Neuroendo Pharm Flashcards

1
Q

Releasing hormones from the hypothalamus and hormones from adenohypophysis

A

GHRH–GH

CRH–ACTH

TRH–TSH

GnRH–FSH

GnRH–LH

TRH–PRL

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2
Q

Hormones from the neurohypophysis (posterior pituitary)

A

ADH

oxytocin

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3
Q

Hypothalamic dwarfism

A

Treat with GH replacement

Doesn’t work in bone age >15 (closed epiphyses)

Doesn’t work in pts that cant make IGF1

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4
Q

GH preparations

Somatropin

A

Exact match with HGH

Administered in evening (1/day) mimics when GH is normally elevated

If GH is low and works then give recombinant to restore growth

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5
Q

Sermoreline

A

Synthetic GHRH

No longer used

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6
Q

Additional uses of GH

A

Reduced size or growth but not very sensitive to GH

Turner’s syndrome

Prayer-willi

Chronic renal insufficiency

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7
Q

GH therapy

Side effects

A

Inc ICP

Diabetogenic

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8
Q

Human recombinant IGF-1

A

Treat growth deficiency due to IGF-1 (cant use GH)

Laron Dwarfism! Mutation in GH receptor

ADR: hypoglycemia and lipohypertrophy: give before or after meal

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9
Q

Laron Dwarfism

A

Mutations in GH receptor

Rx: human recombinant IGF-1

GH doesnt work!!!

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10
Q

Xs GH

Due to

A

GH secreting adenoma

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11
Q

Xs GH

Can cause

A

acromegaly in adults and gigantism in children

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12
Q

Tx acromegaly in adults and gigantism in children

A

Somatostatin analog

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13
Q

Octreotide and lanreotide

A

Somatostatin analog

Longer acting

Inhibit GH secretion (red levels of IGF1)

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14
Q

Octreotide and lanreotide

ADR

A

GI: diarrhea, nausea, abdominal pain

Slow gall bladder–gallstones

Dec thyrotopin (used for thyrtrope adenoma)

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15
Q

Pegvisomant

A

Used when can’t handle somatostatin analog

Competitive GH receptor antagonis, reduces levels of IGF-1

2nd line

ADR: monitor liver fxn, lipohypertrophy at injection site

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16
Q

Hyperprolactinemia

Results in

A

Infertility

suppresses GnRH (and then FSH and LH)

Due to dec dopamine (lesion in hypothalamus)

Or pituitary adenoma

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17
Q

Hyperprolactinemia

Sx

A

Amenorrhea, galactorrhea and infertility and impotence

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18
Q

Hyperprolactinemia

Rx

A

Dopamine receptor agonists

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19
Q

Cabergoline and bromocriptine

A

Stimulate dopamine D2 receptors to inhibit spontaneous and TRY induced release of prolactin

Cabergoline: preferred, longer half life and greater D2 selectivity

Bromocriptine also for acromegaly

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20
Q

Cabergoline and bromocriptine

ADR

A

ADR more prominent in bromocriptine

Induce nausea

Hypotension and dizziness

cabergoline: linked to valvular disease

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21
Q

Protirelin

A

TRH analog synthetic

Diagnostic analog for hypothyroidism
(Tell what level lesion is at hypothalamus, pituitary, thyroid)

Low T4, T3

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22
Q

Cosyntropin

A

ACTH synthetic analog

Diagnostic: determine primary (adrenal gland doesn’t respond) vs secondary adrenal insufficiency

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23
Q

HCG

A

Gonadotropin mimic drug

Placental hormone

Mimics action of LH (promotes ovulation and ext sex development in males:: inc testosterone)

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24
Q

HCG

Use

A

Stimulate ovulation in anovulatory women and treat male infertility and cryptorchidism

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25
Q

Menotropins

A

Gonadotropin mimic drugs

Human menopausal gonadrotropins (urine extract)

Equal amounts partially degraded FSH and LH

For infertility to development of ovarian follicles

Drives spermatogenesis

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26
Q

Urofollitropin

A

Gonadotropin mimic drugs

Pull out LH leaving FSH (allows timing ovulation)

Similar to mentropins

27
Q

Follitropin beta and alpha

A

Recombinant FSH

28
Q

Choriogonadotropin alpha

A

Recombinant LH

29
Q

Gonadotropins

ADR

A

Risk for multiple births

Ovarian hyperstimulation syndrome: ovarian cysts, ascites, hypotension (sore abdomen, nausea, fever):: stop tx

Males: gynecomastia

30
Q

Clomiphene

A

Estrogen receptor antagonist

Inc gonadotropin secretion and ovulation

31
Q

Clomiphene

Use

A

Infertility due to polycystic ovary syndrome, manifests with irregular menstrual periods, infertility, hirsutism, xs anadrogens

32
Q

Clomiphene

MOA

A

Inc levels of LH and FSH by inhibiting estrogen negative feedback at level of hypothalamus

33
Q

Clomiphene

ADR

A

Multiple births

Antiestrogenic effects on developing follic, ovarian cysts endometrium and cervical region

34
Q

Gonadorelin

A

LH and FSH stimulant

Synthetic GnRH

Given via pump to mimic endogenous GnRH release

35
Q

Leuprolide, goserelin, nafarelin and histrelin

A

Anti estrogen and anti androgen drugs

Long acting synthetic GnRH agonists

Down regulates receptor (no pulses)

Subs at pos 6 (resistance to proteolysis) and c terminus (for receptor binding)

36
Q

Leuprolid, goserelin, nafarelin and histrelin

What happens

A

Transient stimulation of gonadotropin secretion

Then down regulate GnRH receptor and inhibit gonadotropin secretion

Reduces estrogen and testosterone

37
Q

Leuprolid, goserelin, nafarelin and histrelin

Uses

A

Endometriosis

uterine fibroids, advanced prostate cancer, breast cancer, central precocious puberty

38
Q

Leuprolid, goserelin, nafarelin and histrelin

ADR

A

Hot flashed, dec bone density, vaginal dryness, ED

39
Q

Flutamide, bicalutamide

A

Androgen receptor antagonist

Prevent testosterone and androgen binding

Red effects of androgens at level of prostate tumor

40
Q

Flutamide, bicalutamide

Effect and Given with

A

Blocking receptor, inc LH, then inc testosterone

Give with leuprolide to shut down feed back and block this

41
Q

Flutamide, bicalutamide

ADR

A

Liver damage

42
Q

Finasteride

A

5a-reductase inhibitor

Blocks conversion of testosterone to dihdrotestosterone

Prostate tissue shrinks (BPH)

43
Q

DI

Due to

A

Central defect: low ADH

Nephrogenic: kidney doesn’t respond to ADH

44
Q

Central DI

Due to

A

Surgical or traumatic head injury near hypothalamus of pituitary

Hypothalamic or pituitary tumors

CNS ischemia

Brain infxn

45
Q

Nephrogenic DI

Due to

A

Congenital or acq.

Hypercalcemia, hypokalemia

Postobstructive renal failure

Li!!!! For bipolar. 1 in 3 gets this

46
Q

DI

Sx

A

Polyuria, polydipsia, dilute urine

47
Q

DI

Dx test

A

Administration of synthetic vasopressin

If it induces inc in urine osmolality then central DI

If no effect on urine osmolality then nephrogenic DI

48
Q

Desmopressin

A

For central DI

Synthetic analogue of ADH

Reduced vasopressin activity, but enhanced anti diuretic activity

49
Q

Desmopressin

Other use

A

For Von willebrand disease type 1 (inc factor VIII and Von willebrand factor)

Primary nocturnal enuresis

50
Q

DI

ADR

A

Vasopressin activity due to activation of V1 (facial pallor, inc in GI and nausea, constriction of coronary aa

Overstimulation of V2 results in water intoxication

V1 hit by vasopressin not so much by desmopressin

51
Q

DI

Drug interactions

Chlorpropamide and carbamazepine

A

Inc the sensitivity of collecting duct to vasopressin

52
Q

DI

Drug interactions

Li and demeclocycline

A

Inhibit action of vasopressin on collecting duct

Li: AS MANY AS ONE IN 3 DEVELOP NEPROGENIC DI!

Li: disrupts cAMP

53
Q

Tx of nephrogenic DI

A

Adequate water intact: thiazide. Diuretics

Front line therapy

Reduce urine volume by 50%

54
Q

Nephrogenic DI

Tx

Thiazide

MOA

A

Water contraction sensed by nephron

Shifts water reabsorption to PCT

55
Q

Neprhogenic DI

Amiloride

A

Blocks li uptake by na channel in collecting duct

Counters li induced nephrogenic DI

56
Q

SIADH

A

Malignancy (lung)

CNS

Drugs (ssri, tricyclics antidepressants, sulfonylureas

57
Q

SIAH

Sx

A

Plasma hypotonicity,letargy, anorexia, nausea

58
Q

SIADH

Rx

A

Fluid restriction!

Demeclocyline: antagonizes xs ADH

Conivaptan: V1 and V2 receptor antagonist

Tolvaptan: V2 receptor antagonist

59
Q

SIDH

Other Rx

A

Hypertonic saline

Loop diuretics

60
Q

Oxytocin

Uses

A

For hemorrhaging

Facilitate Milk ejection

Induction of child birth

61
Q

Synthetic oxytocin

ADR

A

Overstimulation: trauma to mother or fetus, uterine rupture, water intoxication and allergic runs

62
Q

Oxytocin

Preparations

A

Synthetic oxytocin

IV: induce labor

IM: control post abortion hemorrhage

Intranasal: induce lactation

63
Q

Nephrogenic DI

Caused by what drug

A

Li

64
Q

Li can cause what?

A

Nephrogenic DI