Pharm-Neuroendocrine-Melissa Flashcards by Leah Stalnaker

Release of the following hormones from the hypothalamus will induce/inhibit the release of which hormones from the anterior pituitary:
GHRH, CRH, TRH, GnRH, Dopamine

GHRH--> GH
CRH--> ACTH
TRH--> TSH, PRL 
GnRH--> FSH +LH
DA--> INHIBITON of PRL release

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What are the two hormones released by the posterior pituitary?

oxytocin

- ADH/ vasopressin

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Describe the two negative feedback mechanisms imposed upon hypothalamic/ anterior pituitary system:

Target organ hormone–> Inhibit Pit + hypothalamus

Pit Hormone–> Inhibit hypothalamus

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Which two hypothalamic hormones regulate the release of GH from the anterior pituitary?
What is the function of GH?

GHRH–> ^ Release GH
Somatostatin –> INHIBIT Release GH

GH induces synthesis of IGF-1 which regulates growth

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How do we treat hypothalamic dwarfism; what is deficient in the disease?
What are 4 CI’s for this method of treatment?

Hypothalamic dwarfism = Deficient GHRH
Treat with GH replacement (+ sex hormones at puberty)

CI for GH therapy:

closing epiphyses
over 15 yoa
Inability to make IGF-1 (Laron dwarfism)
active malignancy

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What are the GH preparations used to treat patients with hypothalamic dwarfism? (2)

Somatropin

- Sermorelin

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Somatropin: what is the drug and what does it treat?

How is it administered?

Recombinant DNA match for human GH
Treats hypothalamic dwarfism etc.
Administer SQ 1x/ day

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Sermorelin: what is the drug and what does it treat?

Synthetic GHRH
Formerly used to treat hypothalamic dwarfism etc.
Fell out of favor bc not as effective as direct GH therapy

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List all the uses for GH therapy (6):

hypothalamic dwarfism
turner’s syndrome
prader willi (without obesity or sleep apnea = DEATH)
chronic renal insufficiency
idiopathic short stature
AIDS waisting (anabolic effects)

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Two ADRS associated with GH therapy:

^ ICP early in treatment
diabetogenic effects
Note: kids generally tolerate treatment well

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Human recombinant IGF-1:
Therapeutic use (2)?
How is it administered?
ADRs (2)?

Treat growth problems assts with low IGF-1:

Laron dwarfism (GH-R mutations)
Pts with Abs against GH

Administer SQ 1-2x/day, preferably after meal to avoid hypoglycemia

ADRs:

Hypoglycemia
Lipohypertrophy

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What is the problem with Laron Dwarfism?

Mutant GH-Rs–> Can not make IGF-1

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Excess GH: effects in adults and kiddos

Kiddos: gigantism
Adults: Acromegaly

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What are two somatostatin analogs used to treat ^GH in adults and kids? How do they work? ROA?

PAY ATTENTION TO SPECIAL NOTE REGARDING OCTREOTIDE ON OTHER SIDE OF THIS CARD. CAME FROM RX QUESTIONS!!!!

Octreotide + Lanreotide–>
Somatostatin analogs w longer t 1/2–>
INHIBIT GH secretion + DECREASE IGF-1

Administer SQ

–Special fact about octreotide: it inhibits gastric secretions and vasoconstricts: used to treat carcinoid syndrome!!

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What are some of the ADRs associated with Octreotide and Lanreotide?

GI PROBLEMS: N/V/D/ Abdominal pain

- Gall stones (Decrease biliary cntrxn, GI time)

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What is one possible alternative use for octreotide and lanreotide?

Treat thyrotrope adenomas because they decrease thyrotropin secretion

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Pegvisomant:

MOA, Therapeutic use, ROA, ADRs (2)

MOA:
Competitive GH-R ANTAGONIST–> DECREASE IGF-1
Tx: ^^^ GH
ROA: SQ
ADR: Lipohypertrophy at injection site, Hepatotoxic
**Monitor liver function

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What are 5 problems that can cause excessive prolactin release?

Hypothalamic lesion–> DECREASE DA
Antipsychotic DA-R antagonists
Prolactin secreting pituitary adenoma
Renal insufficiency (decrease breakdown prolactin)
Excess TRH (hypothyroidism)

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Describe the hallmark sx of hyperprolactinemia (4):

amenorrhea
infertility ***
impotence
galactorrhea

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Cabergoline + Bromocriptine:

MOA, Therapeutic use, differences between drugs–which is preferred?

MOA: D1 + D2 AGNONISTS
Tx: Hyperprolactinemia

Differences:

Cabergoline = preferred drug, selective D2 + longer t1/2
Bromocriptine also indicated for acromegaly

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***ADRs asstd. with Cabergoline + Bromocriptine:

N/V/ Dizziness; LESS with cabergoline

- Valvular disease (cabergoline only)

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Which drug do we use to diagnose hypothyroidism?

How do we know if the problem is primary, secondary, or tertiary?

PROTIRELIN: synthetic TRH–> ^ TSH release

^TSH–> ^ T3/T4 = Hypothalamic defect (tertiary)
NO ^TSH–> NO ^ T3/T4 = Pituitary defect (secondary)
^ TSH–> NO ^ T3/T4 = Thyroid defect (primary)

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Cosyntropin:

MOA, Therapeutic use

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MOA: synthetic ACTH analog (^ cortisol release)
Tx: Dx primary vs secondary adrenal insufficiency

Describe the mechanism of GnRH naturally and how that is manipulated by long acting GnRH agents:

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Normal:
PULSITILE GnRH–> FSH + LH release–> ^ E/ P/ T

Long Acting Agents:
CONSTANT GnRH–> DECREASE # GnRH-R’s–>
DECREASE FSH + LH release–> DECREASE E/ P/ T

How does hCG work to ^ fertility?

mimics actions od LH--> | ^ female ovulation (LH surge) + ^ male external sexual development (^ T)

What are the indications for hCG therapeutic use? (2)

- stimulating ovulation in women | - threat male infertility and cryptorchidism

Menotropins (hMG) What are the active components in these drugs? What are the two therapeutic uses?

- Contain equal LH and FSH - treats female infertility (^ follicular dvlpmt.) - ^ male spermatogenesis

Urofollitropin: What is the active component of this drug? What are the two therapeutic uses?

- Menotropin with most of LH removed; ^ FSH - treats female infertility (^ follicular dvlpmt.) - ^ male spermatogenesis

What are the gonadotropin mimicking drugs (2)? | What is their MOA and what are they used to treat?

Follitropin beta + alpha (recombinant FSH) - use like urofollitropin ``` Choriogonadotropin alpha (recombinant LH) - use like hCG ```

What are some ADRs associated with gonadotroipins? (3)

- multiple births - ovarian hyperstimulation syndrome - gynecomastia (^E)

What is ovarian hyper stimulation syndrome?

Leaky ovarian capillaries cause fluid to fill abdominal cavity --> painful abdomen

**Chlomiphene: MOA Therapeutic uses ADRS

MOA: Estrogen receptor ANTAGONIST--> INHIBIT E negative feedback to hypothalamus--> ^ LH + ^ FSH--> ^ fertility Therapeutic uses: - Infertility due to ovulatory disorder i.e. PCOS ADRs: - multiple births - antiestrogenic effects (endometrium, ovarian cysts, developing follicle)

Gonadorelin: MOA, therapeutic use?

- Synthetic GnRH - Administered via pump--> ^ endogenous FSH +LH - Treats infertility in females

Leuprolide, Goserelin, Nafarelin, Histrelin: | MOA, Dosing regimine?

Long acting Synthetic GnRH AGONIST MOA: DOWNREGULATES GnRH-R + INHIBIT GnRH Secretion Dosing: Admin continuously for 2-4 weeks

``` Leuprolide, Goserelin, Nafarelin, Histrelin: Therapeutic uses (4)? ```

Long acting Synthetic GnRH AGONIST - Endometriosis - Uterine fibroids - Prostate and breast cancers - Precocious puberty

Leuprolide, Goserelin, Nafarelin, Histrelin: ADRs?

Long acting Synthetic GnRH AGONIST: Problems with too low E and T... (like in menopause) 1. Hot flashes, vaginal atrophy 2. osteoporosis 3. erectile dysfunction

Flutamide + Bicalutamide: | MOA, Therapeutic use

MOA: Androgen receptor ANTAGONISTS Therapeutic use: * **Combo treatment with long acting GnRH analogs - Treats metastatic prostate disease

Why should Flutamide + Bicalutamide not be administered alone?

^ LH synthesis due to DECREASED testosterone mediated negative feedback--would ultimately lead to INCREASE in Testosterone production

Flutamide + Bicalutamide: ADRs

BLACK BOX: Reversible Hepatotoxicity; check liver function prior to use

Finasteride: | MOA, Therapeutic use?

MOA: 5-a reductase inhibitor; STOP T--> DHT Therapeutic use: BPH, prostate cancer, male pattern baldness

Describe the difference between central and nephrogentic DI-- How are the two diagnosed?

Central: inadequate ADH - synthetic vasopressin = INCREASE urine osmolality Nephrogentic: Kidneys fail to repsond to ADH - synthetic vasopressin NO EFFECT ON urine osmolality

What are two HIGH yield causes of nephrogenic DI?

LITHIUM + Dimiclocyclin!!

What are the symptoms of DI (both types)?

- polyuria and polydipsia | - dilute urine

Desmopressin: | MOA (3), therapeutic use (3)?

MOA: - Exogenous vasopressin w REDUCED (V1) vasopressor activity and INCREASED (V2) antidiuretic effects - ^ factor VIII - ^ VWF Therapeutic use: - CENTRAL DI - von Willibrand disease type1 - primary nocturnal enuresis

What are 3 of the ADRs associated with vasopressive therapy; with which drug are they worse?

- Facial pallor - ^GI motility (N/Cramping) - OVERSTIMULATION of V2 receptors--> H2O toxicity **Note that ADRs are worse with vasopressin than desmopressin

***How do Lithium and Demeclocycline cause nephrogenic DI?

Lithium + Demeclocycline--> INHIBIT V2-Rs in collecting duct! 1/3 of all patients on lithium will get this!!!

How do we treat/ prevent lithium induced nephrogenic DI? | What is the MOA here?

Administer AMILORIDE--> | BLOCKS Li+ uptake at the Na+ channel in the collecting duct--> reverse/ inhibit V2 effects

Amiloride: therapeutic use?

Treat nephrogenic DI induced by Lithium

What are three treatments used for nephrogenic DI?

- ^ H2O intake - Administer THIAZIDE diuretics - Na+ restriction

What is SIADH/ how does it present? | What 4 drug causes?

^^^ ADH--> hyoposmolality and hyponatremia Patients present with lethargy, N/V, cramping, convulsion, death 4 drug causes: - SSRI - TCA - Sulfadrugs - vinka alkaloids

Which tetracycline antibiotic is used to treat SIADH and how does it work?

Demeclocycline--> Inhibits vasopressin actions on collecting duct

What are the two vaptan drugs? | How do they work and what do they treat?

Conivaptan (V1 + V2 ANTAGONIST) Tolvaptan (V2 ANTAGONIST) Therapeutic Use: Euvolemic and hypervolemic hyponatremia asstd. with SIADH

What are the three methods used to treat SIADH?

- fluid restriction +/- hypertonic saline +/- loop diuretics - demeclocycline - vaptans

What are the therapeutic uses for pharmacologic oxytocin (4)? Describe the ROA for each use.

- abortion - induction of labor (IV) - postpartum hemorrhage (IM) - induction of lactation (intranasal)

What are 2 ADRs associated with synthetic oxytocin use?

- excessive uterine contraction--> harm mom and newborn | - water intoxication due to ^ resorption (has ADH effects)

Pharm-Neuroendocrine-Melissa Flashcards

(55 cards)