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PHCOL 401 > 11.20.17 Vasopressin & Oxytocin > Flashcards

11.20.17 Vasopressin & Oxytocin Flashcards

1
Q

Vasopressin
Targets (3):
Principal action (3):

A

Vasopressin
Targets (3): kidney, blood vessel, anterior pituitary
Principal action (3): Water retention, vasoconstriction, ACTH release

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2
Q

Oxytocin
Targets (2):
Principal action (2):

A

Oxytocin
Targets (2): Uterus, mammary
Principal action (2): Contraction of smooth muscle, alveoli

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3
Q

Vasopressin (ADH) main function is to conserve water by reducing ______ output, regulate kidney ______ production and trafficking.

A

Vasopressin (ADH) main function is to conserve water by reducing urine output, regulate kidney aquaporin production and trafficking.

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4
Q 
V1 receptors
-G protein-coupled, \_\_\_\_\_ receptor system
Describe its effect on:
-vascular smooth muscle
-liver \_\_\_\_\_\_\_\_\_\_\_
-\_\_\_\_\_\_\_ release
-\_\_\_\_\_\_\_ synthesis
A 
V1 receptors
-G protein-coupled, phosphatidyl inositol (IP3) receptor system
Describe its effect on:
-vascular smooth muscle
-liver glycongenolysis
-ACTH release
-Prostaglandin synthesis
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5
Q

V2 receptors:

  • G protein-coupled _____ receptor system
  • Increases water resorption in the kidney by increasing water permeability of ______ channels in renal luminal membranes
A

V2 receptors:

  • G protein-coupled adenylyl cyclase (cAMP) receptor system
  • Increases water resorption in the kidney by increasing water permeability of aquaporin-2 channels in renal luminal membranes
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6
Q

Vasopressin binds receptors in ____ or ____ of the kidney. It promotes the reabsorption of water. The tubules are impermeable to _____ without vasopressin.

A

Vasopressin binds receptors in distal or collecting duct of the kidney. It promotes the reabsorption of water. The tubules are impermeable to water without vasopressin.

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7
Q

Vasopressin stimulates insertion of “water channels” or _______ into the membranes of kidney tubules. Insertion results in transport of solute-free water through tubular cells and into blood:

  • _______ in plasma osmolarity
  • _______ in urine osmolarity
A

Vasopressin stimulates insertion of “water channels” or aquaporins into the membranes of kidney tubules. Insertion results in transport of solute-free water through tubular cells and into blood:

  • decrease in plasma osmolarity
  • increase in urine osmolarity
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8
Q

Kidneys express aquaporin __ and __.

A

Kidneys express aquaporin 2 and 3.

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9
Q

Aquaporin-3: resides constitutively on the ________, allows water to flow out of the cell after entering _____ channels

A

Aquaporin-3: resides constitutively on the basolateral membrane, allows water to flow out of the cell after entering aquaporin-2 channels

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10
Q

Aquaporin-2: regulated by V2R stimulated cAMP, is a target for cAMP mediated ____ phosphorylation. Vesicles containing aquaporin-2 fuse to _____ when the cell is stimulated by vasopressin.

A

Aquaporin-2: regulated by V2R stimulated cAMP, is a target for cAMP mediated PKA phosphorylation. Vesicles containing aquaporin-2 fuse to apical membrane when the cell is stimulated by vasopressin.

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11
Q

_____ takes up water from lumen, ____ facilitates its movement into the blood.

A

AQP2 takes up water from lumen, AQP3 facilitates its movement into the blood.

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12
Q

Vasopressin causes _____ in blood pressure by contraction of small arteries, in healthy individuals this effect is _____.

A

Vasopressin causes an increase in blood pressure by contraction of small arteries, in healthy individuals this effect is minimal.

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13
Q

Vasopressin receptors are widely dispersed in _____ regions. It cannot cross the ____. It can promote _____ in rodents and has been implicated in _____ formation.

A

Vasopressin receptors are widely dispersed in brain regions. It cannot cross the BBB. It can promote social recognition in rodents and has been implicated in memory formation.

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14
Q

V1R antagonists may have ___ and ____ actions.

A

V1R antagonists may have anti-anxiety and anti-depressant actions.

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15
Q

Hypothalmic osmoreceptors detect plasma ____.

  • Dehydration results in _____ secretion
  • Overhydration results in _____ secretion
A

Hypothalmic osmoreceptors detect plasma osmolarity.

  • Dehydration results in increased secretion
  • Overhydration results in decreased secretion
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16
Q

Other factors that increase secretion of ADH are decreases in _____ and ____, sensed by stretch receptors in heart and large arteries. Not as

A

Other factors that increase secretion of ADH are decreases in BP and volume, sensed by stretch receptors in heart and large arteries.

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17
Q

Decreases in blood pressure and volume are (more/less) sensitive as increases in osmolarity. Loss of 15-20% of blood volume results however in massive secretion of vasopressin.

A

Decreases in blood pressure and volume are (less) sensitive as increases in osmolarity. Loss of 15-20% of blood volume results however in massive secretion of vasopressin.

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18
Q

Another stimulus of vasopressin is ____ and ____ which are controlled by regions in the brain with links to the hypothalamus.

A

Another stimulus of vasopressin is nausea and vomiting which are controlled by regions in the brain with links to the hypothalamus.

19
Q

Vasopressin dysregulation results in two forms of diabetes insipidus, describe:

A
  1. Neurogenic diabetes insipidus: deficiency in secretion of vasopressin, causes varied (head trauma, infections/tumors of hypothalamus, genetic mutations to the vasopressin gene)
  2. Nephrogenic diabetes insipidus: kidney unable to respond to vasopressin, common cause is renal disease, less common is mutations in the vasopressin receptor gene or AQP2 gene
20
Q

A major symptom of diabetes insipidus is _______, diagnosis and treatment must differentiate from polydipsia. Rarely life-threatening if adequate water is available.

A

A major symptom of diabetes insipidus is excessive urine, diagnosis and treatment must differentiate from polydipsia. Rarely life-threatening if adequate water is available.

21
Q

Syndrome of inappropriate antidiuretic hormone (SIADH) is characterized by _____. It can lead to ___ and ___. Causes may include CNS injuries/malignancies, psychotropic drugs (haloperidol, TCA, vinca alkaloids, sulfonylureas).

A

Syndrome of inappropriate antidiuretic hormone (SIADH) is characterized by excessive release of vasopressin. It can lead to hyponatremia and hypoosmolality. Causes may include CNS injuries/malignancies, psychotropic drugs (haloperidol, TCA, vinca alkaloids, sulfonylureas).

22
Q

Vasopressin treats (4):

A
  • neurogenic diabetes insipidus
  • acute bleeding d/t esophageal varices or colonic diverticula
  • CPR, as first line alternative to epinephrine, also in v-fib with epinephrine.
  • vasodilatory shock
23
Q

Desmopressin is degraded (faster/slower) than vasopressin, and has ___ effect on BP.

A

Desmopressin is degraded (slower) than vasopressin, and has little effect on BP.

24
Q

Desmopressin treats (4):

A
  • neurogenic diabetes insipidus
  • nocturnal enuresis
  • hemophilia A (VIII deficiency)
  • von Willebrand syndrome (I and IIa only)
25
Q

Treatment is cautioned in conditions aggravated by _____. Also in patients with ________.

A

Treatment is cautioned in conditions aggravated by water retention (heart failure, hypertension, intracranial pressure, renal failure, elderly). Also in patients with cystic fibrosis.

26
Q

Avoid in cardiac insufficiency and conditions treated with _____, or patients with vascular disease due to ______.

A

Avoid in cardiac insufficiency and conditions treated with diuretics, or patients with vascular disease due to vasoconstriction.

27
Q

In renal impairment, treatment will be (more/less) effective and excreted (quickly/slowly)

A

In renal impairment, treatment will be (less) effective and excreted (slowly)

28
Q

Avoid use in _____ due to _____ effect in the third trimester.

A

Avoid use in pregnancy due to oxytocic effect in the third trimester.

29
Q

_____ block prostaglandin synthesis in kidneys and (antagonizes/enhances) vasopressin action.

A

NSAIDs block prostaglandin synthesis in kidneys and (enhance) vasopressin action.

30
Q

_____ causes polyuria and acts as an (agonist/antagonist) to vasopressin.

A

Lithium causes polyuria and acts as an (antagonist) to vasopressin.

31
Q

Describe demeclocycline’s MOA.

A

Demeclocycline antagonizes vasopressin actions on kidney downstream of V2R.

32
Q

What class of drug is conivaptan, tolvaptan, lixivaptan? Which are specific?

A

V1a/V2R antagonist: conivaptan

V2R specific antagonist: tolvaptan, lixivaptan

33
Q

Vasopressin receptor antagonists could be useful for _____ associated with (3):

A

Vasopressin receptor antagonists could be useful for hyponatremia associated with (3):

  • SIADH
  • CHF leading to edema
  • cirrhosis-induced edema
34
Q

Oxytocin is involved in the contraction of _____ and ____.

A

Oxytocin is involved in the contraction of uterine muscles and mammary alveoli.

35
Q

Oxytocin is increased in ______ during birth. _______ of an infant stimulates release of oxytocin during feeding.

A

Oxytocin is increased in cerebrospinal fluid during birth. Continued suckling of an infant stimulates release of oxytocin during feeding.

36
Q

Oxytocin secreted from the pituitary can’t re-enter the brain because of the BBB. Effects of oxytocin are due to release from _______.

A

Oxytocin secreted from the pituitary can’t re-enter the brain because of the BBB. Effects of oxytocin are due to release from centrally projecting hypothalamic neurons.

37
Q

Oxytocin acts through the oxytocin receptor–>G protein-coupled _____ receptor–>mobilization of ____, leading to increased ____ & ____ smooth muscle contraction

A

Oxytocin acts through the oxytocin receptor–>G protein-coupled IP3 receptor–>mobilization of Ca2+, leading to increased uterine & mammary smooth muscle contraction

38
Q

Sensory input from environment–>CNS (______)–>______ releases oxytocin–>target glands (_____ & _____)–>contraction.

How does positive feedback regulate oxytocin secretion?

A

Sensory input from environment–>CNS (hypothalamus)–>posterior pituitary releases oxytocin–>target glands (uterine & mammary smooth muscle)–>contraction.

Contraction positively feeds back to the hypothalamus

39
Q

Oxytocin secretion is sensitive to ______. Oxytocin neurons are repressed by catecholamines.

A

Oxytocin secretion is sensitive to acute stress. Oxytocin neurons are repressed by catecholamines.

40
Q

Production of oxytocin and response to it are modulated by circulating levels of _______. Increase in uterine oxytocin receptors late in gestation results from increase in circulating _____. Burst of oxytocin at birth is triggered by declining ____.

A

Production of oxytocin and response to it are modulated by circulating levels of sex steroids. Increase in uterine oxytocin receptors late in gestation results from increase in circulating estrogen. Burst of oxytocin at birth is triggered by declining progesterone.

41
Q

_______ degrade oxytocin in a variety of tissues: ____ is produced in the placenta and appears in maternal plasma during pregnancy, It is thought to protect against premature uterine contractions.

A

Enzymes degrade oxytocin in a variety of tissues: oxytocinase is produced in the placenta and appears in maternal plasma during pregnancy, It is thought to protect against premature uterine contractions.

42
Q

Carbetocin, demoxytocin

A

Class: Synthetic oxytocin analogs
Form: IM/IV, does not cross BBB (destroyed in GI)
TX: induce labor and support labor in case of non-progession of birth

43
Q

Ergometrine

A

*prep of ergot, chemically similar to LSD, can be combined with oxytocin as syntometrine
MOA: smooth muscle in blood vessels narrowing, reduces blood flow.
TX: facilitate delivery of placenta and prevent bleeding after childbirth

44
Q

Misoprostol

A

Class: prostaglandin E1 analog
MOA: causes uterine contractions and ripening of cervix
TX: induce labor (more effective than other drugs for labor induction–cervix may not be ripe), nonsurgical abortions

PHCOL 401 (14 decks)

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