Pharmacology Flashcards

Question

Anaerobes above the diaphragm: Clostridium perfringens Bacteroides (anaerobic lung abscess) Gram+: Invasive GAS pyogenes

Answer 1

CLINDAMYCIN May cause... Pseudomembranous colitis

Answer 2

Inhibits protein synthesis by binding to 50S subunit and preventing formation of initiation complex.

Answer 3

OXAZOLIDINONES Linezolid May cause... Serotonin syndrome Bone marrow suppression/Thrombocytopenia Peripheral neuropathy Resistance by... Point mutation of rRNA

Answer 4

Inhibit protein synthesis by binding to 23S rRNA of 50S subunit to block translocation. Note - Fidaxomicin inhibits the sigma subunit of RNA polymerase instead

Answer 5

MACROLIDES Azithromycin Clarithromycin (P450 inhibition) Erythromycin (P450 inhibition) Fidaxomicin (treats c. diff) ``` May cause... Prolonged QT Gastrointestinal motility issues Cholestatic hepatitis Rash Eosinophilia Myopathy with Statins (metabolized by P450) ``` Resistance by... Methylation of 23S rRNA-binding site

Answer 6

Inhibit folate synthesis via inhibition of dihydropteroate synthase.

Answer 7

SULFONAMIDES Sulfamethoxazole (SMX) Sulfisoxazole Sulfadiazine ``` May cause (slow acetylators)... Hypersensitivity reactions Photosensitivity Hemolysis in G6PD deficiency Tubulointerstitial nephritis Kernicterus in infants ``` Resistance by... Altered dihydropteroate synthase Decreased uptake Increased PABA (precursor) synthesis

Answer 8

DAPSONE Combine with Rifampin May cause... Hemolysis in G6PD deficiency Methemoglobinemia

Answer 9

Inhibits folate synthesis by inhibiting Dihydrofolate Reductase and thus THF production Note - Sulfamethoxazole inhibits an earlier enzyme (dihydropteroate synthetase)

Answer 10

TRIMETHOPRIM-SULFAMETHOXAZOLE ``` May cause... Megaloblastic anemia (folate deficiency) Leukopenia (folate deficiency) Granulocytopenia (folate deficiency) Teratogen (neural tube defects) Hyperkalemia ```

Answer 11

Inhibits DNA replication by inhibition of topoisomerase II (DNA gyrase) and topoisomerase IV.

Answer 12

FLUOROQUINOLONES Ciprofloxacin Levofloxacin (Respiratory) ``` May cause... Myalgia Tendonitis/tendon rupture (>60 y/o, with prednisone) Cartilage damage (children, pregnant/nursing mothers) Prolonged QT Skin rash Headache and dizziness GI upset ``` Resistance by... Mutation in DNA gyrase or efflux pumps

Answer 13

Lipopeptide disrupts cell membrane of Gram+ cocci.

Answer 14

DAPTOMYCIN May cause... Myopathy Rhabdomyolysis

Answer 15

Forms toxic free radical metabolites which damage DNA.

Answer 16

METRONIDAZOLE May cause... Disulfiram-like reaction Metallic taste Headache

Answer 17

Inhibits DNA-dependent RNA polymerase.

Answer 18

RIFAMYCINS Rifampin (increased cytochrome P-450 - avoid in HIV) Rifabutin (combine with Dapsone for leprosy) May cause... Orange body fluids Resistance by... Monotherapy rapidly leads to reduced binding to RNA polymerase

Answer 19

Decreased synthesis of mycolic acids in mycobacterial cell wall - Requires activation by catalase-peroxidase (KatG)

Answer 20

ISONIAZID May cause... Hepatotoxicity (slow acetylators) Vit B6 deficiency Resistance by... Underexpression of KatG

Answer 21

PYRAZINAMIDE May cause... Hepatotoxicity Hyperuricemia

Answer 22

ETHAMBUTOL ``` May cause... Optic neuropathy (R-G color blindness) ```

Answer 23

STREPTOMYCIN ``` May cause... Tinnitus Vertigo Ataxia Nephrotoxicity ```

Answer 24

Amoxicillin

Answer 25

Ceftriaxone Ciprofloxacin Rifampin

Answer 26

Penicillin G

Answer 27

Polymyxins B and E (colistin)

Answer 28

AMPHOTERICIN B Binds ergosterol (unique to fungi) forming membrane pores that allow leakage of electrolytes through cell wall Supplement K and Mg because of altered renal tubule permeability ``` May cause... Fever/chills (shake and bake) Hypotension Nephrotoxicity (hydrate) Electrolyte abnormalities Anemia (low EPO) IV phlebitis ```

Answer 29

NYSTATIN Same mechanism as Amphotericin B - too toxic to be used systemically

Answer 30

FLUCYTOSINE Inhibits DNA and RNA biosynthesis by conversion to 5-fluorouracil by cytosine deaminase May cause... Bone marrow suppression

Answer 31

Inhibit fungal Ergosterol synthesis via inhibition of cytochrome P-450 - Converts Lanosterol to Ergosterol May cause... Testosterone synthesis inhibition (i.e. Ketoconazole) Liver dysfunction

Answer 32

Fluconazole

Answer 33

Itraconazole

Answer 34

Clotrimazole | Miconazole

Answer 35

TERBINAFINE Inhibits fungal enzyme Squalene Epoxidase - Inhibiting Ergosterol synthesis ``` May cause... Hepatotoxicity Taste disturbance GI upset Headaches ```

Answer 36

Inhibit cell wall synthesis by inhibiting synthesis of B-glucan.

Answer 37

ECHINOCANDINS Caspofungin Anidulafungin Micafungin May cause... Flushing (histamine release) GI upset

Answer 38

GRISEOFULVIN Interferes with microtubule function disrupting mitosis - deposits in keratin-containing tissues ``` May cause... Teratogenic Carcinogenic Confusion Headaches ```

Answer 39

Permethrin - Na channel blocker (neurotoxicity) Malathion - AchE Lindane - GABA blockade (neurotoxicity)

Answer 40

CHLOROQUINE Blocks detoxification of heme into hemozoin - heme accumulates and is toxic to plasmodium Resistance in P. falciparum due to membrane pump that decreases intracellular concentration May cause... Retinopathy Pruritus

Answer 41

Mefloquine Atovaquone/Proguanil Artemether/Lumefantrine

Answer 42

Quinidine | Artesunate

Answer 43

OSELTAMIVIR, ZANAMIVIR Inhibits influenza neuraminidase - Impaired release of viral progeny

Answer 44

Guanosine nucleoside analogs that are monophosphorylated by HSV/VZV Thymidine Kinase leading to DNA chain termination - Not phosphorylated in uninfected cells and so few adverse effects May cause... Obstructive crystalline nephropathy/ARF (hydration) Resistance by... Mutated viral thymidine kinase

Answer 45

GANCICLOVIR 5'-monophosphate nucleoside formed by CMV viral kinase - Preferentially inhibits viral DNA polymerase May cause... Bone marrow suppression (leukopenia, neutropenia, thrombocytopenia) Renal toxicity Resistance by... Mutated viral kinase

Answer 46

FOSCARNET Does not require viral kinase ``` May cause... Nephrotoxicity Hypocalcemia (calcium chelator) Hypomagnesemia Seizures ``` Resistance by... Mutated DNA polymerase

Answer 47

CIDOFOVIR Does not require viral kinase May cause... Nephrotoxicity (given with Probenecid and IV NaCl)

Answer 48

2 NRTIs + 1 integrase inhibitor

Answer 49

Competitively inhibit nucleotide binding to reverse transcriptase and terminate chain (lack 3' OH) - Only Tenofovir (nucleotide) does not need to be phosphorylated ``` May cause... Bone marrow suppression (give G-CSF) Type IV hypersensitivity with HLA-B57:01 (Abacavir) Lipodystrophy Pancreatitis (Didanosine) Lactic acidosis (not Tenofovir) ```

Answer 50

Zidovudine

Answer 51

Bind at different site than NRTIs - do not require phosphorylation ``` May cause... SJS-TEN Hepatotoxicity Vivid dreams (Efavirenz) Teratogen (Efavirenz, Delavirdine) ```

Answer 52

Prevent maturation of new viruses by preventing cleaving of polypeptide products into functional parts

Answer 53

RITONAVIR Alternatively - Rifampin contraindicated with PIs due to induction of P-450 ``` May cause... Hyperglycemia Lipodystrophy (Cushing-like) GI intolerance Nephropathy Hematuria (Indinavir) ```

Answer 54

Inhibits HIV genome integration into host cell - Prevent mRNA transcription by RNA Pol III May cause... Elevated CK

Answer 55

Maraviroc binds CCR5 on surface of T cells/monocytes inhibiting interaction with gp120 Enfuvirtide binds gp41 inhibiting viral entry May cause... Skin reaction at injection site

Answer 56

INF-A IFN-b used in MS, and IFN-y used in CGD ``` May cause... Flu-like symptoms Depression Neutropenia Myopathy ```

Answer 57

RIBAVIRIN May cause... Hemolytic anemia Severe teratogen

Answer 58

SOFOSBUVIR Not monotherapy - use with Ribavirin or Peginterferon alfa May cause... Fatigue Headaches Nausea

Answer 59

SIMEPREVIR Not monotherapy - use with Ledipasvir (NS5A inhibitor) May cause... Photosensitivity Rash

Answer 60

Cell membrane disruption, Protein denaturation Cell membrane disruption, Cytoplasm coagulation Free radical production (sporicidal) Halogenation of proteins/nucleic acids (sporicidal)

Answer 61

``` Sulfonamides (kernicterus, neural tube) Aminoglycosides (ototoxicity) Fluoroquinolones (cartilage damage) Clarithromycin (embryotoxic) Tetracycline (discolored teeth, inhibition of bone growth) Ribavirin (teratogen) Griseofulvin (teratogen) Chloramphenicol (gray baby syndrome) ```

Answer 62

``` Vancomycin Fluoroquinolones Penicillin Aminoglycosides Cephalosporins Metronidazole ``` Also... TMP-SMX

Answer 63

Km = [S] at 1/2Vmax Km = Inversely related to affinity of the enzyme for its substrate (i.e less substrate required to reach 1/2Vmax) Vmax = directly proportional to enzyme concentration

Answer 64

``` Slope = Km/Vmax 1/Vmax = y-intercept -1/Km = x-intercept ``` Noncompetitive inhibitors change y-intercept Competitive inhibitors change x-intercept

Answer 65

Unchanged Increased Decreased potency E.g. Flumazenil

Answer 66

Decreased Unchanged Decreased efficacy

Answer 67

Decreased Unchanged Decreased efficacy E.g. Phenoxybenzamine

Answer 68

Amount in body/Amount in plasma ``` Low = 3-5 L (plasma) Medium = 15 L (interstitial) High = 40 L (intracellular) ```

Answer 69

Increased Vd

Answer 70

Low (blood)

Answer 71

Medium (CSF)

Answer 72

Large (all tissues including fat)

Answer 73

Rate of elimination/Plasma concentration OR Vd x Ke (elimination constant) - increased Vd means more volume has to be cleared per same unit time to excrete the same amount of drug

Answer 74

(0.7 x Vd)/CL 4-5 half-lives to reach steady state (independent of loading/maintenance dosing)

Answer 75

(Cp x Vd)/F ``` Cp = target plasma concentration at steady state F = bioavailability or (AUC PO x IV dose)/(AUC IV x PO dose) ``` Unchanged in renal/liver disease

Answer 76

(Cp x CL x T)/F T = dosage interval if not administered continuously Decreased in renal/liver disease Note - CL and T should match in units (minutes or hours)

Answer 77

Permissive interaction

Answer 78

Tachyphylactic

Answer 79

In additive the total effect is equal to the sum of the individual effects (e.g. APAP, ASA), while in synergistic the total effect is only higher than each individual effect (e.g. Clopidogrel, ASA).

Answer 80

ZERO-ORDER ELIMINATION Capacity-limited elimination - Phenytoin, Ethanol, ASA at toxic doses Half-life is not constant - decreases with decreasing concentration

Answer 81

FIRST-ORDER ELIMINATION Flow-dependent elimination - most drugs Half-life is constant

Answer 82

Trapped in basic environment - alkalinization of weak acid (protonated HA) makes species charged (A-), trapping it in the urine for elimination

Answer 83

Trapped in acidic environment - acidification of a weak base (deprotonated B) makes species charged (protonated BH+), trapping it in the urine for elimination Note - Alternatively some weak bases (TCAs) are treated by NaHCO3 rather than elimination. Alkalinization of a base (protonated BH+) makes species uncharged (deprotonated B), allowing it to move out of the blood and back into fat to be secreted slowly over time

Answer 84

Redox Hydrolysis with cytochrome P-450 Slightly polar, often active product

Answer 85

Conjugation (Methylation, Glucuronidation, Acetylation, Sulfation) Very polar, inactive metabolites for renal elimination

Answer 86

Vmax - Increased y-value = increased Vmax Partial agonists have less efficacy than full agonists

Answer 87

EC50 - left-shifting = decreased EC50 = increased potency

Answer 88

Decreased Independent Decreased efficacy E.g. Buprenorphine

Answer 89

TD50 - ED50

Answer 90

``` Sweat glands (M) Adrenal medulla (Nn - same as autonomic ganglia) ```

Answer 91

Cholinergic innervation | Nm receptor

Answer 92

Ligand-gated Na/K channels

Answer 93

a2 Autoreceptor - often on presynaptic membrane for feedback inhibition

Answer 94

b2 Note - a2 inhibition of insulin release predominates over b2 induced release

Answer 95

``` a1 = q a2 = i b1 = s b2 = s b3 = s M1 = q M2 = i M3 = q D1 = s D2 = i H1 = q H2 = s V1 = q V2 = s ```

Answer 96

Activates Phospholipase C Converts PIP2 to DAG and IP3 DAG activates Protein Kinase C IP3 increases Ca influx (smooth muscle contraction)

Answer 97

``` Activates Adenylate cyclase Converts ATP to cAMP Activates Protein Kinase A Phosphorylation of Phospholamban Increased Ca influx Increased inotropy ``` cAMP-dependent Protein Kinase A (PKA) activated Inhibition of Myosin light chain kinase Vasodilatation

Answer 98

Inhibition of Adenylate cyclase

Answer 99

Amphetamines use NET to enter presynaptic terminal Use VMAT to enter neurosecretory vesicles Displace NE from vesicles NE reaches conc. threshold in presynaptic terminal NET action is reversed and NE is expelled

Answer 100

Tyramine normally degraded by MAO Excess Tyramine enters presynaptic vesicles Other neurotransmitters (e.g. NE) displaced Increased active presynaptic neurotransmitters Increased diffusion into synaptic cleft Increased sympathetic stimulation

Answer 101

Inhibits uptake of Dopamine into vesicles (antipsychotic) where conversion to NE takes place (antihypertensive)

Answer 102

Cholinomimetic - Activates bowel and bladder smooth muscle (M3) and is resistant to AChE Postoperative ileus Neurogenic ileus Urinary retention

Answer 103

Cholinomimetic direct agonist - Copy of acetylcholine Glaucoma

Answer 104

Cholinomimetic direct agonist - Stimulates muscarinic receptors in airway when inhaled Asthma challenge test

Answer 105

Cholinomimetic direct agonist... Contracts ciliary muscle of eye Contracts pupillary sphincter Open-angle glaucoma (ciliary) Closed-angle glaucoma (pupillary) Xerostomia in Sjogren's (sweat, tears, saliva) Note - Resistant to AchE

Answer 106

Cholinomimetic indirect agonist/anticholinesterase Alzheimer's Note - Can also treat with Vit E (antioxidant)

Answer 107

Cholinomimetic indirect agonist/anticholinesterase Diagnosis of Myasthenia Gravis - If response then increase AchEi dose, if no response then cholinergic crisis and stop AchEi

Answer 108

Cholinomimetic indirect agonist/anticholinesterase ``` No CNS penetration (quaternary amine) Postoperative ileus Neurogenic ileus Urinary retention Myasthenia gravis Postoperative NMJ blockade reversal ```

Answer 109

Cholinomimetic indirect agonist/anticholinesterase Crosses blood-brain barrier (tertiary amine) Atropine overdose

Answer 110

Cholinomimetic indirect agonist/anticholinesterase No CNS penetration (quaternary amine) Myasthenia gravis

Answer 111

``` Asthma (M3 bronchoconstriction) COPD (M3 bronchoconstriction) Peptic ulcers (M3 exocrine secretion) ```

Answer 112

ORGANOPHOSPHATE POISONING Atropine - Competitive inhibitor of muscarinic receptors Pralidoxime (2-PAM) for nicotinic symptoms - regenerates AChE

Answer 113

Muscarinic antagonist Parkinson's disease Acute dystonia

Answer 114

Muscarinic antagonist Preoperative reduction in airway secretions Drooling Peptic ulcers

Answer 115

Muscarinic antagonist Antispasmodics for IBS

Answer 116

Muscarinic antagonist - Reduce bronchoconstriction and mucus production COPD Asthma

Answer 117

Muscarinic antagonist Overactive bladder

Answer 118

Muscarinic antagonist RCA MI (reduces vagal tone/bradycardia) Mydriasis induction Cycloplegia ``` May cause... Hot as a hare (decreased sweating) Dry as a bone Red as a beet Blind as a bat Mad as a hatter Bowel and bladder lose their tone Heart runs alone (tachycardia) Increased IOP/Glaucoma ```

Answer 119

Gardener's pupil Due to Jimson weed (Datura) an alkaloid with muscarinic antagonist action

Answer 120

b2 > b1 agonist Asthma COPD

Answer 121

b1 >> b2, a1 agonist - Increased cAMP causes increased intracellular Ca (inotropy) and nodal Na channel activation (chronotropy) Refractory HF Cardiogenic shock (acute MI) Cardiac stress testing May increase oxygen requirement and thus potentiate ischemia Note - Little effect on PVR

Answer 122

D1 = D2 > b > a agonist Note - beta induced inotropy/chronotropy and low doses, alpha induced vasoconstriction at higher doses Shock Heart failure Bradycardia

Answer 123

b > a agonist Note - Alpha effects predominate at higher doses increasing diastolic BP (decreased at low doses) Anaphylaxis Asthma

Answer 124

D1 agonist Postoperative hypertension Hypertensive crisis with renal failure Promotes natriuresis May cause... Hypotension Tachycardia

Answer 125

Non-selective b agonist Evaluation of tachyarrhythmias May worsen ischemia

Answer 126

a1 agonist Autonomic insufficiency/Postural hypotension May exacerbate supine hypertension

Answer 127

a1 >> a2 > b1 agonist Hypotension Shock

Answer 128

a1 > a2 agonist Hypotension Ocular procedures (pupillary dilator) Rhinitis (decongestant) May cause... HTN CNS stimulation/anxiety

Answer 129

Indirect general agonist (promotes release) and reuptake inhibitor Narcolepsy ADHD Obesity

Answer 130

Blocks dopamine reuptake channel ``` Vasoconstriction (DAT binding) Local anesthesia (Na channel blockade) ```

Answer 131

NOREPINEPHRINE (a1 > a2 > b1) Dramatic increase in PVR due to unopposed a1 Greater increase in systolic pressure (via b1) relative to increase in diastolic (high PVR = high venous return) Widened pulse pressure and increased MAP resulting in reflex bradycardia - no net effect on CO

Answer 132

EPINEPHRINE (b > a) Decrease in PVR and diastolic BP via b2 > a1 (low doses) Increased systolic pressure (less than NE) due to increased contractility and HR via b1 Widened pulse pressure and slightly increased MAP - increased CO overall

Answer 133

Sympatholytic - a2 agonists Hypertensive urgency ADHD Tourette's ``` May cause... CNS depression Bradycardia Hypotension Respiratory depression Miosis Rebound hypertension (Clonidine) ```

Answer 134

Sympatholytic - a2 agonists Hypertension in pregnancy May result in... Direct Coombs+ hemolysis SLE-like syndrome

Answer 135

Nonselective, irreversible a-blocker Preoperative Pheochromocytoma to prevent hypertensive crisis May cause... Orthostatic hypotension with reflex tachycardia

Answer 136

Nonselective, reversible a-blocker Given to patients on MAOi who eat Tyramine May cause... Orthostatic hypotension with reflex tachycardia

Answer 137

a1 selective a-blocker BPH PTSD (Prazosin) Hypertension May cause on first dose... Orthostatic hypotension Note - Tamsulosin cannot be used in HTN as it is selective for a1-AD (prostate) rather than a1B (vascular)

Answer 138

a2 selective a-blocker Depression May cause... Sedation Increased appetite Increased serum cholesterol

Answer 139

``` Decreased HR/Inotropy decrease O2 demand Decreased AV conduction velocity Decreased CO/Renin (b1 on JGA cells) Decreased sympathetic activation Decreased secretion of aqueous humor Decreased hepatic venous pressure gradient/portal HTN ```

Answer 140

``` Erectile dysfunction Bradycardia AV block Asthma/COPD exacerbation HF Seizures Dyslipidemia (Metoprolol) ```

Answer 141

``` Acebutolol Atenolol Betaxolol Esmolol Metoprolol ```

Answer 142

Nadolol Pindolol Propranolol Timolol May cause... Hypoglycemia masking Cause hyperkalemia by interfering with B2 mediated K uptake in cells

Answer 143

Carvedilol | Labetalol

Answer 144

Cardiac-selective b1-blockade | Stimulation of b3 activating vascular NO synthase

Answer 145

ANTIHISTAMINES First generation: Diphenhydramine, Dimenhydrinate, Chlorpheniramine, Hydroxyzine, Promethazine, Meclizine, Cyproheptadine Second generation: Loratadine, Fexofenadine, Desloratadine ``` First generation may cause... Sedation Antimuscarinic Anti-a-adrenergic (postural hypotension) Serotonergic (appetite stimulation) ```

Answer 146

Guaifenesin - Thins respiratory secretions NAC - Mucolytic liquefies mucus in COPD patients by disrupting disulfide bonds

Answer 147

Antitussive - NMDA receptor antagonist May cause... Serotonin syndrome Mild opioid effects (Naloxone as antidote)

Answer 148

Competitive antagonist of Endothelin-1 receptor leading to decreased pulmonary vascular resistance May cause... Hepatotoxicity

Answer 149

Inhibits cGMP PDE-5, prolonging vasodilatory effect of NO via PKG ``` May cause... Flushing Headache Dyspepsia Cyanopica (blue-tinted vision) Hypotension with nitrates ```

Answer 150

PGI2 (Prostacyclin) with direct vasodilatory effects on pulmonary and systemic arterial vascular beds - inhibits platelet aggregation May cause... Flushing Jaw pain

Answer 151

Fluticasone, Budesonide Inactivate NF-kB decreasing production of inflammatory cytokines (e.g. TNF-a)

Answer 152

Ipratropium Competitively blocks muscarinic receptors preventing bronchoconstriction

Answer 153

Montelukast/Zafirlukast block LTD4 receptors (CysLT1) in ASA-induced asthma Zileuton is a 5-LOX inhibitor blocking conversion of arachidonic acid to leukotriene (hepatotoxicity) Note - Second line to steroids as drugs that work on late response to mediators (e.g. inflammation leading to bronchial hyperreactivity)

Answer 154

Anti-IgE monoclonal antibody blocks binding to FceRI Allergic asthma resistant to inhaled corticosteroids and long-acting b2 agonists (e.g. Salmeterol, Formoterol)

Answer 155

Increased tubular fluid osmolarity increases urine flow Elevated ICP or intraocular pressure Note - Contraindicated in anuria or HF due to risk of pulmonary edema

Answer 156

Carbonic anhydrase inhibitor causes self-limited NaHCO3 diuresis ``` Glaucoma Urinary alkalinization Metabolic alkalosis Pseudotumor cerebri Altitude sickness ``` May cause... Proximal RTA NH3 toxicity Sulfa allergy

Answer 157

Inhibits NaK2Cl cotransporter in TALH Abolishes medullary hypertonicity (urinary concentration) Increases Ca excretion Edematous states Hypertension Hypercalcemia ``` May cause... Hypokalemic metabolic alkalosis (contraction) Ototoxicity Dehydration Allergy (sulfa) Interstitial nephritis Gout ```

Answer 158

Non-sulfa inhibitor of NaK2Cl cotransporter in TALH Diuresis in patients with sulfa allergies - higher risk of ototoxicity

Answer 159

Inhibits NaCl cotransporter in early DCT Decreases Ca excretion ``` Hypertension HF Calcium stones (hypercalciuria) Nephrogenic diabetes insipidus (free water loss) Osteoporosis ``` ``` May cause... Allergy (sulfa) Hyponatremia (maintain corticomedullary conc gradient) Hypokalemic metabolic alkalosis (contraction) Hypercalcemia (basolateral NCX) Hyperglycemia Hyperlipidemia Hyperuricemia ```

Answer 160

Spironolactone/Eplerenone competitive antagonists of aldosterone receptor in cortical collecting tubule Triamterene/Amiloride block ENaC in cortical collecting tubule ``` HF Hyperaldosteronism (Conn syndrome) Hypokalemia Hepatic ascites (Spironolactone) Nephrogenic diabetes insipidus (Amiloride) ``` May cause... Hyperkalemia Gynecomastia (Spironolactone) Metabolic acidosis

Answer 161

Prevents ACE conversion of ATI to ATII and inactivation of bradykinin - Increased Renin because of loss of feedback Hypertension Post-MI HF Diabetic nephropathy - Decreased intraglomerular pressure (afferent dilation) slows GBM thickening ``` May cause... First dose hypotension Cough Angioedema Hyperkalemia Increased Cr (decreased GFR) ARF if bilateral RAS Teratogen (fetal anuria) ``` Note - Angioedema (may be delayed) from increased bradykinin; contraindicated in C1 esterase inhibitor deficiency Note - Increased Cr/decreased GFR due to inability to preferentially constrict efferent arteriole (above 30% is dangerous)

Answer 162

Selectively blocks ATII binding to AT1 receptor (smooth muscle, adrenal cortex) - No effect on bradykinin and good for patients with ACEi intolerance ``` Hypertension Post-MI HF Proteinuria Diabetic nephropathy (decreased intraglomerular pressure slows GBM thickening) ``` ``` May cause... Hypotension Hyperkalemia Increased Cr (decreased GFR) Teratogen ```

Answer 163

Direct Renin inhibitor Hypertension May cause... Hypotension Hyperkalemia Increased Cr (decreased GFR)

Answer 164

Thromboembolic events | Hypertension

Answer 165

IDIOSYNCRATIC DRUG REACTION (TYPE B)

Answer 166

Reversible blockade of Gs H2-receptors decreasing gastric acid secretion by parietal cells in response to Histamine from ECL cells Peptic ulcer Gastritis Mild esophageal reflux May cause... Antiadrenergic effects Decreased renal excretion of Cr (Cimetidine, Ranitidine)

Answer 167

Irreversible inhibition of H/K ATPase in parietal cells Peptic ulcer Gastritis Esophageal reflux Zollinger-Ellison syndrome May cause... Increased C. diff risk Pneumonia Hypomagnesemia with long-term use

Answer 168

Hypokalemia Decreased drug bioavailability Delayed gastric emptying Aluminum hydroxide: Constipation Hypophosphatemia Osteodystrophy Calcium carbonate: Hypercalcemia (milk-alkali syndrome) Rebound HCl secretion Chelation of Tetracyclines Magnesium hydroxide: Diarrhea

Answer 169

Binds to ulcer base providing physical barrier and allowing HCO3 secretion to reestablish pH gradient mucosal layer Ulcer healing Traveler's diarrhea

Answer 170

PGE1 analog increasing production and secretion of gastric mucous, while decreasing gastric acid production (Gi) NSAID ulcer Induction of labor May cause... Diarrhea Abortifacient

Answer 171

Somatostatin analog - Decreases stomach, pancreatic, and gallbladder secretions Acute variceal bleeding VIPoma Carcinoid Acromegaly May cause... Steatorrhea Cholelithiasis (CCK inhibition)

Answer 172

OSMOTIC LAXATIVES

Answer 173

Combination of Sulfapyridine and 5-ASA activated by colonic bacteria UC Crohn's colitis May cause... Sulfonamide toxicity Reversible oligospermia

Answer 174

u-opioid agonist slowing gut motility - Poor CNS penetration means low addictive potential Good for IBS, Diarrhea

Answer 175

5-HT3 antagonist decreasing vagal stimulation in area postrema Antiemetic (postoperative, chemotherapy) May cause... Prolonged QT

Answer 176

D2 receptor antagonist... Increases LES tone Decreases pyloric tone Increases peristalsis (no effect on colonic transit time), Inhibits D2 action in area postrema (near NTS) ``` Diabetic/Postoperative gastroparesis Central antiemetic (e.g. migraines) ``` ``` May cause... Parkinsonism (contraindicated) Tardive dyskinesia Sedation Contraindicated in small bowel obstruction ``` Note - Drug interactions with Digoxin, diabetic agents

Answer 177

Inhibits gastric and pancreatic lipase decreasing absorption of dietary fats (weight loss) May cause... Steatorrhea Vit A, D, E, K deficiency

Answer 178

Nontoxic bile acid - Increases bile secretion and decreases cholesterol secretion Primary biliary cirrhosis Gallstone prevention or dissolution

Answer 179

Inhibition of cAMP phosphodiesterase - Results in bronchodilation May cause... GI disturbance Seizure Arrhythmias Note - Metabolized by Cytochrome P-450

Answer 180

Proline residues to prevent polymerization (e.g. Regular) and allow rapid absorption Note - Absorption is delayed in long-acting forms by adding Protamine (NPH), fatty acid (Detemir), Acidic groups (Glargine)

Answer 181

Regular insulin - IV form available

Answer 182

BIGUANIDES Increases peripheral glucose uptake and insulin sensitivity (no islet cell function needed) while decreasing gluconeogenesis - Causes modest weight loss May cause... GI disturbance Lactic acidosis in renal insufficiency Note - Always obtain baseline renal function tests

Answer 183

SULFONYLUREAS Close K channel in beta cell membranes causing cell depolarization and Ca influx - endogenous insulin release so need some islet cell function (e.g. not T1DM) May cause... Weight gain Hypoglycemia (especially in renal insufficiency)

Answer 184

GLITAZONES/THIAZOLIDINEDIONES Binds PPAR-y nuclear transcription regular leading to... Insulin sensitivity (GLUT4) Adiponectin production (b-oxidation) Decreased TNF-a, Leptin ``` May cause... Weight gain (Leptin) Edema HF exacerbation Osteoporosis No risk of hypoglycemia ``` Note - Safe to use in renal insufficiency

Answer 185

MEGLITINIDES Bind different K channel site than Sulfonylureas - Useful for post-prandial high glucose (short-acting) May cause... Weight gain Hypoglycemia (especially in renal insufficiency)

Answer 186

GLP-1 ANALOGS Bind G-protein and increased glucose-dependent insulin release while inhibiting glucagon - Causes modest weight loss May cause... Nausea/Vomiting (inhibit gastric emptying) Pancreatitis

Answer 187

DPP-4 INHIBITORS Inhibits DPP-4 enzyme that deactivates GLP-1 May cause... Nasopharyngitis Note - No hypoglycemia because glucose-dependent

Answer 188

AMYLIN ANALOGS Decreased gastric emptying and glucagon May cause... Hypoglycemia Nausea

Answer 189

SGLT-2 INHIBITORS ``` May cause... Glucosuria UTIs/Vaginal yeast infections Hyperkalemia Orthostatic hypotension (dehydration) ``` Note - Always get baseline renal function tests as these drugs need a working PCT to be effective

Answer 190

A-GLUCOSIDASE INHIBITORS Inhibit intestinal brush-border a-glucosidases delaying carbohydrate hydrolysis and glucose absorption - leads to decreased postprandial hyperglycemia May cause... GI upset

Answer 191

THIONAMIDES Block thyroid peroxidase preventing oxidation and organification of iodine PTU/Propranolol also blocks 5-deiodinase decreasing peripheral conversion of T4 to T3 ``` May cause... Agranulocytosis (sore throat, fever) ANCA vasculitis Skin rash Aplastic anemia Hepatotoxicity Cholestasis Teratogen (Methimazole) ```

Answer 192

ADH ANTAGONISTS Used in SIADH to block action at V2 receptor

Answer 193

OCTREOTIDE Inhibits GH and release of most GI hormones

Answer 194

ADH ANTAGONIST (TETRACYCLINE) May cause... Photosensitivity Bone and teeth abnormalities

Answer 195

``` Cushing syndrome Adrenocortical atrophy Peptic ulcers Steroid diabetes Steroid psychoses Cataracts ```

Answer 196

ALDOSTERONE ANALOG Mineralocorticoid replacement in primary adrenal insufficiency ``` May cause... Edema HF Hyperpigmentation Cortisol-like effects ```

Answer 197

Sensitizes Ca-sensing receptor (CaSR) in parathyroid gland decreasing PTH - Useful for dialysis patients May cause... Hypocalcemia Note - Sevelamer binds phosphate to decrease GI absorption in dialysis patients

Answer 198

LEUPROLIDE GnRH analog which is an agonist when pulsatile, and antagonist when continuous

Answer 199

Hypothalamic estrogen receptor antagonist - prevents feedback inhibition of LH and FSH ``` May cause... Multiple pregnancies Visual disturbances Hot flashes Ovarian enlargement ```

Answer 200

Tamoxifen is an estrogen receptor antagonist at the breast, but agonist at bone and uterus - increases the risk of DVT and endometrial cancer Raloxifene is an estrogen receptor antagonist at the breast and uterus, but agonist at bone - increases risk of DVT only Note - SERMs can also be used to treat gynecomastia in ADT patients

Answer 201

AROMATASE INHIBITORS ER+ breast cancer in postmenopausal women

Answer 202

PROGESTINS Includes Levonorgestrel, Medroxyprogesterone, Etonogestrel, Norethindrone, and Megestrol Decreases growth of endometrium, thickens cervical mucus (mini-pill, IUD), and decreases LH/FSH (combined OCP) Note - Presence of withdrawal bleeding excludes anatomic defects (e.g. Asherman) and chronic anovulation

Answer 203

B2-agonists that relax the uterus - Decreases contraction frequency during labor

Answer 204

Synthetic androgen that acts as partial agonist at androgen receptor ``` May cause... Hepatotoxicity Decreased HDL Weight gain Edema Acne, hirsutism, masculinization ```

Answer 205

TESTOSTERONE, METHYLTESTOSTERONE

Answer 206

Ketoconazole - Inhibits steroid synthesis by Desmolase Spironolactone - Inhibits steroid binding, 17a-hydroxylase, and Desmolase May cause... Gynecomastia Amenorrhea

Answer 207

5a-reductase inhibitor decreases conversion of testosterone to DHT

Answer 208

MINOXIDIL Direct arteriolar vasodilator

Answer 209

Reversible COX inhibitor - CNS only so not anti-inflammatory

Answer 210

Irreversible COX1/2 inhibitor by covalent acetylation ``` Low dose (< 300) - Decreases platelet aggregation Medium dose (< 2400) - Antipyretic and Analgesic High dose (< 4000) - Antiinflammatory ``` ``` May cause... Increased bleeding time (normal PT, PTT) Gastric ulceration Tinnitus Interstitial nephritis Respiratory alkalosis early in overdose Mixed metabolic alkalosis-respiratory acidosis later ```

Answer 211

Reversible inhibition of COX2 - Inducible by IL-1/TNF-a Spares COX1 (constitutive) - Maintains gastric mucosa and produces TXA2 May cause... Thrombosis Impaired renal perfusion Sulfa allergy

Answer 212

Reversible inhibition of COX1/2 May cause... Gastric ulceration Interstitial nephritis Renal ischemia Note - Naproxen, Indomethacin can be used for acute gout attacks

Answer 213

Reversibly inhibits Dihydroorotate Dehydrogenase - disrupts Pyrimidine synthesis and T cell proliferation Rheumatoid arthritis Psoriatic arthritis ``` May cause... Diarrhea Hypertension Hepatotoxicity Teratogen ```

Answer 214

Pyrophosphate analog binds Hydroxyapatite in bone - inhibits osteoclast activity ``` Osteoporosis Hypercalcemia Paget (osteitis deformans) Metastatic bone disease Osteogenesis imperfecta ``` May cause... Pill esophagitis (take with water, sit upright after) Osteonecrosis of jaw Atypical stress fractures

Answer 215

Recombinant PTH analog - increases osteoblastic activity May cause... Transient hypercalcemia

Answer 216

Competitive inhibitor of Xanthine Oxidase preventing conversion of Hypoxanthine and Xanthine to Urate Used in... Gout control Uric acid stones Lymphoma/Lymphoma (tumor lysis syndrome) May cause... DRESS (fever, lymphadenopathy, rash, organ dysfunction) Note - Also increases levels of Azathioprine and 6-Mercaptopurine as they are metabolized by Xanthine Oxidase

Answer 217

Recombinant Uricase converts Urate to Allantoin - more water soluble Pegloticase - Gout control Rasburicase - Tumor lysis

Answer 218

Binds OAT - Inhibits reabsorption of uric acid in PCT Gout control May cause... Uric acid stones Note - Diuretics and ASA prevent tubular secretion

Answer 219

Binds and stabilizes Tubulin - Inhibits microtubule polymerization and thus Neutrophil chemotaxis and degranulation Acute gout attack May cause... GI disturbance

Answer 220

ETANERCEPT Fusion protein (TNF-a receptor, IgG Fc) acts as TNF decoy receptor

Answer 221

INFLIXIMAB, ADALIMUMAB Anti-TNFa monoclonal antibody

Answer 222

HEPARIN Inhibits II (Thrombin) and Xa - Follow PTT May cause... HIT Bleeding Osteoporosis Note - Antidote is Protamine sulfate

Answer 223

LMWH More specific for Xa - Does not require lab monitoring Note - Better bioavailability and longer half life, but no antidote

Answer 224

DIRECT THROMBIN INHIBITORS Argatroban Dabigatran Bivalirudin Does not require lab monitoring May cause... Bleeding Note - No antidote, but may attempt activated prothrombin complex concentrate (PCC) or fibrinolytics (tranexamic acid)

Answer 225

WARFARIN Prevents y-carboxylation of Vit K - acts in liver May cause... Bleeding Skin/tissue necrosis Teratogen (stippled epiphyses) Note - Reverse rapidly with FFP, slowly with Vit K

Answer 226

DIRECT FACTOR XA INHIBITORS DVT/PE prophylaxis Afib stroke prevention May cause... Bleeding Note - No reversal agent

Answer 227

THROMBOLYTICS Aid conversion of plasminogen to plasmin cleaving thrombin and fibrin clots - Follow PT and PTT ``` Avoid if... Bleeding risk Severe hypertension (ICH) ``` Treat toxicity with Aminocaproic acid, and possible FFP/Cryo Note - Platelet count normal

Answer 228

ADP RECEPTOR INHIBITORS Irreversible blockade of ADP receptors on platelets prevents expression of GpIIb/IIIa ACS Coronary stenting Thrombotic stroke prophylaxis May cause... Neutropenia (Ticlopidine) TTP

Answer 229

Phosphodiesterase III inhibitors - Increase cAMP results in increased contractility, arterial vasodilation, and decreased platelet aggregation Intermittent claudication Vasodilation Stroke/TIA prevention (with ASA) ``` May cause... Nausea Headache Facial flushing Hypotension Abdominal pain ```

Answer 230

GPII/IIIA INHIBITORS Bind to receptors and prevent platelet aggregation - Abciximab is made from monoclonal antibody Fab fragments Unstable angina Coronary angioplasty May cause... Bleeding Thrombocytopenia

Answer 231

AZATHIOPRINE 6-Mercaptopurine (metabolite of Azathioprine) Purine analog activated by HGPRT - Prevents de novo purine synthesis May cause... Myelosuppression GI toxicity Liver toxicity Note - Metabolized by Xanthine Oxidase so increased toxicity with Allopurinol or Febuxostat Note - Mutation in Thiopurine Methyltransferase also increase toxicity

Answer 232

CLADRIBINE Purine analog inhibitor of DNA polymerase May cause... Myelosuppression Nephrotoxicity Neurotoxicity

Answer 233

CYTARABINE (ARABINOFURANOSYL CYTIDINE) Pyrimidine analog inhibitor of DNA polymerase May cause... Myelosuppression Megaloblastic anemia Pancytopenia

Answer 234

5-FLUOROURACIL Pyrimidine analog bioactivated to 5-FdUMP and inhibits Thymidylate Synthesis - Decreased dUMP to dTMP May cause... Myelosuppression especially with Leucovorin Note - Potentiated with Leucovorin

Answer 235

METHOTREXATE Folic acid analog competitively inhibits Dihydrofolate Reductase - Decreased dTMP synthesis ``` May cause... Myelosuppression Hepatotoxicity Mucositis (mouth ulcers) Pulmonary Fibrosis ``` Note - Rescue with Leucovorin

Answer 236

BLEOMYCIN Induces free radical formation leading to breaks in DNA strands - works in G2 phase May cause... Pulmonary fibrosis Skin hyperpigmentation Note - Minimal myelosuppression

Answer 237

DACTINOMYCIN (ACTINOMYCIN D) Intercalates in DNA May cause... Myelosuppression

Answer 238

DOXORUBICIN/DAUNORUBICIN Generates free radicals and intercalates with DNA May cause... Cardiotoxicity - prevent with Dexrazoxane Myelosuppression Alopecia

Answer 239

BUSULFAN May cause... Severe myelosuppression Pulmonary fibrosis Hyperpigmentation

Answer 240

CYCLOPHOSPHAMIDE, IFOSFAMIDE Requires bioactivation by liver May cause... Myelosuppression Hemorrhagic cystitis - prevent with Mesna or NAC

Answer 241

NITROSOUREAS Requires bioactivation - crosses BBB May cause... Convulsions Dizziness Ataxia

Answer 242

PACLITAXEL/TAXOLS Hyperstability polymerized microtubules to prevent anaphase May cause... Myelosuppression Neuropathy Hypersensitivity

Answer 243

VINCRISTINE/VINBLASTINE Bind b-tubulin and inhibit polymerization preventing mitotic spindle formation May cause... Peripheral neuritis, areflexia Paralytic ileus Note - Vincristine for Hodgkin's, Vinblastine for non-Hodgkin's

Answer 244

CISPLATIN, CARBOPLATIN Cross-links DNA May cause... Nephrotoxicity - Prevent with Amifostine/Diuresis Ototoxicity Peripheral neuropathy

Answer 245

ETOPOSIDE, TENIPOSIDE Inhibits Top II increasing DNA degradation May cause... Myelosuppression Alopecia

Answer 246

IRINOTECAN, TOPOTECAN Inhibits Top I preventing DNA unwinding and replication May cause... Severe myelosuppression Diarrhea

Answer 247

HYDROXYUREA Inhibits Ribonucleotide Reductase (UDP to dUDP) - Decreasing DNA synthesis (S-phase specific) Also increases HbF May cause... Severe myelosuppression

Answer 248

Antibody against VEGF - Inhibits angiogenesis May cause... Hemorrhage Blood clots Impaired wound healing Note Bevacizumab/Ranibizumab may both also treat wet macular degeneration

Answer 249

EGFR tyrosine kinase inhibitor May cause... Rash

Answer 250

Monoclonal antibody against EGFR May cause... Rash Elevated LFTs Diarrhea

Answer 251

Tyrosine kinase inhibitor of bcr-abl and c-kit May cause... Fluid retention

Answer 252

Monoclonal antibody against CD20 - B-cell marker May cause... Increased risk of PML

Answer 253

Monoclonal antibody against HER-2 (c-erbB2) tyrosine kinase receptor - prevents intracellular signaling and induces antibody-dependent cytotoxicity May cause... Cardiotoxicity

Answer 254

Small molecule inhibitor of BRAF oncogene+ (V600E) melanoma

Answer 255

Decreases synaptic transmission by closing pre-synaptic Ca channels and opening post-synaptic K channels Note - No tolerance to miosis or constipation Note - May cause biliary colic (sphincter of Oddi contraction)

Answer 256

k-opioid agonist and u-opioid antagonist May cause... Opioid withdrawal with full antagonist

Answer 257

k-opioid agonist and u-opioid partial agonist Used in severe pain - Partial agonist so less respiratory depression May cause... Opioid withdrawal with full agonist

Answer 258

Very weak opioid agonist Serotonin and NE reuptake inhibitor May cause... Opioid symptoms Decreases seizure threshold Serotonin syndrome

Answer 259

Blocks thalamic T-type Ca-channels ``` May cause... GI disturbance Headache Urticaria SJS ```

Answer 260

Blocks Na channels - Zero order kinetics ``` May cause (Dose-dependent saturation)... CNS symptoms (ataxia, nystagmus) Megaloblastic anemia Gingival hyperplasia Hirsutism SJS DRESS Teratogen (NTD, craniofacial, nail hypoplasia) ``` Note - Metabolized by Cytochrome P-450

Answer 261

Blocks Na channels increasing refractory period ``` May cause... Agranulocytosis/Aplastic anemia Hepatotoxicity SJS DRESS SIADH Teratogen ```

Answer 262

Induces Na channels Inhibits GABA transaminase increasing GABA ``` May cause... GI distress Fetal hepatotoxicity - measure LFTs Pancreatitis Weight gain Tremor Teratogen (neural tube defects) ``` Note - Vigabatrin also inhibits GABA transaminase

Answer 263

Inhibits voltage-gated Ca channels - acts as GABA analog May cause... Sedation Ataxia

Answer 264

Blocks Na channels Increases GABA activity May cause... Sedation Mental dulling Kidney stones Note - Tiagabine inhibits GABA reuptake

Answer 265

Blocks Na channels May cause... SJS

Answer 266

Facilitates GABA by increasing Cl channel duration May cause... Respiratory depression CV depression

Answer 267

Lorazepam Oxazepam Temazepam Note - Normally Diazepam/Chlordiazepoxide prefered due to self-tapering profile

Answer 268

Triazolam Oxazepam Midazolam (endoscopy) Alprazolam Lorazepam Temazepam Note - Less active metabolites

Answer 269

ACt on BZI subtype of GABA receptor May cause... Ataxia Headaches Confusion Note - Alternative is Ramelteon (melatonin agonist)

Answer 270

Decreased solubility in blood - Rapid induction Increased solubility in lipids - Increased potency Note - Potency = 1/MAC

Answer 271

INHALED ANESTHETICS ``` Hepatotoxicity (centrilobular) Nephrotoxicity Proconvulsant Expansion of trapped gas in body cavities Hypotension ``` Note - Increase cerebral blood flow

Answer 272

PROPOFOL Potentiates GABA - High lipophilicity rapidly redistributes from high flow organs (brain, heart, liver, kidneys) to lower flow organs (muscle, skin, fat) Note - Less postoperative nausea

Answer 273

THIOPENTAL Note - Decreases cerebral blood flow

Answer 274

Small myelinated fibers Small unmyelinated fibers Large myelinated fibers Large unmyelinated fibers Note - Loss of sensation (first to last) is Pain > Temperature > Touch > Pressure

Answer 275

Acidic tissue makes alkaline anesthetics more charged and thus unable to penetrate the membrane Note - Block inner portion of channel

Answer 276

POLARIZING NEUROMUSCULAR BLOCKER Strong Ach receptor agonist produces sustained depolarization Diminished TOF response (phase I) followed by progressive reduction (phase II) Can only reverse with AcheE inhibitors in Phase II (repolarized but desensitized) May cause... Hyperkalemia Hypercalcemia Malignant hyperthermia

Answer 277

NONDEPOLARIZING NEUROMUSCULAR BLOCKERS Competitive antagonists of Ach receptors - Reverse with AchE inhibitor (Neostigmine, Edrophonium) Progressive reduction with TOF due to additional presynaptic blockade May cause... Flushing Bronchoconstriction Hypotension Note - Give AchE inhibitor (Physostigmine, Neostigmine) with Atropine to prevent muscarinic toxicity

Answer 278

Activates GABA-b receptors at spinal cord level - Induces skeletal muscle relaxation Note - Cyclobenzaprine is a central acting relaxant (TCA-like) Note - Tizanidine (a2 agonist) also used

Answer 279

``` Dopamine agonist (Ergot) Dopamine agonist (non-Ergot) Increased Dopamine release, Decreased uptake Peripheral DOPA decarboxylase inhibitor MAO-B inhibitors COMT inhibitors (peripheral, central) Antimuscarinic - Tremor/Rigidity ``` Note - Amantadine may cause Ataxia/Livedo Reticularis

Answer 280

``` NMDA antagonist (Confusion, Hallucinations) AChE inhibitors ```

Answer 281

Hydralazine Labetalol Methyldopa Nifedipine

Answer 282

Dimercaprol (British anti-Lewisite) or DMSA EDTA, Succimer Deferoxamine

Answer 283

Neurokinin 1 (NK1) receptor antagonists in area postrema Chemotherapy antiemetic

Answer 284

Partial nicotinic acetylcholine receptors - Reduces cravings and rewards (competitive)

Answer 285

Monoclonal antibody Receptor molecule Kinase inhibitor Note - For antibodies, -xi- is chimeric -zu- is humanized

Answer 286

Highly soluble gas saturates the blood more slowly leading to slower brain saturation and thus onset time Higher solubility in peripheral tissues means more drug is needed for blood saturation thus increasing onset time

Answer 287

Hydralazine Procainamide Isoniazid Note - Slow acetylators

Answer 288

Depletion of Substance P

Answer 289

DIHYDROPYRIDINES Amlodipine, Clevidipine, Nicardipine, Nifedipine, Nimodipine (Post-SAH) May cause... Peripheral edema Flushing/Dizziness Gingival hyperplasia

Answer 290

Increases cAMP causing smooth muscle relaxation - Mostly affects Arterioles (afterload) May cause... Reflex tachycardia (Angina/CAD) Fluid retention Angina

Answer 291

Inhibits late phase of Na current - Reduces diastolic wall tension and oxygen consumption with no effect on HR or Inotropy May cause... Long QT

Answer 292

MDR1 P-glycoprotein (ATP efflux pump)

Answer 293

BILE ACID RESINS Liver uses cholesterol to make more bile acid Upregulates HMG-CoA (synergy) May cause... Hypertriglyceridemia GI upset Malabsorption Note - Ezetimibe inhibits cholesterol absorption directly instead of bile acid resins but may cause transaminitis

Answer 294

FIBRATES Upregulates LPL to increase TG clearance Activates PPAR-a to decrease hepatic VLDL production Induce HDL synthesis May cause... Myopathy (with Statins) Cholesterol gallstones

Answer 295

NIACIN (VIT B3) Inhibits hormone sensitive lipase Reduces hepatic VLDL production May cause... Red, flushed face (treat with NSAID) Hyperglycemia Hyperuricemia

Answer 296

HF - Increased Ca release from SR increases inotropy Afib - Increased vagal tone decreases HR ``` May cause... Cholinergic syndromes Color abnormalities AT with AV block Hyperkalemia (poor prognosis) ```

Answer 297

Na channel blockade... Increased AP duration Slowed conduction speed Increased QT interval Includes... Quinidine, Procainamide (WPW), Disopyramide May cause... Cinchonism (Headache, Tinnitus) SLE Torsades Note - Treat Torsades with Mg

Answer 298

Na channel blockade... Decreased AP duration Normal conduction speed Preferentially affects ischemic tissue Includes... Lidocaine, Tocainide, Mexiletine May cause... CNS symptoms CV depression

Answer 299

Na channel blockade... Normal AP duration Slowed conduction speed Preferentially affects AV node and accessory tracts Includes... Moricizine, Flecainide, Propafenone May cause... Arrhythmias post MI Contraindicated in structural/ischemic heart disease Note - Stronge use-dependence - Due to slow dissociation from Na channels increased HR increases effect of drug (wide QRS)

Answer 300

B-blockers... Decreased slope of phase 4 - Slowed sinus discharge Decreased cAMP - Slows conduction and prolongs ERP ``` May cause... Impotence COPD/Asthma Bradycardia Hypoglycemia masking (CNS sedation) Dyslipidemia (Metoprolol) Vasospasm (Propranolol) ``` Note - Treat overdose with Atropine/Glucagon

Answer 301

K channel blockers... Increased AP duration Normal conduction velocity Increased QT interval Includes... Amiodarone, Ibutilide, Dofetilide, Sotalol ``` May cause... Bradycardia Pulmonary fibrosis (Amiodarone) Hepatotoxicity (Amiodarone) Thyroid toxicity (Amiodarone) Photodermatitis (Amiodarone) Lower Torsades risk ``` Note - Check LFTs, PFTs, and TFTs before using Amiodarone Note - Show reverse use-dependency so slower HR results in more prolonged QT

Answer 302

Non-dihydropyridines (Verapamil, Diltiazem)... Slowed sinus discharge Slows conduction and prolongs ERP ``` May cause... Constipation Bradycardia AV block Contraindicated in CHF (negative inotrope) ``` Note - May mask ischemia during stress test

Answer 303

Increased K efflux hyperpolarizes cell and decreases Ca influx ``` May cause... Flushing Hypotension Chest pain Sense of impending doom Bronchospasm ``` Note - Decreased effectiveness with Caffeine and Theophylline

Answer 304

Converts Fe2+ to Fe3+ (MetHb) which binds CN removing it from Cytochrome C Oxidase in ETC

Answer 305

CALCINEURIN INHIBITOR (NFAT) Blocks T-cell activation by inhibiting IL-2 transcription ``` May cause... Nephrotoxicity Neurotoxicity Metabolic disorder Gingival hyperplasia (Cyclosporine) Myopathy (with Statins) ```

Answer 306

MTOR INHIBITOR Blocks T-cell activation and B-cell proliferation by inhibiting response to IL-2 May cause... Pancytopenia Metabolic disorder

Answer 307

Monoclonal antibodies blocking IL-2 May cause... Edema HTN Tremor

Answer 308

Inhibits IMP dehydrogenase preventing purine synthesis ``` May cause... GI upset Pancytopenia Invasive CMV infection Metabolic disorder ```

Answer 309

Recovery of bone marrow

Answer 310

HCV, HBV, Kaposi, Melanoma MS Chronic granulomatous disease

Answer 311

Thrombocytopenia

Answer 312

Antibody against a4-integrin (WBC adhesion) May cause... PML (JC virus)

Answer 313

Antibody against RANKL - Inhibits osteoclast maturation by mimicking Osteoprotegerin

Answer 314

Antibody against RSV F protein - For high risk-infants

Answer 315

Prevent conversion of HMG-CoA to Mevalonate Upregulation of LDLR further reduces circulating LDL

Answer 316

Phenobarbital, Phenytoin, Carbamazepine (CYP-450) Aromatase inhibitors, Medroxyprogesterone GnRH agonists PPIs Steroids, Unfractionated Heparin, Thiazolidinediones