用戶:Jsjsjs1111/沙盒3
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臨床資料 | |
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商品名 | Cleocin, Daclin |
其他名稱 | 7-氯-林可黴素 7-氯-7-去氧林可黴素 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682399 |
核准狀況 |
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懷孕分級 |
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給藥途徑 | 口服、外用、靜脈注射、陰道內 |
ATC碼 | |
法律規範狀態 | |
法律規範 |
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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% |
藥物代謝 | 肝臟 |
生物半衰期 | 2–3小時 |
排泄途徑 | 膽汁和腎臟(約20%) |
識別資訊 | |
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CAS號 | 18323-44-9 ![]() |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEMBL | |
化學資訊 | |
化學式 | C18H33ClN2O5S |
摩爾質量 | 424.98 g/mol |
3D模型(JSmol) | |
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克林黴素(rINN:Clindamycin,發音: /klɪndəˈmaɪsɪn/)是一種林可酰胺類抗生素。這種藥物通常被用於治療厭氧細菌引起的感染,但有時也可用於治療一些原生動物感染,如瘧疾。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
[編輯]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]
細菌感染
[編輯]抗菌譜
[編輯]It is most effective against infections involving the following types of organisms:
- Aerobic Gram-positive cocci, including some members of the Staphylococcus and Streptococcus (e.g. pneumococcus) genera, but not enterococci.[7]
- Anaerobic, Gram-negative rod-shaped bacteria, including some Bacteroides, Fusobacterium, and Prevotella, although resistance is increasing in Bacteroides fragilis.
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檢驗
[編輯]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]
痤瘡的聯合治療
[編輯]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
[編輯]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]
寄生蟲感染
[編輯]瘧疾
[編輯]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
[編輯]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]
劑型
[編輯]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
[編輯]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]
化學性質
[編輯]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]
作用機理
[編輯]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]
藥物相互作用
[編輯]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.
獸藥用途
[編輯]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.
參考資料
[編輯]- ^ 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.
- ^ 2.0 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.
- ^ 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
- ^ 4.0 4.1 Cleocin I.V. Indications & Dosage. RxList.com. 2007 [2007-12-01].
- ^ 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.
- ^ Feldman S, Careccia RE, Barham KL, Hancox J. Diagnosis and treatment of acne (PDF). Am Fam Physician. 2004, 69 (9): 2123–30. PMID 15152959. 已忽略未知參數
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- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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
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- ^ 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.
- ^ 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
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. PMID 9624465. 已忽略未知參數
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- ^ 31.0 31.1 31.2 Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006.
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- ^ 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.
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- ^ Magerlein, B. J.; Birkenmeyer, R. D.; Kagan, F. Chemical modification of lincomycin. Antimicrobial agents and chemotherapy. 1966, 6: 727–736. PMID 5985307.
- ^ Clindamycin University of Michigan. Retrieved July 31, 2009
- ^ 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.
- ^ 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.
- ^ al Ahdal O, Bevan DR. Clindamycin-induced neuromuscular blockade. Can J Anaesth. 1995, 42 (7): 614–7. PMID 7553999. doi:10.1007/BF03011880.
- ^ 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.
- ^ (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.
- ^ (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.
外部連結
[編輯]- Clindamycin drug information from Lexi-Comp. Includes dosage information and a comprehensive list of international brand names.(英文)
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