FRS Progestin

Question 1

Progestins

Answer 1

• Prototype- norethindrone acetate
• Natural hormone progesterone
• Secreted mainly by corpus luteum in small amounts by testis, large amount secreted by placenta, and by adrenal cortex
• used as contraceptive with estrogen - treat amenhorrea and functional uterine bleeding
• e.g levenorgestrel - once available as implant to prevent pregnancy (norplant), available as uterine insert (minera)
• used as morning-after pill (Preven, Plan B)

Question 2

Progestin Use

Answer 2

• medroxyprogesterone (Provera)- P.O to treat amenhorrea, by injection for cancer palliation therapy
• Norethindrone (Aygestin) - To treat amenhorrea and as combination oral contraceptive
• Norgestrel ( Orvette) - oral contraceptive
• Desogestrel & Drospirenone - combination form as contraceptive

Question 3

Progestin Therapeutic Action & Indication

Answer 3

• Progestins transform the proliferative endometrium into a secretory endometrium, inhibit the secretion of FSH and LH.
• Prevent follicle maturation and ovulation, inhibit uterine contractions.
• Indicated for contraception, for treatment of amenorrhea & treatment for functional uterine bleeding

Question 4

Progestin Pharmacokinetics

Answer 4

• Well absorbed , undergo hepatic metabolism; excreted in the urine
  Cross placenta and enter breast milk
• Not to be used during pregnancy or lactation
• Oral
• Onset – varies
• Peak – unknown
• Duration - unknown

Question 5

Progestin Contraindications & Cautions

Answer 5

• Contraindicated in the presence of any known allergies, pregnancy, idiopathic vaginal bleeding, breast cancer, history of thromboembolic disorder – due to increased risk of thrombus and embolus development.
• Caution in patients with epilepsy, migraine headaches, asthma or cardiac or renal dysfunction (exacerbation of condition)

Question 6

Progestin Drug Interactions

Answer 6

• Barbiturates, carbamazepine, phenytoin or rifampin may reduce effects of progestin

Question 7

Progestin Adverse Effects

Answer 7

• Venous thromboembolism, loss of vision, diplopia, migraine headache, rash, acne, alopecia, breakthrough bleeding and spotting, Increased weight, fluid retention, edema