Topical anesthesia - ANSWER The ability of an anesthetic to penetrate the axon
membrane is determined by
1. Molecular size
2. Lipid solubility
3. Degree of ionization at tissue ph
Lidocaine - ANSWER Injectable, gels
Lido with epi to constrict blood flow and prolongs anesthesia and decrease risk of
toxicity
Mu receptors - ANSWER Responses to activation of these receptors include:
analgesia, respiratory depression, euphoria, sedation, and physical dependence
Most important receptors for opioids because they act primarily by activating mu
receptors
Kappa receptors - ANSWER Activation of these receptors can produce: analgesia and
sedation
Kappa activation my underly psychotomimetic effects seen with certain opioids
Delta receptors - ANSWER Generally opioids don't interact with these
Pure opioid agonists - ANSWER Activate mu and kappa receptors
can produce analgesia, euphoria, sedation, respiratory depression, physical
dependence, constipation, and other effects
Morphine - ANSWER Strong opioid agonist
, Codeine - ANSWER Moderate to string opioid agonist
Agonist antagonist opioid - ANSWER Pentazocine, nalbuphine, butorphanol,
buprenorphine
When administered alone produces analgesia
If admined with pure opioid agonist, can antagonize analgesia caused by the pure
agonist
Pure opioid antagonists - ANSWER Naloxone (Narcan) our prototype
Antagonist at mu and kappa receptors
Do not produce analgesia or any of the other effects caused by opioid agonists
Reversal of respiratory and cns depression caused by overdose with opioid agonist
Not available in oral forms
Methyl naltrexone - ANSWER Used to treat opioid induced constipation
Only work on mu receptors in the bowel
Naltrexone - ANSWER Used to treat opioid and alcohol abuse
Prevents euphoria if the abuser takes opioid
Doesn't prevent craving for opioid
Candidates for treatment must be rendered opioid free before naltrexone is started
Morphine - ANSWER Source: poppy seed plant
Therapeutic use: relief of pain
Relieves pain without affecting other senses (like sight, touch, smell, and hearing)
No loss of consciousness
MOA: relieves pain by mimicking actions of endogenous opioid peptides, primarily at mu