Amity Institute of Pharmacy

Heamatinics

AMITY INSTITUTE OF PHARMACY

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

• 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.

Stem Erythroid
Bone marrow
cells precursors

erythropoietin

Kidney
Erythropoiesis

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 Anaemia Amity Institute of Pharmacy

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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 Amity Institute of Pharmacy

drug toxicity (e.g. anticancer drug)

radiation therapy
disease of bone marrow
reduce production of erythropoietin (e.g. chronic renal failure, 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.

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 Symptoms of Anaemia Amity Institute of Pharmacy

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 Amity Institute of Pharmacy

A. IRON
1. Oral preparations of iron (Fe2+) 2. Parenteral preparations of iron (Fe3+)

Ferrous sulfate Iron dextran

Ferrous succinate Iron-sorbitol-citric acid
Iron sucrose
Ferrous aminoate Ferric carboxymaltose
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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 IRON Amity Institute of Pharmacy

• 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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 Haemoglobin molecule Amity Institute of Pharmacy

• 1 Hb = 4 protein chain (globins)+ 4

heam moiety. Protein
chains
• Haem consists of : Tetrapyrrole
porphyrin ring containing ferrous
(Fe 2 +)ion.

• O2 molecule binds reversibly to Fe

2+ and to a histidine residue in the Iron-containing
(haem) group
globin chain.

The haemoglobin molecule

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 Iron : Absorption Amity Institute of Pharmacy

• Site of absorption - duodenum and upper jejunum.

• In stomach iron dissolves and binds to mucoprotein (carrier).

Dietary iron in ferric form (Fe 3 +) is low soluble in neutral pH and not absorb.

Ascorbic acid

Reduce to ferrous form (Fe 2 +) + vitamin C.

Soluble iron-ascorbate chelate

Absorption occurs.

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 Iron : transport Amity Institute of Pharmacy

Iron enters in plasma in ferrous form

oxidise

Immediately into ferric form

Complex with transferrin a carrier (glycoprotein)

Storage in the mucosal cell To the plasma

as ferritin
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 Iron : Storage & Excretion Amity Institute of Pharmacy

• In two forms : Ferritin & Haemosiderin.

Aggregates
Apoferritin + ferric (Fe 3 +) Haemosiderin

Ferritin

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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 Iron Preparations Amity Institute of Pharmacy

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.
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 Parenteral Iron Preparations Amity Institute of Pharmacy

• 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 Amity Institute of Pharmacy

• 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 Amity Institute of Pharmacy

• 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
Amity Institute of Pharmacy

• A B12 deficiency will cause a pernicious

Oesophagus
Vitamin B12
anemia and it take up to two years to
ingested
develop.
• Source: In food, meat, fish, eggs Stomach
IF Intrinsic
• Vitamin B12 is essential for cell growth and factor

multiplication

• Absorption of B12 : binds with intrinsic

factor (IF) in the stomach. The B12-IF Distal ileum
complex then travels through the small
intestine and is absorbed in the distal ileum.

Site of B12 absorption

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 Maturation factors : Vitamin B12
Amity Institute of Pharmacy

• 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
Amity Institute of Pharmacy

• Source in food – yeast, egg yolk, liver and leafy vegetables.

• Folic Acid is absorbed in the small intestines.

• Folic acid 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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 Uses of Folic acid Amity Institute of Pharmacy

1) In megaloblastic anaemia due to inadequate dietary intake of folic acid

• Can be due to chronic alcoholism, malabsorption syndromes, cancer or
hepatic disease.

2) Increased demand : pregnancy, lactation, premature infancy, RA, etc.

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 Haemopoietic Growth Factors
Amity Institute of Pharmacy

• 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
Amity Institute of Pharmacy

Anaemia due to:

• Chronic renal failure.

• Cancer chemotherapy.

• AIDS.

• Premature infants.

• Chronic inflammatory disorders (RA).

• In Chronic Heamolytic Anaemia.

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 Refrence Amity Institute of Pharmacy

• 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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