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PROTEIN SYNTHESIS INHIBITORS Cheat Sheet by

pharmacology

TETRAC­YCLINES

Indications
Ricket­tsial infections (rocky mountain spotted fever), chlamydia, lyme disease, mycopl­asmal infect­ions, chronic severe acne, cholera, gastri­c/d­uodenal ulcer caused by H. pylori
PK
Excreted in bile, urine, breast milk, undergo entero­hepatic circul­ation
GI
GI, deposition of drug in bones and teeth, liver failure, photot­oxi­city, vertigo, avoid in pregnant

TETRAC­YCLINES

SHORT
CHLORTETRACYCLINE
 
TETRAC­YCLINE
 
OXYTETRACYCLINE
INTERM­EDIATE
DEMECLOCYCLINE
treats SIADH
 
METHAC­YCLINE
LONG
DOXYCY­CLINE
treat infections in pts with anuria (elimi­nates via bile, feces)
 
MINOCY­CLINE
achieves high CNS concen­tra­tions in the absence of inflam­mation, metabo­lized in liver

MACROL­IDE­S/K­ETO­LIDES

AZITHROMYCIN
show cross-­res­istance with erythr­omycin
longest t1/2

Adva­nta­ges: less GI distur­bances
CLARITHROMYCIN
show cross-­res­istance with erythr­omycin

Adva­nta­ge: lower incidence of GI distur­bances, less frequent dosing
ERYTHR­OMYCIN
MOA: Interferes with aminoacyl transl­oca­tion, preventing the transfer of the tRNA bound at the A site of the 50S rRNA complex to the P site of the rRNA complex

Destroyed by gastric acid and must be enteric coated
shortest t1/2
TELITH­ROMYCIN
Effective against macrol­ide­-re­sistant organisms

Indi­cat­ions: respir­atory tract infect­ions, including commun­ity­-ac­quired bacteria pneumonia, acute exacer­bations of chronic bronch­itis, sinusitis and strepto pharyn­gitis
Indi­cat­ions: community acquired pneumonia (mycop­lasma, legion­ella, chlamy­dia), pertussis, campyl­obacter jejuni gastro­ent­eritis, MAC (azalides)

PK: Well distri­buted, CNS penetr­ation limited except with inflam­mation.
Most of drug is concen­trated in the liver and excreted in the bile, some inacti­vated in the liver by demeth­yla­tion.

AE: GI, jaundice, ototox­icity

Bacter­ios­tatic, bacter­icidal at high doses
 

OTHERS

CLINDA­MYCIN
Indi­cat­ions: pencil­lin­-re­sistant anaerobic infections
Clinical use: SSTI
Phar­mac­olo­gy: high bone concen­tra­tions
Toxi­city: diarrhea, allergy, skin rashes, pseudo­mem­branous colitis caused by overgrowth of C. diff
CHLORAMPHENICOL
Indi­cat­ions: Ricket­tsiae (typhus and Rocky Mountain spotted fever); bacterial meningitis
Clinical use: eye infections
AE: GI distur­bances, gray baby syndrome, aplastic anemia
PEARL: Because of its toxicity and resist­ance, its use is restricted to life-t­hre­atening infections for which no altern­ative exists

STREPT­OGR­AMINS

QUINUP­RIS­TIN­-DA­LFO­PRISTIN
AE: venous irrita­tion, athralgia and myalgia, hyperb­ili­rub­inemia

OXAZOL­IDI­NONES

LINEZOLIDE
PK: completely absorbed, widely distri­buted throughout the body, excreted renally and non-re­nally
AE: GI upset

AMINOG­LYC­OSIDES

STREPTOMYCIN
2nd line agent for the treatment of tuberc­ulosis in combin­ation with other agents to prevent emergence of resistance
AE: vestibular distur­bances
GENTAMICIN
Intrat­hecal
Indi­cat­ions: mainly used in combo for severe infections (sepsis and pneumonia) caused by resistant strains of gram negative bacteria, infected burns/­wou­lds­/le­sions, prevention of catheter infections
GENT+B­-LACTAM
Synerg­istic effect against pseudo­monas, proteus, entero­bacter, klebsi­ella, serratia, stenot­rop­hom­onas, and other gram negative rods that are resistant to multiple antibi­otics
TOBRAMYCIN
Inhalation
Cautioned in pts with preexi­sting renal, vestibular or hearing disorders
STREPTO+PCN
Used for tuleremia and entero­coccal carditis
KANAMYCIN (topical only)
Kanamy­cin­-re­sistant strains may be cross-­res­istant to amikacin
AMIKACIN
Semisy­nthetic derivative of kanamycin, less toxic
Indi­cat­ions: tx microo­rga­nisms resistant to gentamicin and tobramycin
NEOMYCIN (topical only)
Indi­cat­ions: reduce the risk of infections during bowel surgery
SPECTI­NOMYCIN
Indi­cat­ions: altern­ative treatment for drug-r­esi­stant gonorrhea or gonorrhea in pcn-al­lergic pts
No cross-­res­istance with other drugs used in gonorrhea
AE: pain at injection site, fever, nausea
AE: Otot­oxi­city (rever­sible), neph­rot­oxi­city (rever­sible), neurom­uscular blockade

PK: Levels in most tissue are low. No CNS penetr­ation. High accumu­lation in renal cortex and lymph of inner ear. Excreted into the urine by glomerular filtra­tion. Accumu­lation occurs in patients with renal failure, not metabo­lized

Used against aerobic gram negative bacilli
Exhibit concen­tra­tio­n-d­epe­ndent killing
Postan­tib­iotic effect

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