Lecture 63 Hypothalamic/Pituitary Pharm

Question 1

Somatropin

used for, effect, route, type, adverse effects

Answer 1

Used for pituitary Dwarfism
Replacement therapy- bc not enough GH from ant pituitary
Given IV
Goal is to increase linear growth & lean body mass
rhGH; 191 AA’s
adverse effects rare in children

Question 2

Pegvisomant

used for, type, MOA

Answer 2

For Acromegaly in combo w other drugs
GH antagonist
binds to GH receptor, doesnt activate JAK-STAT signaling, or IGF-1

Question 3

Mecasermin

used for, type, MOA, adverse effects

Answer 3

used for Laron Syndrome- lack of responsiveness to GH (mutated GH receptor or antibodies to GH receptor)
rIGF-1 - can be combined w rIGFBP-3 (increases half-life)
Acts on target tissue
Side effect- hypoglycemia, should be given just after a snack

Question 4

Sermorelin

used for, type, clinical use

Answer 4

Used for Diagnostic purposes
GHRH
tx of GH deficiency and weight loss associated w AIDS

Question 5

Octreotide

type, uses, MOA

Answer 5

Somatostatin analog (agonist)- bc of somatostatin short half life (1-3mins)
45x more potent in suppressing GH secretion
Used for GH over activity, acromegly-> to reduce GH, IGF-1 levels
Use 2- suppression of ectopic hormone production by tumors
Slow-release depot preparation in biodegradable polymer

Question 6

Pituitary Drugs- ant, post (chars)

Answer 6

Anterior Pituitary (FLAT PEG)- Somatropin, Pegvisomant
Post Pituitary (OT, ADH)- Desmpressin, Conivaptan
   Post- easy to synthesize, IV admin

Question 7

Hypothalamus Drugs

Answer 7

Sermorelin, Octreotide, Bromocriptine

Hypothalamus is a SOB

Question 8

Bromocriptine

type, used for, Pharmacokinetics, adverse effects, Route, previous use

Answer 8

Dopamine analog- agonist at Dopamine receptors
Used to tx hyperprolactinemia- reduces circulating prolactin and at higher doses also GH
Prolactin-secreting adenomas can cause the hyperprolactinemia
Oral availability is only 7% (7% makes it past the liver)
Side effects- GI problems (nausea/ vomiting)
Divided does(milder on GI), or vaginal admin (skips GI)
Not used for Parkinsons anymore due to toxicity- had too give a bunch to get to brain but caused too many side effects

Question 9

GH related drugs

Answer 9

Somatropin
Pegvisomant
Mecasermin
Sermorelin
Octreotide

PM SOS

Question 10

Oxytocin

use, route

Answer 10

Given for labor induction/support- stimulates uterine contraction
Route- IV, can be nasally (must monitor carefully)

Question 11

ADH (vasopressin)

MOA, receptors, use

Answer 11

MOA- water retention- decreased urine prod, increased BP
2 main receptors- V1, V2
V1- on arteriolar smooth m., acts through IP3/DAG Ca 2ndary messenger system
V2- in distal and collecting duct of kidneys, affects mediated by cAMP
use- emergency to activate V1 receptors- vasoconstriction attenuates pressure and bleeding

Question 12

Desmopressin

(use, MOA, duration, activity, route, adverse effects,

Answer 12

Used for central diabetes insipidus (if receptor problem this wont help)
Synthetic analog of vasopressin SELECTIVE for V2
Long-lasting
Activity 400x over ADH
route- orally (1% bioavailable), nasally, IV
Side effects- hyponatremia (low Na)

Question 13

Conivapton

use, MOA

Answer 13

Used for SIADH (Syndrome of Inappropriate secretion of ADH)

Nonpeptide ADH antagonist w high affinity for V2 receptors (in kidneys)