Selective Estrogen Receptor
Modulator
By
Dr Zarish Ghafoor

Estrogens
• Estrogen is a category of sex hormone
responsible for the development and regulation
of the reproductive system and secondary sex
characteristics.

Source of estrogen
• Ovaries (max)
• Fat tissue
• Adrenal gland

Mechanism of action
Receptor sites
• Hypothalamus
• Pituitary
• Breast
• Bone
• Uterus
• Heart

Effect of estrogen drugs
• Estrogen agonist
• Antagonist
• Mixed agonist antagonist

Selective estrogen receptor modulators
(SERMS)
• Functions of SERMs
• Tissue selective action
• Estrogenic action in some tissues
• Antiestrogenic action in other tissues

EFFECTS OF SERMS ON TISSUES

SERMs

Pharmacological Effects of SERMs
Estrogenic effects
• Bone………Decrease
resorption……Decreases chances of fracture
• Liver…..decrease LDL increase HDL,
• Protein…….increase protein synthesis
• Blood…..increase coagulation…. Increase
deep venous thrombosis

Pharmacological Effects of SERMs
• Estrogenic effects
• Uterus….increase endometrial proliferation
except clomiphene
• Ovary …….increase ovarian
stimulation.(Clomiphen)
Anti estrogenic effects
• Breast…..decrease breast cell proliferation

CLINICAL USES of SERMs
1)As Replacement therapy
Primary Hypogonadism
(Turner’s syndrome)
Premature ovarian failure
Surgical removal of the ovaries.
Menopause

CLINICAL USES of SERMs
1)Other uses:
Contraception
Dysfunctional uterine bleeding (DUB)
Prostate cancer
Dysmenorrhea
Osteoporosis
Amenorrhea
Hirsutism
Breast cancer
Gynecomastia

ADVERSE EFFECTS of SERMs
1) Ovarian hyper stimulation-Multiple pregnancies
2) Polycystic ovaries
3) Increase risk of endometrial cancer
4) Increase risk of deep venous thrombosis
5) Pulmonary embolism
7) Retention of salt and water Hypertension
8) Hot Flushes
9) Leg cramps
10) Nausea
11)Vomiting

Hormonal Oral Contraceptives
OCPs

Hormonal Oral Contraceptives (OCPs)
• Preparations of OCPs:
• Combined oral contraceptive pills
• Monophasic
• Multiphasic
• Progesterone only pills (Mini pills)
• Emergency Pills (Post coital pills)

Hormonal Oral Contraceptives (OCPs)
Routes of administration of OCPs:
Oral pills
S/C Implants
Transdermal patches
Injections (long acting)
Intra-uterine devices (IUDs)
Vaginal rings.

Hormonal Oral Contraceptives (OCPs)
Mechanism of action
• Inhibition of ovulation (feedback inhibition of
pituitary (causing abolition of LH surge)
• Thickening of cervical mucus
• Decreased motility and secretions of the fallopian
tubes
• Making endometrium unfavourable for
implantation

Hormonal Oral Contraceptives (OCPs)
Clinical uses:
1) Osteoporosis
2) Ovarian Cysts
3) Menstrual Cycle Irregularities
4) Dysmenorrhea
5) Benign Breast Disease
6) Menorrhagia
7) Ectopic Pregnancy
8) Pelvic Inflammatory Disease (PIDs)

Hormonal Oral Contraceptives (OCPs)
Adverse effects:
Mild:
• Nausea, edema, break through bleeding, Migraine,
Breast discomfort
Moderate:
• Break through bleeding, Weight gain, Hyper
pigmentation, Acne, Hirsutism, Vaginal infection,
Amenorrhea

Hormonal Oral Contraceptives (OCPs)
Adverse effects:
Severe:
• Venous thromboembolic disease
• Cerebrovascular disease
• cholelithiasis
• hepatic adenoma
• Breast cancer
• Alopecia