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PM&R Recap > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Natural opioids include?

A

morphine and codeine

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2
Q

What is the MOA of opioids?

A

Binding to mu, kappa, delta receptors lowers presynaptic Ca2++ influx and increases postsynaptic K+ transport; which together reduce synaptic action potential transmission of central pain fibers

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3
Q

What are the different roles of the receptors that opioids act on?
Mu1
Mu2
Kappa
Delta

A

Mu1 = pain reduction (#1 opioid receptor)
Mu2 = respiratory depression, nausea/vomiting
kappa = respiratory depression
delta = pain reduction

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4
Q

What are notable side effects of opioid medications?

A
  • Respiratory depression/death
  • hypogonadism/low testosterone (low motivation, diminished personality)
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5
Q

Special indication for codeine in stroke patients?

A

Aborting intractable tension headaches, especially in neurologic disease (stroke)

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6
Q

Which opioid is also an NMDA antagonist?

A

Methadone

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7
Q

Which opioid has mixed agonist-antagonist activity?

A

Buprenorphine

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8
Q

Which opioid is a mu agonist and seratonin-norepinephrine reuptake inhibitor with increased risk of seratonin syndrome?

A

Tramadol

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9
Q

MOA of acetaminophen?

A

inhibiting prostaglandin production (COX enzyme) in CNS - inhibits pain and fevers centrally

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10
Q

Why are NSAIDs sometimes contraindicated following procedures/surgery?

A

To allow for proper healing and pro-inflammatory response

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11
Q

which NSAIDs are COX-2 selective?

A

Celecoxib, meloxicam

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12
Q

What is the MOA for the analgesic properties of amitriptyline?

A

modulation of descending inhibitory pathways that arise in the brain stem centers and synapse within the dorsal horn of the spinal cord

Neurons in these tracts are primarily seratonergic and noradrenergic

*can contribute to seratonin syndrome

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13
Q

Side effects of amitriptyline?

A

QT prolongation
Anticholinergic side effects (dry mouth, urinary retention, constipation)

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14
Q

MOA of Gabapentin/Pregabalin?

A

Blocks L-type Ca2++ channels in the CNS (inhibits synaptic transmission)

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15
Q

Which indications is pregabalin FDA approved?

A

diabetic neuropathic pain
postherpetic neuralgia
fibromyalgia

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16
Q

MOA of duloxetine?

A

SNRI

*can contribute to seratonin syndrome

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17
Q

MOA of carbamazepine?

A

Inhibits Na+ channels on neurons, preventing signal transmission along nerves

*trigeminal neuralgia

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18
Q

MOA of capsaisin?

A

depletes substance P

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19
Q

MOA of corticosteroids?

A

Inhibits PLA2 enzyme (thus inhibiting arachidonic acid production and prostaglandin production)

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20
Q

Which steroids are particulate?
Which steroid is nonparticulate?

A

particulate: triamcinolone, methylprednisolone

non-particulate: dexamethasone

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21
Q

MOA of baclofen?

A

Centrally acting Gaba(B) agonist
- GABAb1 binding inhibits presynaptic Ca2++ into neuron
-GABAb2 binding increases postsynaptic K+ conductance

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22
Q

Side effects of baclofen?

A

sedation
constipation
lowers seizure threshold

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23
Q

signs of baclofen withdrawal?

A

ITB - Itchy, twitchy, bitchy

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24
Q

Clearance of baclofen?

A

Renally cleared

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25
Q

MOA of diazepam (spasticity)?

A

centrally acting GABAa agonist
- GABAa binding increases presynaptic Cl- influx into neuron

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26
Q

Clearance of diazepam?

A

Hepatically cleared

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27
Q

MOA of tizanidine?

A

centrally acting alpha-2 agonist (as is clonidine) –> inhibits spinal reflex arc

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28
Q

Signs of tizanidine withdrawal?

A

HTN, tachycardia, anxiety, worsened spasticity

29
Q

Clearance of tizanidine?

A

Hepatically cleared - check LFTs prior to starting and monitor once starting

30
Q

MOA of Dantrolene?

A

peripherally acting - binds ryanodine receptors on sarcoplasmic reticulum, inhibits influx of Ca2++ from SR into cell

31
Q

Clearance of dantrolene?

A

hepatically cleared, check LFTs prior to starting, monitor while starting med

32
Q

MOA of botulinum toxin?

A

Inhibit presynaptic syntaxin, synaptobrevin, and SNAP-25 proteins which store ACh prior to being released into synapse

33
Q

Black box warning for botulinum toxin?

A

distant toxin spread may cause dysphagia, respiratory depression

34
Q

Docusate MOA

A

“grease the groove” - stool softener that allows water and fat into stool

35
Q

MOA of senna?

A

stimulant that irritates the bowel wall to promote peristalsis

36
Q

MOA of polyethylene glycol (miralax)?

A

osmotic laxative that pulls fluid into bowel lumen, promoting urgency of BM

37
Q

Lactulose MOA?

A

traps NH3 in bowel, allowing it to be excreted, also a powerful osmotic laxative

*consider KUB to r/o bowel obstruction before starting

38
Q

Bisacodyl MOA?

A

rectal wall irritant that is used to stimulate rectal propulsion and evacuation of stool

39
Q

Lubiprostone (Amitiza) MOA for chronic constipation?

A

increases intestinal fluid secretion and promotes GI motility through activation of type 2 Cl- channels

40
Q

Methylnaltrexone (relistor) MOA?

A

Blocks Mu receptors outside CNS to improve GI motility

Indicated for opioid-related constipation

41
Q

Oxybutynin/Tolterodine MOA?

A

strong anticholinergic medication that inhibits cholinergic activity upon muscarinic detrusor muscle to spastically contract

indicated for spastic detrusor activity

SE: dry mouth, constipation, sedation

42
Q

Mirabegron MOA?

A

beta-3 agonist that acts selectively on bladder wall beta receptors to promote bladder storage

**Acts via sympathetic noradrenergic pathway

43
Q

Bethanechol MOA?

A

pro-cholinergic medication that increases detrusor activity - promotes bladder emptying by stimulating muscarinic ACh receptors in bladder wall

*Cholinergic S/E: runny noise, hypersalivation, diarrhea

44
Q

Tamsulosin MOA for bladder use?

A

alpha-1 blocker that acts in urinary bladder neck to inhibit sympathetic (noradrenergic) action - relaxes smooth muscle to open bladder neck

45
Q

Duration of anticoagulation in SCI population?

A

Incomplete: on AC until IPR discharge

Complete, uncomplicated: 8 weeks

Complete, complicated: 12 weeks

46
Q

Heparin MOA?

A

activates antithrombin 3, which then inhibits Factor Xa

*Rapid reversal with protamine sulfate

Monitor platelets, risk of HIT

47
Q

Enoxaparin MOA?

A

binds to antithrombin III, a serine protease inhibitor, forming a complex that irreversibly inactivates factor Xa

Also reversed with protamine sulfate

48
Q

Amantidine MOA?

A

NMDA receptor antagonist and direct dopamine agonist

Neurostimulation agent used to improve arousal

Can lower seizure threshold

49
Q

Modafanil MOA?

A

exact mechanism unknown, thought to be related to dopamine re-uptake inhibition

50
Q

Methylphenidate MOA?

A

Norepinephrine-dopamine reuptake inhibitor

Useful for ADHD, neurostimulant in stroke/TBI

*does not lower seizure threshold

51
Q

Donepezil MOA?

A

Cholinesterase inhibitor that promotes ACh accumulation in the brain (cholinergic)

May be useful neurostimulant in anoxic brain injury, addresses behavior and cognitive symptoms in Alzheimer patients

52
Q

Valproate MOA?

A

Voltage-gated Na+ channel blockade; mechanism not fully understood

Can cause excessive sedation; can check blood level

53
Q

Carbamazepine MOA?

A

Inhibits Na+ channels on neurons; thus preventing signal transmission along nerves

*Useful for trigeminal neuralgia
Also used as mood stabilizer in TBI pts

54
Q

Trazodone MOA?

A

Serotonin reuptake inhibitor that is used as a combination antidepressant sleep-aid

*Risk of serotonin syndrome

55
Q

Mirtazapine MOA?

A

Increases central serotonergic and noradrenergic activity

Useful to increase appetite, improve mood and serve as sleep aid

56
Q

Pyridostigmine MoA?

A

Anticholinesterase - prevents breakdown of ACh in synaptic cleft

57
Q

Riluzole MoA?

A

Blocks glutamate action in the CNS

Prolongs survival by a few months in ALS patients

58
Q

Medications for SMA treatment?

A

Nusinerson - alters splicing activity of SMN2 gene so that it produces more SMN protein

Onasemnogene abeporvovec - replaces mutated SMN1 gene, creates functional SMN1 protein

Risdiplam - modifies splicing pattern of SMN2 RNA so cell makes more SMN2 protein

59
Q

MoA of local anesthetics? (lidocaine, bupivacaine, ropivacaine)

A

Na+ channel inhibitors, thus inhibiting action potential transmission

60
Q

MoA of Dalfampridine (ampyra)?

A

potassium channel blocker that increases ACh release at the neuromuscular junction and in the central nervous system

Improves walking speed in patients with all forms of MS

61
Q

Which drug in transplant patients can cause AMS including hallucinations?

A

Tacrolimus (especially at supratherapeutic levels)

Delirium often improves as tacrolimus level falls into therapeutic range

62
Q

Spasticity medication that is contraindicated w/ IV ciprofloxacin?

A

Tizanidine

Cipro inhibits cytochrome P450-1A2 resulting in decreased hepatic metabolism of tizanidine - increasing plasma concentration

63
Q

Medications that increase PT/INR?

A

sulfonamides, acetaminophen, amiodarone, aspirin, NSAIDs

64
Q

Medications that decrease PT/INR

A

Adrencorticoids, antacids, antihistamines, cabamazepine, haloperidol, vitamin C

65
Q

Which drug class is cyclobenzaprine similar to?

A

TCAs (first studied as antidepressant)

66
Q

Rituximab MOA?

A

binds B-lympcytes CD20 surface antigens and depletes the B cell population

67
Q

Etanercept MOA?

A

TNF alpha antagonist

68
Q

Abatacept MOA?

A

blocks co-stimulatory molecules and T-cell activation

69
Q

Anakinra MOA?

A

inhibits interleukin-1 type receptors

PM&R Recap (10 decks)

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