B-adrenergic Receptor Antagonists HTN

Question 1

Define Sympathetic Adrenergic nervous System

Answer 1

Increases the bodies readiness for strenuous muscular activity and “fight or flight reaction”

Question 2

SNS can make what kind of changes?

Answer 2

Increase arterial pressure, heart rate, cardiac output, blood flow to muscles and heart, respiration, oxygen consumption, blood glucose levels, glycolysis in liver and muscles and mental activity
Decreased blood flow to GI and kidneys

Question 3

Main effectors of the SNS are?

Answer 3

NE and Epinephrine

Question 4

Define NE

Answer 4

Synthesized in sympathetic nerve terminals and CNS as a neurotransmittor

Question 5

Define Epi

Answer 5

Synthesized in adrenal medulla Chromaffin cells as a hormone and in CNS as a neurotransmitter

Question 6

Who is Otto Loewi?

Answer 6

Father of neuroscience

Believe in neurotransmitters not electrical impulses

Question 7

How do you make NE and Epi?

Answer 7

Tyrosine via tyrosine hydroxylase → DOPA via DOPA decarboxylase → Dopamine via dopamine beta hydroxylase→ NE via PNMT→ Epi

Question 8

What is the rate limiting step of NE and Epi creation?

Answer 8

Tyrosine → DOPA via tyrosine hydroxylase

Question 9

Where does the synthesis of NE and Epi occur?

Answer 9

Inside the sympathetic nerve terminal

Tyrosine has to come in via transporters

Question 10

Release, action and termination of NE

Answer 10

NE is released into the synaptic cleft and binds to B1 or a1 on the postsynaptic cleft, uptaken by the postsynaptic cleft, bind to a2 or B2 or be reuptaken by receptor on the presynaptic cleft

Question 11

NE binding to B2 stimulates?

Answer 11

Release more NE

Question 12

NE binding to a2 stimulates?

Answer 12

Stop releasing NE

Question 13

NE that is taken back up into the presynaptic cleft?

Answer 13

Either is recycled and used again or inactivated by MAO and released as metabolites

Question 14

NE that is taken up into the post-synaptic cleft?

Answer 14

Is inactivated via COMT to normetanephrine and released to diffuse out

Question 15

Alpha 1 Receptors

Answer 15

Post-synaptic

Coupled to Gq which increases stuff

Question 16

Alpha 2 Receptors

Answer 16

Pre-synaptic

Coupled to Gi which decrease cAMP

Question 17

Beta 1 Receptors

Answer 17

Post-synaptic

Myocardium

Question 18

Beta 2 Receptors

Answer 18

Can be Pre or post-synaptic

SM

Question 19

NE prefers?

Answer 19

Alpha receptors

Question 20

Epi prefers?

Answer 20

Beta receptors

Question 21

NE and Epi can?

Answer 21

Bind to all 5 receptors

Question 22

Beta 3 Receptors

Answer 22

Adipose tissue

Question 23

All beta receptors are coupled to?

Answer 23

Gs which increased cAMP

Question 24

Alpha 1 Adrenoceptors expression and effects?

Answer 24

Blood vessels (arteries and veins) cause vasoconstriction and kidneys help with Na reabsorption

Question 25

Beta 1 Adrenoceptors expression and effects?

Answer 25

Heart cause + chrono, dromo and inotropic effects and juxtaglomerular cells in kidney causing renin release

Question 26

Beta 2 Adrenoceptors expression and effects?

Answer 26

SM of arterioles: vasodilation Bronchial SM: dilation and increased secretion Skeletal muscles and liver cells: glycogenolysis and gluconeogenesis Ciliary muscle: relaxation and intraocular pressure

Question 27

Beta 3 Adrenoceptors expression and effects?

Answer 27

Adipocytes: lipolysis

Question 28

Renin does what?

Answer 28

Increase BP

Question 29

Beta-Adrenoceptor Antagonists 1st Generation

Answer 29

Non-selective B1 and B2 antagonists

Question 30

Beta-Adrenoceptor Antagonists 2nd Generation

Answer 30

Selective B1 Antagonists

Question 31

Beta-Adrenoceptor Antagonists 3rd Generation

Answer 31

Non-selective and selective Beta antagonists with additional effects

Question 32

Beta-Adrenoceptor Antagonists Site of Action

Answer 32

Cardiovascular system | Profound effect when sympathetic activity is high (HTN, stress, exercise)

Question 33

Beta-Adrenoceptor Antagonists Chronotropic effect

Answer 33

Decreased heart rate

Question 34

Beta-Adrenoceptor Antagonists Ionotropic effect

Answer 34

Decreased contractile force

Question 35

Beta-Adrenoceptor Antagonists Chronotropic + Ionotropic effect =

Answer 35

Decrease cardiac output

Question 36

Short term effect of non-selective beta-blockers?

Answer 36

Decrease cardiac output → decrease BP → reflector sympathetic activation → increase NE/Epi → activation of alpha receptors → increased peripheral resistance

Question 37

Long term effect of non selective beta blockers

Answer 37

Peripheral resistance returns to initial values and CO continues to be lowered

Question 38

Beta-Adrenoceptor Antagonists Dromotropic effect

Answer 38

Decrease cardiac rhythm and automaticity which reduce sinus rate, decreases automaticity, slow conduction velocity in AV node and increased AV node refractory period All of which decreases CO

Question 39

Beta-Adrenoceptor Antagonists in HTN patients

Answer 39

Reduction of CO (Beta1) | Inhibition of renin release (Beta1)

Question 40

Beta-Adrenoceptor Antagonists in the respiratory system?

Answer 40

Bronchoconstriction and decrease secretion from bronchial glands (non-selective blockers via B2 blockade)

Question 41

Beta-Adrenoceptor Antagonists in the eyes?

Answer 41

Reduction of intraocular pressure (non-selective blockers via B2 blockade)

Question 42

Beta Adrenoceptors Antagonists in Energy metabolism and endocrine systems?

Answer 42

Decrease glycogenolysis and gluconeogenesis (non-selective blockers via B2 blockade) --> delayed recovery from hypoglycemia WATCH IN DIABETES PTS

Question 43

Beta Adrenoceptors Antagonists Uses?

Answer 43

``` HTN Angina pectoris Cardiac arrhthmias MI Glaucoma Migraine prophylaxis ```

Question 44

Beta Adrenoceptors Antagonists Name

Answer 44

End in -olol

Question 45

Beta Adrenoceptors Antagonists Adverse Reactions in CV?

Answer 45

Worse heart failure Induce life-threatening arrhthmias Worsen symptoms of peripheral vascular disease Sexual dysfunction

Question 46

Beta Adrenoceptors Antagonists Abrupt discontinuation can induce?

Answer 46

Angina pectoris (myocardial ischemia) and increase the risk of death

Question 47

Beta Adrenoceptors Antagonists Adverse Pulmonary Effects?

Answer 47

Worsen problems in asthma or COPD

Question 48

Beta Adrenoceptors Antagonists Adverse CNS Effects

Answer 48

Sedation, sleep disurbances and depression

Question 49

Beta Adrenoceptors Antagonists Adverse Metabolic effects

Answer 49

Mask hypoglycemia-induced tachycardia in diabetes | Increase plasma levels of TGs