Antihypertensives part 2 Flashcards
What are the different groups of sympathetic antagonist agents
Alpha
Beta
*mix of the two
Adrenergic blocking drugs
What are the sites of action for sympathoplegic drugs
Peripherally
Centrally
Ganglionic
What drugs block sympathetic system at the peripheral level
Prazosin
Doxazosin
Metoprolol
Pindolol
What drugs block the sympathetic system centrally
Clonidine
What drugs block the sympathetic system ganglionically
Trimethaphan
What is the indication for clonidine
Menopausal flushing
opioid/alcohol withdrawal
tourettes
2nd line for ADHD
What is the MOA for clonidine
Blocks release of norepinephrine and inhibits sympathetic outflow from the brain
What are the pharmacokinetics of clonidine
Oral
don’t take with food
crosses placenta
narrow TI
dose adjust for renal patients
What are some side effects / contraindications of clonidine
dysrhythmias
bradycardia
AV block
anorexia
confusion / delirium
Where are alpha 1 receptors found
smooth muscle
Where are alpha 2 receptors found
Brain stem AND smooth muscle
What are non-selective alpha blocker drugs
Phenoxybenzamine
Phentolamine
What is the indication of phenoxybenzamine
Sweating and HTN associated with pheochromocytoma
What is the MOA of phenoxybenzamine
Irreversible, non-selective blockade of peripheral alpha 1&2 receptors
-decrease vasoconstriction
What are the pharmacokinetics of phenoxybenzamine
Oral / IV
Long lasting effects
What are the side effects / adverse reactions of phenoxybenzamine
Reflex tachycardia
Orthostatic hypotension
nasal stuffiness / N/V
Inhibit ejaculation
What is the indication of phentolamine
Dx / Tx of pheochromacytoma
particular associated with HTN emergencies
Tx of dermal necrosis following extravasation of norepinephrine
What is the MOA of phentolamine
Reversible, non-selective blockade of peripheral alpha 1&2 receptors
What are the pharmacokinetics of phentolamine
IM or IV
effects last 4 hours
What are the side effects of phentolamine
Reflex tachy
orthostatic hypotension
What are the alpha-1 selective blockers
Prazosin
doxazosin
What are prazosin & Doxazosin used for
-HTN
-Benign prostatic hyperplasia d/t prostate muscle relaxation
-PTSD associated nightmares
What are the MOA of selective alpha-1 blockers
Selective a1 inhibition = decrease vasoconstriction
What are the side effects of prazosin and doxazosin
Dizziness
lack of energy
nasal congestion
HA
Drowsiness
orthostatic hypotension
What selective alpha 1 blocker is longest acting `
Doxazosin
What drugs are nonselective beta antagonists
Propranolol
nadolol
pindolol
timolol
What is the indication for propranolol
performance anxiety
postural tremor
migraine prophylaxis
thyrotoxicosis
portal HTN
What is the MOA of propranolol
Nonselective B1 & B2 inhibition
What is the pharmacokinetics of propranolol
oral admin 1x/day
extensively metabolized and excreted in urine
What are the adverse effects / side effects of propranolol and nadolol
Bronchoconstriction
dizziness
lethargy
visual disturbance
short term memory loss
vivd dreams
What is the indication of Nadolol
HTN
Management of chronic angina
more potent that propranolol (rarely used)
What is the MIA of nadolol
Non-selective Beta 1&2 inhibition
What are the pharmacokinetics of nadolol
Oral admin
1/2t of 14-24 hours
What is the indication of pindolol
HTN
What is the MOA of pindolol
PARTIAL beta 1&2 agonist
*at high doses, posses similar effects of epi
What are the adverse effects / contraindications of pindolol
Bronchoconstriction
Dizziness
Hallucinations
Short term memory loss
vivid dreams
*Avoid in patients with previous MI / angina
What is the indication for timolol
Chronic glaucoma management (open angle)
What is the MOA of timolol
Non-selective beta 1&2 inhibition
reduces production of aqueous humor in the eye
What is the pharmacokinetics of timolol
Topical
oral can be used for HTN (rare)
What are the selective beta 1 sympathetic antagonists
Metoprolol
atenolol
nebivolol
What is the indication for metoprolol
HTN
Stable / unstable angina
acute MI
SVT / Vtach
Tachycardia
Chronic stable HF
Migraine prophylaxis
What is the pharmacokinetics of metoprolol
Oral
Extensively metabolized
1/2t = 3-4 hours
What are the side effects / contraindications of metoprolol
Bradycardia
decrease CO
AV heart block
**NOT approved for acute HF
What is the indication of atenolol
Same as metoprolol just less effective
What is the pharmacokinetics of atenolol
Excreted primarily in urine
1/2t = 6hours
What are the side effects of atenolol
Bradycardia
reduced CO
AV heart block
What is the indication for nebivolol
HTN
HF
Which selective beta 1 blocker is MOST cardio selective
Nebivolol
What is the side effects of nebivolol
Bradycardia
Reduced CO
AV heart block
what does nebivolol stimulate
beta 3 receptors in peripheral vasculature = vasodilation from being nitric oxide potentiating
Which drugs are both alpha and beta blockers
Carvedilol
Labetolol
What is the indication for carvedilol
Primarily in chronic stable HF
-decreases mortality rates in patients after MI
What is the MOA of carvedilol and labetolol
Nonselectively blocked alpha 1, beta 1, beta 2
peripheral vasodilation
What is the pharmacokinetics of carvedilol
Oral
1x/day
What is the pharmacokinetics of labetolol
Oral / IV
SAFE IN PREGNANCY (often used in preeclampsia)
can be taken up to 3x daily
What are the side effects of labetolol and cavedilol
Orthostatic hypotension
dizziness
hypoglycemia
Which drugs are cardio-selective calcium channel blockers? (non-dihydropyridines)
Verapamil
Diltiazem
What is the indication of use for verapamil and diltiazem
stable / vasospastic angina
essential HTN
dysrhythmias
What is the MOA for non-dihydropyridine ca2+ channel blockers
-Selectively blocks Ca2+ channels in the myocardium = decr arterial pressure, incr coronary perfusion, decr heart rate, decr AV nodal conduction, decr force of contraction
What are the pharmacokinetics of verapamil
Oral or IV
hepatic metabolism
dose adjust for renal impairment
What is the pharmacokinetics of diltiazem
oral
50% bioavailability
effects begin quickly and peak in 30min
What are the side effects / contraindications of verapamil and diltiazem
Constipation
bradycardia
AV block
HF
hypotension
LE edema
Contra in patients with heart block and heart failure
Which drugs are dihydropyridines
Nifedipine
amlodipine
What is the indication for nifedipine
HTN
stable / vasospastic angina
migraine
reynauds
What is the indication of amlodipine
HTN
Stable and vasospastic angina
**VERY COMMON
What is the MOA of nifedipine and amlodipine
Blocks Ca2+ channels in arterioles (vasodilation)
-Does not alter conduction through AV node
What are the side effects of nifedipine
-Flushing, dizziness, headache, LE edema, gingival hyperplasia, reflex tachycardia
-Avoid in pts w HF, grapefruit juice
What is the side effects of amlodipine
Lightheadedness, hypotension, bradycardia, LE edema
-Avoid in pts w HF, grapefruit juice
What drugs are venous vasodilators
Isosorbide dinitrate
Nitroglycerine
what is the indication for nitroglycerine
All types of angina
severe HTN
What is the MOA for venous vasodilators
Converted to nitric oxide in the body -> vasodilation -> decr cardiac O2 demand
What is the indication for isosorbide dinitrate
angina prophylaxis
esophageal spasm
HF tx in black people in combo with hydralazine
What is the pharmacokinetics of nitroglycerine
Sublingual
IV, path, or ointment also available
-pro-drug
What is the pharmacokinetics of isosorbide dinitrate
Sublingual / oral taken daily
What are the side effects / contraindications of nitroglycerine and Isosorbide dinitrate
HA
Hypotension
tachycardia
*tolerance can rapidly develop
* drug interactions with PDE-5i
What are arterial vasodilator drugs
Hydralazine
Diazoxide
minoxidil
What is the indication of hydralazine
Essential HTN
Almost always given w/ beta blocker
-used to decrease after load in pts. w/ HF
What is the MOA of hydralazine
-Exact MOA unknown
-Selective dilation of arterioles -> decr peripheral resistance and decr BP
What is the pharmacokinetics of hydralazine
oral / IV
Inactivated by acetylation
*dose adjust in acetylators
What is the side effects / contraindications of hydralazine
Postural hypotension
HA
N
reflex tachy
SLE syndrome
What is the indication of minoxidil
Patient with severe HTN who are unresponsive to safer drugs
*stimulant for hair growth
What is the MOA for minoxidil
Opens K+ channels in vascular smooth muscle -> K+ flows out, decr cells ability to contract -> arteriolar dilation -> decr periph resistance and decr BP
What is minoxidil metabolized into
minoxidil sulfate
What are the side effects of minoxidil
Reflex tachycardia
Na+ / H2O retention
excessive hair growth
What is the indication of Diazoxide
Acute / malignant HTN
Hypoglycemia (prevents insulin release from pancreas)
What is the MOA of Diazoxide
Long acting K+ channel opener = Na+ and water retention
What is the side effects of diazoxide
Excessive hypotension
-some cases resulted in stroke and MI
What drugs are vasodilators for both arteries and veins
Nitroprusside
What is the indication for sodium Nitroprusside
HTN emergencies
What is the MOA for Nitroprusside
Breaks down and releases nitric oxide, activates guanylate cyclase = catalyze the production of cyclic GMP = relaxation in smooth muscles in arterioles and veins to decrease BP
What is the pharmacokinetics of nitroprusside
Continuous IV infusion
*Effects begin w/in seconds
What are the side effects of nitroprusside
Cyanide poisoning
thiocyanate toxicity
What agents are centrally acting (alpha 2 blockers)
Clonidine
Methyldopa
what is the indication of clonidine
Menopausal flushing
opioid / alcohol withdrawal / Tourettes
*second line agent for ADHD
What is the indication for methyldopa
Mostly for HTN during pregnancy
What is the MOA of clonidine and methyldopa
Agonist at centrally located a2 receptors = inhibits further release of norepi and inhibits sympathetic outflow from the brain
What are the side effects of clonidine
Rebound hypertension
lethargy
sedation
xerostoma
constipation
What are the side effects of mehtyldopa
Sedation
occasional lactation
*Long term can lead to autoimmune hemolytic anemia
Which patients should be started on combination therapy immediately for hypertension
BP is greater than 20mmHg above systolic goal OR 10mmHg above diastolic goal
What drug classes are best for treating high risk angina pectoris
Beta blockers (1st choice)`
calcium channel blockers
What drug classes are best for treating hypertension in diabetics
Diuretics
ACE inhibitors
ARBs
Which drugs should be used for treating HTN in someone who had a stroke
ACE inhibitors
Which drugs should be used for treating HTN in HF
Diuretics
Beta blockers
ACE-i
ARBs
Aldosterone receptor antagonists
Which drugs should be used to treat HTN in someone with a history of MI
Beta clockers
ACE-i
Aldosterone receptor antagonists
If someone has CKD, how would you treat NTN
ACE-i
ARBs