Adrenergic pharmacology DSA
What drug class is phenylephrine (Neo-Synephrine) and clonidine (Catapres)? - answer
alpha agonist
Which receptors does phenylephrine act on? - answer alpha 1 > alpha 2 >>>>> ß
Which receptors does clonidine act on? - answer alpha 2 > alpha 1 >>>>> ß
What drug class is Norepinephrine (Lavished) and Epinephrine (Adrenalin)? - answer
mixed alpha and beta agonist
Which receptors does norepinephrine act on? - answer- alpha 1 = alpha 2
- ß1 >> ß2
Which receptors does epinephrine act on? - answer alpha 1, alpha 2, ß1, ß2 equally
(least selective Adreno mimetic)
What drug class is Dobutamine (doubter), Isoproterenol (Isuprel), and Albuterol (Proair,
Proventil, Ventolin)? - answer Beta agonist
Which receptors does dubutamine act on? - answerß1 > ß2 >>>> alpha
Which receptors does Isoproterenol act on? - answerß1 = ß2 >>>> alpha
Which receptors does albuterol act on? - answerß2 >> ß1 >>>> alpha
What class of adrenomimetic are alpha, beta, and mixed agonists? - answerdirect
acting
What drug class is Cocaine? - answer- Dopamine (DA) and NE re-uptake inhibitors
- Indirect adrenomimetics
What drug class is Selegiline (Eldepryl) and Phenelzine (Nardil)? - answer- Monoamine
oxidase (MAO) inhibitors
- indirect adrenomimetics
What drug class is Amphetamine, Methylphenidate (Ritalin), and Tyramine? - answer-
Reverse NE and DA uptake mechanisms and releasing agent (enhance release)
- indirect adrenomimetics
, What is the drug class and action of Ephedrine? - answer- releasing agent (enhance
release) as well as a direct acting
- indirect adrenomimetic
Which nervous system do adrenergic drugs act on? - answersympathetic bc adrenergic
R primarily located at target organs innervated by post-ganglionic N. of SNS.
Define adrenomimetics (aka sympathomimetics)
Define antiadrenergic drugs (aka sympatholytics) - answerdrugs that act on adrenergic
R. to mimic effects of endogenous NTs/hormone
drugs that inhibit/prevent effects of endogenous NTs/hormone
Which endogenous neurotransmitters/hormones do adrenomimetic and antiadrenergic
drugs mimic and inhibit, respectively? - answerIn both cases:
- norepinephrine (NT)
- epinephrine (hormone)
- dopamine (NT)
Name the G protein associated with the following adrenergic R.
- alpha 1
- alpha 2
- beta (all types)
- D1
- D2 - answer"QISS I" = "Kiss Me"
What type of G protein are alpha 1 receptors? Effect? - answer- Gq
- Increases IP3, DAG
- Most innervated vascular smooth muscle = contraction
- Pupillary dilator muscle = contraction (dilates pupil)
- Prostate = contraction
- Heart = increase force of contraction
What type of G protein are alpha 2 receptors? Effect? - answer- Gi
- Decrease cAMP
- Neurons = modulates transmitter release
- Platelets = aggregation
- Adrenergic and cholinergic nerve terminals = inhibits transmitter release
- Some vascular smooth muscle = inhibits transmitter release
- fat cells - inhibits lipolysis
What type of G protein are Beta 1, 2, and 3 receptors? - answer- Gs
- Increase cAMP
What drug class is phenylephrine (Neo-Synephrine) and clonidine (Catapres)? - answer
alpha agonist
Which receptors does phenylephrine act on? - answer alpha 1 > alpha 2 >>>>> ß
Which receptors does clonidine act on? - answer alpha 2 > alpha 1 >>>>> ß
What drug class is Norepinephrine (Lavished) and Epinephrine (Adrenalin)? - answer
mixed alpha and beta agonist
Which receptors does norepinephrine act on? - answer- alpha 1 = alpha 2
- ß1 >> ß2
Which receptors does epinephrine act on? - answer alpha 1, alpha 2, ß1, ß2 equally
(least selective Adreno mimetic)
What drug class is Dobutamine (doubter), Isoproterenol (Isuprel), and Albuterol (Proair,
Proventil, Ventolin)? - answer Beta agonist
Which receptors does dubutamine act on? - answerß1 > ß2 >>>> alpha
Which receptors does Isoproterenol act on? - answerß1 = ß2 >>>> alpha
Which receptors does albuterol act on? - answerß2 >> ß1 >>>> alpha
What class of adrenomimetic are alpha, beta, and mixed agonists? - answerdirect
acting
What drug class is Cocaine? - answer- Dopamine (DA) and NE re-uptake inhibitors
- Indirect adrenomimetics
What drug class is Selegiline (Eldepryl) and Phenelzine (Nardil)? - answer- Monoamine
oxidase (MAO) inhibitors
- indirect adrenomimetics
What drug class is Amphetamine, Methylphenidate (Ritalin), and Tyramine? - answer-
Reverse NE and DA uptake mechanisms and releasing agent (enhance release)
- indirect adrenomimetics
, What is the drug class and action of Ephedrine? - answer- releasing agent (enhance
release) as well as a direct acting
- indirect adrenomimetic
Which nervous system do adrenergic drugs act on? - answersympathetic bc adrenergic
R primarily located at target organs innervated by post-ganglionic N. of SNS.
Define adrenomimetics (aka sympathomimetics)
Define antiadrenergic drugs (aka sympatholytics) - answerdrugs that act on adrenergic
R. to mimic effects of endogenous NTs/hormone
drugs that inhibit/prevent effects of endogenous NTs/hormone
Which endogenous neurotransmitters/hormones do adrenomimetic and antiadrenergic
drugs mimic and inhibit, respectively? - answerIn both cases:
- norepinephrine (NT)
- epinephrine (hormone)
- dopamine (NT)
Name the G protein associated with the following adrenergic R.
- alpha 1
- alpha 2
- beta (all types)
- D1
- D2 - answer"QISS I" = "Kiss Me"
What type of G protein are alpha 1 receptors? Effect? - answer- Gq
- Increases IP3, DAG
- Most innervated vascular smooth muscle = contraction
- Pupillary dilator muscle = contraction (dilates pupil)
- Prostate = contraction
- Heart = increase force of contraction
What type of G protein are alpha 2 receptors? Effect? - answer- Gi
- Decrease cAMP
- Neurons = modulates transmitter release
- Platelets = aggregation
- Adrenergic and cholinergic nerve terminals = inhibits transmitter release
- Some vascular smooth muscle = inhibits transmitter release
- fat cells - inhibits lipolysis
What type of G protein are Beta 1, 2, and 3 receptors? - answer- Gs
- Increase cAMP
