Anti-Anemic Drugs, Hematinic

1. Anti-Anemic Drugs(Hematinics)
(Pharmacology & Therapeutics-1)
Lecture By
Dr. Syed Baqir Raza Naqvi
(BSc, Pharm-D, M. Phil-Pharmacology)
Nazar College of Pharmacy
DAKSON Institute of Health Sciences, Islamabad
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2. Anti-Anemics (Hematinics)
• Those agents/drugs which are used in the treatment of anemia are called anti-
anemic or hematinic drugs.
Anemia
• Anemia is the reduction in oxygen transporting capacity of blood due to
reduction in normal limits of total circulating red blood cell mass and hemoglobin
concentration.
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3. 3
Signs and symptoms of anemia

4. Major causes of anemia
1. Blood loss
• Acute i.e. due to trauma.
• Chronic i.e. due to GIT lesions.
2. Inadequate RBC’s production
• 1. Deficiency of essential factors
• Iron deficiency: which leads to hypochromic microcytic anemia.
• Intrinsic factor deficiency which leads to pernicious anemia.
• Vitamin-B12 deficiency leading to megaloblastic anemia.
• 2. Endocrine Deficiency
• Less erythropoietin (EPO) production.
• Bone marrow invasion: may be caused by; a). Leukemia b). Secondary carcinoma.
• Stem cell failure: the stem cell failure is cause aplastic anemia.
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5. 3. Increased RBC’s destruction
• It is also called as hemolytic anemia.
• 1. Intra-erythrocytic defects
• These may includes
• a). Hereditary spherocytosis. b). Thalassemia
• 2. Extra-erythrocytic defects
• a). Erythroblastosis fetalis b). Transfusion reactions c). Malaria
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6. 4. Drugs induced anemia
• A large number of drugs cause toxic effects on blood cells,
hemoglobin production or erythropoietic organs, which, in turn, may
cause anemia. For example Chloramphenicol, Thiouracil etc.
5. Nutritional anemia's
• Nutritional anemia’s are caused by dietary deficiencies of substances
such as iron, folic acid and vitamin B-12 (Cyanocobalamin) that are
necessary for normal erythropoiesis.
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7. Classification of Anti anemic drugs
Drugs used for iron
deficiency anemia.
• Ferrous sulphate
• Ferrous gluconate
• Ferrous succinate
• Ferrous pyrophate
• Iron dextran
• Iron sorbitol
Drugs for
megaloblastic
anemia.
• Vitamin B.12
• Folic acid
Hematopoietic
growth factors.
• Erythropoietin
• Interleukin-3
• Stem cell factors.
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Oral
Parenteral

8. General Pharmacodynamics (MOA) of Hematinic
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9. IRON
• Iron is the part of many important body constituents i.e.
hemoglobin, myoglobin and myoglobin enzymes etc.
• Iron concentration in hemoglobin is 0.34%.
• Iron is stored in intestinal mucosal cells, liver, spleen and bone
marrow as ferritin (which is a non-protein complex) until needed by
the body.
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10. Causes of iron deficiency in body
• Iron deficiency is due to acute or chronic blood loss, insufficient
intake during periods of accelerated growth in children, and in
heavily menstruating or pregnant women.
• Iron deficiency results from a negative iron balance due to depletion
of iron stores and/or inadequate intake, culminating in hypochromic
microcytic anemia (due to low iron and small-sized red blood cells).
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11. Symptoms of iron deficiency
• Iron deficiency also causes Koilonychia
(upward curvature of the finger and toe
nails).
• Soreness and cracking at the corners of
the mouth.
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Iron deficiency anemia may cause pica
(hunger for ice, dirt, paper, etc.).

12. Sources of Iron
• Food that contains high iron content include
organ meat (Liver, Heart), yeast, egg yolks &
certain dried beans and fruits.
• Foods that contains intermediate iron supply
include muscle meat, fish, green vegetables
and most cereals.
• Food, low in iron contents includes milk &
milk products and most non-green
vegetables.
• Iron cooking utensils sharply raise the iron
content of food.
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Daily requirements
• Men= 0.5 – 1 mg
• Women= 2 mg
• Pregnant’s= 5 - 6 mg
• In patients with iron
deficiency anemia, 150 to
180 mg/day of oral
elemental iron is
administered two to
three times daily.

13. Mechanism of action
• Iron is mainly involved in the formation of hemoglobin, which is the
protein found in red blood cells responsible for carrying oxygen from
the lungs to the rest of the body.
• The iron is incorporated into the “heme” portion of hemoglobin,
which helps to bind and carry oxygen.
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• When iron is absorbed through the diet, it is
transported to the bone marrow where it is
used to make new red blood cells.

14. • Iron also plays a crucial role in the production of myoglobin, another
protein that stores oxygen in muscle tissue.
• Iron is also involved in several enzyme reactions in the body, which are
essential for cellular metabolism and energy production.
• Iron is constantly being recycled in the body through a process known as
erythropoiesis, where old red blood cells are broken down and the iron is
released and reused for the production of new red blood cells, ensuring
that the body has a constant supply of this essential minerals.
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15. Absorption
• The absorption of iron occurs in the duodenum. Iron supplements are usually taken
orally and absorption is affected by the form of iron and the presence of other dietary
factors. Ferrous (Fe2+) and ferric (Fe3+) forms of iron are the most commonly used iron
supplements in clinical practice.
Distribution
• Iron is transported in the blood, bound to the protein transferrin. Transferrin delivers
iron to the tissues where it is stored in ferritin and used for various metabolic processes
such as the synthesis of hemoglobin, myoglobin, and iron-containing enzymes.
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Pharmacokinetics of iron

16. Metabolism
• Iron metabolism is regulated by a protein called hepcidin, which is produced
in the liver. It inhibits the absorption of iron by reducing the expression of iron
transporters in the intestine and promoting its sequestration into storage sites.
Elimination
• Iron is excreted from the body through the shedding of skin, hair, nails and
through the loss of blood during menstruation and childbirth. The body has
limited ability to excrete excess iron.
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17. Clinical Uses
• Iron is used in hypochromic microcytic anemia (Iron deficiency anemia)
Two types of iron preparations are available.
1. Oral iron Supplements
• These preparations are used in iron deficiency in infants, Children during
rapid growth periods and pregnant/lactating women.
2. Parenteral iron preparations
Used in patients with extensive chronic blood loss due to Past gastractomy
condition, mal absorption syndrome.
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18. Adverse effects of iron supplement
• Gastrointestinal (GI) disturbances caused by local irritation (abdominal
pain, constipation, diarrhea, etc.) and dark stools are the most common
adverse effects of oral iron supplements.
• Parenteral iron formulations may be used in those who cannot tolerate oral
iron.
• Fatal hypersensitivity and anaphylactic reactions can occur in patients
receiving parenteral iron (mainly iron dextran formulations).
• Antidote of iron: Excessive iron can cause toxicities that can be reversed
using chelators such as deferoxamine (Antidote of iron).
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19. Adverse effects of iron supplements
• Gastrointestinal side effects: Iron supplements can cause gastrointestinal side effects
such as nausea, vomiting, constipation, and diarrhea. These side effects can often be
minimized by taking iron supplements with food or using slow-release formulations.
• Iron overload: Excessive iron intake can lead to iron overload, a condition known as
hemochromatosis. Iron overload can damage the liver, pancreas, and heart and can
cause joint pain, fatigue, and other symptoms.
• Interference with absorption of other nutrients: High doses of iron can interfere with the
absorption of other nutrients such as calcium, zinc, and magnesium, which can lead to
• Allergic reactions: Some people may experience allergic reactions to iron
supplements, characterized by symptoms such as swelling, and difficulty breathing. 19

20. • Folic acid, also known as folate, is a water-soluble B vitamin that plays a
crucial role in many processes in the body.
• When folic acid is consumed from the diet or supplements, it is converted
to its active form, 5-methyltetrahydrofolate (5-MTHF), which is involved in
several important biochemical reactions in the body.
Sources
• Folic acid is found in liver extracts, in addition to liver, kidney, mushrooms,
yeast and particularly green leaves & grass contains this factor.
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FOLIC ACID (Vitamin-B9)

21. Causes of Folate deficiency
• Vitamin B9, is an essential nutrient that cannot be synthesized by
the body and must be obtained through the diet or supplements.
• Folic acid deficiency occurs when the body does not receive enough
folic acid to meet its needs. Some common causes of folic acid
deficiency include;
• Inadequate intake & Mal absorption.
• Certain medications.
• Alcoholism & Increased demand of folate.
• Deficiency in folic acid can lead to a wide range of health problems,
including megaloblastic anemia & Spina Bifida. Folic acid is
especially important for pregnant women who require extra folic
acid for proper fetal development.
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22. Mechanism of Actions of Folic Acid
1. DNA Synthesis: Folic acid plays a crucial role in this process by providing methyl groups for the
synthesis of DNA, RNA, and other important molecules in the body.
2. Amino acid metabolism: Folic acid plays role in the metabolism of amino acids, which are the
building blocks of proteins. It helps convert the amino acid homo-cysteine to methionine, which
can be used to synthesize proteins.
3. Red blood cell production: Folic acid is essential for the production of red blood cells in the
bone marrow. It is required for the synthesis of DNA during cell division, which is critical for the
maturation of red blood cells.
4. Pregnancy: Folic acid is crucial for a healthy pregnancy, as it plays a role in the development of the
nervous system in the fetus. Adequate folic acid intake before and during pregnancy can help
prevent neural tube defects, congenital malformations of the brain and spinal cord.
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23. Clinical Uses:
• Folic acid is used in the treatment &
prevention of folic acid deficiency which
cause megaloblastic anemia.
Adverse effects:
• Folic acid is non toxic to man because it is
promptly excreted in urine.
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24. • Vitamin B12 serves as a cofactor for several essential biochemical reactions in
human body.
• Deficiency of Vitamin B12 leads to anemia,
gastrointestinal symptoms and neurologic abnormalities.
Sources:
• Vitamin B12 is not found in plants.
• It is synthesized by microorganisms and is only found in bacteria and animal
tissues.
• Liver and kidneys are the chief source of vitamin B12. but it also occur in milk,
eggs & fish.
• Another source in men may be the intestinal bacteria.
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VITAMIN B12 (Cyanocobalamine)

25. • Deficiencies of vitamin B12 can result from either low dietary levels or
poor absorption of the vitamin due to the failure of gastric parietal
cells to produce intrinsic factor (as in pernicious anemia).
• Intrinsic factor is a glycoprotein produced by the parietal cells of the
stomach, and it is required for vitamin B12 absorption.
• In patients with bariatric surgery (surgical treatment for obesity),
vitamin B12 supplementation as cyanocobalamin is required in large
oral doses, sublingually or once a month by the parenteral route.
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26. • In addition to general signs and
symptoms of anemia, vitamin B12
deficiency anemia may cause
• Tingling (pins and needles) in the
hands and feet.
• Difficulty walking, dementia.
• In extreme cases, hallucinations,
paranoia or schizophrenia.
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27. Clinical uses:
• Used in the treatment of Vit.B12
deficiencies for e.g.;
• Used in megaloblastic anemia.
• Pernicious anemia.
• Neuropathy (specifically functional
disturbance in peripheral nervous
system).
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Daily requirements
• 2 mg (in both males & females)

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Adverse effects
• Parenteral injections of liver extracts
can causes mild to severe allergic
reactions.
• Local effects resembles a type Arthus
phenomenon (Inflammatory lesions)
without necrosis).
• General effects includes;
• Headache, chill, fever, dyspnea, itching,
urticaria and shocks.

29. Thank you ! 
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