Antimicrobial 1: Agents that Target the Bacterial Cell Wall or Folic Acid Metabolism Flashcards
what are antivirals?
classification?
Describes drugs that kill viruses
• Antivirals are not considered antimicrobials
Bactericidal
- agents that interfere with bacterial cell wall
synthesis or inhibit crucial enzymes that kill bacteria
Bacteriostatic
- agents that inhibit protein synthesis and prevent
bacterial growth and/or replication
what different conditions/disorders (both acute and chronic) are the result of bacterial infections
– Food Poisoning – Sexually Transmitted Infections (STIs) – Whooping Cough – Pneumonia – Tuberculosis – Respiratory Tract Infections
Name 2 classes of antibiotics Targeting Folate Synthesis
– Sulfonamides (sulfa antibiotics)
– Folic acid antagonists (trimethoprim, pyrimethamine)
Sulfonamides
drugs
– Sulfanilamide – Sulfamethoxazole – Sulfasalazine (GI, RA) – Sulfadiazine – Sulfadoxine (Anti-Malarial)
Sulfonamides
MOA?
- Are structural analogs of PABA and competitively inhibit dihydropteroate synthetase which turns PABA to dihydropteroic acid and later dihydrofolic acid
- Folic acid is required to synthesize purines & pyrimidines, which are required by bacteria to synthesize DNA and RNA
Sulfonamides
AE? (4)
– *Hepatitis – Hypersensitivity reactions (Stevens-Johnson syndrome) – *Bone marrow depression – *Acute renal failure – *Cyanosis – Nausea, Vomiting, Headache – Depression
Folic acid antagonists
name 2
– Trimethoprim
– Pyrimethamine
Folic acid antagonists
MOA
- Are folate antagonists that structurally resemble the pteridine moiety of folate, thereby inhibiting the bacterial dihydrofolate reductase
– When combined with sulfonamides you get potentiated actions on decreasing bacterial DNA/RNA synthesis
Folic acid antagonists
AE
– *Folate deficiency – *Megaloblastic anemia – Nausea, Vomiting – Blood disorders/dyscrasias – Rashes
β-Lactam Antibiotics
4 classes
target peptidoglycan synthesis
– Penicillins
– Cephalosporins
– Carbapenems
– Monobactams
β-Lactam Antibiotics
MOA
inhibit bacterial transpeptidase and thereby inhibit
peptidoglycan cross-linking/synthesis
- Are selective and irreversible inhibitors of the enzymes (penicillin binding proteins
(PBPs)) processing the developing peptidoglycan layer.
– This enzyme is one of the PBP (carboxypeptidase, endopeptidase, transpeptidase), normally reside in inner membrane and perform construction,
repair and housekeeping.
β-Lactam Antibiotics
how does resistance occur
- β-lactamase are enzyme produced by the bacteria that catalyze the hydrolysis of β-lactam ring and inactivate the β-lactam antibiotic before they reach the PBPs.
- They resemble in function and somewhat structure to the cell wall transamidases
β-Lactam Antibiotics
Penicillins
prototype?
narrow, extended, broad spectrum?
– Prototype (Penicillin G, Penicillin V)
– Narrow-spectrum (Cloxacillin, Oxacillin, Nafcillin)
– Extended-spectrum (Ampicillin, Amoxicillin)
– Broad-spectrum (Piperacillin, Ticarcillin)
β-Lactam Antibiotics
Penicillins
indications?
– Bacterial meningitis – Bone and joint infections – Skin/soft tissue infections – Pharyngitis – Bronchitis – Pneumonia – Urinary tract infections – Sexually transmitted infections (e.g. gonorrhea, syphilis)
β-Lactam Antibiotics
Penicillins
AE? (1)
MOA?
– Hypersensitivity reactions
– Skin rashes & fever
– Anaphylactic shock
– GI disturbances and infection via penicillin-insensitive microorganisms
– *Proconvulsant effect (if penicillin G given intrathecally)
- Irreversible inhibition of the PBPs