Progestogens, GNRH, HRT, TXA, MFA Flashcards
Desogestrel drug class
Clinical Indications?
Progestogen
WOCBAs; hormonal contraception in women who require highly effective reversible contraception
HRT in women with early menopause
Desogestrel MOA
Elimination
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
Side effects of Desogestrel ?
Irregular bleeding and mood changes Progestogens DO NOT increase the risk of VTE or CVD Breast abnormalities Headache Decreased libido Nausea
Contraindications/ cautions of Desogestrel
Pts with acute porphyrias
Pts with ongoing breast cancer
Important interactions of Desogestrel
Concurrent use of cytochrome P450 inducers e.g. rifampicin may reduce efficacy
Route and dose of Desogestrel
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
Explain Desogestrel instructions to patient and what to do in case of a missed pill
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
Leuprorelin drug class and clinical indications
GNRH analogue
Prostate cancer
Endometriosis
Reduction of uterine fibroids/ bleeding before surgery
Preservation of ovarian function
Leuprorelin MOA
Elimination
It works by decreasing gonadotropin and therefore decreasing testosterone and estradiol
Renal elimination
SEs of Leuprorelin?
Hot flushes Mood swings Insomnia Headaches Pain at the site of injection/ injection site necrosis Can cause QT prolongation
Contraindications/ cautions of Leuprorelin?
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
Important interactions of leuprorelin
yet to find out
Route and dose of Leuprorelin
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
What is hormone replacement therapy?
This drug made using patient.info
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
Describe the monthly cyclical HRT
Who is it indicated for?
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
Describe the continuous combined HRT
When is it indicated?
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
Which type of HRT is indicated for the following?
Hysterectomy?
IUS for contraception
Mainly genital symptoms e.g. vaginal dryness or bladder symptoms
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
Non hormonal treatments for HRT
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
Tell me a about clonidine:
Drug class MOA Indications Side effects Dose
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
Clinical indications for HRT generally speaking
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
Benefits of HRT
Improved vasomotor and other symptoms of menopause (including mood, urogenital and joint symptoms)
Improved quality of life
Reduced the risk of osteoporosis and fractures
Risks of HRT
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
Contraindications to HRT
Undiagnosed abnormal bleeding Endometrial hyperplasia or cancer Breast cancer Uncontrolled hypertension Venous thromboembolism Liver disease Active angina or myocardial infarction Pregnancy
