ペントキシフィリン
WordNet
- a drug (trade name Trental) used to treat claudication; believed to increase the flexibility of red blood cells so they can flow through the blood vessels to the legs and feet (同)Trental
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/01/14 21:33:49」(JST)
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Pentoxifylline
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|
Systematic (IUPAC) name |
3,7-Dimethyl-1-(5-oxohexyl)-3,7-dihydro-1H-purine-2,6-dione |
Clinical data |
Trade names |
Trental |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a685027 |
Licence data |
US FDA:link |
Pregnancy
category
|
|
Legal status |
- AU: Prescription Only (S4)
- CA: ℞-only
- UK: POM
- US: ℞-only
|
Routes |
Oral |
Pharmacokinetic data |
Bioavailability |
10-30%[1] |
Metabolism |
Hepatic and via erythrocytes |
Half-life |
0.4-0.8 hours (1-1.6 hours for active metabolite)[1] |
Excretion |
Urine (95%), faeces (<4%)[1] |
Identifiers |
CAS number |
6493-05-6 Y |
ATC code |
C04AD03 |
PubChem |
CID 4740 |
DrugBank |
DB00806 |
ChemSpider |
4578 Y |
UNII |
SD6QCT3TSU Y |
KEGG |
D00501 Y |
ChEMBL |
CHEMBL628 Y |
Chemical data |
Formula |
C13H18N4O3 |
Molecular mass |
278.31 g/mol |
SMILES
- O=C2N(c1ncn(c1C(=O)N2CCCCC(=O)C)C)C
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InChI
-
InChI=1S/C13H18N4O3/c1-9(18)6-4-5-7-17-12(19)10-11(14-8-15(10)2)16(3)13(17)20/h8H,4-7H2,1-3H3 Y
Key:BYPFEZZEUUWMEJ-UHFFFAOYSA-N Y
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Y (what is this?) (verify) |
Pentoxifylline (INN, BAN, USAN) or oxpentifylline (AAN)[2][3] is a drug commonly sold by Sanofi under the brand name Trental. Its chemical name is 1-(5-oxohexyl)-3, 7-dimethylxanthine. Pentoxifylline is a xanthine derivative. Other brand names include Pentox, Pentoxil and Flexital.
Contents
- 1 Medical uses
- 2 Adverse effects
- 2.1 Contraindications
- 2.2 Interactions
- 3 Mechanism
- 4 See also
- 5 References
- 6 External links
Medical uses
Its primary use in medicine is in treating the symptoms of intermittent claudication resulting from peripheral artery disease.[4] This is its only FDA, MHRA and TGA-labelled indication.[3][5][6]
Other indications for which the literature supports its use in include:
- Multi-infarct dementia[7]
- Peyronie's disease[8]
- Sarcoidosis[9]
- Peripheral neuropathy[10]
- Sickle cell disease[11]
- Alcoholic[12] and non-alcoholic steatohepatitis[13]
- Endometriosis[14]
- Radiation-induced fibrosis[15][16]
- Pentoxyphylline is also used to prevent renal toxicity in cases of alcoholic hepatitis. [17]
Adverse effects
Adverse effects by frequency:[1][2][3][5][6]
Common (1-10% frequency):
- Dizziness
- Headache
- Nausea
- Vomiting
- Indigestion
- Flushing
Uncommon (0.1-1% frequency):
Rare (<0.1% frequency):
- Hypersensitivity
- Itchiness
- Rash
- Hives
- Bleeding
- Hallucinations
- Arrhythmias
- Aseptic meningitis
Contraindications
Contraindications include:[1]
- Intolerance to pentoxifylline or other xanthine derivatives
- Recent retinal or cerebral haemorrhage
- Risk factors for haemorrhage
Interactions
Co-administration of pentoxifylline and sodium thiopental may cause death by acute pulmonary edema in rats.[18]
This drug is passed into the breast milk. Animal studies have shown no evidence of teratogenicity at high doses.
Mechanism
Like other methylated xanthine derivatives, pentoxifylline is a competitive nonselective phosphodiesterase inhibitor[19] which raises intracellular cAMP, activates PKA, inhibits TNF[20][21] and leukotriene [22] synthesis, and reduces inflammation and innate immunity.[22] In addition, pentoxifylline improves red blood cell deformability (known as a haemorrheologic effect), reduces blood viscosity and decreases the potential for platelet aggregation and thrombus formation.[23] Pentoxifylline is also an antagonist at adenosine 2 receptors.[24]
See also
- Lisofylline, an active metabolite of pentoxifylline
References
- ^ a b c d e "Trental, Pentoxil (pentoxifylline) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 3 February 2014.
- ^ a b Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust. ISBN 978-0-9805790-9-3. edit
- ^ a b c "PRODUCT INFORMATION TRENTAL® 400" (PDF). TGA eBusiness Services. sanofi-aventis australia pty limited. 25 March 2010. Retrieved 3 February 2014.
- ^ Salhiyyah, Kareem; Senanayake, Eshan; Abdel-Hadi, Mohammed; Booth, Andrew; Michaels, Jonathan A (Jan 18, 2012). Salhiyyah, Kareem, ed. "Pentoxifylline for intermittent claudication". Cochrane Database Syst Rev 1 (1): CD005262. doi:10.1002/14651858.CD005262.pub2. PMID 22258961.
- ^ a b "PENTOXIFYLLINE tablet, extended release [Apotex Corp.]". DailyMed. Apotex Corp. February 2013. Retrieved 3 February 2014.
- ^ a b "Trental 400 - Summary of Product Characteristics (SPC)". electronic Medicines Compendium. Sanofi. 10 October 2013. Retrieved 3 February 2014.
- ^ "European Pentoxifylline Multi-Infarct Dementia Study". European neurology 36 (5): 315–21. 1996. doi:10.1159/000117279. PMID 8864715.
- ^ Brant, WO; Dean, RC; Lue, TF (February 2006). "Treatment of Peyronie's disease with oral pentoxifylline". Nature Clinical Practice Urology 3 (2): 111–115. doi:10.1038/ncpuro0409. PMID 16470210.
- ^ Beegle, SH; Barba, K; Gobunsuy, R; Judson, MA (2013). "Current and emerging pharmacological treatments for sarcoidosis: a review." (PDF). Drug Design, Development and Therapy 7: 325–38. doi:10.2147/DDDT.S31064. PMC 3627473. PMID 23596348.
- ^ Laczy, B; Cseh, J; Mohás, M; Markó, L; Tamaskó, M; Koszegi, T; Molnár, GA; Wagner, Z; Wagner, L; Wittmann, I (Jun 2009). "Effects of pentoxifylline and pentosan polysulphate combination therapy on diabetic neuropathy in type 2 diabetes mellitus.". Acta diabetologica 46 (2): 105–11. doi:10.1007/s00592-008-0064-5. PMID 18839054.
- ^ Sherer, JT; Glover, PH (Sep 2000). "Pentoxifylline for sickle-cell disease.". The Annals of pharmacotherapy 34 (9): 1070–4. doi:10.1345/aph.19397. PMID 10981255.
- ^ Akriviadis, E; Botla, R; Briggs, W; Han, S; Reynolds, T; Shakil, O (December 2000). "Pentoxifylline improves short-term survival in severe acute alcoholic hepatitis: A double-blind, placebo-controlled trial". Gastroenterology 119 (6): 1637–1648. doi:10.1053/gast.2000.20189. PMID 11113085.
- ^ Li, W; Zheng, L; Sheng, C; Cheng, X; Qing, L; Qu, S (April 2011). "Systematic review on the treatment of pentoxifylline in patients with non-alcoholic fatty liver disease.". Lipids in health and disease 10: 49. doi:10.1186/1476-511X-10-49. PMC 3088890. PMID 21477300.
- ^ Alborzi, S; Ghotbi, S; Parsanezhad, ME; Dehbashi, S; Alborzi, S; Alborzi, M (Jan–Feb 2007). "Pentoxifylline therapy after laparoscopic surgery for different stages of endometriosis: a prospective, double-blind, randomized, placebo-controlled study.". Journal of minimally invasive gynecology 14 (1): 54–8. doi:10.1016/j.jmig.2006.06.024. PMID 17218230.
- ^ Okunieff, P; Augustine, E; Hicks, JE; Cornelison, TL; Altemus, RM; Naydich, BG; Ding, I; Huser, AK; Abraham, EH; Smith, JJ; Coleman, N; Gerber, LH (Jun 1, 2004). "Pentoxifylline in the treatment of radiation-induced fibrosis.". Journal of clinical oncology : official journal of the American Society of Clinical Oncology 22 (11): 2207–13. doi:10.1200/JCO.2004.09.101. PMID 15169810.
- ^ Delanian, S; Porcher, R; Rudant, J; Lefaix, JL (2005). "Kinetics of response to long-term treatment combining pentoxifylline and tocopherol in patients with superficial radiation-induced fibrosis,". J Clin Oncol 23 (34): 8570–8579. doi:10.1200/JCO.2005.02.4729. PMID 16260695.
- ^ [1]
- ^ Pereda, J; Gómez-Cambronero, L; Alberola, A; Fabregat, G; Cerdá, M; Escobar, J; Sabater, L; García-De-La-Asunción, J; Viña, J; Sastre, J (2006). "Co-administration of pentoxifylline and thiopental causes death by acute pulmonary oedema in rats". British Journal of Pharmacology 149 (4): 450–5. doi:10.1038/sj.bjp.0706871. PMC 1978439. PMID 16953192.
- ^ Essayan DM. (2001). "Cyclic nucleotide phosphodiesterases". J Allergy Clin Immunol. 108 (5): 671–80. doi:10.1067/mai.2001.119555. PMID 11692087.
- ^ Deree J, Martins JO, Melbostad H, Loomis WH, Coimbra R. (2008). "Insights into the Regulation of TNF-α Production in Human Mononuclear Cells: The Effects of Non-Specific Phosphodiesterase Inhibition". Clinics (Sao Paulo). 63 (3): 321–8. doi:10.1590/S1807-59322008000300006. PMC 2664230. PMID 18568240.
- ^ Marques LJ, Zheng L, Poulakis N, Guzman J, Costabel U (February 1999). "Pentoxifylline inhibits TNF-alpha production from human alveolar macrophages". Am. J. Respir. Crit. Care Med. 159 (2): 508–11. doi:10.1164/ajrccm.159.2.9804085. PMID 9927365.
- ^ a b Peters-Golden M, Canetti C, Mancuso P, Coffey MJ. (2005). "Leukotrienes: underappreciated mediators of innate immune responses". J Immunol. 174 (2): 589–94. doi:10.4049/jimmunol.174.2.589. PMID 15634873.
- ^ Ward, A; Clissold, SP (1987). "Pentoxifylline. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic efficacy". Drugs 34 (1): 50–97. doi:10.2165/00003495-198734010-00003. PMID 3308412.
- ^ Rodríguez-Morán M, Guerrero-Romero F (February 2008). "Efficacy of pentoxifylline in the management of microalbuminuria in patients with diabetes". Curr Diabetes Rev 4 (1): 55–62. doi:10.2174/157339908783502343. PMID 18220696.
External links
- Trental information from Aventis[dead link]
- Reprinted article on veterinary use subscription required
Peripheral vasodilators (C04)
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|
2-amino-1-phenylethanol derivatives |
- Isoxsuprine
- Buphenine
- Bamethan
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|
Imidazoline derivatives/
Alpha blockers |
|
|
Niacin and derivatives |
- Niacin
- Nicotinyl alcohol
- Inositol nicotinate
- Ciclonicate
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|
Purine derivatives |
- Pentifylline
- Xantinol nicotinate
- Pentoxifylline
- Etofylline nicotinate
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|
Ergot alkaloids |
- Ergoloid
- Nicergoline
- Dihydroergocristine
|
|
Other peripheral vasodilators |
- Cyclandelate
- Phenoxybenzamine
- Vincamine
- Moxisylyte
- Bencyclane
- Vinburnine
- Sulcotidil
- Buflomedil
- Naftidrofuryl
- Butalamine
- Visnadine
- Cetiedil
- Cinepazide
- Ifenprodil
- Azapetine
- Fasudil
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Index of the circulatory system
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Description |
- Anatomy
- Arteries
- head and neck
- arms
- chest
- abdomen
- legs
- Veins
- head and neck
- arms
- chest
- abdomen and pelvis
- legs
- Lymph vessels
- Development
- Cells
- Physiology
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Disease |
- Congenital
- Neoplasms and cancer
- Lymphatic vessels
- Injury
- Vasculitis
- Other
- Symptoms and signs
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Treatment |
- Procedures
- Drugs
- beta blockers
- channel blockers
- diuretics
- nonsympatholytic vasodilatory antihypertensives
- peripheral vasodilators
- renin–angiotensin system
- sympatholytic antihypertensives
- vasoprotectives
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Phosphodiesterase inhibitors
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|
PDE1 |
- MMPX
- SCH-51866
- Vinpocetine
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|
PDE2 |
|
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PDE3 |
- Amrinone
- Anagrelide
- Bucladesine
- Cilostamide
- Cilostazol
- Enoximone
- KMUP-1
- Milrinone
- Quazinone
- RPL-554
- Siguazodan
- Trequinsin
- Vesnarinone
- Zardaverine
|
|
PDE4 |
- Apremilast
- Arofylline
- Atizoram
- Cilomilast
- Denbutylline
- Drotaverine
- Etazolate
- Filaminast
- Glaucine
- HT-0712
- Ibudilast
- ICI-63197
- Irsogladine
- Luteolin
- Mesembrine
- Piclamilast
- Roflumilast
- Rolipram
- Ro20-1724
- RPL-554
- YM-976
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|
PDE5 |
- Acetildenafil
- Aildenafil
- Avanafil
- Dipyridamole
- Icariin
- Lodenafil
- Mirodenafil
- MY-5445
- Nitrosoprodenafil
- Sildenafil
- Sulfoaildenafil
- T-0156
- Tadalafil
- Udenafil
- Vardenafil
|
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PDE6 |
|
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PDE7 |
|
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PDE9 |
|
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PDE10 |
- Papaverine
- PF-2545920
- Tofisopam
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|
PDE11 |
BC11-38
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Nonselective |
- Caffeine
- Doxofylline
- IBMX
- Pentoxifylline
- Propentofylline
- Theophylline
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Adenosinergics
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Receptor
(ligands)
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AR
|
- Agonists: 2-(1-Hexynyl)-N-methyladenosine
- 2-Cl-IB-MECA
- 2'-MeCCPA
- 5'-N-ethylcarboxamidoadenosine
- Adenosine
- Apadenoson
- ATL-146e
- BAY 60–6583
- Binodenoson
- Capadenoson
- CCPA
- CGS-21680
- CP-532,903
- GR 79236
- LUF-5835
- LUF-5845
- N6-Cyclopentyladenosine
- Regadenoson
- SDZ WAG 994
- Selodenoson
- Sonedenoson
- Tecadenoson
- UK-432,097
- Antagonists: 8-Chlorotheophylline
- 8-Phenyl-1,3-dipropylxanthine
- 8-Phenyltheophylline
- Acefylline
- Aminophylline
- ATL-444
- Bamifylline
- Cafedrine
- Caffeine
- Caffeine citrate
- Cartazolate
- CF-101
- CGS-15943
- Choline theophyllinate
- CPX
- CVT-6883
- Dimethazan
- Dyphylline
- DPCPX
- Enprofylline
- Etazolate
- Fenethylline
- IBMX
- Istradefylline
- KF-26777
- MRE3008F20
- MRS-1220
- MRS-1334
- MRS-1706
- MRS-1754
- MRS-3777
- Paraxanthine
- Pentoxifylline
- Preladenant
- Propentofylline
- Proxyphylline
- PSB-10
- PSB-11
- PSB 36
- PSB-603
- PSB-788
- PSB-1115
- Rolofylline
- SCH-442,416
- SCH-58261
- Theobromine
- Theodrenaline
- Theophylline
- Tozadenant
- Tracazolate
- VUF-5574
- ZM-241,385
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Transporter
(blockers)
|
ENTs
|
- Dilazep
- Dipyridamole
- Hexobendine
- Pentoxifylline
- Propentofylline
- Barbiturates
- Ethanol
- Benzodiazepines
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UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
English Journal
- A membrane-based microfluidic device for mechano-chemical cell manipulation.
- Ravetto A1, Hoefer IE2, den Toonder JM3,4, Bouten CV5,6.
- Biomedical microdevices.Biomed Microdevices.2016 Apr;18(2):31. doi: 10.1007/s10544-016-0040-8.
- We introduce a microfluidic device for chemical manipulation and mechanical investigation of circulating cells. The device consists of two crossing microfluidic channels separated by a porous membrane. A chemical compound is flown through the upper "stimulus channel", which diffuses through the memb
- PMID 26941177
- Pentoxifylline during steroid window phase at induction to remission increases apoptosis in childhood with acute lymphoblastic leukemia.
- Gonzalez-Ramella O1,2, Ortiz-Lazareno PC3, Jiménez-López X1,2, Gallegos-Castorena S1,2, Hernández-Flores G3, Medina-Barajas F1,2, Meza-Arroyo J3, Jave-Suárez LF3, Lerma-Díaz JM3,4, Sánchez-Zubieta F1,2, Bravo-Cuellar A5,6.
- Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico.Clin Transl Oncol.2016 Apr;18(4):369-74. doi: 10.1007/s12094-015-1376-x. Epub 2015 Sep 2.
- PURPOSE: Pentoxifylline (PTX) has been shown to increase chemotherapy-induced apoptosis. A clinical trial was developed to evaluate the effect of the addition of PTX to the induction steroid window phase in children with acute lymphoblastic leukemia (ALL).METHODS: Thirty-two children were enrolled o
- PMID 26329293
- The effects of pentoxifylline and caffeic acid phenethyl ester in the treatment of d-galactosamine-induced acute hepatitis in rats.
- Taslidere E1, Vardi N2, Esrefoglu M3, Ates B4, Taskapan C5, Yologlu S6.
- Human & experimental toxicology.Hum Exp Toxicol.2016 Apr;35(4):353-65. doi: 10.1177/0960327115586820. Epub 2015 May 13.
- The aim of this study was to investigate histological changes in hepatic tissue and effects of pentoxifylline (PTX) and caffeic acid phenethyl ester (CAPE) on these changes using histochemical and biochemical methods in rats, in which hepatitis was established by d-galactosamine (d-GAL). Rats were d
- PMID 25977259
Japanese Journal
- 薄い子宮内膜による着床障害への対応 (特集 生殖補助医療(ART)の基礎と実際)
- Protein array technology to investigate cytokine production by monocytes from patients with advanced alcoholic cirrhosis : An ex vivo pilot study
- TAZI Khalid A.,QUIOC Jean-Jacques,ABDEL-RAZEK Wael,TELLIER Zera,GUICHARD Cecile,OGIER-DENIS Eric,LEBREC Didier,MOREAU Richard
- Hepatology research : the official journal of the Japan Society of Hepatology 39(7), 706-715, 2009-07-01
- NAID 10025326756
Related Links
- ※この商品に関係するニュース記事へのリンクがページ最下部にあります。 「有効成分」 ペントキシフィリン(Pentoxifylline BP) 「同一成分含有商品」 トレンタール 400 (ペントキシフィリン)400mg (15錠) 530 円 Trental 400 ...
- Pentoxifyllineとは?goo Wikipedia (ウィキペディア) 。出典:Wikipedia(ウィキペディア)フリー百科事典。 Pentoxifyllineとは - goo Wikipedia (ウィキペディア) gooトップ サイトマップ スタートページに設定 RSS ヘルプ メニューへスキップ ...
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