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40 Cards in this Set
- Front
- Back
Vasopressin Antagonist
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Conivaptan (Vaprisol®)
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Vasopressin Agonists
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Desmopressin (Stimate ®)
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Vasopressin (ADH-antidiuretic hormone)
2 types |
Lysine
vs Arginine |
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Vasopressin Receptors
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V1a – peripheral smooth muscle. Promotes contraction. Coronary vasospasms.
V1b – Central nervous system. Function unclear. V2 – Located in cortical collecting ducts. Promote synthesis of water channels. |
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Desmopressin (Stimate®) TX
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central diabetes insipidus
bedwetting sleep apnea (tablet, NOT NASEL SPRAY) promote release of VonWillebrand factor for some anemias diagnostic workups to distinguish central and nephrogenic diabetes insipidus |
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Desmopressin (Stimate®) general
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Synthetic vasopressin replacement (modified vasopressin)
Stimulates V2 receptors to promote urine retention Administered nasally, intravenously, or as a tablet. |
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Conivaptan (Vaprisol®) general
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vasopressin receptor antagonist
non-peptide inhibits V1a and V2 subtypes approved for treating hyponatremia from syndrome of inappropriate antidiuretic hormone (SIADH) Causes iatrogenic nephrogenic diabetes insipidus. |
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Adverse Effects: Conivaptan (Vaprisol®)
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Blocks vasopressin receptors in the cortical collecting ducts.
Interferes with insertion of aquaporin channels, that normally promote water reabsorption from the cortical collecting duct. Blockade results in WATER loss. Promotes formation of copius amounts of dilute urine (like the astronauts, deep sea divers). |
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Vasopressin Disorders
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Central Diabetes Insipidus
Nephrogenic Diabetes Insipidus Syndrome of Inappropriate Secretion of Antidiuretic Hormone (SIADH) |
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Central Diabetes Insipidus
causes/Tx/condition |
Condition: reduced pituitary vasopressin production/release
Causes: head trauma, drugs, alcohol, genetic Treatments: Desmopressin (Stimate®) Chlorpropamide (Insulase®)- a sulphonylurea used to treat diabetes mellitus Thiazide diuretics – in diabetes insipidus, sodium excretion seems to trigger water retention. Mechanism unknown. Carbamazepine (tricyclic antidepressant) |
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Nephrogenic Diabetes Insipidus
causes/Tx/condition |
Condition: reduced renal responsiveness to vasopressin
Causes: metabolic, drugs (ie lithium), genetic Treatments: Adequate water intake (replacement) thiazide diuretics – in nephrogenic diabetes insipidus, sodium excretion seems to trigger water retention. Mechanism unknown. Amiloride (Midamor®) (potassium sparing) – Off Label: blocks lithium reabsorption from the cortical collecting tubule to control lithium-induced diabetes insipidus |
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Syndrome of Inappropriate Secretion of Antidiuretic Hormone (SIADH)
condition/cause/TX |
Hormone (SIADH)
Condition: Impaired excretion of water, hyponatremia and hypo-osmolality due to inappropriate elevations in vasopressin. Causes: unclear Treatments: Managed restrictions on water intake Conivaptan (Vaprisol®) to blockV1a and V2 receptors. Available only for parenteral preperation. Lithium – consider if unresponsive to other therapies. DANGER of renal damage after long-term therapy. Demeclocycline (Declomycin®) – Off Label - tetracycline antibiotic that also inhibits V2 receptors. Tolvaptan (Samsca) NOT FDA approved, orally administered vasopressin antagonist. |
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Arginine Vasopressin
from |
Humans, horses, squirrels
|
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Lysine Vasopressin
from |
Hippopotamuses, pigs, Syrian hamsters…
|
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Vasopressin (ADH-antidiuretic hormone
source |
posterior pituatary
|
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Stimulus of ADH
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-increased plasma osmolarity
-hypothalamic input -“volume receptors” (suppress) |
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Effect of ADH
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-vasoconstriction via V1 receptors
-circulates to kidney cortical collecting duct -stimulates renal synthesis of aquaporin (V2 receptors) -permits renal H2O reabsorption -restores plasma osmolarity |
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Vasopressin stimulates “V? receptors” in the cortical collecting tubules.
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V2
|
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V2 receptors drive synthesis of _____ that increase water permeability in the duct.
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aquaporins in CCD
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What? Creates the path for water passage through the collecting tubule.
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aquaporins in CCD
|
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V1a
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peripheral smooth muscle. Promotes contraction. Coronary vasospasms.
|
|
What receptor?
peripheral smooth muscle. Promotes contraction. Coronary vasospasms. |
V1a
|
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V1b
|
Central nervous system. Function unclear.
|
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What receptor?
Central nervous system. Function unclear. |
V1b
|
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V2
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Located in cortical collecting ducts. Promote synthesis of water channels.
|
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What receptor?
Located in cortical collecting ducts. Promote synthesis of water channels. |
V2
|
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What Osmolraity?
Low ADH |
LOW
|
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What Osmolraity?
HIgh ADH |
high
|
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Vasopressin Agonist
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Desmopressin (Stimate®)
|
|
Vasopressin Antagonist
|
Conivaptan (Vaprisol®)
|
|
What drug?
Stimulates V2 receptors to promote urine retention |
Desmopressin (Stimate®)
|
|
What drug?
Administered nasally, intravenously, or as a tablet. |
Desmopressin (Stimate®)
|
|
non-peptide******
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Conivaptan (Vaprisol®)
|
|
inhibits V1a and V2 subtypes
|
Conivaptan (Vaprisol®)
|
|
Causes iatrogenic nephrogenic diabetes insipidus.
|
Conivaptan (Vaprisol®)
|
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Promotes formation of copius amounts of dilute urine (like the astronauts, deep sea divers).******
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Conivaptan (Vaprisol®)
|
|
Conivaptan (Vaprisol®)
Adverse effect:***** |
Hyporvolemia and increased blood osmolarity.
|
|
sodium excretion seems to trigger water retention. Mechanism unknown.*****
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Thiazide diuretics – in diabetes insipidus,and Nephrogenic Diabetes Insipidus
|
|
reduced renal responsiveness to vasopressin
|
Nephrogenic Diabetes Insipidus
Causes: metabolic, drugs (ie lithium), genetic Treatments: Adequate water intake (replacement) thiazide diuretics – in nephrogenic diabetes insipidus, sodium excretion seems to trigger water retention. Mechanism unknown. Amiloride (Midamor®) (potassium sparing) – Off Label: blocks lithium reabsorption from the cortical collecting tubule to control lithium-induced diabetes insipidus |
|
: reduced pituitary vasopressin production/release
|
Central Diabetes Insipidus
Causes: head trauma, drugs, alcohol, genetic Treatments: Desmopressin (Stimate®) Chlorpropamide (Insulase®)- a sulphonylurea used to treat diabetes mellitus Thiazide diuretics – in diabetes insipidus, sodium excretion seems to trigger water retention. Mechanism unknown. Carbamazepine (tricyclic antidepressant) |