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94 Cards in this Set
- Front
- Back
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Name the synthetic GHRH?
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SERMORELIN
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What is the MOA of Sermorelin?
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It is a synthetic GHRH that stimulates Growth hormone release
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What are the clinical uses of GHRH?
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Pituitary Dwarfism treatment
or to determine the cause of short stature |
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What does a lack of GHRH cause?
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-low GH levels
-low IGF-1 levels (liver has no stimulation from GH) |
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Lack of GHRH is a primary, secondary or tertiray cause of GH deficiency?
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TERTIARY
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What are two recombinant forms of GH?
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SOMATREN and SOMATROPIN
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What r some benefits of giving SOMATREN or SOMATROPIN?
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-have slow release and depot preparations
-improve muscle and bone strength -helps in AIDS associated wasting syndrome |
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What inhibits GH release?
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somatostatin and IGF-1
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Where is Somatostatin found?
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CNS
GIT Pancreas |
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How does Somatostatin inhibit GH release?
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Somatostatin inhibits GH release by decreasing cAMP and Ca2+ from the anterior pituitary
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What else does Somatostatin inhibit the release of?
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Insulin
Glucagon Gastrin Thyrotropin |
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Name the Somatostatin analogues.
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OCTREOTIDE and LANREOTIDE
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How r the Somatostatin analogues different?
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They have a longer duration of action
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What's the clinical use of Somatostatin analogues?
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They are used in treatment of
-ACORMEGALY -Carcinoid tumors -Gastrinomas -Glucagonomas |
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What are the A/E of OCTROTIDE and LANREOTIDE?
(somatostation analogue) |
Gallstones and Pancreatitis
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What is the dosage of the Somatostatin analogues?
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20mg every 2hrs for four mths
Tablet form called Sandostatin comes in 10, 20 and 30mg |
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What treatment is used in GH insensitivity of the liver?
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Recombinant IGF-1
MECASERMIN |
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What is the clinical use of MECASERMIN?
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-Laron Dwarfism (GH insensitivity)
-GH deficiency or -Ab against GH |
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What is an A/E of recombinant IGF-1 Mecasermin?
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Can cause DIABETES if abused
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What are the leves of GH and IGF-1 in GH insensitivity?
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Elevated GH and
Low IGF-1 levels |
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Pegvisomant is?
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Competetive antagonist of GH receptor
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How does Pegvisomant work?
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It binds to the GH receptor but DOES NOT increase cAMP and Ca2+
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What is another drug used to treat Acromegaly? (besides somatostatin analogues)
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Pegvisomant
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What causes Acormegaly ?
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Pituitary tumor secreting GH
The tumors can also secrete prolactin |
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What drugs are used to decrease the size of a pituitary tumor?
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Dopamine agonists
BROMOCRIPTINE CABERGOLIDE PERGOLIDE |
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What stimulates GH release?
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Serotonin
Hypoglycemia also insulin induced Hypoglycemia Clonidine |
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What supresses GH release?
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free fatty acids
hyperglycemia IGF-1 |
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What does GH excess cause in kids?
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Gigantism
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What does GH deficiency cause in kids?
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Dwarfism (normal inteligence)
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What hormone level is used to diagnose Acromegaly?
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increased levels of GHor IGF-1
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When is the maximum amplitude of GH?
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at night after deep sleep onset
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What can be used to diagnose ACTH secretion by a pituitary adenoma or adrenal or ectopic tumor?
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CRH
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How is CRH used to diagnose a Primary adrenal tumor?
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Administration of CRH will NOT increase ACTH or cortisol levels
The cortisol produced by the tumor supresses the pituitary response to CRH |
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How is CRH used to diagnose a Pituitary adenoma?
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Administration of CRH will stimulate and acute rise in ACTH and cortisol levels
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How is CRH used to diagnose an Ectopic ACTH-secreting tumor?
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Administration of CRH will NOT increase ACTH or cortisol levels
The cortisol stimulated by the tumor's secretion of ACTH supresses the pituitary ACTH procuction |
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What is an example of an Ectopic ACTH-secreting tumor?
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Small cell carconoma of the lung
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Name the synthetic GnRH
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LEUPROLIDE-a synthetic non-peptide
HISTRELIN NAFARELIN GOSERELIN |
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How is Leuprolide given?
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In pulsatile doses
resembling physiological cycling |
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What is the difference between GnRH analougues and GnRH?
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GnRH has a short half-life
Analogues have long half-lives |
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Which GnRH analogue is adminstrated as a Nasal Spray?
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NAFARELIN
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How is Goserelin administered?
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depot injected 1x per month
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How does the GnRH analogues work?
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They cause Continuous stimulation of the Ant pituitary and lead to down regulation of the GnRH receptors
-This leads to reduction in the release of LH and FSH (gonadotrophins) |
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What is the disadvantage of using GnRH analogues to suppress LH and FSH release?
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The supression does not occur immediately
-There is a transient increase in LH and FSH (flare up) before supression occurs |
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What is used to block this initial flare up?
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FLUTAMIDE
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What is the clinical use of GnRH analogues?
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Used in the treatment of gonadotropin dependent conditions
-Prostate CA -Uterine Fibroids -Endometriosis -Precocious puberty -Cryptorchism |
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What is GnRH used in the diagnosis of?
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Hypogonadal conditions
-Amenorrhea -Infertility |
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Name 3 GnRH antagonists?
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Ganirelix
Cetrorelix Abarelix |
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What is the use of Ganirelix and Cetrorelix?
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Used in controlled ovarian hyperstimulation to avoid multiple pregnancies
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What is the use of Abarelix?
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for Palliative care in
Prostrate CA |
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What is Urofollitropin?
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A glycoprotein purified from post-menopausal women
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What is the use of Urofollitropin
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It is used clinically to provide FSH activity
It stimulates gametogenesis and follicle development in women |
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How is Urofollitropin useful in men?
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It stimulates spermatogenesis in men
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When is Uforfollitropin used?
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To treat infertility in males and females
-to treat hypogonadotropic hypogonadism and assoc. oligospermia |
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What is the major stimulant of gonadal steroid production?
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LH -leutenizing hormone
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What is another function of LH?
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It regulates:
-follicular development and -ovulation |
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Is there any pure preparation of LH available?
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NO
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What other gonadotropin has significant LH effects?
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hCG -human chorionic gonadotropin
Extracted from the placenta |
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hCG is used in?
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Infertility
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MENOTROPIN is a combo of what hormones?
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LH, FSH with added hCG
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Where is Menotropin extracted from?
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Urine of post-menopausal women
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What is the use of Menotropin?
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Used in Hypogonadal states in both males and females
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What is the drug used to assess thyroid function?
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PROTERILIN (TRH)
it tests the abilitiy of the Anterior pit. to secrete TSH NB.TRH stimulates prolactin release |
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How does Prolactin affect Dopamine?
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It increases Hypothalmic Dopamine synthesis and secretion
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How does Dopamine affect Prolactin?
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Dopamine inhibits prolactin secretion
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Name a Dopamine agonist that inhibit prolactin secretion?
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BROMOCRIPTINE
Used in Hyperprolactinemia |
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What can drugs can stimulate Proclatin release?
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Antipsychotics ( used in Schzophrenia)
They are dopamine antagonists They cause hyperprolactinemia |
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What is the effect of too much Prolactin in females?
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-Prolactin interferes with GnRH synthesis and release
-This causes infertility due to failure of Ovulation -decrease in Estrogen production (may lead to risk of Osteoperosis) -Galactorrhea -Amenorrhea is a common symptom TREATMENT- use dopamine agonist to inhibit prolactin secretion BROMOCRIPTINE, CABERGOLINE QUINAGOLINE These drugs can induce ovulation and permit patients with prolactionomas to become pregnant They have NO detrimental effects on fetus |
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What is a Prolactinoma? What are the symptoms?
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A benign tumor in the pit. that secretes prolactin.
Symptoms are due to hyperprolactinemia or by pressure on the surrounding tissues -headache, vision loss -hypogonnadism, infertility, menstrual irregularity -decreased testosterone in men TREATMENT- use dopamine agonist to inhibit prolactin secretion and shrink tumor(e.g BROMOCRIPTINE-ergot derivative given orally) |
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What are the types of Prolactionma?
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Micro - <10mm diameter
Macro - >10mm |
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How is this tumor diagnosed?
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MRI/CT
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Can Dopamine be used in Hyperprolactinemia?
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NO
it has peripheral effects and cannot be given orally Use Bromocriptine, a dopamine agonist Bromocriptine shrinks the tumor and stops lactation. It also inhibits prolactin and GH in Acromegaly |
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Bromocriptine is C/I in what disease?
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Schizophrenia
-It is a stimulant of Dopamine receptors in the CNS |
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What is another Dopamine agonist, that is useful in Parkinsonism?
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Pergolide
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Which drugs are most effective in postpartal or post abortal lactation?
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BROMOCRIPTINE,
CABERGOLINE QUINAGOLINE They also restore sexual potency in males with hyperprolactinemia |
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How does Reserpine contribute to Hyperprolactinemia?
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It depletes dopamine stores in CNS
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What other drugs cause Hyperprolactinemia?
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TCS
Methyldopa amphetamines antidepressants Opioids |
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What is Sheehan's syndrome? What is the Treatment?
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Sheehan's syndrome is decreased functiong of the ant. pit. gland caused by blood loss and hypovolemic shock during and after childbirth.
The gland undergoes necrosis TREATMENT is lifelong hormone substitution medication for pit. insufficiency It includes Estrogen, Progestorone. Thyroid and Adrenal hormones are also advised |
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What are the symptoms of Sheehan's syndrome?
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Fatigue
Anorexia Poor lactation Loss of axillary and pubic hair |
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How would you distinguish primary from secondary HYPOthyroidism?
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Give TSH
It stimulates adenylyl cyclase in the Thyroid gland wich leads to: -stimulation of iodine uptake by the gland -it causes TH synthesis |
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What is Water- House Frederichsen syndrome?
What is the treatment? |
This is a massive hemorrhage that occurs in one or both of the adrenal gland that is commonly caused by menigococcal septicemia
TREATMENT : Ceftrioxone (kills organisms) Benzyl-penicillin used to be the DOC HYDROCORTISONE is ust to reverse the hypoadrenal shock |
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What is the clinical use of ACTH? Name the synthetic analogues.
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ACTH is almost exclusively used to diagnose Adrenal Insufficiency (patients will show no rise in adrenal hormones)
2 Analogues of ACTH: COSYNTROIN TETRACOSACTIDE |
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What is the DOC in infantile spasms?
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ACTH analogue:
TETRACOSACTIDE (mechanism unclear) |
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Where is OXYTOCIN synthesized and stored?
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Synthesized in the Para-ventricular nuclei in the Hypothalmus
Stored at the synaptic boutons of the axons in the Post. pituitary where it is released into circulation |
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What is the action of Oxytocin?
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Stimulates Uterine contraction-used to induce or enhance labour
-Contracts the myoepithelial cells of the breasts-cause milk let down (used as a nasal spray in lactating women) -control postpartal and postabortal bleeding |
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What are the A/E of Oxytocin?
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Hypertensive epiosdes
Uterine rupture |
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Name two synthetic analogues of oxytocin?
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PITOCIN
SYNTOCINON |
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Where is ADH synthesized and stored?
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Synthesized in the Supra-optic nuclei in the Hypothalmus
Stored at the synaptic boutons of the axons in the Post. pituitary where it is released into circulation |
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What 2 receptors does ADH act on ?
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V1 and V2 by cAMP dependent mechainsms
V1 -present on arterioles, mediates vasoconstriction (think V1 like alpha1 receptors soing the same thing) V2 -present in nephrons -stimulate expression of water channels in collecting duct (think V2 for H2O) |
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What stimulates ADH secretion?
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Increased Plasma osmolality -due to presence of osmoreceptors
This causes an antidiuretic effect (retention of water) |
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What are the two effects of ADH?
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Increase water reabsorption
Maintains vascular tone |
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Name a synthetic analogue of ADH.
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DESMOPRESSIN- long acting on V2 receptors only (nasal spray)
Used in Diabetes Insipidus caused by surgery, trauma, or cranial radiotherapy NB - Overdos can lead to volume overload |
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What are the adverse effects of high doses of ADH(Vssopressin)?
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HTN,
Headache, Nausea Abdominal cramps |
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What is the clinical use of ADH (Vasopressin)?
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Used to boost Factor VIII (8) in mild to moderate Hemophillia
Used in bleeding from varices prior to definitive treatment for Portal HTN |
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Well u knw this Lecturer is all over the place
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I hope the cards were'nt.
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