DRUGS

THERAPEUTIC
USES

ADVERSE
EFFECT

CONTRA
INDICATION

ESTROGEN
Estradiol
Oral micronized
Transdermal patch
Vaginal cream
IM injections
Premarin
Conjugated estrogen
Oral form
Ethinyl estradiol and
mestranol
Synthetic estrogen
Oral form

Oral contraception
(+progesterone)

Hypo-ovarian conditions ;
[ 1ry ovarian failure,
premenopausal hysterectomy]

Primary hypogonadism in
young women to induce
2ndry sexual characters
Menses
Optimal growth
Prevent osteoporosis
Given in cycles : 21 days every
month
st
After 1 uterine bleeding
combine with progestins

Alleviate menopausal
symptoms

Osteoporosis

Dysmenorrhea

Treatment of hirsutism and

amenorrhea

Prostatic carcinoma

GIT upsets (oral)

Withdrawal uterine bleeding

Thromboembolism

Oedema

Long term therapy gall

bladder disease and
endometrial carcinoma

In treatment of prostatic
cancer gynaecomastia and
impotence

Women with estrogendependent neoplasm

Pregnancy

Patients with predisposing

tendency to
thromboembolism

Hypertension

Liver disease / gallstones

Diabetes

fibroids

SEX STEROIDS
PROGESTINS

Natural ; Progesterone

Synthetic ;
Medroxyprogesterone
acetate
Norethindrone
Norgestrel

Contraception used
either alone or with
estradiol
Hormone replacement
therapy + estrogen
Large dose of
medroxyprogesterone is
given to suppress the
production of FSH and LH
and ovulation and
subsequent amenorrhea
used in :
Severe dysmenorrhea
Endometriosis
Uterine bleeding disorder

Increase blood pressure

Decrease HDL
Delay resumption of
ovulation after
termination of therapy
Androgen like progestins
( norgestrel) :
Acne
Hirsutism
Weight gain

ANDROGENS

Anabolic steroid
Synthetically prepared androgens.
They increase anabolism directly
thru increasing the incorporation of
amino acids to protein and
stimulation of RNA polymerase
activity in skeletal. Indirectly by
antagonizing the protein catabolic
action of glucocorticoid
Nandrolone
phenpropionate IM/wk
Methandrostenolone
oral/day

Androgen replacement
therapy in men (pre and postpubertal hypogonadism)

Gynecological disorder
+ with estrogen to decrease
menopausal symptom
Estrogen dependent breast
cancer (but now replaced by
tamoxifen)

Refractory anemia (large dose)

Osteoporosis

Protein anabolic agents

Anabolic steroid : treatment of

Short stature
Hypoproteinaemia of
nephrosis
Debilitated postoperative
patients, burns and premature
babies

Virilization
Precocious puberty
Azoospermia and 2ndry
gonadotropin suppression
(over 6wks period)
Enhances growth of prostatic
tumors
Fluid retention (Na and Cl)
Cholestatic jaundice

SELECTIVE ESTROGEN RECEPTORS MODULATORS

TAMOXIFEN

RALOXIFENE

Bone
Agonist

Agonist

ACTIONS ER in
breast
endometrium
antagonist
agonist
Endometrial
Hyperplasia

antagonist

no effect

CLINICAL USE

ADVERSE EFFECT

Breast cancer in
postmenopausal
patients

Postmenopausal
osteoporosis

Venous
thromboembolism
Hot flushes
Nausea / vomiting
High risk of endometrial
cancer
venous
thromboembolism
hot flushes

SEX STEROIDS INHIBITORS

ESTROGEN INHIBITOR ; CLOMIPHENE
Non steroidal drug that have some
anti-estrogenic properties
Mechanism of action :
Drug competitively blocks the
estrogen receptors in hypothalamus
and AP prevent normal estrogenmediated ve feedback inhibition of
GnRH release increase the
secretion and release of pituitary LH
and FSH ovarian stimulation
Therapeutic use :
Induction of ovulation in
anovulatory infertility of
women with functioning
hypothalamo-pituitary axis and
whose blood estrogen levels
are within normal
Adverse effects :
Ovarian enlargement + ovarian
cyst
Cyclic ovarian pain
Hot flushes and discomfort
Blurring of vision
Nausea
Abnormal uterine bleeding
Breast engorgement
Contraindication :
Suspected pregnancy
Liver disease
Bleeding of undetermined
origin (sign of an undiagnosed
neoplasm)

PROGESTERONE INHIBITORS
A. MIFEPRISTONE
Progesterone receptors
antagonist
Used in induce abortion in
early pregnancy
Given as single oral dose
followed by misoprostol
Low incidence of serious
toxicity
B. DANAZOL
Partial agonist on progesterone
receptors
Used for endometriosis &
fibrocystic disease of the
breast
Adverse effect :

Androgenic effect

Headache

Hot flushes

Change in libido

Muscle cramps

ANTIANDROGEN
A. LEUPROLIDE
GnRH agonist
Used for treatment of prostate
cancer
B. FINASTERIDE
Alpha reductase inhibitor
Prevent activation of testerone
into dihydrosterone
Used for ;
Benign prostate hyperplasia
Prevent hair loss in men
C. FLUTAMIDE
Androgen receptor antagonist
Used for cancer prostate
D. CRYPROTERONE &
SPIRONLOACTONE
Androgen receptor antagonist
Used for hirsutism