Antithyroid Substances - The Three Best Known Antithyroid Drugs

Drugs that are known to inhibit the secretion of thyroidsenses a decrease in the concentrations of thyroxine
hormones are generally known as antithyroidand triiodothyronine, it secretes more TSH. The higher
substances. Three of the best known antithyroidlevels of TSH then causes overgrowth of the thyroid
substances are propylthiouracil, thiocyanate, andgland but still, the gland fails to produce enough
inorganic iodides. Each of this drugs blocks thyroidamounts of hormone. This leads to the formation of an
secretion in a different way and the differentenlarged thyroid gland, also known as goiter.
mechanisms by which they do so are furtherInorganic Iodides
explained.Inorganic iodides inhibit most of the activities only when
Propylthiouracilin very high concentrations, as in 100 times the normal
Propylthiouracil -- and its relatives, methimazole andplasma levels of iodides. This effect, however, remains
carbimazole -- decrease thyroid hormone formation byonly for a few weeks.
preventing its formation from iodides and tyrosine. ThisThis inhibitory effect of iodides on the thyroid gland is
drug acts by blocking the peroxidase enzyme that isdue to the reduction in the rate of iodide trapping of
necessary in the first step of the formation of thyroidthe gland, which also decreases the rate of production
hormones, which is the oxidation of iodine so it canof thyroxine and triiodothyronine. Even more so, the
combine to tyrosine. Propylthiouracil also blocks thenormal endocytosis of colloid from the follicles by the
coupling of two iodinated tyrosines that are needed tothyroid glandular cells is paralyzed in the face of
form thyroxine or triiodothyronine, the two kinds ofextremely high iodide concentrations. As this is the first
thyroid hormone.step in the release of thyroid hormones, thyroid
Propylthiouracil does not prevent the formation ofhormone secretion is shut down almost immediately.
thyroglobulin. Since it only blocks the formation ofThe mechanisms by which inorganic iodides work on
thyroxine and triiodothyronine, the absence of both inthe thyroid gland decreases the size of the thyroid and
the thyroglobulin can stimulate the pituitary gland toits blood supply due to its inactivity. This is the opposite
secrete more thyroid-stimulating hormone. This thenof the previous two drugs, which only serve to
promotes the growth of glandular tissue despite itsincrease the size of the gland.
being unable to produce the two hormones and formsPropylthiouracil and Iodides in Thyroidectomy
a goiter..Hyperthyroid patients must undergo several weeks of
Thiocyanatepreparation before going under the knife. It was found
Thiocyanate ions decrease iodide trapping, thethat these procedures could spell the difference
mechanism by which the thyroid gland acquires iodinebetween life and death for a patient and patient
from the circulating blood. The same pump thatmortality has been greatly reduced since the
transports the iodide ions necessary for normal thyroiddevelopment of these preoperative procedures.
function can also pump thiocyanate ions, perchlorateSeveral weeks prior to the operation, the patient is
ions, and nitrate ions. Increased concentrations ofadministered with the antithyroid substance
thiocyanate ions then compete with the transport ofpropylthiouracil until such time that the basal metabolic
iodide ions into the thyroid cells.rate of the patient reaches normal levels. One to two
Like propylthiouracil, the decreased availability of iodideweeks before the operation, the patient receives high
does not stop the formation of thyroglobulin.doses of iodides, which causes the gland to recede in
Thiocyanate can only prevent the iodination ofsize and its blood supply to diminish. This is done to
thyroglobulin and in consequence, prevents thedecrease the necessary amount of surgery -- an
formation of thyroid hormones.enlarged thyroid means a larger cut -- and to
As with propylthiouracil, when the pituitary glanddecrease the amount of bleeding.