Pharmaceutical Stimulants and Substance Abuse

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Questions and Answers

What estimated annual cost does methamphetamine use account for in the United States?

$23.4 billion (correct)

$15 billion

$10 billion

$30 billion

Which pharmacotherapy is specifically mentioned for the treatment of panic attacks?

Haloperidol

Alprazolam (correct)

Chlorpromazine

Fluoxetine

How many Americans aged 12 and older reported abusing cocaine at least once in 2009?

2.5

6.5

5.7

4.8 (correct)

What mechanism do the antibodies in new immunological treatments target when someone uses cocaine?

They bind to it and prevent it from reaching the brain Signup and view all the answers

Which drug is noted as being 50 times more potent than chlorpromazine?

Haloperidol Signup and view all the answers

Which stimulant is commonly prescribed to treat attention deficit disorders in children?

Ritalin (methylphenidate) Signup and view all the answers

What are the medical uses of pharmaceutical stimulants?

Control of narcolepsy Signup and view all the answers

Which of the following stimulants is derived from the coca plant?

Cocaine Signup and view all the answers

Which pharmaceutical stimulant is used to treat obesity?

Preludin (phenmetrazine) Signup and view all the answers

How does Ritalin help improve symptoms of ADHD?

By selectively activating the mesolimbic pathway Signup and view all the answers

Which stimulant is identified as an illicit drug with potential for addiction?

Cocaine Signup and view all the answers

What condition could be treated with the use of methamphetamine?

Weight control Signup and view all the answers

What is a common use of caffeine, categorized as a methylxanthine?

Stimulant for alertness and endurance Signup and view all the answers

What is the primary method through which cocaine penetrates the blood-brain barrier?

Insufflation Signup and view all the answers

Which of the following describes the half-life of cocaine?

50-90 minutes Signup and view all the answers

What psychoactive compound is formed when alcohol interacts chemically with cocaine?

Cocaethylene Signup and view all the answers

Which statement accurately describes the pharmacodynamics of cocaine?

It blocks reuptake of monoamines. Signup and view all the answers

What is a significant cardiac risk associated with the use of cocaethylene?

Greater cardiac toxicity Signup and view all the answers

What acute effect is commonly experienced at moderate doses of cocaine?

Amelioration of fatigue Signup and view all the answers

How does cocaine primarily affect neurotransmitters in the brain?

Blocks monoamine reuptake. Signup and view all the answers

What is the primary sympathetic effect of cocaine?

Increased energy and alertness Signup and view all the answers

What is a common acute effect of cocaine at high doses?

Hyper-vigilance Signup and view all the answers

Which of the following is NOT a long-term effect of amphetamines?

Drowsiness Signup and view all the answers

Which symptom is part of the withdrawal process from cocaine?

Intense craving Signup and view all the answers

What is a potential medical consequence of chronic amphetamine use?

Brain hemorrhage Signup and view all the answers

Which of the following best describes how amphetamines affect neurotransmitters?

They enhance actions of adrenaline and noradrenaline. Signup and view all the answers

Which of the following is a distinguishing characteristic of methamphetamine compared to amphetamine?

Typically smoked. Signup and view all the answers

Which condition is classified as a withdrawal symptom from methamphetamine?

Hunger Signup and view all the answers

What physiologic effect do amphetamines have on heart rate?

Increase heart rate Signup and view all the answers

Which of the following symptoms is associated with stimulant psychosis?

Visual hallucinations Signup and view all the answers

What is one of the chronic effects of methamphetamine use?

Skin infections Signup and view all the answers

Study Notes

Stimulants Overview

Stimulants are substances that increase activity in the central nervous system (CNS)
They can increase alertness, energy, and focus.
Various types of stimulants exist, including synthetics (pharmaceuticals and illicitly manufactured) and organics (naturally occurring)
Some stimulants are medically used, while others are used recreationally.

CNS Stimulants

Cocaine (crack or hydrochloride): A naturally occurring alkaloid from coca leaves. Used for religious, mystical, social, and medicinal purposes to help with endurance, well-being, and alleviating hunger.
Amphetamines (e.g., D-amphetamine, methamphetamine, methylphenidate): Synthetic stimulants that mimic the structure of adrenaline, noradrenaline and dopamine. They enhance biological processes controlled by these neurotransmitters, and are used in obesity treatment, ADHD medication, and narcolepsy treatment.
Khat: Contains cathinone and methamphetamine.
Methylxanthines (e.g., caffeine, theophylline, theobromine): Naturally occurring stimulants. Caffeine sourced from coffee and tea, and theobromine from chocolate.

Pharmaceutical Stimulants & Medical Uses

Used for treating narcolepsy, hyperactivity in children, and fatigue. They are also used for mild depression treatment and appetite control.
Further uses include prevention and treatment of surgical shock, Parkinson's disease, and the maintenance of blood pressure during surgery and enhancing the action of analgesic drugs.

Cocaine Production

Coca paste is extracted from soaked and mashed coca leaves (60-80% cocaine).
Cocaine powder is made by mixing the paste with hydrochloric acid.
Freebase/crack cocaine is extracted from the powder by mixing it with baking soda.

Cocaine Pharmacokinetics

Absorption routes: insufflation (snorting), intravenous injection, inhalation (freebase), and oral ingestion
Plasma cocaine concentration varies depending on the administration route and can be measured over time.

Cocaine Pharmacokinetics: Distribution and Metabolism

Cocaine and amphetamines easily penetrate the blood-brain barrier.
Cocaine has a half-life of approximately 50 to 90 minutes.
Amphetamine half-life is approximately 5 to 10 hours.
Methamphetamine half-life is about 12 hours.
Metabolites of cocaine and amphetamine include active and inactive compounds.
Cocaine also undergoes autometabolism in the blood in addition to normal liver metabolism, where it's broken down into norcocaine, ecgonine methyl ester, and benzoylecgonine.

Cocaethylene

Alcohol inhibits cocaine metabolism, creating cocaethylene.
Cocaethylene has similar effects to cocaine but with greater cardiac toxicity and a longer half-life (3-5x longer than cocaine.)
It is associated with seizures, liver damage, and a compromised immune system.

Cocaine Pharmacodynamics

Cocaine is an indirect agonist for dopamine (DA), norepinephrine (NE), and serotonin (5-HT).
It blocks the reuptake of these monoamines.
Mechanisms also include effects on glutamate.

Two Primary Effects of Cocaine

Powerful sympathomimetic effect, similar to amphetamines (but more rapid).
Local anesthetic effect, which prevents neural firing when in direct contact with peripheral neurons.

Acute Effects of Cocaine (Moderate Doses)

Alleviation of fatigue (insomnia)
Increased resistance to boredom
Anorectic effect (suppression of appetite)
Elevated mood and sociability (emotional instability)

Acute Effects of Cocaine (High Doses)

Present-oriented/stimulus-bound behavior.
Hypervigilance
Psychomotor stimulation

Chronic Effects of Cocaine

Cardiomyopathy, stroke, renal damage, and liver damage.

Tolerance and Withdrawal (Cocaine)

Tolerance to the effects of cocaine and withdrawal symptoms (coke bugs) occur with repeated use.
Intense cravings and stimulant psychosis may develop.

Cocaine Withdrawal Symptoms

Symptoms from stopping cocaine use: vivid/unpleasant dreams, depression, hunger, fatigue, insomnia, hypersomnia, and psychomotor agitation.

Amphetamine Overview

A synthetic analog of ephedrine, active in mahuang.
Used in Chinese medicine (ma huang) for asthma.
Methamphetamine and methylphenidate (Ritalin) are very similar.
Medically used for obesity, ADHD, and narcolepsy.

How Amphetamines Work

Chemical structures mimic neurotransmitters (adrenaline, noradrenaline, and dopamine.)
Biological processes controlled by these neurotransmitters are enhanced.
Amphetamines are not rapidly metabolized.

Amphetamine Pharmacodynamics

Indirect agonist for dopamine (DA), norepinephrine (NE), and serotonin (5-HT).
Mechanisms include blockade of monoamine reuptake, inhibition of vesicular storage, and MAO metabolism, as well as reversing reuptake.

Short-Term Effects of Amphetamines

Enhancement of adrenaline, noradrenaline, and dopamine actions
Increased adrenaline and noradrenaline from nerve endings
Increased heart rate, blood pressure, and urinary retention
Nausea, vomiting, diarrhea, loss of appetite and weight loss, euphoria, and decreased sleep

Short-Term Effects of Amphetamines (Continued)

Increased alertness and energy
Focus narrowing
Thirst suppression
"Rush" effect

Long-Term Effects of Amphetamines

Tolerance
Psychosis
Exhaustion
Malnutrition
Interpersonal problems
Cognitive defects
Paranoia
Mood swings
Trouble breathing
Seizures
Brain hemorrhage
Heart failure
Hyperpyrexia
Coma

Methamphetamine

Derivative of amphetamine
First synthesized in Japan
Typically smoked
Associated with meth labs and is illegal in Canada.

Long-Term Effects of Methamphetamine

Dental problems
Undernourishment
Skin infections
Heart failure
Psychosis
Brain abnormalities

Tolerance, Withdrawal, and Addiction (Amphetamines)

High abuse potential.
Physical and psychological dependence.
Tolerance to euphoria, and appetite suppression.
Withdrawal symptoms include physical mild to moderate dysphoric syndrome symptoms and decreased activity, amotivation, and intense boredom for 1-10 weeks post-withdrawal.

Cost of Methamphetamine Use (2008)

13 million Americans used meth at least once.
6-8% of the total cost of drug abuse in the U.S..
Significant costs related to lost lives, productivity, drug treatment, law enforcement, and crime.

National Survey on Drug Use and Health (2009)

Cocaine use and methamphetamine use in the U.S.; 4.8 million Americans used cocaine, 788K used non-cocaine prescription-like stimulants, 387K of them used methamphetamines.

Use in Canada (2013-2017)

Rates of cocaine and meth possession incidents per 100,000 population showed increases in meth cases, but cocaine rates were consistently higher.

Inpatient Hospitalizations, Canada (2007-2014)

Inpatient hospitalizations related to cocaine and other CNS stimulants show a general decline over time in the period in question.

Pharmacotherapies

Treatment of withdrawal: Chlorpromazine (DA antagonist), Haloperidol (antipsychotic), Alprazolam (Xanax - benzodiazepine), and Antidepressants (fluoxetine or desipramine), Diazepam (Valium)

New Treatment Approaches (Immunological)

Antibodies against cocaine to break down the molecule and stop effects.
Phase III trials underway.
Inactivated cholera toxin protein attaching to inactivated cocaine.
Immune system creating antibodies.
Antibodies preventing cocaine reaching the brain when taken into the body, leading to reduced use desire.

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Description

This quiz explores key concepts related to pharmaceutical stimulants and their impact on substance abuse. It covers various drugs, their medical uses, and statistics regarding their abuse in the United States. Test your knowledge on the treatment of conditions like ADHD and panic attacks.