Exam 2: Analgesics 3 Flashcards
At lest 20 Distinct alkaloids are derived from the juice of the poppy
Opium
Group of mainly synthetic agents that act at opioid receptors to produce analgesic effcts
Opiod Drugs
Naturally occuring drugs extracted from opium
Opiates
Analgesia and stupor bordering on general anesthesia
Narcosis
Analgesia and annesic state produced by administration of a neuroleptic and narcotic
Neuroleptanalgesia
Opiods have effects on which parts of the nociception pathway
- perception
- Transduction
- Modulation
What are the 3 types of receptors that opiods act on?
- mu
- Kappa
- Delta
Where are opioid receptors located?
brain and SC
What are the endogenous ligands for Mu receptors?
B endrophins and endomorphins
What are the main effects of mu receptors?
Analgesia, sedation, respiratory, and GI depression
What is the endoenous ligand for kappa receptors?
Dynorphin
What is the main effects of kappa receptors
Analgesia and sedation
Where are mu receptors located
Brain, SC, joint capsules
What is the purpose of mu-1 receptors?
Supraspinal analgesia
What is the purpose of mu-2 receptors?
spinal analgesia
Which opioid receptor is weakly affected by opioid dugs?
kappa
Which opioid receptor causes euphoria
Mu
Which opioid receptor causes GI motility
Mu and kappa
Which opioid receptor causes CV depression
Delta
What are the 6 Full Mu agonist opioids?
- Morphine
- Oxymorphine
- Hydromorphone
- Methadone
- Fentanyl
- Remifentanil
What is the one full Mu antagonist?
Noloxone
What is the one partial Mu agonist?
Buprenorphine
What is the one mixed agonist-antagonist?
Butorphanol
What are the 2 special opioids?
- Tramadol
2. Hydrocodone
Explain controlled drug scheduling
1-5
1 is the most controlled
What schedule of controlled drug is opioids?
2-4
2: full mu agonists
3: buprenorphine
4: tramadol
T/F. opioids can cross the BBB but not the placenta.
F. Can cross both
How are opioids metabolized and excreted?
conjugation to glucuronic acid and excreted in urine
how do opioids effect thermoregulation in dogs? in cats?
Dog= Hypothermia Cat= Hyperthermia
Opioids cause Miosis (constriction) is what spp, and Mydriasis (Dilation) in what spp?
Miosis in dogs
Mydriasis in cats
How do opioids effect the Respiratory system>
Dose dependent respiratory depression
What resp. sign can be seen in dogs at therapeutic doses?
panting
What are the CV effects caused by opioid use?
Minimal
Brady cardia and hypotension due to vasodilation
GI symptoms of Opioid use
Nausea, vomiting, regurgitation salivation, ileus, Constipation
Hydromorphone is associated with what GI symptome
Nausea
T/F Methadone is highly emetogenic (induce v+)
F. less
Emetic of choice in dogs
Apomorphine
T/F Apomorphine is toxic to cats
T
Apomorphine acts on which receptor?
D2
Opioid effect on urinary system
Urinary retention
Opioid effect on immune system
Histamine release
T/F. Opioids offer excellent visceral analgesia
T
T/F. Opioids are used in epidurals
T
Agonism of which receptors causes the most sedative effects
kappa
Which opioids can be antitussive
Butrophanol, hydrocodone
What is the MOA of opioids?
inhibit Substance P
Which full Mu Agonist is a prototypical analgesic
Morphine
What is the risk of morphine in dogs
histamine release
Why would you pick hydromorphone over morphine?
less histamine release
Similar to hydromorphone but less emetogenic
Oxymorphone
Opioid that causes smooth sedation in cats and pedeatric patients
Oxymorphone
Used as alternative opioid in pre-anesthetic and analgesia protocols in dogs and cats
Methadone
Why would you pick Methadone over Morphine?
- Less hist. release
2. less GI signs (V+)
Why might you pick morphine over methadone?
more sedation with Morphine
Potent, short acting opioid that can be used CRI
Fentanyl
Similar to fentanyl but more potent
Remifentanil
What is the shortest acting opioid
Remifentanil
Semisynthetic partial mu agonist
Buprenorphine
Which opioid experiences the celing effect
Buprenorphine
T/F. Buprenorphine strongly binds to receptors at every site
F. not at every site
T/F Buprenorphine has less apparent adverse side effects than full mu agonists
T
What is the mixed opioid recptor agonist-antagonist we talked about?
Butorphanol
What is the MOA of Butorphanol
Synthetic kappa agonist and mu antagonist
T/F Butorphanol has less of an analgesic profile than pure mu agonists
T
Butorphanol works better for visceral or somatic pain?
visceral
T/F. Butorphanol can be used as a antitussive
T
T/F Butorphanol can be used as anxiety relief and sedation which facilitates airway relaxation and breathing
T
What is the full opioid mu receptor antagonist we talked about in class?
naloxone
What is the MOA of naloxone
competitive mu receptor antagonist
What is naloxone used for>
reversal of opioid induced adverse effects
T/F. Naloxone will reverse analgesic effects of opioids
T
What are the 2 special opioids we talked about?
Tramadol
Hydrocodone
What DEA schedule is Tramadol?
4
What is the MOA of Tramadol
Weak opioid mu agonist
Tramadol inhibits ____ and ____ reuptake
Serotonin and NE
T/F. Tramadol increases an animals seizure threshold?
F. lowers
Hydrocodone is a DEA schedule _ drug
2
Semisynthetic opioid used mostly as an antitussive
Hydrocodone
What is apomorphine used for?
emetic in dogs
T/F. Apomorphine is used as an emetic in cats
F. Toxic to cats
Can you give opioids to dogs with ileus
NO
T/F. Full mu agonists can be fully reversed
T
T/F. Hypothermia in cats is common after opioid use
F. Hyperthermia!!!!!
Rank the opioid agonist based on their ability to provide analgesia
Mu > kappa
Which opioid receptor provides the best sedation
kappa
