Narcotic and Non-Narcotic Analgesics

Question 1

Endogenous opiates regulate CNS activity of pain, thermoregulation, appetite, reward

Answer 1

ok

Question 2

POMC forms

Answer 2

Beta Endorphins

Question 3

POMC produced only in CNS in what areas

Answer 3

Arcuate Nucleus of hypothalamus and Nucleus Tractus Solitarius.

Question 4

Conduction of afferent peripheral nerve is blocked by goltage gated Na channel blockers known as:

Answer 4

-caines

Question 5

NMDA receptor blockers used for what?

Answer 5

Preemptive blockade of NMDA can prevent surgery induced wind-up.

Question 6

Some NMDA receptor blockers are

Answer 6

Ketamine

Dextrmethorphan

Question 7

Ketamine may cause

Answer 7

hallucinations, amnesia, hypertension

Question 8

Dextromethorphan

Answer 8

dizziness, confusion, fatigue

Question 9

Carbamezapine

Answer 9

voltage gated Na channel blocker used to treat Trigeminal Neuralgia and Neuropathic pain.

Question 10

Interruption of the initial signal in peripheral tissues during pain signal transduction is accomplished by what kind of drugs

Answer 10

NSAIDS

Question 11

Na channel blockers block signal conduction in nociceptive fibers.

Answer 11

These are local anesthetics

Question 12

Why is calcium essential in promoting signal tranduction

Answer 12

It is necessary for the fusion of synaptic vesicles with presynaptic endplate to release neurostransmitters into the synaptic cleft

Question 13

What substances can inhibit calcium entry to the pre-synaptic terminal

Answer 13

Norepinephrine, GABA, endorphin and encephalin (both endogenous opiates)

Question 14

Post synaptically, norep, GABA, endorphin and encephalin do what?

Answer 14

They activate potassium channels thus hyperpolarizing the membrane and reducing the likelihoood of a depolarization threshold being reached and thus interrupting the pain signal

Question 15

The simplified mechanism of opiate analgesics

Answer 15

They work both pre and post-synaptically by activating the mu opiate receptor which in turn leads to decreased pre-synaptic calcium influx an increased post-synaptic calcium efflux.

Question 16

Central sensitization phenomenon

Answer 16

Sustained activation of pain pathways leads to short and long term post-synaptic changes in protein expression and function, resulting in an increased sensitivity to post-synaptic depolarization thus increasing the intensity of onward pain transmission signals

THE NMDA receptor plays a prominent role in this phenomenon.

Question 17

How do Ketamine and Dextromethorphan work>

Answer 17

Block NMDA receptors

Question 18

Phantom limb pain

Answer 18

neuropathic pain symtpom

Question 19

Slide 21

Answer 19

good review

Question 20

OP-1=

Answer 20

Opiate Receptor 1, Delta:

- Cortical and spinal analgesia, altered hormone and NT release

Question 21

OP-2=

Answer 21

Opiate receptor 2, Kappa:

- Cortical and spinal analgesia, psychomimetic and decreases GI transit

Question 22

OP-3

Answer 22

Opiate receptor 3, Mu

- COrtical and spinal analgesia, induces respiration, Lower Gi transit, altered hormone and NT release

Question 23

Low oral to IV dose ratio means what?

Answer 23

That oral doses must be higher to account for losses in absorption

Question 24

For all of the opioid agonists, what receptor mediates all of the effects (both beneficial and adverse?

Answer 24

Mu– OP-3

Question 25

Transdermal patches of Fentanyl provide what length of relatively stable drug delivery?

Answer 25

48-72 hours of stable drug delivery

Question 26

What drugs can be delivered rectally?

Answer 26

Occasionally Morphoine and morphones

Question 27

Does Morphine have high first pass metabolism?

Answer 27

YES...KNOW

Question 28

Codeine and oxycodone are effective how?

Answer 28

Orally due to low first pass effects

Question 29

Opiates distribute where in the body?

Answer 29

Distribute to high bloodflow organs first (muscle is the bigget reservoir)

Question 30

Know that opiates can distribute into adipose tissue with high continual dosing

Answer 30

ok

Question 31

Opiod receptors are what type of receptors

Answer 31

G-PCR....Realize that binding eventually leads to internalization (desensitization of the receptor) via the GRK-2 Beta Arrestin interaction. Endogenous opioids like ENK allow receptors to eventaully recycle and thus you have re-sensitization. Exogenous opioids don't let the receptors recycle as efficiently.

Question 32

Recycling of opioid receptors facilitated by?

Answer 32

GRK-2 and Beta Arrestin

Question 33

Know the potential adverse effects of opioid analgesics

Answer 33

ok

Question 34

Which of these potential adverse effects will not go away?

Answer 34

Miosis (closing the eyes), constipation, convulsions

Question 35

Most common adverse effect is

Answer 35

Constipation----because it won't go away you should always give a laxative.

Question 36

What if a laxative doesn't work for opiate induced constipation

Answer 36

Give an opioid antagonist.

Question 37

Why does constipation occur

Answer 37

Because the presence of opioid receptors in the GI system produces anti-cholinergic actions which slows down GI movement since Ach is the major stimulatory transmitter in regards to peristalsis.

Question 38

Nausea and vomitting generally occur when?

Answer 38

WHen the opioid dose is given too quickly.

Question 39

N/V generally does not persist as tolerance develops

Answer 39

ok

Question 40

Respiratory distress is really only a risk when?

Answer 40

- Drug given too quickly - Given with sleep apnea - Combined with a sedative or hypnotic

Question 41

What can be given to reverse respiratory depression

Answer 41

Naloxene

Question 42

What type of opiates cause histamine release?

Answer 42

morphine

Question 43

Opiate Overdose triad

Answer 43

COMA- Decreased cortical activity , RESPIRATORY ACIDOSIS from decreased drive to breathe , PINPOINT PUPILS- from modulation at Edinger Westphal nucleus

Question 44

Sedatives + Opiates

Answer 44

Increased CNS depression esp respiratory depression

Question 45

Antipsychotics + opiates

Answer 45

Sedation and CV effects

Question 46

MAOIs

Answer 46

contraindicated with opiates because hyperpyrexic coma and HTN

Question 47

All opiates are contraindicated in renal failure except

Answer 47

hydromorphone and fentanyl

Question 48

Meperidine metabolite with CNS toxicity

Answer 48

Normepridine

Question 49

Alcohol withdrawal looks like

Answer 49

Delirium, seizures, HTN, Tachycardia

Question 50

Cholinergic intox looks like

Answer 50

SLUDGEBBB

Question 51

Sympathomimetic intox?

Answer 51

agitation, tachycardia, HTN