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FS V, Module I > 7. Antipsychotics > Flashcards

7. Antipsychotics Flashcards

1
Q

II. PHARMACOLOGICAL ACTIONS

Anti-Adrenergic: ____ Blockade

Anticholinergic: Blockade
____ [CNS], M-2 [CV] and M-3 [smooth muscle] sites

Antihistaminic: ____ Blockade
In LP phenothiazines (e.g., chlorpromazine)

____

____ Blockade
Dopamine Theory of Schizophrenia
Current evidence: schizophrenia due to ____ of central dopaminergic systems (especially mesolimbic).

Central DA —–> ____ in CSF.

Plasma HVA (pHVA) accumulates in part from central DA.
Elevated ____ levels:
Ø found in post-traumatic stress disorder (PTSD)
• one recent study:
control subjects = 0.48 ng/mL PTSD = 1.53 ng/mL
Ø may ____ response to antipsychotic treatment:
• in schizophrenia:
non-responders = < 12 ng/mL
responders: = > 14 ng/mL

A

alpha1
M1
H1
hypothermic

dopamine
hyperactivity

pHVA
predict

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2
Q

D-2 Sites
All effective ‘typical’ antipsychotic agents have good degree of binding.
Correlation of antipsychotic action to binding at ____ sites:
n as degree of binding (in vitro & in vivo) increases, antipsychotic efficacy ____ (fewer mg needed; HP)

<60 % - ____
<70% - ____
70-80% - ____
> 80% - ____ (more side effects)

A 
D2
increase
none/minimal
some
significant
significant
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3
Q

D-1 Sites
Linked to ____ receptors (D-1 effects may occur via D-2 pathways).
‘____’ antipsychotics also block D-1 sites.

A

D2

atypical

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4
Q

• PET Scan
• For D2 receptors
• Control patients light up, but those are ____ (he calls it Haldol) does not light up
because they are blocked
o Haloperidol is a complete block of lighting up
• ____ barely lights up

A

haloprediol

cluzapine

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5
Q

III. USES
Psychosis
Symptoms likely to respond to therapy include:
____ combativeness delusions hallucinations hostility hyperactivity insomnia negativism

Not as effective in improving: ____
judgment
____

Acute: efficacy may occur within ____ days
Chronic: several weeks of drug administration may be required initial dose increased over several days)

A

anorexia
insight
memory
1-2

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6
Q 
III. USES
\_\_\_\_ mania (especially when starting lithium therapy)

Organic mental syndromes delirium
dementia

Severe ____ unresponsive to other drugs (e.g., anxiolytics)

Ballismus (continual flinging of extremities [usually arms])

Alcoholic ____

Antiemetic
PHENOTHIAZINES
____ PHENERGAN THORAZINE TORECAN TRILAFON VESPRIN

BUTYROPHENONE
____
INAPSINE (droperidol)
[injection only]

Gilles de la Tourettes Syndrome

____Disease

Intractable hiccough

Pruritus (following drugs are phenothiazines):
____ (promethazine)
TACARYL (methdilazine)
TEMARIL (trimeprazine)

A 
acute
anxiety
hallucinosis
compazine
haldol
huntingdon's
phenergan
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7
Q

IV. ADRs
Antipsychotics: generally safe medications; ____ therap. index.

ANS
Anticholinergic actions greater with ____ agents.

____ vision Mydriasis
Dry mouth Constipation Urinary retention
____

A

high
lower potency (LP)
blurred
tachycardia

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8
Q

IV. ADRs

Endocrine 
Amenorrhea 
Galactorrhea
Ø inc secretion of \_\_\_\_ (normally inhibited by DA) (contrast: bromocriptine [PARLODEL]; \_\_\_\_ used to dec lactation in women who do not want to breast-feed) 
Ø avoid in patients with \_\_\_\_

____
Ø probably also due to DA blockade

Inhibition of ____ (without interfering with erection);
Ø anticholinergic effect could also be a factor

____ gain

A

prolactin
DA agonist
breast CA

gynecomastia
ejaculation
weight

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9
Q

IV. ADRs

CV
More likely with ____ agents.
Hypotension, possibly orthostatic (related to alpha1-ABA)
Reflex ____ ECG abnormalities

Hypersensitivity
____ (dermatitis)
Skin discoloration (gray-blue pigmentation; rare)
Jaundice Photosensitivity

CNS
____, confusion, drowsiness (prob. due to anticholinergic action; greater in LP)

A

LP
tachycardia
skin rash
sedation

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10
Q

IV. ADRs (continued)
CNS (continued)
Extrapyramidal Reactions (EPRs)
Most frequent occurrence with ____ derivatives (e.g., piperazines [Stelazine]; butyrophenones [Haldol]).
Less frequent occurrence with low potency antipsychotics (e.g., CPZ) possibly because of strong ____ actions.
Minimal with ____

A

HP
anticholinergic
clozapine

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11
Q

IV. ADRs (continued)
CNS (continued)

Early onset (days to weeks)

Akathisia
Ø \_\_\_\_ motor restlessness
Ø primarily in lower extremities
Ø does not represent agitation or \_\_\_\_
Ø treatment options include: 
• reduce dose
• change to \_\_\_\_ agent
• pharmacologic intervention
-\_\_\_\_ (propranolol [INDERAL]) 
- anticholinergic (benztropine [COGENTIN]) 
- \_\_\_\_ (lorazepam [ATIVAN]) 
-alpha-adren.agonist (clonidine [CATAPRES])
Dystonia (Torticollis)
Ø muscle spasms of \_\_\_\_, tongue, neck
Ø trismus (lockjaw)
Ø treatment options include
• \_\_\_\_ [COGENTIN] (IM &amp; then p.o.)
• \_\_\_\_ [BENADRYL] (IM &amp; then p.o.)
Ø pt usually develops \_\_\_\_
A 
uncontrollable
anxiety
LP
beta-adrenergic antagonist
benzodiazepine

face
benztropine
diphenhydramine
tolerance

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12
Q

IV. ADRs

Early onset (days to weeks)

Parkinson-like syndrome (Pseudoparkinsonism)
____-related
Usually develops early (days -weeks after therapy begins)

Characteristics:
Ø \_\_\_\_ (immobility; rigidity) 
Ø bradykinesia (slow movements) 
Ø \_\_\_\_ gait
Ø tremor at rest
Usually observed in children and geriatric pts
Treatment options include: 
Ø reduce \_\_\_\_
Ø change to \_\_\_\_ agent 
Ø pharmacotherapy
• \_\_\_\_ (benztropine [COGENTIN])
• \_\_\_\_ (amantadine [SYMMETREL])
Extrapyramidal Reactions (continued)
Clinical evidence that \_\_\_\_ receptor occupancy is a major factor:
A 
dose
akinesia
shuffling
dose
LP
anticholinergic
DA agonist
D2
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13
Q

IV. ADRs

Late onset (months –> years)
Tardive Dyskinesia (TD)
Ø any type of ____ agent can induce TD
Ø occurs in 15-20% of patients on chronic therapy
Ø repetitive, involuntary movements of jaw, lips & tongue
Ø may involve ____: neck; trunk (esp. in young ♂)
Ø abnormal movements cease while patient sleeps
Ø possibly related to compensatory increases in ____ activity within CNS due to chronic blockade of DA receptors
Ø may remain even after drug is ____
Ø best preventative measures:
• ____ use of antipsychotics
• ____ therapy when TD appears
(TD may increase in intensity during ____)

A 
neuroleptic
extremities
DA
discontinued
conservative
terminate
withdrawal
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14
Q

IV. ADRs

Neuroleptic Malignant Syndrome (NMS)
Ø more likely with \_\_\_\_ antipsychotics
Ø appears to be severe form of Parkinsonism
Ø characterized by:
• \_\_\_\_
• tremor
• ANS instability (e.g, \_\_\_\_; unstable HR &amp; BP)
Ø in past: fatal in 10% of patients
Ø currently: significantly dec chance of fatality due to: 
• more careful \_\_\_\_
• rapid \_\_\_\_ of offending drug
• rapid initiation of treatment
- \_\_\_\_ (PARLODEL) 
- \_\_\_\_ (DANTRIUM)
A 
HP
catatonia
hyperthermia
monitoring
D/C
bromocriptine
dantrolene
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15
Q

IV. ADRs

Hematological 
Leukocytosis
Leukopenia 
\_\_\_\_
0.1% ( 1 per 1000) with \_\_\_\_ (THORAZINE)
 1.0% - 2.0% (10 - 20 per 1000) with \_\_\_\_ (CLOZARIL)
Priapism
Persistent abnormal erection of \_\_\_\_:
Ø painful
Ø prolonged:
• congestion &amp; swelling
• increased intracavernous pressure (≈ 80-120 mm Hg)
Ø does not result from sexual desire 
Ø due to failure of detumescence
Should be considered a urologic emergency.
A

agranulocytosis
chlorpromazine
clozapine

penis

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16
Q

IV. ADRs

Priapism (continued)
If not treated within 4 - 6 hours may lead to:
Ø ____
Ø permanent ____

Etiology:
Ø Primary (\_\_\_\_): ≈33% 
Ø Secondary causes include:
• \_\_\_\_ injury (≈12%) 
• sickle-cell anemia (≈11%)

• intracavernous injection of vasoactive substances (e.g., ____; papaverine) for
diagnosis and treatment of impotence (≈6%)
• ____ abuse or drug therapy (≈21%)
® antihypertensive meds
® antipsychotics

A 
fibrosis
impotence
idiopathic
traumatic
prostaglandin E1
alcohol
17
Q

IV. ADRs

ØAntipsychotic-induced:

• ____% of all medication-induced cases
• apparently unrelated to ____ or duration of Tx other adverse effects of neuroleptics on sexual
function are dose-related)
• suggests dysregulation of ANS (cholinergic-adrenergic imbalance)

• higher rates with:
- thioridazine (MELLARIL) [____ piperidine phenothz] - chlorpromazine (THORAZINE) [____ aliphatic phenothz]
• may be due to ____ activity

• treatment options include: 
- \_\_\_\_
- \_\_\_\_ agonists (e.g., epinephrine; phenylephrine)
- decompressive surgery
(when duration >24 hours or
failure of other procedures
A 
20
dose
LP
LP
alpha-1-ABA
ice packs
alpha-1-adrenergic
18
Q

• Just an example case of IV promethazine that went into tissue area rather than blood stream
o Causes ____

A

gangrene

19
Q

Clozapine
Newer agent which–at present–is employed only for patients who have ____ response to other antipsychotics.

Reason: higher incidence of ____.

Advantage: lower incidence of ____

Mechanism:
Weak blockade of ____ receptors but also blockade of other receptors, all of which are ____ than its D2 antagonism:

Similar to other antipsychotics: M1, M2 and M3 ____
alpha1 adrenergic ____

Different than most other antipsychotics:
____ antagonist
____ antagonist

A 
poor
agranulocytosis
EPS
D2
stronger
antagonist
antagonist
D1
5-HT2
20
Q

ADRs

Clozapine
Hematologic
Agranulocytosis: ____ must be performed once per week!

normal range: 4500-11000 WBC/mm3
mild leukopenia: 3000-3500 WBC/mm3 -----> CBC \_\_\_\_ a week
leukopenia: <3000 WBC/mm3
OR -------------> IMMEDIATE \_\_\_\_
<1500 granulocytes/mm3
agranulocytosis: <1000 WBC/mm3 OR
<500 granulocytes/mm3
* Average recovery time = \_\_\_\_ weeks

Pt who develops agranulocytosis can NOT receive ____ again.

A 
CBC
twice
D/C
2
clozapine
21
Q

Clozapine

CNS
Confusion, sedation
Seizures:
Ø higher rate than with other antipsychotics
Ø mostly ____ (tonic-clonic)
Ø ____ is effective
Psychotic relapse (prolonged) following abrupt ____

A

grand mal
carbamazepine
withdrawal

22
Q

Paliperidone (INVEGA®)

Active metabolite of ____. Same pharmacological profile ____ and IM dosage forms.

Effectiveness in the acute Tx of ____ established in three 6-week, placebo-controlled trials conducted in North America, Europe and Asia.

1665 participating adults evaluated for full array of signs
and symptoms of schizophrenia. Doses ranged from 3 mg -> 15mg daily. Effectiveness of Invega at relieving symptoms of schizophrenia > placebo treatment. Recommended dose range is 3 mg to 12 mg daily.

Commonly reported ADRs include ____, extrapyramidal Symptoms, tachycardia, orthostatic hypotension, sleepiness.

Not approved for ____-related psychosis.

INVEGAR SUSTENNATM indicated for the ____ and maintenance Tx of schizophrenia in adults.

A 
resperidone
schizophrenia
restlessness
dementia
acute
23
Q

Paliperidone (INVEGA)

DOSAGE AND ADMINISTRATION

For patients who have never taken oral paliperidone or oral or injectable risperidone, tolerability should be established with oral ____ or oral risperidone prior to initiating Tx.

Initiate with dose of 234 mg on treatment day 1 and ____ mg one week later, both administered in the deltoid muscle.

Recommended monthly maintenance dose is 117 mg; some patients may benefit from lower or higher maintenance doses within the recommended range of 39 mg to 234 mg based on individual patient tolerability and/or efficacy.

Following second dose, monthly maintenance doses can be administered in either the deltoid or gluteal muscle.

Administer by ____ injection only, using appropriate needle sizes. For deltoid injection, use 11⁄2-inch 22G needle for pts ≥ 90 kg (≥ 200 lb) or 1-inch 23G needle for pts < 90 kg (< 200 lb).

A

paliperidone
156
intramuscular

24
Q

• We have clozirel/clozapine
o Has ability to cause ____ but cannot cause Parkinson’s
• We compare this to aripiprazole – we don’t have ____
o They figured out what part of the molecule was causing the agranulocytosis and altered it so it wouldn’t cause it anymore
• Mechanistically there is some blockage of ____receptors
o There is D2 blockage, but there is a greater blockage of ____
§ “This is where the atypicals live”

A

agranulocytosis
agranulocytosis
5HT-2A
5HT-2A

25
Q 
LONG-ACTING INJECTABLE ANTIPSYCHOTICS — Other antipsychotic medications currently available in the US as LA injections are.
       Aripiprazole
       Fluphenazine
       Haloperidol
       Olanzapine

• ____ blockade&raquo_space;> D-2 Blockade; also FDA warning for rapid decline to 27% 12 hrs later

Aripipazole: ____ agonist
Quietapine: agonist at ____ ≈ sedation
Ziprasidone: blocks reuptake of ____ – useful in assoc. depression

Positive Symptoms incl: hallucinations; delusions;
reality distortions
Negative Symptoms incl: anhedonia; social withdrawal
Cognitive deficits incl: alterations of attention, working
memory & executive functions

A

5HT-2A
partial DA
H1
NE and DA

26
Q

ANTIMANIC DRUGS

Lithium
CIBALITH
ESKALITH; ESKALITH CR (Controlled Release) 
LITHANE
LITHOBID

Pharmacological Action
Lithium does not have any ____ CNS depressant effects; does not induce ____.
Has a ‘____’ effect.

Mechanism of action remains unknown:
Ø does not appear to affect post-synaptic ____ receptors
Ø may impair release of ____

A

specific
euphoria
mood-stabilizing

catecholamine
catecholamines

27
Q

Lithium

Pharmacokinetics
T1⁄2: ____ hours.
Onset of therapeutic effect: ____ days

Safe therapeutic plasma range is approximately 0.75 - 1.25 mEq/L.
Ø usually achieved at dose of 900 mg daily
Ø blood sample drawn right before ____ dose: usually 12 hrs after ____ dose (plasma levels most stable before dosing)

Low therapeutic index: ____
Ø depletion of ____ (e.g., by diuretics [esp. thiazides], loss of ____ [e.g., diarrhea) can cause greater retention of Li+ and induce ADRs
Ø in heavy ____, however, Li+ may be secreted > Na+

A

20-24
6 to 10
AM
PM

2 or 3
Na+
fluid
sweating

28
Q

Lithium

Uses
Best use: ____ of manic-depressive illness (bipolar)
Tricyclic antidepressants alone are not recommended in ____ disorder; may switch patient to mania.

Others:
Acute mania (severe cases [delusions; hallucinations] best
treated with neuroleptic) Prevention of mania
Prevention of depression (efficacy similar to TCAs) Alcoholism if 2° to primary mood disorder
Aggressive behavior (efficacy ____ of effect on mood)

A

prevention
bipolar
independent

29
Q

Lithium

ADRs
Initiation of dosage: plasma levels ____ a week.
Stable patients: determine plasma levels every two ____. Toxic reactions can occur at levels below ____ mEq/L.

Mild Intoxication (> 1.5 mEq/L) Ataxia
Abdominal pain
Diarrhea
Nausea/vomiting Small tremors \_\_\_\_ 
\_\_\_\_ (aspirin can also cause)

Mod. (1.5 ® 2.5 mEq/L) to Severe Intoxication (> 2.5 mEq/L) Confusion—> coma—> ____
Respiratory depression
Major tremors/EPS Seizures

CV
____
Hypotension

A

twice
months
1.0

sedation
tinnitus

death

arrhythmias

30
Q

Lithium

ADRs
Other
____
Weight gain

Edema

Increased urination (polyuria): ____-dependent
____ (polydipsia)
Possible kidney damage:
Ø regular monitoring of serum ____ if > 1.6 mg/dL
____ taste

A 
hypothyroidism
dose
thirst
creatinine
metallic
31
Q

Lithium

Drug Interactions
Increased Li+ concentrations by:
____ diuretics > Loop diuretics (e.g., furosemide)
____ Inhibitors
____ (e.g., indomethacin) but apparently not by ASA or
acetaminophen

A

thiazide
ACE
NSAIDs

32
Q

Anticonvulsants
All of the following anticonvulsants have been employed in treatment of ____ disorder.

It must be noted that–at present–these uses are ____.

ADRs will be given whenever anticonvulsants presented in course.

Carbamazepine (TEGRETOL)
Efficacy similar to ____ in both treatment of acute mania and prophylaxis of bipolar disorder.
Evidence that it is superior in:
Ø more ____ mania
Ø rapid ____ with more previous admissions
Ø pts ____ family history of mania
– ____ pain

Induces its own ____ + that of TCAs Ø may need to ____ dose after one week

A 
manic
unlabeled
lithium
severe
cycling
without
biotransformation
increase
nerve
33
Q

Anticonvulsants

Clonazepam (KLONOPIN)
Shown to have efficacy in ____ (first week) treatment of acute mania.
Less effective in ____ of bipolar disorder

Valproic Acid (DEPAKENE)
Depakote is the ____-release tablet.
Significant antimanic action occurs within ____ days following establishment of therapeutic serum levels (same as for ____: 8-12 ug/mL)

Gabapentin (NEURONTIN)

Lamotrigine (LAMICTAL)

A 
early
prophylaxis
delayed
1 to 4
epilepsy
34
Q

Anticonvulsants

Topiramate (TOPAMAX).
Clinical evidence for efficacy of these anticonvulsants is more impressive for ____ mania than for long-term maintenance of bipolar disorder.

Some investigations indicate particular effectiveness of lamotrigine in ____ depression.

Currently, other than for valproic acid, there is no FDA approval of anticonvulsant administration in bipolar disorder; this can limit ____ coverage for these meds.

A

acute
bipolar
insurance

FS V, Module I (7 decks)

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