Antianemic Drugs from Katzung's Basic and Clinical Pharmacology

Iron Preparations

1. Iron (Ferrous Sulfate, Ferrous Gluconate, Ferrous Fumarate)

o MOA: Iron is a component of hemoglobin, myoglobin, and various enzymes. It is
essential for oxygen transport and cellular respiration.
o Pharmacokinetics:
 Absorption: Primarily in the duodenum and upper jejunum.
 Distribution: Bound to transferrin in the plasma.
 Metabolism: Stored in the liver as ferritin or hemosiderin.
 Excretion: Minimal, mostly via shedding of intestinal mucosal cells.
o Adverse Reactions: GI disturbances (nausea, constipation, diarrhea), dark stools,
iron toxicity in overdose.
o Clinical Use: Treatment and prevention of iron-deficiency anemia.
o Side Effects: GI upset, metallic taste, staining of teeth (liquid preparations).
2. Parenteral Iron (Iron Dextran, Sodium Ferric Gluconate, Iron Sucrose)
o MOA: Same as oral iron preparations but used when oral administration is not
possible or effective.
o Pharmacokinetics:
 Absorption: Bypasses the gastrointestinal tract.
 Distribution: Similar to oral iron.
 Metabolism: Deposited in reticuloendothelial cells.
 Excretion: Slow release from storage sites.
o Adverse Reactions: Injection site reactions, allergic reactions, hypotension,
fever, arthralgia.
o Clinical Use: Iron-deficiency anemia in patients who cannot tolerate or absorb
oral iron.
o Side Effects: Local pain, skin staining, risk of anaphylaxis (iron dextran).

Vitamin B12 (Cobalamin) and Folate

1. Vitamin B12 (Cyanocobalamin, Hydroxocobalamin)

o MOA: Essential for DNA synthesis and nuclear maturation, particularly in
rapidly dividing cells. It acts as a cofactor for methionine synthase and
methylmalonyl-CoA mutase.
o Pharmacokinetics:
 Absorption: Requires intrinsic factor from gastric parietal cells.
 Distribution: Stored in the liver.
 Metabolism: Converted to active forms in the body.
 Excretion: Via bile and urine.
o Adverse Reactions: Generally well-tolerated; possible hypersensitivity reactions.
o Clinical Use: Treatment of vitamin B12 deficiency (e.g., pernicious anemia,
malabsorption syndromes).
o Side Effects: Rare but can include allergic reactions.
2. Folate (Folic Acid, Folinic Acid)
 o MOA: Necessary for DNA synthesis and repair, acts as a coenzyme in the
transfer of single-carbon units.
o Pharmacokinetics:
 Absorption: Rapidly absorbed in the proximal small intestine.
 Distribution: Widely distributed, stored in the liver.
 Metabolism: Converted to tetrahydrofolate, the active form.
 Excretion: Urinary excretion.
o Adverse Reactions: Generally well-tolerated.
o Clinical Use: Treatment of folate deficiency anemia, prevention of neural tube
defects in pregnancy.
o Side Effects: Rare; potential masking of vitamin B12 deficiency symptoms.

Erythropoiesis-Stimulating Agents (ESAs)

1. Erythropoietin (Epoetin Alfa, Darbepoetin Alfa)

o MOA: Stimulates erythroid progenitor cells to proliferate and differentiate into
mature red blood cells. Acts on erythropoietin receptors in the bone marrow.
o Pharmacokinetics:
 Absorption: Administered subcutaneously or intravenously.
 Distribution: Primarily acts in the bone marrow.
 Metabolism: Minimal hepatic metabolism.
 Excretion: Renal clearance.
o Adverse Reactions: Hypertension, thrombotic events, headache, seizures.
o Clinical Use: Anemia due to chronic kidney disease, chemotherapy-induced
anemia.
o Side Effects: Increased risk of cardiovascular events and tumor progression.

Prostaglandins from Katzung's Basic and Clinical Pharmacology

1. Prostaglandin E1 (PGE1) - Alprostadil

o Receptors: EP receptors (EP1-EP4)
o Location: Smooth muscle, gastrointestinal tract, vasculature
o Effects: Vasodilation, inhibition of platelet aggregation, smooth muscle
relaxation.
o Clinical Use: Erectile dysfunction, maintaining patent ductus arteriosus.
2. Prostaglandin E2 (PGE2) - Dinoprostone
o Receptors: EP receptors (EP1-EP4)
o Location: Uterus, gastrointestinal tract, vasculature
o Effects: Cervical ripening, labor induction, vasodilation, fever induction.
o Clinical Use: Induction of labor, abortion.
3. Prostaglandin F2α (PGF2α) - Carboprost
o Receptors: FP receptors
o Location: Uterus, eye
o Effects: Uterine contraction, increased aqueous humor outflow.
o Clinical Use: Postpartum hemorrhage, second-trimester abortion.
Histamines from Katzung's Basic and Clinical Pharmacology

1. Histamine H1 Receptors
o Location: Smooth muscle, endothelium, brain
o Effects: Vasodilation, bronchoconstriction, increased vascular permeability,
pruritus.
o Clinical Use: Antihistamines for allergic reactions.
2. Histamine H2 Receptors
o Location: Gastric parietal cells, heart, brain
o Effects: Increased gastric acid secretion, increased heart rate.
o Clinical Use: H2 blockers for peptic ulcer disease, GERD.
3. Histamine H3 Receptors
o Location: CNS, some peripheral nerves
o Effects: Modulation of neurotransmitter release.
o Clinical Use: Potential targets for neurological conditions (research ongoing).
4. Histamine H4 Receptors
o Location: Hematopoietic cells
o Effects: Chemotaxis of immune cells.
o Clinical Use: Potential targets for inflammatory and immune disorders (research
ongoing).

This comprehensive guide covers the essential aspects of antianemic drugs, prostaglandins, and
histamines as detailed in Katzung's Basic and Clinical Pharmacology, tailored for exam
preparation