PACKAGE LEAFLET TETRACYCLIN capsules Tetracycline

COMPOSITION Capsules containing tetracycline hydrochloride equivalent to 250 mg tetracycline. PROPERTIES AND ANTIMICROBIAL SPECTRUM Tetracyclin is a wide-spectrum bacteriostatic antibiotic (also bactericidal in high doses), belonging to the group of tetracyclines with high activity against extraand intracellularly multiplying microorganisms. Tetracyclin suppresses the protein synthesis in the bacterial cell by inhibition of 30 S - ribosomal subunit binding to aminoacyl tRNA. The antimicrobial spectrum of the antibiotic includes causatives of severe and particularly dangerous infections - Brucella sp., Pasteurella sp., Chlamydia, Mycoplasma sp., Rickettsia, Treponema, Spirocheta, Vibrio cholerae, Vibrio comma, Vibrio fetus, Leptospira, Protozoa (Plasmodium falciparum, Entamoeba histolytica, Balantidium coli), Bartonella baciliformis, Borrelia baciliformis, Borrelia burgdorferi. gram-positive microorganisms - Staphylococcus sp. (infections of the skin and soft tissues), Streptococcus sp., Corynebacterium acne, Listeria sp.; gram-negative microorganisms - Escherichia coli, Salmonella typhi, Shigella, Bacteroides sp., Fusobacterium, Acinetobacter sp., Legionella pneumophilia, Moraxella

catarrhalis,

Bordetella

pertusis,

Haemophilus

influenzae,

Haemophilus ducreyi, Coxiella sp. Laboratory sensitivity test is recommended 1

to determine the susceptibility of the causative microorganism prior to the initiation of treatment, since many strains of these groups of bacteria have been shown to be resistant to the antibiotic. PHAMACOKINETICS Following oral administration up to 60% of the Tetracyclin dose is absorbed from the gastrointestinal tract. Food interferes considerably with the antibiotic’s absorption. Peak plasma concentration is attained within 1-3 hours after oral administration, 3-4 h after intramuscular administration and 0.5 h after intravenous administration. Tetracyclin binds to the plasma proteins to the extent of between 24% and 65%. The drug’s plasma half-life is about 6-10 h, but becomes many-fold increased in case of renal insufficiency. The antibiotic penetrates well in the body tissues and fluids. It is to be found in significant concentrations in the lungs, prostate, gall bladder, tumor tissues. Tetracyclin deposits in the bones and teeth. The antibiotic hardly penetrates the blood-brain barrier in case of healthy meninges, but in presence of inflammatory process may attain therapeutic concentrations in the liquor. It passes transplacentally from mother into fetus.The concentrations of the antibiotic found in the breast-milk amount to 60% of the plasma concentrations. After oral administration significant percentage of the antibiotic (20-30%) is excreted by the bile (up to 20 times higher than the plasma concentration) and up to 50% is excreted with the urine by glomerular filtration. The excretion with the urine is increased in case of urine alkalization. INDICATIONS Tetracyclin is a drug of choice in the treatment of the so called particularly dangerous infections: Q-fever, Rocky Mountain spotted fever, ornithosis actinomycosis, rickettsialpox, tick fever, tularemia, plaque, cholera, brucellosis, dysentery, balantidiasis, mycoplasma pneumonia. The antibiotic

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is suitable for the treatment of severe cases of acne, as well as uncomplicated gonorrhoea, granuloma inguinale. Tetracyclin is used for the treatment of infections caused by Tetracyclin - susceptible microorganisms in the following cases: respiratory tract infections, urogenital infections, biliary infections, infections

of

the

skin

and

soft

tissues,

ophthalmic

and

otorhinolaryngological infections. In case of contraindicated penicillin administration, Tetracyclin is the alternative treatment for infections caused Neisseria gonorrhoeae, Treponema pallidum and Treponema pertenue, Listeria monocytogenes, Clostridium sp., Bacillus anthracis, Fusobacterium fusiforme, Actinomyces sp. In acute intestinal amebiasis Tetracyclin may be useful adjunctive therapy to the amebicides. The antibiotic can be used in malaria and protozoic diseases in case of resistance to the other antibiotics. CONTRAINDICATIONS Hypersensitivity to tetracyclin preparations, severe impairment in the liver and renal function. Tetracyclin should not be administered in children under 8 years of age, due to binding with calcium complex and depositions in the bones and teeth, with subsequent hypoplasia of the enamel, permanent discoloration of the teeth and retardation of the bone growth. Tetracyclin

administration

during

pregnancy

and

brest-feeding

is

contraindicated. Tetracyclin use in patients with system lupus erythematodes should be avoided.

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ADVERSE EFFECTS Tetracyclin may cause anorexia, nausea, vomiting, diarrhea, lesions of the oral cavity mucosa and esophagus (for that reason it should be swallowed with sufficient liquid and in sitting position). Skin allergic reactions, Quincke’s edema, photosensitivity may be observed. Transitory disorders in hematopoiesis (leucopenia) have been observed in isolated cases. Long-term high dose Tetracyclin treatment may cause neurotoxic effects (paresthesia, headache, vertigo, ataxia), hepatotoxic and nephrotoxic effects (intensifies the present liver and renal insufficiency); development of candidiasis. PRECAUTIONS Great care should be taken in patients with liver or renal impairment, hematological changes or intensive sun irradiation. In case of oral administration, Tetracyclin should not be taken simultaneously with certain food products (milk and dairy products) or pharmaceuticals (antianemic, antiacid), iron, magnesium, calcium, bismuth, manganese, zinc, aluminium containing drugs. The antibiotic should not be administered concurrently with potent hepatotoxic and nephrotoxic preparations. Prolonged sun irradiation should be avoided during Tetracyclin medication. DRUG INTERACTIONS Tetracyclin forms insoluble complex with bivalent ions of calcium, iron, aluminium, bismuth, magnesium, zinc. Concomitant administration of diuretics enhances the nephrotoxic effect of Tetracyclin. Simultaneous use of retinoids may cause benign increase of the intracranial pressure. In rare cases the antibiotic may enhance the toxic effect of ergoalkaloids and methotrexat. Tetracyclin reduces the effect of oral contraceptives. Concurrent use of penicillin is not recommended due to the antagonistic effect. Tetracyclin may

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enhance the effect of oral anticoagulants, since it affects the prothrombin action and vitamin K synthesis. The antibiotic may interact with certain diagnostic tests, including determinations of catecholamines and sugar in the urine. DOSAGE AND MODE OF ADMINISTRATIONS In the treatment of system infections Tetracyclin is usually administered orally. For adults - orally administered Tetracyclin is usually in doses of 250 mg or 500 mg every 6 h, preferably 1 h before or 2 h after meals. In severe cases Tetracyclin is administered parenterally - as a slow intravenous infusion every 12 h, as a solution containing no more than 0.5% Tetracyclin (prepared by the aid of saline or 5% glucose solution). The usual daily dosage is 1 g, but can be raised up to 2 g in patients with normal renal functions on physician’s opinion. For children (over 8-12 years of age) Tetracyclin is administered orally in doses of 25-50 mg/kg daily, divided in 4 intakes, up to 1 g daily, preferably 1 h before or 2 h after meals. The dosage should not exceed 250 mg daily in case of intramuscular administration. PACKAGE Capsules of 250 mg; blister strip of 10 capsules; 2 blister strips in a box. STORAGE In dry places, protected from direct sunlight, at temperature, not exceeding 25oC. SHELF LIFE Three years for all forms. MANUFACTURED BY: Balkanpharma - Razgrad, Bulgaria.

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