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Neuro 2 > Pharm 1 > Flashcards

Pharm 1 Flashcards

1
Q

Barbiturates

A
  • insomnia drug
  • MOA: bind to and increase GABA actions
  • AE: sedation –> hypnosis –> anesthesia –> coma
  • not as safe as benzodiazepines
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2
Q

Benzodiazepines

A
  • insomnia drug
  • MOA: modulates alpha subunit of GABA receptors, shifts dose-response curve to the left (allosteric modulation)
  • conjugation and renal excretion
  • AE: sedation, cognitive impairment, rebound insomnia, causes withdrawal (anxiety, irritatilbity, resp depression)
  • schedule 4, category X
  • contra: liver dz, COPD, depression, driving, other CNS depressants, glaucoma
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3
Q

BZ 1-3 alpha receptor subgroup

A

BZ1 - sedation/amnesia
BZ2 - anxiolysis
BZ3 - myorelaxation/anticonvulsant

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4
Q

Estazolam

A
  • benzodiazepine for insomnia
  • CYP3A4, doesn’t accumulate
  • quick elim, short t1/2
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5
Q

Flurazepam

A
  • benzodiazepine for insomnia

- CYP3A4, does accumulate

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6
Q

Quazepam

A
  • benzodiazepine for insomnia

- CYP2D6>CYP3A4, accumulates

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7
Q

Temazepam

A
  • benzodiazepine for insomnia

- no cyps (conjugation)!! doesn’t accumulate

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8
Q

Triazolam

A
  • benzodiazepine for insomnia

- CYP3A4, no accumulation (rapidly inactivated)

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9
Q

Benzodiazepine receptor agonist

A
  • for insomnia
  • similar MOA as benzos but safer
  • AE: sedation, cog impairment, rebound insomnia, withdrawal (anxiety, irritability, restlessness, sleep apnea, resp depression)
  • schedule 4, CYP interactions
  • category C
  • contra liver dz, COPD, depression, CNS drugs
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10
Q

Zolpidem

A
  • for insomnia
  • aka Ambien
  • benzo receptor agonist
  • most prescribed hypnotic
  • can get as sublingual (only one that can be used in middle of night) and oral spray
  • use lower dose in women
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11
Q

Zaleplon

A
  • for insomnia
  • benzo receptor agonist
  • ald dehydrogenase
  • variable dose in Asians
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12
Q

Eszopiclone

A

Benzo receptor agonist for insomnia

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13
Q

Flumazenil

A
  • benzo antagonist to reverse effects of benzos/benzo agonists
  • IV quick acting
  • can cause abrupt awakening with dysphoria, agitation, can cause seizures, withdrawal
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14
Q

Melatonin

A
  • made in pineal gland, produces drowsiness involved in circadian rhythm
  • GPCRs
  • MT1 - attenuates SCN activity (sleepy)
  • MT2 - maintains circadian rhythms
  • MT3 not involved in sleeep
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15
Q

Ramelteon

A
  • melatonin receptor agonist, not scheudled
  • no morning impairment, abuse, or resp depression
  • AE: HA, somnolence, nausea, insomnia, URTI, nasopharyngiitis
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16
Q

Antidepressants

A
  • can be used for insomnia but not intended
  • AE of sedation
  • int with CYPs, other depressants, EtOH, BBW for suicide
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17
Q

Doxepin

A
  • antidepressant that can be used for insomnia
  • primarily anti H1 at low doses
  • SE: sedation, muscarinic blocker, SNRI
  • the only one that’s actually approved
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18
Q

Mirtazapine

A
  • antidepressant that can be used for insomnia

- primarily alpha 2 antagonism (reinforces 5HT and NE release)

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19
Q

Trazodone

A
  • antidepressant that can be used for insomnia

- sedation with a little 5HTRI

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20
Q

1st gen antihistamines

A
  • for insomnia
  • cross BBB, produce sedation through anti H1
  • AE: zerostomia, blurred vision, urinary retention (anticholinergic), inc. ocular P
  • rapid tolerance can develop
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21
Q

Diphenhydramine and doxylamine

A
  • 1st gen antihistamines for insomnia
22
Q

GABA receptor

A

a GPCR that gates entry of Cl- ions into cell

23
Q

At really high doses, ______ can actually activate and open the GABA channel on their own

A

barbiturates

24
Q

Tension headache tx

A

pts usually self medicate with NSAIDs (Ibuprofen, Naproxen)

25
Q

Cluster headache tx

A

nasal/SC triptans or ergots

steroids (prednisone)

26
Q

for mild/moderate menstrual HA

A

give NSAIDs

27
Q

for moderate/severe HA

A

give short acting triptan (Sumatriptan)

28
Q

Prophylaxis of migraine

A

AMITRYPTILLINE - TCA/SNRI/antichol, ae aggresion/wt gain/xerostomia/sedation
TOPIRAMATE - blocks Na and glutamate/ inc GABA, ae parasthesia/nausea/fatigue/narrow therapeutic range
VALPROATE - Na channel blocker, inc GABA, CatX, hepatotoxic, highly protein bound
PROPANOLOL AND TIMOLOL - dec vasodilation, dec NE induced lipolysis, ae fatigue/asthma/DM/AV block/exercise intolerance
METOPROLOL
BOTOX - no vascular or systemic effect

29
Q

Pregnancy and HA meds

A
  • never Ergots
  • acetometophen in 1st TM
  • add opiods later if needed
  • no NSAIDs in 3rd TM
30
Q

Migraine and OCPs

A
  • OCPs inc stroke risk

- migraine with aura also inc stroke risk

31
Q

NSAID DDIs

A

diuretics
b blockers
vasodilators (a2 agonists, a1 blockers)

32
Q

What should you worry about with acetometophen?

A

G6PD deficiency - b/c depleted glutathione can cause rbi oxidative damage and result in anemia

33
Q

Butalbital

A
  • Barbiturate for HAs
  • GABA sedative
  • strongly linked to overuse syndrome
  • cyp metab
34
Q

Caffeine

A
  • for HA
  • causes vasoconstriction
  • watch out for your hearrt
35
Q

Triptans

A
  • for HA
  • selective 5HT1 B (blood vessels) and 5HT1 D (nerve terminals) –> dec release of CGRP and Substance P
  • AE: worst with SC sumotriptan, chest pain, coronary vasospasm, contra heart dz/ischemic bowel disease/diabetes
  • don’t use within 24 hours: ergots, MAOIs, propanolol, CYP3A4 drugs, SSRI
36
Q

The slowest triptan

A

Frovatriptan (Frova is slowa)

37
Q

Ergots Alkaloids

A
  • for HA
  • cause vasoconstriction of small arteries
  • acts on lots of receptors so lots of DDIs: b blockers, dopa, no triptans for 24h
  • Cat X
  • contra HTN, vascular dz, sepsis, MI
38
Q

Ergotamine

A
  • ergot for HAs

- available as oral/suppository

39
Q

Dihydroergotamine

A
  • ergot for HAs

- available as SC, IV, nasal spray

40
Q

Anti-emetics

A
  • for HAs

- act on dopamine in the floor of the 4th ventricle and ACh in the vestibular system

41
Q

Metoclopromide

A
  • anti emetic for HA that is a central D2 blocker
  • prokinetic in stomach
  • inc. prolactin
42
Q

Prochlopermazine

A
  • anti emetic for HA that acts on D2 blocker
  • also cholinergic/alpha adrenergic blocker
  • AE: opp of SLUDGEBBB, glaucoma, dyskinesia, BPH
43
Q

Chlorpromazine

A
  • anti emeetic for HA that acts on D2 blocker
  • also cholinergic and alpha adrenergic blocker
  • AE: opp of SLUDGEBBB, glaucoma, dyskinesia, BPH
44
Q

Promethazine

A
  • anti emetic for HA that acts on cholinergic blockade
  • anti H1 and weak D2 blocker
  • parkinsonsm, opp of sludge BBB, BPH
45
Q

the only drug approved for pediatric migraine prophylaxis

A

propanolol

46
Q

General tx for brain tumors

A

steroids (dec. edema)
anticonvulsants
surgery!!
chemo (hard b/c of BBB)

47
Q

resistance mechanisms of brain tumors

A

dec. drug uptake
dec. drug activation
inc. drug metabolism/efflux
repair of drug induced DNA damage
binding site alteration
inc. sulhydryl scavengers
alteration of target proteins (BCL2)

48
Q

Temozolomide

A
  • Label: Astrocytoma/GBM, Off: malignant glioma/melanoma
  • prodrug DNA methylator
  • oral/IV
  • AE: myelosuppression, leukopenia, N/V, chills….CAT X
  • resistance: tumor cells that express 06-MGMT (which hematopoeitic cells have low of :( )
49
Q

Carmustine

A
  • Nitrosurea for astrocytoma, mets, malignant gioma, medullo-
  • DNA alkylator with low cross resistance
  • very lipophilic (crosses BBB)
  • AE: usuals + pulm fibrosis, endorcrine dysfunction (inc. PRL, dec. T3/T4), encephalopathy, seizures, dementia, inc. LFTs
  • also carbamoylates (inh DNA repair)
  • parenteral, implants as a wafer
50
Q

Lomustine

A
  • Nitrosurea for malignant glioma
  • DNA alkylator with low cross resistance
  • very lipophilic (crosses BBB)
  • AE: usuals + pulm fibrosis, endocrine dysfunction (inc. PRL, dec. T3/T4), encephalopathy, seizures, dementia, inc. LFTs
  • given oraly
51
Q

Convection enhanced delivery

A
  • delivering chemo and viral vectors via infusion with a positive pressure catheter
  • still in clinical trials
52
Q

Chemo fog

A
  • long term AE of chemo
  • damage to hippo, amyg, cerebellum
  • maybe from inc. TNFalpha which can cross the BBB and damage mitochondria

Neuro 2 (6 decks)

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