Pharmacology

Question 1

6-mercaptopurine (6-MP)
6-thioguanine (6-TG)
Azathioprine (prodrug of 6-MP)

Answer 1

purine analogs

inhibit de novo purine synthesis

pathway 1:: activated by hypoxanthineguanine phosphoribosyl transferase (HGPRT) to make active metabolites resulting in purine synthesis inhibition (cytotoxic)

pathway 2: Allopurinol competitively inhibits Xanthine oxidase(XO) and thiopurine methyltransferase (TPMT) in the liver and preventing formation of inactive metabolites. Results in shunting to pathway 1 and increased activation

use: IBD and maintenance of cancer remission, organ rejection, RA, SLE, steroid weaning off

Question 2

Mycophenolate and ribavirin

Answer 2

inhibits inosine monophosphate dehydrogenase

IMP –x—> GMP

Question 3

Hydroxyurea

Answer 3

Inhibits ribonucleotide reductase in purine and pyrimidine synthesis in s phase

for myeloproliferative disorders and sickle cell (increased levels of HbF)

Question 4

Methotrexate (MTX), trimethoprim (TMP), Pyrimethamine

Answer 4

inhibits dihydrofolate reductase (decrease dTMP)

humans (methotrexate)
bacteria (trimethoprim)
protozoa(pyrimethamine)

Question 5

5-fluorouracil (5-FU)

Answer 5

prodrug: capecitabine

forms 5-F-dUMP which inhibits thymidylate synthase (decrease dTMP) and decreases DNA synthesis

cancer drug

AR:handfoot syndrome (palmarplantar erythrodysesthesia)

Question 6

allopurinol and febuxostat

Answer 6

Treatment for Lesch-Nyhan syndrome (HGPRT)

allopurinol which prevents hypoxanthine from becoming xanthine –> chronic gout tx

Or

febuxostat which prevents xanthine from becoming uric acid —> chronic gout tx

Question 7

Actinomycin D

Answer 7

inhibits RNA polymerase in both prokaryotes and eukaryotes

Question 8

Rifampin

Answer 8

inhibits DNA dependent RNA pol in prokaryotes

Question 9

Quabain

Answer 9

cardiac glycoside that inhibits Na-K ATPase by binding to K site

Question 10

digoxin and digitoxin

Answer 10

cardiac glycosides

inhibit the Na-K ATPase and indirect inhibition of Na/Ca exchange

increase in Ca concentrations

increased contractility

Question 11

lumacaftor and ivacaftor

Answer 11

lumacaftor - corrects misfolded proteins and transport to cell surface

ivacaftor- opens Cl- channels

for CF

Question 12

Fomepizole

Answer 12

FOMEpizole

inhibits alcohol dehydrogenase

For Overdose of Methanol or Ethylene Glycol

Question 13

Disulfiram

Answer 13

DIScourage drinking by causing hangover

inhibits acetaldehyde dehydrogenase

acetaldehyde accumulates

Question 14

Electron transport inhibitors

Answer 14

Directly inhibit electron transport

RotenONE inhibits complex I
Antimycin A inhibits complex III (an-THREE-mycin)
CyanIDE, carbon monoxIDE, axIDE (the “ides” –> 4 letters –> complex IV)

Question 15

ATP synthase inhibitors

Answer 15

oligomycin

increases proton gradient and no ATP produced

Question 16

Cyclosporine

Answer 16

immunosuppressant (Calcineurin inhibitor)

binds cyclophilin and blocks IL-2 transcription –> no T cell activation

use: prevent transplant rejection and inflammatory disorders

AR: metabolized by CYP 3A4 therefore avoid grapejuice, Highly NEPHROTOXIC, gingical hyperplasia, hirsutism

Question 17

Tacrolimus

Answer 17

immunosuppressant (calcineurin inhibitor)

binds FK506 binding protein

Blocking T cell activation by preventing IL-2 transcription

use: prevent transplant rejection and inflammatory disorders

AR: NEPHROTOXIC and increased risk of diabetes

Question 18

Sirolimus (Rapamycin)

Answer 18

Immunosuppressant and for kidney transplant rejection prophylaxis “kidney sir-vives”

AR: pancytopenia, not nephrotoxic

Question 19

Basiliximab

Answer 19

immunosuppresant and for kidney transplant rejection prophylaxis

Blocks IL-2R

AR: edema, tremor, HTN

Question 20

Azathioprine

Answer 20

Immunosuppresant

blocks lymphocyte proliferation by blocking nucleotide synthesis. “azathioPURINE”

degraded by xanthine oxidase

AR: panyctopenia

Question 21

Mycophenolate

Mofetil

Answer 21

immunisuppresant

For lupus nephritis

inhibits IMP dehydrogenase –> preventing purine synthesis

Less nephrotoxic and neurotoxic

AR: pancytopenia, HTN, hyperglycemia

Question 22

Glucocorticoids

Answer 22

immunosuppressant

Inhibits NFkB.

Decreasing transcription of many cytokines and induces T cell apoptosis

AR: cushings, osteoporosis, hyperglycemia, amenorrhea, peptic ulcers, psychosis, cataracts, avascular necrosis (femoral head).

Used to treat inflammation in graves opthalmopathy

Adrenal insufficiency may develop if drug is stopped abruptly after chronic use –> hypotension and shock

Question 23

Epoetin alfa (EPO analog)

Answer 23

Bome marrow stimulation
Erythropoietin

used for anemia

especially in renal failure

can cause an increased risk of thromboembolic events and hypertension

Question 24

Filgrastim (G-CSF)

Sargramostim (GM-CSF)

Answer 24

Bone marrow stimulation

Used for leukopenia

Question 25

Romiplostim | Eltrombopag

Answer 25

Bone marrow stimulation Romiplostim is a TPO analog Eltrombopag is a TPO receptor agonist "Pag=bag for TPO" Used for autoimmune thrombocytopenia

Question 26

Aldesleukoin

Answer 26

Immunotherapy of IL2 increases activity of T cells and NKC used for renal cell carcinoma and metastatic melanoma

Question 27

IFN-α

Answer 27

immunotherapy of interferon Used for chronic hep B and renal cell carcinoma

Question 28

IFN-β

Answer 28

immunotherapy of interferon used for multiple sclerosis

Question 29

IFNγ

Answer 29

immunotherapy of interferon used for chronic granulomatous disease

Question 30

Alemtuzumab

Answer 30

Therapeutic antibodies Targets CD52 Used for CLL (chronic lymphocytic leukemia) and MS think: aLYMtuzumab

Question 31

Bevacizumab

Answer 31

Therapeutic antibodies Targets VEGF to inhibit angiogenesis Used for colorectal cancer, renal cell carcinoma, non small cell lung cancer, treatment for wet age related macular degeneration

Question 32

Cetuximab

Answer 32

Therapeutic antibodes Targets EGFR --> decrease KRAS--> decreased cellular growth Used for stafe 4 colorectal cancer and head/neck cancer resistance due to mutation in KRAS that activates it

Question 33

Rituximab

Answer 33

Therapeutic antibodies Targets CD20 used for B cell non-hodgkin lymphoma, CLL, RA, ITP, multiple sclerosis AR: progressive multifocal leukoencephalopathy

Question 34

Trastuzumab

Answer 34

Therapeutic antibodies Targets HER2 Breast cancer and gastric cancer think HER2 -->tras2zumab

Question 35

Adalimumab Certolizumab Golimumab Infliximab

Answer 35

Autoimmune disease therapy anti TNF α ( key mediatory in inflammatory process by accelerating neutrophil migration, macrophage phagocytosis, lymphocyte proliferation, cytokine synthesis) Used for autoimmune disorders like IBD, RA, AS, psoriasis AR: TB risk and drug induced lupus

Question 36

Daclizumab

Answer 36

Autoimmune disease therapy Targets CD25 (part of IL-2 receptor) Used for relapsing MS

Question 37

Eculizumab

Answer 37

Autoimmune disease therapy Targets complement protein C5 Used for paroxysmal nocturnal hemoglobinuria

Question 38

Natalizumab

Answer 38

targets α4 integrin which is important for WBC adhesion USed for MS, crohns disease Risk of PML in patients with JC virus

Question 39

Ustekinumab

Answer 39

Targets IL12 and IL23 Used for psoriasis and psoriatic arthritis

Question 40

Abciximab

Answer 40

targets platelet glycoproteins IIb/IIIa used as an antiplatelet agent

Question 41

Denosumab

Answer 41

mimics osteoprotegerin and targets RANKL think DenOSumab affects OSteoclasts in OSteoporosis

Question 42

Digoxin immune Fab

Answer 42

Targets Digoxin antidote for digoxin toxicity ( yellow tinting seen on objects. REnally cleared with small therapeutic window therefore increasing age --> decreased renal function --> increased risk of digoxin toxicity high K+ is also a sign of digoxin toxicity

Question 43

Omalizumab

Answer 43

refractory allergic asthma thats not responding to inhaled steroids and long acting beta2agonists prevents IgE binding for FcERI

Question 44

Palivizumab

Answer 44

Monoclonal antibody directed against the fusion protein of RSV. prevents infection of the host cell used as RSV prophylaxis for high risk infants think PaliVIzumab - VIrus

Question 45

Penicillin

Answer 45

D-Ala-D-Ala structural analog binds penicilin binding proteins (covalently binds transpeptidase) and blocks crosslinking of peptidoglycan cell wall Used: Gram + organisms mostly, syphilis, spirochette AR:hemolytic anemia and intersitital nephritis

Question 46

Amoxicillin | Ampicillin

Answer 46

Aminopenicillins (amoxi is greater bioavailability) MOA: same as penicillin but wider spectrum. Combine with clavulanic acid to pretoect against β-lactamase destruction ("they are AMPed up penicillins) Used: Same as penicillin but wider spectrum AR: pseudomembranous colitis, rash, hypersensitivity Resistance: Penicillinase is a type of β-lactamase

Question 47

Dicloxacillin Nafcillin Oxacillin

Answer 47

Penicillinase-resistant penicillins MOA: bulky R group that blocks access of β-lactamase to β-lactam ring Use: S aureus "naf for saph" AR: hypersensitivity, interstitial nephritis note: beta lactamase function degrade penicillin and cephalosporins

Question 48

Piperacillin | Ticarcillin

Answer 48

Antipseudomonal penicillins

Question 49

β-lactamase inhibitors

Answer 49

CAST Clavulanic acid Avibactam Sulbactam Tazobactam

Question 50

Cephalosporins

Answer 50

MOA: β-lactam drugs that inhibit cell wall synthesis by irreversibly binding to penicillin binding proteins (i.e. transpeptidase) note: same as penicillins note: resistance forms by inhibiting the binding of ceftriaxone via changing the structure of the penicillin binding proteins

Question 51

First generation cephalosporins

Answer 51

Cefazolin - prior to surgery to prevent S aureus | Cephalexin

Question 52

2nd gen cephalosporins

Answer 52

Cefaclor Cefoxitin Cefuroxime Cefotetan

Question 53

3rd gen cephalosporins

Answer 53

Ceftriaxone Cefotaxime Cefpodoxime Ceftazdime ---> pseudomonas can cross BBB therefore use Ceftriaxone for meningitis, gonorrhea, dissemniated lyme disease note: add ampicillin when tx infant meningitis because if it is due to listeria then 3rd gen wont cover it due to it being intracellular

Question 54

Cefepime

Answer 54

4th gen cephalosporins gram (-) organisms with increased activity against pseudomonas and gram +

Question 55

Ceftaroline

Answer 55

5th gen cephalosporin Also covers Listeria, MRSA and enterococcus faecalis does NOT cover pseudomonas

Question 56

Doripenem Imipenem Meropenem Ertapenem

Answer 56

Carbapenems - beta lactamase inhibitors Imipenem is always given with cilastatin (an inhibitor of renal dehydropeptidase I) to decrease inactivation of drug in renal tubules Meropenem is decreased risk of seizures and is stable to dehydropeptidase I Use: LAST RESORT AR: seizures at high plasma levels

Question 57

Aztreonam

Answer 57

Monobactam MOA: Binds to penicillin binding protein 3 and prevents cross linking. Synergistic with animnoglycosides. Use: if pt allergic to penicillin, in pt with renal insufficiency and cant handle aminoglycosides

Question 58

Vancomycin

Answer 58

MOA: inhibits cell wall peptidoglycan formation by binding D-Ala-D-Ala use: Gram + only , serious multidrug resistant organisms (i.e. s epidermidis) AR: Nephrotoxicity, Ootoxicity, Thrombophlebitis, Diffuse flushing (Red man syndrome), eosinophilia and systemic symptoms (DRESS syndrome)

Question 59

``` Gentamicin Neomycin Amikacin Tobramycin Streptomycin ```

Answer 59

Aminoglycosides MOA: binding of the 30S subunit. requires O2 therefore ineffective against anaerobes. Also, pseudomonas is resistant by inactivating enzyme by acetylation or increasing efflux systems Use: severe gram (-) rod infections because cant penetrate the cell wall of gram +. Therefore if want to treat gram + too then use with penicillin or some cell wall inhibitor Neomycin for bowel surgery AR: Nephrotoxicity, Neuromuscular blockade, Ototoxicity, teratogen

Question 60

Tetracycline Doxycycline Minocycline

Answer 60

Tetracyclines MOA: bind to 30S and prevent attachment of aminoacyltRNA Note: Ca, antacids (Mg), Fe Use: Doxycycline is fecally eliminated and can be used for pt with renal failure . Accumulates intracellularly --> good for intracellular organisms. For Acne and MRSA AR: discoloration of teeth due to accumulation in dentin and enamel, inhibition of bone growth in children, photosensitivity, CONTRAINDICATED in pregnancy because crosses placenta

Question 61

Tigecycline

Answer 61

Glycylcycline MOA: Binds 30S use: broad spectrum, multiresistant, and infections that require deep tissue penetration AR: GI sx

Question 62

Chloramphenicol

Answer 62

Blocks peptidyltransferase at 50S ribosomal subunit use: Low cost but toxicity --> used in developing countries AR: anemia (dose dependent aka reversible), APLASTIC ANEMIA (dose independent aka irreversible), gray baby syndrome (lack liver UDP glucuronosyltransferase), leukopenia, thrombocytopenia

Question 63

Clindamycin

Answer 63

MOA: blocks 50S use: anaerobic infections ABOVE the diaphragm in aspiration pneumonia, lung abcsess, and oral infections. Also invasive group A strep AR: pseudomembranous colitis due to C diff

Question 64

Linezolid

Answer 64

Oxazolidinones MOA: binds to 50S subunit USe: Gram + species including MRSA and VRE AR: bone marrow suppression causes thrombocytopenia, peripheral neuropathy, SEROTONIN SYNDROME due to MAOI activity when used with SSRI

Question 65

Azithromycin Clarithromycin Erythromycin

Answer 65

Macrolides MOA: 23S rRNA of the 50S Use: atypical pneumonias, STIs, gram + cocci, pertussis AR: GI motility issues, prolonged QT interval, acute cholestatic hepatitis, eosinophilia.

Question 66

Colistin (polymyxin E), polymyxin B

Answer 66

MOA: cation polypeptides that bind to phospholipids and disrupt cell membrane integrity Use: salvage therapy for multidrug resistant gram - bacteria Polymyxin B is part of a triple antibotic ointment AR: nephrotoxicity, neurotoxicity, resp failure

Question 67

Sulfamethoxazole (SMX) Sulfisoxazole Sulfadiazine

Answer 67

Sulfonamides Inhibit dihydropteroate synthase in folate synthesis. AR: tubulointerstitial nephritis, stevens johnson syndrome, kernicterus in infants

Question 68

Dapsone

Answer 68

Similar to sulfonamides but structurally distint use: Leprosy and prophylaxis for pneumocystis jirovecii AR: hemolysis if G6PD deficient, methemoglobinemia

Question 69

Trimethoprim

Answer 69

Inhibits bacterial dihydrofolate reductase Used with sulfonamides to cause block of folate synthesis. AR: Bone marrow effects like megaloblastic anemia, Leukopenia, granulocytopenia --> use folinic acid to avoid these

Question 70

Ciprofloxacin Enoxacin Norfloxacin Ofloxacin Respiratory: gemifloxacin Levofloxacin moxifloxacin

Answer 70

Fluoroquinolones MOA: inhibit topo II (DNA gyrase) and topo IV. DO NOT take with antacids AR: contraindicated in pregnant women, nursing mothers, and children <18 yo due to possible damage to cartilage. May cause tendonitis or tendon rupture in people >60 yo and in patients taking prednisone.

Question 71

Daptomycin

Answer 71

MOA: disrupts cell membranes of gram + cocci by creating transmembrane channels causing intracellular ion leakage leading to cell death Use: MRSA, bacteremia, endocarditis, VRE AR: myopathy and rhabdomyolysis note: cant use for pneumo because inactivated by surfactant

Question 72

Metronidazole

Answer 72

MOA: forms toxic free radical metabolites that damage DNA Use: treats anaerobic infections BELOW the diaphragm. Can be used to replace amoxicillin for tx of H pylori if penicillin allergy. Bacterial vaginosis and trichomoniasis. GIARDIA AR: severe flushing, metallic taste. disulfiram like reaction shrotly after ethanol consumption

Question 73

Rifampin | Rifabutin

Answer 73

Rifamycins MOA: Inhibits DNA dependent RNA pol Use: TB, leprosy (use with dapsone to delay resistnace), meningococcal prophylaxis, chemoprophylaxis if in contact with kids with H influenza type b AR: hepatotoxicity, red/orange body fluids, rapid resistance if used alone Resistance: rapid resistance if monotherapy

Question 74

Isoniazid

Answer 74

MOA: decrease synthesis of mycolic acid Use: mycobacterium tuberculosis AR: hepatotoxicity, p450 inhibition, drug induced SLE, anion gap metabolic acidosis, can cause sideroblastic anemia due to B6 synthesis def NOTE: administer vitamin B6 with it because deficiency can cause peripheral neuropathy and sideroblastic anemia.

Question 75

Pyrazinamide

Answer 75

prodrug of pyrazinoic acid Works best at acidic pH Use for mycobacterium tuberculosis AR: hyperuricemia, hepatotoxicity

Question 76

Ethambutol

Answer 76

MOA: decrease carb polymerization of mycobacterium cell wall by blocking arabinosyltransferase use for mycobacterium tuberculosis AR: optic neuropathy (red green colorblind). think "eyethambutol"

Question 77

Streptomycin

Answer 77

MOA: interferes with 30S component of ribsosome use: mycobacterium tuberculosis (2nd line) AR: tinnitus, vertigo, ataxia, nephrotoxicity

Question 78

Prophylaxis for high risk of endocarditis and undergoing surgical or dental procedures

Answer 78

amoxicillin

Question 79

Prophylaxis for exposure to gonorrhea

Answer 79

Ceftriaxone also give doxycycline and macrolides (azithromycin and eryhtromycin for chlamydia co infection)

Question 80

Prophylaxis for history of recurrent UTIs

Answer 80

TMP-SMX

Question 81

Prophylaxis for exposure to meningococcal infection

Answer 81

ceftriaxone, ciprofloxacin, or rifampin

Question 82

Prophylaxis for women carrying group B strep

Answer 82

intrapartum penicillin G or ampicillin

Question 83

Prophylaxis for prevention of gonococcal conjunctivitis in newborn

Answer 83

Erythromycin ointment on eyes

Question 84

Prophylaxis for prevention of postsurgical infection due to S aureus

Answer 84

Cefazolin

Question 85

Prophylaxis for strep pharyngitis in child with prior rheumatic fever

Answer 85

Benzathine penicillin G or oral penicillin V

Question 86

Prophylaxis for exposure to syphilis

Answer 86

Benzathine penicillin G

Question 87

Prophylaxis for HIV patients <200

Answer 87

TMP-SMX for pneumocystis pneumonia

Question 88

Prophylaxis for HIV patients <100

Answer 88

TMP-SMX for pneumocystis and toxoplasmosis

Question 89

Prophylaxis for HIV patient <50

Answer 89

Azithromycin or clarithromycin for mycobacterium avium complex

Question 90

Amphotericin B

Answer 90

MOA: bind ergosterol think B=binds to and " amphoTEARicin "Tears" holes into fungal membrane" "tears holes into kidney becuase nephrotoxic and allows changes in MG AND K (SIDE EFFECT)" AR: Fever/chills, NEPHROTOXICITY due to vasoconstriction (supplement with K+ and Mg2+ and hydrate) --> hypokalemia and arythmias

Question 91

Nystatin

Answer 91

Same as amphotericin B. Topical only because too toxic for systemic use use: swish and swallow for thrush. topical for diaper rash and vaginal candidiasis

Question 92

Flucytosine

Answer 92

MOA: inhibits DNA and RNA biosynthesis by conversion to 5-fluorouracil by cytosine deaminase use: systemic fungal infetions in combination with ampho B (cryptococcal) AR: bone marrow suppression

Question 93

``` Clotrimazole Fluconazole Isavuconazole Itraconazole Ketoconazole Miconazole Voriconazole ```

Answer 93

Azoles inhibiting conversion of lanosterol to ergosterol use: local and serious systemic mycoses. Fluconazole - cryptococcal meningiis in AIDS patients and candidal infections of all types AR: testosterone synthesis inhibition (gynecomastia, ESPECIALLY with ketoconazole)

Question 94

Terbinafine

Answer 94

MOA: inhibits the fungal enzyme squalene epoxidase use: dermatophytes, especially onychomycosis AR: GI, headache, hepatotoxicity, taste disturbance

Question 95

Anidulafungin Caspofungin micafungin

Answer 95

Echinocandins MOA: inhibit cell wall synthesis by inhibiting synthesis of beta glucan (major cellw all component is 1,3-BEta, D-glucan) Use: invasive aspergillosis, candida AR: GI upset, flushing (by histamine release)

Question 96

Griseofulvin

Answer 96

MOA: interferes with microtubule function in keratin Use: oral treatment of superficial infections. inhibits growth of dermatophytes Adverse effects: teratogen, carcinogenic, icnrease cytochrom P450 and warfarin metabolism

Question 97

Pyrimethamine

Answer 97

toxoplasmosis

Question 98

Suramin | Melarsoprol

Answer 98

trypanosoma brucei

Question 99

Nifurtimox

Answer 99

T cruzi

Question 100

Sodium stibogluconate

Answer 100

leishmaniasis

Question 101

Anti mite therapy used to tx scabies and mites

Answer 101

Permethrin- Inhibits Na channel deactivation --> neuronal membrane depolarization Malathion- (acetylcholinesterase inhibitor) Lindane- (blocks GABA channels --> neurotoxicity)

Question 102

Chloroquine

Answer 102

MOA: blocks detoxification of heme into hemozoin. Heme accumulates and is toxic to plasmodia P falciparum is resistant ( due to membrane pump that has decreased intracellular concentration of drug) AR: retinopathy, pruritis especially in dark skinner people

Question 103

Oseltamivir (tamiflu) | Zanamivir

Answer 103

MOA: sialic acid analog. Inhibit influenza A and B neuraminidase which decreases release of progeny virus (aggregates on host cell surface) Beginning therapy within 48 hours Why? normally newly formed virus particles initially remain attached to cells and respiratory tract mucins through hemagglutinin binding of glycoconjugate receptors. Neuraminidase cleaves the terminal sialic acid residues on these receptors and allows the release of attached virions and subsequent spread. Inhibition of neuraminidases prevents this

Question 104

Acyclovir Famciclovir Valacyclovir (prodrug of acyclovir, more bioavailable)

Answer 104

MOA: guanosine analogs. Monophosphorylated by HSV/VSV thymidine kinase and not phosphorylated in uninfected cells --> few adverse effects. Preferentially inhibits viral DNA pol by incorporating into replicating viral DNA chain chain termination AR: obstructive crystalline nephropathy and acute renal failure if not adequately hydrated

Question 105

Ganciclovir

Answer 105

Guanosine analog. 5'-monophosphate formed by a CMV viral kinase. first line for CMV colitis Triphosphate formed by cellular kinases that interferes with human host cell DNA synthesis Prferentially inhibits viral DNA polymerase AR: neutropenia. if combined with TMP-SMX will cause bone marrow suppression (TMP SMX inhibits tetrahydrofolic acid production)

Question 106

Foscarnet

Answer 106

Viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor. Binds to pyrophosphate-binding site of enzyme. Does not require any kinase activation think FOScarnet=pyroFOSphate analog use: CMV retinitis or colitis when ganciclovir fails or acyclovir resistant HSV AR: nephrotoxic and electrolyte abnormalities can lead to seizures due to chelation (hypomagnesia and hypocalcium )

Question 107

Cidofovir

Answer 107

MOA: preferentially inhibits viral DNA polymerase. Does not require phosphorylation by viral kinase use: CMV retinitis in immunocompromised patients; acyclovir resistant HSV AR: nephrotoxicity

Question 108

HAART therapy

Answer 108

Highly active antiretroviral therapy (HAART) in HIV 3 drug regimen: 2 NRTIs and a integrase inhibitor resistance in pol gene over time (resistance to protease inhibitors and transcriptase inhibitors)

Question 109

``` Abacavir (ABC) Didanosine (ddl) Emtricitabine (FTC) Lamivudine (3TC) Stavudine (d4T) Tenofovir (TDF) Zidovudine (ZDV) ```

Answer 109

HIV - need to be phosphorylated to be active nucleoside reverse transcriptase inhibitor which inhibitsvnucleotide binding and terminate the SNA chain (lack 3'OH) all are nucleosides EXCEPT Tenofovir (think nucleoTide) AR: bone marrow suppression, peripheral neuropathy, lactic acidosis due to nucleosides, anemia with ZDV, pancreatitis with ddl ABC contraindicated in HLA B5701 mutation pt because of increase hypersensitivity risk

Question 110

Delavirdine Efavirenz Nevirapine

Answer 110

for HIV Bind to reverse transcriptase at site different from NRTIs. Does not require phosphorylation AR: rash and hepatotoxicity are common. Efavirenz causes vivid dreams and other CNS symptoms. Delavirdine and efavirenz are contraindicated in pregnancy

Question 111

``` Atazanavir Darunavir Fosamprenavir Indinavir Lopinavir Ritonavir Saquinavir ```

Answer 111

-navir = protease inhibitros which prevent maturation of new viruses by preventing cleavage of the polypeptide products of HIV mRNA into fxional parts Ritonavir boost other drug concentrations by inhibiting cytochrome P450 AR: hyperglycemia due to insulin resistance, GI, lipodystrophy (chusing like syndrome and fat redistribution), nephropathy, hematuria, thrombocytopenia (indinavir),

Question 112

Dolutegravir Elvitegravir Raltegravir

Answer 112

-tegravir = integrase inhibitors Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase AR: increase in creatine kinase

Question 113

Enfuvirtide

Answer 113

fusion inhibitor for HIV binds gp41 and inhibits viral entry think enFUvirtide inhibits FUsion note: gp120 exoses underlying glycoprotein gp41 which mediates fusion

Question 114

Maraviroc

Answer 114

fusion inhibitor for HIV Binds CCR-5 (chemokine receptor on surface of T cells/monocytes to inhibit interaction with gp 120 think MaravirOC inhibits dOCking

Question 115

Interferons

Answer 115

Interferons for HIV tx MOA: glycoproteins normally synthesized by virus infected cells, exhibiting a wide range of antiviral and antitumoral properties use: chronic HBV, HCV, kaposi sarcoma, hairy cell leukemia, condyloma cuminatum, renal cell carcinoma, malignant melanoma, MS, CGD Adverse effects: flu like, depression, neutropenia, myopathy

Question 116

HCV is treated via monotherapy or polytherapy?

Answer 116

polytherapy!

Question 117

Ledipasvir

Answer 117

TX for HCV viral phosphoprotein (NS5A) inhibitor NS5A plays important role in replication

Question 118

Ribavirin

Answer 118

TX for HCV and RSV interferes with the duplication of viral genetic material inhibits synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate dehydrogenase AR: hemolytic anemia and severe teratogen

Question 119

Simeprevir

Answer 119

HCV protease (NS3/4A); prevents viral replciation photosensitiviy reactions

Question 120

Sofosbuvir

Answer 120

inhibits HCV RNA dependent RNA polymerase (NS5B) acting as a chain terminator

Question 121

Antibiotics to avoid in pregnancy: ``` Sulfonamides Aminoglycosides Fluoroquinolones Clarithromycin Tetracyclines Ribavirin Griseofulvin chloramphenicol ```

Answer 121

``` Sulfonamides --> kernicterus Aminoglycosides --> ototoxicity Fluoroquinolones --> cartilage damage Clarithromycin --> embryotoxic Tetracyclines --> discolored teeth, inhibition of bone growth Ribavirin- teratogen Griseofulvin-teratogenic chloramphenicol - gray baby syndrome ```

Question 122

Sympathetic G protein linked second messengers ``` alpha1 alpha2 beta1 beta2 beta3 ```

Answer 122

alpha1 (q) --> vasoconstriction, mydriasis/dilation, sphincter mm contaction alpha2 (i) --> decrease sympathetic (adrenergic) outflow, decrease insulin, lipolysis etc beta1 (s) --> 1 heart (increased contractility) beta2(s) --> 2 lungs ( bronchodilation etc) beta3 (s) -->thermogenesis in skeletal mm and bladder relaxation "qisss"

Question 123

Parasympathetic G protein linked second messengers M1 M2 M3

Answer 123

M1 (q) --> higher cognition and enteric NS M2 (i) --> decrease HR and contractility M3 (q) --> increase exocrine, gut peristalsis, bladder cotnraction, bronchoconstriction etc

Question 124

Dopamine G protein linked second messengers D1 D2

Answer 124

D1 (s) --> relaxes renal vascular smooth mm | D2 (i) --> modulates NT release in brain

Question 125

Histamine G protein linked second messengers H1 H2

Answer 125

H1 (q) --> nasal and bronchial mucus production, pruritis etc. H2 (s) --> increase gastric acid secretion

Question 126

Vasopressin G protein linked second messengers V1 V2

Answer 126

V1 (q) --> increase vascular smooth mm contraction | V2(s) --> aquaporin2

Question 127

Gq

Answer 127

--> phospholipase C--> eventually protein kinase C --> increases [Ca] --> smooth mm contraction

Question 128

Gs and Gi

Answer 128

Gs --> + adenylyl cyclase --> ATP becomes cAMP --> protein Kinase A --> increase [Ca] in heart and inhibits myosin light chain kinase (smooth mm) Gi --> (-) adenylyl cyclase

Question 129

Amphetamine MOA

Answer 129

They use Noradrenergic nerve endings 1) use NE transporter to enter presynaptic terminal 2) use vesicular monoamine transporter (VMA) to enter neurosecretory vesicles 3) NE displaced from vesicle 4) presynaptic threshold 5) expelled 6) drug effects

Question 130

Cholinomimetic agents

Answer 130

enhance the PNS watch for exacerbations of COPD, asthma, and peptic ulcers in susceptible patients

Question 131

Bethanechol

Answer 131

Direct agonists (cholinomimetic agents) activates bowel and bladder smooth mm resistant to AChE

Question 132

Carbachol

Answer 132

Direct agonists (cholinomimetic agents) carbon copy of acetylcholine but resistant to AChE Use for contricting pupil and relieving intraocular pressure in open angle glaucoma

Question 133

Methacholine

Answer 133

Direct agonists (cholinomimetic agents) stimulate muscarinic receptors in airway for dx of asthma (methacholine challenge beacause it constricts the bronchioles and increases mucus productions --> further illicit asthma smyptoms) good for patients with asthma signs but normal spirometery test

Question 134

Pilocarpine

Answer 134

Direct agonists (cholinomimetic agents) potent stimulator of swear, tears, and saliva Resistant to AChE and crosses BBB open angle (Contracts ciliary mm of eye) and (Contracts pupillary sphincter) closed angle glaucoma, xerostomia (sjogren syndrome)

Question 135

Donepezil Rivastigmine Galantamine

Answer 135

Indirect agonists (anticholinesterases) increases ACh used for alzheimers dz

Question 136

Endrophonium

Answer 136

``` Indirect agonists (anticholinesterases) increase ACh ``` in past it was used to dx myasthenia gravis

Question 137

Neostigmine

Answer 137

``` Indirect agonists (anticholinesterases) increase ACh ``` "neo" think No CNS penetration used for myasthenia gravis, or NMJ blockade etc

Question 138

Physostigmine

Answer 138

``` Indirect agonists (anticholinesterases) increase ACh ``` think phreely crosses BBB (only one that penetrates CNS and PNS) antidote for anticholinergic toxicity from atropine overdose

Question 139

Pyridostigmine

Answer 139

``` Indirect agonists (anticholinesterases) increase ACh ``` increases mm strength think pyRIDostiGMine - gets RID of Myasthenia Gravis does not penetrate CNS

Question 140

Cholinesterase inhibitor poisoning

Answer 140

usually due to organophosphates which irreversibly inhibit AChE. Antidote is atropine a competitive inhibitor +pralidoxime which regenerates AChE if given early atropine does not address the nicotinic effects of (mm weakness, paralysis, fluctuations) therefore must add pralidoxime

Question 141

Atropine Homatropine Tropicamide

Answer 141

Muscarinic agents eye mydriasis and cycloplegia Atropine is a competitive muscarinic receptor antagonist that opposes the effects of acetylcholine resulting in decreased muscle contraction intensity

Question 142

Benztropine | Trihexyphenidyl

Answer 142

Muscarinic agents CNS parkinsons dz and acute dystonia related to antipsychotics "park my benz"

Question 143

Glycopyrrolate

Answer 143

Muscarinic agents GI and resp preop to reduce airway secretions

Question 144

Hyoscyamine | Dicyclomine

Answer 144

Muscarinic agents GI antispasmodics for IBS

Question 145

Ipratropium | tiotropium

Answer 145

Muscarinic agents Resp COPD, asthma "I pray to breathe soon"

Question 146

Oxybutynin Solifenacin Tolterodine

Answer 146

Muscarinic agents GI reduce bladder spasms and urge urinary incontinence

Question 147

Scopolamine

Answer 147

Muscarinic agents CNS motion sickness

Question 148

Atropine

Answer 148

Muscarinic antagonist (blocks M2) increase in HR without affecting BP used to tx bradycardia by decreasing vagal influence on AV and SA node and for ophthalmic applications risk of glaucoma due to increased intraocular pressure and angle closure blocks DUMBBELSS AR: hot as a hare, Dry as a bone, red as a beet, blind as a bat, mad as a hatter, full as a flask. Can cause acute angle closure glaucoma in elderly due to mydriasis. Urinary retention in men with prostatic hyperplasia

Question 149

Albuterol Salmeterol Terbutaline

Answer 149

Sympathomimetics with B2>B1 Albuterol --> acute asthma or COPD Salmeterol --> long term asthma or COPD Terbutaline --> acute bronchospasm in asthma and tocolysis

Question 150

Dobutamine

Answer 150

Sympathomimetics with B1>B2 and alpha HF, cardiogenic shock, cardiac stress testing

Question 151

Dopamine

Answer 151

Sympathomimetic with D1=D2>B>A unstable bradycardia, HF, shock Alpha effects at high doses Beta effects at low doses

Question 152

Epinephrine

Answer 152

Sympathomimetics B>A anaphylaxis, asthma, open angle glaucoma, alpha effects predominate at high doses AR: limits insulin use by insulin sensitive tissues and stimulates hepatic glycogenolysis and gluconeogenesis (like glucagon)

Question 153

Isoproterenol

Answer 153

Sympathomimetics Beta1=Beta2 eval of tachyarrhythmias. worsens ischemia

Question 154

Midodrine

Answer 154

Sympathomimetics alpha1 autonomic insufficiency and postural HTN

Question 155

Mirabegron

Answer 155

Sympathomimetics Beta3 urinary urge incontinence or overactive bladder "Mira begs ron" to get out of the bathroom"

Question 156

Norepinephrine

Answer 156

Sympathomimetics alpha1>alpha2>Beta1 Hypotension and septic shock reflex bradycardia

Question 157

Phenylephrine

Answer 157

Sympathomimetics alpha1>alpha2 hypotension (vasoconstrictor), ocular procedures because mydriatic, rhinitis (decongestant), ischemic priapism

Question 158

Amphetamine

Answer 158

indirect Sympathomimetics indirect general agonist, reuptake inhib, releases stored catecholamines good for ADHD, narcolepsy, obesity

Question 159

Cocaine

Answer 159

indirect Sympathomimetics indirect general agonist, reuptake inhib vasodilation and local anesthesia dont give beta blocks with it because can lead to unopposed alpha1 activation which can cause extreme HTN and coronary vasospasm

Question 160

Ephedrine

Answer 160

indirect Sympathomimetics indirect general agonist and releases stored catecholamines for nasal decongestion (pseudoephedrine), urinary incontinence, hypotension

Question 161

Clonidine | Guanfacine

Answer 161

Sympatholytics (alpha2 agonists) used for hypertensive emergency, ADHD, Tourette syndrome, opioid withdrawal AR: CNS depression, bradycardia, hypotension, resp depression, miosis, rebound hypertension with abrupt cessation

Question 162

alpha-methyldopa

Answer 162

Sympatholytics (alpha2 agonists) first line for HTN in pregnancy AR: direct coombs + hemolysis, drug induced lupus

Question 163

Tizanidine

Answer 163

Sympatholytics (alpha2 agonists) Relief of spasticity, especially in MS "TICanadine" AR: Hypotension, weakness, xerostomia

Question 164

Phenoxybenzamine

Answer 164

Nonselective alpha blocker Irreversible. Used for pheochromocytoma (preop) to prevent catecholamine (Hypertensive) crisis AR: ortho hypotension and reflex tachy

Question 165

Phentolamine

Answer 165

Nonselective alpha blocker Used for epinephrine reversal Reversible. Give to pt on MAO inhibitors who eat tyramine containing foods and for severe cocaine induced HTN AR: ortho hypotension and reflex tachy

Question 166

Prazosin Terazosin Doxazosin Tamsulosin

Answer 166

alpha1 selective antagonist "osin" decreases arteriole and venous resistance and decreases the tone of urinary sphincters. used for urinary sx of BPH Prazosin can be used for PTSD Hypertension except for tamsulosin AR: ORTHOSTATIC HYPOTENSION and vertigo. "first dose" syncope

Question 167

Mirtazapine

Answer 167

alpha 2 selective antagonist, potent 5HT2 and 5HT3 receptor antagonist and H1 antagonist used for depression (atypical antidepressant) AR: increased serum cholesterol, increased appetite, weight gain, dry mouth

Question 168

``` Acebutolol Atenolol Betaxolol Bisoprolol Carvedilol Esmolol Labetalol metoprolol Nadolol Nebivolol pindolol propanolol timolol ```

Answer 168

Beta blockers decrease HR and contractility and ultimately O2 consumption -Timolol - Glaucoma to decrease aq humor production -Propanolol for symptom control of Hyperthyroidism used for HTN by decreasing CO and DECREASES RENIN SECRETION - Metoprolol and esmolol for supraventricular tachycardia by decreasing AV conduction velocity (class II antiarrhythic) - Nadolol, propranolol, carvedilol for variceal bleeding by decreasing hepative venous pressure gradient and portal HTN also for hypertrophic cardiomyopathy (decrease HR, increase fill time, relieve obstruction) and for decreasing mortality from MI AR: erectile dysfunction, brady, AV block, HF, seizures, sleep problems, dyslipidemia (metoprolol), and asthma/COPD exacerbation. HYPOGLYCEMIA because hides signs and symptoms that blood sugar is low (palpitations, tremor)

Question 169

B1 selective blockers

Answer 169

think 1st half of the alphabet (all the ones that are A to M) . With the exception of carvedilol and labetalol acebutolol(partial),atenolol, betaxolol,bisoprolol,esmolol,metoprolol

Question 170

Nonselective blockers

Answer 170

think 2nd half of the alphabet (N to Z) B1=B2 nadolol,pindolol (partial), propranolol, timolol

Question 171

Nonselective alpha and B antagonists

Answer 171

Have a different suffix of "-ilol and alol" carvedilol labetalol

Question 172

This beta blocker combines B1 adrenergic blockade with stimulation of B3 receptors

Answer 172

Nebivolol increases NO activates NO synthase in the vasculature and decreases systemic vascular resistance

Question 173

Drugs to avoid according to the beers criteria

Answer 173

alpha blockers due to increased risk of hypotension anticholinergics, antidepressants, antihistamine, opiods Benzodiazepines NSAIDs PPIs (increased risk of c diff

Question 174

Treatment for HTN with DM

Answer 174

ACEi and ARBs are protective against diabetic nephropathy

Question 175

Treatment for HTN with asthma

Answer 175

ARBs CA channel blcokers Thiazide diuretics selective Beta blockers (avoid nonselective to prevent B2 receptor induced bronchocontriction) avoid ACEi to prevent confusion between drug or asthma related cough

Question 176

Treatment for HTN in pregnancy

Answer 176

Hydralazine Labetalol Methyldopa Nifedipine

Question 177

``` Amlodipine Clevidipine Nicardipine Nifedipine Nimodipine Diltiazem Verapamil ``` note: dihydropyridines act on arterial smooth mm and are nifedipine, amlodipine, felodipine note: nondihydropyridines affect the myocardium and are verapamil and diltiazem

Answer 177

"-dipine" Block voltage dependent L type calcium channels of cardiac and smooth mm nimodipine (dihydropyridine that acts on vascular smooth mm) --> subarachnoid hemorrhage by preventing cerebral vasospasm. All other dihydropyridines are for HTN, angina, raynauds Verapamil (nondihydropyridines that act on the heart, think V=Ventricles) --> HTN, angina, a fib/flutter amlodipine and nifedipine best for vascular smooth muscle but cause PERIPHERAL EDEMA Nicardipine and clevidipine is used fot HRN urgency and emergency

Question 178

Hydralazine

Answer 178

MOA: increase cGMP --> smooth mm relaxation which vasodilates arterioles > veins. Afterload reduction

Question 179

Treatment of hypertensive emergency

Answer 179

``` Clevidipine fenoldopam labetalol nicardipine nitroprusside ```

Question 180

Nitroprusside

Answer 180

short acting increases cGMP via direct release of NO. Can release and cause cynaide toxicity

Question 181

Fenoldopam

Answer 181

Dopamin D1 receptor agonist - coronary, peripheral, renal, and splanchnic vasodilation decrease BP and increase natriuresis use post op as antihypertensive

Question 182

Nitroglycerin Isosorbide dinitrate Isosorbide mononitrate

Answer 182

Nitrates vasodilate by increasing NO in vascular smooth mm --> increase in cGMP and smooth mm relaxation Dilates veins >>>arteries and decreases preload use: angina, acute coronary syndrome, pulmonary edema AR: reflex tachy that can be prevented with beta blockers, tolerance can develop, severe headaches, cutaneous flushing, hypotension contraindicated in right ventricular infarction (due to reduced preload and CO), hypertrophic cardiomyopathy (due to increased outflow tract obstruction), and those on PDE inhibitors (synergy causes increase in risk of severe hypotension)

Question 183

Ranolazine

Answer 183

inhibits the late phase of sodium current thereby reducing diastolic wall tension and oxygen consumption. No effect on HR or contractility use: angina refractory to other medical therapies AR: QT prolongation

Question 184

Milrinone

Answer 184

MOA: selective PDE3 inhibitor. In cardiomyocytes: Increase cAMP-->increase Ca influx --> increase inotrophy and chronotropy in vascular smooth mm: Increase cAMP --> inhibition of MLCK activity --> general vasodilation used for short term in acute decompensated HF AR: arrhythmias, hypotension

Question 185

Lovastatin | Pravastatin

Answer 185

HMG-CoA reductase inhibitors that increases HDL but decreases TGs and LDL MOA: inhibit conversion of HMG-CoA to mevalonate a cholesterol precursor. This results in upregulation of LDL receptors to increase uptake of circulatin LDL AR: hepatotoxicity and myopathy(serum creatinine kinase 10xnormal limit). If used with erythromycin there is inhibition of CYP 3A4 and will result in acute renal failure

Question 186

Cholestyramine Colestipol Colesevelam

Answer 186

Bile acid resins that prevent intestinal reabsorption of bile acids; liver must use cholesterol to make more. Decreases LDL, increases HDL, increases TG (hypertriglyceridemia) AR: decreases absorption of drugs and fat soluble vitamins

Question 187

Ezetimibe

Answer 187

prevents cholesterol absorption at small intestine brush border Decreases LDL, increases or nothing for HDL, Decreases or nothing for TG

Question 188

Gemfibrozil Bezafibrate Fenofibrate

Answer 188

Fibrates Decreased hepatic VLDL production and upregulate LPL --> increase TG clearance Activates PPAR alpha to induce HDL synthesis AR: MYOPATHY WHEN USED WITH STATINS, cholesterol gallstones due to inhibition of cholesterol 7alpha-hydroxylase

Question 189

Niacin (B3)

Answer 189

MOA: inhibits lipolysis (hormone sensitive lipase) in adipose tissue; reduces hepatic VLDL synthesis and TGs AR: red flushed face, hyperglycemia, hepatotoxic, hyperuricemia(acute flare of gouty arthritis) due to decreased renal excretion of uric acid

Question 190

Alirocumab | Evolocumab

Answer 190

PCSK9 inhibitors MOA: inactivation of LDL receptor degradation, increasing amount of LDL removed from bloodstream AR: myalgias, delirium, dementia, other neurocognitive effects

Question 191

digoxin

Answer 191

Cardiac glycosides MOA: direct inhibition of Na/K ATPase (decreased Na efflux)--> indirect inhibition of Na/Ca exchanger (decreased Ca efflux)--> increase Ca concentrations --> positive inotropy. It also stimulates vagus neve --> decrease in HR Use: Increase contractility in HF, decrease conduction in AV node and also depress SA node for a fib. Can be used for a fib AR: cholinergics side effects, hyperkalemia (poor prognosis), life threatening cardiac dysrhythmia note: patients with hypokalemia have higher risk of toxicity because available spots on Na/K ATPase for digoxin to bind ( classic drug interaction between digozin and loop diuretics) antidote: normalize K+ and give anti-digoxin Fab fragments, Mg

Question 192

Class I antiarrhythmics

Answer 192

slow or block conduction (esp in depolarized cells) decrease phase 0 slope selectively depress tissues that are frequently depolarized

Question 193

Class IA antiarrhythmics

Answer 193

Quinidine Procainamide Disopyramide Increase AP duration, effective refractory period, QT interval Used for atrial and ventricular arrhythmias AR: chinchonism (headache,tinnitus with quinidine), reversible SLE like syndrome with procainamide, HF with disopyramide. Thrombocytopenia and torsades

Question 194

Lidocaine | Mexiletine

Answer 194

Class IB antiarrhythmics (can include phenytoin) Decrease AP duration. Prefers depolarized or ischemic tissue, has little effect on normal cardiac tissue Used for post MI acute V arrhythmias and digitalis induced arrhythmias AR: CNS stimulation/depression, CV depression

Question 195

Flecainide | Propafenone

Answer 195

Class IC antiarrhythmics MOA: prolongs ERP in AV node and accessory bypass tracts ONLY Use: SVT, a fib, last resort for refractory VT AR: proarrhythmic, contraindicated post-MI and structural or ischemic heart disease

Question 196

``` Metoprolol Propranolol Esmolol (very short acting) Atenolol Timolol Carvedilol ``` note: b1 is in renal and cardiac but not smooth mmemes

Answer 196

Antiarrhythmics - (class II) - Beta blockers MOA: decrease SA and AV nodal activity by decreasing cAMP, Ca currents. Decreases slope of phase 4 Use: SVT, Ventricular rate control for a fib and a flutter AR: impotence, COPD and asthma exacerbation, sedation, may mask signs of hypoglycemia. Metoprolol can cause dyslipidemia Propranolol can exacerbate vasospasm in prinzmetal angina Beta blockers can cause unopposed alpha1 agonism if given alone for pheochromocytoma or cocaine toxicity

Question 197

Amiodarone Ibutilide Dofetilide Sotalol

Answer 197

Antiarrhythmics - potassium channel blockers (Class III) MOA: increase AP duration, ERP, QT interval Use: A fib, a flutter and ventricular tachy (amiodarone and sotalol). spells AIDS AR: - Sotalol: torsades, excessive beta blockade - Ibutilide: torsades

Question 198

Verapamil | Diltiazem

Answer 198

Antiarrhythmics - calcium channel blockers (class IV) MOA: decrease conduction velocity, increase ERP, increase PR interval use: prevent nodal arrhythmias and rate control in a fib AR: flushing, PERIPHERAL EDEMA, HF, av block (negative chronotropic effect), sinus node depression, COSTIPATION, worsening Congestive HF in patients wiht reduced LV function due to negative inotropic effect

Question 199

Adenosine

Answer 199

increase K+ out of cell which hyperpolarizes cell and decreases Ica --> decreases AV node conduction for SVT/paroxysmal supraventricular tachycardia very short acting. Theophylline and caffeine are adenosine receptor antagonists AR: flushing, hypotension, chest pain, sense of impending doom, bronchospasm. CORONARY STEAL

Question 200

Ivabradine

Answer 200

MOA: selective inhibition of funny sodium channels (If), prolonging slow depolarization (phase 4) decreases SA node firing; negative chronotropic effect without inotropy. Reduces cardiac O2 requirement Use: chronic stable angina in pt who cant take beta blockers and for chronic HF with reduced EF AR: luminous phenomena/visual brightness, HTN, bradycardia

Question 201

What do you give for torsades and digoxin toxicity

Answer 201

Mg 2+

Question 202

What is first line drug for DM type 2

Answer 202

metformin

Question 203

What type of insulin is preferred for DKA, hyperkalemia, stress hyperglycemia

Answer 203

Regular short acting insulin

Question 204

Rapid acting insulin

Answer 204

1 hr peak lispro aspart glulisine there is no "LAG"

Question 205

Short acting insulin

Answer 205

2 -3 hr peak regular

Question 206

intermediate acting insulin

Answer 206

4-10 hr peak NPH

Question 207

Long acting insulin

Answer 207

No real peak detemir glargine

Question 208

Pramlintide

Answer 208

amylin analog decreases glucagon release, gastric emptying increases satiety For DM management

Question 209

Exenatide | Liraglutide

Answer 209

GLP 1 analogs decrease glucagon release, gastric emptying increase glucose dependent insulin release and satiety AR: pancreatitis commonly used to lose weight "my ex lira lost weight" For DM management

Question 210

Metformin

Answer 210

Biguanides inhibits mGPD to prevent hepatic gluconeogenesis and the action of glucagon. It increases glycolysis and peipheral glucose uptake AR: lactic acidosis (caution in renal insufficiency), B12 deficiecny promotes weight loss! For DM management

Question 211

Chlorpropamide | Tolbutamide

Answer 211

first generation sulfonylureas close K+ channel in pancreatic beta cell membrane --> depolarization --> ca influx --> insulin release For DM management AR: hypoglycemia (increased risk with renal failure), weight gain, disulfiram like effects

Question 212

Glimepiride Glipizide Glyburide

Answer 212

Second geneation sulfonylureas close K+ channel in pancreatic beta cell membrane --> depolarization --> ca influx --> insulin release AR: hypoglycemia (increased risk with renal failure) in the elderly, weight gain For DM management

Question 213

Nateglinide | Repaglinide

Answer 213

Meglitinides close K+ channel in pancreatic beta cell membrane --> depolarization --> ca influx --> insulin release BUT DIFFERENT BINDING SITE FROM SULFONYLUREAS For DM management AR: hypoglycemia (increased risk with renal failure), weight gain

Question 214

Linagliptin Saxagliptin Sitagliptin

Answer 214

DPP-4 inhibitors inhibit DDP4 enzyme that deactivated GLP-1. For DM management: decrease in glucagon release, gastric emptying. Increase in glucose dependent insulin release, satiety AR: urinay and resp infections

Question 215

Pioglitazone | Rosiglitazone

Answer 215

For DM management by improving insulin sensitivity works via alterations in gene transcription and activation and therefore takes few weeks to start working PPAR gamma activator (intranuclear receptor)--> increases insulin sensitivity but upregulating GLUT 4 and levels of adiponectin(increases number of adipocytes sensitive to insulin) AR: weight gain, water weight gain, increased risk of fractures

Question 216

Canagliflozin Dapagliflozin Empagliflozin

Answer 216

Sodium glucose co transporter 2 (SGLT2) inhibitors block reabsorption of glucose in proximal convoluted tubule AR: glucosuria causes UTIs and vaginal yeast infection, hyperkalemia, dehydratiom, weight loss (check BUN and creatinine first)

Question 217

Acarbose | Miglitol

Answer 217

inhibit intestinal brush border alpha glucosidases--> decrease postprandial hyperglycemia AR: not recommended if kidney fx is impaired

Question 218

Thioamides

Answer 218

Propylthiouracil Methimazole MOA: block thyroid peroxidases and blocks 5'-deiodinase ( decreased conv and creation) Used for hyperthyroidism PTU for first trimester prgnancy treatment because methimazole is a teratogen and cause aplasia cutis. Use methimazole in 2nd and 3rd due to risk of PTU induced hepatotoxicity. note: agranulocytosis and consequent neutropenia is a serious complication of antithyroid drugs

Question 219

Levothyroxine (T4) | Liothyronine (T3)

Answer 219

thyroid hormone replacement used for hypothyroidism and myxedema may be abused for weight loss AR: similar to hyperthyroid sx

Question 220

Conivaptan | Tolvaptan

Answer 220

ADH antagonists - blocks action of ADH at V2 in SIADH

Question 221

Desmopressin

Answer 221

central DI, von willebrand disease, sleep enuresis, hemophilia A helps central DI via adenylate cyclase

Question 222

GH

Answer 222

GH deficiency | turners syndrome

Question 223

Oxytocin

Answer 223

labor induction milk letdown controls uterine hemorrhage

Question 224

Somatostatin (octreotide)

Answer 224

Acromegaly, carcinoid syndrome, gastrinoma, glucagonoma, esophageal varices

Question 225

Demeclocycline

Answer 225

MOA: ADH antagonist (member of tetracycline family) Used for SIADH AR: nephrogenic DI, photosensitivity, abnormalities of bone and teeth

Question 226

Fludrocortisone

Answer 226

MOA: synthetic analog of aldosterone with little glucocorticoid effects Use: mineralocorticoid replacement in primary adrenal insufficiency AR: hyperpigmentation, HF exacerbations, similar to glucocorticoids

Question 227

Cinacalcet

Answer 227

MOA: sensitizes Ca sensing receptor (CaSR) in parathyroid gland and decrease PTH "Cin-sitive for Calc-ium" Used for refractory hypercalcemia

Question 228

Sevelamer

Answer 228

MOA: nonabsorbable phosphate binder that prevents phosphate absorption from the GI tract Use: hyperphosphatemia in CKD AR: hypophosphatemia "SEVER ABS OF LAME PHOSPHATE IN GI"

Question 229

Cimetidine Ranitidine Famotidine Nizatidine

Answer 229

Histamine 2 blockers for acid suppression AR: antiandrogenic effects (proalctin release, gynecomastia, impotence, decreased libido in males), crosses BBB and placenta, cimetidine multidrug interactions "tidine" sounds like "histamine"

Question 230

``` Omeprazole Lansoprazole Esomeprazole Pantoprazole Dexlansoprazole ```

Answer 230

Proton pump inhibitors irreversibly inhibit H+/K+ ATPase AR: 1) increased risk of c diff 2) Decrease in Mg and Ca increases risk of fracture in elderly (osteoperosis)

Question 231

Aluminum hydroxide unique side effects

Answer 231

antacid constipation and hypophosphatemia proximal mm weakness osteodystrophy seizures "aluMINIMUM amount of feces"

Question 232

Calcium carbonate unique side effects

Answer 232

antacid AR: rebound acid increase can chelate and decrease effectiveness of other drugs

Question 233

Magnesium hydroxide unique side effects

Answer 233

antacid diarrhea, hyporeflexia, cardiac arrest MG= Must Go ….to bathroom

Question 234

Bismuth | Sucralfate

Answer 234

binds to ulcer base, providing physical protection and allowing HCO3 secretion to reestablish pH gradient in the mucous layer require acidic environment good for ulcer healing and travelers diarrhea (bismuth) "bisMOUTH of ulcer and SURFACE=SUCRALFATE"

Question 235

Misoprostol

Answer 235

PGE1 analog : increases gastric mucous barrier and decreases acid production (reverses COX 1 inhibition effect of NSAID that induce peptic ulcer) AR: contraindicated in women of childbearing potential because its abortifacient (MIScariage)

Question 236

Octreotide

Answer 236

long acting somatostatin analog used for acute variceal bleeds, acromegaly, VIPoma, carcinoid tumors increased risk of cholelithiasis due to CCK inhibition

Question 237

Sulfasalazine

Answer 237

a combo of sulfapyridine (antibacterial) and 5-aminosalicylic acid (anti inflammatory). activated by colonic bacteria use: ulcerative colitis, crohns disease AR: sulfonamide toxicity, reversible oligospermia

Question 238

Loperamide

Answer 238

agonist at u-opioid receptors low addictive potential (poor CNS penetration) used for diarrhea

Question 239

Ondansetron

Answer 239

5-HT3 antagonist, central acting used for postop vomiting and cancer chemotherapy vimiting AR: QT prolongation

Question 240

Metoclopramide

Answer 240

D2 receptor antagonist. use: diabetic and post surgery gastroparesis,antiemetic, persistent GERD AR: increase parkinsonian effects, tardive dyskinesia contraindicated in patients with small bowel obstruction or parkinsons disease due to D2 receptor blockage

Question 241

Orlistat

Answer 241

Inhibits gastric and pancreatic lipase to reduce the absorption of dietary fat use: weight loss AR: decreased absorption off fat soluble vitamins

Question 242

aprepitant

Answer 242

substance P antagonist that blocks NK1 receptors in the brain use: antiemetic for chemo induced "a Prep for chemo nausea"

Question 243

Psyllium | Methylcellulose

Answer 243

bulk forming laxatives soluble fiber draws water into lumen

Question 244

Magnesium hydroxide Magnesium Citrate Polyethylene glycol Lactulose

Answer 244

Osmotic laxative lactulose also treats hepatic encephalopathy: gut flora degrade lactulose into metabolites (lactic acid and acetic acid) that promote nitrogen excretion as NH4

Question 245

Senna

Answer 245

Stimulants of enteric nerve cause colonic contraction "Senna S-timulates EN-teric N-erves" AR:melanosis coli

Question 246

Docusate

Answer 246

Emollients promotes incorporation of water and fat in stool "Doc-U-SAid I have water and fat in my stool???" AR: diarrhea

Question 247

Cromolyn sodium

Answer 247

prevents mast cell degranulation (used for asthma prophylaxis)

Question 248

Dimercaprol | EDTA

Answer 248

first line treatment for foot and wrist drop associated with lead poisonin "is there LEAD in my DIME" "MDMA abuse LEADS to drugs"

Question 249

Succimer

Answer 249

chelation for kids with lead poisoning "SUCks to be a kid who eats LEAD"

Question 250

Heparin

Answer 250

MOA: activates antithrombin which decreases action of IIa (thrombin) and factor Xa. Follow via PTT Use: immediate anticoag . Does not cross the placenta AR: heparin induced thrombocytopenia (HIT)

Question 251

Heparin antidote

Answer 251

Protamine sulfate "Herpes is (-) and needs (+) protamine" Positively charged molecule that binds negatively charged heparin

Question 252

Low molecular weight heparin - enoxaparin - dalteparin

Answer 252

activates antithrombin and acts mostly on factor Xa rather than IIa (thrombin) 2-4X longer half life than unfractionated heparin BUT not easily reversible Safe for pregnancy but switch to normal heparin at time of birth to prevent bleeding

Question 253

Heparin induced thrombocytopenia (HIT)

Answer 253

antibody-heparin PF4 complex activates platelets --> thrombosis and thrombocytopenia

Question 254

Direct thrombin inhibitors

Answer 254

Bivalirudin Argatroban Dabigatran (only oral agent)

Question 255

Warfarin

Answer 255

MOA: interferes with gamma carboxylation of vitamin K dependent clotting factors (II, VII, IX,X, and protein C and S). Metabolism by vitamin K epoxide reductase complex (VKORC1). in lab: increases PT CANNOT use in pregnant women (teratogen) because lipid soluble and can cross the placenta. Heparin is safe because water soluble. cytochrome p450 interaction with rifampin, phenobarbital, phenytoin, st johns wort which decrease anticoagulation

Question 256

Why is there an initial risk of hyper coagualtion with warfarin? how can it be avoided?

Answer 256

protein C has a shorter half life than factors II and X. Existing protein C depletes before existing factors II and X deplete, and before warfarin can reduce factors II and X production --> hypercoagulation. Tissue necrosis is due to small vessel microthrombosis avoided via heparin bridging - use heparin when starting warfarin. Heparins activation of antithrombin enables anticoagulation during intitail, transient hypercoagulable state caused by warfarin.

Question 257

How do you reverse warfarin

Answer 257

vitamin k for rapid reversal give fresh frozen plasma (FFP) or PCC "during the war there was blood and plasma everywhere" ingestion of rat poison has same effects as warfarin overdose (brodifacoum)

Question 258

Apixaban | Rivaroxaban

Answer 258

Direct factor Xa inhibitors Use: DVT, PE, Stroke AR: not easy reversible

Question 259

Alteplase (tPa) Reteplase (rPA) Streptokinase Tenecteplase (TNK-tPA)

Answer 259

Thrombolytics MOA: plasminogen to plasmin which cleaves thrombin and fibrin clots. Increase PT and PTT because affects common pathway, no change in platelet count AR: INTRACEREBRAL HEMORRHAGING

Question 260

Clopidogrel Prasugrel Ticagrelor (reversible) Ticlopidine

Answer 260

ADP receptor inhibitors (P2Y12) and inhibit platelet agGREgation ("-grel"). Prevent expression of glycoproteins IIb/IIIa CLOPIDOGREL IS AS GOOD AS ASPIRIN. USE IF ALLERGIC TO ASPIRIN AR: neutropenia (ticlopidine)

Question 261

Cilostazol | Dipyridamole

Answer 261

MOA: phosphodiesterase inhibitors; increase cAMP in platelets, resulting in inhibition of platelet aggregation, vasodilators Use: claudication, prevention of stroke or TIAs (combined with aspirin), Adverse effects: facial flushing, CORONARY STEAL

Question 262

Abciximab Eptifibatide Tirofiban

Answer 262

MOA: Bind to the glycoprotein receptor IIb/IIIa Use: unstable angina, percutaneous coronary intervention

Question 263

Cladribine

Answer 263

antimetabolites - cancer drug MOA: purine analog Use: Hairy cell leukemia "CLAN" AR: myelosuppression, nephrotoxicity, and neurotoxicity

Question 264

Cytarabine (arabinofuranoyl cytidine)

Answer 264

antimetabolites - cancer drug MOA: pyrimidine analog --> DNA chain termination. At higher concentrations, inhibits DNA polymerase Use: Leukemias (AML) and lymphomas AR: megaloblastic anemia. CYTarabine causes panCYTopenia

Question 265

Methotrexate

Answer 265

antimetabolites - cancer drug MOA: folic acid analogy that competitively inhibits dihydrofolate reductase (results in accumulation of dihydrofolate polyglutamate)--> decrease dTMP --> decrease DNA synthesis. undergoes polyglutamination and accumulates in cells USE: cancers, ectopic pregnancy, medical abortion, RA, psoriasis, IBD, vasculitis AR: myelosuppression which is reversible with leucovorin "rescue", pulmonary fibrosis, folate deficiency

Question 266

Bleomycin

Answer 266

Antitumor antibiotics MOA: induces free radical formation which causes breaks in DNA strands Use: testicular cancer, hodkin lymphoma AR: pulmonary fibrosis

Question 267

Dactinomycin (actinomycin D)

Answer 267

Antitumor antibiotics MOA: Intercalates into DNA, preventing RNA synthesis Use: wilms tumor, ewing sarcoma, rhabdomyosarcoma. used for childhood tumors

Question 268

Doxorubicin | Daunorubicin

Answer 268

Antitumor antibiotics MOA: generate free radicals. Intercalate in DNA to create breaks in DNA and decrease replication. It interferes with topoisomerase II enzyme Use: solid tumors, leukemias, lymphomas AR: cardiotoxicity (dialted cardiomyopathy), Dexrazoxane (iron chelating agent) used to prevent cardio toxicity

Question 269

Busulfan

Answer 269

Alkylating agents MOA: cross linsk DNA Use: used to ablate patients bone marrow before bone marrow transplantation AR: pulmonary fibrosis

Question 270

Cyclophosphamide | Ifosfamide

Answer 270

Alkylating agents MOA: cross link DNA at guanine, requires bioactivation by liver, a nitrogen mustard Use: solid tumor, leukemia, lymphomas AR: hemorrhagic cystitis, prevented with mesna (thiol group of mesna binds toxic metabolities) or adequate hydration

Question 271

Nitrosoureas

Answer 271

Alkylating agents MOA: requires bioactivation. Cross blood brain barrier to CNS. Cross links DNA Use: brain tumors (including glioblastoma multiforme) AR: CNS toxicity (convulsions, dizziness, ataxia)

Question 272

Procarbazine

Answer 272

Alkylating agents MOA: cell cycle phase - nonspecific alkylating agent, Use: hodgkin lymphoma, brain tumors AR: pulmonary toxicity

Question 273

Paclitaxel | Other Taxanes

Answer 273

MOA: hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur) Use: ovarian and breast carcinomas "Taxes stabilize society"

Question 274

Vincristine | Vinblastine

Answer 274

MOA: vinca alkaloids that bind beta tubulin and inhibit mitotic spindle formation (M phase arrest) Use: hodgkin (vinblastine) and non hodgkin (vincristine) lymphomas AR: Vincristine is neurotoxic (affects MT formation in axons) and causes peripheral neuropathy. It "crisps" the nerves Vinblastine is bone marrow suppression. It blasts the bone marrow

Question 275

Cisplatin | Carboplatin

Answer 275

MOA: cross link DNA Use: Testicular, bladder, ovary, and lung carcinomas AR: Nephrotoxicity, OTOTOXICITY Prevent nephrotoxicity with amifostine (free radical scavenger) and chloride (saline) diuresis

Question 276

Etoposide | Teniposide

Answer 276

MOA: inhibit topoisomerase II --> increases DNA degradation Use: solid tumors (particularly testicular and small cell lung cancer), leukemias, lymphomas AR: alopecia " topoisomerase now needs two toupee"

Question 277

Irinotecan | Topotecan

Answer 277

MOA: inhibit topoisomerase I (He had 1 TEa CAN TO POur) Use: Colon cancer (irinotecan), ovarian and small cell lung ancers (topotecan)

Question 278

Erlotinib

Answer 278

MOA: EGFR tyrosine kinase inhibitor Use: non small cell lung carcinoma AR: rash

Question 279

Imatinib

Answer 279

MOA: tyrosine kinase inhibitor of BCR-ABL (philadelphia chromosome fusion gnee in CML) and c-kit (GI stromal tumors) Use: CML, GI stromal tumors (GIST) AR: fluid retention

Question 280

Bortezomib | Carfilzomib

Answer 280

MOA: proteasome inhibitors, induce arrest at G2-M phase and apoptosis "zomibs inhibit the proteaZOMES" Use: multiple myeloma, mantle cell lymphoma AR: peripheral neuropathy, herpes zoster reactivation

Question 281

Tamoxifen | Raloxifene

Answer 281

MOA: selective estrogen receptor modulatorys (SERMs) - receptor antagonists in breast and agonists in bone. Use: breast cancer treatment (tamoxifen only, active metabolite is endoxifen) and prevention. Raloxifene also useful to prevent osteoporosis AR: Tamoxifen - increase the risk of endometrial cancer because agonist effect in endometirum Both increase risk of thromboembolic events

Question 282

Vemurafenib

Answer 282

"VEmuRAF-enib" is for "V600E-MUtated bRAF INHIBition" Use: metastatic melanoma

Question 283

Rasburicase

Answer 283

MOA: recombinant urate oxidase that catalyzes metabolism of uric acid to allantoin Use: prevention and treatment of tumor lysis syndrome (can also use allopurinol)

Question 284

Common chemotoxicity: Cisplastin/Carboplatin

Answer 284

Ototoxicity Nephrotoxicity

Question 285

Common chemotoxicity: Vincristine

Answer 285

peripheral neuropathy

Question 286

Common chemotoxicity: Bleomycin, Busulfan

Answer 286

pulmonary fibrosis

Question 287

Common chemotoxicity: Doxorubicin

Answer 287

cardiotoxicity

Question 288

Common chemotoxicity: Trastuzumab (herceptin)

Answer 288

cardiotoxicity

Question 289

Common chemotoxicity: Cyclophosphamide

Answer 289

hemorrhagic CYstitis

Question 290

Acetaminophen

Answer 290

MOA: REVERSIBLY inhibits COX mostly in CNS instead of aspirin to avoid Reye syndrome in children

Question 291

Aspirin

Answer 291

MOA: IRREVERSIBLY inhibits COX1 and COX2 by covalent acetylation that decreases synthesis of TXA2 and prostaglandins . This increases bleeding time without an effect on PT, PTT. AR: gastric ulceration, tinnitus (CN VII), Reyes syndrome, aspirin exacerbated airway disease results from the dysregulation of arachidonic acid metabolis, due to COX inhibition (increased diversion of arachidoic acid down the 5-lipooxygenase pathway and reduced inhibition via prostaglandin E2). this results in increased formation of bronchoconstrictive leukotrienes

Question 292

Celecoxib

Answer 292

MOA: Inhibits COX 2 for inflammation and pain. Spares Cox 1 and so helps maintain gastric mucosa and spares TXA2 production use: RA, OA AR: thrombosis, sulfa allergy

Question 293

``` Ibuprofen Naproxen Indomethacin Ketorolac Diclofenac Meloxicam Piroxicam ```

Answer 293

NSAIDs MOA: inhibit COX1 and COX2 Indomethacin is for PDA closure

Question 294

Leflunomide

Answer 294

MOA: reversibly inhibits dihydroorotate dehydrogenase, preventing pyrimidine synthesis. suppresses T cell proliferation Use: RA, psoriatic arthritis AR: hepatotoxic and teratogen

Question 295

Alendronate Ibandronate Risedronate Zoledronate

Answer 295

Bisphosphonates "-dronate" MOA: pyrophosphate analogs bind hydroxyapatite in bone, inhibiting osteoclast activitiy Use: osteoporosis, hypercalcemia, paget disease of bone, metastatic bone disease, osteogenesis imperfecta AR: esophagitis, osteonecrosis of jaw and femur

Question 296

Teriparatide

Answer 296

MOA: recombinant PTH analog. Increase osteoblastic activity when administered in pulsatile fashion Use: osteoporosis AR: increased risk of osteosarcoma therefore avoid if pt has pagets disease of bone or unexplained elevation of alkaline phosphatase

Question 297

Probenecid

Answer 297

Chronic gout inhibits reabsorption of uric acid in PROximal convoluted tubule (also inhibits secretion of penicillin and enhances its efficacy) can ppt uric acid calculi

Question 298

Pegloticase

Answer 298

Chronic gout recombinant uricase catalyzing uric acid to allantoin ( a more water soluble product)

Question 299

NSAIDs+ Glucocorticoids +Colchicine

Answer 299

Acute gout drugs careful with salicylates because it may decrease uric acid secretion Colchicine works by binding and stabilizing tubulin to inhibit microtubule polymerization, impairing neutrophil chemotaxis and degranulation

Question 300

Etanercept

Answer 300

TNF alpha inhibitor (decoy receptor for TNF alpha) --> impaired cell mediated immunity Think "Etanercept intercepts TNF" Use: RA, psoriasis, AS AR: predisposition to infection and reactivation of latent TB because TNF is important in granuloma formation and stabilization. Drug induced lupus

Question 301

``` Diazepam Lorazepam Triazolam Temazepam Oxazepam Midazolam Chlordiazepoxide ```

Answer 301

Benzodiazepines MOA: Allosteric activation! GABAa action increased by increasing frequency of Cl- channel opening. Decreases REM sleep Use triazolam or lorazepam for reduced day time somnolence while gapping SSRI therapy AR: dependence, alcohol use dangerous, avoid other sedative drugs like first gen anithistiamines, less risk of resp and CV depression than barbs

Question 302

Phenobarbital pentobarbital thiopental secobarbital

Answer 302

Barbiturates - increase DURATions of Cl channel opening causes increased GABAa inihitory firing which decreases neuronal firing use: sedative. thiopental specific for anesthesia AR: resp and CV depression that can be fatal, CNS depression (worse with alcohol), CYP450 interactions contraindicated in porphyria

Question 303

Zolpidem Zaleplon Eszopiclone

Answer 303

Nonbenzodiazepine hypnotics its Esz to ZZzzz MOA: act on the BZ1 subtype of the GABA receptor. sleep cycle less affected compared to benzos use: insomnia Less dependence risk than benzos

Question 304

Suvorexant

Answer 304

MOA: orexin (hypocretin) receptor antagonist use: insomnia contraindicated in patients with strong CYP3A4 inhibitors

Question 305

Ramelteon

Answer 305

MOA: melatonin receptor agonist Use: insomnia (safe in elderly) AR: no dependence.nausea

Question 306

Sumatriptan

Answer 306

triptans/dihydroergotamine MOA: 5-HT 1B/1D agonist. inhibits the trigeminal nerve activation and prevents vasoactive peptide release; induce vasoconstriction use: acute migraine or cluster headaches (for prophylaxis you can give verapamil) AR: coronary vasospasm therefore contraindicated in patients with CAD or prinzmetal angina, serotonin syndrome, can cause hypertensive emergency

Question 307

How do you treat overdose of benzo (also nonbenzo hypnotics)

Answer 307

flumazenil (competitive antagonist at GABA benzodiazepine receptor)

Question 308

Benzo, barbs, and alcohol all bind the ____ receptor which is a ligand gated ____ channel

Answer 308

GABAa Cl-

Question 309

What benzo is safe to give for liver dz patients

Answer 309

Oxazepam Temazepam Lorazepam

Question 310

What benzos have addictive potential

Answer 310

Alprazolam, riazolam,oxazepam, midazolam are short acting and therefore higher addictive potential

Question 311

Parkinson disease drugs

Answer 311

due to loss of dopaminergic neurons and excess cholinergic activity Bromocriptine, Amantadine, Levodopa with carbidopa, selegiline and COMT inhibitors, antimuscarinics (BALSA)

Question 312

Bromocriptine (ergot) Pramipexole (non-ergot) Ropinirole (non-ergot)

Answer 312

Dopamine agonists for parkinsons dz AR: impulse control disorder, postural hypotension, hallucinations/confusion bromocriptine also used for hyperprolactinemia

Question 313

Amantadine

Answer 313

increase dopamine availability in parkinsons dz increase release and decrease reuptake AR: ataxia and livedo reticularis

Question 314

Selegiline | Rasagiline

Answer 314

selective MAO type B inhib --> prevents dopamine conversion into DOPAC --> increase dopamine availability prevent dopamine breakdown in parkinsons dz post-BBB (centrally) used with L-DOPA but can increase adverse effects of L-DOPA

Question 315

Entacapone

Answer 315

COMT inhibitor (central and peripheral) blocks conversion of dopamine to 3-MT or methoxytyramine by inhibiting central COMT prevents peripheral L-DOPA degradation to 3-O-methyldopa (3-OMD) by inhibiting COMT used in conjunction with levodopa

Question 316

Carbidopa/levodopa

Answer 316

DOPA decarboxylase inhibitor carbidopa prevents peripheral conversion of L-DOPA to dopamine --> increase L-DOPA entering into CNS--> increase L-DOPA available for conversion to dopamine in the CNS **dopamine cant cross BBB but L-DOPA can AR: long term use can lead to dyskinesia or the "on-off" phenomenon, postural hypotension from increased production of catecholamines in periphery, increased central NS dopamine can cause severe anxiety and agitation

Question 317

Tetrabenazine | Reserpine

Answer 317

MOA: inhibit vesicular monoamine transporter (VMAT) dopamine --> decreases vescile packaging and release use: huntington chorea and tardive dyskinesia

Question 318

Riluzole

Answer 318

MOA: decrease neuron glutamate excitotoxicity use: ALS/Lou Gehrig disea "riLOUzole"

Question 319

Memantine

Answer 319

for alzheimers think memantine=memory and time moa: NMDA receptor antagonist; helps prevent excitotoxicity (mediated by Ca) AR: dizziness, confusion, hallucinations

Question 320

``` Desflurane Halothane Enflurane Isoflurane Sevoflurane Methoxyflurane N2O ```

Answer 320

Inhaled anesthetics myocardia depression, resp depression, increased cerebral blood flow, decreased cerebral metabolic demand AR: hepatotoxicity (halothane hepititis) Nephotoxicity (methoxyflurane) proconvulsant (enflurane, epileptogenic) expansion of trapped gas in body cavity (N2O)

Question 321

Thiopental

Answer 321

IV anesthetics MOA: faciliatate GABAa by increasing duration use: short surfical procedures AR: decreased cerebral blood flow high lipid solubility

Question 322

Midazolam

Answer 322

IV anesthetics MOA: facilitate GABAa by increasing freq use: procedural sedation and anesthesia induction AR: severe postop rresp depression, decreased bp, anterograde amnesia

Question 323

Propofol

Answer 323

IV anesthetics MOA: propentiates GABAa use: rapid anesthesia induction due to lipophilic and accumulation in tissues with high blood flow, short procedures, ICU sedation

Question 324

Ketamine

Answer 324

IV anesthetics MOA: NMDA receptor antagonist use: dissociative anesthesia AR: increased cerebral blood flow, emergence reaction possible with disorientation, hallucination, vivid dreams

Question 325

Procaine Tetracaine Benzocaine Chloroprocaine

Answer 325

Ester local anesthetic (have one "I") MOA: block Na channels if infected tissue then need more anesthetic because alkaline anesthetics are charged and cannot penetrate the acidic tissue AR: CNS excitation, methemoglobinemia with benzocaine

Question 326

Lidocaine Mepivacaine Bupivacaine Ropivacaine

Answer 326

Amide local anesthetic (have two "I") given if allergic to esters severe cardiovascular toxicity with bupivacaine

Question 327

CNS drugs must be _____ soluble to cross the BBB or be actively transported

Answer 327

lipid soluble

Question 328

Low solubility in blood for anesthetics

Answer 328

rapid induction and recovery times

Question 329

High solubility in lipids for anesthetics

Answer 329

increased potency = 1/MAC MAC= minimal alveolar conventration (of inhaled anesthetic) required to prevent 50% of subjects from moving in response to noxious stimulus

Question 330

Malignant hypertension

Answer 330

inhaled anesthetics or succinylcholine induce fever and severe mm contractions mutations in voltage-sensitive ryanodine receptor (RYR1 gene) cause increase Ca release from sarcoplasmic reticulum

Question 331

treatment for malignant hypertension

Answer 331

dantrolene a ryanodine receptor antagonist

Question 332

order of nerve blcokade

Answer 332

small diameter > large diameter Myelianted > unmyelinated size > myelination small myelinated > small unmyelinated> large myelinated fibers > large unmyelinated fibers loss (1) pain, (2) temp, (3) touch (4)pressure

Question 333

Succinylcholine

Answer 333

depolarizing neuromuscular blocking drugs MOA: strong ACh receptor agonist that produces a sustaine depol and prevents mm contraction AR: hypercalcemia, SEVERE HYPERKALEMIA, malignant hyperthermia

Question 334

``` Atracurium Cisatracurium pancuronium Rocuronium tubocurarine vecuronium ```

Answer 334

Nondepolarizing neuromuscular blcoking drugs

Question 335

Dantrolene

Answer 335

MOA:prevents release of Ca from the SR of skeletal mm by binding to the ryanodine receptor AR: malignant hyperthermia and neuroleptic malignant syndrome

Question 336

Baclofen

Answer 336

MOA: skeletal mm relaxant as a GABAb receptor agonist in spinal cord Use: mm spasticity due to MS or other, dystonia, ms

Question 337

Cyclobenzaprine

Answer 337

MOA: skeletal mm relaxant acts within the CNS Use: muscle spasms AR: anticholinergic side effects. Sedation

Question 338

Opiod analgesics

Answer 338

MOA: agonist at opioid receptors to modulate synaptic transmission- close presynaptic Ca channel, open postsynaptic K channels and decrease synaptic transmission. Inhibit release of ACH, NE, 5 HT, glutamate, substance P

Question 339

Pentazocine

Answer 339

κ opioid agonist μ opioid receptor weak antagonist or partial agonist opioid withdrawal if also taking full opioid

Question 340

Butorphanol

Answer 340

κ opioid receptor agonist and μ opioid receptor partial agonist use: severe pain with less resp depression than full opioid agonists AR: withdrawal thats not easily reversed with naloxone

Question 341

Tramadol

Answer 341

very weak opioid agonist that also inhibits 5-HT receptors use: chronic pain adverse effects: similar to opiods. decreases seizure threshold. serotonin syndrome

Question 342

Timolol Betaxolol Carteolol

Answer 342

Glaucoma drug - beta blcoker decrease aq humor synthesis by epithelial cells no pupilalry or vision changes

Question 343

Epinephrine Apraclonidine Brimonidine

Answer 343

alpha blocker decrease aq humor synthesis for glaucoma mydriasis due to alpha 1 therefore do not use in closed angle glaucoma, ocular hyperemia, foreign body sensation, ocular pruritus

Question 344

Acetazolamide

Answer 344

Glaucoma drug - diuretics decrease aq humor synthesis via inhibition of carbonic anhydrase no pupillar or vision changes

Question 345

Bimatroprost | Latanoprost

Answer 345

Glaucoma drug - prostaglandins first line increase outflow of aq humor via decreased resistance of flow through uveoscleral pathway Darkens color of iris (browning), eyelash growth

Question 346

pilocarpine carbachol physostigmine echothiophate

Answer 346

Glaucoma drug - cholinomimetics (M3) Direct: pilocarpine, carbachol Indirect: physostigmine , echothiophate increase outflow of aq humor via contraction of ciliary mm and opening of trabecular meshwork AR: miosis and cyclospasm

Question 347

Use _____ in acute angle closure glaucoma because it is very effective at opening meshwork into canal of schlemm

Answer 347

pilocarpine, a cholinomimetic (M3)

Question 348

Reversal of nondepolarizing neuromusuclar blocking drugs i.e. side effect reversal due to tx of myasthenia gravis with cholinesterase inhibitors

Answer 348

neostigmine with atropine or glycopyrrolate

Question 349

morphine, heroin, meperidine, methadone, codeine

Answer 349

full agonist -opioid note: mu opioids like morphine cause contraction of smooth muscles in the sphincter of oddi leading to increased pressure in the common bile duct and the gallbladder

Question 350

buprenorphine

Answer 350

partial agonist - opioid

Question 351

Nalbuphine | pentazocine

Answer 351

mixed agonist/antagonist-opioid

Question 352

Naloxone Naltrexone Methylnaltrexone

Answer 352

antagonist -opioid

Question 353

which opioid is used for cough suppression

Answer 353

dextromethorphan

Question 354

which opioid is used to tx diarrhea -note: slows motility

Answer 354

loperamide | diphenoxylate

Question 355

Opioid used for maintenance programs for heroin addicts

Answer 355

methadone buprenorphine naloxene

Question 356

opioid toxicity tx? relapse prevention?

Answer 356

naloxone naltrexone once detoxed

Question 357

Benzodiazepines

Answer 357

first line for acute status epilepticus MOA: increases GABAa action and postsynaptic chloride influx

Question 358

Carbamzepine

Answer 358

commonly used for patial/focal seizures also used for tonic clonic seizures first line for trigeminal neuralgia MOA: blocks Na channels AR:blood dyscrasias(agranulocytosis, aplastic anemia due to bone marrow suppression), liver toxicity, teratogenesis, cytochrome P450, SIADH, steven johnsons syndrome

Question 359

Ethosuximide

Answer 359

USe: absence seizures MOA: blocks thalamic T type Ca channels AR:urticaria, steven johnson syndrome

Question 360

Gabapentin

Answer 360

used for partial focal seizures and peripheral neuropathy, postherpetic neuralgia MOA: primarily inhibits high voltage activated Ca channels and designed as a GABA analog

Question 361

Lamotrigine

Answer 361

USed for partial (focal), tonic clonic, abscence seizures blocks voltage gated Na channels, inhibits the release of glutamate AR: may cause stevel johnsons syndrome, titrate slowly

Question 362

Levetiracetam

Answer 362

used for partial/focal and tonic clonic seizures AR: neuropsychiatric symptoms

Question 363

Phenobarbital

Answer 363

Used for partial(focal),tonic clonic, status epilepticus. First line in neonates "phenobabytal" increases GABAa action AR: dependence, cytochrome P450,cardioresp depression

Question 364

Phenytoin | Fosphenytoin

Answer 364

first line for reccurrent status epilepticus blocks Na channels AR: P450, Hirsutism, enlarged gums, nystagmus, yellow brown skin, teratogen, osteopania, inhibited folate absorption, neuropathy, stevenjohnson,/dress syndrome, sLE like syndrome

Question 365

Tiagabine

Answer 365

partial/tonic seizures increase GABA by inhibiting reuptake

Question 366

Topiramate

Answer 366

partial/focal and tonic clonic and fo rmigraine prevention blocks Na channels and increases GABA action AR: mental dulling, word finding difficulty, kidney stones, weight loss, glaucoma

Question 367

Valproic acid

Answer 367

partial/focal, tonic clonic, abscence increase Na channel inactivation, increase GABA concentration by inhibiting GABA transaminase AR: GI distress, fatal hepatotoxicity, pancreatitis, neural tube defects, tremor, weight gain, contraindicated in pregnancy

Question 368

Vigabatrin

Answer 368

for partial/focal increase GABA, irreversible GABA transaminase inhibitor vigaBATrin Permanent visual loss --> BLACK BOX WARNING

Question 369

first line for exlampsia seizures

Answer 369

MgSO4

Question 370

Preferred med for: ADHD

Answer 370

stimulants - methylphenidate and amphetamines

Question 371

Preferred med for: alcohol withdrawal note: chronic alcohol consumption leads to decreased GABA sensitivity and alcohol tolerance develops. Abrupt cessation decreases inhibitory tone and results in CNS excitation (withdrawal)

Answer 371

Benzodiazepines

Question 372

Preferred med for: bipolar disorder

Answer 372

Lithium, valproic acid, carbamazepine, lamotrigine, atypical antipsychotics

Question 373

Preferred med for: bulimia nervosa

Answer 373

SSRI

Question 374

Preferred med for: depression

Answer 374

SSRI

Question 375

Preferred med for: general anxiety disorder

Answer 375

SSRI and SNRI

Question 376

Preferred med for: OCD

Answer 376

SSRIs, venlafaxine, clomipramine

Question 377

Preferred med for: panic disorder

Answer 377

SSRI, venlafaxine, benzodiazepine

Question 378

Preferred med for: PTSD

Answer 378

SSRI

Question 379

Preferred med for: social anxiety disorder

Answer 379

SSRIs, venlafaxine perforamnce only: beta blockers and benzodiazepines

Question 380

Preferred med for:Tourette syndrome

Answer 380

antipsychotics

Question 381

Methylphenidate Dextroamphetamine Methamphetamine

Answer 381

CNS stimulants MOA: increase catecholamine in the synaptic cleft, especially NE and dopamine Use: ADHD and narcolepsy AR: nervousness, agitation, anxiety, insomnia, tachycardia, hypertension, weight loss, tics

Question 382

Typical antipsychotics

Answer 382

``` Haloperidol Primozide Trifluoperazine Fluphenazine Thioridazine Chlorpromazine ``` MOA: block dopamine D2 receptor (incrase cAMP) High potency: Trifluoperazine, Fluphenazine, Haloperidol have more neuro side effects Low potency: chlorpromazine, thioridazine have more anticholinergic and antihistamine and alpha1 blockade effects AR:Lipid soluble and therefore stored in fat and slow to be removed from body

Question 383

Major adverse effects of typical antipsychotics

Answer 383

Endocrine: dopamine receptor antagonism causing hyperprolactinemia --> galactorrhea, oligomenorrhea, gynecomastia Metabolic: dyslipidemia, weight gain, hyperglycemia Antimuscarinic: dry mouth and constipation Antihistamine: sedation Alpha1blcokade: orthostatic hypotension Cardiac:QT prolongation Ophthalmologic: chlorpromazine causes corneal deposits. Thioridazine causes retinal deposits. Neuroleptic malignant syndrome

Question 384

Timeline of major adverse effects of typical antipsychotics

Answer 384

hours to days: acute dystonia Days to months: akathisia (restlessness) and parkinsonism (bradykinesia) Months to years: Tardive dyskinesia(orofacial chorea)

Question 385

``` Aripiprazole Asenapine Clozapine Olanzapine Quetiapine Iloperidone Paliperidone Risperidone Lurasidone Ziprasidone ```

Answer 385

Atypical antipsychotics MOA: most are D2 antagonists. Aripiprazole is D2 partial agonist Use: schizophrenia positive and negative symptoms, Use Clozapine for tx resistant schizo or schizoaffective disorder and for suicidality in schizophrenia. Bipolar, OCD, anxiety disorder, depression, mania, tourette syndrome AR: all cause a prolonged QT interval, fewer EPS and anticholinergic side effects than typical antipsychotics Clozapine-agranulocytosis (monitor WBS) and seizures (dose related) Risperidone- hyperprolactinemia (amenorrhea, galactorrhea, gynecomastia) Olanzapine and clOzapine cause obesity and must have their metabolic perameters monitored for diabetes

Question 386

Lithium note: toxicity can occur if a patient takes thiazide diuretics, ACE I, and NSAIDS

Answer 386

Used as a mood stabilizer for bipolar disorder. Treat acute manic episodes and prevents relapse AR: HYPOTHYROIDISM, EBSTEIN anomaly with heart, DIABETES INSIPIDUS by antagonizing vasopressin in the colelcting tubules(nephrogenic diabetes insipidus), Unwanted movements tremor

Question 387

``` Fluoxetine Fluvoxamine Paroxetine Sertraline Escitalopram Citalopram ```

Answer 387

Selective Serotonin Reuptake Inhibitors MOA: inhibit 5-HT reuptake AR: fever than TCAs, GI distress, DIADH, sexual dysfunction (anorgasmia, decreased libido) it takes 4-8 weeks to have an effect

Question 388

``` Venlafaxine Desvenlafaxine Duloxetine Levomilnacipran Milnacipran ```

Answer 388

serotonin-norepinephrine reuptake inhibitors MOA: SNRIs inhibit 5-HT and NE reuptake AR: increase BP, stimulant effects, sedation, nausea

Question 389

Tranylcypromine Phenelzine Isocarboxazid Selegiline

Answer 389

Monoamine oxidase inhibitors MOA: nonselective MAO inhibition increases levels of amine NT (norephinephrine, 5 HT, dopamine) used for depression, anxiety, and parkinsons disease (selegiline) AR: CNS stimulation; hypertensive crisis with tyramine ingestion (aged cheese, draft beer etc), contraindicated with SSRIs, TCAs, St Johns wort, meperidine, dextromethorphan (to prevent serotonin syndrome) wait 2 weeks after stopping to start serotonergic drugs or stopping dietary restrictions

Question 390

``` Amitriptyline Nortriptyline Imipramine Desipramine Clomipramine Doxepin Amoxapine ```

Answer 390

Tricyclic antidepressants MOA: TCAs inhibit 5-HT and NE reuptake Imipramine can also be used for nocturnal enuresis AR: convulsions, coma, cardiotoxicity (due to arrhythmias from blocking fast sodium channel conduction) , respiratory depression, hyperpyrexia, confusion and hallucinations in the elderly due to anticholinergic side effects, URINARY RETENTION use NaHCO3 to prevent arrhythmias overdose treated with sodium bicarbonate

Question 391

Methadone

Answer 391

opioid withdrawal and detox long acting opiate used for heroin detox or long term maintenance therapy

Question 392

Buprenorphine + naloxone

Answer 392

opioid withdrawal and detox sublingual buprenorphine (partial agonist) is absorbed and used for maintence therapy Naloxone (antagonist) is added to lower IV abuse potential

Question 393

Naltrexone

Answer 393

opioid withdrawal and detox Long acting mu opioid receptor blockade given IM or as a nasal spray to treat acute overdose in unconscious individuals relapse prevention once detoxified ALSO FIRST LINE THERAPY FOR MODERATE TO SEVERE ALCOHOL ABUSE DISORDER. REDUCES CRAVINGS

Question 394

Trazodone

Answer 394

Atypical antidepressant Primarily blocks 5-HT2, alpha1adrenergic, and H1 receptors, also weakly inhibits 5-HT reuptake Used for insomnia because high doses are needed for antidepressant effects AR: sedation, nausea, priapism, postural hypotension, male specific side effects

Question 395

Varenicline

Answer 395

Atypical antidepressant Nicotinic ACh receptor partial agonist. Used for smoking cessation. toxicity: sleep disturbances, may depress mood, Varenicline helps nicotine cravings decline

Question 396

Vilazodone

Answer 396

Atypical antidepressant inhibits 5-HT reuptake; 5- HT1A receptor partial agonist. Used for major depressive disorders. AR: headache, diarrhea, nausea, increased weight, anticholinergic effects. MAy cause serotonin syndrome if taken with other drugs

Question 397

Vortioxetine

Answer 397

Atypical antidepressant Inhibits 5-HT reuptake; 5HT1A receptor agonist 5HT3 receptor antagonist Used for major depressive disorder toxicity: sexual dysfunction, sleep disturbances (abnormal dreams), anticholinergic effects

Question 398

Acetazolamide

Answer 398

MOA: carbonic anyhdrase inhibitor that causes self limited NaHCO3 diuresis and decreased total body HCO3 stores Use: glaucoma, metabolic alkalosis, altitude sickness, pseudotumor cerebri, alkalinizes urine AR: proximal renal tubular acidosis "ACIDazolamide", paresthesias, NH3 toxicity, sulfa allergy, hypokalemia. Promotes calcium phosphate stone formation (insoluble at high pH)

Question 399

Furosemide Bumetanide Torsemide MOST POTENT diuretics

Answer 399

sulfonamide loop diuretics MOA: inhibit cotransport system (Na/K/2Cl) of thick ascending limb of loop of henle. Abolish hypertonicity of medulla, preventing concentration of urine. Stimulate Prostaglandin E release (vasodilatory effect on afferent arteriole); inhibited by NSAIDs, increase Ca excretion Use: edematous states, hypertension, hypercalcemia AR: ototoxicity, Hypokalemia, Hypomagnesemia, Dehydration, Allergy (sulfa), metabolic alkalosis, Nephritis (interstitial), Gout

Question 400

Ethacrynic acid

Answer 400

MOA: nonsulfonamide inhibitor at thick ascending limb of loop of henle use: diuresis in patient allergic to sulfa drugs AR: more ototoxic "loop earing hurts your ear"

Question 401

Thiazide diuretics

Answer 401

Hydrochlorothiazide Chlorthalidone Metolazone moa: inhibit NaCl reabsorption in early DCT --> decreased Na and Cl --> decreased intravascular volume --> RAAS activation --> increased excretion of potassium and hydrogen (hypokalemia and metabolic alkalosis) decreased diluting capacity of nephron and decreases Ca excretion (good for calcium oxalatae stone prevention and for osteoperosis) AR: hypokalemic metabolic alkalosis (due to activation of RAAS) causing muscle weakness and cramps, hyponatremia, hyperglycemia (decreased isnulin and increased resistance), hyperlipidemia, hyperuricemia (increased resoprtion), hypercalcemia (increased resorption), sulfa allergy

Question 402

Potassium sparing diuretics

Answer 402

Spironolactone Eplerenone Amiloride Triamterene MOA: spironolactone and eplerenone are competitive aldosterone receptor antagonists in cortical collecting tubule Triamterene and amiloride block Na channels in the cortical collecting tubule Use: Hyperaldosteronism, K depletion, HF, hepatic ascites (spironolactone), nephrogenic DI (amiloride) antiandrogen AR: hyperkalemia (leads to arrhythmias), endocrine effects with spironolactone

Question 403

Captopril Enalapril Lisinopril Ramipril

Answer 403

Angiotensin converting enzyme inhibitors inhibits ACE which decreases formation of ATII and decreases GFR by preventing constriction of efferent arterioles. This increases renin due to loss of negative feedback. Inhibition of ACE also prevents inactivation of bradykinin as potent vasodilator Use: HTN, HF, proteinuria, diabetic nephropathy. AR: cough, angioedema (due to increase in bradykinin therefore contraindicated in C1 esterase inhibitor deficiency), teratogen, increase creatinine , Use with caution in bilateral renal artery stenosis because ACEi will further decrease GFR and thus result in renal failure

Question 404

Losartan Candesartan Valsartan

Answer 404

(ARBs) MOA: selectively block binding of angiotensin II at AT1 receptor. Do not increase bradykinin Use: HTN, HF, proteinuria, or chronic kidney disease AR: hyperkalemia, decrease GFR, hypotension, teratogen

Question 405

Aliskiren

Answer 405

Direct renin inhibitor, blocks conversion of angiotensinogen to angiotensin I. Used for HTN AR: hyperkalemia, decrease GFR, hypotension, angioedema. RElatively contraindicated in patients already taking ACE inhibitors or ARBs. Contraindicated in pregnancy

Question 406

Leuprolide

Answer 406

MOA: GnRH analog with agonist properties when used in pulsatile fashion. Has antagonist properties when used in continuous fashion because it downregulates GnRH receptor in pituitary and thus decreases FSH and LH (initial rise in LH/testosterone and then decrease in testosterone) Use: uterine fibroids, endometriosis, precocious puberty, prostate cancer, infertility AR: hypogonadism, decreased libido, erectile dysfunction "leuprolide in lieu of GnRH"

Question 407

Ethinyl estradiol DES Mestranol

Answer 407

Estrogens AR: clear cell adenocarcinoma of vagina in females exposed to DES in utero

Question 408

Raloxifene

Answer 408

selective estrogen receptor modulator antagonist at breast, uterus agonist at bone increases risk of thromboembolic events but no increased risk of endometrial cancer( vs tamoxifen) used to treat osteoporosis

Question 409

Anastrozole Letrozole Exemestane

Answer 409

Aromatase inhibitors MOA: inhibit peripheral conversion of androgens to estrogen Use:ER + breast cancer in postmenopausal women

Question 410

``` Levonorgestrel Medroxyprogesterone Etonogestrel Norethindrone Megestrol ```

Answer 410

Progestins MOA: bind progesterone receptors, decrease growth and increase vascularization of endometrium, thicken cervical mucus Use: contraception, endometrial cancer, abnormal uterine bleeding. Progestin challenge: presence of withdrawal bleeding excludes anatomic defects and chronic anovulation without estrogen

Question 411

Mifepristone | Ulipristal

Answer 411

Antiprogestins MOA: competitive inhibitors of progestins at progesterone receptors Use: termination of pregnancy (mifepristone with misoprostol). Emergency contraception (ulipristal)

Question 412

Copper intrauterine device

Answer 412

MOA: produces local inflammatory reaction toxic to sperm and ova, preventing fertilization and implantation, hormone free AR: heavier or longer menses, dysmenorrhea.

Question 413

Danazol

Answer 413

MOA: synthetic androgen that acts as partial agonist at androgen receptors use: endometriosis, hereditary angioedema AR: weight gain, edema, acne, hirsutism, masculinization, decrease HDL levels, hepatotoxicity, pseudo tumor cerebri

Question 414

Testosterone | Methyltestosterone

Answer 414

MOA: agonist at androgen receptor Use: treat hypogonadism and promote development of secondary sex characteristics. Stimulate anabolism to promote recovery after burn or injury AR: Premature closure of epiphyseal plates. Increase LDL and decrease HDL

Question 415

Tamsulosin

Answer 415

alpha1 antagonist used to treat BPH by inhibiting smooth mm contraction selective for α1A/D receptors found on prostate vs vascular α1B receptors

Question 416

Sildenafil Vardenafil Tadalafil

Answer 416

Phosphodiesterase type 5 inhibitors MOA: increase in cGMP and thus prolonged smooth muscle relaxation in response to NO. Use: erectile dysfunction, pulmonary hypertension, BPH (tadalafil) "-fil" they "fill" the penis AR: hot and sweaty, headache, heartburn, HTN DO NOT USE WITH NITRATES BECAUSE BOTH ACT VIA cGMP AND CAUSE PROFOUND HYPOTENSION

Question 417

Flutamide

Answer 417

Nonsteroidal competitive inhibitor at androgen receptors used for prostate carcinoma

Question 418

Ketoconazole

Answer 418

Inhibits steroid synthesis (inhibits 17,20 desmolase/17 alpha hydroxylase) used in PCOS to reduce androgenic symptoms. can cause gynecomastia and amenorrhea

Question 419

Spironolactone

Answer 419

Inhibits steroid binding, 17,20 desmolase/17alpha hydroxylase used in PCOS to reduce androgenic symptoms. can cause gynecomastia and amenorrhea

Question 420

Diphenhydramine Dimenhydrinate Chlorpheniramine

Answer 420

First generation histamine 1 blockers reversible inhibitors of H1 histamine receptors allergy, motion sickness, sleep aid note: diphenhydramine can be used to treat neuroleptic malignant syndrome AR: sedation, antimuscarinic, antiα adrenergic

Question 421

Loratadine Fexofenadine Desloratadine Cetirizine

Answer 421

Second generation histamine 1 blockers use: allergy AR: far less sedating that first gen because of decreased entry into CNS

Question 422

Guaifenesin

Answer 422

expectorant thins respirator secretions does not suppress cough reflex

Question 423

N-acetylcysteine

Answer 423

mucolytic - liquifies mucus in chronic bronchopulmonary disease by disrupting disulfide bonds antidote for acetaminophen overdose

Question 424

Dextromethorphan

Answer 424

Antitussive (antagonizes NMDA glutamate receptors) synthetic codeine analog has mild opioid effect when used in excess. Can cause serotonin syndrome if combined with other serotonergic agents give naloxone if overdose

Question 425

Pseudoephedrine | Phenylephrine

Answer 425

α adrenergic agonist used in nasal decongestants Used to reduce hyperemia, edema, nasal congestion. Opens obstructed eustachian tubes AR: hypertension. rebound congestion if used more than 4-6 days. can also cause CNS stimulation/anxiety (pseudoephedrine)

Question 426

Bosentan

Answer 426

Endothelin receptor antagonists-pulmonary hypertension drugs decrease in pulmonary vascular resistance AR: hepatotoxic therefore monitor LFTs

Question 427

Epoprostenol | Iloprostenol

Answer 427

Prostacyclin analogs-pulmonary hypertension drugs PGI2 (prostacyclin) with direct vasodilatory effects on pulmonary and systemic arterial vascular beds inhibits platelet aggregation AR: flushing and jaw pain

Question 428

Albuterol

Answer 428

Asthma drug - target inflammatory processes and parasympathetic tone MOA: relaxes bronchial smooth mm via short acting beta1-agonist. Used during acute exacerbation

Question 429

Salmeterol | Formeterol

Answer 429

Asthma drug - target inflammatory processes and parasympathetic tone beta2agonist - long acting agents for prophylaxis of asthma symptoms AR: tremor and arrhythmia

Question 430

Fluticasone | Budesonide

Answer 430

inhaled corticosteroids inhibit the synthesis of virtually all cytokines. Inactivate NF-KB, the transcription factor that induces production of TNF alpha and other inflammatory agents first line therapy for chronic asthma can cause oral thrush therefore use spacer or rinse mouth after use

Question 431

Tiotropium | Ipratropium

Answer 431

Muscarinic antagonists Asthma drug - preventing bronchoconstriction used for COPD Tiotropium is long acting

Question 432

Zileuton

Answer 432

Antileukotrienes 5-lipoxygenase pathway inhibitor that blocks conversion of arachidonic acid to leukotrienes. Hepatotoxic

Question 433

Theophylline

Answer 433

Methylxanthines causes bronchodilation by inhibiting phosphodiesterase and increasing cAMP levels due to decrease in cAMP hydrolysis limited usage because there is a narrow therapeutic index (cardiotoxicity, neurotoxicity). SEIZURES and TACHYARYTHMIAS metabolized by cytochrome P450 Blocks actions of adenosine

Question 434

Cromolyn | Nedocromil

Answer 434

Mast cell stabilizers Prevent release of inflammatory mediators from mast cells. used for prevention of bronchospasm not for acute bronchodilation

Question 435

Methacholine

Answer 435

nonselective muscarinic receptor (M3) agonist used in brnchial challenge test to help diagnose asthma

Question 436

This drug decreases hepatic synthesis of TGs and VLDL levels and reduces clearance of HDL but puts you at risk of developing acute gouty arthritis

Answer 436

Niacin

Question 437

Class II antiarrhythmics antidote

Answer 437

tx overdose with saline, atropine, glucagon

Question 438

First line treatment for wilsons disease

Answer 438

D-penicillamine which contains a free sulfhydryl group and functions as a copper chelator

Question 439

first line treatment for lead poisoning

Answer 439

edate calcium disodium increases urinary excretion of lead

Question 440

first line treatment for iron overdose

Answer 440

deferoxamine binds iron and converts it to ferroxamine which is water soluble form

Question 441

first line treatment for cerebral toxoplasmosis

Answer 441

combination of pyrimethamine and sulfadiazine along with leucovorin (folinic acid)

Question 442

first line treatment for cerebral toxoplasmosis in someone with a sulfa allergy

Answer 442

pyrimethamine and clindamycin in case of sulfa drug hypersensitivity along with leucovorin (folinic acid).

Question 443

Antibiotics contraindicated in pregnancy

Answer 443

tetracyclines Chloramphenicol Trimethoprim/sulfamethoxazole Aminoglycosides

Question 444

Birth defect associated with tetracyclines

Answer 444

teeth staining

Question 445

Birth defect associated with chloramphenicol

Answer 445

gray baby

Question 446

Birth defect associated with trimethoprim/sulfamethoxazole

Answer 446

neural tube defects

Question 447

Birth defects associated with aminoglycosides

Answer 447

ototoxicity | vestibulotoxicity

Question 448

ACEi durigng pregnany

Answer 448

CONTRAINDICATED causes renal anuria, impairs renal function, and oligohydramnios

Question 449

What to give a patient with acute gouty arthritis that is in renal failure, has peptic ulcer disease, or cant take NSAIDS

Answer 449

colchicine which binds tubulin and prevents tubulin polymerization into microtubules. This impairs leukocyte migration and phagocytosis which decreases inflammation. But also neatively impacts GI mucosal cells MT formation causes diarrhea, vomiting, nausea, abdominal pain

Question 450

Erythropoiesis-stimulating agents (ESAs) side effects

Answer 450

erythropoietin darbepoetin alpha anemia of chronic kidney disease treatment AR: thromboembolic events and hypertension

Question 451

treatment for enterococcal endocarditis

Answer 451

aminoglycoside prevents formation of 30s intiation complex by preventing binding of formylmethionine-tRNA

Question 452

side effect for aminoglycosides

Answer 452

ototoxicity | nephrotoxicity

Question 453

What antibiotic do you use to treat extended spectrum beta lactamse producing e coli

Answer 453

carbapenems

Question 454

What is an adverse side effect of inhaled glucocorticoid use in asthma and how can you avoid it

Answer 454

oral cadidiasis use spacer with inhaelr or oral rinse

Question 455

What do you give a patient whose valsalva manuever hasfailed and for initial treatment of paroxysmal SVT

Answer 455

adenosine

Question 456

treatment for giant cell arteritis

Answer 456

monoclonal antibody against IL6 tocilizumab

Question 457

MEdications to avoid in patients with hypertrophic cardiomyopathy

Answer 457

Vasodilators because they decrease systemic vascular resistance (eg, dihydropyridine calcium channel blockers, nitroglycerin, and ACE inhibitors) and leading to decreased afterload and lower LV volumes. Diuretics decrease LV venous filling (preload) and also result in greater outflow obstruction. Patients with HCM have dynamic left ventricular outflow tract (LVOT) obstruction that worsens with decreased left ventricular (LV) volume (as can be caused by decreased preload and/or reduced systemic vascular resistance).

Question 458

first line treatment for malaria

Answer 458

chloroquine mefloquine is resistant

Question 459

malaria drugs

Answer 459

chloroquine mefloquine tovaquone-proguanil artemisinins P vivax and P ovale have dormant liver forms (hypnozoites) that require additional primaquine therapy.

Question 460

aminoglycoside resistnace mostly due to

Answer 460

antibiotic modifying enzymes add chemical groups to antibiotic and reduce ability to bind 16s ribosomal RNA within the 30S ribosomal subunit

Question 461

Loop diuretics cause

Answer 461

ototoxicity

Question 462

beta blocker overdose treatment

Answer 462

glucagon activates g protein coupled receptors in cardiac myocytes --> + adenylate cyclase --> increase cAMP --> Ca release --> Sa node firing --> increases HR and cardiac contractility --> increase HR and BP in minutes note: independent of adrenergic receptors

Question 463

first line treatment for arsenic poisoning (insecticides )

Answer 463

Dimpercaprol

Question 464

Immediate treatment for panic disorder note: normal healthy patient comes in shaking and saying "I feel like im going to die" and with chest pain

Answer 464

benzodiazepines

Question 465

long term treatment for panic disorder

Answer 465

SSRI/SNRI because takes weeks to take effect

Question 466

what drugs ppt withdrawal in opiod addicts

Answer 466

partial agonists/antagonists liek buprenorphine

Question 467

what antihypertensive medication is good for someone with proteinuria

Answer 467

ACEi and ARBS

Question 468

what seizure drug causes gingival hyperplasia

Answer 468

phenytoin

Question 469

phenytoin adverse effects

Answer 469

Phenytoin toxicity is mainly characterized by CNS manifestations. Its effect on the cerebellum and vestibular system can cause ataxia and nystagmus. Long-term therapy with phenytoin may cause gingival hyperplasia, coarsening of the facial features, and hirsutism. Phenytoin interferes with the metabolism of folic acid and may cause megaloblastic anemia. Phenytoin induces the P450 cytochrome oxidase system. It increases the metabolism—and therefore decreases the blood level—of many medications. If taken during pregnancy, phenytoin may cause fetal hydantoin syndrome.

Question 470

Most common adverse effect of statin use

Answer 470

myopathy can also cause hepatotoxicity (check liver function)

Question 471

IF patient has both absence and otnic clonic seizures

Answer 471

use valproate not ethosuximide

Question 472

amiodarone

Answer 472

think amIODarone 30% iodine and can cause thyroid adverse effects (hypothyroid or hyperthyroid)

Question 473

clozapine is for what kind of schizophrenia

Answer 473

treatment resistent (it has its CLOZ in your) neutropenia and agranulocytosis are the major adverse effect. Seizures too patients must have their neutrophil count continuosly measured

Question 474

first line treatments for bipolar

Answer 474

First-line medications for bipolar maintenance treatment include lithium, the anticonvulsant valproate, and the second-generation antipsychotic quetiapine.

Question 475

first line for narcolepsy

Answer 475

modafinil

Question 476

valproate use during preganancy can cause

Answer 476

neural tube defects

Question 477

Treatment for psoriasis that activates a nuclear transcription factor

Answer 477

calcipotriene vitamin D analog that binds the vitamin D receptor and inhibits keratinocyte proliferation and stimulate keritinocyte differentiation

Question 478

first line treatment for trigemnial nerualgia is

Answer 478

carbamazepine AR: SIADH and boen marrow suprression (aplastic anemia)

Question 479

treatment for lyme disease

Answer 479

early lyme: doxycyline | mid-late lyme: ceftriaxone

Question 480

What vitamin supplementation do you give to a pt with measles

Answer 480

vitamin A

Question 481

First line therapy for RA in DMARDS therapy

Answer 481

methotrexate

Question 482

Isotretinoin

Answer 482

potent teratogen and absolutely ocntraindicated in pregnancy requires a negative pregnancy test Retinoids

Question 483

Treatment for motion sickness

Answer 483

antimuscarinics (anticholinergics) antihistamines

Question 484

Treatment for chemotherapy induced emesis

Answer 484

dopamine receptor antagonists (D1) Serotonin receptor antagonists Neurokinin 1 receptor antagonists 5ht3 for GI upset H1 and M1 for motion sickness/vergibo D2 for emetogenic substances

Question 485

Treatment of acute agitation and psychosis in delirium for elderly

Answer 485

haloperidol "a halo because theyre old and close to the angels"

Question 486

treatment for cryptococcal meningitis

Answer 486

ampho B and flucytosine once pt stabilized do fluconazole

Question 487

treatmment for restless leg syndrome

Answer 487

dopamine agonists | treat iron deficiency because can imapct dopamine pathway

Question 488

treatment for cyanide toxicity due to nitroprusside

Answer 488

mitochondrial toxin that binds Fe3+ on cytochrome oxidase C inhibiting the electron transport chain bright red venous blood and lactic acidosis sodium thiosulfate is antidote (provides additional sulfur groupes for rhodanese enhancing CN detox)

Question 489

rifaxamin

Answer 489

nonabsorbable antibiotic that alters GI flora to decrease intenstinal productiona nd absorption of ammonia used with lactulose treats hepatic encephalopathy

Question 490

What to give ina spirochete infection

Answer 490

penicillin because gram - with peptidoglycan cell wall

Question 491

treatment of acute intermittent poryphyria

Answer 491

glucose hemin causing down regulation of ALAS

Question 492

preventing recurrnece of herpes outbreak via

Answer 492

daily valcyclovir, acyclovir, famciclovir

Question 493

treat serotonin syndrome with

Answer 493

seretonin receptor antagonists like cyproheptadine

Question 494

fidaxomicin

Answer 494

macrocyclic antibiotic inhibits sigma subunit of RNA polymerase for c diff

Question 495

Why are the elderly prone to benzo side effects

Answer 495

increased volume of distribution secondary to decreased total body water, decreased total body mass, and increased body fat reduced hepatic size and blood flow

Question 496

Why does cocaine cause nasal perforation

Answer 496

vasal congestion note: there is decreased REUPTAKE of NE, dopamine, and serotonin

Question 497

Major amiodarone side effects

Answer 497

Amiodarone (Class I,II,III,IV effects) INTERSTITIAL PNEUMONITIS Hepatoxicitiy (check PFT, LFT, and TFTs), Hypo/hyperthyroid Acts as hapten (corneal deposits and blue/gray deposits resulting in photodermatitis).

Question 498

ethylene glycol poisoning

Answer 498

flank pain hematuria oliguria high anion gap metabolic acidosis

Question 499

Drug that inhibit mTOR blocking cell cycle between the G1 to S phase to reduce smooth muscle cell proliferation over cardiac stents

Answer 499

everolimus prevents neointimal hyperplasia and stent restenosis

Question 500

Drugs that prolong the QT interval

Answer 500

``` Quinidine Procainamide Sotalol Amiodarone (LOWER RISK THAN OTHERS) Disopyramide Dofetilide Phenothiazine Tricyclic antidepressants ```

Question 501

What antihypertensive drugs cause dyslipidemia in patients?

Answer 501

metoprolol and thiazides

Question 502

How does phentolamine administration reverse the effects of epinephrine

Answer 502

Epinephrine is a nonselective alpha and beta adrenergic agonist that increases BP administration of phentolamine, a nonselective alpha-antagonist, and then readministration of epinephrine will cause stimulation of only beta receptors. This will drop BP

Question 503

The treatment of choice for pseudomonas pneumonia

Answer 503

double coverage with 2 or 3 of the following: - antipseudomonal beta lactam (or aztreonam) - aminoglycoside - respiratory fluoroquinolone

Question 504

How do beta blockers lower BP

Answer 504

- reducing myocardial contractility and heart rate - decreasing renin release by the kidneys (regulated by B1 receptors in juxtaglomerular cells) which prevents conversion of angiotensinogen to angiotensin I

Question 505

Adenosine and acetylcholine both have what effect on cardiac action potentials?

Answer 505

prolong phase 4 and reduce rate of spontaneous AP in pacemaker cells

Question 506

Neprilysin

Answer 506

metalloprotease that inactivates several peptide hormones, including bradykinin, glucagon, enkephalins, and natriuretic peptides

Question 507

All antidepressants carry a risk of inducing

Answer 507

mania in a susceptible patient (bipolar) antidepressants should be stopped and a mood stabilizer inititated

Question 508

Major side effect of bupropion note: no weight gain or sexual side effects is a positive (does not affect serotonin)

Answer 508

INHIBITS REUPTAKE OF NE AND DOPAMINE can cause seizures avoid in patients that suffer from anorexia, bulimia, or seizure disorders

Question 509

Treatment for enterobiasis due to E. vermicularis

Answer 509

Pinworm infection first line is albendazole second line In a pregnant patient is pyrantel pamoate

Question 510

Treatment for drug induced parkinsonism

Answer 510

- give benztropine (anticholinergic will reduce ach) and increase Dopamine to ach ratio - DO NOT give levodopa because will ppt psychotic features (i.e. if someone is on antipsychotic that antagonizes D2)

Question 511

Treatment for androgenic alopecia

Answer 511

Finasteride is a 5alpha-reductase inhibitor. Prevents conversion of testosterone to DHT

Question 512

Treatent for hypertensive crisis

Answer 512

fenoldopam selective dopamine 1 agonist arteriolar dilation, increased renal perfusion, promotes diuresis and natruises