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Pituitary
Pharm
117
Medical
Kindergarten
04/27/2010

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Term
What is bromocriptine?
Definition
Dopamine Agonist
Term
What is Cabergolide?
Definition
Dopamine Agonist
Term
What is Octreotide?
Definition
Somastatin Analog
Term
What are Androgen Receptor antagonists used to treat?
Definition
Prostate Cancer
Term
What are the 2 Androgen Receptor Antagonists?
Definition
Flutamide and Bicalutamide
Term
What are some ways endocrine drugs can be used?
Definition
Repair Deficiency, Produce a supraphysiological response, Correct over secretion of hormone, or to test the responsiveness of the endocrine system
Term
The hypothalamus secretes peptides to which gland?
Definition
Pituitary Gland
Term
Where do hormones released from the pituitary act?
Definition
Trophic Tissues
Term
How are levels of circulating hormone controlled?
Definition
Negative Feedback to the hypothalamus or Pituitary
Term
What happens if someone is treated with a synthetic glucocorticoid?
Definition
The endogenous CRH/ACTH/Cortisol secretion pathway is shut down
Term
What are the main endocrine products of the pituitary gland?
Definition
GH, ACTH, TSH, FSH, LH, and Prolactin
Term
What are the main endocrine products of the Hypothalamus?
Definition
GRH, Somatostatin, CRN, TRH, GnRH, PIN (Dopamine), and PRH
Term
What is PRH (Prolactin Releasing Hormone) thought to be composed of?
Definition
TRH and VIP (Vasoactive Intestional Peptide) Combonation
Term
What structural type of pepetide is released from the pitutary gland?
Definition
Peptide Hormones
Term
What structural type of hormone is typically produced by target organs?
Definition
Steroid Hormones
Term
What type of hormone is Insulin and where is it produced?
Definition
Peptide hormone produced by the Beta cells of the pancreas
Term
What type of hormone is Calcitonin and where is it produced?
Definition
Peptide hormone produced by the C cells of the Thyroid Gland
Term
What type of hormone is Somatostatin and where is it produced?
Definition
Peptide Hormone produced all over the body
Term
What are the characteristics of a peptide Hormone?
Definition
Shorter Plasma Half-life, Poorly Bound to Carrier Proteins, Water Soluble
Term
Where are the receptors for peptide hormones located?
Definition
All Peptide receptors are on the outside of the cell
Term
Are Peptide Hormones orally active or bioavailable?
Definition
No they must be administered IM or Subcutaneously
Term
Which peptide hormone can be administered intrnasally?
Definition
Calcitonin
Term
What are some examples of steroid hormones?
Definition
Estradiol, Testosterone, Vitamin D, and Thyroid Hormones
Term
What are some characteristics of Steroid Hormones?
Definition
Long Plasma Half-life, Extensively Bound to Carrier Proteins, Fat Soluble
Term
Where are the receptors located for Steroid Hormones?
Definition
Intracellular Receptors that act in the nucleus, Steroid Hormones easily cross the plasma membrane due to lipid solubility
Term
Once a receptor is bound by a Peptide hormone is the signalling pathway slow or rapid?
Definition
Rapid onset, also rapid off
Term
Once a recpetor is bound by a Steroid Hormone is the signalling pathway slow or rapid?
Definition
Slow onset, cause increase in transcription of specific genes
Term
Are Steroid Hormones orally active?
Definition
Yes, think of Oral Contraceptives
Term
What are the two Single Chain Peptide Hormones?
Definition
Growth Hormone and Prolactin
Term
Which Hormones are Two Chain Peptide Hormones?
Definition
Thyrotropin, FSH, and LH
Term
What is the precursor molecule for ACTH?
Definition
POMC
Term
Is thyrotropin homrone used pharmacologically?
Definition
No
Term
Which Peptide hormones are used for fertility induction?
Definition
FSH and LH
Term
What is another name for GH and where is it produced?
Definition
Somatotropin and the Pituitary Gland
Term
What hormones control the relaese of GH from the Pituitary gland?
Definition
GHRH which increases production and Somatostatin which decreases release, both are products of the hypothalamus
Term
When is GH release increased?
Definition
1 hour after falling asleep and during stress
Term
Why is it hard to test athletes for GH abuse?
Definition
Short Half-life of only 20 minutes
Term
What is the longer acting effect of GH?
Definition
Increases production and release of Insulin-like Growth Factor 1 in the liver
Term
What are the two effects of GH and IGF-1?
Definition
They stimulate the production of cartilage and skeletal muscle, while having an anti-insulin effect resulting in more utilization of fat
Term
WHy would athletes abuse GH?
Definition
Stimulates muscle growth while increases fat loss
Term
What signalling pathway does GH utilize?
Definition
Jak-Stat which activates STAT transcription factors
Term
What Hormone is used to treat reduced muscle mass in Conditions like Turner's Syndrome
Definition
Chronic Kidney DIsease, or Idiopathic Short Stature?,GH
Term
Which hormone is used to treat muscle wasting in AIDS or Burn Patients?
Definition
GH
Term
How is GH administered?
Definition
Subcuatneous, peptide hormones are not orally bioavailiable
Term
What are the side effects of GH?
Definition
Hyperglycemia, Glucosuria, Gyneocomastia, Fluid Rentention so Swollen Feet and Increased ICP
Term
Which hormone can cause gynecomastia?
Definition
GH
Term
What is the hold up on GH treatment?
Definition
Price, Tens of Thousands a year
Term
What is a cheaper alternative to GH?
Definition
Sermorelin Acetate
Term
What is the MOA of Sermorelin Acetate?
Definition
It is a Synthetic form of GHRH, so can stimulate functional Somatotrophs to release GH
Term
When is Sermorelin Acetate not effective?
Definition
When the defect is in the production of GH, but works well when the problem is release
Term
What hormone is important for mammary gland development and lactation during breast feeding?
Definition
Prolactin
Term
When is prolactin production increased?
Definition
During sleep, stress, pregnancy, and with suckling
Term
What does TRH
Definition
VIP, and Estrogen stimulate the release of?,Prolactin by the Pituitary Gland
Term
What hormone prevents Prolaction production in the pituitary gland?
Definition
Dopamine released from the Hypothalamus
Term
Is Prolactin used pharmacologically?
Definition
Nope only applicable due to conditions causing Hyperprolactemia
Term
What are infertile patients first screened for?
Definition
Hyperprolectinemia
Term
Which hormone condition can cause infertility?
Definition
Hyperprolactinemia
Term
What conditions can cause Hyperprolactinemia?
Definition
Pituitary Tumor, Pregnancy, Estrogen replaemement therapy, and Oral Contraceptives that contain Estrogen
Term
If dopamine is is blocked from the pituitary gland what will happen to prolactin levels?
Definition
Increase
Term
Which drugs can block Dopamine causing Hyperprolactenemia?
Definition
Phenzothiazines, Sulpride, Metoclopramide, and Haloperidol
Term
Which drugs can deplete dopamine from nerve terminals causing hyperporlactenimia?
Definition
Reserpine or Alpha Methyl Dopa
Term
A 12 year old is diagnosed with GH deficiency and treated with recombinant GH. The plasma level of what peptide is a senstitive measure of treatment efficacy?
Definition
C. Insulin LIke Growth Factor 1
Term
If Insulin like Growth Factor 1 is administered to an individual
Definition
plasma levels of growth hormone will likely?,C. Decrease: exogenous hormone treatment shuts down endogenous production
Term
What is the main regulator of Prolactin secretion?
Definition
Dopamine blocks Prolactin secretions
Term
What is the treatment for hyperprolactenimia?
Definition
Bromocriptine, dopamine D2 receptor agonist
Term
Why isnt dopamine used to treat hyperprolatimenia?
Definition
Due to its short half life it would have to be constantly infused
Term
What is bromocriptine aderivative of?
Definition
Ergot-alkaloid
Term
What are the two Ergot Derivatives?
Definition
Bromocriptine and Ergonovine
Term
Where does Ergonovine have active effects?
Definition
Stimulates Uterine Contractility
Term
What drug is used to treat hyperprolactenimia and Amenhorrea?
Definition
Bromocriptine
Term
Which drug has weak antagonistic alpha-recpetor activity?
Definition
Bromocriptine will cause postural hypotension
Term
Which drug is used to stop milk production after a miscarriage?
Definition
Bromocriptine
Term
Which drug can reduce the size of a prolactin secreting pituitary tumor before surgery?
Definition
Bromocriptine
Term
How is bromocriptine used in acromegaly due to GH secreting tumors?
Definition
It can decrease the size of the Pituitary tumor
Term
What drug is used to treat Parkinson's Symptoms and has also been shown to improve Type II Diabetes?
Definition
Bromocriptine
Term
What drug can cross the BBB and cause Mental Disturbances
Definition
Hallucinations, and Nightmares?,Bromocriptine
Term
What is Parlodel LA and Cabergoline?
Definition
Bromocriptine alternatives with fewer side effects
Term
What is Octreotide?
Definition
Somatostatin analog
Term
Which hormone decreases GH and TSH secretion?
Definition
Somatostatin
Term
Where is Somatostatin mainly produced?
Definition
GI tract, but some production all over the body
Term
What other effects does Somatostatin have other than decreasing GH and TSH secretion?
Definition
Reduces Gastric Acid Secretion, Gastric Emptying, BIle Flow, and Water Transport
Term
Is somatostain typically inhibitory or stimulatory?
Definition
Inhibitory
Term
How many amino acids compose somatostatin?
Definition
14
Term
Which chain is physiologically active in TSH
Definition
FSH, and LH?,Beta
Term
Which chain of FSH
Definition
LH, and TSH are antibodies made against?,Beta
Term
What is Octreotide?
Definition
Synthetic Somatostatin with a longer half life
Term
What is the half life of Octreotide compared to Somatostatin?
Definition
3-4 Hours instead of 3-4 Minutes
Term
How is Octreotide administered?
Definition
SubCue or IM (microspheres) but is still a peptide so not orally active
Term
What drug is used in the treatment of TSH secreting pituitary tumors?
Definition
Octreotide to reduce the size
Term
What drug is used in carcinoid tumors that cause neuroendocrine hyper-function?
Definition
Octreotide
Term
What is the most common use of Octreotide?
Definition
To treat Diahrrhea, so has a side effect of Constipaiton
Term
What are the side effects of Octreonine?
Definition
Constipation, Hypothyroidism, Sinus Bradycardia
Term
Where is GnRH released?
Definition
From the Hypothalamus in men and women
Term
What hormone stimulates FSH production important for estrogen production?
Definition
GnRH
Term
What hormone stimulates LH secretion important in Testosterone production by Leydig Cells?
Definition
GnRH
Term
How does GnRH have to be realeased from the Hypothalamus in order to assure maximum receptor activity on Gonadotrophs?
Definition
Pulsatile about every 30-60 minutes
Term
What happens if GnRH is secreted in any other pattern than the Pulsatile?
Definition
Initial increas in LH followed by long latent periods without LH due to downregulation of GnRH receptors on Gonadotrophs
Term
What can cause shrunken gonads?
Definition
GnRH hypersecretion or Exogenous Administration wihtout pulsatile administration
Term
What is the Short-Acting GnRH analog given in pulsatile manner?
Definition
Gonadorelin
Term
What is Gonadorelin given in a pulsatile fashion used to treat?
Definition
Hypogonadism, Delayed Puberty, Cryptorchidism, To determine if Pituitary is normally producing LH or FSH
Term
What are the two longer acting GnRH analogs?
Definition
Leuprolide and Goserelin, 25x more active then GnRH
Term
What is the MOA of Leuprolide and Goserelin?
Definition
GnRH Analog that lead to down regulation of LH and FSH receptors and production
Term
What drugs are used to treat prostate cancer
Definition
breast cancer, endometriosis, and LH/FSH infertility?,Leuprolide and Goserelin, Long acting GnRH analogs
Term
What Drugs can cause Hot Flashes
Definition
Loss of Libido, Vaginal Dryness, and an intial Testoterone Surge?,Goserelin and Leuprolide
Term
What drugs produce a chemical castration?
Definition
Goserelin and Leuprolide
Term
What is Degarelix?
Definition
GnRH Anatagonist 4th Generation
Term
What is the main problem with GnRH Antagonist Drugs?
Definition
Cause release of a lot of Histamine leading to hypersensitivity reaction
Term
What is Degarelix used to treat?
Definition
Prostate Cancer
Term
Does a GnRH Antagonist lead to the down regulaiton of LH/FSH receptors?
Definition
No
Term
Hypothalamus releases GnRH whic causes release of?
Definition
LH by the Pituitary Gonadotrophs
Term
LH secretion stimulates?
Definition
Testoterone production from the Testis
Term
Once testosterone is circulatind what can happen?
Definition
It can be 5-alpha Reduced into Dihydrotestosterone which is more potent androgen
Term
Which androgen is given to a man to cause a Negative feedback reduction in LH/FSH production?
Definition
Estrogen
Term
What is estrogen used to treat in male patients?
Definition
Prostate Cancer, Negative Feedback on LH/FSH
Term
What are Flutamide and Bicalutimide?
Definition
Androgen Receptor Antagonists
Term
Which drugs are used to block the testoterone initial flair up caused by GnRH analogs?
Definition
Flutamide and Bicalutamide
Term
Which drug inhibits 5-Alpha-Reductase and prevents the formation of Dihydrotestosterone (more potent form of Testoterone)?
Definition
Finasteride
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