Mechanism of Action
The tetracyclines are primarily bacteriostatic and are thought to exert their antimicrobial effect by the inhibition of protein synthesis. The tetracyclines, including minocycline, have similar antimicrobial spectrum of activity against a wide range of gram-positive and gram-negative organisms. Cross-resistance of these organisms to tetracycline is common.
Brands of Minocycline in Kenya
Minocycline is indicated in the treatment of the following infections due to susceptible strains of the designated microorganisms:
- Rocky Mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsialpox and tick fevers caused by rickettsiae.
- Respiratory tract infections caused by Mycoplasma pneumoniae.
- Lymphogranuloma venereum caused by Chlamydia trachomatis.
- Psittacosis (Ornithosis) due to Chlamydophila psittaci.
- Trachoma caused by Chlamydia trachomatis, although the infectious agent is not always eliminated, as judged by immunofluorescence.
- Inclusion conjunctivitis caused by Chlamydia trachomatis.
- Nongonococcal urethritis, endocervical, or rectal infections in adults caused by Ureaplasma urealyticum or Chlamydia trachomatis.
- Relapsing fever due to Borrelia recurrentis.
- Chancroid caused by Haemophilus ducreyi.
- Plague due to Yersinia pestis.
- Tularemia due to Francisella tularensis.
- Cholera caused by Vibrio cholerae.
- Campylobacter fetus infections caused by Campylobacter fetus.
- Brucellosis due to Brucella species (in conjunction with streptomycin).
- Bartonellosis due to Bartonella bacilliformis.
- Granuloma inguinale caused by Klebsiella granulomatis.
Minocycline is indicated for the treatment of infections caused by the following gram-negative microorganisms when bacteriologic testing indicates appropriate susceptibility to the drug:
- Escherichia coli.
- Enterobacter aerogenes.
- Shigella species.
- Acinetobacter species.
- Respiratory tract infections caused by Haemophilus influenzae.
- Respiratory tract and urinary tract infections caused by Kiebsiella species.
Minocycline is indicated for the treatment of infections caused by the following gram-positive microorganisms when bacteriologic testing indicates appropriate susceptibility to the drug:
- Upper respiratory tract infections caused by Streptococcus pneumoniae.
- Skin and skin structure infections caused by Staphylococcus aureus. (Note: Minocycline is not the drug of choice in the treatment of any type of staphylococcal infection).
- When penicillin is contraindicated, minocycline is an alternative drug in the treatment of the following infections:
- Uncomplicated urethritis in men due to Neisseria gonorrhoeae and for the treatment of other gonococcal infections.
- Infections in women caused by Neisseria gonorrhoeae.
- Syphilis caused by Treponema pallidum subspecies pallidum.
- Yaws caused by Treponema pallidum subspecies pertenue.
- Listeriosis due to Listeria monocytogenes.
- Anthrax due to Bacillus anthracis.
- Vincent’s infection caused by Fusobacterium fusiforme.
- Actinomycosis caused by Actinomyces israelii.
- Infections caused by Clostridium species.
- In acute intestinal amebiasis, minocycline may be a useful adjunct to amebicides.
- In severe acne, minocycline may be useful adjunctive therapy.
Oral minocycline is indicated in the treatment of asymptomatic carriers of Neisseria meningitidis to eliminate meningococci from the nasopharynx. In order to preserve the usefulness of minocycline 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 prophylactic use of minocycline be reserved for situations in which the risk of meningococcal meningitis is high.
Oral minocycline is not indicated for the treatment of meningococcal infection.
Although no controlled clinical efficacy studies have been conducted, limited clinical data show that oral minocycline hydrochloride has been used successfully in the treatment of infections caused by Mycobacterium marinum.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of minocycline and other antibacterial drugs, minocycline ,should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
This drug is contraindicated in persons who have shown hypersensitivity to any of the tetracyclines or to any of the components of the product formulation.
Minocycline , like other tetracycline-class antibiotics, can cause fetal harm when administered to a pregnant woman.
All tetracyclines form a stable calcium complex in any bone-forming tissue. A decrease in the fibula growth rate has been observed in premature human infants given oral tetracycline in doses of 25 mg/kg every six hours. This reaction was shown to be reversible when the drug was discontinued.
Use in Pregnancy
Results of animal studies indicate that tetracyclines cross the placenta, are found in fetal tissues, and can have toxic effects on the developing fetus (often related to retardation of skeletal development). Evidence of embryotoxicity has been noted in animals treated early in pregnancy.
Drug Rash with Eosinophilia and Systemic Symptoms (DRESS) including fatal cases have been reported with minocycline use. If this syndrome is recognized, the drug should be discontinued immediately.
The antianabolic action of the tetracyclines may cause an increase in blood urea nitrogen (BUN). While this is not a problem in those with normal renal function, in patients with significantly impaired function, higher serum levels of tetracycline may lead to azotemia, hyperphosphatemia, and acidosis.
Photosensitivity manifested by an exaggerated sunburn reaction has been observed in some individuals taking tetracyclines. This has been reported with minocycline.
Central Nervous System
Central nervous system side effects including light-headedness, dizziness, or vertigo have been reported with minocycline therapy. 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 usually disappear rapidly when the drug is discontinued.
Clostridium difficile Associated Diarrhea
Clostridium difficile associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including minocycline hydrochloride tablets, and may range in severity from mild diarrhea to fatal colitis.
Body as a whole: Fever, and discoloration of secretions.
Gastrointestinal: Anorexia, nausea, vomiting, diarrhea, dyspepsia, stomatitis, glossitis, dysphagia, enamel hypoplasia, enterocolitis, pseudomembranous colitis, pancreatitis, inflammatory lesions (with monilial overgrowth) in the oral and anogenital regions. Instances of esophagitis and esophageal ulcerations have been reported in patients taking the tetracycline-class antibiotics in capsule and tablet form.
Hepatic toxicity: Hyperbilirubinemia, hepatic cholestasis, increases in liver enzymes, fatal hepatic failure, and jaundice. Hepatitis, including autoimmune hepatitis, and liver failure have been reported
Skin: Alopecia, erythema nodosum, hyperpigmentation of nails, pruritus, toxic epidermal necrolysis, vasculitis, maculopapular rash and erythematous rash. Exfoliative dermatitis has been reported. Fixed drug eruptions have been reported. Lesions occurring on the glans penis have caused balanitis. Erythema multiforme and Stevens-Johnson syndrome have been reported.
Respiratory: Cough, dyspnea, bronchospasm, exacerbation of asthma, and pneumonitis.
Renal toxicity: Interstitial nephritis. Elevations in BUN have been reported and are apparently dose related
Musculoskeletal: Arthralgia, arthritis, bone discoloration, myalgia, joint stiffness, and joint swelling.
Hypersensitivity reactions: Urticaria, angioneurotic edema, polyarthralgia, anaphylaxis/anaphylactoid reaction (including shock and fatalities), anaphylactoid purpura, myocarditis, pericarditis, exacerbation of systemic lupus erythematosus and pulmonary infiltrates with eosinophilia have been reported. A transient lupus-like syndrome and serum sickness-like reactions have also been reported.
Blood: Agranulocytosis, hemolytic anemia, thrombocytopenia, leukopenia, neutropenia, pancytopenia, and eosinophilia have been reported.
Central Nervous System: Convulsions, dizziness, hypesthesia, paresthesia, sedation, and vertigo. Bulging fontanels in infants and benign intracranial hypertension (pseudotumor cerebri) in adults have been reported
Other: Thyroid cancer has been reported in the post-marketing setting in association with minocycline products. When minocycline therapy is given over prolonged periods, monitoring for signs of thyroid cancer should be considered.
- Because tetracyclines have been shown to depress plasma prothrombin activity, patients who are on anticoagulant therapy may require downward adjustment of their anticoagulant dosage.
- Since bacteriostatic drugs may interfere with the bactericidal action of penicillin, it is advisable to avoid giving tetracycline-class drugs in conjunction with penicillin.
- Absorption of tetracyclines is impaired by antacids containing aluminum, calcium, or magnesium, and iron-containing preparations.
- The concurrent use of tetracycline and methoxyflurane has been reported to result in fatal renal toxicity.
- Concurrent use of tetracyclines with oral contraceptives may render oral contraceptives less effective.
- Administration of isotretinoin should be avoided shortly before, during, and shortly after minocycline therapy. Each drug alone has been associated with pseudotumor cerebri
- Increased risk of ergotism when ergot alkaloids or their derivatives are given with tetracyclines.
DOSAGE AND ADMINISTRATION
- The usual dosage of minocycline is 200 mg initially followed by 100 mg every 12 hours. Alternatively, if more frequent doses are preferred, two or four 50 mg tablets may be given initially followed by one 50 mg capsule 4 times daily.
- Uncomplicated gonococcal infections other than urethritis and anorectal infections in men: 200 mg initially, followed by 100 mg every 12 hours for a minimum of 4 days, with post-therapy cultures within 2 to 3 days.
- In the treatment of uncomplicated gonococcal urethritis in men, 100 mg every 12 hours for 5 days is recommended.
- For the treatment of syphilis, the usual dosage of minocycline hydrochloride should be administered over a period of 10 to 15 days. Close follow-up, including laboratory tests, is recommended.
- In the treatment of meningococcal carrier state, the recommended dosage is 100 mg every 12 hours for 5 days.
- Mycobacterium marinum infections: Although optimal doses have not been established, 100 mg every 12 hours for 6 to 8 weeks have been used successfully in a limited number of cases.
- Uncomplicated urethral, endocervical, or rectal infection in adults caused by Chlamydia trachomatis or Ureaplasma urealyticum: 100 mg orally, every 12 hours for at least 7days.
Ingestion of adequate amounts of fluids along with capsule and tablet forms of drugs in the tetracycline-class is recommended to reduce the risk of esophageal irritation and ulceration.
The pharmacokinetics of minocycline in patients with renal impairment (CLCR <80 mL/min) have not been fully characterized. Current data are insufficient to determine if a dosage adjustment is warranted. The total daily dosage should not exceed 200 mg in 24 hours. However, due to the anti-anabolic effect of tetracyclines, BUN and creatinine should be monitored
WHERE TO BUY MINOCYCLINE IN KENYA:
Minocycline is a prescription only medicine and hence can only be bought if you have a valid prescription from a doctor.
Clinical | Pharmacokinetic data
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