Hypothalamic-Pituitary Pharm

Front 1

What drugs stimulate the synthesis and release of GH? and Why would you use these?

Back 1

sermorelin, hexarelin (GHRH analogs)
Used diagnostically, to determine if children of short stature have pituitary dwarfism. If there's low GH and these GHRH increase GH, then the problem must be hypothalamic.

Front 2

What drugs are analogs of GH and how do they work?

Back 2

somatotropin, somatrem.
They work on JAK/STAT receptors and stimulate long bone growth, muscle formation, lipolysis and increased plasma glucose, all due to an increase in IGF-1.

Front 3

What are GH analogs used for? What are the criteria?

Back 3

Until a satisfactory height is reached or the epiphyseal plates close.
To reverse catabolic states (AIDS, wasting diseases, long-term steroids).
Improve GI function in short bowel syndrome patients.
Long-term treatment of children with idiopathic short stature.

Front 4

What are the adverse effects of GH analogs?

Back 4

Diabetes --> monitor plasma glucose levels
Hypothyroid --> monitor thyroid
Carpal tunnel, swelling

Front 5

What are contraindications for GH analogs?

Back 5

Prader-Willi syndrome who are severley obese or w/ severe respiratory impairment.

Front 6

What's mecasermin?

Back 6

a recombinant IGF-1 with IGF-binding protein-3 that's used for children with growth failure and IGF deficiency who don't respond to GH (due to neutralizing antibodies, GH-R mutations).

Front 7

What's pegvisomant?

Back 7

A GH-R antagonist made with a PEG (polyethylene glycol) derivative of mutant GH. 2nd line for treating acromegaly.

Front 8

What are the GH-release inhibiting drugs?

Back 8

somatostatin, octreotide

Front 9

How do somatostatin and octreotide work?

Back 9

decrease release of GH from the ant pituity, also inhibits gastrin, pepsin, glucagon and gastric acid secretions. Monthly IM injections.

Front 10

What are the uses for somatostatin and octreotide?

Back 10

-reduce GH in acromegaly patients
-treate gastrinoma and glucagonoma and severe (diabetic, secretory) diarrhea

Front 11

What are AEs for somatostatin and octreotide?

Back 11

gastrointestinal and cardiac.
Also vitamin B12 deficiency,
Caution with hepatic/renal impairment.

Front 12

What are the systemic effects of hyperprolactinemia?

Back 12

Suppresses gonadotropin secretion and reproductive function.
Females: galactorrhea, amenorrhea, infertility, hypogonadism
Males: loss of libido, impotence, glactorrhea, hypogonadism

Front 13

What drugs do you use to treat a prolactinoma and how do they work?

Back 13

bromocriptine, pergolide, (cabergoline).
Oral dopamine agonists, and so decrease the release of prolactin.

Front 14

What are the therapeutic uses of bromocriptine and pergolide?

Back 14

Treat hyperprolactinemia.
Inhibit postpartum lactation.

Front 15

What are the adverse effects of bromocriptine and pergolide?

Back 15

nausea, light-headedness, orthostatic hypotension, constipation.
Cause vasoconstriction, so don't use in pregnant women.
Dopamine-analogs, so don't use if there's a hx of schizophrenia.

Front 16

What does ADH do in the body? What receptors does it bind?

Back 16

It's released in response to decreased plasma tonicity or decreased blood pressure.
V2-R at the distal tubules --> cAMP --> increase water channels and permeability (retain water)
V1-R cause vasoconstriction.

Front 17

What are the therapeutic uses for vasopressin and desmopressin?

Back 17

Diabetes insipidus (polydipsia, polyusira and dehydration due to absent ADH)
Primary nocturnal enuresis (bedwetting)-- no longer used b/c cause hyponatremia.
Vasopressin: for esophageal variceal bleeding and colonic diverticular bleeding.
Desmopressin: for coagulopathies.

Front 18

What are the side effects of vasopressin and desmopressin?

Back 18

nausea, headache, abdominal cramps, hyponatremia.
large doses: cardiac (anginal attacks for vasopressor activity).

Front 19

What's the difference between vasopressin and desmopressin?

Back 19

desmopressin is longer-acting and can be used twice a day intranasally. vasopressin is only for transient diabetes insipidus. Both now have po formulations.

Front 20

What would you use for SIADH?

Back 20

demeclocycline (tetracycline that antagonizes the action of ADH on renal tubules)

Front 21

What are the vasopressin receptor antagonists and when would you use them?

Back 21

conivaptan, (tolvaptan). Used for euvolemic hyponatremia.
note: conivaptan is a CYP3A4 inhibitor, don't combine with others.
AE: hypokalemia, orthostatic hypotension, polyuria.
CI: hypovolemic hyponatremia

Front 22

What are the systemic effects of oxytocin?

Back 22

Works through GPCR and PIP-Ca, induces uterine contractions, helps maintain labor, enhances cervical dilation, elicits milk ejection.
MOA: alters ion currents across the myometrial smooth muscle cells (uterus is sensitized during pregnancy)

Front 23

What are the therapeutic uses for oxytocin?

Back 23

-induce and support labor for an early vaginal delivery
-low dose: increased force and frequency of uterine contractions
-high dose: prolonged uterine contractions, vascular smooth muscle relaxation, may decrease BP.
-nasal spray: induce lactation post-partum

Front 24

What has now replaced oxytocin to control post-partum uterine hemorrhage?

Back 24

methylegonovine maleate, (ergonovine maleate)
more rapid and prolonged control than oxytocin, with less toxicity

Front 25

What non-hypothalamic/pituitary axis-based drugs can be given to induce labor? What else do they do?

Back 25

PGE1 (gemeprost), PGE2 (dinoprostone), PGF2alpha (carboprost)
Also control post-partum bleeding and induce first and second trimester abortions.

Front 26

What are the adverse effects of gemeprost, dinoprostone, carboprost?

Back 26

diarrhea, hyperthermia, bronchoconstriction

Front 27

Why would you use b2-agonists during pregnancy? Which b2-agonists would you use?

Back 27

Used to relax a pregnant uterus to prevent or delay premature parturition.
Use ritodrine or terbutaline.
AE: skeletal muscle tremor, tachycardia

Front 28

What are the contraindications for ritodrine and terbutaline?

Back 28

(these are b2-agonists)
maternal cardiac disease, pregnancy-induced HTN, uncontrolled diabetes mellitus, hyperthyroid, hypobolemia, multiple gestation.

Front 29

What is a use for magnesium sulfate in pregnancy?

Back 29

Relax the uterus to prevent or delay premature parturition

Front 30

po drugs

Back 30

bromocriptine, pergolide, vasopressin, desmopressin, demecocycine, methylergonovine, ritodrine, terbutaline.

All the rest are peptides or not orally available for some other reason.