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41 Cards in this Set
- Front
- Back
What receptors do EPINEPHRINE act on?
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a1, a2, B1, B2
B1 receptor is most sensitive to epi at LOW [ ]'s (B LOW) |
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What are the clinical uses of EPINEPHRINE?
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Cardiac stimulant.
Prevents superficial bleeding from small arterioles or capillaries. Prevents spread of local anesthetics. Bacterimic shock. Anaphylactic shock. Asthma. |
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What are the toxic effects of EPINEPHRINE?
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1. tremor
2. CNS - anxiety, headache, fear 3. Cerebral hemorrhage 4. Cardiac dysrhythmias |
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How is EPI usually administered?
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Patenterally by inhalation and by topical administration
NOT ORALLY |
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Does EPI cross the BBB?
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NO, b/c it is very polar
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How is the action of EPI terminated?
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MAO, COMT, Uptake 1 and Uptake 2
mostly by Uptake 1 |
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What are the metabolic actions of EPI?
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1. increase body temp and O2 consumption (calorigenic effect)
2. increase blood concentration of glc, lactic acid, K+, FFA, glycerol |
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What receptor does NE act on?
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a1, a2 > B1 agonist
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What receptor does PHENYLEPHRINE act on?
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a1 agonist
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What are the clinical uses for PHENYLEPHRINE?
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1. Allergic Rhinitis (b/c its a nasal decongestant)
2. Mydriatic 3. reduces aqueous humor and intraocular pressure 4. maintains BP during general and local anesthetic |
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What receptors does ISOPROTERENOL act on?
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B1 and B2
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What is the clinical use of ISOPROTERENOL?
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powerful cardiac stimulant
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What is the side effect of ISOPROTERENOL?
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arrhythmias
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What receptor does ALBUTEROL, TERBUTALINE, SALMETEROL, FORMOTEROL, and RITODRINE act on?
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B2
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Which two B2 agonists prevent premature uterine contractions?
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Terbutaline and Ritodrine
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Which two B2 agonist are long acting drugs that prevent asthmatic attacks?
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Salmeterol and Formoterol
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What B2 agonist is a short acting drug used in acute asthma attacks?
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Albuterol
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What are the toxic effects of B2 Agonists?
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1. Tachycardia
2. Tremor 3. Hyperglycemia 4. Hypokalemia |
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ISOPROTERENOL reduces ____________ BP
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ISOPROTERENOL reduces
__diastolic____ BP |
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What receptor does DA act on?
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DA is a selective B1 agonist
some a1,B2, D1, D2 activity |
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What does DA do at LOW doses?
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At low doses DA increases BF in renal/mesenteric vascular beds (D1 receptors) and induces vomitting (D2 receptor)
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What does DA do at MODERATE doses?
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At moderate doses DA has a positive inotropic effect on the heart (B1)
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What does DA do at HIGH doses?
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At high doses DA causes vasoconstriciton (a1)
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How is DA administered?
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IV infusion
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DA is a precursor for what?
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Epi and NE
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Is DA more or less likely to cause tachycardia and dyshythmias than isoproterenol?
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less likely
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How does DOBUTAMINE differ from DA?
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DOBUTAMINE :
1. does not increase renal or mesenteric BF 2. does not activate DA receptors in the area postrema 3. does not release NE (no local ischemia at IV injection site) |
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What is the duration of DOBUTAMINE?
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short (t1/2 is 2 min)
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What physiologic effects of a1 receptor agonists?
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vasoconstriction - increases TPR
contraction of the radial muscle -mydriasis contraction of smooth muscle (splenic capsule, sphincters) |
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What physiologic effects of a2 receptor agonists?
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inhibit release of NE,
relaxes GI smooth muscle by inhibiting the release of ACh in the enteric nervous system, reduces secretion of insulin from the pancreas, reduces outflow of the SNS and lowers BP |
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What are the physiologic effects of B1 receptor agonists?
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increase rate and force of contraction of cardiac muscle,
increase the secretion of renin from juxtaglomerular cells |
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What are the physiologic effects of B2 receptor agonists?
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dilation of the bronchioles,
inhibition of the release of inflammatory mediators from mast cells, relaxation of visceral smooth muscle (urinary bladder, GI smooth muscle), dilation of blood vessels, increases the secretion of glucagon from the pancreas, relaxation of the uterus during the 3rd trimester |
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What are the physiologic effects of B3 receptor agonists?
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activates phosphoralase - increases glc blood levels,
activates lipase - increases FFA blood levels |
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What are the physiologic effects of D1 receptor agonists?
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increases BF in the renal and mesenteric vascular beds.
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What receptors does PHENYLEPHRINE act on?
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a1>a2 agonist
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What are the clinical uses of PHENYLEPHRINE?
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opthalmic surgery (pupil dilation), vasoconstriction, neurogenic shock, allergic rhinitis, maintains BP during general and local anesthetic
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What receptor does CLONIDINE act on?
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centrally acting a2 agonist,
decreases central adrenergic outflow |
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What are the clinical uses of CLONIDINE?
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1. HTN
2.migraine headaches 3. opiate withdrawl |
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What is the mechanism of TYRAMINE?
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TYRAMINE is a catecholamine releasing agent
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What metabolizes TYRAMINE?
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MAO
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What is can happen to a person taking MAO inhibitors that ingests too much TYRAMINE?
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increase release of stored catecholamines causes an increase in BP (HTN), headache, could possible blow vessel in brain
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