DRUGS FOR HEMATOLOGIC

DISORDERS
GROUP 3:
JARAVATA, MARIE JULE
ORALLO, MA. ELENA
PADILLA, ANGELI MARIE
HEMATINIC AGENTS
General term for those nutrients, including iron, folic
acid, and vitamin B12, required for the formation and
development of blood cells in bone marrow (the
process of haematopoiesis), deficiency of which may
result in anaemia.
Treatment of anemia
Increase the number of RBC or hemoglobin content of
RBC or both when there is deficiency
Anemia
Not a single disease
 Results from a number of different pathologies
 Defined as a reduction from the normal quantity of
Hb in blood
WHO defines anemia as Hb levels less than 13 g/dl for
males and less than 12 g/dl for females
Low Hb levels results in decreased oxygen carrying
capacity of blood
Causes of Anemia
chronic blood loss,
bone marrow abnormalities,
increased hemolysis,
infections, malignancy,
 endocrine deficiencies,
renal failure
AGENTS USED TO TREAT ANEMIAS
A. Iron deficiency anemias
 Iron
Pharmacokinetics :
Absorption:
Absorbs 5–10% of iron ingested or about 0.5–1 mg daily.
Normally absorbed in the duodenum and proximal
jejunum.
Absorption increases in response to low iron stores or
increased iron requirements
STORAGE
primarily as ferritin, in macrophages in the liver, spleen,
and bone, and in parenchymal liver cells. Apoferritin
synthesis is regulated by the levels of free iron.
Ferritin is detectable in serum. Since the ferritin present
in serum is in equilibrium with storage ferritin in
reticuloendothelial tissues, the serum ferritin level can
be used to estimate total body iron stores.
Transport:
transported in the plasma bound to transferrin, a -globulin
that specifically binds two molecules of ferrous iron
The transferrin-iron complex enters maturing erythroid cells by
a specific receptor mechanism. Transferrin receptors
internalize the transferrin-iron complex through the process
of receptor-mediated endocytosis.
Increased erythropoiesis is associated with an increase in the
number of transferrin receptors on developing erythroid cells.
Iron store depletion and iron deficiency anemia are associated
with an increased concentration of serum transferrin.
ELIMINATION
Small amounts are lost in the feces by exfoliation of
intestinal mucosal cells, and trace amounts are
excreted in bile, urine, and sweat.
 Oral iron therapy
SimD
Class IRON
MOA Supplementation with elemental iron corrects
the iron deficiency. The CDC recommends 150 to 180 mg/day
of oral elemental iron administered in divided doses two to three
times daily for patients with iron deficiency anemia.
Uses Prophylactic use : 1) pregnancy- from 4th month to lactation. 2)
Menstruation 3) Infancy and childhood 4) Premature babies and babies
weaned late 5) Professional blood donors
Therapeutic use : 1) Iron deficiency anemia 2) Iron deficiency anemia
due to: - menorrhagia - peptic ulcer - piles - hook worm infestation 3)
Malabsorption syndrome 4) Anemia of pregnancy 5) Treatment of
severe pernicious anemia
SE nausea,epigastric discomfort, abdominal cramps, constipation, and
diarrhea, black stools
Notes
 Ferrous gluconate
SimD
Class IRON
MOA Ferrous gluconate is used in the prevention and treatment of iron-
deficiency anaemia. It replaces Fe found in Hb, myoglobin and enzymes.
It also allows transportation of oxygen via Hb
Uses Iron-deficiency anaemia

SE GI: GI discomfort, anorexia, nausea, vomiting, heartburn, constipation or

diarrhroea, faecal impaction, dark stools, dental discolouration.
Genitourinary: Urine discolouration.
Dermatologic: Allergic reactions, contact dermatitis.
Notes Less elemental iron, but similar tolerability to
ferrous sulfate
 Ferric ammonium citrate

SimD

Class IRON

MOA It exerts haematinic action by being an essential constituent of

haemoglobin. It is necessary for the oxidative process of living tissues

Uses Iron-deficiency anaemia

SE Gastrointestinal problems
Stomach pain
Black stools

Notes •Less bioavailable than ferrous salts

• Must be reduced to ferrous form in the intestine
 Ferrous fumarate

SimD

Class Vitamins & Minerals

MOA Ferrous fumarate replaces Fe found in Hb, myoglobin, and enzymes. It

allows the transportation of oxygen via Hb

Uses Iron-deficiency anaemia

SE GI: Nausea, vomiting, GI discomfort, epigastric pain, constipation or

diarrhoea, anorexia, dark stool, dental discolouration, heartburn.
Genitourinary: Urine discolouration.

Notes •Similar effectiveness and tolerability to ferrous

sulfate
• Almost no taste compared to other iron salts
 Ferrous sulfate
SimD Ferrous sulfate, anhydrous
Class Vitamins & Minerals
MOA Ferrous sulfate facilitates O2 transport via Hb. It is used as iron source as
it replaces Fe found in Hb, myoglobin and other enzymes.
Uses Iron-deficiency anaemia

SE GI: Epigastric pain, GI discomfort, nausea, vomiting, constipation or

diarrhoea, faecal impaction, dark stools, anorexia, reversible dental
staining.
Genitourinary: Urine discoloration.
Dermatologic: Allergic reactions.
Notes •Most common oral iron supplement
• Low cost with good effectiveness and tolerability
Ferrous sulfate, anhydrous:
•Extended-release formulation of ferrous sulfate
(once daily dosing)
• Higher cost than ferrous sulfate
 Carbonyl iron
SimD
Class Vitamins & Minerals
MOA Iron formulations exerts haematinic action by being an essential
constituent of haemoglobin. It is necessary for the oxidative process of
living tissues.
Uses Iron-deficiency anaemia

SE Nausea, Epigasttric distress, Vomiting, Constipation,Diarrhoea,Black

stools, Temporary staining of teeth with liquid formulations
Notes •Microparticles of puried iron
• Dissolves in the stomach to form HCl salt to be
absorbed
• Less toxic than iron salts due to slower absorption
rate (continued iron release for 1 to 2 days)
 Polysaccharide-iron complex
SimD
Class Vitamins & Minerals
MOA Ferrous sulfate facilitates O2 transport via Hb. It is used as iron source as
it replaces Fe found in Hb, myoglobin and other enzymes
Uses Iron-deficiency anaemia

SE GI: Epigastric pain, GI discomfort, nausea, vomiting, constipation or

diarrhoea, faecal impaction, dark stools, anorexia, reversible dental
staining.
Genitourinary: Urine discoloration.
Dermatologic: Allergic reactions
Notes • Tasteless and odorless
• Similar bioavailability to ferrous sulfate
Parenteral iron therapy
Iron dextran
SimD
Class IRON
MOA Iron dextran is used for the treatment of iron-deficiency anaemia where
oral therapy is ineffective or impracticable. Released iron replaces the
depleted iron stores in the bone marrow where it is used in the
synthesis of haemoglobin
Uses Fe-deficiency anaemia
SE headache, light-headedness, fever,
arthralgias, nausea and vomiting, back pain, flushing, urticaria,
bronchospasm, and, rarely, anaphylaxis and death
Notes Absorption: IM admin: Absorbed mainly through the lymphatic
system. IV admin: Taken up by cells of the reticuloendothelial system;
especially in the liver and spleen.
Excretion: Urine and feces via reticuloendothelial system.
 Sodium ferric gluconate complex
SimD

Class IRON

MOA Iron formulations exerts haematinic action by being an essential

constituent of haemoglobin. It is necessary for the oxidative process of
living tissues.

Uses Treatment of Iron deficiency in patients undergoing chronic

haemodialysis who are receiving supplemental erythropoietin therapy

SE Diarrhoea, Nausea, Vomiting, Anorexia, Fever, Flue like syndrome,

Arthralgia, Myalgia, Headache, Dizziness, Malaize, Rashes, Brdycardia,
Tachycardia, Myocardial infarction, Angina, Sepsis, Flatulence, Fatigue,
Injection site reactions, Hypersensitivity reactions

Notes
 Iron Sucrose Complex
SimD
Class IRON
MOA IV Iron Sucrose Normal erythropoiesis depends on the concentration
of iron and erythropoietin available in the plasma, both being decreased
in renal failure. Exogenous administration of erythropoietin increases red
blood cell production and iron utilization, contributing to iron deficiency
in hemodialysis patients.

Uses Fe deficiency anemia

SE Hypotension, chest pain, HTN, hypervolemia, CHF, cramps,
musculoskeletal pain, diarrhea, nausea, vomiting, abdominal pain,
elevated liver enzymes, skin irritation, pruritus, application site reaction,
dizziness, dyspnea, pneumonia, cough, headache, fever, asthenia,
malaise.
Notes
 Ferric carboxymaltose

SimD

Class Iron preparations

MOA Ferric carboxymaltose is a colloidal iron (III) hydroxide in complex

with carboxymaltose, a carbohydrate polymer that releases iron.

Uses Fe deficiency when oral Fe prep are ineffective or cannot be used.

SE Hypophosphataemia; headache, dizziness; flushing, HTN; nausea;

inj/infusion site reactions

Notes
 Ferumoxytol
SimD
Class Iron Preparations
MOA comprised of a superparamagnetic iron oxide that is coated with a
carbohydrate shell, aiding in the isolation the bioactive iron from plasma
components until the iron-carbohydrate complex enters the
reticuloendothelial system macrophages of the liver, spleen and the bone
marrow 17.
Uses treatment of iron deficiency anemia (IDA) in adult patients:
who have intolerance to oral iron or have had unsatisfactory response to
oral iron or who have chronic kidney disease (CKD)
SE diarrhea, headache, nausea, dizziness, hypotension, constipation, and
peripheral edema.
Notes
 Deferoxamine

SimD

Class IRON CHELATORS

MOA Chelates excess iron

Uses Acute iron poisoning; inherited or

acquired hemochromatosis

SE Rapid IV injection: Flushing, urticaria, hypotension and shock. SC or IM

injection: Local pain. Prolonged SC: Pruritus, erythema and swelling. GI
disorders, dysuria, fever, allergic skin rashes, tachycardia, cardiac
arrhythmias, convulsions and leg cramps; visual disturbances, cataract
formation, hearing loss; may retard growth in very young childn.
Pulmonary syndrome with high IV doses.

Notes
B. Vitamin deficiency Anemia
Folacin
SimD Pteroylglutamic acid, leucovorin
Class FOLIC ACID
MOA Precursor of an essential donor of methyl groups used for synthesis of
amino acids, purines, and deoxynucleotide
Uses Folic acid deficiency, which manifests as megaloblastic anemia, and
prevention of congenital neural tube defects

SE Cardiac disorders: Flushing.
Gastrointestinal disorders: Anorexia, nausea, abdominal distention,
flatulence.
Immune system disorders: Allergic reactions.
Nervous system disorders: Malaise.
Respiratory, thoracic and mediastinal disorders: Bronchospasm.
Skin and subcutaneous tissue disorders: Erythema, pruritus, skin rash,
hypersensitivity.

Notes
C. Red cell deficiency anemia
Epoetin alfa
SimD Darbepoetin alfa
Class Hematopoetic agents
MOA Agonist of erythropoietin receptors expressed by red cell progenitors
Uses Anemia, especially anemia associated with chronic renal failure, HIV
infection, cancer, and prematurity • prevention of the need for
transfusion in patients undergoing certain types of elective surgery
SE Edema, Pruritus, Nausea/Vomiting,Hypertension, CVA, Thrombosis
Notes Darbepoetin alfa: Long-acting glycosylated form administered weekly
• Methoxy polyethylene glycol-epoetin beta: Long-acting form 
administered 1–2 times per month
D. Sideroblastic anemias
Pyridoxine
SimD
Class Vitamin b complex
MOA Pyridoxine is a water-soluble vitamin which functions in the
metabolism of carbohydrates, proteins and fats. It is essential in Hb
formation and GABA synthesis within the CNS. It also aids in the
release of glycogen stored in the liver and muscles
Uses Treatment of sideroblastic anemia
SE Severe peripheral neuropathies (with long-term admin of large doses).
Notes
 Cyanocobalamin/B12

SimD Hydroxocobalamin

Class VITAMIN B12

MOA Cofactor required for essential enzymatic reactions that form

tetrahydrofolate, convert homocysteine to methionine, and
Metabolize l-methylmalonyl-CoA

Uses Vitamin B12 deficiency, which manifests as megaloblastic anemia and is

the basis of pernicious anemia; hydroxocobalamin is also used as a
cyanide antidote

SE Injection site pain, Arthralgia, Dizziness, Headache, Nasopharyngitis

Anaphylaxis

Notes Parenteral vitamin B12 is required for pernicious anemia and other
malabsorption syndromes
Toxicity: No toxicity associated with excess vitamin B12
E. Sickle cell anemia
Hydroxyurea
SimD
Class Cytotoxic chemotherapy
MOA Hydroxyurea is converted to a free radical nitroxide (NO) in vivo, and
transported by diffusion into cells where it quenches the tyrosyl free
radical at the active site of the M2 protein subunit of ribonucleotide
reductase, inactivating the enzyme.
Use can reduce the frequency of painful sickle cell crises, treat chronic
myelogenous leukemia and polycythemia vera
SE Nausea, vomiting, diarrhea, anorexia, leukopenia, anemia,
thrombocytopenia, headache, alopecia
Notes
 Pentoxifylline
SimD
Class Haemorrheologicals
MOA Pentoxifylline is a xanthine derivative. The exact mechanism of action
has not been fully elucidated. But it is thought to decrease blood
viscosity, increase leukocyte deformability and erythrocyte flexibility,
and decrease neutrophil adhesion/activation. It also improves
microcirculation and peripheral tissue oxygenation by increasing
blood flow.
Use Treatment for sickle cell anemia
SE Anaphylactic reaction, angina, transient hypotension, reduction in
coronary artery perfusion, arrhythmia.
Notes