this ppt referes to pharma cology 2 which is a 5th semister subject of B pharmacy 3rd YEAR

1. Haematinics , coagulants and anticoagulants
PHARMACOLOGY-II
BP-503T
UNIT-II
By
Navya Manyala
Academic year-2023-24

2. HAEMATINICS are the agents used for formation of blood to treat various types of anemia's. These
include: Iron, Vitamin B and Folic Acid.
• Deficiency in Hematinics can lead to anemia.
• MOA: These drugs increase renal and non-renal Erythropoietin (EPO) , which is a hormone that stimulates
erythropoiesis and increase the hemoglobin content of the blood.
• Uses of haematinics: this are generally used in treatment of different anaemic conditions as follows:
a) Blood loss:
• Acute haemorrhagic anaemia
• Chronic haemorrhagic anaemia
• Surgery
b) Impaired red cell formation:
• Deficiency of essential factors i.e. IRON, Vit.B12,,Folic acid
• Bone marrow depression(hypoplastic anaemia)
• Infection, renal failure, liver disease, cancer etc.
c) Increased destruction of RBCs
• Due to corpuscular defects(intrinsic abnormality)
• Due to abnormal haemolysis(Extrinsic defects)

3. Side effects of Heamatinics:
•Heartburn
•Stomach pain
•Loss of appetite
•Nausea
•Vomiting
•Diarrhea
•Constipation
•A change in the color of your stools.

4. Classification:

5. Coagulation is the process by which blood forms clots, in
this process blood loses its fluidity and becomes a jelly-
like mass. Clotting factors and anticoagulants are made in
the liver. They have the ability to turn on or turn off as
needed.
Clotting factors and
anticoagulants are made in the
liver. They have the ability to turn
on or turn off as needed.
Clotting factor VI is unknown.

6. Coagulation
It is the process by which blood forms clots, in this process blood loses its fluidity and becomes a jelly-
like mass. Clotting factors and anticoagulants are made in the liver. They have the ability to turn on or
turn off as needed.
The drugs which promote blood coagulation & used in the treatment of hemorrhagic disorders are
called as coagulants. They are also called hemostatic agents.
• These drugs are of two types –
Coagulant
Depending on their action Depending on their Nature

7. Systemic coagulants: Vitamin-K
• Vitamin K (Coagulation vitamin) is essential for the coagulation process.
• It is not directly involved in the clotting process but required for the synthesis of four clotting factors in the
liver: Factor II,VII,IX and X.It occurs naturally in two forms: – Phylloquinone (K1) from plant source and –
Menaquinone (K2) which is synthesized by colonic bacteria (E.coli) in the colon.
• K3 is the synthetic form and is available as – Fat-soluble forms (Menadione, Acetomenaphthone) and –
water-soluble forms (Menadione sod. Bisulfate and Menadione sod. Diphosphate).
Dietary sources:
– Green leafy vegetables such as cabbage, spinach and liver, cheese, cereals, nuts, and egg yolk etc.
– Wheat germ oil is the richest source.
Physiological functions: – Vit-K is essential for formation of clotting factor-II, VII, IX, X, protein-C & S.
Cause of Deficiency: 1. Vit-K is only temporarily concentrated in liver and this store can be exhausted
within one week. 2. The deficiency of vit-K occurs due to liver disease, obstructive jaundice, malabsorption,
long-term antimicrobial therapy, which alters intestinal flora.
Deficiency Symptoms- The most important manifestation is bleeding tendency due to lowering of the levels
of prothrombin and other clotting factors in blood.
(a) Dietary deficiency
(b) Prolonged antimicrobial therapy
(c) Obstructive jaundice or malabsorption syndromes
(d) Liver disease (cirrhosis, viral hepatitis)
(e) Newborns & Overdose of oral anticoagulants.
Useof vitK

8. • It occur as bright yellow crystal, insoluble in water.
• It has very faint acrid acid.
• It get metabolized in liver by glucuronidation to give inactive metabolites.
site of Action: It is a vitamin k3 and is involved as a cofactor in the carboxylation of glutamic acid residues of
certain protein in the body. These protein are vitamin K dependent coagulation factors II, VII, IX and X.
Uses: 1. It is used in treatment of hypothrombinemia 2. It is used in nutritional supplement in animal feed as it
has some vitamin K activity.
• It is white solid, very soluble in water and is stable under normal temperature and pressure.
• It must be stored in tightly closed in container.
Mechanism of Action: It maintain normal blood clotting and act by reducing excessive bleeding.
Uses: It is used to treatment of coagulation disorder due to vitamin K deficiency.
Menadione
Acetomenapthone
Fat soluble Coagulant

9. In vivo used drugs
A. Parenteral anticoagulants
(i) Indirect thrombin inhibitors: Heparin, Low
molecular weight heparins, Fondaparinux, Danaparoid
(ii) Direct thrombin inhibitors: Lepirudin, Bivalirudin,
Argatroban
B. Oral anticoagulants
(i) Coumarin derivatives: Bishydroxycoumarin ,
Warfarin sod, Acenocoumarol, Ethylbiscoumacetate
(ii) Indandione derivative: Phenindione.
(iii) Direct factor Xa inhibitors: Rivaroxaban
(iv) Oral direct thrombin inhibitor: Dabigatran
etexilate
Anticoagulants, commonly referred to as blood thinners, are chemical substances that
prevent or reduce coagulation of blood, prolonging the clotting time. Drug used to
reduce the coagulability of blood
Used in vitro
A. Heparin:
150 U to prevent clotting of 100 ml blood.
B. Calcium complexing agents:
• Sodium citrate: 1.65 g for 350 ml of blood; used to
keep blood in the fluid state for transfusion.
• Anti coagulant acid citrate dextrose solution : 2.2
g/100 ml (75 ml is used for 1 unit of blood).
• Sodium oxalate:
10 mg for 1 ml blood
Sodium edetate:
2 mg for 1 ml blood
used in blood taken for
investigations

10. Heparin
• As because at first it was obtained from liver so it is named as Heparin.
• It is present in all tissues containing mast cells; richest sources are lung, liver and intestinal mucosa. Commercially it
is produced from ox lung and pig intestinal mucosa.
• Heparin is of two types : Unfractioned Heparin & Low molecular weight heparin.
• Heparin is a powerful and instantaneously acting anticoagulant, effective both in vivo and in vitro.
Mechanism of action of heparin, LMW heparin & Fondaparinux:
• Heparin acts indirectly by activating plasma antithrombin III (AT III, a serine proteinase inhibitor).
The heparin-AT III complex then binds to clotting factors of the intrinsic and common pathways (Xa, IIa, IXa, XIa, XIIa
and XIIIa) and inactivates them.
• At higher doses inhibits platelet aggregation and prolongs bleeding time.
• At low concentrations of heparin, factor Xa mediated conversion of prothrombin to thrombin is selectively affected.
• The anticoagulant action is exerted mainly by inhibition of factor Xa as well as thrombin (IIa) mediated conversion of
fibrinogen to fibrin.
• Heparin Inhibitory action requires contact between Xa & AT III as well as contact between IIa with AT III & GAG
of heparin (Ternary complex)
• LMW heparin Inhibitory action of requires contact between LMW heparin,Xa & AT III
• Fondaparinux Inhibitory action requires contact between fondaprinux,Xa & AT III

12. Contraindications
1. Bleeding disorders, history of heparin induced thrombocytopenia.
2. Severe hypertension (risk of cerebral haemorrhage),threatened abortion, piles, g.i. ulcers (risk of aggravated
bleeding).
3. Subacute bacterial endocarditis (risk of embolism), large malignancies (risk of bleeding in the central necrosed area
of the tumour), tuberculosis (risk of hemoptysis).
4. Ocular and neurosurgery, lumbar puncture.
5. Chronic alcoholics, cirrhosis, renal failure.
6. Aspirin and other antiplatelet drugs should be used very cautiously during heparin therapy
Therapeutic uses:
1. Preferred anticoagulant during pregnancy.
2. Used for patients undergoing open heart surgery & renal dialyses.
3. Low dose therapy is used to prevent post operative venous thrombosis.
4. Used for treating disseminated intravascular coagulation(complex disorder ,where fibrin clots are formed
throughout vascular system).
5. Used as an adjuvant for the thrombolytic therapy for acute MI
Pharmacokinetics: Heparin is a large, highly ionized molecule; therefore not absorbed orally.
• Injected i.v. it acts instantaneously, but after s.c. injection anticoagulant effect develops after ~60 min.
• Bioavailability of s.c. heparin is inconsistent.
• Heparin does not cross blood-brain barrier or placenta (it is the anticoagulant of choice during pregnancy).
• It is metabolized in liver by heparinase and
• fragments are excreted in urine.

13. ORAL ANTICOAGULANTS
Warafarin sodium
It is most popular oral anticoagulant because it interfering with the synthesis of vit K dependent clotting factors in liver,
so it only act by in vivo not by invitro. The another reason of using oraly is It is very soluble in water.
Uses: It is commonly used to treat blood clots such as deep vein thrombosis and pulmonary embolism.
Used to prevent stroke in people who have atrial fibrillation, valvular heart disease or artificial heart valves.
Adverse effects:
1. Bleeding: Causes Haematuria(bleeding in urine), Gingival bleeding(bleeding gums), Epistaxis (bleeding from
nose), Haemoptysis(blood with sputum during cough ), melena(blood in stools due to bleeding in upper GIT).
2. Heparin induced Thrombocytopenia: This occurs by the formation of Heparin complex with PF4, which
produces IgG. This IgG binds with complex and forms platelet plug leading to clot. This PF4-Heparin-IgG
complex is destroyed in spleen which causes destruction of Platelets leading to thrombocytopenia.
3. Transient & reversible Alopecia
4. Osteoporosis
5. Hypersensitivity reactions.

14. Side effects