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Neurological System > 2-Pharmacology > Flashcards

2-Pharmacology Flashcards

Movement Disorders, Sedative Hypnotics

1
Q

Compare the site of action for barbituates and benzodiazepines.

A

Barbituates: bind to GABA receptors and act as AGONISTS

Benzodiazepines: bind alternate site on GABA receptor and modulate activity of GABA (no effect unless free GABA present)

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2
Q

What drug is commonly used for pre-op sedation?

Mech. and Adverse effects?

A

Phenobarbital: GABA agonist, can induce hyperactivity in children and infants

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3
Q

Describe secobarbital.

A

GABA agonist that was used to treat short-term insomnia and acute psychosis.

No longer used in US due to toxicity and high level of sedation produced.

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4
Q

How do benzodiazepines modulate the GABA effect on receptors from alternate site?

A

Increase Cl- conductance

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5
Q

What is a strong advantage of benzodiazepines?

A

No potential for overdose due to them acting indirectly on the GABA receptors.

Body still modulates its own level of inhibition.

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6
Q

Are benzodiazepines addictive?

A

yes they can cause a physical dependence when used for prolonged periods of time (>2-3wks)

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7
Q

What do all the benzodiazepine drugs end with?

A

-pam

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8
Q

Describe the use of alprazolam.
Advantage?
Contraindications?

A 
Panic disorders (xanax)
Short half-life
Can exacerbate resp. failure, so avoid in lung comprimised.
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9
Q

What receptor does zolpidem and zaleplon act on?

A

Zolpidem (ambien): act on GABAa type 1. Rapid onset. Before bed to help with insomnia

Zaleplon (sonanta): GABA type 1. May reduce anxiety.

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10
Q

Describe the mech. of propofol. What is its use?

A

Stimulates GABA release

Ambulatory surgery anesthesia care

Metabolized rapidly (good for surgical monitoring.

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11
Q

Contraindications of propofol?

A

Can cause acidosis in children.

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12
Q

If a patient experiences pain at the IV site resulting from Propofol use for anesthesia, what can be used the next time?

A

Fospropofol

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13
Q

What anesthsia is best for use in the elderly? Why?

A

Etomidate: good for pts. with low cardiovascular output (doesnt lower BP)

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14
Q

What are some points of consideration when administering Etomidate for anesthesia?

A

Used in elderly and cardio comprimised.

Not an analgesic so concurrent opiods also needed.

Slower recovery time post-op (slower metabolism)

Can cause pain at IV site, myoclonus in limb. post-op nausea/vomiting (possibly administer anti-emetic?)

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15
Q

What is the mechanism of action of buspirone? Use? Advantages? Adverse?

A

Acts on 5HT1A to inhibit release of 5HT.

Used for LONG-TERM anxiety. (no potential for abuse or withdrawl)

Has less motor depression due to MOA
Can be used with other CNS drugs and even ALCOHOL

Not Benzodiazepine tolerant so must taper patient off these before administration.

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16
Q

Describe the MOA and use of Ramelteon.

A

Melatonin receptor agonist

Sleep aide with no rebound insomnia or withdrawl symptoms.

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17
Q

Describe the guidlines for the use of benzodiazepines?

A

Used for severe insomnia (interferes with daily life).

Only rx for SHORT period of use.

If pt doesnt respond to first drug. Do NOT prescribe any of the others.

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18
Q

What is the DOC for treating panic disorder?

A

Alprazolam (xanax)

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19
Q

What is the clinical indication for meprobamate?

A

short-term anxiety, sedative-hypnotic

Generally replaced by BZs due to less side-effects.

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20
Q

What drug is generally the DOC for generalized anxiety disorder and alcohol withdrawl?

A

Lorazepam

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21
Q

What is the drug combination commonly used for monitored anesthesia care?

A

Midazolam - pre-op anxiolytic, little bit of anesthesia, and anterograde amnesia.

Propofol - anesthesia

Opoids or Ketamine - analgesics/sedation

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22
Q

What drug combo is used for Conscious sedation?

A

IV diazepam/midazolam and Propofol

Patient remains verbally responsive

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23
Q

What drug combo is used for deep sedation?

A

IV thiopental, midazolam, propofol.

24
Q

Why is buspirone indicated well for anxiety disorders, but not for panic disorders?

A

Slow onset of action (2-4 weeks)

Great for anxiety due to its low level of dependence and abuse/withdrawl symptoms.

25
Q

FDA recommended what in 2007, with regard to hypnotic agents?

A

Required strengthened product labeling to include strong language about potential risks (driving/operating)

26
Q

What is the DOC for nocturnally predominant pain?

A

Clonazapam.

27
Q

What is the clinical indication of sinemet? What two drugs is it composed of?

A

Parkinson syndrome DOC

L-Dopa (Levodopa) - precursor to dopamine, crosses BBB and metab. into dopamine.

Carbidopa - inhibits Levodopa met. into dopamine in the periphery only (doesn’t cross BBB) to improve selectivity of L-dopa.

28
Q

What is the “on-off” phenomenon? What is the treatment for it?

A

Seen in treatment of parkinson syndrome with L-Dopa

Off periods = akinesia (no movement

On periods = dyskinesia (too much movement)

Treat off periods with apomorphine.

29
Q

What class of drugs is used to improve/prolong the antiparkinsonian effect of L-dopa? Why is this beneficial?

A

MAO-B inhibitors.

Great because it allows for lower doses of L-Dopa, thus decreasing onset of decreased effectiveness and adverse phenomena.

30
Q

What are the MAO-B inhibitor drugs commonly used?

A

Selegine (conjunctive treatment)

Rasagiline: more potent , DOC for use to prevent MPTP- induced parkinson symptoms.
- Used by itself in early symptomatic treatment.

31
Q

What MAO-B inhibitor is used as monotherapy for early symptoms of parkinson?

A

Rasagiline

32
Q

What are the contraindications of MAOB inhibitors?

A

Meperidine

Anti-depressants

33
Q

What is the use for COMT inhibitors?

A

Useful in patients experiencing fluctuations (on-off, prolonged on, etc).

They decrease the initial metabolism of L-Dopa in the periphery prior to it crossing the BBB.

34
Q

What is the basis for inhibiting COMT in the periphery using Entacapone?

A

COMT metabolizes L-Dopa in the periphery preventing it from crossing the BBB via competion by 3-O-methyldopa byproduct that is transported the same way (decreasing effectiveness/duration of action) due to less reaching the CNS.

Inhibition can help with this
Entacapone is DOC due to less side effects.

35
Q

What is the reason Tolcapone requires signed consent prior to administration?

A

increased incidence of liver toxicity

36
Q

What is the use of Stalevo in Parkinson patients?

A

Combo drug (L-dopa, carbidopa, entacapone)

Meets all goals of treatment and simplifies drug regimen.

37
Q

Describe the advantages and use of Direct Dopamine agonists?

A

Bromocriptine, Pramipexole, Ropinerole.

No metabolic conversion needed, no toxic metabolites, no competition to cross BBB, Less side effects.

38
Q

What is the older form of DAs used to treat parkinson?

A

Bromocriptine (Ergot derived)

39
Q

What are the New DAs used to treat parkinson?

A

Ropinirole (D2 agonist)

Pramipexole (D3 agonist)

40
Q

Give the clinical uses of pramipexole? MOA?

A

Mild parkinsons: monotherapy

Advanced parkinsons: adjunctive therapy (decrease fluctuation symptoms)

41
Q

What symptoms of parkinson can be improved using Ach blockers?

A

Tremor and Rigidity

No effect on bradykinesia

42
Q

What are the Ach blockers used in PD treatment?

A

Benztropine

43
Q

What drug is DOC for postural tremor symptomatic treatment?

A

Propanolol (non-selective B blocker)

Metpropolol won’t work because it is B1 selective and the tremors are B2 in origin.

44
Q

4 drugs are used to treat essential tremors?

A

Propanolol
Primidone, topiramate - antiepileptics
Alprazolam: BZdiazepine

45
Q

3 drugs are used to treat Huntington disease?

A

Perphenazine, Haloperidol - Dopa agonists

Reserpine - prevent dopamine storage in neurons.

Tetrabenzine- dopamine metabolism inhibitor (VMAT)

46
Q

Which drug has less side effects (reserpine vs tetrabenzine)?

A

Tetrabenzine preferred

47
Q

What drug is approved for ALS?

A

Riluzole - only drug specific to ALS

Inhibits glutamate signalling (prevent excitotoxicity)

48
Q

DOC in treatment of Restless leg syndrome.

A

Ropinerol - Dopamine agonist

49
Q

Describe best treatment for Wilson Disease?

A

Remove copper (chelation, reduce GI absorption)

Chelators: penicillamine, tirentine

Absorption: potassium disulfide, zinc sulfate

50
Q

What can be caused if L-Dopa and MAOAi are given at the same time?

A

Hypertensive crisis

51
Q

What populations should be prescribed L-Dopa with caution?

A

Melanoma patients - can contribute to malignancy

Angle-closure glaucoma - increases IOP

52
Q

Describe the 5 classes of drugs that can be used in treatment of Tics.

A
  1. Dopamine agonists - Haloperidol, Pimizole
  2. Antiepileptics: carbemazepine
  3. Antipsychotics: fluphenazine
  4. Benzodiazepines: Clonazepam
  5. Adrenergic agonist: Clonidine.
53
Q

How would you start to treat an acute dystonic attack?

A

Benztropine

54
Q

How would you begin to treat a Long-Term Dyskinesia?

A

Haloperidol or fluphenazine

55
Q

Specific indication for apomorphine?

A

Potent dopamine agonist used to treat “off” portion of on-off phenomenon seen in Sinemet parkinson treatment.

Neurological System (10 decks)

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