Minocycline in Brief
- Generic name : Minocycline hydrochloride
- Brand names: Dynacin, Minocin, Solodyn
- Therapeutic class: Antibiotic
- Pharmacologic class: Tetracycline
- FDA Approved: June 30, 1971
- Pregnancy Category: D
- Originally discovered: 1960s, Lederle Laboratories,
Minocycline is a highly lipophilic semisynthetic second-generation tetracycline antibiotic.
Its antimicrobial spectrum is very similar to that of doxycycline
with one important addition: minocycline has much more antistaphylococcal activity.
The first tetracycline, chlortetracycline, was discovered in 1948 during
systematic screening of soil specimens for antibiotic-producing microorganisms.
Chlortetracycline and oxytetracycline come from Streptomyces aureofaciens
and Streptomyces rimosus, respectively. Tetracycline is produced semisynthetically
from chlortetracycline. Minocycline is a
semisynthetic derivative of tetracycline.
Minocycline was synthesized by Lederle Laboratories in 1967 and became
widely available under the brand name Minocin in 197216.
Lederle Laboratories, founded in 1902, is a pharmaceutical division
of Cyanamid, a large diversified American chemical manufacturer.
FDA approved uses
- Rocky Mountain spotted fever, typhus fever and the typhus group,
Q fever, rickettsialpox and tick fevers
- Respiratory tract infections: laryngotracheitis, tracheobronchitis,
bronchitis, bronchiolitis, bronchiectasis, bronchopneumonia, pneumonia
(single lobe and multilobe), lung abscess.
- Psittacosis (Ornithosis)
- Inclusion conjunctivitis
- Nongonococcal urethritis, endocervical, or rectal infections in
- Relapsing fever
- Campylobacter fetus infections
- Granuloma inguinale
- Urinary tract infections: cystitis, pyelonephritis
- Skin and skin structure infections: abscess, acne, cellulitis, infected dermatitis, folliculitis,
furunculosis, impetigo, lymphadenitis, suppurative hydradenitis, paronychia,
- Gonococcal infections
- Vincentís infection
- Infections caused by Clostridium species
- Intestinal amebiasis: Minocycline may be a useful adjunct to amebicides
Off-label & Investigational uses
Minocycline is used as a disease-modifying anti-rheumatic drug
(DMARD) in the treatment of rheumatoid arthritis. Rheumatoid arthritis
is a chronic inflammatory disease affecting about 1% of the adult population.
Although rheumatoid arthritis is not an infection, minocycline may
improve the signs and symptoms of this disease. It may slow the progression
of joint damage in arthritis and prevent disability. There is evidence
that, besides its antibiotic effects, minocycline can reduce body's inflammatory responses. It decreases the production of substances
causing inflammation, such as prostaglandins and leukotrienes, while
increasing production of interleukin-10, a substance that reduces inflammation.
Minocycline has a slow onset - it may take 1-3 months after the start of therapy to observe an improvement. And the most benefits are seen when minocycline is used in early disease.
Results of a 48-week multicenter clinical study20
of 219 adults with rheumatoid arthritis show that minocycline reduces
joint pain and swelling and is safe in mild to moderate disease. Minocycline
may slow down the progression of disease and provide relief from swollen,
According to the
College of Rheumatology, "Minocycline is prescribed for patients with symptoms of mild rheumatoid arthritis.
It is sometimes combined with other medications to treat patients with persistent symptoms of
this form of arthritis."
Minocycline has been shown to increase bone mineral density, improve
bone strength and formation, and slow bone resorption in old laboratory
animals with surgically-induced menopause21.
- Lyme disease
Lyme disease, or borreliosis, is an emerging infectious disease caused
by the bacterium Borrelia burgdorferi and is transmitted to
humans by the bite of infected blacklegged ticks. Minocycline may
be useful for the treatment of Lyme disease19.
Sarcoidosis is a disease that results from a specific type of inflammation
of tissues of the body.
Studies24 indicate that
minocycline may be beneficial for the treatment of cutaneous sarcoidosis.
- Cystic fibrosis22-23
Cystic fibrosis (also known as CF, mucoviscoidosis, or mucoviscidosis)
is a hereditary disease that affects mainly the exocrine (mucus) glands
of the lungs, liver, pancreas, and intestines, causing progressive
disability due to multisystem failure.
Periodontitis is a dental disorder that results from progression of
gingivitis, involving inflammation and infection of the ligaments
and bones that support the teeth. Minocycline is used to control bacteria
and reduce the size of periodontal pockets. The periodontist puts
the minocycline micro-spheres into the pockets after scaling and root
planing. The particles release minocycline slowly over time.
- Gougerot-Carteaud Syndrome 17, an uncommon dermatosis of unknown etiology.
Minocycline "pros" and "cons"
- Less photosensitizing. Photosensitivity is least likely than with other tetracyclines25-26.
- High concentrations in the tissues. Minocycline is widely
distributed in body tissues27,
with higher concentrations being found in cerebrospinal fluid and
sputum than with other tetracyclines. As in blood, the
concentration in tissues is generally 2 to 4 times higher with minocycline
than with tetracycline. Equivalent blood and tissue levels achieved
whether administered intravenously or orally.
- Long half-life (from 11 to 23 hours).
- Broader spectrum of antimicrobial activity. Against certain
pathogens, minocycline is more potent than the other tetracyclines.
Minocycline has excellent in vitro inhibitory activity against both
Staphylococcus aureus and coagulase-negative staphylococci, particularly
methicillin-resistant S. aureus and methicillin-resistant S. epidermidis
- Can be used in renal impairment. Most tetracyclines should be avoided in patients with renal insufficiency. However, minocycline can be used in patients with malfunction of the kidneys. It is eliminated through the hepatobiliary and gastrointestinal tracts.
- Low rate of bacterial resistance. Minocycline produces
less antibiotic resistance than tetracycline.28-29
Bacterial cell membranes contain a lipid layer. One mechanism of building
up a resistance to an antibiotic is to produce a thicker lipid layer.
This layer makes it difficult for an antibiotic to penetrate. Minocycline
chemical structure makes it the most lipid soluble of all the tetracyclines.
- Expensive. Minocycline is considerably more expensive than
the other generic tetracyclines.
- Contraindicated in children. May cause enamel hypoplasia
and permanent teeth discoloration.
- Lupus-like syndrome. Minocycline is more likely than other
tetracyclines to produce a lupus-like syndrome. Minocycline-induced
lupus is characterized by the development of non-specific symptoms
after long-term consumption of the drug, and the patient usually continues
to take minocycline despite their illness as the association is not
immediately obvious1. These
abnormalities tend to occur after prolonged therapy (often longer
than 12 months).
- Serum sickness-like reaction. Minocycline induced serum sickness
like reaction (SSLR) was first reported in 199030.
This is a type of delayed allergic reaction, in which the immune system
interprets the antibiotic as a foreign threat. A serum sickness-like
reaction (SSLR) to drug usually consists of cutaneous rash, arthralgia/arthritis,
and, often, fever.
- Vasculitis, usually resembling cutaneous polyarteritis nodosa, may occur in association with minocycline use.
- Intracranial hypertension (pseudotumor cerebri) is an accumulation
of fluid around the brain. Minocycline can cause the rare condition
of secondary intracranial hypertension31
which has initial symptoms of headache, visual disturbances, and confusion.
- Dizziness and other vestibular side effects, that not generally shared by other tetracyclines. Minocycline
can cause quite severe dizziness, nausea, vertigo and vomiting32.
Vertigo has been reported in as many as 86% of individuals in some
- Hyperpigmentation. Unlike other tetracyclines, minocycline
can cause a potentially irreversible slate-grey hyperpigmentation
of the skin. Blue or blue-black oral pigmentation was seen in 10%
of patients taking minocycline for at least 1 year; the rate increased
to 20% after 4 years of continuous use2.
Large daily doses of ascorbic acid (vitamin C) may prevent this phenomenon34.
Mode of action
The tetracyclines are primarily bacteriostatic and are thought to exert
their antimicrobial effect by the inhibition of protein synthesis.
Minocycline is a semisynthetic derivative of tetracycline and is active
against many tetracycline resistant strains of organisms such as staphylococci,
streptococci and E. coli. Thus the combined results of many studies
show its activity against approximately 87% of tetracycline resistant
staphylococci. Minocycline is also active against many strains of staphylococci
which are resistant to penicillin G and certain semisynthetic penicillins.
Minocycline and other tetracycline derivatives have neuroprotective
effects unrelated to their antimicrobial properties. Minocycline has
the greatest permeability of all tetracyclines through the blood-brain
barrier and is well suited for treatment of CNS disorders.
Minocycline can reduce neuronal death after excitotoxicity and ionizing
radiation in culture6-7
and in animal models of stroke7-9,
Huntington's disease12, and
amyotrophic lateral sclerosis13.
The neuroprotective effects of minocycline have been attributed both
to reduced inflammation and a direct effect on neuronal survival.
Minocycline induces anti-inflammatory and antinociceptive effects unrelated
to its antimicrobial activitiy15.
Although the exact mechanisms of minocycline anti-inflammatory effects
are still poorly understood, they may include the inhibition of matrix
metalloproteinase-2 activity, the inhibition of inducible nitric oxide
E2, caspase-1, caspase-3, and COX-2 expressions and the impairment of
Time to clear out of the system
Minocycline half-life is 16 hours (range: 11-23 hours).
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Minocycline-induced lupus: clinical features and response to rechallenge.
Rheumatology 2001; 40: 329-335 PubMed
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Williams TW Jr. Minocycline as an alternative anti-staphylococcal
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Koistinaho J. Tetracycline derivatives and ceftriaxone protect neurons against apoptosis induced
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H, Hara H. Minocycline inhibits oxidative stress and decreases
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KB, Zhu S, Bian J, Guo L, Farrell LA, Hersch SM, Hobbs W, Vonsattel
JP, Cha JH, Friedlander RM. Minocycline inhibits caspase-1
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Published: July 01, 2008
Last updated: July 24, 2014
- Minocycline is the least frequently prescribed of the three tetracyclines, but it has the largest fraction of repeat prescriptions.
- In addition to its antibiotic activity, minocycline has anti-inflammatory
- Minocycline may cause rare but very serious side effects, including
hypersensitivity syndrome, autoimmune hepatitis, and lupus.
- Aside from its antimicrobial properties, minocycline has been
found to have beneficial effects on inflammation, microglial activation,
matrix metalloproteinases, nitric oxide production, and apoptotic