Tetracycline Capsule 250 mg

Tetracycline Capsule 250 mg

Category :

Antibacterial , antiprotozoal, antiacne agent , antimalarial . ( USP DI 2001)

Composition :

Each Capsule Contains 250 mg of Tetracycline hydrochloride .

Chemistry :

4 – ( dimethylamino ) – 1 , 4 , 4a, 5 , 5a , 6 – 11 , 12a – octahydro – 3 , 6 , 10 , 12 , 12a – Pentahydroxy – 6 – methyl – 1 , 11 – dioxo – 2 – naphthacenecarboxamide. C22 H25CLN 2O2 Molecular weight : 480 . 93 . ( Merck Index 1996 ).

Mechanism of Action :

The Tetracycline is primarily bacteriostatic and is thought to exert their antimicrobial effect by the inhibition of protein synthesis. Tetracycline is active against a wide range of gram – negative and gram – positive organisms. The drugs in the Tetracycline class have closely similar antimicrobial spectra, and cross – resistance among them is common . ( PDR 2002 )

Pharmacokinetics :

Tetracycline is readily absorbed and is bound to plasma proteins in varying degrees . It is concentrated by the liver in the bile and excreted in the urine and feces at high concentrations and in a biologically active form . (PDR 2002 )

Absorption :

Tetracycline Absorbed orally (%) = 75 – 77 Effect of food on absorption= decreased

Distribution :

Readily distributed to most body fluids , including bile, sinus secretions , and synovial, pleural , ascitic and gingival crevicular fluids. Tetracyclines tend to localize in bone, liver, spleen , tumors, and teeth . Tetracyclines also cross the placenta and distribute in to breast milk.

Time to peak concentration :

2-3 days may be necessary to achieve therapeutic concentrations of Tetracycline . (USPDI 2001 )

Indications :

- Tetracycline is indicated as adjunctive treatments for acne.
- Systemic Tetracycline is indicated in the treatment of actinomycosis in patients who cannot take Penicillins.
- Tetracycline is indicated as treatment adjuncts for acute intestinal amebiasis.
- Systemic Tetracycline is indicated in the treatment of anthrax who cannot take Penicillins .
- Systemic Tetracycline is indicated for the treatment of bartonellosis caused by Bartonella bacilliformis .
- Systemic Tetracycline, in conjunction with streptomycin, are indicated in the treatment of brucellosis.
- Systemic Tetracycline is indicated in the treatment of chancroid caused by Haemophilus ducreyi.
- Oral Tetracycline is indicated in the treatment of cholera caused by Vibrio cholerae.
- Oral Tetracycline is indicated in the treatment of inclusion conjunctivitis caused by Chlamydia trachomatis .
- Systemic Tetracycline is indicated in the treatment of genitourinary tract infections.
- Systemic Tetracycline is indicated for the treatment of uncomplicated gonorrhea caused by Neisseria gonorrhoeae in patients who cannot take Penicillins.
- Systemic Tetracycline is indicated in treatment of listeriosis caused by Listeria monocytogenes in patients who cannot take Penicilins .
- Systemic Tetracycline is indicated in the treatment of Lymphogranuloma venereum caused by Chlamydia sp.
- Systemic Tetracycline is indicated in the treatment of plague caused by yersinia pestis.
- Systemic Tetracycline is indicated in the treatment of pneumonia caused by Mycoplamsa pneumoniae.
- Systemic Tetracycline is indicated in the treatment of respiratory tract infections caused by susceptible strains of Haemophilus influenzae and kelbsiella sp.
- Sysemic Tetracycline is indicated in the teatment of skin and soft tissue infections .
- Oral Tetracycline is indicated in the treatment of syphilis caused by Treponella pallidum.
- Systemic Tetracycline is indicated in the treatment of trachoma.
- Systemic Tetracycline is indicated in the treatment of urinary tract infection caused by Klebsiella species.
- Systemic Tetracycline is indicated in the treatment of chlamydial infections . (USPDI 2001 )

Contraindications :

This drug is contraindicated in persons who have shown hypersensitivity to any of the Tetracyclines . (PDR 2002 )

Warnings :

The use of Tetracycline during tooth development ( last half of pregnancy, infancy and childhood to the age of 8 years ) may cause permanent discoloration of the teeth. Tetracycline ,therefore, should be used in this age group unless other drugs are not likely to be effective or are contraindicated. If renal impairment exists, usual oral doses may lead to excessive systemic accumulation of the drug and possible liver toxicity. Under such conditions lower than usual total doses are indicated. Photosensitivity manifested by an exaggerated sunburn reaction has been observed in some individuals taking Tetracycline . (PDR 2002)

Pregnancy :

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. FDA pregnancy Category D. ( USPDI 2001 )

Breast- feeding :

Tetracycline is distributed into breast milk , 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. (USPDI 2001 ) .

Precautions :

Pseudotumor cerebri in adults has been associated with the use of Tetracycline. The usual clinical manifestations are headache and blurred vision. Bulging fontanels have been associated with the use of Tetracycline in infants . As with other antibiotics preparations, use of this drug may result in overgrow of nonsusceptible organisms , including fungi . If superinfection occurs, the antibiotic should be discontinued and appropriate therapy should be instituted. In venereal diseases when coexistent syphilis is suspected, dark field examination should be done befor treatment is started and blood serology repeated monthly for at least 4 months . All infections due to group A beta – hemolytic streptococci should be treated for at least ten days . (PDR 2002)

Drug Interactions :

Concurrent use of Tetracycline with oral contraceptives may render oral contraceptives less effective. Since bacteriostatic drugs, such as the Tetracycline may interfere with bactericidal action of Penicillins, it is not advisable to administer these drugs concomitantly. Patients who are on anticoagulant therapy may require down ward adjustment their anticoagulant dosage because of Tetracycline effecting to depress plasma prothrombin activity . (PDR 2002 )

Adverse Reactions :

1 - Gastrointestinal : Anorexia , nausea, vomiting, diarrhea, glossitis , dysphagia, enterocolitis , pancreatitis . In creases in liver enzymes have been reported rarly. Rare instances of esophagitis and esophageal ulceration have been reported in Patients took the medication immediately before going to bed.
2- Skin: Rashes, exfoliative dermatitis is uncommon. Photosensitivity is discussed above . (See warnings )
3 - Renal toxicity : Rise in BUN is apparently dose related.
4- Hypersensitivity reaction: Urticaria , angioneurotic edema, anaphylaxis and exacerbation of systemic lupus erythematosus.
5- Blood : Hemolytic anemia, thrombocytopenia, neutropenia and eosinophily have been reported.
6- CNS : Pseudotumor cerebri ( benign intracranial hypertension ) in adults and bulging fontanels in infants . Dizziness, tinnitus, and visual disturbances have been reported.
7- Other : When given over prolonged periods , Tetracycline has been reported to produce brown – black microscopic discoloration of thyroid glands . No abonormalitis of thyroid function studies are known to occur. (PDR 2002 )

Dosage and Administration :

Usual adult prescribing limits :

4 grams daily .

Usual pediatric dose :

For all infections : Children older than 8 years of age : Oral , 6.25 to 12.5 mg per kg of body weight every six hours, or 12.5 to 25 mg per kg of body weight every twelve hours. For Lyme disease : Children older than 8 years of age : Oral , 6.25 to 12.5 mg per kg of body weight four times a day. (USP DI 2001 )

Storage :

Store below 40ºC , in a tight , light – resistant container . (USPDI 2001 )

How Supplied :

Tetracycline hydrochloride 250 mg is available as two – piece ,hard shell , opaque capsules with red cap and yellow body in boxes of 100 . There are 10 blisters of 10’s in a box of 100’s. 82-2-16-2