CNS Depressants & Stimulants

Treatment for anxiety

• Antidepressants

  • If s/s over 2 weeks

  • Preferred first line

• Benzodiazepines

  • Mostly short-term Tx

  • Long term tx

    • Second line

Benzodiazepines Examples

• Used for anxiety

• Diazepam (Valium)

• Lorazepam (Ativan)

• Alprazolam (Xanax)

• Midazolam (Versed)

Benzodiazepines

• Used for anxiety & other indications

• Wide therapeutic index

• Schedule IV

  • Controlled substance

  • Long term use can cause dependance

  • Can cause tolerance 

• DO NOT STOP ABRUPTLY

  • Withdrawal s/s will occur

  • Taper gradually

  • if we stop abruptly, and pt has a history of a seizure disorder, the patient may get a seizure 

Benzodiazepines Pharmacokinetics 

• Long half-life

• Requires 5-7 days to reach steady-state serum levels

• Highly protein bound

• IV = works fast = 1-5 minutes

Benzodiazepines with older adults

• Metabolize slower 

• May be more sensitive to effects

• May contribute to falls

• Start slow and taper up gradually

Benzodiazepines used in critical care

• To relieve stress/anxiety/agitation

• Calming effect decreases cardiac workload

• Helps with tolerating treatment

  • Esp. ventilator

Benzodiazepines Adverse Effects

• Dizziness

• Drowsiness

• Depression w/wo suicidal ideation

• Diminished sexual interest

• Dry mouth

• Slurred speech

• Shallow breathing

• Memory/confusion issues

• Restlessness

• Irritability

• Loss of bladder control

• Rash/itching

Benzodiazepines Contraindications

• COPD

• Severe liver/kidney disease

• Hx of ETOH or other drug abuse

• DO NOT combine with alcohol

• Pregnant/breast feeding

• Concurrent use with any other CNS depressants

• Hypersensitivity reaction

Benzodiazepine Overdose Treatment 

• Flumazenil (Romazicon) to reverse overdose of benzodiazepines

Benzodiazepines Black Box Warning

• Do NOT combine with opioid analgesics

• That combo increases risk of serious adverse reactions including DIB and death

Other uses for Benzodiazepines

• Pre-procedural

  • Preoperatively we usually give Midazolam (Versed)

  • Sedation

  • Seizure cessation

• Psychotic episode

• Alcohol withdrawal (DT prevention)

  • DT = delirium tremens 

• Back pain/muscle spasms

Depression

• Deficiency of norepi and/or serotonin

• Clinical depression is suspected if symptoms persist for more than 2 weeks & they interfere with daily living  

Factors affecting depression

• Depression affects:

  • 50% more women vs men

  • Older Adults 

    • it is not a normal part from aging however a lot of older adults do benefit from antidepressants

• Factors:

  • Environmental factors

  • Immune factors

  • Genetics 

Clinical Manifestation Depression

• Agitation

• Anxiety

• Panic attacks

• Insomnia

• Irritability

• Hostility

• Impulsivity

• Akathisia (urge to keep moving)

• hypomania, mania

  • mania isnt only for depression, it can also be for bipolar disorder 

• Hypersensitive or exaggerated responses

• Suicidal ideations/attempts

What does serotonin affect?

• Sleep

• Mood

• Appetite

• Energy level

• Cognitive & psychomotor functions

Treatments for depression

• Tricyclic Antidepressants (TCA)

• Selective serotonin reuptake inhibitors (SSRIs)

• Serotonin-norepinephrine reuptake inhibitors (SNRIs) 

• Monoamine oxidase inhibitors (MAOS)

• Atypical antidepressants

• Mood-stabilizing agents

Tricyclic antidepressant examples (TCA)

• Imipramine (Tofranil)

• Amitriptyline

Selective Serotonin Reuptake Inhibitors Examples

• Fluoxetine (Prozac)

• Paroxetine (Paxil)

• Citalopram (Celexa)

• Escitalopram (Lexapro)

• Sertraline (Zoloft)

Serotonin-norepinephrine reuptake inhibitors examples

• Venlafaxine (Effexor XR)

• Duloxetine (Cymbalta)

Atypical Antidepressants Examples

• Bupropion (Wellbutrin XL)

• Mirtazapine (Remeron)

• Trazodone

Mood-stabilizing Agents Examples

• Lithium carbonate (Lithobid)

• Olanzapine (ZyPREXA)

• Aripiprazole (Abilify)

• Quetiapine (Seroquel)

Characteristics of Antidepressants

• Takes 2-4 weeks minimally to see improvement.

  • Have extensive first-pass metabolism before passing into the systemic circulation

• DO NOT STOP ABRUPTLY

  • Can cause antidepressant discontinuation syndrome

  • Taper off over 6-8 weeks to avoid these issues (unless anaphylaxis or other life-threatening condition arises.

Antidepressant Discontinuation Syndrome

• Flu like s/s

• imbalance

• sensory issues (whirling or fan sound in their ears)

• hyperarousal

Choice on which drug to take depends on several factors 

• Patients age, medical condition, previous hx of drug response (if any)

• Often they consider the specific adverse effects from the drug chosen

• Cost

Other uses for antidepressants

• Anxiety

• Nerve pain

  • Esp. neuropathy

• Eating disorders

• Obsessive-compulsive disorder

Tricyclic Antidepressants (TCAs)

• Blocks reuptake and Increases the action of norepinephrine and serotonin

• Peak levels in 2-6 hours

• not a first line med, but may be second 

Tricyclic Antidepressants (TCAs) Adverse Effects 

• Sedation

• orthostatic hypotension

• dysrhythmias

• anticholinergic s/s

• weight gain

Tricyclic Antidepressants (TCAs) Black Box Warning

Increased risk of suicidal ideations up to 24 yrs of age

Older Adults on Tricyclic Antidepressants 

• Watch for anticholinergic effects

• May aggravate other conditions

• Monitor VS, serum drug levels and ECG regularly

Tricyclic Antidepressants (TCAs) Cautions

• Clients with liver issues

• Do not stop abruptly - wean

• Preop: Reacts with anesthesia

  • Must stop several days prior to sx

• Not for use in pregnancy

Tricyclic Antidepressants (TCAs) Nursing Implications

• Take at bedtime

• No grapefruit juice & no alcohol

• Start with small dose increase to full dose over 1-2 weeks

• Draw drug/Plasma levels

• Interacts with many meds

Selective serotonin reuptake inhibitors (SSRIs)

• Blocks reabsorption of neurotransmitter serotonin in the brain

• Peak levels in 6-8 hours

• Steady state is slow over weeks

• Crosses into breast milk

• Fewer side effects than TCA’s

Selective Serotonin Reuptake Inhibitors other uses

• anxiety

• OCD

• bulimia nervosa

• premenstrual dysphoric disorder (PMDD)

  •  super painful; cramping & mood

    • similar to PMS but its far worse

Older Adults Taking Selective Serotonin Reuptake Inhibitors

• Drug of choice r/t less anticholinergic effects

• Elimination of drug is slower

  • may need smaller doses 

Selective Serotonin Reuptake Inhibitors Cautions

• Clients with liver issues

• Do not stop abruptly - wean

• Preop: Reacts with anesthesia/use with caution

• Caution with pregnancy

• Shouldn’t take these with NSAIDs, Aspirin, Clopidogrel or anticoagulants

  • increased risk for bleeding

Selective Serotonin Reuptake Inhibitors Black Box Warning 

• Increased risk of suicidal ideations up to 24 yrs of age

Selective Serotonin Reuptake Inhibitors Adverse Effects

• GI s/s

• GI bleed

• Sexual dysfunction

  • decreased sex drive

• CNS stimulation

• Hypoglycemic effect in DM patients

• Serotonin syndrome

• Can’t combine with MAO inhibitor, other SSRIs, or SNRI

Selective Serotonin Reuptake Inhibitors Contraindications

• Known sensitivity to MAO inhibitors or thioridazine

Serotonin Syndrome

• too much serotonin

  • treatment: we stop the ssri & we treat the symptoms 

Serotonin Syndrome Signs & Symptoms

• Changes to mental state

• Dry mouth

• Sweating or fever.

• Hyperthermia and shock-

• Diarrhea or nausea

• Tremors or reflex changes

• Muscle rigidity

Selective Serotonin Reuptake Inhibitors Nursing Implications

• Watch compatibility

• Take in the morning

• Take with food

• Use sugar-free gum/candies for dry mouth

• Discontinue slowly

Serotonin-Norepinephrine Reuptake Inhibitors

• Inhibits uptake of norepinephrine, serotonin, and dopamine

• Crosses placenta and enters breast milk

• Similar to SSRI for therapeutic effects

Serotonin-Norepinephrine Reuptake Inhibitors Uses

• depression

• anxiety

• social phobia

• panic disorders

Serotonin-Norepinephrine Reuptake Inhibitors Black Box Warning

• Increased risk of suicidal ideations up to 24 yrs of age

Serotonin-Norepinephrine Reuptake Inhibitors Adverse Effects

• Increased nervousness or anxiety 

• insomnia, dreams

• anorexia (decrease in appetite), weight loss

• sweating & itching 

• Vasodilation = lowers blood pressure

• Genitourinary

• Hostility

Serotonin-Norepinephrine Reuptake Inhibitors Contraindications

• Known sensitivity to MAO inhibitors

• Use of MAO inhibitors

• Pregnancy

Serotonin-Norepinephrine Reuptake Inhibitors Nursing Implications

• Take with food

• Can open capsules & put in applesauce

• Take am/pm at the same time

  • something like 8:00am; 8:00pm

Older Adults Taking Serotonin-Norepinephrine Reuptake Inhibitors

• Potential unwanted weight loss

• Recommend smaller initial dose / increase gradually

• Risk of SIADH or hyponatremia

  • SIADH = syndrome of inappropriate antidiuretic hormone 

    • pt is holding water; diluting sodium

  • Monitor sodium levels

Serotonin-Norepinephrine Reuptake Inhibitor Cautions 

• Clients with liver/kidney issues

• Do not stop abruptly - wean

Bupropion (Wellbutrin)

• Inhibits reuptake of serotonin and norepinephrine

• Peak plasma level after 2 hours

• Similar to SSRI for therapeutic effects

Bupropion (Wellbutrin) Uses

• Tx of depression

• SAD

  • Seasonal Affective Disorder

• smoking cessation

• Used often in addition to SSRI if not getting enough response alone

Bupropion (Wellbutrin) Cautions

• May cause seizures w/ high doses or previous seizure disorder

• CNS stimulant effects

• dry mouth

• Reduce doses in renal/hepatic patients

• Risk of congenital malformations during pregnancy

Bupropion (Wellbutrin) Black Box Warning

• Neuropsychiatric reactions if used for smoking cessation

  or discontinuation of the drug

Mirtazapine (Remeron)

• Blocks multiple receptors which increase release of norepinephrine

Mirtazapine (Remeron) Uses

• depression

• anxiety

• agitation

• insomnia

• migraines

Mirtazapine (Remeron) Adverse Effects

• Dizziness

• Drowsiness

• increased appetite

• wt gain

• dry mouth

• constipation

Mirtazapine (Remeron) Nursing Implications

• DO NOT take concurrently with MAO inhibitor, ETOH, benzo, or any other antianxiety or hypnotic agents r/t increased sedation

• Report any c/o sore throat, stomatitis or signs of infection

• Monitor for agranulocytosis or severe neutropenia

  • Neutropenia = agranulocytosis

    • low WBCs; pt is at risk for infection 

    • pt must report any signs of infection

Trazodone

• For sedation and sleep more than depression

• Higher doses needed for antidepressant effects which can cause excessive sedation

• Often given concurrently with other drugs for depression

Trazodone Nursing Implications

• Administer with food for max absorption

Trazodone Adverse Effects

• Sedation

• dizziness

• edema

• dysrhythmias

• priapism

Lithium carbonate (Lithobid)

• Drug of choice to treat & prevent manic episodes

• these are used for bipolar disorder

  • bipolar disorder pts have manic episodes

• this drug is given for long term therapy 

• Narrow therapeutic index

• we dont want to take this with diuretics either

Manic

• mood is either very high or very low 

• manic = hyperactive, you feel invincible, pt may stop taking meds and become hypomanic 

  • hypomania = very low mood 

• Manic patients have a decreased need for sleep

Lithium carbonate (Lithobid) Special Considerations

• Baseline renal/cardiac/thyroid status

• Baseline electrolytes (esp. sodium)

• When therapy begins you need levels 2-3 times per week in the morning and after the last dose at night

• Serum lithium levels every 3 months during maintenance therapy

Lithium carbonate (Lithobid) Adverse Effects

• Metallic taste

• N/D

• Polyuria (increased urination)

• Polydipsia (increased thirst)

• Muscular weakness

• Hand tremors

• Fatigue

• Dehydration = Lithium toxicity risk increase

• Edema

• Weight gain

Lithium carbonate (Lithobid) Contraindications

• Pregnancy as cardiac malformations common

Lithium carbonate (Lithobid) Nursing Indications

• Watch compatibility

• Take at night

• Take with food

• Use sugar-free gum/candies

• Discontinue slowly

• Start low dose and increase gradually

• Must get serum drug levels for correct dosage

  • Narrow therapeutic index

• Do not take with diuretics

Aripiprazole (Abilify)

• Treats mania phase of bipolar disorder

Aripiprazole (Abilify) Adverse Effects

• HA

• dizziness

• somnolence

• sedation

• fatigue

• N/V

Aripiprazole (Abilify) Black Box Warning

• Abilify: risk of compulsive or uncontrollable urges to gamble/shop/eat/sex

Olanzapine (Zyprexa)

• Treats manic phase of bipolar disorder

• In combo with other drugs for depression

Olanzapine (Zyprexa) Adverse Effects

• Somnolence

• extrapyramidal symptoms

• dizziness

• wt gain

• constipation

• dry mouth

• DO NOT use if pregnant

Extrapyramidal Symptoms

• lip smacking

• dyskinesia (difficulty in walking)

• involuntary contractions 

Olanzapine (Zyprexa) Black Box Warning

• DRESS

  •  low eosinophils, we need to monitor for this 

• decreased reproductive function both male/female

• rash

• exfoliative dermatitis

• pancreatitis

• nephritis

• pneumonitis

Quetiapine (Seroquel)

• Antagonist on serotonin and dopamine

• Antipsychotic for bipolar and schizophrenia

Quetiapine (Seroquel) Adverse Effects

• dizziness,

• Drowsiness

• vision issues,

• fatigue,

• weight gain

• Decreased reproductive function in male/female

Quetiapine (Seroquel) Nursing Implications

• DO NOT give with food – will increase serum levels

• DO NOT give if pregnant

Psychosis

• Can Be Acute or Chronic

• Can be sudden onset or gradual

• May be precipitated by drug/ETOH intoxication and/or withdrawal

• May be precipitated by physical disorders

• Also called "confusion" or "delirium"

• Schizophrenia has periods of psychosis 

Goal for psychosis therapy 

• Takes 1-2 months

• Relieve symptoms w/ minimal or tolerable adverse effects

• Decrease symptoms (aggression, agitation, combativeness, hostility

• Normalize patterns of sleeping and eating

• Increase ability for self-care

• Increase socialization

• Long term goal to increase coping and prevent acute episodes/hospitalizations

Haloperidol (Haldol)

• First Generation Antipsychotic

• Blocks postsynaptic dopamine receptors

• Control symptoms of psychotic disorders & schizophrenia 

Haloperidol (Haldol) Black Box Warning

• Increased risk of death in older adults with dementia or 

  dementia related psychosis

Haloperidol (Haldol) Routes

• Oral: onset 2 hours

• IM: onset 20-30 minutes

  • IM = sometimes we cant get an IV on patients when their behavior isn't under control 

Haloperidol (Haldol) Adverse Effects

• Cardiovascular effects:

  • abnormal T waves, prolonged ventricular depolarization, QT prolongation, torsade de pointes, tachycardia, and sudden death

• CNS effects:

  • akathisia, hyperthermia, dystonia, extrapyramidal effects, neuroleptic malignant syndrome, parkinsonism, seizures, and vertigo

• Dermatologic effects:

  • photosensitivity, hyperpigmentation, contact dermatitis, and alopecia

• Genitourinary effects:

  • anticholinergic adverse effects such as urinary retention, sexual dysfunction, amenorrhea, breast engorgement and galactorrhea (women), and priapism and gynecomastia (men)

• Metabolic effects:

  • hyperglycemia, hypoglycemia, and hyponatremia

• Respiratory effects:

  • bronchospasm or laryngospasm

Haloperidol (Haldol) Contraindications

• Parkinson's

• Seizure disorders

• Severe depression

Haloperidol (Haldol) Nursing Implications

• Take with full glass of water or milk

• Take with food

• Keep in light protected container

• Periodic renal & hepatic function monitoring

• Discontinue slowly

• Many drug interactions

  • ETOH, NSAIDS, Antacids

ADHD

• Persistent hyperactivity

• Impulsiveness

• Short attention span

• Restlessness

• Difficulty completing assigned tasks

Dextroamphetamine and amphetamine (Adderall)

• Amphetamines

• Management of ADHD and narcolepsy

• Increases amounts of norepinephrine and dopamine in the brain

• Suppresses appetite, increases alertness, elevates mood, improves physical performance

Dextroamphetamine and amphetamine (Adderall) Black Box Warning 

User must be aware of potential for misuse and for sudden death or serious cardiovascular events

Dextroamphetamine & amphetamine (Adderall) Adverse Effects

• Agitation

• confusion

• hyperactivity,

• difficulty concentrating,

• nervousness.

• anxiety,

• restlessness,

• insomnia

• Can cause sympathetic nervous system stimulation

  • Increased heart rate,

  • increase BP,

  • pupil dilation,

  • slowed Gl motility

• Nausea,

• constipation or diarrhea,

• weight loss

• anorexia  

• Cardiovascular = can cause tachycardia, dysrhythmia, 

  • Monitor ECG, BP, esp if pt has history of cardiovascular disorders 

• Schedule II: high incidence of abuse and dependence

  • Commonly misused and sold on the street

Dextroamphetamine & amphetamine (Adderall) OD

• can result in:

  • psychosis,

  • convulsions,

  • CVA,

  • cardiac arrest

  • death

Dextroamphetamine & amphetamine (Adderall) Contraindications

• Angina, dysrhythmias, HTN

• Anxiety/agitation

• Glaucoma

• Hyperthyroidism

• Hx of drug abuse

• Pregnancy/lactation

Dextroamphetamine & amphetamine (Adderall) Nursing Implications

• 1st dose: Take upon awakening or early in the day Last dose: 6 hours before bed

• Obtain baseline EKG

• Capsules may be opened and added to food

  • Optimal to take 45 min before meal to minimize appetite suppression effects

Things that increase the effects of Dextroamphetamine & amphetamine (Adderall)

• Albuterol, TCAs, antacids & MAOIs increase the effect

Things that decrease the effects of Dextroamphetamine & amphetamine (Adderall)

• Caffeine/acidic food/juices decrease the effect

Methylphenidate (Ritalin)

• Amphetamine related CNS stimulant

• Management of ADHD and narcolepsy

• Blocks reuptake of norepinephrine and dopamine

• Suppresses appetite, increases alertness, elevates mood, improves physical performance

Methylphenidate (Ritalin) Black box warning 

• User must be aware of risk for drug dependence, abuse, also responsible for increased ED visits

Methylphenidate (Ritalin) Adverse Effects

• Cardiovascular

  • Tachycardia

  • dysrhythmias

  • HTN

• CNS

  • Anxiety,

  • Hyperactivity,

  • Nervousness

  • Insomnia

  • Tremors

  • Convulsion

  • Psychosis

• GI

  • Gastritis,

  • N/D

  • Constipation

  • Anorexia

  • Weight loss

• Dermatologic

  • Rash

  • Alopecia

  • Exfoliative dermatitis

• Hematologic

  • Leukopenia (decreased WBC)

  • Anemia (Decreased Hemoglobin)

Methylphenidate (Ritalin) Contraindications

• Angina, dysrhythmias

• Agitation

• Glaucoma

• Hyperthyroidism

• Pregnancy

• Drug abuse history

• CAUTION with seizure disorders

Methylphenidate (Ritalin) Nursing Implications

• 1st dose: Take upon awakening or early in the day, Last dose: 6 hours before bed

• For kids: “drug holiday” when not in school

  • give them a break from the med