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Oral contraceptives
and Fertility agents
I.=STEROIDAL , NATURAL
A. ESTRADIOL ( ESTRADIOL 17B, E2)
B. ESTRONE (E1)
C. ESTRIOL (E3)
ESTRADIOL- IS THE MAJOR ESTROGEN
SYNTHESIZED AND SECRETED BY THE
NORMAL OVARY
ADVERSE EFFECTS:
6. HOT FLUSHES
7. OVARIAN ENLARGEMENT
8. MULTIPLE PREGNANCY -10%
1. TAMOXIFEN- MECH. OF ACTION – COMPETES
FOR BINDING OF ESTROGEN TO THE RECEPTOR
ADVERSE EFFECT :
6. HOT FLUSHES
7. NAUSEA AND VOMITING
8. MENSTRUAL IRREGULARITIES
THE PROGESTINS
PROGESTATIONAL AGENTS
ARE SYNTHETIC CHEMICALS CLOSELY RELATED
TO PROGESTERONE
2 TYPES
A. 21CARBON COMPOUND- WHICH CAN PRODUCE
A SECRETORY ENDOMETRIUM AND MAINTAIN
PREGNANCY
C-21 PROGESTERONE
PROGESTERONE
6 METHYL-17α ACETOXYPROGESTERONE
(MEDROXYPROGESTERONE)
17α –ACETOPROGESTERONE
6 α- METHYL-6 DEHYDRO-17α
ACETOXYPROGESTERONE
CLINICAL USES
8. PROGESTIN CHALLENGE TEST –TO TEST FOR
THE DIFFERENTIAL DIAGNOSES OF
AMENORRHEA.
9. DYSFUNCTIONAL UTERINE BLEEDING
3. CONTINOUS PROGESTIN THERAPY TO TREAT
a) ENDOMETRIOSIS
b) ENDOMETRIAL CA- MEGESTROL ACETATE
4. LUTEAL PHASE DEFECT ASSOC. WITH HABITUAL
ABORTION
5. CONTRACEPTION- MEDROXYPROGESTERONE
ACETATE AND NORETHINDRONE ENANTHATE
ADVERSE EFFECTS:
8. EDEMA AND DEPRESSION
9. ANDROGEN LIKE PROGESTINS ( NORGESTREL
AND NORETHINDRONE CAN INCREASE RATIO OF
LDL TO HDL –
10. AND MAY CAUSE THROMBOPHLEBITIS,
11. PULMONARY EMBOLISM
12. ACNE ,HIRSUTISM AND WT. GAIN
ANTIPROGESTIN
MIFEPRISTONE ( RU486 )- IS A POTENT
ANTIGLUCOCORTICOID THAT HAS A PARTIAL
PROGESTERONE ANTAGONIST- AGONIST
ACTIVITY. IT IS AN ABORTIFACIENT AGENT.
ORAL CONTRACEPTIVES
3 CLASSIFICATION
7. FIXED COMBINATION –CONTAIN CONSTANT
AMOUNTS OF ESTROGEN (ETHINYL ESTRADIOL
AND A PROGESTIN ( NORETHINDRONE )
2. MULTIPHASIC COMBINATION – CONTAIN
CONSTANT AMOUNTS OF ESTROGEN BUT
VARIABLE DOSE OF PROGESTIN
MECHANISM OF ACTION :
6. INHIBIT MID-CYCLE LHsurge, THUS INHIBITING
OVULATION
7. THICKENS CERVICAL MUCUS
8. ALTERS SECRETORY CHANGES OF
ENDOMETRIUM
9. ALTERS TUBAL TRANSPORT
OTHER KINDS OF HORMONAL
CONTRACEPTION
1. PROGESTIN IMPLANTS- LEVONOGESTREL
CONTAINDICATIONS
10. CVA
11. ESTROGEN DEPENDENT CA
12. LIVER DISEASE
13. MIGRAINE
SELECTIVE ESTROGEN RECEPTOR MODULATOR
( SERM )-
RALOXIFENE (EVISTA) = HAS SELECTIVE AGONIST
OR ANTAGONIST ACTIVITIES ON TISSUES
RESPONSIVE TO ESTROGEN. IT ACTS AS AN
AGONIST ON BONE AND PARTIALLY ON
CHOLESTEROL METABOLISM
(DECREASE TOTAL AND LDL CHOLESTEROL)
IT IS AN ANTAGONIST ON HYPOTHALAMUS OR IN
UTERINE AND BREAST TISSUES
ASSOC. WITH INCREASE RISK OF VENOUS
THROMBOEMBOLIC EVENT
USES: REPLACEMENT THERAPY IN CLIMATERIC
FOR PREVENTION OF OSTEOPOROSIS , TO
DECREASE SYMPTOMS OF MENOPAUSE
DRUGS AND DIETARY SUPPLEMENTS USED
IN THE TREATMENT OF OSTEOPOROSIS
1. ALENDRONATE
-DECREASES BONE TURNOVER,
-INHIBITS OSTEOCLAST ACTIVITY
2. CALCITONIN SPRAY
-INTERFERES WITH OSTEOCLASTS AND INHIBITS
BONE RESORPTION
3. CALCIUM CARBONATE SUPPLEMENTS-
1,200mgs /day
4. ESTROGENS ( COMBINED WITH A PROGESTIN )
5. SERM- RALOXIFEN