药品详细
Probenecid(丙磺舒)
化学结构式图
中文名
丙磺舒
英文名
Probenecid
分子式
C13H19NO4S
化学名
4-(dipropylsulfamoyl)benzoic acid
分子量
Average: 285.359
Monoisotopic: 285.103478791
Monoisotopic: 285.103478791
CAS号
57-66-9
ATC分类
M04A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy. [PubChem]
生产厂家
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Lannett co inc
- Lederle laboratories div american cyanamid co
- Merck and co inc
- Mylan pharmaceuticals inc
- Watson laboratories inc
封装厂家
- Atlantic Biologicals Corporation
- Caremark LLC
- Concord Labs
- Dispensing Solutions
- Kaiser Foundation Hospital
- Lannett Co. Inc.
- Major Pharmaceuticals
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Nucare Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Pharmedix
- Physicians Total Care Inc.
- Prescript Pharmaceuticals
- Rising Pharmaceuticals
- Sandhills Packaging Inc.
- Southwood Pharmaceuticals
- Watson Pharmaceuticals
参考
| Synthesis Reference | Not Available |
| General Reference |
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剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | For the reduction of serum uric acid concentrations in chronic gouty arthritis and tophaceous gout in patients with frequent disabling gout attacks. Has also been effectively used to promote uric acid excretion in hyperuricemia secondary to the administration of thiazide and related diuretics. |
| Pharmacodynamics | Probenecid is a uricosuric and renal tubular blocking agent and is used in combination with colchicine to treat chronic gouty arthritis when complicated by frequent, recurrent acute attacks of gout. It inhibits the reabsorption of urate at the proximal convoluted tubule, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Effective uricosuria reduces the miscible urate pool, retards urate deposition, and promotes resorption of urate deposits. At the proximal and distal tubles, probenecid competitively inhibits the secretion of many weak organic acids including penicillins, most cephalosporins, and some other β-lactam antibiotics. This results in an increase in the plasma concentrations of acidic drugs eliminated principally by renal secretion, but only a slight increase if the drug is eliminated mainly by filtration. Thus, the drug can be used for therapeutic advantages to increase concentrations of certain β-lactam antibiotics in the treatment of gonorrhea, neurosyphilis, or pelvic inflammatory disease (PID). |
| Mechanism of action | Probenecid inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Probenecid may also reduce plasma binding of urate and inhibit renal secretion of uric acid at subtherapeutic concentrations. The mechanism by which probenecid inhibits renal tubular transport is not known, but the drug may inhibit transport enzymes that require a source of high energy phosphate bonds and/or nonspecifically interfere with substrate access to protein receptor sites on the kidney tubules. |
| Absorption | Not Available |
| Volume of distribution | Not Available |
| Protein binding | 75-95% |
| Metabolism |
Not Available
|
| Route of elimination | Excreted principally in the urine as monoacyl glucuronide and unchanged drug. Alkalinization of urine increases renal probenecid excretion. |
| Half life | 6-12 hours |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acetylsalicylic acid | Acetylsalicylic acid decreases the uricosuric effect of probenecid. |
| Bismuth Subsalicylate | The salicylate, bismuth subsalicylate, decreases the uricosuric effect of probenecid. |
| Cefaclor | Probenecid may increase the serum level of cefaclor. |
| Cefadroxil | Probenecid may increase the serum level of cefadroxil. |
| Cefamandole | Probenecid may increase the serum level of cefamandole. |
| Cefazolin | Probenecid may increase the serum level of cefazolin. |
| Cefepime | Probenecid may increase the serum level of cefepime. |
| Cefixime | Probenecid may increase the serum level of cefixime. |
| Cefmetazole | Probenecid may increase the serum level of cefmatzole. |
| Cefonicid | Probenecid may increase the serum level of cefonicib. |
| Cefotaxime | Probenecid may increase the serum level of cefotaxime. |
| Cefotetan | Probenecid may increase the serum level of cefotetan. |
| Cefoxitin | Probenecid may increase the serum level of cefoxitin. |
| Cefprozil | Probenecid may increase the serum level of cefprozil. |
| Cefradine | Probenecid may increase the serum level of cefradine. |
| Ceftizoxime | Probenecid may increase the serum level of ceftizoxime. |
| Cefuroxime | Probenecid may increase the serum level of cefuroxime. |
| Cephalexin | Probenecid may increase the serum level of cephalexin. |
| Cephaloglycin | Probenecid may increase the serum level of cephaloglycin. |
| Cephalothin Group | Probenecid may increase the serum level of cephalothin. |
| Diflunisal | Probenecid increases toxicity of diflunisal |
| Ganciclovir | Probenecid increases the effect and toxicity of ganciclovir/valganciclovir |
| Glycerol Phenylbutyrate | Probenecid may inhibit the renal excretion of metabolites of glycerol phenylbutyrate including PAGN and PAA. |
| Indomethacin | Probenecid increases the effect/toxicity of indomethacin |
| Ketorolac | Probenecid increases toxicity of ketorolac |
| Loracarbef | Probenecid may increase the serum level of loracarbef. |
| Magnesium salicylate | The salicylate, magnesium salicylate, decreases the uricosuric effect of probenecid. |
| Methotrexate | Probenecid increases the effect and toxicity of methotrexate |
| Moxalactam Derivative | Probenecid may increase the serum level of the moxalactam derivative. |
| Pralatrexate | Decreases renal clearance of pralatrexate thus increasing exposure. Monitor for adverse effects. |
| Salicylate-sodium | The salicylate, salicylate-sodium, decreases the uricosuric effect of probenecid. |
| Salsalate | The salicylate, salsalate, decreases the uricosuric effect of probenecid. |
| Silodosin | Strong UGT2B7 inhibitors may increase levels of silodosin. Monitor concomitant therapy closely. |
| Tapentadol | Increases the AUC of tapentadol by 57%. These changes are not considered clinically relevant and no change in dose is required. |
| Trisalicylate-choline | The salicylate, trisalicylate-choline, decreases the uricosuric effect of probenecid. |
| Valganciclovir | Probenecid may decrease excretion of Valganciclovir. Monitor for increased serum concentration and toxicity of Valganciclovir. |
| Zidovudine | Rash, malaise, myalgia |
食物相互作用
- Increase liquid intake, avoid alcohol.
- Take with food to reduce irritation.
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