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Drugs Flashcards

1
Q

Amytal

A

barbituate, blocks complex I (NADH dehydrogenase) in ETC

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2
Q

Rotenone

A

pesticide, blocks complex I (NADH dehydrogenase) in ETC

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3
Q

Antimycin A

A

antibiotic, blocks complex III (cytochrome b-c1 complex)

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4
Q

Cyanide

A

smoke, industrial chemical; blocks complex IV (cytrochrome c oxidase)

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5
Q

Carbon monoxide

A

combustion product, blocks complex IV (cytrochrome c oxidase)

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6
Q

Azide

A

antimicrobial agent, AZT; blocks complex IV (cytrochrome c oxidase)

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7
Q

Oligomycin

A

antibiotic, blocks complex V (ATP synthase)

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8
Q

AZT (zidovudine)

A

anti-retroviral drug, blocks DNA pol-gamma which is the mitochondrial DNA replication enzyme

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9
Q

Dinitrophenol

A

explosive, chemical uncoupler

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10
Q

Salicylate

A

product of aspirin metabolism, chemical uncoupler

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11
Q

Tetracycline

A

antibiotic, blocks binding of aminoacyl-tRNA to A-site of ribosome; acts only on bacteria

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12
Q

Streptomycin

A

antibiotic, prevents the transition from translation initiation to chain elongation and also causes miscoding; acts only on bacteria

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13
Q

Chloramphenicol

A

antibiotic, blocks the peptidyl transferase reaction on ribosomes; acts only on bacteria

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14
Q

Erythromycin

A

antibiotic, binds in the exit channel of the ribosome and thereby inhibits elongation of the peptide chain; acts only on bacteria

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15
Q

Rifamycin

A

antibiotic, blocks initiation of RNA chains by binding to RNA polymerase (prevents RNA synthesis); acts only on bacteria

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16
Q

Puromycin

A

antibiotic, causes premature release of nascent polypeptide chains by its addition to the growing chain end; acts on bacteria and eukaryotes

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17
Q

Actinomycin D

A

antibiotic, binds to DNA and blocks the movement of RNA polymerase (prevents RNA synthesis); acts on bacteria and eukaryotes

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18
Q

Cycloheximide

A

antibiotic, blocks the translocation reaction on ribosomes; acts only on eukaryotes

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19
Q

Anisomycin

A

antibiotic, blocks the peptidyl transferase reaction on ribosomes; acts only on eukaryotes

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20
Q

a-Amanitin

A

antibiotic, blocks mRNA synthesis by binding preferentially to RNA polymerase II; acts only on eukaryotes

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21
Q

Penicillin

A

acts against gram + organisms, has short half-life due to renal excretion

Paired with probenecid which impairs renal secretion

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22
Q

Penicillin V

A

oral form of penicillin

penicillin targets penicillin binding proteins in cell membrane of bacteria and prevents the cross-linking of peptidoglycan to cell membrane

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23
Q

Penicillin G

A

IV form of penicillin

Targets the penicillin binding proteins involved in cross-linking peptidoglycan to the cell membrane

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24
Q

Benzathine

A

IM form of penicillin, longer lasting

associated with irritation and local pain

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25
Aztreonam
cell wall inhibitor that binds to penicillin binding protein only works on gram-negative bacteria! use if have an allergy to penicillin
26
What are the three antibiotics that inhibit penicillinases?
Clavulanate, Sulbactam, and Tazobactam
27
What are the two antistaphlococcal penicillins and what makes them different than penicillin?
Naficillin and dicloxacillin have same mechanism as penicillin but have larger R group so resistant to penicillinases have a narrower spectrum
28
What are the two aminopenicillins?
Ampicillin and amoxicillin
29
What is the spectrum, mechanism, and combination drugs that are associated with ampicillin and amoxicillin?
Spectrum: gram-negative bacteria Mechanism: inhibit cross-linking of peptidoglycans to cell membrane by binding to penicillin binding proteins Ampicillin - Sulbactam Amoxicillin - Clavulanate
30
What are the antipseudomonal penicillins?
Ticarcillin and Piperacillin
31
What is the spectrum, mechanism and combo drugs associated with Tircacillin and Piperacillin?
Spectrum: broad, gram-negative bacilli (including Pseudomonas!) Mechanism: same as penicillin, ineffective against penicillinases Ticarcillin - Clavulanate Piperacillin - Tazobactam
32
Cephalosporins are a subclass of penicillin. What is the mechanism, bactericial/static, and where are they processed?
Mechanism: same as penicillin, bind to penicillin binding proteins which inhibit cell wall synthesis Bactericidal Cephalosporins are primarily excreted by the kidneys. Alter dosage for renal insufficiency.
33
Cephalosporins have multiple generations. What are some features of he first generation (cefazolin)?
Spectrum: gram+ | Does not cross blood-brain barrier (BBB)
34
What are some features of the 2nd generation of cephalosporins (cetoxitin, cefuroxime)?
Spectrum: more gram-negative activity, weaker gram-positive activity Doesn't cross BBB used for prophylasis treatment; can inhibit vitamin K production (prolongs bleeding); causes a disulfiram-like reaction
35
What are some features of the 3rd generation of cephalosporins (ceftriaxone, cefotaxime)?
Spectrum: streptococci and more serious gram-negative infections Can cross BBB Ceftriaxone interacts with calcium to form crytsals that precipitate in the lungs and kidneys
36
What are some features of the 4th generation of cephalosporins (cefepime)?
Cefepime = 1st (cefazolin) + 3rd (ceftazidime) Spectrum: broadest, gram+/- including Pseudomonas
37
What are some features of 5th generation cephalosporins (ceftaroline)?
Engineered to bind penicillin-binding protein 2a in MRSA (Staph. aureus)
38
Carbapenems are a subclass of penicillin. What are the carbapenem drugs and what is the spectrum, mechanism, and combo drugs associated?
Drugs: Imipenem and meropenem Spectrum: broad, but MRSA resistant Mechanism: binds to penicillin-binding proteins, low susceptibility to bate-lactamases Imipenem - Cilastatin -- if treat without, there will be renal affects
39
What is the spectrum, mechanism, and side effects of Vancomycin?
Spectrum: gram-positive, esp MRSA, C. difficile Mechanism: inhibits release of bactoprenol carrier -- prevents peptidoglycan synthesis Side effects: excreted by kidneys, nephrotoxic
40
What is the mechanism and side effects of Bacitracin?
Mechanism: inhibits dephosphorylation of bactoprenol carrier; inhibits peptidoglycan cell wall synthesis Side effects: nephrotoxic, rarely used except for opthalmic and dermatologic preparations
41
Polymyxin B is used in triple antibiotic ointment. What is the spectrum, mechanism, side effects, and bactericial/static status of polymyxin B?
Spectrum: treats MDR gram-negative, including Pseudomonas Mechanism: binds to phosphatidylethanolamine creating holes in cell membrane and release of cellular contents Side effects: nephrotoxicity Bactericidal
42
What is the spectrum, mechanism, bactericidal/static status of daptomycin?
Spectrum: gram-positive Mechanism: binds to cell membrane leading to depolarization of membrane --> cell death Bactericidal When lysine added to cell membrane, daptomycin is repelled due to positive charge
43
Rifampin: mechanism, spectrum, resistance, adverse effects, bactericidal/static
Mechanism: binds to RNA polymerase at active site, blocks mRNA elongation Spectrum: gram+/- , mycobacteria tuberculosis Resistance: intrinsic - drug unable to bind; acquired - mutation in RNA pol preventing binding Adverse effects: GI tract effects, hepatotoxic due to cytochrome P450 Note: body fluids turn orange-red!!!
44
Fixaxomicin: bactericidal/static, mechanism, spectrum, adverse effects
Bactericidal Mechanism: inhibits RNA polymerase by binding to sigma factor subunit Spectrum: narrow, used to treat recurrent C. diff infections Adverse effects: low absorption, nausea, vomiting
45
Fluoroquinolones inhibit _____ ______________?
DNA replication
46
What are the drugs within the fluoroquinolone class of drugs?
Ciprofloxacin, levofloxacin, and moxifloxacin
47
Ciprofloxacin, levofloxacin, and moxifloxacin: bactericidal/static, mechanism, spectrum, resistance, adverse effects
Bactericidal Mechanism: binds to bacterial topo II and IV topo II -- prevents relaxation of + supercoiling, gram- topo IV -- interferes with DNA separation, gram+ Spectrum: broad, gram+/- and mycoplasma Resistance: efflux of drug through transporters, gram- Adverse effects: GI, tendon rupture, prolonged QT interval Notes: chelate cations from Ca2+, Fe, Al; renal dysfunction, levofloxacin good for UTIs
48
Sulfamethoxazole: bactericidal/static, mechanism, spectrum, resistance, adverse effects
Bacteristatic Mechanism: competitive inhibitor of dihydropteroate synthetase with PABA Spectrum: don't act against bacteria, but folate pathway Resistance: increased product of PABA, increased efflux Adverse effects: crystalluria, hemolysis (G6PDH), kernitcterus (albumin-bilirubin)
49
Trimethoprim: bactericidal/static, mechanism, adverse effects, disease treatment
Bacteristatic Mechanism: sequential block of folate pathway, DHFR Adverse effects: bone marrow suppression, hyperkalemia (increased K-- heart arrythmia) Diseases treated: UTIs, Shigella, Salmonella, Pneumocystis (fungi)
50
Bactrin
combo of sulfamethoxazole and trimethoprim (TMP-SMX) sequential block of folate pathway causes these two drugs to become bactericidal
51
Metronidazole: bactericidal/static, mechanism, spectrum, adverse effects
Bactericidal Mechanism: becomes reduced (electron sink), generates free radicals to break DNA uses ferredoxin in reduced form (aerobes would have oxidized ferredoxin) Spectrum: protozoa, anaerobic bacteria including C. difficile Adverse effects: nausea, diarrhea, headache, metallic taste Note: involved in disulfiram reaction --> hangover
52
Nitofurantoin: bactericidal/static, mechanism, spectrum, adverse effects
Bactericidal Mechanism: reduce flavoproteins to reactive intermediates --> inhibits DNA, RNA synthesis Spectrum: broad Adverse effects: vomiting and pulmonary toxicity Note: ineffective outside of lower urinary tract
53
What is the disulfiram reaction?
Ethanol --ADH--> Acetaldehyde --ALDH-> Acetate Metronidazole inhibits ALDH causing an accumulation of acetaldehyde causing a hangover 2nd generation cephalosporins involved too...?
54
Linezolid
Bacteriostatic Mechanism: binds to 23S on 50S subunit Spectrum: gram-positive, including MRSA and VRE Adverse Effects: bone marrow suppression, Serotonin syndrome Note: excellent bioavailability!
55
Aminoglycosides - GNATS
Gentamicin, neomycin, amikacin, tobramycin, streptomycin Bactericidal Mechanism: prevents formation of initiation complex, misreads mRNA, induces early termination; acts on 30S subunit Spectrum: gram-negative aerobes! - need energy to enter cell Adverse Effects: Nephrotoxicity, Ototoxicity, Teratogenic (not for use by pregnant women!) Notes: large single dose more effective
56
Tetracyclines - TDM
``` Bacteriostatic Mechanism: binds to 30S subunit, preventing tRNA attachment in A-site Spectrum: broad, less now due to widespread resistance Adverse Effects: form stable chelates, GI irritation, pregnancy class D drug ```
57
Macrolides - EAC
Bacteriostatic Mechanism: inhibits translocation, binds to 23S on 50S subunit Spectrum: broad coverage of respiratory pathogens Adverse effects: GI discomfort, hepatic failure, inhibitor of cytochrome P450s Note: Clarithromycin not safe during pregnancy!
58
Chloramphenicol
Bacteriostatic Mechanism: binds to 50S, prevents peptide bond formation - peptidyltransferase Spectrum: extended, limited due to severe side effects Adverse Effects: bone marrow suppression, TOXIC, aplastic anemia, gray baby syndrome (low activity of glucuronyl transferase)
59
Clindamycin
Bacteriostatic Mechanism: blocks translocation at 50S subunit Spectrum: gram-positive, includes anaerobes Resistance: has cross-resistance with macrolides and streptogramins (Q/D) Adverse Effects: diarrhea, hypersensitivity, superinfection with C. difficile, ab pain
60
Quinupristin/Dalfopristin (Streptogramins)
Bacteriostatic (self); Bactericidal (combined) Mechanism: binds to 50S to inhibit translocation Spectrum: reserved for infections caused by MDR gram-positive bacteria Adverse Effects: inhibits cytochrome P450s

Foundations of Medicine (8 decks)

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