PHARMA | ENDOCRINE

REVIEWER

I. HYPOTHALAMIC AGENTS Antagonists of GnRH like degarelix and ganirelix

are used as treatment for:
- can inhibit or stimulate the release of hormones
from the anterior pituitary using hormones or • advanced prostate cancer
factors. However, not all of these hormones are • inhibition of premature LH surge in
available for pharmacological use. women undergoing controlled ovarian
stimulation for fertility.
Stimulating factors (agonists) include:
PHARMACOKINETICS
• (GHRH) growth hormone-releasing
hormone
ROUTE ONSET PEAK DURATION
• (TRH) thyrotropin-releasing hormone
IM depot 4h Variable 1,2,3, or 4 mo
• (GnRH) gonadotropin-releasing
T1/2: 3h
hormone Metabolism:
• (CRH) corticotropin-releasing hormone unknown
• (PRH). prolactin-releasing hormone Excretion:
unknown
GENERIC AND BRAND NAMES

CLASSIFICATION GENERIC BRAND

CONTRAINDICATIONS AND CAUTIONS
NAME NAME
Agonists Goserelin Zoladex Allergy to any component of the drug
histrelin Vantas -
Leuprolide Lupron - • To prevent hypersensitivity reactions.
Nafarelin Synarel - Peripheral vascular disorders
Tesamorelin Egrifta -
Antagonists Degarelix - • Can alter absorption of drugs.
ganirelix antagon -
Rhinitis

THERAPEUTIC ACTION • Alters absorption of nafarelin nasal

spray.
- Not clearly identified as there are only minute
quantities found. Renal or hepatic impairment

- Not all of them are used as pharmacological • Interfere with drug metabolism and
agents. Some are used for: excretion.

• diagnostic purposes only and Pregnancy or lactation

• primarily used as antineoplastic agents.
- Tesamorelin is used to stimulate GH and its
lipolytic effects, helping to decrease the excess
abdominal fat in HIV-infected patients with
lipodystrophy.
- Hypothalamic hormones are not all available
for pharmacological use; those that are available
are used mostly for:
• diagnostic testing
• treating some forms of cancer
• adjuncts in fertility programs
- Agonists like goserelin, histrelin, leuprolide,
and nafarelin are analogues of GnRH.
• They decrease production of sex
hormones.
• They are used as treatment for
precocious puberty, endometriosis, and
advanced prostate cancer.
• Potential adverse effects to fetus or
neonates.
NURSING CONSIDERATIONS
The specific nursing care of patient who is
receiving hypothalamic releasing factor is
related to the hormone(s) that the drug is
affecting.
INTERACTIONS
Drug interactions of hypothalamic agents are
related to the specific hormones that the drug is
affecting. They will be discussed in detail as each
agent for specific hormones will be covered in
this study guide.
ADVERSE EFFECTS
Agonists
• increased release of sex hormones
• ovarian overstimulation
• flushing
• increased temperature and appetite
• fluid retention
PHARMA | ENDOCRINE
REVIEWER

Antagonists GROWTH HORMONE AGONISTS

• decreased testosterone level Growth Hormone Agonists are responsible for:

• loss of energy
• linear skeletal growth
• decreased sperm count and activity
• growth of internal organs
• alterations in secondary sex
• protein synthesis
characteristics (decrease in female sex
• stimulation of processes required for
hormones, amenorrhea)
normal growth.
• fluid and electrolyte changes
• Disease Spotlight: GH Deficiency
• insomnia
• irritability Hypopituitarism

I.PITUITARY AGENTS - often seen as GH deficiency before any other

signs and symptoms occur. It occurs as a result of
Pituitary gland
the following:
• located in the skull in the bony sella
developmental
turcica under a layer of dura mater.
• It is divided into three lobes: • Abnormalities
- an anterior lobe • congenital defects of the pituitary
(Produces stimulating hormones in • circulatory disturbances (e.g.
response to hypothalamic stimulation.) hemorrhage)
- a posterior lobe • acute or chronic inflammation of the
(Stores ADH and oxytocin. The pituitary
intermediate lobe produces endorphins) • Pituitary tumors.
- intermediate lobe
(Produces endorphins and enkephalins Dwarfism
to modulate pain perception) - is the GH deficiency in children which results to
GENERIC AND BRAND NAMES short stature.

CLASSIFICATIO GENERIC BRAND Somatotropin deficiency syndrome (SDS)

N NAME NAME - a condition in adults with hypopituitarism
Anterior pituitary drugs caused by pituitary tumors or trauma, or may
Growth somatropin Nutropin, have been treated for GH deficiency as children,
hormone saizen,
resulting in a shutdown of the pituitary
agonist humatrop
production of somatotropin.
e
- Growth bromocriptin pariodel THERAPEUTIC ACTION
Hormone e
Antagonists replacing human GH and stimulate skeletal
lantreolide Somatuline - growth, growth of internal organs, and protein
depot synthesis.
octreotide Sandostatin -
pegvisomant Somavert - INDICATIONS
Other drugs Chorionic chorex • long-term treatment of children with
affecting gonadotropin growth failure associated with various
anterior
deficiencies, girls with Turner’s
pituitary
syndrome, AIDS wasting and cachexia,
hormones
GH deficiency in adults, and treatment of
corticotropin Acthar -
cosyntropin Cotrosyn - growth failure in children of small
menotropin Pergonal - gestational age who do not achieve
Thyrotropin thyrogen - catch-up growth by 2 years of age.
alfa • Somatropin (Nutropin, Saizen,
Posterior Pituitary Hormone Drugs Genotropin, Serostim) and somatropin
Drugs affecting conivaptan Vaprisol rDNA origin (Zorbtive) are used for GH
posterior replacement today.
pituitary
hormones
desmopressin DDAVP -
tolvaptan - -
PHARMA | ENDOCRINE
REVIEWER
PHARMACOKINETICS
ROUTE ONSET PEAK DURATION
IM, subcu Varies 5 – 7.5 -
h impossible, hypersecretion of GH causes
T1/2: 15-20min
Metabolism:
liver
Excretion:
urine, feces
CONTRAINDICATIONS AND CAUTIONS
Allergy to any component of the drug
• To prevent hypersensitivity reactions.
Closed epiphyses and cranial lesions
• Risk of serious complications with
somatropin.
Abdominal surgery and acute illness secondary
to complications of open-heart surgery.
• Potential problems with healing.
Pregnancy or lactation
• Potential adverse effects on the fetus.
ADVERSE EFFECTS
• development of antibodies to GH
• inflammation and autoimmune-type
reactions (swelling, joint pain)
• endocrine reactions (hypothyroidism,
insulin resistance).
INTERACTIONS
- change in metabolism with drugs using P450
liver enzyme system
NURSING CONSIDERATIONS
Assess for contraindications or cautions
(e.g. history of allergy, pregnancy, serious
infection after open heart surgery, etc.) to avoid
adverse effects.
Assess height, weight, thyroid function tests,
glucose tolerance tests, and GH levels to
determine baseline status before beginning
therapy and for any potential adverse effects.
GROWTH HORMONE ANTAGONISTS
DISEASE SPOTLIGHT: HYPERTUITARISM
GH hypersecretion is usually caused by pituitary
tumors and can occur at any time of life.
Gigantism occurs before the epiphyseal plates
of the long bones fuse and cause accelerationin
linear skeletal growth. Individuals with
gigantism can reach 7 to 8 feet in height with
fairly normal body proportions.
Acromegaly is a form of hyperpituitarism after
epiphyseal closure (adults). As linear growth is
enlargement in the peripheral parts of the body
such as hands and feet as well as internal
organs (heart).
THERAPEUTIC ACTION
• acting directly on postsynaptic
dopamine receptors in the brain to
inhibit GH secretion
• Octreotide and lanreotide are
somatostatin analogues which are more
potent in inhibiting GH release with less
of an inhibitory effect on insulin release.
They are used instead of somatostatin.
INDICATIONS
• Treatment of Parkinson’s disease,
• hyperprolactinemia associated with
pituitary adenomas
• female infertility associated with
hyperprolactinemia
• Acromegaly
• short-term treatment of amenorrhea
or galactorrhea.
• Bromocriptine is a semisynthetic ergot
alkaloid and a dopamine agonist which
is frequently used to treat acromegaly.
- It may also be used as adjunct to
irradiation.
CONTRAINDICATIONS AND CAUTIONS
Allergy to any component of the drug.
• To prevent hypersensitivity reactions.
Pregnancy or lactation
• Potential adverse effects on the fetus.
Diabetes, thyroid dysfunction
• May be exacerbated by blocking GH.
ADVERSE EFFECTS
CNS:
• headache
CV:
• sinus bradycardia
• arrhythmias
GI:
• nausea
• vomiting
• abdominal cramps
• constipation
PHARMA | ENDOCRINE
REVIEWER

• diarrhea
• acute cholecystitis
Digoxin, ACEI, ARBs, potassium-sparing
• cholestatic jaundice
Diuretics
• biliary tract obstruction
• pancreatitis • Risk of hyperkalemia with tolvaptan and
conivaptan
Others:
Telithromycin
• decreased glucose tolerance
• inflammation at injection sites • Severe tolvaptan toxicity.

PHARMACOKINETICS NURSING CONSIDERATIONS

ROUTE ONSET PEAK DURATION Assess for contraindications or cautions
PO Varies 1 – 3 h 14 h
T1/2: 3h, 45-50 • (e.g. history of allergy, pregnancy, renal
h dysfunction, etc.) to avoid adverse
Metabolism: effects.
liver
Assess skin for lesions; orientation, affect, and
Excretion: bile
reflexes; blood pressure and pulse; respiration
and adventitious sounds; abdominal
INTERACTIONS examination; renal function tests; and serum
electrolytes, to determine baseline status before
Erythromycin - Increased toxicity with
beginning therapy and for any potential adverse
bromocriptine
effects.
Phenothiazine - Decreased effectiveness of
II. ADRENOCORTICAL AGENTS
bromocriptine
Adrenocortical agents are
Opioids - Higher doses of pegvisoman will be
required • drugs used as short-term treatment to
suppress immune system in patients
NURSING CONSIDERATIONS
with inflammatory disorders.
Assess for contraindications or cautions • They are also used for replacement
therapy to maintain hormone levels
(e.g. history of allergy to the drug, other
when adrenal glands are not functioning
endocrine disturbances, pregnancy and
adequately.
lactation, etc.) to avoid adverse effects.
• These agents are classified into three:
Assess orientation, affect, and reflexes; blood - glucocorticoids
pressure, pulse, and orthostatic blood pressure; - Mineralocorticoids
abdominal examination; glucose tolerance tests; - androgens.
and GH levels to determine baseline status
GENERIC AND BRAND NAMES
before beginning therapy and for any potential
adverse effects. Glucocorticoids & Mineralocorticoids:
DRUGS AFFECTING POSTERIOR PITUITARY CLASSIFICATION GENERIC NAMEBRAND
HORMONES NAME
Glucocorticoids Beclomethasone Beclovent
ADVERSE EFFECTS
Betamethasone Celestone -
• Water intoxication, Drowsiness, light- Budesonide Rhinocort, -
headedness, headache, coma, Entocort EC
convulsions Dexamethasone Decadron -
Hydrocortisone Cortef -
• GI: abdominal cramps, flatulence,
Methylprednisolone Medrol -
nausea, vomiting, constipation, dry
Prednisolone Delta-Cortef -
mouth
Mineralocorticoids Fludrocortisone Florinef
• Local reaction at injection site
Hydrocortisone Cortef -
INTERACTIONS

Carbamazepine, chlorpropamide

• Increased antidiuretic effects if with

desmopressin
PHARMA | ENDOCRINE
REVIEWER

DISEASE SPOTLIGHT: ADRENAL INSUFFICIENCY Acute infection

AND CRISIS
• Can be exacerbated by the blocking
Adrenal insufficiency effects of the drug on inflammation and
immune system.
is a condition when patients experience a
shortage of adrenocortical hormones and Diabetes
develop signs and symptoms
• Glucose-elevating effect of the drug can
• confusion, disrupt glucose control
• hyperpigmentation
Other endocrine disorders
• hypoglycemia
• poor response to stress • Potential of imbalance.
This can occur when a patient does not produce Pregnancy
enough ACTH, when the glands are not able to
respond to ACTH, when an adrenal gland is • Potential adverse effects on the fetus
damaged and cannot produce enough hormones INDICATIONS
(Addison’s disease) or secondary to surgical
removal of glands. A prolonged use of • short-term treatment of inflammatory
corticosteroid hormones is a more common disorders by blocking the actions of
cause of adrenal insufficiency. arachidonic acid leading to decrease in
formation of prostaglandins and
Adrenal crisis leukotrienes.
occurs when patients who have an adrenal • Local agents are used to treat local
insufficiency experience a period of extreme inflammation. Systemic use is indicated
stress like vehicle accidents, massive infections, for treatment of some cancers,
or a surgical procedure. The body is not able to hypercalcemia associated with cancer,
supplement the energy-consuming effects of the hematological disorders, and some
sympathetic reaction. This is characterized by neurological infections.
physiological exhaustion, hypotension, fluid • When combined with
shift, shock, and even death. mineralocorticoids, some of these drugs
can be used in replacement therapy for
Patients in adrenal crisis adrenal insufficiency
are treated with massive infusion of replacement PHARMACOKINETICS
steroids, constant monitoring, and life support
procedures.
ROUTE ONSET PEAK DURATION
GLUCOCORTICOIDS PO Varies 1 – 2 h 1 – 1.5 d
T1/2: 3.5 h
THERAPEUTIC ACTION Metabolism:
liver
• bind to cytoplasmic receptors of target
Excretion: urine
cells to form complex reactions needed
to reduce inflammation and to suppress
immune system. ADVERSE EFFECTS
• Other glucocorticoids like
• increased methylprednisolone toxicity
hydrocortisone, cortisone, and
among African Americans
prednisone also have mineralocorticoid
• growth retardation
activity so they can affect potassium,
sodium, and water levels. They can also • local inflammation and infections
limit the activity of lymphocytes to act • burning and stinging sensation at
within the immune system. injection site.

CONTRAINDICATIONS AND CAUTIONS INTERACTIONS

Allergy to any component of the drug • Erythromycin, ketoconazole,

troleandomycin. Increased toxic effects.
• To prevent hypersensitivity reactions. • Salicylates, barbiturates, phenytoin, or
rifampin. Decreased serum level and
effectiveness if with.
PHARMA | ENDOCRINE
REVIEWER

NURSING CONSIDERATIONS ADVERSE EFFECTS

• Assess for contraindications or cautions CNS:

(e.g. history of allergy, pregnancy, acute
• Headache
infections, etc.) to avoid adverse
• weakness
effects.
• Assess weight; temperature; orientation CV:
and affect; grip strength; eye
examination; blood pressure, pulse, • edema
peripheral perfusion, and vessel • hypertension
evaluation; respiration and adventitious • heart failure
breath sounds; glucose tolerance, renal Others:
function, serum electrolytes to
determine baseline status before • possible hypokalemia
beginning therapy and for any potential • allergic reactions from skin rash to
adverse effects. anaphylaxis.

MINERALOCORTICOIDS INTERACTIONS

THERAPEUTIC ACTION Salicylates, barbiturates, hydantoins, rifampin,

• aldosterone increases sodium
reabsorption in the renal tubules and
increases potassium and hydrogen
excretion, leading to water and sodium
retention.
CONTRAINDICATIONS AND CAUTIONS
Allergy to any component of the drug
• To prevent hypersensitivity reactions.
Severe hypertension, heart failure, or cardiac
Disease
• Resultant increased blood pressure
Lactation
and anticholinesterase. Decreased effectiveness
of these drugs.
NURSING CONSIDERATIONS
• Assess for contraindications or cautions
(e.g. history of allergy to drug, history of
heart failure, hypertension, etc.) to
avoid adverse effects.
• Assess blood pressure, pulse, and
adventitious breath sounds; weight and
temperature; tissue turgor; reflexes and
bilateral grip strength; and serum
electrolyte levels, to determine baseline
status before beginning therapy and for
any potential adverse effects.

• Potential adverse effects to the baby.

Infection

• Can alter adrenal response

High sodium intake

• Severe hypernatremia can occur.

INDICATIONS

partial replacement therapy in cortical

insufficiency conditions, treatment of salt-losing
adrenogenital syndrome; off-label use:
treatment of hypotension.

PHARMACOKINETICS

ROUTE ONSET PEAK DURATION

PO Gradual 1 – 7 h 18 – 36 h
T1/2: 3.5 h
Metabolism:
liver
Excretion:
urine
PHARMA | ENDOCRINE
REVIEWER
ANTIDIABETIC AGENTS
ANTIDIABETIC DRUGS - are a group of drug
structurally unrelated to sulfonylureas and are
effective when used in combination with insulin
or sulfonylureas.
Lists of Antidiabetic drugs:
• alpha-glucosidase inhibitors
• biguanides
• dipeptidyl
• peptidase-4 (DPP-4) inhibitors
• human amylin
• incretin mimetics,
• meglitinides
• thiazolidinediones
ALPHA-GLUCOSIDASE INHIBITORS
acarbose and miglitol inhibit alpha-glucosidase,
an enzyme that breaks down glucose for
absorption. Therefore, they delay the absorption
of glucose.
BIGUANIDE METFORMIN decrease the
production and increases the uptake of glucose.
MEGLITINIDES NATEGLINIDE AND
REPAGLINIDE are newer agents that act like
sulfonylureas to increase insulin release.
SYNTHETIC HUMAN AMYLIN
PRAMLINTIDE works to modulate gastric
emptying after a meal to cause a feeling of
fullness or satiety.
INCRETIN MIMETICS EXENATIDE AND
LIRAGLUTIDE mimic the effects of GLP-1:
enhancement of glucose-dependent insulin
secretion by the beta cells in the pancreas,
depression of elevated glucagon secretion, and
slowed gastric emptying to help moderate and
lower blood glucose levels.
DPP-4 INHIBITORS LINA-, SAXA-, AND
SITAGLIPTIN slow the breakdown of GLP-1 to
prolong the effects of increased insulin secretion,
decreased glucagon secretion, and slowed GI
emptying.
THIAZOLIDINEDIONES PIOGLITAZONE
AND ROSIGLITAZONE decrease insulin
resistance.
INSULIN is a drug that is used to control glucose
in patients with diabetes mellitus. It is the only
parenteral antidiabetic agent available for
exogenous replacement of low levels of insulin.
DIABETES MELLITUS (literally, “honey
urine”) is a condition wherein there is a complex
disturbance in the metabolism of carbohydrates,
proteins, and fats.
Diabetes is classified into two: type 1 and
type 2.
TYPE 1 - is common in younger people and
is connected with cases of viral destruction of
beta cells of the pancreas.
TYPE 2 - is adult-onset and is associated
with not enough insulin to maintain glucose
control
HYPERGLYCEMIA (high blood sugar)
results when there is an increase in glucose in
the blood
.
THYROID AND ANTI-THYROID
AGENTS
THYROID GLAND is located in the middle
of the neck and surrounds the trachea like a
shield.
It produces two hormones: thyroid hormone
and calcitonin.
HYPOTHYROIDISM is a lack of
sufficient levels of thyroid hormones to
maintain a normal metabolism. This is the
most common type of thyroid dysfunction
and is common among older women and
men. It occurs when excessive amounts of
thyroid hormones are produced and released
into circulation.
CRETINISM is a condition in children who
are born without a thyroid gland or who have
a non-functioning gland.
THIOAMIDES lower thyroid hormones by
preventing the formation of thyroid hormone
in the thyroid cells.
THIOAMIDES: increased bleeding with
oral anticoagulants and PTU
IODINE SOLUTIONS: changes in the
metabolism and level of anticoagulants,
theophylline, digoxin, metoprolol, and
propranolol.
PHARMA | ENDOCRINE
REVIEWER

PARATHYROID AGENTS
PARATHYROID AGENTS are drugs used
to treat disorders that affect serum calcium
levels. The parathyroid glands are four very
small groups of glandular tissue located on
the back of the thyroid gland.
This can be either
ANTIHYPOCALCEMIC AGENT OR
ANTIHYPERCALCEMIC AGENT
(further classified into bisphosphonates and
calcitonins).
PARATHYROID DYSFUNCTION
involves either absence of PTH
(hypoparathyroidism) or overproduction of
PTH (hyperparathyroidism). This can affect
any age group.
HYPOPARATHYROIDISM is a rare
condition characterized by absence of PTH
resulting to low calcium level
(hypocalcemia).
HYPERPARATHYROIDISM is a
condition characterized by excessive
production of PTH leading to elevated
calcium level (hypercalcemia).

Primary hyperparathyroidism occurs more

often in women between 60-70 years of age.
Secondary hyperparathyroidism occurs
most frequently in patients with chronic renal
failure.

PAGET’S DISEASE is a genetically linked

disorder characterized by overactive
osteoclasts that are eventually replaced by
enlarged and softened bony structures.
Manifestations include deep bone pain,
headaches, and hearing loss.
POSTMENOPAUSAL OSTEOPOROSIS
occur when dropping levels of estrogen allow
calcium to be pulled out of the bone, resulting
in a weakened and honeycombed bone
structure.
BISPHOSPHONATE is used to treat and
prevent osteoporosis in postmenopausal
women and in men. It is also used to treat
glucocorticoid-induced osteoporosis as well
as to treat Paget’s disease.

CALCITONIN is used for treatment of

Paget’s disease, postmenopausal
osteoporosis, and emergency treatment of
hypercalcemia.