Flashcards in Sympathomimetics Deck (116)
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1
Constitute a group of drugs used for
Cardiovascular
Respiratory
Other conditions
adrenomimetics
2
Type of adrenomimetics based on mode of action
Bind to and activate the adrenoceptors
Result to sympathetic stimulation
DIRECT-ACTING SYMPATHOMIMETICS
3
INDIRECT-ACTING SYMPATHOMIMETICS
Displacement of stored cathecolamines in the synapse
releasers
4
example of releasers
tyramine, amphetamine
5
INDIRECT-ACTING SYMPATHOMIMETICS
Inhibit the reuptake of cathecolamines by nerve terminals
Reuptake inhibitors
6
example of Reuptake inhibitors
Cocaine, tricyclic antidepressants
7
Constitute a third class of adrenoceptors
Drugs mentioned have little effect on dopamine receptors
May act as a potent dopamine receptor agonist itself
Intermediate doses activate beta receptors
Large doses activate alpha receptors
DOPAMINE
8
dopamine
Intermediate doses activate -- receptors
beta
9
dopamine
Large doses activate --receptors
dopamine
10
Drug preferentially binds to one subgroup of receptors at concentrations too low to interact with another receptor
RECEPTOR SELECTIVITY
11
Parent compound of sympathetic drug
phenylethylamine
12
effect of Increasing the size of alkyl substituents
Enhanced activity for beta 2 receptors
Lowers alpha receptor activity
13
Methyl substitution on NE yields ----
Effect:
Enhanced activity for beta 2 receptors
epinephrine
Effect: Enhanced activity for beta 2 receptors
14
Isopropyl substitution on NE yields
isoproterenol
15
-OH groups at the C? and C? positions yield cathecolamines
c3 and c4
16
effect of Absence of one or both –OH group
Increases bioavailability after oral administration
COMT resistant
Increase distribution to the CNS
Amphetamine and ephedrine
17
effect of C. Substitution on the alpha carbon
Add methyl group
MAO resistant
Amphetamine and ephedrine
18
effect of D. Substitution on the beta carbon
Add OH group
Facilitates activation of adrenoceptors
For storage of cathecolamines
Direct-acting sympathomimetics
Dopamine does not contain beta-OH group
19
does dopamine contain a beta-OH group
Dopamine does not contain beta-OH group
20
comparative competency for alpha receptors
E > NE> isoproterenol
21
receptor responsible for
Increase in phosphatidyl inositol (IP3)
Release of calcium
alpha 1
22
receptor responsible for decrease cAMP
D1 and alpha 2
23
comparative competency BETA RECEPTOR ACTIVATION
Isoproterenol > epinephrine > NE
24
receptors responsible for increase cAMP
B1, B2, B3
25
Penetrates the CNS producing stimulant effects
Amphetamine
26
ORGAN SYSTEM EFFECTS
B. EYE
Pupillary dilator responds with mydriasis
Accommodation is not significantly affected
Alpha agonists reduce intraocular pressure by increasing outflow of aqueous humor
27
---- agonists reduce intraocular pressure by increasing outflow of aqueous humor
Alpha
28
ALPHA agonists reduce intraocular pressure by
increasing outflow of aqueous humor
29
EFFECT OF BETA ANTAGONISTS IN AQUEOUS HUMOR
Beta antagonists decrease production of aqueous humor
30
