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Pharm Drug Flashcards > Exam 5 > Flashcards

Exam 5 Flashcards

0
Q

Penicillin V

A

Natural penicillin
Like G, but acid stable
Narrow spec, Gm+, destroyed by beta-lactamase
Given orally, absorption is unstable

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1
Q

Penicillin G

A

Natural penicillin
Narrow spec, mostly Gm+
Destroyed by beta-lactamase
Given IV/IM w/ procaine, hydrolized in stomach acid

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2
Q 
Naficillin
Oxacillin
Cloxacillin
Dicloxacillin
Methicillin
A 
Beta-lactamase resistant penicillins
Narrow spec
Naficillin- Not AFfected by beta-lactamase
Ox- resistant to change
Methicillin- not used, toxic MRSA
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3
Q 
Amoxicillin
Ampicillin
Ticarcillin
Piperacillin
Mezlocillin
Carbenicillin
A

Broad/extended spec penicillins
None are penicillinase resistant!
Ampicillin- causes rash in px with mononucleosis

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4
Q

Sublactam

Clavulanic acid

A

Non-antibiotic beta-lactam ring compounds
Inhibit penicillinase
Usually given in combo with broad spec penicillins to occupy penicillinase

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5
Q

Cephalosporins

Ceph- or cef-

A

Broader spec
Greater resistance to beta-lactamases
Each generation has more Gm- activity & greater resistance than previous
SE: some allergic rxn in penicillin-sensitive px
Possibility of superinfxn

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6
Q

Imipenem

A 
Carbapenem (penicillin analog)
Very broad spec
Given IV
Better vs Gm+
Metabolized in kidney to nephrotoxin, given with cilastatin to inh that enzyme
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7
Q

Meropenem

A 
Carbapenem (penicillin analog)
Resistant to beta-lactamase
Very broad spec
Given IV, enters CNS more readily
More effective against Gm-
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8
Q

Aztreonam

A 
Monobactam
IV/IM
Not affected by beta-lactamases
Only useful with aerobic Gm- (E. coli)
Not x-reactive with penicillin allergic px
SE: seizures
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9
Q

Vancomycin

A

Binds to dialanine residues on subunits of cell walls
Prevents x-linking
Used vs Gm+ staph infxn
IV, except for pseudomembranous colitis (given oral, pseudotopical)
SE: nephrotoxic
Ototoxic
Rapid IV -> causes histamine release (redman/redneck syndrome)
Resistance (dialanine substituted by lactic acid)

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10
Q

Televancin

Dalbavancin

A 
Lipoglycopeptides
Act both like vancomycin and cell membrane distruptors
SE: renal damage
       Fetal damage
       Metallic taste in mouth
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11
Q

Bacitracin

A

Inh recycling of bactoprenol carrier
Used vs Gm+ cells
Only given topically, extremely nephrotoxic

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12
Q

Fosfomycin

A

Blocks synth of n-acetylmuramic acid
Used vs Gm- (E. coli)
For uncomplicated UTI

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13
Q

Cycloserine

A

Inh incorporation of alanine into n-acetylmuramic acid
Used vs Mycobacterium TB
SE: sedation, tremor, psychosis

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14
Q

Erythromycin

A 
Macrolide
Reversible binds to 50s subunit
Inhibits translocation of mRNA
Inhibits binding of tRNA to P site of ribosome 
SE: GI upset
      Strong inh of P450
      Liver damage, cardiac arrhythmias
Used vs Gm+
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15
Q

Clarithromycin
Azithromycin
Telithromycin

A

Macrolides
Inhibit bacterial protein synth by inhibiting an enzyme
C- oral stability, H. pylori
Az- T1/2 of 3 days
T- induces less resistance, readily transported out of cell
SE: inh P450
Severe hepatotoxicity
Worsening MG
Block cholinergic receptors in mm (atropine)

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16
Q

Streptomycin

A 
Aminoglycoside
Irreversibly binds to 30S subunit
Can inh tRNA binding all along mRNA 
Including initiation site
Irreversible in mRNA, given IM
SE: very ototoxic
       very nephrotoxic (most common cause of drug-related nephrotox)
       High doses --> decrease ACh and ACh receptors
       Preg cat D
Targets aerobic Gm-
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17
Q 
Gentamycin
Tobramycin
Neomycin
Amikacin
Kanamycin
Netilmicin
A

Aminoglycosides
Inhibit bacterial protein synth by inhibiting an enzyme
Neomycin- VERY nephrotoxic, used topically or orally

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18
Q

Tetracycline

A

Reversible binds to 30S subunit (static!)
Inh binding of tRNA to A site
SE: binds to cations Ca++, Fe++, Al+++
Deposited in bones & teeth of fetus (Preg Cat D)
Degrades with time into renal/hepatotoxin
Targets: rickettsia, spriochetes, helicobacter, legionella

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19
Q

Doxycycline
Minocycline
Tigecycline

A

Tetracyclines
Inh binding of tRNA to A site by binding to 30S subunit
Degrades into renal/hepatotoxin
Less likely to bind to Ca++

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20
Q

Chloramphenicol

A 
Inhibits peptidyl transferase
SE: inh P450
       aplastic anemia
       Grey Baby Syndrome
        metab by Phase II enz, not active in newborn, vasomotor collapse
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21
Q

Clindamycin

Lincomycin

A

Lincosamides
Like erythromycin, inh translocation in ribosome
SE: severe superinfxn with C. difficile
Target: severe anaerobic infxns (penetrating gut wound)
Dental prophy with heart valve

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22
Q

Quinupristin + dalfopristin

A 
Always used together
Q- inh A & P sites
D- inh P site
SE: mm pain
Target: Gm+
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23
Q

Linezolid

A

Inh binding of methionyl tRNA to P site
Prevents initiation of synth process
SE: anemia, pseudomembranous colitis (like all strong antibiotics)

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24
Q

Daptomycin

A 
Lipopeptide
Disrupts bacterial cell membranes
Forms pores in cell membrane
SE: mm pain/weakness
      Eosinophilic pneumonia 
Targets: aerobic Gm+ (staph/strep skin infxn)
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25
Q

Fidaxomycin

A

Inhibits C. difficile RNA polymerase

Given orally, not systemically absorbed

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26
Q

Ciprofloxacin

Other -floxacins

A

Inhibit topoisomerase II/IV
No effect on mammalian topoisomerase
SE: may damage developing cartilage (no kids or prego)
Tendonitis, Achilles’ tendon rupture
Phototoxicity
Worsen MG
Target: broad spec acid fast & Gm+/-

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27
Q

Sulfonamides

A 
Reversible inh dihydropterate synthetase
SE: Stevens Johnson Syndrome
      Hemolytic anemia in G6PDH deficient px
      Megaloblastic anemia
Target: UTI
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28
Q

Trimethoprim

A

Inh bacterial dihydrofolate reductase
Like methotrexate for bacteria
Used in conjunction with sulfamethoxazole
SE: megaloblastic anemia (avoided w leucovorin)
Target: Gm- bacteria
UTIs, concentrates in acidic prostate/vaginal tissue

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29
Q

Metronidazole

A

Prodrug- activated to free radical maker by obligate anaerobes
IV for severe anaerobic infxns
IV for protozoal infxns (trichomonas, giardiasis)
SE: seizures, peripheral neuropathy

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30
Q

Nitrofurantoin

A

Reduced by bacteria to highly active molecule
UTI
SE: cough, chest pain, brown urine

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31
Q

Polymixin B

A

Binds to (-) charged side of LPS of Gm- bacteria
Increases membrane permeability
Topical
SE: nephrotoxic
neurotoxic
Reversible neuromuscular blocker (ataxia, perioral paresthesia)

32
Q

Gramicidin

A

Mix of 3 peptide antibiotics
Forms pores in Gm+ bacteria
SE: systemic toxicity

33
Q

Neomycin

A

Aminoglycoside

Topical only

34
Q

Retapamulin

A

Inh peptidyl transferase

Topical Tx of skin staph/strep infxn

35
Q

Mupirocin

A

Inhibits bacterial isoleucyl tRNA synthesis
For staph infxns
Very specific target

36
Q

Isoniazid

A 
Antimycobacterial enzyme inhibitor
Prodrug, produces inhibitor of multiple mycobac. enzymes
Inhibits cell wall synthesis
Used for prophy 
Metabolized by acetylation
SE: increased excretion of vit B6 (leads to pellegra)
      Peripheral neuropathy
      Optic neuritis
      Hepatotoxic
37
Q

Rifampin

A 
Antimycobacterial enzyme inh
Inh DNA-dependent RNA polymerase
SE: hepatotox
       Red color in all body fluids
       Strongly induces P450 (little surprise story)
38
Q

Pyrazinamide

A

Prodrug- converts in macrophages where TB lives
Inh fatty acid synth by TB
SE: gout, hepatitis

39
Q

Ethambutol

A

Inh arabinosyl transferase
Necessary for cell wall synth
SE: optic neuritis
Impaired R/G discrimination

40
Q

Bedaquiline

A

Inh mycobacterial ATP synthetase
SE: arrhythmias, death
Always used with at least 3 other anti TB drugs

41
Q

Dapsone

A

Related to sulfonamides

For mycobacterium leprae (Leprosy)

42
Q

Nystatin

A

Topical polyene antifungal for skin infxn
Bind to ergosterol in cell membranes and forms pores
Can be given pseudoorally (topical in gut)

43
Q

Natamycin

A

Topical polyene antifungal for skin infxn

Only antifungal approved for use in eye

44
Q

Tolnaftate
Ciclopirox
Terbinafine
Other -fines

A

Topical antifungals for ringworm

Terbinafine - liver damage

45
Q

Griseofulvin

A

Systemic antifungal for nail fungal infxn
Taken up by growing skin cells, concentrated in keratin
Binds to fungal microtubules, inhibits mitosis
SE: headache
Induces P450
Allergic rxn (derived from penicillium mold)

46
Q

Terbinafine

A 
Inhibits ergosterol synthesis
Inh squalene epoxidase (enzyme)
Decrease in ergosterol synth (malformed membrane)
Increase in squalene buildup (toxic)
Metabolized by & inh P450
47
Q

Amphotericin B

A 
Systemic polyene antifungal
DOC for systemic fungal infxn
Binds to ergosterol and forms pores in cell membrane
Treat for 2-4 mo. IV or intrathecal
SE: "amphoterrible B"
      Impaired renal fxn >80%
      Fever, chills, vomiting
      Convulsions, severe headaches
      Anemia
48
Q

Imidazole
Miconazole
Ketoconazole

A

Inh fungal CYP450, including ionosterol 14-alpha demethylase
Inhibits ergosterol synthesis
Used topical vs candida and ringworm
SE: nausea, GI
Hepatotoxic
Inh of human P450
Decreased adrenal/gonadal steroid synth

49
Q

Fluconazole

A

Triazole derivative conazoles
Fungistatic
Lowest effect on human P450
SE: teratogenic, hallucinations, hepatotox

50
Q

Itraconazole

A

Fungistatic triazole deriv for systemic fungal infxn
Strongest effect on man P450
Worsens CHF and arrhythmias

51
Q

Posaconazole

Voriconazole

A

Fungistatic triazole derivs
Inhibit fungal P450
V-can cause visual disturbances

52
Q

Flucytosine

A 
Antifungal pyramidine analog
Inh thymidine synthelase 
Prodrug, doesn't enter mammalian cells as readily
Converted to 5-flurorouracil in fungi
SE: used in combo with ampho B
       GI upset
       Bone marrow depression
       Hepatotoxic
53
Q

Caspofungin
Micafungin
Anidulafungin

A

Fungicidal
Inh synth of fungal cell wall component
Given slow IV over 91 hours
SE: rash, fetal damage

54
Q

Acyclovir

A

Herpes simplex and zoster
Prodrug, inh viral DNA polymerase
Must be phosphorylated by a viral kinase
Active form incorporates into viral DNA
Higher affinity for viral DNA polymerase than human
SE: GI upset, renal damage, delirium when given IV

55
Q

Valacyclovir

A

Prodrug, converts into acyclovir after first pass metabolism
Given orally
Inhibits viral DNA polymerase

56
Q

Famciclovir

A

Prodrug, herpes
Converted by first pass into acyclovir analog
Inhibits viral DNA polymerase

57
Q

Ganciclovir

A

CMV
Prodrug, activated by viral kinase
Inh viral DNA polymerase
SE: neutropenia, thrombocytopenia, teratogenic

58
Q

Valganciclovir

A

CMV
Converted into ganciclovir by first pass
Inh viral DNA polymerase

59
Q

Cidofovir

A

CMV
Prodrug, converted by HOST kinase
Only used when virus changed its viral kinase
SE: nephrotoxic

60
Q

Foscarnet

A

CMV
Not a prodrug, directly inh viral DNA polymerase
Given IV 3x/daily
SE: Renal damage

61
Q 
Lamivudine
Adefovir
Telbivudine
Tenofovir
Entecavir
A

Inh Hep B reverse transcriptase
LATTE
Ade- SE: liver, renal damage
TTE- SE: lactic acidosis, hepatomegaly

62
Q

Ribavirin

A 
For RSV, not used often
Phosphorylated in cell
Inhibits RNA-dependent DNA polymerase
SE: $1000/day
       Preg Cat X
       Hemolytic anemia
       Deceased pulmonary fxn in infants & cardiac arrest
63
Q

Palivizumab

A 
RSV
Humanized immune system MAB 
Blocks fusion of virus to target cell by blocking antigen site on RSV
Blocks a receptor
Used only prophylactically
64
Q

Amantadine

Rimantidine

A

Influenza A
Widespread resistance
Blocks transporter/ion channel
Prevents H+ channels from forming in endosomes
SE: renal failure
Teratogenic
CNS –> dizziness, slurred speech, confusion, nausea

65
Q

Zanamivir

Oseltamivir

A 
Influenza A & B
Neuraminidase inhibitor
Prevents virus from budding off host cell
SE: nausea, diarrhea
       Psychosis, hallucinations
66
Q

Recombinant interferon alpha

A 
Hep C
Cytokines, multiple mechanisms
Enhances normal immune cell fxn
Inh mRNA processing
SE: fatigue
      flu-like symptoms
      depression
      hypertension 
      retinopathy
      myelosuppression
67
Q

Boceprevir
Telaprevir
Simeprevir

A

Hep C protease inhibitors

Used in combo with interferon alpha

68
Q

Sofosbuvir

A

Prodrug
Inh Hep C RNA-dependent RNA polymerase
Ledipasvir + sofosbuvir = binds protein for HCV replic.

69
Q 
Didanosine
Abacavir
Zidovudine
Lamivudine
Emtricitabine
Stavudine
Telbivudine
A

Nucleoside analog Reverse Transcriptase Inhibitor
DAZ LES-T
Phosphorylated in cell, bind to reverse transcriptase
SE: life threatening hepatomegaly & lactic acidosis
myopathy, anemias, pancreatitis, neuropathies

70
Q

Nevirapine

A

NNRTI 1st gen
Binds to nonactive on RT
hepatotoxicity, S-J syndrome

71
Q

Delaviridine

A

NNRTI 1st gen
Hepatotoxic
P450 inhibitor

72
Q

Efavirenz

A

NNRTI 1st gen
CNS tox (hallucinations, memory loss)
Rash
Street drug

73
Q

Etravirine

Rilpivirine

A

NNRTI 2nd gen

Higher potency, longer T1/2, less SEs

74
Q 
Saquinavir
Ritonavir
Indinavir
Nelfinavir
Atazanavir
Darunavir
A

Protease inhibitors -navirs
Prevent formation of active viral proteins from peptide precursors
Ritonavir- most potent P450 inhibitor
SE: altered fat distribution (skinny limbs face, fat gut chest back)
increased diabetes

75
Q

Tipranavir

Fosamprenavir

A

Protease inhibitors -navirs

Contain sulfur molecule, allergy possible

76
Q

Enfuvirtide

A

Fusion inhibitor
Binds to target binding site on virus
SE: insomnia

77
Q

Maraviroc

A

Fusion inhibitor
Binds to binding site on Macrophage
SE: hepatotox, allergic rxn, increase risk of MI

78
Q

Reltegravir
Dolutegravir
Elvitegravir

A

Integrase inhibitor
Inh HIV-1 integrase
-tegravirs

Pharm Drug Flashcards (4 decks)

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