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Penicillin's Exam 1 Drug List Flashcards

1
Q

Beta-Lactams Common Characteristics

A

Broad class of antibiotics with several sub-groups

Share common structure featural beta-lactam ring.

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2
Q

Beta-Lactam Antibiotic Subgroups

A

Penicillins

Cephalosporins

Carbapenems

Monobactams

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3
Q

Beta-Lactams (Penicillin V, Benzathine/Procaine Penicillin G, Amoxicillin, Amoxicillin/clavulanate) MOA

A

Inhibition of cell wall synthesis

Bind to PBPs

Inhibits final stage of cell wall construction

Weakens cell wall leading to cell lysis

Especially in dividing bacteria

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4
Q

Beta-Lactam Indications

A

Respiratory tract infections

UTIs

Skin soft tissue infections

Septicemia

Meningitis (ceftriaxone)

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5
Q

Beta-Lactams Efficacy Depends on?

A

Time-Dependent Killing
Duration at which concentration exceeds the MIC of the pathogen for 40-60% of dosing interval

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6
Q

Beta-Lactams are most effective against?

A

Rapidly replicating organisms

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7
Q

Bacterial enzymes responsible for cell wall/peptidoglycan synthesis

A

Transpeptidase
Carboxypeptidase
Endopeptidase

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8
Q

Beta-Lactam Penicillin absorption

A

Penicillin V (PO) GI tract, presence of food delays/decreases, take on empty stomach

Procaine Penicillin G (IM) slow and prolonged, sustained blood levels

Benzathine Penicillin G (IM) Very slow, very low but prolonged blood levels

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9
Q

Beta-Lactam Penicillin Distribution

A

Widely distributed throughout body Penetrates tissues and body fluids.

Limited penetration into the CSF unless meninges are inflamed

Penicillin V (PO) 80% protein-bound in plasma

Procaine/Benzathine penicillin G (IM) 60% protein-bound in plasma

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10
Q

Beta-Lactam Penicillin Metabolism

A

Penicillin V (PO) minimal metabolism, inactive metabolites in liver.

Procaine penicillin G (IM) minimal metabolism, procaine is hydrolyzed to PABA

Benzathine penicillin G (IM) minimal metabolism

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11
Q

Beta-Lactam Penicillin Excretion

A

Primarily by kidneys

Dose adjustment in renal impairment

90% renal by active tubular secretion

Penicillin V (PO) drug is unchanged in urine within 24 hrs.

Procaine penicillin G (IM) Majority of drug is unchanged in urine.

Benzathine penicillin G (IM) Majority of drug is unchanged in urine.

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12
Q

Common Beta-Lactam Side effects

A

GI upset, rash, allergic reactions

IM injection site reactions

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13
Q

Serious Beta-Lactam Side effects

A

Hypersensitivity reactions including

Steven-Johnson Syndrome

Toxic epidermal necrolysis

C-Diff

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14
Q

Beta-Lactam Contraindications

A

Hypersensitivity to beta-lactams

Cross-sensitivity with penicillins and cephalosporins

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15
Q

What things cause Beta-Lactam Resistance?

A

Beta-Lactamase production (hydrolysis beta-lactam ring)

Use clavulanic acid, tazobactam to counter act beta-lactamase

Altered PBPs (Reduces affinity of beta-lactams)

Efflux pumps and porin changes (cell membrane permeability)

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16
Q

Need to know Penicillins

A

Penicillin V (PO)
Penicillin G (IM)
Amoxicillin
Amoxicillin/clavulanate

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17
Q

Natural Penicillins

A

Penicillin V (PO)
Penicillin G (IM)

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18
Q

Penicillin V and Benzathine/Procaine Penicillin G MOA

A

Inhibits bacterial cell wall synthesis binding PBPs leading to cell lysis

19
Q

Common Side Effects of Penicillin V (PO), Benzathine/Procaine Penicillin G (IM)

A

Nausea, Vomiting, diarrhea, rash, anaphylaxis (rare)

Injection site reaction (Pain, redness, swelling)

20
Q

Penicillin V Monitoring

A

Renal function

Signs of allergic reactions

Hematologic parameters in prolonged therapy

21
Q

Black Box Warning for Penicillin V

A

No black box warning

22
Q

Black Box Warning for Procaine/Benzathine Penicillin G

A

Avoid injections near veins and arteries. Can cause cardiac arrest.

23
Q

Major ADRs Penicillin V

A

Anaphylaxis, SJS, toxic epidermal necrolysis, C-Diff, Hemolytic anemia, thrombocytopenia, leukopenia

24
Q

Major ADRs Benzathine Penicillin G (IM)

A

Severe allergic reactions
SJS
Toxic epidermal necrolysis
C-Diff
Hemolytic anemia
Thrombocytopenia
Leukopenia
Neurotoxicity (High doses, or renal impairment can lead to seizures)

25
Q

Is Benzathine/Procaine Penicillin G (IM) Penicillin V (PO) Bacteriostatic or Bactericidal?

A

Bactericidal (kills rather than inhibiting)

26
Q

What do penicillins bind to?

A

Plasma protein Bound

27
Q

Do Penicillins cross the placenta and breast milk?

A

Yes

28
Q

Natural penicillins are active against?

A

Aerobic, gram-positive organisms, streptococcus species (S. Pneumoniae, Group A beta-hemolytic streptococcus, some enterococcus, Some non-penicillinase producing staphylococci.

29
Q

5-15% of Community-aquired staphylococcus aureus remain susceptible to natural penicillins because

A

Penicillinase hydrolyzes the beta-lactam ring rendering them completely ineffective

30
Q

Penicillin-Resistant Streptococcus Pneumoniae prevalence is down because

A

Vaccinations PCV 13,15,20

31
Q

Beta-Lactam Aminopenicillins

A

Amoxicillin
Amoxicillin/clavulanate

32
Q

Amoxicillin MOA

A

Inhibition of cell wall synthesis

Bind to PBPs

Inhibits final stage of cell wall construction

Weakens cell wall leading to cell lysis

33
Q

Amoxicillin/Clavulanate MOA

A

Inhibition of cell wall synthesis

Bind to PBPs

Inhibits final stage of cell wall construction

Weakens cell wall leading to cell lysis

Inhibits beta-lactamase produced by bacteria, protecting amoxicillin, extending spectrum activity

34
Q

Amoxicillin Indications

A

CAP
Acute Otitis media
Sinusitis
Lyme disease
Chronic bronchitis
DRSP

35
Q

Amoxicillin/clavulanate Indications

A

CAP
Serious or resistant infections
Acute exacerbation of chronic bronchitis
Acute otitis media/sinusitis
Animal bites

36
Q

Amoxicillin/clavulanate excellent activity against?

A

Staphylococcus aureus (MSSA), Streptococcus, enterococcus, H influenzae, N meningitidis, salmonella, some shigella species

37
Q

Amoxicillin and Amoxicillin/Clavulanate Common Side Effects

A

GI upset
Rash
Allergic reactions

38
Q

Amoxicillin and Amoxicillin/Clavulanate Monitoring

A

Renal function (specifically those with renal impairment)

Signs of allergic reaction (rash, itching, swelling, respiratory difficulties)

Hepatic function during prolonged therapy (clavulanate can cause hepatic dysfunction)

39
Q

Amoxicillin and Amoxicillin/Clavulanate ADRs

A

Severe allergic reactions
SJS
Toxic epidermal necrolysis
C-Diff
Hemolytic anemia
Thrombocytopenia
Leukopenia
Hepatic dysfunction (jaundice/hepatitis more common with clavulanate)

40
Q

Is Amoxicillin and Amoxicillin/Clavulanate Bacteriostatic or Bactericidal?

A

Bactericidal

41
Q

Do Amoxicillin and Amoxicillin/Clavulanate cross BBB, placenta, and into the breast milk

A

Only if meninges are inflamed

Yes, cross placenta (Safe during pregnancy when indicated

Yes, small amounts are excreted into breast milk (can cause GI upset and allergic reactions to nursing infant)

42
Q

Leading Risk Factors leading to Resistance

A

Recent use of antimicrobials

Multiple medical comorbidities

Recent hospitalization or other skilled healthcare contact

43
Q

Bactericidal

A

Refers to 99.9% eradication of a bacterial colony in vitro in 24 hrs by an antimicrobial.

44
Q

Bacteriostatic

A

Refers to an abx that kills bacteria but the result is less than 99.9% eradication in a 24hr period.

advanced pharm (50 decks)

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