Acenocoumarol

CLINICAL USE

Anticoagulant

DOSE IN NORMAL RENAL FUNCTION

4–12 mg on 1st day; 4–8 mg on 2nd dayMaintenance dose usually 1–8 mg daily according to INR

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :353.3

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>98

%Excreted unchanged in urine &nbsp &nbsp : <0.2

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.16–0.18 R(+) enantiomer; 0.22–0.34 S(–) enantiomer

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :8–11/Probably unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unknown dialysability. Dose as in normal renal function

HDF/high flux &nbsp :Unknown dialysability. Dose as in normal renal function

CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

There Are Many Significant Interactions With Coumarins. Prescribe With Care With Regard To The Following:Anticoagulant effect enhanced by: alcohol, amiodarone, anabolic steroids, aspirin, azithromycin, aztreonam, bicalutamide, cephalosporins, chloramphenicol, cimetidine, ciprofloxacin, clarithromycin, fibrates, clopidogrel, cranberry juice, danazol, dextropropoxyphene, dipyridamole, disulfiram, erythromycin,esomeprazole, ezetimibe, fluconazole, flutamide, fluvastatin, grapefruit juice, itraconazole, ketoconazole, levamisole, levofloxacin, macrolides, methylphenidate, metronidazole, miconazole, nalidixic acid, neomycin, norfloxacin, NSAIDs, ofloxacin, omeprazole, pantoprazole, paracetamol, penicillins, propafenone, ritonavir, rosuvastatin, SSRIs, simvastatin, sitaxentan, sulfinpyrazone, sulphonamides, tamoxifen, testosterone, tetracyclines, levothyroxine, tigecycline, toremifene, tramadol, trimethoprim, valproate, voriconazole

Anticoagulant effect decreased by:acitretin, azathioprine, barbiturates, carbamazepine, griseofulvin, mercatopurine, mitotane, oral contraceptives, phenytoin, primidone, rifampicin, St John’s wort (avoid concomitant use), sucralfate, vitamin K

Anticoagulant effects enhanced/reduced by: amprenavir, anion exchange resins, corticosteroids, dietary changes, tricyclics

Analgesics: increased risk of bleeding with IV diclofenac and ketorolac – avoid concomitant use

Antidiabetic agents: enhanced hypoglycaemic effect with sulphonylureasCiclosporin: there have been a few reports of altered anticoagulant effect; decreased ciclosporin levels have been seen rarely

Cytotoxics: increased risk of bleeding with erlotinib and imatinib; enhanced effect with etoposide, fluorouracil, ifosfamide and sorafenib

ADMINISTRATION

Reconstition

–

Route

Oral

Rate of Administration

–

Comments

–

OTHER INFORMATION

Acenocoumarol prolongs the thromboplastin time within approximately 36–72 hoursDecreased protein binding in uraemia

Tags: post-by-auto-php