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Minocycline

A broad spectrum bacteriostatic antibiotic with a long half life.

Trade name Minocin

An oral agent.

Bioavailability is 100%.

Metabolism occurs in the liver.

Biological half-life11–22 hours

Excretion is mostly fecal, with remainder renal.

A broad-spectrum tetracycline antibiotic, with a broader spectrum than other members of the group.

It is a bacteriostatic antibiotic.

Classified as a long-acting type agent, and generally has serum levels 2–4 times that of the simple water-soluble tetracyclines.

The most lipid-soluble of the tetracycline-class antibiotics, giving it the greatest penetration into the prostate and brain.

Has the greatest amount of central nervous system (CNS)-related side effects in tetracycline group of drugs, such as vertigo as a result of its CNS lipid solubility.

A common side effect is diarrhea, while uncommon side effects include skin discoloration and autoimmune disorders.

A relatively poor tetracycline-class antibiotic choice for urinary pathogens sensitive to this antibiotic class, as its solubility in water and levels in the urine are less than all other tetracyclines.

Minocycline is metabolized by the liver and has poor urinary excretion.

Synthesized semi-synthetically from natural tetracycline antibiotics.

 

Minocycline 100mg capsules.

Minocycline and doxycycline are frequently used for the treatment of acne vulgaris.

Both of these closely related antibiotics have similar levels of efficacy, although doxycycline has a slightly lower risk of adverse side effects.

Acne that is caused by antibiotic resistant bacteria is a growing problem because symptoms are caused by bacteria (primarily Propionibacterium acnes) that are resistant to these antibiotics.

Minocycline is also used for other skin infections such as MRSA as well as Lyme disease.

Its activity against Lyme disease is enhanced by its superior ability to cross the blood-brain barrier.

Has a broader spectrum of activity, compared with other members of the tetracycline group.

Both minocycline and doxycycline have shown effectiveness in asthma due to immune suppressing effects.

Minocycline has modest effectiveness in treating rheumatoid arthritis, and is a DMARD agent

A list of indications include;

Amoebic dysentery

Anthrax

Bubonic plague

Cholera

Ehrlichiosis

Gonorrhea when penicillin cannot be given

Hidradenitis suppurativa

HIV adjuvant to HAART

Periodontal disease

Perioral dermatitis

Respiratory infections such as pneumonia

Rocky Mountain spotted fever

Rosacea

Syphilis when penicillin is contraindicated

Urinary tract infections, rectal infections, and infections of the cervix caused by sensitive organisms.

Contrary to most other tetracyclines antibiotics may be used in those with kidney disease.

May aggravate systemic lupus erythematosus or trigger autoimmune hepatitis.

Can cause secondary intracranial hypertension which has initial symptoms of headache, visual disturbances, dizziness, vomiting, and confusion.

Brain swelling, and autoimmune rheumatoid arthritis are rare side effects.

Minocycline, like most tetracyclines, becomes dangerous past its expiration date, and can cause serious damage to the kidney due to the formation of a degradation product, anhydro-4-epitetracycline.

Minocycline’s absorption is impaired if taken at the same time of day as calcium or iron supplements.

Patients taking this drug should avoid prolonged or excessive exposure to direct sunlight.

Side effects include: upset stomach, diarrhea, dizziness, unsteadiness, drowsiness, mouth sores, headache and vomiting, increased sensitivity to sunlight, may affect quality of sleep, and rarely has also been linked to cases of lupus.

Prolonged use can lead to blue-gray skin, fingernails and staining of scar tissue.

Permanent blue discoloration of gums or teeth discoloration may occur.

Side effects include: fever, yellowing of the eyes or skin, stomach pain, sore throat, vision changes, and mental changes.

Occasionally may result in autoimmune disorders.

Women are the most likely to develop minocycline induced lupus.

Recovery occurs in most people who develop minocycline induced autoimmune problems within a period of a couple of weeks to a year of cessation of therapy.

Autoimmune problems emerge during chronic therapy but can sometimes occur after only short courses of therapy.

Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) syndrome can occur during the first few weeks of therapy with minocycline.[29]

Can cause vestibular disturbances with dizziness, ataxia, vertigo and tinnitus due to its ability to penetrate into the central nervous system.

Vestibular side effects are much more common in women than in men, occurring in 50% to 70% of women exposed, and is rarely used in female patients.

Rarely causes idiopathic intracranial hypertension, which is more common in female patients, potentially leading to permanent vision damage.

Thyroid cancer has been reported in association with minocycline products, and when minocycline therapy is given over prolonged periods, monitoring for signs of thyroid cancer should be considered.

Has demonstrated neurorestorative as well as neuroprotective properties.

Neurodegenerative diseases such as Huntington’s disease and Parkinson’s disease have shown beneficial response to minocycline in research studies.

An antipsychotic benefit has been found in people with schizophrenia and minocycline is proposed as a possible add-on therapy.

Indirectly inhibit inducible nitric oxide synthase (NOS).

As an anti-inflammatory, minocycline inhibits apoptosis via attenuation of TNF-alpha, downregulating pro-inflammatory cytokine output.

Has a direct action on the activated T cells and on microglia, which results in the decreased ability of T cells to contact microglia which impairs cytokine production in T cell-microglia signal transduction.

Inhibits microglial activation, through blockade of NF-kappa B nuclear translocation.

May be beneficial in ischemic stroke, and schizophrenia.

Adverse effects include diarrhea, vertigo, or do immune disorders, and hyperpigmentation.

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