PARATHYROID

AGENTS
PARATHYROID AGENTS
PARATHYROID AGENTS
1. ANTIHYPOCALCEMIC
AGENTS
• Deficient levels of PTH (Parathyroid Hormone) result
in hypocalcemia (calcium deficiency). Vitamin D
stimulates calcium absorption from the intestine and
restores the serum calcium to a normal level.
• Hypoparathyroidism is treated primarily with vitamin
D and, if necessary, dietary supplements of calcium.
However, there is one PTH available for therapeutic
use, teriparatide (Forteo), a PTH genetically
engineered from Escherichia coli bacteria using
recombinant DNA technology.
1. ANTIHYPOCALCEMIC
AGENTS
• The drug was approved in 2002 to increase bone
mass in postmenopausal women and men with
primary or hypogonadal osteoporosis who are at
high risk for fracture.
• Additional hypocalcemic agents include calcitriol
(Rocaltrol), which is the most commonly used
form of vitamin D.
Therapeutic Actions and Indications
• Vitamin D compounds regulate the absorption of
calcium and phosphate from the small intestine,
mineral resorption in bone, and reabsorption of
phosphate from the renal tubules.
• Working along with PTH and calcitonin to regulate
calcium homeostasis, vitamin D actually functions as a
hormone. With the once-daily administration,
teriparatide stimulates new bone formation, leading
to an increase in skeletal mass.
Therapeutic Actions and Indications
• It increases serum calcium and deceases serum
phosphorus.
• Indicated for the management of hypocalcemia in patients
undergoing chronic renal dialysis.
• For the treatment of hypoparathyroidism.
• TERIPARATIDE is also used for the treatment of
postmenopausal or hypogonadal osteoporosis and
osteoporosis associated with sustained systemic
glucocorticoid therapy, which could lead to fractures.
Pharmacokinetics
• Calcitriol is well absorbed from the GI tract and widely
distributed throughout the body. It is stored in the
liver, fat, muscle, skin, and bones.
• Calcitriol has a half-life of approximately 5 to 8 hours
and a duration of action of 3 to 5 days.
• After being metabolized in the liver, it is primarily
excreted in the bile, with some found in the urine.
 Pharmacokinetics
• Contraindications and Cautions for use of these drugs
during pregnancy and lactation).
• Teriparatide is given by subcutaneous injection every day.
It is rapidly absorbed from the subcutaneous tissues,
reaching peak concentration within 3 hours. The half-life
of teriparatide is about 1 hour. Serum calcium levels will
begin to decline after about 6 hours and return to baseline
16 to 24 hours after dosing.
• PTH is believed to be metabolized in the liver and excreted
through the kidneys.
Contraindications and Cautions
• These drugs should not be used in the presence of any
known allergy to any component of the drug, to avoid
hypersensitivity reactions, or hypercalcemia or
vitamin D toxicity, which would be exacerbated by
these drugs.
• At therapeutic levels, these drugs should be used
during pregnancy only if the benefit to the mother
clearly outweighs the potential for adverse effects on
the fetus.
Contraindications and Cautions
• Calcitriol has been associated with hypercalcemia
(excessive calcium levels in the blood) in the baby
when used by nursing mothers; therefore, another
method of feeding the baby should be used if these
drugs are needed during lactation.
• Caution should be used with a history of renal stones
or during lactation, when high calcium levels could
cause problems.
Contraindications and Cautions
• Teriparatide is associated with osteosarcoma—a bone
cancer—in animal studies, so its use is limited to
postmenopausal women who have osteoporosis, are
at high risk for fractures, and are intolerant to
standard therapies.
Contraindications and Cautions
• To men with primary or hypogonadal osteoporosis or
patients on sustained systemic glucocorticoid therapy
who are at high risk for fracture and are intolerant to
standard therapies.
• Patients should be informed of the risk of
osteosarcoma. These patients should also take
supplemental calcium and vitamin D, increase
weightbearing exercise, and decrease risk factors such
as smoking and alcohol consumption.
 Adverse Effects
• The adverse effects most commonly seen with these
drugs are related to GI effects: metallic taste, nausea,
vomiting, dry mouth, constipation, and anorexia.
• CNS effects such as weakness, headache, somnolence,
and irritability may also occur. These are possibly related
to the changes in electrolytes that occur with these drugs.
• Patients with liver or renal dysfunction may experience
increased levels of the drugs and/or toxic effects.
 Drug–Drug Interactions
• The risk of hypermagnesemia increases if these
drugs are taken with magnesium-containing
antacids. This combination should be avoided.
• Reduced absorption of these compounds may
occur if they are taken with cholestyramine or
mineral oil because they are fat-soluble vitamins. If
this combination is used, the drugs should be
separated by at least 2 hours.
NURSING ACTIONS
• Assessment: History and Examination
■ Assess for history of allergy to any component of the
drugs, hypercalcemia, vitamin toxicity, renal stone, and
pregnancy or lactation, which could be cautions or
contraindications to use of the drug.
■ Assess for the presence of any skin lesions; orientation
and affect; liver evaluation; serum calcium, magnesium,
and alkaline phosphate levels; and radiographs of bones as
appropriate, to determine baseline status before beginning
therapy and any potential adverse effects.
ANTIHYPERCALCEMIC
AGENT
• Drugs used to treat PTH excess or
hypercalcemia include the bisphosphonates
and calcitonin salmon.
• These drugs act on the serum levels of
calcium and do not suppress the
parathyroid gland or PTH.
 Therapeutic Actions and Indications
• Bisphosphonates
• The bisphosphonates act to slow or block bone
resorption; by doing this, they help to lower serum
calcium levels, but they do not inhibit normal bone
formation and mineralization.
• Bisphosphonates include etidronate (Didronel),
ibandronate (Boniva), pamidronate (Aredia),
risedronate (Actonel), tiludronate (Skelid), alendronate
(Fosamax), and zoledronic acid (Zometa).
 Therapeutic Actions and Indications
• Bisphosphonates
• These drugs are used in the treatment of Paget’s
disease and of postmenopausal osteoporosis in
women, and alendronate is also used to treat
osteoporosis in men.
• Zoledronic acid is also used to prevent new fractures in
patients with low trauma hip fractures and to treat
patients with multiple myeloma or documented bone
metastases from solid tumors.
 Therapeutic Actions and Indications
• Calcitonins
• The calcitonins are hormones secreted by the thyroid
gland to balance the effects of PTH.
• Currently the only calcitonin readily available is
calcitonin salmon (Fortical, Miacalcin).
• This hormone inhibits bone resorption, lowers serum
calcium levels in children and in patients with Paget’s
disease, and increases the excretion of phosphate,
calcium, and sodium from the kidney.
 Pharmacokinetics
• Bisphosphonates
• These drugs are well absorbed from the small intestine
and do not undergo metabolism. They are excreted
relatively unchanged in the urine. The onset of action is
slow, and the duration of action is days to weeks.
Patients with renal dysfunction may experience toxic
levels of the drug and should be evaluated for a dose
reduction. See Contraindications and Cautions for use of
these drugs during pregnancy and lactation.
 Pharmacokinetics
• Calcitonins
• These drugs are metabolized in the body tissues to inactive
fragments, which are excreted by the kidney.
• Calcitonins cross the placenta and have been associated with
adverse effects on the fetus in animal studies.
• Inhibit lactation in animals; it is not known whether they are
excreted in breast milk.
• Salmon calcitonin can be given by injection or by nasal spray. By
either route, peak effects are seen within 40 minutes, and the
duration of effect is 8 to 24 hours.
 Contraindications and Cautions
• Bisphosphonates
• These drugs should not be used in the presence of
hypocalcemia, which could be made worse by lowering
calcium levels, or with a history of any allergy to
bisphosphonates to avoid hypersensitivity reactions.
• Fetal abnormalities have been associated with these drugs
in animal trials, and they should not be used during
pregnancy unless the benefit to the mother clearly
outweighs the potential risk to the fetus or neonate.
 Contraindications and Cautions
• Bisphosphonates
• Extreme caution should be used when nursing because of
the potential for adverse effects on the baby. Alendronate
should not be used by nursing mothers because of
potential risk for adverse effects on the baby.
• Caution should be used in patients with renal dysfunction,
which could interfere with excretion of the drug, or with
upper GI disease, which could be aggravated by the drug.
 Contraindications and Cautions
• Bisphosphonates
• ALENDRONATE, IBANDRONATE, AND RISEDRONATE need to
be taken on arising in the morning, with a full glass of
water, fully 30 minutes before any other food or beverage,
and the patient must then remain upright for at least 30
minutes; taking the drug with a full glass of water and
remaining upright for at least 30 minutes facilitates
delivery of the drug to the stomach. These drugs should
not be given to anyone who is unable to remain upright for
30 minutes after taking the drug because serious
 Contraindications and Cautions
• Bisphosphonates
• ZOLEDRONIC ACID should be used cautiously in aspirin-
sensitive asthmatic patients. It may be given as an IV
infusion once every 2 years for osteoporosis.
• ALENDRONATE AND RISEDRONATE are now available in a
once-a-week formulation to decrease the number of times
the patient must take the drug, which should increase
compliance with the drug regimen. Ibandronate is available
in a once-a-month formulation.
 Contraindications and Cautions
• CALCITONINS
• This drug should be used in pregnancy only if the benefit to
the mother clearly outweighs the potential risk to the
fetus.
• It should not be used during lactation because the calcium-
lowering effects could cause problems for the baby.
• Calcitonin salmon should not be used with a known allergy
to salmon or fish products.
• Caution in patients with renal dysfunction or pernicious
anemia, which could be exacerbated by these drugs.
 Adverse Effects
• BISPHOSPHONATES
• The most common adverse effects are headache, nausea,
and diarrhea.
• There is also an increase in bone pain in patients with
Paget’s disease, but this effect usually passes after a few
days to a few weeks.
 Adverse Effects
• CALCITONINS
• The most common adverse effects seen with this drug is
flushing of the face and hands, skin rash, nausea and
vomiting, urinary frequency, and local inflammation at the
site of injection.
• Many of these side effects lessen with time, the time
varying with each individual patient
 Drug–Drug Interactions
• BISPHOSPHONATES
• Oral absorption of bisphosphonates is decreased if they
are taken concurrently with antacids, calcium products,
iron, or multiple vitamins.
• If these drugs need to be taken, they should be separated
by at least 30 minutes.
• GI distress may increase if bisphosphonates are
combined with aspirin; this combination should be
avoided if possible.
Drug–Drug Interactions
• CALCITONINS
• There are have been no clinically important drug–drug
interactions reported with the use of calcitonin.
 NURSING ACTIONS
• Assessment: History and Examination
■ Assess for history of allergy to any of these products or to fi
sh products with salmon calcitonin to avoid hypersensitivity
reaction; pregnancy or lactation; hypocalcemia; and renal
dysfunction, which could be cautions or contraindications to
use of the drug.
■ Assess for the presence of any skin lesions; orientation and
affect; abdominal examination; serum electrolytes; and renal
function tests, to determine baseline status before beginning
therapy and for any potential adverse effects.
END