ID: SHAEER PACKET (PART 7 (1 of 2): ANTIBIOTICS, NATURAL PCNS -> MONOBACTAMS)

Penicillin G brand name? Dosage form?

Pfizerpen; dosed IV

Penicillin G procaine brand name? Dosage form?

Wycillin; dosed IM

Penicillin G benzathine brand name? Dosage form?

Bicillin L-A; dosed IM

Penicillin G procaine and benzathine brand name? Dosage form?

Bicillin C-R; dosed IM

Penicillin VK brand name? Dosage form?

Pen-Vee K, Veetids; dosed PO

Natural penicillins (PCNs) include? (five)

Pen G

Pen G procaine

Pen G benzathine

Pen G procaine + benzathine

Pen VK

Natural penicillins cover what gram positive bugs? (seven)

1. Strep A, B, C, F, G

2. Strep pneumoniae

3. Strep viridans group

5. Enterococcus spp.

6. Bacillus spp.

7. Corynebacterium spp.

Natural penicillins cover what gram negative bugs? (two)

1. Neisseria meningitidis

2. Pasteurella multocida

Natural penicillins cover what anaerobes? (three)

1. Clostridium spp. (excluding Cdiff)

2. Peptostreptococcus

3. Cutibacterium

Natural penicillins cover what spirochetes? (two)

1. Treponema palladium

2. Leptospira interrogans

Mechanism of action of natural penicllins?

Inhibit cell wall synthesis by binding to penicillin binding protein

T/F: Natural penicillins are low-risk and routinely used in pregnancy.

True

Side effects associated with natural penicillins WITHOUT procaine? (excluding allergic) (two)

GI (N/V/D)

Seizures (risk higher in high doses, renal impairment)

Side effects associated with natural penicillins + procaine? (five)

Dizziness

Palpitations

Auditory/visual disturbances

Fear of impending death

Transient psychotic episodes resolving within 15-30 minutes (Hoigne's syndrome)

T/F: PCN G is the drug of choice for syphilis.

True

Clinical uses for natural penicillins? (five)

1. Syphilis

2. S. pneumoniae

3. Streptococcus spp. (pharyngitis, endocarditis)

4. Neisseria meningitidis

5. Clostridium spp. (excluding C diff)

T/F: Natural penicillins are effective in treating against Staphylococcus spp.

False; nearly 90% penicillinase production

Why give PCN G IV over PCN G IM? (what circumstances)

Severe/complicated infections (PNA, meningitis)

Penicillinase-resistant penicillins (antistaph penicillins) include... (four)

1. Methicillin

2. Oxacillin

3. Nafcillin

4. Dicloxacillin

Oxacillin brand name? Dosage form?

Bactocil, dosed IV

Nafcillin brand names? (two) Dosage form?

Unipen, Nafcil; dosed IV

Dicloxacillin brand names? (three) Dosage form?

1. Dynapen

2. Diclocil

3. Dycil

Mechanism of action of penicillinase-resistant penicillins?

Inhibit cell wall synthesis by binding to penicillin binding protein

T/F: Penicillinase-resistant penicillins have NO MRSA or MRSE coverage.

True

T/F: Penicillinase-resistant penicillins have limited gram negative activity.

False; cover no gram negatives.

Aminopenicillins include? (two)

1. Ampicillin

2. Amoxicillin

T/F: Aminopenicillins spectrum of activity can be described as similar to natural penicillins with improved Enterococcus spp. and gram-negative coverage.

True

B-lactam/B-lactamase inhibitor combinations include? (four)

1. Amoxicillin-Clavulanate

2. Ampicillin-sulbactam

3. Piperacillin/tazobactam

4. Sulbactam/durlobactam

Two mechanisms of action of b-lactamase inhibitors?

1. Irreversibly bind to catalytic site of the B-lactamase thereby prohibiting hydrolysis of the B-lactam antibiotic

2. Binding to the penicillin-binding proteins of the bacteria, which increases antibacterial activity of the antibiotic

T/F: B-lactam/B-lactamase inhibitor combinations have the same spectrum of activity as ampicillin and amoxicillin + B-lactamase producing strains of some other species.

True

Side effects associated with B-lactam/B-lactamase inhibitor combinations?

GI (N/V/D)

Inc risk of acute nephrotoxicity (w/ vanco)

Examples of clinical uses for Augmentin? (four)

1. Upper respiratory tract infection

2. Lower respiratory tract infection

3. UTI

4. Bite wounds

Examples of clinical uses for ampicillin/sulbactam? (five)

1. Gynecologic

2. Intra-abdominal

3. Skin/soft tissue infection

4. Pneumonia

5. Bites

First Generation Cephalosporins include? (six)

1. Cefazolin (Ancef)

2. Cephalexin (Keflex)

3. Cefadroxil (Duricef)

4. Cephradine (Velosef)

5. Cephalothin (Keflin)

6. Cephapirin (Cefadyl)

Background on first gen cephalosporins?

Good gram positive activity, limited gram negative activity; poor CSF penetration

Brand name Cefazolin? Dosage form?

Ancef; dosed IV, IM

Brand name Cephalexin? Dosage form?

Keflex; dosed PO

Brand name Cefadroxil? Dosage form?

Duricef; dosed PO

Mechanism of action of first-gen cephalosporins?

Inhibit cell wall synthesis by binding to penicillin binding protein

Second generation cephalosporins? (nine)

1. Cefamandole (Mandol)

2. Cefaclor (Ceclor)

3. Cefuroxime acetil (Ceftin, Zinacef)

4. Cefonicid (Monocid)

5. Cefoxitin (Mefoxin)

6. Cefotetan (Cefoten)

7. Cefmetazole (Zetazone)

8. Cefprozil (Cefzil)

9. Loracarbef (Lorabid)

Which generation of cephalosporins has *better* staphylococcus spp. coverage?

A. First gen

B. Second gen

A. First gen

Third generation cephalosporins? (ten)

1. Cefoperazone (Cefobid)

2. Cefixime (Suprax)

3. Cefpodoxime proxetil (Vantin)

4. Ceftibuten (Cedax)

5. Cefdinir (Omnicef)

6. Cefotaxime (Claforan)

7. Ceftizoxime (Cefizox)

8. Ceftriaxone (Rocephin)

9. Ceftazidime (Fortaz, Tazicef)

10. Cefditoren (Spectracef)

Which three Third Gen Cephalosporins can penetrate the CSF?

1. Ceftriaxone

2. Cefotaxime

3. Ceftazidime

Fourth generation cephalosporin? (one)

Cefepime

T/F: Fourth generation cepalosporins are the broadest spectrum of all cephalosporins.

True

Side effects associated with fourth generation cephalosporins? (two)

1. GI (N/V/D)

2. Neurotoxicity (rare, presents as confusion, temporospatial disorientation, myoclonus)

Clinical uses for fourth generation cephalosporins? (seven)

1. Bacteremia

2. Febrile neutropenia

3. Intra-abdominal infections (w/ metronidazole)

4. Meningitis

5. Pneumonia

6. Skin & soft tissue infections

7. Uncomplicated and complicated UTIs

T/F: Fifth-generation cephalosporins are also described as anti-MRSA cephalosporins.

True

Fifth-generation cephalosporins include? (two)

1. Ceftaroline (Teflaro)

2. Ceftobiprole (Zevtera)

T/F: Ceftaroline (Teflaro) has extensive gram-positive coverage.

True

Mechanism of action of ceftaroline?

Prodrug; rapidly transformed from ceftaroline fosamil into ceftaroline in plasma. Bactericidal activity mediated through inhibiting cell well synthesis by binding penicillin binding protein.

T/F: The fifth-generation cephalosporins are prodrugs with extended gram-positive spectrums.

True

What is the relationship between cephalosporin generation number and gram positive coverage?

Generally, from first to fifth generation, cephalosporins *increase* in gram negative coverage and *decrease* in gram positive coverage.

T/F: Fifth generation cephalosporins cover pseudomonas.

False

T/F: Cefepime covers pseudomonas.

True

Cephalosporin/B-lactamase inhibitor (BLI) combinations include... (four)

1. Ceftaroline/avibactam (phase III clinical trials rn)

2. Ceftrazidime/avibactam (Avycaz)

3. Ceftolozane/tazobactam (Zerbaxa)

4. Cefepime/enmetazobactam (Exblifep)

Mechanism of action of cephalosporin/B-lactamase inhibitor (BLI) combinations?

Cephalosporins all inhibit cell wall synthesis by binding to PBP

BLI inactivates some B-lactamases and protects the cephalosporin from degradation by certain B-lactamases

Clinical uses for cephalosporin/BLI combinations? (three)

1. Complicated IA infections w/ metronidazole

2. Complicated UTIs, including pyelonephritis

3. HAP and ventilator-associated bacterial pneumonia

Sidopheres include? (one drug)

Cifederocol (Fetroja)

T/F: Cifederocol has no clinically relevant gram negative activity.

False; no clinically relevant gram *positive* activity.

Mechanism of action of Cifederocol?

Passive diffusion via porin channels; siderophore moiety sequesters environmental iron, then the iron-siderophore is *actively* transported across the outer cell membrane of bacteria into the periplasmic space using a siderophore iron uptake mechanism (trojan horse mechanism); designed to evade bacteria defenses. Then, complex dissociates for the antibiotic to exert its antibacterial activity by inhibiting cell wall synthesis via PBP binding.

Read that twice bro what a mouthful.

Clinical use for cifederocol?

Pretty much exclusively pylonephritis or HABP/VABP in adults as a last line option

T/F: Carbapenems are the broadest coverage of all B-lactams.

True

Carbapenems include...? (four)

1. Imipenem-cilastatin (Primaxin)

2. Meropenem (Merrem)

3. Ertapenem (Invanz)

4. Doripenem (Doribax)

MOA of carbapenems?

Inhibit cell wall synthesis by binding PBP

Clinically significant drug interactions of carbapenems? (two)

1. Reduction in VPA conc. leading to breakthrough seizures

2. Generalized seizures w/ ganciclovir + impenem/cilastatin

Side effects associated with carbapenems? (one, excluding PCN allergy)

1. Seizures (but especially imipenem!)

Clinical uses for carbapenems? (seven)

Nosocomial infections of any of the following varieties

1. Bacteremia

2. Bone and soft tissue infections

3. Intra-abdominal infections

4. Obstetrics and gynecologic infections

5. Complicated UTIs

6. Pneumonia

7. Sepsis

Carbapenem/BLI combinations include...? (two)

1. Meropenem/vaborbactam (Vabomere)

2. Imipenem/cilastatin/relebactam (Recarbrio)

Which carbapenems penetrate CSF? (four, with caveat)

1. Imipenem

2. Meropenem

More so than...

3. Ertapenem

4. Doripenem

Beta-lactam antibiotics include.... (five antibiotic (classes?)?

1. PCN

2. AminoPCN

3. Cephalosporins

4. Carbapenems

5. Monobactams

Monobactams include... (two)

1. Aztreonam (Azactam)

2. Aztreonam/avibactam (phase III clinical trials rn)

T/F: Monobactams are *only* active against gram negative aerobic bacteria.

True

MOA of monobactams?

Inhibit cell wall synthesis by binding PBP

T/F: Monobactams can penetrate CSF.

True

Clinical uses for monobactams? (six)

1. Bacteremia

2. Complicated and uncomplicated UTIs

3. Gynecological infections

4. Intra-abdominal infections

5. Lower respiratory tract infections

6. Skin and soft tissue infections