5 - Sex Hormones Flashcards
What are three groups of drugs when considering sex hormones?
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Why do drugs based on sex hormones take a while for a response?
They are steroid hormones so act through nuclear receptors so longer response
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What are the actions and side effects of oestrogen?
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What are the actions and side effects of progesterone?
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What are the actions and side effects of testosterone?
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What are the different routes of administration for sex steroid hormones?
- Oral
- Transdermal patch
- Implants
- Nasal
- Vagina
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How are sex steroids transported in the blood?
- Transport bound to SHBG (except progesterone) and albumin
- SHBG production upregulated by oestrogens – protects against hepatic metabolism
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What are some side effects of the combined pill?
- Thromboembolic disease (higher in obese, hypertensives, smokers, long term users and over 35)
- Mood swings
- Decreased glucose tolerance
- Mood swings
- Hypertension
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How are sex hormone drugs metabolised and excreted?
- CYP450 in liver
- Metabolites are excreted in faeces and urine as glucuronides and sulphates, respectively
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What is the mechanism of action for the COCP and POP?
COCP:
- Suppression of ovulation (inhibits FSH, LH)
- Thickens cervical mucus (more viscous)
- Prevents secretory phase in endometrium (remains atrophic)
POP: (low dose)
- Thicken cervical mucous
- Atrophy endometrium
- High dose implant stops ovulation but this doesn’t
- Need constant oestrogen as progestrone receptors only present when oestrogen around so not good if woman producing low oestrogen
What are some side effects of POP?
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In the COCP, which progestins are prescribed?
- Medroxyprogesterone acetate
- Norethisterone
- Levonorgesterel
In the COCP, which oestrogens are prescribed?
ethinylestradiol
How are sex hormones synthesised?
From cholesterol
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What drug-drug interactions can occur with the POP and COCP?
Metabolised by CYP450 so the following enzyme inducing drugs can lower the drugs response:
- Antiepileptics like carbamazepine and phenytoin
- Rifampicin and rifabutin
- St John’s Wort
- Soya protein for perimenopausal symptoms can enhance oestrogen absorption and reduce its storage in adipose so half life from 15 to 7 hours