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Flashcards in Pharmacology Deck (147):
1

Penicillin/Aminoglycosides

Increases the penetration of aminoglycosides since penicillin will break down cell walls

2

Postantibiotic Effect

Persistent effect of antibiotic effect on growth after only brief exposure to the drug

*Exhibited by aminoglycosides and fluoroquinolones

3

Prevents the cross linking of peptidoglycan by inhibiting transpeptidases

Penicillin / Cephalosporins / Carbapenems / Aztreonam

4

Inhibitor of peptidoglycan synthetase

Vancomycin

5

Inhibitors of 30s ribosome

Aminoglycosides

6

Inhibitors of peptidyl transferase

Chloramphenicols

*Decreased peptide bond formation

7

Inhibitors of 50s ribosome

Erythromycin / Clindamycin / Linomycin

"Macrolides"

8

Inhibits binding of aminoacyl tRNA to ribosome

Tetracyclines

9

Binds the 23s ribosome

Linezolid / Streptogramins

10

Cationic Detergents (Interference w/ cell membrane)

Polymixin B / Colistin

11

Inhibits DNAP

Rifampin

12

Inhibits action of DNA gyrase

Fluoroquinolones

*Inhibits the negative supercoiling of bacterial DNA

13

Inhibitors of lipid synthesis

Isoniazid

14

Inhibitors of folic acid synthesis

Sulfonamides / Trimethoprim

15

Reasons why you might start empiric coverage

1. Site of infection is difficult to culture
-Brain abscess, pneumonia, middle ear infxn

2. Serious or life-threatening condition

3. Empiric therapy- given as a broad treatment

16

Drugs that interfere w/ Warfarin

Bactrim & Erythromycin

17

Drugs that interfere w/ Theophylline

Ciprofloxacin

18

Drugs that interfere w/ SSRIs

Linezolid

19

What antibiotics do antacids interfere with?

FQNs and Tetracycline

20

Bactrim

Trimethoprim + Sulfamethoxazole

Treats Gram + (minus MRSA & VRE), ^PEK and CE, and Chlamydia, Cloroquine (R) malaria, Toxoplasmosis, and Pneumocystis carinii

Interactions: Warfarin => Potentiates effects causing excess clotting

Methotrexate => Increases free methotrexate in the blood

21

Which drugs inadequately reach the lungs?

Aminoglycosides

22

Abscesses and antibiotics

Must be drained before antibiotics can adequately do their job

23

"Piddly" Gram neg organisms

Haemophilus, Morganella, Moraxella, Shigella, Salmonella


(Neisseria, Providencia)

24

"Fence" Gram neg organisms

Proteus, E. Coli, Klebsiella

25

SPACE Gram neg organisms

Serratia

Pseudomonas

Acinetobacter

Citrobacter

Enterobacter

26

"Atypical" Orgs

Legionella

Mycoplasma

Chlamydia

27

Anerobic Gram neg organisms

Bacteroides

Clostridium

Peptostreptococcus

28

SPACE bug antibiotic coverage

Cell Wall Inhibitor + FQN OR Aminoglycoside

(Penicillin/Cephalosporin/Carbapenem)+ (Ciprofloxacin/Levofloxacin) OR (Gentramycin/Topramycin)

*Ace in the hole = Aztreonam

29

Penicillin General Structure

1. Thiazolodine Ring (House)

2. B-lactam ring (Garage)

3. Acyl side group (chimney)

30

Targets of B-lactam antibiotics

PBPs

31

Cockroft-Gault Equation

(140-age)(Weight in kg)/([Creatinine])(72)

*Must account for renal insufficiencies

*If female, multiply by .85

Used to calculate renal excretion

32

Poor areas of penicillin distribution

Insoluble in lipid

=>CNS, Brain, Prostate

33

Adverse effects of penicillin

Allergic rxn =>Maculopapular rash

Interstitial nephritis (especially w/ methicillin)

Pseudomembranous colitis

34

Anti-staphylococcal penicillins

Methicillin, Oxacillin, Nafcillin

35

Aminopenicillins

Ampicillin / Amoxicillin

-Amino group allows for penetration into cell walls

-Treats strep, proteus, entero, salmonella, shigella, haemophilus

*Drug of choice for Enterococcus

36

Carboxypenicillins

Carbenicillin / Ticaricillin

-Has increased permeability to cell walls

-Works against PIDDLYs, SPACE, and Strep

*Can be causes dysfunctional platelets; Ticarcillin has high Na+ content

37

Ticarcillin hazards

Dangerous for CHF patients due to the high Na+ content

-Can also cause platelet dysfunction

*Replace w/ piperacillin

38

Augmentin

Amoxicillin + Clavulonic Acid

=>B-lactamase inhibitor adds Staphylococcus and anaerobe coverage

39

Timentin

Ticarcillin + Clavulonic Acid

=>B-lactamase inhibitor adds Staph and anaerobes to the spectrum

40

Cephalosporin Structure

1. Dihydrothiazine ring (House)

2. B-lactam ring (Garage)

3. Acyl Side Chain (Chimney)

*Cephalosporins have TWO R-groups; one on the acyl side chain and one on the dihydrothiazine ring

R1= Spectrum of Activity

R2= Stabilizer; increases t^1/2

41

Cephalosporin Distribution

Well-distributed; oral form is completely absorbed by the GI tract

-CSF penetration is extra efficacious w/ inflammation

*Usually use 4x Ceftriaxone

42

Elimination of Cephalosporins

Hepatic => Ceftriaxone, Cefoperazone

Renal => Everything else`

43

Adverse effects of Cephalosporins

*Presence of NMTT side chain on certain drugs can interfere w/ Vitamin K dependent clotting factors => bleeding

(Cefamandole, Cefoperazone)

*Presence of NMTT along w/ alcohol consumption => severe sickness

*10% cross reactivity w/ penicillin => Possible allergies

44

1st Generation Cephalosporins

Cefazolin

Good for treating Gram + and Piddly Gram -

45

2nd Generation Cephalosporins

Cefuroxime

Good for treating Gram + and Gram - H. flu and PEK (fence)

46

2nd Generation Cephalosporins (Cephamycins)

Cefoxitine and Cefotetan

Good against Gram +, H. flu and PEK, AND ANAEROBES

47

Third Generation Cephalosporins

Ceftriaxone and Cefotaxime

Covers Strep and up to SACE gram negs

48

Third Generation Cephalosporins (antipseudonomal)

Ceftazidime and Cefoperazone

Covers SPACE

49

Fourth Generation Cephalosporins

Cefapime

Gram + and SPACE

50

5th Generation Cephalosporin

Ceftarazine

Staph, Strep, and Enterococcus and SCE

51

Drugs used for surgical prophylaxis

Cefazolin

-Will cover Staph aureus infxns that can occur when penetrating the skin

52

Imipenem

Treats all bacteria except for the atypicals

Undergoes extensive renal metabolism; add cilastatin to prevent

*Toxicity => Seizures, possible hematologic disorders

53

Ertapenem

Weaker version of imipenem/meropenem that doesn't cover enterococcus or psedomonas

*Requires less doses

54

Aztreonam

Good against all gram neg organisms but saved for severe, life-threatening conditions

Monobactam antibiotic: structured much like penicillin

*Can also be used if penicillin allergy present

55

Problems with Aminoglycoside Distribution

Poor concentrations to the lungs and CSF w/ inflammation

*Also has poor absorption in the gut

56

Adverse Effects of Aminoglycosides (Neomycin)

Nephrotoxicity- occurs when the trough levels are too high

Ototoxicity- occurs when the peak levels are too high

57

Treatment of TB

Streptomycin

58

Indications for use of neomycin

1. Surgical prophylactic for colorectal surgery- suppresses growth of intestinal flora

2. Hepatic coma- decreases number of NH4 forming flora

3. Hyperlipidemia- decreased flora => decreased cholesterol absorption

59

Vancomycin Absorption and Distribution

Must use IV for systemic infxn
-Oral route only used for C. dificile infxn (might want to just drink IV $$$$$$$$$$$$)

Distributed freely but only to the CSF w/ inflammation

60

Adverse Effects of Vancomycin

Red-Man Syndrome: Histamine-like allergic rxn; must slow the infusion

Hypersensitivity w/ Maculopapular rash

Nephrotoxicity and Ototoxicity

61

Vancomycin Indications

Serious infxn by B-lactam resistant gram pos organisms

Pseudomembranous colitis that is non-responsive to metronidazole

Surgical prophylactic for major surgeries involving implantation of prosthetics

Surgical prophylactic for pts. w/ beta-lactam allergies

Surgical prophylactic for pts. w/ serious endocarditis

62

Vancomycin Dosing

Nomogram for initial dose; then adjust by 3rd administration given peak and trough values

Typically 1-15 g/12 hr

63

Synercid

Dalfopristin/Quinupristin

Good for MRSA, PCN-resistant S. pneumo, and VRE

*Requires central line placement

Could use if Vancomycin doesn't work

BUT...

*NOT GOOD AGAINST E. FAECALIS

64

Linezolid

Good for MRSA, VRE, PCN-resistant S. pneumo

*Common side effect = Thrombocytopenia

*Co-administration w/ SSRI => SEROTONIN STORM

65

Mupirocin

Topical treatment used to eradicate MRSA from the nares

66

Colistin

Used as a LAST RESORT to pan-resistant gram negative orgs

Will also cover the SPACE orgs

67

Fosfomycin

Used on UTIs only and in patients w/ multiple antibiotic allergies

Covers Gram pos, neg, MRSA, and ESBL

68

Daptomycin

Coverage: Gram + (MRSA and VRE), Right-sided endocarditis from IV drug users

Adverse Effects: Rhabdomylosis

*Rapidly inactivated by pulmonary surfactant

=>>No good for pneumonia

69

Telavancin

Coverage: Skin and soft tissue infxns; Gram +

Adverse: Red Man Syndrome, QT prolongation, Nephrotoxicity

*Similar to vancomycin

70

Sulfonamides

Mechanism: Competes w/ PABA for dihyrdopteroate synthetase and decreases bacterial folic acid synthesis

Spectrum: Gram +, PEK

Adverse: Nephrotoxicity
Steven-Johnson Syndrome (separation of epidermis from dermis)
*Kernicterus if given to pregnant women in 3rd trimester
=>increased unconjugated bilirubin

Resistance: Bacteria can structurally alter dihydropteroate synthetase or overproduce PABA

*Treats uncomplicated UTI, nocardosis, toxoplasmosis, malaria if chloroquine (R)

71

Trimethoprim

Mechanism: Inhibits dihydrofolate reductase => decreased THF

Spectrum: Gram +, Gram -, and Pneumocystis carinii in combo w/ dapsone

Adverse: Caution in pts. w/ folate deficiency
(Pregnant women, alcoholics, malnourished)

*Treats uncomplicaed UTI or recurrent UTI prophylaxis AND TRAVELER's DIARRHEA (caused by ETEC)

72

Trimethoprim/Sulfamethoxazole (Bactrim)

Spectrum: UTIs, respiratory infxns, STD, Traveler's Diarrhea

*Potentiates the effects of Warfarin and Methotrexate

73

Nitrofurantoin

Spectrum: Gram + (including MRSA and Enterobacter), Gram - excluding Pseud. and up to CE

Adverse Effects: Pulmonary Reactions; peripheral neuropathy

*Used exclusively for UTI due to high urine concentration; can't use in males due to PROSTATE TISSUE

74

Methenamine

Mechanism: Denatures bacterial proteins when activated

Adverse: Avoid in hepatic insufficiency (NH4+ byproduct) and Renal Failure (Acidosis)

*Used for UTI prophylaxis, NOT NORMAL UTI; works for virtually all bacteria

*Frequent voiding of the bladder via catheterization will decrease the formaldehyde allowing the bacteria to survive

75

Erythromycin

Spectrum: Covers Gram +, atypicals, and Peddlys (except M. cat and H. flu)

Absorption: Better when fasting; dissolved by gastric acid if not made with stearate
-Estolate form is unaffected by food, however, is extra bad for pregnant women

Adverse: Severe GI symptoms (cramps, nausea)
Ototoxicity
Cholestatic Hepatitis
Hypersensitivity to Estolate compound causing fever

*Stimulates motilin receptor => gastric emptying
Interferes w/ p-450 enzymes =>decreased metabolism of Theophylline, Warfarin, Cyclosporin

76

Clarithromycin

Spectrum: Gram +, atypicals, M. cat*, H. flu*, H. pylori

Adverse: Not as severe as erythromycin

*Interferes w/ p-450 enzymes

77

Azithromycin

Spectrum: Gram +, atypicals, M. cat*, H. flu*

Excretion: Excreted in feces via biliary; slow release from tissues

Adverse: Less severe than erythromycin

*DOES NOT inactivate p-450 enzymes

78

Clindamycin

Spectrum: Gram +, anaerobes

Adverse: Diarrhea and *C.diff infxns* (wipes away anaerobes in gut)

79

What bacteria do cephalosporins typcially NOT cover?

Atypicals

Enterococcus (ex. Ceftaroline)

MRSA (ex. Ceftaroline)

80

Tigecycline

Used for complicated abdominal infxns

Good against: Broad-spectrum resistant gram negs, Acinetobacter, and anaerobes

*Doesn't reach adequate blood levels

*Go to if you have a CARBAPENEM- RESISTANT ENTEROBACTERIA

81

Major drug that can cause interstitial nephritis

Methicillin

82

Prevpak

Treatment for H. Pylori

Combination of Clarithromycin and Amoxicillin

83

Chloramphenicols

MOA: Reversibly binds to the 50s ribosomal subunit

Absorption: Must be hydrolyzed in the intestines to be activated; IV form not as effective

*Excellent CSF distribution

SOA: Gram pos, Gram neg, Anaerobes, Rickettsia, Chlamydia

ADR: *Bone marrow hypoplasia (Anemia)

*Gray-baby syndrome

Indications: Bacterial Meningitis, Rickettsia

84

Gray-Baby Syndrome

Toxicity in newborns due to the excessive inhibition of mitochondrial protein synthesis

-GRAY COLOR, hypothermia, respiratory collapse, vomiting

*Occurs due to excess chloramphenicols in the system because newborns lack the proper hepatic fnxn to conjugate and clear the drug

85

What is the one time oral vancomycin is used?

Treating pseudomembranous colitis from C diff after metronidazole has been ineffective

86

Quinolones

MOA: Inhibits DNA gyrase and blocks the negative supercoiling of DNA
*Inhibits a post-antibiotic effect

ADR: QT prolongation
CNS symptoms in elderly (confusion, dizziness)
Arthopathy (in young athletes) and tendon rupture (in elderly on steroids)

Interactions: Theophylline (Ciprofloxacin doubles conc.)
Warfarin (Ciprofloxacin increases effect)
Avoid antacids

SOA: Gram + (levofloxacin better), ^SPACE, atypicals
*Moxicillin covers anaerobes

Indications: PID, LRIs, bone and joint infxns, intrabdominal infxns (must add metronidazole to cipro or levo, can use moxi alone)

87

Best drug for Pseudomonas

Ciprofloxacin

88

Hepatobiliary excreted tetracyclines

Doxycycline and Minocycline

89

Tetracylines

MOA: Binds to the 30s ribosomal subunit

Absorption: Better on fasting state

ADR: Photosensitivity, yellow teeth, *Diabetes Insipidus
*Concept sometimes used to treat SIADH
Fanconi-like syndrome (N/V, proteinurea, lethargy, acidosis)

Interactions: Decreased absorption w/ dairy products or metallic ion consumption

-Increased INR

Indications: Broad spectrum coverage, good for inxns from atypicals, Rocky Mountain Spotted Fever, H.pylori (used w/ clarithromycin)

90

Brucellosis

Consumption of unpasteurized dairy products leads to infxns of the heart or CNS

-Recurrent fever, joint pain, headache

TREATMENT: Tetracycline + Gentamicin

91

Cholera

Infxn by V. cholerae resulting in prod. of watery diarrhea; can lead to lethal dehydration

TREATMENT: Tetracyclines

92

Lyme Disease

Infxn by Borrelia burgdorferi resulting in a "target" shaped rash along w/ joint pain and headaches

TREATMENT: Tetracyclines

93

What is the only drug that is harmful after the expiration date?

Tetracyclines

94

Penicillin G

Used for Gram + orgs (minus Staph)

95

Piperacillin Spectrum

Bacteroides fragilis

Streptococcus, Enterococcus

PEK, SPACE

*Used in place of ticarcillin in hypertensive pts.

96

Timentin

Ticarcillin/Clavulonic Acid

97

Unasyn

Ampicillin/Sulbactam

98

Enterococcus treatment

Ampicillin + Gentamycin

99

Indications for neomycin (oral AGC)

1. Suppression of IF for colorectal surgery

2. Hepatic coma (decreases amount of NH4+ forming bacteria)

3. Hyperlipidemia (decreases intestinal cholesterol absorption)

100

Macrolides are found in high concentration in what type of cell?

Phagocytic (PMNs and Macros)

=>>treat Intracellular organisms that survive in these cells

Ex.- Mycoplasma, Chlamydia, Legionella

101

Go-to drug for ESBL organisms

Carbapenems

102

Common culprits of HAP

SPACE bugs

=>Empiric treatment should cover these

103

Treatment for CAP

Beta-lactam + Macrolide

104

Which FQN is used for complicated intra-abdominal infxns?

Moxifloxacin

*Is also the only one you can't use for UTIs due to reasons

105

Which FQNs cover Staph and Strep best?

Levofloxacin and Moxifloxacin

106

Most potent FQN against Pseudomonas

Ciprofloxacin; also covered by levofloxacin

107

Amphotericin B

MOA: Binds to ergosterol on the fungal cell membrane increasing the permeability and resulting in lysis

Distribution: Must give intrathecally if CSF desired

ADR: Nephrotoxicity (direct effect on afferent renal arterioles)
Anemia
Fever - *Should premedicate w/ NASAIDs or meperidine to prevent

Spectrum: Broad (Candida, Aspergillus, Histoplasmosis, Coccidiomyces)

*Lipid formulations (ABLC) => Useful for patients who are intolerant for the normal drug and are less nephrotoxic while equally efficacious (may require higher doses though)

108

Flucytosine

MOA: Penetrates the fungal cell wall where is transformed to 5-fluorouracil and inhibits pyrimidine synthesis

ADR: Bone marrow hypoplasia; esp. w/ Amphotericin-B

Indications: Serious cryptococcal infxns (must use in synergy)

109

Azoles

MOA: Interferes w/ C-P450 fnxn inhibiting lanosterol conversion to ergosterol

ADR: Depression of ACTH and Testosterone
=>gynecomastia, hypogonadism, decreased libido

(Mostly by ketoconazole)

110

Fluconazole

Rapidly absorbed and not affected by acid or food; readily distributed to the CSF

*Drug of choice for Cryptococcus and Coccidiomycoses meningitis

*Candida prophylactic

111

Itraconazole

Mostly used for treatment of aspergillosis but has a wide spectrumis not well distributed to the CSF

*Use Amphotericin-B first, then switch to this

112

Voriconazole

Used to treat invasive aspergilosis

Contraindicated if pt. is on: Rifamipin (Decreased Voriconazole AUC), Quinidine, or Sirolimus (Increased)

113

Posaconazole

Can be used if itraconazole not available

114

Caspofungin Acetate

Blocks fungal wall cell synthesis (glucan)

*Used in invasive aspergillosis if pt. has not responded to other drugs

*Can cause left-shift, phlebitis, fever

115

Griseofulvin

MOA: Disrupts mitotic spindle of fungal cells arresting division

Absorption: Microsize- Increased w/ fats
Ultrasize- Completely absorbed

*Used for dermatophytosis if topical agents fail

*Is a CYP-450 inducer => Increase Warfarin dose if pt. is currently taking this medication

116

Terbinafine

MOA: Inhibits squalene oxidase inhibiting ergosterol formation

Indications: Onychomosis

*Clearance of terbinafine is increased 100%w/ co-administration of rifampin

*Should not be used for pregnant women or liver/renal dysfunction patients

*Assoc. w/ headache and rash

117

Drug of choice for CAP

Ceftriaxone

118

Drug of choice for ESBL

Meropenem

119

Penicillin-Binding Protein

Transpeptidase

120

Red-Man Syndrome

Slow down the infusion rate or give antihistamines

121

Ideal treatment of walking pneumonia

Macrolides

122

Only Tetracycline that causes Diabetes insipidus

Dimiclocycline (Tigecycline)

123

Inactivated Vaccines

Use large amounts of antigen to elicit an immune response w/o risk of infxn

*Safe to use in pts. who may have allergies to other vaccines

*Administered w/ adjuvants to enhance uptake into DCs and macros
-Most are precipitated w/ alum

124

Toxoid Vaccine

Inactivated toxin that is completely safe because it HAS NO CHANCE of causing disease

-Because there is no bacteria present!

125

Conjugate Vaccines

Polysaccharides linked to protein carriers

*Polysaccharides alone CANNOT elicit a T-dependent immune response in children

126

Inactivated Vaccine Disadvantages

Immunity is not life-long (requires boosters)

Immunity is only humoral

Does not elicit an IgA response

127

Live Vaccine

Immunity is long-lived and elicits a response similar to that of the infection

*Vaccine is attenuated by growth in improper conditions causing it to lose its virulence factors

*Dangerous to give these to IC patients

128

Acyclovir

MOA: Drug is phosphorylated to monophosphate form and then triphosphate form via HSV or VZV ultimately resulting in chain termination
=>>Ultimately a polymerase inhibitor

ADR: Nephrotoxicity (like AGCs) and some CNS abnormalities

Indications: Herpes/Varicella infxns
-Excellent CSF penetration so used for meningitis also

129

Valacyclovir

MOA: Rapidly converted to acyclovir via intestinal and hepatic metabolism

*Is the pro-form (oral) of acyclovir

-Reaches nearly the same levels w/ less toxicity but it does take longer

130

DOC for viral encephalitis

Acyclovir

131

Ganciclovir

Similar to acyclovir

*Much more potent to CMV; is FIRST LINE of treatment for
CMV retinitis

ADRs include neutropenia and thrombocytopenia

132

Valaganciclovir

Pro-drug of galanciclovir

*Is surgically implanted in CMV retinitis in AIDS pts.

133

Penciclovir/Famicyclovir (Pro)

-Similar to acyclovir

*Topical treatment for herpes cold sores

134

Cidovir

MOA: Interacts w/ DNA polymerase as alternative substrate or inhibitor

ADR: Severe nephrotoxicity
*Must administer w/ saline to limit

Indication: Treatment of CMV retinitis after ganciclovir has failed
(5mg/kg for 2 weeks, then continue until ADR is too severe)

-Administer w/ Probenecid

135

Foscarnet

MOA: Competes for pyrophosphate in viral DNA polymerases

ADR: Nephrotoxicity, seizures, anemia (increased with Zidovudine) , EKG changes

*Used as last ditch effort in CMV-retinitis AIDS pts.
-Avoid if possible due to ADRs

-Also used in HSV-AIDS pts. If acyclovir doesn't work

136

Interferons

Type I (a and b) => Hep B, Hep C, Kaposi's Sarcoma

Type II => MS

ADR: Flu-like symptoms, personality changes (in kids), neurotoxicity, alopecia

137

Lamivudine

MOA: Inhibits reverse trancscriptase

ADR: SEVERE Lactic Acidosis, Hepatosplenomegaly, Rash, Peripheral neuropathy

Indications: Treat HBV w/ interferon
AIDS

138

DOC for RSV pneumonia

Ribavirin; touted as wide-spectrum antiviral

139

Amantadine/Rimantidine

MOA: Prevents viral entry into host

*Amantadine needs renal adjustment for dosage

ADR: Confusion, neurological symptoms (worse w/ Amantadine)
=>>Use rimantadine in elderly patients

Indications: Influenza A

140

Osteltamivir/Zanamivir

MOA: Inhibits viral release from cell by inhibiting neuroaminidase

Osteltamivir => PO can cause GI symptoms

Zanamivir =>>Drug is delivered by inhalation and can cause bronchospasm (avoid in COPD pts.)

Indications: Influenza A AND B

141

Allyamines

Inhibits squalene conversion and ultimately ergosterol synthesis

142

Azoles not affected by antacids

Fluconazole and Voriconazole

143

Drug of choice for Coccidiomycoses meningitis

Fluconazole

144

Which penicillin covers anaerobes?

Piperacillin (Bacteroides)

145

Which FQN does not cover UTIs?

Moxifloxacin

146

Concentration dependent antibiotics

FQNs and AGCs

147

Paracoccidiomycosis follow-up therapy

Sulfonamides