- Tetracyclines:
broad spectrum antibiotics: protein synthesis
inhibitors
Bacteriostatic: many
gram-positive and gram-negative bacteria including
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- chlamydiae
- mycoplasma
- some protozoa (amebas).
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- Antibacterial spectrum is similar
between tetracyclines although bacteria resistant
to tetracyclines may remain sensitive to
minocycline
Resistance:
Tetracyclines
- Most common mechanism for gram-negative bacterial resistance: insertion
of a plasmid-encoded active-efflux
pump that translocates tetracycline out
of the cell.
- Mechanisms for gram-positive bacterial resistance may be
either through this active efflux
mechanism or through changes in its
ribosomal target.
- Three mechanisms for
resistance:
- decreased
intracellular concentration by
decreased influx or increased
efflux
- decreased
tetracycline ribosomal binding
- enzymic
inactivation of tetracycline
Archer,G.L.
and Polk, R.E. Treatment and Prophylaxis
of Bacterial Infections, In Harrison's
Principles of Internal Medicine 14th
edition, (Isselbacher, K.J., Braunwald,
E., Wilson, J.D., Martin, J.B., Fauci,
A.S. and Kasper, D.L., eds) McGraw-Hill,
Inc (Health Professions Division), 1998,
p. 859. |
Chambers,
H.F., Chloramphenicol, Tetracyclines,
Macrolides, Clindamycin and
Streptogramins, in Basic and Clinical
Pharmacology,(Katzung, B. G., ed)
Appleton-Lange, 1998, p. 745. |
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- Classification: short-acting
(tetracycline (Achromycin), oxytetracycline,
chlortetracycline: 1/2 life: 6-12 h)
intermediate-acting (demeclocycline (Declomycin),
methacycline: 1/2 life 12 h) long-acting
(doxycycline (Vibramycin, Doryx), minocycline
(Minocin), 1/2 life: 16-18h).
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Clinical Use
A
tetracycline is the drug of choice for
treating these infections:
- Mycoplasma
pneumoniae
- chlamydiae
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- rickettsia
- some spirochetes.
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- Used in combination with
other drugs to treat gastric and duodenal
ulcer casue by Helicobacter pylori.
- May be used in a variety
of gram-positive and gram-negative
bacterial infections in the absence of
resistance.
- No longer recommended for
treatment of gonococcal disease due to
the emergence of resistant strains.
- Tetracyclines + aminoglycoside
for: plague tularemia and brucellosis.
May be used in treatment of protozoal
infections: Entamoeba histolytica
or Plasmodium falciparum
- Other uses: acne, bronchitis,
Lyme disease leptospirosis some
mycobacterial infections (nontuberculous)
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Adverse reactions
- GI: Nausea, vomiting--most
common
- Bone-Teeth: Tetracyclines
bind to calcium incorporated into newly
formed bone (young children) leading to
discoloration; in the case of
incorporation into bone, deformity or
growth inhibition may occur.
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