Adrenergic drugs

Question 1

Effects of Epi on vascular tone

Answer 1

Increase systolic BP

May decrease disatolic BP and total PVR

Vascular constriction in skin vessels and mucous membranes

Vascular dilation or constriction in skeletal muscle

Question 2

What are the non-selective α-adrenoreceptor antagonists?

(direct acting antiadrenergic drugs)

Answer 2

Phentolamine

Phenoxybenzamine

Question 3

Effects of beta-blockers on blood vessels

Answer 3

Initial rise in PVR

Chronic use leads to a decrease in PVR which lowers BP in hypertensive individuals

Question 4

What direct acting adrenomimetics are mixed alpha and beta agonists?

Answer 4

Norephinephrine (Levophed**)

Epinephrine (Adrenalin)

Question 5

Effects of isoproterenol

Answer 5

Positive inotropic and chronotropic action, increases CO (β1)

Vasodilator, decreases arterial pressure (β2)

Bronchodilation (β2)

Question 6

Effects of Clonidine

Answer 6

Decreases sympathetic outflow, reduces BP, bradycardia by acting on the lower brainstem area

Regulates release of NE by binding to presynaptic α₂ receptors

Question 7

Effects of beta-blockers on the respiratory system

Answer 7

increase airway resistance

Question 8

α2 receptor type activation utilizes what type of GPCR?

Answer 8

Gi

Question 9

Effects of Epinephrine on cardiac function

Answer 9

Increase force of contraction

Increase HR

Increase conduction velocity of AV node

Question 10

What direct acting adrenomimetics are beta agonists?

Answer 10

Dobutamine β₁ > β₂

Isoproterenol β₁ = β₂

Albuterol (Ventolin) β₂ > β₁

Question 11

Locations of α1 adrenoreceptors

What is the outcome of receptor activation?

Answer 11

Most vascular smooth m.
Pupillary dilator m.
Prostate
Heart

Contraction

Question 12

Effects of Dopamine

Answer 12

D1 receptors lead to vasodilation

D2 receptors suppress NE release

Question 13

What dopamine receptors utilize Gi GPCRs?

Answer 13

D2, D3 and D4

Question 14

What drug is an inhibitor of norephinephrine release?(indirect acting antiadrenergic drugs)

Answer 14

Guanethidine

Question 15

What are the non-selective β-blockers? (direct acting antiadrenergic drugs)

Answer 15

Propranolol

Pindolol

Nadolol

Question 16

What are the α₁ selective α-adrenoreceptor antagonists?

Answer 16

Prazosin

Tamsulosin

Doxazosin

Question 17

Locations of α2 adrenoreceptors (action)

Answer 17

Postsynaptic CNS neurons

Platelets (aggregation)

Adrenergic OR cholinergic nerve terminals (inhibits NT release)

Some vascular smooth m.

Fat cells (inhibits lipolysis)

Question 18

Location of β2 adrenoreceptors

Answer 18

Respiratory, uterine and vascular smooth m. (relaxation)

Skeletal m. (K+ uptake)

Human liver (activate gluconeogenesis and glycogenolysis)

Question 19

Effects of phenylephrine

Answer 19

mydriatic and decongestant

severe vasoconstriction and subsequent increase in BP

severe bradycardia

Question 20

Location of β1 adrenoreceptors (action)

Answer 20

Heart ( + inotropy, + chronotropy)

Juxtaglomerular cells (increase renin release)

Question 21

Indirect adrenomimetic that is a releasing agent and a direct adrenergic receptor agonist

Answer 21

Ephedrine

Question 22

What are the mixed blockers?

(direct acting antiadrenergic drugs)

Answer 22

Labetalol (β and α₁ antagonist)

Carvedilol (β and α₁ antagonist)

Question 23

Adverse effects of adrenergic agonists

Answer 23

Elevated BP

Increased cardiac work leading to MI or HF

Sudden death d/t arrhythmias

Insomnia

Lack of appetite

Anxiety

Psychoses, convulsions

Hemorrhagic stroke

Question 24

Effects of Epi on respiratory system

Answer 24

Relaxes bronchial smooth m. (β2)

Decreases bronchial secretion and congestion within bronchial mucosa (α1)

Question 25

Effects of Phenelzine and Selegiline

Answer 25

Inhibit MAO and increase NE stores in CNS Antidepressant action

Question 26

Effects of Epi on skeletal m.

Answer 26

Tremor (β2) Increase K+ uptake (β2)

Question 27

Indirect acting adrenomimetics that reverse NE and DA uptake mechanisms and increase their release

Answer 27

Amphetamines Methylphenidate *(Ritalin)* Tyramine (a byproduct of tyrosine metabolism, **not a drug**)

Question 28

β receptor type activation utilizes what type of GPCR?

Answer 28

Gs

Question 29

Location of D1 receptors

Answer 29

Smooth m. (dilates renal blood vessels)

Question 30

Adverse effects of alpha antagonists

Answer 30

Postural HoTN Tachycardia Retention of fluid and salt Impaird ejaculation Nasal stuffiness

Question 31

Clinical use of beta blockers

Answer 31

HTN Angina pectoris MI Cardiac arrhythmias HF Glaucoma Hyperthyroidism

Question 32

What is the receptor preference for phenylephrine?

Answer 32

α1 \> α2 \>\>\>\> β

Question 33

Effects of Dobutamine

Answer 33

Potent inotropic action Has α1 receptor activity (can act as an agonist or antagonist)

Question 34

Effects of Tyramine

Answer 34

Releases stored NE from presynaptic terminals May increase BP in patients taking MAO inhibitors

Question 35

Adverse effects of beta-blockers

Answer 35

Sedation Sleep disturbances Depression Increase airway resistance Bronchospasms Decrease HR and contractility Hypoglycemic episodes

Question 36

Clinical use of alpha antagonists

Answer 36

Pheochromocytoma Chronic (essential) HTN ED BPH

Question 37

Effects on beta-blockers on the heart

Answer 37

Negative inotropic effect Negative chronotropic effect Slow AV node conduction

Question 38

What dopamine receptors utilize Gs GPCRs?

Answer 38

D1 and D5

Question 39

What are the β₁ selective β-adrenoreceptor blockers?(direct acting antiadrenergic drugs)

Answer 39

Metopr**_olol_** Betax**_olol_** Acebut**_olol_** Aten**_olol_**

Question 40

What direct acting adrenomimetics are dopamine agonists?

Answer 40

Dopamine

Question 41

What drug is an inhibitor of tyrosine hydroxylase? (indirect acting antiadrenergic drugs)

Answer 41

Metyrosine

Question 42

What drug is an indirect acting adrenomimetic that inhibits re-uptake of dopamine and norepinephrine?

Answer 42

Cocaine

Question 43

Effects of NE

Answer 43

Reduces HR Potent vasoconstrictor NO bronchodilation and vasodilation Increases PVR and BP

Question 44

Location of D2 receptors

Answer 44

Nerve endings (modulate NT release)

Question 45

What is the receptor preference of NE?

Answer 45

α1 = α2 β1 \>\> β2

Question 46

What drugs are indirect acting adrenomimetics that inhibit MAO (monoamine oxidase)?

Answer 46

Selegiline Phenelzine

Question 47

Effects of Albuterol

Answer 47

Bronchodilation Relaxation of uterus

Question 48

α1 receptor type activation utilizes what type of GPCR?

Answer 48

Gq

Question 49

What direct acting adrenomimetics are alpha agonists?

Answer 49

Phenylephrine (α₁ \> α₂) Clonidine (α₂ \> α₁)

Question 50

Location of β3 adrenoreceptors

Answer 50

Bladder (relaxes detrusor m.) Fat cells (activation of lipolysis)

Question 51

What is the receptor preference for Clonidine?

Answer 51

α2 \> α1 \>\>\>\> β

Question 52

Effects of beta-blockers on the eye

Answer 52

Reduced intraocular pressure through reduced production of aqueous humor

Question 53

Clinical use of Ephedrine

Answer 53

Nasal decongestant Increase BP Stress incontinence in women

Question 54

Clinical use of adrenergic agonists

Answer 54

Hypotensive emergencies Chronic hypotension Cardiogenic shock HF HTN Cardiac arrest or complete AV block Narcolepsy ADHD Obesity Asthma Decongestion Anaphylaxis