Podcast
Questions and Answers
What Chinese medicine herb is the source of amphetamines?
What Chinese medicine herb is the source of amphetamines?
Ma huang
Who synthesized alpha-methylphenethylamine (AMPH) to treat asthma?
Who synthesized alpha-methylphenethylamine (AMPH) to treat asthma?
Edeleanu
Which of the following is the least potent amphetamine?
Which of the following is the least potent amphetamine?
What type of reactions can amphetamines cause in the body?
What type of reactions can amphetamines cause in the body?
Signup and view all the answers
How is meth synthesized?
How is meth synthesized?
Signup and view all the answers
What routes can amphetamines be administered?
What routes can amphetamines be administered?
Signup and view all the answers
What is the half-life of Ice, the HCl salt smokable form of methamphetamine?
What is the half-life of Ice, the HCl salt smokable form of methamphetamine?
Signup and view all the answers
What are the acute effects of amphetamines?
What are the acute effects of amphetamines?
Signup and view all the answers
Amphetamines elevate the availability of DA, NE, and _____ in the brain.
Amphetamines elevate the availability of DA, NE, and _____ in the brain.
Signup and view all the answers
Amphetamines require the firing of DA-ergic neurons to be effective.
Amphetamines require the firing of DA-ergic neurons to be effective.
Signup and view all the answers
What is a possible consequence of acute dosing of amphetamines?
What is a possible consequence of acute dosing of amphetamines?
Signup and view all the answers
What physical and psychological issues can arise from AMPH withdrawal?
What physical and psychological issues can arise from AMPH withdrawal?
Signup and view all the answers
Study Notes
Amphetamine Origins and Synthesis
- Amphetamines are derived from the Chinese medicine herb Ma huang.
- Edeleanu synthesized alpha-methylphenethylamine (AMPH) to treat asthma.
- Amphetamine potency increases from L-amphetamine to D-amphetamine to methamphetamine.
Amphetamine Structure and Neurotransmitter Interactions
- Amphetamine's structure is similar to neurotransmitters, allowing it to bind to their transporters.
- AMPH is phenylethylamine, similar to dopamine (DA) and norepinephrine (NE), which are catecholamines.
Methamphetamine Synthesis
- Methamphetamine can be synthesized using the Nagai or Leuckart synthesis methods.
Amphetamine Administration, Distribution, Metabolism, and Excretion (ADME)
- Amphetamines can be taken orally (70% bioavailability), injected, snorted (80% bioavailability), or smoked (70-99% bioavailability). Smoking is the fastest route of administration.
- Ice, the smokable form of methamphetamine hydrochloride, has a half-life of 12 hours, resulting in a longer-lasting high than cocaine.
- The distribution half-life is 30 to 120 minutes.
- Amphetamines are metabolized more slowly, with CYP2D6 primarily responsible for metabolizing methamphetamine (half-life 12+ hours, duration 10-20 hours) and amphetamine (half-life ~11 hours, duration 3-12 hours).
- Amphetamines are excreted in the urine, sweat, and saliva, eliminating active metabolites such as norephedrine and 4-hydroxyamphetamine.
Acute and Adverse Effects of Amphetamines
- Increase in norepinephrine release causes sympathomimetic effects.
- Increased serotonin (5HT) release leads to delusional parasitosis and perceptual disturbances.
- Increased dopamine release results in increased locomotor activity, such as punding.
- Adverse effects include poisoning from contaminants and enhanced stimulatory effects due to polypharmacy.
Cellular Mechanisms of Amphetamines
- Amphetamines increase the availability of dopamine, norepinephrine, and serotonin without requiring the firing of dopamine neurons.
- They enter the synapse via dopamine transporter (DAT) or diffusion.
- Amphetamines block reuptake by DATs, NETs (norepinephrine transporter), and SERTs (serotonin transporter).
- They form a complex with the transporter (AMPH-TAAR) and cause intracellular dopamine to build up, reversing the DAT.
- Leakage into the synapse occurs.
- The spike in dopamine can activate postsynaptic cells.
- Amphetamines increase the release of dopamine, norepinephrine, and serotonin into the synapse.
- They also inhibit monoamine oxidase (MAO) at high concentrations.
- Amphetamines cause a dopamine surge in the basal ganglia, but their small size allows the transporter to complete its cycle, so they do not completely block the transporter.
Tolerance to Amphetamines
- Tolerance develops due to neurotransmitter depletion through displacement of serotonin, dopamine, and norepinephrine.
- Amphetamines inhibit tyrosine hydroxylase, reducing dopamine and norepinephrine synthesis.
- Acute dosing can reduce dopamine transporter function.
- Reverse tolerance targets motor function ganglia.
Amphetamine Withdrawal
- Amphetamine withdrawal presents both physical and psychological symptoms.
- These include cravings, depression, lethargy, muscle pain, abnormal sleep patterns, anhedonia, and emotional volatility.
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
Related Documents
Description
Explore the origins, synthesis, and pharmacokinetics of amphetamines in this quiz. Learn about their structure, neurotransmitter interactions, and various methods of administration. Test your knowledge on the intricacies of amphetamine compounds and their effects on the body.
