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Questions and Answers
What is the primary mechanism by which ergot derivatives decrease hyperperfusion of the basilar artery vascular bed?
Which of the following is a contraindication for the use of triptans?
Which triptan is indicated for use in children aged 6-17 years for acute migraines?
What is a common pharmacokinetic property of triptans?
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What adverse effects may occur with triptan use?
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What physiological function do interneurons in the spinal cord serve in relation to pain transmission?
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Which of the following correctly identifies a potential risk of opioid agonists?
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Which routes of administration for opioid agonists provide varying rates of absorption?
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What is one common adverse effect associated with opioid agonists?
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Which indication is commonly associated with the therapeutic use of opioid agonists?
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In which condition should caution be taken when prescribing opioid agonists?
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What type of metabolic process do opioid agonists typically undergo?
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Which of the following interactions could pose a risk when using opioid agonists?
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Which of the following accurately describes the pharmacokinetics of lasmiditan?
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What is a common adverse effect associated with the use of lasmiditan?
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Which of the following substances is primarily indicated for the prevention of migraine headaches?
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What caution should be noted regarding the use of CGRP inhibitors?
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Which drug interactions are of concern for lasmiditan and gepant CGRP inhibitors?
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What is one of the main therapeutic actions of opioid agonists?
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Which of the following is NOT an indication for opioid agonists?
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Which adverse effect is most commonly associated with opioid antagonists?
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What is a common caution for prescribing opioid agonists?
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What pharmacokinetic property is true for opioid agonists?
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Which of the following indicates a situation where an opioid antagonist would be indicated?
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Which adverse effect is less likely to occur with opioid agonists compared to other opioids?
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What is a significant drug–drug interaction to consider when administering opioid antagonists?
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Which part of the nervous system primarily regulates muscle contraction and relaxation?
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What distinguishes simple reflexes from complex reflexes?
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What is the primary role of the pyramidal tract?
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Muscle spasms can often result from which of the following?
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What condition is primarily associated with an increase in excitatory influences within the CNS?
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What is a common adverse effect associated with centrally acting skeletal muscle relaxants?
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Which of the following best describes direct-acting skeletal muscle relaxants?
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What is a contraindication for the use of Dantrolene?
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Which type of pain is associated with the transmission of unpleasant stimuli to the brain?
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Which neurotransmitter release is inhibited by Botulinum toxins?
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What effect might Dantrolene have on liver function?
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What is the primary function of antimigraine drugs?
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What may occur as a drug-drug interaction with Botulinum toxins?
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Which type of fibers primarily transmit pressure, stretch, and vibration sensations?
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Study Notes
Muscle Relaxants
- Muscle contraction and relaxation is regulated by spinal motor neurons, influenced by the basal ganglia, cerebellum, and cerebral cortex.
Types of Spinal Reflexes
- Simple Reflexes: Directly involve a sensory neuron and a motor neuron.
- Complex Reflexes: Involve interneurons connecting to brain centers for communication.
Brain Control of Movement
- Pyramidal Tract: Responsible for precise voluntary movements.
- Extrapyramidal Tract: Modulates involuntary muscle activity and helps maintain posture and balance.
Neuromuscular Abnormalities
- Muscle Spasms: Result from musculoskeletal injuries causing a flood of sensory impulses to the spinal cord.
- Muscle Spasticity: Caused by CNS neuron damage, often due to imbalanced excitatory and inhibitory signals.
Centrally Acting Skeletal Muscle Relaxants
- Therapeutic Actions: Interfere with CNS reflexes causing spasms; called spasmolytics.
- Indications: Used for pain relief in acute musculoskeletal conditions, often alongside therapy.
- Pharmacokinetics: Rapid absorption, liver metabolism, urine excretion.
- Contraindications: Allergies and spasms due to rheumatic disorders.
- Cautions: Care needed for conditions like epilepsy, cardiac dysfunction, or pregnancy.
- Adverse Effects: CNS depression, GI issues, hypotension, urinary problems, liver toxicity concerns with tizanidine.
Direct-Acting Skeletal Muscle Relaxants
- Therapeutic Actions: Prevent contraction directly, e.g., dantrolene blocks calcium release.
- Indications: Manage spasticity from neuromuscular diseases.
- Pharmacokinetics: Dantrolene is slowly absorbed, with a half-life of 4 to 8 hours; crosses the placenta.
- Contraindications: Allergies, certain spastic conditions, active liver disease.
- Cautions: Special consideration for women over 35, or those with a history of liver disease.
- Adverse Effects: CNS depression, potential liver damage, botulinum toxins cause various neurological effects.
Opioid Agonists
- Actions: Activate opioid receptors for analgesia, sedation, and euphoria; controlled substances with dependence potential.
- Indications: Used for severe pain relief, preoperative medication, and tailored analgesia.
- Pharmacokinetics: Fastest effect via IV; metabolized in the liver, excreted via urine.
- Contraindications: Known allergies, certain GI obstructions, and specific respiratory conditions.
- Cautions: Risk factors for respiratory issues, head injuries, and substance use disorders.
- Adverse Effects: Include respiratory depression, GI distress, orthostatic hypotension, and neurologic issues.
- Drug Interactions: Caution with other CNS depressants and certain drug classes like SSRIs.
Opioid Agonists-Antagonists
- Actions: Partial agonists at mu receptors, antagonists at kappa receptors; provide analgesia and sedation.
- Indications: Moderate to severe pain and opioid use disorder treatment.
- Pharmacokinetics: Readily absorbed, metabolized by the liver and excreted in urine.
- Contraindications: Known allergies, particularly to sulfites (for nalbuphine).
- Cautions: Need for caution in patients with physical dependence on opioids and respiratory conditions.
- Adverse Effects: May cause respiratory depression, nausea, psychiatric side effects, but lower dependence risk.
Opioid Antagonists
- Actions: Block opioid receptors to reverse opioid effects; essential for overdose treatment.
- Pharmacokinetics: Widely distributed, metabolized in the liver, excreted in urine.
- Contraindications: Allergies to the medication.
- Adverse Effects: Acute withdrawal syndrome and CNS excitability, potential cardiovascular effects.
Triptans
- Actions: Bind to serotonin receptors to cause cranial vessel vasoconstriction; used for acute migraines.
- Pharmacokinetics: Rapid absorption with liver metabolism; crosses placenta.
- Contraindications: Include known allergies, pregnancy, and CAD.
- Adverse Effects: Potential CNS and GI issues; almotriptan noted for fewer side effects.
- Drug Interactions: Care advised with ergot-containing drugs.
Calcitonin Gene-Related Peptide (CGRP) Inhibitors and Serotonin Agonists
- Actions: CGRP inhibitors block vasodilatory effects during migraines; specific serotonin agonists target migraine treatment.
- Pharmacokinetics: CGRP inhibitors absorbed via GI; monoclonal antibodies have long half-lives.
- Contraindications: Allergy signs.
- Adverse Effects: Risks include dizziness, hypersensitivity, GI upset, injection site reactions.
- Drug Interactions: Caution with CNS depressants and CYP3A4 inhibitors.
Key Questions
- Opioid agonists are prescribed for severe pain relief, especially during anesthesia (correct option: B).
- Rizatriptan is suitable for migraines in children aged 6-17 (correct option: C).
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Description
Explore the intricacies of muscle relaxants and their interaction with spinal motor neurons in Chapter 25. This quiz covers the regulatory influences of the brain on muscle movement and various types of spinal reflexes. Test your understanding of both simple and complex reflex mechanisms.
