Pharmacology Flashcards
Loop Diuretics MOA
inhibits Na+/K+/CI- in ascending loop of henle which allows more water and CI- to travel to distal tubule
Loop diuretics MOA in HTN
Arteriolar vasodilator and diuretic effect (decreases peripheral resistance)
AE of loop diuretics
Orthostatic hypotension / Hypokalemia / hypomagnesemia / hypochloremia / hyponatremia / metabolic acidosis
What is Elperenone and its MOA
New aldosterone agent that selectively binds to mineralocorticoid receptors and blocks aldosterone
Feature of Elperenone
It has less affinity for steroid receptors compared to spironolactone
Canrenoate & Canrenone are…
metabolites of spironolactone
What do the 2 metabolites of spironolactone do and treat
they bypass hepatic metabolism and treat primary or secondary hyperaldosteronism / HTN / CHF / ascites due to hepatic cirrhosis
Which of the following are vasodilators ?
sodium nitropursside / nesirite / hydralazine / minoxidil
What is sodium nitroprusside and what does it do ?
It is a vasodilator and it decreases cardiac work + no reflux tachycardia + decreases pre load on heart
MOA of sodium nitroprusside
It makes RBCs convert nitropursside to NO - also relaxation by non-enzymatically to NO by glutathione
What are the AE of sodium nitroprusside ?
palpitation / abdomen pain / cyanide toxicity / lactic acidosis
What causes SE of sodium nitroprusside ?
the release of cyanide (thiocyanate)
Kinetics of nitroprusside
during biotransformation of nitroprusside. cyanice is produced which is then converted to thiocynate in the liver and excreted by the kidneys
What is Nesiritide
a recombinant form of human natriuretic peptide
Where does nesiritide release from and what does it do ?
it is secreted by the ventricles and increases cGMP
what does nesiritide cause ?
natriuresis
MOA of hydralazine
molecules combine with receptors in the endothelium of arterioles -> NO release -> relaxation of vascular smooth muscle -> fall in BP
How is hydralazine taken ?
combination with isosorbide dinitrate
What do beta blockers do for CHF
decrease reflux tachycardia + load on heart
What is an advantage of carvedilol ?
it reduces free radical induced lipid peroxidation and prevents cardiac and vascular smooth muscle mitogenesis
What is a SE of non-specific BB carvedilol ?
bronchoconstriction with higher doses
What are DI of carvedilol and what does the CYP one do ?
CCB / Cimetidine / CYP2D6 –> increases levels of carvedilol
What are the positive inotropes and what does inotrope mean ?
Digoxin, dopamine, dobutamine, milrinone / it means contraction
What can positive inotropes lead to ?
Lusitrophy
What does digoxin treat and what is the moa for each one ?
CHF -> increases calcium availability which reverses HF
Atrial fibrillation -> decrease HR / blocks A-V nodal conduction
Another MOA is the Na+/K+ ATPase
-> more Na+ in
When Digoxin reverses HF, what does that lead to ?
CO returns to normal with dilated heart, with tachycardia / and also decreases peripheral edema + congestion
Main ADRs of digoxin ?
Hallucination, disturbed vision
What are digoxins digital toxicities
Narrow therapeutic index / depends on electrolytes
What are the non-digital positive inotropes that resemble NE
Dopamine / dobutamine / amrinone / milrinone
What type of drugs are amrinone and milrinone
Theophylline drugs that inhibit phosphodiesterase and have positive inotropic activity and are inotropic vasodilators
Whats the MOA of non-inotropic drugs
inhibit peak III cAMP phosphodiesterase isoenzyme in cardiac + vasculature
Whats a DI of non-inotropic drugs
forms precipitate with IV furosemide
Whats the ARNI + ARB combination
Sacubtril + valsartan = entresto
What kind of drug is entresto ?
nephrylism inhibitor
what is nephrylism ? and what amplifys its effect
endopeptidase that has naturetic + vasodilatory effects
valsartan amplifies the effects
is sacubitril a pro-drug or not and if it is what is is activated by
it is a pro drug and it is activated by esterase hydrolysis
what does entresto do for patients with CHF
reduces risk of cardiovascular death + hospitalization with reduced ejection rate for patients with reduced ejection fraction
what kind of drug is Ivabradine and its MOA
1) HR lowering drug
MOA - selectively inhibits the “funny” channel pacemaker in SA node -> HR + more blood flow to myocardium
What kind of patients is ivabradine good for ?
patients with ejection rate of < or equal to 35% and has less SE
Which ones are the OD and what are OD and hypertonic solutions used for
mannitol, sorbitol, and isosorbital and used for cerebral edema and acute renal failure
What are features of ODs
LMW + hydrophilic and pass through bowmans capsule into renal tubules
What does mannitol decrease
intraocular + intracranial pressure
what is used to treat metabolic acidosis
sodium bicarbonate
what are examples of hyperkalemia agents
calcium chloride/gluconate, sodium bicarbonate, dextrose-insulin infusion, albuterol nebulizer, furosemide, kayexalate
What can hyperkalemia drugs lead to
cardiac arrest
What are drugs that treat hyperphosphotemia
calcium carbonate/acetate, sevelamer & lanthanum, aluminum hydroxide gel
What kind of disease is sevelamer used for and what does it do
used in patients with chronic renal disease and binds directly to phosphate
Lanthanum MOA
Breaks down in acid environment of the GI tract -> release lanthanum ions bind to dietary phosphate which is why its taken with food
Everything about erythropoietin stimulating agents
- used for anemia of chronic renal failure
- 2 types -> erythropoietin alpha and darbepoetin alpha
- recombinant human erythropoietin
MOA of desmopressin and what is it used for
- increase cyclic AMP in renal tubular cells which lead to retention of water in the body
- bleeding and diabetes insipidus
Everything about potassium chloride
1) slows down HR
2) used for hypokalemia because it increases K+
What are the DIs of potassium chloride and why are they an interaction
ACE inhibitors and K-sparing diuretics (Sprinolactone, Traimetene, Amilornone) and because they elevate a persons K+ levels
What does calcium gluconate do and treat ?
increase calcium levels + treats hyperkalemia
What is Cinacalet and what does it do ?
it is a calcium sensitizer that decreases PTH in patients with renal failure
What is Doxercalciferol ?
It is a vitamin D2 analog that undergoes metabolic activation in vivo to 1a,25-dihydroxyvitamin D2, a naturally occurring, biologically active form of vitamin D2
Everything about vaptans
1) Tolvapatan (1st one) / Conviaptan
2) Hyponatremia is defined as serum sodium concentration <135
3) Vaptans are nonpeptide vasopressin receptor antagonists (VRA)
4) VRAs offer a novel therapy for water retention
5) Conivaptan is a V1 a/V2 nonselective VRA approved for euvolemic and hypervolemic hyponatremia
