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
Q

Aztreonam

A

cell wall inhibitor that binds to penicillin binding protein

only works on gram-negative bacteria!

use if have an allergy to penicillin

26
Q

What are the three antibiotics that inhibit penicillinases?

A

Clavulanate, Sulbactam, and Tazobactam

27
Q

What are the two antistaphlococcal penicillins and what makes them different than penicillin?

A

Naficillin and dicloxacillin

have same mechanism as penicillin but have larger R group so resistant to penicillinases

have a narrower spectrum

28
Q

What are the two aminopenicillins?

A

Ampicillin and amoxicillin

29
Q

What is the spectrum, mechanism, and combination drugs that are associated with ampicillin and amoxicillin?

A

Spectrum: gram-negative bacteria
Mechanism: inhibit cross-linking of peptidoglycans to cell membrane by binding to penicillin binding proteins

Ampicillin - Sulbactam
Amoxicillin - Clavulanate

30
Q

What are the antipseudomonal penicillins?

A

Ticarcillin and Piperacillin

31
Q

What is the spectrum, mechanism and combo drugs associated with Tircacillin and Piperacillin?

A

Spectrum: broad, gram-negative bacilli (including Pseudomonas!)

Mechanism: same as penicillin, ineffective against penicillinases

Ticarcillin - Clavulanate
Piperacillin - Tazobactam

32
Q

Cephalosporins are a subclass of penicillin. What is the mechanism, bactericial/static, and where are they processed?

A

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
Q

Cephalosporins have multiple generations. What are some features of he first generation (cefazolin)?

A

Spectrum: gram+

Does not cross blood-brain barrier (BBB)

34
Q

What are some features of the 2nd generation of cephalosporins (cetoxitin, cefuroxime)?

A

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
Q

What are some features of the 3rd generation of cephalosporins (ceftriaxone, cefotaxime)?

A

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
Q

What are some features of the 4th generation of cephalosporins (cefepime)?

A

Cefepime = 1st (cefazolin) + 3rd (ceftazidime)

Spectrum: broadest, gram+/- including Pseudomonas

37
Q

What are some features of 5th generation cephalosporins (ceftaroline)?

A

Engineered to bind penicillin-binding protein 2a in MRSA (Staph. aureus)

38
Q

Carbapenems are a subclass of penicillin. What are the carbapenem drugs and what is the spectrum, mechanism, and combo drugs associated?

A

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
Q

What is the spectrum, mechanism, and side effects of Vancomycin?

A

Spectrum: gram-positive, esp MRSA, C. difficile

Mechanism: inhibits release of bactoprenol carrier – prevents peptidoglycan synthesis

Side effects: excreted by kidneys, nephrotoxic

40
Q

What is the mechanism and side effects of Bacitracin?

A

Mechanism: inhibits dephosphorylation of bactoprenol carrier; inhibits peptidoglycan cell wall synthesis

Side effects: nephrotoxic, rarely used except for opthalmic and dermatologic preparations

41
Q

Polymyxin B is used in triple antibiotic ointment. What is the spectrum, mechanism, side effects, and bactericial/static status of polymyxin B?

A

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
Q

What is the spectrum, mechanism, bactericidal/static status of daptomycin?

A

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
Q

Rifampin: mechanism, spectrum, resistance, adverse effects, bactericidal/static

A

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
Q

Fixaxomicin: bactericidal/static, mechanism, spectrum, adverse effects

A

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
Q

Fluoroquinolones inhibit _____ ______________?

A

DNA replication

46
Q

What are the drugs within the fluoroquinolone class of drugs?

A

Ciprofloxacin, levofloxacin, and moxifloxacin

47
Q

Ciprofloxacin, levofloxacin, and moxifloxacin: bactericidal/static, mechanism, spectrum, resistance, adverse effects

A

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
Q

Sulfamethoxazole: bactericidal/static, mechanism, spectrum, resistance, adverse effects

A

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
Q

Trimethoprim: bactericidal/static, mechanism, adverse effects, disease treatment

A

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
Q

Bactrin

A

combo of sulfamethoxazole and trimethoprim (TMP-SMX)

sequential block of folate pathway causes these two drugs to become bactericidal

51
Q

Metronidazole: bactericidal/static, mechanism, spectrum, adverse effects

A

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
Q

Nitofurantoin: bactericidal/static, mechanism, spectrum, adverse effects

A

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
Q

What is the disulfiram reaction?

A

Ethanol –ADH–> Acetaldehyde –ALDH-> Acetate
Metronidazole inhibits ALDH causing an accumulation of acetaldehyde causing a hangover

2nd generation cephalosporins involved too…?

54
Q

Linezolid

A

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
Q

Aminoglycosides - GNATS

A

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
Q

Tetracyclines - TDM

A
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
Q

Macrolides - EAC

A

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
Q

Chloramphenicol

A

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
Q

Clindamycin

A

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
Q

Quinupristin/Dalfopristin (Streptogramins)

A

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