Week 3 (Exam 1) Flashcards
ACE inhibitors and pregancy
No no no!
Eplerenone
More selective (than spironolactone) aldosterone antagonist for Post-MI HF or for HTN
Caution in giving Chlorthalidone in patients with
Gout
Clinical uses for a-Methyldopa
HTN, but notably its a drug of choice for Gestational HTN
b1 Adrenergic Receptors
Increase HR, contractility, Renin
Clinical applications for Amiloride
Counteracts K+ loss from other diuretics given for HTN or heart failure
a1 Adrenergic Receptors
Vasoconstriction (increased Veinous Return)
Candesartan
Irreversibly binding Angiotensin II receptor Inhibitor
Nebivolol MOA
Induces NO (cardioselective and vasodilatory)
Phentolamine
HTN emergency drug
induces catecholamine excess
Amlodipine
Dihydropyridine CCB used in CAD and HT, but its got a super long 30-50 hour half life
Toxicities of Catopril
Cough and Angioedema
Valsartan
Non-ProDrug Angiotensin II Receptor Inhibitor
Major toxicities associated with a-Methyldopa
Positive Coombs Test, SLE-like Sx
Angina, Bell’s, Rash, amenorrhea, impotence, anemia…
Where do Sodium channel blockers and Spironolactone act on the Loop of Henle?
Cortical Collecting Duct
Major Toxicities associated with Hydrochlorothiazide
Sulfonamide: associated hypersensitivity
Hypokalemia, -magnesemia, -natremia, -chloremic acidosis
Effects of Clonidine
Transient increase in BP when given IV
Reduced Sympathetic Outflow
Nifedipine Clinical Applications
First line treatment for HTN (being a Ca channel blocker)
Off label use for HTN emergency in pregnancy and Pulmonary HTN
a2 Adrenergic Receptors
In brain and periphery, decrease sympathetic tone
Clinical applications for Cilostazol
Intermittent Claudication
Clevidipine
HTN emergency drug
Contraindications: soy, egg allergies and lipid metabolism problems
Losartan MOA
Nonpeptide angiotensin II receptor antagonist
What does aliskirin do?
Prevents Angiotensinogen cleavage to Angiotensin I via Direct Renin Inhibition
Dobutamine receptor target
B1 receptors of the heart for increased rate and contractility, peripheral vasodilation
Toxicities of Diltiazem
Edema, Headache mostly
DA target in treating Shock
b-receptors at lower doses
+a-receptors at high doses
First line treatment of HTN with Aortic Disease
b-Blockers
Clinical applications of Spironolactone
Counteracts K+ Loss from other diuretics in HTN/HF
Reduces Fibrosis in HFrEF and Post-MI HF
Off label for HFpEF hirsutism, acne, female alopecia
How to treat black adults for HTN (as long as they don’t have HF or CKD)
Thiazide-type diuretic or CCB
Try for 2+ antihypertensives
Esmolol
HTN emergency drug
Contraindicated with b-blocker use, bradycardia, decompensated HF
High doses block b2 and hurt lungs in reactive airway dz
What Angiotensin II effects are spared by ARBs?
Vasodilation, cell growth, apoptosis
Clinical Uses for Verapamil
IV: supraventricular Tach
Oral: HTN
Off Label: Migraine Prevention, Cardiac Hypertrophy
Prazosin MOA
Competitive a1-adrenergic antagonist
Systolic Murmurs
Mr As
Differentiate presentations of platelet defects vs clotting factor defects
Platelet: Mucocutaneous bleeding, petechiae
Factor: Deep tissue bleeding, delayed
Nitroprusside MOA
Direct Venous and Arteriolar SM Dilation
Nicardipine
HTN emergency drug
Contraindicated in advanced aortic stenosis
Labetalol
HTN emergency drug
Contraindicated with reactive airway disease or chronic obstructive pulmonary disease.
Really great for Hyperandrenergic syndromes
May worsen HF and shouldn’t be given w 2/3 heart block or bradycardia
Diltiazem MOA
Non-Dihydropyridine Slow Channel Ca Blocker
Cardioselective
Effects of Diltiazem
Coronary Vascular SM relaxation / Dilation
Slows AV conduction
Hydrochlorothiazide MOA
K+-Losing Thiazide Diuretic
What is the half-life of Catopril?
1.7 hours (longer in renal impairment)
Clinical applications of Prazosin etc
HTN: Late choice because you can get a stroke and CHF with doxazosin compared to chlorthalidone
Off label for PTSD
Clinical uses for Clonidine
HTN (not initial)
XRs for ADHD
Cancer Pain, Opioid withdrawal
Where do Osmotic Diuretics act on the Loop of Henle?
Thin Descending Loop
Benazepril
ACE inhibitor with longer half life with 1xday dosing
Key Differences between Nifedipine and Verapamil
Nifedipine Increases HR and CO (SNS reflex activation)
B/c more dilation w/ less inoptropy and no chronotropy
a-1 Blockers Side Effect
Orthostatic Hypotension
Preferred thiazide diuretic
Chlorthalidone
Drug related to pedal edema
Dihydropyridines (CCB)
Where do Vaptans act on the Loop of Henle?
Collecting Duct (ADH-related water absorption)
Na Nitroprosside
HTN emergency drug
Monitor BP for overshoot, lower it for oldies
Prolonged use might do cyanide toxicity, tx w/ thiosulfate
Diastolic Murmurs
Ms Ts Ar/i
What do ARBs do?
Prevent Angiotensin II from binding AT1 receptors
AT1: Vasoconstriction, aldosterone secretion, sodium retention, Sympathetics, vasopressin, angiogenesis, feedback inhibition of renin
PAD and ABI
Ankle-branchial index: PAD indicated below 0.9
1 - 1.4 is normal
First line treatment of HTN with Stable Ischemic Heart Disease
b-Blocker, then a CCB if needed
Cilostazol Effects
Inhibits platelet aggregation
Vasodilates
Reasons to discontinue ACE inhibitor
Cough, Angioedema (deadly)
Antiplatelet MOA
Block Arterial White Clot Formation
Hydralazine
HTN emergency drug
Side effects of prazosin etc
Orthostatic HPTN
Retrograde Ejaculation
Catopril MOA
ACE inhibitor (lowers Angiotensin II)
Phenoxybenzamine
Old a-adrenergic blocker that’s a non-competitive antagonist with side effects like phentolamine plus mitosis and angioedema
Lisnopril
ACE inhibitor with longer half life with 1xday dosing
Phenylephrine receptor target
a-receptors, increase in BP can reflexly decrease HR and contractility due to withdrawal of sympathetic tone
Clinical Applications of Diltiazem
IV: A Fib and PSVT
Oral: Primary HTN and Chronic Stable Angina
Off Label: Anal Fissures, Reynaud
What is the indication for Ethacrynic Acid?
Non-sulfonamide Loop Diuretic just for people with a Sulfa Allergy
Toxicities associated with Amiloride
Hyperkalemia!
Hyponatremia, hypovolemia, hyperchloremic metabolic acidosis
Triamterene
Similar to Amiloride for edema and off-label HTN
Guanethidine
Displaces NE from synaptic vesicles (sparing EPI)
Decreases CO, TPR, RBF, GFR
Causes bad orthostatic HPTO, BP slowly increases
Propanalol MOA
b1 blocker: Decreases HR/BP
b2 blocker: blunts bronchodilator and vasodilation in SM
Amiloride MOA
Blocks ENaC channels in Collecting duct (responsible for (Na/K exchange), so there’s a small increase in Na excretion.
Thiazide Diuretic MOA
Blocks Na-Cl Cotransporter in DCT, resulting in more Ca reabsorption in PCT
Fenoldopam
HTN emergency drug
Contraindicated with intraocular pressure or intracranial pressure and sulfite allergy
Minoxidil MOA
Relaxes SM arterioles via cAMP
Stimulates hair growth secondarily to vasodilation
b2 Adrenergic Receptors
Skeletal muscle vasodilation
Bisoprolol
Highest b-1 blockade effects
How to treat HTN in pregnancy
Can use: Methyldopa, Nifedipine, Labetalol
Cant use: ACE inhibitors, ARBs, Direct Renin Blockers
Side Effects of Nifedipine
Flushing, Peripheral Edema
Palpitations
Gingival Hyperplasia
In what circumstances can you use Phenylephrine to treat shock?
Only if NE causes arrhythmias or continue to have high CO with low TPR
a-methyldopa MOA
a2-adrenergic AGONIST: sympatholytic for HTN
Cilostazol Black Box Warning
Patients with Heart Failure: Decreased survival of Class III and IV patients
Off-Label use for Losartan
Marfan syndrome
Enalapril (enalaprilat)
ACE inhibitor prodrug, taken IV
In what circumstance can you substitute DA for NE to treat shock?
With Bradycardia
NE target in treating shock
a and b1 receptors in heart and kidney
NOT b2 receptors
Clinical application of Hydrochlorothiazide
HTN, not in patients with low GFR
Off-label for Calcium Nephrolithiasis
Anticoagulant MOA
Block Thrombin Activation / Fibrin Formation: Red Clots
Serum creatinine increases with:
Falling GFR from ACE inhibition
Effects of Spironolactone
K+ sparing diuretic: blocks aldosterone-regulated Na-K exchange in the collecting duct (decreased Na entry though luminal Na channels, decreased basolateral NaK ATPase)
Decreases Fibrosis effects of Aldosterone
Phentolamine
Old a-adrenergic blocker with a short half life, that caused HPTN episodes and orthostatic HPTN, Tachycardia, arrhythmias, nasal stuffiness and diarrhea
Nitroglycerin
HTN emergency drug
Only with acute coronary syndrome, Pulmonary Edema
Don’t use with volume depleted patients
Metabolic Syndrome Criteria
3 of: Abdominal Obesity, TAGs over 150, HDL below 40(m)/50(f), BP above 130/85, fasting glucose below 100
Where do Loop Diuretics act
Thick Ascending Loop
Resperine
Blocks NE incorporation into synaptic vesicles
Least effective sympatholytic
Crosses BBB to make you depressed and want to kys
What is a major contraindication for b-blockers like propanalol?
People with peripheral vascular disease
this is because it can cause cold extremities
Verapamil MOA
Non-Dihydropyridine Slow-Channel Ca Blocker
Cardioselective
Whats so special about tamsolusin, terazosin, etc?
Like prazosin except marketed for BPH and helping pass kidney stones
Atenolol MOA
b-1 Selective blocker: decreases HR/BP
When would you use dobutamine to treat shock?
Refractory shock/systolic HF when there’s low cardiac output despite adequate filling pressure
First line treatment of HTN with CKD
b-Blocker, than an ACE inhibitor if needed
Nifedipine MOA
Dyhydropyridine Ca Channel Blocker
What is the MOA of clonidine?
a2-adrenergic angtagonist
Crosses BBB!
Vasopressin receptor targets
V1, V2 (kidneys)
Vasoconstrictor
Longer lasting version of Hydrochlorothiazide?
Chlorthalidone (40-60 hr half life)
Where do Thiazide Diuretics Act on the Loop of Henle?
DCT
Hydralazine
Direct arteriole vasodilation used to treat HF, but especially Hypertensive Emergency in Pregnancy
Hexamethonium MOA and adverse effects
Nn receptor blocker in both SNS and pSNS
SNS: difficult to maintain CO/BP when upright
pSNS: Higher resting HR/BP (SLUDGEM)
Cilostazol MOA
Type 3 PDE inhibitor: prolongs cAMP in platelets and cells
Enalaprilat
HTN emergency drug
Contraindicated in pregnancy, acute MI, bilateral renal artery stenosis.
Really great for high plasma renin.
slow onset, unpredictable BP response
The role of Corticosteroids in septic shock
Only improves shock reversal: without shock, corticosteroids are useless in septic patients
Metoprolol
b-1 Selective blocker with more likely CNS effects
Toxicities of Clonidine
Drowziness
Xerostomia
Rebound HTN with missed dose
Where in the loop of Henle do Osmotic Diuretics and Carbonic Anhydrase Inhibitors act?
PCT
Antidote to Heparin
Protamine
Why is unfreactionated Heparin given parenterally
Highly negatively charged, cannot cross membranes
Enoxaparin (delteparin, tinazeparin) MOA
Low molecular weight heparin (cannot complex with thrombin and antithrombin III, but inhibits Xa)
Prevents Red Clots
Fondaparinux MOA
Synthetic Super Low Weight Heparin (inhibits Xa)
Like Enoxaparin with more bleeding
Indications for Fondaparinux
Give with warfarin for DVT or PE
Sub Q daily but not reversible with Protamine
Does not cause HIT
Bivalirudin MOA
Synthetic Direct Reversible Thrombin Blocker
Indications for Bivalirudin
Given with aspirin for those doing coronary angioplasty
IV, Expensive, Doesn’t require antithrombin, less blood
No Antidote
Argatroban MOA
Direct Thrombin Inhibitor at Catalytic Site
Indications for Argatroban
HIT
Warfarin MOA
Vit K antagonist
Decreases Ca-Dependent F-II, VII, IX, X, S, C
Crosses Placenta
Cutaneous Necrosis from a drug
Warfarin
Rivaroxaban MOA
Direct Factor X (thrombin) Inhibitor
Like warfarin but better
Andexanet Alfa recently approved as antidote
CYP3A4
Dabigatran MOA
Reversible Direct Thrombin Inhibitor
Idarucizumab is the antidote
