Exam 1; Antihypertensive Agents Flashcards
What is the definition of hypertension
any prolonged elevation in blood pressure
most common cardiovascular disease
most are untreated
What is the desirable blood pressure
115/75
What category of blood pressure is pre-hypertensive
120/80-139/89
What category of blood pressure is stage 1 hypertension
140/90
What category of blood pressure is stage 2 hypertension
180/110
What category of blood pressure is hypertensive urgency
220/120
Every increase in blood pressure of what increases likelihood of cardiovascular incident by two fold
20/10
What is the result if 220/120 blood pressure is untreated for the long term
60% die within 6 months
80% dies within the year
What is it about hypertension that makes it so dangerous
it is generally asymptomatic until its final stages; can cause stroke, heart attack, aneurysms, and renal failure
True or False
There is a clear treatment option for hypertension
True
What is secondary hypertension (5-10%)
Know exactly what the problem/cause is (renal, tumor, etc.)
What is primary or essential hypertension
the cause is unknown
What is malignant hypertension
220/120+
A baroreceptor on the blood vessel stimulates what center of the brain
vasomotor center
In the vasomotor center of the brain, what occurs upon receiving a signal from the baroreceptor
NE is released to an α1 receptor which increases sympathetic flow
NE also autostimulates an α2 receptor which decreases sympathetic flow
The synapse from the vasomotor center relays to what
a paravertebral ganglia
From the paravertebral ganglia, what two places does the signal from the vasomotor center go
β1 receptors on the heart to increase cardiovascular output
α1 receptors on the blood vessel to stimulate vasoconstriction
A calcium influx into the blood vessel causes what to occur
constriction
A potassium efflux out of the blood vessel causes what to occur
relaxation
An increase cyclicGMP activity in the blood vessel causes what to occur
relaxation
Stimulation of an endothelium receptor on a blood vessel causes what to occur
constriction
Stimulation of a DA (dopamine) receptor on a blood vessel causes what to occur
relaxation
Stimulation of the angiotension II receptor by angiotension II on a blood vessel causes what to occur
constriction
The neuronal-vascular control loop is what kind of response to blood pressure changes
extremely rapid response (sudden dizziness upon sitting up quickly)
reflex blood pressure control
The kidney control loop system is what kind of response to blood pressure changes
long term regulation of blood pressure
renin-angiotension-aldesterone system
A decrease in renal blood pressure or decrease in Na in the kidney stimulates what
increases renin secretion by the kidney
Renin from the kidney is a precursor to what, via angiotensionogen
angiotension I
Angiotension 1 is converted to what via angiotension converting enzyme
angiotension II
Angiotension II has what three effects
vasoconstriction
Na retention in the kidney
secretion of aldesterone
This is converted to an inactive product by angiotension converting enzyme
bradykinin
What three effects does bradykinin have
dilates arteries - decreasing blood pressure
causes capillary leakage (edema)
activates sensory nerves (pain/itching)
What is the main treatment for hypertension
behavorial modification; stress, diet, weight management, smoking
Drugs like diuretics (thiazides) or a low Na diet cause this to occur, which can treat hypertension
decrease fluid volume
What are three characteristics of hypertension drugs
interrupt “normal” BP control
do not “cure” hypertension
must be taken for life
What is the one side effect that is common for all anti-hypertensives
risk of hypotension
Any drug that can enter the CNS can have what kind of effects
behavioral effects
This is a pro-drug metabolized to α-methyl NE which activates/stimulates α2 receptors
α-methyl DOPA
What are the 5 side effects of α-methyl DOPA
depression drowsiness dry mouth impaired ejaculation hepatic dysfunction
This drug is an α2 agonist which has unlabeled uses
clonidine
What are the four unlabeled uses of clonidine
fibromyalgia
insomnia
Tourette’s
opiate withdrawal
What are the 4 side effects of clonidine
depression
drowsiness
dry mouth
impaired ejaculate
This is a β blocker drug that has central and peripheral effects
propranolol
This is a drug that inhibits the enzyme tyrosine hydroxyls which prevents the synthesis of E and NE; used to treat tumor of adrenal gland (pheochromoctyoma)
α-methyl tyrosine
This drug causes depletion of post-ganglionic neuron neurotransmitter
reserpine
What are the side effects of reserpine
depression
drowsiness
diarrhea
Which family of drugs block the α1 receptor on vascular smooth muscle
-osin’s
prazosin, terazosin, etc.
These three drugs are α1 blockers and used only to treat benign prostatic hypertrophy (BPH)
tamsulosin
alfuzosin
silodosin
What is the main side effect of the α1 site inhibitors (-osin’s)
first dose effect; rapid dose in BP
orthostatic or postural hypotension
This drug blocks all β blockers (β1 and β2)
propranolol
Propranolol blocks β1 receptors on the heart and cause what
prevents any increase in heart rate and contraction force; decreases renin secretion
What are the four “lesser” side effects of propranolol
gets into the CNS; depression
bradycardia; fatigue
impotence
decreases HDL and increases triglycerides
What is the main side effect of propranolol
worsens asthma (β2 = bronchodilators)
How many specific β1 blockers are there on the market
13
the -olol’s
What are the side effects of the β1 blockers, the -olol’s
fewer CNS effects
bradycardia
fatigue (with exercise)
Labetalol and carvedilol block which receptors
α1, β1, β2
What are the side effects of labetalol andcarvedilol
postural hypotension
dry mouth
Which family of drugs are angiotension receptor blockers (ARBs)
-artans
Angiotension RecepTor ANtagonists
What effect does the antiogention receptor blockers induce (-artans)
block the angiotension II receptor
decreasing secretion of aldosterone
*What is the main side effect of ARBs
can cause fetal abnormalities; like all agents that alter the angiotension system class X pregnancy drugs
Which family of drugs are the endothelian blockers
-entan’s
What are -entan’s the treatment for specifically
pulmonary artery hypertension
What are the three side effects of endothelin blockers
fetal damage
hepatic toxicity
testicular atrophy
This drug is a prodrug which is involved with opening potassium channels in arterial smooth muscle;
efflux leads to hyper polarization
for very refractory patients
minoxidil
What are two side effects of minoxidil
hypertichosis (hair growth); discontinuation = hair loss
edema - pericardial effusion; leads to cardiac tamponade
This is a vasodilator which increases cGMP which causes smooth muscle relaxation
hydralazine
What is the side effect of hydralazine
in slow acetylators - lupus like syndrome
This drug acts by opening potassium channels decreasing insulin secretion from β cells
diazoxide
This is the drug of choice in hypertensive emergencies
nitroprusside
Nitroprusside acts within seconds via an IV to do what
dilate both arteries and veins equaling a rapid drop in blood pressure
Why must nitroprusside be stored in powder form
because it degrades in solution (saline) into other molecules including cyanide
What is the meaning behind “Minnie Hid the Diamonds in the Nitro” because she was KG KG
Minoxidil = potassium hydralazine = cGMP diazoxide = potassium mitroprusside = cGMP
What family of drugs are calcium channel blockers
-ipine’s
The calcium channel blockers have what effect
inhibit Ca++ influx into vascular smooth muscle; prevents vasoconstriction
What are two side effects of calcium channel blockers
can cause heart burn
may worsen heart failure
This family of drugs are angiotension converting enzyme inhibitors (ACE)
-pril’s
ACE inhibiting drugs have what three effects
inhibits ACE that is required for conversion of angiotension I to II
prevents breakdown of bradykinin (vasodilation)
decreases aldosterone secretion
What are the five side effects of ACE inhibitors
rash dry cough angioneurotic edema (swelling of URT) taste alteration fetal damage
This is a renin inhibitor (directly inhibits renin)
aliskiren
What are the four side effects of aliskerin
fetal damage
cough
angioedema
diarrhea
This agent activates D1 receptors; given in IV for hypertensive emergencies
fenoldpam