| |
|
| TETRACYCLINE-HAKIM |
| :: Antibacterial, antiprotozoal, Antiacne agent (Systemic, topical) :: |
|
 Cap. 250 mg |
| Top. ointment 3% |
|
|
|
|
|
|
|
Pharmacologic category
Antibacterial (systemic , topical) ; Antiprotozoal (systemic) ; Antiacne agent (systemic)
Mechanism of action
Antibacterial (systemic , topical) ; Antiprotozoal –Tetracycline is broad – spectrum bacteriostatic agent that acts by inhibiting protein synthesis by blocking the binding of aminoacyl – tRNA (transfer RNA ) to the mRNA (messenger RNA ) – ribosome complex . Reversible binding occurs primarily at the 30 S ribosomal subunit of susceptible organisms . Bacterial cell wall synthesis is not inhibited .
Antiacne agent (topical) –Topical tetracycline is thought to suppress the growth of Propionibacterium acnes (Corynebacterium acnes) , an anaerobe found in sebaceous glands and follicles . P. acnes produces proteases , hyaluronidases, lipases , and chemotactic factors , all of which can produce inflammatory components or inflammation directly.
Indications
Systemic tetracycline – Acne vulgaris (treatment adjunct); Actinomycosis ; Intestinal amebiasis (treatment adjunct) ; Anthrax ; Bartonellosis ; Brucellosis ; Chancroid ; Cholera ; Inclusion conjunctivitis ; Genitourinary tract infections ; Necrotizing ulcerative gingivostomatitis ; Gonorrhea ; Granuloma inguinale ; Listeriosis ; Lymphogranuloma venereum ; Plague ; Mycoplasmal pneumonia ; Psittacosis ; Q fever ; Rickettsial pox ; Rocky Mountain spotted fever ; Typhus infections ; Relapsing fever; Respiratory tract infections ; Skin and soft tissue infections ; Syphilis ; Trachoma ; Tularemia ; Urinary tract infections ; Yaws ; Extraintestinal amebiasis ; Gonococcal arthritis ; Chlamydial infections ; Lyme disease ; Malaria ; Ocular rosacea
Topical tetracycline (ointment) – Minor bacterial skin infections (treatment and prophylaxis) ; Dermal ulcer (treatment)
Side/Adverse effects
Systemic tetracycline – Staining of infant’s or children’s teeth ; Photosensitivity ; Nephrogenic diabetes insipidus ; Pigmentation of skin and mucous membranes ; Benign intracranial hypertension (anorexia , bulging fontanel in infants , headache , papilledema , visual changes , vomiting) ; Pancreatitis ; Dizziness ; Cramps or burning of the stomach ; Diarrhea ; Nausea or vomiting ; Fungal overgrowth (itching of the rectal or genital areas , sore mouth or tongue) ; Hypertrophy of the papilla (darkened or discolored tongue)
Topical tetracycline – pain , redness , swelling , or other sign of irritation not present before therapy
Contraindications
Hypersensitivity to tetracycline or any component of the formulation ; Do not administer to children < or = 8 years of age ; Pregnancy
Warnings / Precautions
Use with caution in patients with renal or hepatic impairment ; Use protective measure to avoid photosensitivity
Pregnancy
FDA pregnancy category D. Tetracycline crosses the placenta ; use is not recommended during the last half of pregnancy since tetracycline may cause permanent discoloration of teeth , enamel hypoplasia , and inhibition of skeletal growth in the fetus.
Breast–Feeding
Tetracycline is distributed into breast milk ; although tetracycline may form nonabsorbable complexes with breast – milk calcium , use is not recommended because of the possibility of their causing permanent staining of teeth , enamel hypoplasia , inhibition of linear skeletal growth , photosensitivity reactions , and oral and vaginal thrush in infants.
Drug Interactions
Systemic tetracycline – Concurrent use with antacids , calcium supplements such as calcium carbonate , choline and magnesium salicylates , iron supplements , magnesium salicylates , magnesium – containing laxatives and sodium bicarbonate may result in formation of nonabsorbable complexes ; also , concurrent use with antacids or sodium bicarbonate may result in decreased absorption of tetracycline because of increased intragastric pH ; patients should be advised not to take these medications within 1 to 3 hours of oral tetracycline . Concurrent use with cholestyramine or colestipol may result in binding of oral tetracycline , thus impairing their absorption ; an interval of several hours between administration of cholestyramine or colestipol and oral tetracycline is recommended . Concurrent long – term use of oral estrogen – containing contraceptives with tetracycline may result in reduced contraceptive reliability and increased incidence of breakthrough bleeding . Although no cases of clinical toxicity have been reported , concurrent use of oral tetracycline with digoxin may increase serum digoxin concentrations in some individuals . Concurrent use with tetracycline may increase the potential for nephrotoxicity of methoxyflurane . Since bacteriostatic drugs may interfere with the bactericidal effects of penicillins in the treatment of meningitis or in other situations where a rapid bactericidal effect is necessary, concurrent therapy of penicillins with tetracycline is not recommended. Concurrent use of vitamin A with tetracycline has been reported to cause benign intracranial hypertension . Aminoglutethimide , carbamazepine , nafcillin , phenobarbital , phenytoin , and rifamycins may decrease the levels/effects of tetracycline . Tetracycline may increase the levels/effects of benzodiazepines , calcium channel blockers , cyclosporine , sildenafil , tacrolimus , and venlafaxine . Warfarin with tetracycline may result in increased anticoagulation.
Topical tetracycline – Combinations containing any of the following medications , depending on the amount present , may interact with this medication : Abrasive or medicated soaps or cleaners; Other topical acne preparations ; Topical alcohol – containing preparations , such as after – shave lotions , astringents , perfumed toiletries , or shaving creams or lotions ; Cosmetics or soaps with a strong drying, effect ; Isotretinoin ; Medicated cosmetics or “cover – ups” ; Preparations containing topical peeling agents, such as benzoyl peroxide , resorcinol , salicylic acid , or sulfur. Concurrent use with topical tetracycline may cause a cumulative irritant or drying effect , especially with the application of peeling , desquamating , or abrasive agents , resulting in excessive irritation of the skin.
Monitoring Parameters
Renal , hepatic , and hematologic function test , temperature , WBC , cultures and sensitivity , appetite , mental status
Dietary Considerations
Tetracycline serum concentrations may be decreased if taken with dairy products.
Administration and dosage
Systemic tetracycline:
-
Usual adult and adolescent dose:
Antiacne agent – Oral , 500 mg to 2 grams per day in divided doses initially , as adjunctive therapy , in moderate to severe cases . When improvement is noted (usually after three weeks) , dosage should be reduced gradually to maintenance dose of 125 mg to 1 gram per day . Adequate remission of lesions may also be possible with alternate – day or intermittent therapy.
Brucellosis – Oral , 500 mg 4 times a day for 3 weeks , in combination with IM streptomycin 1 gram two times a day for the first week and 1 gram once a day for the second week .
Gonorrhea – Oral , 1.5 grams initially , then 500 mg every 6 hours for four days , for a total dose of 9 grams.
Lyme disease – Oral , 250 to 500 mg four times a day .
Syphilis – Oral , 30-40 grams over a period of 10 to 15 days.
Uncomplicated endocervical , rectal , or urethral infections caused by Chlamydia trachomatis – Oral, 500 mg 4 times a day for at least 7 days .
For all other infections: Oral , 250-500 mg every 6 hours ; or 500 mg to 1 gram every 12 hours.
- Usual adult prescribing limits: 4 grams daily.
-
Usual pediatric dose:
Lyme disease – Children older than 8 years of age : Oral , 6.25 to 12.5 mg per kg of body weight 4 times a day.
For all other infections: Children older than 8 years of age : Oral , 6.25 to 12.5 mg per kg of body weight every 6 hours ; or 12.5 to 25 mg per kg of body weight every 12 hours.
Topical tetracycline: Antibacterial –Topical , to the skin , one or two times a day.
How Supplied
- Capsule 250 mg
- Topical Ointment, 15 gram, contains 3% tetracycline hydrochloride
Storage
- Capsule, store below 30°C. Protect from light and moisture.
- Topical Ointment, Store below 30°C.
References
- USP DI, 2004
- Up To Date, Vol. 13.1 (2005)
- Martindale, The Complete Drug Reference, 33 rd edition 2002
|
