This document discusses haematinics, which are substances required for blood formation and used to treat anaemias. It defines anaemia and lists common causes such as blood loss, increased red blood cell destruction, and deficiencies in iron, vitamin B12, or folic acid. The document categorizes and describes common haematinics including oral and parenteral iron preparations, vitamin B12, folic acid, and erythropoietin. It provides details on absorption, transport, storage and excretion of iron as well as clinical uses of various haematinics to treat different types of anaemia.

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AMITY UNIVERSITY UTTAR
PRADESH
AMITY INSTITUTE OF PHARMACY
LUCKNOW
2018-20Presented by-
Afreen Hashmi
M.Pharm.(Pharmacology)
1st
sem
Enroll no. A8454918005
Guided by-
Dr. Himani Awasthi
Associate Professor
Department of Pharmacology
Amity Institute of Pharmacy
Heamatinics

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Haematinics
• Haematinics are substances required in the formation of blood, and are used for
treatment of anaemias.
• Hematopoiesis : Production of circulating erythrocytes, leukocytes and platelets from
bone marrow stem cells, is called hematopoiesis.
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Kidney
Bone marrow
erythropoietin
Erythroid
precursors
Stem
cells
Erythropoiesis

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Anaemia is reduced concentration of haemoglobin in the blood i.e. deficiency in
oxygen-carrying erythrocytes.
Normal values: Male = 13.2 -17.0 g/dL
Normal values: Female = 12.0 -16.0 g/dL
Causes :
• Anaemia occurs when balance between production and destruction of RBCs are
disturbed by :
i) Blood loss (acute or chronic) for eg. In menstruation and trauma conditions.
ii) Increased destruction of RBCs ( i. e. hemolytic anemia)
iii) Impaired red cell formation due to
– Deficiency of iron, Vitamin B12, folic acid.
– Bone marrow depression caused by :
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Anaemia

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drug toxicity (e.g. anticancer drug)
radiation therapy
disease of bone marrow
reduce production of erythropoietin (e.g. chronic renal failure, RA, AIDS)
Types of Anaemia
1.Microcytic Anaemia : deficiency of Iron.
2.Macrocytic Anaemia : deficiency of folic acid and B12.
3.Pernicious Anaemia : Lack of intrinsic factor INF.
4.Aplastic Anaemia : due to Bone marrow dysfunction.
5.Haemolytic anaemia : Excessive haemolysis.
6.Sickle cell anaemia : Sickle shaped RBCs. 4

5. Amity Institute of PharmacySymptoms of Anaemia
The main symptom of anaemia is fatigue but, especially if it is chronic, is often
surprisingly asymptomatic.
Other symptoms include :
•weakness,
•pale skin,
•rapid heartbeat,
•shortness of breath.
•chest pain,
•dizziness,
•irritability (in children with anaemia),
•coldness in hands and feet.
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Classification of Haematinics
A. IRON
1. Oral preparations of iron (Fe2+
)
Ferrous sulfate
Ferrous succinate
Ferrous aminoate
Ferrous fumarate
Ferrous gluconate
Carbonyl iron
B. Maturation factor :
Vitamin B12 : Cyanocobalamin, Hydroxocobalamin, Methylcobalamin.
Folic acid : Folinic acid (Leucovorin, Fastovorin ).
C. Hematopoietic Growth Factors :
Erythropoietin: Epoetin alfa, Epoetin beta, Darbepoetin alfa
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2. Parenteral preparations of iron (Fe3+
)
Iron dextran
Iron-sorbitol-citric acid
Iron sucrose
Ferric carboxymaltose

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IRON
• All body cells need iron. It is crucial for oxygen transport, energy production, and cellular
growth and proliferation.
• The human body contains an average 3.5 g of iron (males 4 g, females 3 g).
• Typical daily normal diet contains 10–20 mg of iron. 5 - 10% of ingested iron is absorbed i.e.
1-2mg.
• Daily loss is about – 0.5-1mg.
Distribution :
• About 65% iron circulates in blood as haemoglobin.
• 25% stored in Liver, spleen and bone marrow as Ferritin and haemosiderin available for
haemoglobin synthesis.
• Rest present in Myoglobin, cytochrome and various enzymes.
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8. Amity Institute of PharmacyHaemoglobin molecule
• 1 Hb = 4 protein chain (globins)+ 4
heam moiety.
• Haem consists of : Tetrapyrrole
porphyrin ring containing ferrous
(Fe2 +
)ion.
• O2 molecule binds reversibly to Fe 2+
and to a histidine residue in the
globin chain.
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Protein
chains
Iron-containing
(haem) group
The haemoglobin molecule

9. Amity Institute of PharmacyIron : Absorption
• Site of absorption - duodenum and upper jejunum.
• In stomach iron dissolves and binds to mucoprotein (carrier).
Dietary iron in ferric form (Fe3 +
) is low soluble in neutral pH and not absorb.
Reduce to ferrous form (Fe2 +
) + vitamin C.
Soluble iron-ascorbate chelate
Absorption occurs.
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Ascorbic acid

10. Amity Institute of PharmacyIron : transport
Iron enters in plasma in ferrous form
oxidise
Immediately into ferric form
Complex with transferrin a carrier (glycoprotein)
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Storage in the mucosal cell
as ferritin
To the plasma

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Iron : Storage & Excretion
• In two forms : Ferritin & Haemosiderin.
Apoferritin + ferric (Fe3 +
) Haemosiderin
Excretion by:
• Exfoliation/ desquamation of GI mucosal cells (ferritin stored in it) : the process is
called ferritin curtain.
• Small amount in bile, sweat and urine.
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Aggregates
Ferritin

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Iron Preparations
Oral Iron Preparations :
•Preferred route.
•Dissociable ferrous salts : inexpensive, increased iron content, better absorbed.
– Ferrous Sulfate - Cheapest form of Iron and one of the most widely used.
– Side Effects are extremely mild:
• Nausea, upper abdominal pain, constipation or diarrhea.
Parenteral Iron Preparations
May be given when-
•Oral iron not tolerated : bowel upset is too much.
•Not absorbed orally : malabsorption, surgical procedures, inflammatory condition
(RA).
•In patients with : chronic renal failure, chemotherapy-induced anaemia. 12

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Parenteral Iron Preparations
• Iron-dextran: slow iv or deep im (50mg/ml)
circulated without binding to transferrin, not excreted in urine or in bile.
• Iron-sorbitol-citric acid: only im (not favored now because producing higher side
effects.
• Iron sucrose : iv injection
Less side effects, safer drug than older preparations.
• Ferric carboxymaltose : iv only
less side effects, anaphylaxis is rare.
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Toxicity of Iron Overload
• Acute iron toxicity
• Chronic iron toxicity
• Treated by : Desferrioxamine – an iron chelator (DOC)
- It bound with ferric & unbound iron, not absorbed from the gut & prevent its
absorption.
- In severe poisoning, it is given by slow iv infusion.
Deferiprone - orally absorbed iron chelator
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Clinical Uses of Iron
• To treat iron deficiency anaemia which can be caused by:
-chronic blood loss (e.g. menorrhagia, trauma, colon cancer)
-increased demand (e.g. in pregnancy and premature babies, menstruating
womens)
-Inadequate dietary intake
-Inadequate absorption (e.g. following gastrectomy)
• In GI Bleeding due to: Ulcers, Aspirin, Excess consumption of coffee
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Maturation factors : Vitamin B12
• A B12 deficiency will cause a pernicious
anemia and it take up to two years to
develop.
• Source: In food, especially in liver and
kidneys.
• Vitamin B12 is essential for cell growth and
multiplication
• Absorption of B12 : binds with intrinsic
factor (IF) in the stomach. The B12-IF
complex then travels through the small
intestine and is absorbed in the distal ileum.
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Distal ileum
Site of B12 absorption
Oesophagus
Stomach
IF Intrinsic
factor
Vitamin B12
ingested

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Maturation factors : Vitamin B12
• Cyanocobalamine
• Hydroxycobalamine
• Methylcobalamine
Actions
• Vitamin B12 is required for two main reactions :
– The conversion of methyl-FH4(inactive) to FH4(active). Necessary for
normal DNA synthesis.
– The conversion of methylmalonyl-CoA to succinyl-CoA.
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Maturation factors : Folic acid
• Source in food – yeast, egg yolk, liver and leafy vegetables.
• Folic Acid is absorbed in the small intestines.
• Folic Acid deficiency (F.A. Deficiency) is also called Will’s Disease.
• Deficiency may produce megaloblastic anemia; teratogenic effects.
• Folic acid and vitamin B12 required for maturation of haemoglobin.
Actions of Folic acid
• Folic acid is inactive and is converted to tetrahydrofolate by dihydrofolate reductase.
• This enzyme reduces dietary folic acid to FH4 and also regenerates FH4 from FH2.
• It is generally given orally.
• Folinic acid is synthetic preparation of folic acid.
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19. Amity Institute of PharmacyUses of Folic acid
1) In megaloblastic anaemia due to inadequate dietary intake of folic acid
• Can be due to chronic alcoholism, malabsorption syndromes, cancer or
hepatic disease.
1) Increased demand : pregnancy, lactation, premature infancy, RA, etc.
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Haemopoietic Growth Factors
• Erythropoietin is required for erythropoiesis.
• Erythropoietin is a hormone produced in juxtatubular cells in the kidney which
regulated division and differentiation of blood cells.
• Erythropoietin deficiency also results in anaemia.
• Erythropoietin preparations :
1.Epoeitin α and β (recombinant erythropoietin) ; given parenteraly only.
2.Darbopoeitin ; is longer acting preparation.
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Clinical Uses of Epoietin
Anaemia due to:
• Chronic renal failure.
• Cancer chemotherapy.
• AIDS.
• Premature infants.
• Chronic inflammatory disorders (RA).
• In Chronic Heamolytic Anaemia.
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Refrence
• Rang & Dale’s Pharmacology 6th Edition
• Bertram G.Katzung Basic And Clinical Pharmacology
• Principles Of Pharmacology Hl.Sharma Kk.Sharma
• http://slideshare.com
• http://slideplayer.com
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