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Sympathomimetcs & Parasympatholytics RC 195
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Sympathomimetics Drugs that “mimic” the actions of the sympathetic neurotransmitters Stimulate Alpha, Beta-1, and Beta-2 receptors Also known as Adrenergics or Catecholamines
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Epinephrine (Adrenalin) Note: The larger the sub-group on the terminal amine, the more Beta-2 specific the drug will be
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Epinephrine (Adrenalin) Strengths: 1:100, 1:1000, 1:10000 Actions: Alpha=3*, Beta-1=4*, Beta-2 = 2* Uses: Asthma,Bleeding/Prolonging anesthesia, Stimulating the heart and raising blood pressure during cardiac arrest
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Epinephrine (Adrenalin) Duration = 120-180 minutes Is metabolized by COMT R & D: Aerosol, Sub-Q, IV Aerosol dose is.25-.7ml Q4 Side effects: tachycardia, hypertension, headache, N&V, thickened secretions
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Isoproterenol (Isuprel)
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Strengths: 1% and.5% (most common) Actions: Beta-2 = 5*, Beta-1 = 4* Is the most potent beta-2 that is approved by the FDA! Also stimulates cilia No alpha stimulation
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Isoproterenol (Isuprel) Duration: 20-120 minutes Aerosol dose:.125-.5ml Q4 of.5% Can also be given IV Side effects: tachycardia (never give with epinephrine!), hypertension, agitation/tremors, N&V, headache, tolerance, and worsening of hypoxemia (!?!?)
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Racemic Epinephrine (Vaponephrin, Micronefrin) Is an isomer of epinephrine
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Racemic Epinephrine Strength: 2.25% Actions: Alpha=3*, Beta1 and 2=2* Uses: Upper Airway Inflammation Croup Smoke inhalation Post-extubation glottic and sub-glottic edema
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Racemic Epinephrine Duration: 120-180 minutes Aerosol dose:.25-.7ml Q4 Side effects: tachycardia, headache, hypertension, N&V, agitation/tremors, drying of mucosa and secretions
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Isoetharine (Bronkosol, Bronkometer)
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Strength: 1% Actions: Beta-2=3*, Beta-1=1* Duration: 90-180 minutes Aerosol dose:.25-1ml Q4 Dilution should be 1:3 Side effects: Headache,hypertension, tachycardia, N&V, tremors/agitation Turns brown when its too old to use Turns clear sputum pink
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Metaproterenol (Alupent, Metaprel)
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Metaproterenol (Metaprel, Alupent) Strength: 5% Actions: Beta-2=4*, Beta-1=1 or 2* Duration: 2-6 hours Aerosol dose:.2-.3ml Q4 Side effects: tachycardia, headache, N&V, tremors and agitation
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Terbutaline (Breathine)
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Strength:.1% Actions: Beta-2=4*, Beta-1=2* Also stimulates cilia Duration: 3-7 hours R&D:Usually oral or sub-Q; if aerosolized give.25-2.5 mg Q4-Q8 Side effects: Like Metaproterenol; tremors and agitation may be prominent Severe agitation seen when administered to children
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Albuterol/Salbutamol (Proventil, Ventolin)
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Strength:.5% Actions: Like Metaproterenol and Terbutaline Duration: 4-6 hours R&D: Oral, IV and Aerosol Aerosol dose is.5ml of.5% Q4-6 Side effects: Like Metaprel and Terbutaline but usually not as severe
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Levo-Albuterol (Xopenex) An isomer of Albuterol/Salbutamol that has even less side effects than Albuterol and may have a longer duration in some patients
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Fenoterol (Berotec)
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Strength:.5% Actions: Beta-2 =4*, Beta-1=1* Duration: up to 8 hours R&D: Oral and Aerosol Aerosol dose is.5ml of.5% Q6-8 Minimal side effects Is not legal in the USA!
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Ephedrine Old time drug that is similar to epinephrine Active ingredient in many “combo” drugs: Quibron,Tedral, Marax Stimulates all sympathetic receptors equally and weakly Taken orally (not aerosolized) Not used much now because of (1)minimal beta-2, (2) CNS stimulation, (3), tolerance
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Bitolterol (Tornalate)
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Activated by esterases in lung and becomes colterol May last up to 8 hours Usually aerosolized by MDI 2-3 puffs Q4-6 May cause tremors and agitation Always watch for any Beta-1 effects
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Pirbuterol (MaxAir)
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Good beta-2 (like Albuterol) but comes on quickly (within 5 minutes) Duration: 5 (sometimes 6) hours Given by breath-activated MDI
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Salmeterol (Serevent)
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Very long-acting: 12 hours Administered BID via MDI Is for prevention, not relief!
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Formoterol (Foradil) Similar to salmeterol Lasts for 12 hours Given from a breath activated dry powder inhaler
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Carbuterol and Clenbuterol New bronchodilators not yet approved by the FDA
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Phenylephrine Pure alpha stimulant (5*) Used for rhinitis (decongestant effect) Side effects due to alpha stimulation: Hypertension Headache Mucosal drying Rebound congestion
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Parasympatholytics (Anticholinergics) Blocking the parasympathetic (cholinergic) system is similar to stimulating the sympathetic (adrenergic) system
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Atropine Actions: cholinergic blockade Decreased c-GMP so decreased bronchospasm and decreased mast cell degranulation May potentiate beta-2 activity of sympathomimetics Decreased secretions (secretions may get thick and dry) May also be helpful in rhinitis Aerosol dose is 1 mg of 1% Q4-6 Side effects: tachycardia, dry mouth and dry thick secretions, ataxia
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Ipratropium Bromide (Atrovent) Like Atropine but seems to have less side effects and lasts a little longer Can be nebulized or given via MDI Often given with sympathomimetics either concurrently or alternating Seems to be very effective in COPD patients who have “twitchy airways”
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Tiotropium Bromide (Spiriva) Like Atrovent, but only taken once per day Very good with COPD
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Glycopyrrolate (Robinul) Like Atropine and Atrovent Usually only via nebulizer; 1 mg Q4-6
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