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Pharm final > hypothalamic and pituitary hormones > Flashcards

hypothalamic and pituitary hormones Flashcards

1
Q

what kind of receptors do Growth hormone and prolactin act on?

A

JAK/STAT superfamily

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2
Q

TSH, FSH, LH, Adrenocorticotropic hormone

act on what receptors?

A

GPCRs

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3
Q

what type of hormones are:

  1. Somatropin
  2. somatrem

Administration

A
  1. Recombinant GH (recombinant longer word just like somatropin is longer than analog)
  2. GH analog

Admin: Subcutaneous admin.

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4
Q 
Recominant Growth hormone:- Somatropin
AE in 
children
Adults:
CI
A 
Children
• Generally well tolerated
• Scoliosis (during rapid growth)
• Hypothyroidism
• Intracranial hypertension (rare)
• Otitis media (increased risk for Turner Syndrome patients)
• Pancreatitis, gynecomastia & nevus growth
• Diabetic syndrome (chronic use)
Adults:
• Peripheral edema, myalgias & arthralgias (hands & wrists
especially)
• Carpal tunnel syndrome
• Proliferative retinopathy (rare)

CI:
• Cytochrome P450 inducer
• Patients with a known malignancy

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5
Q

IGF-1 Analog:
Name
Structure

A

Mecasermin
• Complex of recombinant human IGF-1 and recombinant
human IGF-binding protein-3

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6
Q

Mecasernin AE

A
  • Hypoglycemia (eat 20 min before or after admin.)
  • Intracranial hypertension (rare)
  • Asymptomatic elevation of liver enzymes (rare)
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7
Q

GH secreting adenomas tx.

Small vs Large

A

• Small GH-secreting adenomas can be treated with GH
antagonists:
• GH receptor antagonists;
• somatostatin analogs; or
• dopamine receptor agonists
• Larger pituitary adenomas require surgery or radiation

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8
Q

Somatostatin Analog
Name
Activity
PK

A

Octreotide
• Somatostatin inhibits release of GH, TSH glucagon, insulin
& gastrin

Pharmacokinetics
• 45 x more potent in inhibiting GH release than
somatostatin
• 2 x more potent in reducing insulin secretion
• t ½ = ~ 80 min (30 x somatostatin)
• Octreotide acetate long-acting suspension can be given
at 4 week intervals

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9
Q

Somatostatin Analog
Octreotide
CA:

A

Clinical Applications
• Reduces symptoms caused by hormone-secreting
tumors: acromegaly, carcinoid syndrome, gastrinoma,
glucagonoma, nesidioblastosis, watery diarrhea,
hypokalemia, achlorhydria syndrome & diabetic diarrhea.
• Localizing neuroendocrine tumors
• Acute control of bleeding from esophageal varices

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10
Q

Somatostatin Analog

Octreotide AE:

A

• Nausea, vomiting, abdominal cramps, flatulence,
steatorrhea (with bulky bowel movements)
• Constipation
• Biliary sludge & gallstones (20-30% patients after 6 month
use)
• Sinus bradycardia (25%) & conduction disturbances(10%)
• Vitamin B12 deficiency (may occur with long-term use)
• Pain at injection site = common (esp. with long-acting)

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11
Q

Dopamine agonists
names?
PK?

A

Bromocriptine, Cabergoline

Pharmacokinetics
• Oral or as vaginal inserts
• Bromocriptine t1/2 = ~7 h
• Cabergoline t1/2 = ~65 h

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12
Q

Dopamine agonists:

Bromocriptine, Cabergoline AE

A

Adverse Effects
• Nausea (bromocriptine>cabergoline), headache, lightheadedness,
orthostatic hypotension, fatigue
• Psychiatric manifestations occasionally occur
• High doses = cold-induced peripheral digital vasospasm
• Chronic high-dosage therapy = pulmonary infiltrates

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13
Q

what are Menotropins

A

Menotropins or human menopausal gonadotropins
(hMG):
Purified extract of FSH and LH

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14
Q

Follitropin and Urofollitropin?

A

Purified FSH :
Follitropin alpha and follitropin Beta (rFSH): recombinant FSH
Urofollitropin (uFSH): purified human FSH extract

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15
Q

Human Chorionic Gonadotropin?

pK

A

• Extracted and purified from urine (given IM)
• Choriogonadotropin alpha (rhCG): recombinant form
(given SC)
Pharmacokinetics
• SC or IM injection (usually daily)

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16
Q

Gonadotropin AE

for men and women

A

Women
• Ovarian hyperstimulation syndrome
• Multiple pregnancies (15-20%)
• Headache, depression, edema, precocious puberty

Men
• Gynecomastia

17
Q

Gonadotropin releasing hormones and analogs
which ones are more potent and last longer?
PK?
Admin?

A

Gonadorelin = gonadotropin-releasing hormone
- IV or SC

Goserelin, leuprolide, nafarelin = gondatropin-releasing hormone analogs

  • SC, IM, nasal spray (nafarelin) or as sc implant
  • more potent and longer lasting
18
Q

Gonadotropin releasing hormones and analogs

secretions type?

A

• GnRH binds to GPCRs on gonadotroph cell membranes
• Pulsatile GnRH secretion is required to stimulate release
of LH and FSH
• Sustained nonpulsatile admin. of GnRH inhibits FSH
and LH release (men & women) leading to hypogonadism

19
Q

uses of GnRH analogs:

A

Suppression
Agents are more commonly used for suppression of
gonadotropin release

• Controlled ovarian hyperstimulation (leuprolide,
nafarelin): Critical to suppress endogenous LH surge that
could prematurely trigger ovulation

• Endometriosis (leuprolide, goserelin, nafarelin): Pain
often decreased by abolishing exposure to cyclical changes in estrogen & progesterone concentrations
during menstrual cycle. Treatment limited to 6 months

• Uterine Leiomyomata (fibroids) (leuprolide, goserelin,
nafarelin): Can reduce fibroid size and combined with
supplemental iron can improve anemia

• Prostate Cancer (leuprolide, goserelin): Combined
therapy with continuous GnRH agonist and an androgen
receptor antagonist is effective as castration in reducing
serum testosterone

• Central Precocious Puberty (leuprolide, nafarelin):
Must confirm diagnosis before treatment begins

• Advanced Breast and Ovarian Cancer

• Treatment of Amenorrhea & Infertility in women with
Polycystic Ovary Disease

• Thinning of Endometrial lining: Preparation for endometrial ablation procedure in women with dysfunctional uterine bleeding

Women
• Menopausal symptoms (hot flushes, sweats, headaches)
• Depression, diminished libido, generalized pain, vaginal
dryness & breast atrophy can occur
• Ovarian cysts (generally resolve)
• Reduced bone density & osteoporosis (long treatment)

20
Q

Gonadorelin - AE

A

• Headache, light-headedness, nausea, flushing
• Swelling at SC injection site
• Generalized hypersensitivity dermatitis (long-term admin.)
• Rare acute hypersensitivity reactions
• Sudden pituitary apoplexy & blindness (reported in
patients with a gonadotropin-secreting pituitary tumor)

Men
• Hot flushes, sweats, edema, gynecomastia, decreased
libido, decreased hematocrit, reduced bone density,
asthenia, & injection site reactions

CI: Pregnant and breast feeding women

21
Q

GnRH receptor anatagonist

CA?

A

Cetrorelix, ganirelix = Competitive antagonists of GnRH receptors

Clinical Applications
• Suppression of Gonadotropin Production: Prevent LH
surge during controlled ovarian hyperstimulation

22
Q

Adrenocorticotropic hormone analogs

MOA?

A

Corticotropin, cosyntropin = ACTH analogs
Limited utility as a therapeutic agents (less predictable
and convenient than corticosteroid therapy)
MOA:
• Act via MC2R (GPCR –> increase cAMP) to stimulate adrenal cortex to secrete glucocorticoids, mineralocorticoids and androgen precursor
• ACTH normally released from pituitary in pulses with
highest concentration at ~ 6am and lowest in evening.
Secretion also stimulated by stress
• Cortisol suppresses its release (-ve feedback)

23
Q

Adrenocorticotropic hormone analogs CA?

AE?

A

Clinical Applications
• Diagnostic tool for differentiating between primary adrenal insufficiency (Addison’s disease) and secondary adrenal insufficiency (inadequate ACTH secretion)
• Infantile spasm (West Syndrome) treatment

AE: similar to glucocorticoids

24
Q

Oxytocin - pharmacodynamics?

pK?

A

• Acts on GPCRs –> stimulates release of prostaglandins &
leukotrienes that augment uterine contraction
• Small doses increase force & frequency of contractions
• Higher doses evoke sustained contractions. Weak
antidiuretic & pressor activity (vasopressin R activation)
• Contraction of myoepithelial cells surrounding mammary
alveoli –> milk ejection

Pharmacokinetics
• IV used for initiation & augmentation of labor
• IM used for control of postpartum bleeding
• t1/2 = 5 min

25
Q

Oxytocin CA

A

• Labor Induction: When early vaginal delivery is required
(Rh problems, maternal diabetes, preeclampsia, ruptured
membranes)
• Augment Normal Labor: When labor is protracted or
displays arrest disorder
• Control of uterine hemorrhage

26
Q

oxytocin AE

A

• Severe toxicity is rare
• Excessive stimulation of uterine contractions: Fetal
distress, placental abruption, uterine rupture
• Inadvertent activation of vasopressin receptors:
Excessive fluid retention, water intoxication 
hyponatremia, heart failure, seizures, death
• Bolus injections can lead to hypotension: Administer
IV as dilute solution at a controlled rate

27
Q

oxytocin CI

A
  • Fetal distress
  • Prematurity
  • Abnormal fetal presentation
  • Cephalopelvic disproportion
  • Uterine rupture predisposition
28
Q

OXYCTOCIN ANTAGONIST?

A

ATOSIBAN

- used for treatment of preterm labor (NOT IN US)

29
Q

Desmopressin

A
  • Long-acting synthetic analog of vasopressin
  • Minimal V1 activity
  • Antidiuretic-to-vasopressor ratio 4000 x vasopressin
30
Q

Vasopressin agonistis
PD
PK

A

Vasopressin and desmopressin:

Pharmacodynamics
• 2 GPCRs activated
• V1R = vascular smooth muscle –> vasoconstriction
• V2R = renal tubule cells –> increased water permeability &
water reabsorption

Pharmacokinetics
• Vasopressin: IV, IM (t1/2 = ~15 min)
• Desmopressin: IV, SC, intranasally or orally (t1/2 = 1.5-2.5h)

31
Q

DOCs for Diabetes insipidus

A
  • Vasopressin agonist

• Vasopressin: Esophageal variceal bleeding & colonic
diverticular bleeding
• Desmopressin: Coagulopathy treatment in Hemophilia A
and von Willebrand’s disease

32
Q

Vasopressin agonist AE

A
  • Headache, nausea, abdominal cramps, allergic reactions

* Overdosage = hyponatremia & seizures

33
Q

Vasopressin antagonist

A

Conivaptan
• Approved for use in patients with hyponatremia (due to
elevated vasopressin)
• Conivaptan has high affinity for V1 & V2 R’s

Pharm final (19 decks)

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