Showing posts with label CNS-Active Sympathomimetic Agent. Show all posts
Showing posts with label CNS-Active Sympathomimetic Agent. Show all posts

Methamphetamine (Desoxyn, various street names)

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Name: Methamphetamine (Desoxyn, various street names)

Class: CNS-Active Sympathomimetic Agent (Indirect)

Mechanism: Release of DA, NE, & 5HT from nerve terminals. Some blockade of reuptake of DA, NE, & 5HT. Weak inhib. of MAO. Produces elev. of mood, euphoria, ­ alertness, ¯ sense of fatigue, ¯ food intake, periph. sympathomimetic effects.

Absorption: Oral ® good bioavail.

Dist.: Crosses BBB.

Metabolism.:

Excretion, :

Toxicity/S.E.s: Neurosis, paranoia, frank psychosis. Tolerance, but not as strong as opiates. Acute toxicity ® hypertension, stroke, seizures, cardiac arrhythmias. Very strong psych. dependence. Mild physical dependence. W/drawal ® ­ appetite, fatigue, depression.

Utility: Treat narcolepsy, ADHD. Off-label uses. Ice = smokable version.

Special Features: Not Metabolism. by COMT. Decreased Metabolism. by MAO. Higher ratio of CNS/PNS actions than amphetamine.

 

Tyramine

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Name: Tyramine

Class: CNS-Active Sympathomimetic Agent (Indirect)

Mechanism: Releases NE from storage vesicles.

Absorption:

Dist.:

Metabolism.: Metabolism. by MAO

Excretion, :

Toxicity/S.E.s: MAO inhibitors ® hypertensive crisis

Utility:

Special Features: Normal byproduct of tyrosine Metabolism. Found in fermented foods (e.g., cheese, wine).

 

Methylphenidate (Ritalin)

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Name: Methylphenidate (Ritalin)

Class: CNS-Active Sympathomimetic Agent (Indirect)

Mechanism: Indirect agonist of symp. receptors. Potent CNS and peripheral effects. Displaces catecholamines from storage vesicles. Reverses Uptake I transporter ® NE release. Causes ­ systolic & diastolic BP. HR often reflexively slowed. Contraction of urinary sphincter. Typical symp. effects.

Absorption: Oral ® good bioavail.

Dist.: Crosses BBB.

Metabolism.:

Excretion, :

Toxicity/S.E.s:

Utility: Treat ADHD.

Special Features: Not Metabolism. by COMT. Decreased Metabolism. by MAO.

 

Amphetamine

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Name: Amphetamine

Class: CNS-Active Sympathomimetic Agent (Indirect)

Mechanism: Indirect agonist of symp. receptors. Potent CNS and peripheral effects. Displaces catecholamines from storage vesicles. Reverses Uptake I transporter ® NE release. Causes ­ systolic & diastolic BP. HR often reflexively slowed. Contraction of urinary sphincter. Typical symp. effects.

Absorption: Oral ® good bioavail.

Dist.: Crosses BBB.

Metabolism.:

Excretion, :

Toxicity/S.E.s:

Utility: Treat narcolepsy, ADHD.

Special Features: Not Metabolism. by COMT. Decreased Metabolism. by MAO.