Minocycline, sold under the brand name Minocin among others, is a tetracycline antibiotic medication used to treat a number of bacterial infections such as some occurring in certain forms of pneumonia.[ It is generally (but not always) less preferred than the tetracycline doxycycline.][ Minocycline is also used for the treatment of acne and rheumatoid arthritis.]
Common side effects include nausea, diarrhea, dizziness, allergic reactions, and kidney problems.[ Serious side effects may include anaphylaxis, a lupus-like syndrome, and photosensitivity.][ Use in the later part of pregnancy may harm the baby and safety during breastfeeding is unclear.][
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Minocycline was patented in 1961 and came into commercial use in 1971.
Medical uses
Acne
Minocycline and doxycycline are frequently used for the treatment of acne vulgaris.
Historically, oral minocycline has been an effective treatment for acne vulgaris.
Oral minocycline is used to treat acne for up to 3 to 4months.
Other infections
Minocycline is also used for other skin infections such as methicillin-resistant Staphylococcus aureus.
Although minocycline's broader spectrum of activity, compared with other members of the group, includes activity against Neisseria meningitidis,
It may be used to treat certain strains of methicillin-resistant S. aureus infection and a disease caused by drug-resistant Acinetobacter spp.
A list of uses includes:
Minocycline has been reported to be effective in the eradication of UTIs and prostatitis.
Available forms
Minocycline is available in the form of 50 and 100mg oral capsules, among a variety of other formulations.
Contraindications
The drug is contraindication in people with known hypersensitivity to tetracycline antibiotics, as there is complete cross sensitivity in this group. It is also contraindicated in people with severe liver impairment and after the 16th week of pregnancy.
Side effects
Minocycline may cause abdominal pain, diarrhea, dizziness, unsteadiness, somnolence, mouth sores, migraines, and vomiting. It increases photophobia, and may affect the sleep quality and rarely causes .
Occasionally, minocycline therapy may result in autoimmune disorders such as drug-related lupus and autoimmune hepatitis, which usually occurs in men who also developed minocycline-induced lupus; however, women are more likely to develop minocycline-induced lupus. Significant or complete recovery occurs in most people who develop minocycline-induced autoimmune problems within a period of a few weeks to a year of cessation of minocycline therapy. Autoimmune problems emerge during chronic therapy, but can sometimes occur after only short courses of a couple of weeks of therapy.
Minocycline, but not other tetracyclines, can cause vestibular disturbances, including symptoms of dizziness, ataxia, vertigo, and tinnitus.
Symptoms of an allergic reaction include rash, itching, swelling, severe dizziness, and trouble breathing.
Contrary to most other tetracycline antibiotics (doxycycline excluded), minocycline may be used in those with kidney disease, but may aggravate systemic lupus erythematosus.
Minocycline can cause the rare condition of secondary intracranial hypertension, which has initial symptoms of headache, visual disturbances, dizziness, vomiting, and confusion.
Minocycline, like most tetracyclines, becomes dangerous past its expiration date.["Principles and methods for the assessment of nephrotoxicity associated with exposure to chemicals". Environmental health criteria: 119. World Health Organization (WHO). . ISSN 0250-863X. 1991] While most prescription drugs lose potency after their expiration dates, tetracyclines are known to become toxic over time. Expired tetracyclines can cause serious damage to the kidney due to the formation of a degradation product, anhydro-4-epitetracycline.
Minocycline, like other tetracyclines, is associated with esophageal irritation and ulceration if insufficient fluids are taken with the drug before sleep.[Drugs.com 'Minocycline Disease Interactions'. Retrieved 12 February 2017.]
A 2007 study suggested that minocycline harms amyotrophic lateral sclerosis (ALS) patients. Patients on minocycline declined more rapidly than those on placebo. The mechanism of this side effect is unknown, although a hypothesis is that the drug exacerbated an autoimmune component of the primary disease. The effect does not seem to be dose-dependent because the patients on high doses did not do worse than those on the low doses.
Other possible rare side effects of minocycline include hyperpigmentation and hypersensitivity reactions, among others.
Minocycline is another drug known to cause leukopenia.
Minocycine has shown thyroid toxicity in animals, including in rodents, mini pigs, dogs, and monkeys.
The use of minocycline to treat acne has been associated with skin and gut dysbiosis (see antibiotic misuse).
Overdose
Symptoms of minocycline overdose may include dizziness, nausea, and vomiting.
Interactions
The combination of minocycline with dairy, antacids, calcium and magnesium supplements, iron products, laxatives containing magnesium, or bile acid sequestrants may decrease minocycline's effectiveness by forming . Combining it with isotretinoin, acitretin or other can increase the risk for intracranial hypertension. Minocycline significantly reduces concentrations of the anti-HIV drug atazanavir in the body.
Pharmacology
Pharmacodynamics
Antibiotic activity
Minocycline mediates its antibiotic activity by binding to the 30S ribosomal subunit of bacteria and thereby inhibiting protein synthesis.
Other activities
Minocycline shows a number of off-target activities in addition to its antibiotic activity.
Some other reported activities of minocycline include:
Pharmacokinetics
Absorption
Minocycline is quickly and nearly completely absorbed from the upper part of the small intestine. Taking it together with food, including milk, has no relevant influence on resorption. It reaches highest blood plasma concentrations after 1 to 2hours.
Distribution
The drug has a plasma protein binding of 70 to 75%. It penetrates into almost all tissues; very high concentrations are found in the gallbladder and liver. It crosses the blood–brain barrier better than doxycycline and other tetracyclines, reaching therapeutically relevant concentrations in the cerebrospinal fluid and also in inflamed meninges.
Metabolism
Minocycline is inactivated by drug metabolism in the liver to about 50%. It is primarily metabolized into 9-hydroxyminocycline.
Elimination
The rest is predominantly excreted into the gut (in part via the gallbladder, in part directly from blood vessels) and eliminated via the feces. About 10–15% are eliminated via the kidneys. It is excreted about 5 to 10% unchanged in urine.
Chemistry
Minocycline is a tetracycline derivative.
The drug is used in form of minocycline hydrochloride dihydrate,
The partition coefficient (P) of minocycline has been reported to be 39.4 (i.e., log P of 1.60).
History
Minocycline was patented in 1961, was first described in the scientific literature in 1967,
Society and culture
Brand names
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Minomycin
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Minostad (in Europe, for the treatment of acne vulgaris)
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Akamin
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Minocin
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Minoderm
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Cyclimycin
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Arestin (1-mg doses administered locally into periodontal pockets, after scaling and root planing, for treatment of periodontal disease.)
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Nomika (in Indonesia)
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Aknemin
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Solodyn (extended-release, for the treatment of acne)
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Dynacin
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Sebomin
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Mino-Tabs
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Acnamino
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Minopen (in Japan)
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Maracyn 2 (for treatment of bacterial infections in aquarium fish and amphibians)
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Quatrocin (in Syria)
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Minox (in Ireland)
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Minoz (in India and Romania)
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Divaine (in India)
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Vinocyclin 100 (100-mg dose approved for treatment of acne in Vietnam)
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Dentomycin (2% minocylcine gel for use in periodontal pockets)
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Amzeeq (4% foam, approved for treatment of acne United States)
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Zilxi (1.5% foam, approved for treatment of rosacea in the United States)
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Cleeravue-M
Generic availability
It is available as a generic medication.[
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Research
Neuropsychiatric disorders
Depression
Minocycline has been studied in the treatment of depression.
Schizophrenia
Early research has found a tentative benefit from minocycline in schizophrenia,
Other conditions
Some early studies suggest that minocycline may be beneficial as an add-on treatment for moderate-to-severe obsessive-compulsive disorder (OCD) when used with a selective serotonin reuptake inhibitor (SSRI).
Stroke and neurodegenerative diseases
In ongoing research and trial, minocycline demonstrated efficacy and seems a promising Neuroprotection agent in acute stroke patients, especially in AIS subgroup. Further RCTs are needed to evaluate the efficacy and safety of minocycline among ICH patients.
Research is examining the possible Neuroprotection and anti-inflammatory effects of minocycline against the progression of a group of neurodegenerative disorders including multiple sclerosis, rheumatoid arthritis, Huntington's disease, and Parkinson's disease.
A trial found no difference between minocycline and placebo in people with Alzheimer's disease.
Multiple sclerosis
A 2007 study reported the impact of the antibiotic minocycline on clinical and magnetic resonance imaging (MRI) outcomes and serum immune molecules in 40 MS patients over 24 months of open-label minocycline treatment. Despite a moderately high pretreatment relapse rate in the patient group prior to treatment (1.3/year pre-enrollment; 1.2/year during a three-month baseline period), no relapses occurred between months 6 and 24 on minocycline. Also, despite significant MRI disease-activity pretreatment (19/40 scans had gadolinium-enhancing activity during a three-month run-in), the only patient with gadolinium-enhancing lesions on MRI at 12 and 24 months was on half-dose minocycline. Levels of interleukin-12 (IL-12), which at high levels might antagonize the proinflammatory IL-12 receptor, were elevated over 18 months of treatment, as were levels of soluble Blood vessel cell adhesion molecule-1 (VCAM-1). The activity of matrix metalloproteinase-9 was decreased by treatment. Clinical and MRI outcomes in this study were supported by systemic immunological changes and call for further investigation of minocycline in MS.
Delirium
A 2024 randomized controlled trial found that prophylaxis minocycline provided a small but significant decrease in delirium incidence in critically ill patients.
Hearing protection
Several preclinical studies (in vitro cell cultures and animal models) suggest that minocycline may have otoprotective benefits. Animal models indicate it could potentially reduce noise-induced and blast-induced hearing loss, possibly by protecting and mitigating inflammation.
Other uses
Both minocycline and doxycycline have shown effectiveness in asthma due to immune-suppressing effects.
Minocycline also has been used as a "last-ditch" treatment for toxoplasmosis in AIDS patients.
Minocycline has been suggested as a possible treatment for post-COVID-19 syndrome ("long COVID"), but no quality clinical trials exist.
