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Therapeutics Exam 5 > HTN > Flashcards

HTN Flashcards

1
Q

Aging in HTN

A

decreased CO + increased peripheral resistance

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2
Q

Preganglionic neurons

A

primary neurotransmitter is acetylcholine

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3
Q

Postganglionic neurons

A

PNS: primary is acetylcholine

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

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4
Q

PSNS

A

cholinergic receptors

acetylcholine: endogenous
muscarinic: exogenous
nicotinic: exogenous

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5
Q

SNS

A

adrenergic receptors

norepinephrine: endogenous
epinephrine: endogenous

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6
Q

Alpha 1

A

vasoconstriction
pupillary dilation
ejaculation
gi inhibition

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7
Q

Alpha 2

A

vasoconstriction
inhibit NE release
decrease CV

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8
Q

Beta 1

A

cardiac stimulation
secretion of renin

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9
Q

Beta 2

A

bronchodilation
uterine relaxation
gi inhibition
vasodilation

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10
Q

Baroreceptor reflex

A

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

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11
Q

Targets for antihypertensive drugs

A

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

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12
Q

Where are Alpha 1 receptors located?

A

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

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13
Q

Where are Alpha 2 receptors located?

A

CNS

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14
Q

Where are Beta 1 receptors located?

A

cardiac muscle and CNS

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15
Q

Alpha-1 antagonists

A

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

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16
Q

Alpha 1 antagonists structure

A

Quinazoline ring allowing for alpha 1 specificity

Piperazine ring and acyl moiety allowing for PK activity

17
Q

Alpha 1 antagonists effect

A

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

18
Q

Alpha 1 antagonists indications

A

HTN, BPH, and Raynaud’s disease

19
Q

Alpha 2 agonists

A

Inhibits the release of NE causing reduced CO from the brain

results in decreased HR, contractibility, renin release, vasoconstriction

20
Q

Clonidine (Alpha 2 agonist)

A

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

21
Q

Guanfacine/Guanabenz (alpha 2 agonist)

A

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

22
Q

Methyldopa and Methyldopate (alpha 2 agonist)

A

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

23
Q

Beta blockers

A

effect: decrease cardiac output and inhibits the release of renin

structure: aryloxypropanolamine: aromatic ring + bulky R group

24
Q

Propranolol

A

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

25
Q

Nadolol

A

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

26
Q

Timolol

A

Thiadiazole nucleus with morpholine ring

Route of administration: oral, eye drops

glaucoma HTN, agina, migraine

27
Q

Pindolol

A

non-selective beta receptor antagonist

“Intrinsic sympathomimetic activity”–> partial activation and blockage–> partial agonist

reduced ability to cause bradycardia

oral

HTN, angina, migraine

28
Q

Carteolol

A

nonselective beta receptor antagonist

“Intrinsic sympathomimetic activity”–> partial activation and blockage–> partial agonist

reduced ability to cause bradycardia

oral, eye drops

HTN, glaucoma

29
Q

Metoprolol/Bisoprolol

A

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

30
Q

Atenolol

A

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

31
Q

Esmolol

A

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)

32
Q

Nebivolol

A

3rd generation

beta 1 receptor antagonist

low lipid solubility

vasodilation due to NO production

HTN

33
Q

Labetalol

A

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

34
Q

Carvedilol

A

Nonselective beta receptor antagonist + alpha 1 receptor antagonist

both enantiomers are alpha 1 antagonist
only S enantiomer is beta antagonist

oral

HTN, CHF

35
Q

Beta blocker side effects

A

bradycardia

AV block

sedation

mask hypoglycemia symptoms

withdrawal

36
Q

Beta blocker contraindications

A

asthma

COPD

CHF

TAPER DOSE WHEN D/C

37
Q

Dopamine receptor agonist

A

Fenoldopam

severe HTN

avoid in glaucoma due to increase in IOP

maintains/increases renal perfusion while lowering blood pressure

Therapeutics Exam 5 (11 decks)

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