Neuropharm Antipschotics Flashcards
(157 cards)
1
Q
Antipsychotic drugs
A
Treat positive symptoms of schizophrenia, psychosis, Tourette’s syndrome and acute episodes of mania
2
Q
How do antipsychotic drugs work
A
Blocking dopamine D2 receptors, increasing cAMP
3
Q
Antipsychotics are highly ____ soluble. Where stored
A
Lipid
Fat
Removed very slowly from the body
4
Q
2 categories of antipsychotics
A
High and low potency
5
Q
Side effects of antipsychotics
A
Common
Endocrine and muscarinic to motor
6
Q
___ is an endocrine side effect to dopamine antagonism
A
Galactorrhea
7
Q
___ ___ is a stereotypic oral-facial movement, typically lip smacking, which is often seen in patients taking antipsychotic medications
A
Tardive diskinesia
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
9
Q
Side effect antipsychotic drug
A
Neuroleptic malignant syndrome and extrapyramidal symptom
10
Q
Indications for antipsychotic drugs
A
Schizophrenia, psychosis, mania and tourettes
11
Q
What antipsychotic is used to treat tourettes
A
Fluphenazine
12
Q
What is Tourette’s
A
An inherited neuropsychiatric disease characterized by motor tics and phonic tics
13
Q
MOA antipsychotics
A
Stored in fat and slowly removed, having a long half life
Block dopamine receptors D2
14
Q
Where is D2
A
Mesolimbic and mesocortical areas of the CNS
15
Q
What happens when block D2
A
Increase in intracellular concentration of cAMP
16
Q
Side effects of antipsychotic drugs
A
Galactorrhea
Tardive dyskinesia
Anticholinergic
Alpha 1 antagonist
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
18
Q
Antipsychotics and tardive dyskinesia
A
Common extrapyramidal side effect seen in patients with long term treatment with antipsychotic drugs
Lip smacking
19
Q
Anticholinergic and antipsychotic drugs
A
Antipsychotic drugs also. Block cholinergic receptors, leading to antimuscarinic effects.
20
Q
Anticholinergic symptoms
A
Dry mouth and constipation
21
Q
A1 antagonism and antipsychotics
A
Can lead to hypotension
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
23
Q
Chlorpromazine and thioridazine
A
Antipsychotics low potency
24
Q
Indications for low potency antipsychotics
A
Schizophrenia, mania psychosis and anxiety
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How do low potency antipsychotics work
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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Thioridazine side effects
Retinal deposits
A blockade-hypotension and anorgasmia
Anticholinergic effects
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Chlorpromazine side effects
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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Thioridazine indications
Schizophrenia and psychosis
Can lead to extrapyramidal symptoms, neuroleptic malignant syndrome, impotence and autonomic side effects
Retinal deposits
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A1 antagonist effects of low potency antipsychotic drugs
A1 antagonists effects lead to hypotension and impotence or anorgasmia
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Anticholinergic effects of low potency antipsychotics
Dry mouth, urination difficulty, constipation, induction of glaucoma, postural hypotension, and sinus tachycardia
Less common in low potency though!
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High potency antipsychotics are used for what
Schizophrenia, mania, agitation , delirium, anxiety and tourettes
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How do high potency antipsychotics work
Blocking D2 receptors which by various pathways lead to increased cAMP.
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Examples of high potency antipsychotic medications
Fluphenazine, trifluoperaine, heloperidol
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Side effects of high potency antipsychotic drugs
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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Risk of antipsychotic medications
Neuroleptic malignant syndrome
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Fluphenazine
Treats psychosis and schizoprenia
| Half like 15-30 hours
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Trifluoperazine
Treat schizophrenia and anxiety
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Haloperidol
Schizophrenia, acute psychosis and delirium
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Prob with haloperidol
Serious side effects and is very potent.
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Side effects of high potency antipsychotics
Extrapyramidal symptoms
Short term-dystonia and torticollis
Long term-tardive dyskinesia and parkinson-like symptoms
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Extrapyramidal symptoms
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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Dystonia
Sustained muscle contraction, which can displayed by repetitive twitching and abnormal posture.this is an acute extrapyramidal symptom
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Parkinson like symptoms
After weeks of treatment with high potency antipsychotics
| Patients display muscle stiffness, pill-rolling tremor and decreased movement
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Atypical antipsychotics
Tranquillizing drugs used to treat psychiatric disorders
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Indications for atypical antipsychotics
Positive and negative symptoms of schizophrenia, mania, tourettes, bipolar, OCD, and depression
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MOA atypical antipsychotics
Varied effects on 5HT2 dopamine a and H1 receptors
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Side effects atypical antipsychotics
Less anticholinergic and extrapyramidal side effects than typical counterparts but can cause seizure, prolonged QT syndrome, agranulocytosis and weight gain
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Examples of atypical antipsychotic drugs
Olanzapine, clozapine, quetiapine, risperdone, aripiprazole and ziprasidone
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Which atypical antipsychotic has been linked to prolonged AT interval
Ziprasidone
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Which atypical antipsychotic causes seizures more often
Clozapine
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Which atypical antipsychotic causes agranulocytosis
Clozapine-monitor weekly
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Which atypical antipsychotics cause weight gain
Olanzapine and clozapine
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Atypical antipsychotics have ___ extrapyramidal side effects than typical antipsychotics
Fewer
More favorable!
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Atypical antipsychotics have ___ anticholinergic side effects than typical antipsychotics.
Fewer
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Neuroleptic malignant syndrome
Severe neurological complication of typical antipsychotic and neuroleptic medications
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Symptoms of neuroleptic malignant syndrome
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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Reversal agent used to treat neuroleptic malignant syndrome
Dantrolene sodium
Or
Bromocriptine
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Dantrolene sodium
Direct acting skeletal muscle relaxing agent and is very effective in treating neuroleptic malignant syndrome
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Bromocriptine
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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Why get fever with NMS
Hypothalamic dopamine receptor blockade
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How high are CPK enzymes in NMS
100 IU/L
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Haloperidol
Most common used first generation antipsychotic medication
| High potency antipsychotic
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How does haloperidol (haldol) work
Dopamine antagonist to decrease activity of the dopaminergic tracts in the CNS and lowers the therapeutic effects of levodopa
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Indication for haloperidol (haldol)
Migraine, schizophrenia, psychosis, mania, delirium
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Why haloperidol treat schizophrenia
Schizophrenia associated with excess levels of dopamine in the brain
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Side effects of haloperidol
Extrapyramidal symptoms, weight gain, long QT syndrome, restlessness
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Extrapyramidal symptoms of haloperidol
Early-acute dystonia, Parkinsonism, akathisia
| Later symptoms-tardive dyskinesia that manifests as repetitive and involuntary movements
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Why haloperidol cause weight gain
Affects hormonal levels and metabolic processes that affect glucose levels, lipid levels, and ultimately leads to weight gain
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Haloperidol and long QT syndrome
Blocks potassium channels and results in serious cardiac dysarrhythmias .
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What drugs should we avoid giving haloperidol with
Other QT prolonging drugs such as amiodarone or erythromycin because it may potentiating cardiac dysrhythmias
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How can we decrease chance of QT prolongation in patients on haloperidol
Have ECG and potassium test completed prior to treatment
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Haloperidol (haldol) and restlessness
Block dopaminergic transmission in the brain
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How can we fix akathisia in patients on haloperidol
Switch to a low potency antipsychotic or using other medications (beta blockers, benzodiazepines, anticholinergic)
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Who should we not give haloperidol to
Seizure patients
| Antipsychotics lower the seizure threshold and therefore increase the risk of seizures,
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Haloperidol and NMS
Yes
Sudden hyperthermia and autonomic instability characterized by fluctuations in bp, heart rhythms, altering levels of consciousness, seizures and comas
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Chlorpromazine (thorazine)
Low potency antipsychotic, first generation antipsychotic (FGA) used to treat schizophrenia, manic phase of bipolar, schizoaffective disorder, and intractable hiccups
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Side effects chlorpromazine (Thorazine)
Sedation, orthostatic hypotension, weight gain, anticholinergic effects, QT prolongation, hiccups, and neuroendocrine effects
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Who should chlorpromazine (Thorazine) be used with caution in
Patients at risk for seizures bc it lowers the seizure threshold
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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
Ok
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MOA chlorpromazine
Dopamine antagonist in CNS anticholinergic and alpha adrenergic blocking effects
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Indications for chlorpromazine
Schizophrenia , bipolar, schizoaffective
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Positive symptoms of schizophrenia such as delusions and hallucinations may respond better to treatment with ___
Chlorpromazine
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Negative symptoms (lack of interest, or lack of facial expression) respond well to chlorpromazine
Nope
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Initial improvement in patient condition with chlorpromazine can occur within one to two days when will significant improvement be seen
Weeks
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Why is chlorpromazine no longer a first line choice for hiccups
Side effects
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Side effects chlorpromazine
Sedation, weight gain, orthostatic hypotension, anticholinergic effects, QT prolongation, neuroendocrine effects, caution in seizure patients, corneal deposits
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Weight gain and chlorpromazine
Weight gain, diabetes, dyslipidemia-big reason for noncompliance
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Orthostatic hypotension and chlorpromazine
Blood vessels are unable to vasoconstrict, a mechanism needed to increase blood pressure. Stand slowly
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Anticholinergic effects and chlorpromazine
Block acetylcholine , inhibiting parasympathetic nerve activity
Dry mouth, blurred vision, photophobia, urinary retention, constipation, tachycardia,
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Risk of long QT
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
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Neuroendocrine effects of chlorpromazine
```
Dopamine antagonist
Increase prolactin
Increase breast growth (gynecomastia)
Promote nippple discharge (galactorrhea)
Menstrual irregularities
```
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Why not give FGA to seizure patients
Can lower the seizure threshold in patients,
| Don’t give to epileptics (increase anti seizure medication dose if have that going on )
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Corneal deposits and chlorpromazine
Yup and formation of cataracts
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Clozapine ((clozaril)
Typical second generation (SGA) antipsychotic agent
Atypical antipsychotic given to patients who are unresponsive to other atypical medications for the treatment of psychosis
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MOA clozapine
Antagonizing serotonergic and dopaminergic receptors
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Indication for clozapine (clozaril)
Schizophrenia, espicially in patients in whom other treatments have failed
Parkinson’s disease, the drug can be used to manage levodopa-induced psychosis
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Side effects clozapine
Agranulocytosis, weight gain and other metabolic effects , sedation feelings and myocarditis or orthostatic hypotension
Weekly lab tests should be done
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Clozapine, being an atypical antipsychotic is less likely to cause what
Extrapyramidal symptoms
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Schizophrenia and clozapine
Given if intolerant to other meds or people who have treatment resistant schizophrenia
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Clozapine and levodopa induced psychosis
Yup
| Furthermore it can also dismiss the tremor and dyskinesia associated with Parkinson’s disease
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Weight gain clozapine
Impaired glucose metabolism, diabetes, dyslipidemias, metabolic syndrome
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Hypersalivation clozapine
Sialorrhea
| -can cause aspiration, chronic cough, and hoarseness
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Myocarditis and clozapine
Check CRP and troponin levels
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Sedation and clozapine
Dopaminergic block more common side effect
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Orthostatic hypotension and clozapine
Anticholinergic effects which may lead to decreased catecholamine release
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Other anticholinergic symptoms
Acute glaucoma, dry mouth, urinary retention, constipation
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Constipation and clozapine
Can lead to ileus, gastric outlet obstruction and peritonitis with bowel infarction or perforation
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Consideration with clozapine
Weekly lab tests
WBC
ANC
CRP
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Pregabalin (lyrica
GABA analog that binds to the nerve terminals of calcium channels and prevent calcium influx
Inhibits the release of certain NT
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Indication for pregabalin
Seizures, neuropathic pain and fibromyalgia
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Side effects pregabalin (lyrica)
Dizziness, somnolence, weight gain, headache, and angioedema, rhabdomyolysis or drug dependence
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Pregabalin GABA analog MOA
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
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Indications for pregabalin
```
Seizures
Neuropathic pain (fibromyalgia, diabetes pain)
```
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Side effects pregabalin
Headache, dizziness, somnolence, weight gain, angioedema, rhabdomyolysis, dependence
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Angioedema and pregabalin
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
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Dependence and pregabalin
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
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Risperidone (risperdal)
Atypical antipsychotic drug used to manage schizophrenia and manic episodes associated with bipolar disorder I
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How does risperidone (risperdal) work
High affinity for dopamine and serotonin receptors
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Indications for risperidone (risperdal)
Schizophrenia (positive and negative symptoms), bipolar mania, autism associated irritability
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Side effects risperidone
Extrapyramidal symptoms, or drug induced movements, and akathisia or generalized restlessness , agitation
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Administration of risperidone
Oral but also IM given every two weeks
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What is risperidone
Second generation atypical antipsychotic med which is used to treat psychiatric conditions
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Why is risperidone used over typical antipsychotics like haloperidol
Less likely to cause extrapyramidal motor control issues
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MOA risperidone
Blocking dopaminergic and serotonergic receptors in the CNS
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Indications for risperidone
Schizophrenia bipolar mania and autism associated irratibility
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Schizophrenia and risperidone
Treat both positive and negative symptoms of schizophrenia
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Why does risperidone treat both
Binds both dopaminergic and serotonergic receptors int he brain
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Risperidone is the only medication currently approved for irritability that is associated with _____
Autism
Long acting injectable form
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Side effects risperidone
Extrapyramidal symptoms, hyperprolactinemia, amenorrhea , prolonged QT
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Hyperprolactinemia and risperidone
Gynecomastia, galactorrhea
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Risperidone and amenorrhea
Imbalances in the hypothalamic.pituitary axis causes lack of menstruation. Some also have fertility issues
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Intramuscular long acting (depot) form risperidone
Long acting intramuscular form of the drug which is given every two weeks given to patient with trouble of oral routine
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Aripiprazole (abilify)
2nd generation atypical antipsychotic drug that affects certain NT receptors
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Indication for aripiprazole (abilify)
Schizophrenia, manic episodes of bipolar disorder, and depression
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Side effects aripiprazole (abilify)
Headache, nausea, vomiting, insomnia anxiety and dizziness
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Considerations aripiprazole
Include drugs low potential of weight gain and low risk of developing extrapyramidal symptoms
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MOA aripiprazole
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)
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Indications for aripiprazole
Schizophrenia, bipolar, depression
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Why use 2nd generation drug over 1st generation for bipolar
Lower risk of causing sedation, orthostatic hypotension and weight gain
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Side effects aripiprazole
Headache , dizziness (vertigo), nausea and vomiting, insomnia, anxiety
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Considerations
Low risk of extrapyramidal symptoms
| Lowest risk of weight gain
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Why aripiprazole low risk
Since it modulates dopamine receptors instead of simply activating or blocking them, the drug has a low risk of causing extrapyramidal symptoms (EPS).
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Why do aripiprazole cause low risk of weight gain compared to other antipsychotic medications
Weight gain may lead to development of diabetes and dyslipidemia
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Lithium
Dry for mood stabilization in patients with mood disorders such as bipolar disorder , manic episodes and SIADH
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MOA lithium
Lithium works bu the use of seconds messengers such as IP3 (an initial-triphosphate) and DAG (diacylglycerol)
146
Side effect of lithium
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)
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Contradiction to lithium
Pregnancy
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What happens if have lithium in first trimester
Ebsteins anomaly in the fetus, which is described as atrialization of the right ventricle
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Indication for lithium
Bipolar , acute manic episodes , SIADH (drug causes excessive urination)
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MOA lithium
Related to second messsengers IP3 and DAG
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Ebsteins anomaly
Fetal cardiac abnormalities
| Atrialization of the right ventricle and tricuspid regurgitation
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Tardive dyskinesia
Present as an adverse reaction to long term use of antipsychotic medications
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Characteristics of tardive dyskinesia
Unusual tongue and facial movements, difficulty swallowing and stuff neck
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What drugs cause tardive dyskinesia
Typical antipsychotics and sometimes atypical
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What do if patient has tardive dyskinesia
Stop taking anti psychotic meds immediately to prevent the symptoms from becoming irreversible
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AIMS
Tool to assess tardive dyskinesia focuses on examination of facial, oral, extremity, and trunk movements
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Signs and symptoms of tardive dyskinesia
```
Bizarre facial movements
Bizarre tongues movement
Increased extremity movements
Stiff neck
Dysphagia (from tongue situation)
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