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Neurology Boards Review > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Entacapone

A
  • COMT inhibitor (catechol-o-methyltransferase)
  • Dopamine is metabolized by COMT –> 3-o-methyldopa
  • by inhibiting conversion, it extends plasma half-life of dopamine
  • administered concomitantly with levodopa
  • increase duration of action of levodopa, reduce off periods
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2
Q

Levodopa

A
  • dopamine precursor
  • after ingestion, it is converted in the brain and peripherally to dopamine by dopa-decaroboxylase
  • peripheral conversion –> SE (nausea & dyskinesias due to dose and duration of therapy); carbidopa inhibits peripheral conversion (that is why it is adminsitered with levodopa)
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3
Q

Pramipexole & Ropinirole

A
  • dopamine agonists at D2 and D3 receptors
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4
Q

Rasagiline, Selegiline

A
  • selective MAOB inhibitors (involved in dopamine metabolism)
  • SE selegiline: insomnia (converted into methamphetamine)
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5
Q

Trihexyphenidyl

A
  • anticholinergic
  • treatment of tremor (thought to result from excess Ach)
  • SE: cognitive dysfunction (esp older), constipation, dry eyes/mouth, urinary retention
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6
Q

Amantadine

A
  • antiglutamatergic
  • also used in treatment of PD
  • increases presynaptic dopamine release, inhibits reuptake of synaptic dopmaine
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7
Q

Barbiturates

A
  • phenobarb, pentobarb, thiopental, secobarbital
  • facilitate GABAa action by increasing duration of Cl- channel opening, thus decreasing neuron firing
  • OD can cause CNS depression, respiratory and cardiovascular depression, induces CYP 450
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8
Q

Benzodiazepines

A
  • Diazepam, lorazepam, midazolam
  • facilitate GABAa action by increasing frequency of Cl- channel opening
  • most have long T1/2 (except midazolam)
  • CNS depression, less risk of resp depression and coma than with barbiturates
  • tx OD with flumazenil
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9
Q

Memantine

A

NMDA receptor antagonist; used for tx of alzheimers dementia (moderate-severe disease in adjunct to a AchE inhibitor, usually donepezil)

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10
Q

AchE inhibitors

A

Donepezil, galantamine, rivastigmine

- rivastigmine can also be used in Parkinson’s dementia

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11
Q

Pimavanserin

A

new 5-HT2A receptor inverse agonist that has been shown to reduce psychosis in Parkinson’s disease without worsening motor symptoms

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12
Q

Fingolimod

A
  • acts on sphingosine-1 phosphate receptors (S1P1 receptor) –> decrease in release of lymphocytes
  • first oral agent for treatment of MS
  • side effects: macular edema, bradycardia
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13
Q

Antipsychotics associated with TD

A

fluphenazine and haldol

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14
Q

Drugs used to tx essential tremor

A
  • combo of primidone and propranolol shown to be more effective than either alone (each reduces tremor by 50%)
  • can also use topiramate, gabapentin, and benzo (clomazepam)
  • in severely resistant cases, can consider DBS to ventra intermediate nucleus of thalamus
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15
Q

Tysabri (Natazulimab)

A

Monoclonal AB for relapsing MS

  • MOA: selectively binds to alpha-4 subunit of integrin (cell adhesion molecule)
  • reduces ability to inflammatory cells to cross BBB into CNS –> decreased inflammation
  • need to screen for JC virus
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16
Q

Teriflunomide (Aubagio)

A

For RRMS

  • selectively and reversibly inhibits DHOD (dihydroorate dehydrogenase) which is mitochondrial enz necessary for pyrimidine synthesis
  • immunomodulatory effects which is useful in MS
  • may cause transaminitis
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17
Q

Alemtuzumab (Lemtrada)

A

monoclonal AB useful for relapsing MS

  • binds to CD52 (T and B lymphocytes)
  • has serious side effects (emergency of 2/2 autoimmune dx)
  • only approved to pts who have failed 2 other MS medications
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18
Q

Ocrelizumab (Ocrevus)

A
  • target of action is CD20 (B cell marker); same as rituximab
  • ## approved to relapsing and progressive MS
19
Q

Antidepressants to be avoided in epilepsy

A

bupropion, TCAs, clomipramine, amoxapine

20
Q

Antidepressants which precipitate and exacerbate RLS

A

TCAs, SSRIs, and lithium

21
Q

Dalfampridine (Ampyra)

A
  • potassium channel blocker, increases conduction of action potential in demyelinated axons (MS)
  • improves gait function in 1/3 of MS patients
  • SE: seizures and anxiety
22
Q

Risperidone

A
  • se: orthostatic hypotension, dizziness (alpha 1 blockade), headaches
  • more likely to cause TD at higher doses than other atypical antipsychotics
23
Q

Galantamine

A
  • used in tx of AD

- acetylcholinesterase inhibition and modulation of nicotinic Ach R to increase presynaptic Ach

24
Q

dextromethorphan-quinidine

A

used for tx of pseudobulbar affect

25
Q

OCD treatment

A

First line: SSRI (fluoxetine, fluvoxamine, sertraline, paroxetine, escitalopram, citalopram)

26
Q

Triptans

A
  • work on the 5-HT 1D, 1B, and 1F receptors (agonist)
  • used as migraine abortives
  • use contraindicated in those with severe liver disease, pregnancy, cerebro-vascular disease, uncontrolled HTN, and CAD/PVD
27
Q

Ergots (DHE)

A
  • used as migraine abortive
  • act on 5-HT 1B, 1D, and other 1 subtypes (agonist)
  • also have agonist activity on D2 receptors (pre-treat with DA blockers to prevent side effects)
28
Q

SNRI

A
  • selective inhibition of both serotonin and NE

- duloxetine, venlafaxine, desvenlafaxine

29
Q

Bupropion

A
  • weak reuptake inhibitor of both DA and NE
30
Q

Mirtazapine

A
  • antagonist of presynaptic α2‐adrenergic autoreceptors and a2-heteroreceptors
  • antagonist at post-snaptic 5-HT2, 5-HT3, and H1 receptors
31
Q

Buspirone

A
  • selective partial agonist activity at the 5-HT1A receptor (pre-synaptic)
  • inhibitory effect on DA D2 Receptors
32
Q

Dimethyl fumurate (Tecfidera)

A
  • activating the nuclear erythroid 2-related factor 2 (Nrf2)

- side effects: flushing and GI distress

33
Q

Most likely secondary antipsychotic to increase likelihhood of seizures

A

clozapine

34
Q

Tertiary TCA

A
  • amitriptyline, clomipramine, doxepin, imipramine

- block serotonin transporters and inhibit serotonin reuptake –> increased serotonin synaptic levels

35
Q

Secondary TCA

A
  • nortriptyline, protriptyline, desipramine

- block NE transporters and inhibit uptake of NE

36
Q

TCA Side effects

A
  • anticholinergic: dry mouth, constipation, urinary retention
  • headache, weight gain, sweating
  • cardiac arrhythmias
37
Q

MAOI

A
  • increase in synaptic serotonin, dopamine, and NE
  • lots of SE: orthostatic hypotension, edema, weight gain, dizziness
  • interactions with tyramine containing food
  • need to wait for 3-4 week washout period before initiating SSRI, SNRI, TCA, dextromethorphan, ephedrine, and stimulants
38
Q

SSRI

A
  • fluoxetine, paroxetine, sertraline, citalopram, and escitalopram
  • block serotonin reuptake; decrease in 5-HT1a receptors
  • SE: diarrhea, anorgasmia, suicidality, serotonin syndrome
39
Q

Disulfiram

A
  • used in tx of alcohol dependence
  • binds irreversibly to aldehyde dehydrogenase –> accumulation of aldehyde when alcohol is consumed –> flushing, nausea, vomiting, headache, & confusion
40
Q

Naloxone

A
  • short acting mu opioid receptor antagonist (high affinity) and kappa and delta opioid receptor antagonist (low affinity)
  • used to treat opioid overdose –> withdrawal
41
Q

Naltrexone

A
  • long acting competitive opioid antagonist that blocks the subjective effects of opiates; does not block cravings
42
Q

Methadone

A

long acting opioid agonist used as maintenance treatment of opioid dependence

43
Q

Buprenorphine

A

mu-opioid receptor partial agonist (high affinity) and kappa-opioid receptor antagonist (lower affinity) used to treat opioid dependence. Allow for accelerated withdrawal without significant distress

44
Q

Clonidine

A
  • centrally acting alpha-adrenergic agonist
  • used off label to treat opioid withdrawal
  • most effective for autonomic signs and symptoms

Neurology Boards Review (8 decks)

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