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Pharm2 Lect 2

Pharm2 Adrenomimetics

QuestionAnswer
How does B2 receptors affect K+ movement in skeletal muscle? B2 are present on skeletal muscle cells and activate K/Na pumps. **Shifts K+ INTO the cell.
What can be used to treat hyperkalemia? B2 agonist
What is the cause of skeletal muscle tremor (seen in stage fright)? B2 receptors, activated with the release of EPI
Drug Info: Epi/NE 1.Low oral bioavailability. 2.Short plasma halflife. 3.Inactivated in gut/liver by MAO and COMT
Direct acting adrenomimetics: Dipivefrin 1.Mech of action: Prodrug converted to EPI. 2.From: Topicl/opthalmic agent. 3.Used to treat open angle glaucoma.
Direct acting adrenomimetics: Dopamine 1.Mech of action: Activates Dopamine,B1 & Aplha agonist. 2.Used to treat shock. 3.Adverse effects: Palpitations, tachycardia, rebound nasal congestion. 4.Contraindic: CVD, HYPERthyroid, Diabetes.
Direct acting adrenomimetics: A1 selective agonist 1.Phenylephrine (sudafed PE). 2.Metaraminol (parenteral). 3.Xylometazoline (Nasal). 4.Oxymetazoline (Nasal). 5.Midodrine (Oral). **3&4 are only nasal
3 contraindications for Direct acting adrenomimetics 1.CV Disease. 2.Hyperthyroidism. 3.Diabetes.
Adverse effects of A1 selective agonists 1.Red peripheral BF. 2.Inc BP. 3.VC at infusion site. 4.Rebound nasal congestion.
Direct acting adrenomimetics: Metaraminol 1.Mech of action: A1 agonist (Gq). 2.Parenteral. 3.Used to treat NASAL CONGESTION.
Direct acting adrenomimetics: Xylometazoline 1.Mech of aciton: A1 selective agonist (Gq). 2.Topical, Nasal. 3.Bioav: Long. 4.Used to treat NASAL CONGESTION.
Direct acting adrenomimetics: Phenylephrine 1.Mech of action: A1 selective agonist (Gq) causing VC and shrinks swollen mucosa. 2.Topical-Nasal or Skin, Oral. 3.Bioav: Short. 4.Used to treat NASAL CONGESTION, hypotension (also dilates pupil).
Direct acting adrenomimetics: Oxymetazoline 1.Mech of action: A1 selective agonist (Gq). 2.Topical, Nasal. 3.Bioav: long. 4.used to treat NASAL CONGESTION.
Direct acting adrenomimetics: Midodrine 1.mech of action: A1 agonist (Gq). 2.Oral.
Direct acting adrenomimetics: A2 selective agonists 1.Brimonidine. 2.Apraclonidine. **both are topical-eye.
Direct acting adrenomimetics: Brimonidine 1.Mech of actio: A2 agonist (Gi) Dec aq humour production & Dec IOP. 2.Topical-Eye. 3.used to treat glaucoma (no blurred vision). 4. Adverse effects: VC of vessels at infusion site.
Direct acting adrenomimetics: Apraclonidine 1.Mech of action: A2 selective agonist (Gi) Dec aq humour production & Dec IOP. 2.Topical-EYE. 3.glaucoma. 4.Adverse effects: VC of vessels at infusion site.
Direct acting adrenomimetics: Isoproterenol 1.Mech of action: Non-selective B agonist (Gs) that Inc AV node conduction via B1. 2.Parenteral. 3.Used to treat AV block. 4.Adverse effects: Palpitations, tachycardia, arrhythmias, tremor, hyperglycemia.
Direct acting adrenomimetics: Dobutamine 1.mech of action: B1 selective agonist (Gs). 2.Parenteral. 3.used to treat shock. 4.Adverse effects: Palpitations, tachycardia, arrhythmias, tremor, hyperglycemia
Direct acting adrenomimetics: B2 selective agonists 1.Albuterol. 2.Metaproterenol. 3.Pirbuterol. 4.Terbutaline. 5.Salmeterol. 6.Formoterol. 7.Arformoterol **use Gs
Direct acting adrenomimetics: Albuterol 1.Mech of action: B2 selective agonist (Gs) to relax bronchiole smooth muscle & VD them. 2.Inhalation. 3.Bioav: Short. 4.used to treat asthma/COPD. 5.Adverse effects: Palpatations, tachycardia, arrhythmias, hyperglycemia, tremor.
Direct acting adrenomimetics:Metaproterenol. 1.Mech of action: B2 selective agonist (Gs). 2.Inhalation. 3.Bioav: short. 4.Adverse effects: Hyperglycemia, tremor.
Direct acting adrenomimetics: Pirbuterol 1.Mech of action: B2 selective agonist (Gs). 2.Inhalation. 3.Bioav: short. 4.Adverse effects: Hyperglycemia, tremor.
Direct acting adrenomimetics: Terbutaline 1.Mech of action: B2 selective agonist (Gs) Inc uterine smooth muscle relax. 2.Oral, Parenteral. 3.Bioav: short. 4.used to treat asthma/COPD & Preterm labor (Parenteral only). 5.Adverse effects: Palpitations, tachycardia, arrhythmia, hypergly, tremor
Direct acting adrenomimetics: Salmeterol 1.Mech of action: B2 selective agonist (Gs). 2.Inhalation. 3.Bioav: Long. 4.used to treat asthma/COPD. 5.Adverse effects: Palpitations, tachycardia, arrhythmia, hypergly, tremor.
Direct acting adrenomimetics: Formoterol 1.Mech of action: B2 selective agonist (Gs). 2.Inhalation. 3.Bioav: Long. 4.used to treat Asthma/COPD. 5.Adverse effects: Palpitations, tachycardia, arrhythmia, hyperglyc, tremor.
Direct acting adrenomimetics: Arformoterol 1.Mech of action: B2 selective agonist (Gs). 2.Inhalation. 3.Bioav: Long. 4.Adverse effects: Hyperglycemia, tremor.
What B2 Selective agonists have a LONG bioavailability? 1.Salmeterol. 2.Formoterol. 3.Arformoterol. **all 3 are inhaled.
Key vasoconstricting therapeutic uses of Epi 1.Hemorrhage from minor cuts. 2.VC of vessels at infusion site
What is the only oral nasal decongestant? Oral phenylephrine (sudafed PE).
What A1 selective agonists have a LONG bioavailability? 1.Xylometazoline. 2.Oxymetazoline.
What is the biggest problem with chronic A1 selective agonist use? Rebound Nasal congestion. **causes a down regulation of A1 receptors on nasal mucosa which leads to congestion. After you stop taking agonist, there isnt enough endogenous NE to activate remaining receptors.
Key therapuetic uses of Epi during Anaphylaxis 1.Histamine:VD & Angioedema, EPI: A1 VC capillaries. 2.Histamine: Bronchoconstr, EPI: B2 Bronchodil. 3.Histamine: Pruritus & Urticaria, EPI: B supress release of mediators from mast cells. 4.Histamine: Hypotension, EPI: A1+B1 Inc BP.
What Direct acting adrenomimetics would be best to treat Hypovolemic shock? DOPAMINE: 1.Dopaminergice receptors on renal vasculature Inc renal BF (VD). 2.B1 receptors Inc CO & BP (RAAS). 3.A1 receptores Inc PVR & BP.
What Direct acting adrenomimetics would be best to treat Cardiogenic shock? (Heart isnt pumping/beating enough) DOBUTAMINE: 1.B1 receptors on heart will Inc CO, HR, and BP.
What Direct acting adrenomimetic would be best to treat distributive shock? (excessive VD, septic) NE: 1.A1 receptors would cause Inc PVR & BP. **better than dopmaine b/c volume is fine, bad for cardiogenic since it would only Inc Afterload.
Created by: WeeG
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