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Pharmacology > Pharmacology - Block 3_2 > Flashcards

Pharmacology - Block 3_2 Flashcards

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1
Q

B-lactams

A

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

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2
Q

Penicillins

A

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

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3
Q

Amoxicillin

A

Penicillins
G+ and G-
alternative for lyme disease

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4
Q

Ampicillin

A

Penicillins
G+ and G-
alternative for lyme disease

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5
Q

Penicillin G & V

A 
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
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6
Q

Piperacillin

A

penicillin
broad G-
Pseudomonas and Klebsiella

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7
Q

Ticarcillin

A

penicillin
broad G-
pseudomonas
some anaerobes

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8
Q

Oxacillin

A

penicillin

For B-lactamase-producing Staphylcocci

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9
Q

Clavulanic acid

A

B-lactamase inhibitor

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10
Q

Tazobactam

A

B-lactamase inhibitor

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11
Q

Cephalosporins

A

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

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12
Q

Cefazolin

A

1st gen cephalosporin

Most G+ activity

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13
Q

Cephalexin

A

1st gen cephalosporin

can be oral

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14
Q

Cefuroxime

A

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

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15
Q

Cefotetan

A

2nd gen cephalosporin

Good for anaerobes and Bacteriodes

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16
Q

Ceftriaxone

A

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

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17
Q

Ceftazidime

A

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

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18
Q

Cefepime

A

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

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19
Q

Imipenem

A 
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
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20
Q

Aztreonam

A 
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
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21
Q

Vancomycin

A

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

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22
Q

Fosfomycin

A

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

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23
Q

Bacitracin

A

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

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24
Q

Polymyxin B

A

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

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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

Pharmacology (8 decks)

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