Drugs Flashcards
Dipyridamole
o Phosphodiesterase Inhibitor → ↑ cAMP → COX inhibition (↓ TXA2 → ↓ platelet aggregation) -AND- ↑ PKA/PKG activity (→ ↑ MLCP → ↓ MLC → vasodilation)
o Inhibition of adenosine deaminase → ↑ adenosine → ↑ coronary vasodilation
Dipyridamole Side Effects
Dizziness
Elderly – Orthostatic Hypotension and GI Issues
Cilostazol
Oral Antiplatelet AND Vasodilator
MOA – Phosphodiesterase III inhibitor → ↑ cAMP → ↓ platelet aggregation and ↑ vasodilation
Cilostazol Side Effects
Headache
GI Side Effects (diarrhea, abnormal stools, pain)
POSITIVELY alters the lipid profile (decreases plasma triglycerides; increases HDL)
Contraindicated w/ any congestive heart failure
Catecholamines
Dopamine, Norepinephrine, Epinephrine
Always have a benzene ring with 2 hydroxyl groups
Clopidogrel (Plavix)
Selectively inhibits ADP binding to platelet receptor and subsequent ADP-mediated activation of glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation
Reduce atherosclerotic events
Clopidogrel (Plavix) Side Effects
Dermatologic: Rash (4%), pruritus (3%)
Hematologic: Bleeding (major 4%; minor 5%), purpura/bruising (5%), epistaxis (3%)
Alprostadil
Prostaglandin E1. Causes smooth muscle dilation, inhibition of platelet aggregation, intestinal and uterine smooth muscle stimulation (may stimulate upregulation of cAMP). Specifically keeps the Ductus Arteriosus patent in cyanotic congenital heart disease.
Alprostadil Side Effects
Apnea, fever, sepsis and seizures have been reported.
Indomethacin
NSAID that reversibly inhibits COX. Used for acute gouty arthritis as well as close a Patent Ductus Arteriosus.
Indomethacin Side Effects
Headache and GI Issues
Nitroglycerin
Vasodilation via mitochondrial conversion to NO → guanalyl cyclase → cGMP → PKG → phospho of MLCP → dephospho of MLC → relaxation
Nitroglycerin Side Effects
Hypotension, Bradycardia, Increased intercranial pressure
Baby Aspirin
o Inhibits platelet COX-1 synthesis of prostaglandins → decreased thromboxane A2 → decreased platelet aggregation
o Dosing not high enough to inhibit COX-2 in endothelial cells → continued production of PGI2 (prostacyclin) → vasodilation still intact
Baby Aspirin Side Effects
Bleeding, Erosive Gastritis, Ulcers, Renal Function, Gout (affects that transporter)
Aspirin
o Inhibits COX-1 and COX-2 → decreased prostaglandin synthesis → decreased thromboxane A2 and PGI2 (prostacyclin) → decreased platelet aggregation and decreased vasodilation
o Endothelial cells will upregulate COX-2 to increase PGI2 production
Aspirin Side Effects
Bleeding, Tinnitus, Erosive Gastritis, Ulcers, Renal Function, Gout (affects that transporter)
Ramipril
Undergoes liver saponification → ramiprilat → binding of ACE → ↓ angiotensin II → ↓ vasoconstriction, ↓ aldosterone, AND ↓ Na+ resorption in distal convoluted tubules → ↓ H2O resorption → ↓ BP
Atorvastatin
Inhibits HMG-CoA Reductase → ↓ de novo synthesis of cholesterol → ↑ LDL receptors → ↑ uptake of serum LDL → ↓ serum LDL
Atorvastatin Side Effects
Increased Hb A1c, Hepatotoxicity, Auto-immune related myopathy, Rhabdomyolysis
Ramipril Side Effects
↑ bradykinin → cough, angioedema, hyperkalemia, hypotension / syncope
Phosphodiesterase Inhibitors
Sildenafil (cGMP - Viagra)
Dipyridamole (cAMP)
Cilostazol (cAMP)
Sildenafil
Phosphodiesterase Type V (PDE 5) inhibitor → ↑ cGMP → vasodilation in corpus cavernosum and pulmonary arterioles
Cardiac Side Effect of Erythromycin
Blocks rapid K+ channel (IKr current) → prolongation of QT Interval and possible Torsades de Pointes if have genetic LQTS
Specifically may trigger M Cell depolarization in left ventricular wall due to differences in the electrical activity of these cells
Cardiac Side Effect of Diphenhydramine (Benadryl)
Blocks fast sodium channels and, at high doses, repolarizing K+ channels → QT elongation and possible TdP if have genetic LQTS
Cardiac Side Effect of Amitriptyline (antidepressant)
Blocks rapid K+ channels for repolarization → elongation of QT Interval and possible TdP if have genetic LQTS
Class I Antiarrhythmics
Na+ channel blockers
Class Ia Antiarrhythmics
Moderate block of v-g Fast Na+ channels and K+ channels
o Ventricular myocytes →
• ↓ phase 0 upstroke and ↑ repolarization time
o SA Node →
• Shift of thresholds to ↑ positive potentials → ↓ rate reaching threshold
• ↓ slope of phase 4 depolarization → ↓ rate reaching threshold
Class Ib Antiarrhythmics
Blocks v-g Na+-channels in ventricular myocytes → ↓ phase 0 upstroke and may ↑ repolarization time
USE dependent – when Class IA’s aren’t working
Class Ic Antiarrhythmics
Marked block of v-g Na+-channels in ventricular myocytes → ↓ phase 0 upstroke
USE dependent – when the Class IA and Class IB’s aren’t working
Class II Antiarrhythmics
β-blockers
• Antagonize β1-adrenergic receptors in SA and AV nodal cells → ↓ cAMP → ↑ opened K+-channels and ↓ opened Na+-channels →
• ↓ slope of phase 4 depolarization (important @ SA Node) → ↓ rate reaching threshold
• ↑ repolarization time (important @ AV Node)
Metoprolol
Selective β1-blocker with little effect on β2 →↓ cAMP → ↑ opened K+-channels and ↓ opened Na+-channels → reduction in cardiac output, contractility
o ↓ slope of phase 4 depolarization (important @ SA Node) → ↓ rate reaching threshold → ↓ chronotropicity
o ↑ repolarization time (important @ AV Node) → ↓ chronotropicity
Class III Antiarrhythmics
K+ channel blockers
• Block K+-channel → longer action potential plateau → ↑ repolarization time
Lisinopril
Long-acting ACE inhibitor →
o ↓ Angiotensin II →
• ↓ NaCl resorption → ↓ H2O resorption → ↓ BP
• ↓ arteriolar vasoconstriction
• ↓ aldosterone synthesis
• ↓ ADH (vasopressin) release → ↓ aquaporin channels → ↓ H2O resorption
o Inhibit degradation of bradykinin → vasodilation (like NO) and cough
Class IV Antiarrhythmics
Ca2+-channel Blockers
• Preferentially block cardiac Ca2+-channels → slow action potential upstroke in SA and AV nodal tissue → prolonged time of AP → slower transmission of AP →↓ HR
Metoprolol Side Effects
o Bradyarrhythmia
o AV Block
o Bronchospasm
Digitalis (Digoxin)
o Directly inhibits Na+/K+-ATPase → ↑ intracellular Na+ → ↓ activity of the Na+/Ca2+ exchanger (sodium in – calcium out) → ↑ intracellular Ca2+ → ↑ SR Ca2+-ATPase activity → ↑ SR storage of Ca2+ → ↑ efflux from SR during next AP → ↑ contractility
o ↑ Ca2+ current during the AP → plateau of the AP → prolongation of the AP
o ↑ intracellular Na+ → ↓ extracellular Na+ → ↓ rate of depolarization of automaticity cells → ↓ HR
o ↓ Maximum Diastolic Potential → ↓ rate of phase 0 depolarization and conduction velocity
Lisinopril Side Effects
o Pain the ass COUGH (due to ↑ bradykinin)
o Angioedema
o Agranulocytosis
o Neutropenia
Aspirin Side Effects
o Angioedema – rapid swelling of the dermis, subcutaneous tissue, mucosa and submucosal tissues
o Bleeding
Digitalis (Digoxin) Side Effects
o Arrhythmias w/ and w/out AV Block
o Premature Ventricular Contraction (PVC)
o Supraventricular Tachycardia
Furosemide
Loop Diuretic
Blocks resorption of Na+/K+/2Cl- in the kidney tubules ascending loop of Henle → profound increase in urine output → ↓ blood volume → ↓ BP
Atorvastatin
Inhibits HMG-CoA Reductase → ↑ LDL receptors on cell membranes → ↓ blood LDL
Digoxin-Immune-Fab
o Digoxin immune antigen-binding fragments (Fab) are specific antibodies for digitalis → binding digoxin (renal clearance) or digitoxin (hepatic clearance) → excreted by the kidneys and removed from the body
Atorvastatin Side Effects
o Myopathy
o Rhabdomyolysis
o Hepatotoxicity
o Dermatomyositis – inflammation of the skin and muscles (less commonly the heart)
Warfarin
Prevents the reduction of oxidized Vitamin K thereby → decreased activation of Factors II, VII, IX, X, C & S
Dobutamine
o Synthetic catecholamine and a direct-acting inotropic agent
o It stimulates the β-receptors of the heart which produces hypertensive, mild chronotropic, vasodilative, and arrhythmogenic effect
Furosemide Side Effects
INTERACTION: Diuretic-induced hypokalemia may potentiate digoxin-related cardiac toxicity
o Hypokalemia (Na+/K+ exchanger – Na+ resorption / K+ excretion)
o Hypotension
o Pancreatitis
o Stevens-Johnson Syndrome (epidermis separates from the dermis)
o Aplastic or hemolytic anemia
o Leukopenia & Thrombocytopenia
Carvedilol
o Nonselective β-adrenergic blocking agent with α1-adrenergic blocking activity and no intrinsic sympathomimetic activity
o NOTE: beneficial effect in congestive heart failure is not known, but may be attributable to β-blockade and vasodilation
Heparin
Combines with antithrombin inhibiting the activation of Factor X and activated Factor II (thrombin) thereby preventing the formation of Factor Ia (Fibrin)
Phenylephrine
Powerful postsynaptic α-adrenergic stimulant with little effect on β-receptors in the heart → ↑ vascular resistance → ↑ BP → reflex bradycardia, which can sometimes fix atrial fibrillation
Dobutamine Side Effects
o Tachycardia
o Ventricular Ectopy
o Increased BP
→ Interactions – Be VERY careful w/ MAOI
Carvedilol Side Effects
o Hypotension and Bradycardia o Dizziness o Hyperglycemia o Diarrhea or Weight Gain o Weakness
Phenylephrine Side Effects
- Hypertensive headaches
* Cardiac irregularities
Naloxone
o Pure opioid antagonist with greatest affinity for the mu receptor (10X)
o It acts by competing for the mu, kappa, and sigma opiate receptor sites in the CNS
Naloxone Side Effects
o No pharmacologic effect other than antagonizing the opioid receptors
o Dr. Wiki says – change in mood, increased sweating, nausea, nervousness, restlessness, trembling, vomiting, allergic reactions such as rash or swelling, dizziness, fainting, fast or irregular pulse, flushing, headache, heart rhythm changes, seizures, sudden chest pain
Albuterol
Selective β2-adrenergic receptor agonist → ↑ intracellular adenyl cyclase activity → ↑ cAMP → bronchial smooth muscle relaxation
Bupropion Side Effects
Increases risk of suicidal thinking and behavior in children → young adults with major depressive disorder and other psychiatric disorders
Hydrochlorothiazide
Blocks the early distal tubule’s Na+/Cl- symporter → preventing sodium (and water that follows) reabsorption → diuresis and ↓ ECF volume
Hydrochlorothiazide Side Effects
o hyponatriemia, hypokalemia, hyperglycemia, and metabolic alkalosis and hypercalcemia
o ↓ Na+ reabsorption @ prox dist tubule → ↑ Na+/H+ antiport @ dist dist tubule → ↓ H+ and ↑ Bicarb → poss. alkalosis
Albuterol Side Effects
Tremor, tachycardia, restlessness, apprehension, and anxiety
Varenicline
o Partial Neuronal α₄β₂ nicotinic acetylcholine receptor agonist that prevents nicotine stimulation of mesolimbic dopamine stimulation → ↓ withdrawal symptoms and ↓ nicotine cravings
o Acts as antagonist at nicotinic receptors mitigating the dopamine-enhancing effect
Varenicline Block Box
o Can cause emotional lability and acute psychosis in patients with and without pre-existing psychiatric disease
o Must monitor all patients for behavioral changes and psychiatric symptoms
Bupropion
o Inhibits reuptake of 5-HT, dopamine, and norepinephrine with demonstrated efficacy in smoking cessation
o Increased dopaminergic neurotransmission in the mesolimbic reward pathway, which may buffer nicotine withdrawal-induced cravings
Spironolactone
Antagonizes the aldosterone intracellular receptor →:
o ↓ sodium reabsorption via ↓ mobilization of ENaC to the membrane and ↓ numbers that are open as well as ↓ Na/K-ATPase activity
o ↓ potassium excretion via ↓ mobilization of K-channels to the membrane and ↓ movement from the interstitium due to ↓ Na/K-ATPase activity
Spironolactone Side Effects
o Endocrine metabolic: Gynecomastia
o Gastrointestinal: Diarrhea, Nausea and vomiting
o Neurologic: Somnolence
o Reproductive: Disorder of menstruation, Impotence
Enalapril
ACE inhibitor → prevention of enzymatic cleavage of ANG I into ANG II →
o dilation of efferent arteriole → ↓ GFR
o ↓ direct Na+ reabsorption
o ↓ aldosterone → ↓ Na+ reabsorption
Ketorolac
NSAID Reversible COX pathway inhibitor
Ketorolac Side Effects
o Fatal peptic ulcers
o GI bleeding and/or perforation of the stomach or intestines
Fomepizole
Competitive inhibitor of alcohol dehydrogenase thereby mediating the toxic effects of methanol and ethylene glycol ingestion whereby the alcohols are excreted by the kidneys instead
Fomepizole Side Effects
Hypertriglyceridemia; lightheadedness; nausea; headache
Amlodipine
Calcium channel blocker → ↓ influx of calcium into the cardiac (just a lil’) and vascular smooth muscles → ↓ contractility of the myocytes (just a lil’) and relaxation of vascular smooth muscle → ↓ peripheral resistance and BP
Amlodipine Side Effects
Flushing, constipation (GI smooth muscle relaxation as well), dizziness, headache, fatigue, hypotension
Tolvaptan
Oral ADH V2 receptor antagonist indicated for the treatment of euvolemic and hypervolemic hyponatremia
Tolvaptan Side Effects
Hepatic Injury (CYP3A4), pyrexia (fever), polydipsia, asthenia (lack of strength)
Procainamide
- Class IA Antiarrhythmic; Na-channel blocker
- Moderate blockade of fast Na-channels
- Significantly decreases phase 0 upstroke
- Prolonged action potential duration and refractory period can extinguish re-entrant circuits
Lidocaine
- Class IB Antiarrhythmic; Na-channel blocker
- Mild blockade of fast Na-channels
- Slight increase in phase 0 upstroke
- Blocks Na channels that normally remain open during Phase 2, thus increasing net cation (K+) efflux and shortening the action potential
- Exhibits use-dependentblockade; Does not prolong QT interval
Flecainide
- Class IC Antiarrhythmic; Na-channel blocker
- Significant blockade of fast-Na channels resulting in decreased rate of phase 0 depolarization
- Little to no effect on action potential duration
- Decreases nodal, myocardial, and purkinje conduction velocity; Prolongs atrial, AV, and ventricular refractory periods
Propranolol
- Non-selective beta adrenergic antagonist; Class II Antiarrhythmic
- Competes with catecholamines for beta-1 and beta-2 adrenergic receptors
- Inhibits sympathetic stimulation of the heart
- Reduces resting heart rate, cardiac output, systolic/diastolic blood pressure, and reflex orthostatic hypotension
Procainamide Side Effects
- Arrhythmias
- In high concentrations may induce A-V block or abnormal automaticity and spontaneous firing, the prolonged action potential may lead someone with long QT into TdP
- Agranulocytosis, bone marrow depression, neutropenia, and thrombocytopenia.
Lidocaine Side Effects
- Drowsiness, light-headedness, paresthesia, sensory disturbances, hypotension, bradycardia
- Seizures and respiratory arrest
Flecainide Side Effects
- Palpitations; Nausea; Dizziness; Headache; Dyspnea; Fatigue
- Cardiac arrest; Cardiac dysrhythmias; Cardiogenic shock
Propanolol Side Effects
Assume is the same as the other olol’s:
• Bradyarrhythmia
• AV Block
• Bronchospasm
Amiodarone
- Class III Antiarrhythmic; K-channel blocker
- Inhibits cardiac myocyte K-channels, prolonging effective refractory period and lengthening the action potential
- Exhibits Na-channel and Ca-channel blockade, and non-competitive alpha- and beta-adrenergic antagonism
- Exhibits use-dependent blockade, and does not prolong the QT interval
Amiodarone Side Effects
- Arrythmias, asystole, bradycardia, heart block, heart failure, hypotension, sinus arrest
- Neutropenia, pancytopenia
- Hepatic failure, severe pulmonary toxicity
Ibutilide
- Class III Antiarrhythmic; K-channel blocker
- Inhibits delayed rectifier current prolonging repolarization; Enhances slow inward Na current, further prolonging repolarization
Ibutilide Side Effects
Prolonged QT interval; Torsades de Pointes; Bradyarrhythmias; Heart block; Renal failure
Verapamil
- Class IV Antiarrhythmic; Ca-channel blocker
- Inhibits voltage-dependent L-type Ca-channels, decreasing Phase 0 depolarization of Ca-dependent cells
- Exerts majority of effect on SA and AV nodal tissues, minimal effect on ventricular myocytes
- Causes smooth muscle dilation of vasculature
- Reduces cardiac ionotropy and chronotropy, causing a reduction in heart rate and blood pressure
Verapamil Side Effects
- Rare cardiac arrhythmia, AV block, bradyarrhythmia, exacerbation of heart failure
- Peripheral edema, syncope, gingival hyperplasia, dizziness
Diltiazem
- Class IV Antiarrhythmic; Ca-channel blocker
- Inhibits L-type Ca-channels in cardiac myocytes
- Increases Ca efflux from cell by stimulating Na-Ca and Na-K-ATPases
- Decreases slope of Phase 0 depolarization of Ca-dependent cells
- Exerts majority of effect on AV nodal tissue with minimal effect on ventricular myocytes
- Negative inotropic effects not seen at clinical doses
- Results in mild vasodilation
Diltiazem Side Effects
- Rare cardiac arrhythmia, AV block, bradyarrhythmia, exacerbation of heart failure
- Peripheral edema, syncope, gingival hyperplasia, dizziness
Isoproterenol
- Non-selective β-agonst
- Direct-acting synthetic catecholamine that stimulates both β1- and β2-adrenergic receptors
- Positive inotropy, chronotropy, and dromotropy
- β-2 effect causes vasodilation and reduces peripheral vascular resistance
Isoproterenol Side Effects
- VFib, cerebral hemorrhage, severe hypertension
* Headache, nervousness, tremor, hypertension, palpitations, tachycardia
Theophylline
- Methylxanthine – CNS Stimulant
- Phosphodiesterase inhibitor increasing cAMP levels resulting in bronchodilation
- Relieves airflow obstruction in chronic asthma and decreases symptoms
Theophylline Side Effects
- AFib, Tachyarrhythmia, cerebral hemorrhage, seizure
* Nausea, vomiting, headache, insomnia, tremor, irritability, restlessness
Cromolyn
- Mast cell stabilizer
- Stabilize plasma membrane of mast cells and eosinophils
- Prevents release of histamine, leukotriene, and other mediators of airways inflammation
Cromolyn Side Effects
Nausea and vomiting
Zileuton
- Leukotriene pathway inhibitors
- Selective inhibitor of 5-lipoxygenase, which catelyzes leukotriene formation
- Decreased leukotriene formation, reducing inflammatory response to allergens
Zileuton Side Effects
Hepatotoxicity
Omalizumab
- Anti-IgE Monoclonal Antibody
- Inhibits binding of IgE to high-affinity IgE receptor on mast cells and basophils
- Limits degree of release of mediators of allergic response (asthma)
Omalizumab Side Effects
Injection site reaction, viral disease, upper respiratory infection, sinusitis, headache, pharyngitis
