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Week 2 (Neuro 2) > PHARM - Sleep & MS drugs > Flashcards

PHARM - Sleep & MS drugs Flashcards

1
Q

what is the role of the ventrolateral preoptic nucleus (VLPO) in sleep induction?

A

sleep promotion

  1. throughout the day, ATP is broken down to adenosine
  2. accumulating adenosine binds to A1 & A1 receptor on VLPO, a thalamic nucleus
  3. in resopnse, the VLPO releases GABA & galanin (inhibitory NTs)
  4. GABA opens Cl- channels, hyperpolarizing the membrane
  5. APs are mitigated -> sleep induction
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2
Q

what is the role of the lateral nucleus in sleep?

A

alertness

  1. lateral nucleus of hypothalamus releases orexin
  2. orexin projects to arousal regions of the brain:
    • locus coerelulus
    • tuberomamillary nucleus
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3
Q

what is the role of histaminergic neurons in sleep?

A

promote alertness

project to tuberomamillary nucleus, an arousal center

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4
Q

list the roles of GABA, melatonin, orexin, histamine in modulating sleep

A
  • GABA - promote sleep
  • melatonin - promote sleep
  • orexin - promote arousal
  • histamine - promote arousal
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5
Q

what are the four classes of hyponotic drugs?

A
  1. benzodiazepine-like drugs (GABA enhancers) - induce sleep
  2. melatonin agonists - induce sleep
  3. orexin antagonists - block arousal
  4. histamine 1 receptor antagonists - blcck arousal
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6
Q

what are the two classes of benzodiazepines?

list the drug names, clinical use, and MOA of the drugs belonging to each class.

A

both classes work by enhancing the affects of GABA.

  • benzodiazepine like drugs (BLZs)
    • include: zolpidem, zaleplon, eszopiclone
    • clinical use: for hypnosis
    • MOA: bind selectively alpha-1 subunit containing GABAA receptors
  • benzodiazepines
    • include: triazolam, - pams
    • clinical use: for anxiolysis > hyponosis, anesthesia, muscle relaxation
    • MOA: bind less selectively to alpha-1,2,3,5 containing GABAA receptors
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7
Q

describe the structure of GABAA receptors.

why is this clinically relevant?

A
  • all made of 5 subunits: 2 alpha, 2 beta, 1 gamma
    • the specific structure of the a-subunit can vary: a1, a2, a,3, a5
      • BLZs (hypnotics):
        • specifically bind a1 containg receptors
      • benzodiazepines (anxiolytics):
        • less specifically bind a1-a5 containing receptors
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8
Q

benzodiazepine like drugs

  • includes what drugs?
  • clinical use
  • MOA
  • AE / CI / drug-drug interactions
A
  • drugs: zolpidem, zaleplon, eszolpiclone
  • clinical use: for hypnosis
  • MOA: bind to alpha-1 containing GABAA receptors & enhance their affinity for GABA
  • PK: metabolized by CYP-3A4
  • AE / CI / drug-drug interactions:
    • AE: drowsiness / insomnolence
    • CI: in pt on CNS depressants - opiods, barbituates, ethanol
    • drug-drug interactions:
      • CYP-3A4 inhibitors: cimetidine, corbistat, ritonavir
      • CYP-3A4 inducers: rifampin
      • Flumenzenil
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9
Q

BZ-like drugs should be used with caution with patients taking what other drugs?

A

zolpedem, azleplon, escopiclone

  • CYP-3A4 inhibitors (increase half life)
    • cimetidine
    • cobiscistat
    • ritonavir
  • CYP-3A4 inducers (decrease half life): rifampin
  • competitive antagonists: flumazenil
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10
Q

administration of BZ-like drugs with which other drugs will limit their ability to induce sleep?

why?

A

zolpidem, zaleplon, eszopiclone

  • rifapmin: induces CYP-450, which metabolizes BZ-like drugs
  • flumazenil: a competitive antagonist at the BZ-like drug binding site
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11
Q

BZ-like drugs are absolutely contraindicated in patients taking what other drugs?

A

zolpidem, zaleplon, escopiclone

  • CNS depressants:
    • opiates
    • ethanol
    • barbiturates
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12
Q

what is flumazenil?

A

a competitive antagonist for BZ-like drugs

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13
Q

zolpidem is what kind of drug?

A

BZ-like drug

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14
Q

zaleplon is what kind of drug?

A

BZ like drug

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15
Q

eszopiclone is what kind of drug?

A

BZ-like drug

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16
Q

which BZ-like drug is most likely to cause rebound insonmia?

how does this rebound insomnia present?

A

zolpidem

insomnia the 1st night after discontinuation after chronic usage

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17
Q

suforexant

  • clinical use
  • MOA
  • AE/CI
A
  • clinical use: hypnotic
  • MOA: orexin antagonist -> inhibits arousal
  • AE/CI
    • AE: CNS depressant [Schedule IV]
    • CI: other CNS depressants
18
Q

H1 receptor antagonists

  • includes what drugs
  • clinical use
  • MOA
  • AE/CI
A
  • includes: doxepin, diphenhydramine
  • clinical use: for hypnosis
  • MOA: histamine antagonists - prevent arousal
  • AE/CI:
    • AE
      • CNS depression - dopexin worse
      • anti-cholinergic affects - diphenhydramine worse*
    • CI: other CNS depressants
19
Q

doxepin

  • clinical use
  • MOA
  • AE/CI
A
  • clinical use: for hypnosis
  • MOA: histamine antagonists - prevent arousal
  • AE/CI:
    • AE: CNS depression > anti-cholinergic affects
    • CI: other CNS depressants
20
Q

diphenhydramine

  • clinical use
  • MOA
  • AE/CI
A
  • clinical use: for hypnosis
  • MOA: histamine antagonists - prevent arousal
  • AE: anti-cholinergic affects > CNS depression
    • dry mouth
    • constipation
    • urinary retention
    • blurred vision

*remember that in the treatment of headaches, diphenhydramine can be used to reverse akinesa caused by anti-emetics

21
Q

ramelteon

  • clinical use
  • MOA
  • AE
A
  • clinical use: for hypnosis - weak drug
  • MOA: agonist at melatonin receptors - MT1 & MT2
  • AEs: posssible inc in serum prolactin
22
Q

what is an advantage of ramelteon over other hypnotic agents?

A

has little abuse potential

23
Q

loss of orexin neurons leads to what major pathologies?

A
  • narcolspey: loss of sharp wake to sleep transitions
  • cataplexy: sudden loss of motor function
24
Q

what drugs are used to treat narcolepsy?

A
  • - dafinil: modafinil, armodafinil
  • sodium oxybate (xyrem)
25
what drugs are used to treat cataplexy?
* **venlafaxine** * sodium oxybate (Xyrem)
26
modafinil * clinical use * MOA * AE
* clinical use: **narcolspey** * MOA: unknown * AEs: * **headaches** * nausea / chills / back pain
27
armodafinil * clinical use * MOA * AE
* clinical use: **narcolspey** * MOA: unknown * AEs: * **headaches** * nausea / chills / back pain
28
sodium oxybate
* clinical use: * **narcolepsy** * **cataplexy** * MOA: unknown * AE/CI: * **respiratory depressant** * **CNS depressant**
29
sodium oxybate is contraindicated in patient taking what other drugs?
CNS depressants AND respiratory depressants
30
venlafaxine * clinical use * MOA * AE/CI
* clinical use: **cataplexy** * MOA: **SNRI -** increases daytime arousal * AE/CI: minor GI effects
31
the drugs used to treat multiple sclerosis (MS) fall belong to what major classes? what is the therapuetic goal is each class?
* glucocorticoids: **for acute attacks** - initial episode or relapses * immunosuppressive biologics: **disease modifying** * ​relapsing remitting * secondary progressive * primary progressive
32
what is an AE of all drugs used to treat MS? why?
increased infection risk they are all immunosuppresive.
33
INF-B * what kind of drug * clinical use * MOA * AE
* MS disease modifying drug * clinical use: **​relapsing-remitting** **AND** **secondary progressive MS** * MOA: possibly T-cell proliferation * AE * **fever** * **chills** * **myalgia**
34
glatiramer acetate * what kind of drug * clinical use * MOA * AE
* disease modifying MS drug * clinical use: relapsing remitting MS - **also, is pregnancy class B** * MOA: unknown, T-cell related * AE: n/a
35
natalizumab * * clinical use * MOA * AE
* disease modifying MS drug * clinical use: relapsing remitting MS * MOA: **inhibits alpha-4 integrins (VCAM-1 receptors), inhibiting vascular adhesion** * AE: **increases risk** **multifocal leukoencephalopathy (PML)**, a fatal, progressive disaese caused by JK virus
36
what must patient be tested for prior to being described natalizumab?
* antibodies against JC virus, which can cause polymultifocal leukoencephalopathy (PML) * natalizumab increases risk of PML developing from JC virus
37
fingolimod * clinical use * MOA * AE/CI
* disease modifying MS tx * clinical use: relapsing - remitting MS * **MOA:** binds to s**phinosin-1-phosphate** (S-1-P) receptors, preventing lymphocytes from entering circulatation * **AE:** * ​herpes simplex / herpes zoster * retinal edema * cardiac conduction block
38
alemtuzumab * what kind of drug * clinical use * MOA * AE/CI
* disease modifying MS tx * clinical use: relatpsing remitting MS * MOA: **monoclonal antibody against CD52** * AE/CI: * **T**hyroid-associated AEs * **T**hryoid papillary carcinoma * **T**hrombocytopenia * myelosuppresion
39
ocrelizumab * what kind of drug * clinical use * MOA * AE/CI
* disease modifying MS drug * clinical use: **relapsing remitting AND primary progressive multiple sclerosis** * MOA: antibody against **CD-20 marker on mature B-cells** -\> depletes mature B-cells * AE: * infusion rx * Hep-B reactivation
40
which disease modifying MS drug can be used to treat secondary progressive MS?
INF-B
41
which disease modyfing MS drug can be used to treat primary progressive MS?
ocrelizumab

Week 2 (Neuro 2) (9 decks)

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