IV and Opthalmic Ointmens

IV for resistant & serious aerobic/anaerobic G+/- bacteria

Associated with Fatal Blood Dyscrasias

Mechanism: inhibits bind of aminoacyl-tRNA to acceptor site

Problem: Also inhibits mammalian peptidyltransferase. RBCs are most sensitive (leucopenia, thrombocytopenia, fatal aplastic anemia)

Also inhibits CytoP450

Gray Baby Syndrome caused by:

-insufficient glucoronyl transferase

-underdeveloped renal function

-CV collapse

-cynasosi

streptogamins given IV for MRSA & vancomycin resistant infections. Synergistic together.

Mechanism: Quinupristin release peptidyl-tRNA from donor site. Dalfopristin inhibits binding of aminoacyl-tRNAto acceptor site and peptidyl-tRNA to donor site

Inhibits CYP3A

Rarely used because its only IV

Side Effects: superinfection, myalgias, venous irritation, hyperbilirubinemia

For enterococcus faecium, MSSA,MRSA, and other vancomycin-resistant bacteria

Static or Cidal depending on bacteria

Oral & IV

Mechanisim: inhibits formation of initiation complex

May cause serrotonin syndrome (restlessness, tremor, delirium, rigidity, myoclonus, hyperthermia, hyperflexia, sweating...)

Chronic use ( >28days) leads to reversible optic neuropathy, irreversible peripheral neuropathy, lactic acidosis

risk of pseudomembranous colitis

Penetrates most tissues except for CNS (even if inflammed)

Many dosage forms - topical acne, oral, IV, vaginal suppository

Mechanism: Inhibits translocation from A to P

G- Organisms

Very nephro and neurotoxic

Limited to topical use (IV and oral rarely)

Uses: Common bacterial infection of the conjunctiva & eye lids

Available alone or with other drugs

aka Polymyxin E

Cidal cationic detergent

Very neprho and neurotoxic

IV/IM for various G- rods

related to aminoglycosides but static not cidal.

Use only as 2gm IM dose for gonorhea in patients allergic to PCN or PCN-resistant strains

for travelers diarrhea from noninvasive E. Coli

no significant system abortion

Mechanis: Binds to DNA-dependent RNA polymerase

Side effects: flatulence, abdominal pain, urgency to defecate

Ointment and cream

Use: Impetigo for Group A Strep or S. Aureus

Mechanism: Inhibits bacterial isoleucyl tRNA synthase

Use for impetigo

Topical Ointment

1st drug in a new class called pleuromutilins

Mechanism: blocks acceptor and donor sites for peptidyl transferase

prevetion and treatment of G+/- UTIs

Concentrates in renal tubules

Mechanism:  reduced by UT bacteria to reactive intermediates that damage DNA, cell wall, ribosomes, etc

Brown Urine

Pulmonary reactions reported  and may cause death

Cidal injectable lipopeptide for G+ and MRSA skin and systemic infections

Inactivated by pulmonary surfactant (not for pneumoniae)

Mechanism: depolarizes cytoplasmic membrane and inhibits DNA, RNA, & protein synthesis

Side Effects: increase creatanine kinase

excreted by kindeys unchanged

IV for life-threatening Plasmodium Falciparum

Can cause arythmias

penetrates tissues and biofilm well. Effective against most G+/- organisms (including staph & MRSA)

Mechanism: Inhibits DNA-dependent RNA polymerase

Kills intra and extra cellular

Penetrates through cavities and abscesses

Excreted mostly through bile (enterohepatic recirculation)

use for at least 2 weeks

Side effects

• red-orange color to urine, feces, sweat, tears
• rash, fever, naseua, vomitting
• jaundice (fatality rare)
• hepatitis (rare)