Pharmacology Flashcards
1
Q
Penicillin/Aminoglycosides
A
Increases the penetration of aminoglycosides since penicillin will break down cell walls
2
Q
Postantibiotic Effect
A
Persistent effect of antibiotic effect on growth after only brief exposure to the drug
*Exhibited by aminoglycosides and fluoroquinolones
3
Q
Prevents the cross linking of peptidoglycan by inhibiting transpeptidases
A
Penicillin / Cephalosporins / Carbapenems / Aztreonam
4
Q
Inhibitor of peptidoglycan synthetase
A
Vancomycin
5
Q
Inhibitors of 30s ribosome
A
Aminoglycosides
6
Q
Inhibitors of peptidyl transferase
A
Chloramphenicols
*Decreased peptide bond formation
7
Q
Inhibitors of 50s ribosome
A
Erythromycin / Clindamycin / Linomycin
“Macrolides”
8
Q
Inhibits binding of aminoacyl tRNA to ribosome
A
Tetracyclines
9
Q
Binds the 23s ribosome
A
Linezolid / Streptogramins
10
Q
Cationic Detergents (Interference w/ cell membrane)
A
Polymixin B / Colistin
11
Q
Inhibits DNAP
A
Rifampin
12
Q
Inhibits action of DNA gyrase
A
Fluoroquinolones
*Inhibits the negative supercoiling of bacterial DNA
13
Q
Inhibitors of lipid synthesis
A
Isoniazid
14
Q
Inhibitors of folic acid synthesis
A
Sulfonamides / Trimethoprim
15
Q
Reasons why you might start empiric coverage
A
- Site of infection is difficult to culture
- Brain abscess, pneumonia, middle ear infxn - Serious or life-threatening condition
- Empiric therapy- given as a broad treatment
16
Q
Drugs that interfere w/ Warfarin
A
Bactrim & Erythromycin
17
Q
Drugs that interfere w/ Theophylline
A
Ciprofloxacin
18
Q
Drugs that interfere w/ SSRIs
A
Linezolid
19
Q
What antibiotics do antacids interfere with?
A
FQNs and Tetracycline
20
Q
Bactrim
A
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
Q
Which drugs inadequately reach the lungs?
A
Aminoglycosides
22
Q
Abscesses and antibiotics
A
Must be drained before antibiotics can adequately do their job
23
Q
“Piddly” Gram neg organisms
A
Haemophilus, Morganella, Moraxella, Shigella, Salmonella
Neisseria, Providencia
24
Q
“Fence” Gram neg organisms
A
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
