Progestin drugs Flashcards

1
Q

Progestins

A

Progesterone
Norethindrone
Ethynodiol diacetate
Levonorgestrel
Noregestimate
Desogestrel
Etonogestrel
Drospirenone
Medroxyprogesterone acetate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

1st generation progestin names

A

Progesterone
Norethindrone
Ethynediol diacetate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

1st gen progestin properties

A

19-nor, 17 ethynyl steroids (oral contraceptives)
17-ethnyl group increases oral bioavailability
19-methyl group not necessary
Replacement of 19 methyl with H enhances activity
Replacement of 17 acetyl with OH increases oral bioavailability
Ester groups are rapidly hydrolyzed in vivo

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Levonorgestrel

A

2nd gen progestin
Levo isomer of norgestrel, which is a racemic mix
Only levo form is active
High oral bioavailability
Used in IUDs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Norgestimate

A

Prodrug
Converted to levonorgestrel oxime and then to levonogestrel in vivo

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Desogestrel

A

3rd generation progestin
Prodrug
Rapidly metabolized to etonogestrel
High bio availability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Etonogestrel

A

Active form of Desogestrel
Structurally analogous to levonorgestrel
Used in the subdermal implant (Nexplanon) or the vaginal ring

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Drospirenone

A

4th gen progestin
Relatively weak progestogenic activity (10% of levonorgestrel)
Anti mineralocorticoid activity
Negates Side effects of ethynyl estradiol in combination therapy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Medroxyprogesterone acetate

A

1st gen progestin
Used for depot injection
as a long acting progesterone-only contraceptive

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Drug interactions

A

Other steroids
OCs may increase the blood levels of other steroids by interfering with their metabolism (i.e glucocorticoids)
Anticonvulsants
Phenytoin - induces drug-metabolizing enzymes in the liver
Antibiotics
Rifampin - induces drug metabolizing enzymes in the liver
increases the rate of metabolism of many other drugs
Tetracyclines
Suppresses gut flora that participate in enterohepatic recycling

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Ulipristal acetate

A

Selective progesterone receptor modulator (SPRM)
Used as an emergency contraceptive
Can be effective up to 5 days after unprotected sex
SE: Nausea, abdominal pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Mifepristone

A

RU-486
Progesterone antagonist
Abortificant
used in combo with misoprostol (PGEI derivative, oral prostaglandin) up to 70 days
SE: Nausea, vomiting, bleeding (5%) requires intervention admin only by physicians

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Danazol

A

Weak androgen, weak progestin, and antiestrogen
Effective for endometriosis
inhibits the surge of LH and FSH and suppress ovarian function; causes atrophy of the endometrium
Adverse effects: mostly from weak androgenic activity
Weight gain, decreased breast size, acne, oily skin, hirsutism
Contraindication
Hepatic dysfunction
Pregnancy and breast feeding

How well did you know this?
1
Not at all
2
3
4
5
Perfectly