Thyroid and Antithyroid Drugs

The thyroid gland produces three hormones:

thyroxine, triiodothyronine, and calcitonin
Thyroxine (also called T4) contains four atoms of
iodine and triiodothyronine (also called T3)
contains three atoms of iodine
T3 is more potent than T4 and has a more rapid
onset but a shorter duration of action
Production of T3 and T4 depends on the presence
of iodine and tyrosine in the thyroid gland
Thyroid hormones are released into the circulation
when the thyroid gland is stimulated by thyroid-
stimulating hormone (thyrotropin or TSH) from the
anterior pituitary gland
Thyroid hormones control the rate of cellular
metabolism and thereby influence the functioning
of virtually every cell in the body
The heart, skeletal muscle, liver, and kidneys are
especially responsive to the stimulating effects of
thyroid hormones
The brain, spleen, and gonads are less responsive
Thyroid hormones are required for normal growth
and development and are considered especially
critical for brain and skeletal development and
maturation
Thyroid hormones also influence linear growth,
brain function, including intelligence and memory,
neural development, dentition, and bone
development
Some physiologic effects of thyroid hormones:
- increased rate of cellular metabolism and oxygen
consumption with a resistant increase in heat
production
- increased heart rate, force of contraction, and
cardiac output (increased cardiac workload)
- increased CHO metabolism
- increased fat metabolism, including increased
lipolytic effects of other hormones and metabolism
of cholesterol to bile acids
- inhibition of pituitary secretion of TSH
Hypothyroidism

Primary hypothyroidism occurs when disease or

destruction of thyroid gland tissues causes
inadequate production of thyroid hormones
Congenital hypothyroidism (cretinism) occurs
when a child is born with a poorly functioning or
absent thyroid gland
Adult hypothyroidism (myxedema) may be
subclinical or clinical and occurs much more often
in women than in men
If the thyroid gland cannot secrete enough
hormone despite excessive release of TSH,
hypothyroidism occurs, and a goiter (visible
enlargement of the thyroid gland) may occur from
the overstimulation
Hyperthyroidism

Hyperthyroidism is characterized by excessive

secretion of thyroid hormone and usually involves
an enlarged thyroid gland that has an increased
number of cells and increased rate of secretion
Thyroid storm or thyrotoxic crisis is a rare but severe
complication characterized by extreme symptoms
of hyperthyroidism, such as severe tachycardia,
fever, dehydration, heart failure and coma
General Characteristics of Thyroid and
Antithyroid Drugs

Mechanism of Action
✓Thyroid drugs such as the synthetic drug
levothyroxine provide an exogenous source of
thyroid hormone
✓Antithyroid drugs act by decreasing production or
release of thyroid hormone
The thioamide drugs inhibit synthesis of thyroid
hormones
Iodine preparations inhibit the release of thyroid
hormones and cause then to be stored within the
thyroid gland. Radioactive iodine emits rays that
destroy the thyroid gland tissue
Indications for Use
❖Thyroid drugs are indicated for primary or
secondary hypothyroidism, cretinism, and
myxedema
❖Antithyroid drugs may be necessary for
hyperthyroidism associated with Graves’ disease,
nodular goiter, thyroiditis, overtreatment with
thyroid drugs, functioning thyroid carcinoma, and
pituitary adenoma that secretes excessive
amounts of TSH
❖Antithyroid drugs may also be indicated for thyroid
storm
Contraindications to Use
❑Iodine preparations and thioamide antithyroid
drugs are contraindicated in pregnancy, because
they can lead to goiter and hypothyroidism in the
fetus or newborn
❑Radioactive iodine is contraindicated during
lactation as well
❑Because radioactive iodine may cause cancer
and chromosome damage in children, it should be
used only for hyperthyroidism that cannot be
controlled by other drugs or surgery
Individual Drugs:
Thyroid Drugs (Used in Hypothyroidism)

Levothyroxine (Synthroid, Levothroid), a synthetic

preparation of T4, is the drug of choice for long-
term treatment of hypothyroidism and serves as
the prototype
Takin medication on an empty stomach increases
absorption; malabsorption syndromes cause
excessive fecal loss
Antithyroid Drugs (Used in
Hyperthyroidism)

Propylthiouracil (PTU) is the prototype of the

thioamide antithyroid drugs
Can be used alone to treat hyperthyroidism, as
pat of the preoperative preparation for
thyroidectomy, before or alter radioactive iodine
therapy, and in the treatment of thyroid storm
PTU acts by inhibiting production of thyroid
hormones and peripheral conversion of T4 to the
more active T3
Methimazole (Tapazole) is similar to PTU in actions,
uses, and adverse reactions
It is also well absorbed with oral administration and
rapidly reaches peak plasma levels
Strong iodine solution (Lugol’s solution) and
saturated solution of potassium iodide (SSKI) are
iodine preparations sometimes used in short-term
treatment of hyperthyroidism
These drugs inhibit release of thyroid hormones,
causing them to accumulate in the thyroid gland
Lugol’s solution is usually used to treat thyrotoxic
crisis and to decrease the size and vascularity of
the thyroid gland before thyroidectomy
Sodium iodide 131 is a radioactive isotope of
iodide
Therapeutic doses act by emitting beta and
gamma rays, which destroy thyroid tissue and
thereby decrease production of thyroid hormones
It is also used to treat thyroid cancer
Propanolol (Inderal) is an antiadrenergic, not an
antithyroid drug
It does not affect thyroid function, hormone
secretion, or hormone metabolism
Used to treat cardiovascular conditions, such as
dysrhythmias, angina pectoris and hypertension
Nursing Process: Assessment

Assess for signs and symptoms of thyroid disorders

Check laboratory reports for serum TSH when
available. An elevated serum TSH is the first
indication of primary hypothyroidism and
commonly occurs in middle-aged women, even in
the absence of other signs and symptoms
Nursing Process: Nursing Diagnoses

Decreased cardiac output related to disease- or

drug-induced thyroid disorders
Imbalanced nutrition: less than body requirements
with hyperthyroidism
Ineffective thermoregulation related to changes in
metabolism rate and body heat production
Deficient knowledge: disease process and drug
therapy
Nursing Process: Planning

Achieve normal blood levels of thyroid hormone

Receive or take drugs accurately
Experience relief of symptoms of hypothyroidism or
hyperthyroidsim
Nursing Process: Interventions

Environmental temperature
- regulate for the patient’s comfort, when possible.
Patients with hypothyroidism are very intolerant of
cold, due to their slow metabolism
- patients with hyperthyroidism are very intolerant of
heat and perspire excessively, due to their rapid
metabolism rate
Diet
- hypothyroid patients are often overweight
because of slow metabolism rate. Low-calorie,
weight –reduction diet may be indicated; increased
intake of high-fiber is usually needed to prevent
constipation as a result of decreased GIT secretions
and motility
- hyperthyroid patients are often underweight
because of a rapid metabolism rate; need extra
calories and nutrients to prevent tissue breakdown;
avoid seasoned and high-fiber foods because they
may increase diarrhea
Fluids
- hypothyroidism, patient needs adequate intake of
low-calorie fluids to prevent constipation
- hyperthyroidism, patient needs large amount of
fluids unless contraindicated by cardiac or renal
disease
Activity
- hypothyroidism, encourage activity to maintain
cardiovascular, respiratory, gastrointestinal, and
musculoskeletal function
- hyperthyroidism, encourage rest and quiet,
nonstrenuous activity
Skin care
- hypothyroid patients are likely to have edema and
dry skin. When edema is present, inspect pressure
points, turn often, and avoid trauma when possible
Eye care
- hyperthyroid patients may have exophthalmos. In mild
cases, use measures to protect the eye like dark glasses,
local lubricants and patching of the eyes at night may
be needed
Diuretic drugs and elevating the head of the bed may
help reduce periorbital edema and eyeball protrusion
Principles of Therapy: Goal

The goal of treatment with thyroid drugs is to

restore the individual to a euthyroid state with
normal metabolism
Thyroid Drugs: Drug Selection

Synthetic levothyroxine is the drug of choice for

thyroid hormone replacement because of uniform
potency, once-daily dosing, and low cost
In patients with symptomatic hypothyroidisim,
levothyroxine therapy is definitely indicated. In
addition to improvement of metabolism,
treatment may also improve cardiac function,
energy level, mood muscle function, and fertility
In myxedema coma, levothyroxine is given IV,
along with intervention to relieve precipitating
factors and to support vital functions until the
thyroid hormone becomes effective, often within
24 hours
Thyroid Drugs: Drug Dosage

Dosage is gradually increased at approximately 2-

week intervals until symptoms are relieved and a
normal serum TSH level is re-established
Maintenance dosage for long-term therapy is
based on the patient’s clinical status and periodic
measurement of serum TSH
Thyroid Drug: Duration of Therapy

Thyroid replacement therapy in the patient with

hypothyroidism is lifelong
Hypothyroidism and the Metabolism of
Other Drugs

Most drugs given to patients with hypothyroidism

have a prolonged effect, because drug
metabolism in the liver is delayed and the
glomerular filtration rate of the kidneys is
decreased
Drug absorption from the intestine or a parenteral
injection site also may be slowed
With hypothyroidism are especially likely to
experience respiratory depression and myxedema
coma with opioid analgesics and other sedating
drugs
Adrenal Insufficiency

Hypothyroidism and adrenal insufficiency coexist,

the adrenal insufficiency should be treated with a
corticosteroid drug before starting thyroid
replacement
Thyroid hormones increase tissue metabolism and
tissue demands for adrenocortical hormones
Antithyroid Drugs

If the cause is an adenoma or multinodular goiter

surgery or radioactive therapy is recommended,
especially in older patients
If the cause is Grave’s disease, antithyroid drugs,
radioactive iodine surgery, or a combination of
these methods may be warranted
Antithyroid Drugs: Drug Selection

The antithyroid drugs include the thioamide

derivatives (propylthiouracil and methimazole)
and iodine preparations (Lugol’s solution and SSKI)
The thioamide drugs are used as the primary
treatment (for which they may be given 6 months
to 2 years) or to decrease blood levels of thyroid
hormone before radioactive iodine therapy or
surgery
Radioactive iodine is a frequently used treatment
One disadvantage is hypothyroidism, which
usually develops within a few months and requires
lifelong thyroid hormone replacement therapy
Another disadvantage is the delay in therapeutic
benefits
Results may not be apparent for 3 months or
longer during which time severe hyperthyroidism
must be brought under control with one of the
thioamide antithyroid drugs
A thioamide drug is given to produce a euthyroid
state, and an iodine preparation is given to
reduce the size and vascularity of the thyroid
gland to reduce the risk of excessive bleeding
Maximal effects are reached in approximately 10
to 15 days of continuous therapy, and this is
probably the primary advantage
Although giving a thioamide drug followed by an
iodine preparation is standard preparation for
thyroidectomy, the opposite sequence of
administration is unsafe.
If the iodine preparation is given first and followed
by PTU or methimazole, the patient is likely to
experience acute hyperthyroidism because the
thioamide causes release of the stored thyroid
hormones
Drug Dosage

Dosage of the thioamide antithyroid drug is

relatively large until a euthyroid state is reached,
usually in 6 to 8 weeks
Radioactive iodide is usually given in a single dose
to middle-aged and elderly people on an
outpatient basis
Duration of Therapy

No clear cut guidelines exist regarding duration of

antithyroid drug therapy because exacerbations
and remission occur
It is usually continued until the patient is euthyroid
for 6 to 12 months
The therapeutic effects of radioactive iodide are
delayed for several weeks or as long as 6 months.
During this time, symptoms may be controlled with
thioamide drugs or propanolol
Hyperthyroidism and the Metabolism of
Other Drugs

Treatment of hyperthyroidism changes the rate of

body metabolism, including the rate of many
drugs
Use in Special Population: Children

For hypothyroidism, replacement therapy is

required because thyroid hormone is essential for
normal growth and development
As in adults, levothyroxine is the drug of choice in
children and dosage needs may change with
growth
For congenital hypothyroidism (cretinism), drug
therapy should be started within 6 weeks of birth
and continued for life
Delay in replacement therapy may result in
permanent retardation despite resolution of the
symptoms that resulted from thyroid deficit
For hyperthyroidism, PTU or methimazole is used.
Potential risks for adverse effects are similar to those in
adults.
Radioactive iodide may cause cancer and
chromosome damage in children, therefore, this
agent should be used only for hyperthyroidism that
cannot be controlled by other antithyroid drugs or
surgery
Use in Special Population: Older Adults

Signs and symptoms of thyroid disorders may

mimic those of other disorders that often occur in
older adults (e.g. congestive heart failure)
For hypothyroidism, levothyroxine is given. Thyroid
hormone replacement increases the workload of
the heart and may cause serious adverse effects
in older adults, especially those with
cardiovascular disease
Periodic measurements of serum TSH levels are
indicated to monitor drug therapy, and doses can
be adjusted when indicated
Blood pressure and pulse should be monitored
regularly.
As a general rule, the drug should be given if the
resting heart rate is more than 100 beats per
minute
For hyperthyroidism, PTU or methimazole may be
used, but radioactive iodine is often preferred
because it is associated with fewer adverse effects
than other antithyroid drugs or surgery
Use in Special Population: Patients with
Renal Impairment

Some thyroid and antithyroid drugs are excreted

by the kidneys, and dosage adjustment may be
required in the presence of renal impairment.
Example: PTU
Most drugs given to patients with hypothyroidism
have a prolonged effect, because the glomerular
filtration rate of the kidneys is decreased
Use in Special Population: Patients with
Hepatic Impairment

Presence of hepatic impairment, drugs may

accumulate and cause adverse effects.
Drug metabolism in the liver is delayed in patients
with hypothyroidism, so most drugs given to these
patients have a prolonged effect
Individuals who are hyperthyroid metabolize drugs
more slowly than in the euthyroid state
Use in Special Population: Patients with
Critical Illness

Individuals in thyroid storm or thyrotoxic crisis are

commonly managed in the critical care unit.
The hypermetabolic state increases the
metabolism of medications, so increased or more
frequent dosing may be necessary
Use in Special Population: Home Care

Home care nurse may be involve in assessing the

patient’s response to therapy, teaching about the
disease process, managing symptoms, and
preventing and managing adverse drug effects
The End!