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Pharmacology I

Opioids
Objectives
Discuss the basic pharmacology of opioids
Discuss clinical implications of opioid use
Identify opioid antagonists
Explain nursing implications related to opioid use
Discuss non-opioid centrally acting analgesics
Endogenous Opioids Peptides
Enkephalins
Endorphins
Dymorphins
Opioid Receptors
Mu-morphine binds to mu
Analgesia, respiratory depression, sedation, euphoria, physical
dependence, and decreased GI motility

Kappa
Analgesia, sedations, and decreased GI motility

Delta
Opioid analgesics do not interact with delta
Classification
Pure opioid agonists

Agonist-antagonists

Pure opioid antagonists


Strong Opioid Analgesics

Prototype: Morphine- binds to mu


Schedule II - moderate to high abuse potential
Therapeutic Uses
Analgesia
More effective against dull pain, than sharp intermittent
Post operative pain, cancer pain, labor and delivery pain
Can be used for MI, dyspnea with heart failure
Mechanism of Action
Binds to mu receptors
Strong Opioid Analgesics
Prototype: Morphine
Adverse Effects
Push slow, dilute w saline
Respiratory depression

Elevated intracranial pressure-ppl with
Constipation

head injury shouldnt get morphine bc
Orthostatic hypotension

it could make it worse due to reduced
Urinary retention- with a history of prostate
issue and then adding this- makes worse ventilation which causes increased CO2
Cough suppression- this is bad if they are post buildup
op, could develop pneumonia-atelectasis Euphoria/Dysphoria
Biliary colic- dont give to anyone with Sedation
gallbladder pain-will cause spasm of sphincter Miosis-pinpoint pupils
Emesis
Birth defects
Neurotoxicity
Strong Opioid Analgesics
Prototype: Morphine
Pharmacokinetics
Routes of administration-pca pumps, epidural drip
Po, IV, IM, subQ, epidural, and intrathecal
Poor lipid solubility-can cross the BBB in infants
Does not cross the blood brain barrier easily
Inactivated by the liver
Eliminated through the kidneys
Strong Opioid Analgesics
Prototype: Morphine
Tolerance
With MSO4 tolerance develops to analgesia, euphoria, sedation, and
respiratory depression-if taking for a long time, higher doses will be
needed
Tolerance does not develop to constipation or miosis
Cross tolerance exists among other opioid agonists
Strong Opioid Analgesics
Prototype: Morphine
Physical Dependence- methadone also used as alternative, it
doesnt need to be dosed as frequently as morphine
Abstinence syndrome when withdrawn
Intensity of withdrawal parallels the degree of physical dependence
DO NOT WITHDRAWAL ABRUPTLY- between 7-10 days there is a risk of
withdrawl
Abstinence syndrome
Strong Opioid Analgesics
Prototype: Morphine
Precautions
Decreased respiratory reserve-pts w preexisting resp drive- if supressed even more
this causes more problems
Labor and delivery- can supress uterine contraction- used at certain stages in labor
Head injury
Old and young
Liver impairment- use decreased doses
Drug Interactions
CNS depressants, anticholinergic drugs- cause constipation too, hypotensive drugs,
Mao inhibitors-risk for hypertensive crisis, opioids,
Strong Opioid Analgesics-morphine, dilauded,
fentanyl
Prototype: Morphine
Dosage Guidelines
Fixed schedule- every 4 hours for example, has to do with the plateau.
Have to get pain under control.
Can also alternate opiate with another drug so pt not getting as much
opiod but still have outcome
Monitor vital signs, especially respiratory rate- if pt cant stay awake but
says they have more pain- not arouasable, low RR etc- hold med and notify
MD
Strong Opioid Analgesics
Other strong opioids
Fentanyl- given IV and thru patch. The patch takes up to 48 hours to get the full
effect. May need little breakthrough doses. Sign date and initial new patches Patch,
opioid, the breakthru pain up till 48 hrs, causes resp depression
Parenteral
Transdermal (Patch)
Transmucosal
Lozenge on a stick AKA Fentanyl pop- for breakthrough cancer pts
Intranasal for fractures
Methadone- long acting morphine, used in hospice
Hydromorphone
Meperidine
Moderate to Strong Opioids-codine
Produce less analgesia and respiratory depression
Produce sedation and euphoria
Lower abuse potential
Adverse Effects
Similar to MSO4(morphine)

Codeine
10% of the codeine dose is converted to MSO4 in the liver
Some people lack the gene to metabolize codeine so it is ineffective

Administered oral and parenterally


Moderate to Strong Opioids
Codeine
Either alone or in combination with non-opioid analgesics (ASA or acetaminophen)
Combination are effective because they relieve pain by different mechanisms
Schedule II
Combination products are Schedule III
Only administered orally
Effective cough suppressant

Nursing mothers should be alert for signs of infant toxicity such as excessive
sleepiness, breathing difficulties, poor feeding---seek medical attention
Moderate to Strong Opioids
Oxycodone, Oxycontin
Oxycontin was reformulated in 2010 due to abuse
New formulation bears the imprint OP the old formulation bears the
imprint OC
New formulation are harder to crush and if exposed to water or alcohol it
turns into a gummy blobcan not inject
Hydrocodone
Combined with acetaminophen or ibuprofen
Agonist-Antagonist Opioids
Pentazocaine still get pain relief, limited resp depression. If someone
is already taking opiotes and then take this, pt will go into withdrawl
Agonist at kappa receptors
Antagonist at mu receptors

Limited respiratory depression


Adverse effects similar to MSO4
Can precipitate withdrawal in persons physically dependent on pure
opioids
Agonist-Antagonist Opioids
Buprenorphine
Schedule III
Partial agonist at mu receptors
Antagonist at kappa

Analgesic effects similar to MSO4


Causes some respiratory depression
Can precipitate withdrawal in persons physically dependent on pure
opioids
Agonist-Antagonist Opioids
Buprenorphine
Used in patients with severe chronic pain

Solution for injection, transdermal patches, sublingual tablets,


sublingual film

Patches and solution for pain


Sublingual products are used for opioid addiction
Using Opioids
Pain assessment
Prior to administration and 1 hour after
What do we ask in a pain assessment????- what does it feel like, scale od 1-
10- when start, better or worse, any other symptoms with it
Dosing
Individual variation- dosed on a set schedule to get drug leve. Fixed
schedule dosing
Dosing schedule
Fixed
Specific Pain Treated with Opioids
Postoperative
Obstetrical
Myocardial Infarction
Head Injury
Cancer Related Pain
Chronic Noncancer Pain
*Physical Dependence/Abuse/Addiction
****Physical Dependence
Abstinence syndrome occurs if the dependence producing drug is
abruptly withdrawn
Abuse
Drug use inconsistent with medical or social norms
Addiction
A disease process characterized by continued use of a psychoactive
substance despite physical, psychological, or social harm

Patient fears about addiction-ask


**Patient Controlled Analgesia
Self delivery of medication-pt gives themselves meds- NOT family.
If pt cant press button- not a good method of pain control.
Pump set with timing schedule- for example it resets every 10 minutes-
lockout interval
Need to have narcan readily available
Vitals pulse ox RR-4 hrs
Drug and dosages
Patient and family education
Risk Evaluation and Mitigation Strategy
Introduced in 2011 by the FDA
Purpose: Reduce injuries and death from prescription opioids
Companies that market opioids develop and pay for training
Content of material is reviewed by the FDA

Training for prescribers


Voluntary
Focus on patient selection
Balancing risks and benefits
Monitoring treatment
Recognizing misuse, abuse, and addiction
Education on how to counsel patients about the safe use of opioids
Opioid Antagonists
Naloxone (Narcan)- the only opioid antagonist-takes away the pain
relief- wakes them up-makes them bbreathe- takes away euphoria
Blocks opioid actions
Will reverse effects of opioids if patient is receiving opioids
Analgesia, respiratory depression, sedation, euphoria
Can precipitate withdrawal in an opioid dependent patient
Routes
IV, IM, subQ
Opioid Antagonists
Methylnaltrexone (Relistor)
Used for opioid induced constipation
Selective mu receptors

Route
subQ
Adverse Effects
Diarrhea
Abdominal pain
Flatulance
Nausea
Dizziness
Nonopioid Centrally Acting Analgesics
Tramadol
Weak activity at mu receptors
Spinal inhibition of pain
Used for mild to moderate pain
Clonidine
Alpha 2 agonist
Blocks nerve pathways that transmit pain in the spinal cord
Used for severe cancer pain not relieved by opioids
Key Points
Patient/family education
Pain assessment
Identifying high risk patients
Continuous evaluation