Showing posts with label Centrally Acting Antiadrenergic Agent. Show all posts
Showing posts with label Centrally Acting Antiadrenergic Agent. Show all posts

Methyldopa (Aldomet)

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Name: Methyldopa (Aldomet)

Class: Centrally Acting Antiadrenergic Agent

Mechanism: Stimulates inhibitory a2 receptors in central cardiovasc pathways involving EPI or NE. a2 are G-protein coupled to inhibit adenylyl cyclase ®
¯ cAMP ® ¯ central symp. activity.

Absorption:

Dist.: Act at medullary and spinal sites.

Metabolism.:

Excretion, :

Toxicity/S.E.s: Prominent sedation, dry mouth, nightmares, depression, movement disorders, endocrine disturbances (lactation), anemia, rare hypersensitivity of skin and liver. Possible toxic psychosis if given w/levodopa.

Utility: Treat hypertension.

Special Features: Activates a2 via Metabolismolite methylnorepinephrine (false transmitter). Probably the most used hypotensive agent in mgt. of pregnant E.

 

Guanabenz (Wytensin)

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Name: Guanabenz (Wytensin)

Class: Centrally Acting Antiadrenergic Agent

Mechanism: Stimulates inhibitory a2 receptors in central cardiovasc pathways involving EPI or NE. a2 are G-protein coupled to inhibit adenylyl cyclase ®
¯ cAMP ® ¯ central symp. activity.

Absorption: Oral.

Dist.: Acts at medullary and spinal sites.

Metabolism.:

Excretion, :

Toxicity/S.E.s: Prominent sedation, dry mouth, depression in those so inclined, constipation. May potentiate actions of other CNS depressants. Rebound hypertension, nervousness, insomnia if w/drawn too quickly.

Utility: Treat hypertension.

Special Features: Direct a2 activation. CV reflexes remain intact; normal homeostatic responses to exercise are maintained.

 

Clonidine (Catapres)

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Name: Clonidine (Catapres)

Class: Centrally Acting Antiadrenergic Agent/Opioid Withdrawal Suppressant

Mechanism: Stim. inhib. a2 receptors in central cardiovasc pathways involving EPI or NE. a2 are G-protein coupled to inhibit adenylyl cyclase ®
¯ cAMP ® ¯ central symp. activity.

Absorption:

Dist.: Act at medullary and spinal sites.

Metabolism.:

Excretion, :

Toxicity/S.E.s: Prominent sedation, dry mouth.

Utility: Treat hypertension. DOC for treating opioid w/drawal (probably substitutes for opioid depression of adenylate cyclase in locus coeruleus & pregang. symp. neurons. No abstinence synd. when withdrawn.

Special Features: Direct a2 activation. Very potent (<0.5>

 

Methyldopa (Aldomet)

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Name: Methyldopa (Aldomet)

Class: Centrally Acting Antiadrenergic Agent

Mechanism: Stim. inhib. a2 receptors in central cardiovasc pathways involving EPI or NE. a2 are G-protein coupled to inhibit adenylyl cyclase ®
¯ cAMP ® ¯ central symp. activity.

Absorption:

Dist.: Act at medullary and spinal sites.

Metabolism.:

Excretion, :

Toxicity/S.E.s: Prominent sedation, dry mouth, nightmares, depression, movement disorders, endocrine disturbances (lactation), anemia, rare hypersensitivity of skin and liver. Possible toxic psychosis if given w/levodopa.

Utility: Treat hypertension.

Special Features: Activates a2 via Metabolismolite, methylnorepinephrine (false transmitter). Probably the most used hypotensive agent in mgt. of pregnant E.

 

Clonidine (Catapres)

Post a comment

Name: Clonidine (Catapres)

Class: Centrally Acting Antiadrenergic Agent/Opioid Withdrawal Suppressant

Mechanism: Stim. inhib. a2 receptors in central cardiovasc pathways involving EPI or NE. a2 are G-protein coupled to inhibit adenylyl cyclase ®
¯ cAMP ® ¯ central symp. activity.

Absorption: Oral, transdermal.

Dist.: Acts at medullary and spinal sites.

Metabolism.:

Excretion, :

Toxicity/S.E.s: Prominent sedation, dry mouth, depression in those so inclined, constipation. S.E.s may be reduced by transdermal admin. May potentiate actions of other CNS depressants. Rebound hypertension, nervousness, insomnia if w/drawn too quickly.

Utility: Treat hypertension. DOC for treating opioid w/drawal. No abstinence synd. when withdrawn.

Special Features: Direct a2 activation. Very potent (<0.5 style=""> CV reflexes remain intact; normal homeostatic responses to exercise are maintained.