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Pharm-1-Pain-Control

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hpaul2's version from 2017-04-06 16:20

Section

General
Question Answer
Define painunpleasant sensory & emotion experience in response to actual or potential tissue damage
How is pain inhibited by the bodydescending pathways from midbrain & brain stem inhibit dorsal horn transmission
What are the NTs of descending inhibitionopioid peptides, 5-hydroxytryptamine, norepinephrine, adenosine
What fibers and receptors are associated with wind-up painc-fibers, NMDA & substance P receptors activated
What is hyperalgesiasensitization to noxious stimuli
What is allodyniapain with non-noxious stimulus
Describe the peripheral sensitization pathwaynoxious stimulus = C-fiber activity → inflammation → sensitizing soup = mediator & neuropeptide release + NGF production → excitation of transmission neuron → pain 

Peripheral Sensitization leads to the formation of the sensitization soup which results in Transduction Sensibility
The Sensitizing Soup has what effect on the Threshold Nociceptorslowers the threshold (how from high-threshold to low-threshold nociceptors)
Multimodial analgesia is used to prevent whatwind-up pain
What receptors does multimodal analgesia activateNMDA receptors
What are the three mechanisms multimodal analgesia interferes withsensitizing soup, gate control, CNS neurotransmission
What does the gate control mechanism preventnon-painful stimuli from stimulating never terminals of CNS
What are the two fibers which carry signals from tissue to spinal cordlarge (Aβ fibers) & small (Ad and C fibers)
What signals do small fibers sendthermal & mechanical
What signals do large fingers sendpressure & touch/position
Which fibers can open the ‘gate’ and create painsmall fibers
memorize

 

Opioids - General
Question Answer
How do opioids affect the pain pathwaysstimulate descending pathways & inhibit ascending pathways
In what species do opioids cause depression and excitationdepression - humans & dogs; excitation - horses & cats
What are the effects of opioids on the respiratory systemdose dependent depression
What are the effects of opioids on the GITincreased sphincter tone (constipation)
What are the endogenous ligands of opioid receptorsenkephalines, dynorphines, & endorphins
What kind of receptors do opioids act ong-protein coupled (Gi & Go)
Prolonged opioid receptor activation can lead tolong-term adaptive changes (dependence)
What are the three types of opioid receptorsμ, δ, κ (mu, delta, capa)
How can opioids be givenorally, IM, SC
What is a downside to oral administrationfirst-pass effect (erratic plasma concentration)
Opioids distribute well in the body because they arelipophilic weak bases
memorize

 

Opioids - drugs
Question Answer
What are the effects of opioids (8)supraspnial/spinal/peripheral analgesia, resp. depression, myosis, ↓ GI motility, euphoria, dysphoria, sedation, dependance
Which receptor can have all opioid effects except dysphoriaμ
What opioid effects does δ have (3)spinal analgesia, respiratory depression, & ↓ GI motility
What opioid effects does κ have (6)spinal & peripheral analgesia, myosis, ↓ GI motility, dysphoria, sedation, dependance
What are the 4 types of opioidsendogenous peptides, pure agonists, partial/mixed agonists, & antagonists
Name the opioid endogenous peptidesβ-endorphins, leu-enkephalin, met-enkephalin, dynorphin
Name the opioid pure agonistscodeine, morphine, hydromorphone, oxymorphone, methadone, meperidine, ethorphine, fentanyl (Can My Horse Open My Mail Every Friday)
Name the opioid partial/mixed agonistspentazocine, nalbuphine, nalorphine, buprenorphine, butorphanol
Name the opioid antagonistsnaloxone, naltrexone (ex addict)
What partial/mixed agonists antagonize μ receptorspentazocine, nalbuphine, & naloprphine
What partial/mixed agonsits antagonize κ receptorsbuprenorphine
What drugs don’t act on δ receptorshydromorphone, oxymorphone, methadone, nalorphine, buprenorphine, butrophanol (3 agonists + 3 mixed agonists)
What drugs don’t act on κ receptorsleu-enkephalin, met-enkephalin, hydroorphone, oxymorphone, methadone, fentanyl (both endogenous with K in the name + 4 agonsits)
What opioid is highly lipophilic and redistributes easilyfentanyl
memorize

 

Opioids - Clinical Use
Question Answer
What drugs are morphine & methadone commonly used withα2 agonists
What are morphine & methadone commonly used forpremed, anesthesia, analgesia
What do morphine & methadone cause in horsesexcitation
What are butorphanol, nalbuphine, & pentazocine used for (mixed agonists)short acting analgesia in horses with colic
Which drug offers a slow onset but long duration of actionbuprenorphine
What are the adverse effects of opioidsnausea/vomiting, bradycardia, resp. depression (long-term), constipation/urinary retention, histamine release, excitatory effects (horses & cats), hyperalgesia (long-term), tolerance
memorize

 

Tramadol
Question Answer
Tramadol acts where in the bodycentrally
Tramadol is a ____ compoundchiral
What are the two forms of tramadol+ and -

The + form does whatμ agonist, M1 antagonist, inhibit serotonin re-uptake
The - form does whatM1 antagonist, inhibit nor-epi re-uptake
What is tramadol’s plasma elimination 1/2 life2 hours (dogs)
What can tramadol cause in catsdysphoria
What are the side effects of tramadolsedation, nausea, anorexia, vomiting, constipation
memorize

 

α2 Agonists (review previous memorize)
Question Answer
How are α2 agonists administered for analgesiaparenteral, oral, epidural
What parts of the body do α2 agonists affecthead, neck & body (not extremities)
How do α2 agonists cause analgesiainhibit release of nociceptive NTs at dorsal horn neurons
What drugs do α2 agonists act in synergy withopioids, locals, NMDA-antagonists
memorize

 

Local Anesthetics
Question Answer
How are locals administered (5)cutaneous/topical, infiltration, nerve block, spinal, epidural
What are the two forms of localsactive & inactive
What is the difference between the active and inactive formsactive - hydrophilic, ionized, poor membrane passage; inactive - lipophilic, non-ionized, excellent membrane passage
Local anesthetics are (pKa related)weak bases
Describe the mechanism of action of localsinactive form enters nerve fiber → active form blocks Na channel → membrane depolarization inhibited
memorize

 

NMDA Antagonists
Question Answer
What are the 2 NMDA antagonistsketamine, tiletamine (+ zolazepam)
What do NMDA antagonists preventglutamate induced depolarization
Do NMDA antagonists cause muscle relaxationno
memorize

 

Anti-epileptic Drugs
Question Answer
What are the anti-epileptic drugsGabapentin, pregabalin, & carbamazepine
Where do gabapentine and pregabalin bindsubunits (α2d1 & α2d2) of voltage gated Ca channels
What do anti-epileptic drugs do once boundinhibit NT release
If a sensory neuron is damaged, what happens to the subunitsup-regulated
How does carbamazepine workblocks voltage gated Na channels (trigeminal neuralgia)
What happens to Na channels after nerve damageup-regulated (↑ pain sensitization)
memorize

 

Tricyclic Antidepressants
Question Answer
What do tricyclic antidepressants treatneuropathic pain (dogs)
Name the tricyclic antidepressantamitriptyline
Where does amitriptyline actcentral descending pain control systems (potentiate inhibitory pathways - dorsal horn)
How does amitriptyline workinhibits nor-epi & serotonin re-uptake
memorize

 

COX (Cyclooxygenase) & NSAIDs
Question Answer
COX is an ____ which produces ____enzyme, prostaglandins
COX-1 mainly does whatmaintain stomach linking, kidney & platelet function
COX-2 mainly does whatinflammatory response
Which COX is it preferable to inhibitCOX-2 (anti-inflammatory)
Name the specific COX-2 inhibitorsrobenacoxib, firocoxib, mavacoxib ("cox")
What are the preferential COX-2 inhibitorsNimesulide, meloxicam, naproxen, ketorolac, carprofen (normal sounding stuff)
What are the preferential COX-1 inhibitorsflunixin meglumine, phenylbutazone, acetyl-salicylic-acid (crazy names)
What drug binds to COX-1 irreversibly (causing clotting disorders)acetyl-salicylic-acid
What is a problem of many NSAIDsnon-selectively inhibit COX-1 & COX-2
What are side effects of NSAIDsGI ulcers, renal toxicity, coagulation
What causes GI side-effects with NSAIDs? Treatments?PCE2 activity; misoprostol
What causes renal toxicity with NSAIDsPG needed for regulation of renal blood flow
What can worsen renal toxicity with NSAIDsother nephrotoxic drugs, shock, dehydration, surgery
How can NSAIDs cause coagulationCOX-1 inhibited, thromboxane inhibition
memorize