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Introduction
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women (with menstrual blood loss or pregnancy), in adolescents (increased demand) and in
vegetarians or persons with malnutrition (inadequate dietary iron intake).
Iron preparations: Treatment or prevention of iron deficiency anemia is the only clinical
indication for the use of iron preparations.
The preferred route of iron administration is oral. Elemental iron quantity per dose should be
taken into consideration. Oral preparations contain ferrous (Fe2+) salts (sulfate, glutamate,
aspartate, fumarate, gluconate, succinate, etc.). Ferric (Fe3+) salts are also available (Ferric
hydroxide polymaltose complex, Iron polysaccharide, etc.), but ferrous (Fe2+) salts are
supposed to be better absorbed. A number of iron combinations (with vitamins, minerals,
amino acids, etc.) are marketed, but should be considered irrational due to lower iron
content.
About 50100 mg of iron can be incorporated into hemoglobin daily, and about 25% of oral
iron can be absorbed. Full haemopoetic response in adults is usually achieved with
administration of 200 mg elemental iron daily p.o. in 2 or 3 divided doses after or in
between meals. Absorption of iron is much better when taken in empty stomach, but side
effects may limit patient compliance. For prophylactic use, a daily dose of 30 mg elemental
iron is sufficient.
Parenteral iron preparations are indicated only in case of: severe deficiency with chronic
bleeding; intolerance to oral iron; malabsorption or inflammatory bowel disease;
erythropoietin therapy (to meet the increased needs of induced erythropoiesis). Parenteral
forms contain organically complexed salts of unionized iron: Iron dextran, Iron sucrose
complex, etc. (See Classification). A sensitivity test with a small test dose must be
performed before parenteral administration of iron to avoid any risk of hypersensitivity
reactions.
In severe anemia, treatment with oral iron should be continued for at least 3 months after
correction to replenish iron stores.
Desferrioxamine (Deferoxamine), an iron chelator, is a specific antidote that is given
systematically to remove iron.
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intrinsic factor (a protein produced by parietal cells of the gastric mucosa). Parenteral injections of
vitamin B12, but not oral preparations, are effective for treatment of pernicious anemia.
Vitamin B12
Cyanocobalamin (vitamin B12 amp. 250 mcg/1 ml i.m.). Cyanocobalamin and
hydroxocobalamin are complex cobalt-containing compound present in diet and referred to
as vitamin B12. Vitamin B12 is essential for cell growth and multiplication. Along with folic
acid, it is involved in the DNA synthesis as a cofactor in the transfer of 1-carbon units.
Two biochemical reactions require vitamin B12: conversion of methylmalonyl-coenzyme A
(CoA) to succinyl-CoA and conversion of homocysteine to methionine. Methylcobalamin
and deoxyadenosylcobalamin are the active forms of the vitamin.
Hydroxocobalamin is highly protein-bound and longer acting, but is associated with the
development of antibodies (hence lesser in use).
Folic acid
Humans do not synthesize folic acid and meet theirs requirements from green leafy
vegetables, fruit, mushrooms, liver, meat, kidney, eggs, milk and yeast. In the intestinal
mucosa of jejunum folic acid is reduced by dihydrofolate reductase to tetrahydrofolic acid.
Tetrahydrofolic acid through 1-C carbon transfer reactions is involved in the synthesis of
purines and pyrimidines which are essential for DNA synthesis.
Deficiency of folic acid leads to megaloblastic anaemia and teratogenic effects (spina bifida,
etc.). Vitamin B9 prophylactically can be used during pregnancy and lactation 0.4 mg p.o.
daily)
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neutropenia and neutropenia associated with aplastic anaemia. Pegfilgrastim is a PEGilated
(covalently conjugated to PolyEthylene Glycol polymer chain) form of filgrastim with a
much longer t1/2 than the recombinant G-CSF.
Megakaryocythe Growth Factors. Oprelvekin (IL-11) and Thrombopoietin stimulate the
growth of megakaryocytic progenitors and increase the number of peripheral platelets. They
are used to treat thrombocytopenia following cancer chemotherapy.
OUESTIONS 1
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Answers: 1B; 2D; 3C; 4B, C; 5D; 6D; 7C; 8A, B; 9A; 10A, C, D; 11C.
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1. All of the following drugs are used for iron deficiency anemia, except: A) Ferrous sulphate;
B) Folic acid; C) Ferrous glutamate; D) Ferrous fumarate.
2. The recommended dose of elemental iron for oral supplementation is: A) 50 mg daily; B)
100 mg daily; C) 150 mg daily; D) 200 mg daily.
3. An adverse effect of oral iron therapy is: A) Anemia; B) Thrombocytopenia; C)
Constipation; D) Headache.
4. Iron preparations for parenteral use are: A) Ferrous aspartate; B) Iron dextran; C) Iron
isomaltoside; D) Ferric hydroxide polymaltose complex.
5. Iron sucrose complex can be administered: A) Orally; B) Subcutaneously; C)
Intramuscularly; D) Intravenously.
6. Which of the following is used for treatment of pernicious anemia? A) Erythropoetin B)
Oral Vitamin B12; C) Iron; D) Parenteral Vitamin B12.
7. Which of the following statements about Folic acid is correct? A) It is used for treatment of
trombocytopenia; B) It is contraindicated in pregnancy; C) It is used for treatment of
megaloblastic anemias; D) Its clinical use is limited by serious side effects.
8. Select the correct statements about Desferrioxamine: A) It is specific antidote in acute iron
overdose; B) It is an iron chelator; C) It is a drug of choice for treatment of iron deficiency;
D) Both B and C are correct.
9. Erythropetin is used for: A) Treatment of anemia associated with chronic renal failure; B)
Treatment of neutropenia associated with radiotherapy; C) Treatment of thrombocytopenia
associated with cancer chemotherapy; D) Prevention of congenital neural tube defects.
10. Which of the following drugs influence leucopoiesis? A) Filgrastim; B) Erythropoetin; C)
Doxorubicin; D) Sargramostim.
11. This drug is used for treatment of thrombocytopenia following cancer chemotherapy: A)
Vitamin B12; B) Filgrastim; C) Oprelvekin; D) Molgramostim.
Conclusions:
Recommended References: Katzung B et al (2009) Basic & Clinical Pharmacology. Katzung B and A Trevor
(2010) Pharmacology Examination and Board Review. Tripathi KD (2008) Essentials of Medical Pharmacology.
Sharma HL et al (2007) Principles of Pharmacology. Rang H et al (2011) Pharmacology. Clark S (2009) Current
Opinion in Gastroenterology 25: 122128. Novak J et al (2008) Curr Opin Nephrol Hypertens 17 (6):580-8. Castro R et
al (2010) California Journal of Health-System Pharmacy March/April: 5-14. Testa U (2010) Expert Opin. Emerging
Drugs 15(1):119-138. Pasricha S-R et al (2010) MJA 193: 525532. Zhu A et al (2010) Dig Dis Sci (2010) 55:548559.
McKoy J et al (2008) Transfusion 48(8):1754-1762. Locatelli F et al (2012) Expert Opin. Pharmacother. 13(4):495-503.
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Gejsler B (2010) Expert Opin. Biol. Ther. 10(8): 1209-1216. Foote MA et al (2002) Cytokines, Cellular & Molecular
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