Indication |
Used to treat bacterial infections such as Rocky Mountain spotted
fever, typhus fever, tick fevers, Q fever, rickettsialpox and
Brill-Zinsser disease. May be used to treat infections caused by
Chlamydiae spp., B. burgdorferi (Lyme disease), and upper respiratory
infections caused by typical (S. pneumoniae, H. influenzae, and M.
catarrhalis) and atypical organisms (C. pneumoniae, M. pneumoniae, L.
pneumophila). May also be used to treat acne. Tetracycline may be an
alternative drug for people who are allergic to penicillin. |
Pharmacodynamics |
Tetracycline is a short-acting antibiotic that inhibits
bacterial growth by inhibiting translation. It binds to the 30S
ribosomal subunit and prevents the amino-acyl tRNA from binding to the A
site of the ribosome. It also binds to some extent to the 50S ribosomal
subunit. This binding is reversible in nature. Additionally
tetracycline may alter the cytoplasmic membrane of bacteria causing
leakage of intracellular contents, such as nucleotides, from the cell. |
Mechanism of action |
Tetracycline passively diffuses through porin channels in the
bacterial membrane and reversibly binds to the 30S ribosomal subunit,
preventing binding of tRNA to the mRNA-ribosome complex, and thus
interfering with protein synthesis. |
Absorption |
Bioavailability is less than 40% when administered via
intramuscular injection, 100% intravenously, and 60-80% orally (fasting
adults). Food and/or milk reduce GI absorption of oral preparations of
tetracycline by 50% or more. |
Volume of distribution |
Not Available |
Protein binding |
20 - 67% protein bound |
Metabolism |
Not metabolized |
Route of elimination |
They are concentrated by the liver in the bile and excreted in the
urine and feces at high concentrations in a biologically active form. |
Half life |
6-12 hours |
Clearance |
Not Available |
Toxicity |
LD50=808mg/kg (orally in mice) |