DRUGS ACTING ON BLOOD AND BLOOD FORMING ORGANS

 

DRUGS ACTING ON BLOOD AND BLOOD FORMING ORGANS

PREPARED BY MR. ABHIJIT DAS


HEMATINIC AGENTS

DEFINITION

Hematinic agents are medications or supplements that help in the formation of red blood cells or improve the production of hemoglobin, which is essential for carrying oxygen in the blood. These agents typically contain iron, vitamin B12, or folic acid, and they are commonly used to treat various types of anemia.

CLASSIFICATION

1.     Iron supplements: These agents contain iron and are used to treat iron-deficiency anemia.

Examples: Ferrous sulfate, ferrous gluconate, and ferrous fumarate.

2.     Vitamin B12 supplements: These agents provide vitamin B12 and are used to treat pernicious anemia or other conditions resulting from vitamin B12 deficiency.

Examples: Cyanocobalamin and methylcobalamin.

3.     Folic acid supplements: These agents contain folic acid and are used to treat folate-deficiency anemia.

Examples: Folic acid and various folate derivatives.

4.     Combination supplements: Some hematinic agents combine iron, vitamin B12, and folic acid to address multiple deficiencies and support overall red blood cell production.

Examples: Combination formulations like ferrous sulfate with folic acid and cyanocobalamin.

 

 

ANTICOAGULANTS

DEFINITION

Anticoagulants are medications that prevent blood clot formation, reducing the risk of blood clots and promoting blood flow.

CLASSIFICATION

A.   Parenteral anticoagulants: heparin, low molecular weight heparin.

B.   Oral anticoagulants:

i.                   Coumarin derivatives: bishydroxycoumarin(dicumarol), warfarin sod, acenocoumarol(nicoumalone).

ii.                 Indandione derivative: phenindione

HEPARIN

MOA

It enhances the activity of antithrombin, a natural protein in the blood. By doing so, heparin helps antithrombin in its role to inhibit clotting factors, specifically thrombin and factor Xa, preventing the formation of blood clots.


(Clotting factor Xa is a key component of the blood coagulation process. It is an enzyme that plays a crucial role in the formation of blood clots. When activated, factor Xa converts prothrombin into thrombin, which then helps convert fibrinogen into fibrin, a mesh-like protein that forms the basis of blood clots.)

ADVERSE EFFECTS

1.     Bleeding: Heparin can make you more prone to bleeding, from mild bruising to serious internal bleeding.

2.     Heparin-induced Thrombocytopenia (HIT): Sometimes, heparin triggers a condition where your platelet levels drop, increasing the risk of clotting.

3.     Osteoporosis: Long-term use of heparin may weaken your bones and increase the risk of fractures.

THERAPEUTICAL USES

1.     Preventing and treating blood clots: Heparin is widely used to prevent and treat blood clots in various conditions like deep vein thrombosis, pulmonary embolism, and during surgeries where clotting risks are high.

2.     During dialysis: Heparin is often used during hemodialysis to prevent clotting in the bloodlines and the dialysis machine, ensuring a smooth and effective treatment.

3.     Heart attacks and unstable angina: Heparin is given in combination with other medications during certain heart conditions to prevent further clot formation and improve blood flow to the heart.

WARFARIN

MOA

It works by inhibiting the synthesis of vitamin K-dependent clotting factors in the liver. By doing so, warfarin interferes with the blood clotting process and helps prevent the formation of blood clots.

{Examples of vitamin K-dependent clotting factors include:

1.     Prothrombin (Factor II): Prothrombin is a precursor to thrombin, an essential enzyme in the blood clotting cascade.

2.     Factor VII (Proconvertin): Factor VII activates Factor X, which plays a central role in the clotting process.

3.     Factor IX (Christmas Factor): Factor IX activates Factor X, contributing to the formation of fibrin and blood clotting.

4.     Factor X (Stuart-Prower Factor): Factor X is a key component in converting prothrombin to thrombin, which leads to the formation of fibrin.}

 

ANTI-PLATELET AGENTS

DEFINITION
Antiplatelet drugs are medications that help prevent blood platelets from sticking together and forming clots, reducing the risk of blood vessel blockages and certain cardiovascular conditions.

ASPIRIN

MOA

Aspirin works as an antiplatelet agent by blocking the COX-1 enzyme in platelets, which reduces the production of thromboxane A2. This prevents platelet aggregation and helps prevent blood clot formation.

CLOPIDOGREL

MOA

Clopidogrel acts as an antiplatelet drug by blocking ADP receptors on platelets, reducing platelet activation and preventing blood clot formation in individuals at risk of cardiovascular events or after certain medical procedures.

{ ADP receptors, also known as P2Y12 receptors, are cell surface receptors found on platelets, which are small cell fragments in the blood involved in clot formation. These receptors are part of the purinergic receptor family and play a crucial role in platelet activation.

When platelets are activated due to blood vessel injury or other factors, ADP is released from damaged cells and platelets themselves. ADP binds to the P2Y12 receptors on nearby platelets, initiating a signaling pathway that promotes platelet aggregation and clot formation. This activation leads to a change in the shape and stickiness of platelets, making them more likely to adhere to each other and form a clot at the site of injury.}

ADVERSE EFFECTS

1.     Bleeding: The most significant concern with antiplatelet medications like clopidogrel is an increased risk of bleeding. Since clopidogrel inhibits platelet aggregation, it can make it harder for blood to clot, leading to potential bleeding issues. Severe bleeding, although rare, can occur and may manifest as gastrointestinal bleeding, nosebleeds, or easy bruising.

2.     Gastrointestinal Upset: Some individuals may experience gastrointestinal side effects such as nausea, vomiting, indigestion, or abdominal discomfort while taking clopidogrel.

3.     Allergic Reactions: In rare cases, clopidogrel can trigger allergic reactions, which may range from mild skin rashes to more severe allergic responses like swelling of the face, tongue, or throat, difficulty breathing, and anaphylaxis.

THERAPEUTICAL USES

1.     Prevention of Cardiovascular Events: Clopidogrel is commonly used to reduce the risk of heart attacks, strokes, and other cardiovascular events in patients with a history of atherosclerosis or those who have undergone procedures like stent placement.

2.     Treatment of Acute Coronary Syndrome: Clopidogrel is used in combination with other medications for the management of acute coronary syndrome, such as unstable angina and non-ST-segment elevation myocardial infarction (NSTEMI).

3.     Post-Cardiovascular Event Management: After experiencing a heart attack or stroke, patients may be prescribed clopidogrel as part of their long-term treatment to prevent further clot formation and recurrent cardiovascular events.

 

THROMBOLYTIC DRUGS

DEFINITION

Thrombolytic drugs, also known as clot-busting drugs, are medications used to dissolve or break down blood clots that have formed within blood vessels.

STREPTOKINASE AND UROKINASE

MOA

Streptokinase activates plasminogen to form plasmin, a powerful enzyme. Plasmin then breaks down fibrin, the protein that creates blood clots, leading to clot dissolution and restored blood flow.

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