TETRACYCLINES

Rupshree Gupta
INTRODUCTION

1. Tetracyclins are bacteriostatic antimicrobials.

2. Exhibit activity against a wid range of microorganisms
including the gram positive and negative bacteria hence
they are a broad spectrum antibiotics
3. Due to the absence of major side effects has lead to their
extensive use in therapy of humans and animal infections.
4. Active against intracellular pathogen like
chlymdia,Rickettsia,Mycoplasma
 TETRACYCLINS
• i) The first member of the family was
chlortetracycline derived
• from the soil organism Streptomyces aureofaciens.
It was introduced by Benjamin M. Duggar in 1948
• ii) This was followed by oxytetracycline produced
from Streptomyces rimosus.
• iii) In 1952 by removing the chlorine atom from
chlortetracycline, tetracycline was produced.
• iv) mutant strains of Streptomyces aureofaciens They are so named for their four
led to discovery of demethyltetracyclin first (“tetra-”) hydrocarbon rings
member of demecocyclin (“-cycl-”) derivation (“-ine”)
CLASSIFICATION

Doxycycline and
• other tetracycline derivatives such as
minocycline exhibit
• anti-inflammatory effects along with in
vitro antiviral activity against several
RNA viruses. 20 Use of these agents
has been associated with clinical
improvement.
• reversal of cytokine storm in some
infections caused by
• RNA viruses, such as dengue fever.

• Doxycyclin can also be used to treat

mild to moderate acne as it has anti-
inflammatory properties and it can
kill the bacteria that causes
inflammation.
 MECHANISM OF ACTION

• Tetracyclines bind reversibly to the 16S rRNA

of the 30S on the A site
subunit and inhibit protein synthesis by blocking
the binding of aminoacyl tRNA to the A site on the
mRNA-ribosome complex. This action prevents
the addition of further amino
acids to the nascent peptide.
Gram positive-it enters via energy dependent
transport system and for the gram-negative it
enters via porin(outer membrane)and energy
dependent transport across cytoplasmic
membrane
ANTIBACTERIAL SPECTRUM
i) Tetracyclines have broad spectrum of
activity covers both gram
positive and gram negative bacteria,
Rickettsia, Traponema
pallidum, mycoplasmas, and Chlamydiae, etc.
They are primarily bacteriostatic.
• ii) Gram positive bacilli e.g. Clostridia,
Listeria, Corynebacteria,
• B. anthracis are inhibited.
• iii) Gram negative bacterias like H.ducreyi,
Calmmatobacterium granulomatis
V.cholerae. are sensitive to tetracyclines
Resistance develops in graded
manner.
ii) Bacteria acquire capacity to
pump out the tetracycline out of
the cell
iii) Acquire a plasmid mediated
synthesis of a protection protein
which protects the ribosomal
binding site from tetracycline.
iv) Nearly complete cross
resistance is seen among different
members of tetracycline
SIDE EFFECTS
• Liver damage
• Kidney damage only if there is pre
damage.
• Phototoxicity
• Diabetis insipidus(def of ADH and
vasopressin on posterior lobe of pitutary
gland)
• Deposition of tetracyclin chelate in teeth
and bones
ADMINISTRATION AND TOXICITY
• Mostly through oral route
but is also given in
intramuscular(oxytetracycli
n and tetracyclin) and
intravenous forms.

• High dose can lead to liver

failure and even
death,they are not
dialyzable
USES
• Empirical therapy
• ii) First choice drugs in:
Venereal diseases, Atypical
pneumonia,Cholera,
• Brucellosis, Plague, Relapsing
fever etc.
• iii) Second choice drugs in:
Tetanus, anthrax, lasteria,
patients allergic to new study shows that
methacycline, a
• penicillin etc. commonly used
• iv) Urinary tract infections, antibiotic, can reduce
the neurological
Amoebiasis , acne vulgaris. damage caused by
Zika virus infections in
mice.