1. Week 10 Anti-psychotics/Antianxiety Antidepressants,
Psychomotor Stimulants, & Lithium;
Anti-seizure medications;
and Sedative-Hypnotic & Alcohol
Chapters 13, 14, 16, and 12

2. Chapter 13
Antipsychotic & Antianxiety Drugs

3. Mental Illness
Psychosis is a mental condition characterized by disturbed thought processes, delusions, and hallucinations.
Anxiety is a common emotion occurring whenever there is uncertainty or fear.
Dopamine and serotonin are two neurotransmitters involved in psychotic behaviors.
Learning Outcomes
13.1 Explain the importance of dopamine and serotonin in relationship to psychosis and antipsychotic drug therapy.
Antipsychotic drugs are used to suppress the symptoms of schizophrenia and other psychotic conditions. The main site of action of antipsychotic drugs is on neural pathways involving the cerebral cortex and limbic system.
Dopamine and Serotonin are two neurotransmitters involved in psychotic behaviors. Antipsychotic drugs primarily antagonize both the D2 and 5HT2A receptors.
There are four classes of antipsychotic drugs; phenothiazines, butyrophenones, thioxanthenes, and atypical antipsychotic drugs.

4. Antipsychotic Drugs
Antipsychotic drugs are used to suppress the symptoms of schizophrenia and other psychotic conditions.
There are four classes of antipsychotic drugs:
Phenothiazines
Butyrophenones
Thioxanthenes
Atypical antipsychotic drugs
Learning Outcomes
13.1 Explain the importance of dopamine and serotonin in relationship to psychosis and antipsychotic drug therapy.
Antipsychotic drugs are used to suppress the symptoms of schizophrenia and other psychotic conditions. The main site of action of antipsychotic drugs is on neural pathways involving the cerebral cortex and limbic system.
Dopamine and Serotonin are two neurotransmitters involved in psychotic behaviors. Antipsychotic drugs primarily antagonize both the D2 and 5HT2A receptors.
There are four classes of antipsychotic drugs; phenothiazines, butyrophenones, thioxanthenes, and atypical antipsychotic drugs.

5. Side effects of Antipsychcotics
*The more dopamine is suppressed/blocked in the CNS the more the risk of EPS!*
What is EPS?

6. Symptoms-Extrapyramidal Symptoms (EPS)
Tremors
Muscle rigidity
Bradykinesia (slow movement)
The above three together are the classic triad of Parkinson’s
Postural instability
Dystonic reactions
Akathisia
Tardive Dyskinesia
Often postural hypotension
Tremors: hands and head develop palsy like motion of shakiness at rest. Pin rolling.
Muscle Rigidity: most noticable symptom. Pts have difficulty initiating movement and controlling fine muscle movements. Walking becomes difficult and pts shuffle their feet. Including a mask-like face
Postural instability: pts may hunch over and easily loose balance. Frequent falls. Pt looks like they are stooped over
Dystonic reactions (acute reaction): muscle spasms, twitching, facial grimacing, and torticollis (neck is twisted)
Akathasia (acute reaction): continuous body movement, pt is restless or constantly paces
Drug Treatments may lead to:
Tardive dyskinesia (slow reaction): involuntary movemnts of lips, jaw, tongue, and extremities
Neuroleptic malignant syndrome (NMS) (acute reaction): idiopathic syndrome characterized by hyperthermia, muscular rigidity, catatonia, and ANS instability: all leading to coma and death unless treated.

7. Antipsychotic Drugs Learning Outcomes
13.1 Explain the importance of dopamine and serotonin in relationship to psychosis and antipsychotic drug therapy.
Antipsychotic drugs are used to suppress the symptoms of schizophrenia and other psychotic conditions. The main site of action of antipsychotic drugs is on neural pathways involving the cerebral cortex and limbic system.
Dopamine and Serotonin are two neurotransmitters involved in psychotic behaviors. Antipsychotic drugs primarily antagonize both the D2 and 5HT2A receptors.
There are four classes of antipsychotic drugs; phenothiazines, butyrophenones, thioxanthenes, and atypical antipsychotic drugs.

8. Phenothiazines MOA: Block dopamine and serotonin receptors
Reduce bizarre behavior of psychosis without depressing intellectual functions
USE: Suppresses sx of schizophrenia and other psychotic conditions
Profile Drug: chlorpromazine (Thorazine)
Adverse effects:
Dry mouth, constipation, visual disturbances, and sedation
Extrapyramidal syndrome (EPS)
NC: Monitor for EPS
Learning Outcomes
13.2 List the different pharmacologic actions of the phenothiazine drugs and describe the adverse neurological effects associated with these drugs.
The term phenothiazine refers to the basic chemical structure of a large number of drugs similar in structure and pharmacological action. These drugs block D2 receptors to a greater degree than they block 5HT2A receptors. In addition to an antipsychotic effect, they possess anticholinergic, antihistaminic, alpha-adrenergic-blocking, and antiemetic effects.The main effects of the antipsychotic drugs are to reduce the bizarre behavior, hallucinations, and irrational thought disorders of psychosis without significantly depressing other intellectual functions.
Common adverse effects, such as dry mouth, constipation, visual disturbances, and sedation, are due to anticholinergic and antihistaminic actions. Alpha-blocking actions may reduce blood pressure and cause postural hypotension.
Dystonic reactions are characterized by muscle spasms, twitching, facial grimacing and torticollis (wryneck). Akathisia refers to continuous body movement in which the individual is restless or constantly paces about. Parkinsonism involves the development of muscular rigidity, tremors and other disturbances of movement.Tardive dyskinesia involves involuntary movements of the lips, jaw, tongue and extremeties. Neuroleptic malignant syndrome is also associated with the use of antipsychotic drugs. This syndrome is characterized by hyperthermia, muscular rigidity, catatonia and autonomic nervous system instability.

9. Butyrophenones
MOA: Block dopamine receptors more than serotonin receptors
Ind: Suppresses sx of schizophrenia and other psychotic conditions
Lower incidence of peripheral effects, but greater movement disturbances
Profile Drug: haloperidol (Haldol)
Adverse effects similar to phenothiazines:
Higher incidence of EPS
Tardive dyskinesia
Neuroleptic malignant syndrome
From a sudden marked reduction in dopamine activity
Related to a withdrawal of dopamine
Seen as hyperthermia, muscular rigidity, catatonia
Learning Outcomes
13.3 Compare the pharmacologic actions and adverse effects of the butyrophenones with the phenothiazines.
Butyrophenones are high-potency drugs that block D2 receptors more than 5HT2A receptors. The butyrophenones produce a lower incidence of peripheral effects (alpha-adrenergic blockade, anticholinergic, and antihistaminic), but greater movement disturbances.
The adverse effects of the butyrophenones are similar to those of the phenothiazines. However, the butyrophenones, haloperidol in particular, produce the highest incidence of extrapyramidal symptoms (EPS). There is also the potential for development of tardive dyskinesia and neuroleptic malignant syndrome.

10. Thioxanthenes
MOA: Block dopamine receptors more than serotonin receptors
Ind: Suppresses sx of schizophrenia and other psychotic conditions
Profile Drug: thiothixene (Navane)
High-potency drugs that are associated with higher incidences of EPS
Adverse effects:
Drowsiness
Postural hypotension
EPS
Learning Outcomes
13.4 Describe the actions and adverse effects of the thioxanthine antipsychotic drugs.
Thioxanthenes have chemical structures very similar to those of phenothiazines. Like phenothiazines and butyrophenones, thioxanthenes exert antipsychotic effects by blocking D2 receptors more than 5HT2A receptors.
Thiothixene is a high potency drug that is associated with higher incidences of EPS. Thiothixene generally causes less sedation and fewer anticholinergic and alpha-blocking effects than those of chlorpromazine.
The most frequent adverse effects of the thioxanthenes include drowsiness and postural hypotension. Patients who become allergic to these drugs may develop dermatitis, obstructive jaundice, or blood disorders (anemia and leukopenia). Like other antipsychotic drugs, the thioxanthenes may cause parkinsonian symptoms and other extrapyramidal disturbances of movement.

11. Atypical Antipsychotic Drugs
MOA -Block serotonin receptors more than dopamine receptors
SE:
Potential for EPS, tardive dyskinesia, and neuroleptic malignant syndrome
Associated with several metabolic disturbances such as weight gain, hyperlipidemia, and diabetes mellitus
NC:
Pregnancy Category D
Monitor for EPS
Monitor Blood Glucose
Monitor temp
Learning Outcomes
13.5 Explain the actions and advantages of the atypical antipsychotic drugs when compared to the typical antipsychotic drugs.
Unlike the phenothiazine, butyrophenone, and thioxanthene drugs, the atypical antipsychotic drugs affect and reduce the activity of 5HT2A receptors more than they interfere with D2 receptors.
As with all antipsychotic drugs there is the potential for development of EPS, tardive dyskinesia, and neuroleptic malignant syndrome. Atypical drugs are associated with several metabolic disturbances such as weight gain, elevated triglycerides (hyperlipidemia), and development of diabetes mellitus.
Aripiprazole (Abilify), clozapine (Clozaril), risperidone (Risperdal) and olanzapine (Zyprexa) are all atypical antipsychotics.
Antipsychotics should not be used in pregnancy unless the benefits outweigh the risks. Many of the antipsychotic drugs produce anticholinergic, alpha-blocking, antihistaminic, and central nervous system (CNS) depressing effects. Therefore, these drugs will interact with all other drugs that also produce these pharmacologic effects.

12. Atypical Antipsychotic Drugs
aripiprazole (Abilify)
olanzapine (Zyprexa)
quetiapine (Seroquel)
risperidone (Risperdal)
Learning Outcomes
13.5 Explain the actions and advantages of the atypical antipsychotic drugs when compared to the typical antipsychotic drugs.
Unlike the phenothiazine, butyrophenone, and thioxanthene drugs, the atypical antipsychotic drugs affect and reduce the activity of 5HT2A receptors more than they interfere with D2 receptors.
As with all antipsychotic drugs there is the potential for development of EPS, tardive dyskinesia, and neuroleptic malignant syndrome. Atypical drugs are associated with several metabolic disturbances such as weight gain, elevated triglycerides (hyperlipidemia), and development of diabetes mellitus.
Aripiprazole (Abilify), clozapine (Clozaril), risperidone (Risperdal) and olanzapine (Zyprexa) are all atypical antipsychotics.
Antipsychotics should not be used in pregnancy unless the benefits outweigh the risks. Many of the antipsychotic drugs produce anticholinergic, alpha-blocking, antihistaminic, and central nervous system (CNS) depressing effects. Therefore, these drugs will interact with all other drugs that also produce these pharmacologic effects.

13. Anxiety
Anxiety is caused by uncertainty and situations that are interpreted as threatening or dangerous.
Dangers may be real or due to insecurities or psychological conflicts.
Prolonged anxiety causes behavioral and emotional changes.
Other drug classes include:
Benzodiazepines
BuSpar
Learning Outcomes
13.6 Compare the mechanism of action and pharmacologic effects of the antianxiety benzodiazepines with buspirone.
Anxiety, tension, and nervousness are effects caused by uncertainty and various situations that are interpreted as being threatening or potentially dangerous. The perceived dangers may be real or due to personal insecurities or unconscious psychological conflicts.
When an anxiety condition is prolonged, there are significant behavioral and emotional changes. Antianxiety drugs, also referred to as anxiolytics, are used to calm individuals and reduce the unpleasant aspects of anxiety and hyperemotionalism.

14. Drugs used to treat anxiety are called anxiolytics.
Antianxiety Drugs
Drugs used to treat anxiety are called anxiolytics.
Anxiolytics work to:
Calm individuals
Reduce anxiety
Reduce hyperemotionalism
Learning Outcomes
13.6 Compare the mechanism of action and pharmacologic effects of the antianxiety benzodiazepines with buspirone.
When an anxiety condition is prolonged, there are significant behavioral and emotional changes. Antianxiety drugs, also referred to as anxiolytics, are used to calm individuals and reduce the unpleasant aspects of anxiety and hyperemotionalism.
The most important antianxiety drugs belong to a chemical class known as the benzodiazepines. Diazepam (Valium) and chlordiazepoxide (Librium) were the first benzodiazepines introduced and have been available for almost 50 years.

15. buspirone (BuSpar)
Used primarily as an antianxiety drug (Class: Anxiolytic)
USE: Does not cause sedative, hypnotic, anticonvulsant, or skeletal muscle relaxant actions like the benzodiazepines do
USE: Is a suitable alternative to the benzodiazepines, especially when drug dependence and drug abuse problems are an issue
SE: syncope, rash, fatigue
Learning Outcomes
13.6 Compare the mechanism of action and pharmacologic effects of the antianxiety benzodiazepines with buspirone.
Buspirone is a drug that is used primarily as an antianxiety drug. It does not demonstrate useful sedative, hypnotic, anticonvulsant, or skeletal muscle relaxant actions like the benzodiazepines.
In general, buspirone is well tolerated and there appear to be few contraindications for its use. It serves as a suitable alternative to the benzodiazepines, especially when drug dependence and drug abuse problems with the benzodiazepines are an issue.

16. Chapter 14
Antidepressants, Psychomotor Stimulants,
and Lithium

17. Depression and Mania
Depression is linked to low levels of norepinephrine and/or serotonin.
Mental state characterized by a depressed mood, with feelings of frustration and hopelessness
Mania is linked to high levels of norepinephrine and/or serotonin.
Mental state of excitement, hyperactivity, and excessive elevation of mood
Bipolar mood disorder is alternating cycles of depression and mania.
Learning Outcomes
14.1 Identify the different types of depression and the importance of neurotransmitter function in the cause and treatment of depression.
In some cases of depression, there are alternate periods of hyperexcitability and elation known as mania. Individuals who experience these alternating cycles of depression and mania are classified as manic depressive. Another term for this condition is bipolar mood disorder.
Low levels of norepinephrine and/or serotonin are associated with mental depression, while high levels of norepinephrine and/or serotonin may be involved in mania. This concept involving norepinephrine and serotonin is known as the Monoamine Theory of Mental Depression.
Definitions from pg 188

18. Drugs Used to Treat Depression
Drugs that increase the level of norepinephrine and serotonin are used in the treatment of depression.
Major antidepressant drug classes:
Serotonin reuptake inhibitors (SSRIs)
Atypical SSRIs
Tricyclic antidepressants (TCAs)
Monoamine oxidase inhibitors (MAOIs)
Pyschomotor Stimulants
Lithium
Learning Outcomes
14.1 Identify the different types of depression and the importance of neurotransmitter function in the cause and treatment of depression.
Drugs that can increase the level of norepinephrine or serotonin in the brain are useful in the treatment of mental depression. They are referred to as antidepressants, or mood elevators. The major antidepressant drug classes include the selective serotonin reuptake inhibitors (SSRIs), atypical SSRIs, tricyclic antidepressants (TCAs), and monoamine oxidase inhibitors (MAOIs).

19. Selective Serotonin Reuptake Inhibitors
MOA:
SSRIs block the reuptake of serotonin back into the serotonergic nerve endings.
This increases the serotonin available to work on the system.
USE: SSRIs are the preferred treatment for major depression and effective for PTSD and OCD.
Learning Outcomes
14.2 Describe the mechanism of action and adverse effects profile of the selective serotonin reuptake inhibitors (SSRIs).
The SSRIs are a group of drugs that have a very selective action to block the reuptake of serotonin (5HT) back into the serotonergic nerve endings. This action increases the concentration of 5HT in the synaptic cleft, which results in increased stimulation of serotonin receptors. The increase in 5HT activity in the limbic and cerebral cortical areas of the brain is believed to contribute to the antidepressant effect.
The SSRIs have become preferred therapy for treatment of major depression. SSRIs are also effective in the treatment of most anxiety disorders such as posttraumatic stress disorder (PTSD) and obsessive-compulsive disorder (OCD).
All the SSRIs listed cause GI disturbances including nausea, diarrhea, dry mouth, and anorexia. SSRIs also have been associated with sexual dysfunction, most commonly reduced sexual interest and delayed orgasm. Other CNS effects include headache, nervousness, insomnia, and tremors.
14.1 on page 191. under adverse effects 3rd paragraph
“S/S of overdose most commonly include confusion, fever, tremor agitation, restlessness, and other signs of CNS excitation. These signs are referred to a serotonin syndrome.”
Sudden discontinuation of SSRI treatment has been associated with disconnection syndrome,. Symptoms include dizziness, nausea, insomnia, and anxiety. The dosage of SSRIs and related drugs should be gradually reduced over time when treatment is stopped. (page 191)

20. Selective Serotonin Reuptake Inhibitors
Adverse effects:
GI disturbances
Dry mouth
Sexual dysfunction
Headache
Nervousness
Insomnia
Tremors
Serotonin syndrome:
Related to overdosage
Symptoms include confusion, fever, tremor, agitation, restlessness, and other signs of CNS stimulation
May lead to coma or death if not treated
Learning Outcomes
14.2 Describe the mechanism of action and adverse effects profile of the selective serotonin reuptake inhibitors (SSRIs).
The SSRIs are a group of drugs that have a very selective action to block the reuptake of serotonin (5HT) back into the serotonergic nerve endings. This action increases the concentration of 5HT in the synaptic cleft, which results in increased stimulation of serotonin receptors. The increase in 5HT activity in the limbic and cerebral cortical areas of the brain is believed to contribute to the antidepressant effect.
The SSRIs have become preferred therapy for treatment of major depression. SSRIs are also effective in the treatment of most anxiety disorders such as posttraumatic stress disorder (PTSD) and obsessive-compulsive disorder (OCD).
All the SSRIs listed cause GI disturbances including nausea, diarrhea, dry mouth, and anorexia. SSRIs also have been associated with sexual dysfunction, most commonly reduced sexual interest and delayed orgasm. Other CNS effects include headache, nervousness, insomnia, and tremors.

21. SSRI Nursing Considerations
Do not stop abruptly, taper
Takes approximately 2 weeks for effectiveness
Monitor for Serotonin Syndrome
Usually occurs 72 hours after starting the drug
Monitor for suicidal ideation

22. Selective Serotonin Reuptake Inhibitors
Fluoxetine (Prozac)
Paroxetine (Paxil)
Sertraline (Zoloft)
Learning Outcomes
14.2 Describe the mechanism of action and adverse effects profile of the selective serotonin reuptake inhibitors (SSRIs).
The SSRIs are a group of drugs that have a very selective action to block the reuptake of serotonin (5HT) back into the serotonergic nerve endings. This action increases the concentration of 5HT in the synaptic cleft, which results in increased stimulation of serotonin receptors. The increase in 5HT activity in the limbic and cerebral cortical areas of the brain is believed to contribute to the antidepressant effect.
The SSRIs have become preferred therapy for treatment of major depression. SSRIs are also effective in the treatment of most anxiety disorders such as posttraumatic stress disorder (PTSD) and obsessive-compulsive disorder (OCD).
All the SSRIs listed cause GI disturbances including nausea, diarrhea, dry mouth, and anorexia. SSRIs also have been associated with sexual dysfunction, most commonly reduced sexual interest and delayed orgasm. Other CNS effects include headache, nervousness, insomnia, and tremors.

23. Atypical SSRIs
MOA: They block reuptake of serotonin and act on other neurotransmitters and receptors as well.
Like the SSRIs, they have little effect in blocking cholinergic, adrenergic, or histamine receptors.
Learning Outcomes
14.3 Explain the major difference between the SSRIs and the atypical SSRI antidepressants.
The atypical SSRI antidepressant drugs block reuptake of serotonin like the SSRIs but have additional actions on other neurotransmitters and receptors. The atypical drugs affect serotonin and other neurotransmitters such as norepinephrine and dopamine.

24. Atypical SSRIs SE/NC Sedation Orthostatic hypotension Monitor BP
Advise to get up slowly, especially initially
Hepatotoxicity
Monitor LFTS
Monitor for Suicidal Ideation

25. Atypical SSRIs Bupropion (Wellbutrin) Duloxetine (Cymbalta)
Trazodone (Desyrel)
Venlafaxine (Effexor)
Learning Outcomes
14.3 Explain the major difference between the SSRIs and the atypical SSRI antidepressants.
The atypical SSRI antidepressant drugs block reuptake of serotonin like the SSRIs but have additional actions on other neurotransmitters and receptors. The atypical drugs affect serotonin and other neurotransmitters such as norepinephrine and dopamine.

26. Tricyclic Antidepressants
MOA: Drugs that block the reuptake of norepinephrine and serotonin back into the neuronal nerve endings
Produce varying degrees of sedation, anticholinergic effects, and alpha-adrenergic blockade
USE: Treating major depression
Learning Outcomes
14.4 Describe the mechanism of action and the adverse effects profile of the tricyclic antidepressants (TCAs).
Tricyclic antidepressant drugs (TCAs or tricyclics) are so named because of the characteristic triple ring structure that they possess. The main action of the tricyclics and related antidepressant drugs is to block the reuptake of norepinephrine and serotonin back into the neuronal nerve endings. The tricyclics and related drugs produce varying degrees of sedation, anticholinergic effects, and alpha-adrenergic blockade.

27. TCAs Adverse Effects/Nursing Considerations
Produce a varying degree of sedation
Anticholinergic effects (dry mouth)
Teach pt to chew gum or hard candy to prevent dry mouth
Alpha-adrenergic blockade (postural hypotension)
Teach pt to rise slowly to minimize dizziness
Constipation
Teach pt to increase dietary fiber to prevent constipation
CNS stimulation (tremors, restlessness) –report to MD
Taper, do not stop abruptly
Monitor for suicidal ideation

28. Tricyclic Antidepressants
Nortiptyline (Aventyl)
Amitriptyline (Elavil)
Imipramine (Tofranil)
Learning Outcomes
14.4 Describe the mechanism of action and the adverse effects profile of the tricyclic antidepressants (TCAs).
Tricyclic antidepressant drugs (TCAs or tricyclics) are so named because of the characteristic triple ring structure that they possess. The main action of the tricyclics and related antidepressant drugs is to block the reuptake of norepinephrine and serotonin back into the neuronal nerve endings. The tricyclics and related drugs produce varying degrees of sedation, anticholinergic effects, and alpha-adrenergic blockade.

29. Monoamine Oxidase Inhibitor aka MAOIs
MOA: Breakdown NE and serotonin metabolites; so NE and serotonin can increase and be available (to elevate mood)
Disadvantages of MOAIs:
(NC): Interacts with MANY medications
(NC): Dietary restrictions—tyramines
NO wine, beer, herring, certain cheeses
Adverse effects:
Dry mouth
Urinary retention
Hypotension
Restlessness
Seizures
Suicidal Ideation
Learning Outcomes
14.5 Explain the mechanism of action of the MAO inhibitors and describe the adverse effects and dietary restrictions relating to these drugs.
One of the main disadvantages of MAO inhibitor therapy is the dietary restrictions. Many foods contain a substance known as tyramine, which causes the release of norepinephrine. When MAO is inhibited, tyramine may produce a massive release of norepinephrine, which can result in serious consequences, such as hypertensive crisis or cerebral stroke.
Foods that normally contain tyramine include wine, beer, herring, and certain cheeses. In addition, certain sympathetic drugs used in the treatment of cold symptoms (decongestants and bronchodilators) interact with the MAO inhibitors.
Common adverse effects include dry mouth, urinary retention, constipation, blurred vision, hypotension, weight gain, and sexual dysfunction. A variety of CNS disturbances including restlessness, dizziness, insomnia, tremors, and seizures may occur. These effects are intensified with overdosage. In addition, they can produce a type of liver damage that may be fatal.

30. Monoamine Oxidase Inhibitor
Learning Outcomes
14.5 Explain the mechanism of action of the MAO inhibitors and describe the adverse effects and dietary restrictions relating to these drugs.
One of the main disadvantages of MAO inhibitor therapy is the dietary restrictions. Many foods contain a substance known as tyramine, which causes the release of norepinephrine. When MAO is inhibited, tyramine may produce a massive release of norepinephrine, which can result in serious consequences, such as hypertensive crisis or cerebral stroke.
Foods that normally contain tyramine include wine, beer, herring, and certain cheeses. In addition, certain sympathetic drugs used in the treatment of cold symptoms (decongestants and bronchodilators) interact with the MAO inhibitors.
Common adverse effects include dry mouth, urinary retention, constipation, blurred vision, hypotension, weight gain, and sexual dysfunction. A variety of CNS disturbances including restlessness, dizziness, insomnia, tremors, and seizures may occur. These effects are intensified with overdosage. In addition, they can produce a type of liver damage that may be fatal.

31. Psychomotor Stimulants
Include the amphetamines and other closely related drugs
MOA: Stimulate the CNS by increasing the activity of norepinephrine and dopamine in the brain
Used to treat narcolepsy, elevate mood, and increase psychomotor activity
Learning Outcomes
14.6 Discuss the use of psychomotor stimulants in the treatment of narcolepsy, hyperkinetic syndrome, and obesity.
The psychomotor stimulants include the amphetamines and other closely related drugs, which are really not classified as antidepressants. Their role in the treatment of depression is extremely limited. Psychomotor stimulants are occasionally used during the first few weeks of treatment to elevate mood and increase psychomotor activity.
Amphetamines also are used to treat narcolepsy (uncontrolled tendency to fall asleep) and hyperkinesis in children. Amphetamines stimulate the reticular formation, which increases wakefulness and alertness and reduces the number of attacks of narcolepsy.
The amphetamines stimulate the CNS by increasing the activity of norepinephrine and dopamine in the brain. Amphetamines increase neurotransmitter activity by several different mechanisms. They act directly to stimulate norepinephrine and dopamine receptors, they stimulate the release of norepinephrine and dopamine from the nerve endings, and they inhibit the reuptake of these neurotransmitters back into the nerve endings

32. Psychomotor Stimulants
Disadvantages/SE:
Drug tolerance and dependence
Increase activity of sympathetic nervous system
Dry mouth
Rapid heartbeat
Increased blood pressure
Restlessness
Insomnia
NC:
Monitor HR
Monitor for agitation/insomnia
Learning Outcomes
14.6 Discuss the use of psychomotor stimulants in the treatment of narcolepsy, hyperkinetic syndrome, and obesity.
Amphetamines have the disadvantage of producing drug tolerance and drug dependence. The amphetamines are among the leading “street drugs” that are abused and illegally marketed.
The psychomotor stimulants increase the activity of the sympathetic nervous system, producing dry mouth, rapid heartbeat, increased blood pressure, restlessness, and insomnia. Toxic doses may produce severe agitation and a paranoid type of psychosis.

33. Psychomotor Stimulants
Amphetamine
Dextramphetamine (Dexadrine)
Methylphenidate (Ritalin)
Learning Outcomes
14.6 Discuss the use of psychomotor stimulants in the treatment of narcolepsy, hyperkinetic syndrome, and obesity.
Amphetamines have the disadvantage of producing drug tolerance and drug dependence. The amphetamines are among the leading “street drugs” that are abused and illegally marketed.
The psychomotor stimulants increase the activity of the sympathetic nervous system, producing dry mouth, rapid heartbeat, increased blood pressure, restlessness, and insomnia. Toxic doses may produce severe agitation and a paranoid type of psychosis.

34. Lithium MOA: Lithium interferes with nerve conduction:
Decrease in excitability of nerve tissue
It is administered as a salt:
Profile Drugs: Eskalith and Eskalith CR
Sodium helps with excretion of lithium.
One to two weeks are required before a therapeutic effect is observed.
Learning Outcomes
14.7 Explain the use of lithium in mania and bipolar disorder and the adverse effects associated with its use.
Lithium is used for the treatment of mania and bipolar mood disorder. It is often used in combination with antidepressant drugs in the manic-depressive or bipolar form of psychosis.
Both lithium (Li+) and sodium (Na+) exist in body fluids as charged particles, or ions. However, whereas Na+ is normally required for conduction of nerve impulses, Li+ interferes with nerve conduction. As a result, there is a decrease in the excitability of nerve tissue.
Lithium is administered as a salt, lithium carbonate, in the form of capsules (Eskalith) or controlled release and slow-release tablets (Eskalith CR, Lithobid). Usually 1 to 2 weeks of treatment are required before therapeutic effects are observed.

35. Lithium Uses: For mania and bipolar disorders
Disorders alternating in cycles of depression and mania
Hyperactive and excessive mood elevation
Including wide shifts in mood

36. Lithium Side effects Toxic levels Nausea Tremors Vomiting
Ringing in ears (tinnitus)
Frequent urination
Toxic levels
Heart and kidney damage
Learning Outcomes
14.7 Explain the use of lithium in mania and bipolar disorder and the adverse effects associated with its use.
Adequate sodium intake is necessary for proper urinary excretion of lithium. Decreased sodium intake and hyponatremia (low sodium levels) promote the retention of lithium and can lead to toxicity.
Side effects are common with lithium, even at therapeutic doses. Initially, most patients experience some nausea or tremors that usually disappear with continued treatment. With overdose, vomiting, diarrhea, drowsiness, loss of equilibrium, ringing in the ears, and frequent urination are common. At toxic levels, the heart and kidneys may be damaged, leading to the development of cardiac arrhythmias or nephritis.
Lithium has been designated FDA Pregnancy Category D and therefore should not be used during pregnancy

37. Lithium –Nursing Considerations
Takes one to two weeks for therapuetic effectis
Monitor serum levels
Pregnancy Category D

38. 1. Except effects to occur within 12 hours.
A nurse is reinforcing teaching to a client who is starting amitriptyline (Elavil)for treatment of depression. Which of the following should the nurse include? (select all that apply)
1. Except effects to occur within 12 hours.
2. Stop taking this medication after a week of improved mood.
3. Change positions slowing to minimize dizziness.
4. Decrease dietary fiber intake to control diarrhea.
5. Chew sugarless gum to prevent dry mouth.
Correct answers are 3 & 5.
refer to slide 14-40
Advise clients to change positions slowly to minimize effects of orthostatic hypotension., such as dizziness and lightheadedness. Advise clients to chew sugarless gum to minimize mouth. Therapeutic effects may take several weeks to be achieved. Medications should not be stopped abruptly, and therapy will most likely last 6 to 12 months to prevent relapse. Clients should increase dietary fiber to prevent constipation.

39. Anticholinergic effects Hypernatremia
A nurse is caring for an older adult client who is prescribed paroxetine (Paxil) for two days. The client suddenly develops a high fever, hallucinations and anxiety. Which of the following adverse reactions is the client likely to be experiencing?
Bruxism
Serotonin syndrome
Anticholinergic effects
Hypernatremia
Correct answer is B
Refer to slide , notes at very bottom.
The client is likely to be experiencing serotonin syndrome, which may occur within 72 hours of beginning a prescriptions of an SSRI antidepressant, such as paroxetine (Paxil). The manifestations of serotonin syndrome do not resemble those of bruxism, anticholinergic effects or hypernatremia.
Bruxism is the excessive grinding of the teeth and/or excessive clenching of the jaw.
anticholinergic effects – F/F responses
Hypernatremia - These can include nausea, emesis, headache, seizures, lethargy, development of focal neurologic deficits, respiratory depression, and coma.

40. A client stated taking lithium a month ago tells the nurse she has just begun to have ringing in the ears and loss of balance. What instructions does the nurse give this client?
These are initial side effects and will probably disappear with continued treatment.
She needs to be seen by her doctor as soon as possible. She will need someone to escort her.
She should drink a cup of broth to increase her electrolytes.
She should take an extra dose and lay down for nap.
Correct answer is B
These are early signs of overdose
LO 14.7 page 197 in textbook.

41. Antiepileptic Drugs Drugs for Seizures
Chapter 16
Antiepileptic Drugs
Drugs for Seizures

42. Seizures - Disturbances of Electrical Activity in the Brain
Symptom of underlying disorder
May affect consciousness, motor activity, sensation
Caused by abnormal or uncontrollable neuronal discharges in the brain
Electroencephalogram (EEG) measures this activity
All seizures are not convulsions
Not a disease in itself.
But all convulsions are seizures.
This is why we call drugs antiseizure instead of anticonvulsants.
Infectious diseases
Trauma
Metabolic disorders
Vascular diseases
Pediatric disorders
Neoplastic disease
Meds
Pregnancy
Sleep deprivation
Strobe or flickering lights

43. Pregnancy and seizures
Eclampsia- pregnancy cause disorder resulting from pre- eclampsia
Characterized by HTN, HA, and edema
Some antiseizure meds may decrease effectiveness of oral contraceptives
Can also cause folic acid deficiency
Most antiseizure meds are pregnancy category D
Must weigh risk/benefit ratio with MD. Woman may stay on antiseizure med.

44. Tonic-Clonic and Partial-Seizure Drugs
The drugs used for epilepsy possess anticonvulsant properties.
An anticonvulsant is a drug that terminates convulsive seizures.
An antiepileptic can be used prophylactically to reduce or prevent epileptic seizures.
Learning Outcomes
16.2 Compare the mechanism of action and uses of phenobarbital with those of phenytoin, carbamazepine, and valproic acid.
16.3 Identify the mechanism of action of the drugs primarily effective for partial seizures.
All of the primary drugs used to treat epilepsy possess anticonvulsant properties. An anticonvulsant is defined as a drug, usually administered IM or IV, that terminates convulsive seizures. The term antiepileptic infers that the drug, usually administered orally, can be used prophylactically to reduce or prevent epileptic seizures.
All barbiturates have anticonvulsant properties, but only a few, such as phenobarbital and mephobarbital, have the additional property of being antiepileptic.

45. Choice of Anti-seizure Drug Depends on:
Type of seizure
Patient’s previous medical history
Diagnostic studies
Pathological process causing the seizures

46. Drug Therapy
Effective seizure management depends on strict adherence to drug therapy
Initial dose is low
Dose gradually increased until seizures are controlled
Side effects of drug may prevent increases in dose
Blood levels of drug may be checked

47. Drug Therapy Continued
If seizure activity continues, a different med is added in small doses while dose of first drug is reduced
Medication is withdrawn over weeks
Why?
Seizures are likely to occur with abrupt withdrawl.

48. Drug Therapy Goals
1. To suppress neuronal activity just enough to prevent abnormal or repetitive firing
2. To increase the electrical threshold- the excitable levels at which the neuron must fire
If threshold is increased, this decreases possibility of abnormal firing and seizures.

49. Gamma-aminobutric acid (GABA)
Primary inhibitory neurotransmitter in the brain
Several antiseizure meds act by changing (intensifying) the action of GABA
Suppresses the ability of neurons to fire and causes CNS depression

51. Anti-seizure Drug Classes
Hydantoins
Hydantoin like drugs (2 drug cards)
(Depakote and Tegretol)
Succinimides
Benzodiazepines
Barbiturate
Miscellaneous agents

52. Hydantoins Potent antiepileptic:
MOA: Prolongs the inactivation of neuron ion channels and neurotransmitter functions. This prevents the spread of disruptive electrical charges in the brain that produce seizures
Used in partial and tonic-clonic seizures
Learning Outcomes
16.2 Compare the mechanism of action and uses of phenobarbital with those of phenytoin, carbamazepine, and valproic acid.
16.3 Identify the mechanism of action of the drugs primarily effective for partial seizures.
The most important drug from this class is phenytoin (Dilantin). Phenytoin is a very potent antiepileptic drug, and it can be used in several types of epilepsy. A significant advantage of phenytoin is that it produces little sedation. Phenytoin is used for all types of partial seizures and for tonic-clonic generalized seizures. It also can be administered IV in acute situations to arrest convulsive seizures including the treatment of status epilepticus.
The mechanism of action of phenytoin and the other hydantoins is complex and affects the activity of both neuron ion channels (Na+, K+, Ca++) and neurotransmitter functions. The primary effect of phenytoin is believed to prolong the inactivation period of sodium (Na+) channels in the nerve membrane.
The most common adverse effects of hydantoins involve the cerebellum. The symptoms are dizziness, ataxia, visual disturbances, and postural imbalance. Other adverse effects include skin rashes, hirsutism, and gingival hyperplasia.

53. phenytoin (Dilantin) Oldest and most prescribed hydantoin
Nursing Considerations:
Narrow therapeutic range
Must carefully monitor serum levels!
Interacts with many other drugs
Draw CBC, See Dentist (good oral hygiene)
Adverse Effects:
Can cause dysrhythmias
Peripheral neuropathy with long term use
Agranulocytosis, aplastic anemia
Connective tissue reactions (i.e.- gingival hypertrophy)
Dizziness, ataxia, postural imbalance
visual disturbances
hirsutism
Narrow therapeutic range- difference between therapeutic and toxic dose is small.
Agranulocytosis- reduction in granulocytes (WBCs).
Aplastic anemia- anemia due to failure of bone marrow to make RBCs.

54. Hydantoin Like Drugs MOA: same as hydantoins Includes drugs like:
carbamezepine (Tegretol)
valproic acid (Depakene, Depakote)

55. carbamazepine (Tegretol)
Related to tricyclic antidepressants:
Works similarly to phenytoin (MOA)
Used to treat partial and tonic-clonic seizures, mania, and bipolar disorder
Adverse effects:
Dizziness, nausea, vomiting, diplopia, liver disturbances and bone marrow depression
Learning Outcomes
16.2 Compare the mechanism of action and uses of phenobarbital with those of phenytoin, carbamazepine, and valproic acid.
16.3 Identify the mechanism of action of the drugs primarily effective for partial seizures.
Carbamazepine is structurally related to the tricyclic antidepressants. The mechanism of action is similar to that of phenytoin and involves an action to prolong the inactivation of Na + channels. This decreases the neuronal influx of sodium ions and inhibits high-frequency and repetitive firing of neurons.
Carbamazepine is used in the treatment of all types of partial seizures and generalized tonic-clonic seizures. It also is indicated for the treatment of mania and bipolar disorder.
Common side effects include nausea, vomiting, diplopia, drowsiness, and dizziness. More serious effects involve liver disturbances, jaundice, and bone marrow depression, which may lead to aplastic anemia.

56. valproic acid (Depakene, Depakote)
MOA: Inhibits high-frequency firing of neurons, blocks excitatory (NMDA) receptors, and increases inhibitor effects of GABA
Used for all types of epilepsy
Adverse effects:
Nausea, vomiting, diarrhea, tremor, and risk of potentially fatal liver toxicity
Learning Outcomes
16.2 Compare the mechanism of action and uses of phenobarbital with those of phenytoin, carbamazepine, and valproic acid.
16.3 Identify the mechanism of action of the drugs primarily effective for partial seizures.
Valproic acid is one of the few drugs that can be used in all types of epilepsy. Like carbamazepine and phenytoin, valproic acid decreases the influx of Na+ ions and inhibits high-frequency firing of neurons. In addition, valproic acid blocks excitatory glutamate (NMDA) receptors and increases the inhibitor effects of GABA.
The most common side effects of valproic acid are nausea, vomiting, diarrhea, and tremor. The most serious problem with valproic acid has been the development of a potentially fatal liver toxicity, especially in young patients.

57. Succinimides
MOA: Delay the entry of calcium into neurons by blocking channels; increases the electrical threshold
Use: primarily for absence seizures; secondary drug for other types of seizures
Adverse effect- psychosis or extreme mood swings (including depression with suicidal intent); GI disturbances (N, V, & D); drowsiness and dizziness
Nursing Consideration: Watch for suicidal ideation
Profile Drug: ethosuximide (Zarontin)

58. Benzodiazepines
MOA: intensify effect of GABA, thus suppressing neuronal firing
Nursing Consideration:
Tolerance may develop- doses periodically readjusted
Dependency is also a problem
No ETOH or other CNS depressants
Used in combination with other anti-seizure drugs for short term control
One of most widely prescribed classes of drugs…not just for seizure control
What else???
Not used alone.
Anti-anxiety, sedation, muscle spasms, alcohol withdraw symptoms, as well as anticonvulsant.

59. Commonly used benzodiazepines for seizure control
clonazepam (Klonopin)
diazepam (Valium)
**lorazepam (Ativan) - used for status epilepticus
Temazepam (Restoril)
Reversal Agent: flumazenil (Romazicon)
Do not take with alcohol or other CNS depressants b/c of combined sedation effects.
Used for short term control b/c of risk of tolerance and dependency.

60. Barbiturates Nursing Considerations:
As a class, have a low margin of safety (can cause serious CNS depression) – monitor serum levels
High potential for dependency
May take several weeks for optimal effects
MOA: Enhance the action of GABA; suppresses the ability of neurons to fire causing CNS depression
USE: tx both general and partial seizures
Example- phenobarbital (Luminal)

61. Side Effects Drowsiness
With overdose- resp depression, CNS depression, coma, and death
High potential for dependency
Nursing considerations r/t ETOH or other CNS depressants?
Do not take with alcohol or other CNS depressants. Alcohol and CNS depressants potentiate action of barbiturates, increasing the risk of life threatening resp depression or cardiac arrest.
May take several weeks to achieve optimal effects.

62. Miscellaneous Agents gabapentin (Neurontin) tiagabine (Gabatril)
levetiracetam (Keppra)
topiramate (Topamax)
Also act by intensifying action of GABA.

63. Preferred Treatment of Seizures
Generalized Tonic-Clonic and Partial Seizures:
Phenytoin, valproic acid, carbamazepine
Lamotrigine and topiramate useful in children
Absence Seizures:
Ethosuximide, especially in children
Valproic acid and lamotrigine, in adults
Status Epilepticus:
lorazepam (Ativan)
Learning Outcomes
16.6 Identify the preferred therapies for the different types of epileptic seizures.
For Generalized Tonic-Clonic Seizures: Phenytoin (Dilantin) is considered the drug of choice. Valproic acid (Depakene) and carbamazepine (Tegretol) are also first-line drugs. Lamotrigine (Lamictal) and topiramate (Topamax) are also effective and particularly useful in children because of the lower incidence of adverse effects.
For Partial Seizures: There are a number of drugs that are equally effective for partial seizures. Phenytoin (Dilantin), carbamazepine (Tegretol), and valproic acid (Depakene) are usually the preferred drugs. Newer drugs such as lamotrigine (Lamictal) and topiramate (Topamax) are also effective and serve as alternate therapy.
For Absence Seizures: Ethosuximide (Zarontin) has usually been the drug of choice for these seizures, especially in children. Valproic acid (Depakene) and lamotrigine (Lamictal) are also effective drugs and may be preferred in adults, especially when other seizure types are also present.
For Status Epilepticus: The drug of choice to arrest status epilepticus is now considered to be lorazepam (Ativan) administered IV. Diazepam is equally effective but has a shorter duration of action when administered IV and may require additional administrations.

64. Question #1
Why should women of childbearing age be counseled regarding antiseizure medications?
A. They can be teratogenic
B. They interfere with oral contraceptives
C. They produce folic acid deficiency
D. All of the above D

65. Question #2
What is the most important reason benzodiazepines are not used for chronic seizure control?
A. Patients tend to develop tolerance to the drug
B. Too many side effects
C. Respiratory depression occurs with chronic use
D. No antidote exists A

66. Question #3
What is the major concern in making antiseizure therapy successful?
A. Minimizing CNS depression
B. Making sure the patient complies with medication
C. Maintaining proper drug levels in the bloodstream
D. All of the above D

67. Question #4
An infant is brought to the ED with observable twitching of the extremities and a temperature of degrees F reported by the parents. The priority action is to:
A. Take vital signs
B. Call a health care provider
C. Check the airway
D. Take a history C

68. Question #5
You are caring for a patient with epilepsy who was hospitalized and successfully treated for status epilepticus. Which drug did the patient most likely receive?
A. lorazepam (Ativan)
B. phenobarbital (Luminal)
C. naloxone (Narcan)
D. ibuprofen (Motrin) A

69. Sedative-Hypnotic & Alcohol
Chapter 12
Sedative-Hypnotic & Alcohol

70. The sleep cycle is divided into two stages:
Nonrapid eye movement (NREM)
Rapid eye movement (REM)
Learning Outcomes
12.1 Describe the stages of the sleep cycle and the main characteristics of each stage.
The normal sleep cycle is divided into two different states: non-rapid eye movement (NREM) and rapid eye movement (REM) sleep.

71. Nonrapid eye movement Sleep Cycle Stage 1 Stage 2 Stages 3 & 4
Aware of surroundings but relaxed
Stage 2
Unaware of surroundings but easily awakened
Stages 3 & 4
Deeper stages of sleep, particularly important for physical rest and restoration
Learning Outcomes
12.1 Describe the stages of the sleep cycle and the main characteristics of each stage.
NREM has been divided into four stages. Progression from stage 1 to stage 4 is characterized by a deeper level of sleep and usually takes 60 to 90 minutes.
Stage 1 NREM-Individuals are somewhat aware of surroundings but relaxed; the eyes are usually closed. Alpha waves predominate in this stage. Stage 1 normally lasts a few minutes and occupies 4 to 5 percent of total sleep time.
Stage 2 NREM-Individuals become unaware of surroundings but can be easily awakened. Brain waves in stage 2 are increased in amplitude compared to alpha waves in stage 1 but occur at a lower frequency. Stage 2 occupies about 50 percent of total sleep time
Stage 3 and 4 NREM-Stages 3 and 4 are referred to as “slow-wave sleep” because of the high-amplitude, low-frequency delta waves observed on the electroencephalogram (EEG). These are deeper stages of sleep and are particularly important for physical rest and restoration. They occupy approximately 20 to 25 percent of total sleep time.

72. Barbiturate Sedatives and Hypnotics
High Doses
Depress the CNS
Increase stage 2 sleep
Decrease stages 3 & 4 sleep
Suppress REM sleep
Low Doses
Promote sedation or sleep
Learning Outcomes
12.3 Describe the adverse effects of barbiturates, the addiction liability, and treatment of barbiturate
At lower doses, the barbiturates bind to their drug receptors on the GABA receptor-mediated chloride ion channel. This increases the influx of chloride ions and results in hyperpolarization of nerve membranes. In the reticular formation, these inhibitory actions decrease the activity of the reticular activating system (RAS) and promote either sedation or sleep, depending on the dosage.
At higher doses, barbiturates also cause a general depression of the entire CNS that is similar to the actions of the general anesthetics. When used as hypnotics the barbiturates usually increase stage 2 sleep but decrease slow-wave sleep (stages 3 and 4). In addition, barbiturates suppress REM sleep.
When barbiturates are discontinued, patients often spend excess time in REM sleep during the next night or two so as to make up for the lost REM sleep (REM rebound).

73. MOA of Sedative-Hypnotic Drugs
The activity of the brain is affected by various neurotransmitters.
Main inhibitory neurotransmitter is GABA:
When GABA binds to the receptor, it inhibits neuronal activity.
Hypnotic drugs bind to these receptors and increase the inhibitory effects.
Learning Outcomes
12.2 Explain the mechanism of action of the sedative-hypnotic drugs in relationship to their actions with GABA and the chloride ion channel.
The activity of the brain is in large part dependent upon the action of various neurotransmitters. Each neurotransmitter is released from a specific nerve ending and functions to either stimulate or inhibit neuronal activity.
One of the most important inhibitory neurotransmitters is gamma-aminobutyric acid (GABA). Neuronal function is in large part also dependent upon the action of various ions such as sodium (Na+), potassium (K+), and chloride (Cl−). Each of these ions moves in through (influx) or out of (efflux) the neuronal membrane through specific ion channels.
Nerve action potentials are inhibited when Cl− ions influx through chloride channels to hyperpolarize (inside more negative) the nerve membrane. The neurotransmitter that regulates the chloride channel is GABA. When GABA binds to the GABAA receptor, the channel opens and Cl− ions influx into the nerve, causing hyperpolarization. This reduces generation of action potentials and inhibits neuronal activity.
These hypnotic drugs increase GABAA receptor-mediated chloride influx by binding to their specific drug receptor sites on the chloride channel.

74. Common Sedative-Hypnotic Drugs
Barbiturates
phenobarbital (Luminal)
Benzodiazpines
temazepam (Restoril)
Misc.
ETOH

75. Miscellaneous Hypnotic Drugs
These are a diverse group of drugs with differing chemical structures and pharmacologic characteristics.
MOA: These drugs bind selectively to a subunit of the benzodiazepine receptor to increase the inhibitory effects of GABA.
USE: They do not interrupt the sleep cycle like benzodiazepines and barbiturates do. Better sleep by patients
SE: HA, dizziness, nausea, sleep walking/eating; elderly –confusion and memory disturbances; pt may experience drug tolerance, dependency, and w/d reaction
NC: don’t stop abruptly, taper
Learning Outcomes
12.5 Explain the mechanism of action of eszopiclone, zaleplon, and zolpidem and the advantages of these drugs over barbiturates and benzodiazepines.
The miscellaneous drugs are a diverse group of drugs with differing chemical structures and pharmacologic characteristics. These drugs bind selectively to a subunit of the benzodiazepine receptor to increase the inhibitory effects of GABA.
Eszopiclone is rapidly Common adverse effects include dizziness, headache, dry mouth, and mild impairment of memory. Zaleplon is rapidly absorbed and provides a short duration of action. It is useful for individuals having difficulty falling asleep; not increasing total sleep time. Adverse effects include dizziness, headache, and minor GI disturbances.
Zolpidem is rapidly absorbed and has a rapid onset of action. It decreases awakenings during the night and increases total sleep time. Common adverse effects include headache, dizziness, and nausea. Ramelteon is classified as a melatonin agonist. Adverse effects include headache, dizziness, and minor GI disturbances such as nausea and
diarrhea.
Chloral hydrate is an old drug and is related to alcohol. The main use of chloral hydrate is as a hypnotic, particularly in the elderly. Side effects usually involve excessive CNS depression and gastric irritation

76. Miscellaneous Hypnotic Drugs
eszopiclone (Lunesta)
zaleplon (Sonata)
zolpidem (Ambien)
Learning Outcomes
12.5 Explain the mechanism of action of eszopiclone, zaleplon, and zolpidem and the advantages of these drugs over barbiturates and benzodiazepines.
The miscellaneous drugs are a diverse group of drugs with differing chemical structures and pharmacologic characteristics. These drugs bind selectively to a subunit of the benzodiazepine receptor to increase the inhibitory effects of GABA.
Eszopiclone is rapidly Common adverse effects include dizziness, headache, dry mouth, and mild impairment of memory. Zaleplon is rapidly absorbed and provides a short duration of action. It is useful for individuals having difficulty falling asleep; not increasing total sleep time. Adverse effects include dizziness, headache, and minor GI disturbances.
Zolpidem is rapidly absorbed and has a rapid onset of action. It decreases awakenings during the night and increases total sleep time. Common adverse effects include headache, dizziness, and nausea. Ramelteon is classified as a melatonin agonist. Adverse effects include headache, dizziness, and minor GI disturbances such as nausea and
diarrhea.
Chloral hydrate is an old drug and is related to alcohol. The main use of chloral hydrate is as a hypnotic, particularly in the elderly. Side effects usually involve excessive CNS depression and gastric irritation
**Zolpidem (Ambien) is a commonly used sedative-hypnotic. Question 1 refers to this slide, to compare this to benzodiazepines’ SE. **

77. Alcohol Adverse Effects
Acute inebriation:
Extensive CNS depression
Chronic consumption:
Progressive changes in cell function
Physical dependence
disulfiram (Antabuse) is used to treat alcoholism:
Interferes with metabolism of alcohol
Produces nausea, vomiting, headache, and hypotension
Most widely used, self-prescribed sedative-hypnotic and antianxiety agent
Depresses brain, dilates blood vessels, and increases excretion of urine
Is metabolized at a constant rate by the liver no matter how much is consumed
Learning Outcomes
12.6 Describe the major pharmacologic effects and adverse reactions of ethyl alcohol.
The adverse effects associated with the use of alcohol are separated into acute and chronic effects. Acute intoxication (inebriation) produces extensive CNS depression. Chronic consumption of alcohol is associated with progressive changes in cell function. Elevated blood alcohol levels for long periods result ultimately in drug tolerance and physical dependence.
Alcohol should not be consumed during pregnancy. It should never be combined with other CNS depressant medications. Alcohol is contraindicated in patients who have hepatic or renal disease, ulcers, hyperacidity, or epilepsy.
Alcohol can be used as a topical treatment for cooling effects of as a bactericidal agent.
Disulfiram is a drug used to treat chronic alcoholism. It interferes with the metabolism of alcohol. It produces nausea, vomiting, headache, and hypotension when combined with alcohol. This is known as a disulfiram reaction.
Alcohol (ethanol, whiskey, ethyl alcohol, or grain alcohol) is probably the most widely used (self-prescribed) nonprescription sedative-hypnotic and anti-anxiety agent.
After drinking alcohol, there are several effects to the body, including depression of the of the excitatory and inhibitory fibers of the brain, dilation of blood vessels, increased appetite, increased excretion of urine and can affect the nutritional state of individuals.
Unlike other drugs, alcohol is metabolized at a constant rate in the liver. No matter how much alcohol is consumed, only 10 to 15 ml of pure alcohol per hour is metabolized, which is the amount of alcohol in one beer, a glass of wine, or an average-size cocktail. This limits the amount of alcohol that can be consumed without producing intoxication.

78. Chlordiazepoxide (Librium) Temazepam (Restoril) Zolpidem (Ambien)
A nurse is caring for several clients who have prescriptions of sedative-hypnotic medications. Which of the following medications should the nurse realize had the lowest risk for causing physical dependence?
Alprazolam (Xanax)
Chlordiazepoxide (Librium)
Temazepam (Restoril)
Zolpidem (Ambien)
Correct answer is D.
Use Zolpidem (Ambien), a non-benzodiazepine medicaiton, to treat insomnia. It has a very low risk for dependence, tolerance and abuse. Alproazolam, cholrdiazepoxide, and temazepam are all benzodiazepines and may cuase physical dependence in clients. Refer to slides & 12-12

79. obsessive-compulsive disorder (OCD). Benzodiazepine overdose.
A client should receive a dose of flumazenil (Romazicon) to treat symptoms of which of the following?
obsessive-compulsive disorder (OCD).
Benzodiazepine overdose.
Panic disorder.
Serotonin syndrome.
Correct answer is B.
Flumazenil reverses the sedative effects of benzodiazepines and is used as an antidote to treat benzodiazepine overdose. It is not indicated to treat OCD, panic disorder or serotonin syndrome.
Refer to slide 12-10

80. “I should not take this medication at bedtime.”
A nurse is reinforcing teaching to a client who is prescribed diazepam (Valium) for anxiety. Which of the following statements indicates the client understands the teaching?
“I should not take this medication at bedtime.”
“I should not take this medication if I am taking acetaminophen.”
“I will tell my doctor before I stop taking this medication.”
“I will need to take this medication for the rest of my life.”
Correct answer is C.
Abrupt discontinuation of diazepam, a benzodiazepine, may cause withdrawal symptoms. The medication may need to be tapered for several weeks before discontinuing. Taking the medication at bedtime can promote sleep. There in not indication the medicaiton cannot be taken while taking acetaminophen. A shot-term course of diazepam may resolve the client’s anxiety. Life-long therapy in not always necessary.
Refer to slide s 13-27