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Flashcards in Pharmacology - Block 3_2 Deck (99):
1

B-lactams

bactericidal
G+, G-
most effective on actively growing bacteria
inhibit PBP cross-linking (competitive, irreversible)
time-dependent killers
resistance: B-lactamase or altered PBPs

2

Penicillins

B-lactams
well distributed, short half lives, time-dependent
mostly renal excretion
adverse: allergic rxn, severe
fever, diarrhea, enterocolitis
hepatotoxicity, hemolytic anemia, seizures
can be given with B-lactamase inhibitors

3

Amoxicillin

Penicillins
G+ and G-
alternative for lyme disease

4

Ampicillin

Penicillins
G+ and G-
alternative for lyme disease

5

Penicillin G & V

penicillin
V is more acid-stable
G+, G- cocci
G+ anaerobes, not B. fragilis
Strep pneumonia, other strep
Neisseria meningitidis
syphilis
also anthrax, listeria, Actinomyces

6

Piperacillin

penicillin
broad G-
Pseudomonas and Klebsiella

7

Ticarcillin

penicillin
broad G-
pseudomonas
some anaerobes

8

Oxacillin

penicillin
For B-lactamase-producing Staphylcocci

9

Clavulanic acid

B-lactamase inhibitor

10

Tazobactam

B-lactamase inhibitor

11

Cephalosporins

Well distributed, only some to the CNS
Most require injection
short half lives
mechanism like other B-lactams
resistances similar to penicillins
adverse: allergic rxn, nausea, GI, hepatocellular damage
1st gen: G+, surgical prophylaxis of skin flora
2nd gen: more G-, less Staph
3rd gen: more G-, good for Klebsiella, enterobacter, proteus
4th gen: IV, more resistant to B-lactamases

12

Cefazolin

1st gen cephalosporin
Most G+ activity

13

Cephalexin

1st gen cephalosporin
can be oral

14

Cefuroxime

2nd gen cephalosporin
can be oral, also gets to CNS
Good for Haemophilus

15

Cefotetan

2nd gen cephalosporin
Good for anaerobes and Bacteriodes

16

Ceftriaxone

3rd gen cephalosporin
Gets into CNS, choice for bacterial meningitis
also choice for gonorrhea

17

Ceftazidime

3rd gen cephalosporin
Good for Ps. aeruginosa
Gets into CNS

18

Cefepime

4th gen cephalosporin
Gets into CNS, less susceptible to B-lactamases
choice for serious inpatient infxns

19

Imipenem

B-lactam
broad spectrum, G+ G-, aerobe, anaerobe
resistant to many B-lactamases
NOT good for MRSA or meningitis
used for mixed or ill-defined infxns
adverse: hypersensitivity, seizures, GI

20

Aztreonam

B-lactam
G- aerobic rods
resistant to many B-lactamases
can be used in penicillin hypersensitive
given IV, well distributed
seizures, cramps, GI, EKG changes, anaphylaxis

21

Vancomycin

Glycopeptide antibiotic
bactericidal
inhibits cell wall synthesis, binds D-ala
G+ only
MRSA 1st line
also C. diff
not absorbed, so IV for systemic or oral for GI only
primarily for serious infxns
'red-man' syndrome, nephrotoxicity, phlebitis, ototoxicity

22

Fosfomycin

Inhibits peptidoglycan building block synthesis, inactivates enolpyruvyl transferase
used for uncomplicated UTIs caused by E. coli, enterococcus
long duration
headache, GI, vaginitis

23

Bacitracin

Interferes w/ cell wall synthesis via lipid carrier
Topical use only
G+
sides: rare allergic dermatitis

24

Polymyxin B

Polymyxin
cationic detergent that binds LPS in outer membrane
G-
topical use for pseudomonas
systemic use has serious nephro and neurotoxicity side effect

25

Daptomycin

Cyclic lipopeptide
binds to bacterial ctoplasmic membrane, causes rapid depolarization
bacteriocidal
used for complicated skin infxns (MRSA, Staph, Strep, Entero)
also for staph bacteremia
IV admin
sides: GI, muscle pain

26

Quinolones

Inhibit DNA gyrase, bactericidal
resistance: altered gyrase, decreased permeability
sides: GI, nausea, enterocolitis, dizzyness, headache, depression
rare seizures, peripheral neuropathy, arthropathy, tendon rupture
not for pregnant or children
can get serious photosensitive rashes and EKG irregs

27

Norfloxacin

fluorinated Quinolone
used for UTIs (entero, some P. aug, Staph)

28

Ciprofloxacin

fluorinated Quinolone
used for UTIs (entero, some P. aug, Staph)
infectious diarrhea, skin infxns, bone and joint infxns, anthrax, chlamydia

29

Moxifloxacin

fluorinated Quinolone
better G+ activity
used for resp infxns, not strep throat
CA-pneumonia, bacterial bronchitis

30

Nitrofurantoin

makes free radicals, damages bacterial DNA
used for UTIs
sides: GI, peripheral neuropathy, hypersensitivity, pulmonary rxns, liver damage, granulocytopenia, hemolytic anemia

31

Rifampin

Binds RNA polymerase, inhibits bacterial mRNA synthesis, bactericidal
used for pulmonary TB and prophylaxis for meningicoccal and H. influenza meningitis
sides: hepatotoxicity, strongly induces P450s, orange color

32

Fidaxomicin

Inhibits RNA polymerase, bactericidal
used as last-ditch C. diff drug
oral, poorly absorbed
sides: GI upset, expensive

33

Metronidazole

Anaerobes reduce nitro group-> DNA damage, bactericidal
used for anaerobes, C. diff (1st choice), H. pylori, G. vaginalis
sides: GI, leuko/neutropenia, thrombophlebitis, fungal superinfxns

34

Aminoglycosides

Bactericidal
NOT orally
transported into cell via AEROBIC process
binds to ribosome, stops initiation, mRNA misreading
long duration due to post-antibiotic effect
concentration dependent killers
resistance: modification of drug
more G-, only aerobes
toxic, only for serious,, nephro/ototoxicity, sometimes neuromuscular blockade
poor CSF penetration

35

Gentamicin

Aminoglycoside antibiotic

36

Tobramycin

Aminoglycoside antibiotic

37

Amikacin

Aminoglycoside antibiotic
most resistant to bacterial resistance

38

Tetracyclines

Bacteriostatic
transported into cells, binds 30S ribosome, prevents tRNA attachment
resistance: transport drugs out of cell
resistance is widespread
used for: rickettsia, chlamydia, Mycoplasma, Ureaplasma, Borrelia
alternative for syphilis and gonorrhea
oral admin, Ca inhibits absorption
sides: GI, enterocolitis, photosensitive rash, teeth discolorization

39

Doxycycline

Tetracycline antibiotic
longer half life, more lipophilic

40

Minocycline

Tetracycline antibiotic
longer half life, more lipophilic

41

Tigecycline

Bacteriostatic
Similar to Minocycline
also binds unique ribosome site so not cross-resistant
broad spectrum
used for skin infxns, complicated intrabdominal infxns, and CA pneumonia
IV only
sides: like tetracyclines
FDA alert: death risk, less efficacious

42

Chloramphenicol

Bacteriostatic
inhibits tRNA binding to 50S ribosome and inhibits peptide bond formation
broad specturm, G+, G-, aerobe, anaerobe
very serious side effects
used for alternate for meningitis and brain abcesses
causes bone marrow depression, fatal aplastic anemia
grey baby syndrome, optic neuritis, GI effects

43

Macrolides

Bacteriostatic
bind 50S ribosome, blocks translocation
resistance: efflux pumps, methylate

44

Erythromycin

Macrolide antibiotic
G+, alternative to B-lactams
effective for: Strep, some Staph, chlamydia, mycoplasma, legionella, bordetella
sides: increased GI motility, inhibits CYP3A4, arrhythmias

45

Clarithromycin

Macrolide antibiotic
slightly wider spectrum than erythromycin
used for pharyngitis, resp infxns
plus: Haemophilus, Moraxella, and pen-resistant Strep pneumonia
also Helicobacter pylori and atypical mycobacteria (MAC prophylaxis, bactericidal)
less GI effects, but more prolonget QT interval

46

Azithromycin

Macrolide antibiotic
used for respiratory infxns
better G- than the others
also genital chylamidia, gonorrhea (2nd)
long excretion half-life, better respirator penetrance
fewer GI probs, few drug interactions

47

Clindamycin

Macrolide-like antibiotic
used for G+ and anaerobes, incl B. fragilis
limited use due to serious colitis risk
also hepatotoxicity, GI irritation

48

Linezolid

bacteriostatic
binds 50S, prevents formation of 70S ribo
G+ aerobes only
used for: VRE, Staph aureus (MRSA), Strep
IV or oral, high penetrance
sides: inhibitor of MAO
GI effects, bone marrow suppression

49

Sulfonamides

Bacteriostatic
inhibit folate synthesis, inhibit sihydropteroate synthase
used for UTIs, bacillary dysentery, typhoid fever
sides: hypersensitivity, rashes, GI, renal damage from crystalluria (less soluable metabolites), inhibits CYP2C9

50

Sulfamethoxazole

Sulfonamide antibiotic
often given with trimethoprim

51

Silver Sulfadiazine

Sulfonamide antibiotic
topical use for burn patients (prophylaxis and treatment)

52

Trimethoprim

Bacteriostatic
inhibits folate synthesis, inhibits dihydrofolate reductase
used with sulfamethoxazole -> bacteriocidal
used for UTIs, upper respiratory and ear infxns, and Pneumocystis, salmonella, shigella
NOT for anaerobes
sides: GI, bone marrow suppression

53

Isoniazid

antimycobacterial (TB)
inhibits synthesis of mycolic acids
prodrug activated by KatG, targets InhA, which blocks fatty acid elongation
most important anti-TB drug
there are slow and rapid acetylators
sides: neurotoxicity, peripheral neuritis, hepatotoxicity

54

Rifampin

antimycobacterial (TB)
inhibits RNA polymerase, bactericidal
never used alone, oral
also used for Leprosy
sides: hepatotoxicity, induces multiple CYPs, orange color

55

Ethambutol

antimycobacterial (TB)
interferes with arabinosyl transfewrase, blocks cell wall synthesis
tuberculostatic
sides: well tolerated, optic neuritis

56

Pyrazinamide

antimycobacterial (TB)
blocks mycolic acid synthesis by inhibitis fatty acid synthase I
bactericidal
important for short-term therapy, usually withdrawn
widely dist, incl CSF
sides: hepatic damage, GI

57

Streptomycin

antimycobacterial (TB)
aminoglycoside, bactericidal
reserved for most serious TB
doesnt get into cells or into CNS
sides: nephro/ototoxicity

58

Rifabutin

atypical antimycobacterial
rifampin analog
used for M avium-intracellulare (MAC) in AIDS pts
sides: similar to, less than rifampin, less potent CYP inducer

59

Dapsone

Anti-leprosy
mechanism same as sulfonamides (inhibits folic acid synthesis), bacteriostatic
used for Pneumocystis in AIDS
widely distributed
slow and fast acetylators
sides: hemolytic anemia, methemoglobinemia

60

Clofazimine

anti-leprosy
mechanism unknown, binds DNA
sides: well tolerated, red color

61

Amphotericin B

anti-fungal
effective broad spectrum for serious systemic infxns
very lipophilic, binds ergosterol, causes membrane leakage
IV for 6-12 weeks
can be used topically for Candida
not absorbed via GI, oral for GI ifxns
total cumulative dose determines renal toxicity
"amphoterrible" sides: fever, GI, hypotension, nephrotoxicity, anemia, hypokalemia, tachypnea

62

Flucytosine

anti-systemic-fungal
fungi convert 5-FC to 5-FU, metabolites of 5-FU block nucleic acid synthesis
used for serious Candida and Cryptococcus
used in cunjunction w/ Amphotericin
sides: GI, leukopenia, thrombocytopenia, elevated liver enzymes
use w/ caution with renal insufficiency or bone marrow suppression

63

Imidazoles, Triazoles

Anti-fungals
inhibit 14a-sterol demethylase (fungal P450), blocks final step of ergosterol synthesis, fungistatic
sides: nausea, GI, hepatotoxicity, inhibits metabolism of many drugs

64

Fluconazole

anti-fungal
used for Cryptococcus meningitis
narrowest Candida
good CNS penetrance
also used for vaginal/urinary/oral Candida

65

Itraconazole

anti-fungal
used for: Blastomyces, Histoplasma
middle Candida
also 3-month therapy for nail infxns
NO CNS
contraindicated w/ drugs that inhibit CYP3A4

66

Voriconazole

anti--systemicfungal
used for Aspergillus
broadest Candida
also for Oral/esophageal Candida
some CNS penetrance
sides: visual disturbance, photosensitive rash

67

Caspofungin

anti-systemic-fungal
used for Aspergillus (2nd)
broad Candida coverage
inhibits cell wall synthesis
sides: well tolerated, fever, GI, phlebitis

68

Miconazole

anti-superficial fungal
same mechanism as fluconazole
creams for vaginal Candida
also for dermatophytes
sides: burning, irritation

69

Clotrimazole

anti-superficial-fungal
oral or vaginal Candida
also for dermatophytes
mechanism similar to fluconazole
topical use
sides: may cause abnormal liver function tests

70

Nystatin

anti-superficial-fungal
used for Candida
similar to Amphotericin B
seldom toxic as topical
oral: bad taste

71

Natamycin

anti-opthalmic fungal
used for fungal eye infxns
similar to amphotericin B
sides: chemosis, hyperemia

72

Tolnaftate

"Tinactin"
anti-dermatophyte
cream/spray/powder (topical)
NOT for Candida
no sides

73

Terbinafine

anti-dermatophyte
topical use or
oral 12-week nail infxn therapy
inhibits squalene epoxidase, fungicidal due to squalene buildup
sides: diarrhea, GI pain

74

Ciclopirox

anti-dermatophyte
topical use for nail infxns
few sides

75

Griseofulvin

anti-dermatophyte
long-term oral treatment for recalcitrant superficial mycoses
good for children, esp tinea capitis
narrow spectrum
sides: rare, not for use with liver disease, increased metabolism of other drugs, caution with penicillin allergies

76

Amantadine

Anti-viral
prophylaxis and treatment of influenza A
some resistant strains now
blocks viral uncoating by interfering with M2
sides: CNS effects

77

Ostelamivir

anti-viral
prodrug
inhibitor of NA, blocks viral release
treatment of influenza A+B (w/in 48hrs),, also prophylaxis
sides: nausea, bronchitis

78

Trifluridine

anti-viral
thymidine analog, blocks DNA synthesis
Ophthalmic use, Herpes simplex 1,2

79

Acyclovir

anti-viral
inhibits herpes DNA polymerase,, inhibitor of dGTP, DNA chain terminator,, phosphorylated form produced 100x by herpes thymidine kinase
IV: servious systemic herpes simplex, severe genital herpes
Oral: primary genital herpes, herpetic gingivostomatosis
Topical: apply early to primary genital herpes
Also for chickenpox
well tolerated, rash, nausea

80

Famciclovir

anti-viral
prodrug converted to Penciclovir, then phosphorylated
similar to Acyclovir, blocks DNA polymerase
used for acute herpes zoster and recurrent genital herpes
better absorbed than acyclovir

81

Pencyclovir

anti-viral
similar to acyclovir
Topical only for recurrent face herpes
sides: skin irritation

82

Ganciclovir

anti-viral
similar to acyclovir, but phosphorylated by CMV protein kinase
treat CMV retinitis, phophylaxis
sides: bone marrow suppression

83

Foscarnet

anti-viral
inhibits CMV DNA polymerase, binds pyrophoshate binding site
does not require conversion to be active
used for CMV retinitis and resistant herpes simplex
sides: renal damage, electrolyte imbalance, seizures

84

Lamivudine

anti-viral
nucleoside analog inhibitor of reverse transcriptase of HepB DNA polymerase
used for HepB and HIV
sides: nausea, diarrhea

85

Tenofovir

anti-viral
adenosine monophosphate analog, inhibits reverse transcriptase of HepB DNA polymerase
used for HepB and HIV
sides: GI upset

86

Ribavirin

anti-viral
nucleoside analog, blocks viral RNA synthesis, inhibits inosine-5-P dehydrogenase and thus GTP synthesis, inhibits GTP-dependent capping
aerosol use in infants with severe RSV
also for HepC, combo with INFa
clogs respiratory equipment, rash, bone marrow suppression

87

Interferon

anti-virals
host-produced proteins
Condyloma acuminata (venereal warts)
HepB,C
PEG-alfa-2a,b in combo with Ribavarin used for HepC
sides: flu-like, bone marrow suppression, neurotoxicity

88

Boceprevir

anti-viral
inhibitor of HepC NS3 protease, blocks bormation of infxious particles
for HepC(1): use in combo with PEG-INF+ribavarin (all 3)
sides: anemia, CYP3A effectors

89

Zidovudine

anti-HIV (NRTI)
AZT
thymidine analog, phosphorylated by cellular kinases, inhibits reverse transcriptase, also DNA chain terminator
sides: bone marrow suppression, interaction with drugs that inhibit glucuronyl transferase, myopathy

90

Lamivudine

anti-HIV (NRTI)
similar mechanism to AZT
synergistic with AZT
sides: nausea, diarrhea

91

Tenofovir

anti-HIV (NRTI)
nucleotide prodrug, inhibits RT by competing with dATP, DNA chain termination
well-tolerated

92

Emtricitabine

anti-HIV (NRTI)
similar to Lamivudine
3TC analog, inhibits RT, competes for dCTP incorporation, DNA chain termination

93

Abacavir

anti-HIV (NRTI)
nucleoside analog inhibitor of RT
sides: hypersensitivity, assoc w/ HLA-B*5701 antigen (6%)

94

Efavirenz

anti-HIV (NNRTI)
inhibits RT, does not need activation
sides: rash, CNS, nightmares

95

Lopinavir

anti-HIV
protease inhibitor
prevents viral processing of Gag-pol polypeptide
results in non-infxious particles
used in combo, much decreased viral load
sides: diabetes, altered lipids, fat redist, CYP3A effects

96

Ritonavir

anti-HIV
boosts protease inhibitor levels
sides: CYP3A effects

97

Enfuvirtide

anti-HIV
used for HIV-1, when still viral load after other therapy
inhibits fusion of HIV-1 to cellular CD4
binds gp41 subunit
subcutaneous injection 2/day
sides: local injection site reaction, diarrhea

98

Maraviroc

anti-HIV
used for CCR5-tropic HIV-1
CCR5 antagonist, blocks entry
sides: hepatotoxicity, CV events

99

Raltegravir

anti-HIV
used for resistant HIV-1
inhibits HIV-1 integrase, prevents DNA integration
well-tolerated