Exam 1 Drugs

Penicllin Drugs

Penicillin G

Penicillin VK

Ampicillin

Amoxicillin

Pivmecillianam (prodrug)

SOA for Penicillin G, Penicillin VK, Ampicillin, and Amoxicillin

Gram+ anaerobes

• peptococcus finegoldia

• anaeroccous

T. Pallidum (Syphilis)

STREP

MOA for Penicillins, Penicillinase Resistant PCNs, Extended Spectrum PCNS (carboxy and ureido), and ß-lactamase combinations

Prevents cross linking of PBPs (transpeptidases)

Which oral penicillins should be taken on an empty stomach?

Penicillin VK, Ampicillin

SOA for Pivmecillianam

E. coli

proteus mirabilis

Staph. Saprophyticus

This penicillin needs renal adjustment

ampicillin

ADE of pivecillinam

Nausea

diarrhea

Contraindicated in: beta-lactam allergic patients, carnitine deficiency, and porphyria (heme deficiency)

Penicillinase resistant PCNs drugs

Oxacillin, Nafcillin, Methicillin, cloxacillin, dicloxacillin

SOA for pencillinase ressitant PCNs

STAPH not MRSA

What else does Nafcillin and Dicloxacillin cover?

MSSA

Which Pencillinase resistant PCNs need renal adjustment?

methicillin, cloxacillin, dicloxacillin

Dicloxacillin has best…

bioavailability

Which penicillinase resistant PCN(s) can cause interstitial nephritis

Methicillin (most)

Oxacillin, Nafcillin (less)

What is special about the elimination route of oxacillin and nafcillin?

hepatic

ß-lactamase combination drugs

Amoxicillin/Clavulanate (augmentin)

Ampicillin/Sulbactam (Unasyn)

Piperacillin/Tazobactam (Zosyn)

Which ß-lactamase combination is oral?

Augmentin

ß-lactamase combination coverage. Zosyn also covers what?

Gram+ anaerobes

• peptococcus finegoldia

• anaeroccous

T. Pallidum (Syphilis)

STREP

H. influenzas

Zosyn: pseudomonas

1st gen cephalosporin drugs

Cefazolin (ancef), Cephradine, Cephalexin (Keflex), Cefadroxil

Cephalosporin MOA

Suicide inhibitions of PBPs

Prevents cross-linking of peptidoglycan synthesis

Activation of autolytic enzymes leading to cell death

1st gen Cephalosporin coverage

Gram+

Some Gram-

True or false. 1st gen Cephalosporins penetrate the CNS.

False.

Which 1st gen Cephalosporin does NOT have crossreactivity of penicillins?

Cefazolin (Ancef)

2nd Gen Cephalosporin drugs

cefuroxime, cefuroxime axetil (cefitin), ceprozil

2nd gen Cephalosporin coverage

Gram+

Gram- ADD H. flu

Which 2nd gen Cephalosporin can have a disulfiram like reaction?

Major 2nd gen Cephalosporin ADE

Increase PT time — increase bleeding risk through inhibition of vitamin K epoxide reductase

3rd gen Cephalosporin drugs

cefotaxime (clafor

3rd gen Cephalosporin coverage

Gram+

Mostly Gram-

Which 3rd gen Cephalosporin is hepatically eliminated?

ceftriaxone

Which 3rd gen Cephalosporin can have a disulfiram-like reaction when combined with alcohol?

Ceftriaxone

Which 3rd gen Cephalosporin should you avoid taking iron supplements with?

cefdinir

Cephalosporin Antipseudomonal Drugs

Ceftazidime, Cefepime, Cefiderococol

Ceftazidime Coverage

Gram-

Pseudomonas

Cefepime coverage

Gram-

Pseudomonas

Some gram+

Cefiderococol Coverage

gram-

P. aeruginosa

Carbapenem resistance organisms

Special MOA of cefiderococol

chelates ferric ions and uses bacterial transports to enter the cells

5th gen cephalosporin drug

Ceftaroline

Ceftaroline coverage

Gram+

• MRSA

• PRSP

• VRE

• E. faecalis

Gram-

NOT pseudomonas

Advanced generation cephalosporin drug

Ceftobiprole

Ceftobiprole coverage

MRSA

MSSA

S. pneumonia (including resistant)

E. Faecalis

Gram-

• K. pneumoniae

• E. coli

  • Pseudomonas aeruginosa

Ceftobiprole has a high affinity for ____.

PBP 2a

Cephalosporin/ ß-lactamase combos drugs

Ceftolozam/tazobactam

Ceftazidime/avibactam

Cetolozam/tazobactam coverage

Gram-

• pseudomonas

• ESBL

Ceftazidime/avibactam coverage

Gram-

• pseudomonas

• ESBL

• KPC

Monobactam drug

Aztreonam

Monobactam MOA

Binds to PBP-3

Aztreonam coverage

Gram-

• pseudomonas

Is there cross allergy between penicillin allergy and aztreonam?

No

Monobactam/ß-lactamase inhibitor drug

Aztreonam/avibactam

Monobactam/ß-lactamase inhibitor drug

Aztreonam/avibactam

Monobactam/ß-lactamase inhibitor MOA

prevents/decreases the cross linking of peptidoglycan synthesis

Aztreonam/avibactam coverage

Gram-

• multidrug resistant organisms

Carbapenem drugs

Imipenem/Cilastatin, Meropenem, Ertapenem

Imipenem/Cilastatin and meropenem coverage

Gram+

Gram-

Anaerobes

Pseudomonas aeruginosa

Ertapenem coverage

Gram+

Gram-

NOT pseudomonas, NOT enterococci

_____ are the broadest spectrum of beta-lactams

Carbapenems

Cilastatin inhibits…

the renal tubular dipeptidase

Carbapenem/ß-lactamase drug

Meropenem Vaborbactam

Meropenem Vaborbactam coverage

vaborbactam protects meropenem from degredation of serine B-lactamases

In-vitro activity against ESBLs

True or false. You adjust for renal impairment for meropenem Vaborbactam

True

Fluroquinolone drugs

Ciprofloxacin, Levofloxacin, Moxifloxacin, Delafloxacin

Fluroquinolone MOA

Inhibits enzyme topoisomerase IV

Ciprofloxacin Coverage

Gram-

Levofloxacin coverage

Gram-

S. Pneumonia

Moxifloxacin coverage

Gram+

Delafloxacin coverage

MRSA

Psuedomonas

FDA warnings for Fluroquinolones (4)

1. tendinitis/tendon rupture

2. Peripheral neuropathy

3. CNS effects

4. exacerbation of myasthenia gravis

Do not take what with Fluroquinolones?

antacids

Which fluroquinolone goes through hepatic elimination?

Moxifloxacin

Aminoglycoside Drugs

Amikacin, Gentamicin, Tobramycin, Streptomycin

Aminoglycoside MOA

Bind to 30S and block the tRNA at the P-site

Aminoglycoside coverage

Gram-

• pseudomonas

Gram+ synergy for staph or enterococcus

What renal effects do aminoglycosides have?

Renal elimination

Renal toxicity

How do penicillins effect aminoglycosides?

Inactived in vitro by PCNs, admin 0.5hours apart

What kind of toxicity do you see in aminoglycosides?

Ototoxicity — can lead to permanent hearing loss

Macrolides drugs

Erythromycin, Azithormycin, Clarithromycin

Macrolides MOA

Binds reversibly to 50s subunit between the A and P sites

Macrolides Coverage

Gram+

• S. pneumo

• Atypicals

Macrolides ADE

QTc prolongation

GI upset — erythromycin most

CYP3A4 inhibition — clarithromycin and erythromycin

Macrolides are ____ eliminated.

Hepatically

Tetracycline Drugs

Tetracycline, Doxycycline, Minocycline, Demeclocycline, Oxytetracycline

Tetracycline MOA

Binds to 30S and blocks tRNA at the A-site

Tetracycline coverage

Some strains of MRSA

Minocycline coverage

May have activity against Acinetobacter baumannii

Tetracycline ADEs

Teeth discoloration, photosensitivity, hepatic toxicity

Avoid tetracyclines in who?

Children <8

Pregnant patients

Can you take tetracycline or minocycline with food?

No, food causes absorption impairment

Avoid what type of food while taking doxycycline?

dairy, calcium containing products or supplements

Glycycline Drugs

tigecycline, eravacycline, omadacyline

Tigecycline coverage

MRSA

PCN-resistant

S. pneumoniae

VRE

ESBL producing organisms

• acinetobacter baumanii

• bacteroides fragilis

Eravacycline coverage

MRSA

VRE

ESBLs

some CRE

Eravacycline ADEs

GI (N/V)

Infusion site reactions

Omadacyline coverage

S. pneumo

S pyogenes

MRSA

VRE

B. fragilis

K. pneumonia

Acinetobacter spp.

Stenotrophomonas maltophilia

Omadacyline ADEs

N/V

infusion reactions

AST/ALT/GGT

Hypertension

H/A

Constipation

Diarrhea

Tigecycline is bacterio____

Bacteriostatic

Sulfonamide drug

Timethoprim/Sulfamethoxazole

Sulfonamide coverage

Gram+

Gram- (not pseudomonas)

H. Flu

Bactrim is _____ eliminated.

Renally

bactrim ADEs

Photosensitivity, hypersensitivity

Glycopeptide Drug

Vancomycin