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维基百科，自由的百科全书
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Jsjsjs1111/沙盒3
臨床資料
商品名（英语：Drug nomenclature）Cleocin, Daclin
其他名稱7-氯-林可霉素
7-氯-7-脱氧林可霉素
AHFS/Drugs.comMonograph
MedlinePlusa682399
核准狀況
懷孕分級
  • 澳: A
给药途径口服、外用、靜脈注射、陰道內
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度90%（口服）
4–5%（外用）
血漿蛋白結合率95%
药物代谢肝脏
生物半衰期2–3小时
排泄途徑膽汁和腎臟（約20%）
识别信息
  • methyl 7-chloro-6,7,8-trideoxy-6[(4R)-1-methyl-4-propyl-L-prolyl]amino1-thio-L-threo-α-D-galacto-octopyranoside
CAS号18323-44-9  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
化学信息
化学式C18H33ClN2O5S
摩尔质量424.98 g/mol
3D模型（JSmol（英语：JSmol））
  • Cl[C@@H](C)[C@@H](NC(=O)[C@H]1N(C)C[C@H](CCC)C1)[C@H]2O[C@H](SC)[C@H](O)[C@@H](O)[C@H]2O
  • InChI=1S/C18H33ClN2O5S/c1-5-6-10-7-11(21(3)8-10)17(25)20-12(9(2)19)16-14(23)13(22)15(24)18(26-16)27-4/h9-16,18,22-24H,5-8H2,1-4H3,(H,20,25)/t9-,10+,11-,12+,13-,14+,15+,16+,18+/m0/s1 checkY
  • Key:KDLRVYVGXIQJDK-AWPVFWJPSA-N checkY

克林霉素（rINN：Clindamycin，發音： /klɪndəˈmaɪsɪn/）是一种林可酰胺类抗生素。这种药物通常被用于治疗厌氧细菌引起的感染，但有时也可用于治疗一些原生动物感染，如疟疾。它是一種用於痤瘡治療的專門藥，亦於對抗某些抗藥性金黃色葡萄球菌（methicillin-resistant Staphylococcus aureus，縮寫MRSA）見效[1]。

The most severe common adverse effect of clindamycin is Clostridium difficile-associated diarrhea (the most frequent cause of pseudomembranous colitis). Although this side effect occurs with almost all antibiotics, including beta-lactam antibiotics, it is classically linked to clindamycin use.[2]

Clindamycin is marketed under various trade names, including Dalacin, ''Daclin''. Combination products include Duac, BenzaClin, Clindoxyl and Acanya (in combination with benzoyl peroxide), and Ziana (with tretinoin). Clindamycin is also available as a generic drug.

用途

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Clindamycin is used primarily to treat anaerobic infections caused by susceptible anaerobic bacteria, including dental infections,[3] and infections of the respiratory tract, skin and soft tissue infections, and peritonitis.[4] In patients with hypersensitivity to penicillins, clindamycin may be used to treat infections caused by susceptible aerobic bacteria, as well. It is also used to treat bone and joint infections, particularly those caused by Staphylococcus aureus.[4][5] Topical application of clindamycin phosphate can be used to treat mild to moderate acne.[6]

细菌感染

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抗菌谱

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It is most effective against infections involving the following types of organisms:

Most aerobic Gram-negative bacteria (such as Pseudomonas, Legionella, Haemophilus influenzae and Moraxella) are resistant to clindamycin,[7][8] as are the facultative anaerobic Enterobacteriaceae.[9] A notable exception is Capnocytophaga canimorsus, for which clindamycin is a first-line drug of choice.[10]

D检验

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When testing a Gram-positive culture for sensitivity to clindamycin, it is common to perform a "D-Test" to determine if there is a macrolide-resistant sub-population of bacteria present. This test is necessary because some bacteria express a phenotype known as MLSB, in which susceptibility tests will indicate that the bacteria is susceptible to clindamycin, but in vitro the pathogen displays inducible resistance.

To perform this test, an agar plate is inoculated with the bacteria in question and two drug-impregnated disks (one with erythromycin, one with clindamycin) are placed 15-20 mm apart on the plate. If the area of inhibition around the clindamycin disk is "D" shaped, the test result is positive and clindamycin should not be used due to the possibility of resistant pathogens and therapy failure. If the area of inhibition around the clindamycin disk is circular, the test result is negative and clindamycin can be used.[11]

痤疮的联合治疗

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Multiple studies have shown the use of clindamycin in conjunction with benzoyl peroxide, which is available both through prescription or over-the-counter, to be more effective in the treatment of acne than the use of either product by itself.[12][13][14] A single-blind study comparing this combination to adapalene, a retinoid, also found it to work faster and be significantly better tolerated than adapalene, as well as more effective.[15]

Clindamycin and adapalene in combination are also more effective than either drug alone, although adverse effects are more frequent;[16] a single study found pretreatment with adapalene (application of adapalene 3–5 minutes before clindamycin) to significantly increase the penetration of clindamycin into the skin, which may enhance efficacy.[17]

其他

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It can also be useful in skin and soft tissue infections caused by methicillin-resistant Staphylococcus aureus (MRSA);[1] many strains of MRSA are still susceptible to clindamycin; however, in the United States spreading from the West Coast eastwards, MRSA is becoming increasingly resistant.

Clindamycin is used in cases of suspected toxic shock syndrome,[18] often in combination with a bactericidal agent such as vancomycin. The rationale for this approach is a presumed synergy between vancomycin, which causes the death of the bacteria by breakdown of the cell membrane, and clindamycin, which is a powerful inhibitor of toxin synthesis. Both in vitro and in vivo studies have shown that clindamycin reduces the production of exotoxins by staphylococci;[19] it may also induce changes in the surface structure of bacteria that make them more sensitive to immune system attack (opsonization and phagocytosis).[20][21]

Clindamycin has been proven to decrease the risk of premature births in women diagnosed with bacterial vaginosis during early pregnancy to about a third of the risk of untreated women.[22]

寄生虫感染

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疟疾

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Given with chloroquine or quinine, clindamycin is effective and well tolerated in treating Plasmodium falciparum malaria; the latter combination is particularly useful for children, and is the treatment of choice for pregnant women who become infected in areas where resistance to chloroquine is common.[23][24] Clindamycin should not be used as an antimalarial by itself, although it appears to be very effective as such, because of its slow action.[23][24] Patient-derived isolates of Plasmodium falciparum from the Peruvian Amazon have been reported to be resistant to clindamycin as evidenced by in vitro drug susceptibility testing.[25]

其他

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The combination of clindamycin and quinine is the standard treatment for severe babesiosis.[26]

Clindamycin may also be used to treat toxoplasmosis,[7][27][28] and, in combination with primaquine, is effective in treating mild to moderate Pneumocystis jirovecii pneumonia.[29]

剂型

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Clindamycin preparations for oral administration include capsules (containing clindamycin hydrochloride) and oral suspensions (containing clindamycin palmitate hydrochloride).[23] Oral suspension is not favored for administration of clindamycin to children, due to its extremely foul taste and odor. Clindamycin is formulated in a vaginal cream and as vaginal suppositories for treatment of bacterial vaginosis.[22] It is also available for topical administration, in gel form and in a foam delivery system (both containing clindamycin phosphate) and a solution in ethanol (containing clindamycin hydrochloride) and is used primarily as a prescription acne treatment.[12]

Several combination acne treatments containing clindamycin are also marketed, such as single-product formulations of clindamycin with benzoyl peroxide—sold as BenzaClin (Sanofi-Aventis), Duac (a gel form made by Stiefel), and Acanya, among other trade names—and, in the United States, a combination of clindamycin and tretinoin, sold as Ziana.[30] In India, vaginal suppositories containing clindamycin in combination with clotrimazole are manufactured by Olive Health Care and sold as Clinsup-V. In Egypt, vaginal cream containing clindamycin produced by Biopharmgroup sold as Vagiclind indicated for vaginosis.

Clindamycin is available as a generic drug, for both systemic (oral and intravenous) and topical use.[23]

副作用

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Common adverse drug reactions (ADRs) associated with clindamycin therapy — found in over 1% of patients — include: diarrhea, pseudomembranous colitis, nausea, vomiting, abdominal pain or cramps, rash, and/or itch. High doses (both intravenous and oral) may cause a metallic taste, and topical application may cause contact dermatitis.[31][32] Diarrhea, vomiting, and nausea are common if the individual lies down for an extended period of time within 30 minutes of taking clindamycin. In addition, severe heartburn can be expected for up to three days if the individual does not stay in an elevated position for at least 30 minutes.

Pseudomembranous colitis is a potentially lethal condition commonly associated with clindamycin, but which occurs with other antibiotics, as well.[2][33] Overgrowth of Clostridium difficile, which is inherently resistant to clindamycin, results in the production of a toxin that causes a range of adverse effects, from diarrhea to colitis and toxic megacolon.[31]

Rarely — in less than 0.1% of patients — clindamycin therapy has been associated with anaphylaxis, blood dyscrasias, polyarthritis, jaundice, raised liver enzyme levels, and/or hepatotoxicity.[31]

化学性质

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Clindamycin is a semisynthetic derivative of lincomycin, a natural antibiotic produced by the actinobacterium Streptomyces lincolnensis. It is obtained by 7(S)-chloro-substitution of the 7(R)-hydroxyl group of lincomycin.[34][35] The synthesis of clindamycin was first announced by BJ Magerlein, RD Birkenmeyer, and F Kagan on the fifth Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) in 1966.[36] It has been on the market since 1968.[32]

作用机理

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Clindamycin has a bacteriostatic effect. It is a bacterial protein synthesis inhibitor by inhibiting ribosomal translocation,[37] in a similar way to macrolides. It does so by binding to the 50S rRNA of the large bacterial ribosome subunit.[7]

The structures of the complexes between several antibiotics (including clindamycin) and a Deinococcus radiodurans ribosome have been solved by X-ray crystallography by a team from the Max Planck Working Groups for Structural Molecular Biology, and published in the journal Nature.[38]

药物相互作用

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Clindamycin may prolong the effects of neuromuscular-blocking drugs, such as succinylcholine and vecuronium.[39][40][41] Its similarity to the mechanism of action of macrolides and chloramphenicol means they should not be given simultaneously, as this causes antagonism[8] and possible cross-resistance.

兽药用途

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The veterinary uses of clindamycin are quite similar to its human indications, and include treatment of osteomyelitis,[42] skin infections, and toxoplasmosis, for which it is the preferred drug in dogs and cats.[43] Toxoplasmosis rarely causes symptoms in cats, but can do so in very young or immunocompromised kittens and cats.

参考资料

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  1. ^ 1.0 1.1 Daum RS. Clinical practice. Skin and soft-tissue infections caused by methicillin-resistant Staphylococcus aureus. N Engl J Med. 2007, 357 (4): 380–90. PMID 17652653. doi:10.1056/NEJMcp070747. 
  2. ^ 2.0 2.1 Thomas C, Stevenson M, Riley TV. Antibiotics and hospital-acquired Clostridium difficile-associated diarrhoea: a systematic review (PDF). J Antimicrob Chemother. 2003, 51 (6): 1339–50. PMID 12746372. doi:10.1093/jac/dkg254. 
  3. ^ Brook I, Lewis MA, Sándor GK, Jeffcoat M, Samaranayake LP, Vera Rojas J. Clindamycin in dentistry: more than just effective prophylaxis for endocarditis? Oral Surg Oral Med Oral Pathol Oral Radiol Endod. 2005 ;100:550-8
  4. ^ 4.0 4.1 Cleocin I.V. Indications & Dosage. RxList.com. 2007 [2007-12-01]. 
  5. ^ Darley ES, MacGowan AP. Antibiotic treatment of gram-positive bone and joint infections (PDF). J Antimicrob Chemother. 2004, 53 (6): 928–35. PMID 15117932. doi:10.1093/jac/dkh191. 
  6. ^ Feldman S, Careccia RE, Barham KL, Hancox J. Diagnosis and treatment of acne (PDF). Am Fam Physician. 2004, 69 (9): 2123–30. PMID 15152959.  已忽略未知参数|month=（建议使用|date=） (帮助)
  7. ^ 7.0 7.1 7.2 7.3 Lincosamides, Oxazolidinones, and Streptogramins. Merck Manual of Diagnosis and Therapy. Merck & Co. 2005 [2007-12-01].  已忽略未知参数|month=（建议使用|date=） (帮助)
  8. ^ 8.0 8.1 Bell EA. Clindamycin: new look at an old drug. Infectious Diseases in Children. 2005 [2007-12-01].  已忽略未知参数|month=（建议使用|date=） (帮助)
  9. ^ Gold, Howard S.; Robert C. Moellering, Jr. Macrolides and clindamycin. Root, Richard E.; Francis Waldvogel, Lawrence Corey, Walter E. Stamm (编). Clinical infectious diseases: a practical approach. Oxford: Oxford University Press. 1999: 291–7. ISBN 0-19-508103-X.  Retrieved January 19, 2009 through Google Book Search.
  10. ^ Jolivet-Gougeon A, Sixou JL, Tamanai-Shacoori Z, Bonnaure-Mallet M. Antimicrobial treatment of Capnocytophaga infections. Int J Antimicrob Agents. 2007, 29 (4): 367–73. PMID 17250994. doi:10.1016/j.ijantimicag.2006.10.005.  已忽略未知参数|month=（建议使用|date=） (帮助)
  11. ^ Woods, Charles. Macrolide-Inducible Resistance to Clindamycin and the D-Test (PDF). [6/16/2012]. 
  12. ^ 12.0 12.1 Cunliffe WJ, Holland KT, Bojar R, Levy SF. A randomized, double-blind comparison of a clindamycin phosphate/benzoyl peroxide gel formulation and a matching clindamycin gel with respect to microbiologic activity and clinical efficacy in the topical treatment of acne vulgaris. Clin Ther. 2002, 24 (7): 1117–33. PMID 12182256. doi:10.1016/S0149-2918(02)80023-6. 
  13. ^ Leyden JJ, Berger RS, Dunlap FE, Ellis CN, Connolly MA, Levy SF. Comparison of the efficacy and safety of a combination topical gel formulation of benzoyl peroxide and clindamycin with benzoyl peroxide, clindamycin and vehicle gel in the treatments of acne vulgaris. Am J Clin Dermatol. 2001, 2 (1): 33–9. PMID 11702619. doi:10.2165/00128071-200102010-00006. 
  14. ^ Lookingbill DP, Chalker DK, Lindholm JS; et al. Treatment of acne with a combination clindamycin/benzoyl peroxide gel compared with clindamycin gel, benzoyl peroxide gel and vehicle gel: combined results of two double-blind investigations. J Am Acad Dermatol. 1997, 37 (4): 590–5. PMID 9344199. doi:10.1016/S0190-9622(97)70177-4. 
  15. ^ Langner A, Chu A, Goulden V, Ambroziak M. A randomized, single-blind comparison of topical clindamycin + benzoyl peroxide and adapalene in the treatment of mild to moderate facial acne vulgaris. Br J Dermatol. 2008, 158 (1): 122–9. PMID 18047518. doi:10.1111/j.1365-2133.2007.08308.x. 
  16. ^ Wolf JE, Kaplan D, Kraus SJ; et al. Efficacy and tolerability of combined topical treatment of acne vulgaris with adapalene and clindamycin: a multicenter, randomized, investigator-blinded study. J Am Acad Dermatol. 2003, 49 (3 Suppl): S211–7. PMID 12963897. doi:10.1067/S0190-9622(03)01152-6. 
  17. ^ Jain GK, Ahmed FJ. Adapalene pretreatment increases follicular penetration of clindamycin: in vitro and in vivo studies. Indian J Dermatol Venereol Leprol. 2007, 73 (5): 326–9. PMID 17921613. doi:10.4103/0378-6323.34010. 
  18. ^ Annane D, Clair B, Salomon J. Managing toxic shock syndrome with antibiotics. Expert Opin Pharmacother. 2004, 5 (8): 1701–10. PMID 15264985. doi:10.1517/14656566.5.8.1701. 
  19. ^ Coyle EA, Society of Infectious Diseases Pharmacists. Targeting bacterial virulence: the role of protein synthesis inhibitors in severe infections. Insights from the Society of Infectious Diseases Pharmacists. Pharmacotherapy. 2003, 23 (5): 638–42. PMID 12741438. doi:10.1592/phco.23.5.638.32191. 
  20. ^ Gemmell CG, O'Dowd A. Regulation of protein A biosynthesis in Staphylococcus aureus by certain antibiotics: its effect on phagocytosis by leukocytes. J Antimicrob Chemother. 1983, 12 (6): 587–97. PMID 6662837. doi:10.1093/jac/12.6.587. 
  21. ^ Gemmell CG, Peterson PK, Schmeling D; et al. Potentiation of Opsonization and Phagocytosis of Streptococcus pyogenes following Growth in the Presence of Clindamycin. J Clin Invest. 1981, 67 (5): 1249–56. PMC 370690 可免费查阅. PMID 7014632. doi:10.1172/JCI110152. 
  22. ^ 22.0 22.1 Lamont RF. Can antibiotics prevent preterm birth—the pro and con debate. BJOG. 2005, 112 (Suppl 1): 67–73. PMID 15715599. doi:10.1111/j.1471-0528.2005.00589.x. 
  23. ^ 23.0 23.1 23.2 23.3 Lell B, Kremsner PG. Clindamycin as an Antimalarial Drug: Review of Clinical Trials (PDF). Antimicrobial Agents and Chemotherapy. 2002, 46 (8): 2315–20. ISSN 0066-4804. PMC 127356 可免费查阅. PMID 12121898. doi:10.1128/AAC.46.8.2315-2320.2002. 
  24. ^ 24.0 24.1 Griffith KS, Lewis LS, Mali S, Parise ME. Treatment of malaria in the United States: a systematic review (PDF). JAMA. 2007, 297 (20): 2264–77. PMID 17519416. doi:10.1001/jama.297.20.2264. 
  25. ^ Dharia NV, Plouffe D, Bopp SE, González-Páez GE, Lucas C, Salas C, Soberon V, Bursulaya B, Kochel TJ, Bacon DJ, Winzeler EA. Genome scanning of Amazonian Plasmodium falciparum shows subtelomeric instability and clindamycin-resistant parasites. Genome Research. 2010, 20 (11): 1534–44. PMC 2963817 可免费查阅. PMID 20829224. doi:10.1101/gr.105163.110. 
  26. ^ Homer MJ, Aguilar-Delfin I, Telford SR, Krause PJ, Persing DH. Babesiosis (PDF). Clin Microbiol Rev. 2000, 13 (3): 451–69. PMC 88943 可免费查阅. PMID 10885987. doi:10.1128/CMR.13.3.451-469.2000.  已忽略未知参数|month=（建议使用|date=） (帮助)
  27. ^ Pleyer U, Torun N, Liesenfeld O. Okuläre Toxoplasmose [Ocular toxoplasmosis]. Ophthalmologe. 2007, 104 (7): 603–16. PMID 17530262. doi:10.1007/s00347-007-1535-8 （German）. 
  28. ^ Jeddi A, Azaiez A, Bouguila H; et al. Intérêt de la clindamycine dans le traitement de la toxoplasmose oculaire [Value of clindamycin in the treatment of ocular toxoplasmosis]. Journal français d'ophtalmologie. 1997, 20 (6): 418–22. ISSN 0181-5512. PMID 9296037 （French）. 
  29. ^ Fishman JA. Treatment of Infection Due to Pneumocystis carinii (PDF). Antimicrobial Agents and Chemotherapy. 1998, 42 (6): 1309–14. ISSN 0066-4804. PMC 105593 可免费查阅. PMID 9624465.  已忽略未知参数|month=（建议使用|date=） (帮助)
  30. ^ Waknine, Yael. FDA Approvals: Ziana, Kadian, Polyphenon E (free registration required). Medscape Medical News. December 1, 2006 [2007-12-01]. 
  31. ^ 31.0 31.1 31.2 Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006.
  32. ^ 32.0 32.1 Mark C. H. de Groot, Eugène P. van Puijenbroek. Clindamycin and taste disorders. British Journal of Clinical Pharmacology. 2007-10, 64 (4): 542–545 [2019-06-25]. ISSN 0306-5251. PMC 2048568 可免费查阅. PMID 17635503. doi:10.1111/j.1365-2125.2007.02908.x （英语）. 
  33. ^ Starr J. Clostridium difficile associated diarrhoea: diagnosis and treatment. BMJ. 2005, 331 (7515): 498–501. PMC 1199032 可免费查阅. PMID 16141157. doi:10.1136/bmj.331.7515.498. 
  34. ^ Birkenmeyer, R. D.; Kagan, F. Lincomycin. XI. Synthesis and structure of clindamycin, a potent antibacterial agent. Journal of Medicinal Chemistry. 1970, 13 (4): 616–619. PMID 4916317. doi:10.1021/jm00298a007. 
  35. ^ Meyers BR, Kaplan K, Weinstein L. Microbiological and Pharmacological Behavior of 7-Chlorolincomycin. Appl Microbiol. 1969, 17 (5): 653–7. PMC 377774 可免费查阅. PMID 4389137. 
  36. ^ Magerlein, B. J.; Birkenmeyer, R. D.; Kagan, F. Chemical modification of lincomycin. Antimicrobial agents and chemotherapy. 1966, 6: 727–736. PMID 5985307. 
  37. ^ Clindamycin University of Michigan. Retrieved July 31, 2009
  38. ^ Schlünzen F, Zarivach R, Harms J; et al. Structural basis for the interaction of antibiotics with the peptidyl transferase centre in eubacteria. Nature. 2001, 413 (6858): 814–21. PMID 11677599. doi:10.1038/35101544. 
  39. ^ Fogdall RP, Miller RD. Prolongation of a pancuronium-induced neuromuscular blockade by clindamycin. Anesthesiology. 1974, 41 (4): 407–8. PMID 4415332. doi:10.1097/00000542-197410000-00023. 
  40. ^ al Ahdal O, Bevan DR. Clindamycin-induced neuromuscular blockade. Can J Anaesth. 1995, 42 (7): 614–7. PMID 7553999. doi:10.1007/BF03011880. 
  41. ^ Sloan PA, Rasul M. Prolongation of rapacuronium neuromuscular blockade by clindamycin and magnesium (PDF). Anesth Analg. 2002, 94 (1): 123–4, table of contents. PMID 11772813. doi:10.1097/00000539-200201000-00023. 
  42. ^ (February 8, 2005) "Osteomyelitis", in Kahn, Cynthia M., Line, Scott, Aiello, Susan E. (ed.): The Merck Veterinary Manual, 9th ed., John Wiley & Sons. ISBN 0-911910-50-6. Retrieved 14 December 2007.
  43. ^ (February 8, 2005) "Toxoplasmosis: Introduction", in Kahn, Cynthia M., Line, Scott, Aiello, Susan E. (ed.): The Merck Veterinary Manual, 9th ed., John Wiley & Sons. ISBN 0-911910-50-6. Retrieved 14 December 2007.

外部链接

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