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Pharmacology > Neuropharm Antipschotics > Flashcards

Neuropharm Antipschotics Flashcards

1
Q

Antipsychotic drugs

A

Treat positive symptoms of schizophrenia, psychosis, Tourette’s syndrome and acute episodes of mania

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2
Q

How do antipsychotic drugs work

A

Blocking dopamine D2 receptors, increasing cAMP

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3
Q

Antipsychotics are highly ____ soluble. Where stored

A

Lipid
Fat
Removed very slowly from the body

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4
Q

2 categories of antipsychotics

A

High and low potency

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5
Q

Side effects of antipsychotics

A

Common

Endocrine and muscarinic to motor

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6
Q

___ is an endocrine side effect to dopamine antagonism

A

Galactorrhea

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7
Q

___ ___ is a stereotypic oral-facial movement, typically lip smacking, which is often seen in patients taking antipsychotic medications

A

Tardive diskinesia

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8
Q

How do antipsychotic drugs work

A

Block cholinergic receptors causing patients to display antimuscarinic effects, such as constipation and dry mouth
Block a1 receptors leading to hypotension

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9
Q

Side effect antipsychotic drug

A

Neuroleptic malignant syndrome and extrapyramidal symptom

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10
Q

Indications for antipsychotic drugs

A

Schizophrenia, psychosis, mania and tourettes

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11
Q

What antipsychotic is used to treat tourettes

A

Fluphenazine

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12
Q

What is Tourette’s

A

An inherited neuropsychiatric disease characterized by motor tics and phonic tics

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13
Q

MOA antipsychotics

A

Stored in fat and slowly removed, having a long half life

Block dopamine receptors D2

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14
Q

Where is D2

A

Mesolimbic and mesocortical areas of the CNS

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15
Q

What happens when block D2

A

Increase in intracellular concentration of cAMP

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16
Q

Side effects of antipsychotic drugs

A

Galactorrhea
Tardive dyskinesia
Anticholinergic
Alpha 1 antagonist

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17
Q

Galactorrhea and antipshycotics

A

Endocrine side effect related to dopamine antagonism

Spontaneous outflow of milk from the breasts due to hyperprolactinemia stemming from dopamine antagonism

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18
Q

Antipsychotics and tardive dyskinesia

A

Common extrapyramidal side effect seen in patients with long term treatment with antipsychotic drugs
Lip smacking

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19
Q

Anticholinergic and antipsychotic drugs

A

Antipsychotic drugs also. Block cholinergic receptors, leading to antimuscarinic effects.

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20
Q

Anticholinergic symptoms

A

Dry mouth and constipation

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21
Q

A1 antagonism and antipsychotics

A

Can lead to hypotension

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22
Q

Low potency antipsychotic drugs

A

More favorable in some patients due to low potency-which allowspatients to control daily dosing with more freedom

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23
Q

Chlorpromazine and thioridazine

A

Antipsychotics low potency

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24
Q

Indications for low potency antipsychotics

A

Schizophrenia, mania psychosis and anxiety

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25
Q

How do low potency antipsychotics work

A

Block D2 receptor in mesolimbic and mesocortical areas of CNA leading to an increase of intracellular concentration of the second messenger cAMP

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26
Q

Thioridazine side effects

A

Retinal deposits
A blockade-hypotension and anorgasmia
Anticholinergic effects

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27
Q

Chlorpromazine side effects

A

Deposited in cornea and is phototoxic . After sunlight exposure it can lead to color blindness or corneal pigmentation
A blockade effects which can lead to hypotension and anorgasmia
Anticholinergic effects
Antihistamine-which counteract the extrapyramidal symptoms experienced with antipsychotics

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28
Q

Thioridazine indications

A

Schizophrenia and psychosis
Can lead to extrapyramidal symptoms, neuroleptic malignant syndrome, impotence and autonomic side effects
Retinal deposits

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29
Q

A1 antagonist effects of low potency antipsychotic drugs

A

A1 antagonists effects lead to hypotension and impotence or anorgasmia

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30
Q

Anticholinergic effects of low potency antipsychotics

A

Dry mouth, urination difficulty, constipation, induction of glaucoma, postural hypotension, and sinus tachycardia

Less common in low potency though!

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31
Q

High potency antipsychotics are used for what

A

Schizophrenia, mania, agitation , delirium, anxiety and tourettes

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32
Q

How do high potency antipsychotics work

A

Blocking D2 receptors which by various pathways lead to increased cAMP.

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33
Q

Examples of high potency antipsychotic medications

A

Fluphenazine, trifluoperaine, heloperidol

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34
Q

Side effects of high potency antipsychotic drugs

A

Extrapyramidal symptoms and neuroleptic malignant syndrome-long period of time after take drug

Dystonia, torticollis -short term (hours to days after drug)

Parkinsonian symptoms and can display various forms of tardive dyskinesia

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35
Q

Risk of antipsychotic medications

A

Neuroleptic malignant syndrome

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36
Q

Fluphenazine

A

Treats psychosis and schizoprenia

Half like 15-30 hours

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37
Q

Trifluoperazine

A

Treat schizophrenia and anxiety

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38
Q

Haloperidol

A

Schizophrenia, acute psychosis and delirium

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39
Q

Prob with haloperidol

A

Serious side effects and is very potent.

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40
Q

Side effects of high potency antipsychotics

A

Extrapyramidal symptoms
Short term-dystonia and torticollis
Long term-tardive dyskinesia and parkinson-like symptoms

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41
Q

Extrapyramidal symptoms

A

Movement disorders related to administration of high potency antipsychotics, as well as antiemetics,and SSRI.
Dystonia, tortocollis, akathisia, and Parkinsonism seen more often with high potency antipsychotics

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42
Q

Dystonia

A

Sustained muscle contraction, which can displayed by repetitive twitching and abnormal posture.this is an acute extrapyramidal symptom

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43
Q

Parkinson like symptoms

A

After weeks of treatment with high potency antipsychotics

Patients display muscle stiffness, pill-rolling tremor and decreased movement

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44
Q

Atypical antipsychotics

A

Tranquillizing drugs used to treat psychiatric disorders

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45
Q

Indications for atypical antipsychotics

A

Positive and negative symptoms of schizophrenia, mania, tourettes, bipolar, OCD, and depression

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46
Q

MOA atypical antipsychotics

A

Varied effects on 5HT2 dopamine a and H1 receptors

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47
Q

Side effects atypical antipsychotics

A

Less anticholinergic and extrapyramidal side effects than typical counterparts but can cause seizure, prolonged QT syndrome, agranulocytosis and weight gain

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48
Q

Examples of atypical antipsychotic drugs

A

Olanzapine, clozapine, quetiapine, risperdone, aripiprazole and ziprasidone

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49
Q

Which atypical antipsychotic has been linked to prolonged AT interval

A

Ziprasidone

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50
Q

Which atypical antipsychotic causes seizures more often

A

Clozapine

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51
Q

Which atypical antipsychotic causes agranulocytosis

A

Clozapine-monitor weekly

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52
Q

Which atypical antipsychotics cause weight gain

A

Olanzapine and clozapine

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53
Q

Atypical antipsychotics have ___ extrapyramidal side effects than typical antipsychotics

A

Fewer

More favorable!

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54
Q

Atypical antipsychotics have ___ anticholinergic side effects than typical antipsychotics.

A

Fewer

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55
Q

Neuroleptic malignant syndrome

A

Severe neurological complication of typical antipsychotic and neuroleptic medications

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56
Q

Symptoms of neuroleptic malignant syndrome

A

FEVER
Fever, encephalopathy (delirium, stupor coma), unstable vital signs as a result of autonomic instability (tachycardia, hypertension, dyspnea, diaphoresis), elevated CPK enzymes, rigidity of their muscles (lead pipe rigidity with increased tone and stable resistance to all ranges of motion)

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57
Q

Reversal agent used to treat neuroleptic malignant syndrome

A

Dantrolene sodium
Or
Bromocriptine

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58
Q

Dantrolene sodium

A

Direct acting skeletal muscle relaxing agent and is very effective in treating neuroleptic malignant syndrome

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59
Q

Bromocriptine

A

Dopaminergic agonist
Bc NMS occurs as a result of dopaminergic receptor blockade , dopaminergic agonists are used to treat this condition (it restores lost dopaminergic tone in patients with neuroleptic malignant syndrome)
Use for 10 days then taper down

*can also use amantadine

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60
Q

Why get fever with NMS

A

Hypothalamic dopamine receptor blockade

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61
Q

How high are CPK enzymes in NMS

A

100 IU/L

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62
Q

Haloperidol

A

Most common used first generation antipsychotic medication

High potency antipsychotic

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63
Q

How does haloperidol (haldol) work

A

Dopamine antagonist to decrease activity of the dopaminergic tracts in the CNS and lowers the therapeutic effects of levodopa

64
Q

Indication for haloperidol (haldol)

A

Migraine, schizophrenia, psychosis, mania, delirium

65
Q

Why haloperidol treat schizophrenia

A

Schizophrenia associated with excess levels of dopamine in the brain

66
Q

Side effects of haloperidol

A

Extrapyramidal symptoms, weight gain, long QT syndrome, restlessness

67
Q

Extrapyramidal symptoms of haloperidol

A

Early-acute dystonia, Parkinsonism, akathisia

Later symptoms-tardive dyskinesia that manifests as repetitive and involuntary movements

68
Q

Why haloperidol cause weight gain

A

Affects hormonal levels and metabolic processes that affect glucose levels, lipid levels, and ultimately leads to weight gain

69
Q

Haloperidol and long QT syndrome

A

Blocks potassium channels and results in serious cardiac dysarrhythmias .

70
Q

What drugs should we avoid giving haloperidol with

A

Other QT prolonging drugs such as amiodarone or erythromycin because it may potentiating cardiac dysrhythmias

71
Q

How can we decrease chance of QT prolongation in patients on haloperidol

A

Have ECG and potassium test completed prior to treatment

72
Q

Haloperidol (haldol) and restlessness

A

Block dopaminergic transmission in the brain

73
Q

How can we fix akathisia in patients on haloperidol

A

Switch to a low potency antipsychotic or using other medications (beta blockers, benzodiazepines, anticholinergic)

74
Q

Who should we not give haloperidol to

A

Seizure patients

Antipsychotics lower the seizure threshold and therefore increase the risk of seizures,

75
Q

Haloperidol and NMS

A

Yes
Sudden hyperthermia and autonomic instability characterized by fluctuations in bp, heart rhythms, altering levels of consciousness, seizures and comas

76
Q

Chlorpromazine (thorazine)

A

Low potency antipsychotic, first generation antipsychotic (FGA) used to treat schizophrenia, manic phase of bipolar, schizoaffective disorder, and intractable hiccups

77
Q

Side effects chlorpromazine (Thorazine)

A

Sedation, orthostatic hypotension, weight gain, anticholinergic effects, QT prolongation, hiccups, and neuroendocrine effects

78
Q

Who should chlorpromazine (Thorazine) be used with caution in

A

Patients at risk for seizures bc it lowers the seizure threshold

79
Q

Chlorpromazine has alow risk of (early) extrapyramidal reaction , but there is still a risk of tardive dyskinesia (a late reaction) as there is with other first generations antipsychotics

80
Q

MOA chlorpromazine

A

Dopamine antagonist in CNS anticholinergic and alpha adrenergic blocking effects

81
Q

Indications for chlorpromazine

A

Schizophrenia , bipolar, schizoaffective

82
Q

Positive symptoms of schizophrenia such as delusions and hallucinations may respond better to treatment with ___

A

Chlorpromazine

83
Q

Negative symptoms (lack of interest, or lack of facial expression) respond well to chlorpromazine

84
Q

Initial improvement in patient condition with chlorpromazine can occur within one to two days when will significant improvement be seen

85
Q

Why is chlorpromazine no longer a first line choice for hiccups

A

Side effects

86
Q

Side effects chlorpromazine

A

Sedation, weight gain, orthostatic hypotension, anticholinergic effects, QT prolongation, neuroendocrine effects, caution in seizure patients, corneal deposits

87
Q

Weight gain and chlorpromazine

A

Weight gain, diabetes, dyslipidemia-big reason for noncompliance

88
Q

Orthostatic hypotension and chlorpromazine

A

Blood vessels are unable to vasoconstrict, a mechanism needed to increase blood pressure. Stand slowly

89
Q

Anticholinergic effects and chlorpromazine

A

Block acetylcholine , inhibiting parasympathetic nerve activity
Dry mouth, blurred vision, photophobia, urinary retention, constipation, tachycardia,

90
Q

Risk of long QT

A

Qt represents the depolarization and depolarization of the cardiac ventricles

Serious risk of cardiac problems including torsades de points which is a serious arrhythmia that can lead to fatal ventricular tachycardia

91
Q

Neuroendocrine effects of chlorpromazine

A 
Dopamine antagonist 
Increase prolactin 
Increase breast growth (gynecomastia)
Promote nippple discharge (galactorrhea)
Menstrual irregularities
92
Q

Why not give FGA to seizure patients

A

Can lower the seizure threshold in patients,

Don’t give to epileptics (increase anti seizure medication dose if have that going on )

93
Q

Corneal deposits and chlorpromazine

A

Yup and formation of cataracts

94
Q

Clozapine ((clozaril)

A

Typical second generation (SGA) antipsychotic agent
Atypical antipsychotic given to patients who are unresponsive to other atypical medications for the treatment of psychosis

95
Q

MOA clozapine

A

Antagonizing serotonergic and dopaminergic receptors

96
Q

Indication for clozapine (clozaril)

A

Schizophrenia, espicially in patients in whom other treatments have failed
Parkinson’s disease, the drug can be used to manage levodopa-induced psychosis

97
Q

Side effects clozapine

A

Agranulocytosis, weight gain and other metabolic effects , sedation feelings and myocarditis or orthostatic hypotension
Weekly lab tests should be done

98
Q

Clozapine, being an atypical antipsychotic is less likely to cause what

A

Extrapyramidal symptoms

99
Q

Schizophrenia and clozapine

A

Given if intolerant to other meds or people who have treatment resistant schizophrenia

100
Q

Clozapine and levodopa induced psychosis

A

Yup

Furthermore it can also dismiss the tremor and dyskinesia associated with Parkinson’s disease

101
Q

Weight gain clozapine

A

Impaired glucose metabolism, diabetes, dyslipidemias, metabolic syndrome

102
Q

Hypersalivation clozapine

A

Sialorrhea

-can cause aspiration, chronic cough, and hoarseness

103
Q

Myocarditis and clozapine

A

Check CRP and troponin levels

104
Q

Sedation and clozapine

A

Dopaminergic block more common side effect

105
Q

Orthostatic hypotension and clozapine

A

Anticholinergic effects which may lead to decreased catecholamine release

106
Q

Other anticholinergic symptoms

A

Acute glaucoma, dry mouth, urinary retention, constipation

107
Q

Constipation and clozapine

A

Can lead to ileus, gastric outlet obstruction and peritonitis with bowel infarction or perforation

108
Q

Consideration with clozapine

A

Weekly lab tests
WBC
ANC
CRP

109
Q

Pregabalin (lyrica

A

GABA analog that binds to the nerve terminals of calcium channels and prevent calcium influx
Inhibits the release of certain NT

110
Q

Indication for pregabalin

A

Seizures, neuropathic pain and fibromyalgia

111
Q

Side effects pregabalin (lyrica)

A

Dizziness, somnolence, weight gain, headache, and angioedema, rhabdomyolysis or drug dependence

112
Q

Pregabalin GABA analog MOA

A

Bind nerve terminal calcium channels
Inhibits calcium influx
Decreases release of glutamate, norepinephrine, and substance P.
Decrease in NT controls seizures and releif of neuropathic pain
Does not enhance GABA inhibition actions

113
Q

Indications for pregabalin

A 
Seizures
Neuropathic pain (fibromyalgia, diabetes pain)
114
Q

Side effects pregabalin

A

Headache, dizziness, somnolence, weight gain, angioedema, rhabdomyolysis, dependence

115
Q

Angioedema and pregabalin

A

Rapid swelling of the face, tongue, lips, throat, and larynx is caused by hypersensitivity reactions. Small percentage of patients have reported allergic type symptoms including angioedema

116
Q

Dependence and pregabalin

A

Can get euphoria from it
Risk for abuse and dependency in patients seeking pain relief
Classified under schedule V of the drug enforcements agency’s controlled substances act

117
Q

Risperidone (risperdal)

A

Atypical antipsychotic drug used to manage schizophrenia and manic episodes associated with bipolar disorder I

118
Q

How does risperidone (risperdal) work

A

High affinity for dopamine and serotonin receptors

119
Q

Indications for risperidone (risperdal)

A

Schizophrenia (positive and negative symptoms), bipolar mania, autism associated irritability

120
Q

Side effects risperidone

A

Extrapyramidal symptoms, or drug induced movements, and akathisia or generalized restlessness , agitation

121
Q

Administration of risperidone

A

Oral but also IM given every two weeks

122
Q

What is risperidone

A

Second generation atypical antipsychotic med which is used to treat psychiatric conditions

123
Q

Why is risperidone used over typical antipsychotics like haloperidol

A

Less likely to cause extrapyramidal motor control issues

124
Q

MOA risperidone

A

Blocking dopaminergic and serotonergic receptors in the CNS

125
Q

Indications for risperidone

A

Schizophrenia bipolar mania and autism associated irratibility

126
Q

Schizophrenia and risperidone

A

Treat both positive and negative symptoms of schizophrenia

127
Q

Why does risperidone treat both

A

Binds both dopaminergic and serotonergic receptors int he brain

128
Q

Risperidone is the only medication currently approved for irritability that is associated with _____

A

Autism

Long acting injectable form

129
Q

Side effects risperidone

A

Extrapyramidal symptoms, hyperprolactinemia, amenorrhea , prolonged QT

130
Q

Hyperprolactinemia and risperidone

A

Gynecomastia, galactorrhea

131
Q

Risperidone and amenorrhea

A

Imbalances in the hypothalamic.pituitary axis causes lack of menstruation. Some also have fertility issues

132
Q

Intramuscular long acting (depot) form risperidone

A

Long acting intramuscular form of the drug which is given every two weeks given to patient with trouble of oral routine

133
Q

Aripiprazole (abilify)

A

2nd generation atypical antipsychotic drug that affects certain NT receptors

134
Q

Indication for aripiprazole (abilify)

A

Schizophrenia, manic episodes of bipolar disorder, and depression

135
Q

Side effects aripiprazole (abilify)

A

Headache, nausea, vomiting, insomnia anxiety and dizziness

136
Q

Considerations aripiprazole

A

Include drugs low potential of weight gain and low risk of developing extrapyramidal symptoms

137
Q

MOA aripiprazole

A

2nd generation atypical antipsychotic aripiprazole is a 2nd generation atypical antipsychotic that blocks H1, 5HT2 and alpha1 receptors. Acts as a partial agonist at 5HT1 and D2 receptors. Instead of simply activating or blocking dopamine activity depending on the amount of dopamine present (DSS)

138
Q

Indications for aripiprazole

A

Schizophrenia, bipolar, depression

139
Q

Why use 2nd generation drug over 1st generation for bipolar

A

Lower risk of causing sedation, orthostatic hypotension and weight gain

140
Q

Side effects aripiprazole

A

Headache , dizziness (vertigo), nausea and vomiting, insomnia, anxiety

141
Q

Considerations

A

Low risk of extrapyramidal symptoms

Lowest risk of weight gain

142
Q

Why aripiprazole low risk

A

Since it modulates dopamine receptors instead of simply activating or blocking them, the drug has a low risk of causing extrapyramidal symptoms (EPS).

143
Q

Why do aripiprazole cause low risk of weight gain compared to other antipsychotic medications

A

Weight gain may lead to development of diabetes and dyslipidemia

144
Q

Lithium

A

Dry for mood stabilization in patients with mood disorders such as bipolar disorder , manic episodes and SIADH

145
Q

MOA lithium

A

Lithium works bu the use of seconds messengers such as IP3 (an initial-triphosphate) and DAG (diacylglycerol)

146
Q

Side effect of lithium

A

Nephrogenic diabetes insipidus (counters SIADH!)

Hypothyroidism and the development of papillary thyroid function tests

Movement disorders such as tremor ataxia
Heart block and other arrhythmias (1st degree and complete heart block)

147
Q

Contradiction to lithium

148
Q

What happens if have lithium in first trimester

A

Ebsteins anomaly in the fetus, which is described as atrialization of the right ventricle

149
Q

Indication for lithium

A

Bipolar , acute manic episodes , SIADH (drug causes excessive urination)

150
Q

MOA lithium

A

Related to second messsengers IP3 and DAG

151
Q

Ebsteins anomaly

A

Fetal cardiac abnormalities

Atrialization of the right ventricle and tricuspid regurgitation

152
Q

Tardive dyskinesia

A

Present as an adverse reaction to long term use of antipsychotic medications

153
Q

Characteristics of tardive dyskinesia

A

Unusual tongue and facial movements, difficulty swallowing and stuff neck

154
Q

What drugs cause tardive dyskinesia

A

Typical antipsychotics and sometimes atypical

155
Q

What do if patient has tardive dyskinesia

A

Stop taking anti psychotic meds immediately to prevent the symptoms from becoming irreversible

156
Q

AIMS

A

Tool to assess tardive dyskinesia focuses on examination of facial, oral, extremity, and trunk movements

157
Q

Signs and symptoms of tardive dyskinesia

A 
Bizarre facial movements 
Bizarre tongues movement 
Increased extremity movements
Stiff neck
Dysphagia (from tongue situation)

Pharmacology (52 decks)

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