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Tetracyclines slide contains full information about uses, adverse effect, marketed preparation, precaution, route of drug administration, antimicrobial spectrum, mechanism of action, pharmacokineticks and pharmacodynamics of tetracyclines. This slide is very helpful for pharmacy and pharmacology student for the study about tetracyclines.

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  1. 1. Abdul Waheed M pharm-Pharmacology Department of pharmacology Amity University, Noida 1
  2. 2. INTRODUCTION • Obtained from soil actinimycetes. • Introduced in 1948 by Benjamin Minge Duggar (chlortetracycline, aureomycin). • Tetracyclines is broad spectrum antibiotic having four cyclic ring nucleus. • All tetracyclines are slightly bitter solids, weakly water soluble, their hydrochlorides are more soluble. • Aqueous solutions are unstable. 2
  3. 3. • Tetracyclines available in India for clinical use:- Tetracycline, Oxytetracycline, Demeclocycline, Doxycycline, Minocycline. 3
  4. 4. MECHANISM OF ACTION • Tetracyclines are primarily bacteriostatic. • Inhibit protein synthesis by binding to 30s ribosome in susceptable organism. • Inhibit binding of aminoacyl tRNA to the acceptor site of mRNA peptide chain fails to grow. 4
  5. 5. TRANSPORT OF TETRACYCLINES • Sensitive organism have active transport process which concentrate tetracyclines intracellularly. • In gram negative bacteria tetracyclines diffuse through “Porin” channel. • Some lipid soluble member (Doxycycline and Minocycline) enter by passive diffusion. 5
  6. 6. ANTIMICROBIAL SPECTRUM • Inhibit all type of pathogen except Fungi and Viruses. • Cocci: All gram positive and gram negative cocci were originally sensitive but Strep. pyogenes, Staph. aureus and enterococci have become resistant. • Sensitive gram positive bacilli: Clostridia and other anaerobes, Listeria, Corynebacteria, B. anthracis are inhibited but not Mycobacteria. • Sensitive gram nagetive bacilli: H. ducreyi, H. pylori, Yersinia pestis, Y. enterocolitica, and many anaerobes. H.influenzae have become insensitive. • All rickettsiae and chlamydiae are highly sensitive. • Mycoplasma & Actinomyces are moderately sensitive. • E. histolytica & Plasmodia are inhibited at high concentration 6
  7. 7. RESISTANCE • Tetracyclines concentrating mechanism become less effective. • Bacteria acquire capacity to pump tetracyclines out. • Plasmid mediated synthesis of a “Protection” protein which protects the ribosomal binding site from tetracyclines. 7
  8. 8. PHARMACOKINETICS • Incompletely absorbed by g.i.t. • Absorption is better if taken in empty stomach. • Doxycycline & Minocycline are completely absorbed irrespective of food. • Tetracyclines have chelating property with calcium and other metals forms insoluble and unabsorbable complexes. • Milk, iron preparation, nonsystemic antacids and sucralfate reduces their absorption. • Concentrated in liver and spleen and bind to the connective tissue in bone and teeth. 8
  9. 9. Continue… • Widely distributed in body • Variable degree of protein binding: high (Demeclocycline, Doxycycline, & Minocycline,) moderate (tetracycline) low (Oxytetracycline) • Primarily excreted in urine by glomerular filtration. • They are secreted in milk and affect the infant. 9
  10. 10. ADMINISTRATION • Most commonly used dosage form- Oral capsule. • The capsule should be taken 1/2hr before or 2hr after food . • Tetracyclines are not recommended by i.m. route. (painful & poor absorption). • i.v. injection may be given in sever cases. • Topical preparation are available but should not be used because of high risk of sensitization. 10
  11. 11. ADVERSE EFFECT • Epigastric pain, nausea, vomiting and diarrhoea by their irritant property. • Liver damage and jaundice occurs occasionally. • All Tetracyclines except Doxycycline accumulate and enhance renal failure. • Tetracyclines have chelating property and affect the teeth and bones. • Reduces protein synthesis and induces negative nitrogen balances increase blood urea. 11
  12. 12. PRECAUTION • Should not be used during pregnancy, lactation and in children. • Should be avoided in patients on diuretics increases blood urea. • Do not mix injectable Tetracyclines with Penicillin causes inactivation. • Do not inject Tetracyclines intrathecally. 12
  13. 13. USE • Broad spectrum antibiotics • Atypical pneumonia • Cholera • Brucellosis • Plague • Rickettsial infection 13
  14. 14. PREPARATIONS • TERRAMYCIN 250, 500 mg cap, 50 mg/ml in 10 ml vial inj. • ACHROMYCIN, HOSTACYCLINE, RESTECLIN 250, 500 mg cap. • LEDERMYCIN 150, 300 mg cap/tab. • TETRADOX, NOVADOX 100 mg cap. • CYANOMYCIN 50, 100 mg cap. 14
  15. 15. Reference • Tripathi KD, Essentials of Medical Pharmacology, Jaypee Publishers, New Delhi. • Sharma HL, Sharma KK, Principles of Pharmacology, Paras Medical Publishers, New Delhi 15
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