Antihypertensive Agents Flashcards
Which drugs have a side effect of a cough and what is the cause of that?
the ACE inhibitors cause cough due to reduced inactivation of bradykinin (more active)
How can ace inhibitors result in hyperkalemia
If patient already on potassium-sparing diuretics.
What are side effects of ACE inhibitors
hyperkalemia, hypotension, cough, taste changes, skin rash, angioedema
What are the curable forms of hypertension?
RECAP ABCDE
R: renal disease. E: estrogens. C: Coarctation
A: Aldosteronism P: Pheochromocytoma
A: Alcoholisms B: Brain lesions C: Cushings syndrome D: Drugs Sympathomimetic
E: excessive thyroxine or para.t.hormone
What is the function of ACE inhibitors, Angiotensin Receptor Blockers, and Renin Inhibitors?
The goal of all 3 is to decrease Angiotensin II, the most potent vasoconstrictor of the body, and decrease aldosterone production.
What are Angiotensin II effects on the body
- decreased output of sympathetic NS
- vasodilation of vascular smooth muscle
- Increased levels of bradykinin
All three lead to decreased blood pressure
What is Aldosterone’s effect on the body?
Reduced retention of sodium and water, leading to reduced blood pressure
What are the 2 drug names to remember as ACE Inhibitors?
Captopril and Enalapril (both are oral)
What are the uses of ACE inhibitors?
Congestive heart failure, hypertension, and diabetic renal vascular disease (nephroprotective)
When are ACE Inhibitors contraindicated?
Pregnancy due to fetotoxicity
Excessive response after renal artery stenosis
What drugs are the Angiotensin II receptor blockers (2)
Losartan and Candesartan.
What is the action of Angiotensin II Receptor Blockers?
Inhibit Angiotensin II vasoconstriction
Inhibit aldosterone release
- do NOT alter bradykinin (less cough)
- do NOT adversely affect lipid levels, glucose, uric acid
What are the side effects associated with Angiotensin II Receptor Blockers?
Hyperkalemia Neutropenia Elevation of serum AST and ALT Angioedema Contraindicated in pregnant women (fetotoxicity)
What is the name of the renin inhibitor?
Aliskiren. Same function as ACE and ARB
What are the names of the Calcium channel blockers to remember (4)
Amlodipine, Diltiazem, Nifedipine, Verapamil
What do calcium channel blockers do?
Block Type L Calcium Channels, which reduces constriction, promote excretion of sodium.
Some Calcium channel blockers cause bradycardia and tachycardia. Which ones cause brady and which ones cause tachy?
Tachycardia occurs Nifedipine (all the PINES), and bradycardia occurs with Verapamil and Diltiazem. All dilate coronary vessels, but only Verapamil and Diltiazem decrease AV conduction.
What are some side effects of Verapamil and Diltiazem?
Bradycardia, hypotension, CHF, Skin rash, Constipation
What are side effects of dihydropyridines?
PINES: Reflex tachycardia, hypotension, dizziness, skin rash, peripheral edema, constipation
Which antihypertensives should diabetics avoid?
Calcium channel blockers, these reduce glucose tolerance
What drugs have sympatholytic action?
Non-selective alpha blockers: Phenoxybenzamine and Phentolamine.
Selective alpha 1 blockers: Doxazosin
Non-selective Beta blockers: Propranolol
Selective B1 blockers: metoprolol
Which alpha blocker can be given oral, IV, or IM? Which one just Oral?
Phentolamine all 3, Phenoxybenzamine just oral
What are side effects of Alpha non-selective blockers?
postural hypotension, tachycardia, nasal congestion, impotence, increased GI motility
What are side effects of selective alpha 1 blockers?
dizziness and headache, may increase HDL (good cholesterol), can cause orthostatic hypotension with first dose or increasing dose. Experience Na/water retention so combine with diuretic.
What are side effects of Beta Blockers?
N,V,D. Heart failure, hypotension, increased airway resistance, depression, fatigue, impotence, decreased libido.
What are contraindications to beta blockers
Diabetes and asthma
Sudden withdrawal of beta blockers can lead to what?
exacerbation of angina and myocardial infarction
Do patients on Beta Blockers tend to show an increase or decrease in LDL/TAGs?
Increase
What is the mechanism of Beta Blockers?
reduce beta 1 activation of heart: decrease in CO
Reduce renin release: decreased resistance, decreased aldosterone which leads to decreased sodium/water retention. all these work to decrease BP.
What are the names of the non-selective beta blockers we need to know?
Carteolol, Penbutolol, Pindolol, Propranolol, Timolol (most potent)
What are the names of the Beta 1 selective blockers (3)
Acebutolol, Atenolol, Metopropolol
What are the combined Alpha 1 and Beta Blockers?
Carvedilol and Labetalol. Carvedilol used in patients with CHF, structural changes in heart blocked.
What is the name of a selective beta 1 blocker with direct vasodilation action
Nebivolol.
What are the Third step drugs for hypertension?
the peripheral adrenergic antagonists. Guanadrel and guanethidine.
What is the action of Guanadrel and Guanethidine
Guanadrel is rapid and Guanethidine is longer acting. Both treat severe hypertension by interfering with release/storage of Norepi. “Big Guns” with many side effects
What are the side effects of Guanadrel and Guanethidine?
orthostatic hypotension, exercise hypotension, sexual dysfunction, diarrhea.
What medications can inhibit the function of Guanethedine and Guanadrel?
tricyclic antidepressents, phenothiazines and ephedrine can inhibit uptake and decrease the antihypertensive effects of guanadrel and guanethidine.
Reserpine does what in the body?
Inhibits neuronal and vesicular catecholamine uptake, preventing storage and leading to depletion of NTs. It treats hypertension.
What are side effects of Reserpine?
severe mental depression, nasal congestion, diarrhea
Where do the sympatholytic anti-hypertensives bind?
They bind to the alpha-2 receptors and imidazoline receptors pre-synaptically to decrease sympathetic outflow from the CNS.
What are the effect of the central sympatholytic anti-hypertensives?
Reduce TPR and Blood pressure
CO and Blood flow to vital organs is unchanged
Limited reflex responses compared to peripherally acted drugs
What are the drugs with central sympatholytic actions
Clonidine
Guanabenz
Guanfacine
Methyldopa
What are side effects of methyldopa
Coomb’s positive hemolytic anemia
false positive tests in diagnosis of pheochromocytoma
sedation and drowsiness
Often given with diuretic
What are side effects of all centrally acting sympatholytics?
sexual dysfunction (impotence, decrease libido, impaired ejaculation, gynecomastia) and rebound hypertension with rapid withdrawal in all but methyldopa
What are the arteriolar dilators?
Diazoxide, Hydralazine, Minoxidil, Nitroprusside, Fedoldapam
What is the mechanism for the arteriolar dilators and what are they used for?
act directly on arteriolar vascular smooth muscle to cause relaxation
increase renin release
rapidly reduces BP in hypertensive crisis, hypertensive encephalopathy, eclampsia
- baroreceptor activation limits their long term use
What is the action of Diazoxide?
acts as a potassium channel activator, can cause hyperglycemia
Hydralazine has what side effects?
chronic high doses can produce a lupus-like syndrome
may precipitate angina or myocardial infarctions
Headache, tachycardia, palpitations, sweating, flushing
What are side effects of Minoxidil
Headache, tachycadia, sodium and water retention (use with diuretic), hypertrichosis (hair growth on face and body - found in shampoos), marked fluid retention can lead to pericardial effusion
What are the side effects of nitroprusside?
Light sensitive formula so comes in brown bottle, prolongued in overly rapid infusion causes cyanide poisoning
What is the action of Fenoldapam?
D1 receptor agonist, increases renal perfusion while decreasing BP systemically
Which ganglionic blocking agents are used in hypertensive emergencies?
Mecamylamine, trimethaphan
Which diuretics are used anti-hypertensives?
thiazides
Furosemides
Spironolactone
What is the action the thiazides and name the hallmark drug
inhibits Na+/Cl pump in distal tubule, to increase excretion of sodium and water follows. Drug - Hydrochlorothiazide (HCTZ)
What are the uses of thiazides?
Antihypertensive, decrease renal excretion of calcium, fluid reduction in congestive heart failure
What are adverse effects of diuretics acting in distal tubule?
Hyperuricemia, Hypokalemia, Hyponaturemia, Hyperglycemia, Hypercalcemia, Hypokalemic metabolic alkalosis, volume depletion. Efficacy of thiazides decreases with acute kidney issues.
Where do the loop diuretics act and what is the Hallmark drug?
These inhibit the Na+/K+/Cl- pump in the ascending limb. Drug - Furosemide/Lasix.
What are the uses for loop diuretics?
Rapidly remove fluids in ascites, acute pulmonary edema, CHF (within minutes, urine production).
Decrease serum calcium concentration (give hydration + electrolytes with diuretic)
combat chronic kidney disease and to pull fluid off lungs
What are adverse effects of loop diuretics?
Hypokalemic alkalosis, hyperuricemia, hypokalemia, hypocalcemia
What are the Potassium sparing diuretics?
Spironolactone, Eplerenone, Amiloride, Triamterene
Which potassium sparing diuretics inhibit aldosterone receptor?
Spironolactone and Eplerenone - spare potassium, waste sodium
Which potassium sparing diuretics inhibit sodium channels?
Amiloride, Triamterene
What are the uses for potassium sparing diuretics like Spironolactone?
- Treat hyperaldosteronism since Spironolactone is a competitive inhibitor of the Aldosterone receptor,
- as an adjunct diuretic to potassium wasting diuretic
- as an adjunct to ACE inhibitors, Beta Blockers, thiazides and digoxin
What are adverse effects of the Potassium sparing diuretics?
Hyperkalemia, Hyperchloremic acidosis, endocrinological effects of gynecomastia, impotence, menstrual irregularities
Rules for potassium sparing diuretics
don’t give K+ supplements
don’t combine with other K+ sparing diuretics
Careful when combining with Ace Inhibitors
NSAIDs can reduce effects
Which drugs can cause sexual dysfunction?
Thiazides, Sympatholytics, Beta Blockers
