Med Chem- Dr. Delfin Flashcards
What is Inotropy
-Altered contractility
What is lusitropy
-Altered relaxation
What is chronotropy
- Altered contraction rate
- SA node conduction
What is dromotropy
-Altered AV node conduction
Adrenergic receptors important in treating ADHF and shock
- Alpha 1 (smooth muscle)
- Beta 1 (heart, kidneys)
Alpha adrenergic receptor agonism
- Increases Ca2+ in smooth muscle cells
- Promotes Actin myosin cross bridging
- SMC contraction
- Vasoconstriction
- Increased BP
Examples of drugs that agonize Alpha 1
- Epinephrine
- Norepinephrine
- Dopamine
- Phenylephrine
Which adrenergic receptor subtype is used to reverse anaphylactic shock with epinephrine
-Alpha 1
Which adrenergic receptor subtype is used to reverse cardiac arrest/ asystole with epinephrine
-Beta 1
Which Adrenergic receptor subtype is responsible for the reversal of bronchospasm
-Beta 2
Beta adrenergic antagonism
- Increases calcium within cardiomyocytes and promotes:
- negative inotropy
- Reduces cardiomyocyte contraction
- Reduces actin myosin cross bridging
Beta adrenergic agonism
- Increases calcium within cardiomyocytes and promotes:
- Actin myosin cross bridging
- Cardiomyocyte contraction
- Positive inotropy
Do alpha and beta adrenergic receptors use the same GPCR mechanism when activated?
-NOOO
Drugs that agonize Beta 1
- Epinephrine
- Norepinephrine
- Dopamine
- Dobutamine
- Isoproterenal
PDEis mechanism of action
- Downstream inhibition of cAMP degradation
- Also promotes activation of this pathway
Milrinone
- PDE3 antagonist
- Positive inotropy
- Vasodilator
- Prevents break down of cAMP
Dopamine
- Adrenergic agonist
- Simplest catecholamine
- Causes release of NE
- Low doses activate dopamine
- Mid to high dose = Beta1
- Very high dose = alpha 1
Which atoms within a functional group can participate in hydrogen bonding?
- Nitrogen
- Hydrogen
- Oxygen
Norepinephrine
- Is an adrenergic agonist
- Leading to inotropy and vasoconstriction
- Potent Beta 1 and alpha1 agonist
- Weak Beta2 activator
Epinephrine
- Adrenergic agonist
- Inotropy and vasoconstriction
- Activates: Beta1, Alpha1, and Beta2
Dobutamine
- Synthetic
- Beta 1 activation predominates
V1Rs
- Located in vascular smooth muscle cells
- Activation causes vasoconstriction and positive inotropy
V2Rs
- Located in the kidney
- AC mechanism
- cAMP activation causes antidiuresis (aquaporin mediated reabsorption)
Does Vasopressin go up or down in hemorrhagic and septic shock?
- Decreases!
- Agonist of VRs
