DR. LEAL - ENDOCRINE DRUGS

Question 1

○ Autosomal dominant genetic disease
associated with growth failure, obesity, and carbohydrate intolerance.
○ GH treatment
decreases body fat
increases lean body mass, linear growth, and energy expenditure.

Answer 1

Prader-Willi Syndrome

Question 2

shown to increase final height in girls with Turner syndrome by 10–15 cm (4–6 inches).

Answer 2

GH TREATMENT

Question 3

● For treatment of severe IGF-I deficiency that is not
responsive to GH.
● Recombinant human IGF-I
● Adverse effect: hypoglycemia

Answer 3

MECASERMIN

Question 4

Initial therapy of choice for GH-secreting adenomas

Answer 4

Endoscopic Transsphenoidal Surgery

Question 5

reduce the production of GH.

Answer 5

Somatostatin analogs
dopamine receptor agonists

Question 6

GH receptor antagonist;
prevents GH from activating GH signaling pathways.

Answer 6

PEGVISOMANT

Question 7

reserved for patients
with inadequate response to surgical and medical therapies.

Answer 7

RADIATION THERAPY

Question 8

○ 14-amino-acid peptide.
○ Found in the hypothalamus, parts of CNS,
pancreas, and other sites in the GIT.
○ Functions primarily as an
Inhibitory Paracrine Factor and
Inhibits the release of GH, TSH, glucagon, insulin, and gastrin.
○ Rapidly cleared from the circulation, with a half-life of 1-3 minutes.
○ Short duration of action.

Answer 8

SOMATOSTATIN

Question 9

○ 14-amino-acid peptide.
○ Found in the hypothalamus, parts of CNS,
pancreas, and other sites in the GIT.
○ Functions primarily as an Inhibitory Paracrine Factor and Inhibits the release of GH, TSH, glucagon, insulin, and gastrin.
○ Rapidly cleared from the circulation, with a
half-life of 1-3 minutes.
○ Short duration of action.

Answer 9

SOMATOSTATIN

Question 10

○ Somatostatin analog
○ 45x more potent than somatostatin in inhibiting GH release but only 2x as potent in reducing insulin secretion.
○ Reduced effect on pancreatic beta cells, hyperglycemia rarely occurs during treatment.

Answer 10

OCTREOTIDE

Question 11

useful in localizing neuroendocrine tumors having somatostatin receptors
helps predict the response to octreotide therapy.
○ Useful for the acute control of bleeding from esophageal varices.

Answer 11

radiolabeled octreotide

Question 12

Somatostatin analog
Approved for the treatment of acromegaly
Appears to have effects comparable to those of octreotide in reducing GH levels and normalizing IGF-I concentrations.

Answer 12

LANREOTIDE

Question 13

GH receptor antagonist used to treat Acromegaly

Does not inhibit GH secretion and may lead to increased GH levels and possible adenoma growth

Answer 13

PEGVISOMANT

Question 14

● Used in states of infertility to stimulate spermatogenesis in men and to induce follicle development and ovulation in women.
● Most common clinical use for controlled ovarian stimulation, which is the cornerstone of assisted reproductive technologies such as in vitro fertilization (IVF).

Answer 14

FSH, LH, AND HCG

Question 15

● aka Human Menopausal Gonadotropin (hMG)
● Obtained from the urine of post-menopausal women.
● Partially broken down into FSH and LH in the body.

Answer 15

MENOTROPIN

Question 16

○ Purified preparation of human FSH.
○ Extracted from the urine of postmenopausal women.
○ Withdrawn from the US market in 2015.

Answer 16

Urofollitropin (uFSH)

Question 17

○ First and only recombinant form of human LH.
○ Withdrawn in 2012.
○ SQ injection: has a half-life of about 10 hours.

Answer 17

LUTROPIN ALFA

Question 18

○ For stimulation of follicular development in
infertile hypogonadotropic hypogonadal women with profound LH deficiency (<1.2 IU/L).
○ May also be of benefit in certain subgroups of normogonadotropic women

Answer 18

Lutropin alfa with follitropin alfa

Question 19

Produced by the human placenta and excreted into
the urine, hence it can be extracted and purified.

Answer 19

HUMAN CHORIONIC GONADOTROPIN

Question 20

○ A recombinant form of hCG.
○ Purified from human urine.
○ Administered by SQ or IM injection.
○ Injection for those who want to get pregnant.

Answer 20

Choriogonadotropin alfa (rhCG)

Question 21

○ Used to induce follicle development and ovulation in women with anovulation that is secondary to hypogonadotropic hypogonadism, polycystic ovary syndrome, and other causes.
○ Also used for controlled ovarian stimulation in assisted reproductive technology procedures.

Answer 21

GONADOTROPINS

Question 22

○ Two primary risks of ovulation induction:
- Multiple pregnancies (twins or triplets)
- Ovarian hyperstimulation syndrome

Answer 22

GONADOTROPINS

Question 23

required to stimulate the gonadotrophs to produce and release LH and FSH.

Answer 23

Pulsatile GnRH secretion

Question 24

used to induce gonadal suppression in men with prostate cancer or children with central precocious puberty.

Answer 24

GnRH agonists

Question 25

○ Use in controlled ovarian stimulation procedures.
○ Absorbed rapidly after subcutaneous injection.
○ 0.25 mg daily maintains GnRH antagonism.
○ Adverse effects: nausea and headache.

Answer 25

GANIRELIX
CETRORELIX

Question 26

○ Advanced prostate cancer.
○ Initiation: 240 mg administered as two
subcutaneous injections.
○ Maintenance: 80 mg subcutaneous injection
every 28 days.
○ Adverse effects: androgen deprivation (hot
flushes and weight gain).

Answer 26

ABARELIX
DEGARELIX

Question 27

● 198 amino acid peptide hormone.
● Structure resembles growth hormone.
● Principal hormone for lactation.
● Milk production is stimulated by prolactin when
appropriate circulating levels of estrogens,
progestins, corticosteroids, and insulin are present.

Answer 27

PROLACTIN

Question 28

a result of hyperprolactinemia.
○ Infertility (inhibition of GnRH release).
○ Oligomenorrhea or amenorrhea, and
galactorrhea in premenopausal women.
○ Loss of libido, erectile dysfunction, and
infertility in men.

Answer 28

HYPOGONADISM

Question 29

● Act in the pituitary to inhibit prolactin release.
● Standard first-line treatment for
hyperprolactinemia.
● Shrink pituitary prolactin-releasing tumors,

Answer 29

DOPAMINE AGONISTS

Question 30

○ Ergot derivatives.
○ High affinity for dopamine D2 receptors.

Answer 30

● Bromocriptine and Cabergoline

Question 31

○ Non-ergot agent.
○ High affinity for dopamine D2 receptors.

Answer 31

Quinagolide

Question 32

○ Non-ergot D2 agonists used in Parkinson’s disease.

Answer 32

PRAMIPREXOLE
ROPINIROLE

Question 33

○ Half-life: 65 hours
○ Longest duration of action.
○ Initiation at 0.25 mg twice weekly orally or
vaginally, can be increased gradually, according to serum prolactin determinations, up to a maximum of 1 mg twice weekly.

Answer 33

CABERGOLINE

Question 34

○ Half-life: 7 hours
○ Safe to use during early pregnancy.
○ Used in Parkinson’s disease to improve motor function and reduce levodopa requirements.
○ Adverse effect: valvular heart disease.
○ Can reduce growth hormone release in
patients with acromegaly (not as effective)

Answer 34

BROMOCRIPTINE

Question 35

● Stimulates muscular contractions in the uterus and myoepithelial contractions in the breast.
● Involved in parturition and the letdown of milk.
● During the 2nd half of pregnancy
● Administered IV for initiation and augmentation of labor.

Answer 35

OXYTOCIN

Question 36

● Can be administered IM for control of postpartum bleeding.
● Stimulates the release of prostaglandins and leukotrienes that augment uterine contraction.
● Not bound to plasma proteins

Answer 36

OXYTOCIN

Question 37

High concentrations of oxytocin with activation of vasopressin receptors

Answer 37

excessive fluid retention, or water intoxication, leading to hyponatremia, heart failure, seizures, and death.

Question 38

Contraindications of OXYTOCIN

Answer 38

○ Fetal distress
○ Fetal malpresentation
○ Placental abruption
○ Predispositions for uterine rupture

Question 39

○ Oxytocin receptor antagonist
○ Used in the treatment (tocolysis) for
preterm labor.

Answer 39

ATOSIBAN

Question 40

● Also known as antidiuretic hormone, ADH
● Released by the posterior pituitary (see Figure 35) in response to rising plasma tonicity or falling blood pressure.
● Possesses antidiuretic and vasopressor
properties.

Answer 40

VASOPRESSIN

Question 41

deficiency of Vasopressin

Answer 41

DIABETIC INSIPIDUS

Question 42

Activates two subtypes of G protein-coupled receptors.

found on vascular smooth
muscle cells and mediate vasoconstriction via the
coupling protein Gq and phospholipase C.

Answer 42

V1 RECEPTORS

Question 43

found on renal tubule cells and reduce diuresis through increased water permeability and water resorption in the collecting
tubules via Gs and adenylyl cyclase.

Answer 43

V2 RECEPTORS

Question 44

● Treatments of choice for pituitary Diabetes Insipidus.
● Administered by IV or IM injection

● Vasopressin infusion is effective in some cases of
esophageal variceal bleeding and colonic
diverticular bleeding.
● High-dose vasopressin as a 40-unit IV bolus injection may be given to replace epinephrine in the Advanced Cardiovascular Life Support (ACLS) resuscitation protocol for pulseless arrest.

Answer 44

VASOPRESSIN AND DESMOPRESSIN

Question 45

Overdosage can result in hyponatremia and seizures.

Answer 45

VASOPRESSIN AND DESMOPRESSIN

Question 46

○ Also used for the treatment of
coagulopathy in hemophilia A and von
Willebrand disease
○ Can be administered intravenously,
subcutaneously, intranasally, or orally.

Answer 46

DESMOPRESSIN

Question 47

ameliorates nocturnal enuresis by
decreasing nocturnal urine production.

Answer 47

Bedtime desmopressin therapy

Question 48

VASOPRESSIN ANTAGONIST

High affinity for both V1a and V2 receptors.

Answer 48

CONIVAPTAN

Question 49

VASOPRESSIN ANTAGONIST
○ 30-fold higher affinity for V2 than for V 1 receptors.
○ Treatment duration is limited to 30 days due to the risk of hepatotoxicity, including life-threatening liver failure.

Answer 49

TOLVAPTAN