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Step1 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

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

A

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

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2
Q

Mycophenolate and ribavirin

A

inhibits inosine monophosphate dehydrogenase

IMP –x—> GMP

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3
Q

Hydroxyurea

A

Inhibits ribonucleotide reductase in purine and pyrimidine synthesis in s phase

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

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4
Q

Methotrexate (MTX), trimethoprim (TMP), Pyrimethamine

A

inhibits dihydrofolate reductase (decrease dTMP)

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

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5
Q

5-fluorouracil (5-FU)

A

prodrug: capecitabine

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

cancer drug

AR:handfoot syndrome (palmarplantar erythrodysesthesia)

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6
Q

allopurinol and febuxostat

A

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

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7
Q

Actinomycin D

A

inhibits RNA polymerase in both prokaryotes and eukaryotes

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8
Q

Rifampin

A

inhibits DNA dependent RNA pol in prokaryotes

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9
Q

Quabain

A

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

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10
Q

digoxin and digitoxin

A

cardiac glycosides

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

increase in Ca concentrations

increased contractility

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11
Q

lumacaftor and ivacaftor

A

lumacaftor - corrects misfolded proteins and transport to cell surface

ivacaftor- opens Cl- channels

for CF

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12
Q

Fomepizole

A

FOMEpizole

inhibits alcohol dehydrogenase

For Overdose of Methanol or Ethylene Glycol

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13
Q

Disulfiram

A

DIScourage drinking by causing hangover

inhibits acetaldehyde dehydrogenase

acetaldehyde accumulates

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14
Q

Electron transport inhibitors

A

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)

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15
Q

ATP synthase inhibitors

A

oligomycin

increases proton gradient and no ATP produced

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16
Q

Cyclosporine

A

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

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17
Q

Tacrolimus

A

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

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18
Q

Sirolimus (Rapamycin)

A

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

AR: pancytopenia, not nephrotoxic

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19
Q

Basiliximab

A

immunosuppresant and for kidney transplant rejection prophylaxis

Blocks IL-2R

AR: edema, tremor, HTN

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20
Q

Azathioprine

A

Immunosuppresant

blocks lymphocyte proliferation by blocking nucleotide synthesis. “azathioPURINE”

degraded by xanthine oxidase

AR: panyctopenia

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21
Q

Mycophenolate

Mofetil

A

immunisuppresant

For lupus nephritis

inhibits IMP dehydrogenase –> preventing purine synthesis

Less nephrotoxic and neurotoxic

AR: pancytopenia, HTN, hyperglycemia

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22
Q

Glucocorticoids

A

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

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23
Q

Epoetin alfa (EPO analog)

A

Bome marrow stimulation
Erythropoietin

used for anemia

especially in renal failure

can cause an increased risk of thromboembolic events and hypertension

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24
Q

Filgrastim (G-CSF)

Sargramostim (GM-CSF)

A

Bone marrow stimulation

Used for leukopenia

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25
Q

Romiplostim

Eltrombopag

A

Bone marrow stimulation
Romiplostim is a TPO analog
Eltrombopag is a TPO receptor agonist “Pag=bag for TPO”

Used for autoimmune thrombocytopenia

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26
Q

Aldesleukoin

A

Immunotherapy of IL2

increases activity of T cells and NKC

used for renal cell carcinoma and metastatic melanoma

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27
Q

IFN-α

A

immunotherapy of interferon

Used for chronic hep B and renal cell carcinoma

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28
Q

IFN-β

A

immunotherapy of interferon

used for multiple sclerosis

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29
Q

IFNγ

A

immunotherapy of interferon

used for chronic granulomatous disease

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30
Q

Alemtuzumab

A

Therapeutic antibodies

Targets CD52

Used for CLL (chronic lymphocytic leukemia) and MS

think: aLYMtuzumab

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31
Q

Bevacizumab

A

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

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32
Q

Cetuximab

A

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

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33
Q

Rituximab

A

Therapeutic antibodies
Targets CD20

used for B cell non-hodgkin lymphoma, CLL, RA, ITP, multiple sclerosis

AR: progressive multifocal leukoencephalopathy

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34
Q

Trastuzumab

A

Therapeutic antibodies
Targets HER2
Breast cancer and gastric cancer

think HER2 –>tras2zumab

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35
Q

Adalimumab
Certolizumab
Golimumab
Infliximab

A

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

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36
Q

Daclizumab

A

Autoimmune disease therapy

Targets CD25 (part of IL-2 receptor)

Used for relapsing MS

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37
Q

Eculizumab

A

Autoimmune disease therapy

Targets complement protein C5

Used for paroxysmal nocturnal hemoglobinuria

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38
Q

Natalizumab

A

targets α4 integrin which is important for WBC adhesion

USed for MS, crohns disease

Risk of PML in patients with JC virus

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39
Q

Ustekinumab

A

Targets IL12 and IL23

Used for psoriasis and psoriatic arthritis

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40
Q

Abciximab

A

targets platelet glycoproteins IIb/IIIa

used as an antiplatelet agent

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41
Q

Denosumab

A

mimics osteoprotegerin and targets RANKL

think DenOSumab affects OSteoclasts in OSteoporosis

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42
Q

Digoxin immune Fab

A

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

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43
Q

Omalizumab

A

refractory allergic asthma thats not responding to inhaled steroids and long acting beta2agonists

prevents IgE binding for FcERI

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44
Q

Palivizumab

A

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

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45
Q

Penicillin

A

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

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46
Q

Amoxicillin

Ampicillin

A

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

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47
Q

Dicloxacillin
Nafcillin
Oxacillin

A

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

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48
Q

Piperacillin

Ticarcillin

A

Antipseudomonal penicillins

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49
Q

β-lactamase inhibitors

A

CAST

Clavulanic acid
Avibactam
Sulbactam
Tazobactam

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50
Q

Cephalosporins

A

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

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51
Q

First generation cephalosporins

A

Cefazolin - prior to surgery to prevent S aureus

Cephalexin

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52
Q

2nd gen cephalosporins

A

Cefaclor
Cefoxitin
Cefuroxime
Cefotetan

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53
Q

3rd gen cephalosporins

A

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

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54
Q

Cefepime

A

4th gen cephalosporins

gram (-) organisms with increased activity against pseudomonas and gram +

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55
Q

Ceftaroline

A

5th gen cephalosporin

Also covers Listeria, MRSA and enterococcus faecalis

does NOT cover pseudomonas

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56
Q

Doripenem
Imipenem
Meropenem
Ertapenem

A

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

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57
Q

Aztreonam

A

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

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58
Q

Vancomycin

A

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)

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59
Q 
Gentamicin
Neomycin
Amikacin
Tobramycin
Streptomycin
A

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

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60
Q

Tetracycline
Doxycycline
Minocycline

A

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

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61
Q

Tigecycline

A

Glycylcycline

MOA: Binds 30S

use: broad spectrum, multiresistant, and infections that require deep tissue penetration

AR: GI sx

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62
Q

Chloramphenicol

A

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

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63
Q

Clindamycin

A

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

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64
Q

Linezolid

A

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

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65
Q

Azithromycin
Clarithromycin
Erythromycin

A

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.

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66
Q

Colistin (polymyxin E), polymyxin B

A

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

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67
Q

Sulfamethoxazole (SMX)
Sulfisoxazole
Sulfadiazine

A

Sulfonamides

Inhibit dihydropteroate synthase in folate synthesis.

AR: tubulointerstitial nephritis, stevens johnson syndrome, kernicterus in infants

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68
Q

Dapsone

A

Similar to sulfonamides but structurally distint

use: Leprosy and prophylaxis for pneumocystis jirovecii

AR: hemolysis if G6PD deficient, methemoglobinemia

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69
Q

Trimethoprim

A

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

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70
Q

Ciprofloxacin
Enoxacin
Norfloxacin
Ofloxacin

Respiratory:
gemifloxacin
Levofloxacin
moxifloxacin

A

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.

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71
Q

Daptomycin

A

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

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72
Q

Metronidazole

A

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

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73
Q

Rifampin

Rifabutin

A

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

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74
Q

Isoniazid

A

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.

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75
Q

Pyrazinamide

A

prodrug of pyrazinoic acid
Works best at acidic pH

Use for mycobacterium tuberculosis

AR: hyperuricemia, hepatotoxicity

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76
Q

Ethambutol

A

MOA: decrease carb polymerization of mycobacterium cell wall by blocking arabinosyltransferase

use for mycobacterium tuberculosis

AR: optic neuropathy (red green colorblind). think “eyethambutol”

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77
Q

Streptomycin

A

MOA: interferes with 30S component of ribsosome

use: mycobacterium tuberculosis (2nd line)

AR: tinnitus, vertigo, ataxia, nephrotoxicity

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78
Q

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

A

amoxicillin

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79
Q

Prophylaxis for exposure to gonorrhea

A

Ceftriaxone

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

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80
Q

Prophylaxis for history of recurrent UTIs

A

TMP-SMX

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81
Q

Prophylaxis for exposure to meningococcal infection

A

ceftriaxone, ciprofloxacin, or rifampin

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82
Q

Prophylaxis for women carrying group B strep

A

intrapartum penicillin G or ampicillin

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83
Q

Prophylaxis for prevention of gonococcal conjunctivitis in newborn

A

Erythromycin ointment on eyes

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84
Q

Prophylaxis for prevention of postsurgical infection due to S aureus

A

Cefazolin

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85
Q

Prophylaxis for strep pharyngitis in child with prior rheumatic fever

A

Benzathine penicillin G or oral penicillin V

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86
Q

Prophylaxis for exposure to syphilis

A

Benzathine penicillin G

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87
Q

Prophylaxis for HIV patients <200

A

TMP-SMX for pneumocystis pneumonia

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88
Q

Prophylaxis for HIV patients <100

A

TMP-SMX for pneumocystis and toxoplasmosis

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89
Q

Prophylaxis for HIV patient <50

A

Azithromycin or clarithromycin for mycobacterium avium complex

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90
Q

Amphotericin B

A

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

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91
Q

Nystatin

A

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

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92
Q

Flucytosine

A

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

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93
Q 
Clotrimazole
Fluconazole
Isavuconazole
Itraconazole
Ketoconazole
Miconazole
Voriconazole
A

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)

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94
Q

Terbinafine

A

MOA: inhibits the fungal enzyme squalene epoxidase

use: dermatophytes, especially onychomycosis

AR: GI, headache, hepatotoxicity, taste disturbance

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95
Q

Anidulafungin
Caspofungin
micafungin

A

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)

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96
Q

Griseofulvin

A

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

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97
Q

Pyrimethamine

A

toxoplasmosis

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98
Q

Suramin

Melarsoprol

A

trypanosoma brucei

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99
Q

Nifurtimox

A

T cruzi

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100
Q

Sodium stibogluconate

A

leishmaniasis

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101
Q

Anti mite therapy used to tx scabies and mites

A

Permethrin- Inhibits Na channel deactivation –> neuronal membrane depolarization

Malathion- (acetylcholinesterase inhibitor)

Lindane- (blocks GABA channels –> neurotoxicity)

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102
Q

Chloroquine

A

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

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103
Q

Oseltamivir (tamiflu)

Zanamivir

A

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

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104
Q

Acyclovir
Famciclovir
Valacyclovir (prodrug of acyclovir, more bioavailable)

A

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

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105
Q

Ganciclovir

A

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)

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106
Q

Foscarnet

A

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 )

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107
Q

Cidofovir

A

MOA: preferentially inhibits viral DNA polymerase. Does not require phosphorylation by viral kinase

use: CMV retinitis in immunocompromised patients; acyclovir resistant HSV

AR: nephrotoxicity

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108
Q

HAART therapy

A

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)

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109
Q 
Abacavir (ABC)
Didanosine (ddl)
Emtricitabine (FTC)
Lamivudine (3TC)
Stavudine (d4T)
Tenofovir (TDF)
Zidovudine (ZDV)
A

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

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110
Q

Delavirdine
Efavirenz
Nevirapine

A

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

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111
Q 
Atazanavir
Darunavir
Fosamprenavir
Indinavir
Lopinavir
Ritonavir
Saquinavir
A

-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),

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112
Q

Dolutegravir
Elvitegravir
Raltegravir

A

-tegravir = integrase inhibitors

Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase

AR: increase in creatine kinase

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113
Q

Enfuvirtide

A

fusion inhibitor for HIV

binds gp41 and inhibits viral entry

think enFUvirtide inhibits FUsion

note: gp120 exoses underlying glycoprotein gp41 which mediates fusion

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114
Q

Maraviroc

A

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

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115
Q

Interferons

A

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

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116
Q

HCV is treated via monotherapy or polytherapy?

A

polytherapy!

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117
Q

Ledipasvir

A

TX for HCV

viral phosphoprotein (NS5A) inhibitor

NS5A plays important role in replication

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118
Q

Ribavirin

A

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

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119
Q

Simeprevir

A

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

photosensitiviy reactions

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120
Q

Sofosbuvir

A

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

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121
Q

Antibiotics to avoid in pregnancy:

Sulfonamides 
Aminoglycosides
Fluoroquinolones
Clarithromycin
Tetracyclines
Ribavirin
Griseofulvin
chloramphenicol
A 
Sulfonamides --> kernicterus
Aminoglycosides --> ototoxicity
Fluoroquinolones --> cartilage damage
Clarithromycin --> embryotoxic
Tetracyclines --> discolored teeth, inhibition of bone growth
Ribavirin- teratogen
Griseofulvin-teratogenic
chloramphenicol - gray baby syndrome
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122
Q

Sympathetic G protein linked second messengers

alpha1
alpha2
beta1
beta2
beta3
A

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”

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123
Q

Parasympathetic G protein linked second messengers

M1
M2
M3

A

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

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124
Q

Dopamine G protein linked second messengers

D1
D2

A

D1 (s) –> relaxes renal vascular smooth mm

D2 (i) –> modulates NT release in brain

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125
Q

Histamine G protein linked second messengers

H1
H2

A

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

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126
Q

Vasopressin G protein linked second messengers

V1
V2

A

V1 (q) –> increase vascular smooth mm contraction

V2(s) –> aquaporin2

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127
Q

Gq

A

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

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128
Q

Gs and Gi

A

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

Gi –> (-) adenylyl cyclase

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129
Q

Amphetamine MOA

A

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

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130
Q

Cholinomimetic agents

A

enhance the PNS

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

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131
Q

Bethanechol

A

Direct agonists (cholinomimetic agents)

activates bowel and bladder smooth mm

resistant to AChE

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132
Q

Carbachol

A

Direct agonists (cholinomimetic agents)

carbon copy of acetylcholine but resistant to AChE

Use for contricting pupil and relieving intraocular pressure in open angle glaucoma

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133
Q

Methacholine

A

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

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134
Q

Pilocarpine

A

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)

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135
Q

Donepezil
Rivastigmine
Galantamine

A

Indirect agonists (anticholinesterases)

increases ACh

used for alzheimers dz

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136
Q

Endrophonium

A 
Indirect agonists (anticholinesterases)
increase ACh

in past it was used to dx myasthenia gravis

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137
Q

Neostigmine

A 
Indirect agonists (anticholinesterases)
increase ACh

“neo” think No CNS penetration

used for myasthenia gravis, or NMJ blockade etc

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138
Q

Physostigmine

A 
Indirect agonists (anticholinesterases)
increase ACh

think phreely crosses BBB (only one that penetrates CNS and PNS)

antidote for anticholinergic toxicity from atropine overdose

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139
Q

Pyridostigmine

A 
Indirect agonists (anticholinesterases)
increase ACh

increases mm strength

think pyRIDostiGMine - gets RID of Myasthenia Gravis

does not penetrate CNS

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140
Q

Cholinesterase inhibitor poisoning

A

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

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141
Q

Atropine
Homatropine
Tropicamide

A

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

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142
Q

Benztropine

Trihexyphenidyl

A

Muscarinic agents

CNS

parkinsons dz and acute dystonia related to antipsychotics

“park my benz”

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143
Q

Glycopyrrolate

A

Muscarinic agents

GI and resp

preop to reduce airway secretions

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144
Q

Hyoscyamine

Dicyclomine

A

Muscarinic agents

GI

antispasmodics for IBS

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145
Q

Ipratropium

tiotropium

A

Muscarinic agents

Resp

COPD, asthma

“I pray to breathe soon”

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146
Q

Oxybutynin
Solifenacin
Tolterodine

A

Muscarinic agents

GI

reduce bladder spasms and urge urinary incontinence

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147
Q

Scopolamine

A

Muscarinic agents

CNS

motion sickness

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148
Q

Atropine

A

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

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149
Q

Albuterol
Salmeterol
Terbutaline

A

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

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150
Q

Dobutamine

A

Sympathomimetics with B1>B2 and alpha

HF, cardiogenic shock, cardiac stress testing

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151
Q

Dopamine

A

Sympathomimetic with D1=D2>B>A

unstable bradycardia, HF, shock

Alpha effects at high doses
Beta effects at low doses

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152
Q

Epinephrine

A

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)

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153
Q

Isoproterenol

A

Sympathomimetics

Beta1=Beta2

eval of tachyarrhythmias. worsens ischemia

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154
Q

Midodrine

A

Sympathomimetics

alpha1

autonomic insufficiency and postural HTN

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155
Q

Mirabegron

A

Sympathomimetics

Beta3

urinary urge incontinence or overactive bladder

“Mira begs ron” to get out of the bathroom”

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156
Q

Norepinephrine

A

Sympathomimetics

alpha1>alpha2>Beta1

Hypotension and septic shock

reflex bradycardia

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157
Q

Phenylephrine

A

Sympathomimetics

alpha1>alpha2

hypotension (vasoconstrictor), ocular procedures because mydriatic, rhinitis (decongestant), ischemic priapism

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158
Q

Amphetamine

A

indirect Sympathomimetics

indirect general agonist, reuptake inhib, releases stored catecholamines

good for ADHD, narcolepsy, obesity

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159
Q

Cocaine

A

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

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160
Q

Ephedrine

A

indirect Sympathomimetics

indirect general agonist and releases stored catecholamines

for nasal decongestion (pseudoephedrine), urinary incontinence, hypotension

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161
Q

Clonidine

Guanfacine

A

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

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162
Q

alpha-methyldopa

A

Sympatholytics (alpha2 agonists)

first line for HTN in pregnancy

AR: direct coombs + hemolysis, drug induced lupus

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163
Q

Tizanidine

A

Sympatholytics (alpha2 agonists)

Relief of spasticity, especially in MS

“TICanadine”

AR: Hypotension, weakness, xerostomia

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164
Q

Phenoxybenzamine

A

Nonselective alpha blocker

Irreversible. Used for pheochromocytoma (preop) to prevent catecholamine (Hypertensive) crisis

AR: ortho hypotension and reflex tachy

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165
Q

Phentolamine

A

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

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166
Q

Prazosin
Terazosin
Doxazosin
Tamsulosin

A

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

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167
Q

Mirtazapine

A

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

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168
Q 
Acebutolol
Atenolol
Betaxolol
Bisoprolol
Carvedilol
Esmolol
Labetalol
metoprolol
Nadolol
Nebivolol
pindolol
propanolol
timolol
A

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)

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169
Q

B1 selective blockers

A

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

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170
Q

Nonselective blockers

A

think 2nd half of the alphabet (N to Z)

B1=B2

nadolol,pindolol (partial), propranolol, timolol

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171
Q

Nonselective alpha and B antagonists

A

Have a different suffix of “-ilol and alol”

carvedilol
labetalol

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172
Q

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

A

Nebivolol

increases NO

activates NO synthase in the vasculature and decreases systemic vascular resistance

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173
Q

Drugs to avoid according to the beers criteria

A

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

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174
Q

Treatment for HTN with DM

A

ACEi and ARBs are protective against diabetic nephropathy

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175
Q

Treatment for HTN with asthma

A

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

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176
Q

Treatment for HTN in pregnancy

A

Hydralazine
Labetalol
Methyldopa
Nifedipine

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177
Q 
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

A

“-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

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178
Q

Hydralazine

A

MOA: increase cGMP –> smooth mm relaxation which vasodilates arterioles > veins.

Afterload reduction

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179
Q

Treatment of hypertensive emergency

A 
Clevidipine
fenoldopam
labetalol
nicardipine
nitroprusside
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180
Q

Nitroprusside

A

short acting

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

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181
Q

Fenoldopam

A

Dopamin D1 receptor agonist - coronary, peripheral, renal, and splanchnic vasodilation

decrease BP and increase natriuresis

use post op as antihypertensive

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182
Q

Nitroglycerin
Isosorbide dinitrate
Isosorbide mononitrate

A

Nitrates

vasodilate by increasing NO in vascular smooth mm –> increase in cGMP and smooth mm relaxation

Dilates veins&raquo_space;>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)

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183
Q

Ranolazine

A

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

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184
Q

Milrinone

A

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

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185
Q

Lovastatin

Pravastatin

A

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

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186
Q

Cholestyramine
Colestipol
Colesevelam

A

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

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187
Q

Ezetimibe

A

prevents cholesterol absorption at small intestine brush border

Decreases LDL, increases or nothing for HDL, Decreases or nothing for TG

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188
Q

Gemfibrozil
Bezafibrate
Fenofibrate

A

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

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189
Q

Niacin (B3)

A

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

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190
Q

Alirocumab

Evolocumab

A

PCSK9 inhibitors

MOA: inactivation of LDL receptor degradation, increasing amount of LDL removed from bloodstream

AR: myalgias, delirium, dementia, other neurocognitive effects

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191
Q

digoxin

A

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

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192
Q

Class I antiarrhythmics

A

slow or block conduction (esp in depolarized cells)

decrease phase 0 slope

selectively depress tissues that are frequently depolarized

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193
Q

Class IA antiarrhythmics

A

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

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194
Q

Lidocaine

Mexiletine

A

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

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195
Q

Flecainide

Propafenone

A

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

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196
Q 
Metoprolol
Propranolol
Esmolol (very short acting)
Atenolol
Timolol
Carvedilol

note: b1 is in renal and cardiac but not smooth mmemes

A

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

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197
Q

Amiodarone
Ibutilide
Dofetilide
Sotalol

A

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
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198
Q

Verapamil

Diltiazem

A

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

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199
Q

Adenosine

A

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

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200
Q

Ivabradine

A

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

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201
Q

What do you give for torsades and digoxin toxicity

A

Mg 2+

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202
Q

What is first line drug for DM type 2

A

metformin

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203
Q

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

A

Regular short acting insulin

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204
Q

Rapid acting insulin

A

1 hr peak

lispro
aspart
glulisine

there is no “LAG”

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205
Q

Short acting insulin

A

2 -3 hr peak

regular

206
Q

intermediate acting insulin

A

4-10 hr peak

NPH

207
Q

Long acting insulin

A

No real peak

detemir
glargine

208
Q

Pramlintide

A

amylin analog

decreases glucagon release, gastric emptying

increases satiety

For DM management

209
Q

Exenatide

Liraglutide

A

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

210
Q

Metformin

A

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

211
Q

Chlorpropamide

Tolbutamide

A

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

212
Q

Glimepiride
Glipizide
Glyburide

A

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

213
Q

Nateglinide

Repaglinide

A

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

214
Q

Linagliptin
Saxagliptin
Sitagliptin

A

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

215
Q

Pioglitazone

Rosiglitazone

A

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

216
Q

Canagliflozin
Dapagliflozin
Empagliflozin

A

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)

217
Q

Acarbose

Miglitol

A

inhibit intestinal brush border alpha glucosidases–> decrease postprandial hyperglycemia

AR: not recommended if kidney fx is impaired

218
Q

Thioamides

A

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

219
Q

Levothyroxine (T4)

Liothyronine (T3)

A

thyroid hormone replacement

used for hypothyroidism and myxedema

may be abused for weight loss

AR: similar to hyperthyroid sx

220
Q

Conivaptan

Tolvaptan

A

ADH antagonists - blocks action of ADH at V2 in SIADH

221
Q

Desmopressin

A

central DI, von willebrand disease, sleep enuresis, hemophilia A

helps central DI via adenylate cyclase

222
Q

GH

A

GH deficiency

turners syndrome

223
Q

Oxytocin

A

labor induction
milk letdown
controls uterine hemorrhage

224
Q

Somatostatin (octreotide)

A

Acromegaly, carcinoid syndrome, gastrinoma, glucagonoma, esophageal varices

225
Q

Demeclocycline

A

MOA: ADH antagonist (member of tetracycline family)

Used for SIADH

AR: nephrogenic DI, photosensitivity, abnormalities of bone and teeth

226
Q

Fludrocortisone

A

MOA: synthetic analog of aldosterone with little glucocorticoid effects
Use: mineralocorticoid replacement in primary adrenal insufficiency

AR: hyperpigmentation, HF exacerbations, similar to glucocorticoids

227
Q

Cinacalcet

A

MOA: sensitizes Ca sensing receptor (CaSR) in parathyroid gland and decrease PTH

“Cin-sitive for Calc-ium”

Used for refractory hypercalcemia

228
Q

Sevelamer

A

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”

229
Q

Cimetidine
Ranitidine
Famotidine
Nizatidine

A

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”

230
Q 
Omeprazole
Lansoprazole
Esomeprazole
Pantoprazole
Dexlansoprazole
A

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)

231
Q

Aluminum hydroxide unique side effects

A

antacid

constipation and hypophosphatemia
proximal mm weakness
osteodystrophy
seizures

“aluMINIMUM amount of feces”

232
Q

Calcium carbonate unique side effects

A

antacid

AR: rebound acid increase

can chelate and decrease effectiveness of other drugs

233
Q

Magnesium hydroxide unique side effects

A

antacid

diarrhea, hyporeflexia, cardiac arrest

MG= Must Go ….to bathroom

234
Q

Bismuth

Sucralfate

A

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”

235
Q

Misoprostol

A

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)

236
Q

Octreotide

A

long acting somatostatin analog

used for acute variceal bleeds, acromegaly, VIPoma, carcinoid tumors

increased risk of cholelithiasis due to CCK inhibition

237
Q

Sulfasalazine

A

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

238
Q

Loperamide

A

agonist at u-opioid receptors

low addictive potential (poor CNS penetration)

used for diarrhea

239
Q

Ondansetron

A

5-HT3 antagonist,

central acting

used for postop vomiting and cancer chemotherapy vimiting

AR: QT prolongation

240
Q

Metoclopramide

A

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

241
Q

Orlistat

A

Inhibits gastric and pancreatic lipase to reduce the absorption of dietary fat

use: weight loss

AR: decreased absorption off fat soluble vitamins

242
Q

aprepitant

A

substance P antagonist that blocks NK1 receptors in the brain

use: antiemetic for chemo induced

“a Prep for chemo nausea”

243
Q

Psyllium

Methylcellulose

A

bulk forming laxatives

soluble fiber draws water into lumen

244
Q

Magnesium hydroxide
Magnesium Citrate
Polyethylene glycol
Lactulose

A

Osmotic laxative

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

245
Q

Senna

A

Stimulants of enteric nerve cause colonic contraction

“Senna S-timulates EN-teric N-erves”

AR:melanosis coli

246
Q

Docusate

A

Emollients

promotes incorporation of water and fat in stool

“Doc-U-SAid I have water and fat in my stool???”

AR: diarrhea

247
Q

Cromolyn sodium

A

prevents mast cell degranulation (used for asthma prophylaxis)

248
Q

Dimercaprol

EDTA

A

first line treatment for foot and wrist drop associated with lead poisonin

“is there LEAD in my DIME”
“MDMA abuse LEADS to drugs”

249
Q

Succimer

A

chelation for kids with lead poisoning

“SUCks to be a kid who eats LEAD”

250
Q

Heparin

A

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)

251
Q

Heparin antidote

A

Protamine sulfate

“Herpes is (-) and needs (+) protamine”

Positively charged molecule that binds negatively charged heparin

252
Q

Low molecular weight heparin

  • enoxaparin
  • dalteparin
A

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

253
Q

Heparin induced thrombocytopenia (HIT)

A

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

254
Q

Direct thrombin inhibitors

A

Bivalirudin
Argatroban
Dabigatran (only oral agent)

255
Q

Warfarin

A

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

256
Q

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

A

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.

257
Q

How do you reverse warfarin

A

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)

258
Q

Apixaban

Rivaroxaban

A

Direct factor Xa inhibitors

Use: DVT, PE, Stroke

AR: not easy reversible

259
Q

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

A

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

260
Q

Clopidogrel
Prasugrel
Ticagrelor (reversible)
Ticlopidine

A

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)

261
Q

Cilostazol

Dipyridamole

A

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

262
Q

Abciximab
Eptifibatide
Tirofiban

A

MOA: Bind to the glycoprotein receptor IIb/IIIa

Use: unstable angina, percutaneous coronary intervention

263
Q

Cladribine

A

antimetabolites - cancer drug

MOA: purine analog

Use: Hairy cell leukemia “CLAN”

AR: myelosuppression, nephrotoxicity, and neurotoxicity

264
Q

Cytarabine (arabinofuranoyl cytidine)

A

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

265
Q

Methotrexate

A

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

266
Q

Bleomycin

A

Antitumor antibiotics

MOA: induces free radical formation which causes breaks in DNA strands

Use: testicular cancer, hodkin lymphoma

AR: pulmonary fibrosis

267
Q

Dactinomycin (actinomycin D)

A

Antitumor antibiotics

MOA: Intercalates into DNA, preventing RNA synthesis

Use: wilms tumor, ewing sarcoma, rhabdomyosarcoma. used for childhood tumors

268
Q

Doxorubicin

Daunorubicin

A

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

269
Q

Busulfan

A

Alkylating agents

MOA: cross linsk DNA

Use: used to ablate patients bone marrow before bone marrow transplantation

AR: pulmonary fibrosis

270
Q

Cyclophosphamide

Ifosfamide

A

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

271
Q

Nitrosoureas

A

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)

272
Q

Procarbazine

A

Alkylating agents

MOA: cell cycle phase - nonspecific alkylating agent,

Use: hodgkin lymphoma, brain tumors

AR: pulmonary toxicity

273
Q

Paclitaxel

Other Taxanes

A

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”

274
Q

Vincristine

Vinblastine

A

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

275
Q

Cisplatin

Carboplatin

A

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

276
Q

Etoposide

Teniposide

A

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”

277
Q

Irinotecan

Topotecan

A

MOA: inhibit topoisomerase I

(He had 1 TEa CAN TO POur)

Use: Colon cancer (irinotecan), ovarian and small cell lung ancers (topotecan)

278
Q

Erlotinib

A

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

279
Q

Imatinib

A

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

280
Q

Bortezomib

Carfilzomib

A

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

281
Q

Tamoxifen

Raloxifene

A

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

282
Q

Vemurafenib

A

“VEmuRAF-enib” is for “V600E-MUtated bRAF INHIBition”

Use: metastatic melanoma

283
Q

Rasburicase

A

MOA: recombinant urate oxidase that catalyzes metabolism of uric acid to allantoin

Use: prevention and treatment of tumor lysis syndrome (can also use allopurinol)

284
Q

Common chemotoxicity: Cisplastin/Carboplatin

A

Ototoxicity

Nephrotoxicity

285
Q

Common chemotoxicity: Vincristine

A

peripheral neuropathy

286
Q

Common chemotoxicity: Bleomycin, Busulfan

A

pulmonary fibrosis

287
Q

Common chemotoxicity: Doxorubicin

A

cardiotoxicity

288
Q

Common chemotoxicity: Trastuzumab (herceptin)

A

cardiotoxicity

289
Q

Common chemotoxicity: Cyclophosphamide

A

hemorrhagic CYstitis

290
Q

Acetaminophen

A

MOA: REVERSIBLY inhibits COX mostly in CNS

instead of aspirin to avoid Reye syndrome in children

291
Q

Aspirin

A

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

292
Q

Celecoxib

A

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

293
Q 
Ibuprofen
Naproxen
Indomethacin
Ketorolac
Diclofenac
Meloxicam
Piroxicam
A

NSAIDs

MOA: inhibit COX1 and COX2

Indomethacin is for PDA closure

294
Q

Leflunomide

A

MOA: reversibly inhibits dihydroorotate dehydrogenase, preventing pyrimidine synthesis. suppresses T cell proliferation

Use: RA, psoriatic arthritis

AR: hepatotoxic and teratogen

295
Q

Alendronate
Ibandronate
Risedronate
Zoledronate

A

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

296
Q

Teriparatide

A

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

297
Q

Probenecid

A

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

298
Q

Pegloticase

A

Chronic gout

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

299
Q

NSAIDs+ Glucocorticoids +Colchicine

A

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

300
Q

Etanercept

A

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

301
Q 
Diazepam
Lorazepam
Triazolam
Temazepam
Oxazepam
Midazolam
Chlordiazepoxide
A

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

302
Q

Phenobarbital
pentobarbital
thiopental
secobarbital

A

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

303
Q

Zolpidem
Zaleplon
Eszopiclone

A

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

304
Q

Suvorexant

A

MOA: orexin (hypocretin) receptor antagonist
use: insomnia

contraindicated in patients with strong CYP3A4 inhibitors

305
Q

Ramelteon

A

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

306
Q

Sumatriptan

A

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

307
Q

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

A

flumazenil (competitive antagonist at GABA benzodiazepine receptor)

308
Q

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

A

GABAa

Cl-

309
Q

What benzo is safe to give for liver dz patients

A

Oxazepam
Temazepam
Lorazepam

310
Q

What benzos have addictive potential

A

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

311
Q

Parkinson disease drugs

A

due to loss of dopaminergic neurons and excess cholinergic activity

Bromocriptine, Amantadine, Levodopa with carbidopa, selegiline and COMT inhibitors, antimuscarinics

(BALSA)

312
Q

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

A

Dopamine agonists for parkinsons dz

AR: impulse control disorder, postural hypotension, hallucinations/confusion

bromocriptine also used for hyperprolactinemia

313
Q

Amantadine

A

increase dopamine availability in parkinsons dz

increase release and decrease reuptake

AR: ataxia and livedo reticularis

314
Q

Selegiline

Rasagiline

A

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

315
Q

Entacapone

A

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

316
Q

Carbidopa/levodopa

A

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

317
Q

Tetrabenazine

Reserpine

A

MOA: inhibit vesicular monoamine transporter (VMAT) dopamine –> decreases vescile packaging and release

use: huntington chorea and tardive dyskinesia

318
Q

Riluzole

A

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

“riLOUzole”

319
Q

Memantine

A

for alzheimers

think memantine=memory and time

moa: NMDA receptor antagonist; helps prevent excitotoxicity (mediated by Ca)

AR: dizziness, confusion, hallucinations

320
Q 
Desflurane
Halothane
Enflurane
Isoflurane
Sevoflurane
Methoxyflurane
N2O
A

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)

321
Q

Thiopental

A

IV anesthetics

MOA: faciliatate GABAa by increasing duration

use: short surfical procedures

AR: decreased cerebral blood flow
high lipid solubility

322
Q

Midazolam

A

IV anesthetics

MOA: facilitate GABAa by increasing freq

use: procedural sedation and anesthesia induction

AR: severe postop rresp depression, decreased bp, anterograde amnesia

323
Q

Propofol

A

IV anesthetics

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

324
Q

Ketamine

A

IV anesthetics

MOA: NMDA receptor antagonist

use: dissociative anesthesia

AR: increased cerebral blood flow, emergence reaction possible with disorientation, hallucination, vivid dreams

325
Q

Procaine
Tetracaine
Benzocaine
Chloroprocaine

A

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

326
Q

Lidocaine
Mepivacaine
Bupivacaine
Ropivacaine

A

Amide local anesthetic (have two “I”)

given if allergic to esters

severe cardiovascular toxicity with bupivacaine

327
Q

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

A

lipid soluble

328
Q

Low solubility in blood for anesthetics

A

rapid induction and recovery times

329
Q

High solubility in lipids for anesthetics

A

increased potency = 1/MAC

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

330
Q

Malignant hypertension

A

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

331
Q

treatment for malignant hypertension

A

dantrolene a ryanodine receptor antagonist

332
Q

order of nerve blcokade

A

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

333
Q

Succinylcholine

A

depolarizing neuromuscular blocking drugs

MOA: strong ACh receptor agonist that produces a sustaine depol and prevents mm contraction

AR: hypercalcemia, SEVERE HYPERKALEMIA, malignant hyperthermia

334
Q 
Atracurium
Cisatracurium
pancuronium
Rocuronium
tubocurarine
vecuronium
A

Nondepolarizing neuromuscular blcoking drugs

335
Q

Dantrolene

A

MOA:prevents release of Ca from the SR of skeletal mm by binding to the ryanodine receptor

AR: malignant hyperthermia and neuroleptic malignant syndrome

336
Q

Baclofen

A

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

337
Q

Cyclobenzaprine

A

MOA: skeletal mm relaxant acts within the CNS

Use: muscle spasms

AR: anticholinergic side effects. Sedation

338
Q

Opiod analgesics

A

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

339
Q

Pentazocine

A

κ opioid agonist
μ opioid receptor weak antagonist or partial agonist

opioid withdrawal if also taking full opioid

340
Q

Butorphanol

A

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

341
Q

Tramadol

A

very weak opioid agonist that also inhibits 5-HT receptors

use: chronic pain

adverse effects: similar to opiods. decreases seizure threshold. serotonin syndrome

342
Q

Timolol
Betaxolol
Carteolol

A

Glaucoma drug - beta blcoker

decrease aq humor synthesis by epithelial cells

no pupilalry or vision changes

343
Q

Epinephrine
Apraclonidine
Brimonidine

A

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

344
Q

Acetazolamide

A

Glaucoma drug - diuretics

decrease aq humor synthesis via inhibition of carbonic anhydrase

no pupillar or vision changes

345
Q

Bimatroprost

Latanoprost

A

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

346
Q

pilocarpine
carbachol
physostigmine
echothiophate

A

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

347
Q

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

A

pilocarpine, a cholinomimetic (M3)

348
Q

Reversal of nondepolarizing neuromusuclar blocking drugs

i.e. side effect reversal due to tx of myasthenia gravis with cholinesterase inhibitors

A

neostigmine with atropine or glycopyrrolate

349
Q

morphine, heroin, meperidine, methadone, codeine

A

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

350
Q

buprenorphine

A

partial agonist - opioid

351
Q

Nalbuphine

pentazocine

A

mixed agonist/antagonist-opioid

352
Q

Naloxone
Naltrexone
Methylnaltrexone

A

antagonist -opioid

353
Q

which opioid is used for cough suppression

A

dextromethorphan

354
Q

which opioid is used to tx diarrhea

-note: slows motility

A

loperamide

diphenoxylate

355
Q

Opioid used for maintenance programs for heroin addicts

A

methadone
buprenorphine
naloxene

356
Q

opioid toxicity tx? relapse prevention?

A

naloxone

naltrexone once detoxed

357
Q

Benzodiazepines

A

first line for acute status epilepticus

MOA: increases GABAa action and postsynaptic chloride influx

358
Q

Carbamzepine

A

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

359
Q

Ethosuximide

A

USe: absence seizures

MOA: blocks thalamic T type Ca channels

AR:urticaria, steven johnson syndrome

360
Q

Gabapentin

A

used for partial focal seizures and peripheral neuropathy, postherpetic neuralgia

MOA: primarily inhibits high voltage activated Ca channels and designed as a GABA analog

361
Q

Lamotrigine

A

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

362
Q

Levetiracetam

A

used for partial/focal and tonic clonic seizures

AR: neuropsychiatric symptoms

363
Q

Phenobarbital

A

Used for partial(focal),tonic clonic, status epilepticus. First line in neonates “phenobabytal”

increases GABAa action

AR: dependence, cytochrome P450,cardioresp depression

364
Q

Phenytoin

Fosphenytoin

A

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

365
Q

Tiagabine

A

partial/tonic seizures

increase GABA by inhibiting reuptake

366
Q

Topiramate

A

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

367
Q

Valproic acid

A

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

368
Q

Vigabatrin

A

for partial/focal

increase GABA, irreversible GABA transaminase inhibitor

vigaBATrin

Permanent visual loss –> BLACK BOX WARNING

369
Q

first line for exlampsia seizures

A

MgSO4

370
Q

Preferred med for: ADHD

A

stimulants - methylphenidate and amphetamines

371
Q

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)

A

Benzodiazepines

372
Q

Preferred med for: bipolar disorder

A

Lithium, valproic acid, carbamazepine, lamotrigine, atypical antipsychotics

373
Q

Preferred med for: bulimia nervosa

A

SSRI

374
Q

Preferred med for: depression

A

SSRI

375
Q

Preferred med for: general anxiety disorder

A

SSRI and SNRI

376
Q

Preferred med for: OCD

A

SSRIs, venlafaxine, clomipramine

377
Q

Preferred med for: panic disorder

A

SSRI, venlafaxine, benzodiazepine

378
Q

Preferred med for: PTSD

A

SSRI

379
Q

Preferred med for: social anxiety disorder

A

SSRIs, venlafaxine

perforamnce only: beta blockers and benzodiazepines

380
Q

Preferred med for:Tourette syndrome

A

antipsychotics

381
Q

Methylphenidate
Dextroamphetamine
Methamphetamine

A

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

382
Q

Typical antipsychotics

A 
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

383
Q

Major adverse effects of typical antipsychotics

A

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

384
Q

Timeline of major adverse effects of typical antipsychotics

A

hours to days: acute dystonia

Days to months: akathisia (restlessness) and parkinsonism (bradykinesia)

Months to years: Tardive dyskinesia(orofacial chorea)

385
Q 
Aripiprazole
Asenapine
Clozapine
Olanzapine
Quetiapine
Iloperidone
Paliperidone
Risperidone
Lurasidone
Ziprasidone
A

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

386
Q

Lithium

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

A

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

387
Q 
Fluoxetine
Fluvoxamine
Paroxetine
Sertraline
Escitalopram
Citalopram
A

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

388
Q 
Venlafaxine
Desvenlafaxine
Duloxetine
Levomilnacipran
Milnacipran
A

serotonin-norepinephrine reuptake inhibitors

MOA: SNRIs inhibit 5-HT and NE reuptake

AR: increase BP, stimulant effects, sedation, nausea

389
Q

Tranylcypromine
Phenelzine
Isocarboxazid
Selegiline

A

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

390
Q 
Amitriptyline
Nortriptyline
Imipramine
Desipramine
Clomipramine
Doxepin
Amoxapine
A

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

391
Q

Methadone

A

opioid withdrawal and detox

long acting opiate used for heroin detox or long term maintenance therapy

392
Q

Buprenorphine + naloxone

A

opioid withdrawal and detox

sublingual buprenorphine (partial agonist) is absorbed and used for maintence therapy

Naloxone (antagonist) is added to lower IV abuse potential

393
Q

Naltrexone

A

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

394
Q

Trazodone

A

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

395
Q

Varenicline

A

Atypical antidepressant

Nicotinic ACh receptor partial agonist. Used for smoking cessation.

toxicity: sleep disturbances, may depress mood, Varenicline helps nicotine cravings decline

396
Q

Vilazodone

A

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

397
Q

Vortioxetine

A

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

398
Q

Acetazolamide

A

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)

399
Q

Furosemide
Bumetanide
Torsemide

MOST POTENT diuretics

A

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

400
Q

Ethacrynic acid

A

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”

401
Q

Thiazide diuretics

A

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

402
Q

Potassium sparing diuretics

A

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

403
Q

Captopril
Enalapril
Lisinopril
Ramipril

A

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

404
Q

Losartan
Candesartan
Valsartan

A

(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

405
Q

Aliskiren

A

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

406
Q

Leuprolide

A

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”

407
Q

Ethinyl estradiol
DES
Mestranol

A

Estrogens

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

408
Q

Raloxifene

A

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

409
Q

Anastrozole
Letrozole
Exemestane

A

Aromatase inhibitors

MOA: inhibit peripheral conversion of androgens to estrogen

Use:ER + breast cancer in postmenopausal women

410
Q 
Levonorgestrel
Medroxyprogesterone
Etonogestrel
Norethindrone
Megestrol
A

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

411
Q

Mifepristone

Ulipristal

A

Antiprogestins

MOA: competitive inhibitors of progestins at progesterone receptors

Use: termination of pregnancy (mifepristone with misoprostol). Emergency contraception (ulipristal)

412
Q

Copper intrauterine device

A

MOA: produces local inflammatory reaction toxic to sperm and ova, preventing fertilization and implantation, hormone free

AR: heavier or longer menses, dysmenorrhea.

413
Q

Danazol

A

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

414
Q

Testosterone

Methyltestosterone

A

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

415
Q

Tamsulosin

A

alpha1 antagonist used to treat BPH by inhibiting smooth mm contraction

selective for α1A/D receptors found on prostate vs vascular α1B receptors

416
Q

Sildenafil
Vardenafil
Tadalafil

A

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

417
Q

Flutamide

A

Nonsteroidal competitive inhibitor at androgen receptors

used for prostate carcinoma

418
Q

Ketoconazole

A

Inhibits steroid synthesis (inhibits 17,20 desmolase/17 alpha hydroxylase)

used in PCOS to reduce androgenic symptoms. can cause gynecomastia and amenorrhea

419
Q

Spironolactone

A

Inhibits steroid binding, 17,20 desmolase/17alpha hydroxylase

used in PCOS to reduce androgenic symptoms. can cause gynecomastia and amenorrhea

420
Q

Diphenhydramine
Dimenhydrinate
Chlorpheniramine

A

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

421
Q

Loratadine
Fexofenadine
Desloratadine
Cetirizine

A

Second generation histamine 1 blockers

use: allergy

AR: far less sedating that first gen because of decreased entry into CNS

422
Q

Guaifenesin

A

expectorant

thins respirator secretions

does not suppress cough reflex

423
Q

N-acetylcysteine

A

mucolytic - liquifies mucus in chronic bronchopulmonary disease by disrupting disulfide bonds

antidote for acetaminophen overdose

424
Q

Dextromethorphan

A

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

425
Q

Pseudoephedrine

Phenylephrine

A

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)

426
Q

Bosentan

A

Endothelin receptor antagonists-pulmonary hypertension drugs

decrease in pulmonary vascular resistance

AR: hepatotoxic therefore monitor LFTs

427
Q

Epoprostenol

Iloprostenol

A

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

428
Q

Albuterol

A

Asthma drug - target inflammatory processes and parasympathetic tone

MOA: relaxes bronchial smooth mm via short acting beta1-agonist. Used during acute exacerbation

429
Q

Salmeterol

Formeterol

A

Asthma drug - target inflammatory processes and parasympathetic tone

beta2agonist - long acting agents for prophylaxis of asthma symptoms

AR: tremor and arrhythmia

430
Q

Fluticasone

Budesonide

A

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

431
Q

Tiotropium

Ipratropium

A

Muscarinic antagonists

Asthma drug - preventing bronchoconstriction

used for COPD

Tiotropium is long acting

432
Q

Zileuton

A

Antileukotrienes

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

Hepatotoxic

433
Q

Theophylline

A

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

434
Q

Cromolyn

Nedocromil

A

Mast cell stabilizers

Prevent release of inflammatory mediators from mast cells.

used for prevention of bronchospasm not for acute bronchodilation

435
Q

Methacholine

A

nonselective muscarinic receptor (M3) agonist

used in brnchial challenge test to help diagnose asthma

436
Q

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

A

Niacin

437
Q

Class II antiarrhythmics antidote

A

tx overdose with saline, atropine, glucagon

438
Q

First line treatment for wilsons disease

A

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

439
Q

first line treatment for lead poisoning

A

edate calcium disodium

increases urinary excretion of lead

440
Q

first line treatment for iron overdose

A

deferoxamine

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

441
Q

first line treatment for cerebral toxoplasmosis

A

combination of pyrimethamine and sulfadiazine

along with leucovorin (folinic acid)

442
Q

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

A

pyrimethamine and clindamycin in case of sulfa drug hypersensitivity

along with leucovorin (folinic acid).

443
Q

Antibiotics contraindicated in pregnancy

A

tetracyclines
Chloramphenicol
Trimethoprim/sulfamethoxazole
Aminoglycosides

444
Q

Birth defect associated with tetracyclines

A

teeth staining

445
Q

Birth defect associated with chloramphenicol

A

gray baby

446
Q

Birth defect associated with trimethoprim/sulfamethoxazole

A

neural tube defects

447
Q

Birth defects associated with aminoglycosides

A

ototoxicity

vestibulotoxicity

448
Q

ACEi durigng pregnany

A

CONTRAINDICATED

causes renal anuria, impairs renal function, and oligohydramnios

449
Q

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

A

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

450
Q

Erythropoiesis-stimulating agents (ESAs) side effects

A

erythropoietin
darbepoetin alpha

anemia of chronic kidney disease treatment

AR: thromboembolic events and hypertension

451
Q

treatment for enterococcal endocarditis

A

aminoglycoside

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

452
Q

side effect for aminoglycosides

A

ototoxicity

nephrotoxicity

453
Q

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

A

carbapenems

454
Q

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

A

oral cadidiasis

use spacer with inhaelr or oral rinse

455
Q

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

A

adenosine

456
Q

treatment for giant cell arteritis

A

monoclonal antibody against IL6

tocilizumab

457
Q

MEdications to avoid in patients with hypertrophic cardiomyopathy

A

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).

458
Q

first line treatment for malaria

A

chloroquine

mefloquine is resistant

459
Q

malaria drugs

A

chloroquine
mefloquine
tovaquone-proguanil artemisinins

P vivax and P ovale have dormant liver forms (hypnozoites) that require additional primaquine therapy.

460
Q

aminoglycoside resistnace mostly due to

A

antibiotic modifying enzymes

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

461
Q

Loop diuretics cause

A

ototoxicity

462
Q

beta blocker overdose treatment

A

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

463
Q

first line treatment for arsenic poisoning (insecticides )

A

Dimpercaprol

464
Q

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

A

benzodiazepines

465
Q

long term treatment for panic disorder

A

SSRI/SNRI because takes weeks to take effect

466
Q

what drugs ppt withdrawal in opiod addicts

A

partial agonists/antagonists

liek buprenorphine

467
Q

what antihypertensive medication is good for someone with proteinuria

A

ACEi and ARBS

468
Q

what seizure drug causes gingival hyperplasia

A

phenytoin

469
Q

phenytoin adverse effects

A

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.

470
Q

Most common adverse effect of statin use

A

myopathy

can also cause hepatotoxicity (check liver function)

471
Q

IF patient has both absence and otnic clonic seizures

A

use valproate not ethosuximide

472
Q

amiodarone

A

think amIODarone

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

473
Q

clozapine is for what kind of schizophrenia

A

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

474
Q

first line treatments for bipolar

A

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

475
Q

first line for narcolepsy

A

modafinil

476
Q

valproate use during preganancy can cause

A

neural tube defects

477
Q

Treatment for psoriasis that activates a nuclear transcription factor

A

calcipotriene

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

478
Q

first line treatment for trigemnial nerualgia is

A

carbamazepine

AR: SIADH and boen marrow suprression (aplastic anemia)

479
Q

treatment for lyme disease

A

early lyme: doxycyline

mid-late lyme: ceftriaxone

480
Q

What vitamin supplementation do you give to a pt with measles

A

vitamin A

481
Q

First line therapy for RA in DMARDS therapy

A

methotrexate

482
Q

Isotretinoin

A

potent teratogen and absolutely ocntraindicated in pregnancy

requires a negative pregnancy test

Retinoids

483
Q

Treatment for motion sickness

A

antimuscarinics (anticholinergics)

antihistamines

484
Q

Treatment for chemotherapy induced emesis

A

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

485
Q

Treatment of acute agitation and psychosis in delirium for elderly

A

haloperidol

“a halo because theyre old and close to the angels”

486
Q

treatment for cryptococcal meningitis

A

ampho B and flucytosine

once pt stabilized do fluconazole

487
Q

treatmment for restless leg syndrome

A

dopamine agonists

treat iron deficiency because can imapct dopamine pathway

488
Q

treatment for cyanide toxicity due to nitroprusside

A

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)

489
Q

rifaxamin

A

nonabsorbable antibiotic that alters GI flora to decrease intenstinal productiona nd absorption of ammonia

used with lactulose

treats hepatic encephalopathy

490
Q

What to give ina spirochete infection

A

penicillin because gram - with peptidoglycan cell wall

491
Q

treatment of acute intermittent poryphyria

A

glucose
hemin

causing down regulation of ALAS

492
Q

preventing recurrnece of herpes outbreak via

A

daily valcyclovir, acyclovir, famciclovir

493
Q

treat serotonin syndrome with

A

seretonin receptor antagonists like cyproheptadine

494
Q

fidaxomicin

A

macrocyclic antibiotic

inhibits sigma subunit of RNA polymerase

for c diff

495
Q

Why are the elderly prone to benzo side effects

A

increased volume of distribution secondary to decreased total body water, decreased total body mass, and increased body fat

reduced hepatic size and blood flow

496
Q

Why does cocaine cause nasal perforation

A

vasal congestion

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

497
Q

Major amiodarone side effects

A

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).

498
Q

ethylene glycol poisoning

A

flank pain
hematuria
oliguria
high anion gap metabolic acidosis

499
Q

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

A

everolimus

prevents neointimal hyperplasia and stent restenosis

500
Q

Drugs that prolong the QT interval

A 
Quinidine
Procainamide
Sotalol
Amiodarone (LOWER RISK THAN OTHERS)
Disopyramide
Dofetilide
Phenothiazine
Tricyclic antidepressants
501
Q

What antihypertensive drugs cause dyslipidemia in patients?

A

metoprolol and thiazides

502
Q

How does phentolamine administration reverse the effects of epinephrine

A

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

503
Q

The treatment of choice for pseudomonas pneumonia

A

double coverage with 2 or 3 of the following:

  • antipseudomonal beta lactam (or aztreonam)
  • aminoglycoside
  • respiratory fluoroquinolone
504
Q

How do beta blockers lower BP

A
  • 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
505
Q

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

A

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

506
Q

Neprilysin

A

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

507
Q

All antidepressants carry a risk of inducing

A

mania in a susceptible patient (bipolar)

antidepressants should be stopped and a mood stabilizer inititated

508
Q

Major side effect of bupropion

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

A

INHIBITS REUPTAKE OF NE AND DOPAMINE

can cause seizures

avoid in patients that suffer from anorexia, bulimia, or seizure disorders

509
Q

Treatment for enterobiasis due to E. vermicularis

A

Pinworm infection

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

510
Q

Treatment for drug induced parkinsonism

A
  • 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)
511
Q

Treatment for androgenic alopecia

A

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

512
Q

Treatent for hypertensive crisis

A

fenoldopam

selective dopamine 1 agonist

arteriolar dilation, increased renal perfusion, promotes diuresis and natruises

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