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药品详细

Doxycycline (强力霉素 )

化学结构式图
中文名
强力霉素
英文名
Doxycycline
分子式
Not Available
化学名
(4S,4aR,5S,5aR,6R,12aS)-4-(dimethylamino)-3,5,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
分子量
Average: 444.4346
Monoisotopic: 444.153265754
CAS号
564-25-0
ATC分类
A01A 未知;J01A 未知
药物类型
small molecule
阶段
商品名
Alti-Doxycycline;Apo-Doxy;Atridox;Doryx;Doxy 100;Doxy-Caps;Doxy-Lemmon;Doxychel;Doxychel Hyclate;Doxycin;Doxylin;Doxytec;Jenacyclin;Monodox;Novo-Doxylin;Nu-Doxycycline;Oracea;Periostat;Supracyclin;Vibra-Tabs;Vibramycin;
同义名
Doxcycline anhydrous;Doxycycline Hyclate;Doxycycline Monohydrate;Doxytetracycline;
基本介绍

A synthetic tetracycline derivative with similar antimicrobial activity. Animal studies suggest that it may cause less tooth staining than other tetracyclines. It is used in some areas for the treatment of chloroquine-resistant falciparum malaria (malaria, falciparum). [PubChem]

生产厂家
  • App pharmaceuticals llc
  • Baxter healthcare corp anesthesia and critical care
  • Bedford laboratories div ben venue laboratories inc
  • Collagenex inc
  • Corepharma llc
  • Galderma laboratories lp
  • Halsey drug co inc
  • Heather drug co inc
  • Interpharm inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Lannett holdings inc
  • Larken laboratories inc
  • Mayne pharma international faulding pharm
  • Medicis pharmaceutical corp
  • Mutual pharmacal co
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Pfizer laboratories div pfizer inc
  • Pliva inc
  • Private formulations inc
  • Rachelle laboratories inc
  • Ranbaxy laboratories ltd
  • Ranbaxy pharmaceuticals inc
  • Sandoz inc
  • Superpharm corp
  • Teva pharmaceuticals usa inc
  • Tolmar inc
  • Truxton inc
  • Vintage pharmaceuticals inc
  • Warner chilcott bermuda ltd
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
  • Watson pharmaceuticals inc
  • West ward pharmaceutical corp
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Dahl EL, Shock JL, Shenai BR, Gut J, DeRisi JL, Rosenthal PJ: Tetracyclines specifically target the apicoplast of the malaria parasite Plasmodium falciparum. Antimicrob Agents Chemother. 2006 Sep;50(9):3124-31. Pubmed
  2. Hoerauf A, Mand S, Fischer K, Kruppa T, Marfo-Debrekyei Y, Debrah AY, Pfarr KM, Adjei O, Buttner DW: Doxycycline as a novel strategy against bancroftian filariasis-depletion of Wolbachia endosymbionts from Wuchereria bancrofti and stop of microfilaria production. Med Microbiol Immunol. 2003 Nov;192(4):211-6. Epub 2003 Mar 5. Pubmed
  3. Taylor MJ, Makunde WH, McGarry HF, Turner JD, Mand S, Hoerauf A: Macrofilaricidal activity after doxycycline treatment of Wuchereria bancrofti: a double-blind, randomised placebo-controlled trial. Lancet. 2005 Jun 18-24;365(9477):2116-21. Pubmed
剂型
Form Route Strength
Capsule Oral
Gel, metered Periodontal
Tablet Oral
规格
Unit description Cost Unit
Vibramycin 25 mg/5ml Suspension 60ml Bottle 36.29 USD bottle
Adoxa pak 1-150 mg tablet 19.93 USD tablet
Doryx 150 mg Enteric Coated Tabs 17.51 USD tab
Doryx dr 150 mg tablet 16.83 USD tablet
Doxycycline hyc 100 mg vial 14.16 USD vial
Adoxa 100 mg tablet 13.86 USD tablet
Monodox 100 mg capsule 13.46 USD capsule
Adoxa 75 mg tablet 12.77 USD tablet
Oracea 40 mg Delayed Release Capsule 12.44 USD capsule
Oracea 40 mg capsule 11.96 USD capsule
Avidoxy 100 mg tablet 11.52 USD tablet
Monodox 75 mg capsule 11.02 USD capsule
Doryx 100 mg Enteric Coated Tabs 10.31 USD tab
Doryx dr 100 mg tablet 9.91 USD tablet
Adoxa pak 1-100 mg tablet 9.88 USD tablet
Doxycycline Monohydrate 150 mg tablet 9.51 USD tablet
Adoxa 50 mg tablet 9.29 USD tablet
Doxycycline mono 150 mg tablet 9.13 USD tablet
Doryx 75 mg Enteric Coated Tabs 8.76 USD tab
Doryx dr 75 mg tablet 8.42 USD tablet
Vibramycin 100 mg capsule 6.67 USD capsule
Vibra-tabs 100 mg tablet 6.67 USD tablet
Monodox 50 mg capsule 6.0 USD capsule
Doxycycline mono 100 mg tablet 5.98 USD tablet
Periostat 20 mg tablet 5.75 USD tablet
Doxycycline mono 75 mg tablet 5.74 USD tablet
Doxycycline Monohydrate 100 mg tablet 5.12 USD tablet
Doxycycline mono 50 mg tablet 4.17 USD tablet
Doxycycline Monohydrate 50 mg tablet 3.0 USD tablet
Doxycycline hyclate powder 2.56 USD g
Vibramycin 50 mg capsule 2.41 USD capsule
Doxycycline Monohydrate 100 mg capsule 2.22 USD capsule
Vibramycin 100 mg Capsule 1.91 USD capsule
Doxycycline Monohydrate 50 mg capsule 1.51 USD capsule
Doxycycline hyclate 100 mg tablet 1.28 USD tablet
Doxycycline hyclate 20 mg tablet 1.28 USD tablet
Doxycycline Hyclate 100 mg capsule 1.18 USD capsule
Doxycycline Hyclate 50 mg capsule 0.76 USD capsule
Vibramycin 50 mg/5ml Syrup 0.67 USD ml
Vibramycin 50 mg/5 ml syrup 0.64 USD ml
Apo-Doxy 100 mg Capsule 0.61 USD capsule
Apo-Doxy 100 mg Tablet 0.61 USD tablet
Doxycin 100 mg Capsule 0.61 USD capsule
Doxycin 100 mg Tablet 0.61 USD tablet
Novo-Doxylin 100 mg Capsule 0.61 USD capsule
Novo-Doxylin 100 mg Tablet 0.61 USD tablet
Nu-Doxycycline 100 mg Capsule 0.61 USD capsule
Pms-Doxycycline 100 mg Capsule 0.61 USD capsule
Pms-Doxycycline 100 mg Tablet 0.61 USD tablet
化合物类型
Type small molecule
Classes
  • Tetracyclines
Substructures
  • Tetracyclines
  • Hydroxy Compounds
  • Benzyl Alcohols and Derivatives
  • Naphthalenes
  • Phenols and Derivatives
  • Amino Ketones
  • Phenylpropenes
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Alcohols and Polyols
  • Aromatic compounds
  • Cinnamaldehydes
  • Ketenes and Derivatives
  • Phenyl Esters
  • Enols
  • Ketones
适应症
antibacterials 抗细菌;
药理
Indication Doxycycline is indicated for use in respiratory tract infections caused by Mycoplasma pneumoniae, Haemophilus influenzae, Streptococcus pneumoniae, Legionella spp., or Klebsiella spp. It is also used for prophylaxis of malaria. Doxycycline is indicated for a variety of bacterial infections, from Mycobacterium fortuitum and M. marinum, to susceptible E. coli and Brucella spp. It can be used as an alternative to treating plague, tetanus, Campylobacter fetus
Pharmacodynamics Doxycycline, a long-acting tetracycline derived from oxytetracycline, is used to inhibit bacterial protein synthesis and treat non-gonococcal urethritis and cervicitis, exacerbations of bronchitis in patients with COPD, and adult periodontitis.
Mechanism of action Doxycycline, like minocycline, is lipophilic and can pass through the lipid bilayer of bacteria. Doxycycline reversibly binds to the 30 S ribosomal subunits and possibly the 50S ribosomal subunit(s), blocking the binding of aminoacyl tRNA to the mRNA and inhibiting bacterial protein synthesis. Doxycycline prevents the normal function of the apicoplast of Plasmodium falciparum, a malaria causing organism.
Absorption Completely absorbed following oral administration.
Volume of distribution Not Available
Protein binding >90%
Metabolism

Hepatic
Route of elimination They are concentrated by the liver in the bile and excreted in the urine and feces at high concentrations in a biologically active form.
Half life 18-22 hours
Clearance Not Available
Toxicity Symptoms of overdose include anorexia, nausea, diarrhoea, glossitis, dysphagia, enterocolitis and inflammatory lesions (with monilial overgrowth) in the anogenital region, skin reactions such as maculopapular and erythematous rashes, exfoliative dermatitis, photosensitivity, hypersensitivity reactions such as urticaria, angioneurotic oedema, anaphylaxis, anaphyl-actoid purpura, pericarditis, and exacerbation of systemic lupus erythematosus, benign intracranial hypertension in adults disappearing on discontinuation of the medicine, haematologic abnormalities such as haemolytic anaemia, thrombocytopenia, neutropenia, and eosinophilia. LD50=262 mg/kg (I.P. in rat).
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways
Pathway Name SMPDB ID
Smp00291 Doxycycline Pathway SMP00291
理化性质
Properties
State solid
Melting point 201 oC
Experimental Properties
Property Value Source
water solubility 630 mg/L PhysProp
logP -0.2 PhysProp
logS -2.87 [ADME Research, USCD] PhysProp
Predicted Properties
Property Value Source
water solubility 6.30e-01 g/l ALOGPS
logP -0.72 ALOGPS
logP -3.37 ChemAxon Molconvert
logS -2.85 ALOGPS
pKa 4.79 ChemAxon Molconvert
hydrogen acceptor count 9 ChemAxon Molconvert
hydrogen donor count 6 ChemAxon Molconvert
polar surface area 181.62 ChemAxon Molconvert
rotatable bond count 2 ChemAxon Molconvert
refractivity 113.89 ChemAxon Molconvert
polarizability 42.88 ChemAxon Molconvert
药物相互作用
Drug Interaction
Acenocoumarol The tetracycline, doxycycline, may increase the anticoagulant effect of acenocoumarol.
Acitretin Increased risk of intracranial hypertension
Aluminium Formation of non-absorbable complexes
Amobarbital The anticonvulsant, amobarbital, decreases the effect of doxycycline.
Amoxicillin Possible antagonism of action
Ampicillin Possible antagonism of action
Anisindione The tetracycline, doxycycline, may increase the anticoagulant effect of anisindione.
Aprobarbital The anticonvulsant, aprobarbital, decreases the effect of doxycycline.
Attapulgite Formation of non-absorbable complexes
Azlocillin Possible antagonism of action
Aztreonam Possible antagonism of action
Bacampicillin Possible antagonism of action
Butabarbital The anticonvulsant, butabarbital, decreases the effect of doxycycline.
Butalbital The anticonvulsant, butalbital, decreases the effect of doxycycline.
Butethal The anticonvulsant, butethal, decreases the effect of doxycycline.
Calcium Formation of non-absorbable complexes
Carbamazepine The anticonvulsant, carbamazepine, may decrease the therapeutic effect of doxycycline.
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, doxycycline, may increase the anticoagulant effect of dicumarol.
Dihydroquinidine barbiturate The anticonvulsant, dihydroquinidine barbiturate, decreases the effect of doxycycline.
Ethinyl Estradiol Doxycycline may decrease the contraceptive effect of ethinyl estradiol.
Ethotoin The anticonvulsant, ethotoin, decreases the effect of doxycycline.
Etretinate Increased risk of intracranial hypertension
Flucloxacillin Possible antagonism of action
Fosphenytoin The anticonvulsant, fosphenytoin, decreases the effect of doxycycline.
Heptabarbital The anticonvulsant, heptabarbital, decreases the effect of doxycycline.
Hetacillin Possible antagonism of action
Hexobarbital The anticonvulsant, hexobarbital, decreases the effect of doxycycline.
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
Mephenytoin The anticonvulsant, mephenytoin, decreases the effect of doxycycline.
Mestranol This anti-infectious agent could decrease the effect of the oral contraceptive
Methohexital The anticonvulsant, methohexital, decreases the effect of doxycycline.
Methotrexate The tetracycline, doxycycline, may increase methotrexate toxicity.
Methylphenobarbital The anticonvulsant, methylphenobarbital, decreases the effect of doxycycline.
Meticillin Possible antagonism of action
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
Pentobarbital The anticonvulsant, pentobarbital, decreases the effect of doxycycline.
Phenobarbital The anticonvulsant, phenobarbital, may decrease the therapeutic effect of doxycycline.
Phenytoin The anticonvulsant, phenytoin, may decrease the effect of doxycycline.
Piperacillin Possible antagonism of action
Pivampicillin Possible antagonism of action
Pivmecillinam Possible antagonism of action
Primidone The anticonvulsant, primidone, decreases the effect of doxycycline.
Quinidine barbiturate The anticonvulsant, quinidine barbiturate, decreases the effect of doxycycline.
Rifabutin The rifamycin decreases the effect of doxycycline
Rifampin The rifamycin decreases the effect of doxycycline
Secobarbital The anticonvulsant , secobarbital, decreases the effect of doxycycline.
Talbutal The anticonvulsant, talbutal, decreases the effect of doxycycline.
Tamsulosin Doxycycline, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Doxycycline is initiated, discontinued, or dose changed.
Tazobactam Possible antagonism of action
Thiopental Thiopental may decrease the serum levels of Doxycycline. A reduction in antimicrobial effects may occur. An alternative antibiotic may be considered.
Ticarcillin Doxycycline 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 Doxycycline.
Tolterodine Doxycycline may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
Tretinoin Doxycycline may increase the adverse effects of oral Tretinoin. Increase risk of pseudotumour cerebri. Concurrent therapy should be avoided.
Warfarin The tetracycline, doxycycline, may increase the anticoagulant effect of warfarin.
Zinc Formation of non-absorbable complexes
食物相互作用
  • Avoid alcohol.
  • Avoid milk, calcium containing dairy products, iron, antacids, or aluminum salts 2 hours before or 6 hours after using antacids while on this medication.
  • Take with a full glass of water Do not take calcium, aluminum, magnesium or Iron supplements within 2 hours of taking this medication.

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