Pain and Inflammation Medications Flashcards
Which receptors do opioids bind to?
MU receptors
Kappa Receptors
Delta Receptors
Examples of Opioid Strong Agonists
- Morphine Sulfate
Fentanyl
Merperidine (Demerol)
Hydromorphone (Dilaudid)
Methadone
Opioid Moderate to Strong Agonist Examples
- Codeine
Oxycodone
Tramadol (Ultram)
Opioid Agonist-Antagonist Examples
- Butorphanol
Nalbuphine (Nubain)
What do MU Receptors cause?
Analgesia
Respiratory Depression
Euphoria
Miosis
Reduced GI motility
What do Kappa Receptors cause?
Analgesia
Sedation
Respiratory Depression
Dysphoria
Miosis
What do Delta receptors cause?
Analgesia
Which neuropeptides are part of the endogenous analgesia system?
Endorphins
Enkephalins
Dynorphins
Endorphins
Inhibit Pain Signal Transmission
Induce Euphoria
Enkephalins
Inhibit substance P release
Modulate Pain Perception
Dynorphins
Produce analgesia
Morphine Sulfate
They bind to opioid receptors in brain, spinal cord, and peripheral tissues and activate endogenous analgesia system.
Moderate to servere pain
Adverse Effects of Morphine Sulfate
Respiratory depression
CNS depression
Nausea and Vomiting
Orthostatic hypotension
Sedation
Urinary Retention
Pupil Constriction
Itching
Black Box Warning for Morphine Sulfate
Regarding combined use of morphine and other opioid analgesics with benzodiazepines and other CNS depressants. All opioid analgesics – respiratory depression, coma, death, drug abuse and dependence.
CNS Depressants
Alcohol, antidepressants, antipsychotic, barbiturates, benzodiazepines, and sedatives
Meperidine (Demerol)
- Produces neurotoxic metabolite (normeperidine) which accumulates with chronic use, large doses or renal failure.
- CNS Stimulation – Agitation, hallucinations, seizures
- Normeperidine not reversible with sopioid antagonist drugs
Not frequently used
Methadone
- Longer Duration of action
- Therapueutic uses: Servere pain and detoxification and maintenance treatment of opioid use disorder
- Adverse Effects: Lead to fatal dysrhythmias (Torsades de pointes)
Examples of Potent Opioids
Fentanyl and hydromorphone (Dilaudid)
Examples of milder opioids
Oxycodone and Codeine
Black Box Warning: Children who are ultra rapid metabolizers of codeine
Signs of Opioid Toxicity
Classic Triad: Coma, Respiratory Depression, Pinpoint Pupils
Equianalgesic Dosing
An equianalgesic dosing chart is a conversion chart that lists equivalent doses of analgesics
Patient-controlled Analgesia (PCA)
- Patient self-administers
- Preset bolus
- Basal amount
- Lockout period
- Education
Tramadol (Ultram)
MOA: Binds to mu opioid receptors and inhibits norepinephrine and serotonin reuptake
Therapeutic uses:
* Moderate to severe pain
* Older adults
* Fibromyalgia, neuropathic pain
* Chronic pain
Tramadol (Ultram) adverse effects
- Serotonin syndrome
- Respiratory depression
- GI effects
- Hypotension
- Seizures
- Suicidal ideation
Drug interactions: CNS depressants and SSRIs
Opioid Nursing Considerations
- Opioid tolerant vs. Opioid naive
- Pain Assessment
- Sedation Assessment
- Respiratory Assessment
- Orders
- Treatment goals
Opioid Agonist/Antagonist Examples
- Butorphanol
- Nalbuphine (Nubain)
- Buprenorphine
Butorphanol
- Similar to morphine in analgesic effects and respiratory depression risk
- Can induce withdrawal in opioid dependence
- MOA: Act on same pain receptors as other opioid
agonists. Agonists at some receptors and produce
antagonist activity at others.
For moderate to severe pain
Adverse Effects of Butorphanol
Black Box Warning: Potentially fatal respiratory depression, coma, death, drug dependence and abuse potential
Vertigo
Nausea and Vomiting
Possible withdrawal in opioid-tolerant
Signs and Symptoms of Opioid Withdrawal
- Perspiration
- Chills
- N/V/D
- Anxiety, restlessness, insomnia
- Pupil dilation
- Anorexia
- Increased body temperature, RR, BP
- Dehydration
- Muscle cramps
Opioid Antagonist Example
Naloxone (Narcan)
Naloxone (Narcan)
- Antidote for CNS and respiratory depression caused by opioids. Also reverses analgesia
- MOA: Competes with opioids at receptor sites and prevents binding or displaces bound opioids.
- Therapeutic use: Reverse respiratory and CNS depression caused by opioid
overdose
Adverse Effect: Withdrawal
Shorter duration of action than opioids.
Nonnarcotic Analgesic Antipyretic Example
Acetaminophen (Tylenol)
Acetaminophen (Tylenol)
MOA: Mechanism of action for pain response is largely unknown.
Acts on hypothalamus to reduce fever. Does not block prostaglandin synthesis in the periphery, pain relief action
suspected to be via CNS.
Therapeutic uses: Analgesic, antipyretic
Does not have anti-inflammatory properties
Adverse effects of Acetaminophen (Tylenol)
Hepatotoxicity
- Max dose 4 grams/24 hours
- Use in caution with liver or renal impairment
Nephrotoxic in overdose
Overdose
- In multiple combination drugs
- Acetylcysteine (Mucomyst)
Antiprostaglandins/
Cyclooxygenase Inhibitors Examples
Salicylate
NSAIDS (1st and 2nd Generations)
What are the roles of prostaglandins?
- Participate in Inflammatory response
- Formed in response to cellular injury
- Sensitize pain along with other chemical mediators
- Protect GI tract adn kidneys
- Regulate platelet function
- Regulate vascular tone
Aspirin (Acetylsalicylic acid)
MOA: Nonselective inhibitor of cyclooxygenase, suppresses platelet aggregation. Acts centrally and peripherally. Blocks pain response.
