B-lactámicos Flashcards
Benzylpenicillin (Penicillin G)
- Route of admin: Intravenous or intramuscular.
- Mechanism: inhibition of cell wall synthesis mediated through penicillin G binding to PBPs.
- Therapeutic uses: Streptococcal, meningococcal, gonococcal.
Gram + =Strep. pyogenes and pneumoniae.
Gram - cocci= Neisseria meningitidis
Spirochetes= treponema pallidum
Branching gram += Actinomyces
-Adverse reactions: Hypersensitivity reactions, hemolityc anemia, interstitial nephritis, seizures.
Ampicillin
-Route of admin: Intravenous or intramuscular.
+Sulbactam (beta lactamase inhibitor)
-Mechanism of action: Inhibition of cell wall synthesis mediated through Ampicillin binding to PBPs.
-Therapeutic uses: Broad spectrum
gram+ aerobes
gram - rods
- Not Enterobacter spp
Most effective vs: “HHEELPSSS”
- H. pylori
- H. influenzae
- Listeria monocytogenes
- Proteus mirabilis
- Salmonella
- Shigella
- Enterococci
- Spirochetes
- Upper respiratory tract infections (sinusitis, pharyngitis, otitis media)
- Adverse reactions:
- Diarrhea
- Pseudomembranous colitis
- Hypersensitivity reactions
- Drug-induced rash
- Acute intersticial nephritis
Carbenicillin
AR: IV or IM
MA: Acylation of the transpeptidase C-terminal domain > inhibition of cell wall synthesis
TU: Acute and chronic infections of the upper and lower urinary tract and in asymptomatic bacteriuria.
- Escherichia coli
- Proteus mirabilis
- Proteus vulgaris
- Morganella morganii, - Pseudomonas spp.
- Enterobacter spp
- S. faecalis).
AR:
- Hypersensitivity reactions
- GI changes
- Rash
Ticarcillin
RA: IV or IM
MA: Prevention of the cross-linking of peptidoglycan during bacterial cell wall synthesis > inhibition of cell wall synthesis
TU: Extended spectrum of gram (-) as well as bacterial infections by P. aeruginosa.
*Paired with clavulanic acid
AR:
- Hypersensitivity reactions
- Diarrhea
- Rash
Amoxicillin
- Route of admin: Intravenous or Intramuscular
+Clavunate (beta lactamase inhibitor) - Mechanism of action: Inhibition of penicillin binding protein 1 –>inhibition of cell wall synthesis
- Therapeutic uses: Broad spectrum
gram+ aerobes
gram - rods
- Not Enterobacter spp
Most effective vs: “HHEELPSSS”
- H. pylori
- H. influenzae
- Listeria monocytogenes
- Proteus mirabilis
- Salmonella
- Shigella
- Enterococci
- Spirochetes- Upper respiratory tract infections (sinusitis, pharyngitis, otitis media)
- Adverse reactions:
- Diarrhea
- Pseudomembranous colitis
- Hypersensitivity reactions
- Drug-induced rash
- Acute intersticial nephritis
Azlocillin
- Route of admin: Intravenous
- Mechanism of action: Binding to specific PBPs, inhibiting the third stage of cell wall synthesis.
- Therapeutic uses:
Treatment of infections caused by:
- Pseudomonas aureginosa
- Escherichia coli
- Haemophilus influenzae - Adverse reactions:
- Hematologic: anemia, thrombocytopenia, neutropenia, agranulocytosis
*Endocrine: hyperthermia
*Renal: nephrotoxicity, interstitial nephritis
*Hepatic: transient increases in transaminases
*Other: Jarisch-Herxheimer Reaction (fever, chills, sweating, tachycardia, hyperventilation, flushing, and myalgia)
Piperacillin
- Route of admin: Intravenous
+ Tazobactam (beta lactamase inhibitor) - Mechanism of action: Binding to specific PBPs inhibiting the last stage of cell wall synthesis.
- Therapeutic uses: Extended spectrum but penicillinase
gram - rods
-✔ Pseudomonas
anaerobes
gram + aerobes
-✘ S.viridians- Nosomical infections
- pneumonia
- intraabdominal infec.
- urinary tract infec.
- Adverse reactions:
- Hypersensitivity reactions
- Diarrhea
- Constipation
*Trouble sleeping - Nausea
- Headache
Mezlocillin
- Route of admin: Intravenous or intramuscular
- Mechanism of action: Binding to specific PBPs inhibiting the last stage of cell wall synthesis.
- Therapeutic uses: Treatment of gram - infections of the lungs, urinary tract and skin.
—>Stable against beta lactamases
- H. influenzae
- Klebsiella
- Pseudomonas
- Proteus mirabilis
- E. coli
- Enterobacter
- Step. faecelis
- Peptococcus
- Peptostreptococcus
- Bacterodes
- Morangella
- Serratia
- N. gonorrhoeae
- P. vulgaris
- Providencia
- Adverse reactions:
- Urticarial rash
- Angioedema
- Pruritus
- Bronchospasm
- Hypotension
- Anaphylaxis
Clavulanate
- Route of admin: Oral, IM and IV
+ Amoxicillin (penicillin derivative) - Mechanism of action: Beta lactamase inhibitor, contains a beta lactam ring that binds to the beta lactam active site and inactivates the enzyme.
- Therapeutic use: Treatment of bacterial infections that produce beta lactamase.
- Adverse reactions:
- Vomiting
- Nausea
- Loose stools
- Discomfort
- Diarrhea (most common in amoxicillin-clavulanic)
Dicloxacillin
- Route of admin: Oral
- Mechanism of action: Binding to specific PBPs inhibiting the last stage of cell wall synthesis. Bactericidal action during the state of active muktiplication.
- Beta lactamase resistant
- Therapeutic uses:
NARROW spectrum
gram + aerobes- Staphylococcus aureus
✔MSSA
✘ Streptococcus viridians
✘ Enterococci
✘ Listeria
- Staphylococcus aureus
- Skin and soft tissue infections
- Adverse reactions:
*Nausea
*Diarrhea
*Skin rash
*Allergic reactions
Meropenem
- Route of admin: Intravenous
- Mechanism:
Inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs) - Therapeutic uses:
LAST-Resort Drugs - ONLY @life threatening infections or after antibiotics have failed
BROAD spectrum w/ beta-lactamase resistance - gram +
- gram -
- anaerobic
**NOT active against MRSA
Tx of polymicrobial hospital adquired infections = Nosomical Infections - ej. septicaemia
- pneumonia
- complicated urinary infections
-Adverse reactions:
*Bluish lips or skin
*chills
*cold, clammy skin
*confussion
*dizziness
*fainting
*fast heartbeat
*fast, weak pulse
Imipenem
- Route of admin: IV
+Cilastatin
(✘ inactivation by renal enzymes → inhibits dehydropeptidase) - Mechanism:
Inhibition of cell wall synthesis of various gram-positive and gram-negative bacteria. This inhibition of cell wall synthesis in gram-negative bacteria is attained by binding to penicillin-binding proteins (PBPs)
-Therapeutic uses:
LAST-Resort Drugs
- ONLY @life threatening infections or after antibiotics have failed
BROAD spectrum w/ beta-lactamase resistance
* gram +
* gram -
* anaerobic
**NOT active against MRSA
Tx of polymicrobial hospital adquired infections = Nosomical Infections
* ej. septicaemia
* pneumonia
* complicated urinary infections
Adverse reactions:
*Confusion
*convulsions (seizures)
*dizziness
*pain at place of injection
*skin rash, hives, itching, fever, or *wheezing
*tremors
Vancomycin
RA: Mainly IV, Oral only for C. difficile
MA: High affinity binding to D-alanyl-D-alanine = Inhibition of cell wall synthesis
TU:
- Skin and soft-tissue infections
- Bacteremia and endocarditis due to
gram-positive bacteria
- Pneumonia
- Meningitis
- Clostridium difficile
- Surgical prophylaxis
- MRSA
AR:
- Nephrotoxicity
- Ototoxicity
- Red man syndrome
- Nausea, abdominal pain, hypokalemia
Colistin (Polymyxin E)
RA: IV or IM
MA: Surface active agent which penetrates into and disrupts the bacterial cell membrane by changing its permeability.
TU:
Most Pseudomonas, Acinetobacter, and Enterobacteriaceae are susceptible, except for
Proteus and Serratia spp.
- Bacteremia
- Pneumonia
- Bone/joint infections
- Burns
- Cellulitis
- Cystic fibrosis
- Endocarditis
- Meningitis
AR
- Dose related nephrotoxicity
- Weakness, apnea, paresthesia, vertigo.
Polymyxin B
RA: IV or IM
MA: Surface active agent which penetrates into and disrupts the bacterial cell membrane by changing its permeability.
TU: Most Pseudomonas, Acinetobacter, and Enterobacteriaceae are susceptible, except for
Proteus and Serratia spp.
- Bacteremia
- Pneumonia
- Bone/joint infections
- Burns
- Cellulitis
- Cystic fibrosis
- Endocarditis
- Meningitis
Ophthalmic, otic, and
topical use in combination with a variety of other compounds.
AR:
- Dose related nephrotoxicity
- Weakness, apnea, paresthesia, vertigo.
