Penicillins Flashcards
Where in the body do the penicillins NOT distribute?
- Eye 2. Prostate
What factors affect the distribution of penicillins?
- Molecular configuration of the penicillin 2. Protein binding “Penicillins Meet Proteins”
When are adequate concentrations of penicillins in the CSF attained?
Only in the presence of INFLAMED MENINGES when HIGH DOSES of parenteral penicillins are used
Give 2 examples of penicillins that bind to serum proteins and their respective binding percentages.
- Aminopenicillins - 15% 2. Dicloxacillin (Penicillinase-Resistant) - 97%
List the penicillins that are NOT primarily eliminated by the kidneys, and list their appropriate route of elimination.
- Nafcillin (Penicillinase-Resistant Penicillin)
- Elimination via liver - Oxacillin (P-R-P)
- Elimination via liver - Dicloxacillin (P-R-P)
- Renal with some hepatic - Piperacillin (Ureidopenicillin)
- Dual elimination: liver and kidneys - Piperacillin-Tazobactam (Beta-lactamase Inhibitor Combination)
- Dual elimination
Which penicillins are NOT removed during hemodialysis?
- Nafcillin (P-R-P) 2. Oxacillin (P-R-P) 3. Dicloxacillin (P-R-P) THINK: “N.ot O.ut from D.ialysis”
What is the general half-life characteristic for ALL penicillins?
-Relatively short elimination half-life -2 hours half-life
Which penicillins do NOT require dosing changes for renal insufficiency?
- Nafcillin (P-R-P) 2. Oxacillin (P-R-P) 3. Dicloxacillin (P-R-P) THINK: “N.O. D.ose changes”
In what situation would you use aqueous penicillin G (IV)?
-Serious infections in hospitalized patients (rapid effect and high serum concentrations)
What situation would call for penicillin VK (oral)?
-Mild to moderate infections (pharyngitis or prophylaxis) due to low serum concentrations of the drug
Natural penicillins are a drug of choice for which infection types?
- S. pneumoniae (IV or IM): penicillin susceptible or intermediate strains
- Neisseria meningitis (IV)
- Clostridium perfringens or tetani
- Actinomycosis
- Viridans streptococci pharyngitis (PO or IM)
- Treponema Pallidium: syphillis
“Pen CAN Stop The Virulence”
For what type of infection would Benzathine penicillin or aqueous penicillin be a drug of choice?
Streptococci like S. pyogenes
Bacteremia treatment and endocarditis prophylaxis could be accomplished with what classes of penicillins as a drug of choice?
- Natural penicillins (along with an aminoglycoside) 2. P-R-Ps
In treating Treponema pallidum, or syphilis, what would be the drug(s) of choice?
Benzathine penicillin or IV (aqueous) penicillin
What is another name for the Penicillinase-Resistant Penicillins?
Antistaphylococcal Penicillins
What agents are useful for the treatment of infections due to methicillin-susceptible Staphylococcus aureus (MSSA)?
Penicillinase Resistant Penicillins (Antistaphylococcal Penicillins)
Give some examples of diseases caused by MSSA?
-Skin and soft tissue infections -Septic arthritis -Osteomyelitis -Bacteremia -Endocarditis
Oral dicloxacillin is useful for treatment of type of infection?
-Mild to moderate skin and soft tissue infections -As a follow-up therapy after parenteral therapy for the treatment of more serious infections (i.e. osteomyelitis and septic arthritis)
What class of penicillins work best for pathogens of the respiratory tract (i.e. mild to moderate pharyngitis, sinusitis, otitis media, bronchitis)?
Aminopenicillins (PO)
Parenteral Ampicillin is used for treatment of what types of infections?
-Enterococcal infections (with an aminoglycoside for endocarditis) -Listeria monocytogenes (meningitis) “Ampicillin Eats Listeria” or “AmpLE”
Due to their enhanced activity against gram-negative bacteria, which classes of penicillins are useful towards hospital-acquired infections?
Carboxypenicillins and Ureidopenicillins active against: P. Aeruginosa
List some examples of hospital acquired infections.
Serious infections such as:
- Bacteremia
- Pneumonia
- Complicated UTIs
- Peritonitis
- Skin and soft tissue infections
- Bone and joint infections
- Meningitis
What is the most active penicillin for infections due to Pseudomonas aeruginosa?
Piperacillin (Ureidopenicillin class)
Amoxicillin-clavulanate (Augmentin-PO) is useful for treatment of what diseases?
- Otitis media
- Sinusitis
- Bronchitis
- Lower Respiratory Infections
- Bites (human or animal)
“BLOBS”
What group of penicillins are utilized in the treatment of polymicrobial infections (i.e. intra-abdominal infections, gynecological infections, diabetic foot infections)?
Parenteral combination agents (Beta-lactamase Inhibitor Combination Products)
Ampicillin-sulbactam (IV) is useful for the treatment of which type of infections?
Mixed aerobic/anaerobic infections (limited gram-negative coverage)
What is the treatment option for infections caused by Stenotrophomonas maltophilia?
Ticarcillin-clavulanate (IV)
Why is Piperacillin-tazobactam more tolerable than Ticarcillin-clavulanate?
Ticarcillin has a higher sodium load
What does Piperacillin-tazobactam (IV) treat?
- Polymicrobial infections
- Gram-negative, hospital-acquired infections
- Empiric therapy for febrile neutropenia
What is the most frequently occurring side effect of penicillins?
Hypersensitivity (3-10%)
-less frequent with oral administration
What causes cross-allergenicity among natural and semi-synthetic penicillins?
- Their common nucleus
- If allergic to one type of penicillin = allergic to other members of the penicillin family (and caution used with other beta-lactams)
What are some neurologic adverse effects of penicillins?
-Seizures -Irritability -Jerking -Confusion
List some gastrointestinal adverse effects of penicillins?
- Nausea, vomiting
- Diarrhea (esp. amoxicillin-clavulanate)
- Pseudomembranous colitis (C. difficile diarrhea)
What types of penicillins typically cause interstitial nephritis (immune-mediated damage to renal tubules)?
-Methicillin (PRP) -Nafcillin (PRP)
What are some physical manifestations of interstitial nephritis?
- Fever
- Eosinophiluria
- Abrupt increase in serum creatinine
How does Ticarcillin cause hypokalemia?
It acts as non-reabsorbable anions resulting in increased excretion of potassium
What types of penicillin cause sodium overload and fluid retention?
Ticarcillin and piperacillin
