B

Beta-Adrenergic Blockers

USES

Management of hypertension, angina pectoris, arrhythmias, hypertrophic subaortic stenosis, migraine headaches, MI (prevention), glaucoma.

ACTION

Beta-adrenergic blockers competitively block beta₁-adrenergic receptors, located primarily in myocardium, and beta₂-adrenergic receptors, located primarily in bronchial and vascular smooth muscle. By occupying beta-receptor sites, these agents prevent naturally occurring or administered epinephrine/norepinephrine from exerting their effects. The results are basically opposite to those of sympathetic stimulation.

Effects of beta₁ blockade include slowing heart rate, decreasing cardiac output and contractility; effects of beta₂ blockade include bronchoconstriction, increased airway resistance in pts with asthma or COPD. Beta blockers can affect cardiac rhythm/automaticity (decrease sinus rate, SA/AV conduction; increase refractory period in AV node); decrease systolic and diastolic B/P; exact mechanism unknown but may block peripheral receptors, decrease sympathetic outflow from CNS, or decrease renin release from kidney. All beta blockers mask tachycardia that occurs with hypoglycemia. When applied to the eye, reduce intraocular pressure and aqueous production.

BETA-ADRENERGIC BLOCKERS

Name	Availability	Indication	Dosage Range
Acebutolol (Sectral)	C: 200 mg, 400 mg	HTN, ventricular arrhythmia	HTN: Initially, 400 mg once daily or 2 divided doses. Usual dose: 400–800 mg/day Arrhythmia: Initially, 200 mg 2 times/day. Gradually increase to 300–600 mg 2 times/day
Atenolol (Tenormin)	T: 25 mg, 50 mg, 100 mg	HTN, angina, MI	Angina: Initially, 50 mg once daily. May increase to 100 mg once daily after one wk HTN: Initially, 50 mg once daily. May increase to 100 mg once daily after 2 wks MI: 50 mg bid or 100 mg once daily
Bisoprolol (Zebeta)	T: 5 mg, 10 mg	HTN	Initially, 5 mg once daily. May increase to 10 mg/day, then 20 mg/day. Usual dose: 5–10 mg/day
Carvedilol (Coreg)	T: 3.125 mg, 6.25 mg, 12.5 mg, 25 mg C (SR): 10 mg, 20 mg, 40 mg, 80 mg	HF, LVD after MI, HTN	Immediate-Release HF: Initially, 3.25 mg 2 times/day. May increase at 2 wk intervals to 6.25 mg 2 times/day, then 12.5 mg 2 times/day, then 25 mg 2 times/day LVD after MI: Initially, 6.25 mg 2 times/day. May increase q3–10 days to 12.5 mg 2 times/day, then 25 mg 2 times/day HTN: Initially, 6.25 mg 2 times/day. May increase q7–14 days to 12.5 mg 2 times/day, then 25 mg 2 times/day Extended-Release HF: 10–80 mg once daily LVD after MI: 10–80 mg once daily HTN: 20–80 mg once daily
Labetalol (Trandate)	T: 100 mg, 200 mg, 300 mg	HTN	Initially, 100 mg 2 times/day. May increase q2–3 days in 100 mg 2 times/day increments. Usual dose: 200 mg 2 times/day
Metoprolol (Lopressor [IR], Toprol XL [SR])	T (IR): 50 mg, 100 mg T (SR): 25 mg, 50 mg	HTN, angina, HF, MI	IR: Angina: Initially, 50 mg 2 times/day. May increase up to 400 mg/day HTN: Initially, 100 mg once daily. May increase at weekly intervals up to 450 mg/day Post-MI: 100 mg bid SR: Angina: 100–400 mg once daily HF: 12.5–200 mg once daily HTN: 25–400 mg once daily
Nadolol (Corgard)	T: 20 mg, 40 mg, 80 mg	HTN, angina	Angina, HTN: Initially, 40 mg once/day. Usual dose: 40–80 mg once daily
Nebivolol (Bystolic)	T: 2.5 mg, 5 mg, 10 mg, 20 mg	HTN	Initially, 5 mg once daily. May increase at 2 wk intervals up to 40 mg/day
Pindolol (Visken)	T: 5 mg, 10 mg	HTN	Initially, 5 mg 2 times/day. May increase to 10–40 mg/day. Maximum: 60 mg/day
Propranolol (Inderal)	T (IR): 10 mg, 20 mg, 40 mg, 60 mg, 80 mg C (SR): 60 mg, 80 mg, 120 mg, 160 mg S: 4 mg/ml, 8 mg/ml I: 1 mg/ml	HTN, angina, MI, arrhythmias, migraine, essential tremor, hypertrophic subaortic stenosis	IR: Angina: 80–320 mg/day in 2–4 divided doses Arrhythmias: 10–30 mg 3–4 times/day HTN: 40 mg bid up to 240 mg/day in 2–3 divided doses Hypertrophic subaortic stenosis: 20–40 mg 3–4 times/day Post-MI: 180–240 mg/day in 2–4 divided doses Migraine: Initially, 80 mg/day. May increase gradually up to 240 mg/day in divided doses Tremor: Initially, 40 mg 2 times/day. Usual dose: 120–320 mg/day SR: Angina: Initially, 80 mg once daily. May increase q3–7days up to 320 mg/day HTN: 80–120 mg once daily Migraine: Initially, 80 mg once daily. Gradually increase up to 240 mg once daily Hypertrophic subaortic stenosis: 80–160 mg once daily

C, Capsules; HF, heart failure; HTN, hypertension; I, injection; LVD, left ventricular dysfunction; S, solution; SR, sustained-release; T, tablets.

Bronchodilators

USES

Relief of bronchospasm occurring during anesthesia and in bronchial asthma, bronchitis, emphysema.

ACTION

Inhaled corticosteroids: Exact mechanism unknown. May act as anti-inflammatories, decrease mucus secretion.

Beta₂-adrenergic agonists: Stimulate beta receptors in lung, relax bronchial smooth muscle, increase vital capacity, decrease airway resistance.

Anticholinergics: Inhibit cholinergic receptors on bronchial smooth muscle (block acetylcholine action).

Leukotriene modifiers: Decrease effect of leukotrienes, which increase migration of eosinophils, producing mucus/edema of airway wall, causing bronchoconstriction.

Methylxanthines: Directly relax smooth muscle of bronchial airway, pulmonary blood vessels (relieve bronchospasm, increase vital capacity). Increase cyclic 3,5-adenosine monophosphate.

BRONCHODILATORS

Name	Availability	Dosage Range	Side Effects
Anticholinergics
Aclidinium (Tudorza)	Inhalation powder: 400 mcg/actuation	A: 400 mcg 2 times/day	Headache, nasopharyngitis, cough
Ipratropium (Atrovent)	NEB: 0.02% (500 mcg) MDI: 17 mcg/actuation	A (NEB): 500 mcg q6–8h A (MDI): 2 puffs 4 times/day	Upper respiratory tract infection, bronchitis, sinusitis, headache, dyspnea
Tiotropium (Spiriva, Spiriva Respimat)	Inhalation powder: 18 mcg/capsule Aerosol Solution: 1.25 mcg/inhalation	A: Once/day (inhaled twice) Aerosol Solution: 2 inhalations once daily	Xerostomia, upper respiratory tract infection, sinusitis, pharyngitis
Umeclidinium (Incruse Ellipta)	Inhalation powder: 62.5 mcg/blister	A: One inhalation once daily	Nasopharyngitis, upper respiratory tract infection, cough, arthralgia
Bronchodilators
	DPI: 90 mcg/actuation	DPI: 1–2 inhalations q4–6h as needed
Albuterol (ProAir HFA, ProAir Respiclick Proventil HFA, Ventolin HFA)	MDI: 90 mcg/actuation NEB: 2.5 mg/3 ml, 2.5 mg/0.5 ml, 0.63–1.25 mg/3 ml	MDI: 2 inhalations q4–6h as needed NEB: 1.25–5 mg q4–6h as needed	Tachycardia, skeletal muscle tremors, muscle cramping, palpitations, insomnia, hypokalemia, increased serum glucose
Albuterol/ipratropium (Combivent Respimat, DuoNeb)	MDI: 90 mcg albuterol/18 mcg ipratropium/actuation NEB: 2.5 mg albuterol/0.5 mg ipratropium/3 ml	MDI: 1 inhalation 4 times/day as needed NEB: 2.5 mg/0.5 mg 4 times/day as needed	Same as individual listing for albuterol and ipratropium
Formoterol (Foradil, Perforomist)	DPI: 12 mcg/capsule NEB: 20 mcg/2 ml	DPI: 12 mcg q12h NEB: 20 mcg q12h	Diarrhea, nausea, asthma exacerbation, bronchitis, infection
Formoterol/budesonide (Symbicort)	MDI: 80, 160 mcg/4.5 mcg/inhalation	MDI: 2 inhalations 2 times/day	Same as individual listing for formoterol and budesonide
Formoterol/mometasone (Dulera)	MDI: 5 mcg/100 mcg, 5 mcg/200 mcg	MDI: 2 inhalations 2 times/day	Same as individual listing for formoterol and beclomethasone
Indacaterol (Arcapta)	DPI: 75 mcg/capsule	DPI: 75–300 mcg once daily	Cough, oropharyngeal pain, nasopharyngitis, headache, nausea
Levalbuterol (Xopenex)	MDI: 45 mcg/actuation NEB: 0.31, 0.63, 1.25 mg/3 ml, 1.25 mg/0.5 ml	MDI: 2 inhalations q4–6h as needed NEB: 0.31–1.25 mg q6–8h	Tremor, rhinitis, viral infection, headache, nervousness, asthma, pharyngitis, rash
Olodaterol (Striverdi Respimat)	MDI: 2.5 mcg/actuation	MDI: 2 inhalations once daily	Nasopharyngitis, rash, dizziness, cough, bronchitis, upper respiratory tract infections
Olodaterol/tiotropium (Stiolto Respimat)	MDI: 2.5 mcg/2.5 mcg	MDI: 2 inhalations once daily	Nasopharyngitis, cough, back pain
Salmeterol (Serevent Diskus)	DPI: 50 mcg/blister	DPI: 50 mcg q12h	Headache, pain, throat irritation, nasal congestion, bronchitis, pharyngitis
Salmeterol/fluticasone (Advair Diskus, Advair HFA)	DPI: 100, 250, 500 mcg/50 mcg/blister MDI: 45, 115, 230 mcg/21 mcg/inhalation	DPI: 1 inhalation 2 times/day MDI: 2 inhalations 2 times/day	Same as individual listing for salmeterol and fluticasone
Vilanterol/umeclidinium (Anoro)	DPI: 25 mcg/62.5 mcg	DPI: Once daily	Pharyngitis, sinusitis, lower respiratory tract infections, constipation, diarrhea, muscle spasms, neck/chest pain
Inhaled Corticosteroids
Beclomethasone (Qvar)	MDI: 40, 80 mcg/inhalation	MDI: 40–320 mcg 2 times/day	Cough, hoarseness, headache, pharyngitis
Budesonide (Pulmicort Flexhaler, Pulmicort Respules)	DPI: (Flexhaler): 90, 180 mcg/inhalation DPI: (Turbuhaler): 200 mcg/inhalation NEB: (Respules): 0.25, 0.5 mg/2 ml	DPI: (Flexhaler): 180–720 mcg 2 times/day DPI: (Turbuhaler): 400–2,400 mcg/day in 2–4 divided doses NEB: (Respules): 250–500 mcg 1–2 times/day or 1 mg once daily	Headache, nausea, respiratory infection, rhinitis
Ciclesonide (Alvesco HFA)	HFA: 80, 160 mcg/inhalation	HFA: 80–640 mcg 2 times/day	Headache, nasopharyngitis, upper respiratory infection, epistaxis, nasal congestion, sinusitis
Fluticasone (Arnuity Ellipta, Flovent Diskus, Flovent HFA)	DPI: (Flovent Diskus): 50, 100, 250 mcg/blister (Arnuity Ellipta): 100 mcg, 200 mcg/activation MDI: (Flovent HFA): 44, 110, 220 mcg/inhalation	DPI: (Flovent Diskus): 100–1,000 mcg 2 times/day (Arnuity Ellipta): 100–200 mcg once daily MDI: (Flovent HFA): 88–880 mcg 2 times/day	Headache, nasal congestion, pharyngitis, sinusitis, respiratory infections
Formoterol/budesonide (Symbicort)	MDI: 80, 160 mcg/4.5 mcg/inhalation	MDI: 2 inhalations 2 times/day	Same as individual listing for formoterol and budesonide
Mometasone (Asmanex Twisthaler)	DPI: 110–220 mcg/inhalation	DPI: 220–880 mcg once daily in evening or 220 mcg bid	Same as beclomethasone
Salmeterol/fluticasone (Advair Diskus, Advair HFA)	DPI: 100, 250, 500 mcg/50 mcg/blister MDI: 45, 115, 230 mcg/21 mcg/inhalation	DPI: 1 inhalation 2 times/day MDI: 2 inhalations 2 times/day	Same as individual listing for salmeterol and fluticasone
Vilanterol/fluticasone (Breo Ellipta)	DPI: 25 mcg/100 mcg; 25 mcg/200mcg	DPI: 1 inhalation once daily	Nasopharyngitis, upper respiratory infection, headache, oral candidiasis
Leukotriene Modifiers
Montelukast (Singulair)	T: 4 mg, 5 mg, 10 mg	A: 10 mg/day C (6–14 yrs): 5 mg/day C (2–5 yrs): 4 mg/day	Dyspepsia, increased LFT, cough, nasal congestion, headache, dizziness, fatigue
Zafirlukast (Accolate)	T: 10 mg, 20 mg	A, C (12 yrs and older): 20 mg 2 times/day C (5–11 yrs): 10 mg 2 times/day	Headache, nausea, diarrhea, infection
PDE-4 Inhibitor
Roflumilast (Daliresp)	T: 500 mcg	A: 500 mcg once daily	Headache, dizziness, insomnia

A, Adults; C (dosage), children; DPI, dry powder inhaler; HFA, hydrofluoroalkane; MDI, metered dose inhaler; NEB, nebulization; T, tablets.