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Clinical Pharmacology, Therapeutics & Intro to Prescribing > Lecture 9 – Reproductive and post reproductive health > Flashcards

Lecture 9 – Reproductive and post reproductive health Flashcards

1
Q

drug groups which target reproductive and post reproductive health

A
  • Sex steroid hormones
  • Inhibitors and antagonists
  • Mixed agonists/antagonists
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2
Q

sex steroid hormones

A
  • Oestrogens
  • Progestagens
  • androgens
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3
Q

Inhibitors and antagonists

A
  • RU486
  • Finasteride
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4
Q

Mixed agonists/antagonists

A

Selective oestrogen receptor modulators (SERMs) and selective progesterone receptor modulators (SPRMs)

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5
Q

sex steroid hormones are synthesised from

A

cholesterol

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6
Q

sex steroid synthesis

A
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7
Q

Steroid hormone receptors

A
  • Classic nuclear receptor
  • Exert effects through gene transcription (effectively transcription factors)
  • But also a membrane receptor for oestrogen
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8
Q

major effects of oestradiol

A

stimulates growth of the endometriumna and breast

stimulates production of progesterone (PR)

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9
Q

major effects of progesterone

A

stimulates growth of the endometrium and breast

maintains pregnancy

inhibits production of oestrogen

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10
Q

major effect of testosterone

A

In men, it’s thought to regulate sex drive (libido), bone mass, fat distribution, muscle mass and strength, and the production of red blood cells and sperm. A small amount of circulating testosterone is converted to estradiol, a form of estroge

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11
Q

Recap of female reproductive endocrinology:

The menstrual cycle

A
  • 28 day cycle
    • Luteal phase always 14 days
  • Ovulation occurs due to LH surge
  • Oestrogen and progesterone have differing effects on endometrial tissue and on cervical mucus
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12
Q

oestrogen effect on cervical mucus and uterus

A
  • thin cervical mucus- allows fertilisation
  • endometrial and myometrial thickening
  • glands are straight or moderately coiled
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13
Q

progestrone effect on cervical mucus and uterus

A
  • Maintains endometrium and myometrium
  • Causes glands to become highly coiled and secretory
  • thick cervical mucus- act to block further sperm transport
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14
Q

Oestrogen and progesterone together

A

produce suppression of the HPO axis i.e. reduced production of LH and FSH from the AP

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15
Q

actions of oestrogen when used as a drug

A
  • Mild anabolic
  • Sodium and water retention
  • Raises HDL, lowers LDL
  • Decrease bone resorption
  • Impaired glucose tolerance
  • Increase blood coagulability
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16
Q

side effects of oestrogen when used as a drug

A
  • Breast tenderness
  • Nausea, vomiting
  • Water retention
  • Increased blood coag
  • Thromboembolism
  • Impaired glucose tolerance
  • Endometrial hyperplasia and cancer
  • Ovarian metaplasia and cancer
  • Breast hyperplasia and cancer
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17
Q

actions of progesterone when used as a drug

A
  • Secretory endometrium
  • Anabolic
  • Increases bone mineral density
  • Fluid retention
  • Mood changes
  • Maintains pregnancy
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18
Q

side effect of progesterone when used as a drug

A
  • Weight gain
  • Fluid retention
  • Anabolic
  • Acne
  • Nausea/vomiting
  • Irritability
  • Depression, PMS
  • Lack of concentration
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19
Q

action of testosterone when used as a drug

A
  • Male secondary sex characteristics
  • Anabolic
  • Acne
  • Voice change
  • Increased aggression
  • Metabolic
    • Adverse effects on lipid profiles particularly the HDL-c/LDL- C ration (increased risk of atherosclerotic disease in males)
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20
Q

Hormonal contraception- using steroid drugs to prevent pregnancy

A

Interruption of HPG axis..

  • Endometrial and cervical mucus effects
  • Inhibition of ovulation
  • can have short acting reversible contraceptives and LARCs
  • Routes of admin
    • Oral
    • Nasal
    • Transdermal
    • implants
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21
Q

types of hormonal contril

A
  • Combined oestrogen and progesterone
    • COCP
    • patch
    • ring
  • progesterone only pill (POP)​
  • LARC
    • progesterone depot and implant
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22
Q

uses of oestrogen as a drug

A
  • As part of hormonal birth control (COCP)
  • As part of menopausal hormone therapy
  • Transgender hormone therapy
  • Treatment of hormone sensitive cancers e.g. breast cancer and prostate
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23
Q

Pharmacokinetics of oestrogen as a drug

A
  • Natural and synthetic oestrogens well absorbed in GI tract
    • pills
  • Also readily absorbed from skin and mucous membranes
    • e.g. hormone patches
  • Metabolised in the liver
  • Excretion- in the urine as glucuronides and sulphates
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24
Q

Mechanism of action of oestrogen

A
  • Lipophilic so can pass through cell membrane without receptor
  • Bind to oestrogen receptors found within cell
  • Regulate transcription of specific genes
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24
Q
A
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25
Q

Contraindications of oestrogen

A
  • Estrogen hormone receptor sensitive malignancies including breast cancer, ovarian cancer, and endometrial cancers
  • Hypertension
  • Coronary arterial disease
  • History of thromboembolism
  • History of hypercoagulable disease (Factor V Leiden syndrome, Protein C or Protein S deficiencies and metastatic disease)
  • History of ischemic stroke
  • Migraine headaches (e.g. auras)
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26
Q

adverse drug response of oestrogen therapy

A

breast tenderness, bloating, nausea, headaches, leg cramping, and vaginal or “breakthrough” bleeding

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27
Q

drug drug interactions oestrogen

A

aromatase inhibitors, tamoxifen

st johns wort shouldnt be taken with COCP (induces CYP3A4)- reducing [plasma] conc

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28
Q

uses of progesterone as a drug

A
  • birth control
  • help restart menstrual periods that unexpectedly stopped (amenorrhea)
  • treat abnormal uterine bleeding associated with hormonal imbalance
  • symptoms of premenstrual syndrome (PMS).
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29
Q

pharmacokinetics of porgesterone

A
  • oral, intranasal, transdermal, vaginal, rectal, intramuscular, subcutaneous, and intravenous injection.
  • Injected progesterone is bound to albumin with some stored in adipose tissue
    • Long acting
  • Metabolised in liver
  • Metabolised excreted in urine conjugated to glucuronic acid
30
Q

MOA of progesterone therapy

A

The “classical” mechanism by which progesterone elicits its effects is via the progesterone receptor (PR), which, like the estrogen receptor (ER), has classically been described as a nuclear transcription factor, acting through specific progesterone response elements (PRE) within the promoter region of target genes to regulate transcription

31
Q

adverse drug reaction : progesterone

A
  • Spontaneous fetal abortion
  • Ectopic pregnancy
  • Headache
  • Breast tenderness
  • GI issues
32
Q

Contraindications of progesterone

A
  • Breast cancer, cervical cancer, endometrial cancer, endometrial hyperplasia, new primary malignancy, ovarian cancer, uterine cancer, vaginal cancer
  • Infertility
  • CVD risk
  • hypertension
  • Hepatic impairment
33
Q

names of combined pills

A

Microgynon, Rigevidon and Ovranette are combined pills

34
Q

pharmacokinetics of COCP and POP

A
  • COCP and POP contraceptives are metabolised by CYP450
35
Q

mode of action of COCP

A
  • Main action- prevent ovulation – negative feedback of oestrogen and progesterone on LH surge
  • Secondary action- reduce endometrial receptivity to implantation
    • Thickens cervical mucus
36
Q

Disadvantages of COCP

*

A
  • User dependent
  • No STI protection
  • Medication interaction
  • Contraindications
    • Raised BMI
    • Migraine and aura
    • Breast cancer
37
Q

mode of action of POP

A
  • Low dose progesterone
  • Main action – thickens cervical mucus
  • Other actions
    • Reduced cilia activity in fallopian tubes
    • Ovulation not prevented
38
Q

adverse drug response of COCP

A
  • Side effects
    • Menstrual irregularities
    • Breast tenderness
    • Mood disturbances
  • Increased risk of CV disease, stroke, VTE, breast cancer and cervical cancer
    • smoking increases risk substantially
    • also long term use
39
Q

Contraindications of COCP

A
  • Migraines
  • Cancer/ History
40
Q

Drug-drug interaction of COCP

A
  • Oral contraceptive efficacy is reduced by enzyme (CYP450) inducing drugs- increasing the production of CYP450- therefore reduced plasma drug
    • Antiepileptics such as carbamazepine or phenytoin
    • Antibiotics e.g. rifampicin and rifabutin
    • St Johns Wort
  • Soya protein products enhance oestrogen absorption and reduce its storage in adipose and muscle so reduce half-life from 15 to 7 hours
41
Q

menopause (no menstruation for 12 months)

A
  • Ovarian follicle supply depleted
  • Consequently ovarian sex steroid production stops
  • End of female reproductive capacity
  • Loss of oestrogen and progesterone leads to a range of systemic effects as symptoms of menopause
    • Results in increased FSH
42
Q

drug used to help with menopause

A

hormone replacement therapy

43
Q

uses of hormone replacement therapy

A
  • Manage symptoms of menopause
    • E.g. hot flushes/sweats
  • Osteoporosis
  • Not effective for the prevention of heart disease
44
Q

route of admin of HRT

A
  • Oral
  • Transdermal
  • Transvaginal
  • Nasal
45
Q

mode of action of HRT

A

steroid action- binds to intracellular receptors and changes transcription

46
Q

names of hormone replacement therapy

A
47
Q

Adverse drug response of HRT

A
  • Unopposed oestrogen (ERT) increases risk of developing endometrial and ovarian cancers
  • Opposed oestrogen (HRT- Oes with prog) increases risk of breast cancer
  • Increased risk of venous thromboembolism
    • Increases activated protein C resistance
    • Increased thrombin activation
    • Decreased anti-thrombin III activity
    • Decreased protein S levels
    • Decreased factor VII levels and decreased tissue factor pathway inhibitor
  • Increased risk of stroke
    • Use of oral but not transdermal oestrogen is associated with a small increase in the risk of stroke
48
Q

Contraindications of HRT

A

A history of breast cancer. *

A history of endometrial cancer. *

Porphyria.

Severe active liver disease.

Hypertriglyceridemia.

Thromboembolic disorders.

Undiagnosed vaginal bleeding.

Endometriosis.

49
Q

osteoporosis (as a result of menopause) treatment

A

Bisphosphonates (stable analogues of pyrophosphates)

50
Q

name a drug under the class Bisphosphonates (stable analogues of pyrophosphates)

A

alendronic acid

51
Q

Pharmacokinetics of bisphosphonates (alendronic acid)

A
  • Long biological half life
  • Poor gut absorption
  • Absorption affected by food (must be taken on an empty stomach)
52
Q

Uses of alendronic acid (bisphosphonates)

*

A
  • Prophylaxis and treatment of osteoporosis
  • Other uses include management of other disease involving bone
    • Paget’s disease of bone
    • malignancy
53
Q

Mechanism of action of Bisphosphonates (stable analogues of pyrophosphates)

Drug names: Alendronic acid

​

A
  • Reduce bone turnover by controlling osteoclast activity
    • Have an effect on osteoclast membrane meaning they cant bind to bone
54
Q

Adverse drug response of bisphosphonates

A
  • Upper GI effects
    • Oesophagitis (must stay seated or standing 30 mins after taking)
  • Hypocalcaemia
    • Check calcium and Vit D levels prior to initiating treatment
55
Q

2 broad classes of inhibitors and antagonists

A
  • Mifepristone (RU486)
  • Finasteride
56
Q

name a drug under the class of RU486

A

Mifepristone

57
Q

use of RU486 (mifepristone)

A

Termination of pregnancies

58
Q

MOA of RU486 (mifepristone)

A
  • Progesterone and glucocorticoid receptor antagonist
  • Therefore = anti-progesterone
    • Sensitising the myometrium to prostaglandin- induced contractions

Used for termination of pregnancy

59
Q

contraindications of RU486

A

contraindicated in patients with a confirmed or suspected ectopic pregnancy because MIFEPREX is not effective for terminating ectopic pregnancies

60
Q

finasteride uses

A

Finasteride is in a class of medications called 5-alpha reductase inhibitors.

  • Finasteride treats BPH by blocking the body’s production of a male hormone that causes the prostate to enlarge.
  • Finasteride treats male pattern hair loss by blocking the body’s production of a male hormone in the scalp that stops hair growth.
61
Q

MOA of Finasteride

A

nhibiting 5α-reductase and thus preventing DHT (more potent testosterone)production

62
Q

mixed agonists and antagonists

A

SERM- selective oestrogen receptor modulator

SPRM- selective progesterone receptor modulators

63
Q

examples of drugs under the class SERM- selective oestrogen receptor modulator

A

Drug names: Tamoxifen, Raloxifene, Clomiphene

64
Q

MOA of SERM- selective oestrogen receptor modulator

A
  • Pure agonists and pure antagonists
  • Varying effects in different tissue
65
Q

uses of clomiphene

A
  • anovulation
66
Q

mechanism of action of clomiphene

A
  • Competes with oestrogen for ER binding
  • Leads to ovulation induction through increased production of anterior pituitary hormones (LH)
67
Q

uses of tamoxifen

A

breast cancer

68
Q

Mechanism of action : tamoxifen

A
  • pro-drug
    • little affinity for ER
  • metabolised in the liver to active derivatives
    • some isoform of enzymes will not produce active derivative
    • need genotyping before commencing treatment
  • tamoxifen active metabolites compete with oestrogen for bind to ER
69
Q

Adverse drug response: tamoxifen

A

Adverse drug response

  • Acts as a SERM
    • converse effects in breast and endometrial tissue
      • in endometrium = ER agonist
      • in breast = ER antagonist
        • cell cycle arrest
70
Q

name a drug under the class Selective progesterone receptors modulators

A

Ulipristal acetate (e.g. ellaOne)

71
Q

Ulipristal acetate (e.g. ellaOne) uses

A
  • Emergency contraception
  • Uterine fibroids
72
Q

Mode of action: Selective progesterone receptors modulators

A
  • Selective progesterone receptor modulator
  • Delays ovulation
73
Q

summary

A
  • Many sex steroid pharmaceutical preparations available
  • Indicated for contraception, emergency contraception termination of pregnancy
  • In post-menopausal women main indication is for relief of vaso-motor symptoms and symptoms of genital atrophy
  • Mostly well tolerated
  • Risks associated with hormonal contraceptives low
  • ERT risks – ovarian and endometrial cancer
  • HRT – breast cancer and thromboembolism

Clinical Pharmacology, Therapeutics & Intro to Prescribing (39 decks)

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