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Chemical
name2 -
Naphthacenecarboxamide, 4 - (dimethylamino) - 1, 4, 4a, 5, 5a, 6, 11, 12a
- octahydro - 3, 6, 10, 12, 12a, pentahydroxy - 6 - methyl - 1, 11 - dioxo
-, monohydro chloride, [4S - (4α, 4aα, 5aα, 6β, 12aα)] .
CategoryAntibacterial (systemic, topical);
antiprotozoal (systemic), antiacne agent (systemic, topical).
Mechanism of
action
Antibacterial (systemic, topical); antiprotozoal -
Tetracyclines are broad - spectrum bacteriostatic agents and act by
inhibiting protein synthesis by blocking the binding of aminoacyl
tRNA(transfer RNA) to the mRNA(messenger RNA) ribosome
complex. Antiacne agent (topical) - probably due to their antibacterial
activity. Topical tetracyclines are thought to suppress the growth of
propionibacterium acnes, an anaerobe found in sebaceous glands and
follicles. P. acnes produces proteases hyaluronidases, lipases, and
chemotactic factors, alI of which can produce inflammatory components or
inflammation directly.
Indications
Systemic tetracyclines are indicated in the treatment
of: Acne vulgaris - actinomycosis - anthrax - bronchitis - brucellosis
(concurrently with streptomycin) - conjunctivitis, inclusion -
genitourinary tract infections - gingivostomatitis, necrotizing ulcerative
- lymphogranuloma venereum - otitis media - pharyngitis, bacterial -
pneumonia and sinusitis - psittacosis - Q fever - rickettsial pox - rocky
mountain spotted fever - typhus infections - relapsing fever - skin and
soft tissue infections - syphilis - trachoma - urinary tract infections,
bacterial - amebiasis, extraintestinal - malaria - yaws. Topical
tetracyclines are indicated in the treatment of: Ance vulgaris - Skin
infections and dermal ulcer.
Precautions to
consider
Cross - sensitivity and / or related problems: patients
hypersensitive to one tetracycline may be hypersensitive to other
tetracyclines also. Use of systemic tetracyclines during pregnancy or
in infant and children up to 8 years of age, may cause permanent
discoloration of teeth, enamel hypoplasia.
Pregnancy / Breast -
feeding
Tetracyclines cross the placenta. They should not be used
during the last half of pregnancy. Tetracyclines are distributed into
breast milk and use is not recommended during breast - feeding.
Drug
interactions
Combinations containing any of the following medications,
depending on the amount present, may interact with this
medication: Antacids, calcium supplements such as calcium carbonate,
choline and magnesium salicylates, iron supplements, magnesium containing
laxatives, sodium bicarbonate, cholestyramine, cloestipol, contraceptives
(estrogen containing). Tetracyclines may interfere with the
bactericidal effect of penicillins in the treatment of meningitis or when
a rapid bactericidal effect is necessary, it is best to avoid concurrent
therapy. Topical tetracyclines may interact with these
medications: Abrasive or medicated soaps or cleansers - Acne
preparations, topical - Alcohol containing preparations, topical such as
after - shave lotions - Cosmetics - Isotretinoin - peeling agents.
Side / Adverse
effects
Those indicating need for medical attention; Incidence
more frequent: Discoloration of infant's or children's teeth,
photosensitivity. Incidence rare: Benign intracranial hypertension,
hepatotoxicity, pancreatitis. Topical tetracyclines; Those indicating
need for medical attention: pain, redness, swelling, or other sign of
irritation not present before therapy.
Administration and
dosage
Capsules, usual adults and adolescent dose: Antibacterial
(systemic); Antiprotozoal - Oral, 250 to 500 mg every 6 hours; or 500 mg
to 1 gram every 12 hours. Antiacne agent (systemic) - Oral, 500 mg to 2
grams daily in divided doses initially in moderate to severe cases as
adjunctive therapy. When improvement is noted (usually after 3 weeks),
dosage should be reduced gradually to a maintenance dose of 125 to 1000 mg
daily. Gonorrhea - Oral, 500 mg every 6 hours for 5 days. Syphilis -
Oral, 500 mg every 6 hours for 15 days (early syphilis) or for 1 month
(late syphilis). Usual adult prescribing limits: Up to 4 grams
daily. Usual pediatric dose - Children 8 years of age and
over: Oral, 6.25 - 12.5 mg per kg of body weight every 6 hours; 12.5 -
25 mg per kg every 12 hours. Topical ointment: To the skin, one or two
times a day.
How
suppliedBox of 100
capsules. Each capsule contains 250 mg tetracycline hydrochloride.
StorageCapsules: Store below 30° C, protect from
light and moisture. Topical ointment: Store below 30° C.
References1 - USP DI (1997) Vol: 1 -Pages: 2809
-2820. 2 - Drug facts and comparisons (1994). 3 - USP 23 page: 1510.
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