HTN

Question 1

Aging in HTN

Answer 1

decreased CO + increased peripheral resistance

Question 2

Preganglionic neurons

Answer 2

primary neurotransmitter is acetylcholine

Question 3

Postganglionic neurons

Answer 3

PNS: primary is acetylcholine

SNS:
primary: norepinephrine
sweat glands: acetylcholine
adrenal medulla: epinephrine
renal: dopamine

Question 4

PSNS

Answer 4

cholinergic receptors

acetylcholine: endogenous
muscarinic: exogenous
nicotinic: exogenous

Question 5

SNS

Answer 5

adrenergic receptors

norepinephrine: endogenous
epinephrine: endogenous

Question 6

Alpha 1

Answer 6

vasoconstriction
pupillary dilation
ejaculation
gi inhibition

Question 7

Alpha 2

Answer 7

vasoconstriction
inhibit NE release
decrease CV

Question 8

Beta 1

Answer 8

cardiac stimulation
secretion of renin

Question 9

Beta 2

Answer 9

bronchodilation
uterine relaxation
gi inhibition
vasodilation

Question 10

Baroreceptor reflex

Answer 10

Decrease in BP:
-activates sympathetic fibers
-increase in HR by b1 receptors
-vasoconstriction by alpha 1
-inhibits vagus
-result: increased BP

Increase in BP:
-inhibits sympathetic fibers
-decreased HR
-activates vagus
-result: decrease in BP

Question 11

Targets for antihypertensive drugs

Answer 11

Heart: reduce CO by both PSNS and SNS
Decrease resistance of arterioles and veins
Kidneys: reduce fluids and blood volume

Question 12

Where are Alpha 1 receptors located?

Answer 12

vascular smooth muscle, genitourinary smooth muscle, intestinal smooth muscle, heart, liver

Question 13

Where are Alpha 2 receptors located?

Answer 13

CNS

Question 14

Where are Beta 1 receptors located?

Answer 14

cardiac muscle and CNS

Question 15

Alpha-1 antagonists

Answer 15

Prazosin: 3 hrs
Terazosin: 12 hrs
Doxazosin: 12 hrs

Question 16

Alpha 1 antagonists structure

Answer 16

Quinazoline ring allowing for alpha 1 specificity

Piperazine ring and acyl moiety allowing for PK activity

Question 17

Alpha 1 antagonists effect

Answer 17

Produce peripheral vasodilation without causing reflex tachycardia or increased CO–> decreased TPR

Question 18

Alpha 1 antagonists indications

Answer 18

HTN, BPH, and Raynaud’s disease

Question 19

Alpha 2 agonists

Answer 19

Inhibits the release of NE causing reduced CO from the brain

results in decreased HR, contractibility, renin release, vasoconstriction

Question 20

Clonidine (Alpha 2 agonist)

Answer 20

Imidazole drug

Contains a dichlorophenol ring that decreases the pka from 13.6 to 8.0
This creates much less charge in this compound allowing for CNS access

HTN, ADHD

oral, IV, transdermal

Side effects: hypotension, sedation, dry mouth

Question 21

Guanfacine/Guanabenz (alpha 2 agonist)

Answer 21

Open-ring imidazoline ring

Contains a 2-atom bridge to the guanidine group allowing a decrease of pka to that the drug is mostly un-ionized and allows for CNS access

contain dichlorophenol ring

HTN, ADHD

oral

Question 22

Methyldopa and Methyldopate (alpha 2 agonist)

Answer 22

Methyldopa is a prodrug that contains a Zwitterion ion between the amine and carboxylic group on the molecule allowing for less charge and easy access across BBB into CNS

Converted to alpha-methylnorepinephrine

Methyldopate contains a positive amine group on the molecule that interacts with chloride ion forming salt that is very water soluble

HTN (during pregnancy)

Methyldopa is oral and Methyldopate is IV

Question 23

Beta blockers

Answer 23

effect: decrease cardiac output and inhibits the release of renin

structure: aryloxypropanolamine: aromatic ring + bulky R group

Question 24

Propranolol

Answer 24

non-selective beta receptor antagonist
lipophilic due to large bulky group

AVOID IN PT WITH ASTHMA

Decrease CO and HR, reduce renin release, increase VLDL, inhibits lipolysis, inhibit glycogenolysis, increase bronchial airway resistance

HTN, angina, cardiac arrhythmias, migraine, stage fright, CHF

Question 25

Nadolol

Answer 25

non-selective beta receptor antagonist Less lipophilic than propranolol mostly excreted unchanged in the urine oral hypertension, angina, migraine

Question 26

Timolol

Answer 26

Thiadiazole nucleus with morpholine ring Route of administration: oral, eye drops glaucoma HTN, agina, migraine

Question 27

Pindolol

Answer 27

non-selective beta receptor antagonist "Intrinsic sympathomimetic activity"--> partial activation and blockage--> partial agonist reduced ability to cause bradycardia oral HTN, angina, migraine

Question 28

Carteolol

Answer 28

nonselective beta receptor antagonist "Intrinsic sympathomimetic activity"--> partial activation and blockage--> partial agonist reduced ability to cause bradycardia oral, eye drops HTN, glaucoma

Question 29

Metoprolol/Bisoprolol

Answer 29

Beta 1 receptor antagonist Contains a para-substituted phenyl derivative Contains only 1 aromatic ring--> less bulky Moderate lipophilicity-->1/2 life: 3-4 hours First pass metabolism Oral, IV

Question 30

Atenolol

Answer 30

Beta 1 receptor antagonist contains a para-substituted phenyl derivative low lipophilicity-->water soluble-->half life: 6-9 hours--> long lasting oral, IV HTN, angina

Question 31

Esmolol

Answer 31

Beta 1 receptor antagonist contains a para substituted phenyl derivative contains ester group on the substitution-->rapid hydrolysis by esterases-->half life: 9 minutes--> short acting IV supraventricular tachycardia, a-fib, HTN (surgery)

Question 32

Nebivolol

Answer 32

3rd generation beta 1 receptor antagonist low lipid solubility vasodilation due to NO production HTN

Question 33

Labetalol

Answer 33

Nonselective beta receptor antagonist + alpha 1 receptor antagonist 1R, 1'R isomer is beta blocking activity 1S, 1'R is alpha 1 blocking activity Beta blocking activity prevents tachycardia associated with alpha 1 antagonists oral, IV HTN, hypertensive emergency

Question 34

Carvedilol

Answer 34

Nonselective beta receptor antagonist + alpha 1 receptor antagonist both enantiomers are alpha 1 antagonist only S enantiomer is beta antagonist oral HTN, CHF

Question 35

Beta blocker side effects

Answer 35

bradycardia AV block sedation mask hypoglycemia symptoms withdrawal

Question 36

Beta blocker contraindications

Answer 36

asthma COPD CHF TAPER DOSE WHEN D/C

Question 37

Dopamine receptor agonist

Answer 37

Fenoldopam severe HTN avoid in glaucoma due to increase in IOP maintains/increases renal perfusion while lowering blood pressure