CONTRACEPTIVES

Indications
 Prevention of pregnancy.
 Regulation of menstrual cycle.
 Emergency contraception (some products).
 Treatment of heavy menstrual bleeding
 Treatment of premenstrual dysphoric disorder
 Management of acne in women >14 yr
 Increase folate levels
Action
Monophasic Oral Contraceptives: Provide a fixed dosage of estrogen/progestin
over a 21-day cycle.
Biphasic Oral Contraceptives:
Triphasic Oral Contraceptives: Varying doses of estrogen/progestin may more
closely mimic natural hormonal fluctuations.
Fourphasic Oral Contraceptives:Doses of estrogen decrease while doses of
progestin increase over the 28-day cycle.
• Ovulation is inhibited by suppression of follicle-stimulating hormone (FSH) and
luteinizing hormone (LH).
• alter cervical mucus and the endometrial environment
• preventing penetration by sperm and implantation of the egg.
• Therapeutic Effects:
• Prevention of pregnancy.
• Decreased severity of acne.
• Decrease in menstrual blood loss.
• Decrease in premenstrual disphoric disorder.
• Decrease in vasomotor symptoms or symptoms of vulvar and vaginal
atrophy due to menopause.
• Increase in folate levels and prevention of neural tube defects.
Pharmacokinetics
• Absorption:
• Ethinyl estradiol—rapidly absorbed;
• Norethindrone—65% absorbed;
• Desogestrel and levonorgestrel—100% absorbed;
• Dienogest—91% absorbed.
• Others are well absorbed after oral administration.
• Slowly absorbed from implant, subcutaneous or IM injection.
• Some absorption follows intrauterine implantation.
• Distribution: Unknown.
• Protein Binding: Ethinyl estradiol—97– 98%; Drospirenone—97%; Dienogest—90%; Ulipristal
—>94%.
• Metabolism and Excretion: Ethinyl estradiol and norethindrone—undergo extensive first-pass
hepatic metabolism. Mestranol—is rapidly converted to
• ethinyl estradol. Desogestrel—is rapidly metabolized
• to 3-keto-desogestrel, the active metabolite. Most
• agents are metabolized by the liver.
• Half-life: Ethinyl estradiol—6– 20 hr; Levonorgestrel—45 hr; Norethindrone—5– 14 hr;
Desogestrel
• (metabolite)—38 ± 20 hr; Drospirenone—30 hr;
• Norgestimate (metabolite)—12– 20 hr; Dienogest—11 hr; others—unknown; Ulipristal—32 hr.