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Therapeutics > Exam 4 lecture 3 > Flashcards

Exam 4 lecture 3 Flashcards

1
Q

What are warnings for all antipsychotics

A

-Boxed warning- increases risk of death in elderly patients treated with antipsychotics for dementia with related behaviors.

-metabolic adverse effects

-EPS

-Risk of somnolence, postural hypotension and motor/sensory instability increases risk for falls and fractures.

  • Fall risk assessment should be performed
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2
Q

What are some long acting injections?

A

Haloperidol deconate
Risperdal Consta
Perseris
Rykindo (risperidone)
Uzedy (risperidone)
Invega Sustenna (paliperidone)
Invega Trinza
Invega Hafyera
Zyprex relprev (olanzapine)
Abilify maintena (aripiprazole)
Abilify Asimtufil
Aristada
Aristada initio

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3
Q

What are things to know Risperdal Consta

A

Must supplement with oral risperidone (or another oral antipsychotic) for the first few weeks of treatment. (until 3rd injection) (week 4)

1st atypical long acting injection

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4
Q

Things to know about perseris (dose and enzyme substrate)

A

Abdominal SQ injection- 90 m and 120 mg

3A4 inducers- use 120 mg dose or may need oral supplementation

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5
Q

Things to know about rykindo (dosing)

A

Every 2 week IM injection
Oral dose overlap is shorter than risperidal consta (7 days vs 21 days)

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6
Q

Things to know about Uzedy (risperidone) (dosing

A

Abdominal or upper arm SQ injection
Given once monthly or every 2 months

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7
Q

Things to know about Invega susstena (dosing, how to give drug, dose adjustments)

A

Loading dose then booster, then every 4 weeks (starting every 5 weeks after loading injection)

Initial deltoid booster must be given in deltoid to improve absorption consistency

If loading strategy followed, no need for oral overlap antipsychotic treatment.

May require dose adjustment in moderate to severe renal impairement

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8
Q

Things to know about Invega trinza

A

May be initiated for patient who has been on a stable monthly IM injection of INVEGA sustenna.

atleast 4 stable invega susstena doses

recommended to be on deltoid, gluteal administration results in lower climax

not recommended if CRCL<50

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9
Q

Things to know about Invega hafyera

A

Must be initiated after stable invega sustenna for 4 months or stable invega trinza for 3 months

gluteal injection only

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10
Q

Things to know about zyprexa relprev

A

causes post dose delirium sedation syndrome

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11
Q

Things to know about Abilify maintena

A

Deltoid or gluteal injection
Must overlap with oral aripiprazole (or another oral antipsychotic) for atleast 14 days after injection.

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12
Q

Abilify maintena dose adjustments for P450 interactions

A

If taking 2D6 or 3A4 inhibitors for 3A4 inducers for more than 14 days as concomitant therapy.

patients taking 400 mg of abilify maintena
-strong CYP 2D6 OR CYP 3A4 inhibitors adjust dose to 300 mg

CYP2D6 AND 3A4 inhibitors adjust dose to 300 mg

Patients taking 300 mg of abilify maintena
-strong CYP 2D6 OR 3A4 inhibitors- adjust to 200 mg
- sCYP 2D6 AND CYP3A4 inhibitors- adjust dose to 160 mg

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13
Q

Things to know about abilify asimtufii (aripiprazole)

A

Every 2 month dosing
Gluteal injection only

continue Oral aripiprazole for 2 weeks after 1st injection

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14
Q

Things to know about Aristada (aripiprazole lauroxil)

A

Overlap with oral aripiprazole for 3 weeks after 1st injection.

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15
Q

Things to know about aristada initio

A

Developed to avoid need for 21 day oral overlap of antipsychotic

Avoid in patients who are 2D6 poor metabolizers or with strong 3A4 or 2D6

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16
Q

Immediate release antipsychotic injections/psychiatric emergencies

A

Haloperidol (most common)
chlorpromazine
fluphenazine
Olanzapine IR IM
Loxapine for inhalation

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17
Q

What are notable things to know about olanzapine IR IM

A

Can not be given at the same time as benzodiazepine IR injection- boxed warning for respiratory depression.

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18
Q

clinical treatment strategies for EPS

A

Acute dystonia- IM anticholinergic NOW dose
- benztropine 2 mg, diphenhydramine 50 mg)

Drug induced parkinsons- Oral anticholinergics (benztropine, trihexylphenidate, dihenhydramine)

Akathisia- BB (propanolol preferred 1st line)
Benztropine- usually lorazepam

Tardive dyskinesia- VMAT inhibitors

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19
Q

What are the VMAT inhibitors. Notable things about them

A

Tetrabenzine
Valbenzine- 2D6/3A4 substrate. side effects QTc prolongation
Deutetrabenazine- 2D6 substrate. Side effects QTc prolongation

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20
Q

What is neuroleptic malignant syndrome (NMS)? Symptoms?
Side effects? Treatment?

A

Life threatening-IS a medical emergency.

symptoms- Hyperpyrexia, tachycardia, labile blood pressure

muscle rigidity- Elevated (significantly) CK, myoglobin

Treatment is supportive

Future antipsychotic use is NOT contraindicated

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21
Q

Metabolic adverse effects of antipsychotics. Rank atypical antipsychotic risk for atypical antipsychotic risk.

A

Clozapine and olanzapine have the highest risk

Ziprasidone, lurasidone and aripiprazole have the least risk.

22
Q

Monitoring parameters for metabolic advrese effects of antipsychotic

A

Weight every 4 weeks
BP, fasting lipids, FPG/A1C, baseline, 12 weeks and yearly

23
Q

Define Sedative, anxiolytic, hypnotic, narcotic

A

Sedative- Calms anxiety, reduces excitement and activity. Does not produce drowsiness or impair performance

anxiolytic- antianxiety relieves anxiety without sleep or sedation (not all anxiolytics are sedatives)

Hypnotic- Induces sleep, implies restful, refreshing sleep not hypnotized

Narcotic- Actually means “sleep producing, now refers to opioids or illegal drugs

24
Q

What is the reticular formation? Where is it found?

A

It is an intricate system composed of loosely clustered neurons in what is otherwise white matter.

The reticular formation extends through the central core of the medulla oblongata, pons and midbrain.

25
Q

What are the stages of sleep

A

Wakefulness
NREM
REM

26
Q

stages of NREM?

A

Stage 1 (dozing)
stage 2 (unequivocal sleep)
stage 3 (voltage increase, frequency decrease)
stage 4- delta waves

27
Q

What are factors that regulate sleep

A

Age
Sleep history
Drug ingestion
Circadian rhythms

28
Q

what are some biological regulators of sleep

A

-Neurotransmitters (almost all) (main target for current medications is GABA)

-Neuromodulators

29
Q

What are GABAergic neurotransmitters

A

GABAa receptors
GABAb receptors
GABA transporters (GAT-1)
GABA-T (transaminase)

30
Q

GABA receptor is a ______ channel complex

A

Chloride

31
Q

where to BZDs bind to

A

Alosteric sites (alpha 1 and gamma 2)

32
Q

How do BZds affect GABA action

A

Facilitate GABA action., increase frequency.

33
Q

What are some ligands acting at the BZD receptor

A

Benzodiazepines- Increase frequency

non BZDs (Z hypnotics)- BZ receptors of A1

BZD antagonist- Flumazenil

34
Q

How do BZDs modulate GABA receptor

A

increase frequency of channel opening

35
Q

How do barbiturates affect modulation of GABA receptors

A

Increase duration of channel opening and direct effects on GABA (high doses)

36
Q

SAR of benzodiazepines

A

1 position alkylation is the source of active metabolites.

Annealating the 1-2 bond with an electron rich ring yields high affinity and decreased half life

37
Q

which bzd has long half life? BZDs that have a long half life have what in common?

A

diazepam.

slow elimination rates- all have active metabolites.

38
Q

What does diazepam treat

A

Diazepam- prototypical BZD used as anxiolytic, for alcohol withdrawal and for treatment of convulsive disorders (seizures), Accumulation of metabolites.

39
Q

What BZD drugs have intermediate elimination rates?

A

clonazepam (anticonvulsant)
- tolerance may develop with prolonged use, used as an anticonvulsant.

40
Q

Which BZD drugs are rapid elimination rates

A

Midazolam
-rapid anesthesia

41
Q

why are barbiturates more dangerous than BZDs

A

Barbiturates may cause coma. BZDs have an asymptote at anesthesia (ceiling effect)

BZDs increase the frequency of GABA receptors

42
Q

What are some pharmacologic properties of BZDs

A

Decrease REM
Decrease stage 3 and 4
Anticonvulsant activity

43
Q

toxicology of BZD (side effects, precautions and interactions, drug dependence and abuse)

A

side effects- dose dependent (sedation, confusion, weakness)

precautions and interactions- Alcohol, pregnancy and breast feeding.

Drug dependence and abuse- abuse potential low vs barbiturates

44
Q

Benzodiazepine antagonist drug? Use?

A

Flumazenil

Treat BZD overdose

45
Q

What are the non benzodiazepine drugs? What site do they act on?

A

Z hypnotics- act at BZD binding site (BZ1 receptor)

Zolpiden (ambien)- short term treatment of insomnia

Zaleplon (sonata)- short term treatment of insomnia (7=10 days)

Eszopiclone- Long term use

46
Q

Z hypnotics common features

A

Metabolism- CYP3A4

Overdose treatment- Flumazenil

Side effects- cause less negative effects on sleep patterns than BZD

Sleep driving, sleep cooking, sleep eating (warn your residents) (know for exam)

47
Q

What other illicit uses do BZDs and non BZDs have

A

BZDs (clonazepam, flunitrazepam)- roofies

Non BZDs (Zolpidem)- Sexual assault dangers

48
Q

Barbiturates classifications

A

Long acting- Phenobarbital

Short to intermediate acting- Pentobarbital

49
Q

What do barbiturates cause

A

Respiratory depression- death

50
Q

KNOW FOR EXAM. Compare BBT, BZD and Z hypnotics

A

BBT- bind all GABA a 1-5, Increase the duration of channel opening and DIRECT EFFECTS on GABA channel

BZDs- bind to all GABA a-1-5, increase the FREQUENCY of GABA channel

Z hypnotics- bind to GABA BZ receptors of a1, increase frequency of GABA channel opening

51
Q

What is the use and limitation of flumazenil

A

Treats overdoses, but not for BBT

Therapeutics (38 decks)

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