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36 Cards in this Set
- Front
- Back
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504 PHARM SYMPATHOMIMETIC DRUGS
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504 PHARM SYMPATHOMIMETIC DRUGS
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Alpha 1 receptors
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Increase IP3 and DAG
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Alpha 2 receptors
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Decrease cAMP
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Beta 1 and Beta 2 receptors
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Increase cAMP
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Tissue distribution of Beta 1
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Cardia muscle
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Tissue distribution of Beta 2
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Skeletal muscle and
Smooth muscle Liver |
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For Alpha 1
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Vascular smooth muscle
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What receptors are distributed in the CNS?
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All of them (alpha 1,2 and beta 1,2)
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Epinephrine activates which receptors?
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Alpha and Beta, but mainly Beta.
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What is EPI mainly used for?
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Treatment of:
1. cardiac arrest 2. acute bronchospasm 3. shock |
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How is epinephrine given?
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IM or IV or Inhaled.
NOT orally! |
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What is the effect of epi on the lungs and heart?
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Lungs: bronchodilation
Heart: Increase CO and BP Increases blood glucose level |
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How does epi increase BP?
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By:
1. increase HR 2. increase strength of contraction. 3. vasoconstriction in vascular beds. |
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In general, what effect do alpha and beta receptor activation have on vessels?
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Alpha: vasoconstriction
Beta: vasodilation Thus, LOW conc of epi may actually cause vasoDILATION due to preferential Beta receptor activation. At high epi conc, alpha activation overrides the effect of beta activation, and net effect is vasoCONSTRICTION. |
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What receptor does Dobutamine selective for?
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Beta 1 agonist
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What is Dobutamine commonly used for?
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Tx of shock and cardiac arrest
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How is Dobutamine given?
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IM or IV
NOT orally! |
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What receptor is Albuterol selective for?
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Beta 2 agonist
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What is Albuterol commonly used for?
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Tx of asthma
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Side effects of Albuterol?
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Tachycardia and skeletal muscle tremor.
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What receptor is Phenylephrine selective?
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Alpha 1 agonist
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What receptor is Phenylephrine (neosynephrine) selective for?
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Alpha 1 agonist
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What is Phenylephrine used for?
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As a decongestant
A potent vasoconstrictor (decreasing the vol of nasal mucosa) |
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Phenylephrine is contraindicated for?
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HTN
Use of MAO |
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What receptor is Clonidine selective for?
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Alpha 2 agonist
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What is Clonidine used for?
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Tx of HTN
NOTE: this seems counter intuitive since alpha receptor stimulation causes vasoconstriction. However, clonidine exerts its hypertensive effect via alpha 2 receptors in the CNS which suppresses sympathetic activation. |
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Phenelzine's function?
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Inhibits Monoamine Oxidase (MAO) activity.
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What does MAO inhibitors do?
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Increase the action of catecholamines by slowing down its degradation.
Therefore, are indirectly acting sympathomimetic drugs. |
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What is Phenelzine used to treat?
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Depression
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What is the potential fatal crisis of Phenelzine?
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HTN
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What is the trade name for Methylphenidate?
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Ritalin
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What is the action of Methylphenidate?
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Cause catecholamine release, therefore, are indirectly acting sympathomimetic drugs.
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What is Methylphenidate used to treat?
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Tx deficit disorder (ADHD)
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Side effects of Methylphenidate?
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Mild HTN
Tachycardia Insomnia GI problems |
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What is the action of Pseudoephedrine?
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Amphetamine like drug
Bind to transporters and cause catecholamine release. Indirect acting sympathomimetic drug |
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What is the major difference between pseudoephedrine and amphetamine?
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Pseudoephedrine does not cross the blood brain barrier.
Therefore, few CNS side effects. |
