Minocin

MINOCIN*
MINOCYCLINE HYDROCHLORIDE
CAPSULES, SYRUP
ANTIBIOTIC

DESCRIPTION
Each capsule contains minocycline HCl equivalent to the same amount of minocycline.
Each teaspoonful (5 ml.) of the syrup contains 50 mg of minocycline base, with propylparaben 0,10% and butylparaben 0,06% as preservatives with alcohol U.S.P. 5% v/v. It is supplied as a custard flavored preparation.
Minocycline is a new semisynthetic derivative of tetracycline and its chemical name is 7-dimethylamino-6-deoxy-6-demethyltetracycline. Minocycline is unique among the tetracycline
antibiotics in being active against many tetracycline-resistant strains of organisms such a staphylococci, streptococci and E. Coli. Thus, the combined results of many studies show its
activity against approximately 87% of tetracycline-resistant staphylococci. In addition, it is more active than the other tetracycline analogs against the majority of tetracycline-sensitive
organisms. Minocycline is also active against many strains of staphylococci which are resistant to penicillin G and certain semisynthetic penicillins.
Tube-dilution testing: Microorganisms may be considered susceptible it the M.I.C. (minimum inhibitory concentration) is not more than 4,0 mcg/ml., partially resistant if the M.I.C. is 4,0 to
12,5 mcg/ml., and resistant if the M.I.C. is more than 12,5 mcg/ml.

Susceptibility-plate testing: if the Kirby-Bauer method (using a 30 mcg tetracycline disc) gives a zone of 18 mm, or more, the bacterial strain is considered to be susceptible to any tetracycline. For strains resistant to other tetracyclines, minocycline susceptibility powder may be used for additional susceptibility testing.

Minocycline is rapidly absorbed in man after oral administration, reaching peak serum levels in 2 to 3 hours. After single ora1 doses of 150 mg., minocycline has a relatively long serum half-life of about 18 hours and yields drug serum levels which are generally 2 to 3 times higher than those of most other tetracyclines at all time intervals, with measurable concentrations still present up to 96 hours. The urinary and fecal recovery of unmetabolized minocycline is one-half to one-third that of the other tetracyclines and is in a biologically active form.

Minocycline is widely distributed in body tissue, with higher concentrations being found in brain and cerebrospinal fluid than with the other tetracycline analogs. As in the blood, drug concentrations in the tissues are generally 2 to 3 times higher with minocycline then with tetracycline. Peak cerebrospinal fluid levels are reached six hours following a single dose.

INDICATIONS

1. MINOCIN minocycline HCl is indicated in infections caused by the following microorganisms:
• Rickettsial agents of Rocky Mountain spotted fever, typhus fever and the typhus group. Q fever, rickettsialpox, and tick fevers.
• Mycoplasma pneumoniae (PPLO, Eaton agent). MINOCIN is also effective in non gonococcal urethritis, in which Mycoplasma T-Strains may play a causative role.
• Agents of psittacosis and ornithosis.
• Agents of lymphogranuloma venereum and granuloma inguinale.
• The spirochetal agent of relapsing fever (Borrelia recurrentis).
• The following gram-negative microorganisms; Hemophilus ducreyi (chancroid), Pasteurella pestis and Pasteurella tularensis
• Bartonella bacilliformis
• Bactereoides species,
• Vibrio comma and Vibrio fetus
• Brucella species (in conjunction with streptomycin).
2. Because many strains of the following groups of microorganisms have been shown to be resistant to tetracyclines, culture and susceptibility testing are recommended.
• Gram-negative : Escherichia coli, Enterobacter aerogenes (formerly Aerobacter aerogenes),  Shigella species, Mima species and Herellea species, Haemophilus influenza (respiratory infections), Klebsiella species (respiratory and urinary infections).
• Gram-positive : Streptococcus pyogenes (For upper respiratory infections due to Group A beta-hemolytic straptococci, penicillin is the usual drug of choice, including prophylaxis of rheumatic fever) 
• Alpha-hemolytic streptococci (viridans group)
• Enterococcus group (Streptococcus faecalis)
• Diplococcus pneumoniae
• Staphylococcus Aureus
3. When penicillin is contraindicated, tetracyclines are alternative drugs in the treatment of infections due to;
   • Neisseria gonorrhoeae
   • Treponema pallidum and Treponema pertenue (syphilis and yaws)
   • Listeria monocytogenes
   • Clostridium species
   • Bacillus anthracis
   • Fusobacterium fusiforme (Vincent's Infection) 
   • Actinomyces species
4. In addition the following uses have been established; In acute intestinal amebiasis, the tetracyclines may be a useful adjunct to amebicides.
   • In severe acne, the tetracyclines may be useful adjunctive therapy. Minocycline is indicated in the treatment of trachoma, although the infectious agent is not always eliminated, as judged by immunofluorescence.
   • Inclusion conjunctivitis may be treated with oral tetracyclines or with a combination of oral and topical agents.
   • In order to preserve the usefulness of MINOCIN minocyclina HCl in the treatment of asymptomatic meningococcal carriers, diagnostic laboratory procedures, including serotyping and susceptibility testing, should be performed to establish the carrier state and the correct treatment. It is recommended that the drug be reserved for situations in which the risk of meningococcal meningitis is high.

CONTRAINDICATIONS
Minocycline is contraindicated in patients with a history of hypersensitivity to any of the tetracycline antibiotics.

PRECAUTIONS AND ADVERSE EFFECTS
CNS side effects including light headedness, dizziness or vertigo have been reported. Patients who experience these symptoms should be cautioned about driving vehicles or using hazardous machinery while on minocycline therapy. These symptoms may disappear during therapy and always disappear rapidly when the drug is discontinued. The use of drugs of the tetracycline class during tooth development (last half of pregnancy, infancy and childhood to the age of 8 years) may cause permanent discoloration of the teeth (yellow-gray-brown). This adverse reaction is more common during long-term use of the drugs but has been observed following repeated short-term courses. Enamel hypoplasia has also been reported.
All tetracyclines form a stable calcium complex in any bone-forming tissue. A decrease in the fibula growth rate has been observed in prematures given oral tetracycline in doses of 25 mg/kg. every 6 hours. This reaction was shown to be reversible when the drug was discontinued.

The safety of Tetracyclines for use during pregnancy has not been established. (see below under "Animal Pharmacology and toxicology".) Tetracyclines are present in the milk of lactating women.

The antianabolic action of the tetracyclines may cause an increase in BUN, and this effect is apparently dose related, Studies to date with MINOCIN indicate that, in patients with renal impairment, elevation of BUN and drug accumulation are infrequent and minor. Therefore, it is not necessary to reduce the usual dosage of minocycline in the great majority of these patient. In cases of extreme renal insuficiency, reduction of dosage and monitoring of renal function may be advisable.

Photosensitivity manifested by an exaggerated sunburn has been observed in some individuals taking tetracyclines. Patients apt to be exposed to direct sunlight or ultraviolet light should be advised that this reaction can occur with tetracycline drugs, and treatment should be discontinued at the first evidence of skin erythema. Studies to date indicate that photosensitivity does not occur with minocycline.

Most side effects seen during minocycline therapy have consisted of the gastrointestinal disturbances seen with other antibiotics, particularly nausea. Alergic reactions such as skin rashes or urticaria have been rare. As with other antibiotics, use of this drug may result in overgrowth of non-susceptible organisms, including fungi. If superinfectionoccurs, appropriate therapy should be instituted.

Benign intracranial hypertension (resulting in bulging fontanels in infants) has occured after full therapeutic dosage of tetracyclines, but has subsided soon after discontinuance of therapy.

Because the tetracyclines have been shown to depress plasma prothrombin activity, patients who are on anticoagulant therapy may require downward adjustment of their anticoagulant dosage.

As with other tetracyclines, hemolytic anemia, thrombocytopenia, neutropenia and eosinophilia have been reported.

In long-term therapy, periodic laboratory evaluation of organ systems (particularly hematopoietic, renal and hepatic) should be performed.

All infections due to Group A beta hemolytic streptococci should be treated for at least 10 days to decrease the likelihood of rheumatic lever or acute glomerulonephritis.

Since the bactericidal effect of penicillin may be reduced by the action of bacteriostatic drugs, it is advisable to avoid giving penicillin when tetracycline therapy has been initiated.

DOSAGE AND ADMINISTRATION
The usual dosage of minocycline is 200 mg, as an initial dose, followed by a dose of 100 mg. every 24 hours, in the treatment of mild infections. An alternative regimen can be used for patients weighing less than 60 kilos consisting of 100 mg, twice daily without an initial loading dose.
In the management of more severe infections 200 mg, as an initial dose, followed by 100 mg, every 12 hours, is recommended. An alternative regimen can be used, consisting of an initial 200 mg dose followed by 200 mg 12 hours later and then 200 mg every 24 hours. If more frequent doses are preferred, one 50 mg. capsule three or four times daily.

Children: Usual dosage is 1 to 2 mg-per pound (2 to 4 mg/kg) as an initial dose, followed by 0,5 to 1 mg. per pound (1 to 2 mg./kg.) every 12 hours, depending on the severity of the disease. For children weighing over 100 pound. (45.5 kg.), the usual dosage for adults should be used.

For the treatment of syphilis, the usual dosage of MINOCIN should be administered for 10 to 15 days. Close followup, including laboratory tests, is recommended.

Acute gonococcal urethritis has been treated effectively with a single dose of 250 or 300 mg.

Minocycline is indicated in the treatment of asymptomatic carriers of N. meningitis to eliminate meningococci from the nasopharynx. The recommended dose is 100 mg. every 12 hours for five days.

Therapy should be continued for one to three days after the characteristic symptoms or fever have subsided. In the treatment of streptococcal infections, a therapeutic dosage should be administered for at least 10 days.

Studies to date have indicated that the absorption of MINOCIN is not notably influenced by foods and dairy products, iron salts, sodium bicarbonate, and antacids containing aluminum, calcium, or magnesium impair absorption and should not be given concomitantly with oral tetracyclines.

ANIMAL PHARMACOLOGY AND TOXICOLOGY
MINOCIN Minocycline HCl has been found to produce high blood concentrations following oral dosage to various animal species and to be extensively distributed to all tissues examined in 14 C-labeled drug studies in dogs. MINOCIN has been found experimentally to produce discoloration of the thyroid glands. This finding has been observed in rats and dogs. Changes in thyroid function have also been found in these animal species. However no change in thyroid function has been observed in humans.

Code
5300 Minocycline Hard Shell Capsule. 50 mg.
Reg. No. DKL. 8719900601Al
5301 Minocycline Hard Shell Capsule. 100 mg.
Reg. No. DKL. 8719900601Bl
5313 Minocycline Syrup 50 mg/5 ml.
Reg. No. D.6015909

HARUS DENGAN RESEP DOKTER

Processed by Phapros Semarang, Indonesia, for Rajawali under license from American Cyanamid Company (Lederle Laboratories Division)

* Registered trademark of American Cyanamid Company

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