Overview of Receptors and Drugs

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Overview of

Receptors and Drugs

By Kevin Mikielski, D.O.

Department of Cardiology

Receptors and

Actions

Receptors and Actions

Alpha 1

Present on peripheral vasculature

Stimulation results in vasoconstriction

Beta 1

Present in myocardium and conduction system

Stimulation results in enhanced contractility, heart rate and speed on conduction in electrical system of heart

Beta 2

Present in skeletal muscle, lung and vasculature

Stimulation results in vasodilatation and bronchodilatation

Specific Drugs

 EPINEPHRINE

Stimulates Alpha 1

 Vasoconstriction

Stimulates Beta 1

 Increases contractility, heart rate and conduction

 Overall effect is to increase cardiac output

Stimulates Beta 2

 Vasodilates

 Bronchodilates

Will increase cardiac output through Beta 1; Usually will increase blood pressure due to Alpha 1>Beta 2

Norepinephrine

 Norepinephrine

 Stimulates Alpha 1

 In general, this is its major site of action and its major clinical use

 Stimulates Beta 1

 Stimulates Beta 2

Dopamine

 Dopamine

 Actions are dose-dependent but wide variation/range of effects are seen

 1-5 mcg/kg/min

 Stimulates dopamine receptors

 Increased renal blood flow

 Has NEVER been shown to have clinical benefit and “Renal dose dopamine” should not be used

Dopamine (continued)

 5-10 mcg/kg/min

 Primarily stimulates Beta 1 receptors

 10-20 mcg/kg/min

 Primarily stimulates Alpha 1 receptors

 Great amount of overlap between doses and effects

Dobutamine

 Dobutamine

 Stimulates Beta 1 and 2 receptors

 Not a good drug for hypotension unless the etiology is severe LV dysfunction, acute MI with cardiogenic shock, or acute pulmonary embolism where hypotension will improve with increased cardiac output

 Usually will decrease blood pressure due to Beta 2 effects

Phenylephrine / Vasopressin

 Phenylephrine (Neosynephrine)

 Stimulates Alpha 1 receptors

 No Beta effect

 Vasopressin (ADH)

 Stimulates V1 receptors and acts similar to Alpha 1 agonists, but exact mechanisms of vasoconstriction are not completely understood

 Cautious use in patients with ACS and CHF because it can result in coronary spasm and volume retention

Adenosine / Atropine

 Adenosine

Acts via Adenosine 1 receptor in conduction system to slow heart rate/SA/AV block

Need to give rapidly as bolus followed by flush due to ½ life of only 6 seconds

 Atropine

 Acts to inhibit AcH effects on conduction system

Increases sinus rate and AV nodal conduction

Does not directly increase blood pressure

End of Lecture

Thank you for your attendance.

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