BIO 301 Ms.

Lopez
 Relieve pain w/out causing loss of
consciousness
Pain-killers
Main class: opioid analgesics [Opium family]
Originate from opium poppy
Opiate
Drug, either natural or synthetic w/similar actions
to those of morphine
 An unpleasant sensory and emotional
experience associated with either actual or
potential tissue damage.
Personal and individual experience.
 Acute
Sudden onset
Subsides when treated
i.e. postop pain
Chronic
Persistent or recurring
Lasts longer than 3 months
More difficult to treat
 Somatic Vascular
Originates from skeletal Referred
muscle, ligaments, joints
Neuropathic
Visceral
Central
Organs and smooth
muscle
Superficial
Skin and mucus
membrane
Deep
From tissue below skin
surface
 Classified according
to structure or action
at specific receptors
3 main receptors
Mu- most important
Kappa
Delta
Sigma
Epsilon
 Mu Receptors
Activation-response
includes
Analgesia
Respiratory
depression
Euphoria
Sedation
Physical dependence
 Agonists [pure opiate agonist]
Activate mu & kappa receptors
Bind to opiate receptor in brain to elicit response:
analgesia
Mild agonists
Codeine- prototype
Hydrocodone [Vicodin. Lortab]
Propoxyphane [Darvon]*-no longer in use
 Strong agonists
Morphine [MSIR, Roxanol, Kadian, Avinza,
others]-prototype
hydromorphone [Dilaudid]
oxycodone [Oxycontin]
fentanyl [Duragesic]
methadone [Dolophine]
Levorphanol [Levo-Dromoran]
Oxymorphone [Numorphan]
Meperidine [Demerol]
Not recommended for use
Neurotoxicmetabolite-normeperidine-
seizures
 Agonist-antagonist [partial agonist]
Binds to receptor but causes a weaker pain
response
Antagonist
Binds to receptor but does NOT reduce pain signals
Functions as _______________: competes w/and
reverses effects of agonist-antagonist drugs at
receptor sites.
Main function is reversal of ___________________
Prototypical of antagonists________________
 Ability to provide equivalent pain relief and or
routes of administration that provide comparable
analgesia
Basic conversion Equation
24 hr amount of current drug=EA dose of current drug
X EA dose of desired drug

X= amount of desired opioid in 24 h and EA = equianalgesic

dose obtained from chart
 Alleviate moderate to severe types of pain
Strong opioids-used in combo with anesthetics
during surgery-maintain balanced state of
anesthesia [balanced anesthesia]
Fentanyl, sufentanil and alfentanil
Other uses of opioids
Cough suppression
Treat diarrhea
 RESPIRATORY DEPRESSION-most serious
Effects begin with 7 minutes [IV], 30 minutes post
IM & up to 50 minutes post subQ
Determine RR prior
RR <12 breaths per minute or less and shallow
depth, opioid should be withheld and the provider
notified
Monitor closely the young, elderly & those
w/respiratory diseases
Avoid alcohol, other CNS depressant
 Sedation/drowsiness
Constipation
Orthostatic hypotension
Urinary retention
Cough suppression
Biliary colic
Emesis
Elevation of ICP
Euphoria/dysphoria
Miosis pinpoint pupils
neurotoxicity
 Drug allergy
Itching: Pharmacologic effect
Severe asthma
Respiratory insufficiency
Morbid obesity
Sleep apnea
Myasthenia gravis
Severe head injury [elevated ICP]
Paralytic ileus
Pregnancy
 Classic Triad
Respiratory depression
Coma
Pinpoint pupils
 Naloxone [Narcan] 0.4-2 mg q2-3 [not more
than 10 m] IV
IV infusion: 2 mg in 500 mL [titrate to response]
Effects: raised or low BP, dysrhythmias, pulm.
Edema, withdrawal
Naltrexone [ReVia] 25-50 mg PO daily
Effects; nervousness, headache, n/v, pulm.
Edema, withdrawal
 Opioid nave
Describes patients who are receiving opioid analgesics for the first
time and who therefore are not accustomed to their effects.
Opioid tolerance
A normal physiologic condition that results from long-term opioid use,
in which larger doses of opioids are required to maintain the same
level of analgesia and in which abrupt discontinuation of the drug
results in withdrawal symptoms (same as physical dependence).
Opioid tolerant
The opposite of opioid nave; describes patients who have been receiving
opioid analgesics (legally or otherwise) for a period of time (1 week or longer)
and who are at greater risk of opioid withdrawal syndrome upon sudden
discontinuation.
Opioid withdrawal
The signs and symptoms associated with abstinence from or withdrawal of an
opioid analgesic when the body has become physically dependent on the
substance.
 Co-administration with
Alcohol
Antihistamine
Barbiturates
Benzos
Phenothiazines
Other CNS depressants [respiratory
depression]
Combination use w/MAOI:
resp depression, seizures, hypotension
 Abnormal increase in serum levels of
amylase,
LFTs
ALT alanine aminotransferase formerly-
SGPT;
AST Aspartate aminotransferase formerly
SGOT
CK Creatinine Kinase
Lactodehydrogenase
Increase in glucose concentration
 Fentanyl [Duragesic]
High abuse potential: 100x that of morphine]
Schedule II
Routes: Inj. [Sublimaze], transdermal [Duragesic],
buccal lozenges [Fentora], buccal lozenges on
stick lollipol [Actiq]
Potent analgesic
 Transdermal Delivery System
Use for opioid tolerant patients
Not for use in opioid nave patients
NOT for ACUTE PAIN- respiratory depression
Effective to treat various chronic pain syndromes: cancer-related pain
1st patch applied: takes6-12 hours to reach steady state pain control, so
will required supplemental short acting therapy
Adequate pain control achieved in 72 hours
Apply new patch every 72 hours [3 days]
Remove old patch before applying new one, apply to nonhairy area, rotate
sites
Discard patch appropriately by folding and flushing down toilet
Do not expose patch to heat-diffusion of drug is accelerated
 Patients who take at least
60 mg Morphine daily or
30 mg of PO oxycodone daily or
at least 8 mg of PO hydromorphone
daily or
an equianalgesic dose of another
opioid.
 Opioid agonist- Schedule II High abuse potential
Prototypical opioid
Use: severe pain
Dosage forms: ER: MS Contin, Kadian, Avinza
Toxic metabolite: morphine 6-glucuronide-
accumulates in patient w/renal impairment
Route: PO, IM/IV, SQ, supp., epidural, PCA
cartridges
 Natural opioid alkaloid High abuse potential
Schedule II [itself]
Poses a CEILING EFFECT
Commonly used as an ANTITUSSIVE in many
cough preps
Codeine w/acetaminophen [tabs or elixirs[-
Schedule III-control mild to moderate pain
AE: GI tract upsets
Route: PO
 Schedule II
Opioid of choice for detoxification Rx of
opioid addiction in methadone programs
Chronic neuropathic and cancer-related
pain
Half-life- 25 hours
Can cause cardiac dysrhythmias
Route- PO, injectable
 Oxycodone HCL- II
Commonly combined w/acetaminophen
[_____________], ASA [____________]
Immediate-release [Oxy IR]
Sustained release [OxyContin]
Weaker commonly used form is hydrocodone
with acetaminophen [Vicodin] also with ASA
& ibuprofen [III]
Route- PO
 Schedule II
Analgesic properties = to codeine
Route: PO
Use: pain, suppresses cough
Cough suppression properties: combined
w/antihistamine & nasal congestion
 Opioids w/mixed actions
Schedule IV
Bind to mu receptors
They are either competitive agonist or partial
agonist
Antagonist properties can produce withdrawal
symptoms in opioid-dependent patients
Used for short term pain control: obstetric
procedures
Can be used for patients w/h/o opioid addiction
 Buprenorphine [Buprenex]
Butorphanol [Stadol]
Nalbuphine [Nubain]
Petazocine [Talwain]-Prototype
 Acetaminophen [Tylenol]
Analgesic & antipyretic properties
No anti-inflammatory properties
Block pain impulses peripherally by inhibiting
prostaglandin synthesis
Mild to moderate pain, fever, good for those who
cannot take ASA products
Lethal when OD: hepatic necrosis: hepatotoxic
LT use of large dose: nephrotoxicity
Antidote:_____________________________
 Dangerous interactions if combined w/
ALCOHOL
Other hepatotoxic drugs
NOT to be taken in presence of
Allergy
Liver disease
G6PD deficiency
 With acetaminophen Analog of codeine
[Ultracet] AE:drowsiness,dizzy,
Centrally-acting headache,nausea,
Use:pain-relief-moderate constipationand
to severe respiratory depression
Contra: seizures, other Seizures: risk if taking
neuro conditions, MAOI TCA, SSRI, MAOI,
[HYPERTENSIVE neuroleptics or other
CRISIS] drugs that reduce
Interacts with alcohol & seizure threshold
other CNS drugs
 For pain, HTN [Catapres]
Uses: severe cancer NOT relieved by opioid
Effective for NEUROPATHIC PAIN [electrical,
burning or shooting pain]
Route: continuous epidural infusion
Ziconotide [Prialt]
Route: intrathecal
 Related to marigold family
Common Uses
Treatment of migraine headaches, menstrual
cramps, inflammation, and fever
Adverse Effects
Nausea, vomiting, constipation, diarrhea, altered
taste sensations, muscle stiffness, and joint pain
Potential Drug Interactions
increase in bleeding: aspirin and other nonsteroidal
anti-inflammatory drugs, dipyridamole, and warfarin
 Thorough pain assessment: intensity, character,
onset, location, description, relieving factors,
precipitating factors, type, remedies, other tx
Rate pain on scale of 0 to 10
Obtain baseline vital signs, I&O
Assess for potential complications
Be sure to medicate before pain reaches it peak
and becomes severe so as to provide adequate
analgesia and pain control
 Try nonpharmacologic and pharmacologic
interventions
Teach to check with provider regarding other
meds or OTC preps
Administer on a fixed-schedule [ATC]
w/supplements as needed for breakthrough pain
IV injections slowly over 4-5 minutes
Have antagonist available on hand &
resuscitative equipment
 Instruct patients to notify provider for sings of
allergic reaction or adverse effects
PO forms should be taken w/food to minimize
gastric upset
Ensure safety measures: side rails up, bed
lowest position, call bell within reach
Withhold dose and contract provider if a decline
in condition or if vital signs are abnormal
especially RR is less than 10/minute &
SHALLOW
 Monitor urinary output: 600 mL/24 hours
Monitor bowel sounds; decrease peristalsis may
need increased fiber or use a stool softener or
mild laxative, hydration
Assess pupillary reaction: pinpoint=OD possible
Assess pain level after medicating: PO: 1 hour
post and Parenteral: 1/2 hour post adm. &
document
 Constipation: adequate fiber & fluids
Instruct patient to follow directions & keep
record of pain experience and response to tx
Instruct patient to change position slowly to
prevent orthostatic hypotension
Warn against hazardous activities
Instruct hypotension or dizziness can occur
Taper doses over 3 days-DO NOT STOP
ABRUPTLY
 Contact provider immediately if changes in vs
Respiratory depression if RR <10 breaths/minute,
dyspnea, diminished breath sounds or shallow
breathing
Patch
Apply to clean, nonhairy area
Rotate sites to help decrease irritation
Remove old before applying new
Do not share
IV adm: follow manufacturer guidelines and
institution policy
 For PCA use: follow agency protocol, note
amounts and times of dosing
Check all equipment
Monitor IV access site, infusion rate and
document any adverse effects
IV most rapid action-monitor patient