Contraceptives Flashcards
Gonadotrophin-releasing hormone (GnRH) released from ——
Hypothalamus
What hormoes are released during the Luteal phase
GnRH stimulates the Anterior pituitary which –> releases FSH –> Grafffian follicle growth -> Secretes Osterogen–> release of egg
What hormones are released during the Follicular phase ?
GnRH stimulates the Anterior Pituitary –> release LH –> ruptured follicle proliferates and becomes coprus leuteum –> secretes Progesterone
Function of Progesteron release during the luteal phase?
Induce fertilization
(by making cervivak mucus more viscous, less alkaline etc for the sperm)
Note: Progesteorne release stops if no fertilization happens -> mensturation
If Fertilization takes place —- keeps being released, which prevents further ovulation via the hypo. and Anterior pituitary effects
Progesterone
Oral Contraception methods used ?
1) Combo pill (Estrogen/Progesteron components)
2) Progestogens-only
1st generation Combo pill
Ethinylestradiol; mestranol
* not used anymore due to high concentrations of ER and Progesterone
2nd generation COCP
* COCP : combination oral contraceptive pill
1) Oestrogen component: lower dose
+
2) Progesterone: Testosterone derivatives
* Norethisterone, levonorgestrel, ethynodiol
*FIRST LINE*
Progesteron: Testosterone derivates used in Oral contraceptives , used in 2nd gen. COCP
Norethisterone,
levonorgestrel,
ethynodiol
3rd generation COCP
- Oestrogen component: lower dose
PLUS - Progesterone component—desogestrel or gestodene
CU of 3rd Generation COCP
- If 2nd gen. are not tolerated (break-through bleeding)
- given to women w/ acne, depression
CU of 2nd gen COCP
1st line oral contraception method
AE of 2nd generation COCP
- some androgenic activiy
AE of 3rd generation COCP
- Increased risk of Thromboembolism
Adv. of 3rd generation COCP over 2nd?
- more potent
- less androgenic action
- Less change in lipoprotein metabolism
BUT- has a greater risk of thromboembolism
how should the combo pill be taken?
Taken for 21 consecutive days, Followed by 7 pill-free days (mensturation)
MoA of Ostrogen in the Combination oral contraception pill
inhibits secretion of FSH via negative feedback on
anterior pituitary
–> Suppresses development of ovarian follicle
MoA of Progesteron in the Combiantion Oral Contraception pill
Inhibits secretion of LH –> Prevents ovulation -> Thickens cervical mucus: affects sperm passage
AE of COCP
- Weight gain
- Fluid retention or anabolic effects
- Nausea/vomiting
- Breast tenderness
- Flushing (ER is a vasodilator)
- Dizziness
- Depression (mostly 2nd gen)
- Irritability
- Skin changes
- Acne (2nd gen)
- Increase in pigmentation (2nd gen)
- Amenorrhea upon cessation
More sever AE of COCP
1) Cardiovascular risk
- Risk of VTE (3rd gen more than 2nd gen)
- Increased risk of MI/stroke (patients w/ risk factors are more suceptible i.e. >35 yrs, smoking, obesity)
2) Can cause increase in Bp
3) Cancer risk
- reduces risk of ovarian and endometrial cancer but,
- increases risk of Cervical and breast cancer
4) Irregular periods
**Safe in most women**
* risk is small
Contraindications of COCP
- Smokers >35 years old
- CV disease risk factors (CAD,VTE, stroke)
- Migraine
- ER-positive breast cancer
Note: more than one risk factor must be present for contraindication
Pharmacokinetic interactions of COCP
1) Metabolized by CYP450 enzymes
2) Inducers may lead to contraceptive failure
3) Abx may interfere with enterohepatic circulation of estrogen (and progesterone)
- women taking combo pill w/ Abx are adviced to use back up methods
Components of the Progestogen-only pill
Norethisterone, levonorgestrel, ethynodiol
How are Progestogen-only pill used?
taken daily w/o interruption
* if one missed -> conception is likely
MoA Progestogen-only pill?
- Primarily exerts effects on the cervical mucus
-> Inhospitable to sperm - Hinders implantation
CU of Progestogen-Only pill
- Alternative to COCP if estrogen is contraindicated or increased blood pressure
- May be used during breastfeeding
AE of the Progestogen-only pill
1) Less reliable than COCP
(Missing a dose may result in conception)
2) Disturbances of menstruation are common
(e.g. irregular bleeding)
3) Lack of reliable long-term safety data
Long-acting Progestogen-only contraception
1) Medroxyprogesterone
(Progesterone derivative)
2) Levonorgestrel
3) IUD- Impregnated intrauterine device
Adm. of Medroxyprogesterone
IM administration (every 12 weeks)
* Long-acting progestogen-only contraception
AE of Medroxyprogesterone
1) Safe and effective
2) Menstrual irregularities are common
3) Infertility may persist many months after treatment cessation
Adm of Levonorgestrel
SC implantation
* long-acting progestogen-only contraception
AE of LONG-Acting Progestogen Contraceptives
- Weak androgenic effects
- Acne
- Fluid retention
- Weight change
- Depression
- Change in libido
- Breast discomfort
- Premenstrual symptoms
- Irregular menstrual cycles
- Breakthrough bleeding
- Increased incidence of VTE
Contraindications of Progestin contraceptives
1) Undiagnosed vaginal bleeding
2) Liver disease
3) Breast cancer
4) IUD:
- Severe uterine distortion
- Active pelvic infection
- Unexplained abnormal uterine bleeding
If a women wants to take long-acting progesteron contraceptives but has an increased risk of VTE. What will you perscribe her?
Copper IUD or back up methods (Condoms)
How does Levonorgestrel and IUD work?
Release content (progestogen components) up to 5 years
What makes hormonal IUDs better than copper containing devises?
IUDs reduce menstural bleeding comapred to copper (which cause increased unwanted bleeding)
AE of Levonorgestrel
Irregular headache and bleeding (Common)
which long-acting Progestogen-only contraceptive avoids first-pass metabolism?
Levonorgestrel
CU of copper IUDs
an Emergency contraception method (work up to 5 days after intercourse)
Emergency conceptions methods
1) Oral adm. of Levonorgestrol alone or w/ ER –> effective within 72 hrs of intercourse
2) Copper IUD insertion –> work up to 5 DAYS after intercourse
3) Ulipristal (presecribed medication)
Selective progesterin receptor modulator
Ulipristal
(emergency contraception)
AE of Oral adm of Levonorgestrel
Nausea and vomiting are common
(take anti-emetic to reduce that)
how does Hormone replacemnt therapy work?
Cyclic or continuous administration of low doses of one or more oestrogens, with or without a progestogen
Estrogen components used in the HRT
Estradiol, estriol
Progesterone components used in HRT
Norethindone,
Norgestimate,
Levonogestrel,
Norethisterone
Routes of Adm of Estrogen and progesterone components in HRT
- Orally
- Transdermal patch
- Subcutaneous
most effective HRT?
ESTROGEN
Clinical uses of Osterogen in HRT
Relieves menopause symptoms:
1) flushing
2) vaginal dryness
3) prevention and tx of Osteoporosis
CU of Progesteron in HRT
Combined w/ Oestrogen for Osterogen HRT in women w/ an intact uterus, to prevent endometrail hyperplasia and carcinoma
AE of Osterogen replacement therapy
- Cyclical withdrawal bleeding
- Increased risk of endometrial cancer if oestrogen is given unopposed by progestogen
- Increased risk of breast cancer
- Increased risk of venous thromboembolism
- Increased cardiovascular risk
- Adverse effects related to progestogen
Testosterone is synthesized in ——– and ——– in women
Testosterone is synthesized in coprus luteum and adrenal cortex in women
CU of Androgen prepeartions
1) Hormone replacement in male hypogonadism due to pituitary or testicular
disease
2) Female hyposexuality following ovariectomy
routes of adm of androgen preperations
- Subcutaneous
- Transdermal patches
- Intramuscular depot
- Oral
AE of Androgen preperations
- Eventual decrease of gonadotrophin release
- Resultant infertility
- Gonadal atrophy
- Salt and water retention–> Leading to oedema
- Adenocarcinoma of the liver
- Impaired growth in children
- Premature fusion of epiphyses
- Acne
- Increased LDL
- Decreased HDL
- Masculinisation in females
Anabolic steroids
Nandrolone, methyltestosterone
CU of Nandrolone, methyltestosterone
May be effective in treatment of muscle wasting associated with AIDS
AE of Anabolic steroids
Same as androgens Plus
- Cholestatic jaundice
- Liver tumours
- Increased risk of coronary heart disease
MoA of Anabolic steroids
Increase protein synthesis and muscle development
