Pharm Test 3 Hypothalamic and Pituitary Hormones Flashcards
Somatropin (recombinant)
Somatrem (analog)
(Too little GH)
Stimulates Bone growth, increases bone density, increase muscle mass, increase GFR, Increase immune system function, **Anti-insulin actions -> increase glucose -> increase insulin -> Hypoglycemia
MOA: Activates IGF1 via JAK/STAT
Indication: GH deficiency, short stature and fat kids, Unopposed Insulin, Growth failure associated with Noonan, Prader-Willi, Turner synd, wasting in HIV Pts, Short bowel syndrome (improves GI function)
CYP450 inducer
AE in children: Hypothyroid, gynecomastia, Intracranial HTN, SCOLIOSIS, Otitis media, pancreatitis, diabetic syndrome
AE in Adults: Edema, carpal tunnel, retinopathy, myalgia, arthralgia
**DONT GIVE TO MALIGNANCIES
Sermorelin
Too little GH
GHRH analog, stimulates release of GH
Indication: GH deficiency but less effective than somatropin.
**This won’t work in Anterior pit is broken
Mecasermin
Too little GH
IGF1 analog, needs to be combined with IGF binding protein 3.
Indication: Growth failure due to decrease IGF1, GH receptor mutation.
AE: Hypoglycemia (Eat food to prevent), Intracranial HTN, increased liver enzymes
Octreotide
Too much GH
Somatostatin analog but 45x more potent in decreasing GH release
2x: more potent in decrease of insulin and 30x increase in half life
MOA: inhibits release of GH, glucagon, insulin, gastrin
Indication: Acromegaly, carcindoid, gastrinoma, etc
AE: Constipation, Gallstones, Pain at injection site, N/V/Steatorrhea, Sinus bradycardia, B12 deficiency
Bromocriptine Cabergoline (Less AE and longer half life)
(Too much GH)
Dopamine Agonists=inhibit prolactin and GH secretions
Activates postsynaptic Dopamine receptors
Indication: prolactinoma, acromegaly
AE: N/HA/lightheadedness, Psych manifestations (give with antidepressants), orthostatic hTN, fatigue
Menotropins (Purified FSH and LH)
Follitropin (recombinant FSH)
Urofollitropin (extract FSH)
hCG (extract or recombinant)
MOA: acts through GPCR’s aiding in follicular development, ovulation and pregnancy
Indication: Induce ovulation (expensive), Male infertility due to hypogonadism (rqs both FSH and LH)
AE: men: gynecomatia
Women: multiple pregnancies, ovarian hyperstimulation syndrome, HA, depression, edema, precocious puberty
Gonadorelin (GnRH recombinant, t.5=4 min)
Leuprolide
Nafarelin
Goserelin
L/N/G: GnRH analogs with D amino acids at position 6 (Stronger and longer)
MOA: binds GPCR to modify FSH and LH levels in blood
*Pulsatile: stimulates
Continuous: inhibits. Agonist flare for first week but after 1 week it becomes inhibitory. Give flutamide to counter flare
Stimulation indication: Infertility, DX LH responsiveness in delayed puberty
Suppression indication: PCOS, Endometriosis, fibroids, Prostate Cancer, precocious puberty, breast and ovarian cancer
AE: HA/N/flushing, acute hypersensativity rxn. Sudden pituitary apoplexy and blindness
AE continuous TX: MENOPAUSE, decreased libido, hot flushes, sweats, edema, gynecomastia…etc
**Do NOT give to pregnant or breastfeeding mothers
Cetrorelix
Ganirelix
Competative GnRH receptor antagonists
Indication: Suppress gonadotropin production thus preventing LH surge during controlled ovarioan hyperstimulation
Corticotropin
Cosyntropin
ACTH analogs
MOA: stimulate adrenal cortex via MC2R->increases cAMP->steroid hormone secretion
Indication: Limited use as therapy. Differentiate b/w primary(addisons) and secondary adrenal insufficiency.
***ACTH normally secreted from pituitary in pulses, highest at 6am and lowest in evening
Oxytocin
STimulates release of PG and LT that augment uterine contraction, Milk ejection
MOA: binds GPCR, Low dose= increased force and frequency of contraction. High dose=sustained contraction with weak Antidiureticand pressor activity
Indication: IV: initiate and augment labor. IM: control postpartum bleeding
AE: fetal distress, placenta abruption or uterine rupture, excess fluid retention and water intoxication->seizure and death
CI: Prematurity/fetal distress, abnormal fetal presentation
Atosiban
Oxytocin antagonist.
use to prevent preterm labor *NOT used in USA
Vasopressin: V1 and V2 agonist
Desmopressin: long acting V2 only agonist
MOA: ADH analogs binding to GPCR
V1: vasoconstriction
V2: H2O reabsorption via renal tubular cells
Indication: DOC for Diabetes Insipidus
Vasopressin: use to decrease bleeding from esophageal varices and diverticula
Desmopressin: Hemophilia A and vonWillebrand disease
AE: HA/N/Abdominal cramps and allergic reaction, hypo Na and seizures can be seen with overdose
Conivaptan
Vasopressin Antagonist. High Affinity for V1 and V2. Hyponatremia due to elevated vasopressin
