用户名： 密   码：
注册 | 忘记密码？
药品详细

Minocycline (美满 )

化学结构式图
中文名
美满
英文名
Minocycline
分子式
Not Available
化学名
(2E,4S,4aS,5aR,12aS)-2-[amino(hydroxy)methylidene]-4,7-bis(dimethylamino)-10,11,12a-trihydroxy-1,2,3,4,4a,5,5a,6,12,12a-decahydrotetracene-1,3,12-trione
分子量
Average: 457.4764
Monoisotopic: 457.184900233
CAS号
10118-90-8
ATC分类
A01A 未知;J01A 未知
药物类型
small molecule
阶段
商品名
Alti-Minocycline;Apo-Minocycline;Arestin;Dynacin;Gen-Minocycline;Klinomycin;Minociclina [INN-Spanish];Minocin;Minocyclin;Minocycline HCl;Minocyclinum [INN-Latin];Minocyn;Minomycin;Novo-Minocycline;Solodyn;Vectrin;
同义名
minocycline;
基本介绍

A tetracycline analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant staphylococcus infections. [PubChem]

生产厂家
  • Aurobindo pharma ltd
  • Barr laboratories inc
  • Dr reddys laboratories ltd
  • Impax laboratories inc
  • Lederle laboratories div american cyanamid co
  • Matrix laboratories ltd
  • Medicis pharmaceutical corp
  • Medicis Pharmaceutical Corporation
  • Orapharma inc
  • Ranbaxy laboratories ltd
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Triax pharmaceuticals llc
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Link
  2. Link
  3. Gough A, Chapman S, Wagstaff K, Emery P, Elias E: Minocycline induced autoimmune hepatitis and systemic lupus erythematosus-like syndrome. BMJ. 1996 Jan 20;312(7024):169-72. Pubmed
  4. 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: Minocycline inhibits caspase-1 and caspase-3 expression and delays mortality in a transgenic mouse model of Huntington disease. Nat Med. 2000 Jul;6(7):797-801. Pubmed
  5. Tikka TM, Koistinaho JE: Minocycline provides neuroprotection against N-methyl-D-aspartate neurotoxicity by inhibiting microglia. J Immunol. 2001 Jun 15;166(12):7527-33. Pubmed
  6. Nirmalananthan N, Greensmith L: Amyotrophic lateral sclerosis: recent advances and future therapies. Curr Opin Neurol. 2005 Dec;18(6):712-9. Pubmed
  7. Song Y, Wei EQ, Zhang WP, Zhang L, Liu JR, Chen Z: Minocycline protects PC12 cells from ischemic-like injury and inhibits 5-lipoxygenase activation. Neuroreport. 2004 Oct 5;15(14):2181-4. Pubmed
剂型
Form Route Strength
Capsule Oral
规格
Unit description Cost Unit
Minocin PAC 100 mg Kit Box 695.5 USD box
Minocin kit 100 mg combo 668.17 USD kit
Minocin kit 50 mg combo 334.78 USD kit
Minocin 100 mg vial 59.64 USD vial
Arestin 1 mg microsphere 30.0 USD each
Solodyn 135 mg 24 Hour tablet 24.89 USD tablet
Solodyn 45 mg 24 Hour tablet 24.89 USD tablet
Solodyn 65 mg 24 Hour tablet 24.89 USD tablet
Solodyn 90 mg 24 Hour tablet 24.89 USD tablet
Solodyn er 115 mg tablet 23.93 USD tablet
Solodyn er 135 mg tablet 23.93 USD tablet
Solodyn er 45 mg tablet 23.93 USD tablet
Solodyn er 65 mg tablet 23.93 USD tablet
Solodyn er 90 mg tablet 23.93 USD tablet
Minocycline hcl powder 21.0 USD g
Minocycline HCl 135 mg 24 Hour tablet 19.21 USD tablet
Minocycline HCl 45 mg 24 Hour tablet 19.21 USD tablet
Dynacin 100 mg tablet 13.37 USD tablet
Dynacin 75 mg tablet 13.12 USD tablet
Minocin 100 mg capsule 12.05 USD capsule
Minocin 100 mg pelletized cap 11.11 USD pellet
Dynacin 50 mg tablet 8.76 USD tablet
Dynacin 75 mg capsule 7.15 USD capsule
Minocycline hcl 100 mg tablet 6.15 USD tablet
Minocin 50 mg pelletized cap 5.56 USD pellet
Minocin 50 mg capsule 5.24 USD capsule
Minocycline hcl 75 mg tablet 5.14 USD tablet
Dynacin 50 mg capsule 3.85 USD capsule
Minocycline HCl 100 mg capsule 3.53 USD capsule
Minocycline hcl 50 mg tablet 3.5 USD tablet
Minocycline HCl 75 mg capsule 2.06 USD capsule
Minocycline 75 mg capsule 1.98 USD capsule
Minocycline HCl 50 mg capsule 1.77 USD capsule
Minocin 100 mg Capsule 1.34 USD capsule
Apo-Minocycline 100 mg Capsule 1.08 USD capsule
Minocycline 100 mg Capsule 1.08 USD capsule
Mylan-Minocycline 100 mg Capsule 1.08 USD capsule
Novo-Minocycline 100 mg Capsule 1.08 USD capsule
Pms-Minocycline 100 mg Capsule 1.08 USD capsule
Ratio-Minocycline 100 mg Capsule 1.08 USD capsule
Sandoz Minocycline 100 mg Capsule 1.08 USD capsule
Minocin 50 mg Capsule 0.69 USD capsule
Apo-Minocycline 50 mg Capsule 0.56 USD capsule
Minocycline 50 mg Capsule 0.56 USD capsule
Mylan-Minocycline 50 mg Capsule 0.56 USD capsule
Novo-Minocycline 50 mg Capsule 0.56 USD capsule
Pms-Minocycline 50 mg Capsule 0.56 USD capsule
Ratio-Minocycline 50 mg Capsule 0.56 USD capsule
Sandoz Minocycline 50 mg Capsule 0.56 USD capsule
化合物类型
Type small molecule
Classes
  • Tetracyclines
Substructures
  • Tetracyclines
  • Hydroxy Compounds
  • Benzyl Alcohols and Derivatives
  • Naphthalenes
  • Phenols and Derivatives
  • Amino Ketones
  • Aliphatic and Aryl Amines
  • Phenylpropenes
  • Benzene and Derivatives
  • Aminophenols and Derivatives
  • Alcohols and Polyols
  • Aromatic compounds
  • Cinnamaldehydes
  • Ketenes and Derivatives
  • Phenyl Esters
  • Anilines
  • Enols
  • Ketones
适应症
antibacterials 抗细菌;
药理
Indication For the treatment of infections caused by susceptible strains of microorganisms, such as Rocky Mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsial pox and tick fevers caused by Rickettsiae, upper respiratory tract infections caused by Streptococcus pneumoniae and for the treatment of asymptomatic carriers of Neisseria meningitidis.
Pharmacodynamics Minocycline, the most lipid soluble and most active tetracycline antibiotic, is, like doxycycline, a long-acting tetracycline. Minocycline's effects are related to the inhibition of protein synthesis. 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 recomended because of side effects (dizziness and vertigo). Current research is examining the possible neuroprotective effects of minocycline against progression of Huntington's Disease, an inherited neurodegenerative disorder. The neuroprotective action of minocycline may include its inhibitory effect on 5-lipoxygenase, an inflammatory enzyme associated with brain aging.
Mechanism of action Minocycline passes directly through the lipid bilayer or passively diffuses through porin channels in the bacterial membrane. Tetracyclines like minocycline bind to the 30S ribosomal subunit, preventing the binding of tRNA to the mRNA-ribosome complex and interfering with protein synthesis.
Absorption Rapidly absorbed from the gastrointestinal tract and absorption is not significantly impaired by ingestion of food or milk. Oral bioavailability is 100%.
Volume of distribution Not Available
Protein binding 55% to 76%
Metabolism

Hepatic.
Route of elimination Not Available
Half life 11-22 hours
Clearance Not Available
Toxicity Minocycline has been observed to cause a dark discoloration of the thyroid in experimental animals (rats, minipigs, dogs and monkeys). In the rat, chronic treatment with minocycline has resulted in goiter accompanied by elevated radioactive iodine uptake and evidence of thyroid tumor production. Minocycline has also been found to produce thyroid hyperplasia in rats and dogs. LD50=2380 mg/kg (rat, oral), LD50=3600 mg/kg (mouse, oral)
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways
Pathway Name SMPDB ID
Smp00292 Minocycline Pathway SMP00292
理化性质
Properties
State solid
Melting point Not Available
Experimental Properties
Property Value Source
water solubility 52 mg/mL PhysProp
logP 0.5 PhysProp
Predicted Properties
Property Value Source
water solubility 3.31e+00 g/l ALOGPS
logP 0.30 ALOGPS
logP 0.74 ChemAxon Molconvert
logS -2.14 ALOGPS
pKa 7.83 ChemAxon Molconvert
hydrogen acceptor count 10 ChemAxon Molconvert
hydrogen donor count 5 ChemAxon Molconvert
polar surface area 164.63 ChemAxon Molconvert
rotatable bond count 2 ChemAxon Molconvert
refractivity 131.53 ChemAxon Molconvert
polarizability 45.79 ChemAxon Molconvert
药物相互作用
Drug Interaction
Acenocoumarol The tetracycline, minocycline, may increase the anticoagulant effect of acenocoumarol.
Acitretin Increased risk of intracranial hypertension.
Aluminium Formation of non-absorbable complexes
Amoxicillin Possible antagonism of action
Ampicillin Possible antagonism of action
Anisindione The tetracycline, minocycline, may increase the anticoagulant effect of anisindione.
Attapulgite Formation of non-absorbable complexes
Azlocillin Possible antagonism of action
Aztreonam Possible antagonism of action
Bacampicillin Possible antagonism of action
Bismuth Subsalicylate Formation of non-absorbable complexes
Calcium Formation of non-absorbable complexes
Carbenicillin Possible antagonism of action
Clavulanate Possible antagonism of action
Cloxacillin Possible antagonism of action
Cyclacillin Possible antagonism of action
Dicloxacillin Possible antagonism of action
Dicumarol The tetracycline, minocycline, may increase the anticoagulant effect of dicumarol.
Ethinyl Estradiol This anti-infectious agent could decrease the effect of the oral contraceptive
Etretinate Increased risk of intracranial hypertension
Flucloxacillin Possible antagonism of action
Hetacillin Possible antagonism of action
Iron Formation of non-absorbable complexes
Iron Dextran Formation of non-absorbable complexes
Isotretinoin Increased risk of intracranial hypertension
Magnesium Formation of non-absorbable complexes
Magnesium oxide Formation of non-absorbable complexes
Magnesium salicylate Formation of non-absorbable complexes
Mestranol This anti-infectious agent could decrease the effect of the oral contraceptive
Methicillin Acyl-Serine Possible antagonism of action
Methoxyflurane The tetracycline, minocycline, may increase the renal toxicity of methoxyflurane.
Mezlocillin Possible antagonism of action
Nafcillin Possible antagonism of action
Oxacillin Possible antagonism of action
Penicillin G Possible antagonism of action
Penicillin V Possible antagonism of action
Piperacillin Possible antagonism of action
Pivampicillin Possible antagonism of action
Pivmecillinam Possible antagonism of action
Tazobactam Possible antagonism of action
Ticarcillin Minocycline may reduce the effect of Ticarcillin by inhibiting bacterial growth. Ticarcillin exerts its effects on actively growing bacteria. To achieve synergism, Ticarcillin should be administered at least 2 hours prior to using Minocycline.
Tretinoin Minocycline may increase the adverse effects of oral Tretinoin. Increase risk of pseudotumour cerebri. Concurrent therapy should be avoided.
Trisalicylate-choline Formation of non-absorbable complexes
Warfarin The tetracycline, minocycline, may increase the anticoagulant effect of warfarin.
Zinc Formation of non-absorbable complexes
食物相互作用
  • Calcium and iron needs increased with long term use.
  • Do not take Aluminum or magnesium antacids or supplements while on this medication.
  • Take with food.

返回 | 收藏