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PCol Exam 3
Cardiovascular
101
Pharmacology
Graduate
11/18/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Nitroglycerin
Definition
Organic Nitrate
Use: chronic or acute (post-MI IV, acute angina subling)
Term
Isosorbide Dinitrate
Definition
Isordil
Organic Nitrate
Dosed tid
Term
Isosorbide Mononitrate
Definition
Imdur
Organic Nitrate
Dosed qd
Term
Nitrates
Indications, MOA, SOA, ADRs, Tolerance
Definition
Use: angina
MOA: rel. NO from structure -> activates soluble GC -> cGMP -> PKG -> de-P's MLCK -> vasodil/sm musc relax
SOA: veins & coronary arteries
ADRs: dizziness, hypoTN, flushing, methemoglobinemia-> NO oxidizes Fe2 to Fe3+ -> oxygen cannot leave Hb -> bluish skin
Tolerance: There must be a nitrate-free period every day during the time pt is least symptomatic
Term
Ranolazine
Definition
Use: angina
 MOA: causes inhibition of Na channel so decrease ca2+ buildup and therefore decrease preload and increase flow to coronary artery
Term
Direct Vasodilators
Indications, MOA
Definition
Use: HTN, CHF
MOA: act directly on smooth muscle cell to cause vasodil
Term
Minoxidil
MOA, SOA, ADR
Definition
MOA: bind K+ channel on sm musc cell -> (-) hyper polarized as K+ rushes out -> cell cannot contract -> vasodil
SOA: only arterial
ADR: hypertrichosis
Also branded as Rogaine
Term
Diazoxide
MOA, SOA, ADR
Definition
MOA: bind K+ channel on sm musc cell -> (-) hyper polarized as K+ rushes out -> cell cannot contract -> vasodil
SOA: only arterial
ADR: ^glucose; hyperpolarizes pancreatic Beta cells so they cannot release insulin
Also branded as Proglycim
Term
Hydralazine
MOA, SOA, Metabolism, ADR
Definition
MOA: unknown
SOA: only arterial
Metabolism: N-acetyl transferase
ADR: reversible lupus-like syndrome
Term
BiDil
Definition
hydralazine + isosorbide dinitrate
SOA: balanced vasodilator
only approved for blacks
Term
Nitroprusside
MOA, SOA, Metabolism, Indication
Definition
IV only
MOA: releases NO from structure
SOA: balanced vasodilator
Metabolism: thiosulfate in liver converts CN- to thiocyanate & excreted renally; we coadmin thiosulfate to make sure
Use: HTN crisis
Term
3 PAH Pathways
Definition
Endothelin: Sm Musc Receptors EtA (bad:vasocon&sm musc prolif) & EtB (good: vasodil & antiprolif)
NItric Oxide: Sm Musc activation of GC -> cGMP -> PKG -> vasodil & antiprolif
Prostacyclin: Sm Musc Gs/prostacyclin receptor -> cAMP -> PKA -> vasodil & antiprolif
Term
epoprostenol + admin
Definition
Flolan
Prostacyclin Analog
Admin continously via central line; pump always on ice
Term
treprostinil + admin
Definition
Remodulin
Prostacyclin Analog
Admin continuously SC
Term
iloprost + admin
Definition
Ventavis
Prostacyclin Analog
Admin via inhaler q3h
Term
Prostacyclin Analogs
MOA, ADRs
Definition
MOA: mimic Prostacyclin to -> decreased proliferation of sm musc & vasodil
ADRs: some reflex tachycardia, flushing, dizziness, orthostatic hypoTN, pain in mouth/jaw related to prostaglandin
Term
Endothelin Receptor Antagonists
ADRs
Definition
teratogenic: cannot take when pregnant
reversible hepatox
Term
bostentan
Definition
nonselective endothelin receptor antagonist
oral
Use: PAH
Term
ambrisentan
Definition
A-selective endothelin receptor antagonist
oral
Use: PAH
Term
sildenafil
Definition
Revatio (PAH), Viagra (ED)
PDE-5 Inhibitor
Use: PAH & ED
Term
PDE-5 Inhibitors
MOA & ADRs & DDI
Definition
MOA: decreases cGMP breakdown -> more vasodilation
ADRs: dyspepsia via smooth muscle GIT relax; dizziness, flushing, hypoTN, bluish tinted vision
DDI: Nitrates -> you get incrased formation of cGMP from nitrate & decreased breakdown of cGMP from PDE-5i -> massive PKG activation -> massive vasodilation
Term
tadalafil
Definition
Cialis
PDE-5 Inhibitor
Term
vardenafil
Definition
Levitra
PDE-5 Inhibitor
Term
avanafil
Definition
Stendra
PDE-5 Inhibitor
Term
papaverine
Definition
Nonselective PDE Inhibitor
Term
alprostadil
admin
Definition
Caverject-> penis injection
Muse-> transurethral suppository
PGE Analog
Use: erection
Term
PGE Analog
MOA, ADR
Definition
MOA: acts on PG receptor on blood vessels
Use: erection in those with CNS damage
ADR: priapism
Term
3 pathways to activate renin secretion from JG cells
Definition
1.) decreased BP in preglomerular cells
2.) decreased NaCl reabsorption in macula densa of kidney
3.) activation of B1 in JG Cells
Term
2 negative feedback mechanisms to stop renin secretion
Definition
1.) Long Loop: increased BP in preglomerular cells -> Cox2 decrease -> PG decrease -> less cAMP -> less renin
2.) Short Loop: adequate AngII -> binds AT1 on JGC -> Gq -> PLC -> Increased Ca++ -> decreased renin
Term
5 effects of AngII on AT1
Definition
1.) kidney: vasocon of renal arteries -> decreased GFR
& increased Na & Cl reabsorp via aldosterone/ADH
2.) adrenal gland:
cortex: rel. aldosterone -> Na rebsorp
medulla: rel. catecholamines -> increased renin & contractil
3.) vascular sm musc: vasocon
& growth promoting factors
4.) CNS: increased ADH -> increased H2O reabsorp
5.) myocardium: increased contractility
& remodeling eventually
Term
ACEi
MOA & ADR & Use
Definition
MOA:
1.) Block ACE -> decreased AngII -> decreased AT1 activity -> decreased vasocon, decreased Na/H20 rtn, decreased remodeling
2.) inhibit bradykinin bdown -> more bradykinin -> binds B2 Gq -> PLC -> Increased Ca++ -> eNOS -> NO -> cGMP -> vasodil
ADRs:
hypoTN (new dose), dry cough & angioedema (due to bradykinin), hyperkalemia (due to block of aldosterone which sec. K), increased SCr (due to decreased GFR), also beware Triple Whammy of ARF (ACEi, diuretic, NSAID)

Use: HTN, CHF, CKD
Oral prodrugs
Term
3 drugs to slow progress of CKD
Definition
ACEi, ARB, DHP CCBs
Term
ARB
MOA & ADR & Use
Definition
MOA: block AT1 receptor (Gq) -> decreased IC Ca++ -> decreased sm musc contraction -> vasodil
ADR: hypoTN, increased SCr, hyperkalemia
oral qd
Term
ARB Affinity: Two best & two worst
Definition
Best: Azilsartan > Candesartan
Worst: Losartan < Valsartan
Term
Direct Renin Inhibitors
MOA & ADR & Use
Definition
MOA: inhibits active form of renin by binding where angiotensinogen would bind; however since prorenin can still convert some angiotensinogen to AngI via PRR, not all AngII is stopped
Term
aliskiren
Definition
Direct Renin Inhibitor
oral
Use: HTN (investig. CHF & CKD
Term
3 drug classes for treating CHF
Definition
Beta Blockers - bisoprolol, metaprolol, carvedilol
ACEi
Diuretics - Loop (don't decrease mortality)
Term
Glomerulus
fxn & drug
Definition
filter everything :)
Term
proximal convoluted tubule
fxn & drug
Definition
reabsorb most Na & HCO3-
CAi
Term
proximal straight tubule
fxn & drug
Definition
a/b reabsorb
osmotic diuretics
Term
thin descending loop of henle
fxn & drug
Definition
H2O reabsorb
osmotic diuretics
Term
thick ascending limb of henle
fxn & drug
Definition
reabsorb 2nd most Na & Cl
Loop diuretics
Term
distal convoluted tubule
fxn & drug
Definition
reabsorb Na/Cl
TZ diuretics
Term
distal straight tubule & collecting duct
fxn & drug
Definition
fine tune Na reabsorb; couple with K & H secretion
Na channel inhibitors & aldosterone antagonists
Term
CAi
MOA, SOA, e-lyte effects, uses
Definition
MOA: disables Na/H antiport
via inhibition of CA which converts H2CO3 to CO2 + H2O in lumen then back to H2CO3 in cell where it donates a H+ to be secreted while Na is reabsorbed
SOA: PCT
e-lyte effects: acidosis; hypokalemia
uses: alkalosis, urine alkylization, epilepsy, altitude sickness, glaucoma
Term
acetazolamide
Definition
CAi
po/IV
Term
methazolamide
Definition
CAi
po
Term
dorzolamide
Definition
topical
Term
Osmotic diuretics
MOA, SOA, uses
Definition
MOA: filtered but not reabsorbed; increases osmolarity
SOA: thin descending loop & straight proximal tubule
uses: emergency ICP&IOP
Term
mannitol
Definition
osmotic diuretic
IV
Term
glucose
Definition
osmotic diuretic IV
Term
Loop Diuretics
MOA, SOA, e-lyte effs, other ADRs, uses
Definition
MOA: inhibit NaK2Cl symporter -> Na & Cl don't reabsorb ->urine must be diluted -> pee :)
SOA: thick ascending limb
e-lyte effs: hypokalemia (Na exchanges with K in collecting duct), alkalosis (Na exchanges with H in collecting duct), hypocalcemia&hypomagnesemia (Ca & Mg rely on symporter to create membrane potential to absorb via tight jxn)
ADRs: resistance (usu combine w/TZ), hypersensitivity (if sulfa), ototoxicity
Uses: CHF, ARF (works when GFR<30), hypercalcemia due to breast/prostate cancer
Term
furosemide
Definition
Loop Diuretic
Term
bumetanide
Definition
Loop Diuretic
Term
torsemide
Definition
Loop Diuretic
Term
ethacrynic acid
Definition
NonSulfa Loop Diuretic
Term
Thiazide Diuretics
MOA, SOA, e-lyte effs, uses
Definition
MOA: inhibit Na/Cl symporter -> Na & Cl don't absorb -> urine must be diluted -> pee :)
SOA: DCT
e-lyte effs: hypokalemia, hypercalcemia (Ca is reabsorbed at DCT; drug causes more o_o)
uses: HTN
Term
chlorothiazide
Definition
TZ Diuretic
Term
hydrochlorothiazide
Definition
TZ Diuretic
Term
metolazone
Definition
TZ-Like Diuretic
thus effective w/GFR < 30
Term
chlorthalidone
Definition
TZ-Like Diuretic
thus effective w/GFR < 30
Term
Na Channel Inhibitors
MOA, SOA, e-lyte effs, uses
Definition
MOA: bind & inhibit Na channel by bein' similar :)
SOA: straight distal tubule & collecting duct
e-lyte effs: hyperkalemia (due to Na/K exchange being blocked)
Uses: Combo w/TZ or Loop
Term
amiloride
Definition

Na Channel Inhibitor

used Liddle syndrome- mutation in epithelial of channels --> excessive Na+ reabsorption(hypernatremia) and potassium reabsorption(hypokalemia) that causes HTN

Term
triamterene
Definition
Na Channel Inhibitor
Term
Aldosterone Antagonists
MOA, SOA, e-lyte effs
Definition
MOA: binds mineralocorticoid receptor in place of aldosterone -> decreased Na Channels, decreased Na/K ATPase -> decreased Na reasbsorp & K secretion
SOA: distal straight tubule & collecting duct
e-lyte effs: hyperkalemia due to block of secretion
Term
spironolactone + ADR
Definition
aldosterone antagonist
nonsel; also binds progesterone receptor -> hirsutism & manboob
Term
eplerenone + ADR
Definition
aldosterone antagonist
selective; causes worse hyperkalemia thus caution in ACEi or ARF
Term
Vasopressin V2 Effects & Use
Definition
Gs -> increased synthesis & transloc of aquaporins -> more H2O reabsorbed during high blood osmolarity
use: central diabetes insipidus (pt cannot synth ADH)
Term
Vasopressin V1 Effects & Use
Definition
Pressor
Gq -> increased IC Ca -> sm musc contraxn
use: shock/gastric bleeding
Term
Desmopressin/DDAVP
Use, Admin
Definition
V2 agonist
peptide
uses: central diabetes insipidus, nocturnal enuresis, clotting disorders (V2 exists on endothelial cells which sec VWF)
admin: po, iv, in
Term
conivaptan
use, effects, admin
Definition
nonsel vasopressin antagonist
use: SIADH
effects: aquaresis
admin: IV
Term
tolvaptan
use, effects, admin
Definition
V2 selective
use: SIADH
effects: aquaresis
admin: IV, po
Term
6 Vasodilators for CHF
Definition
ACEi (DOC)
ARB
BidiL
nitroprusside (acute)
nitroglycerine (acute)
nisiritide (acute)
Term
4 Drug Classes for CHF
Definition
Diuretics
Vasodilators
(+)Inotropes
B1 Antagonists
Term
5 (+) Inotrope Classes
Definition
B1 agonist (dobutamine) (acute only)
dopamine (Gs) (acute only)
glucagon (Gs) (acute only)
PDE-3 inhibitors (acute only)
digoxin (acute or chronic)
Term
PDE-3 Inhibitors
MOA, SOA, Uses
Definition
MOA: raise cAMP -> increased PKA -> increased phosphorylation of SR -> increased contractility
SOA: heart muscle
Use: CHF
Term
milrinone
Definition
PDE-3 Inhibitor
Term
inamrinone
Definition
PDE-3 inhibitor
ADR of thrombocytopenia
Term
digoxin
MOA, ADRs, Metabolism, Use
Definition
MOA: EC inhibits Na/K ATPase pump (3Na/2K) -> Na buildup -> Na leaves by Na/Ca exchange -> Ca buildup -> increased contractility
ADRs: nausea, yellow tinted vision, arrhythmias
Metabolism: unchanged by kidney
Use: CHF
Term
Nesiritide MOA, Effects, Uses
Definition

Natrecor MOA: binds BNP receptor -> memb guanylate cyclase -> cGMP -> PKG -> sm musc relax/vasodil Effects: decreased preload/afterload & increased GFR & diuresis due to dilation of renal artery

Uses: acute HF (not given chronically can increase mortality and kidney failure)

 

Term
Name 5 causes for arrhythmias
Definition
ectopic beats due to ischemic tissue
e-lyte abnormality e.g. high K
adrenergic drugs increasing HR
digoxin increasing IC Ca++
re-entry circuit
Term
4 Classes of Slow Conduction Tissue Decreasing Agents
Definition
Adenosine
B Blockers
CCB (nonDHP)
Digoxin
Term
Digoxin
2 Effects
Definition
1.) inhibit Na/K ATPase -> increase IC Ca++ -> (+)ino
2.) central vagal (parasymp) effect -> ACh onto Gi (M2/M4)
a.) -> decreases cAMP -> decreased Ca entry into fast conduction tissue -> decreased pacemaker current
b.) -> opens K channels -> fast conduction tissue hyperpolarizes -> longer refractory period
Term
Adenosine
MOA, admin, indications
Definition
MOA: activates A1 receptor on SA/AV Node -> similar to M2/M4 effects of digoxin
Admin: rapid IV bolus so cells don't absorb it all before it reaches the heart (stored for ATP creation)
Uses: SupraVentricular Tachycardia acutely -> actually stops heart for a sec
Term
4 Classes of Antiarrhythmics
Definition
I) Na Channel Blockers
II) Beta Blockers
III) K Channel Blockers
IV) NonDHP CCBs
Term
lidocaine
uses, monitoring
Definition
Class IB Na Channel Blocker
use: IV drip after MI
monitor blood levels -> too high = coma, seizure, slurred speech
Term
mexilitine
Definition
Class IB Na Channel Blocker
Term
Class IB Na Channel Blockers
Tau Recovery
Definition
Rapid dissc from resting state
Preferentially block ischemic tissue bc more are inactive @ a given time due to more depolarized state (-75mV vs -90mV healthy)
Term
flecainide
Definition
Class IC Na Channel Blocker
Term
propafenone
Definition
Class IC Na Channel Blocker
Term
diisopyramide
Definition
Class IA Na Channel Blocker
antimuscarinic ADRs
Term

procainamide

class

metabolism

ADR

Definition

Class IA Na Channel Blocker metabolized by PII N-acetyl transferase --> Lupus like syndrome

Agranulocytosis = decrease in WBC

Term
quinidine
Definition
Class IA Na Channel Blocker
can cause cinchonism -> visual disturbances& ear ringing
Term
ibutilide
Definition
K Channel Blocker
Term
sotalol
Definition
K Channel Blocker
Term
dofetilide
Definition
Tikosyn
K Channel Blocker
excr. unchanged in kidney so monitor levels
Term
amiodarone
benefits & ADRs
Definition
K Channel Blocker
shown to decrease mortality*
really REALLY long t1/2; in your body a year after d/c
ADRs: pulmonary fibrosis, liver dysfxn, thyroid dysfxn, blindness
Term
dronaderone
Definition
K Channel Blocker
shorter t1/2 than amiodarone
Term
Class IC Na Channel Blockers
Tau Recovery
Definition
Very slow dissc from resting state
-> can slow a healthy heartbeat
Term
Na Channel Blocker MOA
Definition
Increases refractory period by taking some inactive receptors out of equilibrium for longer
Term
K Channel Blockers
MOA, ADRs
Definition
MOA: prolong plateau & delays delayed rectifier current -> Na channels stay inactive for longer bc they can't recover yet
ADRs: Torsades de Pointes arrhythmia due to increased IC Ca++
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