Showing posts with label CNS Stimulant. Show all posts
Showing posts with label CNS Stimulant. Show all posts

Dextroamphetamine (Dexedrine)

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Name: Dextroamphetamine (Dexedrine)

Class: CNS Stimulant

Mechanism: CNS Mech = 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, t½:

Toxicity/S.E.s: Irritability & manic behavior (large doses). Prolonged use ® toxic psychosis (looks like paranoid schiz.). Produces very strong psych. dependence (depression on w/drawal), mild phys. dependence. C/I: hyperthyroidism, mod-severe hypertension, hist. of drug abuse, glaucoma, hist. of hypersens. or idiosync. to sympathomimetic amines.

Utility: Treat narcolepsy, ADHD, short term Rx of exogenous obesity.

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

 

Cocaine (Various)

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Name: Cocaine (Various)

Class: CNS Stimulant (Indirect Sympathomimetic Agent)/Local Anesth (Ester)

Mechanism: Inhib. reuptake of catecholamines (DA, NE, 5HT) ® prolonged action. Local anesthetic properties from block of Na+ & Ca2+ channels ® ¯ rate of rise of action potential, failure to propagate action potential, eventual conduction block. Smaller, unmyelinated fibers are more easily blocked and remain blocked longer.

Absorption: : Rapidly absorbed IV & oral. IV absorption can be limited w/a vasoconstrictor. Rapid topical absorption at mucous membranes.

Dist.: Rapidly dist. to highly perfused organs (i.e., brain, liver, kidney, heart

Metabolism.: Rapidly Metabolism. by plasma pseudocholinesterases. Med. duration of anesth action.

Toxicity/S.E.s: Fever, nausea, vomiting, confusion, headache. 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: Used in ENT surgery to produce local anesthesia, hemostasis, vasoconstriction. Crack = smokable version.

Special Features: Does not require concomitant application of a vasoconstrictor. Twice the potency of procaine. Produces elevation of mood, euphoria, ­ self-esteem, ­ energy, ¯ sense of fatigue. Moderate dose ® ­ HR, ­ BP.

 

Methylphenidate (Ritalin)

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Name: Methylphenidate (Ritalin)

Class: CNS Stimulant

Mechanism: CNS 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, t½:

Toxicity/S.E.s: Irritability & manic behavior (large doses). Prolonged use ® toxic psychosis (looks like paranoid schiz.). Produces psych dependence (depression on w/drawal). C/I: hyperthyroidism, mod-severe hypertension, hist. of drug abuse, glaucoma, hist. of hypersens. or idiosync. to sympathomimetic amines.

Utility: Treat ADHD, narcolepsy.

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

 

Cocaine

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Name: Cocaine

Class: CNS Stimulant (Indirect Sympathomimetic Agent)

Mechanism: Inhib. reuptake of catecholamines (DA, NE, 5HT) ® prolonged action. Local anesthetic properties. Also elevation of mood, euphoria, ­ self-esteem, ­ energy, ¯ sense of fatigue. Moderate dose ® ­ HR, ­ BP.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Fever, nausea, vomiting, confusion, headache, seizures.

Utility: Used in ENT surgery to produce local anesthesia, hemostasis, vasoconstriction.

Special Features: