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• The text provided is for study of drugs and related information for medical professionals

Diuretics

• Mostly block sodium and chloride reabsorption
• More water and solutes stay in the nephrons, including sodium and potassium
• Used for edema that is pulmonary, caused by, heart failure, or from hypertension
• Monitor patients for dehydration, hypovolemia, hypotension, and electrolyte imbalances
• Monitoring is also important for hyperglycemia from diabetes and hyperuricemia from gout
• Caution is needed with digoxin, ototoxic drugs, and NSAIDs, which block diuretic effects
• Lithium can cause lithium levels and toxicity from diuretics

Loop Diuretics

• Furosemide as an example
• These can cause reflex tachycardia and lower blood pressure when taken with digoxin
• It is most effective, even with renal impairment
• Watch for hypokalemia, ototoxicity, dehydration, and hypotension

Thiazide and Thiazide-like Diuretics

• HCTZ and chlorthalidone as examples
• These are the the most commonly prescribed
• Watch for hypokalemia and hypotension

Potassium-Sparing Diuretics

• Spironolactone and triamterene as examples
• Used to retain potassium and has limited diuretic efficacy, so is often combined with loop or thiazide diuretics
• Watch for hyperkalemia and endocrine effects
• Caution against salt substitutes

Osmotic Diuretics

• Mannitol as an example
• It is used to lower ICP, IOP, and in renal failure
• Use with a filter needle and in-line filter

Antilipemic Agents

• Used to treat high cholesterol and triglycerides
• Total cholesterol should be less than 200 mg/dL
• HDL cholesterol should be greater than 40 mg/dL
• LDL cholesterol should be less than 100 mg/dL
• Triglycerides should be less than 150 mg/dL

HMG-CoA Reductase Inhibitors (Statins)

• Simvastatin, Lovastatin, Pravastatin, Rosuvastatin, Fluvastatin, Pitavastatin are examples
• This is the first-line drug for cholesterol
• Lowers LDL and VLDL, increases HDL, and lowers triglycerides in some cases
• Non-lipid effects include plaque stability, reduced CV events, and increased bone formation
• The liver makes less cholesterol and responds by increasing LDL receptors, removing cholesterol from the blood
• Used for hypercholesterolemia, prevention of CV events, post-MI therapy, diabetes, and protection against MI and stroke
• Common adverse effects are HA, rash, and GI upset
• Rare adverse effects are myopathy/rhabdomyolysis, hepatotoxicity, and cataracts
• Interacts with other lipid-lowering drugs and grapefruit juice, including CYP3A4 inhibitors
• Pregnancy Category X
• Take in the evening (most cholesterol produced at night)
• Monitor lipids, LFTs, and CK

Cholesterol Absorption Inhibitor

• Ezetimibe as an example
• It blocks cholesterol absorption and lowers total cholesterol, LDL, and apolipoprotein B
• Adverse effects include myopathy, rhabdomyolysis, hepatitis, pancreatitis and thrombocytopenia
• Monitor LFTs and CK
• Interacts with other lipid-lowering drugs, BAS, statins, and fibrates
• Monitor lipids, LFTS, and CK

Bile Acid Sequestrants

• Colesevelam, cholestyramine, and colestipol are examples
• Action is to lower LDL levels, alone or with a statin
• Nonabsorbable resin that binds bile acids and other substance in the GI tract
• Triggers the body to need bile acid for digestion as they are made from cholesterol in the liver
• The liver has to take cholesterol out of the blood
• Constipation is a potential adverse effect
• Can bind with other drugs and inhibit thiazide diuretics, digoxin, and warfarin
• Blocks absorption of many drugs like fat-soluble vitamins, levothyroxine, and oral contraceptives
• Take as a tablet or powder with at least 4-8 oz of fluid
• Take other medications 1 hour before or 4 hours after
• Considered safe during pregnancy

Fibric Acid Derivatives (Fibrates)

• Gemfibrozil, fenofibrate, and fenofibric acid are examples
• Third-line treatment that lowers TG levels (VLDLs) Adverse effects include GI issues, gallstones, myopathy, and hepatotoxicity
• Increases risk of rhabdomyolysis with statins
• Statins increase the risk of myopathy/rhabdo
• Warfarin increases the risk of bleeding
• Check labs such as CK, LFTS, PT/INR if on warfarin
• Take 30 minutes before breakfast or dinner

Niacin (nicotinic acid)

• Reduces LDL and TG levels as well as raises HDL (best)
• Does little to improve CV outcomes and poses more adverse effects than statins
• Intense flushing, GI upset, and liver injury are a few adverse effects along with muscle cramps, headaches, rashes and photosensitivity
• To avoid flushing take one adult strength ASA (325mg) tablet about 30 minutes before the niacin dose

Monoclonal Antibodies

• Alirocumab and evolocumab are examples
• Actions include lowering LDL
• Adverse effects such as a hypersensitivity reaction and injection site reaction may occur

RAAS Drugs: Renin-Angiotensin-Aldosterone System

• Angiotensin-converting enzyme (ACE) inhibitors comes from the lungs, and blocks bradykinin
• Angiotensin II receptor blockers (ARBs) and Aldosterone antagonists work in the system

Direct Renin Inhibitor

• Aliskiren as an example
• Actions include treating hyptertension
• Adverse effects: can cause fetal injury. Cat X, angioedema, rash, cough, hyperkalemia, diarrhea in high doses, and hypotension
• High-fat meals block absorption with interactions such as atorvastatin, ketoconazole and furosemide

ACE Inhibitors (ACEI)

• Considered kidney protectors
• Used for HTN, heart failure, MI, diabetic and nondiabetic nephropathy, and MI/stroke/death prevention in high CV risk patients
• Adverse Effects: First-dose orthostatic hypotension, cough, angioedema, fetal injury (Cat X), and hyperkalemia
• Contraindicated in pregnancy

ARBs

• Actions include HTN, heart failure, MI, diabetic nephropathy/retinopathy, and MI/stroke/death prevention in high CV risk patients
• Angioedema, fetal injury (Cat X), and orthostatic hypotension can occur
• Do not cause cough or hyperkalemia

Aldosterone Antagonists

• Eplerenone and spironolactone, for example
• Actions include treating HTN and heart failure
• Treats PMS, PCOS, and acne in women as well as hyperaldosteronism
• Can cause hyperkalemia and hyponatremia along with flu-like symptoms, endocrine changes, and dizziness/fatigue
• Not recommended during pregnancy and lactation and high potassium, kidney/liver disease, T2DM with microalbuminuria
• Increase risk of hyperkalemia with verapamil, ACEIs, ARBs, K+-sparing diuretics, NSAIDs, ketoconazole, and erythromycin
• Be cautious of salt substitutes as well as lithium
• Diuretics can cause hypotension
• CYP3A4 inhibitors can interact with grapefruit juice

Calcium Channel Blockers: Dihydropyridines

• Nifedipine, amlodipine, felodipine, nicardipine, isradipine, and nislodipine are examples
• Action is to block Ca2+ channels in blood vessels, causing vasodilation
• It is used to treat angina pectoris and HTN
• Vasodilation lowers BP and causes reflex cardiac stimulation, increasing HR, and causing reflex tachycardia
• Giving with a beta blocker slows it down
• Increases contractile force
• Can also result in acute toxicity or orthostatic hypotension and peripheral edema
• Gingival hyperplasia is possible
• Interacts with dihydropyridines
• Cimetidine, famotidine and grapefruit juice can lead to toxicity

Calcium Channel Blockers: Nondihydropyridines

• Verapamil and Diltiazem are examples
• No beta blockers are needed
• Blocks Ca2+ channels and causes vasodilation, lowering BP, and increasing reflex cardiac stimulation and contractile force
• Decreases force and rate in myocardium SA & AV nodes
• Blocks cardiac conduction and relaxes cardiac stimulation, but doesn't change HR, AV conduction, and contractility
• Angina pectoris, HTN, and cardiac dysrhythmias can be treated
• CONSTIPATION, flushing, dizziness, HA, and peripheral edema are adverse effects as well as bradycardia and AV block
• Digoxin, Beta Blockers, and Grapefruit juice can interact
• Heart block and heart failure can occur

Vasodilators

• Selectivity includes hydralazine for arterioles, nitroglycerin for veins, and prazosin for both
• Arterioles decrease cardiac afterload, reduce the amount of cardiac work, increase cardiac output, and increase increase tissue perfusion
• Veins decrease cardiac preload like less cardiac work, decreased cardiac output, and decreased tissue perfusion
• Used to treat hypertension, angina pectoris, heart failure
• Postural hypotension (venous only) and reflex tachycardia as potential adverse effects

Hydralazine

• Causes arterial dilation, decreased cardiac afterload and work, and increased output and tissue perfusion
• HA, dizziness, weakness, fatigue, and SLE-like syndrome
• Reflex tachycardia is common; combine with a beta-blocker and diuretics

Minoxidil Actions

• Arteriole Dilation
• Decrease Cardiac afterload & work
• Increased output and tissue perfusion
• Commonly causes hypertrichosis and pericardial effusion
• Causes nausea, HA, fatigue & breast tenderness
• Causes glucose intolerance & thrombocytopenia.

Sodium Nitroprusside

• Vein & Arteriole dilation
• Drug of choice for hypertensive crisis
• Decreased preload & afterload
• Adverse effects:
  • Headache -Excessive hypotension -Cyanide poisoning, Thiocyanate toxicity -Bradycardia/Tachycardia, EKG changes

Adrenergic Agonists (Alpha and Beta)

• Sympathomimetics that induce a fight-or-flight response
  • Alpha 1 Adrenergic Agonist -Vascular & smooth muscle- - ↑ Force of heart contraction Vasoconstriction → BP Dilate pupils (mydriasis) ↓GI secretions ↑ bladder & prostate contraction
  • Alpha 2 Adrenergic Agonist -Sympathetic nerve endings -↓ Norepinephrine release -Vasodilation → BP -↓GI motility
  • Beta 1- heart- ↑ Heart Rate, ↑ Force of heart contraction ,↑ BP, ↑ renin secretion
  • Beta 2 -smooth muscle- Dilates bronchioles, GI & Uterine relaxation, Blood sugar Dopamine Agonist:Renal vasodilation

Centrally Acting Alpha 2 Agonists

• Used to treat HTN, severe pain, and ADHD
• Centrally Acting Alpha 2 Agonists cause Bradycardia, Decreased cardiac output, vasodilation, rebound HTN
• Causes drowsiness/sedation, constipation, impotence, gyenocomastia, and CNS effects
• Safe during pregnancy

Alpha Adrenergic Antagonist (BLOCKERS)

• Azosin Prazosin, doxazosin, terazosin, tamsulosin
• Selective a₁ blockade that treats HTN, BPH, pheochromocytoma, and Reynaud's disease
• Cause Orthostatic hypotension ("First Dose" Effect), as well as severe postural hypotension and syncope
• Initial dose should be low and given at bedtime

Beta-adrenergic Antagonists: Olol

• Cardioselective (Β₁) - metoprolol, atenolol, esmolol, bisoprolol
• Nonselective (Β₁ heart and Β₂ lungs)- Propranolol, nadolol
• Alpha & Beta- carvedilol, labetalol
• Decreased Heart rate, myocardial contractility, cardiac output , AV node conduction
• Vasodilation =HTN, Angina, Tachydysrhythmias, Heart Failure, MI
• ADRs = -Can trigger orthostatic hypotension and AV Block -Bronchoconstriction and inhibited glycogenolysis
• Caution with breastfeeding and to not use w sinus bradycardia or heart failure
• Caution also with severe allergies, athsma, diabetes and caution with epinephrine

Etiologies and Pathogenesis of Hypertension

• Causes Heart hypertrophy, MI, renal failure, blindness and stroke

Initial drugs of choice for hyper tension include

• ACE inhibitors, ARBs, Thiazides and CCB

Medications that can be used for Hypertensive crisis

• Sodium nitroprusside is drug of choice with nitroglycerin, nicardipine, clevidipine, enalaprilat, esmolol and labetalol

Types of Hypertensive Crisis

• Emergency causes threat of organ damage
• Urgent can be treated at slower rate and has minimal to no threat of organ damage

Medications for Chronic HTN during pregnancy

• Labetolol, nifedipine, methyldopa, hydralazine

Medications to avoid during pregnancy

• ACEIs, ARBs and DRIs

Initial management of an MI

• ABC’s, Cardiac & O2 & ACLS as needed
• ASA 325mg - Aspirin
• Three SL NTG Tabs or spray can provide aid -Administer beta blocker after

Medications to avoid with use of digoxin

• Loop diuretics, ethacrynic acid, aminoglycosides
• monitor BP and hear rate

Adenosine

• Terminates Tachycardia
• Primary indication is PSVT

Organic Nitrates

• Nitroglycerin- can be administered with an oral ER capsule, as a SubLing tablet, as translungial spray or transdermal patch
• used to dilate veins and decrease venous return

Medication Interactions with Antigungal agents

• Monitor for prolonged QT interval and C450 Inhibitors
• Medications cause kidney and hearing damage so monitor closely

Management/Treatment of UTIs

• Use nitrofurantoin
• use trimethoprim-sulfamethoxazole - is combined drug that requires pt to drink with >1200ML to avoid hyperkalemia
• fluoroqinolone, bactocidial that treat gram +/- bacteria that come in the form of pills
• AzO treatment can alter urine color
• Sulfonamides suppress colonization after burns
• Metronidazole is bactericidal

Anti-Infective Pharmacotherapy: Antibiotics

• Antimicrobials are any agent that can kill or suppress microorganisms such as bacteria, viruses, and fungi
• Selective Toxicity is used to harm microbes, but not the body

Classification of antimicrobials

• Classified by the type of bacteria they target to inhibit or treat They interfere with synthesis and integrity of bacterial DNA and RNA

Ways Bacteria becomes resistant to medications include

• Decreased rate of entry
• Increased exit
• Enzymatic Inactivation
• Modification of receptors

Ways to prevent Antibiotic Resistance

• Use drugs Appropriately
• Prevent transmissions
• Diagnose and treat infection correctly

Superinfections

• New infection that appears during course of treatment for a primary infection

Prophylactic Use of Antimicrobials =

• Agents given to prevent infection rather than to treat an established infection: surgery, cardiovascular, suppressed immune system

Misuses of Antibiotics Include

• Using them with viral infections, for fever or unknown origin, wrong dosage, incomplete information

Antibiotics are classified with

• Penicillin-binding proteins with beta-lactam rings that destroy cells
• Can cause Anaphylaxis with classifications by time frames
• Monitor kidney & provide respiratory support

Cephalosporins

• Most widely used group of antibiotics – similar to penicillin Causes allergies, bleeding-disulfiram, and kidney Damage - reduce dosage

Carbapenems-used for serious infections

• causes allergies, Gl and superinfections
• May reduce levels of valproic acid and caution with renal impact

Other cell wall inhibitors

• Vancomycin -commonly used in hospitals due to red man syndrome - slow admin Other: Azteonam, telavancin, fosfomycin

Drugs for Protein Sythesis

• Inhibitors of Protein Synthesis – suppress the replication and growth of bacteria
• Bacteriostatic: Tetracyclines and Macrolides
• Treat various infections of repsiratory or GI origins

Tetracycline

• Tetracycline (-cycline): Borad spectrum and Bacteriostatic (stopping growth)
• Used for skin, GI and reporoductive tract infections
• Not appropriate during lactation due to decrease in oral contraceptives- kidney and liver issues

Macrolide

Macrolide (-thromycin) Bacteriostatic slows bacterial growth Used for allergies of respitory infection cases and pneumonia, etc

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