Hypothalamic and Pituitary Drugs Flashcards
Corticotropin (ACTH) - MoA
Increased activity of cholesterol side-chain cleavage enzyme, causing conversion of cholesterol to pregnenolone. This stimulates of adrenal cortex to produce: cortisol, aldosterone, & androgens.
Corticotropin preparations
Porcine corticotropin
Cosyntropin
Corticorelin ovine triflutate
Cosyntropin - Classification
Synthetic form of human corticotropin
Cosyntropin - Clinical use
Diagnose Adrenal insufficiency (pituitary adenoma vs adrenal tumor)
Distunguish Congenital adrenal hyperplasia from ovarrian hyperandrogenism.
Why is cosyntropin used for diagnosing adrenal insufficiancy?
It increases cortisol levels in healthy individuals but fails to increase cortisol in persons with adrenal insufficiency
Corticorelin ovine triflutate - Classification and Administration
Corticotropin releasing hormone (CRH)
IV administration
Corticorelin ovine triflutate - Clinical use
Diagnostic test to determine the cause of excessive levels of cortisol in persons with Cushing syndrome
Growth hormone (Somatotropin) - MoA
Direct stimulation of lipolysis and antagonize insulin to elevate blood glucose levels
Indirect stimulation of insulin-like growth factor 1 (IGF-1): skeletal muscle growth, amino acid transport, protein synthesis, nucleic acid synthesis, cell proliferation.
Growth hormone preparations
Somatropin
Mecasermin
Somatropin - Classification and Administration
Recombinant form of somatotropin (GH)
Subcutaneous
Somatropin - Clinical use
GH deficiency in children: Idiopathic growth hormone deficiency Turner syndrome Chronic renal failure Prader-Willi syndrome
Somatropin - Contraindications
Malignancies, critically ill patients (increase mortality).
Which group of people are less responsive to somatropin?
Children who received craniospinal irradiation for treatment of childhood malignancy
Somatropin - Adverse effects
None are common
Psuedotumor cerebri Slipped capital femoral Epiphysis Progression of scoliosis Edema Hyperglycemia. Turner: otitis media Myalgias Arthralgia Carpal tunnel syndrome
Mecasermin - Classification
Recombinant human IGF-1
Mecasermin - MoA
IGF-1 mechanisms: skeletal muscle growth, amino acid transport, protein synthesis, nucleic acid synthesis, cell proliferation.
Mecasermin - Clinical use
Growth failure in children with severe IGF-1 deficiency, GH receptor mutation, antibodies to GH
Mecasermin is produced by which bacteria?
E. coli
Mecasermin - Adverse effects
Hypoglycemia
How can you prevent hypoglycemia with the use of Mecasermin?
By eating a meal or snack before or soon after the time of injection
Growth hormone inhibitors
Somatostatin
Octreotide
Lanreotide
Cabergoline
Somatostatin - MoA
Inhibits GH secretion and insulin secretion from pancreas
Somatostatin - Clinical use
Limited use: short duration of action and multiple effects on secretory systems
Octreotide - Classification and Administration
Somatostatin analogue
Subcutaneous
Octreotide - MoA
Suppresses secretion of:
Growth hormone
IGF-1
Serotonin
GI-peptides (gastrin, motilin, secretin, VIP)
Greater effect on GH than insulin secretion
Octreotide - Clinical use
Acromegaly.
Tumors secreting insulin, glucagon, gastrin, thryotropin, and vasoactive intestinal peptide
Carcinoid tumors secreting serotonin and kallikrein
Octreotide - Adverse effects
Nausea, vomiting, abdominal cramps, steatorrhea, gallstones
Arrhythmias (brady, disturb conduction). (Hyper)+ hypoglycemia Constipation Flatulence B12-def in long-term use.
Lanreotide - Classification and Administration
Cyclic octapeptide analogue of somatostatin
Deep subcutaneous
Lanreotide - Clinical use
Acromegaly
Cabergoline - Classification
Selective dopamine 2 agonist
Cabergoline - MoA
Reduce GH, IGF-1 and prolactin
Cabergoline - Clinical use
Acromegaly
Hyperprolactinemia
Parkinson