ID Pharmacology Flashcards
What is the MOA of aminoglycosides? Type of antibiotics?
Examples? (3)
Protein synthesis inhibitor
Irreversibly binds 30S to prevent protein synthesis. Also:
* mRNA misreading
* Impaired initiation
* Premature initiation
- Neomycin, Gentamicin,
Tobramycin
T/F aminoglycosides have time-dependant effects
False
- Concentration-dependent effects
- Single high dose is more effective than a divided daily dose
What are the side effects of aminoglycosides? (3)
- Nephritis (renal toxicity)
- Ototoxicity (hearing loss)
- Headache
What is the MOA of oxazaolidinones?
Examples? (3)
Type of antibiotic?
Protein synthesis inhibitors
Are “P-site inhibitors” that bind 23S unit within 50S to prevent the 50S and 30S subunits from interacting.
Examples:
Linezolid
Tedizolid
Sutezolid
What are the side effects of linezolid (6)
GI, HA, rash
- Bone marrow suppression (myelosuppresion)
- peripheral neuropathy
- lactic acidosis
What is the MOA of tigercycline resisitance
Tigecycline is resistant to Tet pump efflux because of its larger/bulky side chain.
Sulfonamides MOA
Example?
Type of antibiotic
DNA synthesis inhibitor
Structurally resemble PABA, competing with PABA to inhibit dihydroPTEROATE synthase, preventing folate production to slow down DNA synthesis/cell replication.
Example:
Sulfamethoxazole
Why do we add trimethoprim to sulfamethoxazole?
Binds another enzyme called dihydroFOLATE reductase
- much more selective for protozoal/bacterial enzyme
What are side effects of sulfonimides? (6)
GI
Fever
Rash, urticaria, photosensitivity
Anemia in patients with G6PD deficient
Nitrofurantoin MOA (3)
A prodrug that is activated by nitroreductases to generate reactive species that:
- Bind ribosome proteins
- Damage DNA
- Prevent DNA repair
What is special about nitrofurantoin’s PK?
Very quickly absorbed, food increases absorption?
What are Nitrofurantoin side effect profile? (7)
- HA, nausea
- brown-yellow urine; hepatitis
- peripheral neuropathy
- hemolytic anemia (if G6PD deficiency)
- acute or chronic lung reactions (<1 week or >6 months)
What is the MOA of damptomycin?
Type of antibiotic?
A cyclic lipopeptide derived from Streptomyces roseosporus that uses its LIPOPHILIC TAIL to embed itself into the cell membrane to form pores that cause K+ efflux and cell death.
Cell-wall synthesis inhibitor
(similar to vancomycin)
What drug class are antivirals?
MOA?
Class:
- Guanine nucleoside analogues
Undergo many phosphorylation steps, eventually becoming the triphosphate form after being activated by host enzymes,
including viral THYMIDINE KINASE and DNA POLYMERASE, they are incorporated into DNA and causes termination of synthesis
What are the side effects of antivirals? (5)
- N/V/D
- Rash
- Headache
- Nephrotoxicity
- Neurotoxicity
What is gentamicin produced from?
Micromonospora purpurea
What is tobramycin produced from?
Streptomyces tenebarius
What pharmacophore group is in amikacin
Butanamide
What pharmacophore is in fosomycin
Epoxide
What 2 pharmacophores are in linezolid
Morpholine (primary reason for excellent bioavailability)
Oxazolidinone
What pharmacophore is in sulfamethoxazole
Isoxazole
What 2 functional groups are in nitrofurantoin?
Furan
Hydantoin
What is the key functional group in daptomycin
Decanoyl chain
