Drugs for Dementia and Pain Flashcards by Leah Ritter

What is the mechanism of action for memantine and what disease does it treat?

-NMDA (N-methyl-D-aspartate) receptor antagonist
–binds to the Mg2+ site w/ greater affinity
–blocks channel stimulation by glutamate

–Alzheimer Dz (moderate to severe)

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What is neuropathic pain?

-arises from abnormal neural activity secondary to dz, injury, or dysfxn of the nervous system

sympathetically mediated pain
peripheral neuropathic pain (postherpetic neuralgia)
central pain (ex: phantom limb)

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What is allodynia?

-pain resulting from a stimulus (such as light touch) that does not normally elicit pain

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What is hyperesthesia?

-increased sensitivity to stimulation

excluding the special senses

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What is dysesthesia?

-an unpleasant abnormal sensation, whether spontaneous or evoked

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True or False: Delirium can be superimposed on dementia

True

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What is the mechanism of action for rivastigmine and how is it administered?

AchE inhibitor for dementia

- transdermal patch

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In what organ does COX-2 have a physiologic role?

kidney

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With NSAID use (especially in patients w/ a lowered GFR) the serum level of what can rise?

creatinine

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What is the most common clinical complication in advanced dementia?

feeding

-offer finger foods, small portions, favorite foods

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What normally blocks the NMDA receptor pore?

Mg2+

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How is menthol used to treat pain?

-stimulates TRPM8 “cold receptors” as a counterirritant

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What is the mechanism of action of dexmedetomidine?

–alpha2-adrenergic agonist for analgesia/sedation

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What is hypoalgesia?

-diminished response to normally painful stimulus

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What is a black box warning of NSAID’s during pregnancy (past 20wks gestation)?

renal dysfunction

- oligohydramnios

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What is the mechanism of action of gabapentin?

-binds to CNS alpha-2-delta subunit of voltage-gated calcium channels to inhibit release of NTR

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What are three conditions that can be treated with gabapentin?

neuropathic pain (diabetic peripheral neuropathy)
partial focal seizures
restless leg syndrome

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What is the method of administration for lidocaine?

topical analgesic

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What is a potential GI complication of COX inhibitors such as aspirin, ibuprofen, celecoxib?

ulcers

GI bleeding

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True or False: there is no such thing as a “standard dose” of opioids

True

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What is the mechanism of action of tapentadol for pain treatment?

-opioid agonist at mu receptor (moderate to strong)

- -blocks NE re-uptake

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How is capsaicin used to treat pain?

stimulates TRPV1 receptors as a counterirritant
desensitizes/depletes Substance P
treats both nociceptive AND neuropathic pain

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What is the treatment for apathy as a symptom of dementia?

cholinesterase inhibitor
antidepressant
methylphenidate

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Cyclooxygenase (COX) is important in the synthesis of what?

prostaglandins from arachidonic acid

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What are examples of neuropsychiatric symptoms that can occur in 75% of Alzheimer patients that become more prevalent as the disease progresses?

- delusions/hallucinations - euphoria - disinhibition - aggression - depression/anxiety --these symptoms are not improved by AchE inhibitors

What are some side effects of donepezil (centrally active AchE inhibitor) used to treat Alzheimer dementia?

- altered cardiac conduction (prolong QT, bradycardia) - N/V/D - can worsen peptic ulcers, asthma/COPD - bladder outflow obstruction

What is the mechanism of action of dihydroergotamine in the treatment of migraines?

-an ergot alkaloid that binds to multiple receptors to cause vasoconstriction

What is visceral pain?

- pain that arises from viscera stretch receptors - poorly localized - deep, dull, cramping

What is the mechanism of action of duloxetine?

--serotonin and NE re-uptake inhibitor

What can duloxetine be used to treat?

- fibromyalgia - generalized anxiety disorder - major depressive disorder - chronic MSK pain - neuropathic pain d/t DM

What is a side effect of duloxetine?

-increased risk of suicidal thoughts and behavior

How do NSAID's cause a decrease in pain?

-inhibit synthesis of prostaglandins from arachidonic acid | as opposed to steroids which block the release of arachidonic acid

What class of drugs can be used to treat multiple kinds of dementia (off-label) more than just Alzheimer's?

-acetylcholinesterase inhibitors

What common component of dementia is preferred to be treated w/ non-pharmacologic strategies?

sleep disturbances - sleep hygiene - maximize natural light in the morning - daily exercise

What is the mechanism of action in ubrogepant and rimegepant in the treatment of migraines?

- calcitonin gene-related peptide receptor antagonist | - inhibits pathologic dilation of intracranial arteries

What is the mechanism of action of amitriptyline and its use in treating chronic pain?

- tricyclic antidepressant | - major depressive disorder associated w/ chronic pain

What is a side effect of amitriptyline?

-increased risk of suicidal thinking and behavior in children, adolescents, and young adults

What is the mechanism of action of tramadol that is used to treat severe pain?

- -partial agonist at mu-opiate receptors in the CNS | - -inhibits re-uptake of NE and serotonin

What is the mechanism of action of clonidine and its two main pharmaceutical uses?

--alpha2-adrenergic agonist (epidural catheter) - -HTN - -relief of severe pain (blocks pain signal transmission)

Because clonidine and dexmedetomidine stimulate peripheral alpha2-receptors prior to entering the CNS, what can they cause?

-transient HTN

What is hypoesthesia?

-diminished sensitivity to stimulation | excluding special senses

What is the mechanism of action of ziconotide for chronic severe pain that is refractory to other treatments (administered intrathecally)?

--binds to N-type voltage-sensitive calcium channels on nociceptive afferent nerves of the dorsal horn in the spinal cord --blocks release of excitatory NTR's, causing reduced sensitivity to painful stimuli

What is the major clinical application of acetaminophen?

- temporary relief of minor aches, pains, headache | - -NOT an anti-inflammatory

What is the antidote for the acetaminophen hepatotoxicity that occurs when glutathione is depleted?

N-acetylcysteine - -there is a limited dose range b/w safe and toxic - -does NOT impair renal function

What is paresthesia?

- an abnormal sensation, whether spontaneous or evoked | ex: numbness, "pins and needles"

What is nociceptive pain?

-perception of input from a nociceptor, a nerve fiber that is preferentially sensitive to noxious stimuli

What is the mechanism of action for galantamine in the treatment of dementia?

-AChE inhibitor (reversible)

True or False: d/t risk of Reye Syndrome, aspirin should not be used to treat children w/ chicken pox or flu

True

How might long-term aspirin use affect the kidney?

papillary necrosis

What are the effects of aspirin during labor and delivery?

- suppress uterine ctx - premature closure of ductus arteriosus - intensify uterine bleeding

What is the mechanism of action of ketamine and its use?

-NMDA receptor antagonist that blocks glutamate - induction and maintenance of general anesthesia - lower dose for acute and chronic pain - reduces the amount of morphine needed for pain

What is an endogenous opioid in the descending pain inhibitory fibers?

enkephalin

When cyclooxygenase is blocked, what product can still be generated from arachidonic acid via a different pathway?

-leukotrienes that cause bronchoconstriction

Aspirin toxicity causes hyperventilation leading to what, initially?

respiratory alkalosis

What is the only COX-2 inhibitor on the US market?

celecoxib

What is a serious side effect of celecoxib?

- risk of thrombosis - risk of MI - risk of stroke - contraindicated in CABG patients --benefits may outweigh risks in pts w/ GI problems

What is hyperalgesia?

increased response to a stimulus that normally is painful

What is the mechanism of action of naproxen and benefit to taking it over other NSAID's?

- -reversible non-selective COX inhibitor - -long half-life (15hrs) allows once daily dosing - -okay to take even with heart problems

What can happen if you abruptly stop donepezil (AChE inhibitor) or memantine (NMDA receptor antagonist) that are used to treat dementia?

AMS

What SSRI can be used to treat depression in Alzheimer patients?

citalopram -sertraline could be an alternative --AVOID tricyclic antidepressants (amitriptyline)

What is the ascending pain transmission pathway?

spinothalamic tract

True or False: recurrent infections is a common clinical problem in patients with advanced dementia

True

True or False: chronic daily medications should be discontinued in pts with advanced dementia when they are no longer beneficial

True

Does post-herpetic neuralgia cause peripheral nerve damage or autonomic nerve damage?

peripheral

What are prostaglandins?

arachidonic acid metabolites that are important mediators of pain sensation by nociceptors

How is the dorsal horn of the spinal cord important in pain?

-it's where the nociceptor input converges with the descending neuromodulatory input on the neurons transmitting the pain

What is lasmiditan (5-HT1F receptor agonist) used to treat and how does it work?

migraines - decreases stimulation of the trigeminal system - does NOT cause vasoconstriction

What is somatic pain?

- -arises from injury to body tissues - -well-localized - -variable in description and experience

What is the mechanism of action of sumatriptan and what does is treat?

- -selective 5-HT1B and 5-HT1D agonist | - -moderate to severe migraines

What is the mechanism of action of pregabalin and what does it treat?

--binds to alpha-2-delta subunit of voltage-gated calcium channels and inhibits release of NTR's - -neuropathic pain (d/t diabetic neuropathy) - -fibromyalgia - -focal partial seizures

What is the mechanism of action of ibuprofen and what are the major risks?

-reversible COX inhibitor - increased risk of MI and stroke - increased risk of GI bleed

What is the mechanism of action of aspirin?

- irreversible binds COX | - antiplatelet agent