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

What therapeutic effect does modafinil primarily provide?

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

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

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

Which statement best describes methamphetamine?

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

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

<p>Highly addictive nature. (C)</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

Flashcards

Methylxanthines

Substances like caffeine, found in coffee and tea, that prevent an enzyme from working and affect alertness and heart rate.

Amphetamines (Treatment)

Drugs used to treat conditions like ADHD, narcolepsy, and obesity by increasing dopamine and norepinephrine in the brain.

Methylphenidate (Ritalin)

A stimulant primarily affecting dopamine, often used to treat attention deficit hyperactivity disorder (ADHD) and in children.

Atomoxetine (non-stimulant)

A non-stimulant ADHD medication focusing on norepinephrine, for those who don't respond well to stimulants.

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CNS Stimulant Dependence

A high risk of addiction with CNS stimulants requiring patient support to resist cravings.

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CNS Stimulant Adverse Effects

Potential side effects include headaches, dizziness, tremors, insomnia, and appetite suppression (weight loss, growth issues in children).

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Modafinil use

Medication for narcolepsy and sleep disorders. (Little euphoria, low addiction).

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Contraindications for CNS Stimulants

Avoid in those with a history of drug abuse, hyperthyroidism, hypertension, psychosis, significant anxiety or depression.

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Amphetamine (MOA)

Amphetamine increases the levels of norepinephrine and dopamine at the synapse by blocking their reuptake back into the presynaptic neuron.

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Lisdexamfetamine (Prodrug)

A prodrug that converts into amphetamine in the body, used to treat ADHD and obesity. Offers an alternative when tolerance to amphetamine develops.

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Methylxanthines (Caffeine)

A group of drugs that include caffeine, found in coffee and tea. They work by blocking an enzyme called phosphodiesterase, which increases a chemical called cAMP in your brain, leading to alertness. They also block adenosine, a neurotransmitter that makes you sleepy, resulting in increased heart rate and relaxed airways.

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Amphetamines (ADHD Treatment)

A group of stimulant drugs that increase the levels of dopamine and norepinephrine in the brain, helping to improve focus and attention in individuals with ADHD, narcolepsy, and sometimes obesity.

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Methamphetamine (Highly Abused)

A stimulant made in a lab. It is highly addictive due to its strong effects on dopamine and norepinephrine in the brain. It blocks the reuptake of these neurotransmitters, causing a rush of energy and euphoria.

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Ephedrine (Multi-Acting)

A stimulant that acts on both the sympathetic nervous system and the brain. It releases norepinephrine and works as a direct agonist on alpha and beta adrenergic receptors, leading to increased blood pressure and airway relaxation.

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Modafinil (Atypical)

A drug used to treat narcolepsy and other sleep disorders. It promotes wakefulness but has a low risk of addiction and minimal side effects.

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Methylxanthines: MOA

Methylxanthines, like caffeine, block the enzyme phosphodiesterase, increasing cyclic AMP (cAMP) levels in the brain. This boost in cAMP promotes alertness. They also block adenosine, a neurotransmitter that induces sleepiness, thus increasing heart rate and relaxing airways.

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Stimulants: ADHD Treatment

Stimulants like methylphenidate (Ritalin) and amphetamines increase dopamine and norepinephrine levels, which improves focus and attention in individuals with ADHD.

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Atomoxetine (Strattera)

Atomoxetine is a non-stimulant ADHD medication that selectively blocks norepinephrine reuptake. Unlike stimulants, it has fewer dopaminergic effects.

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Methamphetamine: Abuse Potential

Methamphetamine, a stimulant synthesized in labs, is highly abused due to its potent effects on dopamine and norepinephrine. It blocks their reuptake, causing a rush of energy and euphoria.

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Dependence of CNS Stimulants

CNS stimulants, like amphetamines, are highly addictive due to their strong effects on the brain's reward system. They lead to extensive psychological dependence and are classified as Schedule 2 drugs.

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Ephedrine: MOA

Ephedrine acts as both a monoamine releaser and a direct adrenergic receptor agonist, stimulating the release of norepinephrine and activating both alpha and beta receptors.

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Narcolepsy Drugs (Modafinil): Tolerance

Narcolepsy drugs like Modafinil do not have a tolerance, unlike other CNS stimulants. This means they maintain their effectiveness over time.

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General Anesthesia

A state of complete unconsciousness where the patient has no memory of the procedure.

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Regional Anesthesia

Numbs a specific area of the body, often used for procedures like childbirth.

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Local Anesthesia

Similar to regional anesthesia but typically used for smaller areas, like dental procedures.

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Conscious Sedation

A state of decreased consciousness, not full sleep, used to reduce discomfort during procedures.

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Amino Esters

Local anesthetics that have one 'i' in their chemical name and are broken down in the blood.

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Amino Amides

Local anesthetics that have two 'i's in their chemical name and are broken down in the liver.

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Vasodilation

Widening of blood vessels, which can cause local anesthetics to spread quickly, potentially leading to unwanted effects.

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Why is Ephedrine Given with Local Anesthesia?

Ephedrine causes vasoconstriction, which helps to slow down the spread of local anesthetics and prolong their effect.

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Local Anesthetics: Water Soluble vs. Lipophilic

Local anesthetics are water-soluble for injection but must be lipophilic to cross cell membranes and reach their target in the body.

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Cocaine: Local Anesthetic

A local anesthetic with vasoconstriction properties, but only for topical use due to potential for abuse.

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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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