Adrenergic Pharmacology Flashcards

Question

**norepinephrine (Levophed)** Advantages Precautions, adv reactions, interactions

Answer 1

**Advantages** acts quick and for a short period of time Preferred to epinephrine, dobutamine, vasopressine, but any of those works. However, dopamine which was traditionally used increase mortality rate significantly **Precautions, adv reactions, interactions** no real contraindication in life-threatening situations

Answer 2

*Non-selective, yet favoring a1* **Clinical uses** Nasal and eye congestion Allergic conjunctivitis Phenylephrine can be used for emergency hypotension **Pharmacologic effects** vasoconstriction (a1) mydriasis (a1)

Answer 3

**Advantages** vasoconstriction is rapid and intense Oxymetazoline has the highest efficacy Phenylephrine has less central effects **Precautions, adv reactions, interactions** not for prolonged relief (\<10 days) rebound congestion (tachyphylaxis)

Answer 4

**Clinical uses** chronic orthostatic hypotension hypotension due to autonomic neuropathy **Pharmacologic effects** Vasoconstriction (α1)

Answer 5

**Advantages** **Precautions, adv reactions, interactions** safety not established sufficiently! efficacy not established sufficiently! supine hypertension, pruritus, urinary retention in 10-20% of patients

Answer 6

Selectivity Non-selective, full a1 and partial a2A High High Very low Very low Very low

Answer 7

**Clinical uses** hypertension cardiovascular symptoms of alcohol/narcotics/opioids withdrawal adjunctive to relieve pain (reduce opioid requirement) adjunctive in anesthesia (reduce anesthetic require) diarrhea **Pharmacologic effects** Decrease sympathetic drive (a2) Increase parasympathic outflow (a2) Decrease norepinephrine release (a2) Analgesia (a2) Sedation (a2) Stimulate intestin

Answer 8

**Advantages** dosing once a day **Precautions, adv reactions, interactions** may cause CNS depression may reduce attentional performance may cause sexual dysfunction in men prone to rebound hypertension at withdrawal Embryotoxic!

Answer 9

**Clinical uses** Hypertension ADHD (in children only, is not a stimulant **Pharmacologic effects** Decrease sympathetic drive (a2) Increase parasympathic outflow (a2) Decrease norepinephrine release (a2)

Answer 10

**Advantages** The a2A selectivity of Guanfacine does not impair attentional performance: clonidine and guanabenz do **Precautions, adv reactions, interactions** Caution in hypotention, cardiovascular and cerebrovascular disease, liver and renal impairement Avoid use in elderly may cause hypotension (\<10 %), bradycardia (\<2%), and sedation (5-45%) Subject to rebound hypertension Avoid combination with CYP inhibitors, sedatives, hypnotics, antidepressants, benzodiazepines

Answer 11

**Clinical uses** Moderate to severe hypertention Pregnancy-induced hypertension Severe pre-eclampsia hypertension during pregnancy **Pharmacologic effects** decrease sympathetic drive (a2) increase parasympathetic outflow (a2) decrease norepinephrine release (a2)

Answer 12

**Advantages** Not embryotoxic: clonidine, ganfacine and guanabenz are! **Precautions, adv reactions, interactions** avoid with liver and kidney diseases Avoid in elderly because of CNS and cardiovascular effects may cause liver and kidney toxicity CNS depression Hypotension and bradycardia

Answer 13

**Clinical uses** Reduction of intraocular pressure in open-angle glaucoma or ocular hypertension **Pharmacologic effects** Reduction of aqueous humor (a2)

Answer 14

**Advantages** Apraclonidine don’t cross blood-brain **Precautions, adv reactions, interactions** CNS depression (5%), especially children (25-85%) allergic conjunctivitis (\>10%), visual disturbance (5-10%), Burning sensation (5-10%) Dry mouth (5-10%)

Answer 15

Isoproterenol Low Low High High high Non-selective b **Clinical uses** cardiac resuscitation Acute heart failure **Pharmacologic effects** Cardiac stimulation (b1) Bronchodilation (b2) Vasodilatation (b2) (b3)

Answer 16

**Advantages** Efficacy better than Dobutamine, but does it worth the risks! **Precautions, adv reactions, interactions** Avoid with preexisting angina, tachyarrhythmias, coronary artery disease, diabetes, distributive shocks May cause angina, hyper/hypotension, tachyarrhythmias, hypokalemia, hyperglycemia, dypnea, pulmonary edema …. Cardiac ischemia may occur

Answer 17

**Clinical uses** Acute heart failure Cardiogenic shock **Pharmacologic effects** Cardiac stimulation (α1, b1) Vasoconstriction (α1) **Advantages** Increase cardiac output with little vasoconstriction compared to NEPI **Precautions, adv reactions, interactions** Similar to isoproterenol, but with a much lower incidence

Answer 18

**Clinical uses** asthma **Pharmacologic effects** Bronchodilatation (b2) **Advantages** Act quick **Precautions, adv reactions, interactions** tremors, restlessness hypotension, tachycardia hyperglycemia, hyperlipidemia decreases concentration of K

Answer 19

**Clinical uses** adjunctive treatment of asthma Prevention/not treatment of exertion-induced bronchospasm **Pharmacologic effects** Bronchodilatation (b2) **Advantages** Only for uncontrolled asthma Salmeterol is 10000X more lipophilic than Albuterol Formoterol has low efficacy toward internalization of the receptor **Precautions, adv reactions, interactions** Same as Albuterol May increase asthma-related death!

Answer 20

**Clinical uses** Preoperative in pheochromocytoma (both) Adjunctive treatment if pheochromocytoma is inoperable Prevention of necrosis in case of extravasation of sympathomimetics **Pharmacologic effects** hypotension (α1) vasodilatation of arteries and veins (α1) depression baroreflex (α1) **Advantages** phentolamine is reversible **Disadvantages** effects of phenoxybenzamine last more than 24 hrs hypotension, tachycardia extreame nasal stuffiness

Answer 21

**Clinical uses** benign prostate hyperplasia alternative treatment of hypertension **Pharmacologic effects** hypotension (α1) relaxation of smooth muscle (α1) depression baroreflex (α1) **Advantages** Terazosine and Doxazosin are taken once daily **Disadvantages** Prazosin needs to be taken several times/day very strong first dose effect! dizziness 50%, even syncope Nasal stuffiness Hypotension, tachycardia

Answer 22

**Clinical uses** benign prostate hyperplasia **Pharmacologic effects** relaxation of prostate smooth muscle (α1) **Advantages** Selective for prostate lesser first dose effects Alfuzosin also induce apoptosis of prostate smooth muscle **Disadvantages** Same side effects as prazosin, but in less patients and to a lesser degree

Answer 23

**Clinical uses** Adjunctive or alternative treatment of hypertension Angina pectoris tachycardia Myocardial infarction Timolol is used for intraocular hypertention Propranolol is used for situational anxiety **Pharmacologic effects** Reduction of heart rate (β1) Reduction of ventricular contraction (β1) Reduction of renin release (β1) \*Reduce aqueous humor (?) Reduce anxiety (β1 and others) **Advantages** They “work” !!! Especially propranolol Timolol may be less prone to side effects **Precautions, adv reactions, interactions** Cross BBB and cause dizziness (\<10%), insomnia (\<5%), depression (\<5%) May cause Bradycardia, Heart failure, Bronchospasms May potentiate, and mask, signs of hypoglycemia in diabetic May prevent effect of epinephrine in anaphylaxis These effects are more prevalent for propranolol

Answer 24

**Clinical uses** Adjunctive abd alternative treatment of hypertension Alternative treatment of hypertension Tachycardia Situational anxiety **Pharmacologic effects** Reduction of heart rate (partial β1 agonist) Reduction of ventricular contraction (partial β1 agonist) Reduction of renin release (partial β1 agonist) Vasodilatation ( partial β3 agonist) **Advantages** Maintains partial receptor functions Marginally affects basal, but prevents the consequence of elevated sympathetic drive Less subject to rebound tachycardia & hypertension **Precautions, adv reactions, interactions** “Lesser efficacy” than propranolol, \>\>\> yet slightly higher prevalence of side effects Insomnia (\> 10%), dizziness (\<10%), fatigue (\<10%) and depression (up to 8%)

Answer 25

**Clinical use** Adjunctive or alternative treatment of hypertension Angina pectoris Metoprolol is used in hemodynamically stable, acute myocardial infarction (iv) reduces mortality/hospitalization in patients with heart failure in patient already receiving ACE inhibitors, diuretics, and/or digoxin **Pharmacologic effect (Receptor)** Reduction of heart rate (β1) Reduction of ventricular contraction (β1) Reduction of renin release (β1) **Side effects and drug interactions** Metabolism and kinetic Hypotension, Bradychardia Dizziness or Fatigue More with Metroprolol Metoprolol cross BBB

Answer 26

**Clinical use** Intraoperative tachycardia Supraventricular tachycardia Atrial fibrillation/flutter SVT and post-operative hypertension in children **Pharmacologic effect (Receptor)** Reduction of heart rate (β1) Reduction of ventricular contraction (β1) **Side effects and drug interactions** None that will last Hypotension (less than 10%)

Answer 27

**Clinical uses** Adjunctive treatment of hypertension Alternative treatment of hypertension stable Heart failure **Pharmacologic effects** Reduction of heart rate (β1) Reduction of ventricular contraction (β1) Vasodilatation (partial β3 agonist, which activate nitric oxide synthase) Antioxidant (NADPH oxidase inhibitor) **Advantages** Well tolerated Marginally more potent than the first generation Promotes NO release (an advantage in elderly) **Precautions, adv reactions, interactions** headache (\< 10%), dizziness (\<5%), fatigue (\<5%)

Answer 28

**Clinical use** Adjunctive treatment of hypertension Alternative treatment of hypertension Hypertensive emergency Pediatric hypertension hypertension of pregnancy **Pharmacologic effect (Receptor)** Reduction of heart rate (β1) Reduction of ventricular contraction (β1) Not as much as propranolol Vasodilatation (α1) (β2) (β3) Side effects and drug interactions Hypotension (up to 58%) dizziness (up to 20%) Nausea (up to 19%) Fatigue (up to 11%) **Metabolism and kinetic** Negligible amount cross BBB

Answer 29

**Clinical use** Adjunctive treatment of hypertension Alternative treatment of hypertension Mild to severe heart failure Left ventricular dysfunction following myocardial infarction Angina pectoris **Pharmacologic effect (Receptor)** Reduction of heart rate (β1) Reduction of ventricular contraction (β1) Vasodilatation (α1) Antioxidant Anti-proliferative **Side effects and drug interactions** Dizziness (up to 30%) Fatigue (up to 24%) Hypotension (up to 20%) Weight gain and diarrhea (up to 12%) Weakness, bradychardia (up to 10%) **Metabolism and kinetic** Cross BBB