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Wesley mugambi
Tetracyclines:
-a broad-spectrum antibiotics. -It is commonly used to treat acne, infection, and other infections caused by bacteria. -The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
5-methacycline
6-rolitetracycline
Retention of the configuration of the asymmetric centres C-4, C-4a and C-12a is essential, whereas the configurations at C-5, C-5a and C-6 may be altered: 1- The amide hydrogen may be replaced with a methyl group, but larger groups have a deleterious effect except for those which are eliIminated spontaneously in water .
2-The dimethyl amino group may be replaced by a primary amino group without loss of in vitro activity but all other changes so far lead to decreased bacteriostatic action .
The hydrophobic part of the molecule from C-5 to C-9 may be altered in various ways: modifications at C-6 and C-7 in particular afford products having greater chemical stability. increased antibiotic activity and more favourable pharmacokinetics
Dehydrogenation to form a double bond between C-5a and C-11a markedly decreases activity Polar substituents at C-5 and C-6 contribute decreased lipid versus water solubility to the tetracycline
. The drugs are amphoteric, meaning they will form salts with both strong acids and bases. Thus, they may exist as salts of sodium or chloride.
Spectrum:
-The tetracyclines are broad-spectrum antibiotics. -They are active against the following microorganisms: 1_ gram-positive and gram-negative bacteria 2_ spirochetes 3_ mycoplasmas, 4_ rickettsiae, 6_ Candida albicans
7_Mycoplasma pneumoniae 8_Chlamydia trachomatis 9_Borrelia recurrentis. 10_Yersinia pestis 11_Vibrio cholerae 12_ Campylabacter fetus 13_Brucella specie 14_Streptococcus pneumoniee. 15_Neisserie gonorrhoeae
Mechanism of action:
Mechanism of resistance :
There are three types of tetracycline resistance: 1)tetracycline efflux.
Types of tetracyclines:
1-Demeclocycline:
Uses:
-treat cancer patients with SIADH. -treat hyponatremia. -combined with hydrocortisone in a paste used by dentists . -treat trachoma.
Side effect:
Dermatological:-Skin reactions, photosensitivity GIT:-nausea, vomiting, and diarrhea. CNS:-Dizziness,visualdisturbances . Immune System:-allergic reactions.
Pharmacodynamics/Kinetics:
-Absorption: ~50% to 80%. -Protein binding: 41% to 50% -Metabolism: Hepatic. -Half-life elimination: 10-17 hours
2-Chlortetracycline:
Uses: -used as antibacterial and antiprotozoal agent. -In veterinary medicine, it is commonly used to treat conjunctivitis in cats.
3-Oxytetracycline:
Uses: -treat Spirochaetal infection. -treating Non-Specific-Urethritis. -treating Clostridial wound infection and Anthrax.
Side effects:
-Local irritation after intramuscular injection. -Gastrointestinal:-anorexia, nausea, vomiting.
-Renal toxicity.
-Hypersensitivity reactions: Urticaria. -Blood: Hemolytic anemia, thrombocytopenia, neutropenia
1-tetracycline:
Uses: -Tetracycline's primary use is for the treatment of acne vulgaris and rosacea. -It is also used to treat a very wide range of infections.
Side effects:
-Gastrointestinal: anorexia, nausea, vomiting, diarrhea, -Skin: rashes, dermatitis. -Renal Toxicity -Hepatic Cholestasis: -Hypersensitivity Reactions:Anaphylaxis, Miscellaneous: Dizziness and headache
4- Minocycline:
Uses: -typhus fever and Q fever. -Psittacosis Trachoma -Nongonococcal urethritis. -Brucellosis.
Side effects:
-Hypersensitivity reactions:Urticaria,anaphylaxis. -GI :Anorexia, nausea, vomiting, diarrhea. -Hepatic toxicity: Hyperbilirubinemia. -Respiratory:Cough, dyspnea. -Blood:Agranulocytosis, hemolytic anemia.
Pharmacokinetics:
-rapidly absorbed from the GIT. -The peak plasma concentrations slightly decreased. -serum half-life ranged from 11 to 16 hours in hepatic dysfunction, and from 18 to 69 hours with renal dysfunction.
5-doxycyclines
Side Effects:
-Nausea, Vomiting,Diarrhea. -photosensitivity, rash. -dyspepsia -dysphagia.
-Watery diarrhea
-Bloody stools
Because tetracyclines have been shown to depress plasma prothrombin activity, patients who are on anticoagulant therapy may require downward adjustment of their anticoagulant dosage. interfere with the bactericidal action of penicillin, it is advisable to avoid giving tetracycline-class drugs in conjunction with penicillin.
bacteriostatic drugs
oral contraceptives
Concurrent use of tetracyclines with oral contraceptives may render oral contraceptives less effective. Increased risk of ergotism
ergot alkaloids or their derivatives are given with tetracyclines. Bile acid sequestrants
Iron preparations
Methotrexate:
when concurrent with tetracycline) may cause fatal nephrotoxicity; concurrent use is contraindicated. Clearance of methotrexate (highdose therapy) may be decreased by tetracyclines.
Minocycline
Minocin
Oxytetracycline
Terramycin
Tetracycline