Central Nervous System Pharmacology Flashcards
Which antidepressant is least likely to cause xerostomia?
a. Bupropion (Know)
b. Sertraline
c. Chlorpromazine
d. Amitriptyline
e. Trazodone
b. Sertraline
Sertraline, as with other SSRIs, produces a lower incidence of xerostomia than other classes of antidepressants, probably because their anticholinergic activity is significantly weaker. Bupropion, trazodone, and especially amitriptyline have a greater anticholinergic action and incidence of xerostomia. Chlorpromazine is not an antidepressant
Which antidepressant is associated with priapism?
A) Bupropion
B) Tricyclic antidepressants
C) Trazodone
D) Nefazodone
E) Mirtazapine
C) Trazodone
Trazodone is highly sedative and has been associated with priapism requiring surgical intervention and leaving some patients permanently impotent. Bupropion is associated with seizures. Tricyclic antidepressants are associated with anticholinergic effects and cardiac toxicity. Nefazodone carries a black box warning regarding the potential to cause life-threatening liver failure. Mirtazapine causes somnolence, weight gain, constipation, and dry mouth.
DIF: Recall REF: Antidepressant Agents (Other Antidepressants [Trazodone]) | p. 182 OBJ: 5 TOP: NBDHE, 6.0. Pharmacology
All antidepressants will carry a black box warning about the potential for patient suicide.ANS: T
True
- There is an increased risk of suicidality in children, adolescents, and young adults, which are included in the package inserts. All depressed children, adolescents, and adults should be monitored for suicidal ideation and behavior regardless of antidepressant or nontherapy.*
- DIF: Recall REF: Antidepressant Agents (Suicide and Antidepressants) | p. 182 OBJ: 4 TOP: NBDHE, 6.0. Pharmacology*
Which of the following are anticholinergic effects that may be associated with tricyclic antidepressants?
A) Xerostomia
B) Bradycardia
C) Urination
D) Both A and B
E) Both B and C
A) Xerostomia
Tricyclic antidepressants possess distinct anticholinergic effects resulting in xerostomia, blurred vision, tachycardia, constipation, and urinary retention. Some tolerance can develop with continued use. The extension of cholinergic effects are salivation, lacrimation, urination, and defecation. Anticholinergic effects would be the opposite.
DIF: Comprehension
REF: Antidepressant Agents (Tricyclic Antidepressants [Adverse Reactions]) | p. 181 OBJ: 4 TOP: NBDHE, 6.0. Pharmacology
Tardive dyskinesia is characterized by
A) increased compulsive motor activity.
B) resting tremor and rigidity.
C) akinesia.
D) involuntary, repetitive body movements involving the tongue, lips, face, and jaw.
D) involuntary, repetitive body movements involving the tongue, lips, face, and jaw.
All first-generation antipsychotics produce extrapyramidal effects. Tardive dyskinesia is an irreversible dyskinesia involving the tongue, lips, face, and jaw. These involuntary movements can make home care difficult if not impossible. Performing oral prophylaxis is difficult because of the strength of the oral facial and tongue muscles. Akathisia is an increased compulsive motor activity. Parkinsonism is characterized by symptoms of resting tremor, rigidity, and akinesia. Akinesia is a loss of voluntary muscle activity.
DIF: Recall
REF: Antipsychotic Agents (Pharmacologic Effects [First-Generation Antipsychotics]) | p. 177 OBJ: 3 TOP: NBDHE, 6.0. Pharmacology
Which of the following medications is used to treat bipolar depression?
a. Haloperidol
b. Lithium
c. Clozapine
d. Paroxetine
b. Lithium
* Lithium is used in the treatment of bipolar depression, which is characterized by cyclic recurrence of mania alternating with depression. Haloperidol is a high-potency first-generation antipsychotic. Clozapine is a second-generation antidepressant. Paroxetine is an SSRI.*
DIF: Recall REF: Drugs for Treatment of Bipolar Disorder | p. 182 OBJ: 6 TOP: NBDHE, 6.0. Pharmacology
In general, lower potency first-generation antipsychotic agents such as chlorpromazine (Thorazine) will have more of which of the following effects in contrast to the higher potency first-generation antipsychotic agents such as haloperidol (Haldol): (1) sedation, (2) orthostatic hypotension, (3) autonomic effects, (4) extrapyramidal effects?
A) 1, 2, 3, 4
B) 1, 2, 3
C) 2, 3, 4
D) 1, 2
E) 3, 4
B) 1, 2, 3
Chlorpromazine will have more sedation, orthostatic hypotension, and autonomic effects than haloperidol. Lower potency first-generation antipsychotic agents such as chlorpromazine have more sedation, more peripheral side effects, and more autonomic effects. Higher potency first-generation antipsychotics agents such as haloperidol have more extrapyramidal effects and less sedation.
DIF: Application REF: Antipsychotic Agents | p. 175 OBJ: 3 TOP: NBDHE, 6.0. Pharmacology
Which type of agent such as donepezil (Aricept) has been FDA approved for the treatment of dementia?
Cholinergic agents
Anticholinergic agents
Adrenergic agents
Adrenergic blocking agents
ANS: A
Indirect acting, reversible acetylcholinesterase inhibitors are being used to treat Alzheimer Disease (AD) dementia. They have been shown to produce modest improvements in dementia symptoms but they do not slow down, stop, or reverse disease progression. At one time anticholinergic agents were commonly used to reduce tremors associated with Parkinson disease, but at present they are only used occasionally. Some adrenergic agonists have been used to treat attention-deficit disorder (ADD) and narcolepsy.
DIF: Comprehension
REF: Parasympathetic Autonomic Nervous System (Cholinergic (Parasympathomimetic) Agents [Uses]) | p. 38 OBJ: 2 TOP: NBDHE, 6.0. Pharmacology
Indications for the use of anticholinergic agents include
A) stimulation of salivary secretion for xerostomic patients.
B) treatment of gastrointestinal disorders associated with decreased motility.
C) treatment in combination with levodopa for patients with Parkinson disease.
D) use as an antipsychotic.
C) treatment in combination with levodopa for patients with Parkinson disease.
At present, anticholinergic agents are used occasionally in combination with levodopa for the
treatment of Parkinson disease. Before the introduction of levodopa, anticholinergic agents
were commonly used to reduce the tremors and rigidity associated with Parkinson disease.
Patients treated with these agents predictably experienced the side effects of dry mouth and
blurred vision. Anticholinergic agents inhibit the secretions of saliva and bronchial mucus that
can be stimulated by general anesthesia. Many types of gastrointestinal disorders associated
with increased motility or aciNd seRcreItionGhavBe.bCeenMtreated with anticholinergic agents. USNT O
Anticholinergic agents, such as trihexyphenidyl and benztropine, are often administered concurrently with the phenothiazines to reduce rigidity and tremor; however, anticholinergics themselves are not antipsychotic medications.
DIF: Comprehension
REF: Parasympathetic Autonomic Nervous System (Anticholinergic (Parasympatholytic) Agents [Contraindications]) | p. 38 | Parasympathetic Autonomic Nervous System (Anticholinergic
(Parasympatholytic) Agents [Uses]) | p. 38 TOP: NBDHE, 6.0. Pharmacology
Antianxiety and Related Agents
Sedative/Hypnotic Agents – Benzodiazepines
• diazepam (Valium) • lorazepam (Ativan) • alprazolam (Xanax)
Anxiolytics –buspirone (BuSpar)
Hypnotics
–zolpidem (Ambien) –eszopiclone (Lunesta)
Antianxiety and Related Agents
Uses
–Treatment of anxiety and insomnia
• Potentiate GABA
–Treatment of seizures –Treatment of alcohol withdrawal
Adverse effects
– Xerostomia
–CNS sedation –Anterograde amnesia
Antidepressant Agents
Mechanism of action/Types
–Inhibit reuptake of norepinephrine/serotonin
• Tricyclic antidepressants –amitriptyline (Elavil) TCA
• SNRIs
–venlafaxine (Effexor)
–Inhibit reuptake of serotonin only (SSRIs) • citalopram (Celexa)
• escitalopram (Lexapro)
• fluoxetine (Prozac)
- paroxetine (Paxil)
- sertraline (Zoloft)
Antidepressant Agents
Mechanism of action/Types
–Inhibit reuptake of norepinephrine/dopamine
• bupropion (Wellbutrin)
–Serotonin antagonist/reuptake inhibitors (SARIs) • trazodone (Desyrel)
–Inhibit monoamine oxidase (MAOIs) • selegiline (Emsam)
–Inhibit H1, α2 and serotonin 5-HT2,3 receptors • Tetracyclic antidepressants (TeCAs)
–mirtazapine (Remeron)
Antidepressant Agents
Patient care considerations
– Additive adverse effects with other drugs
- CNS depression
- CNS stimulation
- Anticholinergic side effects
– Bruxism
– Increased potential for suicidal thoughts
Psychotherapeutic Agents
Types/Mechanism of action
–Typicals (inhibit dopamine receptors)
• haloperidol (Haldol)
–Atypicals (inhibit dopamine/serotonin receptors) • risperidone (Risperdal)
• olanzapine (Zyprexa)
Uses
–Treatment of schizophrenia, psychoses –Treatment of bipolar disorder
Psychotherapeutic Agents
Patient care considerations –Extrapyramidal symptoms (EPS)
• Dystonia of tongue, jaw and neck –May progress to tardive dyskinesia
–Additive CNS depression with other drugs • Opioids
– Xerostomia
Agents Used to Treat Bipolar Disorder
Lithium carbonate –Mechanism of action
• Inhibits stimulation of neurons causing mania
–Adverse effects
• Headache, sedation • Nausea
• Polyuria
–Patient care considerations
• May cause weakness, poor coordination
• Used as prophylaxis for vascular headaches
Anticonvulsant Agents
Mechanism of action
– Increase seizure threshold
– Decrease abnormal depolarization
Types
© Thomas A. Viola, R.Ph., C.C.P. All Rights Reserved 15
–phenytoin (Dilantin) –phenobarbital
–primidone (Mysoline) –clonazepam (Klonopin) –carbamazepine (Tegretol) –oxcarbazepine (Trileptal)
–topiramate (Topamax) –ethosuximide (Zarontin) –zonisamide (Zonegran) –lamotrigine (Lamictal) –valproate (Depakote)
Anticonvulsant Agents
Uses
–Seizure prophylaxis
–Treatment of bipolar disorder
–Treatment of mood disorders
–Treatment of ADHD
–Treatment of trigeminal neuralgia (Tegretol) –Migraine headache prophylaxis (Topamax)
Anticonvulsant Agents
Adverse effects
– Sedation
–Blood dyscrasias
Patient care considerations
– Xerostomia
–Gingival hyperplasia (Dilantin) –Drug interactions (via liver enzymes)
Agents Used to Treat Neuropathic Pain
Mechanism of Action
–Inhibit pain neurotransmitters in the CNS
Types
–gabapentin (Neurontin) –pregabalin (Lyrica)
Uses
–Treatment of neuropathic pain
- Diabetic peripheral neuropathy
- Postherpetic neuralgia (pain after shingles) • Fibromyalgia (Lyrica only)
Agents Used to Treat Neuropathic Pain
Adverse effects –Sedation, fatigue – Xerostomia
– Impotence
Patient care considerations
–May cause muscular weakness –May cause poor motor coordination –Possible behavioral disorders
• Hostile behavior, mood swings
***These drugs cause significant respiratory depresision when combined with opioids***
Agents Used to Treat Migraine Headache
Serotonin 5HT1D receptor agonists –Mechanism of action
• Promote vasoconstriction in cranial arteries
– Types
• sumatriptan (Imitrex) • rizatriptan (Maxalt)
• naratriptan (Amerge) • zolmitriptan (Zomig)
Agents Used to Treat Migraine Headache
Serotonin 5HT1D receptor agonists (continued) –Adverse effects
- Chest pain, flushing • Nausea, vomiting
- Dizziness, fatigue
–Patient care considerations
May cause neck pain and throat pain
Possible dysgeusia
Possible myalgia, muscle weakness,
Agents Used to Treat Alzheimer’s Disease
NMDA receptor antagonists –Mechanism of action
• Decrease overstimulation of NMDA receptors –Improves cognitive function
– Types
• memantine (Namenda)
–Adverse effects
• Agitation, incontinence, dizziness
–Patient care considerations
• May result in dizziness and poor coordination
Agents Used to Treat Alzheimer’s Disease
Cholinesterase inhibitors –Mechanism of action
• Decrease activity of the enzyme acetylcholinesterase
–Increase acetylcholine activity
– Types
• donepezil (Aricept)
• rivastigmine (Exelon)
Agents Used to Treat Alzheimer’s Disease
Cholinesterase inhibitors (continued) –Adverse effects
- Headache
- Nausea, diarrhea
–Patient care considerations
• Increased incidence of cardiac abnormalities • Possible hypersalivation
Agents Used to Treat Parkinson’s Disease
Dopaminergic Agents –Mechanism of action
• Increase dopamine activity
– Types
• Dopaminergic agents
– levodopa/carbidopa • Dopamine agonists
– Mirapex
– Requip
• Anticholinergic Agents
– benztropine
Agents Used to Treat Parkinson’s Disease
Dopaminergic Agents (continued) –Adverse reactions
- Dizziness
- Sedation
- Hallucinations
–Patient care considerations • Xerostomia
• Dysphagia
***EPS***
