Description

Simple

An anticoagulant or "blood thinner" used to treat or prevent blood clots in various illnesses including heart attacks.

Clinical

An anticoagulant drug used in the prevention of thromboembolic diseases in infarction and transient ischemic attacks, as well as management of deep vein thrombosis and myocardial infarction.

Overview

Acenocoumarol is a coumarin derivative used as an anticoagulant. Coumarin derivatives inhibit the reduction of vitamin K by vitamin K reductase. This prevents carboxylation of vitamin K-dependent clotting factors, II, VII, IX and X, and interferes with coagulation.[6] Hematocrit, hemoglobin, international normalized ratio and liver panel should be monitored. Patients on acenocoumarol are prohibited from giving blood.

Pharmacology

Indication

For the treatment and prevention of thromboembolic diseases. More specifically, it is indicated for the prevention of cerebral embolism, deep vein thrombosis, pulmonary embolism, thromboembolism in infarction and transient ischemic attacks. It is used for the treatment of deep vein thrombosis and my... Read more

Pharmacodynamic

Acenocoumarol inhibits the reduction of vitamin K by vitamin K reductase. This prevents carboxylation of certain glutamic acid residues near the N-terminals of clotting factors II, VII, IX and X, the vitamin K-dependent clotting factors. Glutamic acid carboxylation is important for the interaction b... Read more

Mechanism of action

Acenocoumarol inhibits vitamin K reductase, resulting in depletion of the reduced form of vitamin K (vitamin KH2). As vitamin K is a cofactor for the carboxylation of glutamate residues on the N-terminal regions of vitamin K-dependent clotting factors, this limits the gamma-carboxylation and subsequ... Read more

Absorption

Rapidly absorbed orally with greater than 60% bioavailability. Peak plasma levels are attained 1 to 3 hours following oral administration.

Protein binding

98.7% protein bound, mainly to albumin

Volume of distribution

The volume of distribution at steady-state appeared to be significantly dose dependent: 78 ml/kg for doses < or = 20 microg/kg and 88 ml/kg for doses > 20 microg/kg respectively

Clearance

Information currently not available.

Half life

8 to 11 hours.

Route of elimination

Mostly via the kidney as metabolites

Toxicity

The onset and severity of the symptoms are dependent on the individual's sensitivity to oral anticoagulants, the severity of the overdosage, and the duration of treatment. Bleeding is the major sign of toxicity with oral anticoagulant drugs. The most frequent symptoms observed are: cutaneous bleedin... Read more

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

  • Ensure consistent Vitamin K intake. Examples include spinach, kale and swiss chard.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(1,2,6,7-3H)Testosterone
(1,2,6,7-3H)Testosterone may increase the anticoagulant activities of Acenocoumarol.
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Acenocoumarol.
(S)-Warfarin
The metabolism of Acenocoumarol can be decreased when combined with (S)-Warfarin.
1-Testosterone
1-Testosterone may increase the anticoagulant activities of Acenocoumarol.
18-methyl-19-nortestosterone
18-methyl-19-nortestosterone may increase the anticoagulant activities of Acenocoumarol.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylthioamphetamine is combined with Acenocoumarol.
25-desacetylrifapentine
The risk or severity of bleeding can be increased when 25-desacetylrifapentine is combined with Acenocoumarol.
3,5-Diiodotyrosine
3,5-Diiodotyrosine may increase the anticoagulant activities of Acenocoumarol.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Acenocoumarol.
4-hydroxycoumarin
The risk or severity of bleeding can be increased when Acenocoumarol is combined with 4-hydroxycoumarin.
4-Hydroxytestosterone
4-Hydroxytestosterone may increase the anticoagulant activities of Acenocoumarol.
5-fluorouridine
The risk or severity of bleeding can be increased when 5-fluorouridine is combined with Acenocoumarol.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when 5-methoxy-N,N-dimethyltryptamine is combined with Acenocoumarol.
5beta-dihydrotestosterone
5beta-dihydrotestosterone may increase the anticoagulant activities of Acenocoumarol.
6-Deoxyerythronolide B
The serum concentration of Acenocoumarol can be increased when it is combined with 6-Deoxyerythronolide B.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Acenocoumarol.
7-ethyl-10-hydroxycamptothecin
The serum concentration of Acenocoumarol can be increased when it is combined with 7-ethyl-10-hydroxycamptothecin.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of bleeding and hemorrhage can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Acenocoumarol.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Acenocoumarol.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Acenocoumarol.
6 References
  1. 1 . Cesar JM, Garcia-Avello A, Navarro JL, Herraez MV: Aging and oral anticoagulant therapy using acenocoumarol. Blood Coagul Fibrinolysis. 2004 Oct;15(8):673-6.PubMed: 15613922
  2. 2 . Lengyel M: [Warfarin or acenocoumarol is better in the anticoagulant treatment of chronic atrial fibrillation?]. Orv Hetil. 2004 Dec 26;145(52):2619-21.PubMed: 15724697
  3. 3 . Ufer M: Comparative pharmacokinetics of vitamin K antagonists: warfarin, phenprocoumon and acenocoumarol. Clin Pharmacokinet. 2005;44(12):1227-46.PubMed: 16372822
  4. 4 . Montes R, Ruiz de Gaona E, Martinez-Gonzalez MA, Alberca I, Hermida J: The c.-1639G > A polymorphism of the VKORC1 gene is a major determinant of the response to acenocoumarol in anticoagulated patients. Br J Haematol. 2006 Apr;133(2):183-7.PubMed: 16611310
  5. 5 . Girard P, Nony P, Erhardtsen E, Delair S, Ffrench P, Dechavanne M, Boissel JP: Population pharmacokinetics of recombinant factor VIIa in volunteers anticoagulated with acenocoumarol. Thromb Haemost. 1998 Jul;80(1):109-13.PubMed: 9684795
  6. 6 . Danziger J: Vitamin K-dependent proteins, warfarin, and vascular calcification. Clin J Am Soc Nephrol. 2008 Sep;3(5):1504-10. doi: 10.2215/CJN.00770208. Epub 2008 May 21.PubMed: 18495950