antibiotics mod 2 Flashcards

1
Q

Beta-Lactamase inhibitor combinations

A

Ampicillin-sulbactam

Amoxicillin-clavulanic acid (Augmentin)

Ticarcillin-clavulanic acid (Timentin)

Piperacillin-tazobactam (Zosyn)

Ceftazidime-avibactam (Avycaz)

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2
Q

penicillin

A

MOA:

  • Disrupt the synthesis of the cell wall
  • Bacteria must be growing and dividing
  • Inhibit transpeptidases
    • —Essential for cell wall synthesis
  • Activates autolysis

Works against many different organisms

Low toxicity

Adverse effects: urticaria, pruritis, angioedema

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3
Q

penicillin: uses and SE/AE

A
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4
Q

Different Types of PCNS

A

Natural Penicillins:
- PCN G & PCN V

Penicillinase-Resistant Penicillins:
- nafcillin

Aminopenicillins:
- amoxicillin & ampicillin

Extended-Spectrum Penicillins:
- Piperacillin

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5
Q

Natural pcns:

penicillin g& V

A

Indications: Gram +, gram – cocci, anaerobic bacteria, spirochetes
Can be used with aminoglycosides
- gets into the cell and disrupts protein synthesis

½ life about 30 minutes (unless kidney dysfunction)
Least toxic

SE:
Rash to anaphylaxis allergy to 1 PCN, allergy to ALL

Usually given IV/IM (PO forms available)

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6
Q

Penicillanse resistant PCNs:

nafcillin (iv)

A

Nafcillin is the drug of choice for this class of PCNs

Nafcillin is IV only

Cloxacillin & oxacillin are the oral formulations

Resist breakdown by the penicillanse enzyme

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7
Q

Aminopenicillins:

ampicillin (Augmentin) & amoxicillin

A

ampicillin (Augmentin)
- 1st broad spectrum
AE: Diarrhea and rash

Given PO or IV
If oral, amoxicillin usually better option
Renal sensitive
ampicillin/sulbactam (Unasyn)

amoxicillin

  • Indications: Common for ear, nose, throat, genitourinary and skin infections
  • Less SE compared to ampicillin
  • Very common in pediatric patients
  • Doses are sometimes higher because of strep resistant organisms
  • ONLY PO
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8
Q

Extended-spectrum:

piperacillin (Zosyn)

liver and renal function monitor

A

Wider spectrum than other penicillins
Both ticarcillin & piperacillin ALWAYS given with a beta-lactamase inhibitor
Anti-pseudomonal
Ticarcillin unique side effect: sodium overload & interferes with platelet function
Piperacillin very good for pseudomonas infection
Also affects platelet function
Watch for patients with renal dysfunction

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9
Q

Cephalosporins

1-5 generations

bacterial infections, bacterial cell wall

NO ETOH

A

Structurally similar to PCNs
Inhibit cell wall synthesis through same penicillin-binding protein - activate autolysis
Often resistant to beta-lactamase - cephalosprinase
Low-toxicity
Some cross-sensitivity with PCN allergy
Avoid if PCN anaphylaxis

5 generations:
Increase the spectrum/activity/and ability to penetrate CSF

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10
Q

Cephalosporins

A

Most common adverse effects of all: mild diarrhea, abdominal cramps, rash, pruritis, redness, edema

ok for pregnancy

same indications as PCN

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11
Q

1st generation cephalosporin:

cefazolin & cephalexin (Keflex)

A

Works well for gram + bacteria
Staph and non-enterococcal strep infections
Given PO or IV
Cefazolin is only IV
Cefazolin common for surgical prophylaxis

**no BBB crossing

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12
Q

2nd generation: cephalosporin

cefuroxime& cefotetan

A

More gram – coverage AND the gram + coverage
IV and PO forms available
Cefuroxime does not kill anerobic bacteria

No BBB or pseudomonas

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13
Q

3rd generation: cephalosporins

ceftriaxone
ceftazidime
Cefotaxine

NO LIVER

A

Most potent in fighting gram – bacteria BUT much less activity against gram +
These 2 drugs are IV/IM only

Ceftriaxone is EXTREMELY long-acting (once per day dosing benefit)

BBB - effective in treating meningitis and other infections within the CNS

NO LIVER FAILURE

Ceftazidime works well for pseudomonas

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14
Q

4th generation: cephalosporin

cefepime

A

Works against gram - & + (very broad spectrum)

Uncomplicated/complicated UTIs, skin infections and pneumonia

Also crosses the BBB

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15
Q

5th generation: cephalosporins

ceftaroline

A

Treats MRSA and MSSA works again some VRSA/VISA
***No Enterobacter, Pseudomonas, ESBL, Klebsiella coverage

Needs to be renally dosed
Only IV form

Ceftolozane/tazobactam (Zerbaxa) NEWEST cephalosporin
Treats complicated infections

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16
Q

Carbapenems

imipenem/cilastin (Primaxin)

meropenem

**potential seizure activity infused over 60 mins

A

BROADEST spectrum of ALL antibiotics

Bactericidal & cell wall inhibitor (same as previous two classes)

Typically used as a ‘last resort’ medication

Biggest AE: drug-induced seizure activity (not super common)
ALL are IV and must be INFUSED OVER 60 MINUTES

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17
Q

carbapenems

Imipenem/cilastin (primaxin)

what for seizures

A

Combo of the carbapenem with an inhibitor of enzyme that breaks down imipenem

MOST broad spectrum
Binds to penicillin-binding proteins

VERY RESISTANT TO BETA-LACTAMASE

IV administration only
Can penetrate BBB and meninges

WATCH FOR SEIZURES especially in elderly and with other meds that can induce seizures
Used for complicated infections

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18
Q

carbapenems:

meropenem

A

A little less coverage than imipenem; but still gram + and – aerobes and anaerobes

Doesn’t degrade in kidneys
Less seizure activity

Rash and diarrhea most common side effects

Ertapenem- less spectrum; but only have to give once a day
Doripenem- newest; less seizure activity; NOT FOR PNEUMONIA

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19
Q

carbapenems

A

imipenem/cilastin (Primaxin)
meropenem
Imipenem/cilastin (primaxin)
Meropenem

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20
Q

Vancomycin

gram + ; no BBB; kidney dosing

A

Glycopeptide antibiotic

Destroys by binding to bacterial cell wall, producing immediate inhibition of cell wall synthesis and death

Works on gram + infections - including MRSA and PCN resistant pneumococcus

Oral vancomycin is given to treat clostridium difficile and pseudomembranous colitis

Doesn’t work for CNS infections

Kidneys eliminate drug; decrease doses for renal dysfunction

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21
Q

Vancomycin

red man syndrome

the red man drives the van, listening to music too loudly (ototoxicity) and not drinking enough water (kidney damage)

A

Toxic side effects:
Ototoxicity with high levels (can be reversible)
Immune-mediated thrombocytopenia
Nephrotoxic watch when using with other drugs (aminoglycosides, cyclosporin’s, IV contrast) that affect kidneys

Watch with neuromuscular blockades (paralyzers)

Red Man Syndrome: usually related to rapid infusion
Flushing, rash, pruritis, urticaria, tachycardia, hypotension
Infuse slowly and over longer time periods
Usually NOT harmful

22
Q

Monobactam:

aztreonam (Azactam)

A

Most commonly used for gram – bacteria

Still uses the penicillin binding protein; inhibits cell wall synthesis and cell lysis
Can work for CNS infections- crosses the BBB

Side effects: thrombophlebitis/pain at injection site

23
Q

Televancin(Vibativ)

gram +

A

Inhibits cell wall sysnthesis
IV only: usually for skin infections r/t gram + bacteria (works for MRSA)
Adverse effects: renal toxicity, infusion-related reactions, prolonged QT interval

Dalbavancin & oritavancin are newest and are derivatives of televancin (REALLY long half lives)

24
Q

TEICOPLANIN

A

Semisynthetic glycopeptide

MOA: Inhibits peptidoglycan polymerization, results in inhibition of cell wall synthesis and cell death

Can be give PO to treat C Diff and pseudomembranous colitis

LONG half-life

Treats gram-positive bacterial infections like MRSA and Enterococcus [similar to Vanc]

25
``` Aminoglycosides Lincosamides: clindamycin Macrolides Oxazolindinones Streptogramins Tetracyclines Glycylcycline Fluoroquinolones Cycliclipopeptides Sulfonamides Metronidazole ```
``` All of these Drugs Work by Inhibiting/Altering Protein Synthesis: transcription - Nucleus - Messenger RNA - Cytoplasm ``` translation - Cytoplasm - Ribosomes - mRNA - Add amino acids - ----In a specific sequence - Protein synthesis
26
Aminoglycosides: gentamycin amikacin tobramycin gram - and + with combo therapy
Potent antibiotics that work well on gram (–) bacteria Also work on gram + but need other anti-biotics for synergistic effect UTIs/pyelonephritis, gynecological infections, peritonitis, endocarditis, PNA, osteomyelitis (DM related infections) Severe side effect profile: Nephrotoxicity- 5-25%, usually reversible Ototoxicity- 3-14%, usually permanent Therapeutic drug monitoring - peak/trough levels Transitioned from 3x/day dosing to 1x/day dosing
27
Aminoglycosides: gentamycin ** respiratory distress, cochlear damage
Neuromuscular blockade - can cause PROFOUND respiratory distress [myasthenia gravis] Central nervous system side effects: confusion, depression, disorientation, numbness, and tingling Cochlear damage– ototoxicity, high-frequency hearing loss, high-pitched tinnitus
28
Aminoglycosides uses and indications
gentamycin: IV; intrathecal for meningitis Also available in ophthalmic drops, and topical ointments amikacin: Only IV Used for infections resistant to tobramycin and gentamycin tobramycin: Inhalation for pulmonary infections (esp. CF patients) Topical and ophthalmic solutions available
29
Lincosamides: clindamycin Bactericidal or bacteriostatic– depending on drug concentration **anaerobic infections -- will develop c-diff and pseudomembranous colitis from usage
MOA: binds to ribosomes and inhibits protein synthesis Indications: chronic bone infections, GU tract infections, intraabdominal infections, anaerobic pneumonia, septicemia, serious skin infections; prophylaxis for endocarditis PO & IV available Primarily used to treat: pseudomembranous colitis Monitor use with neuromuscular blockade medications Very toxic- monitor levels - peaks and troughs
30
Macrolides erythromycin azithromycin Legionnaire’s, Listeria, mycoplasma pneumonia can all be treated with macrolides
Bacteriostatic in general, bactericidal in high enough concentrations YUCK drugs - GI side effect profile intense (esp. erythromycin) MOA: inhibit protein synthesis by binding to ribosomes Indications: various infections of upper and lower respiratory infections, skin infections, soft tissue infections; STIs
31
macrolides erythromycin GI issues; no BBB
Used to treat MANY infections Has hypomotility benefits for diabetic gastroparesis & increase gastric motility and emptying Does not cross BBB PO & IV– IV is painful, oral absorption isn’t great Topical and ophthalmic also available Don’t take oral on empty stomach– lots of GI upset Lots of drug-drug interactions
32
Macrolides: azithromycin (Z-pack) no with food, decr absorption
Differs structurally from other macrolides - has some advantages in coverage compared to erythromycin Less GI upset, still some Very good tissue penetration & long duration of action Taking food with drug decreases absorption, so try to take without food
33
Oxazolidinones linezolid Indicated for healthcare-associated pneumonias and infections
MOA: inhibits protein synthesis through non-selective monoamine oxidase (MAO) inhibitors Initially created to treat MRSA and VRE ``` Use with caution: Hypertension Untreated thyroid disease Severe cardiac disease Cerebrovascular disease Pheochromocytoma ```
34
Oxazolidinones linezolid side effects **serotonin
Common adverse effects: headache, nausea, vomiting Watch platelet count thrombocytopenia Available PO and IV Can cause serotonin syndrome with use of SSRIs Avoid foods high in tyramine: wines, smoked meats, aged cheese, soy sauce
35
Streptogramins quinupristin/dafopristin **pot. anaphylaxic shock, need D5W with IV infusion
``` Newest class for ‘superbugs’ quinupristin/dalfopristin used in combination alone bacteriostatic, combination=bactericidal 16x the activity used alone ``` Use for serious, life-threatening infections caused by VRE and complicated skin and skin structures, including MRSA IV only Adverse effects: arthralgias, myalgias (muscle pains); painful/erythema/inflammation at IV site in 75%
36
Tetracyclines tetracycline doxycycline minocycline Broad spectrum; major resistance has developed Contraindications: Pregnant and nursing women, children younger than 8 (teeth)
MOA: bacteriostatic drugs that inhibit protein synthesis by binding to ribosomes ``` Some infections still commonly treated with tetracyclines: Rickettsia (rocky mountain spotted fever) Chlamydia and trichomonas Lyme disease Cholera Pelvic inflammatory disease Mycoplasma pneumonia Acne ``` Adverse effects: discoloration of the permanent teeth and tooth enamel hypoplasia in fetuses and children, photosensitivity, many others
37
tetracycline Concentrates in bone, liver, tumor, spleen & TEETH Causes damage to teeth < 8 years
``` Bacteriostatic Inhibits or retards the growth Not available parenterally Fasting – 75% - 77% absorbed Giving more decreases % absorption ``` Adverse effects: N/V/D, headache, photosensitivity, dizziness Rare: anaphylaxis and angioedema
38
tetracyclines doxycycline minocycline acne primary use
doxycycline Chlamydial and mycoplasmal infections Prophylaxis for STIs Acne and other non-dangerous skin infections minocycline Neisseria meningitides Decreases symptoms of rheumatoid arthritis Solodyn is an extended release (ER) formula - acne
39
tetracycline Glycylcyline: tigecycline **skin infection
Newest form of tetracyclines Effective against many organisms resistant to the other tetracyclines Treats complicated skin and skin structure infections- MRSA, VRE, extended-spectrum beta lactamases Peritonitis and other complicated abdominal infections Nausea and vomiting occur in 20-30% of patients
40
Fluoroquinolones ciprofloxacin, levofloxacin ***GREAT ORAL ABSORPTION gram -
Very potent, broad-spectrum antibiotics Very good oral absorption 1st & 2nd generations not used anymore due to abx resistance MOA: destroy bacteria by altering their DNA Interfere with the bacterial enzymes DNA gyrase and topoisomerase Mostly gram-negative and some gram-positive coverage
41
Fluroquinolone: ciprofloxacin **anthrax, UTI primary, causes joint disease
Used to treat UTIs, some STIs, upper and lower respiratory tract infections, gonorrhea, and other infections Also treats anthrax infection with Bacillus anthracis PO, IV, and topical Works well on rapid and slow growing organisms Prolonged post-antibiotic effects concentrated in the neutrophils Adverse effects: arthropathy (joint disease), often irreversible Avoid in patients under 18 and over 60
42
Fluroquinolone: levofloxacin (Levaquin) 100% bioavailable; respiratory infections, **give no seizure or kidney failure
Most widely used quinolones Broad-spectrum of activity like cipro but advantages is once-daily dosing PO or IV- 100% bioavailability orally Less resistance More activity against pneumococcal and other ‘atypical’ respiratory infections Side effects: CNS disorders that predispose to seizures, kidney failure, can cause prolongation of QT interval, photosensitivity
43
Cyclic Lipopeptides: | daptomycin
MOA: Not completely understood; binds to gram + cells in calcium-dependent process, disrupts the cell membrane potential Long post-antibiotic effect Given IV once per day Used to treat: MRSA, VRE bacteremia, right-sided endocarditis, complicated skin & skin structure infections
44
Sulfonamides: | sulfamethoxale + trimethoprim
MOA: don’t actually destroy bacteria but inhibit their growth= bacteriostatic by preventing the synthesis of folic acid needed for DNA synthesis Indications: uncomplicated UTIs, respiratory infections, salmonella, shigellosis ‘Sulfa allergies’; photosensivity
45
metronidazole (Flagyl) NO ETOH, crohn's disease and c-diff
Antiprotozoal & antibacterial Crohn’s disease Antibiotic-associated diarrhea Anaerobic activity only MOA: inhibits DNA synthesis, similar to fluroquinolones DO NOT TAKE WITH ALCOHOL Adverse effects: N/V, xerostomia, vaginal candidiasis
46
inhibit cell wall growth
``` penicillins cephalosporins carbapenems vancomycin aztreonam telavancin ```
47
abx classes
class
48
abx moa
gram coverage
49
inhibit/alter protein synthesis
``` aminoglycosides lincosamides macrolides oxazolindinones streptogramins tetracyclines glycylcycline flouroquinolones cycliclipopeptides sulfonamides metronidazole ```
50
inhibit cell wall synthesis
``` penicillin cephalosporins carbapenems vancomycin Monobactam - aztreonam telavancin Teicoplanin ```
51
peak
taken 30 minute after medication infusion is complete
52
trough
taken 8-12 hrs after dose is complete