Pituitary Gland Flashcards
GH secretion is regulated by?
- Hypothalamic GH releasing factor (GHRF)
- Somatostatin
- Insulin-like growth factor (IGF)-1
physiological effects of GH
1) Anabolic effects
* Bone growth
* Bone mineral density increase after the epiphyses have closed
* Increased muscle mass
* Protein synthesis
2) Metabolic Effects
* Increased lipolysis
* Gluconeogenesis stimulation
Drug of choice to treat GH deficiency
Somatropin
(Recombinant GH)
Adm of Somatropin
SC
CU of Somatropin
1) Pituitary dwarfism
2) Turner’s syndrome
3) AIDS-associated wasting
4) Used illicitly by athletes
Pituitary Dwarfism is caused by lack of?
GH, GHRF and IGF-1 generation/action
AE of Somatoropin
- Few side effects in children
Adults:
* Peripheral edema
* Carpel tunnel syndrome
* Arthalgias (joint stiffness)
* Myalgia
* Insulin resistance
Recombinant IGF-1
Mecasermin
CU of Mecasermin
Treatment of growth failure in children
caused by
- Lack adequate amounts of IGF
- GH deficiency alternative to recombinant GH
* note: GH is more effective
Adm of Mecasermin
SC injection
Excessive production of GH
* Children -> ——–
* Adults –> ——-
- Children –> Gigantism
- Adults –> Acromegaly
Tx of excessive GH production
Pegvisomant
Bromocriptine
MoA of Pegvisomant
Recombinant modified version of GH –> Highly selective antagonist of GH actions
CU of Pegvisomant
2nd line tx in Excessive GH production
(when somatostain have failed)
CU of Bromocriptin
3rd line tx of execcive GH production
MoA of Bromocriptine
Dopamine agonist –> decreases production of GH from pituitary gland (AP)
1st line tx of Excessive GH production
Somatostatin
MoA of Somatostatin in the Anterior pituitary
Inhibits release of GH and TSH
MoA of Somatostatin in the pancreas
Inhibits insulin and glucagon release
MoA of Somatostain in the GI tract
Reduces gastric acid and pancreatic
secretions
Somatostain analogues
Octreotide
Lanreotide
Favoured tx of Acromegaly?
Somatostain analogue
(Octreotide, lanreotide)
CU of Octreotide
1) Oesophageal Varices
2) Acromegaly due Excessive GH
3) Carcinoid and other hormone-secreting tumours
AE of Somatostain Analogues
1) Injection site pain (SC injection),
2) GI disturbances,
3) gallstones,
4) postprandial hyperglycemia (due to insulin inhibition in the pancrease)
5) hypothyroidism (due to inhibition of TSH)
Fxn of Prolactin
Lactation
What is used in the prevention of lactation?
Bromocriptine (Dopamine agonist)
What is used to stimulate lactation
Dopamine antagonsits
MoA of Dopamine Antagonists in terms of lactation
Stimulate prolactine release –> increase lactatin
MoA of Dopamine Agonists in terms of lactation
Supress prolactine release –> inhibit lactation
CU of Bromocriptine
1) Prevent lactation
2) Galactorrhoea
3) Prolactinoma
4) Tx of Parkinsonism and acromegaly
AE of Bromocriptine
1) Nausea/vomiting
2) Headache
3) Postural hypotension
4) Less frequent : Psychosis/hallucinations, Insomnia
Dopamine anatgonists
Metoclopramide; domperidone
Anti-psychotics may
cause —————- as a
side effect
Galactorrhea
Physiological action Vasopressin receptor 1A (V1A)
Phospholipase C/IP3 system activation –> Contraction of smooth muscle
Physiological effect og Vasopressin receptor 1B [V1B (v3)]
Phospholipase C/IP3 system activation -> Release of adrenocorticotropic hormone (ACTH) from anterior pituitary
Physiological action of V2 receptor
- Stimulation of adenylyl cyclase
- Action in collecting ducts of the nephron
–> Increases permeability to water (aquaporin insertion) - Release of blood coagulation factors
V2 receptor acts on?
Collecting ducts of the nephron –> increases permeabilty to water ( aqaporin insertion)
Vasopressin analogues
1) Terlipressin (V1 selective)
2) Desmopressin (V2 selective)
- pressin
CU of Terlipressin
tx of bleeding in Oesophageal varices
CU of Desmopressin
1) Central diabetes insipidus (not nephrotic DI)
2) Persistent nocturnal enuresis
3) Prophylaxis against bleeding in haemophilia
AE of Vasopressin Analogues V1- mediated AE
1) Facial pallor
2) Increased intestinal activity (nausea/cramps)
3) Spasm of coronary arteries (angina)
4) Reduced CO
- Terlipressin
AE of vasopressin analouge, V2-mediated AE
Water intoxication
(hyperhydration)
* Desmopressin
Vasopressin Antagonists
1) Tolvaptan (oral) - selective V2 anatogonist
2) Conivaptan (IV) - non-selective V1A/V2 antagonist
-aptan
Adm of Tolvaptan
Oral
Adm of Conivaptan
IV
HINT: Conivaptan
MoA of Conivaptan
Non-selective V1A/V2 anatgonist
MoA of Tolvaptan
Selective V2 antagonist
CU of Tolvaptan
1) Treatment of syndrome of inappropriate ADH
secretion (‘SIADH’)
2) Hypervolemic or euvolemic hyponatremia
CU of Conivaptan
Hypervolemic or euvolemic hyponatremia in hospitalized patients
* Emergency tx (IV)
AE of Tolvaptan
1) GI-related adverse effects,
2) hyperglycemia,
3) pyrexia (fever)
AE of Conivaptan
1) Drug-drug interactions preclude chronic use
2) Infusion-site reactions
A Tetracycline drug
Demecolocycline
CU of Demeclocycline
SIADH
AE of Demeclocycline
- Nephrogenic DI
- Photosensitivity
- Abnormalities of bone and teeth
MoA of Demeclocycline
V2 antangonist
Drugs used to test for ACTH production i Cushing’s syndrome
Metyrapone
(anti-adrenal CS -> inhibits the synthesis of endogenous adrenal glucocorticoids)
**
tx of Cushing’s syndrome
ketoconazole
(anti-glucocorticoid)