|
Corticosteroids |   |
Corticosteroid Medications
Dexamethasone (Decadron) is one of the first successfully aerosolized agents (available since 1976) for inhalation, and it has an antiinflammatory potency of 30 times that of hydrocortisone. However, because it does not potentiate the beta2 receptors and the systemic side effects associated with it, the use of aerosolized dexamethasone has declined in favor of newer medications. It is available as a nasal spray (Turbinaire) and MDI (Respihaler). Each activation of the MDI delivers approximately 0.1 mg. Adult dose is 3 puffs TID or QID, up to a maximum of 12 per day. Pediatric dose is 2 puffs TID or QID, up to 8 per day. Each MDI delivers about 170 puffs.
Beclomethasone dipropionate (Vanceril, Beclovent) was the second aerosolized corticosteroid made available in this country, and is indicated for controlling intrinsic, extrinsic, and mixed asthma in patients over six years of age who require steroid therapy. The drug's success as an aerosol in reducing or replacing the use of systemic steroids is due to its high topical to systemic activity ratio (approximately 500 times that of dexamethasone). Beclomethasone has also been reported to minimize symptoms of perennial rhinitis in patients susceptible to antigens such as pollen.
An aerosol dose of 400 mcg of beclomethasone is approximately equivalent to 5-10 mg of oral prednisone. Adult dose is 0.5 to 1 mg QID. For the Vanceril MDI, one to four puffs are given 3-4 times a day. Each puff delivers about 42 mcg. The maximum daily adult dose is 840 mcg, with the pediatric dosage being about half of this. Asthmatic symptoms decrease in about 80% of patients concurrent with an improvement in pulmonary function. This occurs without the systemic side effects of oral steroids, although Candidiasis has been reported in some cases.
Betamethasone is a synthetic corticosteroid indicated for severe inflammation, immunosuppression, or adrenocortical insufficiency. Its duration of action is similar to dexamethasone, and has about 75% of the potency of beclomethasone. Daily dosage is 4 applications of 200 mcg each.
Triamcinolone Acetonide (Azmacort) an aerosol that is also topically active, and was available as Kenalog and Aristocort prior to its release as an aerosol. Available in an MDI preparation with a built-in spacer device, inhalations doses of about 100mcg, four times daily allow most steroid-dependent asthmatics to stop taking oral steroids. Aerosolized triamcinolone can cause hoarseness, voice weakness, and oropharyngeal candidiasis; however, rinsing the mouth and gargling after use generally prevents these side effects.
Flunisolide (AeroBid), another MDI-packaged aerosol that is topically active, is similar to triamincolone in potency but is longer acting. Like beclomethasone, it shows a peak plasma level after inhalation between 2 and 60 minutes, indicating good absorption from the lungs. Because it is more potent than many steroids, its recommended dosage is reduced: two inhalations (250 mcg each) twice daily for adults, with half of this recommended for pediatric patients.
Fluticasone propionate (Flowvent, Flonase) is a further analogue of previous agents with high topical potency, synthesized in order to avoid systemic side effects. It is part of androstane analogues which has a very weak HPA inhibitory activity, but high antiinflammatory effect. Available as a nasal spray and in MDI form in three different strengths, recommended adult dosage is 44-220 mcg BID. Fluticasone propionate is contraindicated in patients with acute status asthmaticus, respiratory tract infections, or tuberculosis.
 |
Budesonide is a topically active inhaled corticosteroid less potent than fluticasone, but greater than beclomethasone. After inhalation with a spacer device, peak plasma concentrations occur between 15-45 minutes with a half-life of 2 hours, and there appears to be minimal metabolism in the lung (about 70% of inhaled dose reaches the circulation). The recommended adult dosage is one puff (200 mcg) BID. Half this dose is used for children using a 50 mcg MDI. Budesonide may be given up to 3 puffs (600 mcg) BID, and is available as a nasal aerosol for treating allergic rhinitis. |
Hydrocortisone (variety of trade names including Hydrocortone, Acticort, and Cetacort) is a steroid that can be administered orally, parenterally, and only rarely by aerosol. Its plasma concentrations of 100-150 mcg/ml are generally high enough to diminish the symptoms of status asthmaticus. The adult daily dose can range from 300 to 2000 mg.
Prednisone (Deltasone) is an oral steroid in tablet form that has an anti-inflammatory potency 3-4 times that of hydrocortisone. Its onset of action is somewhat delayed because it becomes active only after its been converted to prednisolone in the liver. As an aerosol, it is completely ineffective. Indications include severe inflammation or immunosuppression, nephrosis, or acute axacerbations of multiple sclerosis. Adult dosage is PO 1.5-2.5 BID-QID, followed by once daily or QOD, with maintenance dosage up to 250 mg daily.
Prednisolone (numerous trade names include Prelone, Predicort, Key-Pred) is an intermediate acting synthetic steroid that is available by injection, orally, and is rarely aerosolized. Anti-inflammatory potency is 3-4 times that of hydrocortisone but it takes longer to reach its peak effect. The half-life is 2 to 4 hours and pharmacological effects last up to 36 hours. Usual adult dose is PO 2.5-15 mg BID-QID; IM 2-30 mg Q 12 hours; IV 1-30 mg daily..
Methylprednisolone (Duralone, Medralone, Depopred, et al) has 4-5 times times the anti-inflammatory potency of prednisolone, and is used frequently because it has little effect on electrolyte balance. Available orally, but is usually administered intravenously. Methylprednisolone is indicated for severe shock, status asthmaticus, ARDS, and aspiration pneumonia. Onset of action is rapid, half-life is 78-188 minutes, and pharmacological effects remain for up to 36 hours. Dosage varies depending upon symptoms.