Alpha- Beta- Adrenergic Agonists 35

Front 1

Divisions del Nervous system (SN).

En qué parte de la ciudad vives?

Back 1

1. Central (Brain + Spinal Cord)

2. Peripheral (Autonomic + Somatic)

Front 2

Sympathetic and parasympathetic are divisions of...

Back 2

Autonomic nervous system

Front 3

Which body functions are stimulated by the parasympathetic nervous system?

Which neurotransmitter does it primarly use?

Back 3

Sexual arousal

Salivation

Lacrimation

Urination, digestion, and defecation.

Acetylcholine as its neurotransmitter

Front 4

Name two drugs that are inhibitors of NET (Norepinephrine transporter).

Thus prolong its actions at the receptor

Back 4

TCA (eg. imipramine)

Cocaine

Front 5

Name two enzymes that metabolize NA in the nerve terminal

Back 5

MAO

COMP (catechol-O-methyltransferases)

Front 6

Which common part of adrenergic agonist is essential for its adrenergic activity?

What is the general pharmacophore?

Back 6

Essential: Ethylamine chain

Pharmacophore: Primary or secondary amine 2 C away from a substituted benzeno ring

Front 7

What is Adrenaline I.V. used for?

Back 7

1. Treat cardiac arrest and hypotensive crisis (eg. during anaphylactic reactions) due it to its:

Vasoconstrictor

Chronotropic (+)

Inotropic (+)

2. Mixed with local anesthetics (such lidocaine) to produce localized vasoconstriction to prolong duration of action and minimize the local anesthetic systemic effects

Front 8

What does "inotropic" refer to?

Back 8

Strength of contraction of heart muscle (myocardial

Front 9

What is the selectivity of dobutamine for adrenergic receptors?

Back 9

Beta 1 selective

Front 10

Dobutamine

Main use and SE

Back 10

Acute HF

B1 receptor stimulation =

Increase AMPc en myocardium =

However, in this case:

Increase opening of L-type calcium channels:

Enhance CONTRACTILITY

SE: Tachyarrhytmias

Ischemia

Front 11

What is the selectivity of oxymetazoline for adrenergic receptors?

Back 11

Alpha-non selective:

Alpha 1

Alpha 2

Wiki:

Oxymetazoline is a selective α₁ adrenergic receptor agonist and α₂ adrenergic receptor partial agonist. ?????

Front 12

Back 12

Front 13

Have a look at the Adrenaline molecule. How can you improve the α1 receptor affinity?

Name the two drugs obtained and their use in I.V. administration

Back 13

I.V. to maintain systemic blood pressure in hypotensive conditions

Methoxamine

Phenylephrine

Hint 13

Front 14

Name this molecule and its affinity to alpha adrenergic receptors

Back 14

Methoxamine Alpha 1 - selective

Front 15

What is the selectivity of pseudoephedrine for adrenergic receptors?

Back 15

Mixed:

* Alpha-agonist

* Indirect (NA releasing) agent

Front 16

What is dipivefrin?

What does it treat?

How does it achieves it action?

Razona...

Back 16

Cathecol diester PRODRUG of adrenalin

* To treat open-angle glaucoma

* Tissue esterases cleave the ester bonds to regenerate adrenaline

* Adrenaline activates alpha2 receptors on the ciliary body = To decrease aqueous humor production

Front 17

Draw a IMIDAZOLINE ring

Back 17

2 N + 3 C + 1=

Front 18

Name 2 imidazoline derivatives

Which alpha- activity do they have?

How can Alpha 1- activity be increased?

Back 18

* Clonidine

* Oxymetazoline

Alpha 1 and Alpha 2 agonists activity

Pero ojo... oxymetazoline tiene más afinidad por alpha-1... Ahora veremos como la ha conseguido

Front 19

Oxymetazoline:

It is a Selective alpha-agonist (alpha 1 and alpha 2)

How has the alpha-1 agonist activity has been increased

Back 19

With BULKY substitution in para

Front 20

Oxymetazoline: it is used as topical decongestant due to its DIRECT ________ ACTION in the nasal mucosa

Back 20

Vasoconstriction

Front 21

What is systemic administration?

Back 21

Systemic administration is a route of administration of medication, nutrition or other substance into the circulatory system so that the entire body is affecte

Front 22

Clonidine: reduces tonic __________ output from the sistema nervioso _______ by activating __________ alpha-2 adrenoreceptors

Back 22

Clonidine: reduces tonic SYMPATHETIC output from the sistema nervioso CENTRAL by activating CENTRAL alpha-2 adrenoreceptors

Ha quedado claro el concept de CENTRAL ACTING????

Front 23

Terbutaline: Beta2 Agonist

* _______ AMPc in bronquial smooth muscle =

* _______ Ca intracellular =

Broncodilation

Which other effect does it have and which other drug also has the same use?

Back 23

Terbutaline: Beta2 Agonist

* Increase AMPc in bronquial smooth muscle =

* Decrease Ca intracellular =

Broncodilation

Systemically: Slow down premature labour (tocolytics)

Also, ritodrine (beta-2 agonist also)

Front 24

Clonidine sudden withdraw:

Back 24

Enhace SN sympathetic outflow:

HTA

Sweating

Tachycardia

Tremors

Front 25

Apraclonidine

Brimonidine (Alphagan-P)

Are derivatives of _________

They are used topically to selective activate which receptors?

Where?

To treat what?

Back 25

Derivatives of CLONIDINE

Alpha 2 in the EYE

To treat open-angle glaucoma

Front 26

Amphetamine. MA?

Back 26

Only releases CA from sympathetic nerves (indirect action)

Front 27

Main adverse effect of imidizoline nasal decongestants?

Which product is less likely to produce it?

Back 27

Rebound congestion

(Phenylephrine: less likely to produce it)

Front 28

Beta-2 agonist SE?

Ayuda: Piensa en un b2 agonist

Back 28

Tachycardia

Muscle tremors

Insomnia

* Due to their actions at cardiac and other beta-receptors (their selectivity is not absolute)

Respiras, pero corazón a tope, tiemblas y no te duermes 🤪🤪🤪

Front 29

What is this?

Back 29

Primary or secundary amino

2 C away from

Substitured benzene ring

Front 30

Clonidine IV :

Actives central alpha-2 receptors.

Use to treat HTA.

Which SE are associated to this?

Back 30

Bradycardia

Hypotension

Sedation

Dry mouth 🤐

Front 31

Terbutaline: B2 agonist.

How the B2 selectivity was achieved?

Easy peasy! 🤗

Back 31

Changing catechol ring to Resorcinol

Front 32

Which alpha adrenergic receptors have been identified?

Back 32

1A 1B 1D 2A 2B 2C

Front 33

Which types of alpha-adrenoreceptors

Back 33

Vascular smooth muscle has two types of alpha-adrenoceptors: alpha1 (α1) and alpha2 (α2). The α1-adrenoceptors are the predominant α-receptor located on vascular smooth muscle. These receptors are linked to Gq-proteins that activate smooth muscle contraction through the IP3 signal transduction pathway. Depending on the tissue and type of vessel, there are also α2-adrenoceptors found on the smooth muscle. These receptors are linked to Gi-proteins, and binding of an alpha-agonist to these receptors decreases intracellular cAMP, which causes smooth muscle contraction. There are also α2-adrenoceptors located on the sympathetic nerve terminals that inhibit the release of norepinephrine and therefore act as a feedback mechanism for modulating the release of norepinephrine.Alpha-agonists constrict both arteries and veins; however, the vasoconstrictor effect is more pronounced in the arterial resistance vessels. Constriction of the resistance vessels (small arteries and arterioles) increases systemic vascular resistance, whereas constriction of the venous capacitance vessels increases venous pressure.

Front 34

Beta-blocker overdose can be life-threatening.

What is the treatment?

Back 34

Glucagon and dobutamine/milrinone.

Front 35

TCA and cocaine: They prolong the action of ________ at the receptor by inhibition of _________.

Back 35

Name two drugs that are inhibitors of NET (Norepinephrine transporter). Thus prolong its actions at the receptor