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SP- Week 10 Thyroid > Pituitary Gland Hormone Drugs > Flashcards

Pituitary Gland Hormone Drugs Flashcards

1
Q

Hormone released from posterior pituitary

A

ADH = Vasopressin
Oxytocin

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2
Q

Hormones released from anterior pituitary

A

ACTH
Growth hormone (GH)
Prolactin (PRL)

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3
Q

GROWTH HORMONE ; secretion regulated by

A

Most abundant anterior pituitary hormone

  • Secretion regulated by:
     Hypothalamic GH releasing factor (GHRF)
     Somatostatin
     Insulin-like growth factor (IGF)-1
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4
Q

GH Anabolic effects

A

 Bone growth
 Bone mineral density increase after the epiphyses have closed
 Increased muscle mass
 Protein synthesis

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5
Q

Metabolic Effects of GH

A

 Increased lipolysis
 Gluconeogenesis stimulation

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6
Q

SOMATROPIN CLINICAL USES

A
  1. Pituitary dwarfism
    - Lack of GH
    - Lack of GHRF
    - Lack of IGF generation or action
  2. Turner’s syndrome
  3. AIDS-associated wasting
  4. Used illicitly by athletes
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7
Q

SOMATROPIN RoA

A

Recombinant GH: SC

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8
Q

ADVERSE EFFECTS
Of Somatotropin (in kids + adults)

A

-Few side effects in children

-Adults:
 Peripheral edema
 Carpal tunnel syndrome
 Arthalgias
 Myalgia
 Insulin resistance

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9
Q

RECOMBINANT IGF-1 example:

A

Mecasermin

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10
Q

Mecasermin Clinical uses

A

ONLY FOR KIDS

Treatment of growth failure in children:
 Lack adequate amounts
of IGF  GH deficiency alternative
to recombinant GH
 GH is more effective

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11
Q

Mecasermin RoA

A

SC injection

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12
Q

Excessive production of GH

A

Children -> Gigantism
Adults -> Acromegaly

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13
Q

Medication for Acromegaly

A
  • ‘Pegvisomant
  • , Dopamine agonist, bromocriptine, also used
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14
Q

What is Pegvisomant

A

Recombinant modified version of GH

 Highly selective antagonist of GH actions
 Alternative to SST analogues if they have failed

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15
Q

Dopamine agonist PK/PD

A
  • Less effective
  • Decreases production of GH from pituitary gland
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16
Q

SOMATOSTATIN in anterior pituitary

A

 Inhibits release of Growth Hormone (GH)
 Inhibits release of Thyroid Stimulating Hormone (TSH)

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17
Q

SOMATOSTATIN in Pancreas

A

Inhibits insulin and glucagon release

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18
Q

SOMATOSTATIN in GI tract

A

Reduces gastric acid and pancreatic secretions

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19
Q

-SOMATOSTATIN ANALOGUES exs.

A

Octreotide, lanreotide

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20
Q

‘Octreotide, lanreotide Clinical uses

A

 Acromegaly : Favoured treatment
 Carcinoid and other hormone-secreting tumours  Bleeding oesophageal varices: Constricts splanchnic blood vessels

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21
Q

Octreotide, lanreotide AE

A

‘Injection site pain (SC injection), GI disturbances,
gallstones, postprandial hyperglycemia, hypothyroidism

22
Q

PROLACTIN MoA

A

 Mediates mammary development: lactation
 Secreted from the anterior pituitary by lactotroph
(mammotroph) cells

23
Q

Prolactin secretion is under tonic inhibitory
control by hypothalamus
Regulated by:

A

• Dopamine (D2 receptors):

- Dopamine agonists (bromocriptine, cabergoline)
       - Suppress prolactin release 

- Dopamine antagonists
        Stimulate prolactin release
24
Q

Clinical uses of bromocriptine

A
  • to prevent lactation
  • to treat galactorrhea, owing to excessive prolactin secretion
  • to tx prolactin-secreting pituitary tumours (prolactinomas)
  • in the treatment of parkinsonism and of acromegaly
25
Q

DOPAMINE PATHWAYS

A
  1. Nigrostriatial (75%) – corpus striatum – regulates motor function
  2. Mesolimbic – nucleus accumbens and amygdala – regulates emotion
  3. Mesocortical – limbic cortex – regulates attention/cognition
  4. Tuberohypophysial – pituitary gland – regulates prolactin release
26
Q

AE of Dopamine agonists/ bromocriptine

A

-Nausea/vomiting
- Headache
- Postural hypotension
-Less frequent:
 Psychosis/hallucinations
 Insomnia

27
Q

DOPAMINE ANTAGONISTS exs

A

-Metoclopramide; domperidone
Primarily are prokinetics + anti-emetics

28
Q

DOPAMINE ANTAGONISTS clinical uses

A
  • to increase milk supply

 Off-label use during breast-feeding
 Anti-psychotics may cause galactorrhea as a
side effect

29
Q

VASOPRESSIN RECEPTORS

A

V1A, V1B (V3), V2

30
Q

V1A. Physiological actions

A
  • Phospholipase C/IP3 system activation
  • Contraction of smooth muscle
31
Q

V1B (V3) physiological axns

A

‘ Phospholipase C/IP
 Release of adrenocorticotropic hormone (ACTH) from anterior pituitary

32
Q

V2 physiological actions
!

A

 Stimulation of adenylyl cyclase
 Action in collecting ducts of the nephron
- Increases permeability to water (aquaporin insertion)
 Release of blood coagulation factors

33
Q

Desmopressin :
Properties

A

Increased duration of axn (cf ADH)
V2 selective

34
Q

Desmopressin Clinical uses

A

 Central diabetes insipidus
 Persistent nocturnal enuresis
 Prophylaxis against bleeding in haemophilia

35
Q

Terlipressin Properties

A

Increased duration of action (cf ADH)
Minimal anti diuretic properties
More V1 selectivity

36
Q

Terlipressin Clinical use

A

, Initial treatment of bleeding oesophageal varices

37
Q

‘ADVERSE EFFECTS of Vasopressin

A
  • Few unwanted side effects
  • V 1 -mediated:
    •Facial pallor
    • Increased intestinal activity (nausea/cramps)
    • Spasm of coronary arteries (angina)
    • Reduced cardiac output
  • V2-mediated
    •Water intoxication
    [ increased intracranial pressure]
    [ seizures]
38
Q

Tolvaptan Clinical uses

A

‘ Treatment of syndrome of inappropriate ADH secretion (‘SIADH’)
 Hypervolemic or euvolemic hyponatremia

39
Q

Tolvaptan properties + RoA

A

Selective V2 antagonist
Oral

40
Q

Conivaptan clinical use

A

 Hypervolemic or IV
euvolemic hyponatremia in hospitalized patients

41
Q

Conivaptan properties + RoA

A

Non-selective V1A /V2 antagonist
IV

42
Q

Tolvaptan AE

A

GI-related adverse effects, hyperglycemia, pyrexia

43
Q

Conivaptan AE

A

 Drug-drug interactions preclude chronic use
 Infusion-site reactions ( like any injectables)

44
Q

DEMECLOCYCLINE Clinical indication + what to treat it

A

 Tetracycline
 Rarely used as an antimicrobial agent
 Used to treat SIADH
V2 antagonist

45
Q

DEMECLOCYCLINE AE

A

 Nephrogenic DI
 Photosensitivity
 Abnormalities of bone and teeth

46
Q

DRUGS INHIBITING BIOSYNTHESIS

A
  • Metyparone
  • Trilostane
  • aminoglutethimide
  • ketoconazole
47
Q

‘Metyparone properties

A

Test for ACTH production
Cushing’s syndrome

48
Q

Trilostane (no longer used) Properties

A

Cushing’s syndrome
Primary hyperaldosteronism

49
Q

Aminoglutethimide (no longer used)
properties

A

Cushing’s syndrome
Advanced breast/prostate cancer

50
Q

Ketoconazole properties

A

Cushing’s syndrome

SP- Week 10 Thyroid (2 decks)

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