Antihypertensives Flashcards
What are cardiac output and peripheral vascular resistance controlled by
Baroreflexes
&
Renin-angiotensis aldosterone system (RAAS)
What are the different types of hypertension
Essential
Malignant
Resistant
Pulmonary
Pseudo
White coat / office
Isolated systolic
What is the general MOA of diuretics
Increase water and sodium excretion to lower blood volume which in turn will decrease BP
What are end stage complication of uncontrolled HTN
Heart disease
Heart failure
Stroke
CKD
What are the categories of antihypertensive drugs
Diuretics
ACE inhibitos
ARBs
Ca2+ blockers
Beta blockers
Alpha blockers
What are the different categories of diuretics
Distal tubule
K-Sparing
Loop diuretics
Carbon anhydrase inhibitor
Osmotic
What drugs make up distal tubule diuretics (Thiazides)
Hydrochlorothiazide
Chlorthalidone
Metolazone
Indapamide
What is the MOA of thiazide diuretics
Inhibit Na+ and Cl- reabsorption in the distal tubule resulting in increase urine output
What is the indication of use for hydrochlorothiazide
Starting agent for HTN, Chronic edema, Idiopathic hypercalcinuria
*treats CaOx stones in Meneires disease and nephrogenic diabetes insidious
What are the pharmacokinetics of hydrochlorothiazide
Oral (onset 2 hours)
Absorbed rapidly and eliminated mostly unchanged
What are the adverse effects of hydrochlorothiazide
Increased digitalis / lithium toxicity
Hypokalemia if given w/ corticosteroids / ACTH
Orthostatic hypotension with EToH/ Barbituates/ narcotis
Contraindicated in gout
Which type of diuretic can be paired with thiazide or loop diuretics
Potassium sparing to mitigate potassium wasting
What is the indication for chlorthalidone
HTN, HF, hypercalciuria, Diabetes
Which thiazide is available IV
Chlorthalidone
What is the pharmacokinetics of chlorthalidone
Oral / IV
Long 1/2t and low bioavailability
excreted in urine unchanged
What are the side effects of chlorthalidone, metolazone, and indapamide
Hyponatremia, hypochloremia, hypotensions, hypokalemia
What is the indication for metolazone
Additive treatment to loop diuretics for tx of edema in HF
10x more potent that HCTZ
Safe in renal insufficiency
What is the indication for indapamide
HTN in decompensated HF
**Not commonly used
What are the pharmacokinetics of indapamide
Oral
Hepatic metabolism and renal excretion
*AKA excreted in urine and bile
Which drugs make up loop diuretics
Furosemide
Bumetanide
Torsemide
What is the MOA of loop diuretics
Inhibits Cl- and Na+ reabsorption = prevention of passive reabsorption of water
Which loop diuretic is most common
Furosemide
Which loop diuretic is preferred in patients with low GFR and in hypertensive emergencies
Furosemide
What is the indication for furosemide
Needing to move large volumes of fluid
->HF, Decamp. Cirrhosis, acute pulm. edema
Hypercalcemia
*Can combine with thiazide
What are the pharmacokinetics of furosemide
Oral
Diuresis begins 60min post admin and lasts 8 hours
Hepatic metabolism nd renal excretion
Which drugs will inhibit furosemide
Probenecid
indomethacin
What drug interaction will loop diuretics have
Digoxin
K+ sparing diuretics
Lithium
NSAIDS
Which patients do you need to use extra caution with in regards to loop diuretics
Patients with sulfa allergies
What are some common adverse effects with furosemide
Hyponatremia, hypochloremia, dehydration, ototoxicity, hyperglycemia
What is the most potent loop diuretic
Bumetanide
What is the indication for bumetanide
Edema caused by HF
CKD
Cirrhosis
hypercalcemia
What are the pharmacokinetics of bumetanide
Oral
Onset 30-60min
Duration 4-6 hours
What are some adverse effects of bumetanide
Dehydration
severe myalgias
What is the indication of torsemide
Edema caused by HF
CKD
Cirrhosis
Hypertension
Hypercalcemia
What are some adverse reactions to torsemide
Dehydration
ototoxicity
headache
dizziness
What are the K+ sparing diuretics
Spironolactone
Eplerenone
Amiloride
Triamterene
Acetazolamide
Mannitol
What is the MOA of K+ sparing diuretics
inhibits K+ secretion and influence sodium excretion
What is the indication for spironolactone
HTN
Edema in HF
Ascites
nephrotic syndrome
hyperaldosteronism
What is spironolactone often prescribed with
Thiazide/loop diuretics to counteract K+ wasting effect
Which K+ sparing meds are aldosterone antagonists
Spironolactone
eplerenone
What are the pharmacokinetics of spironolactone
Oral
Effects can take up to 48hours to set in
What are the adverse effects of spironolactone
Gynecomastia
hyperkalemia
risk of digitalis toxicity when coadministered
What is the indication for eplerenone
Edema in HF
Resistant HTN
primary Hyperaldosteronism
What are the indications for amiloride
3rd / 4th line to tx HTN, HF
May correct polyuria/polydipsia due to lithium induced nephrogenic diabetes insipidus
What is the MOA of Amiloride
Inhibit K+ loss by direct blockade of Na+/K+ exchange in the distal nephron
What are the adverse reactions with amiloride
Hyperkalemia
Vomiting
Leg cramps
Dizziness
*Glucose intolerance in diabetics
What is the indication for triamterene
HTN
Edema
alone or in combo
What are the pharmacokinetics of triamterene
Oral
Initial response develops within hours
What are the adverse reactions of triamterene
Blue urine
Hyperkalemia
leg cramps
dizziness
What is the indication of Acetazolamide
Chronic open angle glaucoma
prophylaxis of altitude sickness
What is the MOA for Acetazolamide
Inhibits carbonic anhydrase which promotes renal excretion of Na+/K+, bicarb, and water
What are the pharmacokinetics of acetazolamide
Oral / IV
Eliminated renally
What are the adverse reactions of acetazolamide
Metabolic acidosis
renal stones
Hyperammonemia in cirrhotic patients
NO IN SULFA ALLERGIES
What are osmotic diuretic drugs
Mannitol
What is the indication of mannitol
Maintains urine flow following acute toxic ingestion of substances capable of producing acute renal failure (Lithium excretion)
Reduction in ICP
Glaucoma TX
What is the MOA of mannitol
Incr concentration of filtrates in the kidney and blocks reabsorption of water
What are the pharmacokinetics of mannitol
IV
Onset 30-60 min and lasts 6-8 hours
*safe in pregnancy
What are the side effects of mannitol
HA
Nausea
dizziness
polydipsia
dehydration
confusion
chest pain
Why can thiazides not be used in the treatment of hypercalcemia
Thiazides can exacerbate hypercalcemia by increasing tubular calcium resorption
Which drugs are ACE inhibitors
Captopril
Enalapril
Lisinopril
What are the indications of use for ACE inhibitors
Treatment of:
HTN
DM
Stroke
MI
HF
CKD
*preferred in patients with diabetic neuropathy
What is the MOA of ACE inhibitors
inhibits ACE which reduces levels of angiotensin 2, suppress aldosterone excretion, decrease peripheral resistance and increase sodium and water retention
What are some contraindications with ACE inhibitors
Contra in pregnancy
-Interactions w diuretics, antihypertensives, drugs that raise K+ levels, lithium, NSAIDS
What is the pharmacokinetics of captopril
oral 2-3x/day
dose adjust in kidney disease
What are the adverse effect is captopril
First dose hypotension, cough, hyperkalemia, renal failure, angioedema, neutropenia, proteinuria
What are the adverse effects from enalapril
First dose hypotension, cough, hyperkalemia, renal failure, angioedema, proteinuria
What are the pharmacokinetics of enalapril
Oral (pro-drug) / IV
Dose adjust in kidney disease
What are the adverse effects of lisinopril
First dose hypotension, cough, hyperkalemia, renal failure, angioedema, neutropenia, proteinuria
What are symptoms of severe hypercalcemia
Neuromuscular effects
GI effects
Renal effects
CV effects
What is the safest and most effective treatment of hypercalcemic crisis
Saline rehydration
Furosemide diuresis
What is nephrogenic diabetes insipidus
Where kidneys have partial or complete resistance to effects of antidiuretic hormone (vasopressin)
-polyuria / polydipsia are signs
What is the main goal while treating nephrogenic DI
Proper fluid intake and reduction in urine output
What drugs can be used to help treat nephrogenic DI
HCTZ -> corrects hypernatremia
*Sometimes in conjunction with amiloride to help body maintain K+ level
What drug classes make up the renin-angiotensin aldosterone system (RAAS)
ACE inhibitors (ACEi)
Angiotensin receptor blockers (ARBs)
Aldosterone antagonists
Where is Renin released from
Kidneys
What is the main MOA of ACEi
Angiotensin converting enzyme (ACE) is released from the lungs and converts angiotensin 1 into angiotensin 2
angiotensin 2 then stimulates vasoconstriction and causes the adrenals to release aldosterone
Aldosterone then causes the kidneys to increase reabsorption of N+ and Cl- = increase BP
Why are ACEi preferred in patients with diabetic nephropathy
B/c glucose levels are not effected and drugs are renoprotective
Which drugs are in the ARBs class
Losarten
Valsartan
Candesartan
Olmesartan
What is the MOA for ARBs
-Blocks angiotensin II receptors in blood vessels, adrenals, and other tissues, dilation of arterioles and veins
What is the indication for Losartan
HTN
Stroke prevention
diabetic neuropathy
reduces uric acid levels
What was the first ARB approved for HF
Valsartan
What is the indication for olmesartan
HTN (mean BP reduction)
What is the indication for Candestartan
HTN
HF
What is the pharmacokinetics of Losartan
Oral 1x daily
Extensive first pass metabolism
What is the pharmacokinetics of valsartan
Oral
2x daily
What are the pharmacokinetics of candesartan and olmesartan
oral
1x daily dosing
What are the adverse effects / contraindications of losartan, valartan, candesartan
Angioedema, renal failure, dry cough, rash, altered taste
-Drug interactions: additive effect w antihypertensive drugs
-Contra in 2nd and 3rd trimesters of pregnancy
What is the adverse reaction and contraindication of olmesartan
Drug interactions: additive effect w antihypertensive drugs
-Contra in 2nd and 3rd trimesters of pregnancy
What drug is a renin inhibitor
Aliskiren
What is the MOA of Aliskiren
Inhibits renin by binding to it, preventing the cleavage of angiotensinogen
, acting early in the RAAS
What is the indication for aliskiren
HTN
*side effects make it less favorable
What are the side effects / contraindications of aliskiren
Diarrhea
Cough
Angioedema
*contraindicated in pregnancy
What are the pharmacokinetics of aliskiren
Oral
CYP metabolism
Bioavailability low, becomes lower with high fat meal
1/2t 24 hours
What are the endothelia antagonists
Ambrisentan
Bosentan
What is the MOA of ambrisentan
Slectively blocks type A endothelin receptors
What is the indication for ambrisentan
PAH
Improve exercise, delay clinical worsening
*Can be used in combo with tadalafil
What is the indication for bosentan
PAH
Decrease digital ulcerations in patients with scleroderma
What are the adverse effects of Ambrisentan
Edema
nasal congestion
palpitations
abdominal pain
constipation
