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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/03/03 19:19:42」(JST)

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Ceftazidime, sold under the brand names Fortaz among others, is an antibiotic useful for the treatment of a number of bacterial infections. Specifically it is used for joint infections, meningitis, pneumonia, sepsis, urinary tract infections, malignant otitis externa, pseudomonas aeruginosa infection, and vibrio infection. It is given by injection into a vein or muscle.^[1]

Common side effects include nausea, allergic reactions, and pain at the site of injection. Other side effects may include Clostridium difficile diarrhea. It is not recommended in people who have had previous anaphylaxis to a penicillin.^[1] Its use is relatively safe during pregnancy and breastfeeding.^[2] It is in the third-generation cephalosporin family of medications and works by interfering with the bacteria's cell wall.^[1]

Ceftazidime was patented in 1978 and came into commercial use in 1984.^[3] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.^[4] Ceftazidime is available as a generic medication.^[1] The wholesale cost in the developing world is about 2.84 to 16.76 USD per day.^[5] In the United States a course of treatment costs 100 to 200 USD.^[2]

Medical uses

Ceftazidime is used to treat lower respiratory tract, skin, urinary tract, blood-stream, joint, and abdominal infections, and meningitis.^[6] The drug is given intravenously (IV) or intramuscularly (IM) every 8–12 hours (two or three times a day), with dose and frequencing varying by the type of infection, severity, and/or renal function of the patient. Ceftazidime is also commonly prescribed off-label for nebulization in Cystic Fibrosis patients for the suppression of Pseudomonas in the lungs as well as the treatment of pulmonary exacerbations. Those with kidney disease are dosed less frequently.^[6]

Ceftazidime is the first-line treatment for the tropical infection, melioidosis, an important cause of sepsis in Asia and Australia.^[7] ^[8]

Labeled indications include the treatment of patients with:

Pseudomonas aeruginosa infections
other Gram-negative, aerobic infections
neutropenic fever^[9]

As a class, cephalosporins have activity against Gram-positive and Gram-negative bacteria. The balance of activity tips toward Gram-positive organisms for earlier generations; later generations of cephalosporins have more Gram-negative coverage. Ceftazidime is one of the few in this class with activity against Pseudomonas. It is not active against methicillin-resistant Staphylococcus aureus.

Spectrum of activity

Clinically relevant organisms against which ceftazidime has activity include:

Gram-negative aerobes, such as Enterobacter, E. coli, H. influenzae, Klebsiella, Proteus, Pseudomonas, and N. meningitidis
Gram-positive aerobes, such as group B streptococci, Streptococcus pneumoniae, and Streptococcus pyogenes
Anaerobes, such as Bacteroides^[6]

The following represents MIC susceptibility data for a few clinically significant pathogens:

Escherichia coli - 0.015 µg/mL - 512 µg/mL
Pseudomonas aeruginosa - ≤0.03 µg/mL - 1024 µg/mL ^[10]

Side effects

Ceftazidime is generally well-tolerated. When side effects do occur, they are most commonly local effects from the intravenous line site, allergic reactions, and gastrointestinal symptoms. According to one manufacturer, in clinical trials, allergic reactions including itching, rash, and fever, happened in fewer than 2% of patients. Rare but more serious allergic reactions, such as toxic epidermal necrolysis, Stevens-Johnson syndrome, and erythema multiforme, have been reported with this class of antibiotics, including ceftazidime. Gastrointestinal symptoms, including diarrhea, nausea, vomiting, and abdominal pain, were reported in fewer than 2% of patients.^[6]

Another source reported, in addition, blood tests of patients may show increased eosinophils (8%), increased lactate dehydrogenase (6%), increased gamma-glutamyl transferase (5%), positive direct Coombs test (4%), increased platelets (thrombocythemia) (2%), increased ALT (7%), increased AST (6%), or increased alkaline phosphatase (4%).^[9]

Contraindications

Ceftazidime is contraindicated in people with a known allergy to ceftazidime or to any other cephalosporin antibiotic.^[6]

Precautions

Ceftazidime is mainly eliminated by the kidneys into the urine. As such, drug levels in the blood may build up in persons with kidney injury or kidney disease. This includes those on dialysis. In these cases of renal impairment, the drug is dosed less frequently.^[9] No dose adjustment is needed for those with liver disease.

Pregnancy

Ceftazidime falls under the pregnancy category B.^[9] According to the manufacturer, research studies in mice and rats showed no evidence of harm to the fetus, even at up to 40 times the human dose of ceftazidime. Importantly, though, no high-quality research studies of the effects of the drug in pregnant women were conducted.^[6]

Mechanism of action

Third-generation cephalosporins differ from earlier generations in the presence of a C=N-OCH₃ group in their chemical structure (cefuroxime & Cefuzonam also bear this functional group but are only listed as class II). This group provides improved stability against certain beta-lactamase enzymes produced by Gram-negative bacteria. These bacterial enzymes rapidly destroy earlier-generation cephalosporins by breaking open the drug's beta-lactam chemical ring, leading to antibiotic resistance. Though initially active against these bacteria, with widespread use of third-generation cephalosporins, some Gram-negative bacteria known as extended-spectrum beta-lactamases (ESBLs) are even able to inactivate the third-generation cephalosporins. Infections caused by ESBL-producing Gram-negative bacteria are of particular concern in hospitals and other healthcare facilities.^[11]

Chemistry

In addition to the syn-configuration of the imino side chain, compared to other third-generation cephalosporins, the more complex moiety (containing two methyl and a carboxylic acid group) confers extra stability to β-lactamase enzymes produced by many Gram-negative bacteria. The extra stability to β-lactamases increases the activity of ceftazidime against otherwise resistant Gram-negative organisms including Pseudomonas aeruginosa. The charged pyridinium moiety increases water-solubility. Ceftazidime shares the same variable R-group side chain with aztreonam, a monobactam antibiotic; the two drugs share a similar spectrum of activity, including activity against Pseudomonas.

References

^ ^a ^b ^c ^d ^e "Ceftazidime". The American Society of Health-System Pharmacists. Retrieved 8 December 2016.
^ ^a ^b Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 87. ISBN 9781284057560.
^ Fischer, Janos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 495. ISBN 9783527607495.
^ "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Retrieved 8 December 2016.
^ "Ceftazidime". International Drug Price Indicator Guide. Retrieved 8 December 2016.
^ ^a ^b ^c ^d ^e ^f Ceftazidime for Injection(R) [package insert]. Schaumburg, IL: Sagent; 2012. PDF of insert
^ White NJ (2003). "Melioidosis". Lancet. 361 (9370): 1715–722. doi:10.1016/S0140-6736(03)13374-0. PMID 12767750.
^ White, N. J.; Dance, D. A.; Chaowagul, W; Wattanagoon, Y; Wuthiekanun, V; Pitakwatchara, N (1989). "Halving of mortality of severe melioidosis by ceftazidime". Lancet. 2 (8665): 697–701. doi:10.1016/S0140-6736(89)90768-X. PMID 2570956.
^ ^a ^b ^c ^d Lexicomp Online, Lexi-Drugs, Hudson, Ohio: Lexi-Comp, Inc.; 2014; April 20, 2014. http://online.lexi.com/lco/action/doc/retrieve/docid/patch_f/6560
^ http://www.toku-e.com/Assets/MIC/Ceftazidime%20pentahydrate.pdf
^ Sharma M, Pathak S, Srivastava P (October 2013). "Prevalence and antibiogram of Extended Spectrum β-Lactamase (ESBL) producing Gram negative bacilli and further molecular characterization of ESBL producing Escherichia coli and Klebsiella spp". J Clin Diagn Res. 7 (10): 2173–7. doi:10.7860/JCDR/2013/6460.3462. PMC 3843424. PMID 24298468.

English Journal

Gas production of three brands of ceftazidime.

Stiles ML1, Allen LV Jr, Fox JL.
American journal of hospital pharmacy.Am J Hosp Pharm.1991 Aug;48(8):1727-9.
PMID 1910261

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Name: Vazone 1g: Cefoperazone 0.5g + Sulbactum 0.5g Antibiotics Ceftazidime Injection - Pictures ceftazidime injection - patient information, description, dosage and directions. NurseReview.Org - Antibiotics Updates (advanced pharmacology for nurs…

★リンクテーブル★

リンク元	「セフタジジム」
関連記事	「ceptaz」

「セフタジジム」

Ceftazidime
Clinical data
Pronunciation	/sɛfˈtæzᵻdiːm/
Trade names	Fortaz, Tazicef, others
AHFS/Drugs.com	Monograph
MedlinePlus	a686007
Pregnancy; category	AU: B1; US: B (No risk in non-human studies); ;
Routes of; administration	intravenous, intramuscular, inhalation (off-label only)
ATC code	J01DD02 (WHO);
Legal status
Legal status	AU: S4 (Prescription only);
Pharmacokinetic data
Bioavailability	91% (IM)
Metabolism	negligible
Biological half-life	1.6–2 hours
Excretion	90–96% kidney
Identifiers
	IUPAC name (6R,7R,Z)-7-(2-(2-aminothiazol-4-yl)-2-(2-carboxypropan-2-yloxyimino)acetamido)-8-oxo-3-(pyridinium-1-ylmethyl)-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate;
CAS Number	72558-82-8 ;
PubChem CID	5481173;
DrugBank	DB00438 ;
ChemSpider	4587145 ;
UNII	DZR1ENT301;
ChEBI	CHEBI:3508 ;
ChEMBL	CHEMBL201 ;
ECHA InfoCard	100.112.489
Chemical and physical data
Formula	C22H22N6O7S2
Molar mass	546.58 g/mol
3D model (Jmol)	Interactive image;
	SMILES O=C2N1/C(=C(\CS[C@@H]1[C@@H]2NC(=O)C(=NOC(C(=O)O)(C)C)c3nc(sc3)N)C[n+]4ccccc4)C([O-])=O ;
	InChI InChI=1S/C22H22N6O7S2/c1-22(2,20(33)34)35-26-13(12-10-37-21(23)24-12)16(29)25-14-17(30)28-15(19(31)32)11(9-36-18(14)28)8-27-6-4-3-5-7-27/h3-7,10,14,18H,8-9H2,1-2H3,(H4-,23,24,25,29,31,32,33,34)/b26-13-/t14-,18-/m1/s1 ; Key:ORFOPKXBNMVMKC-DWVKKRMSSA-N ;
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　　[★]

英: ceftazidime, CAZ
商: Fortaz, Ceptaz, Tazicer, Taxidime。セパダシン、モダケミン、モダシン、モベンゾシン
関: セファロスポリン系抗菌薬

抗菌薬

βラクタム系抗菌薬

セファロスポリン系抗菌薬

generation III cephalosporin

抗菌スペクトル

セフォペラゾン cefoperazone、セフタジジム ceftazidimeはセファロスポリン系抗菌薬第三世代のなかで緑膿菌に有効な抗菌薬。

効果・効能

モダシン静注用

適応菌種

本剤に感性のブドウ球菌属、レンサ球菌属、肺炎球菌、大腸菌、シトロバクター属、クレブシエラ属、エンテロバクター属、セラチア属、プロテウス属、モルガネラ・モルガニー、プロビデンシア属、インフルエンザ菌、シュードモナス属、緑膿菌、バークホルデリア・セパシア、ステノトロホモナス（ザントモナス）・マルトフィリア、アシネトバクター属、ペプトストレプトコッカス属、バクテロイデス属、プレボテラ属（プレボテラ・ビビアを除く）

適応症

敗血症、感染性心内膜炎、外傷・熱傷及び手術創等の二次感染、咽頭・喉頭炎、扁桃炎（扁桃周囲炎、扁桃周囲膿瘍を含む）、急性気管支炎、肺炎、肺膿瘍、膿胸、慢性呼吸器病変の二次感染、膀胱炎、腎盂腎炎、前立腺炎（急性症、慢性症）、腹膜炎、胆嚢炎、胆管炎、肝膿瘍、バルトリン腺炎、子宮内感染、子宮付属器炎、子宮旁結合織炎、化膿性髄膜炎、中耳炎、副鼻腔炎

「ceptaz」

　　[★]

同: Fortaz, Ceptaz, Tazicer, Taxidime
関: Ceftazidime

[AHFS2016-1] "Ceftazidime". The American Society of Health-System Pharmacists. Retrieved 8 December 2016.

[Ric2015-2] Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 87. ISBN 9781284057560.

[3] Fischer, Janos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 495. ISBN 9783527607495.

[WHO19th-4] "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Retrieved 8 December 2016.

[ERC2014-5] "Ceftazidime". International Drug Price Indicator Guide. Retrieved 8 December 2016.

[Sagent-6] ^ ^a ^b ^c ^d ^e ^f Ceftazidime for Injection(R) [package insert]. Schaumburg, IL: Sagent; 2012. PDF of insert

[7] White NJ (2003). "Melioidosis". Lancet. 361 (9370): 1715–722. doi:10.1016/S0140-6736(03)13374-0. PMID 12767750.

[8] White, N. J.; Dance, D. A.; Chaowagul, W; Wattanagoon, Y; Wuthiekanun, V; Pitakwatchara, N (1989). "Halving of mortality of severe melioidosis by ceftazidime". Lancet. 2 (8665): 697–701. doi:10.1016/S0140-6736(89)90768-X. PMID 2570956.

[Lexi-9] Lexicomp Online, Lexi-Drugs, Hudson, Ohio: Lexi-Comp, Inc.; 2014; April 20, 2014. http://online.lexi.com/lco/action/doc/retrieve/docid/patch_f/6560

[10] ttp://www.toku-e.com/Assets/MIC/Ceftazidime%20pentahydrate.pdf

[11] Sharma M, Pathak S, Srivastava P (October 2013). "Prevalence and antibiogram of Extended Spectrum β-Lactamase (ESBL) producing Gram negative bacilli and further molecular characterization of ESBL producing Escherichia coli and Klebsiella spp". J Clin Diagn Res. 7 (10): 2173–7. doi:10.7860/JCDR/2013/6460.3462. PMC 3843424. PMID 24298468.

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案内

案内

Ceptaz