Pharmacology of Stimulants and Methylxanthines
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Questions and Answers

Which of the following describes the mechanism of action for methylxanthines?

  • Inhibits dopamine reuptake.
  • Blocks phosphodiesterase and adenosine receptors. (correct)
  • Stimulates GABA receptors.
  • Increases serotonin levels in the brain.

    • What is the primary use of lisdexamfetamine?

  • Treat depression and anxiety.
  • Relieve pain from migraines.
  • Treat ADHD and obesity. (correct)
  • Act as a prodrug for methamphetamine.

    • What type of drug is atomoxetine and what condition does it primarily treat?

  • A dopamine agonist; treats schizophrenia.
  • A stimulant; treats narcolepsy.
  • A selective NE reuptake blocker; treats ADHD. (correct)
  • A selective serotonin reuptake inhibitor; treats depression.

    • Which of the following is NOT a common CNS adverse effect associated with CNS stimulants?

    <p>Weight gain</p> Signup and view all the answers

    What therapeutic effect does modafinil primarily provide?

    <p>Treats narcolepsy and obstructive sleep apnea.</p> Signup and view all the answers

    Which of the following conditions indicates that CNS stimulants should be avoided?

    <p>Hypertension</p> Signup and view all the answers

    Which statement best describes methamphetamine?

    <p>A synthetic stimulant with high potential for abuse.</p> Signup and view all the answers

    What is a significant psychological effect of dependence on CNS stimulants?

    <p>Highly addictive nature.</p> Signup and view all the answers

    Methylxanthines are seen in ______, chocolate, and teas.

    <p>caffeine</p> Signup and view all the answers

    Amphetamines are commonly used to treat ______, ADD, narcolepsy, and obesity.

    <p>ADHD</p> Signup and view all the answers

    The prodrug of amphetamine is ______.

    <p>lisdexamfetamine</p> Signup and view all the answers

    Methamphetamine is known to be a highly ______ drug.

    <p>abused</p> Signup and view all the answers

    Atomoxetine is a selective ______ reuptake blocker.

    <p>NE</p> Signup and view all the answers

    Modafinil is used as a treatment for ______ and obstructive sleep apnea.

    <p>narcolepsy</p> Signup and view all the answers

    A common CNS adverse effect of stimulants is ______.

    <p>insomnia</p> Signup and view all the answers

    Xerostomia, or dry mouth, is caused by vasoconstriction decreasing ______.

    <p>salivation</p> Signup and view all the answers

    Methylxanthines block phosphodiesterase, increasing _____ and CNS alertness.

    <p>cAMP</p> Signup and view all the answers

    Ephedrine is known to stimulate presynaptic _____ release.

    <p>NE</p> Signup and view all the answers

    Atomoxetine is the first non-stimulant drug for _____.

    <p>ADHD</p> Signup and view all the answers

    Methamphetamine is primarily used to treat ADHD and _____.

    <p>obesity</p> Signup and view all the answers

    CNS stimulants can cause symptoms such as headache, dizziness, and _____.

    <p>insomnia</p> Signup and view all the answers

    The therapeutic uses of modafinil include narcolepsy and _____ sleep apnea.

    <p>obstructive</p> Signup and view all the answers

    Methylphenidate is primarily a _____ reuptake blocker.

    <p>dopamine</p> Signup and view all the answers

    Physical withdrawal from CNS stimulants is typically _____ and treatment is usually not needed.

    <p>mild</p> Signup and view all the answers

    Lisdexamfetamine is a prodrug of ______.

    <p>amphetamine</p> Signup and view all the answers

    Methamphetamine is known for its high potential for ______.

    <p>abuse</p> Signup and view all the answers

    Atomoxetine works as a selective ______ reuptake blocker.

    <p>NE</p> Signup and view all the answers

    Ephedrine acts as an A/B adrenergic receptor ______.

    <p>agonist</p> Signup and view all the answers

    Methylphenidate is primarily used to treat ______ and ADHD.

    <p>ADD</p> Signup and view all the answers

    Common CNS adverse effects include headache, ______, and irritability.

    <p>dizziness</p> Signup and view all the answers

    The therapeutic effects of modafinil include treating narcolepsy and ______ sleep apnea.

    <p>obstructive</p> Signup and view all the answers

    General anesthesia involves complete loss of ______ and patients won’t remember anything.

    <p>consciousness</p> Signup and view all the answers

    Local anesthesia is similar to regional but is mainly used in ______ medicine.

    <p>dentistry</p> Signup and view all the answers

    Amino ______ are metabolized by the liver in the body.

    <p>amides</p> Signup and view all the answers

    Cocaine is only used for ______ due to its potential for toxicity.

    <p>topical</p> Signup and view all the answers

    Bupivacaine causes slight ______ and is used during labor.

    <p>vasodilation</p> Signup and view all the answers

    Malignant Hyperthermia is characterized by high ______ and can be treated with dantrolene.

    <p>temperature</p> Signup and view all the answers

    Proprofonol is a GABA receptor positive ______, known to cause CNS depression.

    <p>modulator</p> Signup and view all the answers

    Etomidate is a general anesthetic indicated for patients with ______.

    <p>hypertension</p> Signup and view all the answers

    Lidocaine has a rapid ______ and is widely used as a local anesthetic.

    <p>onset</p> Signup and view all the answers

    If there is a decrease in pH, the ______ of the local anesthetic can increase.

    <p>dose</p> Signup and view all the answers

    Study Notes

    Methylxanthines

    • Found in caffeine, chocolate, and teas
    • Mechanism of action: blocks phosphodiesterase, increasing cAMP and CNS alertness; blocks adenosine, increasing heart rate and relaxing bronchial smooth muscles
    • Off-label uses: COPD/Asthma, bradycardia post-heart transplant, acute cardiac decompensation

    Amphetamines

    • Used to treat ADHD, ADD, narcolepsy, and obesity
    • Examples: Amphetamine, Adderall

    Lisdexamfetamine

    • A prodrug of amphetamine
    • Treats ADHD and obesity
    • Useful when tolerance develops to amphetamine/Adderall

    Methamphetamine

    • Used to treat ADHD and obesity
    • Lab-produced
    • Highly abused
    • Mechanism of action: blocks the reuptake of norepinephrine and dopamine, increasing their synaptic terminal levels

    Methylphenidate (Ritalin)

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

    Atomoxetine

    • Selective norepinephrine reuptake blocker
    • First non-stimulant ADHD medication
    • Treats ADHD
    • Fewer dopaminergic effects, more adrenergic effects

    Ephedrine

    • Mechanism of action: mixed-acting monoamine release; stimulates presynaptic norepinephrine release and is an alpha/beta adrenergic receptor agonist.
    • Therapeutic uses: anesthesia-induced hypertension, cardiogenic shock, nasal congestion

    Modafinil

    • Mechanism of action: atypical transporter; not fully understood
    • Low euphoria, adverse effects, and addiction potential
    • Treats narcolepsy and obstructive sleep apnea
    • Used by the military for sustained alertness

    CNS Stimulant Dependence

    • High psychological dependence
    • Highly addictive
    • Schedule II drug
    • Mild physical withdrawal; treatment often unnecessary
    • Help needed for patients to avoid relapse

    CNS Adverse Effects of CNS Stimulants

    • Headache
    • Dizziness
    • Tremors
    • Irritability
    • Insomnia
    • Appetite suppression

    Appetite Suppression from CNS Stimulants

    • Leads to weight loss and growth suppression (children/adolescents)
    • Allow for "drug holidays" to restore appetite

    Xerostomia (Dry Mouth)

    • Caused by vasoconstriction, decreasing saliva production
    • Can contribute to tooth decay

    Cardiovascular (CV) Effects

    • Palpitations
    • Chills
    • Cardiac arrhythmias
    • Chest Pain
    • High doses (acute toxicity): increased heart rate and blood pressure

    Narcolepsy Drugs (e.g., Modafinil)

    • Lack of drug tolerance

    Contraindications for CNS Stimulants

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

    Acute Psychosis from CNS Stimulants

    • Panic states
    • Anxiety
    • Confusion
    • Aggression

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    Description

    This quiz covers the pharmacological aspects of methylxanthines and various stimulant medications used for treating conditions like ADHD and obesity. Explore their mechanisms of action, therapeutic uses, and notable examples to test your knowledge in this important area of pharmacology.

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