Tìm theo
Minocycline
Các tên gọi khác (6 ) :
  • (4S,4AS,5ar,12as)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
  • 7-Dimethylamino-6-demethyl-6-deoxytetracycline
  • Minociclina
  • Minociclinum
  • Minocyclin
  • Minocyclinum
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 10118-90-8
ATC: A01AB23, J01AA08
ĐG : AAIPharma Inc. , http://www.aaipharma.com
CTHH: C23H27N3O7
PTK: 457.4764
A tetracycline analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant staphylococcus infections. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H27N3O7
Phân tử khối
457.4764
Monoisotopic mass
457.184900233
InChI
InChI=1S/C23H27N3O7/c1-25(2)12-5-6-13(27)15-10(12)7-9-8-11-17(26(3)4)19(29)16(22(24)32)21(31)23(11,33)20(30)14(9)18(15)28/h5-6,9,11,17,27,29-30,33H,7-8H2,1-4H3,(H2,24,32)/t9-,11-,17-,23-/m0/s1
InChI Key
InChIKey=DYKFCLLONBREIL-KVUCHLLUSA-N
IUPAC Name
(4S,4aS,5aR,12aS)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
Traditional IUPAC Name
minocycline
SMILES
[H][C@@]12CC3=C(C(O)=CC=C3N(C)C)C(=O)C1=C(O)[C@]1(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@]1([H])C2
Độ hòa tan
5.2E+004 mg/L (at 25 °C)
logP
0.05
logS
-2.2
pKa (strongest acidic)
-2.3
pKa (Strongest Basic)
8.25
PSA
164.63 Å2
Refractivity
122.54 m3·mol-1
Polarizability
45.9 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
9
H Bond Donor Count
5
Physiological Charge
-1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : A tetracycline analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant staphylococcus infections. [PubChem] 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.
Dược Động Học :
▧ Absorption :
Rapidly absorbed from the gastrointestinal tract and absorption is not significantly impaired by ingestion of food or milk. Oral bioavailability is 100%.
▧ Protein binding :
55% to 76%
▧ Metabolism :
Hepatic.
▧ Half Life :
11-22 hours
Độc Tính : 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)
Chỉ Định : 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.
Tương Tác Thuốc :
  • 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
  • Benzylpenicillin Possible antagonism of action
  • Bexarotene Tetracycline derivatives like minocycline may enhance the adverse/toxic effect of Retinoic Acid Derivatives. Due to the risk of developing pseudotumor cerebri (also known as intracranial hypertension), avoid this combination of drugs if possible. If used concomitantly, monitor for evidence of this interaction (eg, dizziness, diplopia, headache).
  • Bismuth Subsalicylate Formation of non-absorbable complexes
  • Calcium Formation of non-absorbable complexes
  • Calcium Acetate Calcium salts such as calcium acetate may decrease the serum concentration of tetracycline derivatives such as minocycline. In general, the coadministration of oral calcium salts and oral tetracycline derivatives should be avoided. Interactions may be able to be minimized by administering oral calcium preparations several hours before or after the dose of the oral tetracycline derivatives. Even with dose separation, therapy may still be compromised. Monitor for decreased therapeutic effect of oral tetracycline derivatives.
  • Calcium Chloride Calcium salts such as calcium chloride may decrease the serum concentration of tetracycline derivatives such as minocycline. In general, the coadministration of oral calcium salts and oral tetracycline derivatives should be avoided. Interactions may be able to be minimized by administering oral calcium preparations several hours before or after the dose of the oral tetracycline derivatives. Even with dose separation, therapy may still be compromised. Monitor for decreased therapeutic effect of oral tetracycline derivatives.
  • Carbenicillin Possible antagonism of action
  • Clavulanate Possible antagonism of action
  • Cloxacillin Possible antagonism of action
  • Colesevelam Bile acid sequestrants such as colesevelam may decrease the absorption of Tetracycline Derivatives. Monitor for decreased therapeutic effects of tetracycline derivatives if coadministered with a bile acid sequestrant. If these agents are used concomitantly, separate doses 2 or more hours to minimize the interaction. The manufacturer of colesevelam suggests that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
  • Cyclacillin Possible antagonism of action
  • Dicloxacillin Possible antagonism of action
  • Dicoumarol 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 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
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aknemin
  • Công ty :
    Sản phẩm biệt dược : Apo-Minocycline
  • Công ty :
    Sản phẩm biệt dược : Arestin
  • Công ty :
    Sản phẩm biệt dược : Dynacin
  • Công ty :
    Sản phẩm biệt dược : Klinomycin
  • Sản phẩm biệt dược : Minocin
  • Công ty :
    Sản phẩm biệt dược : Minoderm
  • Công ty :
    Sản phẩm biệt dược : Minomycin
  • Công ty :
    Sản phẩm biệt dược : Minopen
  • Công ty :
    Sản phẩm biệt dược : Minox
  • Công ty :
    Sản phẩm biệt dược : Minoz
  • Công ty :
    Sản phẩm biệt dược : Solodyn
  • Công ty :
    Sản phẩm biệt dược : Vectrin
  • Công ty :
    Sản phẩm biệt dược : Ximino
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01017
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07225
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05045
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50046515
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0781-5385-31
PharmGKB
http://www.pharmgkb.org/drug/PA450519
Wikipedia
http://en.wikipedia.org/wiki/Minocycline
RxList
http://www.rxlist.com/cgi/generic/minocycline.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/min1270.shtml
Drugs.com
http://www.drugs.com/minocycline.html
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