Penicillin: Difference between revisions

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== Background ==
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==Background==
   
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=== Mechanism of action ===
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===Nomenclature===
   
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*Broadly speaking, formulations of penicillin G are soluble and used for IV or IM administration, and penicillin V is used for oral administration but does not achieve high levels in the serum
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* Directly inhibits [[Penicillin-binding protein|penicillin-binding proteins]]
  
   
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{| class="wikitable"
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[[Category:Beta-lactams]]
  
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!Formulation
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!Other Names
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!Comments
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|-
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|sodium penicillin G
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|sodium benzylpenicillin
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crystalline penicillin
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|soluble, used for IV
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|-
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|procaine penicillin G
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|procaine benzylpenicillin
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procaine penicilli
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|less soluble, used for IM
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|-
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|benzathine penicillin G
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|DBED penicillin
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|less soluble than procaine, used for IM
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|-
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|penicillin V
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|phenoxymethylpenicillin
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|used for PO, but poor absorption
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|}
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===Mechanism of Action===
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*Directly inhibits [[Penicillin-binding protein|penicillin-binding proteins]]
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===Spectrum of Activity===
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*Generally active against Gram-positive cocci, especially [[streptococci]] but some strains of [[Staphylococcus aureus]], most [[clostridia]], [[Neisseria]], and some [[Haemophilus influenzae]]
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*Not active against aerobic Gram-negative bacilli
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*Penicillin G is generally more active than penicillin V across all bacteria
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===Clinical Breakpoints===
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{| class="wikitable"
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! rowspan="2" |Species
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! colspan="3" |Breakpoints (μg/mL)
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! colspan="3" |Breakpoints (mm)
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|-
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!S
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!I
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!R
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!S
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!I
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!R
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|-
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|[[Anaerobes]] except [[Bacteroides]]
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|≤0.5
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|1
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|≥2
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|
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|
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|
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|-
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|[[Enterococcus]]
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|≤8
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|
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|≥16
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|≥15
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|
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|≤14
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|-
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|[[Neisseria gonorrhoeae]]
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|≤0.06
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|0.12-1
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|≥2
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|≥47
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|27-46
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|≤26
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|-
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|[[Neisseria meningitidis]]
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|≤0.06
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|0.12-0.25
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|≥0.5
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|
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|
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|
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|-
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|[[Staphylococcus]]
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|≤0.12
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|
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|≥0.25
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|≥29
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|
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|≤28
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|-
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|[[Streptococcus pneumoniae]]
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|
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|
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|
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|≥20
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|
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|
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|-
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|[[Streptococcus pneumoniae]] IV (nonmeningitis)
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|≤2
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|4
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|≥8
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|
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|
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|
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|-
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|[[Streptococcus pneumoniae]] IV (meningitis)
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|≤0.06
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|
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|≥0.12
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|
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|
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|
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|-
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|[[Streptococcus pneumoniae]] PO (pen V)
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|≤0.06
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|0.12-1
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|≥2
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|
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|
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|
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|-
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|[[Streptococcus]] (β-hemolytic)
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|≤0.12
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|
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|
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|≥24
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|
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|
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|-
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|[[Streptococcus]] (viridans group)
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|≤0.12
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|0.25-2
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|≥4
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|
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|
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|
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|}
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== Dosing ==
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* Benzylpenicillin (penicillin G)
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** Standard dosing: 3 million units (1.8 g) IV q4h, or 4 million units (2.4 g) IV q6h
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** High dose (for critical illness, IE, and CNS penetration): 4 million units (2.4 g ) IV q4h
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=== Renal Dosing ===
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==== Benzylpenicillin (Penicillin G) ====
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{| class="wikitable"
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!GFR (mL/min)
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!Standard Dose
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!High Dose
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|-
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|>50
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|3 MU (1.8 g) IV q4h, or 4 MU (2.4 g) IV q6h
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|4 MU (2.4 g ) IV q4h
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|-
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|10-50
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|3 MU (1.8 g) IV q6h
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|3 MU (1.8 g) IV q4h
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|-
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|<10
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|3 MU (1.8 g) IV load, then 2 MU (1.2 g) IV q8h
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|4 MU (2.4 g) IV load, then 2 MU (1.2 g ) IV q6h
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|-
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|CRRT
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|2 MU (1.2 g) IV q6h
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|3 MU (1.8 g) IV q6h
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|}
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== Safety ==
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=== Adverse Reactions ===
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==== Hypersensitivity Reactions ====
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* Can cause any type of [[hypersensitivity reaction]] (I to IV)
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* Type I: [[anaphylaxis]] and [[urticaria]]
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* Type II: [[autoimmune hemolytic anemia]]
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* Type III: [[serum sickness-like reaction]]
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* Type IV:
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** Delayed maculopapular drug rash
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*** Usually after 7 to 10 days of starting and up to 1 to 3 days after stopping)
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*** Progresses over days, with lesions that are relatively fixed
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*** Can worsen over a few days after stopping, then resolves over 1 to 2 weeks
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*** Pruritis is variable
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*** Most commonly occur in the context of a viral infection
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** [[Contact dermatitis]]
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[[Category:Β-lactams]]

Latest revision as of 14:44, 30 August 2022

Background

Nomenclature

  • Broadly speaking, formulations of penicillin G are soluble and used for IV or IM administration, and penicillin V is used for oral administration but does not achieve high levels in the serum
Formulation Other Names Comments
sodium penicillin G sodium benzylpenicillin

crystalline penicillin

soluble, used for IV
procaine penicillin G procaine benzylpenicillin

procaine penicilli

less soluble, used for IM
benzathine penicillin G DBED penicillin less soluble than procaine, used for IM
penicillin V phenoxymethylpenicillin used for PO, but poor absorption

Mechanism of Action

Spectrum of Activity

Clinical Breakpoints

Species Breakpoints (μg/mL) Breakpoints (mm)
S I R S I R
Anaerobes except Bacteroides ≤0.5 1 ≥2
Enterococcus ≤8 ≥16 ≥15 ≤14
Neisseria gonorrhoeae ≤0.06 0.12-1 ≥2 ≥47 27-46 ≤26
Neisseria meningitidis ≤0.06 0.12-0.25 ≥0.5
Staphylococcus ≤0.12 ≥0.25 ≥29 ≤28
Streptococcus pneumoniae ≥20
Streptococcus pneumoniae IV (nonmeningitis) ≤2 4 ≥8
Streptococcus pneumoniae IV (meningitis) ≤0.06 ≥0.12
Streptococcus pneumoniae PO (pen V) ≤0.06 0.12-1 ≥2
Streptococcus (β-hemolytic) ≤0.12 ≥24
Streptococcus (viridans group) ≤0.12 0.25-2 ≥4

Dosing

  • Benzylpenicillin (penicillin G)
    • Standard dosing: 3 million units (1.8 g) IV q4h, or 4 million units (2.4 g) IV q6h
    • High dose (for critical illness, IE, and CNS penetration): 4 million units (2.4 g ) IV q4h

Renal Dosing

Benzylpenicillin (Penicillin G)

GFR (mL/min) Standard Dose High Dose
>50 3 MU (1.8 g) IV q4h, or 4 MU (2.4 g) IV q6h 4 MU (2.4 g ) IV q4h
10-50 3 MU (1.8 g) IV q6h 3 MU (1.8 g) IV q4h
<10 3 MU (1.8 g) IV load, then 2 MU (1.2 g) IV q8h 4 MU (2.4 g) IV load, then 2 MU (1.2 g ) IV q6h
CRRT 2 MU (1.2 g) IV q6h 3 MU (1.8 g) IV q6h

Safety

Adverse Reactions

Hypersensitivity Reactions

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