Pharmocology- Opiods and NSAIDS

Opoid

•refers to any drug, natural or synthetic, that has actions similar to morphine.

•3 classes of opioid receptors

•Mu- most activated by opiod analgesic
•Kappa
Delta

Mu receptors responses

analgesia, respritory depression, sedation, EUphoria, physical dependance, decreased GI motility

Kappa receptor responses

analgesia, sedation, decreased gi motility

MOA of opioids

appear to mimic the effects of endogenous opioid peptides, primarily at mu receptors.

What is a life-threatening adverse effect of opioids?

Respiratory depression

What is the onset of respiratory depression dependent on?

Route of administration

Do patients develop tolerance to opioid-induced constipation?

No, patients do not develop tolerance to constipation.

How does hypotension related to opioid use change with standing or sitting?

It worsens with standing or sitting.

What adverse effect of opioids could compromise airways?

Cough suppression

How does emesis change with initial and subsequent doses of opioids?

Worsens with the initial dose and improves with more doses.

What are the two potential emotional effects of opioids?

Euphoria and dysphoria

What should be avoided due to sedation from opioids?

Hazardous activities

What is a characteristic pupil response associated with opioid use?

Miosis (pinpoint pupils)

What is a potential neurotoxic effect of opioids?

Myoclonus

What birth defects can be associated with opioid use?

Heart defects and spina bifida

What are two effects of prolonged opioid use?

Hormone changes and decreased immune function

tolerance

does must be increased to maintain effect

Does not develop constipation or miosis

Physical dependance

without continual presence of opioids withdrawal will occur

should be tapered

rearly lethal

What should be known about opioid medications and their regulation?

Opioids are controlled substances, classified as Schedule II with high abuse potential.

What class of drug is Morphine?

Opioid

What is the mechanism of action of Morphine?

mu receptor agonist, weak kappa receptor agonist

What is the primary therapeutic effect of Morphine?

Analgesia

What are some adverse effects of Morphine?

Respiratory depression, hypotension, sedation, constipation, nausea/vomiting, urinary retention, cough suppression, miosis, neurotoxicity, birth defects.

What is the black box warning associated with Morphine?

Avoid concomitant use with benzodiazepines and other CNS depressants including alcohol increased risk of profound sedation, respiratory depression, coma and death.

What are the routes of administration for Morphine?

IV, IM, SQ, PO, SL, PR
PO- long acting

what are the major difference between morphine and fentynyl?

only drug that can be administered transdermally
no renal impairment and doesn't effect BP as much

What class of drug is Fentanyl?

Opioid

What is the mechanism of action of Fentanyl?

mu receptor agonist, weak kappa receptor agonist

What is a primary therapeutic effect of Fentanyl?

Analgesia, substance use disorder

What are some adverse effects of Fentanyl?

Respiratory depression, hypotension, sedation, constipation, nausea/vomiting, urinary retention, cough suppression, miosis, neurotoxicity, birth defects.

What is the black box warning associated with Fentanyl?

Severe sedation, respiratory depression with opioids and other CNS depressing substances.

What are the routes of administration for Fentanyl?

IV, IM, SQ, PO, SL, intranasal, lozenge, transdermal

Hydromorphone compared to morphoine

hydromorphone is more potent need a smaller does

What class of drug is Methadone?

Opioid

What is the mechanism of action of Methadone?

mu receptor agonist, weak kappa receptor agonist, NMDA receptor antagonist

What are the therapeutic effects of Methadone?

Analgesia, substance use disorder

What are some adverse effects of Methadone?

Respiratory depression, hypotension, sedation, constipation, nausea/vomiting, urinary retention, cough suppression, miosis, neurotoxicity, birth defects, prolonged QTc

What is the black box warning associated with Methadone?

Severe sedation, respiratory depression with opioids and other CNS depressing substances

What are the routes of administration for Methadone?

IV, PO
ULTRA long-acting

What class of drug is Hydromorphone?

Opioid

What is the mechanism of action of Hydromorphone?

mu receptor agonist, weak kappa receptor agonist

What is the primary therapeutic effect of Hydromorphone?

Analgesia

What are some adverse effects of Hydromorphone?

Respiratory depression, hypotension, sedation, constipation, nausea/vomiting, urinary retention, cough suppression, miosis, neurotoxicity, birth defects.

What is the black box warning associated with Hydromorphone?

Severe sedation, respiratory depression with opioids and other CNS depressing substances.

What are the routes of administration for Hydromorphone?

IV, IM, SQ, PO

Oxycodone

•Short- and long-acting formulations available
•Available alone or in combination with other drugs

What is Norco? What vary?

Hydrocodone-acetaminophen
Dosage of opioid and acetaminophen varies

Codeine

cough suppressant mild to moderate pain

Meperidine

use declining now primary use is drig-induced rigors or post anesthesia shivering

Agonist-Antagonist Opioids

Lower potential for abuse, and respiratory depression

less powerful analgesic effects

provide opioid option for patients with sever pain

What are opioid antagonists?

Drugs that block the effect of opioid agonists.

What are the uses of opioid antagonists?

Treatment of opioid overdose.
Management of opioid use disorder.
Treatment of opioid-induced constipation.

What class of drug is Naloxone?

Opioid antagonist

What is the mechanism of action of Naloxone?

Competitive antagonist at opioid receptors

What happens if Naloxone is given prior, post or with no opioids?

prior-Blocks opioid effects
already reciving- Reverses analgesia, sedation, and respiratory depression
no opioid- no effect

What are the routes of administration for Naloxone?

IV, IM, SQ, intranasal

Methylnaltrexone class and MOA

opioid antagonist, selective MU opioid antagonist, only in GI tract

Methylnaltrexone therapeutic use

Opioid-induced constipation

Adverse effects of Methylnaltrexone

Abdominal pain, flatulence, nausea, diarrhea.
•Contraindicated in patients with bowel obstruction.

Naltrexone class and MOA

Opioid antagonist
Pure opioids antagonist

Naltrexone theraputic and adverse effects

opiod abuse alcohol abuse
liver injury with excessive use

Why is naltrexone not used very often?

•Prevents euphoria from opioids use, does not stop cravings
•Less effective for opioid use disorder than methadone.

Tramadol therapeutic use and class

Opioid

Weak mu receptor agonist, inhibits reuptake of norepinephrine and serotonin

Tramadol use and contraindications

Moderate to moderately severe pain

contraindicated- epilepsy, MAO inhibitors, suicide risk

A postoperative patient has an epidural infusion of morphine sulfate [Astramorph]. The patient's respiratory rate declines to 8 breaths per minute. Which medication would the nurse anticipate administering?
a) Naloxone [Narcan]
b) Acetylcysteine [Mucomyst]
c) Methylprednisolone [Solu-Medrol]
d) Protamine sulfate

a) Naloxone [Narcan]

The nurse is planning care for a patient receiving morphine sulfate [Duramorph] by means of a patient-controlled analgesia (PCA) pump. Which intervention may be required because of a potential adverse effect of this drug?
a) Administering a cough suppressant
b) Inserting a Foley catheter
c)Administering an antidiarrheal
d) Monitoring liver function tests

b) Inserting a Foley catheter

A nurse administers naloxone [Narcan] to a postoperative patient experiencing respiratory sedation. What undesirable effect would the nurse anticipate after giving this medication?
a) Drowsiness
b) Tics and tremors
c) Increased pain
d) Nausea and vomiting

c) Increased pain

What are the molecules involved in migraines and how do the effect them?

CGRP- increase during migraine, promotes vasodilation and inflammation

5HT (serotonin)- suppress migraine

Abortive headache therapy

drugs that stop an attack
2 classes-
nonspecific analgesics
migraine specific drugs

Preventive headache therapy

drugs that prevent attacks from happening
include-
beta blockers
tricyclic antidepressants
antiepileptic drugs

Abortive medications should be limited to

a few times per week medication overuse headache can develop

Analgesics for headaches

mild to moderate
aspirin, naproxen, acetaminophen, combination

What class of medication is Sumatriptan?

Serotonin receptor agonist

What is the mechanism of action of Sumatriptan?

Selective activation of serotonin receptors 1B and 1D
causing Vasoconstriction and CGRP decline

therapeutic use of sumatriptan

abort migraine headaches, cluster headaches

What are the adverse effects of sumatriptan?

Coronary vasospasm, chest symptoms, teratogenic

What are the contraindications for sumatriptan?

Ischemic heart disease, MI, uncontrolled hypertension, pregnancy

What drug interactions should be considered with sumatriptan?

Ergot alkaloids and other 'triptans,' MAOIs, SSRIs, SNRIs

Lasmiditan

Class: Serotonin receptor agonist

Mechanism of Action:Selective activation of serotonin receptors 1F- does not cause vasoconstriction

can Lasmiditan be used for patient with migraines and heart disease?

does not cause vasoconstriction so can be used

Lasmiditan therapeutic, adverse effects and drug interactions

abort migraine headaches,
AE- euphoria, hallucinations
DI- risk of serotonin syndrome

Ergotamine class ans MOA

class- ergot derivative
´Agonist activity at 1B and 1D serotonin receptors
´Blocks inflammation, Suppresses CGRP, Vasoconstriction

Ergotamine Therapeutic effect

2nd line treatment to abort migraine in patients who did not respond to a triptan.

ergotism

ischemic tissue necrosis and death report symptoms immediately

Ergotamine adverse effects, contraindications and Drug interactions.

AE- nausea vomiting, ergotism, physical dependance
CON_ renal or hepatic impairment, CAD, PVD, HTN
DI- triptans, CYP3A4 inhibitors

Ubrogepant class and MOA

Class: Calcitonin gene-related peptide receptor antagonist

MOA: Blocks CGRP receptors, results in decreased pain and inflammation

Ubrogepant Therapeutic and adverse effects and drug interactions

Therapeutic Effects: Abort migraine headaches

Adverse Effects: Nausea, somnolence

Drug Interactions: Drugs that utilize the CYP3A4 pathway - either inhibitors or inducers.

How long do the benefits of preventative drugs take to develop

4-6 weeks

Preventative migraine treatment indication

•Patients experiencing 3+ migraines/month
•Attacks that are severe
•Those that do not respond well to abortive treatment.

Preventative Therapy: Beta-Blockers

Propranolol or Metoprolol
´
First-line drugs for migraine prevention
-70% reduced
´
side effects include: extreme tiredness, fatigue,
´

Divalproex for headaches

valproic acid
duration and intensity not reduced
nausesa

Topiramate for headaches

expensive
more common side effects

Amitriptyline for headaches

benefits equal to propranolol
side effect -hypotension and anticholinergic effects

Erenumab

Class: Calcitonin gene-related peptide receptor antibodies

Mechanism of Action: Bind to, and blocks effects of CRGP

Therapeutic Effects: Migraine prevention

Adverse Effects: Injection site reaction, constipation and muscle cramping

Menstrual migraines treatment

estrogen supplements (climara) or triptans used for treatment

Botulinum Toxin for headaches

´Approved for chronic migraine (15+ headache days/month)
´Requires 31 injections into the muscles of head/neck/scalp
´Expensive with only modest benefits

cluster headaches

attack last 15 min to 2 hours
unilateral
2-3 attacks/ day x 2-3 months

Drug therapy for cluster headaches

preventative
suboccipital steroid injections- only approved treatment

may work-
´Systemic glucocorticoids
´Verapamil (FIRST-LINE)
Lithium (SECOND-LIFE)

´The nurse is preparing to give ergotamine [Ergomar]. This agent is effective against headaches of which origin?
a) Hypertension
b) Hyperthyroidism
c) Sinus pressure
d) No identifiable cause

d) No identifiable cause