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Pharmacology Flashcards

1
Q

Mechanism of Penicillins.

A

D-Ala-D-Ala structural analog binds PBP transpeptidases and blocks cross-linking of peptidoglycan cell wall - build-up of precursors cause activation of autolytic enzymes.

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2
Q

Gram+:
S. pneumo
S. pyogenes
Actinomyces

Gram- cocci:
N. meningitidis

Others:
T. pallidum

A

PROTOTYPE PENICILLINS

Penicillin G (IV/IM)
Penicillin V (PO)

May cause…
Hypersensitivity reactions
Directs Coombs+ hemolytic anemia

Resistance by…
B-lactamase (Penicillinase)

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3
Q

Gram+:
Listeria
Enterococcus

Gram-:
E. coli
Proteus
Salmonella
Shigella
HIB
H. pylori
A

PENICILLINASE-SENSITIVE PENICILLINS

Amoxicillin (greater oral bioavailability)
Amoxicillin-Clavulanate (Augmentin)
Ampicillin
Ampicillin-Sulbactam (Unasyn)

May cause…
Hypersensitivity reactions
Pseudomembranous colitis

Resistance by…
B-lactamase (Penicillinase)

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4
Q

Gram+

S. aureus (not MRSA)

A

PENICILLINASE-RESISTANT PENICILLINS

Bulky R group blocks binding of B-lactamase

Dicloxacillin
Nafcillin
Oxacillin

May cause…
Hypersensitivity reactions
Interstitial nephritis

Resistance by…
Altered PBP target site on MRSA
ESBL

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5
Q

Gram-:
Enteric rods
Pseudomonas

A

ANTIPSEUDOMONAL PENICILLINS

Piperacillin-Tazobactam (Zosyn)
Ticarcillin-Clavulanate (Co-Ticarclav)

May cause…
Hypersensitivity reactions

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6
Q

Mechanism of Cephalosporins.

A

D-Ala-D-Ala structural analog binds PBP transpeptidases and blocks cross-linking of peptidoglycan cell wall - Excess precursors cause activation of autolytic enzymes

More resistant to B-lactamases than Penicillins

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7
Q

Gram+:
Presurgical coverage of S. aureus
Cocci (staph/strep)

Gram-:
E. coli
Klebsiella
Proteus

A

1ST GENERATION CEPHALOSPORINS

Cefazolin
Cephalexin

May cause...
Hypersensitivity reactions
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vit K deficiency
Increases nephrotoxicity of Aminoglycosides

Resistance by…
Structural changes in PBP
ESBL

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8
Q

Gram+:
Cocci

Gram-:
E. coli
Klebsiella
Proteus
Neisseria
HIB
Enterobacter
Serratia
A

2ND GENERATION CEPHALOSPORINS

Cefaclor
Cefoxitin

May cause...
Hypersensitivity reactions
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vit K deficiency
Increases nephrotoxicity of Aminoglycosides

Resistance by…
Structural changes in PBP
ESBL

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9
Q

Serious Gram- infections

A

3RD GENERATION CEPHALOSPORINS

Ceftriaxone (Neisseria, disseminated Lyme)
Ceftazidime (Pseudomonas)

May cause...
Hypersensitivity reactions
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vit K deficiency
Increases nephrotoxicity of Aminoglycosides

Resistance by…
Structural changes in PBP
ESBL

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10
Q

Serious Gram- infections

Increased activity against Pseudomonas

A

4TH GENERATION CEPHALOSPORINS

Cefepime

May cause...
Hypersensitivity reactions
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vit K deficiency
Increases nephrotoxicity of Aminoglycosides

Resistance by…
Structural changes in PBP
ESBL

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11
Q

Broad Gram- and Gram+ coverage
MRSA
Does not cover Pseudomonas.

A

5H GENERATION CEPHALOSPORINS

Ceftaroline

May cause...
Hypersensitivity reactions
Autoimmune hemolytic anemia
Disulfiram-like reaction
Vit K deficiency
Increases nephrotoxicity of Aminoglycosides
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12
Q

Mechanism of Carbapenems.

A

D-Ala-D-Ala structural analog binds PBP transpeptidases and blocks cross-linking of peptidoglycan cell wall - build-up of precursors cause activation of autolytic enzymes

B-lactamase resistant

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13
Q

Life-threatening…
Gram+ cocci
Gram- rods (e.g. ESBL)
Anaerobes

A

CARBAPENEMS

Ertapenem
Meropenem (decreased seizure risk)
Imipenem-Cilastatin (decreased deactivation in renal tubules by dehydropeptidase I)

May cause…
GI distress
Skin rash
Seizures

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14
Q

Mechanism of Monobactams.

A

D-Ala-D-Ala structural analog binds PBP transpeptidases and blocks cross-linking of peptidoglycan cell wall - build-up of precursors cause activation of autolytic enzymes

More resistant to B-lactamases than Penicillins

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15
Q

Gram- rods for Penicillin-allergic patients, or those with renal insufficiency who can’t tolerate Aminoglycosides.

Note - Pseudomonal coverage

A

MONOBACTAMS

Aztreonam

May cause…
Occasional GI upset

Resistance by…
ESBL

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16
Q

Mechanism of Glycopeptides (Vancomycin, Bacitracin).

A

Inhibits cell wall peptidoglycan synthesis formation by binding D-ala-D-ala portion of cell wall glycoproteins - Prevents transpeptidase from making cross-links

B-lactamase resistant

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17
Q 
Serious Gram+:
MRSA (drug-resistant)
S. epidermidis (biofilm producing)
Enterococcus
Clostridium difficile (bacteriostatic)
A

VANCOMYCIN

May cause...
Nephrotoxicity
Ototoxicity
Thrombophlebitis
Flushing (Red Man Syndrome) - prevent with antihistamines

Resistance by…
Amino acid modification to D-ala-D-lac

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18
Q

Mechanism of Aminoglycosides.

A

Inhibits protein synthesis by irreversible inhibition of initiation complex via binding to 30S subunit

Misreading of mRNA

Synergistic with B-lactams/Vanc - Help it enter the cell

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19
Q

Severe Gram- rod infections (e.g. endocaditis)
Bowel surgery

Note - Ineffective against Anaerobes

A

AMINOGLYCOSIDES

Amikacin
Gentamycin
Neomycin (bowel surgery)
Streptomycin
Tobramycin
May cause..
Nephrotoxicity
Ototoxicity (with loop diuretic)
Neuromuscular blockade
Teratogen (Ototoxicity)

Resistance by…
Transferase inactivation of drug
Mutated Ribosome
Mutated Porin

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20
Q

Mechanism of Tetracyclines.

A

Inhibits protein synthesis by binding to 30S and preventing attachment of aminoacyl-tRNA.

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21
Q

Borrelia burgdorferi
Mycoplasma
Rickettsia/Chlamydia (intracellular accumulation)
Propionibacterium acnes

Do not take with milk (Ca), antacids (Ca, Mg) or Fe as divalent cations inhibit gut absorption

A

TETRACYCLINES

Tetracycline
Doxycycline (fecal elimination; renal failure patients)
Minocycline
Tigecycline (MRSA coverage)

May cause…
GI distress/Pill esophagitis
Photosensitivity
Teratogen (Teeth, Bone)

Resistance by…
Decreased uptake or increased efflux by plasmid-encoded transport pumps

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22
Q

Mechanism of Chloramphenicol.

A

Inhibits protein synthesis by blocking peptidyl transferase at 50S, preventing transfer of growing polypeptide strand to A site.

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23
Q

HIB meningitis
N. meningitidis
S. pneumo meningitis
Rickettsia rickettsii

Toxic but low cost

A

CHLORAMPHENICOL

May cause…
Dose dependent anemia
Dose independent aplastic anemia
Gray baby syndrome if premature (no UDPGT)

Resistance by…
Plasmid-encoded acetyltransferase inactivates drug

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24
Q

Mechanism of Clindamycin.

A

Inhibits protein synthesis by blocking peptide transfer at 50S subunit from A site to P site.

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25
Q

Anaerobes above the diaphragm:
Clostridium perfringens
Bacteroides (anaerobic lung abscess)

Gram+:
Invasive GAS pyogenes

A

CLINDAMYCIN

May cause…
Pseudomembranous colitis

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26
Q

Mechanism of Oxazolidinones.

A

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

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27
Q

Gram+ species including MRSA and VRE.

A

OXAZOLIDINONES

Linezolid

May cause…
Serotonin syndrome
Bone marrow suppression/Thrombocytopenia
Peripheral neuropathy

Resistance by…
Point mutation of rRNA

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28
Q

Mechanism of Macrolides.

A

Inhibit protein synthesis by binding to 23S rRNA of 50S subunit to block translocation.

Note - Fidaxomicin inhibits the sigma subunit of RNA polymerase instead

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29
Q

Atypical pneumonia (Myco/Legion/Chlamy)
Chlamydia
B. pertussis
Prophylaxis for mycobacterium avium (CD4 < 50)
Strep infections in Penicillin-allergic patients

Note - Increases serum concentration of anticoagulants
Note - Using a P450 inhibitor increases blood levels

A

MACROLIDES

Azithromycin
Clarithromycin (P450 inhibition)
Erythromycin (P450 inhibition)
Fidaxomicin (treats c. diff)

May cause...
Prolonged QT
Gastrointestinal motility issues
Cholestatic hepatitis
Rash
Eosinophilia
Myopathy with Statins (metabolized by P450)

Resistance by…
Methylation of 23S rRNA-binding site

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30
Q

Mechanism of Sulfonamides and Dapsone.

A

Inhibit folate synthesis via inhibition of dihydropteroate synthase.

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31
Q

Gram+
Gram-
Nocardia
Chlamydia

Displaces other drugs from albumin (e.g. Warfarin)

A

SULFONAMIDES

Sulfamethoxazole (SMX)
Sulfisoxazole
Sulfadiazine

May cause (slow acetylators)...
Hypersensitivity reactions
Photosensitivity
Hemolysis in G6PD deficiency
Tubulointerstitial nephritis
Kernicterus in infants

Resistance by…
Altered dihydropteroate synthase
Decreased uptake
Increased PABA (precursor) synthesis

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32
Q

Leprosy

A

DAPSONE

Combine with Rifampin

May cause…
Hemolysis in G6PD deficiency
Methemoglobinemia

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33
Q

Mechanism of Trimethoprim.

A

Inhibits folate synthesis by inhibiting Dihydrofolate Reductase and thus THF production

Note - Sulfamethoxazole inhibits an earlier enzyme (dihydropteroate synthetase)

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34
Q 
UTI (E. coli, Klebsiella, Proteus)
Salmonella
Shigella
Pneumocystis
Pneumocystis prophylaxis (CD4 < 200)
Toxoplasmosis prophylaxis (CD4 < 100)
Nocardia ("SNAP")
A

TRIMETHOPRIM-SULFAMETHOXAZOLE

May cause...
Megaloblastic anemia (folate deficiency)
Leukopenia (folate deficiency)
Granulocytopenia (folate deficiency)
Teratogen (neural tube defects)
Hyperkalemia
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35
Q

Mechanism of Fluoroquinolones.

A

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

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36
Q

Gram- rods (GU/GI)
Pseudomonas
Neisseria

Note - Do not take with milk (Ca), antacids (Ca, Mg) or Fe as divalent cations inhibit gut absorption

A

FLUOROQUINOLONES

Ciprofloxacin
Levofloxacin (Respiratory)

May cause...
Myalgia
Tendonitis/tendon rupture (>60 y/o, with prednisone)
Cartilage damage (children, pregnant/nursing mothers)
Prolonged QT
Skin rash
Headache and dizziness
GI upset

Resistance by…
Mutation in DNA gyrase or efflux pumps

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37
Q

Mechanism of Daptomycin.

A

Lipopeptide disrupts cell membrane of Gram+ cocci.

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38
Q

S. aureus (MRSA) cellulitis, bacteremia, endocarditis
VRE

Note - Cannot be used in pneumonia due to surfactant inactivation

A

DAPTOMYCIN

May cause…
Myopathy
Rhabdomyolysis

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39
Q

Mechanism of Metronidazole.

A

Forms toxic free radical metabolites which damage DNA.

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40
Q

Anaerobic infections below the diaphragm:
Clostridium difficile
Bacteroides

("GET Going on the METRO")
Giardia
Entamoeba
Trichomonas
Gardnerella vaginalis

Triple therapy for H. pylori

A

METRONIDAZOLE

May cause…
Disulfiram-like reaction
Metallic taste
Headache

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41
Q

Mechanism of Rifamycins.

A

Inhibits DNA-dependent RNA polymerase.

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42
Q

RIPE drug
Delay resistance to Dapsone when used for leprosy
Meningococcal prophylaxis
HIB chemoprophylaxis for close contacts

A

RIFAMYCINS

Rifampin (increased cytochrome P-450 - avoid in HIV)
Rifabutin (combine with Dapsone for leprosy)

May cause…
Orange body fluids

Resistance by…
Monotherapy rapidly leads to reduced binding to RNA polymerase

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43
Q

Mechanism of Isoniazid

A

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

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44
Q

RIPE drug
Only agent used as solo prophylaxis against TB
Monotherapy for latent TB
Given with Pyridoxine (vit B6)

A

ISONIAZID

May cause…
Hepatotoxicity (slow acetylators)
Vit B6 deficiency

Resistance by…
Underexpression of KatG

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45
Q

RIPE drug working in host phagolysosomes.

A

PYRAZINAMIDE

May cause…
Hepatotoxicity
Hyperuricemia

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46
Q

RIPE drug - Decreases carbohydrate polymerization (cell wall) by blocking arabinosyltransferase

A

ETHAMBUTOL

May cause...
Optic neuropathy (R-G color blindness)
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47
Q

Second line TB drug interfering with 30S component of ribosome.

A

STREPTOMYCIN

May cause...
Tinnitus
Vertigo
Ataxia
Nephrotoxicity
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48
Q

Prophylaxis for patients at high risk of endocarditis.

A

Amoxicillin

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49
Q

Prophylaxis for history of recurrent UTIs.

A

TMP-SMX

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50
Q

Prophylaxis following exposure to meningococcal infection.

A

Ceftriaxone
Ciprofloxacin
Rifampin

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51
Q

Prophylaxis for…
Pregnant women with GBS
Strep pharyngitis with prior rheumatic fever
Exposure to syphilis

A

Penicillin G

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52
Q

Treatment for multidrug resistant Pseudomonas or Acinetobacter.

A

Polymyxins B and E (colistin)

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53
Q 
Serious systemic mycoses (intrathecally for meningitis)...
Aspergillosis
Histoplasma
Blastomyces
Coccidioides
Cryptococcus
Candida
Mucor
A

AMPHOTERICIN B

Binds ergosterol (unique to fungi) forming membrane pores that allow leakage of electrolytes through cell wall

Supplement K and Mg because of altered renal tubule permeability

May cause...
Fever/chills (shake and bake)
Hypotension
Nephrotoxicity (hydrate)
Electrolyte abnormalities
Anemia (low EPO)
IV phlebitis
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54
Q

Rinse for oral candidiasis

Topical for diaper or vaginal candidiasis

A

NYSTATIN

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

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55
Q

Systemic fungal infections

Cryptococcal meningitis with AmphoB

A

FLUCYTOSINE

Inhibits DNA and RNA biosynthesis by conversion to 5-fluorouracil by cytosine deaminase

May cause…
Bone marrow suppression

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56
Q

Mechanism and side effects of Azoles.

A

Inhibit fungal Ergosterol synthesis via inhibition of cytochrome P-450 - Converts Lanosterol to Ergosterol

May cause…
Testosterone synthesis inhibition (i.e. Ketoconazole)
Liver dysfunction

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57
Q

Chronic suppression of cryptococcal meningitis in AIDS

Candidal infections

A

Fluconazole

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58
Q

Blastomyces
Coccidioides
Histoplasma

A

Itraconazole

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59
Q

Topical fungal infections

A

Clotrimazole

Miconazole

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60
Q

Dermatophytoses (i.e. onychomycosis)

A

TERBINAFINE

Inhibits fungal enzyme Squalene Epoxidase - Inhibiting Ergosterol synthesis

May cause...
Hepatotoxicity
Taste disturbance
GI upset
Headaches
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61
Q

Mechanism of Echinocandins.

A

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

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62
Q

Invasive aspergillosis

Candida

A

ECHINOCANDINS

Caspofungin
Anidulafungin
Micafungin

May cause…
Flushing (histamine release)
GI upset

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63
Q

Oral treatment of superficial infections especially dermatophytes (tinea, ringworm).

A

GRISEOFULVIN

Interferes with microtubule function disrupting mitosis - deposits in keratin-containing tissues

May cause...
Teratogenic
Carcinogenic
Confusion
Headaches
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64
Q

Mechanism and side effects of scabies and lice (Pediculus, Pthirus) treatment.

(“PML NAGs you”)

A

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

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65
Q

Treatment of plasmodial species other than P. falciparum.

A

CHLOROQUINE

Blocks detoxification of heme into hemozoin - heme accumulates and is toxic to plasmodium

Resistance in P. falciparum due to membrane pump that decreases intracellular concentration

May cause…
Retinopathy
Pruritus

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66
Q

Treatment of P. falciparum.

A

Mefloquine
Atovaquone/Proguanil
Artemether/Lumefantrine

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67
Q

Treatment of life-threatening malaria.

A

Quinidine

Artesunate

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68
Q

Treatment and prevention of Influenza A/B.

A

OSELTAMIVIR, ZANAMIVIR

Inhibits influenza neuraminidase - Impaired release of viral progeny

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69
Q

Mechanism and adverse effects of -cyclovirs

Includes…
Acyclovir
Valacyclovir
Famciclovir

A

Guanosine nucleoside analogs that are monophosphorylated by HSV/VZV Thymidine Kinase leading to DNA chain termination - Not phosphorylated in uninfected cells and so few adverse effects

May cause…
Obstructive crystalline nephropathy/ARF (hydration)

Resistance by…
Mutated viral thymidine kinase

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70
Q

CMV in immunocompromised patients.

A

GANCICLOVIR

5’-monophosphate nucleoside formed by CMV viral kinase - Preferentially inhibits viral DNA polymerase

May cause…
Bone marrow suppression (leukopenia, neutropenia, thrombocytopenia)
Renal toxicity

Resistance by…
Mutated viral kinase

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71
Q

Ganciclovir-resistant CMV
Acyclovir-resistant HSV

Note - Pyrophosphate analog

A

FOSCARNET

Does not require viral kinase

May cause...
Nephrotoxicity
Hypocalcemia (calcium chelator)
Hypomagnesemia
Seizures

Resistance by…
Mutated DNA polymerase

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72
Q

Ganciclovir-resistant CMV retinitis
Acyclovir-resistant HSV

Note - Nucleotide analog

A

CIDOFOVIR

Does not require viral kinase

May cause…
Nephrotoxicity (given with Probenecid and IV NaCl)

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73
Q

Ideal regimen for HAART.

A

2 NRTIs + 1 integrase inhibitor

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74
Q

Mechanism and adverse effects of NRTIs

Includes...
Tenofovir
ZiDOVudine
LAMivudine
ABACAvir
DIDanosine
EMtricitabine
A

Competitively inhibit nucleotide binding to reverse transcriptase and terminate chain (lack 3’ OH) - Only Tenofovir (nucleotide) does not need to be phosphorylated

May cause...
Bone marrow suppression (give G-CSF)
Type IV hypersensitivity with HLA-B57:01 (Abacavir)
Lipodystrophy
Pancreatitis (Didanosine)
Lactic acidosis (not Tenofovir)
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75
Q

NRTI for general prophylaxis and during pregnancy.

A

Zidovudine

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76
Q

Adverse effects of NNRTIs

Includes…
EfaVIRenz
NeVIRapine
DelaVIRdine

A

Bind at different site than NRTIs - do not require phosphorylation

May cause...
SJS-TEN
Hepatotoxicity
Vivid dreams (Efavirenz)
Teratogen (Efavirenz, Delavirdine)
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77
Q

Mechanism of Protease Inhibitors (-NAVIR).

A

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

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78
Q

Protease inhibitor which can boost other drug concentrations by inhibiting cytochrome P-450.

A

RITONAVIR

Alternatively - Rifampin contraindicated with PIs due to induction of P-450

May cause...
Hyperglycemia
Lipodystrophy (Cushing-like)
GI intolerance
Nephropathy
Hematuria (Indinavir)
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79
Q

Mechanism of integrase inhibitors (-Gravir).

A

Inhibits HIV genome integration into host cell - Prevent mRNA transcription by RNA Pol III

May cause…
Elevated CK

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80
Q

Mechanism of fusion inhibitors (EnFUvirtide, Maraviroc).

A

Maraviroc binds CCR5 on surface of T cells/monocytes inhibiting interaction with gp120

Enfuvirtide binds gp41 inhibiting viral entry

May cause…
Skin reaction at injection site

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81
Q

Chronic HBV, HCV
Kaposi sarcoma
Hairy cell leukemia
Condyloma cuminatum

A

INF-A

IFN-b used in MS, and IFN-y used in CGD

May cause...
Flu-like symptoms
Depression
Neutropenia
Myopathy
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82
Q

Treats HCV by inhibiting synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate dehydrogenase.

A

RIBAVIRIN

May cause…
Hemolytic anemia
Severe teratogen

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83
Q

Treats HCV by inhibiting RNA-dependent RNA polymerase acting as a chain terminator.

A

SOFOSBUVIR

Not monotherapy - use with Ribavirin or Peginterferon alfa

May cause…
Fatigue
Headaches
Nausea

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84
Q

Treats HCV by inhibiting protease preventing viral replication.

A

SIMEPREVIR

Not monotherapy - use with Ledipasvir (NS5A inhibitor)

May cause…
Photosensitivity
Rash

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85
Q 
Mechanism of action of...
Alcohol
Chlorhexidine
Hydrogen Peroxide
Iodide
A

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

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86
Q

Antibiotics to avoid in pregnancy.

“SAFe Children Take Really Good Care”

A 
Sulfonamides (kernicterus, neural tube)
Aminoglycosides (ototoxicity)
Fluoroquinolones (cartilage damage)
Clarithromycin (embryotoxic)
Tetracycline (discolored teeth, inhibition of bone growth)
Ribavirin (teratogen)
Griseofulvin (teratogen)
Chloramphenicol (gray baby syndrome)
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87
Q

Bactericidal antibiotics

“Very Finely Proficient At Cell Murder”

A 
Vancomycin
Fluoroquinolones
Penicillin
Aminoglycosides
Cephalosporins
Metronidazole

Also…
TMP-SMX

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88
Q

Relationship of Km and Vmax in Michaelis-Menten plot.

A

Km = [S] at 1/2Vmax

Km = Inversely related to affinity of the enzyme for its substrate (i.e less substrate required to reach 1/2Vmax)

Vmax = directly proportional to enzyme concentration

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89
Q

Km, Vmax, and slope in Lineweaver-Burk plot.

A 
Slope = Km/Vmax
1/Vmax = y-intercept
-1/Km = x-intercept

Noncompetitive inhibitors change y-intercept
Competitive inhibitors change x-intercept

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90
Q

Effect of reversible competitive antagonists
Resembles substrate
Binds active site
Overcome by increasing [S]…

Vmax
Km/EC50
Pharmacodynamics

A

Unchanged
Increased
Decreased potency

E.g. Flumazenil

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91
Q

Effect of irreversible competitive antagonists
Resembles substrate
Binds active site
Not overcome by increasing [S]…

Vmax
Km/EC50
Pharmacodynamics

A

Decreased
Unchanged
Decreased efficacy

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92
Q

Effect of noncompetitive antagonists
Does not resemble substrate
Does not bind active site
Not overcome by increasing [S]…

Vmax
Km/EC50
Pharmacodynamics

A

Decreased
Unchanged
Decreased efficacy

E.g. Phenoxybenzamine

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93
Q

Volume of distribution (Vd).

A

Amount in body/Amount in plasma

Low = 3-5 L (plasma)
Medium = 15 L (interstitial)
High = 40 L (intracellular)
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94
Q

Effect of liver and kidney disease on Vd (decreased protein binding).

A

Increased Vd

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95
Q

Vd of large/charged molecules and plasma bound proteins.

A

Low (blood)

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96
Q

Vd of small hydrophilic molecules.

A

Medium (CSF)

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97
Q

Vd of small lipophilic molecules, especially if bound to tissue protein.

A

Large (all tissues including fat)

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98
Q

Clearance (CL).

A

Rate of elimination/Plasma concentration

OR

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

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99
Q

Half-life for first-order kinetics drug.

A

(0.7 x Vd)/CL

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

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100
Q

Loading dose.

A

(Cp x Vd)/F

Cp = target plasma concentration at steady state
F = bioavailability or (AUC PO x IV dose)/(AUC IV x PO dose)

Unchanged in renal/liver disease

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101
Q

Maintenance dose.

A

(Cp x CL x T)/F

T = dosage interval if not administered continuously

Decreased in renal/liver disease

Note - CL and T should match in units (minutes or hours)

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102
Q

Type of interaction describing required presence of cortisol for full effect of catecholamine response.

A

Permissive interaction

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103
Q

Acute decrease in response to a drug after initial/repeated administration (MDMA, LSD).

A

Tachyphylactic

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104
Q

Difference between additive and synergistic interactions.

A

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

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105
Q

Rate of elimination is constant regardless of Cp (plasma concentration) - constant amount of drug is eliminated per unit time so that Cp decreases linearly with time.

A

ZERO-ORDER ELIMINATION

Capacity-limited elimination - Phenytoin, Ethanol, ASA at toxic doses

Half-life is not constant - decreases with decreasing concentration

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106
Q

Rate of elimination is directly proportional to Cp - constant fraction of drug is eliminated per unit time so that Cp decreases exponentially with time.

A

FIRST-ORDER ELIMINATION

Flow-dependent elimination - most drugs

Half-life is constant

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107
Q

Mechanism of NaHCO3 induced elimination of weak acids (ASA, Phenobarbital, Methotrexate).

A

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

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108
Q

Mechanism of NH4Cl induced elimination of weak bases (Amphetamines).

A

Trapped in acidic environment - acidification of a weak base (deprotonated B) makes species charged (protonated BH+), trapping it in the urine for elimination

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

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109
Q

Phase I drug metabolism - lost in geriatric patients.

A

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

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110
Q

Phase II drug metabolism - maintained in geriatric patients.

A

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

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111
Q

Pharmacokinetic measure of efficacy - maximum effect a drug can have.

A

Vmax - Increased y-value = increased Vmax

Partial agonists have less efficacy than full agonists

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112
Q

Pharmacokinetic measure of potency - amount needed for a given effect.

A

EC50 - left-shifting = decreased EC50 = increased potency

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113
Q

Effect of partial agonist
Binds active site…

Vmax
Km/EC50
Pharmacodynamics

A

Decreased
Independent
Decreased efficacy

E.g. Buprenorphine

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114
Q

Therapeutic index.

A

TD50/ED50

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115
Q

Therapeutic window

A

TD50 - ED50

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116
Q

Only sympathetic target organs innervated by cholinergic fibers.

A 
Sweat glands (M)
Adrenal medulla (Nn - same as autonomic ganglia)
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117
Q

Innervation type and receptor for somatic system.

A

Cholinergic innervation

Nm receptor

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118
Q

Mechanism of nicotinic Ach receptors.

A

Ligand-gated Na/K channels

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119
Q

Increased vascular smooth muscle contraction (inc. SBP)
Increased pupillary dilator muscle contraction (mydriasis)
Increased intestinal/bladder sphincter muscle contraction

A

a1

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120
Q 
Decreased adrenergic outflow
Decreased insulin release
Decreased lipolysis
Decreased aqueous humor production
Increased platelet aggregation
A

a2

Autoreceptor - often on presynaptic membrane for feedback inhibition

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121
Q

Increased heart rate
Increased contractility
Increased renin release
Increased lipolysis

A

b1

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122
Q 
Vasodilation (dec. DBP)
Bronchodilation
Increased insulin release
Increased lipolysis
Increased aqueous humor production
Decreased uterine tone (tocolysis)
Decreased ciliary muscle tone
A

b2

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

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123
Q

Increased lipolysis

Increased thermogenesis in skeletal muscle

A

b3

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124
Q

Parasympathetic receptor acting in CNS and enteric nervous system

A

M1

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125
Q

Decreased heart rate

Decreased atrial contractility

A

M2

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126
Q

Bronchoconstriction
Increased exocrine gland secretion
Increased insulin secretion
Increased gut peristalsis
Increased bladder contraction
Increased pupillary sphincter muscle contraction (miosis)
Increased ciliary muscle contraction (accommodation)

A

M3

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127
Q

Receptor relaxing renal vascular smooth muscle

A

D1

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128
Q

Receptor modulating transmitter release (CNS)

A

D2

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129
Q 
Increased nasal and bronchial mucus production
Increased vascular permeability
Increased contraction of bronchioles
Pruritus
Pain
A

H1

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130
Q

Receptor increasing gastric acid secretion in addition to M3

A

H2

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131
Q

Receptor increasing vascular smooth muscle contraction in addition to a1

A

V1

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132
Q

Receptor increasing H2O permeability and resorption in collecting tubules of kidneys

A

V2

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133
Q

G-protein class of all G-protein-linked 2nd messengers - a1, a2, b1, b2, b3, M1, M2, M3, D1, D2, H1, H2, V1, V

(“After QISSeS you get a QIQ out of SIQ Super Qinky Sex”)

A 
a1 = q
a2 = i
b1 = s
b2 = s
b3 = s
M1 = q
M2 = i
M3 = q
D1 = s
D2 = i
H1 = q
H2 = s
V1 = q
V2 = s
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134
Q

Mechanism of Gq receptors

A

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

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135
Q

Mechanism of Gs receptors

A 
Activates Adenylate cyclase
Converts ATP to cAMP
Activates Protein Kinase A
Phosphorylation of Phospholamban
Increased Ca influx
Increased inotropy

cAMP-dependent Protein Kinase A (PKA) activated
Inhibition of Myosin light chain kinase
Vasodilatation

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136
Q

Mechanism of Gi receptors

A

Inhibition of Adenylate cyclase

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137
Q

NE/Amphetamine interaction in synaptic cleft

A

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

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138
Q

Mechanism for hypertensive crisis in patients taking MAOi

A

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

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139
Q

Mechanism of Reserpine

A

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

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140
Q

Mechanism and use of Bethanechol

A

Cholinomimetic - Activates bowel and bladder smooth muscle (M3) and is resistant to AChE

Postoperative ileus
Neurogenic ileus
Urinary retention

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141
Q

Mechanism and use of Carbachol

A

Cholinomimetic direct agonist - Copy of acetylcholine

Glaucoma

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142
Q

Mechanism and use of Methacholine

A

Cholinomimetic direct agonist - Stimulates muscarinic receptors in airway when inhaled

Asthma challenge test

143
Q

Mechanism and use of Pilocarpine

A

Cholinomimetic direct agonist…
Contracts ciliary muscle of eye
Contracts pupillary sphincter

Open-angle glaucoma (ciliary)
Closed-angle glaucoma (pupillary)
Xerostomia in Sjogren’s (sweat, tears, saliva)

Note - Resistant to AchE

144
Q

Mechanism and use of Donepezil, Galantamine, and Rivastigmine

A

Cholinomimetic indirect agonist/anticholinesterase

Alzheimer’s

Note - Can also treat with Vit E (antioxidant)

145
Q

Mechanism and use of Edrophonium

A

Cholinomimetic indirect agonist/anticholinesterase

Diagnosis of Myasthenia Gravis - If response then increase AchEi dose, if no response then cholinergic crisis and stop AchEi

146
Q

Mechanism and use of Neostigmine

A

Cholinomimetic indirect agonist/anticholinesterase

No CNS penetration (quaternary amine)
Postoperative ileus
Neurogenic ileus
Urinary retention
Myasthenia gravis
Postoperative NMJ blockade reversal
147
Q

Mechanism and use of Physostigmine

A

Cholinomimetic indirect agonist/anticholinesterase

Crosses blood-brain barrier (tertiary amine)
Atropine overdose

148
Q

Mechanism and use of Pyridostigmine

A

Cholinomimetic indirect agonist/anticholinesterase

No CNS penetration (quaternary amine)
Myasthenia gravis

149
Q

Diseases exacerbated by cholinomimetic agents.

A 
Asthma (M3 bronchoconstriction)
COPD (M3 bronchoconstriction)
Peptic ulcers (M3 exocrine secretion)
150
Q 
Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Excitation of skeletal muscle/CNS
Lacrimation
Sweating
Salivation
A

ORGANOPHOSPHATE POISONING

Atropine - Competitive inhibitor of muscarinic receptors

Pralidoxime (2-PAM) for nicotinic symptoms - regenerates AChE

151
Q

Mechanism and use of Benztropine

A

Muscarinic antagonist

Parkinson’s disease
Acute dystonia

152
Q

Mechanism and use of Glycopyrrolate

A

Muscarinic antagonist

Preoperative reduction in airway secretions
Drooling
Peptic ulcers

153
Q

Mechanism and use of Hyoscyamine, Dicyclomine

A

Muscarinic antagonist

Antispasmodics for IBS

154
Q

Mechanism and use of Ipratropium, Tiotropium

A

Muscarinic antagonist - Reduce bronchoconstriction and mucus production

COPD
Asthma

155
Q

Mechanism and use of Oxybutynin, Solifenacin, Tolterodine

A

Muscarinic antagonist

Overactive bladder

156
Q

Mechanism and use of Atropine, Homatropine, Tropicamide

A

Muscarinic antagonist

RCA MI (reduces vagal tone/bradycardia)
Mydriasis induction
Cycloplegia

May cause...
Hot as a hare (decreased sweating)
Dry as a bone
Red as a beet
Blind as a bat
Mad as a hatter
Bowel and bladder lose their tone
Heart runs alone (tachycardia)
Increased IOP/Glaucoma
157
Q

Gardener with mydriasis.

A

Gardener’s pupil

Due to Jimson weed (Datura) an alkaloid with muscarinic antagonist action

158
Q

Target receptor and use of Albuterol, Salmeterol

A

b2 > b1 agonist

Asthma
COPD

159
Q

Target receptor and use of Dobutamine

A

b1&raquo_space; b2, a1 agonist - Increased cAMP causes increased intracellular Ca (inotropy) and nodal Na channel activation (chronotropy)

Refractory HF
Cardiogenic shock (acute MI)
Cardiac stress testing

May increase oxygen requirement and thus potentiate ischemia

Note - Little effect on PVR

160
Q

Target receptor and use of Dopamine

A

D1 = D2 > b > a agonist

Note - beta induced inotropy/chronotropy and low doses, alpha induced vasoconstriction at higher doses

Shock
Heart failure
Bradycardia

161
Q

Target receptor and use of Epinephrine

A

b > a agonist

Note - Alpha effects predominate at higher doses increasing diastolic BP (decreased at low doses)

Anaphylaxis
Asthma

162
Q

Target receptor and use of Fenoldopam

A

D1 agonist

Postoperative hypertension
Hypertensive crisis with renal failure
Promotes natriuresis

May cause…
Hypotension
Tachycardia

163
Q

Target receptor and use of Isoproterenol

A

Non-selective b agonist

Evaluation of tachyarrhythmias

May worsen ischemia

164
Q

Target receptor and use of Midodrine

A

a1 agonist

Autonomic insufficiency/Postural hypotension

May exacerbate supine hypertension

165
Q

Target receptor and use of Norepinephrine

A

a1&raquo_space; a2 > b1 agonist

Hypotension
Shock

166
Q

Target receptor and use of Phenylephrine/Pseudoephedrine

A

a1 > a2 agonist

Hypotension
Ocular procedures (pupillary dilator)
Rhinitis (decongestant)

May cause…
HTN
CNS stimulation/anxiety

167
Q

Mechanism and use of Amphetamines

A

Indirect general agonist (promotes release) and reuptake inhibitor

Narcolepsy
ADHD
Obesity

168
Q

Mechanism and side effects of Cocaine

A

Blocks dopamine reuptake channel

Vasoconstriction (DAT binding)
Local anesthesia (Na channel blockade)
169
Q 
Sympathomimetic and mechanism resulting in...
Dramatically increased PVR
Increased MAP
Decreased HR
Widened pulse pressure
No change in CO
A

NOREPINEPHRINE (a1 > a2 > b1)

Dramatic increase in PVR due to unopposed a1

Greater increase in systolic pressure (via b1) relative to increase in diastolic (high PVR = high venous return)

Widened pulse pressure and increased MAP resulting in reflex bradycardia - no net effect on CO

170
Q 
Sympathomimetic and mechanism resulting in...
Decreased PVR
Slightly increased MAP
Increased HR
Widened pulse pressure
Increased in CO
A

EPINEPHRINE (b > a)

Decrease in PVR and diastolic BP via b2 > a1 (low doses)

Increased systolic pressure (less than NE) due to increased contractility and HR via b1

Widened pulse pressure and slightly increased MAP - increased CO overall

171
Q

Mechanism and use of Clonidine, Guanfacine

A

Sympatholytic - a2 agonists

Hypertensive urgency
ADHD
Tourette’s

May cause...
CNS depression
Bradycardia
Hypotension
Respiratory depression
Miosis
Rebound hypertension (Clonidine)
172
Q

Mechanism and use of a-Methyldopa

A

Sympatholytic - a2 agonists

Hypertension in pregnancy

May result in…
Direct Coombs+ hemolysis
SLE-like syndrome

173
Q

Mechanism and use of Phenoxybenzamine

A

Nonselective, irreversible a-blocker

Preoperative Pheochromocytoma to prevent hypertensive crisis

May cause…
Orthostatic hypotension with reflex tachycardia

174
Q

Mechanism and use of Phentolamine

A

Nonselective, reversible a-blocker

Given to patients on MAOi who eat Tyramine

May cause…
Orthostatic hypotension with reflex tachycardia

175
Q

Mechanism and use of Prazosin, Terazosin, Doxazosin, Tamsulosin

A

a1 selective a-blocker

BPH
PTSD (Prazosin)
Hypertension

May cause on first dose…
Orthostatic hypotension

Note - Tamsulosin cannot be used in HTN as it is selective for a1-AD (prostate) rather than a1B (vascular)

176
Q

Mechanism and use of Mirtazapine

A

a2 selective a-blocker

Depression

May cause…
Sedation
Increased appetite
Increased serum cholesterol

177
Q 
Mechanism of b-blocker treatment of...
Angina/MI
SVT (Metoprolol, Esmolol)
Hypertension
HF (Metoprolol, Carvedilol, Bisoprolol)
Glaucoma (Timolol)
Variceal bleeding (Propranolol, Nadolol)
A 
Decreased HR/Inotropy decrease O2 demand
Decreased AV conduction velocity
Decreased CO/Renin (b1 on JGA cells)
Decreased sympathetic activation
Decreased secretion of aqueous humor
Decreased hepatic venous pressure gradient/portal HTN
178
Q

Adverse effects of b-blockers

A 
Erectile dysfunction
Bradycardia
AV block
Asthma/COPD exacerbation
HF
Seizures
Dyslipidemia (Metoprolol)
179
Q

B1 selective b-blockers

“1st half of alphabet”

A 
Acebutolol
Atenolol
Betaxolol
Esmolol
Metoprolol
180
Q

Nonselective b-blockers

“2nd half of alphabet”

A

Nadolol
Pindolol
Propranolol
Timolol

May cause…
Hypoglycemia masking
Cause hyperkalemia by interfering with B2 mediated K uptake in cells

181
Q

Nonselective a/b-blockers - do not end in -olol

Note - Can be used in Cocaine HTN

A

Carvedilol

Labetalol

182
Q

Mechanism of Nebivolol

A

Cardiac-selective b1-blockade

Stimulation of b3 activating vascular NO synthase

183
Q

Reversible inhibitors of H1 histamine receptors

Note - May also be used in vestibular nausea

A

ANTIHISTAMINES

First generation: Diphenhydramine, Dimenhydrinate, Chlorpheniramine, Hydroxyzine, Promethazine, Meclizine, Cyproheptadine

Second generation: Loratadine, Fexofenadine, Desloratadine

First generation may cause...
Sedation
Antimuscarinic
Anti-a-adrenergic (postural hypotension)
Serotonergic (appetite stimulation)
184
Q

Mechanism of Expectorants (Guaifenesin, NAC)

Note - Do not suppress cough reflex

A

Guaifenesin - Thins respiratory secretions

NAC - Mucolytic liquefies mucus in COPD patients by disrupting disulfide bonds

185
Q

Mechanism of Dextromethorphan

A

Antitussive - NMDA receptor antagonist

May cause…
Serotonin syndrome
Mild opioid effects (Naloxone as antidote)

186
Q

Mechanism of Bosentan in treating PAH

A

Competitive antagonist of Endothelin-1 receptor leading to decreased pulmonary vascular resistance

May cause…
Hepatotoxicity

187
Q

Mechanism of Sildenafil, Vardenafil, Tadalafil in treating ED

Note - Tadalafil can also be used to treat PAH

A

Inhibits cGMP PDE-5, prolonging vasodilatory effect of NO via PKG

May cause...
Flushing
Headache
Dyspepsia
Cyanopica (blue-tinted vision)
Hypotension with nitrates
188
Q

Mechanism of Epoprostenol and Iloprost in treating PAH

A

PGI2 (Prostacyclin) with direct vasodilatory effects on pulmonary and systemic arterial vascular beds - inhibits platelet aggregation

May cause…
Flushing
Jaw pain

189
Q

Mechanism of inhaled corticosteroids

A

Fluticasone, Budesonide

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

190
Q

Mechanism of muscarinic antagonists used to treat asthma/COPD

A

Ipratropium

Competitively blocks muscarinic receptors preventing bronchoconstriction

191
Q

Mechanism of Montelukast/Zafirlukast and Zileuton

A

Montelukast/Zafirlukast block LTD4 receptors (CysLT1) in ASA-induced asthma

Zileuton is a 5-LOX inhibitor blocking conversion of arachidonic acid to leukotriene (hepatotoxicity)

Note - Second line to steroids as drugs that work on late response to mediators (e.g. inflammation leading to bronchial hyperreactivity)

192
Q

Mechanism and use of Omalizumab

A

Anti-IgE monoclonal antibody blocks binding to FceRI

Allergic asthma resistant to inhaled corticosteroids and long-acting b2 agonists (e.g. Salmeterol, Formoterol)

193
Q

Mechanism and use of of Mannitol

A

Increased tubular fluid osmolarity increases urine flow

Elevated ICP or intraocular pressure

Note - Contraindicated in anuria or HF due to risk of pulmonary edema

194
Q

Mechanism and use of Acetazolamide

A

Carbonic anhydrase inhibitor causes self-limited NaHCO3 diuresis

Glaucoma
Urinary alkalinization
Metabolic alkalosis
Pseudotumor cerebri
Altitude sickness

May cause…
Proximal RTA
NH3 toxicity
Sulfa allergy

195
Q

Mechanism and use of sulfonamide loop diuretics

Includes…
Furosemide
Bumetanide
Torsemide

Note - Inhibited by concurrent NSAID use

A

Inhibits NaK2Cl cotransporter in TALH
Abolishes medullary hypertonicity (urinary concentration)
Increases Ca excretion

Edematous states
Hypertension
Hypercalcemia

May cause...
Hypokalemic metabolic alkalosis (contraction)
Ototoxicity
Dehydration
Allergy (sulfa)
Interstitial nephritis
Gout
196
Q

Mechanism and use of Ethacrynic acid

A

Non-sulfa inhibitor of NaK2Cl cotransporter in TALH

Diuresis in patients with sulfa allergies - higher risk of ototoxicity

197
Q

Mechanism and use of Thiazides

Includes…
Hydrochlorothiazide
Chlorthalidone
Metolazone

A

Inhibits NaCl cotransporter in early DCT
Decreases Ca excretion

Hypertension
HF
Calcium stones (hypercalciuria)
Nephrogenic diabetes insipidus (free water loss)
Osteoporosis
May cause...
Allergy (sulfa)
Hyponatremia (maintain corticomedullary conc gradient)
Hypokalemic metabolic alkalosis (contraction)
Hypercalcemia (basolateral NCX)
Hyperglycemia
Hyperlipidemia
Hyperuricemia
198
Q

Mechanism and use of potassium-sparing diuretics

Includes…
Spironolactone/Eplerenone
Triamterene/Amiloride

A

Spironolactone/Eplerenone competitive antagonists of aldosterone receptor in cortical collecting tubule

Triamterene/Amiloride block ENaC in cortical collecting tubule

HF
Hyperaldosteronism (Conn syndrome)
Hypokalemia
Hepatic ascites (Spironolactone)
Nephrogenic diabetes insipidus (Amiloride)

May cause…
Hyperkalemia
Gynecomastia (Spironolactone)
Metabolic acidosis

199
Q

Mechanism and use of ACEi

Includes...
Captopril
Enalapril
Lisinopril
Ramipril
A

Prevents ACE conversion of ATI to ATII and inactivation of bradykinin - Increased Renin because of loss of feedback

Hypertension
Post-MI
HF
Diabetic nephropathy - Decreased intraglomerular pressure (afferent dilation) slows GBM thickening

May cause...
First dose hypotension
Cough
Angioedema
Hyperkalemia
Increased Cr (decreased GFR)
ARF if bilateral RAS
Teratogen (fetal anuria)

Note - Angioedema (may be delayed) from increased bradykinin; contraindicated in C1 esterase inhibitor deficiency

Note - Increased Cr/decreased GFR due to inability to preferentially constrict efferent arteriole (above 30% is dangerous)

200
Q

Mechanism and use of ARBs

Includes…
Losartan
Candesartan
Valsartan

A

Selectively blocks ATII binding to AT1 receptor (smooth muscle, adrenal cortex) - No effect on bradykinin and good for patients with ACEi intolerance

Hypertension
Post-MI
HF
Proteinuria
Diabetic nephropathy (decreased intraglomerular pressure slows GBM thickening)
May cause...
Hypotension
Hyperkalemia
Increased Cr (decreased GFR)
Teratogen
201
Q

Mechanism and use of Aliskiren

A

Direct Renin inhibitor

Hypertension

May cause…
Hypotension
Hyperkalemia
Increased Cr (decreased GFR)

202
Q

Side effects of EPO

A

Thromboembolic events

Hypertension

203
Q

Unpredictable drug interaction due to genetic differences or complex interactions

A

IDIOSYNCRATIC DRUG REACTION (TYPE B)

204
Q

Mechanism and use of H2 blockers

Includes...
Cimetidine
Ranitidine
Famotidine
Nizatidine
A

Reversible blockade of Gs H2-receptors decreasing gastric acid secretion by parietal cells in response to Histamine from ECL cells

Peptic ulcer
Gastritis
Mild esophageal reflux

May cause…
Antiadrenergic effects
Decreased renal excretion of Cr (Cimetidine, Ranitidine)

205
Q

Mechanism and use of PPI

Includes…
-prazole drugs

A

Irreversible inhibition of H/K ATPase in parietal cells

Peptic ulcer
Gastritis
Esophageal reflux
Zollinger-Ellison syndrome

May cause…
Increased C. diff risk
Pneumonia
Hypomagnesemia with long-term use

206
Q

Side effects of antacids

Includes…
Aluminum hydroxide
Calcium carbonate
magnesium hydroxide

A

Hypokalemia
Decreased drug bioavailability
Delayed gastric emptying

Aluminum hydroxide:
Constipation
Hypophosphatemia
Osteodystrophy

Calcium carbonate:
Hypercalcemia (milk-alkali syndrome)
Rebound HCl secretion
Chelation of Tetracyclines

Magnesium hydroxide:
Diarrhea

207
Q

Mechanism and use of Bismuth, Sucralfate

A

Binds to ulcer base providing physical barrier and allowing HCO3 secretion to reestablish pH gradient mucosal layer

Ulcer healing
Traveler’s diarrhea

208
Q

Mechanism and use of Misoprostol

A

PGE1 analog increasing production and secretion of gastric mucous, while decreasing gastric acid production (Gi)

NSAID ulcer
Induction of labor

May cause…
Diarrhea
Abortifacient

209
Q

Mechanism and use of Octreotide

A

Somatostatin analog - Decreases stomach, pancreatic, and gallbladder secretions

Acute variceal bleeding
VIPoma
Carcinoid
Acromegaly

May cause…
Steatorrhea
Cholelithiasis (CCK inhibition)

210
Q 
Class of drugs including...
Magnesium hydroxide
Magnesium citrate
Polyethylene glycol
Lactulose
A

OSMOTIC LAXATIVES

211
Q

Mechanism and use of Sulfasalazine

A

Combination of Sulfapyridine and 5-ASA activated by colonic bacteria

UC
Crohn’s colitis

May cause…
Sulfonamide toxicity
Reversible oligospermia

212
Q

Mechanism and use of Loperamide

A

u-opioid agonist slowing gut motility - Poor CNS penetration means low addictive potential

Good for IBS, Diarrhea

213
Q

Mechanism and use of Ondansetron

A

5-HT3 antagonist decreasing vagal stimulation in area postrema

Antiemetic (postoperative, chemotherapy)

May cause…
Prolonged QT

214
Q

Mechanism and use of Metoclopramide/Prochlorperazine

A

D2 receptor antagonist…
Increases LES tone
Decreases pyloric tone
Increases peristalsis (no effect on colonic transit time), Inhibits D2 action in area postrema (near NTS)

Diabetic/Postoperative gastroparesis
Central antiemetic (e.g. migraines)
May cause...
Parkinsonism (contraindicated)
Tardive dyskinesia
Sedation
Contraindicated in small bowel obstruction

Note - Drug interactions with Digoxin, diabetic agents

215
Q

Mechanism and use of Orlistat

A

Inhibits gastric and pancreatic lipase decreasing absorption of dietary fats (weight loss)

May cause…
Steatorrhea
Vit A, D, E, K deficiency

216
Q

Mechanism and use of Ursodiol (ursodeoxycholic acid)

A

Nontoxic bile acid - Increases bile secretion and decreases cholesterol secretion

Primary biliary cirrhosis
Gallstone prevention or dissolution

217
Q

Mechanism of Theophylline (bronchial asthma)

A

Inhibition of cAMP phosphodiesterase - Results in bronchodilation

May cause…
GI disturbance
Seizure
Arrhythmias

Note - Metabolized by Cytochrome P-450

218
Q

Mechanism of rapid absorption of Lispro, Aspart, Glulisine

A

Proline residues to prevent polymerization (e.g. Regular) and allow rapid absorption

Note - Absorption is delayed in long-acting forms by adding Protamine (NPH), fatty acid (Detemir), Acidic groups (Glargine)

219
Q

Insulin used in…
DKA
Hyperkalemia
Stress hyperglycemia

A

Regular insulin - IV form available

220
Q

Mechanism of drugs including…

Metformin

A

BIGUANIDES

Increases peripheral glucose uptake and insulin sensitivity (no islet cell function needed) while decreasing gluconeogenesis - Causes modest weight loss

May cause…
GI disturbance
Lactic acidosis in renal insufficiency

Note - Always obtain baseline renal function tests

221
Q 
Mechanism of drugs including...
GlimepirIDE
GlipizIDE
GlyburIDE
ChlorpropamIDE
TolbutamIDE
A

SULFONYLUREAS

Close K channel in beta cell membranes causing cell depolarization and Ca influx - endogenous insulin release so need some islet cell function (e.g. not T1DM)

May cause…
Weight gain
Hypoglycemia (especially in renal insufficiency)

222
Q

Mechanism of drugs including…
PiogliTAZONE
RosigliTAZONE

A

GLITAZONES/THIAZOLIDINEDIONES

Binds PPAR-y nuclear transcription regular leading to…
Insulin sensitivity (GLUT4)
Adiponectin production (b-oxidation)
Decreased TNF-a, Leptin

May cause...
Weight gain (Leptin)
Edema
HF exacerbation
Osteoporosis
No risk of hypoglycemia

Note - Safe to use in renal insufficiency

223
Q

Mechanism of drugs including…
NateGLINIDE
RepaGLINIDE

A

MEGLITINIDES

Bind different K channel site than Sulfonylureas - Useful for post-prandial high glucose (short-acting)

May cause…
Weight gain
Hypoglycemia (especially in renal insufficiency)

224
Q

Mechanism of drugs including…
ExenaTIDE
LiragluTIDE

A

GLP-1 ANALOGS

Bind G-protein and increased glucose-dependent insulin release while inhibiting glucagon - Causes modest weight loss

May cause…
Nausea/Vomiting (inhibit gastric emptying)
Pancreatitis

225
Q

Mechanism of drugs including…
LinagLIPTIN
SaxagLIPTIN
SitagLIPTIN

A

DPP-4 INHIBITORS

Inhibits DPP-4 enzyme that deactivates GLP-1

May cause…
Nasopharyngitis

Note - No hypoglycemia because glucose-dependent

226
Q

Mechanism of drugs including…

Pramlintide SQ injection

A

AMYLIN ANALOGS

Decreased gastric emptying and glucagon

May cause…
Hypoglycemia
Nausea

227
Q

Mechanism of drugs including…
CanaGLIFLOZIN
DapaGLIFLOZIN
EmpaGLIFLOZIN

A

SGLT-2 INHIBITORS

May cause...
Glucosuria
UTIs/Vaginal yeast infections
Hyperkalemia
Orthostatic hypotension (dehydration)

Note - Always get baseline renal function tests as these drugs need a working PCT to be effective

228
Q

Mechanism of drugs including…
Acarbose
Miglitol

A

A-GLUCOSIDASE INHIBITORS

Inhibit intestinal brush-border a-glucosidases delaying carbohydrate hydrolysis and glucose absorption - leads to decreased postprandial hyperglycemia

May cause…
GI upset

229
Q

Mechanism of PTU and Methimazole

A

THIONAMIDES

Block thyroid peroxidase preventing oxidation and organification of iodine

PTU/Propranolol also blocks 5-deiodinase decreasing peripheral conversion of T4 to T3

May cause...
Agranulocytosis (sore throat, fever)
ANCA vasculitis
Skin rash
Aplastic anemia
Hepatotoxicity
Cholestasis
Teratogen (Methimazole)
230
Q

Mechanism of drugs including…
Conivaptan
Tolvaptan

A

ADH ANTAGONISTS

Used in SIADH to block action at V2 receptor

231
Q 
Treats...
Acromegaly
Carcinoid syndrome
Gastrinoma
Glucagonoma
Esophageal varices
A

OCTREOTIDE

Inhibits GH and release of most GI hormones

232
Q

Mechanism of Demeclocycline

A

ADH ANTAGONIST (TETRACYCLINE)

May cause…
Photosensitivity
Bone and teeth abnormalities

233
Q

Side effects of glucocorticoids

A 
Cushing syndrome
Adrenocortical atrophy
Peptic ulcers
Steroid diabetes
Steroid psychoses
Cataracts
234
Q

Mechanism and use of Fludrocortisone

A

ALDOSTERONE ANALOG

Mineralocorticoid replacement in primary adrenal insufficiency

May cause...
Edema
HF
Hyperpigmentation
Cortisol-like effects
235
Q

Mechanism and use of Cinacalcet

A

Sensitizes Ca-sensing receptor (CaSR) in parathyroid gland decreasing PTH - Useful for dialysis patients

May cause…
Hypocalcemia

Note - Sevelamer binds phosphate to decrease GI absorption in dialysis patients

236
Q 
Mechanism of drug used for...
Uterine fibroids
Endometriosis
Precocious puberty
Prostate cancer
Infertility
A

LEUPROLIDE

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

237
Q

Mechanism of Clomiphene in PCOS

A

Hypothalamic estrogen receptor antagonist - prevents feedback inhibition of LH and FSH

May cause...
Multiple pregnancies
Visual disturbances
Hot flashes
Ovarian enlargement
238
Q

Difference in mechanism of Tamoxifen (breast cancer) and Raloxifene (osteoporosis)

A

Tamoxifen is an estrogen receptor antagonist at the breast, but agonist at bone and uterus - increases the risk of DVT and endometrial cancer

Raloxifene is an estrogen receptor antagonist at the breast and uterus, but agonist at bone - increases risk of DVT only

Note - SERMs can also be used to treat gynecomastia in ADT patients

239
Q

Mechanism and use of drugs including…
Anastrozole
Letrozole
Exemestane

A

AROMATASE INHIBITORS

ER+ breast cancer in postmenopausal women

240
Q

Mechanism of drug used for…
Endometrial cancer
Abnormal uterine bleeding
Contraception

A

PROGESTINS

Includes Levonorgestrel, Medroxyprogesterone, Etonogestrel, Norethindrone, and Megestrol

Decreases growth of endometrium, thickens cervical mucus (mini-pill, IUD), and decreases LH/FSH (combined OCP)

Note - Presence of withdrawal bleeding excludes anatomic defects (e.g. Asherman) and chronic anovulation

241
Q

Mechanism of Terbutaline/Ritodrine

A

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

242
Q

Mechanism of Danazol

Used to treat…
Endometriosis
Angioedema

A

Synthetic androgen that acts as partial agonist at androgen receptor

May cause...
Hepatotoxicity
Decreased HDL
Weight gain
Edema
Acne, hirsutism, masculinization
243
Q

Stimulates anabolism to promote recovery after burn or injury

A

TESTOSTERONE, METHYLTESTOSTERONE

244
Q

Mechanism of drugs used in PCOS to reduce androgenic symptoms

A

Ketoconazole - Inhibits steroid synthesis by Desmolase

Spironolactone - Inhibits steroid binding, 17a-hydroxylase, and Desmolase

May cause…
Gynecomastia
Amenorrhea

245
Q

Mechanism of Finasteride - BPH and male pattern baldness

A

5a-reductase inhibitor decreases conversion of testosterone to DHT

246
Q

Used to treat…
Androgenetic alopecia
Severe refractory hypertension

A

MINOXIDIL

Direct arteriolar vasodilator

247
Q

Mechanism of Acetaminophen

A

Reversible COX inhibitor - CNS only so not anti-inflammatory

248
Q

Mechanism and dosages of ASA

A

Irreversible COX1/2 inhibitor by covalent acetylation

Low dose (< 300) - Decreases platelet aggregation
Medium dose (< 2400) - Antipyretic and Analgesic
High dose (< 4000) - Antiinflammatory
May cause...
Increased bleeding time (normal PT, PTT)
Gastric ulceration
Tinnitus
Interstitial nephritis
Respiratory alkalosis early in overdose
Mixed metabolic alkalosis-respiratory acidosis later
249
Q

Mechanism of Celecoxib

Used to treat…
Rheumatoid arthritis
Osteoarthritis

A

Reversible inhibition of COX2 - Inducible by IL-1/TNF-a

Spares COX1 (constitutive) - Maintains gastric mucosa and produces TXA2

May cause…
Thrombosis
Impaired renal perfusion
Sulfa allergy

250
Q

Mechanism of NSAIDs

Includes...
Ibuprofen
Naproxen
Indomethacin
Ketorolac
Diclofenac
Meloxicam
Piroxicam
A

Reversible inhibition of COX1/2

May cause…
Gastric ulceration
Interstitial nephritis
Renal ischemia

Note - Naproxen, Indomethacin can be used for acute gout attacks

251
Q

Mechanism of Leflunomide

A

Reversibly inhibits Dihydroorotate Dehydrogenase - disrupts Pyrimidine synthesis and T cell proliferation

Rheumatoid arthritis
Psoriatic arthritis

May cause...
Diarrhea
Hypertension
Hepatotoxicity
Teratogen
252
Q

Mechanism of Bisphosphonates

Includes...
Alendronate
Ibandronate
RIsedronate
Zoledronate
A

Pyrophosphate analog binds Hydroxyapatite in bone - inhibits osteoclast activity

Osteoporosis
Hypercalcemia
Paget (osteitis deformans)
Metastatic bone disease
Osteogenesis imperfecta

May cause…
Pill esophagitis (take with water, sit upright after)
Osteonecrosis of jaw
Atypical stress fractures

253
Q

Mechanism of Teriparatide - stimulates bone growth in Osteoporosis

A

Recombinant PTH analog - increases osteoblastic activity

May cause…
Transient hypercalcemia

254
Q

Mechanism of Allopurinol and Febuxostat

A

Competitive inhibitor of Xanthine Oxidase preventing conversion of Hypoxanthine and Xanthine to Urate

Used in…
Gout control
Uric acid stones
Lymphoma/Lymphoma (tumor lysis syndrome)

May cause…
DRESS (fever, lymphadenopathy, rash, organ dysfunction)

Note - Also increases levels of Azathioprine and 6-Mercaptopurine as they are metabolized by Xanthine Oxidase

255
Q

Mechanism of Pegloticase, Rasburicase

A

Recombinant Uricase converts Urate to Allantoin - more water soluble

Pegloticase - Gout control
Rasburicase - Tumor lysis

256
Q

Mechanism of Probenecid

A

Binds OAT - Inhibits reabsorption of uric acid in PCT

Gout control

May cause…
Uric acid stones

Note - Diuretics and ASA prevent tubular secretion

257
Q

Mechanism of Colchicine

A

Binds and stabilizes Tubulin - Inhibits microtubule polymerization and thus Neutrophil chemotaxis and degranulation

Acute gout attack

May cause…
GI disturbance

258
Q

Mechanism of TNF-a inhibitor used to treat…

Rheumatoid arthritis
Ankylosing spondylitis
Psoriasis

A

ETANERCEPT

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

259
Q

Mechanism of TNF-a inhibitors used to treat…

IBD
Rheumatoid arthritis
Ankylosing spondylitis
Psoriasis

A

INFLIXIMAB, ADALIMUMAB

Anti-TNFa monoclonal antibody

260
Q

Mechanism of drug used for…

Acute PE
ACS
DVT

Note - Can be used in pregnancy

A

HEPARIN

Inhibits II (Thrombin) and Xa - Follow PTT

May cause…
HIT
Bleeding
Osteoporosis

Note - Antidote is Protamine sulfate

261
Q

Class of drugs including…
Enoxaparin
Dalteparin
Fondaparinux

A

LMWH

More specific for Xa - Does not require lab monitoring

Note - Better bioavailability and longer half life, but no antidote

262
Q

Mechanism of drug used for…

PE/DVT
Afib

Note - Can be used in HIT

A

DIRECT THROMBIN INHIBITORS

Argatroban
Dabigatran
Bivalirudin

Does not require lab monitoring

May cause…
Bleeding

Note - No antidote, but may attempt activated prothrombin complex concentrate (PCC) or fibrinolytics (tranexamic acid)

263
Q

Mechanism of drug used for…

DVT/PE prophylaxis
Afib stroke prevention

A

WARFARIN

Prevents y-carboxylation of Vit K - acts in liver

May cause…
Bleeding
Skin/tissue necrosis
Teratogen (stippled epiphyses)

Note - Reverse rapidly with FFP, slowly with Vit K

264
Q

Mechanism of drugs including…
Apixaban
Rivaroxaban

Note - Do not affect TT

A

DIRECT FACTOR XA INHIBITORS

DVT/PE prophylaxis
Afib stroke prevention

May cause…
Bleeding

Note - No reversal agent

265
Q 
Mechanism of drugs including...
Alteplase
Reteplase
Streptokinase
Tenecteplase
A

THROMBOLYTICS

Aid conversion of plasminogen to plasmin cleaving thrombin and fibrin clots - Follow PT and PTT

Avoid if...
Bleeding risk
Severe hypertension (ICH)

Treat toxicity with Aminocaproic acid, and possible FFP/Cryo

Note - Platelet count normal

266
Q 
Mechanism of drugs including...
Clopidogrel
Prasugrel
Ticagrelor (reversible)
Ticlopidine
A

ADP RECEPTOR INHIBITORS

Irreversible blockade of ADP receptors on platelets prevents expression of GpIIb/IIIa

ACS
Coronary stenting
Thrombotic stroke prophylaxis

May cause…
Neutropenia (Ticlopidine)
TTP

267
Q

Mechanism of drugs including…
Milrinone
Cilostazol
Dipyridamole

A

Phosphodiesterase III inhibitors - Increase cAMP results in increased contractility, arterial vasodilation, and decreased platelet aggregation

Intermittent claudication
Vasodilation
Stroke/TIA prevention (with ASA)

May cause...
Nausea
Headache
Facial flushing
Hypotension
Abdominal pain
268
Q

Mechanism of drugs including…
Abciximab
Eptifibatide
Tirofiban

A

GPII/IIIA INHIBITORS

Bind to receptors and prevent platelet aggregation - Abciximab is made from monoclonal antibody Fab fragments

Unstable angina
Coronary angioplasty

May cause…
Bleeding
Thrombocytopenia

269
Q

Mechanism of antimetabolite (S phase) used to treat…

Transplant rejection prophylaxis
Rheumatoid arthritis
IBD
SLE

Note - Used to wean off steroids or treat steroid-refractory chronic disease

A

AZATHIOPRINE

6-Mercaptopurine (metabolite of Azathioprine)

Purine analog activated by HGPRT - Prevents de novo purine synthesis

May cause…
Myelosuppression
GI toxicity
Liver toxicity

Note - Metabolized by Xanthine Oxidase so increased toxicity with Allopurinol or Febuxostat

Note - Mutation in Thiopurine Methyltransferase also increase toxicity

270
Q

Mechanism of antimetabolite (S phase) used to treat…

Hairy cell leukemia

A

CLADRIBINE

Purine analog inhibitor of DNA polymerase

May cause…
Myelosuppression
Nephrotoxicity
Neurotoxicity

271
Q

Mechanism of antimetabolite (S phase) used to treat…

AML
Lymphoma

A

CYTARABINE (ARABINOFURANOSYL CYTIDINE)

Pyrimidine analog inhibitor of DNA polymerase

May cause…
Myelosuppression
Megaloblastic anemia
Pancytopenia

272
Q

Mechanism of antimetabolite (S phase) used to treat…

Colon cancer
Pancreatic cancer
BCC (topical)

A

5-FLUOROURACIL

Pyrimidine analog bioactivated to 5-FdUMP and inhibits Thymidylate Synthesis - Decreased dUMP to dTMP

May cause…
Myelosuppression especially with Leucovorin

Note - Potentiated with Leucovorin

273
Q

Mechanism of antimetabolite (S phase) used to treat…

ALL
Lymphoma
Choriocarcinoma
Sarcoma
Rheumatoid arthritis
Psoriasis
IBD
Vasculitis
Ectopic pregnancy
Medical abortion (with Misoprostol)
A

METHOTREXATE

Folic acid analog competitively inhibits Dihydrofolate Reductase - Decreased dTMP synthesis

May cause...
Myelosuppression
Hepatotoxicity
Mucositis (mouth ulcers)
Pulmonary Fibrosis

Note - Rescue with Leucovorin

274
Q

Mechanism of drug used to treat…

Testicular cancer
Hodgkin’s lymphoma

A

BLEOMYCIN

Induces free radical formation leading to breaks in DNA strands - works in G2 phase

May cause…
Pulmonary fibrosis
Skin hyperpigmentation

Note - Minimal myelosuppression

275
Q

Mechanism of drug used to treat…

Wilms tumor
Ewing sarcoma
Rhabdomyosarcoma

A

DACTINOMYCIN (ACTINOMYCIN D)

Intercalates in DNA

May cause…
Myelosuppression

276
Q

Mechanism of drug used to treat…

Solid tumors
Leukemias
Lymphomas

A

DOXORUBICIN/DAUNORUBICIN

Generates free radicals and intercalates with DNA

May cause…
Cardiotoxicity - prevent with Dexrazoxane
Myelosuppression
Alopecia

277
Q

Mechanism of Alkylating agent (DNA cross-linking) used to treat…

CML
Bone marrow ablation pre-transplant

A

BUSULFAN

May cause…
Severe myelosuppression
Pulmonary fibrosis
Hyperpigmentation

278
Q

Mechanism of Alkylating agent (DNA cross-linking) used to treat…

Solid tumors
Leukemia
Lymphoma

A

CYCLOPHOSPHAMIDE, IFOSFAMIDE

Requires bioactivation by liver

May cause…
Myelosuppression
Hemorrhagic cystitis - prevent with Mesna or NAC

279
Q

Mechanism of Alkylating agent (DNA cross-linking) used to treat…

Brain tumors (GBM)

A

NITROSOUREAS

Requires bioactivation - crosses BBB

May cause…
Convulsions
Dizziness
Ataxia

280
Q

Mechanism of microtubule inhibitors (M phase) used to treat…

Ovarian carcinomas
Breast carcinomas

A

PACLITAXEL/TAXOLS

Hyperstability polymerized microtubules to prevent anaphase

May cause…
Myelosuppression
Neuropathy
Hypersensitivity

281
Q

Mechanism of microtubule inhibitors (M phase) used to treat…

Solid tumors
Leukemias
Hodgkin’s lymphoma
Non-Hodgkin’s lymphoma

A

VINCRISTINE/VINBLASTINE

Bind b-tubulin and inhibit polymerization preventing mitotic spindle formation

May cause…
Peripheral neuritis, areflexia
Paralytic ileus

Note - Vincristine for Hodgkin’s, Vinblastine for non-Hodgkin’s

282
Q

Mechanism of Platinum agent used to treat…

Testicular cancer
Bladder cancer
Ovarian cancer
Lung cancer

A

CISPLATIN, CARBOPLATIN

Cross-links DNA

May cause…
Nephrotoxicity - Prevent with Amifostine/Diuresis
Ototoxicity
Peripheral neuropathy

283
Q

Mechanism of Topoisomerase inhibitor (S to G2) used to treat…

SCLC
Testicular cancer
Leukemia
Lymphoma

A

ETOPOSIDE, TENIPOSIDE

Inhibits Top II increasing DNA degradation

May cause…
Myelosuppression
Alopecia

284
Q

Mechanism of Topoisomerase inhibitor (S to G2) use to treat…

SCLC
Colon cancer
Ovarian cancer

A

IRINOTECAN, TOPOTECAN

Inhibits Top I preventing DNA unwinding and replication

May cause…
Severe myelosuppression
Diarrhea

285
Q

Mechanism of antimetabolite (S phase) used to treat…

Melanoma
CML
SCD

A

HYDROXYUREA

Inhibits Ribonucleotide Reductase (UDP to dUDP) - Decreasing DNA synthesis (S-phase specific)

Also increases HbF

May cause…
Severe myelosuppression

286
Q

Mechanism of Bevacizumab

Used to treat…
Colorectal cancer
RCC

A

Antibody against VEGF - Inhibits angiogenesis

May cause…
Hemorrhage
Blood clots
Impaired wound healing

Note Bevacizumab/Ranibizumab may both also treat wet macular degeneration

287
Q

Mechanism of Erlotinib

Used to treat…
Non-small cell lung cancer

A

EGFR tyrosine kinase inhibitor

May cause…
Rash

288
Q

Mechanism of Cetuximab

Used to treat…
CRC (wild-type KRAS)
Head and neck cancer

A

Monoclonal antibody against EGFR

May cause…
Rash
Elevated LFTs
Diarrhea

289
Q

Mechanism of Imatinib

Used to treat…
CML
GIST

A

Tyrosine kinase inhibitor of bcr-abl and c-kit

May cause…
Fluid retention

290
Q

Mechanism of Rituximab

Used to treat...
Non-hodgkin's lymphoma
CLL
Rheumatoid arthritis
ITP
A

Monoclonal antibody against CD20 - B-cell marker

May cause…
Increased risk of PML

291
Q

Mechanism of Trastuzumab (Herceptin)

Used to treat…
HER2+ breast cancer
Gastric cancer

A

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

May cause…
Cardiotoxicity

292
Q

Mechanism of Vemurafenib

Used to treat…
Metastatic melanoma

A

Small molecule inhibitor of BRAF oncogene+ (V600E) melanoma

293
Q

Mechanism of opioid analgesics

Includes...
Morphine
Fentanyl
Codeine
Methadone
Meperidine (mydriatic)
Dextromethorphan
Diphenoxylate (anti-diarrheal)
Loperamide (anti-diarrheal)
Pentazocine
A

Decreases synaptic transmission by closing pre-synaptic Ca channels and opening post-synaptic K channels

Note - No tolerance to miosis or constipation

Note - May cause biliary colic (sphincter of Oddi contraction)

294
Q

Mechanism of Pentazocine

A

k-opioid agonist and u-opioid antagonist

May cause…
Opioid withdrawal with full antagonist

295
Q

Mechanism of Butorphanol

A

k-opioid agonist and u-opioid partial agonist

Used in severe pain - Partial agonist so less respiratory depression

May cause…
Opioid withdrawal with full agonist

296
Q

Mechanism of Tramadol

A

Very weak opioid agonist
Serotonin and NE reuptake inhibitor

May cause…
Opioid symptoms
Decreases seizure threshold
Serotonin syndrome

297
Q

Mechanism and side effects of Ethosuximide

A

Blocks thalamic T-type Ca-channels

May cause...
GI disturbance
Headache
Urticaria
SJS
298
Q

Mechanism and side effects of Phenytoin

A

Blocks Na channels - Zero order kinetics

May cause (Dose-dependent saturation)...
CNS symptoms (ataxia, nystagmus)
Megaloblastic anemia
Gingival hyperplasia
Hirsutism
SJS
DRESS
Teratogen (NTD, craniofacial, nail hypoplasia)

Note - Metabolized by Cytochrome P-450

299
Q

Mechanism and side effects of Carbamazepine

A

Blocks Na channels increasing refractory period

May cause...
Agranulocytosis/Aplastic anemia
Hepatotoxicity
SJS
DRESS
SIADH
Teratogen
300
Q

Mechanism and side effects of Valproate

A

Induces Na channels
Inhibits GABA transaminase increasing GABA

May cause...
GI distress
Fetal hepatotoxicity - measure LFTs
Pancreatitis
Weight gain
Tremor
Teratogen (neural tube defects)

Note - Vigabatrin also inhibits GABA transaminase

301
Q

Mechanism and side effects of Gabapentin

A

Inhibits voltage-gated Ca channels - acts as GABA analog

May cause…
Sedation
Ataxia

302
Q

Mechanism and side effects of Topiramate

A

Blocks Na channels
Increases GABA activity

May cause…
Sedation
Mental dulling
Kidney stones

Note - Tiagabine inhibits GABA reuptake

303
Q

Mechanism and side effects of Lamotrigine

A

Blocks Na channels

May cause…
SJS

304
Q

Mechanism and side effects of Barbiturates

Includes...
Phenobarbital
Pentobarbital
Thiopental
secobarbital
A

Facilitates GABA by increasing Cl channel duration

May cause…
Respiratory depression
CV depression

305
Q

Benzodiazepines not metabolized by the liver - Safe to use in alcohol withdrawal with liver failure

A

Lorazepam
Oxazepam
Temazepam

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

306
Q

Benzodiazepines that have a high addictive potential (short acting)

A

Triazolam
Oxazepam
Midazolam (endoscopy)

Alprazolam
Lorazepam
Temazepam

Note - Less active metabolites

307
Q

Mechanism of nonbenzodiazepine hypnotics

Includes…
Zolpidem
Zaleplon
Eszopiclone

A

ACt on BZI subtype of GABA receptor

May cause…
Ataxia
Headaches
Confusion

Note - Alternative is Ramelteon (melatonin agonist)

308
Q

Determinant of induction speed and potency of inhaled anesthetics

A

Decreased solubility in blood - Rapid induction
Increased solubility in lipids - Increased potency

Note - Potency = 1/MAC

309
Q 
Side effects of drugs including...
Halothane
Methoxyflurane
Enflurane
N2O
A

INHALED ANESTHETICS

Hepatotoxicity (centrilobular)
Nephrotoxicity
Proconvulsant
Expansion of trapped gas in body cavities
Hypotension

Note - Increase cerebral blood flow

310
Q

IV anesthetic used for…

ICU
Rapid induction
Short procedures

A

PROPOFOL

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

Note - Less postoperative nausea

311
Q

High potency IV anesthetic used for induction and short procedures - Effect terminated by rapid redistribution into tissue and fat

A

THIOPENTAL

Note - Decreases cerebral blood flow

312
Q

Order of nerve blockade by local anesthetics

Includes…
Esters (Procaine, Cocaine, Tetracaine, Benzocaine)
Amides (Lidocaine, Mepivacaine, Bupivacaine)

Note - If allergic to Ester can give Amide

A

Small myelinated fibers
Small unmyelinated fibers
Large myelinated fibers
Large unmyelinated fibers

Note - Loss of sensation (first to last) is Pain > Temperature > Touch > Pressure

313
Q

Reason for increased local anesthetic dose in infected tissue

A

Acidic tissue makes alkaline anesthetics more charged and thus unable to penetrate the membrane

Note - Block inner portion of channel

314
Q

Mechanism of Succinylcholine

A

POLARIZING NEUROMUSCULAR BLOCKER

Strong Ach receptor agonist produces sustained depolarization

Diminished TOF response (phase I) followed by progressive reduction (phase II)

Can only reverse with AcheE inhibitors in Phase II (repolarized but desensitized)

May cause…
Hyperkalemia
Hypercalcemia
Malignant hyperthermia

315
Q

Mechanism of drugs including…
Tubocurarine
-urium drugs

A

NONDEPOLARIZING NEUROMUSCULAR BLOCKERS

Competitive antagonists of Ach receptors - Reverse with AchE inhibitor (Neostigmine, Edrophonium)

Progressive reduction with TOF due to additional presynaptic blockade

May cause…
Flushing
Bronchoconstriction
Hypotension

Note - Give AchE inhibitor (Physostigmine, Neostigmine) with Atropine to prevent muscarinic toxicity

316
Q

Mechanism of Baclofen

A

Activates GABA-b receptors at spinal cord level - Induces skeletal muscle relaxation

Note - Cyclobenzaprine is a central acting relaxant (TCA-like)

Note - Tizanidine (a2 agonist) also used

317
Q 
Mechanism of Parkinson's drugs...
Bromocriptine
Pramipexole/Ropinirole
Amantadine
Carbidopa
Selegiline
Entacapone/Tolcapone
Benztropine

Note - L-Dopa converted to Dopamine by DOPA decarboxylase

A 
Dopamine agonist (Ergot)
Dopamine agonist (non-Ergot)
Increased Dopamine release, Decreased uptake
Peripheral DOPA decarboxylase inhibitor
MAO-B inhibitors
COMT inhibitors (peripheral, central)
Antimuscarinic - Tremor/Rigidity

Note - Amantadine may cause Ataxia/Livedo Reticularis

318
Q

Mechanism of Alzheimer’s drugs…
Memantine
Donepezil, Galantamine, Rivastigmine, Tacrine

A 
NMDA antagonist (Confusion, Hallucinations)
AChE inhibitors
319
Q

Treatment (4) of HTN in pregnancy

A

Hydralazine
Labetalol
Methyldopa
Nifedipine

320
Q

Treatment of…
Arsenic poisoning
Lead poisoning
Iron poisoning

A

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

321
Q

Mechanism of Aprepitant/Fosaprepitant

A

Neurokinin 1 (NK1) receptor antagonists in area postrema

Chemotherapy antiemetic

322
Q

Mechanism of Varenicline - Smoking cessation

A

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

323
Q

Naming of biological agents…

  • mab
  • cept
  • nib
A

Monoclonal antibody
Receptor molecule
Kinase inhibitor

Note - For antibodies, -xi- is chimeric -zu- is humanized

324
Q

Effect of…
High blood/gas partition coefficient
High AV conc gradient

A

Highly soluble gas saturates the blood more slowly leading to slower brain saturation and thus onset time

Higher solubility in peripheral tissues means more drug is needed for blood saturation thus increasing onset time

325
Q

Causes of Drug-Induced SLE

A

Hydralazine
Procainamide
Isoniazid

Note - Slow acetylators

326
Q

Mechanism of Capsaicin

A

Depletion of Substance P

327
Q

Calcium channel blockers used for…

Angina (e.g. Prinzmetal’s)
Raynaud’s
Hypertension

A

DIHYDROPYRIDINES

Amlodipine, Clevidipine, Nicardipine, Nifedipine, Nimodipine (Post-SAH)

May cause…
Peripheral edema
Flushing/Dizziness
Gingival hyperplasia

328
Q

Mechanism of Hydralazine

Used for…
Severe HRN
HF

A

Increases cAMP causing smooth muscle relaxation - Mostly affects Arterioles (afterload)

May cause…
Reflex tachycardia (Angina/CAD)
Fluid retention
Angina

329
Q

Mechanism of Ranolazine

Used for…
Refractory angina

A

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

May cause…
Long QT

330
Q

Mechanism of drug resistance to hydrophobic chemotherapeutics (e.g. Anthracyclines)

A

MDR1 P-glycoprotein (ATP efflux pump)

331
Q

Mechanism and side effect of Cholestyramine, Colestipol, and Colesevelam

A

BILE ACID RESINS

Liver uses cholesterol to make more bile acid
Upregulates HMG-CoA (synergy)

May cause…
Hypertriglyceridemia
GI upset
Malabsorption

Note - Ezetimibe inhibits cholesterol absorption directly instead of bile acid resins but may cause transaminitis

332
Q

Mechanism and side effect of drugs used to lower TG

Includes…
Gemfibrozil
Bezafibrate
Fenofibrate

A

FIBRATES

Upregulates LPL to increase TG clearance
Activates PPAR-a to decrease hepatic VLDL production
Induce HDL synthesis

May cause…
Myopathy (with Statins)
Cholesterol gallstones

333
Q

Mechanism and side effect of drugs used to decrease LDL and increase HDL

A

NIACIN (VIT B3)

Inhibits hormone sensitive lipase
Reduces hepatic VLDL production

May cause…
Red, flushed face (treat with NSAID)
Hyperglycemia
Hyperuricemia

334
Q

Mechanism of Digoxin in treating HF and Afib

Note - Eliminated by kidney

A

HF - Increased Ca release from SR increases inotropy
Afib - Increased vagal tone decreases HR

May cause...
Cholinergic syndromes
Color abnormalities
AT with AV block
Hyperkalemia (poor prognosis)
335
Q

Mechanism and side effects of Class IA antiarrhythmics used for…

Re-entrant/ectopic SVT and VT

(“Queen Proclaims the Pyramids)

A

Na channel blockade…
Increased AP duration
Slowed conduction speed
Increased QT interval

Includes…
Quinidine, Procainamide (WPW), Disopyramide

May cause…
Cinchonism (Headache, Tinnitus)
SLE
Torsades

Note - Treat Torsades with Mg

336
Q

Mechanism and side effects of Class IB antiarrhythmics used for…

Acute VT (post-MI)
Digitalis toxicity

(“Lettuce Tomato Mayo”)

Note - Not for SVT

A

Na channel blockade…
Decreased AP duration
Normal conduction speed
Preferentially affects ischemic tissue

Includes…
Lidocaine, Tocainide, Mexiletine

May cause…
CNS symptoms
CV depression

337
Q

Mechanism and side effects of Class IC antiarrhythmics used for…

Paroxysmal Afib

(“More Fries Please”)

A

Na channel blockade…
Normal AP duration
Slowed conduction speed
Preferentially affects AV node and accessory tracts

Includes…
Moricizine, Flecainide, Propafenone

May cause…
Arrhythmias post MI
Contraindicated in structural/ischemic heart disease

Note - Stronge use-dependence - Due to slow dissociation from Na channels increased HR increases effect of drug (wide QRS)

338
Q

Mechanism and side effects of Class II antiarrhythmics used for…

Rate control (Afib, Aflutter)

A

B-blockers…
Decreased slope of phase 4 - Slowed sinus discharge
Decreased cAMP - Slows conduction and prolongs ERP

May cause...
Impotence
COPD/Asthma
Bradycardia
Hypoglycemia masking (CNS sedation)
Dyslipidemia (Metoprolol)
Vasospasm (Propranolol)

Note - Treat overdose with Atropine/Glucagon

339
Q

Mechanism and side effects of Class III antiarrhythmics used for…

Afib, Aflutter
VT

(“AIDS”)

A

K channel blockers…
Increased AP duration
Normal conduction velocity
Increased QT interval

Includes…
Amiodarone, Ibutilide, Dofetilide, Sotalol

May cause...
Bradycardia
Pulmonary fibrosis (Amiodarone)
Hepatotoxicity (Amiodarone)
Thyroid toxicity (Amiodarone)
Photodermatitis (Amiodarone)
Lower Torsades risk

Note - Check LFTs, PFTs, and TFTs before using Amiodarone

Note - Show reverse use-dependency so slower HR results in more prolonged QT

340
Q

Mechanism and side effects of class IV antiarrhythmics used for…

Hypertension
Angina
Paroxysmal SVT
Afib with RVR
Aflutter
A

Non-dihydropyridines (Verapamil, Diltiazem)…
Slowed sinus discharge
Slows conduction and prolongs ERP

May cause...
Constipation
Bradycardia
AV block
Contraindicated in CHF (negative inotrope)

Note - May mask ischemia during stress test

341
Q

Mechanism and side effects of Adenosine used for…

Diagnosing or rapid termination of SVTs

A

Increased K efflux hyperpolarizes cell and decreases Ca influx

May cause...
Flushing
Hypotension
Chest pain
Sense of impending doom
Bronchospasm

Note - Decreased effectiveness with Caffeine and Theophylline

342
Q

Mechanism of Nitrates in treating CN toxicity

A

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

343
Q

Mechanism of Cyclosporine and Tacrolimus

Used for…
Transplant rejection prophylaxis
Psoriasis
Rheumatoid arthritis

A

CALCINEURIN INHIBITOR (NFAT)

Blocks T-cell activation by inhibiting IL-2 transcription

May cause...
Nephrotoxicity
Neurotoxicity
Metabolic disorder
Gingival hyperplasia (Cyclosporine)
Myopathy (with Statins)
344
Q

Mechanism of Sirolimus (Rapamycin)

Used for…
Kidney transplant rejection prophylaxis

Note - Not nephrotoxic

A

MTOR INHIBITOR

Blocks T-cell activation and B-cell proliferation by inhibiting response to IL-2

May cause…
Pancytopenia
Metabolic disorder

345
Q

Mechanism of Daclizumab, Basiliximab

Used for…
Kidney transplant rejection prophylaxis

A

Monoclonal antibodies blocking IL-2

May cause…
Edema
HTN
Tremor

346
Q

Mechanism of Mycophenolate

Used for…
Transplant rejection prophylaxis
SLE nephritis

A

Inhibits IMP dehydrogenase preventing purine synthesis

May cause...
GI upset
Pancytopenia
Invasive CMV infection
Metabolic disorder
347
Q

Use of Filgrastim/Sargramostim

A

Recovery of bone marrow

348
Q

Use of…
IFN-a
IFN-b
IFN-y

A

HCV, HBV, Kaposi, Melanoma
MS
Chronic granulomatous disease

349
Q

Use of…
Romiplostim
Eltrombopag
Oprelvekin

A

Thrombocytopenia

350
Q

Mechanism of Natalizumab

Used for…
MS
Crohn’s

A

Antibody against a4-integrin (WBC adhesion)

May cause…
PML (JC virus)

351
Q

Mechanism of Denosumab

Used for…
Osteoporosis

A

Antibody against RANKL - Inhibits osteoclast maturation by mimicking Osteoprotegerin

352
Q

Mechanism of Palivizumab

A

Antibody against RSV F protein - For high risk-infants

353
Q

Mechanism of Statins

A

Prevent conversion of HMG-CoA to Mevalonate

Upregulation of LDLR further reduces circulating LDL

354
Q

Drugs causing osteoporosis by…

Increasing Vit D catabolism
Decreasing Estrogen
Decreasing Testosterone and Estrogen
Decreasing Ca absorption
Decreasing bone formation
A

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

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