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35 Cards in this Set

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Define contraceptives

Are agents used to prevent, stop and even disrupt contraception

How many classes of oral contraceptives exist? List them

4 classes of oral contraceptives


1. Sequential pills 💊


2. Mini pills 💊


3. Post coital contraception ≈ morning after pill 💊


4. Combined oral contraceptives


Currently .......... is the most common pharmacologic intervention for prevention of pregnancy

Interference with ovulation

About sequential pills 💊 : consists of? taken? Success rate is? A.E

Estrogen taken as Estradiol for 14 - 16 days, and progesterone taken for 5-6 days.. Success rate is 80-90% , A.E - risk of endometrial cancer

About mini pills 💊 - also called? consists of? Unpopular b/c? Taken? MOA?

POP progesterone only pills.. Consists of progesterone pills alone.. Unpopular Because it has variable effects on both LH & FSH.. Taken continuously.


MOA - alteration of cervical mucus & prevention of implantation. Uses --


a) contraceptives..


b) primarily to treat menstrual disorders


A. E


Known to make the menstrual cycle irregular with a possibility of pregnancy. i.e irregular bleeding is common..

Primary use of POP

Pop-up progesterone only pills - primarily to treat menstrual disorders

About post coital contraception - also called?

Also called morning after pill

About post coital contraception - also called? Reduces pregnancy probability to? Egs of available preparations

Morning after pill - to 0.2-3%, available preparations -


Orally administered LEVONORGESTREL, alone or + oestrogen taken within 72 hrs of unprotected intercourse and repeated 12 hrs later Egs


1. High doses of progestin i.e 0.75 mg of levonorgestrel


2. High doses of estrogen i.e 100 micrograms of ethinylestradiol + progestin ( 0.5 mg of levonorgestrel)


3. A newer progestin only preparation consisting of a one time dose of 1.5 mg levonorgestrel


4. A single dose of mifepristone


5. However the insertion of an intrauterine device (IUD) is more effective than the hormonal pills method and is effective up to 5 days after the intercourse.. This is unlike the hormonal pill that are effective preferably within 72 hours


Hormonal Vs IUD

IUD is more effective than the hormonal pills method and is effective up to 5 days after the intercourse.. This is unlike the hormonal pill that are effective preferably within 72 hours

About combined oral contraceptives - define, list the estrogen& progesterone components , the 3rd generation progesterone are?

Are very effective contraceptives which combine the use estrogen and progesterone in various compositions ..


Oestrogen components


1. Ethinylestradiol ( in most, 2 generation pill)


2. Menstranol


Progesterone components


1. Norethisterone


2. Levonorgestrel


3. Ethynodiol


4. Desogestrel ( 3rd generation)


5. Gestodene ( 3rd generation) ..


The 3rd generation progesterone are more potent and have less androgenic action + less changes in Lipoprotein metabolism + higher risk of thromboembolism..

About the 3rd generation progesterone

Desogestrel, Gestodene


The 3rd generation progesterone are more potent and have less androgenic action + less changes in Lipoprotein metabolism + higher risk of thromboembolism.. Other progesterone - Norethisterone, levonorgestrel, Ethynodiol

About monophasic combination

Contain a CONSTANT dose of estrogen and progestins , given over 21 DAYS & a 7 days of placebo ..

Biphasic and triphasic contraceptives were created to?

Where created to closely mimic the physiologic concentration of progestins and to decease side effects by lowering the overall dose

MOA of oestrogen and progesterone in combined oral contraceptives

Oestrogen - inhibits the secretion of FSH via NFB on the anterior pituitary, thus suppressing ovarian follicular development


Progesterone inhibits LH, thus preventing ovulation, it also thicken the cervical mucus making it less suitable for sperm passage..


The overall effect is ovulation inhibition...


Estrogen and progesterone act in concert to alter the endometrium thereby discouraging / preventing implantation

Common side effects of OCs

1. N, V


2. Breast tenderness


3. Water retention and weight gain


4. Flushing , dizziness, depression or irritability


5. Skin changes ( acne and / or increased pigmentation


6. Amenorrhoea of variable duration on cessation of drugs


Less frequent but more serious side effects


7. Increased risk of thromboembolic episode, hepatic adenoma


8. Haemorrhagic stroke and MI


9. endometrial cancer


Smoking increases the risk of MI 5 folds in women over 30 years

Other pharmacological effects of OCs

EFFECTS on


1. On CVS


2. CNS


3. Endocrine functions


4. Blood


5. Lipid metabolism


6. Liver


List forms of hormonal contraceptives

1. Estrogen and progesterone


2. Transdermal patch


3. Vaginal rings


4. Injectable progestins


5. Progestins intra uterine device


6. Progestin implants


About Transdermal patch - contains? How to use?

Contains ethinylestradiol and the progestin, norelgestromin ..


How to use - one contraceptive patch is applied each week for 3 weeks to the abdomen, upper torso or buttocks. No patch is worn during the 4th week & withdrawal bleeding occurs. Same MOA, c/i and A.E

About vaginal rings

Is an additional contraceptive option.. Contain ethinyl estradiol and etonogestrel.. The ring is inserted into the vagina and left in place for 3 weeks and then removed.. No ring is used during the fourth week..

MDPA means?

MeDroxyProgesterone Acetate.. Medroxyprogesterone acetate

About injectable progestin - contains?

Medroxyprogesterone acetate is an Injectable contraceptive administered 3 monthly, IM and subcutaneous, weight gain is the most common A.E. also Amenorrhoea, increased predisposition to osteoporosis / fracture so don't use for more than 2 yrs except pt is intolerant to other options

Amenorrhoea is an A.E of injectables progestins, why is it experienced ? List other A.E?

Is usually experienced b/c of the high sustained progestin level & return to fertility maybe delayed for several months following discontinuation. Other side effects of medroxyprogesterone acetate - weight gain ( is the most common), osteoporosis / fracture

About progestins intra uterine device ,define, c/i

It is a levorgestrel releasing intra uterine device system that offers a highly effective method of contraception for 3-5 years depending on the system.


C/i in pt with :


1. PID


2. hx of ectopic pregnancy

About progestin implants - about, ROA, use, advantage, A.E -

Is a subdermal implant containing etonogestrel, can offer long term contraception for ≈ 3 years. A 4 CM capsule placed subdermally in the inner aspect of the upper arm..


Advantage -


1. pt compliance does not affect this method


2. Effectiveness is comparable to sterilization. Highly effective.


Reversal is prompt upon surgical removal...


A. E -


Irregular menstrual bleeding and headaches

About Aromatase inhibitor - recall what Aromatase is? Egs,

Aromatase are enzymes that convert androstenedione and testosterone to estrogen..


1. Letrozole


2. Anastrazole


MOA-Act by blocking Aromatase enzyme so


... Dose - 2.5 - 5 mg / daily on days 2,3,4, & 5 ...


Virtually - no side effects...


Potential of teratogenicity gas limited it's use despite its numerous advantage over Clomiphene..


About metformin

Is an oral biguanide, also an insulin sensitizer.


MOA - reduces insulin secretion and resistance, followed by a reduction in ovarian and androgen production. Metformin doesn't cause hypoglycemia in normal subjects..


Used in PCOS or as a present treatment and Co treatment with Clomiphene citrate.


Dose - 1500 - 2500 mg / day.


GIT side effects are seen in 15 - 20 % of patients

Dopamine agonists aa fertility agents - list Egs

1. Bromocriptine


2. Carbegoline


3. Other ergoline derivatives are


a) pergolide


b) lysuride


c) terguride


d) metergoline


4. Quinagoline


The Dopamine agonists are only useful in infertility due to

1. Hyperprolactinemia


2.

About exemestance - discuss it i.e

Is a steroid molecule, irreversible inhibitor of Aromatase.


Also approves for use in women with advanced breast cancer

About fadrozole

Non-steriodal ( triazole), inhibitor of Aromatase enzyme. Orally active, new agent.. As effective as tamoxifen

List other Aromatase inhibitors. State the general uses of these drugs

1. Exemestance


2. Fadrozole


3. Anastrazole


4. Letrozole ...


1. Treatment of breast cancer


2. Useful adjuncts to androgen antagonist in the treatment of precocious puberty


3. Or as primary treatment in excessive Aromatase syndrome


About fertility agents - definition, Egs

Are those agents that can be used to increase the chances of conception in a woman especially in those that are either sub fertile or infertile. Also uses in fertile women who want to achieve multiple pregnancies . Mostly used to correct anovulation.


Egs:


1. Clomiphene citrate


2. Tamoxifen


3. Aromatase inhibitor


4. Metformin


5. Dopamine agonists


6. Gonadotrophins

DC MAT

Effects of estrogen and progesterone (OC) on lipid metabolism

1. Oestrogen can increase serum TGs and free and esterified cholesterol...


2. Also increased PL and HDL , but LDL are usually decreased.


higher doses i.e 100 mg ( Menstranol, ethinylestradiol) have marked effect than smaller does i.e 50 mg...


Progesterone ( esp the 19-nortestosterone derivative) are antagonistic to these effect of estrogen.. Preparation of small amt of estrogen and progestins may slightly decrease TGs and HDL.


OCs can increase the level of LDL & decrease the HDL predisposing to atheroma

About Clomiphene citrate

Dose is btw 50 - 150 mg, for 5 days starting from menstrual day, 2,3,4, or 5...


A. E


1. Hot flushes


2. Visual disturbance


3. Abdominal distention


4. Ovarian hyper stimulation / cysts


5. Multiple pregnancies


About tamoxifen

It is a SERM. dose is 20- 60 mg, daily for 5 days starting from day 2,3,4 or 5..