Pharmacology: Methylxanthines and Amphetamines
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Questions and Answers

Which of the following is a primary action of Methylxanthines?

  • Block phosphodiesterase (correct)
  • Selective NE reuptake blockage
  • Inhibit dopamine reuptake
  • Stimulate presynaptic NE release

What is a common therapeutic use of Modafinil?

  • Addressing narcolepsy (correct)
  • Managing obesity
  • Treating anxiety disorders
  • Preventing hypertension

Atomoxetine works primarily as which type of medication?

  • Serotonin agonist
  • CNS stimulant
  • Dopamine reuptake inhibitor
  • Selective NE reuptake blocker (correct)

What is a significant side effect associated with the use of CNS stimulants?

<p>Irritability (B)</p> Signup and view all the answers

Which drug is considered as the #1 treatment for children with ADHD?

<p>Methylphendiate (Ritalin) (B)</p> Signup and view all the answers

What is one of the reasons CNS stimulants should be avoided in certain patients?

<p>History of drug abuse (B)</p> Signup and view all the answers

Ephedrine functions through which mechanism of action?

<p>Mixed-acting monoamine release (C)</p> Signup and view all the answers

What condition is not typically treated by Methamphetamine?

<p>Chronic bronchitis (A)</p> Signup and view all the answers

What is the mechanism of action for Methylxanthines?

<p>Block phosphodiesterase and adenosine (C)</p> Signup and view all the answers

Which of the following drugs is a prodrug of amphetamine?

<p>Lisdexamfetamine (B)</p> Signup and view all the answers

Which CNS stimulant is primarily associated with dopamine reuptake inhibition?

<p>Methylphenidate (D)</p> Signup and view all the answers

What is a significant adverse effect associated with high doses of CNS stimulants?

<p>Increased heart rate and blood pressure (C)</p> Signup and view all the answers

Why should CNS stimulants be avoided in certain patient populations?

<p>They can exacerbate anxiety or depression (D)</p> Signup and view all the answers

Which of the following conditions is Modafinil primarily used to treat?

<p>Obstructive sleep apnea (C)</p> Signup and view all the answers

What is the primary use of Ephedrine in a clinical setting?

<p>Anesthesia induced hypertension (B)</p> Signup and view all the answers

Which drug is considered to have less addictive potential compared to traditional CNS stimulants?

<p>Atomoxetine (A)</p> Signup and view all the answers

Flashcards

Methylxanthines

CNS stimulants found in caffeine, chocolate, and tea. They work by blocking phosphodiesterase, increasing cAMP, and boosting alertness, while also blocking adenosine, increasing heart rate, and relaxing bronchial muscles.

Amphetamines

CNS stimulants used to treat ADHD, narcolepsy, and obesity. They block the reuptake of norepinephrine and dopamine, increasing their levels at the synapse.

Lisdexamfetamine

A prodrug of amphetamine, used to treat ADHD and obesity. It converts to amphetamine in the body, offering an alternative when tolerance to amphetamine develops.

Methylphenidate (Ritalin)

A primary dopamine reuptake blocker used to treat ADHD. It is commonly prescribed for children with ADHD.

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Atomoxetine

A non-stimulant ADHD medication that selectively blocks norepinephrine reuptake. It has fewer dopaminergic effects than other ADHD medications.

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CNS Stimulant Dependence

CNS stimulants create significant psychological dependence and are highly addictive. Withdrawal is relatively mild but managing the urge to restart use often needs support.

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CNS Stimulant Adverse Effects

CNS stimulants can cause headaches, dizziness, tremors, irritability, insomnia, appetite suppression, weight loss, and dry mouth (xerostomia). High doses can lead to increased heart rate and blood pressure.

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Contraindications for CNS Stimulants

Avoid prescribing CNS stimulants to patients with a history of drug abuse, hyperthyroidism, hypertension, psychosis, anxiety, or depression.

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Methylxanthines: What are they?

A group of CNS stimulants found in everyday substances like caffeine, chocolate, and tea. They work by blocking phosphodiesterase and adenosine.

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Amphetamine: What does it do?

A CNS stimulant that treats ADHD, narcolepsy, and obesity. It works by blocking the reuptake of norepinephrine and dopamine, leading to increased levels in the synapse.

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Lisdexamfetamine: Why is it used?

A prodrug of amphetamine, used to treat ADHD and obesity. It converts to amphetamine in the body, offering an alternative when tolerance to amphetamine develops.

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Methylphenidate: What is its purpose?

A primary dopamine reuptake blocker used to treat ADHD. It is a common treatment for children with ADHD.

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Atomoxetine: How is it different?

A non-stimulant ADHD medication that selectively blocks norepinephrine reuptake. It has fewer dopaminergic effects than other ADHD medications.

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Modafinil: What is its effect?

A CNS stimulant used to treat narcolepsy and obstructive sleep apnea. It has little euphoria, low adverse effects, and low addiction potential.

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Acute Psychosis from CNS Stimulants: What are the signs?

Overuse of CNS stimulants can lead to acute psychosis characterized by panic, anxiety, confusion, and aggression.

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Study Notes

Methylxanthines

  • Found in caffeine, chocolate, and teas
  • Mechanism of action: blocks phosphodiesterase (increasing cAMP and CNS alertness) and blocks adenosine (increasing heart rate and relaxing bronchial smooth muscle)
  • Off-label uses: airflow obstruction (COPD/asthma), bradycardia after heart transplant, acute cardiac decompensation

Amphetamines

  • Treat ADHD, ADD, narcolepsy, and obesity
  • Mechanism of action: reuptake blocker, blocking the reuptake of norepinephrine (NE) and dopamine, increasing their levels at the synaptic terminal.

Lisdexamfetamine

  • A prodrug of amphetamine
  • Treats ADHD and obesity
  • Can be used if tolerance develops to amphetamine or adderall

Methamphetamine

  • Treats ADHD and obesity
  • Lab-manufactured
  • Highly abused drug
  • Mechanism of action: reuptake blocker, blocking the reuptake of NE and dopamine increasing their levels at the synaptic terminal

Methylphenidate (Ritalin)

  • Primarily affects dopamine
  • First-line treatment for children with ADHD
  • Treats ADD and ADHD

Atomoxetine

  • Selective norepinephrine (NE) reuptake blocker
  • First non-stimulant for ADHD
  • Treats ADHD
  • Fewer dopaminergic effects, more adrenergic effects

Ephedrine

  • Mechanism of action: mixed-acting monoamine release, stimulating presynaptic NE release and acting as an α/β-adrenergic receptor agonist
  • Therapeutic uses: anesthesia-induced hypertension, cardiogenic shock, nasal congestion

Modafinil

  • Mechanism of action: atypical transporter, not fully understood
  • Low euphoria, low adverse effects, low addiction
  • Therapeutic uses: narcolepsy, obstructive sleep apnea, used by the military for wakefulness

CNS Stimulant Dependence

  • High psychological dependence; highly addictive
  • Schedule II drug
  • Mild physical withdrawal; treatment usually not needed
  • Focus on helping patients resist restarting compulsive use

CNS Adverse Effects

  • Neurological: headache, dizziness, tremors, irritability, insomnia
  • Appetite: appetite suppression, weight loss, growth suppression (children/adolescents) - consider "drug holidays"
  • Mouth: xerostomia (dry mouth) due to vasoconstriction decreasing saliva, leading to tooth decay
  • Cardiovascular: palpitations, chills, cardiac arrhythmias, chest pain; high doses lead to increased heart rate and blood pressure

Contraindications for CNS Stimulants

  • History of drug abuse
  • Hyperthyroidism
  • Hypertension
  • Psychosis
  • Anxiety
  • Depression

Acute Psychosis Associated with CNS Stimulants

  • Panic states
  • Anxiety
  • Confusion
  • Aggression

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Description

Explore the mechanisms and uses of methylxanthines and amphetamines in this pharmacology quiz. Learn about their effects on the central nervous system, treatment applications for ADHD, and the implications of drugs like methamphetamine. Test your knowledge on these important pharmacological agents.

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