Estrogen and

antiestrogens
Progestogens and
antiprogestogens Sex
Contraceptive drugs hormones
Drugs acting on uterus and related
and smooth muscle drugs
Three major naturally occurring
oestrogens in women: Estrogens and
antiestrogens
1. Estradiol (E2) - the predominant form

in nonpregnant females

2. Estrone (E1) - produced during

menopause

3. Estriol (E3) - the primary estrogen of

pregnancy
 Pharmacological effects of
estrogens
development of the female genital
tract of the female secondary sex
characteristics
 maintenance of both
proliferative and secretory phases
of the uterine endometrium
Ovulation- increase small doses
or decrease larger doses
 development of the breast and
latescence- increase small doses
or decrease larger doses
Other actions:
decreasing postmenopausal
disturbances in sleep
 increasing aldosterone and
causing water and Na+ retention
 decreasing LDL and increasing
HDL levels in plasma
 increasing factor II, VII, IX, X and
coagulation
SLEEP
estrogen decreases post-menopausal
disturbances in sleep

CARDIOVASCULAR
in post-menopausal women estrogen provides a
protective effort against cardiovascular disease
causing a decrease in LDL and an increase in
HDL levels in plasma

UROGENITAL TRACT
estrogen treatment reverses
postmenopausal atrophy of vulva, vagina,
urethra, and trigone of the bladder
OSTEOPOROSIS
estrogen decreases the resorption of bone but has
no effect on bone formation
 estrogen decreases frequency of hip fracture and
weight-bearing exercise also slow loss of bones
 treatment with estrogen must begin within 2 or 3
years of menopause, earlier if possible
VASOMOTOR
estrogen treatment re-establishes feedback on
hypothalamic control of norepinephrine
section, leading to decreased frequency of “hot
 CLINICAL USES OF ESTROGENS
1.Postmenopausal Syndrome
2. Primary Hypogonadism
3. Menstrual Disorders
4. Conceptions
5. OTHERS:-SUPPRESS LACTATION AFTER CHILD
BITH
-ADVANCE BREAST
CANCER(POSTMENOPAUSAL)AND PROSTATIC
CANCER
ADVERSE EFFECTS OF ESTROGENS

1. ORAL ADMINISTRATION-
NAUSEA,VOMITING,DIARRHEA
2. CARDIOVASCULAR EFFECTS:-RISK OF
VENOUS THROMBOEMBOLISIS
-HYPERTENSION,EDEMA
3. OTHER:-GALLBLADER DISEASE
-RISK OF BREAST AND ENDOMETRIAL
CARCICOMA
 ANTIESTROGENS
1. EFFECTS:-PARTIAL/ANTAGONIST FOR
ESTROGEN RECEPTOR
2.USES:-ANOVULATORY INFERTILITY
-MENSTRUAL DISORDERS
-ADVANCED BREAST CANCER
-FUNCTIONAL AMENORRHEA
3. ADVERSE EFFECTS:-MULTIPLE OVULATION
WITH MULTIPLE PREGNANCY
-OVARY TUMEFACTION
 example
TAMOXIFEN
-NONSTEROID COMPETITIVE ESTROGEN
ANTAGONIST
-USED FOR TREATMENT OF ESTROGEN
DEPENDENT BREAST CANCER
 PROGESTOGENS
PHARMACOLOGICAL EFFECTS
-CONVERTING THE UTERINE EPITHELIUM
FROM THE PROLIFERATIVE TO THE
SECRETORY PHASE
-DEVELOPMENT OF GALACTOPHORE
-THERMOREGULATION:INCREASING BODY
TEMP.
 Progesterone
CLINICAL USES
- MENSTRUAL DISORDERS
-CANCER
ADVERSE EFFECTS
-GI REACTIONS
-EDEMA
-VIRILIZATION
-ACNE
 example

MIFEPRISTONE
-A SYNTHETIC STEROID COMPOUND USED AS A
PHARMACEUTICAL.
-IT IS A PROGESTERONE RECEPTOR ANTAGONIST
USED AS AN ABORTIFACIENT IN THE FIRST 2
MONTHS OF PREGNANCY AND IN SMALLER
DOSES AS AN EMERGENCY CONTRACEPTIVE.
 ANTIPROGESTOGENS

CLINICAL USES:
1.MEDICAL TERMINATION OF INTRAUTERINE
PREGNANCIES OF UP TO 49 DAYS GESTATION
2.TERMINATION OF PREGNANCIES BETWEEN 13 AND 24
WEEKS GESTATION
3.LABOR INDUCTION IN FETAL DEATH IN UTERO
4.EMERGENCY CONTRACEPTIVE
 example

CONTRACEPTIVE DRUGS

-have been identified that inhibit fertility by a

number of different mechanisms
A CONTRACEPTIVE DRUG SHOULD:
-EXTREMELY SAFE AS WELL AS HIGHLY
EFFECTIVE
-ITS ACTION MUST BE QUICK IN ONSET,QUICKLY
AND COMPLETELY REVERSIBLE EVEN AFTER
YEARS OF CONTINUOUS USE
-IT MUST NOT AFFECT LIBIDO
FOR FEMALE:
-INHIBITION OF OVULATION
-PREVENTION OF FERTILIZATION
-INHIBITION OF IMPLANTATION
-USE OF SPERMICIDES IN VAGINA
FOR MALE:
-DIRECT INHIBITION OF SPERMATOGENESIS

-INDIRECT INHIBITION OF SPERMATOGENESIS

ESTROGENS+PROGESTOGENS
1.PHARMACOLOGIGAL EFFECTS:
-INHIBITION OF OVULATION
-INHIBITION OF IMPLANTATION
-INCREASE IN VISCIDITY OF CERVICAL
MUCUS
2.CLINICALUSES
A.ORAL-SHORT AND LONG ACTING
CONTRACEPTIVES
B.LONG ACTING INJECTIONS
C.SLOW RELEASING PREPARATIONS
D.ULTIPHASIC PREPARATIONS
3. ADVERSE EFFECTS
-GI REACTIONS
-MENSTRUAL DISORDER
-VENOUS THROMBOEMBOLISM
-EDEMA,DEPRESION,WEIGHT GAIN,ACNE
. DRUG INTERACTIONS
-HEPTICENZYME IDUCERS ATTENUATE THE
EFFECT OF CONTRACEPTIVE DRUGS
 CONTRACEPTIVE DRUGS-
MALE
GOSSYPOL
-COMPOUND DESTROYS ELEMENTS OF THE
SEMINIFEROUS EPITHELIUM BUT DOES NOT ALTER THE
ENDOCRINE FUNCTION OF THE TESTIS.
*OTHERS:
-CYPROTERONE ACETATE
-ANDROGEN
-PROGESTRONE-ANDROGEN COMPOUND
 DRUGS ACTING ON UTERUS
SMOOTH MUSCLE
STIMULANTS OF UTERUS
-OXYTOCIN

-PITUITRIN
-ERGOT ALKALOID
-PROSTAGLANDINS
RELAXANTS OF UTERUS
-RITODRINE -SALBUTEROL
-TERBUTALINE -MAGNESIUM SULFATE
 oxytocin
A PEPTIDE HORMONE,SYNTHESIZED IN
HYPOTHALAMUS;RELEASED IN LARGE AMOUNTS
PHARMACOLOGICAL EFFECTS
-UTERINE CONTRACTION
CLINICAL USES
-SMALL DOSES:RHYTMIC CONTRACTION;INDUCTION
OF LABOR
-LARGE DOSES:TONIC CONTRACTION;POSTPARTUM
HEMORRHAGE
ADVERSE EFFECTS:
*RECOMMENDED DOSES-RELATIVELY SAFE
WHEN USED AT,AND SIDE EFFECTS ARE
UNCOMMON
*EXESSIVE DOSAGE OR LONGER
ADMINISTRATION-TETANIC UTERINE
CONTRACTIONS,UTERINE RUPTURE,POSTPARTUM
HEMORRHAGE,WATER INTOXICATION,AND
SOMETIMES FATAL
 PITUITRIN
PHARMACOLOGICAL EFFECTS
-CONTACTING VASCULATURES

CLINICAL USES
-USED IN CONTROLLING BLEEDINGS

ADVERSE EFFECTS
-PALE FACE,BP ELEVATION,PALPITATION,ABDOMINAL PAIN
 ERGOT ALKALOID
PHARMACOLOGICAL EFFECTS
-UTERINESMOOTH MUSCLE STIMULATION
-VESSEL-CONTRACTING EFFECTS
-a-RECEPTOR BLOCKING EFFECT
USED IN:
-UTERUS BLEEDING
-POSTPARTUM HEMORRHAGE
-MIGRAINE
ADVERSE EFFECTS
-GI DISTURBANCES,DIARRHEA,NAUSEA,AND
VOMITING PROLONGED VASOSPASM

CONTRAINDICATIONS
-OBSTRUCTIVE VASCULAR,PREGNANCY
 PROSTAGLANDIS
USED IN:
-ABORTION COMBINED WITH MIFEPRISTONE

-FACILITATION OF LABOR
ADVERSE EFFECTS
-GI DISTURBANCE,MAINIT,VOMITING AND ABDOMINAL PAIN
CONTRAINDICATIONS
-BRONCHIAL ASTHMA,GLAUCOMA
 RELAXANTS OF UTERUS
-RITODRINE
-TERBUTALINE
-SALBUTEROL
-MAGNESIUM SULFATE
USED IN:
-DYSMENORRHEA
-PREMATURE BIRTH