Progestogens, GNRH, HRT, TXA, MFA Flashcards

1
Q

Desogestrel drug class

Clinical Indications?

A

Progestogen

WOCBAs; hormonal contraception in women who require highly effective reversible contraception
HRT in women with early menopause

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2
Q

Desogestrel MOA

Elimination

A
Luteinising hormone (LH) and follicle-stimulating hormone (FSH) control
ovulation and ovarian production of oestrogen and progesterone

Oestrogen and progesterone exert predominantly negative feedback on LH and FSH release. In hormonal contraception, desogestrel is given to
suppress LH/FSH release and hence ovulation.

Changes in cervical mucus
Anovulation (97% Desogestrel, 60% traditional POP)
Endometrial changes inhibit implantation
Cilia in fallopian tube slow passage of ovum

Renal excretion

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3
Q

Side effects of Desogestrel ?

A
Irregular bleeding and mood changes 
Progestogens DO NOT increase the risk of VTE or CVD
Breast abnormalities 
Headache 
Decreased libido 
Nausea
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4
Q

Contraindications/ cautions of Desogestrel

A

Pts with acute porphyrias

Pts with ongoing breast cancer

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5
Q

Important interactions of Desogestrel

A

Concurrent use of cytochrome P450 inducers e.g. rifampicin may reduce efficacy

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6
Q

Route and dose of Desogestrel

A

WOCBAs: 75mg QD, taken at the same time each day
START: Day 1 of the cycle and used continuously
MISSED PILL: 12 hours or more

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7
Q

Explain Desogestrel instructions to patient and what to do in case of a missed pill

A

If not taken within 3 hours of normal time (e.g. normally take at 8am and not taken by 11am) then take another pill ASAP
Need additional cover (condoms) for 48 hours
If vomiting occurs within 2 hours – another pill should be taken ASAP
Not great for people with compliance issues – combined better as longer window

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8
Q

Leuprorelin drug class and clinical indications

A

GNRH analogue

Prostate cancer
Endometriosis
Reduction of uterine fibroids/ bleeding before surgery
Preservation of ovarian function

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9
Q

Leuprorelin MOA

Elimination

A

It works by decreasing gonadotropin and therefore decreasing testosterone and estradiol

Renal elimination

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10
Q

SEs of Leuprorelin?

A
Hot flushes 
Mood swings 
Insomnia 
Headaches 
Pain at the site of injection/ injection site necrosis  
Can cause QT prolongation
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11
Q

Contraindications/ cautions of Leuprorelin?

A

Undiagnosed vaginal bleeding
When used for endometriosis use to a max of 6 months- do not repeat

Caution: DM, FHx osteoporosis, risk of SCC in men with prostate cancer

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12
Q

Important interactions of leuprorelin

A

yet to find out

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13
Q

Route and dose of Leuprorelin

A

Endometriosis: SC/ IM: 3.75mg every month for a max of 6 months. Start during first 5 days of menstrual cycle
Uterine fibroids: SC/IM: 3.75mg every month

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14
Q

What is hormone replacement therapy?

This drug made using patient.info

A

HRT contains oestrogen: replaces the oestrogen that the ovaries no longer make after menopause

Oestrogen on it’s own increases thickness of the endometrium hence why a progestogen hormone is taken too. Progesterone needs to be given to prevent endometrial hyperplasia and endometrial cancer secondary to unopposed oestrogen

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15
Q

Describe the monthly cyclical HRT

Who is it indicated for?

A

Oestrogen taken every day but progestogen added in for 14 days of each 28 day cycle treatment. Light period occurs every 28 days

Indicated for women who have menopausal symptoms but are still having regular periods

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16
Q

Describe the continuous combined HRT

When is it indicated?

A

Oestrogen and progestogen pill in one every day. May cause irregular bleeding in the first 3- 6 months but usually stops

Indicated for:

  • Women who have been taking cyclical combined HRT for at least 1 year
  • Women who have had their last period one year ago
  • Postmenopausal women with a uterus
17
Q

Which type of HRT is indicated for the following?

Hysterectomy?
IUS for contraception
Mainly genital symptoms e.g. vaginal dryness or bladder symptoms

A

Hysterectomy: HRT with oestrogen only: The progestogen is only added in to other types of HRT so that the lining of the womb does not build up and increase your risk of developing cancer of the womb. So, if your womb has been totally removed, progestogen is not needed.

IUS: already contains enough progestogen to stop the lining of your womb from building up: so oestrogen only

Genital symptoms: may choose to try some vaginal oestrogen cream or a pessary to help your symptoms. This alone may be enough to relieve symptoms in some women who would prefer this option or who cannot take other forms of HRT for some reason

18
Q

Non hormonal treatments for HRT

A

Lifestyle changes such as improving the diet, exercise, weight loss, smoking cessation, reducing alcohol, reducing caffeine and reducing stress

Cognitive behavioural therapy (CBT)

Clonidine, which is an agonist of alpha-adrenergic and imidazoline receptors

SSRI antidepressants (e.g. fluoxetine)

Venlafaxine, which is a selective serotonin-norepinephrine reuptake inhibitor (SNRI)

Gabapentin

19
Q

Tell me a about clonidine:

Drug class 
MOA
Indications 
Side effects 
Dose
A

Alpha-2 adrenergic receptor and imidazoline agonist

Lowers BP, reduces HR- can be used as antihypertensive medication. Can be helpful for vasomotor symptoms and hot flushes
Dry mouth, headaches, dizziness and fatigue
50mgs BID, 2 weeks initially

20
Q

Clinical indications for HRT generally speaking

A

Replacing hormones in premature ovarian insufficiency, even without symptoms
Reducing vasomotor symptoms such as hot flushes and night sweats
Improving symptoms such as low mood, decreased libido, poor sleep and joint pain
Reducing risk of osteoporosis in women under 60 years

21
Q

Benefits of HRT

A

Improved vasomotor and other symptoms of menopause (including mood, urogenital and joint symptoms)
Improved quality of life
Reduced the risk of osteoporosis and fractures

22
Q

Risks of HRT

A

Note: in women under 60 yo benefits generally outweigh the risk

Increased risk of breast cancer (particularly combined HRT – oestrogen-only HRT has a lower risk)
Increased risk of endometrial cancer
Increased risk of venous thromboembolism (2 – 3 times the background risk)
Increased risk of stroke and coronary artery disease with long term use in older women
The evidence is inconclusive about ovarian cancer, and if there is an increase in risk, it is minimal

23
Q

Contraindications to HRT

A
Undiagnosed abnormal bleeding
Endometrial hyperplasia or cancer
Breast cancer
Uncontrolled hypertension
Venous thromboembolism
Liver disease
Active angina or myocardial infarction
Pregnancy