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850 Exam #4 > Med Chem- Dr. Delfin > Flashcards

Med Chem- Dr. Delfin Flashcards

1
Q

What is Inotropy

A

-Altered contractility

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2
Q

What is lusitropy

A

-Altered relaxation

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3
Q

What is chronotropy

A
  • Altered contraction rate

- SA node conduction

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4
Q

What is dromotropy

A

-Altered AV node conduction

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5
Q

Adrenergic receptors important in treating ADHF and shock

A
  • Alpha 1 (smooth muscle)

- Beta 1 (heart, kidneys)

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6
Q

Alpha adrenergic receptor agonism

A
  • Increases Ca2+ in smooth muscle cells
  • Promotes Actin myosin cross bridging
  • SMC contraction
  • Vasoconstriction
  • Increased BP
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7
Q

Examples of drugs that agonize Alpha 1

A
  • Epinephrine
  • Norepinephrine
  • Dopamine
  • Phenylephrine
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8
Q

Which adrenergic receptor subtype is used to reverse anaphylactic shock with epinephrine

A

-Alpha 1

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9
Q

Which adrenergic receptor subtype is used to reverse cardiac arrest/ asystole with epinephrine

A

-Beta 1

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10
Q

Which Adrenergic receptor subtype is responsible for the reversal of bronchospasm

A

-Beta 2

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11
Q

Beta adrenergic antagonism

A
  • Increases calcium within cardiomyocytes and promotes:
  • negative inotropy
  • Reduces cardiomyocyte contraction
  • Reduces actin myosin cross bridging
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12
Q

Beta adrenergic agonism

A
  • Increases calcium within cardiomyocytes and promotes:
  • Actin myosin cross bridging
  • Cardiomyocyte contraction
  • Positive inotropy
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13
Q

Do alpha and beta adrenergic receptors use the same GPCR mechanism when activated?

A

-NOOO

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14
Q

Drugs that agonize Beta 1

A
  • Epinephrine
  • Norepinephrine
  • Dopamine
  • Dobutamine
  • Isoproterenal
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15
Q

PDEis mechanism of action

A
  • Downstream inhibition of cAMP degradation

- Also promotes activation of this pathway

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16
Q

Milrinone

A
  • PDE3 antagonist
  • Positive inotropy
  • Vasodilator
  • Prevents break down of cAMP
17
Q

Dopamine

A
  • Adrenergic agonist
  • Simplest catecholamine
  • Causes release of NE
  • Low doses activate dopamine
  • Mid to high dose = Beta1
  • Very high dose = alpha 1
18
Q

Which atoms within a functional group can participate in hydrogen bonding?

A
  • Nitrogen
  • Hydrogen
  • Oxygen
19
Q

Norepinephrine

A
  • Is an adrenergic agonist
  • Leading to inotropy and vasoconstriction
  • Potent Beta 1 and alpha1 agonist
  • Weak Beta2 activator
20
Q

Epinephrine

A
  • Adrenergic agonist
  • Inotropy and vasoconstriction
  • Activates: Beta1, Alpha1, and Beta2
21
Q

Dobutamine

A
  • Synthetic

- Beta 1 activation predominates

22
Q

V1Rs

A
  • Located in vascular smooth muscle cells

- Activation causes vasoconstriction and positive inotropy

23
Q

V2Rs

A
  • Located in the kidney
  • AC mechanism
  • cAMP activation causes antidiuresis (aquaporin mediated reabsorption)
24
Q

Does Vasopressin go up or down in hemorrhagic and septic shock?

A
  • Decreases!

- Agonist of VRs

25
Q

Nitric oxide generators

A
  • NO causes vascular smooth muscle relaxation
  • By myosin dephosphorylation
  • Binds to heme of guanylate cyclase
26
Q

Sodium Nitroprusside

A
  • Is a NO donor
  • Reduces preload and after load
  • Promotes vascular smooth muscle relaxation
  • Decreases the work load of the heart
27
Q

Nesiritide

A
  • Recombinant of BNP
  • Produced by the heart
  • Due to excessive stretching of cardiomyocytes
  • Biomarker for heart failure and acute MI
  • Binds to NPRs and promotes vasodilation and diuresis
28
Q

cGMP is key in the activation of what

A
  • Nitroprusside

- Nesiritide

29
Q

A pro-BNP agent used in chronic heart failure treatment is

A

-Sacubitril

30
Q

If epinephrine has already been given, but further vasoconstriction is needed

A

-Milrinone

31
Q

Which signaling pathway does vasopressin work to increase vasoconstriction

A
  • Gq
  • PLC
  • IP3
  • Ca2+ release in vSMC

850 Exam #4 (5 decks)

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