Lippincott: Adrenergic

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Tyrosine is hydroxylated to dihydroxyphenylalaine (DOPA) by what enzyme?

Tyrosine hydroxylase

What is the rate limiting step in synthesis of NE?

Synthesis of DOPA by tyrosine hydroxylase

Reserpine blocks what?

VMAT

Guanethidine blocks what?

NE release

Cocaine and tricyclic antidepressants blocks what?

NE reuptake

EPI prefers alpha or beta receptors?

Alpha

Phenylephrine

Alpha 1

Clonidine

Alpha 2

Alpha 1 activates what secondary enzyme

Phospholipase C - IP3 and DAG. Increases Ca

Alpha 2 activates what secondary enzyme

Inhibit adenylyl cyclase. Decrease cAMP

All B activate what secondary enzyme?

Activates adenylyl cyclase, increases cAMP

Beta 2 has higher affinity for NE or EPI?

EPI

Which adrenoceptor?Vasoconstriction, increased TPR, increased BP, mydriasis, increased closure of internal sphincter of the bladder

Alpha 1

Which adrenoceptor? Inhibition of NE release, inhibition of ACh release, inhibition of insulin release?

Alpha 2

Which adrenoceptor? Tachycardia, increased lipolysis, increased myocardial contractility, increased renin release

Beta 1

Which adrenoceptor? Vasodilation, slightly decreased peripheral resistance, bronchodilation, increased release of glucagon, increased muscle and liver glycogenolysis

Beta 2

Substitution on what increases affinity for beta receptors?

Substitution on the amine nitrogen

What are the four catecholamines?

Epinerphrine, Norepinephrine, dopamine, and dobutamine

How does epi affect systolic and diastolic pressures?

Increases systolic, decreases diastolic

How does epi affect cardiovascular?

Positive inotropic (contractility) and rate (chronotropic) via Beta 1.

How does EPI affect diabetics?

Significant hyperglycemia effects

Anaphlactic shock is what type of hypersensitivit?

Type 1 hypersensitivity

How does NE affect systolic and diastolic pressures?

Increases both

How does NE affect peripheral resistance?

Constricts all blood vessels, causing increased peripheral resistance

How does EPI affect peripheral resistance?

Vasodilates, decreases it

How does NE affect baroreceptor?

Reflex bradycardia

What receptors does isoproterenol affect?

Beta 1 and 2

How does isoproterenol affect rate and contraction of heart?

Increases both.

How does isoproterenol affect systolic and diastolic pressure?

Moderate increase in systolic, markedly decrease in diastolic pressure.

How does isoproterenol affect peripheral resistance?

Significant decrease (hence decrease in diastolic pressure)

Dopamine

Raises blood pressure by stimulating Beta 1 and alpha 1 vasoconstriction, but also enhances perfusion to the kidney and splanchnic areas.

What is dobutamine used for? What receptor?

Increase cardiac output in congestive heart failure. Beta-1

Dobutamine should be used with caution in what types of patients? Why?

Atrial fibrillation patients. Drug increases atrioventricular conduction.

Nasal decongestant, terminate episodes of supraventricular tachyardia.

Phenylephrine (alpha-1 agonist)

Used for attacks of paraoxysmal supraventricular tachycardia

Methoxamine

Clonidine

Alpha 2

HTN and for withdraw from opiate drugs

Clonidine

Metaproterenol

Beta 2 agonist

Nocturnal asthma

Salmeterol and formoterol

What are three main indirect-acting adrenergic agonists?

Amphetamine, tyramine, and cocaine

Found in ripe cheese and wine

Tyramine

Tyramine

Enter nerve terminal and displace stored NE

Cocaine

Block Na/K ATPase for reuptake

Name two main mixed-action adrenergic agonists.

Ephedrine and pseudoephedrine

Which one has less CNS effect? Ephedrine and pseudoephedrine?

Pseudoephedrine

What receptor on ciliary eye muscle?

Beta 2

What drug can be used to increase cardiac output without significant increase in heart rate?

Dobutamine (only beta 1)

Mydriasis, what receptor?

Alpha 1

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