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57 Cards in this Set
- Front
- Back
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Loop Diuretics
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- Block Na-K-2Cl symporter in ascending loop of Henle (25% of Na reabsorption)
- powerful natriuretic effect - Reach site of action in glomerular filtrate and excreted in urine - Well absorbed orally (parenterally if indicated) - Rapid onset, duration ~6 hrs - "Braking Phenomenon" - Typically require second dosage as renal tubules become sodium avid - IV admin in hospital - take w/ K+ supplements or diet SE's: - Hypokalemia (increased Na to collecting duct) - NOT nephrotoxic - Large doses --> ototoxicity |
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Furosemide
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Loop Diuretic (Must Know)
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Bumetanide
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Loop Diuretic (Must Know)
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Ethacrynic Acid
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Loop Diuretic
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Torsemide
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Loop Diuretic
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Thiazide and Thiazide-Like Diuretics
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- Block Na-Cl symporter in distal convoluted tubule
- Most abundantly prescribed diuretic - Less natriuretic potency = less effective for general edema - Used for hypertension (alone or in combination) --> requires less volume reduction than in edema - Longer duration than loop - Hepatic metabolism - Cause Hypokalemia and increase reabsorption of calcium (use for people prone to kidney stones) - Used at GFR > 30 ml/min - Thiazide + loop --> overcome Na retention in relatively diuretic-resistant edematous patients SE's: - Hyperuricemia (reduced urinary excretion of uric acid --> gout) - Glucose intolerance (K+ depletion on pancreatic beta cell fx) - Increased serum cholesterol - Hyponatremia - Allergy (sulfur containing compoud) |
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Chlorothiazide
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Thiazide (most common)
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Chlorthalidone
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Thiazide - like (need to know)
- Longer acting, more potent |
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Hydrochlorothiazide
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Thiazide (most common) - (Need to know)
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Metolazone
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Thiazide-like
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Potassium-Sparing Diuretics
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- Act in the collecting tubule
- Not associated w/ urinary potassium wasting - Not terribly potent natriuretics and often used in combination w/ loop and thiazides as an anti-kaliuretic |
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Amiloride
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- Potassium Sparing
- Blocks apical sodium channels in collecting tubule (ENaC) - Used in Liddle's syndrome |
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Triamterene
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- Potassium Sparing
- Blocks apical sodium channels in collecting tubule |
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Spironolactone
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- Potassium Sparing
- Aldosterone antagonists - Also stimulates NO production and exerts anti-fibrotic actions - Basolateral side of tubular cell - Not widely used, except in CIRRHOSIS (and CHF) in whom 2ndary aldosteronism --> pathogenesis of edema and ascites formation SE's: - Antagonizes androgen and progesterone receptors --> sexual side effects (gynecomastia, menstrual irregularity, impotence) |
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Eplerenone
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- Potassium Sparing
- Aldosterone antagonists - Basolateral side of tubular cell - Not widely used, except in CIRRHOSIS (and CHF) in whom 2ndary aldosteronism --> pathogenesis of edema and ascites formation SE's: - Fewer sexual side effects than spironolactone |
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Acetazolamide
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- Carbonic Anhydrase Inhibitor
- Inhibits Carbonic anhydrase in proximal tubule bicarbonate reuptake which is linked to Na reabsorption - Mild natriuretic effects because Na reabsorption increases elsewhere SE's: - Negative effect on bicarbonate balance may induce hyperchloremic metabolic acidosis |
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Clonidine
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- Oral agent that stimulates central Alpha-2 - adrenergic receptors in brain leading to reduced sympathetic outflow
- Less sedation than methyldopa, no autoimmune effects, can be given transdermally, still used in multiple drug regimens - Short half-life SE's: - Sedation, bradycardia, orthostatic hypotension - Abrupt withdrawal may lead to rebound hypertension and hyperadrenergic symptoms (tachycardia, sweating, restlessness) |
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Methyldopa
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- Oral agent that stimulates central Alpha-2 - adrenergic receptors in brain leading to reduced sympathetic outflow
- Generally only used in pregnancy related hypertension SE's: - Sedation, bradycardia, orthostatic hypotension - Serious autoimmune hemolytic anemia - Abrupt withdrawal may lead to rebound hypertension and hyperadrenergic symptoms (tachycardia, sweating, restlessness) |
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Doxazosin
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- Selective Alpha-1 antagonist
- Blocks NE induced vasoconstriction as vascular smooth muscle sites --> no inhibitory effect at presynaptic Alpha-2 so inhibition of NE release is maintained - Favorable metabolic effects on lipid profiles and insulin resistance - NIH report suggests they may increase risk of heart failure - Still used sparingly in drug regimens - Used for BPH (prostatic obstruction) SE's: - Edema, orthostatic hypotension, nasal congestion |
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Prazosin
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- Selective Alpha-1 antagonist
- Blocks NE induced vasoconstriction as vascular smooth muscle sites --> no inhibitory effect at presynaptic Alpha-2 so inhibition of NE release is maintained - Favorable metabolic effects on lipid profiles and insulin resistance - NIH report suggests they may increase risk of heart failure - Still used sparingly in drug regimens - Used for high BP, anxiety, panic, PTSD SE's: - Edema, orthostatic hypotension, nasal congestion |
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Tamsulosin
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- Selective Alpha-1 antagonist (prostate selective alpha antagonist -> minimal BP effect
- Blocks NE induced vasoconstriction as vascular smooth muscle sites --> no inhibitory effect at presynaptic Alpha-2 so inhibition of NE release is maintained - Favorable metabolic effects on lipid profiles and insulin resistane - NIH report suggests they may increase risk of heart failure - Still used sparingly in drug regimens - Used for BPH (prostatic obstruction) SE's: - Edema, orthostatic hypotension |
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Beta Blockers
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- Depression of renin release, reduced cardiac output, and some suppression of central adrenergic outflow
- Blockade of vasodilating beta receptors may increase PVR initially, but normalizes w/ chronic use - Provide secondary protection among patients sustaining 1st MI - Management of patients w/ tachyarrhythmias and a-fib - enhance survival in patients w/ heart failure SE's: - Doses titrated to HR - Poorly tolerated in patients w/ underlying heart block or bradyarrhythmias - May cause sexual dysfunction |
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Atenolol
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- Beta-1 selective antagonist (B1 in heart)
- Better for COPD and Asthmatics - Fewer disturbances in glucose and lipid metabolism than non-selective |
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Metoprolol
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- Beta-1 selective antagonist (B1 in heart)
- Better for COPD and Asthmatics - Fewer disturbances in glucose and lipid metabolism than non-selective - Lipid soluble --> better IV |
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Propanolol
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- Non-selective beta antagonist
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Labetalol
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- Alpha-blocking and non-selective beta-blocking effects (1:4 a:B)
- CO preserved - Rapid onset, steep dose-titration curve, often employed in resistant hypertension - Oral and IV standard in treating hypertensive emergencies |
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Carvedilol
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- Alpha-blocking and non-selective beta-blocking effects (1:10 a:B)
- Stimulates NO release from endothelial cells and acts as an anti-oxidant - CO preserved - Used in Heart Failure |
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Nebivolol
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- No alpha blocking but is most B1 selective among the group
- Stimulates NO release and has antioxidant effects - Newest on market |
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ACE Inhibitors
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- Bind to ACE and block the generation of Angiotensin II
- ACE normally degrades bradykinins (increases dilator peptide) - Lower peripheral resistance, restore NO response of endothelium, and reduce vascular hypertrophy - 1st line monotherapy - Suppressed PRA patients need diuretics to help - not useful paired w/ beta blockers - Prolong survival in heart failure and post MI --> reverse LVH - Reduce glomerular capillary pressure and reduce proteinuria by dilating efferent arterioles SE's: - Dry, irritative cough - Angioneurotic edema is a rare but serious side effect - Aldo suppression --> hyperkalemia (diabetes and CKD) --> diuretic may offset |
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Inhibitors of RAS
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- Inhibitors reduce BP by blocking both Ang II mediated vasoconstriction and aldosterone release
- Improve function of vascular wall through various antiproliferative, antioxidative, and antiinflammatory actions - Renoprotective effects --> unique action on glomerular microvasculature |
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Angiotension Receptor Blockers
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- Block AII subtype 1 receptor (AT1) that mediates vasoconstriction, aldosterone release, and assortment of nonhemodynamic AII effects
- AT1 receptor blockade includes JGA receptor by which AII inhibits renin secretion --> increased renin, increased Ang II - Increased Ang II --> more stimulation of AT2 receptors which stimulate vasodilation and antiproliferative effects - ARBs may cause greater RAS than ACEi --> blocks Ang II effects from ACE and non-ACE pathways - Same cardiac and renal protective effects as ACEi - Do NOT potentiate bradykinins and do not induce cough SE's: - Angioneurotic edema very rare, generally minimal side effects |
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Direct Renin Inhibitors (DRI)
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- Bind to catalytic site of renin to block interaction w/ renin substrate (angiotensinogen)
- Antihypertensive effect is comparable to that of other RAS inhibitors |
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Aliskiren
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- DRI
- Effective at reducing ventricular hypertrophy and proteinuria |
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Calcium Channel Blockers
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- Block L-type voltage-gated plasma membrane channel
- Two groups; dihydropyridines and non-dihydropyridines - Particularly effective in blacks and elderly (suppressed PRA) - 3rd drug in regimen - prevent stroke in elderly better than other classes do |
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Amlodipine
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- Calcium channel blocker - DHP 2nd gen
- dilate afferent arteriole - may increase proteinuria and accelerate renal damage - used in combination --> preglomerular dilation offset by reductions in systemic pressure and ACEi/ARB-induced postglomerular vasodilation - pure vasodilator w/ little effect on cardiac contractility or conduction SE's: - Local edema, constipation, headache, flushing |
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Felodipine
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- Calcium channel blocker - DHP 2nd gen
- dilate afferent arteriole - may increase proteinuria and accelerate renal damage - used in combination --> preglomerular dilation offset by reductions in systemic pressure and ACEi/ARB-induced postglomerular vasodilation - pure vasodilator w/ little effect on cardiac contractility or conduction SE's: - Local edema, constipation, headache, flushing |
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Nifedipine
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- Calcium channel blocker - DHP 1st gen
- dilate afferent arteriole - may increase proteinuria and accelerate renal damage - used in combination --> preglomerular dilation offset by reductions in systemic pressure and ACEi/ARB-induced postglomerular vasodilation - Modest effects on cardiac contractility; mainly vasodilator SE's: - Local edema, constipation, headache, flushing |
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Verapamil
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- Calcium channel block - non-DHP
- SLOW A-V conduction and depress myocardial contractility - weaker vasodilator (induce less local edema) - CAUTION when conduction problems or Beta Blockers - Avoided in Heart Failure - Used to control tachyarrhythmias and for rate control in atrial fibrillation |
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Diltiazem
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- Calcium channel block - non-DHP
- SLOW A-V conduction and depress myocardial contractility - weaker vasodilator (induce less local edema) - CAUTION when conduction problems or Beta Blockers - Avoided in Heart Failure - Used to control tachyarrhythmias and for rate control in atrial fibrillation |
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Hydralazine
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- Inhibits IP3-induced release of calcium from sarcoplasmic reticulum --> reducing intracellular Ca++
- opens calcium-activated K+ channels, hyperpolarizing membrane potential --> makes it difficult to open L-type Ca++ channels - Widespread vasodilation induces reflex sympathetic activation and sodium retention --> poor monotherapy - Induce reflex tachycardia SE's: - High doses --> Lupus Like Syndrome |
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Minoxidil
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- Vasodilation via sulfated metabolite of minoxidil which opens ATP-dependent K+ channels
- more potent vasodilator than hydralazine - reserved for severe HTN in advanced CKD - Widespread vasodilation induces reflex sympathetic activation and sodium retention --> poor monotherapy - Induce reflex tachycardia SE's: - Hirsutism precluding use in women - topical solution to treat hair loss (male pattern baldness) in both men and women --> Rogaine |
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Nitroglycerine
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- IV vasodilator
- HTN emergencies |
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Sodium Nitroprusside
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- Vasodilator
- HTN emergencies |
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Antibiotic therapy for UTIs
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far majority caused by coliforms --> tx broad gram-negative coverage
- modified pending urine culture and sensitivity test bactrim most common (nitrofurantoin if sulfa allergy) pyelonephritis --> 5-7 days of fluroquinolone (or 14 days bactrim) sicker --> 3rd gen cephalosporin |
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Cephalosporins
(Cephalexin and Cefazolin) |
- Active against: Gram + and -; successive gens of cephalosporins have less gram + activity, more gram -
MOA: Inhibit bacterial cell wall synthesis Key Adverse effects: Allergy |
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Fluoroquinolones
(Ciprofloxacin, Levofloxacin, Ofloxacin, Moxifloxacin) |
- Active against: Most gram +, some gram -
MOA: Inhibits DNA gyrase enzymes required for bacterial replication Key Adverse effects: Tendon rupture, delirium, corneal damage |
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Penicillins
(Ampicillin and Amoxicillin) |
- Active against: Many gram -, most gram + (except staph aureus) including enterococcus
MOA: Inhibit bacterial transpeptidase (used in cell wall synthesis) Key Adverse effects: Allergy |
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Aminoglycosides
(Gentamicin, Tobramycin, Amikacin) |
- Active against: many gram -
MOA: Inhibit translational activity of bacterial ribosomes Key Adverse effects: Ototoxicity, nephrotoxicity |
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Trimethoprim/Sulfamethoxazole
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- Active against: Many gram - and + (including S saphrophyticus)
MOA: Both component drugs are inhibitors of folic acid metabolism Key Adverse effects: Allergy, myelosuppression |
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Nitrofurantoin
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- Active against: E. coli, staph saprophyticus, some enterococcus
MOA: Multiple bacterocidal effects as both a DNA antagonist and antimetabolite Key Adverse effects: Hypersensitivity pneumonitis and pulmonary fibrosis Used if sulfa allergy prohibits Trimethoprim/Sulfamethoxazole |
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Pseudoephedrine
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- Alpha-agonist --> strengthens sphincter tone
- Used for stress incontinence SE's: Increased BP, anxiety, palpitations |
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Oxybutynin
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- Muscarinic antagonists, antispasmodics --> reduces bladder tone through blockade of muscarinic receptors (and ? Ca channels)
- Used for urge incontinence SE's: Dry mouth, constipation, blurred vision, drowsiness, dizziness |
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Tolterodine
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- Muscarinic antagonists, antispasmodics --> reduces bladder tone through blockade of muscarinic receptors (and ? Ca channels)
- Used for urge incontinence SE's: Dry mouth, constipation, blurred vision, drowsiness, dizziness |
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Mirabegron
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- Beta 3 agonist
- Used for urge incontinence |
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Finasteride
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- 5 Alpha-reductase inhibitor --> shrinks prostate tissue
- Used for prostatic obstruction (BPH) SE's: Reduced libido, sexual dysfunction, gynecomastia |
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Dutasteride
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- 5 Alpha-reductase inhibitor --> shrinks prostate tissue
- Used for prostatic obstruction (BPH) SE's: Reduced libido, sexual dysfunction, gynecomastia |
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Tadalafil
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- PDE 5 Inhibitor
- Used for pulmonary arterial HTN, erectile dysfunction, BPH (prostatic obstruction) SE's: headache, indigestion, flushing |
