ERS L11 - Treatment of Pituitary Disorders Flashcards
Somatotropin replacement
For pituitary dwarfism.
Direct stimulation to increase protein synthesis and amino acid uptake. Increase lipolysis (after a few hours). Increase glucose level (after a few hours).
Indirectly stimulate bone growth by stimulation of IGF-1 production from liver.
Increase sulphate uptake into cartilage.
Promote bone growth by stimulating thymidine and uracil incorporation into DNA and RNA respectively.
Follitropin
Recombinant human FSH
Lutropin alpha
Recombinant human LH
Human chorionic gonadotropin
As LH replacement
Human menopausal gonadotropin
For FSH replacement
Mixture of FSH and LH
Choriogonadotropin alpha
Recombinant HCG
FSH replacement
*must add LH replacement for treating hypogonadism
Follitropin
Human menopausal gonadotropin
LH replacement
*add FSH replacement
Lutropin alpha
HCG
Choriogonadotropin alpha
For primary hypoadrenalism, eg Addison’s disease
Hydrocortisone/cortisone + fludrocortisone
Hydrocortisone
Corticosteroid, mainly with glucocorticoid function
Cortisone
Converted to hydrocortisone in liver
Corticosteroid, mainly glucocorticoid function
Fludrocortisone
Mineralosteroid
Secondary hypoadrenalism
Corticosteroid with glucocorticoid function only
Somatotropin: side effects
Hypothyroidism Glucose intolerance Peripheral edema Papilledema, visual changes Increased intracranial pressure, headache
FSH replacement: side effects (X8)
Ovarian hyper simulation syndrome (ovarian enlargement, hydrothorax, ascites, hypovolemia)
Haemoperitoneum Dyspnea Electrolyte imbalance Arterial thromboembolism Fever Multiple births Gynecomastia
LH replacement: side effects
Headache Depression Edema Precocious puberty Gynecomastia
Treatment for hyperprolactinemia
Dopamine D2 receptor agonist
- Bromocriptine
- Cabergoline
- Inhibit prolactin secretion
- Reduction in size of prolactin-producing adenoma
Cabergoline
Dopamine D2 agonist
For hyperprolactinemia, hypersecretion of growth hormone
Bromocriptine
Dopamine D2 agonist
For hyperprolactinemia, hypersecretion of growth hormone
Side effects of bromocriptine / cabergoline
1. Postural hypotension (D1 receptor, vasodilation) 2. Constipation (decrease gut motility) 3. Nausea and vomiting (D2 receptors, chemoreceptor trigger zone --> vomiting centre in medulla) 4. Dizziness
Octreotide
Somatostatin analogue for hypersecretion of GH
- Inhibit release of GH from anterior pituitary
- (minority) Reduce tumour size (reduce blood loss during surgery)
Lanreotide
Somatostatin analogue for hypersecretion of GH
- Inhibit release of GH from anterior pituitary
- (minority) Reduce tumour size (reduce blood loss during surgery)
Octreotide vs Lanreotide
Both somatostatin analogue
Octreotide:
- longer acting
- less hyperglycemic effect
Side effects of octreotide
- GI disturbance: Nausea and vomiting, Abdominal cramps, Flatulence, Steatorrhoea
- Gall stone: ↓ gall bladder motility
- Glucose intolerance: inhibit secretion of insulin from pancreas
Side effects of Lanreotide
- GI disturbance: Nausea and vomiting, Abdominal cramps, Flatulence, Steatorrhoea
- Gall stone: ↓ gall bladder motility
- Glucose intolerance: inhibit secretion of insulin from pancreas
Pegvisomant
GH receptor antagonist
- Block GH signaling
- Inhibit hepatic production of IGF-1
Side effects of Pegvisomant
- Elevated liver enzyme
- Nausea
- Diarrhoea
Treat acromegaly / gigantism
- Somatostatin analogue
Octreotide
Lanreotide - GH receptor antagonist
Pegvisomant - Dopamine receptor agonist
Bromocriptine
Cabergoline
Metyrapone
Treat Cushing’s Syndrome
Inhibit 11-beta-hydroxylase
Trilostane
For Cushing’s Syndrome
Inhibit 3-beta-drhydrogenase (3-beta-HSD)
Side effects of metyrapone
- Hypotension
- Nausea, vomiting
- Headache, dizziness
- Rash
Side effects of trilostane
- Hypotension
- Nausea, vomiting
- Headache, dizziness
- Rash
Treat Cushing’s Syndrome
Metyropone
Trilostane
Treat diabetes insipidus
Vasopressin
Desmopressin
MoA of desmopressin
Agonist of V2R at distal tubule and collecting ducts in kidneys
- Increase aquaporin-2 transcription
- Increase AQP-2 translocation to cell surface
Side effects of desmopressin
- Fluid retention
- Dilutional hyponatremia
- Headache
- Nausea
- Allergy
Side effects of vasopressin
- Fluid retention
- Dilutional hyponatremia
- Headache
- Nausea
- Allergy
Only to vasopressin (less sensitive, bind to V1R…)
- Coronary artery spasm –> angina
- Abdominal and uterine cramps
Treat pituitary dwarfism
Somatotropin
Treat gonadotropin deficiency
FSH + LH replacement
FSH:
- Follitropin
- Human menopausal gonadotropin
LH:
- Lutropin alpha
- Choriogondadotropin alpha
- HCG