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Pharmacology of Blood-Acting Drugs: Hematinics, Coagulants, and Anticoagulants

Detailed exploration of haemoglobin, anaemia types, hematinics, clotting factors, coagulation mechanisms, coagulants, and anticoagulants in pharmacology.

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AUGUST 21, 2026 1 Dr. Rajendra Gode Institute of Pharmacy, University - Mardi Road, Amravati - 444602 Pharmacology – II (BP 503 T) “Pharmacology of drugs acting on Blood” b. Hematinics, Coagulants and Anticoagulants 1 Presented by Ms. Shraddha S. Raut M. Pharm (Pharmacology) Assistant Professor UNIT II
AUGUST 21, 2026 2  Contents Haemoglobin Causes of anaemia Hematinics and Anaemia 1 3 2 Symptoms of anaemia 4 Types of anaemia 5 Classification of Hematinics 6 Individual Agents 7 Clotting Factors Mechanism of Coagulation Coagulants 8 1 0 9 Classification of Coagulants 1 1 Individual Agents 1 2 Anticoagulants 1 3 Classification & Individual Agents 1 4
AUGUST 21, 2026  Hematinics and Anaemia 3 • Hematinics: Substances essential for blood formation and anaemia treatment. • Anaemia: Caused by an imbalance between red blood cell (RBC) production and destruction.
AUGUST 21, 2026 4  Haemoglobin • Haemoglobin is a protoporphyrin, each molecule having 4 iron-containing heme residues. • It has 0.33% iron. • To raise the Hb level of blood by 1 g/dL, about 200 mg of iron is needed. • Iron is stored only in ferric form, in combination with a large protein, apoferritin.
AUGUST 21, 2026 5  Causes of Anaemia
AUGUST 21, 2026 6  Symptoms of Anaemia
AUGUST 21, 2026 7  Types of Anaemia Normocytic / Normochromic Anaemia Microcytic / Hypochromic Anaemia Macrocytic / Megaloblastic Anaemia Pernicious Anaemia Hemolytic Anaemia Sickle Cell Anaemia Aplastic Anaemia 1 2 3 4 5 6 7
AUGUST 21, 2026 8 Normocytic Anaemia It causes due to acute blood loss. Microcytic Anaemia It includes iron deficiency and thalassemia. Macrocytic Anaemia It occurs due to Vitamin B12 and Folic acid deficiency. Pernicious Anaemia Autoimmune lack of intrinsic factor leads to poor B12 absorption. Hemolytic Anaemia It results from the destruction of RBC. Sickle Cell Anaemia Characterised by sickle- shaped RBCs due to a genetic HbS abnormality. Aplastic Anaemia It occurs due to bone marrow disorder.
AUGUST 21, 2026 9  Classification of Hematinics
AUGUST 21, 2026 10 • Iron is a vital mineral essential for oxygen transport and cellular energy production. • Iron is a key component of haemoglobin, cytochromes and respiratory enzymes. • Iron-containing enzymes support cellular oxidation and energy generation. • Iron deficiency leads to anaemia, causing fatigue and weakened immunity. • Iron supplementation helps restore blood iron levels in anaemia. • Adult total body iron ranges from 2.5 to 5 grams, higher in men (50 mg/kg) than women (38 mg/kg). • Iron distribution: 66% in haemoglobin, 25% in storage (ferritin, haemosiderin), 3% in myoglobin, 6% in enzymes and proteins. Iron
AUGUST 21, 2026 11 • Adult male: 0.5–1 mg (13 µg/kg) • Adult female: 1 – 2 mg (21 µg/kg) (menstruating) • Infants: 60 µg/kg • Children: 25 µg/kg • Pregnancy: 3 – 5 mg (80 µg/kg) (last 2 trimesters) Daily Requirement of Iron • Rich: Cod liver oil, egg yolk, dry beans, dry fruits, wheat gram, yeast • Medium: Meat, chicken, fish, spinach, banana, apple • Poor: Milk and its products Daily Sources of Iron
AUGUST 21, 2026 12 Absorption of Iron • It is transported inside mucosal cells by DMT1 & across the basolateral membrane by the FP1 transporter protein. • Iron released into plasma binds to transferrin & is transported to different cells.
AUGUST 21, 2026 13 Vitamin B12: Cobalamine • It occurs as red crystals synthesised in nature only by microorganisms; plants and animals acquire it from them. • Deficiency causes megaloblastic anaemia and neurological damage. • Mechanism of Action: 1. Vitamin B12 is an essential constituent of the human diet, necessary for DNA synthesis and, consequently, for cell proliferation. 2. Vitamin B12 is important in the normal functioning of the nervous system due to its role in the synthesis of myelin and in the maturation of developing red blood cells in the bone marrow. 3. Lifelong therapy is needed in pernicious anaemia. • Dietary sources: Sea fish, egg yolk, meat, legumes, etc. • Daily requirement: 1 - 3 µg; pregnancy and lactation 3 – 5 µg.
AUGUST 21, 2026 14 Vitamin B9: Folic Acid • Chemically, it is Pteroylglutamic acid (PGA) consisting of pteridine + para-aminobenzoic acid (PABA) + glutamic acid. • Folic acid is a precursor needed to make, repair, and methylate DNA; a cofactor in cell division and growth, such as in infancy and pregnancy. • Folate is itself inactive. After absorption, it is converted into the active coenzyme, tetrahydrofolic acid, essential for amino acid and DNA biosynthesis and cell division. • Sources: Yeast, green vegetables, fruits, nuts and cereals • Daily requirements: 1. Adult: 50 mcg/day 2. Pregnant women: 100–200 mcg/day 3. Lactating women: 100–200 mcg/day
AUGUST 21, 2026 15 Copper • Copper is an essential trace element required for normal iron metabolism and erythropoiesis. • Mechanism of action: Copper activates the enzyme ceruloplasmin It converts Fe² → Fe³ ⁺ ⁺, loading of iron onto transferrin It causes iron delivery to bone marrow Leads to Hb synthesis and RBC formation
AUGUST 21, 2026 16 Erythropoietin • Erythropoietin Erythropoietin is a glycoprotein, normally produced by the kidneys, that regulates red blood cell production. • Actions: Induces haemoglobin formation & erythroblast maturation. • Epoetin (α, β) is a recombinant human erythropoietin administered by i.v. or s.c. injection and has a plasma half-life of 6-10 hr.
AUGUST 21, 2026 17  Coagulants • Coagulants are agents that enhance blood clotting by promoting coagulation pathways.  Hemostasis & Role of Coagulants: • Hemostasis prevents blood loss after vascular injury by forming a stable clot. • Used to manage haemorrhage, surgical bleeding and bleeding disorders. • Essential in trauma care, haemophilia and anticoagulant overdose.
AUGUST 21, 2026 18  Clotting Factors 1. Clotting factors as plasma proteins: These are specialised proteins circulating in the blood plasma in an inactive state, ready to respond when vascular injury occurs. 2. Activation by partial proteolysis: When a blood vessel is damaged, specific enzymes cleave these inactive proteins partially, converting them into their active forms. This activation triggers a cascade in which each activated factor stimulates the next, rapidly amplifying the clotting response. 3. Number and location of clotting factors: There are 12 primary clotting factors identified, present not only in the plasma but also within various tissues, ensuring a coordinated response to injury throughout the body. 4. Impact of factor deficiency: A lack or malfunction of any one of these clotting factors can disrupt the clotting cascade, leading to bleeding disorders such as haemophilia, which can cause excessive bleeding even from minor injuries.
AUGUST 21, 2026 19  Clotting Factor Factors Name Trick Factor I Fibrinogen Foolish Factor II Prothrombin People Factor III Tissue thromboplastin Try Factor IV Calcium Ions Climbing Factor V Labile Factor Long Factor VII Stable Factor Slopes Factor VIII Antihemophilic Factor After Factor IX Christmas Factor/ Plasma Thromboplastin Component Christmas Factor X Stuart-Prower Factor Some Factor XI Plasma Thromboplastin Antecedent People Factor XII Hageman Factor Have Factor XIII Fibrin Stabilizing Factor Fallen
AUGUST 21, 2026 20  Mechanism of Coagulation For blood to clot, a cascading series of proteolytic reactions is initiated by: 1. Contact activation of Hageman factor:  Intrinsic system  Slow and takes several minutes to activate factor X 2. Tissue thromboplastin:  Extrinsic system  Activates factor X in seconds  Clotting factors are present in the plasma in the inactive form  Active protease → activates the next factor
AUGUST 21, 2026 21 Coagulation Cascade
AUGUST 21, 2026 22  Classification of Coagulants
AUGUST 21, 2026 23  Vitamin K • Essential for hepatic synthesis of clotting factors II, VII, IX, X and proteins C & S. • Vit K1 – isolated from alfalfa grass • Vit K2 – isolated from Sardine (sea fish) • Deficiency leads to a prolonged bleeding tendency. • Causes: Malabsorption, prolonged antibiotic use, newborn deficiency. • Phytomenadione (K1) is used therapeutically. • Onset of action requires 6 –12 hours for factor synthesis. • Used in warfarin toxicity and neonatal bleeding prophylaxis. • Safe but may cause flushing or hypersensitivity with the IV form. • Dietary Source: Green leafy vegetables like cabbage, spinach and cheese, etc. • Daily Requirement: 50-100 mcg/day Alfalfa Grass Sardine Fish
AUGUST 21, 2026 24 Pharmacokinetics • Vitamin K1 is absorbed actively, while K2 and K3 are absorbed by simple diffusion. • It is stored in the liver. • It is metabolised in the liver by glucuronide conjugation. • Excreted in bile and urine. Uses • Dietary deficiency of Vitamin K • Prolonged antimicrobial therapy • Jaundice or malabsorption syndrome • Liver Disease • New born • Overdose of oral anticoagulants
AUGUST 21, 2026 25  Miscellaneous Fibrinogen • Employed in Hemophilia, antihemophilic globulin (AHG) deficiency & acute afibrinogenemic states. • 0.5 mg i.v. is infused. Antihemophilic Factor • Concentrated human AHG preparation. • Indicated in Haemophilia & AHG deficiency. • Highly effective, short-acting. Desmopressin • Synthetic vasopressin analogue. • Increases Factor VIII and its release from the endothelium. • Effective in mild Haemophilia A & von Willebrand disease.
AUGUST 21, 2026 26 Adrenochrome monosemicarbazone • Reduces capillary fragility & prevents microvessel bleeding. • Dose: 1-5 mg oral, i.m. Rutin • A plant glycoside claimed to reduce capillary bleeding. • Used along with Vit. C, which is believed to facilitate its action. • Dose: 60 mg b.d/t.d.s orally. Ethamsylate • It decreases capillary bleeding when platelets are adequate; probably exerts antihyaluronidase action & improves capillary wall stability. • It is used in capillary bleeding in menorrhagia after abortion and bleeding after tooth extraction.
AUGUST 21, 2026 27  Anticoagulants • Anticoagulants: These are medications designed to inhibit the blood's natural clotting process, reducing the risk of harmful clots forming inside blood vessels. They are crucial in managing conditions like deep vein thrombosis, pulmonary embolism and preventing stroke in patients with atrial fibrillation. • Coagulation initiation: When a blood vessel is injured, the body triggers a rapid response where platelets gather at the site, and clotting factors activate to form a stable clot. This immediate reaction is essential to minimise blood loss and begin tissue repair. • Blood solidification purpose: The transformation of blood from liquid to a gel-like clot serves two main functions: it prevents excessive bleeding by sealing the wound and acts as a barrier to block bacteria and other foreign substances from entering the bloodstream, thereby protecting against infection.
AUGUST 21, 2026 28  Classification of Anticoagulants
AUGUST 21, 2026 29 Heparin • Heparin is a non-uniform mixture of straight- chain mucopolysaccharides with a molecular weight of 10,000 to 20,000 Da. • Composed of polymers of two sulfated disaccharide units: D-glucosamine-L-iduronic acid and D-glucosamine-D-glucuronic acid. • Immediate anticoagulant action when given IV. • Found in all tissues containing mast cells; richest sources include lung, liver and intestinal mucosa. • Does not cross the placenta; safe in pregnancy. Heparin Activates Plasma AT III Heparin - AT III complex Prothrombin Thrombin Fibrinogen Fibrin No fibrin clot formation Inactivates Inactivates Parenteral Anticoagulants
AUGUST 21, 2026 30 Low Molecular Weight Heparins (LMWHs) • LMWHs are defined as heparin salts having an average molecular weight of less than 8000 Da. • These are obtained by various methods of fractionation or depolymerization of polymeric heparin. • Better bioavailability and longer duration. • Enoxaparin, Dalteparin: preferential Xa inhibition.
AUGUST 21, 2026 31 Fondaparinux • The pentasaccharide has a specific sequence that binds to AT-III with high affinity to inactivate factor Xa selectively. • Bioavailability – If injected s.c., is 100%. • Excreted unchanged by the kidneys.
AUGUST 21, 2026 32 Oral Anticoagulants Warfarin • It is a coumarin derivative. • Inhibits Vitamin K epoxide reductase, ↓ synthesis of factors II, VII, IX, X. • Oral administration; onset is slow (3–5 days) due to existing clotting factors. • Narrow therapeutic index requires careful titration. • Used in prosthetic valves and recurrent thrombosis prevention. • Highly protein-bound; numerous drug and food interactions. • Uses: DVT, pulmonary embolism and atrial fibrillation.
AUGUST 21, 2026 33 Mechanism of action of Warfarin
AUGUST 21, 2026 34 Dabigatran etixilate • It is an oral direct thrombin inhibitor. • Dabigatran inhibits thrombin directly. • Reversibly blocks the catalytic site of thrombin and produces a rapid (within 2 hours) anticoagulant effect. • Oral bioavailability is low. • The plasma t½ is 12–14 hours. • Duration of action: 24 hours.
AUGUST 21, 2026 35 Mechanism of action of Dabigatran
36  References 1) Essentials of Medical Pharmacology, 8th Edition by KD Tripathi. 2) Rang and Dale's Pharmacology, 8th Edition by H. P. Rang, J. M. Ritter, R. J. Flower, G. Henderson; Elsevier Churchill Livingstone. 3) Goodman and Gilman's The Pharmacological Basis of Therapeutics, 12th Edition by Laurence L. Brunton and Bjorn C. Knollmann. 4) Principles of Pharmacology by HL Sharma and KK Sharma, 2nd Edition, Paras Publication. AUGUST 21, 2026
T H A N K Y O U 37 AUGUST 21, 2026