Lecture #2 pt.2

Sumatriptan (Imitrex)

(Enteral & Parenteral) (Serotonin Receptor Agonist)

MOA: Binds to receptors on intracranial blood vessels and causes vasoconstriction and diminishes perivascular inflammation. (This reduces swelling and pain signals, helping relieve migraines!)

(It affects all the blood vessels in the body, so pts w/ CAD or HTN are contraindicated!)

Indications:

• Acute treatment for moderate to severe migraine.

• Acute treatment for cluster headache.

• Off label use: Abortive therapy of cyclic vomiting syndrome.

(first-line)

Sumatriptan (Imitrex) Adverse Effects

• Well-tolerated but side effects are transient and mild.

—> Chest symptoms—Heavy arms and chest pressure

• Coronary vasospasm in patient w/ CV history (CAD, uncontrolled HTN, angina)

• Teratogenic

Sumatriptan (Imitrex) Nursing Considerations

• Educate on proper administration for migraine treatment.

• Educate patient to avoid triggers and recognize symptoms of aura that occur prior to onset.

• Avoid in patient w/ significant CV history.

• Educate on contraception due to risk of fetal harm.

Ergotamine (Ergomar)

(PO, Rectal & SL) (Alkaloids)

MOA: Selectively binds and activates serotonin receptors located on intracranial blood vessels, resulting in vasoconstriction and reducing the blood flow in cerebral arteries.

Indications:

• Second-line for migraine attacks in patient who have not responded to triptan.

Ergotamine (Ergomar) Adverse Effects

• Well-tolerated at therapeutic levels

• Can worsen N/V

• Risk of dependence

• Overdose resulting in ergotism (toxicity):

—> Effects includes muscle pain, paresthesia in fingers and toes, and extremities cold and pale.

• Contraindicated for those w/ hepatic or renal impairment, sepsis, CAD, peripheral vascular disease (PVD), uncontrolled HTN.

• Can cause fetal harm.

Ergotamine (Ergomar) Nursing Considerations

• Education for short vs. long term use.

• Ensure adherence to dosage and duration.

• Provide education on signs of overdose and instruct to seek immediate attention.

• Monitor for liver or kidney injury, CV history, and sepsis.

What is muscle spasticity?

It is like a charley horse that never ends (a contraction). Symptoms include: stiff rigid muscles, involuntary contractions or muscle spasms, and overactive reflexes.

Usually will see this in SCIs or Multiple Sclerosis

**Might see in stroke pts…

Baclofen (Lioresal)

(PO) (Centrally-Acting Muscle Relaxer for Spasticity)

MOA: Acts within spinal cord to suppress hyperactive reflexes involved in regulation of muscle movement; may mimic GABA on spinal neurons.

Indications:

• Multiple Sclerosis

• Spinal Cord Injury

Baclofen (Lioresal) Adverse Effects

• CNS depressant-like effects in initial treatment

—>Drowsy, dizzy, weakness, fatigue

• Constipation

• Urinary retention

• Withdrawal from abrupt cessation (so, Taper-off slowly!)

—>Visual hallucinations, paranoid ideations, seizures

Baclofen (Lioresal) Nursing Considerations

• Pre- and post- administration s/s assessment.

• Education of proper use and w/ non-pharmacological treatments.

• Additive CNS depression w/ other similar agents, including alcohol, opioids, or benzodiazepines. (more CNS depression)

• Worsening of pre-existing urinary retention and psychiatry conditions.

Cyclobenzaprine (Flexeril)

(PO) (Centrally-Acting Skeletal Muscle for Muscle Spasm)

MOA: Acts primarily within brainstem to reduce tonic somatic motor activity.

Indications:

• Localized muscle spasms, such as musculoskeletal injury

Cyclobenzaprine (Flexeril) Adverse Effects

• CNS depressant-like effects in initial treatment.

• Anticholinergic effects:

—> Urinary retention, constipation, blurred vision, dry mouth, photophobia.

• Dysrhythmias, including ST segment and conduction delay.

Cyclobenzaprine (Flexeril) Nursing Considerations

• Pre- and post- administration s/s assessment.

• Education on proper use and w/ non-pharmacological treatments, including physical therapy and heat therapy.

• Additive CNS depression w/ other similar agents, including alcohol, opioids, or benzodiazepines

• Education on non-pharmacological methods w/ managing anticholinergic effects, particularly in long-term use.

*Have pt take their first dose in the evening b/c it might cause drowsiness.

Opioid analgesics primarily act on ______ receptors, some _______, not ________.

mu; kappa; delta

For opioid administration, you will always perform a…

pre- and post- administration assessment

T/F: Opioid administration is more effective if given around the clock (ATC) vs as needed (PRN) for the first 24 hours post-op.

True

Morphine

(PO & Parenteral) (Pure Agonist Opioid Analgesic (The Prototype))

MOA: Acts primarily on mu receptors to mimic endogenous opioid peptide actions.

Indications:

• Acute and chronic pain relief (moderate to severe pain)

• Myocardial Infarction (MI)

• Pre-op sedation

• Anxiety

Morphine & Fentanyl (Duragesic) Adverse Effects

• Respiratory depression and cough suppression

• Constipation, emesis, and urinary retention

• Sedation

• Orthostatic hypotension and increased intracranial pressure (ICP) secondary to autoregulatory cerebrovascular dilation.

• Physical dependence, euphoria, and potential for abuse

Morphine Nursing Considerations

• Tolerance, monitor possible physical dependence and abuse.

• Assess and reassess pain, respiratory status, and GI function.

• Manage constipation w/ increased fluid and fiber intake.

• Monitor use w/ other CNS depressants, anticholinergics, antihypertensives, etc.

• Provide ventilatory support and administer antagonist (naloxone) for toxicity.

What medication is used for opioid toxicity?

Narcan (Naloxone)

Fentanyl (Duragesic)

(IM, IV, Transdermal, & Nasal Spray) (Pure Agonist Opioid Analgesic)

MOA: High potency; acts primarily on mu receptors to mimic endogenous opioid peptide actions.

Indications:

• Acute and chronic pain relief

• Surgical analgesia

• Off label: uses of rapid sequence intubation & ICU sedation

Fentanyl (Duragesic) Nursing Considerations

• Transmucosal for breakthrough pain in patient w/ cancer & opioid tolerance only; monitor possible physical dependence and abuse; proper administration for transdermal patch.

• Assess & reassess pain, respiratory status, and GI function

• Most effective if administered ATC vs PRN

• Monitor use w/ other central nervous system (CNS) depressants, anticholinergics, antihypertensives, etc.

• Administer antagonists for toxicity (narcan).

Codeine

(PO tablet or Solution) (Moderate to Strong Opioid Agonist)

MOA: Acts primarily on mu receptors to mimic endogenous opioid peptide actions.

Indications:

• Mild to moderate pain

• Short-term symptomatic relief of cough

Codeine Adverse Effects

• Similar to morphine, but slightly lesser degree.

• Excessive sleepiness, breathing difficulty, lethargy, and poor feeding in infants from nursing mothers on codeine.

Codeine Nursing Considerations

• Same consideration as other opioids.

• Other formulations include those combined w/ other medications, including promethazine, guaifenesin, acetaminophen, or aspirin.

• Assess the patient’s benefits versus risks due to risk of abuse, misuse, and opioid addiction, leading to overdose and death.

Tramadol (Ultram)

(PO) (Opioid/Non-Opioid)

MOA: Pain relief is achieved through weak mu agonist activity and block of norepinephrine and serotonin reuptake for the treatment of moderate to severe pain.

Tramadol (Ultram) Adverse Effects

• Due to weak mu activity, risk for respiratory depression is low and rare.

• Common AE include sedation, dizziness, HA, dry mouth, and constipation.

• Serotonin syndrome if co-administered w/ agents that enhance serotonergic transmission.

Tramadol (Ultram) Nursing Considerations

• Abuse potential lower than pure opioid agents (Schedule IV, per DEA)

• Utilized in suicide attempts in combination w/ other CNS depressants (e.g. benzodiazepines, ETOH, etc.)

• Closely monitor and educate patient on use w/ SSRI, SNRI, Tricyclic, MAOI, and triptan medications. (These all increase serotonin!)

• Formulation also include combination w/ acetaminophen.

Typical Opioid Withdrawal Symptoms

• Cold Shakes

• Chills and Sweating

• Fever-like symptoms

• Mood Swings

• Anxiety and Depression

• Bone Pain

• Vomiting

• Insomina

• Diarrhea

Methadone (Dolophine)

(PO, IM, & IV) (Long-Acting Pure Agonist)

MOA: Acts primarily on mu receptors to mimic endogenous opioid peptide actions.

Indications:

• Pain relief

• Maintenance treatment of opioid use disorder

• Short-term supervision of opioid withdrawal

Methadone (Dolophine) Adverse Effects

• Similar to morphine and fentanyl

• Prolonged QT interval and fatal dysrhythmias, including Torsades de pointes associated w/ higher doses. (The only difference!)

Methadone (Dolophine) Nursing Considerations

• Same considerations as morphine & fentanyl.

• Establish baseline ECG and monitor heart rhythm on telemetry as well as s/s indicative of heart rhythm change.

• Thorough history and assessment of opioid abuse prior to use for addiction to ensure proper methadone substitution dosing.

Buprenorphine/Naloxone (Suboxone)

(Buccal film, Injection, FL, flim, PO, Subdermal implant, and Transdermal Patch) (Agonist-Antagonist Opioid Analgesic)

MOA: Both agonist and antagonist action are mu receptors and antagonist action at kappa receptors. (Agonist at mu and Antagonist at kappa)

(so bascially…it helps prevent withdrawal symptoms and cravings for opioids, reducing the risk of relapse!)

Indications:

• Acute and chronic pain relief

• Opioid use disorder & opioid withdrawal

Buprenorphine/Naloxone (Suboxone) Adverse Effects

• Mild respiratory depression

• Prolonged QT interval and fatal dysrhythmias

Buprenorphine/Naloxone (Suboxone) Nursing Considerations

• Same considerations as morphine & fentanyl.

• Establish baseline ECG and monitor heart rhythm on telemetry as well as s/s indicative of heart rhythm change.

• Thorough history and assessment of opioid abuse prior to use for addiction.

• Naloxone cannot readily reverse toxicity that has already developed.

Naloxone (Narcan)

(IV, IM, SQ, & Intranasal) (Competitive Antagonist)

MOA: Antagonist at opioid receptors that blocks opioid action. (Knocks opioid off receptor and takes over!)

Indications:

• Opioid overdose (respiratory depression, coma, etc.)

• Reversal of post-operative opioid effects

• Reversal of neonatal respiratory depression

Naloxone (Narcan) Nursing Considerations

• Will not see reversal if depression is caused by other agent (benzo, ETOH, etc), but can help rule out opioid etiology if no response after multiple doses.

• Due to short half-life, may need to repeat doses during overdose (e.g., 0.4 mg IV every 2-5 minutes while providing oxygenation and ventilatory support)

• Reversal of effects include onset of pain

• Other formulations can help w/ management of opioid-induced constipation and opioid addiction.