Pain Drugs Flashcards
List the Non-Opioid Analgesics
- Aspirin
- Acetaminophen
- NSAIDs
- Cox-2 Inhibitors
What is the MOA of Non-Opioid Analgesics?
Target inflammatory components of the pain cascade
What is the use of Non-Opioid Analgesics?
Mild to Moderate Pain
-Ex: soft tissue injury, sprain, strain, HA, arthritis
Non-Opioid Analgesics may be beneficial when used synergistically with what types of drugs?
Opioids
What is a major side effect of Acetaminophen?
Hepatotoxicity/Liver Failure
What is a major side effect of Aspirin and NSAIDs
- Gastric Ulcers
2. Inhibition of Platelet aggregation
What is a contraindication of Acetaminophen?
Alcoholics or Liver Disease Pts
What is a contraindication of NSAIDs
Use in patients who are taking Aspirin for CV protection
What are Opioid Receptors?
The opioid receptors are G Protein Coupled Receptors lined to Gi/o. There are 3 types: Mu, Delta and Kappa
What happens upon binding of an Opioid Receptor?
Activation results in inward rectifying K channels, inhibition of Ca channels, and inhibition of Adenylyl Cyclase
Where are Mu receptors found?
- CNS (neocortex, Thalamus, Hippocampus/Amygdala, Nucleus Acumbens)
- Myenteric Neurons of the Gut
- Vas Deferens
What are the physiological effects of Mu Receptor Activation?
- Supraspinal analgesia
- Respiratory Depression
- Euphoria/Dependence
- Constriction of the Gastric Tract
Where are Delta Receptors found?
- Olfactory Bulb
- Nucleus Acumbens
- Caudate and Putamen
- Neocortex
What is the physiological effect of Delta Receptor activation?
- Affects Behavior
Where are Kappa receptors found?
- Cortex
- Nucleus Acumbens
- Spinal Cord
What is the physiological effect of Kappa Receptor activation?
- Spinal Cord Analgesia
2. Sedation
What are the endogenous agonists of Mu receptors?
- Endomorphin 1 and 2
- Enkephalins
- B-endorphin
What are the endogenous agonists of Delta receptors?
- Enkphalins
What are the endogenous agonists of Kappa receptors?
- Dynorphins
Which drugs are Mu receptor agonists?
- Morphine
- Fentanyl
- Methadone
- Meperidine
- Buprenorphine
Which drugs are Mu Antagonists?
- Naloxone
2. Naltrexone
Which drugs are Delta Antagonists?
- Naltrindole
Which drugs are Kappa Agonists?
- Butorphanol
- Pentazocine
- Nalbuphrine
What are the strong Opioid Agonists?
- Morphine
- Hydromorphone
- Hydrocodone
- Methadone
- Heroin
- Oxycodone
- Meperidine
- Fentanyl + Analogs
Which drug is used for moderate-severe acute and chronic pain and for treatment of pain from PE and MI?
Morphine
Which drug is good for chronic pain and antitussive effects?
Hydrocodone
Which drug is good for severe pain? This drug is also a ketone of Morphine, is 7x stronger and has fewer active metabolites.
Hydromorphone
Which drug causes analgesia and is good for controlled withdrawal from opioid due to its long T1/2 and slow tolerance rate?
Methadone
Oxycodone is used for what?
Moderate-Severe pain
Which drug is used for acute analgesia, especially for OB?
Meperidine
Which drug is goof for surgery and post-surgery analgesia, and chronic pain for cancer patients (usually as a patch since the duration is short)?
Fentanyl + analogs
Which drugs are moderate-low agonists?
- Codeine
2. Propoxyphene
Which drug is used as an analgesic + antitussive?
Codeine
Which drugs are mixed agonists/antagonists (partial agonists)?
- Buprenorphine
- Pentazocine
- Butorphanol
- Nalbuphine
Which drug is a partial agonist at Mu Receptors?
Buprenorphine
Pentazocine, Butorphanol and Nalbuphine are partial agonists at what receptor?
Kappa