Pharmacology Test 2 L5 Adrenergic Stimulants

Front 1

What receptors does NE act on?

Back 1

Alpha and B1 (NOT B2!!!)

Front 2

Where does epinephrine get released from?

Back 2

adrenal medulla

Front 3

What receptors does epinephrine act on?

Back 3

alpha 1/2 and beta 1/2

Front 4

What do sympathomimetic drugs do to blood vessels of the skin, kidney, muscous? what receptor?

Back 4

When stimulated,
This leads to constriction of these vessels

Alpha 1

Front 5

What do sympathomimetic drugs do to Skeletal muscle blood vessels? what receptor?

Back 5

Relaxation in skeletal muscle BV's

B2 receptor

Front 6

What do sympathomimetic drugs do to to sweat and salivary glands?

Back 6

increase secretion, Alpha receptors/muscarinic

Front 7

What do sympathomimetic drugs do to smooth muscle of GUT and Bronchial tree? Receptor?

Back 7

These cause Relaxation-
using B2 (B2 agonists are asthma drugs)

Front 8

What do sympathomimetic drugs do to the Heart? receptors?

Back 8

B1/B2
Increases rate/ force of contraction

Front 9

What do sympathomimetic drugs do to in the liver? receptors?

Back 9

B2/B3
increases glycogenolysis

Front 10

What do sympathomimetic drugs do to Insulin and Renin?

Back 10

these modulate their release via B1/A1/A2 receptors

Front 11

What do sympathomimetic drugs do to NT release?

Back 11

inhibits NT release from presynaptic A2 receptors

Front 12

How can you prevent drugs that act indirectly via NE?

Back 12

you can deplete the stores, or remove the presynaptic neuron

Front 13

What does the drug Reserpine do?

Back 13

this depletes NE stores

Front 14

What do alpha receptors respond to best?

Back 14

Epinephrine > NE >>isoproterenol

Front 15

What do Alpha 1 receptors do? mechanism?

Back 15

these are excitatory

Gq linked- (IP3/ DAG)

Front 16

What do alpha 2 receptors do? mechanism? where found?

Back 16

these are inhibitory
found presynaptically

reduces NT release via Gi (lowers cAMP)

Front 17

What is the selective agonist against Alpha 1 receptors?

Back 17

Phenylephrine

Front 18

What does alpha 1 receptor stimulation do to peripheral vasculature?

Back 18

this causes Vasoconstriction (selective agonist is phenylephine)

Front 19

What does alpha 1 receptor stimulation do to nasal mucosa vasculature?

Back 19

this causes vasoconstriction, reducing nasal congestion
(selevtive agonist is phenylephrine)

Front 20

What does alpha 1 receptor stimulation do to the eye?

Back 20

this causes mydriasis (dilation)

Front 21

What does alpha 1 receptor stimulation do to surface hairs?

Back 21

this causes erection of the hair

Front 22

What is the selective agonist against Alpha 2 receptors?

Back 22

Clonidine

Front 23

What does alpha 2 receptor stimulation do to presynaptic nerve terminals?

Back 23

This inhibits NT release
(clonidine)

Front 24

What does alpha 2 receptor stimulation do to vascular smooth muscle?

Back 24

contraction

Front 25

What does alpha 2 receptor stimulation do to insulin?

Back 25

this decrease insulin release a little bit (via clonidine)

Front 26

Does NE have an effect on B2 receptors?

Back 26

No it doesnt

Front 27

What kind of affinity do NE and Epi have for B1 receptors?

Back 27

these are about equal

Front 28

What drug has a very high affinity for ALL B receptors?

Back 28

Isoproterenol

Front 29

What is the mechanism of ALL B receptors?

Back 29

these are all Gs,- which activates adenylyl cyclase, and increases cAMP

Front 30

What is the main receptor type found in the lung?

Back 30

B2- so NE does NOT affect the lung

Front 31

what is the main receptor type found in a majority of blood vessels?

Back 31

Alpha receptors- (so isoprotenernol, the B receptor agonist, cannot affect blood vessels)

Front 32

What are the two main actions of B1 receptors? (based on their locations)

Back 32

Heart/ Kidney
Increases heart contraction/rate

and increases renin secretion from kidney (increases BP??)

Front 33

What is the selective agonist against B1 receptors?

Back 33

Dobutamine

Front 34

What is the selective agonist against B2 receptors?

Back 34

Albuterol (as B2 is found in the lungs...)

Front 35

what is the action of B2 agonism in Respiratory and uterine Smooth Muscle?

Back 35

this causes relaxation

Front 36

what is the action of B2 agonism in blood vessels that supply skeletal muscle?

Back 36

this cause relaxation of these

Front 37

what is the action of B2 agonism against potassium in skeletal muscle?

Back 37

this increase potassium uptake

Front 38

what is the action of B2 agonism in the liver?

Back 38

glycogenolysis

Front 39

What do B3 receptors do when stimulated?

Back 39

these increase lipolysis

Front 40

What does D1 receptor activation lead to?

Back 40

this causes dilation of renal blood vessels

done by stimulating adenylyl cyclase

Front 41

What does D2 receptor activation lead to?

Back 41

this inhibits release of NT's
inhibits adenylyl cyclase

Front 42

What is the backbone for catecholamines?

Back 42

phenylethylamine

Front 43

What are the four catecholamines?

Back 43

NE, Epi, isoproterenol, Dopamine

Front 44

How are catecholamines administered? why?

Back 44

these are given IV, because they are inactivated by the intestinal mucosa

Front 45

How does changing the size of the basic catecholamine affect its receptor selectivity?

Back 45

adding size, makes it more selective for B receptors

Front 46

What can you do to the basic phenylethylamine to inhibit its breakdown by MAO?

Back 46

substitiute something on the alpha carbon

Front 47

are ephedrine or amphetamine catecholamines?

Back 47

No they are not

Front 48

What does alpha receptor stimulation do to small blood vessels?

Back 48

these become constricted- leading to an increase in arterial resistance

Front 49

What does alpha receptor stimulation do to BP?

Back 49

this increases BP, by increasing constriction of peripheral blood vessels

Front 50

What does alpha receptor stimulation do to the eye?

Back 50

Mydriasis- via pupillary dilator muscle. does NOT affect accommodation

Front 51

What does alpha receptor stimulation do to aqueous humor?

Back 51

this increases removal of aqueous humor, can be used to treat glaucoma

Front 52

What does alpha receptor stimulation do to upper airway/ mucous membranes?

Back 52

these have A1 receptors, and when stimulated cause vasoconstriction (just like in the periphery)

this dries up the nose and such

Front 53

What does alpha receptor stimulation do to GI tract?

Back 53

this causes Minor smooth muscle relaxation

Front 54

What does alpha receptor stimulation do to GU?

Back 54

these constrict the bladder base/urethral sphincter- promotes urinary retention

Front 55

What kind of receptors are needed for ejaculation?

Back 55

alpha receptors

Front 56

What does alpha receptor stimulation do to fat cells?

Back 56

Alpha 2 receptor stimulation inhibits lipolysis

(while B3 increase lipolysis)

Front 57

What does alpha receptor stimulation do to insulin and renin secretion?

Back 57

this decreases secretion (opposite of B1 for the kidney)

Front 58

What does beta receptor stimulation do to the heart?

Back 58

this causes increased conduction and increased contractility

Front 59

What does beta receptor stimulation do to skeletal muscle BV's?

Back 59

this causes dilation via B2 receptors in skeletal BV's

Front 60

What does beta receptor stimulation do to the eye?

Back 60

this increases aqueous humor production

Front 61

What does beta receptor stimulation do to respiratory tract?

Back 61

this uses B2 receptors to relax bronchial smooth muscle- treats asthma

Front 62

What does beta receptor stimulation do to GU tract?

Back 62

this relaxes the uterus mainly

Front 63

What does beta receptor stimulation do to renin secretion?

Back 63

this increases it via B1 receptors

Front 64

What does beta receptor stimulation do to the liver?

Back 64

increases glycogenolysis in the liver

Front 65

What does beta receptor stimulation do to insulin secretion?

Back 65

this increases insulin release a little bit, via B2 receptors

Front 66

What is the main effect of Phenylephrine? What receptor?

Back 66

Alpha 1 selective agonist

causes vasoconstriction peripherally

Front 67

What is the main effect Isoproterenol? What receptor?

Back 67

B1 and B2 agonist

increases rate and force of contraction in heart.
Also causes vasodilation in skeletal muscle (via B2)

Front 68

What receptors does Norepinephrine stimulate?

Back 68

Alpha and B1 (NO beta 2!)

Front 69

What does administration of Noreepinephrine do?

Back 69

this causes vasoconstriction peripherally via A1 receptors. increases peripheral resistance

The B1 receptor effect is minor, as the baroreceptor reflex decreases HR in response to increases BP

Front 70

What receptors does Epinephrine act on?

Back 70

Alpha 1, B1 B2

Front 71

What effects does low dose of epinephrine administration produce?

Back 71

B1- gives positive inotropic and chronotropic effects

Alpha 1- causes vasoconstriction (peripherally)

B2- causes skeletal BV dilation

Overall- increases HR/Pulse pressure

Front 72

What negative effect can NE administration (B1 and Alpha receptors) have when injected?

Back 72

This can cause excessive vasoconstriction that leads to necrosis (via Alpha 1 receptors)

Front 73

What does coadiministration of NE and Atropine lead to?

Back 73

this causes much increased BP.
NE's- B1/A1 will increase HR (B1), and vasoconstriction (A1)

Atropine will block the vagal baroreflex that would normally slow the heart (atropne is a muscarinic antagonist)

Front 74

What receptors does Epinephrine work on

Back 74

Alpha, B1, B2

Front 75

What does a low dose of Epinephrine do? (many effects)

Back 75

B1- increased HR/conduction

B2- increased blood flow to muscles (increases pulse pressure by lowing diastolic pressure)

Alpha- Peripheral vasoconstriction

Front 76

What does a a rapid infusion of Epinephrine do?

Back 76

his has a marked pressor effect (a1 vasoconstriction)

Front 77

What are the side effects of epinephrine ?

Back 77

tremor
throbbing headage, increased BP, tachycarida

Front 78

Why does epi cause angina in some people?

Back 78

it will increase the work of the heart by stimulating the B1/B2 receptors (and alpha 1)
this increases the O2 demands of the heart

Front 79

What do low doses of epi do to B receptors on BV's?

Back 79

this causes vasodilation

Front 80

What do High doses of epi do to A receptors in BV's?

Back 80

this causes vasoconstriction

Front 81

What toxic effects can a large injection of Epi cause?

Back 81

extreme blood pressure increase- leading to cerebral hemorrhage, or ventricular arrhythmias

Front 82

What bad things can happen with Epi injection, while on Beta Blockers?

Back 82

this will lead to uninhibited Alpha 1 activation (massive vasoconstriction)

Front 83

What prodrug is Ephedrine like?

Back 83

this is like Epinephrine (should be easy- ephedrine/epinephrine)

Front 84

What receptor does Phenylephrine exclusively act on?

Back 84

This is an Alpha 1 Selective Agonist

Front 85

What is the effect of Phenylephrine?

Back 85

Alpha 1 selective agonism= Increased BP, followed by reflex bradycardia

Front 86

What does pesudoephedine do?

Back 86

this is an Alpha Agonist (looks like all P-eph somethings, (pseudoephedrine/phenylephrine) are all ALPHA agonists)

Front 87

What do Xylometazoline and Oxymetazoline do?

Back 87

Oxymetazoline is Afrin- which inhibits Alpha 2- and causes nasal vasoconstriction to dry out your nose

Front 88

What do drugs ending in Zoline do?

Back 88

these are alpha agonists- used for vasoconstriction mostly

Front 89

What receptor does Clonidine work on? where?

Back 89

this is a selective Alpha 2 Agonist in the brain (presynaptic alpha 2s!!)

Front 90

What is the effect of Clonidine administration in the brain?

Back 90

this acts on alpha 2's in the brain, causing a decrease in NE release globally- REDUCES sympathetic outflow

Front 91

What is the effect on the body after Clonidine administration?

Back 91

Decreased SNS outflow.

So lower BP, reduces cravings

Front 92

What are the side effects of Clonidine?

Back 92

dry mouth, sedation, and sexual dysfunction

Front 93

What are the precautions of using a Clonidine patch?

Back 93

if you get the patch too hot- you can have a massive clonidine release, causing severe Hypotension

Front 94

What receptor does methyldopa act on?

Back 94

this acts on Alpha 2 receptors in the brain

Front 95

What receptor does Araclonidine, and brimonidine act on?

Back 95

these are used in the eye- Alpha 2, and decreases Aqueous humor production due to vasoconstriction

Front 96

What receptor does Tizanidine act on? what does it treat?

Back 96

this is an alpha 2 agonist -
treats muscle spasms

Front 97

What receptors is Isoproterenol very effective against?

Back 97

B1 and B2 agonist- VERY selective

Front 98

What does Isoproterenol administration do to the heart?

Back 98

B1/B2 agonist- cause increase in rate/force of contraction of the heart

B2- some vasodilation

Front 99

What does isoprotenrenol administration do to BP/HR?

Back 99

this will drop BP due to B2- vasodilation

HR will be responsive tachycardia

Front 100

What receptors does Dobutamine work on?

Back 100

this is a selective B1 agonist

Front 101

What is Dobutamine used for?

Back 101

this selective B1 agonist is used in cardiac stress tests, its short half like of 2 min is good.

Front 102

What is Ritrodine used for? what receptor?

Back 102

Selective B2 agonist- used to relax the uterus

Front 103

What are albuterol, pibuterol, and salmeterol used for? receptor?

Back 103

these are selective B2 agonists, that cause bronchodilation in asthma pts

Front 104

What do low doses of Dopamine do? what receptor?

Back 104

this act on the D1 receptor in the renal vascular bed. (D1 is Gs- increases cAMP)

this increases glomerular filtration, and sodium excretion

Front 105

what do high doses of Dopamine do? what receptor?

Back 105

high doses stimulate the B1 receptor- causing a positive inotropic/chronotropic effect

Front 106

What are the side effects of Dopamine administration?

Back 106

nausea and vomiting

Front 107

What receptor does Fenoldopam affect?

Back 107

D1

Front 108

What does Fenoldopam administration do?

Back 108

this causes a decrease in blood pressure due to drop- due to dilation of renal vascular beds

Front 109

What is Amphetamines method of action?

Back 109

this is indirect- causes NE release, by displacing them from vesicles

Front 110

What are the CNS effects of amphetamines?

Back 110

this is a CNS stimulant, causes alertness, decreases need for sleep, appetitie, and euphoria!

Front 111

What are the cardiac effects of amphetamine?

Back 111

this causes tachycardia (NE B1) and hypertenstion (NE B1)

Front 112

How is methamphetamine different then amphetamine?

Back 112

this has more central actions

Front 113

What is the brand name of Methylphenidate?

Back 113

Ritalin- used for ADHD

Front 114

What is the mechanism of action of Cocaine?

Back 114

this inhibits Re-Uptake of DA and NE into nerve terminals (NET)

Front 115

What are the cardiac effects of Cocaine?

Back 115

hypertension, stroke, arrhythmia, myocardial infarction

Front 116

What are the long term effects of cocaine use?

Back 116

psychosis

Front 117

What does Tyramine do?

Back 117

this displaces NE from vesicles

Front 118

What metaboizes Tryamine?

Back 118

MAO in the gut, but if your on an MAOI- injesting tyramine can cause a massive NE release- and HTN