Pentoxifylline

Structural formula
General
Non-proprietary name	Pentoxifylline
other names	3,7-dimethyl-1- (5-oxohexyl) purine-2,6-dione ( IUPAC ) Pentoxifyllinum ( Latin ) BL 191
Molecular formula	C 13 H 18 N 4 O 3
Brief description	white to almost white, crystalline powder
External identifiers / databases
CAS number 6493-05-6 EC number 229-374-5 ECHA InfoCard 100.026.704 PubChem 4740 DrugBank DB00806 Wikidata Q416331
Drug information
ATC code	C04 AD03
Drug class	Peripheral vasodilator Xanthine derivative
properties
Molar mass	278.31 g · mol -1
Physical state	firmly
Melting point	105 ° C
pK s value	0.3 (at 20 ° C)
solubility	soluble in water, slightly soluble in dichloromethane , slightly soluble in ethanol 96%
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS labeling of hazardous substances Caution H and P phrases H: 302 P: no P-phrases
Toxicological data	1170 mg kg −1 ( LD 50 ,  rat ,  oral ) 231 mg kg −1 ( LD 50 ,  rat ,  iv ) 1225 mg kg −1 ( LD 50 ,  mouse ,  oral ) 108 mg kg −1 ( LD 50 ,  mouse ,  iv )
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Pentoxifylline is a drug selected from the group of xanthine - derivatives on the one hand to influence the rheological properties (flow properties) of the blood is used, on the other hand are its anti-inflammatory (anti-inflammatory) properties used.

Clinical information

Indications / possible uses

• Peripheral circulatory disorders
• Circulatory disorders in the eye and hearing area in connection with degenerative vascular processes and reduced vision or hearing (e.g. sudden hearing loss , tinnitus )
• Peripheral arterial occlusive disease (PAVK) - arteriosclerotic or diabetic origin (e.g. with intermittent claudication and pain at rest)
• Cerebral ischemic diseases (as an anti-dementia or nootropic)
• Trophic lesions (e.g. leg ulcers and gangrene )
• Alcoholic steatohepatitis

Contraindications (contraindications)

• Hypersensitivity to the active ingredient pentoxifylline, other methylxanthines
• Mass bleeding and recent cerebral and retinal bleeding (risk of increased bleeding)
• Recent myocardial infarction (heart attack, increased risk of cardiac arrhythmias and drop in blood pressure)
• Hemorrhagic diathesis (a pathologically increased tendency to bleed)
• Ulcers in the stomach and / or intestines

Adverse effects (side effects)

• Dizziness, tremor , headache, fever, restlessness, sleep disorders
• Arrhythmias (such as tachycardia )
• Hypersensitivity reactions with itching, reddening of the skin, urticaria .
• Visual disturbances, conjunctivitis

Pentoxifylline can affect the way diabetes medications and antihypertensive drugs work.

Pentoxifylline can cause aplastic anemia . Regular blood counts should be done while using the drug.

Pharmacological properties

Mechanism of action (pharmacodynamics)

• Hemorheology: Pentoxifylline inhibits the enzyme phosphodiesterase and thus has an influence on the cAMP and further on the vascular tone and apparently has a vasodilating effect. It should lower the blood viscosity by influencing the deformability of the erythrocytes (red blood cells) and lower the plasma fibrinogen level . The consequence would then be an improvement in tissue perfusion (tissue blood flow) by inhibiting blood clotting . It is used, among other things, for tinnitus and sudden hearing loss , as well as arterial occlusive diseases. Pentoxifylline is used as a rheological agent in vascular insufficiency . The prescription of rheological drugs is controversial in medicine, as no convincing proof of effectiveness has been achieved so far.
• Anti-inflammatory effect: Pentoxifylline inhibits the release of interleukins and TNF-alpha . There is an inhibition of degranulation of neutrophilic granulocytes . A synergistic effect with corticosteroids has been shown.

Trade names

Monopreparations

Agapurin (D), Claudicat (D), Haemodyn (A), Pentohexal (A), Pentomer (A), Pentoxi (A), Rentylin (D), Trental (D, A, CH), Vasonit (A), various Generics (D, A, CH)

literature

• P. Zabel: Pentoxifylline in treatment of sarcoidosis. In: Am. J. Respir. Crit. Care Med. Vol 155, No. 5, May 1997, pp. 1665-1669.
• RS O'Shea et al: AASLD Practice Guidelines: Alcoholic Liver Disease. In: Hepatology . 51, 2010, p. 307.

Web links

• drug telegram: pentoxifylline

Individual evidence

1. ↑ ^{a b} European Pharmacopoeia Commission (ed.): EUROPEAN PHARMACOPOE 5TH EDITION . tape 5.0-5.8 , 2006.
2. ^ The Merck Index: An Encyclopedia of Chemicals, Drugs, and Biologicals. 14th edition. (Merck & Co., Inc.), Whitehouse Station, NJ, USA, 2006, ISBN 0-911910-00-X .
3. ↑ Sean Sweetman (Ed.): Martindale: The Complete Drug Reference. 35th edition. Book and CD-ROM. Pharmaceutical Press, 2006, ISBN 0-85369-704-3 .
4. ↑ ^{a b} Datasheet Pentoxifylline from Sigma-Aldrich , accessed on April 18, 2011 ( PDF ).
5. ^ ^{A b c d} A. Kleemann , J. Engel, B. Kutscher, D. Reichert: Pharmaceutical Substances - Synthesis, Patents, Applications. 4th edition. Thieme-Verlag, Stuttgart 2000, ISBN 1-58890-031-2 .
6. ↑ ^{a b} English SPC for Trental ^® (pentoxifylline tablets) by Sanofi-Aventis US - Date of information: October, 2007 ( Memento of 12 October 2007 at the Internet Archive ) (PDF, 38 kB).
7. ↑ Ernst Mutschler, Gerd Geislinger, Heyo K. Kroemer, Sabine Menzel, Peter Ruth: Mutschler drug effects - pharmacology, clinical pharmacology, toxicology. 10th edition. Stuttgart 2013, p. 523.
8. ↑ Red List online, as of October 2009.
9. ↑ AM comp. d. Switzerland, as of October 2009.
10. ↑ AGES-PharmMed, as of October 2009.

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !