CNS Drugs Flashcards

1
Q

Name the barbiturates

A

phenobarbital, pnetobarbital, thiopental, secobarbital

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2
Q

Mechanism of barbiturates

A

facilitate GABAa action by increasing duration of Cl- channel opening, thus decrease neuron firing (increases duration)

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3
Q

Contraindication of barbiturates

A

in porphyria

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4
Q

Use of barbiturates

A

sedative for anxiety, seizures, insombia, induction of anesthesia (thiopental)

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5
Q

Toxicity of barbiturates

A

respiratory and cardiovascular depression
CNS depression (EtOH exacerbated)
INDUCES cytochrome p450

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6
Q

Overdose tx of barbiturates

A

supportive (assist respiration and maintain BP)

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7
Q

Name the benzodiazepines

A

diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, clordiazepoxide, alprazolam

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8
Q

Mechanism of benzodiazepines

A

facilitate GABAa action by increasing frequency of Cl- channel opening
decreases REM sleep

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9
Q

Name the benzos with short-half lives and NO active metabolites

A

Alprazolam, triazolam, oxazepam, midazolam –> higher addictive potential

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10
Q

Use of benzodiazepines

A

anxiety, spasticity, status epilepticus, detoxification (especially alcohol withdrawal and DTs), night terrors, sleepwalking, general anesthetic (amnesia, muscle relaxation), hypnotic (insomnia)

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11
Q

Which benzos used for status epilepticus?

A

lorazepam and diazepam

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12
Q

Toxicity of benzodiazepines

A

dependence, additive CNS depression effects with alcohol

less risk of respiratory depression and coma than with barbiturates

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13
Q

Overdose tx for benzos

A

with flumazenil (competitive antagonist at GABA benzodiazepine receptor)

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14
Q

Name the non-benzo hypnotics

A

zlopidem, zaleplon, esZopiclone

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15
Q

Mechanism of the non-benzo hypnotics

A

act via the BZ1 subtype of the GABA receptor

effects reversed by flumazenil

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16
Q

Use of non-benzo hypnotics

A

insomnia

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17
Q

Toxicity of non-benzo hypnotics

A

ataxia, headaches, confusion
short duration because of rapid metabolism by liver enzymes
only cause modest day-after psychomotor depression and few amnestic effects
decreased dependence risk than benzos

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18
Q

Name the dopamine agonists

A

ergot - bromocriptine

non-ergot (preferred) - pramipexole, ropinirole

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19
Q

Parkinson disease NT levels

A

loss of dopaminergic neurons and excess cholinergic activity

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20
Q

Name drug that increases dopamine availability

A

Amantadine

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21
Q

Mechanism of amantadine

A

increase dopamine release and decrease dopamine reuptake

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22
Q

Uses for amantadine

A

PARKINSON

antiviral against influenza A and rubella

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23
Q

Toxicity of amantadine

A
ataxia
livedo reticularis (skin rash, purple and lace like)
24
Q

How do drugs increase L-DOPA availability pre-BBB?

A

agents prevent peripheral (Pre-BBB) L-dopa degradation (because dopamine cannot cross BBB) –> increased L-DOPA entering the CNS

central L-DOPA available for conversion to dopamine

25
Q

Name the drugs that increase L-DOPA availability entering brain

A

Levodopa (L-DOPA)/carbidopa

Entacapone, tolcapone

26
Q

Mechanism of carbidopa

A

blocks peripheral conversion of L-DOPA to dopamine by inhibiting DOPA decarboxylase

also reduces side effects of peripheral L-dopa conversion to dopamine (nausea, vomiting)

27
Q

Mechanism of entacapone and tolcapone

A

prevent peripheral L-dopa degradation to 3-O-methyldopa (3-OMD) by inhibiting COMT

28
Q

How do drugs prevent dopamine breakdown?

A

agents act centrally (post-BBB) to block breakdown of dopamine –> increased available dopamine

29
Q

Drugs that prevent dopamine breakdown in CNS

A

selegiline and tolcapone

30
Q

Mechanism of selegiline

A

blocks conversion of dopamine to DOPAC by selectively inhibiting MAO-B in brain

31
Q

Mechanism of tolcapone

A

blocks conversion of dopamine to 3-MT by inhibiting central COMT

32
Q

Drugs that curb excess cholinergic activity

A

benztropine

33
Q

Mechanism of benztropine

A

antimuscarinic

improves tremor and rigidity but has little effect on bradykinesia

34
Q

Mechanism of Levodopa/Carbidopa combo

A

increase level of DA in brain

carbidopa inhibits peripheral conversion of L-dopa to DA via inhibition of dopa decarboxylase

35
Q

Can dopamine cross BBB?

A

NO

36
Q

Can L-DOPA cross BBB?

A

YES

37
Q

Use of levodopa/carbidopa

A

parkinson disease

38
Q

toxicity of levodopa/carbidopa

A

arrhythmias from increased peripheral formation of catecholamines
long term can lead to dyskinesia following administration, akinesia between doses = “on/off” phenomenon

39
Q

Mechanism of selegiline

A

selectively inhibits MAO-B, which preferentially metabolizes dopamine over NE and 5-HT, thereby increasing the availability of dopamine in CNS

40
Q

Use of selegiline

A

adjunctive agents to L-dopa in treatment of Parkinsons

41
Q

Toxicity of selegiline

A

may enhance adverse effects of L-dopa

42
Q

Mechanism of memantine

A

NMDA receptor antagonist

helps prevent excitotoxicity (mediated by Ca2+)

43
Q

Toxicity of memantine

A

dizziness, confusion, hallucinations

44
Q

Use of memantine

A

Alzheimer’s disease

45
Q

Mechanism of donepezil, galantamine, rivastigmine, tacrine

A

AChE inhibitors

46
Q

Use of donepezil, galantamine, rivastigmine, tacrine

A

Alzheimer’s disease

47
Q

Toxicity of donepezil, galantamine, rivastigmine, tacrine

A

nausea, dizziness, insomnia

48
Q

Drugs used for Alzheimers

A

memantine (NMDA antagonist)

donepezil, galantamine, rivastigmine, tacrine (AChE Inhibitors)

49
Q

NTs altered in Alzheimers

A

decreased ACh

50
Q

NTs altered in Huntington’s

A

decreased GABA, ACh; increased dopamine

51
Q

Treatments for Huntington’s

A

tetrabenazine and reserpine

haloperidol

52
Q

Mechanism of tetrabenazine and reserpine

A

inhibit vesicular monoamine transporter (VMAT); limit dopamine vesicle packaging and release

53
Q

Mechanism of haloperidol

A

D2 receptor antagonist

54
Q

Mechanism of sumatriptan (and “-triptans”

A

5-HT1b/1d agonists
inhibit trigeminal nerve activation
prevent vasoactive peptide release and induce vasoconstriction

55
Q

Use of sumatriptan

A

acute migraine, cluster headache attacks

56
Q

Toxicity of sumatriptan

A
coronary vasocpasm (contraindicated in patients with CAD or prinzmetal angina)
mild paresthesia