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Pharmacology > 16 The pituitary and the adrenal cortex > Flashcards

16 The pituitary and the adrenal cortex Flashcards

1
Q

16.01 HYPOTHALAMIC HORMONES

Somatostatin analogues: octreotide, lanreotide, pasireotide - actions

A

octapeptide analogues of natural somatostatin
they inhibit various endocrine, neuroendocrine, exocrine and paracrine functions

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2
Q

16.01 HYPOTHALAMIC HORMONES

Somatostatin analogues: octreotide, lanreotide, pasireotide - MOA

A

inhibit pathologically increased secretion of growth hormone (GH) and of peptides and serotonin produced within the gastro-entero-pancreatic endocrine system
octreotide also constricts splanchnic blood vessels

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3
Q

16.01 HYPOTHALAMIC HORMONES

Somatostatin analogues: octreotide, lanreotide, pasireotide - abs/distrib/elim

A

given SC
octreotide: peak action is at 2h, and the suppressant effect lasts for up to 8h

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4
Q

16.01 HYPOTHALAMIC HORMONES

Somatostatin analogues: octreotide, lanreotide, pasireotide - clinical use

A

octreotide: carcinoid, hormone-secreting tumours, acromegaly, bleeding oesophageal varices
lanreotide: thyroid tumours
pasireotide: Cushing’s syndrome when surgery is inappropriate or has been ineffective

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5
Q

16.01 HYPOTHALAMIC HORMONES

Somatostatin analogues: octreotide, lanreotide, pasireotide - adverse effects

A

pain at injection site and GI disturbances
gallstones, post-prandial hyperglycaemia
cases of hepatitis and pancreatitis have also been reported

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6
Q

16.02 HYPOTHALAMIC HORMONES

GnRH analogues: buserelin, leuprorelin, gonadorelin - actions

A

stimulate the synthesis of follicle-stimulating hormone (FSH) and luteinising hormone (LH) and their release

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7
Q

16.02 HYPOTHALAMIC HORMONES

GnRH analogues: buserelin, leuprorelin, gonadorelin - MOA

A

analogues of natural gonadotrophin-releasing hormone (gonadorelin, LHRH or GnRH)
after an initial stimulation of gonadotrophin release, it down-regulates the hypothalamic-pituitary-gonadal (HPG, also called HPO) axis such that a decrease in ovarian steroid secretion into the postmenopausal range occurs

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8
Q

16.02 HYPOTHALAMIC HORMONES

GnRH analogues: buserelin, leuprorelin, gonadorelin - abs/distrib/elim

A

given by SC injection
gonadorelin is rapidly hydrolysed in plasma and excreted in urine with a half-life of ~4 min
buserelin half-life after injection is ~80 min

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9
Q

16.02 HYPOTHALAMIC HORMONES

GnRH analogues: buserelin, leuprorelin, gonadorelin - clinical use

A

evaluation of anterior pituitary hormones
endometriosis, infertility treatment, hormone-dependent tumours

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10
Q

16.02 HYPOTHALAMIC HORMONES

GnRH analogues: buserelin, leuprorelin, gonadorelin - adverse effects

A

weight changes, mood changes, sleep disturbances, GI disturbances, dizziness
risk of skeletal fractures increases with duration of therapy (decrease in bone mass may occur)

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11
Q

16.03 ANTERIOR PITUITARY HORMONES

Prolactin inhibitors: bromocriptine, cabergoline, quinagolide - actions

A

inhibit prolactin secretion

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12
Q

16.03 ANTERIOR PITUITARY HORMONES

Prolactin inhibitors: bromocriptine, cabergoline, quinagolide - MOA

A

inhibit prolactin secretion without affecting normal levels of other pituitary hormones
bromocriptine can also reduce elevated levels of growth hormone (GH) in patients with acromegaly
these effects are due to stimulation of dopamine receptors

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13
Q

16.03 ANTERIOR PITUITARY HORMONES

Prolactin inhibitors: bromocriptine, cabergoline, quinagolide - abs/distrib/elim

A

given orally
metabolised by liver
bromocriptine peak concentrations occur after 2h

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14
Q

16.03 ANTERIOR PITUITARY HORMONES

Prolactin inhibitors: bromocriptine, cabergoline, quinagolide - clinical use

A

prolactinomas
acromegaly
infertility
hyperprolactinaemia
polycystic ovarian syndrome

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15
Q

16.03 ANTERIOR PITUITARY HORMONES

Prolactin inhibitors: bromocriptine, cabergoline, quinagolide - adverse effects

A

nausea, vomiting, dizziness, constipation, postural hypotension

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16
Q

16.04 POSTERIOR PITUITARY HORMONES

Vasopressin and analogues: desmopressin, vasopressin, terlipressin - actions

A

smooth muscle vasoconstriction
renal actions: increase the rate of insertion of aquaporins in collecting duct into luminal membrane

17
Q

16.04 POSTERIOR PITUITARY HORMONES

Vasopressin and analogues: desmopressin, vasopressin, terlipressin - MOA

A

vasopressin binds to V2 receptors in the basolateral membrane of the cells in the distal tubule and collecting ducts of the nephron
main effect in the collecting duct is to increase the rate of insertion of aquaporins into the luminal membrane, thereby increasing permeability of the membrane to water
also activates urea transporter
smooth muscle contraction by acting on V1A receptors
stimulates blood platelet aggregation and mobilisation of clotting factors

18
Q

16.04 POSTERIOR PITUITARY HORMONES

Vasopressin and analogues: desmopressin, vasopressin, terlipressin - abs/distrib/elim

A

given via SC/IM/IV injection or IV infusion
desmopressin can be given by nasal spray
vasopressin is rapidly eliminated with a plasma half-life <10 min and short duration of action

19
Q

16.04 POSTERIOR PITUITARY HORMONES

Vasopressin and analogues: desmopressin, vasopressin, terlipressin - clinical use

A

diabetes insipidus, bleeding oesophageal varices

20
Q

16.04 POSTERIOR PITUITARY HORMONES

Vasopressin and analogues: desmopressin, vasopressin, terlipressin - adverse effects

A

angina (due to coronary vasoconstriction)
headache
nausea

21
Q

16.04 POSTERIOR PITUITARY HORMONES

Vasopressin and analogues: desmopressin, vasopressin, terlipressin - special notes

A

treatment with desmopressin without concomitant reduction of fluid intake may lead to water retention/hyponatraemia

22
Q

16.05 MINERALOCORTICOID

Fludrocortisone - actions

A

acts on the distal renal tubule to increase Na+ reabsorption and increase excretion of K+ and H+

23
Q

16.05 MINERALOCORTICOID

Fludrocortisone - MOA

A

mineralocorticoids interact with intracellular receptors in the kidney controlling transcription of specific genes that cause: ↑number of Na+ channels, ↑number of Na+ pumps

24
Q

16.05 MINERALOCORTICOID

Fludrocortisone - abs/distrib/elim

A

given orally

25
Q

16.05 MINERALOCORTICOID

Fludrocortisone - clinical use

A

used (with a glucocorticoid) for replacement therapy in adrenal insufficiency
postural hypotension

26
Q

16.05 MINERALOCORTICOID

Fludrocortisone - adverse effects

A

few
hypokalaemia can occur and is increased by thiazides and loop diuretics
peripheral oedema (avoid in older people with postural hypotension who already have peripheral oedema)

Pharmacology (34 decks)

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