DRUGS USED TO

TREAT ANEMIA
1.) ERYTHROPOIESIS-STIMULATING
AGENTS
✔ Patients who are no longer able to produce
enough erythropoietin in the kidneys may
benefit from treatment with exogenous
erythropoietin, which is available as the drugs
epoetin alfa (Epogen, Procrit) and darbepoetin
alfa (Aranesp).
✔ Adequate supply of iron is needed to
stimulate the bone marrow to produce healthy
RBCs.
THERAPEUTIC ACTIONS
✔ Epoetin alfa acts like the natural glycoprotein
erythropoietin to stimulate the production of RBCs
given twice to three time a week.
✔ Darbepoetin alfa is an erythropoietin-like protein
produced in Chinese hamster ovary cells with the
use of recombinant DNA technology given once a
week.
✔ Peginesatide (Omontys), the newest drug in this
class, has the advantage of dosing once a month.
✔ These drugs are used in the treatment of
anemia associated with renal failure and for
patients on dialysis; for anemia associated
with AIDS therapy; and for anemia
associated with cancer chemotherapy.
✔ It is not approved to treat other anemias
and is not a replacement for whole blood in
the emergency treatment of anemia.
 PHARMACOKINETICS
✔ These drugs can be given IV or by SQ
injection.
✔ Epoetin alfa is metabolized in the serum
through the normal process that the body uses
to clear erythropoietin.
✔ It has a slow onset and peaks in 5 to 24 hours,
and its duration of effect is usually 24 hours.
✔ It has a half-life of 4 to 13 hours and is
✔ Darbepoetin alfa has a half-life of 21 hours after
intravenous (IV) administration or 49 hours after
subcutaneous administration. It reaches peak effects
in 14 hours (if given IV) or 34 hours
(subcutaneously). Duration of effects is 24 to 72
hours, and excretion is through the urine.
✔ Peginesatide has a half-life of 25-32 hours. It has a
slow onset and reaches peak effects in 48 hours. It
is also cleared in the serum and excreted in the
urine. It is not known whether epoetin alfa or
peginesatide enters breast milk.
 CONTRAINDICATIONS
✔ Presence of uncontrolled hypertension.
✔ Patients with normal renal functioning and
adequate levels of erythropoietin because of
the rebound decrease in erythropoietin that
will occur and when administering them to a
patient with anemia and normal renal
function because this can cause more severe
anemia.
 ADVERSE EFFECTS
✔ Headache, fatigue, asthenia, and dizziness and the
potential for serious seizures, nausea, vomiting, and
diarrhea, hypertension, edema, and possible chest
pain , increased risk of DVTs.
✔ Rapid growth of cancer is seen when hemoglobin
becomes higher than 12 g/dL.
✔ Pure red cell aplasia associated with
erythropoietin-neutralizing antibodies could occur
with all of these products.
 DRUG- DRUG
INTERACTIONS
✔ These drugs should never be mixed
in solution with any other drugs
because of a risk of interactions in the
solution.
 2.) AGENTS USED FOR IRON
DEFICIENCY ANEMIA
✔ Ferrous fumarate (Feostat)
✔ Ferrous gluconate (Fergon)
✔ Ferrous sulfate (Feosol)
✔ Ferrous sulfate exsiccated (Feratab, Slow FE)
✔ Ferumoxytol (Feraheme)
✔ Iron dextran (InFeD)
✔ Iron sucrose (Venofer)
✔ Sodium ferric gluconate complex (Ferrlecit)
 THERAPEUTIC ACTION/
INDICATIONS
✔ Iron preparations elevate the serum iron
concentration.
✔ They are then either converted to hemoglobin or
trapped in reticuloendothelial cells for storage and
eventual release and conversion into a usable form of
iron for RBC production.
✔ Oral iron preparations are often used to help these
patients regain a positive iron balance and may also be
used as adjunctive therapy in patients receiving an
erythropoiesis-stimulating drug.
 CONTRAINDICATIONS
✔ Hemochromatosis (excessive iron)
✔ Hemolytic anemias which may increase serum iron
levels and cause toxicity
✔ Normal iron balance because the drug will not be
absorbed and will just pass through the body
✔ Peptic ulcer, colitis, or regional enteritis because
the drug can be directly irritating to these tissues
and can cause exacerbation of the diseases.
 ADVERSE EFFECTS
✔ GI upset, anorexia, nausea, vomiting, diarrhea, dark stools,
and constipation, direct toxicity to the CNS, causing coma and
even death.
✔ Parenteral iron is associated with severe anaphylactic
reactions, local irritation, staining of the tissues, and
phlebitis.
✔ Ferumoxytol is a supermagnetic iron oxide that can alter
MRI images and interpretation for up to 3 months after
administration; patients should be aware that they have been
given this drug and cautioned to report it before undergoing
any medical testing.
✔ Drugs to counteract metal toxicity are called
chelating agents (from the Greek word for “claw”).
✔ Chelating agents grasp and hold a toxic metal so
that it can be carried out of the body before it has
time to harm the tissues.
✔ It binds the molecules of the metal, preventing it
from damaging the cells within the body.
✔ The complex that is formed by the chelating agent
and the metal is nontoxic and is excreted by the
kidneys.
 DRUG- DRUG
✔ INTERACTIONS
Iron absorption decreases if iron preparations are
taken with antacids, tetracyclines, or cimetidine; if
these drugs must be used, they should be spaced at
least 2 hours apart.
✔ Anti-infective response to ciprofloxacin,
norfloxacin, or ofloxacin can decrease if these drugs
are taken with iron because of a decrease in
absorption; they also should be administered at least
2 hours apart.
✔ Increased iron levels occur if iron
preparations are taken with
chloramphenicol; patients receiving this
combination should be monitored closely
for any sign of iron toxicity.
✔ The effects of levodopa may decrease if it
is taken with iron preparations; patients
receiving both of these drugs should take
them at least 2 hours apart.
 DRUG- FOOD
INTERACTIONS
✔ Iron is not absorbed if taken
with antacids, eggs, milk,
coffee, or tea.
 3.) AGENTS FOR
MEGALOBLASTIC ANEMIAS
✔ Megaloblastic anemia is treated with folic acid
and vitamin B12.
✔ Folate deficiencies usually occur secondary to
increased demand (as in pregnancy or growth
spurts); absorption problems in the small intestine;
because of drugs that cause folate deficiencies; or
secondary to the malnutrition of alcoholism.
✔ Vitamin B12 deficiencies can result from poor
diet or increased demand, but the usual cause is
lack of intrinsic factor in the stomach, which is
necessary for absorption.
✔ Folic acid derivatives include folic acid (Folvite),
leucovorin (Wellcovorin), and generic, which is
available only in an IV form.
✔ Vitamin B12 includes hydroxocobalamin
(Hydro-Crysti-12), and cyanocobalamin
(Nascobal).
 THERAPEUTIC ACTIONS
✔ Folic acid and vitamin B12 are essential for cell
growth and division and for the production of a
strong stroma in RBCs.
✔ Vitamin B12 is also necessary for maintenance of
the myelin sheath in nerve tissue.
✔ For replacement therapy for dietary deficiencies
✔ Replacement in high-demand states such as
pregnancy and lactation.
✔ Folic acid is used as a rescue drug for cells
exposed to some toxic chemotherapeutic
agents.
✔ Leucovorin is used as a rescue drug
following methotrexate therapy to decrease
the toxicity caused by decreased elimination
or overdose of folic acid antagonists such as
trimethoprim and for the treatment of various
megaloblastic anemias.
 PHARMACOKINETICS
✔ Folic acid can be given in oral, IM, IV, and
subcutaneous forms. The parenteral drugs are preferred
for patients with potential absorption problems.
✔ Leucovorin is a reduced form of folic acid that is
available for oral, IM, and IV use. Levoleucovorin is only
available in an IV form.
✔ Hydroxocobalamin must be given intramuscularly
every day for 5 to 10 days to build up levels, then once
a month for life.
✔ It cannot be taken orally because the problem with
pernicious anemia is the inability to absorb vitamin
B12 secondary to low levels of intrinsic factor.
✔ Cyanocobalamin is not as tightly bound to proteins
and does not last in the body. This drug is primarily
stored in the liver and slowly released as needed for
metabolic functions.
✔ It is available as an intranasal gel that allows vitamin
B12 absorption directly through the nasal mucosa.
Nascobal is used once a week as an intranasal spray in
one nostril.
 CONTRAINDICATIONS
✔ They should be used cautiously in
patients who are pregnant or lactating or
who have other anemias
✔ Nasal cyanocobalamin should be used
with caution in the presence of nasal
erosion or ulcers, which could alter the
absorption of the drug.
 ADVERSE EFFECTS
✔ Hydroxocobalamin has been associated
with itching, rash, and signs of excessive
vitamin B levels, peripheral edema and
heart failure.
✔ Mild diarrhea, pain and discomfort can
occur at injection sites, and nasal
irritation.
 4.) AGENT FOR SICKLE CELL
ANEMIA
✔ Patients with sickle cell anemia are treated with
antibiotics to help fight the infections that can occur when
blood flow is decreased to any area.
✔ Pain-relieving activities to help alleviate the pain
associated with the anoxia to tissues, which can range from
heat applied to the area to over-the-counter pain
medications to prescription opioids; and now, for adults,
with hydroxyurea (Droxia).
✔ Hydroxyurea is a cytotoxic antineoplastic drug that is also
used to treat leukemia, ovarian cancer, and melanoma.
 THERAPEUTIC ACTIONS
✔ Hydroxyurea, taken for several months,
increases the amount of fetal hemoglobin
produced in the bone marrow and dilutes the
formation of the abnormal hemoglobin S in
adults who have sickle cell anemia.
✔ This results in less clogging of small vessels
and the painful, anoxic effects associated with
the RBC sickling or stacking.
 PHARMACOKINETICS
✔ Given orally, hydroxyurea is absorbed well
from the GI tract, reaching peak levels in 1
to 4 hours.
✔ It is metabolized in the liver and excreted
in the urine with a half-life of 3 to 4 hours.
✔ It is known to cross the placenta and to
enter breast milk.
 CONTRAINDICATIONS
✔ Severe anemia or leucopenia
because it can cause further bone
marrow suppression.
✔ Pregnancy and lactation
✔ Impaired hepatic and renal functions
 ADVERSE EFFECTS
✔ Anorexia, nausea, vomiting,
stomatitis, diarrhea, or constipation;
rash or erythema, and bone marrow
suppression, headache, dizziness,
disorientation, fever, chills, malaise and
increased risk of cancer development.
 DRUG- DRUG INTERACTION
✔ There is an increased risk of uric acid
levels if this drug is combined with any
uricosuric agents; if this combination
must be used, dose adjustments will be
needed for the uricosuric agent.