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Systemic pharma- Reproductive > Contraceptives > Flashcards

Contraceptives Flashcards

1
Q

Gonadotrophin-releasing hormone (GnRH) released from ——

A

Hypothalamus

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2
Q

What hormoes are released during the Luteal phase

A

GnRH stimulates the Anterior pituitary which –> releases FSH –> Grafffian follicle growth -> Secretes Osterogen–> release of egg

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3
Q

What hormones are released during the Follicular phase ?

A

GnRH stimulates the Anterior Pituitary –> release LH –> ruptured follicle proliferates and becomes coprus leuteum –> secretes Progesterone

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4
Q

Function of Progesteron release during the luteal phase?

A

Induce fertilization
(by making cervivak mucus more viscous, less alkaline etc for the sperm)

Note: Progesteorne release stops if no fertilization happens -> mensturation

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5
Q

If Fertilization takes place —- keeps being released, which prevents further ovulation via the hypo. and Anterior pituitary effects

A

Progesterone

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6
Q

Oral Contraception methods used ?

A

1) Combo pill (Estrogen/Progesteron components)
2) Progestogens-only

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7
Q

1st generation Combo pill

A

Ethinylestradiol; mestranol
* not used anymore due to high concentrations of ER and Progesterone

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8
Q

2nd generation COCP

* COCP : combination oral contraceptive pill

A

1) Oestrogen component: lower dose
+
2) Progesterone: Testosterone derivatives
* Norethisterone, levonorgestrel, ethynodiol

                *FIRST LINE*
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9
Q

Progesteron: Testosterone derivates used in Oral contraceptives , used in 2nd gen. COCP

A

Norethisterone,
levonorgestrel,
ethynodiol

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10
Q

3rd generation COCP

A
  • Oestrogen component: lower dose
    PLUS
  • Progesterone component—desogestrel or gestodene
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11
Q

CU of 3rd Generation COCP

A
  • If 2nd gen. are not tolerated (break-through bleeding)
  • given to women w/ acne, depression
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12
Q

CU of 2nd gen COCP

A

1st line oral contraception method

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13
Q

AE of 2nd generation COCP

A
  • some androgenic activiy
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14
Q

AE of 3rd generation COCP

A
  • Increased risk of Thromboembolism
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15
Q

Adv. of 3rd generation COCP over 2nd?

A
  • more potent
  • less androgenic action
  • Less change in lipoprotein metabolism

BUT- has a greater risk of thromboembolism

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16
Q

how should the combo pill be taken?

A

Taken for 21 consecutive days, Followed by 7 pill-free days (mensturation)

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17
Q

MoA of Ostrogen in the Combination oral contraception pill

A

inhibits secretion of FSH via negative feedback on
anterior pituitary
–> Suppresses development of ovarian follicle

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18
Q

MoA of Progesteron in the Combiantion Oral Contraception pill

A

Inhibits secretion of LH –> Prevents ovulation -> Thickens cervical mucus: affects sperm passage

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19
Q

AE of COCP

A
  • 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
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20
Q

More sever AE of COCP

A

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

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21
Q

Contraindications of COCP

A
  • 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

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22
Q

Pharmacokinetic interactions of COCP

A

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
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23
Q

Components of the Progestogen-only pill

A

Norethisterone, levonorgestrel, ethynodiol

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24
Q

How are Progestogen-only pill used?

A

taken daily w/o interruption
* if one missed -> conception is likely

25
Q

MoA Progestogen-only pill?

A
  • Primarily exerts effects on the cervical mucus
    -> Inhospitable to sperm
  • Hinders implantation
26
Q

CU of Progestogen-Only pill

A
  • Alternative to COCP if estrogen is contraindicated or increased blood pressure
  • May be used during breastfeeding
27
Q

AE of the Progestogen-only pill

A

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

28
Q

Long-acting Progestogen-only contraception

A

1) Medroxyprogesterone
(Progesterone derivative)
2) Levonorgestrel
3) IUD- Impregnated intrauterine device

29
Q

Adm. of Medroxyprogesterone

A

IM administration (every 12 weeks)

* Long-acting progestogen-only contraception

30
Q

AE of Medroxyprogesterone

A

1) Safe and effective
2) Menstrual irregularities are common
3) Infertility may persist many months after treatment cessation

31
Q

Adm of Levonorgestrel

A

SC implantation

* long-acting progestogen-only contraception

32
Q

AE of LONG-Acting Progestogen Contraceptives

A
  • 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
33
Q

Contraindications of Progestin contraceptives

A

1) Undiagnosed vaginal bleeding
2) Liver disease
3) Breast cancer
4) IUD:
- Severe uterine distortion
- Active pelvic infection
- Unexplained abnormal uterine bleeding

34
Q

If a women wants to take long-acting progesteron contraceptives but has an increased risk of VTE. What will you perscribe her?

A

Copper IUD or back up methods (Condoms)

35
Q

How does Levonorgestrel and IUD work?

A

Release content (progestogen components) up to 5 years

36
Q

What makes hormonal IUDs better than copper containing devises?

A

IUDs reduce menstural bleeding comapred to copper (which cause increased unwanted bleeding)

37
Q

AE of Levonorgestrel

A

Irregular headache and bleeding (Common)

38
Q

which long-acting Progestogen-only contraceptive avoids first-pass metabolism?

A

Levonorgestrel

39
Q

CU of copper IUDs

A

an Emergency contraception method (work up to 5 days after intercourse)

40
Q

Emergency conceptions methods

A

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)

41
Q

Selective progesterin receptor modulator

A

Ulipristal
(emergency contraception)

42
Q

AE of Oral adm of Levonorgestrel

A

Nausea and vomiting are common
(take anti-emetic to reduce that)

43
Q

how does Hormone replacemnt therapy work?

A

Cyclic or continuous administration of low doses of one or more oestrogens, with or without a progestogen

44
Q

Estrogen components used in the HRT

A

Estradiol, estriol

45
Q

Progesterone components used in HRT

A

Norethindone,
Norgestimate,
Levonogestrel,
Norethisterone

46
Q

Routes of Adm of Estrogen and progesterone components in HRT

A
  • Orally
  • Transdermal patch
  • Subcutaneous
47
Q

most effective HRT?

A

ESTROGEN

48
Q

Clinical uses of Osterogen in HRT

A

Relieves menopause symptoms:
1) flushing
2) vaginal dryness
3) prevention and tx of Osteoporosis

49
Q

CU of Progesteron in HRT

A

Combined w/ Oestrogen for Osterogen HRT in women w/ an intact uterus, to prevent endometrail hyperplasia and carcinoma

50
Q

AE of Osterogen replacement therapy

A
  • 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
51
Q

Testosterone is synthesized in ——– and ——– in women

A

Testosterone is synthesized in coprus luteum and adrenal cortex in women

52
Q

CU of Androgen prepeartions

A

1) Hormone replacement in male hypogonadism due to pituitary or testicular
disease
2) Female hyposexuality following ovariectomy

53
Q

routes of adm of androgen preperations

A
  • Subcutaneous
  • Transdermal patches
  • Intramuscular depot
  • Oral
54
Q

AE of Androgen preperations

A
  • 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
55
Q

Anabolic steroids

A

Nandrolone, methyltestosterone

56
Q

CU of Nandrolone, methyltestosterone

A

May be effective in treatment of muscle wasting associated with AIDS

57
Q

AE of Anabolic steroids

A

Same as androgens Plus
- Cholestatic jaundice
- Liver tumours
- Increased risk of coronary heart disease

58
Q

MoA of Anabolic steroids

A

Increase protein synthesis and muscle development

Systemic pharma- Reproductive (3 decks)

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