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Pharmacology 1 > Exam 3 Diaz > Flashcards

Exam 3 Diaz Flashcards

1
Q

What does Isoniazid active against?

A

mycobacteria

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2
Q

What are extended spectrum antibiotics?

A

work against gram positive and a significant amount of gram negatives. Ampicillin

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3
Q

What are broad spectrum? Example?

A

affect a variety of microorganisms, but this can affect normal flora and lead to take over of candida albicans. Tetracycline

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4
Q

What are narrow spectrum drugs? Example?

A

Only treats a specific form of bacteria. Isoniazid

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5
Q

What meds are cell membrane inhibitors?

A

Isoniazid
Amphotericin B
Polymyxins

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6
Q

What meds are inhibitors of nucleic acid function or synthesis?

A

Fluoroquinolones

rifampin

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7
Q

What meds are protein synthesis inhibitors?

A 
Tetracyclines
aminoglycosides
macrolides
clindamycin chloramphenicol 
linezolid
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8
Q

Cell wall inhibitors

A 
beta lactams
vancomycin 
telamicin 
fosfomycin 
daptomycin
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9
Q

metabolism inhibitors?

A

sulfonamide

trimethoprim

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10
Q

Types of beta lactam antibiotics

A

penicillin
cephalosporins
carbapenems
monobactams

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11
Q

Types of Beta lactamase inhibitors

A

calvulinic acid
sulbactam
tazobactam

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12
Q

Other antibiotics that are cell wall inhibitors

A 
bacitracin 
Vancomycin
Daptomycin
Fosfomycin
telamycin
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13
Q

Name the penicillins

A 
Amoxicillin
ampicillin
Dicloxacillin
Nafacillin
Oxacillin
Penicillin G 
Penicillin V 
Piperacillin
Ticarcillin
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14
Q

1st Gen cephalosporins

A

Cefaderoxil
Cefazolin
Cephalexin
Cephalotin

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15
Q

2nd Gen Cephalosporins

A 
Cefaclor
Cefamandole
Cefprozil
Cefuroxime
Cefotetan
Cefoxitin
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16
Q

3rd Gen Cefalosporins

A 
Cefdinir
Cefixime
Cefotaxime
Cefotazdime
Ceftibuten
Ceftizoxime
Ceftriaxone
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17
Q

4th Gen Cefalosporins

A

Cefepime

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18
Q

What is the MOA of Penicillins? How is this rationalized?

A

interfere with transpeptide or cross linkage of the last stage of cell wall synthesis. They bind to cell wall receptors and bacterial autolysins synergistically work with penicillins to destroy wall.
This makes bacteria cell wall unstable and more osmotically fragile.

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19
Q

What are Penicillins ineffective against?

A

Mycobacteria
protozoa
fungi
viruses

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20
Q

Where was penicillin first obtained from?

A

The mold Penicillin chrysogenum

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21
Q

Natural Vs. Semi-synthetic penicillins

A 
Natural: 
> Antistaphylococcal
Semi-synthetic: 
> Extended Spectrum 
> Antipseudomonal
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22
Q

What are the standard Penicillins?

CAP-B

A

> Crystalline Penicillin G (IV)
Penicillin V (PO)
Aqueous procaine penicillin G (IM)
Benzathine Penicillin G (IM)

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23
Q

Antistaphycoccal Penicillins (COMND-I)

A 
Cloxacillin (PO)
Oxacillin (IV) 
Methicillin (IV)
Nafcillin (IV)
Dicloxacillin (PO) 
Isoxazloyl Penicillins (IV or PO)
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24
Q

Aminopenicillins

A

Ampicillin (IV/PO)

Amoxicillin (IV/PO)

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25
Q

How is Penicillin G (Benzylpenicillin ) administered?

A

IV/IM

because not resistant to acid

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26
Q

What is Pen G active against?

A 
Strep. Pneumoniae
> Pyogens
> viridans
Neisseria Gonorrhea 
Meningitides 
Clostridium Perfinges
Bacilus Antracis
Corynebacterium diphetriae 
Treponema Pallidum
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27
Q

Pen. V

A

Is more acid stable and can be used in oral infections by anaerobes.

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28
Q

Semi-synthetic Pen G, Extended spectrum

A

Ampicillin
Amoxicillin
(also aminopenicillins)
These are similar to Pen G but more effective against Gram-

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29
Q

What is a natural resistance against penicillin?

A

organism lacking a peptidoglycan cell wall or are impermeable to the drugs.

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30
Q

Acquired resistance to penicillin?

A 
An organism can have a plasmid transfer that leads to other significant problems because it acquires multiple resistance. 
EG: 
Beta- lactamase
Decreased permeability to drug 
Altered penicillin binding proteins
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31
Q

absorption of penicillin

A

most absorbed incompletely after oral intake except Amoxicillin

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32
Q

Excretion of penicillin

A

primary route is renal

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33
Q

Adverse Rxns to penicillins

A

> Hypersensitivity in 5% of pts
Diarrhea
Nephritis
Neurotoxicity (can produce seizures if injected intrathecally)
platelet dysfunction (antipseudomonal)
Cation toxicity

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34
Q

Which cephalosporins are Pen G substitutes?

A 
1st Gen 
Cefadroxil
Cefazolin 
Cephalexin
Cephlotin
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35
Q

How do cephalosporins differ compared to penicillins?

A

they tend to be more resistant to beta lactamases.

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36
Q

How is 2nd gen cephalosporins different?

A

more activity against gram - such as H. Influenza, E. Aerogenes, Neisseria. and weaker against gram positive

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37
Q

2nd gens with activity against bacteroides fragilis

A

cefmetazole, cefotetan, cefoxitin (most potent)

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38
Q

3rd gen cephalosporins

A

inferior to 1st gen with Gram +, but have better activity against gram - bacilli. Same as 2nd gen but with Serratia m.

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39
Q

What are 2 agents of choice against meningitis?

A

ceftriaxone, cefotaxime

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40
Q

cefepime

A

only 4th gen cefalosporin, Must be administered parenterally.

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41
Q

What is cefepime effective against?

A

E. Coli, K. pneumoniae, P. mirabilis and P. aeroginosa.

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42
Q

advanced gen cefalosporin

A

ceftaroline

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43
Q

oral broad spectrum cefalosporin

A

cefitoxime and cefodosime proxetil

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44
Q

administration of cefalosporins

A

IV/IM

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45
Q

cephalosporins for CSF?

A

3rd gen

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46
Q

treatment for neonatal or childhood meningitis caused by H. influenzae

A

ceftriaxone or cefotaxime** (3rd gen)

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47
Q

What is a cephalosporin that has good bone penetration?

A

cephalexin (1st gen)

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48
Q

cephalosporin used for abdominal sepsis or gynecological sepsis?

A

cefoxitin (2nd gen)

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49
Q

how are cephalosporins eliminated?

A

renally, except for cefoperazone or ceftriaxone which is through the bile and excreted

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50
Q

what are some cephalosporins used in renal failure?

A

cefoperazone or ceftriaxone

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51
Q

adverse effects of cephalosporins

A 
disulfiram effect ( when consumed with alcohol ) usually in 2nd and 3rd Gen. 
> allergic manifestations: 5-15% patients with penicillin allergy has allergy to cephalosporins. 
1-2% allergic who do not have penicillin allergy 
> hypothrominemia: due to antivitamin K defects
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52
Q

Which cephalosporin has the longest 1/2 life?

A

Ceftriaxone

53
Q

what are the 1st gen spectrum? (PEcK)

A

Proteus
E. Coli
Klebsiella

54
Q

2nd Gen. spectrum? (HENPEcK)

A 
H. Influenzae
Enterobacter
Neisseria Sp 
Proteus
E. Coli
Klebsiella
55
Q

3rd Gen cephalosporin

A

same as 2nd but with serretia m. +meningitis

56
Q

4th gen active against? KEEP SPS

A

Klebsiella
Enterobacter
E. Coli
Proteus

Staph.
Pseudomonas
Strep.

57
Q

Carbapenems

A

broadest spectrum available, resistant against B-lactamase, hydrolysis and penicillinase producing Gram + and Gram =

58
Q

Types of cerbepenems

A

Imipenem
Ertapenem
Doripenem
Meropenem

59
Q

administration of cerbapenems

A

IV, does not penetrate CSF.

60
Q

excretion of cerbapenems

A

glomerular filtration (renal)

61
Q

adverse effects of carbapenems

A

nausea, vomits and diarrhea

62
Q

patients who are allergic to penicillins and cephalosporins

A

aztreonam (monobactam)

63
Q

aztreonam

A

no action against Gram +
IV
primarily against Gram - rods

64
Q

adverse effects of aztreonam

A

phlebitis, skin rash and abnormal liver function tests.

65
Q

MOA of Vancomycin

A

Inhibits cell wall synthesis of phospholipids and peptidoglycan polymerization

66
Q

What is Vancomycin used against?

A

B Lactamase producing Gram + and Gram -.

Used in pts. allergic to B lactam antibiotics.

67
Q

What diseases are vancomycin used for?

A

antibiotic induced colitis due to slotridium difficile.

MRSA

68
Q

how is Vancomycin administered?

A

through IV for systemic infections and prophylaxis because 90-100% is excreted by the kidney unchanged.

69
Q

Adverse effects of vancomycin

A

fever, chills, phlebitis

RED MAN SYNDROME (shock due to histamine release

70
Q

what drug is DOC for antibiotic-induced colitis

A

Vancomycin

71
Q

Daptomycin

A

MRSA and VRE

Bactericidal

72
Q

What antibiotic is restricted for topical application?

A

Bacitracin

73
Q

Name all the tetra cyclines

A

tetracycline
Demeclocycline
Minocycline
Doxycycline

74
Q

What is the only tetra cycline that has parenteral administration?

A

Doxycycline

75
Q

MOA of tetracyclines

A

Enters through passive diffusion or active transport and binds to 30 S subunit and inhibits bacterial synthesis

76
Q

What is the spectrum of tetracyclines?

A

broad

77
Q

activity of tetracyclines?

A

bacteriostatic

78
Q

Tetracycline is the DOC for what diseases?

A 
Chlamydia
Mycoplasma pneumoniae 
lyme disease 
Cholera 
Rocky mountain spotted fever
79
Q

What are the pharmacokinetics of tetracyclines?

A

if given orally is incompletely absorbed. Chelates with dairy products

80
Q

Where are tetracyclines metabolized?

A

in the liver

81
Q

Resistace to tetracyclines

A 
R factor plasmids
Mg++ dependent
Active efflux
Enzymatic destruction 
Altered target site 
CROSS RESISTANCE
82
Q

SEs of tetracyclines

A 
GI disturbances 
Deposition in bone
teeth discoloration 
stunt growth in children 
fetal hepatotoxicity 
Phtotoxicity 
Vestibular dysfunction 
Pseudotumor cerebri
Superinfections ( broad spectrum)
83
Q

Contraindications of tetracyclines

A

pregnancy
renal impaired pts. (except doxycycline)
Children under 8 yo

84
Q

What tetracycline is safe to give to renal impaired patient?

A

doxycycline

85
Q

What is tetracycline?

A

derivative of minocycline and structurally similar to tetracyclines possessing a broad spectrum

86
Q

MOA of tetracycline

A

30s binding

87
Q

pharmacokinetics of tetracycline

A

parenteral administration

88
Q

SEs of tetracycline

A 
Nausea 
Vomiting 
Photosensitivity
Pseudo tumor cerebri 
Discoloration of teeth
89
Q

MOA of aminoglycosides

A

inhbits bacterial protein synthesis by coupling with the 30s and interfering the assembly of a functional Ribosomal apparatus

90
Q

Parentaral aminoglycosides

A 
Gentamycin 
Amikacin
Tobramycin 
netilmicin
streptomycin
91
Q

Topical/ oral aminoglycosides

A

neomycin. used topically because of severe nephrotoxicity maybe used to reduce intestinal flora in hepatic coma

92
Q

Pharmacokinetics of aminoglycosides

A

bad oral absorption so administered IV , except neomycin

93
Q

spectrum of aminoglycosides

A

bactericidal and effective only against aerobic gram negative bacteria

94
Q

clinical uses of aminoglycoside

A

plague
tuberculosis
tularemia
enterococci

95
Q

What are 2 meds that have synergistic action

A

b lactam antibiotics and aminoglycosides

96
Q

distribution of aminoglycosides

A

poor penetration into CSF, can be used intrethecally. EXCEPT neomycin.
accumulates in renal cortex and endolymphatic channels

97
Q

metabolism of aminoglycosides

A

there is no metabolism and rapidly eliminated in the urine.

98
Q

resistance of aminoglycosides

A

decreased uptake when O2 dependent transport is absent . altered receptor. plasmid associated synthesis which modify and inactivates the drug. CROSS RESISTANCE IS USUAL.

99
Q

adverse effects of aminoglicosides

A

ototoxicity. vertigo. nephrotoxicity. neuromuscular paralysis. allergic reactions

100
Q

factors that encourage SEs in aminoglycosides

A

age. previous exposure to drug. liver disease.

101
Q

macrolide drugs

A

erythromycin…clarithromycin…azythromycin..telithromycin

102
Q

moa of macrolides

A

binds to 50 S. bacteriostatic but at hugh doses is bacteriocidal

103
Q

clinical uses of macrolides

A

chlamydial infections…mycoplasma pneumonia…syphylis..

104
Q

erythromycin

A

effective against organisms sensitive to penicillin G. this can be used as an alternative to pts. allergic to penicillins.

105
Q

clarithromycin

A

spectrum similar to erythromycin but also includes H. influenza and higher effectiveness for chlamydia

106
Q

azithromycin

A

DOC for chlamydia…effective in AIDS pts. with disseminated infection due to mycobacterium avium

107
Q

telithromycin

A

ketolide with similar spectrum to azythromycin

108
Q

resistance to macrolides

A

decreased uptake of drug by organism…decreased affinity for 50s ….increased drug efflux (most common) …cross resistance for clarithromycin, azithromycin and erythromycin but not telithromycin

109
Q

pharmacokinetics of macrolids

A

oral form of erythromycin is destroyed by gastric acid. food interferes with erythromycin a d azithromycin but increases clarithromycin. IV has high incidence for thrombophlebitis for erythromycin

110
Q

distrimution and metabolism of macrolids

A

well distributed except in csf. erythromycin metabolized in liver and interferes with cytochrome p450. clarithromycin interfers with metabolism of teophylline and carbamazepine.

111
Q

excretion of macrolids

A

erythromycin and azithromycin in bile. clarithromycin in liver and kidneys.

112
Q

SEs of macrolids

A

epigastric distress, cholestatic jaundice, transient ototoxicity, phlebitis

113
Q

contraindications of macrolids

A

hepatic dysfunction

114
Q

chloramphenicol

A

restricted to last resort. broad spectrum including anaerobes and rickettsias. depending on the organism can be bacteriostatic or bacteriocidal.

115
Q

moa of cloramphenicol

A

50s

116
Q

resistance to cloramphenicol

A

conferred by R factor

117
Q

pharmacokinetics of cloramphenicol

A

well absorbed orally and distributed including CSF.

118
Q

excretion of cloramphenicol

A

liver, 10%in kidneys

119
Q

adverse effects of chloramphenicol

A

hemolytic anemia…aplastic anemia

120
Q

what is the gray baby syndrome

A

neonates accumulate chloramphenicol which inhibits mitochondrial enzymes leading to poor feeding, depressed breathing and vascular collapse with cyanosis and death.

121
Q

clindamycin

A

50 s..primarily used in infections caused by anaerobic bacteria.

122
Q

what is always resistant to clindamycin

A

clostridium difficile

123
Q

SEs of clindamycin

A

pseudomembranous colitis and skin rash

124
Q

quinupristin/dalfopristin

A

mixture of 2 streptogramins (30:70 ) ratio. both bind to 50s. reserved for VAancomycin resistant tenterococcus faecium (vre)

125
Q

adverse effects of quinupristine/dalfopristin

A

phlebitis, CYP interaction, arthralgia/myalgia, hyperbilirrubinemia

126
Q

linezolid

A

orally effective and binds to 50s. bacteriostatic

127
Q

resistant to linezolid

A

decrease binding to target site

128
Q

spectrum of linezolid

A

gram +

129
Q

SEs of Linezolid

A

irreversible peripheral neuropathies (OPTIC NEURITIS BLINDNESS)

Pharmacology 1 (5 decks)

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