Pharmacology for Dentistry

Glucocorticoids & Sex Hormones 287

weak androgenic activity. It needs to be
given continuously without cyclical
progestogen.

It restores plasma endorphin level in
postmenopausal women and act centrally to
affect the thermoregulatory system.

Adverse effects include weight changes,
ankle edema, dizziness, headache, abdominal
pain, GI disturbances, vaginal bleeding,
arthralgia, myalgia, migraine, visual
disturbances, liver function changes,
increased facial hair, depression, skin rash
and pruritus.

It is indicated in vasomotor symptoms
in estrogen deficiency and osteoporosis
prophylaxis.

ANTIESTROGENS

Also known as estrogen antagonists or
ovulation inducing agents. They act by
binding to estrogen receptors.

CLOMIPHENE CITRATE

It is a triphenyl ethylene compound and
a competitive partial agonist inhibitor of
endogenous estrogen. It can produce
regression of estrogen induced proliferative
endometrium. It can also prolong the luteal
phase in normal menstruating women.

Due to its probable direct effect on
ovaries, it may increase the gonadotrophin
secretion. It also exerts a weak estrogenic
action on endometrium.

It is well absorbed after oral
administration, metabolized and excreted in
bile and main side effects include hot
flushes, ovarian enlargement and cyst
formation which may be due to

overstimulation and can also lead to rupture

and bleeding.

Clomiphene is mainly used in the treatment

of female infertility due to ovulatory failure and

is also found useful to aid in vitro fertilization.

It is also used to promote spermatogenesis

in male due to oligospermia and asthenosper-

mia.

TAMOXIFEN

It is a competitive partial agonist inhibitor

of estradiol at the estrogen receptor and is

used mainly in the treatment of advanced

breast cancer in postmenopausal women. It

is also used in male infertility due to its

weaker estrogen effect and lesser side effects.

It is effective on oral administration and

is excreted in bile.

Adverse effects include hot flushes,

vaginal bleeding, menstrual irregularities,

anorexia, depression and dermatitis.

PROGESTINS

Progesterone is naturally secreted by the

corpus luteum and placenta and functions

to maintain pregnancy after conception.

Their derivatives are of two types, which are

classified as in table 8.3.3.

PROGESTERONE

The physiological functions of

progesterone include:

• Induction of secretory phase of the
  menstrual cycle.


• Development of alveolar system of
  breasts.


• Preparation of endometrium for the
  implantation of fertilized ovum for
  further pregnancy.