Tetracycline

Tetracycline- Pharmacology and popular brands

ParametersDetails
Category of DrugTetracycline is an Anti-Infective drug
Mechanism of Action 1Tetracycline 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.
IndicationsTetracycline is used as an antibiotic in
1. Rocky Mountain spotted fever
2. Typhus
3. Q fever
4. Rickettsiae pox
5. CK fever caused by Rickesiae
6. Respiratory tract infections caused by Mycoplasma pneumonia
7. Urethritis

Tetracycline is also used in ophthalmic conditions, like,
1. Superficial bacterial infection of the eye
2. Mass treatment of trachoma in endemic areas
3. Prophylaxis of neonatal conjunctivitis due to Neisseria
gonorrhea or Chlamydia trachomas.
StructureTetracycline.png
Molecular detailsFormula- C22H24N2O8
Molecular Weight- 444.4 g/mol
IUPAC Name(4S,4aS,5aS,6S,12aR)-4-(dimethylamino)-1,6,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4,4a,5,5a-tetrahydrotetracene-2-carboxamide
Well Known
Pharmaceutical Brands
 
Available dosage formsCapsules/Tablets/Ointments
(Store protected from light and moisture)
RPI Tetracycline Hydrochloride, 25 g Powder - 30UA78|T17000-25.0 - Grainger
Dose1. Adult- 250 mg or 500mg every 6 h, in severe infections.
2. Children- 25 to 50 mg/kg body weight, daily in
three divided doses. (do not use below 8 years.)
Contraindications1. Deposition of tetracyclines in growing bone and teeth
2. Doxycycline may be used in children for treatment and post-exposure prophylaxis of anthrax when an alternative antibacterial cannot be given
3. Hypersensitivity to the tetracycline group of antibiotics
Pharmacodynamic properties 21. short-acting antibiotic
2. binds to the 30S ribosomal subunit, and to some extent to the 50S ribosomal subunit.
3. Prevents the amino-acyl tRNA from binding to the A site of the ribosome.
4. May alter the cytoplasmic membrane of bacteria, causing leakage of intracellular contents, such as nucleotides, from the cell.
Pharmacokinetic properties1. Bioavailability is less than 40% (IM), 100% i(IV), and 60-80% (orally).
2. Food and/or milk reduce GI absorption of oral preparations by 50% or more.
3. Volume of distribution-NA
4. Protein binding- 20 – 67%
5. Metabolism- Not metabolized
6. Route of elimination excreted in the urine and feces (in a biologically active form.)
7. Half-life- 6-12 hours
8. Clearance-NA
Precautions1. Used with caution in patients with hepatic impairment or those receiving potentially hepatotoxic drugs.
2. Prolonged use may lead to overgrowth of non-susceptible organisms
2. Lactation
3. Pregnancy
Adverse Effects1. Nausea
2. Vomiting
3. Diarrhoea
4. Hepatotoxicity
5. Pancreatitis
6. Blood disorders
7. photosensitivity
8. Ophthalmic preparations may show- Rash, Stinging, Burning
Pregnancy Category D

References:

  1. tetracycline mechanism of action
  2. tetracycline molecular details

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