Handbook of clinical drug data - part 8 pptx

ch10.qxd 804 8/13/2001 2:46 PM Page 804 R ESPIRATORY D RUGS Corticosteroids BECLOMETHASONE DIPROPIONATE Beconase, Beclovent, QVAR, Vancenase, Vanceril Pharmacology Potent topical glucocorticoid with little systemic activity because of low systemic bioavailability Administration and Adult Dosage Inhal for asthma (Beclovent, Vanceril) 168840 ␮g bid; (QVAR) 80–320 ␮g bid (See Notes.) Intranasal for nasal congestion 42–84 ␮g/nostril bid–qid (168–336 ␮g/day total dosage) for several days, then decrease dosage (if symptoms not recur) to minimum amount necessary to control stuffiness Special Populations Pediatric Dosage Titrate dosage to the lowest effective dosage Inhal for asthma (Beclovent, Vanceril) (6–12 yr) 42–336 ␮g bid; (>12 yr) same as adult dosage Intranasal for nasal congestion (672 µg 7.5 hr 600 20% Beclomethasone Dipropionate HFA QVAR MDI: 40, 80 µg/puff Adult: 80–160 µg 160–320 mg >320 µg 7.5 hr 600 20% Budesonide Pulmicort DPI: 200 µg/inhal Neb Susp: 125, 250 µg/mL Adult: 200–400 µg Child: 100–200 µg 400–600 µg 200–400 µg >600 µg >400 µg 5.1 hr 980 11% Flunisolide AeroBid AeroBid-M MDI: 250 µg/puff Adult: 500–1000 µg Child: 500–750 µg 1000–2000 µg 750–1250 µg >2000 µg >1250 µg 3.5 hr 330 21% Fluticasone Propionate Flovent MDI: 44, 110, 220 µg/puff DPI: 50, 100, 250 µg/inhal Adult: 88–264 µg Child: 88–176 µg 264–660 µg 176–440 µg >660 µg >440 µg 10.5 hr 1200 1% Page 806 MDI: 42, 84 µg/puff 2:46 PM Beclomethasone Dipropionate Beclovent Vanceril (continued ) ch10.qxd INHALED CORTICOSTEROIDS COMPARISON CHART (continued ) DOSAGE FORMSb DRUG MDI: 100 µg/puff TOPICAL POTENCYc ORAL BIOAVAILABILITYd >2000 µg >1200 µg 3.9 hr 330 11% 500–50 bid — — — Medium (Step 3) High (Step 4) Adult: 400–1000 µg Child: 400–800 µg 1000–2000 µg 800–1200 µg Adult: 100–50 bid 250–50 bid COMBINATION PRODUCTS DPI: Fluticasone 100 µg, salmeterol 50 µg/inhal; Fluticasone 250 µg, salmeterol 50 µg/inhal; Fluticasone 500 µg, salmeterol 50 µg/inhal 807 DPI = dry powder inhaler; MDI = metered-dose inhaler, Neb = nebulizer a Dosage ranges correspond to recommended treatment intensities for steps 2–4 of the NIH guidelines for diagnosis and management of asthma: step = mild intermittent; step = mild persistent; step = moderate persistent; step = severe persistent.20 The most important determinant of appropriate dosage is the clinician’s judgment of the patient’s response to therapy; the clinician must monitor the patient’s response on several clinical parameters and adjust the dosage accordingly The stepwise approach to therapy emphasizes that once control of symptoms is achieved, the dosage of medication should be carefully titrated to the minimum dosage required to maintain control, thereby reducing the potential for adverse effects b MDI dosages are expressed as the actuator dose (the amount of drug leaving the actuator and delivered to the patient), which is the labeling required in the United States This is different from the dosage expressed as the valve dose (the amount of drug leaving the valve, not all of which is available to the patient), which is used in many European countries and in some of the scientific literature DPI doses are expressed as the amount of drug in the inhaler following activation c Potency determined from skin blanching; dexamethasone is the reference drug and has a value of in this assay d Oral bioavailability of the swallowed portion of the dose received by the patient About 80% of the dose from an MDI without a spacer is swallowed Nearly all of the drug delivered to the lungs is bioavailable From 10–30% of an MDI dose is delivered to the lungs, depending on the product and device Both the relative potency and the total bioavailability (inhaled + swallowed) determine the systemic activity of the product From references 20 and 68–70 Page 807 Fluticasone Propionate and Salmeterol Advair Diskus 2:46 PM Triamcinolone Acetonide Azmacort RECEPTOR BINDING HALF-LIFE Low (Step 2) 8/13/2001 DAILY DOSAGEa ch10.qxd 808 INTRANASAL CORTICOSTEROIDS COMPARISON CHART DOSAGE FORMS ADULT DOSAGE PEDIATRIC DOSAGEa 1–2 sprays into each nostril bid–qid spray into each nostril bid–tid Budesonide Rhinocort Aerosol, Metered-Dose 32 µg/spray sprays into each nostril bid or sprays into each nostril q AM, to a maximum of 800 µg/day sprays into each nostril bid or sprays into each nostril q AM, to a maximum of 400 µg/day Flunisolide Nasalide Nasarel Spray, Aqueous 25 µg/spray sprays into each nostril bid, to a maximum of sprays/day into each nostril spray into each nostril tid–qid Fluticasone Propionate Flonase Spray, Aqueous 50 µg/spray sprays into each nostril daily or spray into each nostril bid; maintenance spray into each nostril daily, to a maximum of 200 µg/day (≥4 yr) spray in each nostril daily (100 µg/ day); for nonresponders, sprays in each nostril daily or spray in each nostril bid, decrease to 100 µg/day once a response is achieved Mometasone Furoate Nasonex Spray, Aqueous 50 µg/spray sprays into each nostril once daily (