In vivo anticoagulants or coumarin derivatives

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Chapter: Medicinal Chemistry : Coagulants

i. Bishydroxycoumarin (Dicoumarol) ii. Warfarin (Coumarin, Coumadia) iii. Heparin iv. Ethyl biscoumacetate v. Acenocoumarol


SYNTHESIS AND DRUG PROFILE

In vivo anticoagulants or coumarin derivatives

i. Bishydroxycoumarin (Dicoumarol)


Synthesis


Properties and uses: It is used in postoperative thrombophlebitis, pulmonary embolus, acute embolic, and thrombolic occlusion of peripheral arteries.

 

ii. Warfarin (Coumarin, Coumadia)


Synthesis


Properties and uses: Warfarin sodium is a white hygroscopic powder, soluble in water, alcohol, and acetone, very slightly soluble in methylene chloride. The (–) (S) isomer of warfarin has shown itself to be five to eight times more potent than (+) (R) enantiomer. Warfarin is a synthetic anticoagulant used in patients undergoing orthopaedic surgery.

Assay: Dissolve the sample in 0.01 M sodium hydroxide and measure the absorbance after dilution at the maxima of 308 nm using ultraviolet spectrophotometer.

Dose: The dose for adults is 10–15 mg per day for 2 to 4 days.

Dosage forms: Warfarin tablets I.P., B.P.

 

iii. Heparin

Properties and uses: Heparin sodium is a white hygroscopic powder, soluble in water and used as an anticoagulant.

Assay: It is assayed by adopting spectrophotometric method.

Dosage forms: Heparin injection B.P.

 

iv. Ethyl biscoumacetate


 

v. Acenocoumarol

Properties and uses: Acenocoumarol is a white to buff-coloured powder, practically insoluble in water and ether, slightly soluble in ethanol. It dissolves in aqueous solutions of the alkali hydroxides. Used as vitamin K epoxide reductase inhibitor and as oral anticoagulant.

Assay: Dissolve the sample in acetone and titrate against 0.1 M sodium hydroxide using bromothymol blue as indicator.

Dosage forms: Acenocoumarol tablets B.P.

 

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