Pharmacology 1 Final Exam Drug List

Glycopyrrolate

MOA: Muscarinic antagonist Use: Reduces salivary gland activity SE: Potential for antimuscarinic (anticholinergic) side effects

Pralidoxime

MOA: Binds to cholinesterase and kicks off the phosphate from organophosphate, thereby reactivating cholinesterase Use: Treatment for organophosphate poisoning SE: N/A

Bethanechol

MOA: Muscarinic agonist Use: Treats urinary retention by acting on bladder SE: N/A

Oxybutynin

MOA: Muscarinic antagonist Use: Reduces overactive bladder SE: Potential for antimuscarinic (anticholinergic) side effects

Edrophonium

MOA: Acetylcholinesterase inhibitor that acts primarily on skeletal muscle Use: Treatment and diagnostic test for myasthenia gravis; reversal agent for non-depolarizing neuromuscular blockers SE: Cholinergic side effects when given in excess

Donepezil

MOA: Acetylcholinesterase inhibitor that acts primarily in the CNS Use: Alzheimer's disease SE: Cholinergic side effects

Atropine

MOA: Muscarinic antagonist at muscarinic receptors in the heart and other target organs Use: Treatment for bradycardia; treats parasympathetic symptoms of organophosphate poisoning SE: Anticholinergic side effects

Pancuronium

MOA: Non-depolarizing neuromuscular blocker (competitive antagonist at nicotinic receptors) Use: Skeletal muscle relaxation during surgery or mechanical ventilation SE: Effects can be reversed by acetylcholinesterase inhibitors

Succinylcholine

MOA: Depolarizing neuromuscular blocker at nicotinic receptors Use: Skeletal muscle relaxation during surgery or mechanical ventilation SE: Effects cannot be reversed by acetylcholinesterase inhibitors

Norepinephrine

MOA: Alpha-1 and Beta-1 agonist Use: Hypotension and shock; hypotension not responsive to dopamine SE: N/A

Albuterol

MOA: Beta-2 agonist Use: Asthma SE: Short-acting

Salmeterol

MOA: Beta-2 agonist Use: Asthma SE: Long-acting

Clonidine

MOA: Activation of alpha-2 receptors in the CNS decreasing sympathetic outflow to the heart and vascular smooth muscle Use: Hypertension, anxiety SE: None

Phenoxybenzamine

MOA: Non-competitive Alpha-1 and alpha-2 antagonist Use: Hypertension in pheochromocytoma SE: None

Phentolamine

MOA: Competitive Alpha-1 and alpha-2 antagonist Use: Hypertension in pheochromocytoma SE: Causes reflex tachycardia due to blockade of pre-synaptic alpha-2 receptors

Metoprolol

MOA: Beta-1 blocker; Class 2 antiarrhythmic that blocks beta-1 receptor activity in SA/AV node, slows SA node firing leading to delayed repolarization, slows AV node conduction leading to increase in PR interval Use: Hypertension, angina, acute myocardial infarction; treats supraventricular arrhythmias; prevents ventricular arrhythmia post-MI or in heart failure patients SE: Hypotension, bradycardia, exercise intolerance, sexual dysfunction; don't give to patients with severe asthma

Carvedilol

MOA: Beta and alpha antagonist Use: Hypertension, heart failure SE: Has antioxidant properties; has been shown to improve symptoms and improve mortality in patients with heart failure

Labetalol

MOA: Beta and alpha antagonist Use: Hypertension SE: None

Hydrochlorothiazide

MOA: Thiazide diuretic; inhibits Na/Cl symporter Use: Hypertension, edema associated with heart failure SE: Hypokalemia, can increase uric acid and plasma calcium

Propranolol

MOA: Beta-1 and Beta-2 blocker (Non-selective); Class 2 antiarrhythmic; inhibits conversion of T4 to T3 in peripheral tissues Use: Hypertension, angina; treats cardiovascular symptoms associated with hyperthyroidism SE: Can potentially cause bronchospasm if administered with Beta-2 agonist

Lisinopril

MOA: ACE (angiotensin-converting enzyme) inhibitor; inhibits formation of angiotensin II Use: Hypertension, heart failure, diabetic nephropathy SE: Cough, angioedema, hyperkalemia; first-line treatment for hypertension in patients under 55 (except patients of African/Caribbean family origin would benefit from CCB)

Losartan

MOA: Prevents angiotensin II from binding to its main receptor (AT1 on blood vessels) Use: Hypertension, heart failure, diabetic nephropathy SE: Hyperkalemia

Amlodipine/Nifedipine

MOA: Dihydropyridine calcium channel blocker; binds to and blocks calcium channels in vascular smooth muscle and cardiac smooth muscle (greater effect on peripheral smooth muscle) Use: Hypertension, angina SE: First-line treatment in hypertension in patients over 55 or African/Caribbean family origin at any age; can cause reflex tachycardia

Diltiazem/Verapamil

MOA: Non-dihydropyridine calcium channel blocker; Class 4 antiarrhythmic; binds to and blocks calcium channels in cardiac smooth muscle; slows SA node automaticity and firing leading to lower heart rate and delayed phase 4 repolarization, decreases AV node conduction velocity and increases PR interval Use: Can be used to control rate in atrial fibrillation or atrial flutter, treats angina, supraventricular dysrhythmias SE: Can worsen heart failure

Hydralazine

MOA: Arterial vasodilator Use: Moderate to very severe hypertension; heart failure in patients who can't tolerate an ACE inhibitor SE: Can cause reflex tachycardia; can cause hypotension when given IV; Black patients benefit from Hydralazine + nitrate more than ACE in chronic heart failure

Furosemide

MOA: Loop diuretic; inhibits Na/K/2Cl transporter Use: Hypertension, edema associated with heart failure SE: Hypokalemia, hyponatremia

Spironolactone

MOA: Aldosterone antagonist in kidneys; mineralocorticoid receptor antagonist Use: Hypertension, severe heart failure; used as potassium-sparing diuretic; treats primary hyperaldosteronism caused by bilateral adrenal hyperaldosteronism SE: Hyperkalemia; anti-androgenic effects (gynecomastia); evidence improves mortality in severe heart failure

Nitroglycerin

MOA: Releases nitrous oxide in vascular smooth muscle cells leading to vasodilation, preferentially relaxes venous smooth muscle, reducing cardiac preload Use: Prevent and treat angina attacks SE: Can lead to reflex tachycardia (can use beta-blocker to control this); pharmacological tolerance can develop; skin patches should be removed at least 10 hours each day; can be given as patch, topical ointment, sublingually

Isosorbide mononitrate

MOA: Releases nitrous oxide in vascular smooth muscle cells leading to vasodilation, preferentially relaxes venous smooth muscle, reducing cardiac preload Use: Prevent and treat angina attacks SE: Can lead to reflex tachycardia

Digoxin

MOA: Increases intracellular calcium in the heart by inhibiting the sodium pump (Na+, K+-ATPase); positive inotropic effect (increases contractility), negative chronotropic effect (decreases HR), negative dromotropic effect (decrease in conduction velocity) Use: Systolic heart failure SE: Does not improve survival in patients with heart failure, but can improve symptoms; need to check therapeutic levels on each patient; many drug interactions

Dobutamine

MOA: Beta-1 agonist (helps contractility and heart rate), Beta-2 agonist (peripheral vasodilation, reducing afterload) Use: Decompensated heart failure and cardiogenic shock SE: None

Enalapril

MOA: ACE inhibitor, reduces effects of angiotensin II cardiac remodeling Use: Asymptomatic heart failure; helps cardiac function post-MI (myocardial infarction) SE: Cough, hyperkalemia; decreases mortality in heart failure

Valsartan

MOA: Angiotensin receptor blocker; reduces effects of angiotensin II cardiac remodeling Use: Asymptomatic heart failure; helps cardiac function post-MI (myocardial infarction) SE: Hyperkalemia; less likely to get a cough than with an ACE inhibitor

Sacubitril

MOA: Neprilysin inhibitor; neprilysin normally breaks natriuretic peptides (ANP, BNP) which cause natriuresis and lower blood pressure; by inhibiting breakdown, you get higher levels of natriuretic peptides with more diuretic effects; neprilysin also breaks down Angiotensin II, so neprilysin inhibitor would increase angiotensin II - hence need for combination pill with ARB Use: Heart failure with reduced ejection fraction (combination pill "ARNI" is angiotensin-receptor blocker and neprilysin inhibitor); most common is Entresto (combination of Sacubitril + Valsartan) SE: Hypotension due to increase in natriuretic peptides and RAAS blockade

Amiodarone

MOA: Class 3 antiarrhythmic predominantly; blocks potassium channels to delay repolarization and increase refractory period; no effect on phase 0; prolongs Phase 3 repolarization Use: Antiarrhythmic; good for heart failure patients SE: Many side effects including pulmonary fibrosis; interacts with Digoxin, Simvastatin, and Warfarin, so can adjust dosage of these medications

Atorvastatin

MOA: HMG co-reductase inhibitor (longer) Use: Hyperlipidemia SE: Myopathy, liver dysfunction, rhabdomyolysis; metabolized by the CYP system (so CYP inhibitors can increase the concentration in the blood)

Simvastatin

MOA: HMG co-reductase inhibitor (lower potency) Use: Hyperlipidemia SE: Myopathy, liver dysfunction, rhabdomyolysis; metabolized by the CYP system (so CYP inhibitors can increase the concentration in the blood)

Cosyntropin

MOA: Synthetic formulation of ACTH Use: Used to distinguish congenital adrenal hyperplasia (CAH) from ovarian hyperandrogenism; used to diagnose adrenal insufficiency SE: Not used therapeutically, only for diagnostic purposes

Desmopressin

MOA: Long-acting synthetic analog of vasopressin; acts on V1 receptors in vascular smooth muscle to cause vasoconstriction; acts on V2 receptors in kidneys to increase water reabsorption by causing insertion of water channels (aquaporin channels) Use: Treatment of nocturnal enuresis; treatment of diabetes insipidus; can be used to control bleeding SE: Used with caution in patients with coronary artery disease

Conivaptan

MOA: Dual vasopressin antagonist at V1 and V2 receptors Use: Treatment of euvolemic and hypervolemia hyponatremia SE: None to know

Tolvaptan

MOA: Selective vasopressin antagonist at the V2 receptors Use: Treatment of euvolemic and hypervolemia hyponatremia; treatment of SIADH (Syndrome of inappropriate anti-diuretic hormone) SE: None to know

Estradiol

MOA: Most predominant estrogen in the human body Use: Oral contraception; treatment of primary hypogonadism; treatment as hormone replacement therapy in post-menopausal women SE: Estrogen has many formulations (transdermal, oral); hypertension; thromboembolic disorders; gallbladder disease; giving estrogen alone as HRT increases risk of endometrial cancer

Yasmin

MOA: Progesterone/Estrogen combination; Estrogen reduces FSH secretion; Progesterone inhibits the midcycle LH surge required for ovulation; Drospirenone is an aldosterone antagonist with a weak antiandrogenic effect Use: Oral contraception; treatment of acne vulgaris; treatment of dysmenorrhea SE: Available as 21-day or 24-day hormone regimen; estrogen can produce side effects; beware of interactions with drugs that increase hepatic metabolism of OCP's

Paragard

MOA: Alters the viability and transport of both sperm and ovum, thus preventing pregnancy before fertilization; copper also damages ovum after fertilization but before implantation Use: Contraception SE: Can be used for up to 10 years

Mirena

MOA: Progesterone; prevents pregnancy by producing localized effects on the endometrium Use: Contraception SE: Can be used for up to 8 years

Plan B

MOA: Progesterone formulation; prevents fertilization by inhibition of ovulation and thickening of cervical mucous; unlikely to prevent the implantation of a fertilized egg Use: Emergency contraception SE: Nausea and vomiting; first dose taken within 72 hours of intercourse and second dose taken 12 hours later

Mifepristone

MOA: Glucocorticoid receptor antagonist AND progesterone receptor antagonist; causes endometrial degeneration, leading to detachment of the blastocyst Use: Medical termination of pregnancy through 49 days gestation; treatment of Cushing syndrome SE: Nausea and vomiting; after administration, followed up by giving a prostaglandin (misoprostol) 48 hours later to stimulate uterine contractions

Methimazole

MOA: Thioamide drug which inhibits thyroperoxidase-catalyzed step in thyroid hormone synthesis Use: Grave's disease SE: Maculopapular rash/agranulocytosis; higher risk of birth defects

PTU

MOA: Thioamide drug which inhibits thyroperoxidase-catalyzed step in thyroid hormone synthesis; inhibits the conversion of T4 to T3 in peripheral tissues Use: Grave's disease SE: Maculopapular rash/agranulocytosis; drug of choice before pregnancy and for 1st trimester of pregnancy

Potassium Iodide Solution

MOA: Inhibits the release of thyroid hormones from the thyroid gland Use: Treats patients with acute thyrotoxicosis; prepares patients for thyroid surgery SE: None to know

Radioactive sodium Iodide (I-131)

MOA: Emits Beta-particles that destroy thyroid tissue Use: Treatment of Grave's disease SE: Contraindicated in pregnant women

Prednisone

MOA: Glucocorticoid with some mineralocorticoid activity; inhibits cytokines including interleukins and tumor necrosis factor (TNF) Use: Treats autoimmune conditions, inflammation; adjunctive therapy to DMARD's; can be used in acute treatment of gout attacks SE: Medium potency; 12-36 hours duration of action; Cushing syndrome features; hyperglycemia; weight gain

Dexamethasone

MOA: Glucocorticoid Use: Used in diagnostic cortisol test; treats inflammatory conditions SE: High potency; 24-72 hours duration of action; Cushing syndrome features

Glipizide

MOA: Sulfonylurea; increases release of insulin from pancreatic Beta cells; decreases glucagon secretion Use: Type 2 diabetes SE: Weight gain, hypoglycemia

Acarbose

MOA: Competitively inhibits alpha glucosidase (preventing the conversion of oligosaccharides and disaccharides to glucose) Use: Type 2 diabetes SE: Flatulence and abdominal bloating

Metformin

MOA: Inhibits gluconeogenesis in the liver; increases insulin sensitivity in peripheral tissues; enhances glucose uptake in skeletal muscle and adipose tissue Use: First-line treatment for type 2 diabetes SE: Diarrhea (switch to extended release); contraindicated in renal or hepatic disease due to potential lactic acidosis

Sitagliptin

MOA: DPP-4 inhibitor (DPP-4 naturally inhibits the breakdown of GLP-1); inhibitors thereby cause an increase in GLP-1 levels Use: Type 2 diabetes SE: Not as much weight loss as GLP-1 agonists

Ozempic (Semaglutide)

MOA: Glucagon-like-peptide-1 (GLP-1); stimulates glucose-dependent insulin secretion and inhibition of glucagon secretion, increases glucose uptake by muscle and adipose tissue, slows gastric emptying (decreasing appetite and food intake) Use: Type 2 diabetes SE: Available for once-weekly injection; also available as daily oral medication though this can be cost prohibitive for some patients; slightly increased risk of pancreatitis

Empagliflozin

MOA: Sodium-glucose cotransporter (SGLT2) inhibitor; decreases renal glucose and sodium absorption in the proximal tubule, increasing urinary excretion of glucose and sodium; higher sodium in filtrate sensed by macula densa which leads to afferent vasoconstriction to reduce renal blood flow and transient decrease in glomerular filtration; higher sodium concentration leads to decrease in renin and protective cardiac and renal effects due to chronic inhibition of the RAAS system Use: Type 2 diabetes; heart failure (stable HFrEF, HFmRF, and HFpEF) or patients at high risk of heart failure; chronic kidney disease (GFR above 20) SE: Increase incidence of urinary tract infections and genital yeast infections; can cause volume depletion; reduces cardiovascular mortality when given for heart failure; improves glycemic control in diabetes; reduces declines in glomerular filtration rate in chronic kidney disease

Pioglitazone

MOA: Thiazolidinedione; agonist at the PPAR-gamma receptor; increases insulin sensitivity by increasing the number of GLUT4 glucose transporters in muscle and adipose tissue; also activates PPAR-alpha receptor to improve lipid levels Use: Type 2 diabetes SE: Contraindicated in patients at risk of developing heart failure or in heart failure patients; causes weight gain

Warfarin

MOA: Inhibits vitamin K reductase (inhibits synthesis of clotting factors that require Vitamin K - Factors 2,7,9, and 10) Use: Pulmonary embolism, DVT SE: Monitored by INR; antidote is Vitamin K; metabolized by CYP2C9; CYP2C9 inhibitors can lead to increased amount of Warfarin and increased bleeding risk; CYP2C9 inducers can lead to decreased amount of Warfarin, therefore reducing bleeding risk

Heparin

MOA: Activates antithrombin, inhibits Factor Xa and Factor II (thrombin) Use: Pulmonary embolism, DVT SE: Antidote is Protamine; measure efficacy via aPTT (activated partial thromboplastin time); rare effect of "HIT" or heparin-induced thrombocytopenia (body develops antibodies to heparin-PF4 complex, results in thrombosis development)

Enoxaparin

MOA: Activates antithrombin, inhibits Factor Xa and Factor II (thrombin) Use: DVT prevention in the hospital (used as SubQ injection) SE: Antidote is Protamine; no routine measurement needed; renally excreted

Dabigatran (Pradaxa)

MOA: Direct thrombin inhibitor Use: Pulmonary embolism, DVT; prevention of stroke in patients with atrial fibrillation (based on CHADS2VASC score and risk/benefits of anticoagulation) SE: Contraindications: active bleeding, mechanical heart valve; renally dosed; reversal agent: Praxbind

Rivaroxaban (Xarelto)

MOA: Direct Factor Xa Inhibitor Use: Pulmonary embolism, DVT; prevention of stroke in patients with atrial fibrillation (based on CHADS2VASC score and risk/benefits of anticoagulation) SE: Contraindications: active bleeding, avoid with CYP3A4 inhibitors; renally dosed; reversal agent: Andexxa

Apixaban (Eliquis)

MOA: Direct Factor Xa Inhibitor Use: Pulmonary embolism, DVT; prevention of stroke in patients with atrial fibrillation (based on CHADS2VASC score and risk/benefits of anticoagulation) SE: Contraindications: active bleeding, mechanical heart valve; renally dosed; reversal agent: Andexxa

Aspirin

MOA: Inhibition of cyclooxygenase 1 and 2 (enzyme responsible for making Thromboxane 2, which causes platelets to aggregate) Use: Primary prevention of cardiovascular disease (per USPSFT, adults aged 40-59 years with an ASCVD risk greater than 10

should consider adding aspirin if low bleeding risk); secondary prevention for: history of MI, history of stroke or TIA, history of CABG, history of PAD SE: Effects last for duration of platelet (7-10 days)

Clopidogrel

MOA: Blocks ADP from binding to P2Y12 receptor on platelets (prevents platelet activation/aggregation) Use: Dual therapy for: CAD s/p PCI (coronary artery disease after percutaneous coronary intervention - people with stents), ACS (acute coronary syndrome), high risk patients after stroke/TIA/CABG SE: Effects last for duration of platelet (7-10 days)

Alteplase

MOA: Synthetic tPA; converts plasminogen to plasmin, which lyses fibrin Use: Used in IV infusion to degrade thrombi in patients with MI, thrombotic stroke or PE SE: In acute ischemic stroke, must be initiated within 4.5 hours of stroke onset (preferably 3 hours), and are contraindicated in hemorrhagic stroke

Vitamin K

MOA: Involved in synthesis of clotting factors 2,7,9 and 10 Use: Antidote to too much Warfarin SE: Present in many foods such as Spinach and Kale

Methotrexate

MOA: Multifactorial; reduces purine synthesis; at low doses, inhibits cytokine production and replication of T and B cells; interferes with metabolism of folic acid (folic acid needed for synthesis of DNA and RNA), leading to decrease in proliferation of certain immune cells; also has anti-inflammatory effects Use: Preferred non-biologic DMARD SE: Contraindicated in pregnancy/breastfeeding; check CBC, LFT's and Creatinine for all non-biologics

Leflunomide

MOA: Inhibits autoimmune T-cell proliferation and production of autoantibodies by B cell Use: Non-biologic DMARD SE: Contraindicated in pregnancy/breastfeeding; hepatotoxicity; possibility of SJS (Steven-Johnson's syndrome); check CBC, LFT's and Creatinine for all non-biologics

Sulfasalazine

MOA: Unknown mechanism Use: Non-biologic DMARD SE: Pregnancy Category B (probably safe); can get "lupus-like reaction"; check CBC, LFT's and Creatinine for all non-biologics

Adalimumab (Humira)

MOA: TNF (Tumor necrosis factor) inhibitor Use: 1st line biologic DMARD SE: Increased susceptibility to infections; potential for reactivation of TB - check PPD before use; increased risk of lymphoma

Rituximab

MOA: Non anti-TNF biologic; eliminates B cells Use: 2nd line biologic DMARD SE: Fatal infusion-related reactions; can have HepB reactivation

Probenecid

MOA: Uricosuric drug; competitively inhibits the reabsorption of uric acid by renal tubules (increases renal excretion of uric acid) Use: Chronic Gout SE: Avoid with salicylates and aspirin

Allopurinol

MOA: Decreases production of uric acid by inhibiting xanthine oxidase Use: Prevent gout attacks in persons who overproduce uric acid SE: Nausea and vomiting

Colchicine

MOA: Disrupts microtubules and inhibits motility of inflammatory leukocytes Use: Treatment of acute gout SE: Nausea and vomitin

Praxbind

Reversal of Dabigatran

Andexxa

Reversal of Xarelto and Eliquis

Protamine

Reversal of Heparin

Doxazosin

MOA: A1 antagonist

Indication/Why It’s Given: benign prostatic hypertrophy, relax bladder and prostatic smooth muscle