Mixed amphetamine salts

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Psychostimulant, Amphetamine

Adderall, Adderall XR

Discovered initially in 1887 as a chemical by Lazăr Edeleanu, and then as a drug in the late 1920s. It was initially noted to have a chiral center and two enantiomers, levoamphetamine and dextroamphetamine, the latter of which being significantly more psychoactive.

Experience

👥 2 personal reports · avg efficacy 90.0/100 · avg side-effect burden 30.0/100 · median use 8 months · median dose 17.5 mg/day · 100% still taking it

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Problems

Inattention, Fatigue

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Titration strategies

Start Adderall XR 5 mg first thing in the morning. If insufficent, may take 10 mg the next day. Can increase 5 mg daily up to 30 mg or until effect.

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Effects

so manyso few

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Pharmacokinetics

Absorption: Excellent bioavailability by all knows routes of administration, sources report ">75%" and "~90%". Distribution: The volume of distribution of amphetamine is 4 L/kg, and its plasma protein binding is less than 20%. Metabolism: Amphetamine is oxidized to form 4-hydroxyamphetamine, alpha-hydroxyamphetamine, or norephedrine. Both norephedrine and 4-hydroxyamphetamine are active metabolites and are further metabolized to form 4-hydroxy-norephedrine. The deamination of alpha-hydroxyamphetamine leads to the formation of phenylacetone, which is then metabolized to benzoic acid, its glucuronide conjugate, and hippuric acid, the glycine conjugate. CYP2D6 is crucial in the metabolism of hydroxyamphetamine. Due to the genetic polymorphism of CYP2D6, variations in amphetamine metabolism may occur. Additionally, amphetamine inhibits monoamine oxidase (MAO), and both CYP1A2 and CYP3A4 contribute to its metabolism.cite Elimination: Amphetamine is primarily excreted in the urine as metabolites, including alpha-hydroxy-amphetamine, with approximately 30% to 40% of the dose recovered as unchanged amphetamine. Due to its pKa of 9.9, the urinary elimination of amphetamine is influenced by urine pH and flow rates. An alkaline urine pH reduces ionization, which leads to decreased renal elimination. In contrast, acidic pH and increased urine flow rates enhance renal clearance, surpassing glomerular filtration rates (GFR), which suggests that active tubular secretion plays a significant role in excretion. The half-life of the D-enantiomer is 9 hours in children aged 6 to 12, whereas the L-enantiomer has a half-life of 11 hours. In adolescents aged 13 to 17, the D-enantiomer has a half-life of 11 hours, and the L-enantiomer ranges from 13 to 14 hours. In adults, the D-enantiomer has a half-life of 10 hours, whereas the L-enantiomer has a half-life of 13 hours.

Pharmacodynamics

REUPTAKE INHIBITION. EXCRETION!

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Summary

Classes

Psychostimulant, Amphetamine

Common uses

Distractibility4.0n=1
Excessive daytime sleepiness in shift-work disorder4.0n=1
Impaired persistent attention4.0n=2
Cognitive symptoms in chronic illness3.0n=1
Impulsivity3.0n=1

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Pharmacy

Pharmacology

Routes

Oral, primarily

Onset

rapid

Duration

8-14h

Bioavailability

Oral: ~90%

Pregnancy

Class C

Legal status

Schedule II Controlled Substance

Purported mechanism

Increased production and decreased reuptake of NE and DA

Excellent bioavailability by all knows routes of administration, sources report ">75%" and "~90%".

Distribution:

The volume of distribution of amphetamine is 4 L/kg, and its plasma protein binding is less than 20%.

Metabolism:

Amphetamine is oxidized to form 4-hydroxyamphetamine, alpha-hydroxyamphetamine, or norephedrine. Both norephedrine and 4-hydroxyamphetamine are active metabolites and are further metabolized to form 4-hydroxy-norephedrine.

The deamination of alpha-hydroxyamphetamine leads to the formation of phenylacetone, which is then metabolized to benzoic acid, its glucuronide conjugate, and hippuric acid, the glycine conjugate.

CYP2D6 is crucial in the metabolism of hydroxyamphetamine. Due to the genetic polymorphism of CYP2D6, variations in amphetamine metabolism may occur. Additionally, amphetamine inhibits monoamine oxidase (MAO), and both CYP1A2 and CYP3A4 contribute to its metabolism. cite

Elimination:

Amphetamine is primarily excreted in the urine as metabolites, including alpha-hydroxy-amphetamine, with approximately 30% to 40% of the dose recovered as unchanged amphetamine. Due to its pKa of 9.9, the urinary elimination of amphetamine is influenced by urine pH and flow rates. An alkaline urine pH reduces ionization, which leads to decreased renal elimination. In contrast, acidic pH and increased urine flow rates enhance renal clearance, surpassing glomerular filtration rates (GFR), which suggests that active tubular secretion plays a significant role in excretion. The half-life of the D-enantiomer is 9 hours in children aged 6 to 12, whereas the L-enantiomer has a half-life of 11 hours. In adolescents aged 13 to 17, the D-enantiomer has a half-life of 11 hours, and the L-enantiomer ranges from 13 to 14 hours. In adults, the D-enantiomer has a half-life of 10 hours, whereas the L-enantiomer has a half-life of 13 hours.

Pharmacodynamics

REUPTAKE INHIBITION. EXCRETION!

Indications

Inattention, Fatigue

Dosing and titration

Start Adderall XR 5 mg first thing in the morning. If insufficent, may take 10 mg the next day. Can increase 5 mg daily up to 30 mg or until effect.

Effects

so many

Adverse effects

so few

Contraindications

few