Br Pharmacology: Drugs Used In Hypertension

Front 1

Primary HTN is caused by what?

Back 1

idiopathic

Front 2

Drugs most important for HTN? When is each used?

Back 2

1) thiazides = mild HTN
2) loop diuretics = moderate to severe HTN

Front 3

What is the MOA of clonidine? Which other drug is used for this purpose?

Back 3

1) Acts in CNS to decreases sympathetic outflow as an alpha-2 agonist
2) methyldopa - converted in brain to methylnorepinephrine

Front 4

Is there a compensatory response with clonidine and methyldopa?

Back 4

1) yes salt and water retention

Front 5

What happens if clonidine is discontinued suddenly? How can it be treated?

Back 5

1) severe rebound HTN
2) give clonidine or alpha-blocker phentolamine

Front 6

What are side effects of clonidine?

Back 6

1) dry mouth
2) severe rebound HTN
3) some sedation

Front 7

What are side effects of methyldopa?

Back 7

1) sedation
2) positive Coombs
3) hemolytic anemia

Front 8

Which drugs are powerful anithypertensives because of both sympathetic and parasympathetic blockade? is there compensation with use?

Back 8

1) hexamethonium
2) trimethaphan
3) yes salt and water retention

Front 9

Which drug depletes the adrenergic nerve terminal of NE?

Back 9

reserpine

Front 10

Which drug blocks the release of NE and depletes stores?

Back 10

gaunethidine

Front 11

Is there compensation with reserpine? thiazides? loop diuretics?

Back 11

minimal

Front 12

Does reserpine enter CNS? what about guanethidine? How long do each last?

Back 12

1) yes
2) no
3) both last days to weeks

Front 13

What are toxic effects of reserpine?

Back 13

1) diarrhea
2) nasal stuffiness
3) sedation
4) DEPRESSION

Front 14

What are toxic effects of guanethidine?

Back 14

1) orthostatic hypotension
2) sexual dysfunction

Front 15

Which receptor does guanethidine require for uptake? Which drugs block this receptor?

Back 15

1) uptake 1
2) blocked by cocaine and TCAs

Front 16

MAOIs are no longer used for HTN but when they were how did they work?

Back 16

1) form false neurotransmitter (octopamine) in sympathetic postganglionic neurons and lower BP
2) octopamine is stored in vesicles reducing NE concentration

Front 17

Someone on an MAOI can develop hypertensive crisis if they eat what?

Back 17

1) tyramine

Front 18

Which alpha1 and beta blocker are commonly used in HTN?

Back 18

1) prasozin
2) propanol

Front 19

How do alpha1 blockers effect cardiovascular system?

Back 19

1) decrease vascular resistance
2) decrease venous return

Front 20

Why are non-selective alpha blockers not used in chronic HTN? Which drugs are in this class?

Back 20

1) excessive compensatory responses when used
2) phentolamine
3) phenoxybenzamine

Front 21

Beta blockers reduce CO and later vascular resistance. How do they decrease vascular resistance?

Back 21

reduced angiotensin II because beta-blockers prevent release of renin

Front 22

What are adverse effects of beta blockers?

Back 22

1) sleep disturbances
2) sedation
3) impotence
4) cardiac disturbances
5) asthma

Front 23

How do beta blockers effect sugar and lipid levels?

Back 23

1) VLDL, LDL, TAGs
2) decrease HDL and glucose
Note: use these with caution in diabetics because they cause hypoglycemia and if glucagon shit is bad

Front 24

Hydralazine and Minoxidil work where on the blood vessels?

Back 24

arterioles more than veins

Front 25

What is the MOA of hydralazine?

Back 25

release of NO from endothelial cells by increase of cGMP

Front 26

When is minoxidil used? What is its MOA?

Back 26

1) severe HTN
2) hyperpolarizes vascular smooth muscle via opening K+ channels

Front 27

what are toxic effects of hydralizine? who is it contraindicated in?

Back 27

1) reversible lupus like syndrome without renal effects
2) reflex tachycardia contraindicated in angina/CAD

Front 28

What are toxic effects of minoxidil?

Back 28

1) hirsutism
2) pericardial effusion
3) hypertrichosis = werewolf syndrome from excessive hair
4) reflex tachycardia

Front 29

When are Ca2+ blockers used? what are examples of drugs?

Back 29

1) nifedipine
2) verapamil
3) diltiazem
4) used for chronic HTN of any severity

Front 30

Why are calcium blockers preferred to minoxidil and hydralizine?

Back 30

1) Ca2+ blockers = minor salt and H2O retention
2) minoxidil and hydralazine = marked salt and H2O retention and marked tachycardia

Front 31

When are nitroprusside and diazoxide given?

Back 31

1) IV for hypertensive emergencies
2) short half live

Front 32

What is the MOA of nitroprusside?

Back 32

release of NO from the drug itself

Front 33

What is the MOA of diazoxide?

Back 33

opens K+ channels and hyperpolarizes smooth muscle cells

Front 34

Besides HTN what else can diazoxide be used for?

Back 34

1) hypoglycemia from insulin secreting tumor
2) has effect to reduce insulin release

Front 35

what are toxicities of diazoxide?

Back 35

1) hypotension
2) hyperglycemia
3) salt and water retention

Front 36

What is the MOA of fenoldopam? What is it used for?

Back 36

1) D1 activation
2) marked vasodilation
3) short duration for hypertensive emergencies

Front 37

How many enzymes do ace inhibitors inactivate?

Back 37

1) ACE
2) kininase II
3) peptidyl dipeptidase

Front 38

What is increased and decreased when taking an ACE inhibitor?

Back 38

1) decreased angiotensin II
2) increased bradykinin

Front 39

What are toxic effects of ACE inhibitors? what do they protect?

Back 39

1) cough
2) renal damage in fetus
3) renal damage in pre-existing renal disease
4) protect diabetic kidney

Front 40

What is the MOA of losartan?

Back 40

inhibit angiotensin II at AT1 receptor

Front 41

What are toxic effects of lorsartan?

Back 41

1) renal damage in fetus
2) renal damage in pre-existing renal disease
3) NO COUGH

Front 42

What are toxicities of nifedipine?

Back 42

1) constipation
2) cardiac disturbances
3) flushing

Front 43

What are toxicities of nitroprusside?

Back 43

1) cyanide toxicity
2) thiocyanate toxicity

Front 44

what is the MOA of aliskiren?

Back 44

inhibits renin's action on angiotensinogen

Front 45

What are toxicities of aliskiren?

Back 45

1) headache
2) diarrhea
3) K+ accumulation

Front 46

What is the goal of stepped care?

Back 46

1) reduce toxicity and minimize compensatory responses
2) drugs added and removed as needed
3) 1st drug is usually beta blocker or carvedilol (combined alpha and beta)

Front 47

What type of antihypertensive do older patients and blacks of any age respond best to?

Back 47

beta-blockers instead of ACE-inhibitors

Front 48

What are signals for malignant HTN?

Back 48

1) decreased renal function
2) encephalopathy
3) retinal hemorrhages
4) angina, stroke or MI

Front 49

In malignant HTN which drugs are combined to reduce BP to 140-160/90-110?

Back 49

1) nitroprusside or fenoldopam, or diazoxide with furosemide and beta blocker

Front 50

which Ca2+ blocker works best on vascular smooth muscle?

Back 50

nifedipine> diltazem > verapamil

Front 51

Which Ca2+ blocker works best on the heart?

Back 51

verapamil > diltazem > nifedipine

Front 52

What are clinical uses of Ca blockers?

Back 52

1) HTN
2) angina
3) arrythmias (not nedipine)
4) prinzmentals angina
5) raynauds

Front 53

nitroglycerin and isosorbide dinitrate work where? which volume in heart do they decrease?

Back 53

1) veins>arteries
2) decrease preload

Front 54

What are nitroglyerin and isosorbide dinitrate used for?

Back 54

1) angina
2) pulmonary edema
3) aphrodisiac
4) erection enhancer

Front 55

What are side effects of nitroglycerin and isisorbide dintrate?

Back 55

1) reflex tachycarida from hypotension
2) "monday disease" in industrial workers - develop tolerance during week and lose it over weekend
a. headache, tachycardia and flushing on reexposure

Front 56

What is first line therapy for HTN in pregnancy along with methyldopa?

Back 56

hydralazine

Front 57

Which drugs are used for CHF? Which is contraindicated in uncompensated CHF?

Back 57

1) diuretics
2) ACE inhibitors
3) beta blockers (contraindicated in uncompensated)
4) K+sparing diuretics