Pharmacology Test 2

• Hypovolemia - elctrolyte changes
• Hyperglycemia
• Increased cholesterol and triglycerides
• Decreased potassium (except with PS)(Affects NaCL/K+ pump)
• Hyperuricemia - gout
• Increase calcium with thiazides
• Decrease calcium with loops
• Impotence

Increases Response

• side effects increase
• response plateaus

• Digoxin
• Lithium
• NSAIDS
• ACE inhibitors
• K+ Supplements

• Resistance
• Thiazide sensitivity to renal function

Increase: heart rate, contractility, renin release (vasoconstriction)

Relaxation of vascular, bronchial and uterine smooth muscle; increase glycogenolysis, increase insulin release, increase tremor

Vasoconstriction, mydriasis, piloerection, and increase glycogenolysis

decrease neuronal transmitter release, increase platelet aggregation, decrease lipolysis, decrease insulin release

• Antagonize (block) the b1 and b2
• receptors:
• –Decrease heart rate

–Decrease contractility

• –Decrease renin release (decrease
• angiotensin II) Major vasoconstriction

• Restore heart rate variability - pt may feel worse initially
• Prevent arrhythmia (common cause of death in HF) occurrence by stopping NE at the site
• Prevent/slow remodeling process
• Inhibit renin secretion

• Bronchospasm
• Heart failure
• Bradycardia/bradyarrhythmias
• Vasospasm
• Metabolic abnormalities
• Hyperglycemia/¯ insulin sensitivity
• Decreased HDL
• Depression (all BP drugs increase risk for depression especially BB)
• Withdrawal syndrome (d/c over 1-2 wks) - huge risk for rebound HTN because of increased sensitivity

• Metropolol
• Atenolol
• Bisoprolol
• Betaxolol
• Nibivolol
• Acebutolol
• Esmolol

• Pindolol
• Carvedilol
• Labetilol
• Propanolol

• Acebutolol
• Pindolol
• NEVER USE IN HF

• Carvedilol (Alpha1 Antagonist)
• Nibivolol (increased NO )
• Labetolol (Alpha 1 Antagonist)

• Inhibit calcium influx @ SA/AV node to slow conduction
• cause vasodilation &/or decreased HR & strength of contraction

• Verapamil 
• Diltiazem
• *Cause other drugs to be metabolized differently

• Amlodipine
• Nicardipine
• Clevidipine
• Nifedipine
• Felodipine
• Nimodipine
• Isradipine
• Nisoldipine

Negative inotropic and chronotropic effects

No effects on conduction in vivo

• Headache
• Flushing
• Pedal Edema
• Constipation
• Hypotension
• Reflex tachycardia - DHP
• Bradycardia, CHF, AV Block - Non-DHP

• Hypotension/dizziness
• Cough/Angioedema (bradykinin?)
• Renal Dysfunction
• Highest risk of ARF: Volume depleted, Renal vascular disease, vasoconstricting drugs
• HyperKalemia: Usual increase <1, greatest risk when SCr >1.6

• K+ Supplements
• NSAIDS (especially with diuretic and/or LFV)
• Cyclosporine

• Benazapril
• Captopril
• Enalapril
• Fosinopril
• Moexipril
• Perindopril
• Quinapril
• Ramipril
• Trandolipril
• *When inhibiting ACE you prevent vasoconstriction

• all work in nephron
• Do NOT work in PCT because NaCL would be reabsorbed further down the line
• Loops work regardless of renal function
• Thiazides are sensitive to renal function
• *Make all BP meds work better; preferred initial agent
• *For HF symptomatic improvement only

• Useful step one or two HTN agent - especially those with DM, post-MI, or high CAD risk
• All pt's with EF <40%
• Start low dose and increase slowly "Target Dose"
• Benefits take time
• Opens efferent arteriole
• DO NOT take during pregnancy especially later

• Work later in the RAAS system
• Don't affect bradykinin - no cough/angioedema
• -artan

• Spironolactone and Eplerenone
• Much more expensive option
• choice in low-renin HTN
• Block aldosterone in kidney, hold K+, excrete NaCL
• Bigger effect on HF - decreased mortality and morbidity, reduced NaCL H2O retention, reduced Myocardial and vascular fibrosis

• Candesartan
• Spresartan
• Irbesartan
• Losartan - preferred in pt's with gout
• Olmesartan
• Telmisartan
• Valsartan
• Azilsartan

• Hyperkalemia.  DO NOT USE IF: K+>5.0, impaired renal function, DM with microalbumuria, using K+ diuretic or K+ supplement
• Gynecomastia (not gender specific)
• Drug interactions

• Aliskiren - works on renin by inhibiting renin activity.  Effects last at least 1 month after d/c
• Efficacy comparable to ACEI's and ARB's
• Long absorption and elimination

Doxazosin, Terazosin, Prazosin

• Vasodilate (bc they block constriction) via alpha1 receptor antagonism
• *significant postural hypotension risk.  Risk decreases over time.
• **Never use alone, use with diuretic
• Combination therapy for BPH

Clonidine, Guanifacine, Guanabenz, Methyldopa

• Turn off sympathetic outflow
• MUST BE USED IN COMBINATION WITH DIURETIC BC sodium/H2O retention

• requires metablism to methylnorepinephrine
• AE's include hemolytic anemia, hepatotoxicity

• sedation, dry mouth, bradycardia, partial tachyphylaxis, orthostatic hypotension, constipation, impotence
• **Withdrawal is a big deal - more so than with BB

• Hydralazine
• minoxidil

• fluid retention
• reflex tachycardia
• headache/flushing
• lupus syndrome - rash, joint pain
• hypertrichosis (minoxidil) - hair growth

Strong effect on heart - weak vasodilatory effect

Strong vasodilation - weak effect on heart (increases HR to compensate for vasodilation)