pregabalin, esomeprazole, acetaminophen / hydrocodone, montelukast, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine

Astocort Disease Interaction

Major: GI perforation, infections, prematurity, PUD, vaccinationModerate: (+) tuberculin test, cirrhosis, depression/psychoses, diabetes, electrolyte imbalance, fluid retention, hyperadrenocorticalism, hyperlipidemia, hypothyroidism, liver disease, MI, myasthenia gravis, myopathy, ocular herpes simplex, ocular toxicities, osteoporosis, scleroderma, strongyloidiasis, thromboembolism

Volume of Distribution

The apparent volume of distribution of triamcinolone is 115.2±10L. The mean apparent volume of distribution of triamcinolone acetonide is 1.96L/kg. The apparent volume of distribution of triamcinolone diacetate is 119.7±33.14L.

Elimination Route

A 16mg oral dose of triamcinolone reaches a C_max of 5.23±0.84ng/mL with a T_max of 2.24±0.78h and an AUC of 36.0±6.2ng*h/mL.

A 2mg intravenous dose of triamcinolone acetonide has an AUC of 57.7ng*h/mL. 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. An inhaled dose of triamcinolone acetonide reaches a C_max of 0.92ng/mL with a T_max of 1.74h and an AUC of 5.12ng*h/mL. The fraction of an inhaled dose that is actually absorbed via the pulmonary route reaches a C_max of 0.55ng/mL with a T_max of 0.66h and an AUC of 2.15ng*h/mL.

A 16mg oral dose of triamcinolone diacetate reaches a C_max of 5.33±1.55ng/mL with a T_max of 1.86±0.47h and an AUC of 32.7±9.9ng*h/mL.

Half Life

The half life of triamcinolone is 2.7h. The mean terminal elimination half life following an inhaled dose of triamcinolone acetonide is 2.4h. The half life of triamcinolone diacetate is 2.8h.

Clearance

The clearance of triamcinolone is 28.6±5.6L/h. The mean total body clearance of triamcinolone acetonide is 0.57L/h. The clearance of triamcinolone diacetate is 34.4±10.6L/h.

Elimination Route

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.

Pregnancy & Breastfeeding use

There are no adequate and well-controlled studies in pregnant women on teratogenic effects from topically applied corticosteroids. Therefore, topical corticosteroid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether topical administration of corticosteroid could result in sufficient systemic absorption to produce detectable quantities in breast milk. Systemically administered corticosteroids are secreted into breast milk in quantities not likely to have a deleterious effect on the infant. Nevertheless, caution should be exercised when topical corticosteroids are administered to a nursing woman.

Contraindication

Astocort Acetonide is contraindicated in those patients with a history of hypersensitivity to any of the components of the preparation. It is also contraindicated in tuberculosis of the skin, fungus infections and viral diseases of the skin (Herpes simplex, chickenpox and vaccinia), perioral dermatitis, rosacea and ulcerative conditions.

Acute Overdose

Topically applied corticosteroids can be absorbed in sufficient amounts to produce systemic effects e.g., mild, reversible suppression of adrenal function, ecchymoses of the skin, peptic ulceration, hypertension, aggravation of infection, hirsutism, acne, edema and muscle weakness

Storage Condition

Store in a cool & dry place. Protect from light.

Innovators Monograph

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