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'''Minocycline hydrochloride''', also known as '''minocycline''', is a member of the broad spectrum  [[tetracycline antibiotics]], and has a broader spectrum than the other members. It is a [[bacteriostatic]] antibiotic.  As a result of its long half-life it generally has [[blood plasma|serum]] levels 2-4 times that of most other tetracyclines (150 mg giving 16 times the activity levels compared to 250 mg of [[tetracycline]]  at 24-48 hours). Minocycline was originally discovered by [[American Cyanamid|Lederle Laboratories]] and marketed under the brand name ''Minocin''.<ref>[http://www.scripps.edu/chem/baran/images/grpmtgpdf/Lin_Mar_05revised.pdf]Lin, DW The Tetracyclines March 2005</ref>
'''Minocycline hydrochloride''', also known as '''minocycline''', is a member of the broad spectrum  [[tetracycline antibiotics]], and has a broader spectrum than the other members. It is a [[bacteriostatic]] antibiotic.  As a result of its long half-life it generally has [[blood plasma|serum]] levels 2-4 times that of most other tetracyclines (150 mg giving 16 times the activity levels compared to 250 mg of [[tetracycline]]  at 24-48 hours). Minocycline was originally discovered by [[American Cyanamid|Lederle Laboratories]] and marketed under the brand name ''Minocin''.<ref>[http://www.scripps.edu/chem/baran/images/grpmtgpdf/Lin_Mar_05revised.pdf]Lin, DW The Tetracyclines March 2005</ref>
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[[Category:Tetracycline antibiotics]]
[[Category:Tetracycline antibiotics]]
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Revision as of 17:27, 9 August 2012

Minocycline
Clinical data
Routes of
administration		oral
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
Pharmacokinetic data
Bioavailability100%
Metabolismliver
Elimination half-life11-22 hours
Excretionmostly fecal, rest renal
Identifiers
CAS Number
PubChem CID
DrugBank
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC23H27N3O7
Molar mass457.477

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Minocycline hydrochloride, also known as minocycline, is a member of the broad spectrum tetracycline antibiotics, and has a broader spectrum than the other members. It is a bacteriostatic antibiotic. As a result of its long half-life it generally has serum levels 2-4 times that of most other tetracyclines (150 mg giving 16 times the activity levels compared to 250 mg of tetracycline at 24-48 hours). Minocycline was originally discovered by Lederle Laboratories and marketed under the brand name Minocin.[1]

Indications

It is primarily used to treat acne and other skin infections as the one pill twice daily 100 mg dosage is far easier for patients than the four times a day required with tetracycline or oxytetracycline.

Although minocycline's broader spectrum of activity, compared to other members of the group, includes activity against Neisseria meningitidis, its use as a prophylaxis is no longer recommended because of side effects (dizziness and vertigo).

It may be used to treat certain strains of MRSA infection and disease caused by drug resistant Acinetobacter.

For other uses of minocycline see Tetracycline antibiotics and oxytetracycline as the uses are much the same between Tetracyclines with only minor exceptions.

Cautions

Contrary to all the other tetracycline antibiotics (Doxycyclin excluded), minocycline may be used in renal impairment, but may be aggravating systemic lupus erythematosus.[2]

Also, more so than other tetracyclines, minocycline can cause the rare condition of secondary intracranial hypertension which has initial symptoms of headache, visual disturbances, and confusion. Meningitis and cerebral edema are rare side effects of minocycline.[3]

Minocycline, like all tetracyclines, becomes dangerous past its expiration date. 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 kidneys.

Minocycline's absorption is impaired if taken at the same time of day as calcium or iron supplements. Unlike some of the other tetracycline group antibiotics, it can be taken with calcium rich foods such as milk, although this does reduce the absorption slightly (by ~5%).[citation needed]

Side effects

This medication may cause upset stomach, diarrhea, dizziness, unsteadiness, drowsiness, headache or vomiting. If these symptoms persist or worsen, one should notify their doctor. Minocycline increases sensitivity to sunlight. Prolonged sun exposure should be avoided. Wear protective clothing and use a sunscreen if needed. Very unlikely but should be reported: fever, yellowing of the eyes or skin, stomach pain, sore throat, vision changes and mental changes.

In those cases where this drug must be used for extended periods, blue-gray skin discoloration may occur. In the unlikely event one has an allergic reaction to this drug, immediate medical attention should be sought. Symptoms of an allergic reaction include rash, itching, swelling, severe dizziness, trouble breathing. Other effects not listed above should be reported to the doctor or pharmacist.

Uses

Anti-inflammatory and neuroprotective

Current research is examining the possible neuroprotective and anti-inflammatory effects of minocycline against progression of a group of neurodegenerative disorders including multiple sclerosis (MS), rheumatoid arthritis (RA), amyotrophic lateral sclerosis (ALS), Huntington's disease, and Parkinsons disease,[4] amongst others neurodegenerative diseases.[5][6][7]

The neuroprotective action of minocycline may include its inhibitory effect on 5-lipoxygenase,[8] an inflammatory enzyme associated with brain aging, and is being studied for use in Alzheimer's disease patients.[9] It also has been used as a "last ditch" treatment for toxoplasmosis in AIDS patients. Minocycline is neuroprotective in mouse models of amyotrophic lateral sclerosis (ALS) and Huntington's disease and has been recently shown to stabilize the course of Huntington's disease in humans over a 2-year period.

As an anti-inflammatory, minocycline inhibits apoptosis (cell death) via attenuation of TNF-alpha, downregulating pro-inflammatory cytokine output. This effect is mediated by a direct action of minocycline 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 .[10] Minocycline also inhibits microglial activation, through blockade of NF-kappa B nuclear translocation.

It is thought that minocycline exerts neuroprotective effects independent of its anti-inflammatory properties.[11]

A recent study reported the impact of the antibiotic minocycline on clinical and magnetic resonance imaging (MRI) outcomes and serum immune molecules in MS patients over 24 months of open-label minocycline treatment. Despite a moderately high pretreatment relapse rate in patients in the study prior to treatment, no relapses occurred between months 6 and 24. 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 vascular 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.[12][13][11][14]

Trade names and availability

Minocycline is no longer covered by patent and is therefore marketed under several trade names:

  • Minomycin
  • Minocin
  • Arestin
  • Akamin
  • Aknemin
  • Solodyn
  • Dynacin
  • Sebomin

StoneBridge Pharma also markets Minocycline as Cleeravue-M in combination with SteriLid eyelid cleanser in the treatment of rosacea blepharitis.

Footnotes

  1. ↑ [1]Lin, DW The Tetracyclines March 2005
  2. ↑ Gough A, Chapman S, Wagstaff K, Emery P, Elias E (1996). "Minocycline induced autoimmune hepatitis and systemic lupus erythematosus-like syndrome". BMJ. 312 (7024): 169–72. PMID 8563540.
  3. ↑ Lefebvre N, Forestier E, Farhi D; et al. (2007). "Minocycline-induced hypersensitivity syndrome presenting with meningitis and brain edema: a case report". Journal of Medical Case Reports. 1: 22.
  4. ↑ "Preliminary Study Shows Creatine and Minocycline May Warrant Further Study In Parkinson's Disease" (Press release). National Institute of Health. February 23, 2006.
  5. ↑ Chen M, Ona VO, Li M, Ferrante RJ, Fink KB, Zhu S, Bian J, Guo L, Farrell LA, Hersch SM, Hobbs W, Vonsattel JP, Cha JH, Friedlander RM (2000). "Minocycline inhibits caspase-1 and caspase-3 expression and delays mortality in a transgenic mouse model of Huntington disease". Nat Med. 6 (7): 797–801. PMID 10888929.
  6. ↑ Tikka TM, Koistinaho JE (2001). ["Minocycline provides neuroprotection against N-methyl-D-aspartate neurotoxicity by inhibiting microglia" Check |url= value (help). J Immunol. 166 (12): 7527–33. PMID 11390507.
  7. ↑ Nirmalananthan N, Greensmith L (2005). "Amyotrophic lateral sclerosis: recent advances and future therapies". Curr. Opin. Neurol. 18 (6): 712–9. PMID 16280684.
  8. ↑ Song Y, Wei EQ, Zhang WP, Zhang L, Liu JR, Chen Z (2004). "Minocycline protects PC12 cells from ischemic-like injury and inhibits 5-lipoxygenase activation". Neuroreport. 15 (14): 2181–4. PMID 15371729.
  9. ↑ Uz T, Pesold C, Longone P, Manev H (1998). "Aging-associated up-regulation of neuronal 5-lipoxygenase expression: putative role in neuronal vulnerability". FASEB J. 12 (6): 439–49. PMID 9535216.
  10. ↑ Giuliani F, Hader W, Yong VW (2005). "Minocycline attenuates T cell and microglia activity to impair cytokine production in T cell-microglia interaction". J. Leukoc. Biol. 78 (1): 135–43. doi:10.1189/jlb.0804477. PMID 15817702.
  11. ↑ 11.0 11.1 Maier K, Merkler D, Gerber J, Taheri N, Kuhnert AV, Williams SK, Neusch C, Bähr M, Diem R (2007). "Multiple neuroprotective mechanisms of minocycline in autoimmune CNS inflammation". Neurobiol. Dis. 25 (3): 514–25. doi:10.1016/j.nbd.2006.10.022. PMID 17239606.
  12. ↑ Zabad RK, Metz LM, Todoruk TR, Zhang Y, Mitchell JR, Yeung M, Patry DG, Bell RB, Yong VW (2007). "The clinical response to minocycline in multiple sclerosis is accompanied by beneficial immune changes: a pilot study". Mult. Scler. 13 (4): 517–26. doi:10.1177/1352458506070319. PMID 17463074.
  13. ↑ Zemke D, Majid A (2004). "The potential of minocycline for neuroprotection in human neurologic disease". Clinical neuropharmacology. 27 (6): 293–8. PMID 15613934.
  14. ↑ Popovic N, Schubart A, Goetz BD, Zhang SC, Linington C, Duncan ID (2002). "Inhibition of autoimmune encephalomyelitis by a tetracycline". Ann. Neurol. 51 (2): 215–23. PMID 11835378.

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