Pharmacology Flashcards by Sarah Axelrath

Why are loop diuretics “K wasting”? 2 fold mechanism

Inhibit ascending limb Na/K/2Cl co-transporter, thereby inhibiting reabsorption of 15% of filtered K load
Inhibition of the Na/K/2Cl transporter decreases the passive following (reabsorption) of water; thus, more water remains in the tubule (increased tubular flow) which enhances K+ secretion in the distal segments via flow effects

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Thiazide diuretic - Mechanism

Inhibit NaCl co-transporter in distal tubule; anti-hypertensive effect secondary to decreased plasma volume and decreased CO

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Thiazides - Special considerations

Lose efficacy in later stages of CKD as less drug reaches the distal tubule; loop diuretics indicated at GFR < 30 ml/min

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Spironolactone - Mechanism

Competitively inhibits the mineralocorticoid receptor from binding aldosterone, blocking the aldosterone-dependent up-regulation of Na/K exchange leading to reduced Na resorption and reduced K excretion

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Eplerenone - Mechanism

Competitively inhibits the mineralocorticoid receptor from binding aldosterone

Binds more specifically than aldosterone

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Mannitol - Mechanism, Uses, and Pharmacokinetics

Non-absorbed sugar, produces diuresis by elevating the osmolarity of the glomerular filtrate, decreasing tubular reabsorption of water

Used in management of elevated intracranial pressure

Administered IV

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Acetazolamide - Mechanism, Pharmacokinetics, and Uses

Inhibits carbonic anhydrase in the proximal tubule; leads to sodium bicarbonate loss with increased loss of water

Oral administration

Used to treat metabolic alkalosis and acute mountain sickness

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Loop Diuretics - Adverse Effects

Hypokalemia
Hypomagnesemia
Hypocalcemia 
Uric acid retention (precipitation of gout attack) 
Metabolic alkalosis

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Loop diuretics - 3 individual agents

Furosemide (Lasix) - most commonly used

Ethacrynic Acid - only non-sulfa containing loop or thiazide

Torsemide - improved bioavailability

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3 pharmacological classes for treatment of HTN

ACEIs/ARBs
Calcium Channel Blockers
Diuretics

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Beta blockers - Adverse Effects

Bradycardia
Bronchospasm
Glucose/lipid changes
Decreased libido

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Alpha/Beta blockers

Labetalol

Carvedilol

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Metoprolol vs. Atenolol - elimination

Metoprolol - renal and hepatic elimination

Atenolol - renal elmination only

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Acetazolamide - Uses

Primarily used for metabolic alkalosis, acute mountain sickness; infrequently used as diuretic

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Vasodilators - Mechanism

Induce release of NO, which induces arterial vasodilation

Hydralazine and minioxidil

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Alpha 1 receptor blockers - Adverse Effects & Uses

Orthostatic hypotension, headache, peripheral edema

Primarily used in BPH

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Loop diuretics - Mechanism

Inhibits the Na/K/2Cl co-transporter in the water-impermeable ascending Loop of Henle; this decreases the tonicity of the interstitium, thereby reducing the driving force on the reabsorption of water in the collecting duct

Leads to the excretion of 15-25% of filtered sodium

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Thiazide - Adverse Effects

Hypokalemia
Hyponatremia
Hypomagnesemia
Hyperglycemia and lipid abnormalities 
Hypercalcemia
Uric acid retention and precipitation of gout 
Metabolic alkalosis

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Uses of spironolactone

Resistant HTN
Heart failure
Hyperaldosteronism

Spironolactone - Adverse effects

Hyperkalemia 
Gynecomastia (not seen with eplerenone)

Sodium channel blockers diuretics - 2 examples

Amiloride

Triamterene

Sodium channel blocker diuretics - Mechanism

Block reabsorption of Na+ in the distal tubule leading to decreased Na/water retention; less Na+ influx decreases the driving force on K+ secretion (K-sparing)

Sodium channel blocker diuretics - Adverse effects

Hyperkalemia
Hyperuricemia
Glucose intolerance in diabetes

ACE Inhibitors - Mechanism

Inhibits angiotensin converting enzyme (ACE), blocking the conversion of angiotensin I to angiotensin II; reduces angiotensin II-mediated vasoconstriction and stimulation of aldosterone release; also blocks degradation of bradykinin

ACEIs - Adverse effects

Cough Hyperkalemia Mild increase in serum creatinine; contraindicated with b/l renal artery stenosis Contraindicated in pregnancy

Angiotensin II Receptor Blockers (ARBs)

Irreversibly blocks the actions of angiotensin II at its receptor, preventing vasoconstriction and aldosterone release

ARB - Adverse Effects

Hyperkalemia Mild increase in serum creatinine; contraindicated in bilateral rental artery stenosis Contraindicated in pregnancy *Does not cause cough*

Dihydropyridine CCBs - 3 examples

Amlodipine Felodipine Nifedipine

DHPs - Mechanism

Block L-type Ca2+ channels, causing arterial vasodilation which lowers peripheral vascular resistance; selective for vascular smooth muscle over cardiac tissue (no significant effect on chronotropy or inotropy)

Non-dihydropyridines - 2 examples

Verapamil | Diltiazem

DHPs - Adverse Effects

Peripheral edema Reflex tachycardia Flushing Headache

NDHPs - Mechanism

Block L-type Ca2+ channels, causing vasodilation and decreased peripheral vascular resistance; equally selective for cardiac and vascular L-type Ca2+ channels, also causing negative chronotropic and inotropic effects

NDHPs - Adverse Effects

Conduction defects; contraindicated in 2nd or 3rd degree heart block Nausea Headache

Selective Beta 1 Blockers 2 examples & Pharmacokinetics

Atenolol - eliminated by the kidney | Metoprolol - eliminated by the liver

Non-selective Beta-1/Beta-2 blockers - 2 examples

Propanalol | Timolol

Beta / alpha blockers - 2 examples & mechanism

Carvedilol Labetalol Block beta receptors on heart, decreasing CO; also block alpha receptors on vascular smooth muscle, causing arterial vasodilation and decreased peripheral resistance

Hydralazine

Direct vasodilator Stimulate release of NO, which interferes with intracellular Ca2+ release causing peripheral vasodilation of arterioles

Minoxidil

Direct vasodilator K+ channel opener; causes hyperpolarization of smooth muscle cells

Direct vasodilator - Adverse effects

``` Reflex tachycardia Reflex activation of RAAS leading to Na/H2O retention Headache Anorexia Nauseavomiting Diarrhea ```

Alpha 1 blockers - 3 examples

Prazosin Terazosin Doxazosin

Alpha 1 blockers - Mechanism & Uses

Selectively block alpha-1 adrenergic receptors causing decreased SVR; particularly strong effect on alpha-1 receptors in the prostatic stroma, decreasing urethral resistance and relieving obstruction Most often used in symptomatic BPH

Alpha-1 blocker Adverse Effects

Orthostatic HTN Headache Peripheral edema

Classes of immunosuppression meds

``` Calcineurin inhibitor (Cyclosporine, Tacrolimus) Proliferation inhibitor (MMF, Sirolimus) Predisone ```

Calcineurin inhibitors

Ex: Cyclosporine, Tacrolimus Prevents NFAT-mediated T-cell clonal expansion Adverse effects (Cyclosporine): Nephrotoxicity, gout, HTN, hyperlipidemia

Proliferation Inhibitors - Transplant Meds

MMF, mTOR inhibitors (Sirolimus) Inhibit purine synthesis Adverse effects: leukopenia, anemia

Prednisone - Adverse Effects

HTN Hyperlipidemia Cataracts Weight gain