COAGULANT & ANTICOAGULANTS AGENTS

The medicine used to the clotting of blood is called coagulation and in the process blood to form solid masses or clots.

There are thirty different types of cells and substances in blood affect clotting and the process is initiated by blood platelets.

Platelets produce a substance that combines with calcium ions in the blood to form thromboplastin, which in turn converts the protein prothrombin into thrombin in a complex series of reactions.

Thrombin, a proteolytic enzyme, converts fibrinogen, a protein substance, into fibrin, an insoluble protein that forms an intricate network of minute thread like structures called fibrils and causes the blood plasma to gel.

The blood cells and plasma are enmeshed in the network of fibrils to form the clot.

Anticoagulant agent is used to prevent the formation of blood clots and to maintain open blood vessels.

Anticoagulants are called blood "thinners," but they do not thin the blood, they only prevent or reduce clots, or thrombi.

Anticoagulant is used for the treatment of thromboembolic disorders, such as stroke, heart attack and deep venous thrombosis.

CLASSIFICTAION 

BASED ON MECHANISM

Indirect thrombin inhibitors

- Heparin,

- Fondapatinux,

- Danaparoid

Direct thrombin inhibitors

- Lepirudin,

- Bivalirudin,

- Argatroban

BASED ON PARENT NUCLEUS

Comouarin

- Warfarin

Indanedione

- Anisindione

Thienopyridine

- Clopidogrel

1,4 napthoquinone

- Menadione, Acetomenadione

MECHANISM OF COAGULANT & ANTICOAGULANTS AGENTS

MENADIONE

CHEMICAL STRUCTURE

IUPAC NAME

2-methylnaphthalene-1,4-dione

USES

1. Manadione is used as a nutritional supplement in the place of vitamin K activity.

2. It can serve as a precursor to various types of vitamin K

3. Manadione is used in the treatment of hypoprothrombinemia

ACETOMENADIONE

CHEMICAL STRUCTURE

IUPAC NAME

(4-acetyloxy-3-methylnaphthalen-1-yl) acetate

USES

1. Acetomenadione is used for the treatment of Coagulation disorders due to vitamin K deficiency.

2. Acetomenadione is a medicine that is used for the anticoagulant-induced prothrombin deficiency and other conditions.

WARFARIN

CHEMICAL STRUCTURE

IUPAC NAME

4-hydroxy-3-(3-oxo-1-phenylbutyl)-2H-chromen-2-one

USES

1. Warfarin is used to treat blood clots and it helps to keep blood flowing smoothly in your body by decreasing the amount of clotting proteins in your blood.

2. Warfarin is preventing harmful blood clots helps to reduce the risk of a stroke or heart attack.

3. Warfarin is commonly called a "blood thinner"

Synthesis of Warfarin

ANISINDIONE

CHEMICAL STRUCTURE

IUPAC NAME

2-(4-methoxyphenyl)-1H-indene-1,3(2H)-dione

USES

1. Anisindione is an anticoagulant

2. Anisindione prevents the formation of active procoagulation factors and anticoagulant proteins in the liver by inhibiting the vitamin K–mediated gammacarboxylation.

CLOPIDOGREL

CHEMICAL STRUCTURE

IUPAC NAME

Methyl 2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-c]pyridin5(4H)-yl)acetate

USES

1. Clopidogrel is used to prevent heart attacks and strokes in persons with heart disease, or recent stroke, or blood circulation disease.

2. Clopidogrel is also used with aspirin to treat new/worsening chest pain

3. Clopidogrel works by blocking platelets from sticking together and prevents them from forming harmful clots.