Pharmacology 1 Flashcards

1
Q

What does AVP do to the distal convoluted tubules and collecting ducts?

A

Increases cAMP

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2
Q

What is the result of increased cAMP in the distal convoluted tubules and collecting ducts?

A

Enhances permeability to water and resorption

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3
Q

What does water resorption do to urine volume and osmolality?

A

It reduces urine volume and increases osmolality

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4
Q

True or False: AVP and it’s effects of water resorption should restore DI patients to normal

A

TRUE

Only if it is CENTRAL DI. Nephrogenic DI does not respond to Desmopressin (AVP)

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5
Q

What are 3 other things that AVP can do?

A
  1. Increase vasoconstriction
  2. ACTH and cortisol release
  3. Smooth muscle contraction (some in the gut too)
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6
Q

Will the receptors respond to desmopressin in nephrogenic DM?

A

NO…the receptors are mutated

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7
Q

What 3 effects of neurogenic diabetes insipidus will desmopressin help?

A
  1. Polyuria
  2. Polydypsia
  3. Dehydration
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8
Q

Because of the V1 effect desmopressin has, what is an AE of it?

A

Smooth muscle contractions (vasoconstrictions)

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9
Q

True or False: Desmopressin is a synthetic analog of AVP with a shorter duration of action

A

FALSE… longer duration of action

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10
Q

What type of administration is preferred for desmopressin?

A

Intranasal- Longer action and fewer AE

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11
Q

What are 2 uses for desmopressin other than diabetes insipidus?

A
  1. Nocturnal enuresis
  2. Bleeding with hemophilia A
  3. After pituitary surgery
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12
Q

What are 2 GH analogues?

A
  1. Somatotropin (GH)

2. Somatrem (GH with an extra methionine)

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13
Q

What are the 2 predominant causes of GH deficiency?

A
  1. Diseases of hypothalamus-hypophyseal regions

2. Crainopharyngiomas (mostly due to lack of releaseing factors)

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14
Q

In infants, what 2 things can GH deficiency result in?

A

Hypoglycemia and seizures

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15
Q

What 2 things can lead to a diagnosis of GH deficiency?

A
  1. Growth under 4cm per year

2. Absence of GH response to 2 secretagogues

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16
Q

What is one complication that can arise from GH treatments that requires monitoring?

A

Hypothyroidism

Also cardiac hypertrophy

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17
Q

What are 2 synthetic agonists of somatostatin receptors?

A

Octreotide and lanreotide

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18
Q

What are octreotide and lanreotide used for?

A

Reduce GH production in Acromegalics

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19
Q

What is a GH antagonist?

A

Pegvisomant

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20
Q

What is pegvisomant used for?

A

Acromegaly

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21
Q

How does GH normally work?

A

It binds to 2 dimers fo the GH receptor and both have to be brought in close proximity for the receptor to be activated

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22
Q

What does Pegvisomant due to the GH receptor?

A

It binds to one well, but has reduced affinity for the second site, thus allowing dimerization of the receptor, but blocking the conformational change required for signal transduction

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23
Q

What is DA?

A

A PRL-inhibiting factor (PIF)

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24
Q

What is a DA2 agonist that is used to lower PRL levels?

A

Bromocriptine (an ergot alkaloid)

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25
Q

What is the most common of pituitary cancers?

A

PRL-secreting adenomas

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26
Q

What is used as the initial treatment in PRL-secreting ademonas to reduce tumor size and PRL levels?

A

Bromocriptine

27
Q

What is eventually required for PRL-secreting adenomas??

A

Surgery with or without radiation

28
Q

What is seen in the ovaries of patient with Turners?

A

Absent or rudimentary ovaries

29
Q

What is used to help with Turner’s Syndrome?

A

GH must be combined with gonadal steroids to achieve maximal height effect

30
Q

What receptors are specific to the convulted tubule of the kidney?

A

V2

31
Q

What drug has less V1 activity so it doesn’t increase vascular contraction or release of ACTH like vasopressin?

A

Desmopressin

32
Q

True or False: Desmopressin has longer action than vasopressin for polyuria, polydypsia and dehydration with DI

A

TRUE

33
Q

What 2 places are vasopressin receptors found?

A

Renal tubules and vascular smooth muscle

34
Q

What receptors are on renal tubules?

A

V2

35
Q

At the V2 receptors, what does AVP do?

A

Reduces urine volume and increases urine osmolarity (ANTI-DIURETIC HORMONE)

V2 receptors on Renal Tubules work through Gs receptor —> cAMP —> PKA. This will have a cellular and genomic effect that eventually leads to an increase in Aquaporins in the tubules –> Increased H20 Uptake)

36
Q

At the V1 receptors, what does AVP do?

A

Increase vasoconstriction (AVP on V1 receptors work through the Gq system, so it would raise levels of PLC, PKC, IP3/DAG and Ca++ ultimately leading to smooth muscle contraction.)

V2 receptors on Renal Tubules work through Gs receptor —> cAMP –> PKA. This will have a cellular and genomic effect that eventually leads to an increase in Aquaporins in the tubules –> Increased H20 Uptake)

37
Q

GH acts on membrane receptors via what pathway?

A

JAK-STAT

38
Q

After a few hours, what are the effects of GH?

A
  1. Increase lipolysis

2. Decreased glucose uptake

39
Q

What is released by GH from most tissues?

A

Somatomedins (insulin-like GF)

Mainly synthesized in the liver in response to GH.

40
Q

What do somatomedins do?

A

Increase uptake of sulfate into cartilage and mediate bone growth

(also act in numerous tissues including cardiomyocytes)

41
Q

Before the epiphyseal plates close, GH increases uptake of what 2 things into osteoblasts?

A

Thymidine (DNA)

Uridine (RNA

42
Q

What is a complex of IGFs and the IGF-binding protein what is given in conditions where GH receptor isn’t function or Abs against GH?

A

Mecasermin

43
Q

What is bromocriptine?

A

A synthetic dopamine agonist (ergot alkaloid)

44
Q

What is bromocriptine used for?

A

A variety of hyperprolactinemia syndromes

  1. Infertility
  2. Acromegaly
  3. PRL-secreting pituitary tumors ***
45
Q

What receptors does bromocriptine stimulate?

A

DA2 receptors (associated with psychosis)

46
Q

What if an initial treatment for PRL-secreting adenomas (ammenorrhea-galactorhea) which reduces PRL effectively?

A

Bromocriptine

47
Q

What is a more radical treatment for PRL-secreting Adenmoas?

A

Surgery or irradiation

48
Q

True or False: Bromocriptime can be used alone or in combination with surgery or irradiation for acromegaly?

A

TRUE

49
Q

45,X?

A

Turners Syndrome

50
Q

True or False: Girls with Turners Syndrome have nomral growth hormone (GH) levels, they have reduced responsibeness to GH that often responds to supraphysiologic concentrations of the hormones?

A

TRUE

51
Q

Where is vasopressin produced?

A

PVN, SON, Suprachiasmatic nucleus

along with Neurophysin II

52
Q

Where is vasopressin released from?

A

Neruophypophysis, median eminance, lateral septal nucleus

53
Q

What stimulates Vasopressin release ?

A

Hyperosmotic blood

54
Q

What causes polyuria and polydipsia secondary to an inability to concentrate urine and retain free water?

A

Diabetes insipidus

55
Q

Neurogenic DI versus Nephrogenic DI?

A

Neurogenic: Low AVP secretion
Nephrogenic: Renal insensitivity

56
Q

What 3 things can be used for SIADH?

A
  1. Perfused hypertonic saline plus furosemide
  2. Conivaptan (AVP antagonist) - For hyponatremia
  3. Tolvaptan- Oral
57
Q

How does GH act?

A

Indirect anabolic effects through somatomedins

58
Q

What is a condition where GH levels are too high for a long time?

A

Acromegaly

59
Q

What can acromegaly cause?

A

Frequent CV problems including CAD, ventricular arrhythmias, and CHF (cardiac hypertrophy?)

60
Q

What are 3 things prolactin is involved in?

A
  1. Maternal and sexual behaviors
  2. Induced mitogenesis in lymphocytes
  3. Necessary for milk production in lactating mammals
61
Q

What inhibits PRL release?

A

Dopamine (major catecholamine in brain of tuberoinfundibular origin)

62
Q

So what is DA?

A

PRL-inhibitng factor

63
Q

Bromocriptine stimulates GH in normal people, but does what in acromegalics?

A

Suppresses GH