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Anxiolytics, Sedatives , Hypnotics
Anxiolytics, sedatives: promote relaxation
Hypnotics: produce sleep
All CNS depressants with similar effects
Used (among other medications) to treat
Anxiety
Insomnia
Situational Anxiety
Normal response to a stressful situation
Can be helpful if it motivates towards constructive problem solving
Examples – job interview, exams
anxiety disorders
Severe, prolonged anxiety
Affects activities of daily life
Excessive/Exaggerated response
Insomnia
Prolonged difficulty in going and/or staying asleep
Etiology:
Medical
Neurological
Psychiatric
Environmental
Medications
Herbal Insomnia Tx - Kava
Thought to increase GABA
Adverse Rxn: ↓platelets, lymphocytes, SOB
D-D: Benzodiazepines, antiplatelet drugs, levodopa
Cautions: renal disease, thrombocytopenia, neutropenia ‘
Not used in pregnancy/lactating
Herbal Insomnia Tx - Melatonin
Influences sleep-wake cycles
Caution: hepatic disease
Adverse Rxn: confusion, headache, tachycardia
Herbal Insomnia Tx - Valerian
Thought to increase GABA
Adverse Rxn: blurred vision, cardiac issues,
Caution: hepatic disease, pregnancy
Benzodiazepines (BZD) useful for..
Short-term treatment
Anxiety disorders/insomnia
Relatively safe
Schedule IV
HUGE take away should NOT be abruptly stopped
Short, immediate & long acting
Benzodiazepine onset / half life
Medications with half-lives longer than 24 hours form active metabolites
Tend to accumulate in older adults and those with impaired liver function.
Therapeutic (and adverse) effects are more likely to occur after 2 to 3 days of therapy than initially.
short acting benzos that have a half life of less than 5 hours
alprazolam
triazolam
oxazepam
midazolam
think “ATOM”
intermediate acting benzos that have a half life from 5-24 hrs
temazepam
lorazepam
clonazepam
think “TLC”
long acting benzos with a half life exceeding 24 hrs
clorazepate, chlordiazepoxide
diazepam
flurazepam
think “Clor DF”
benzos not metabolized in the liver and safe for liver failure pts
oxazepam
temazepam
lorazepam
think “Out The Liver”
PROTOTYPE: Diazepam (Valium) MOA / pharm
Enhances the inhibitory effect of GABA
LONG ½ life (20-100 hours)
Can take up to 5-7 days
Pharm: po, IV, IM, liver excretion
Diazepam (Valium) indications
Antianxiety, hypnotic & seizures
Diazepam (Valium) BBW
dont mix benzos and alcohol
Diazepam (Valium) contraindications
Pulmonary conditions, liver disease, hx of ETOH/drug abuse in the past
Pregnancy, glaucoma
CAUTIONS: older patient, renal, hepatic
Diazepam (Valium) nursing considerations
Observe for dependence, withdrawal
Mild withdrawal occurs in ½ of patients taking the medication for 6-12 weeks
Severe more likely if taken in high doses > 4 months then DC
These medications are tapered!
Benzo Toxicity Tx
NEVER assume
Antidote: Flumazenil
IV over 15 seconds
Carries it own set of risks
Benzo Toxicity Clinical Signs
respiratory depression
inability to talk
hallucinations
blurry vision / nystagmus
low blood pressure
dizziness
confusion
drowsiness
weakness
Other Common Benzo - Lorazepam (Ativan)
Anxiety disorders, seizures (initial)
Slow onset- intermediate to prolonged action
IV, po, IM
Other Common Benzo - Alprazolam (Xanax)
Quicker onset, used orally to reduce anxiety & panic disorders
Other Common Benzo - Chlordiazepoxide (Librium)
Most commonly used in alcohol withdrawal
IM, po
NO grapefruit juice
Other Common Benzo - Midazolam (Versed)
Short acting, used preop, before procedures
IM, IV, po
BBW: Profound respiratory depression
If given for pre procedure: considered moderate sedation, must have someone who can protect the airway, must be monitored
Other Common Benzo - Temazepam (Restoril)
Sleep aid, used in the elderly, those with liver disease
Other Common Benzo - Triazolam (Halcion)
Rapid onset, should take while in bed
Liver disease is a contraindication
Non Benzo Sedative Hypnotics - Eszopiclone (Lunesta)
Approved for long-term use
½ life 6 hours, ↑sleep time and onset of sleep
Should not be used in elderly
Taken on an empty stomach, fast onset so at bedtime
Non Benzo Sedative Hypnotics - Ramelteon (Rozarem)
Used to assist with onset of sleep
Short ½ life
Non Benzo Sedative Hypnotics - Zaleplon (Sonata)
Short term use
Rapid onset of sleep, ½ life 1 hour
Non Benzo Sedative Hypnotics - Zolpidem (Ambien)
Short term use of insomnia
½ life 2.5 hours
Postpartum depression
Unipolar
Treated with psychotherapy and antidepressants
Dysthymia depression
Chronically depressed mood, plus 2 additional symptoms X 2 years
Purgatory- no mild and not major depression
General Characteristics of Antidepressants
Effective in depression
Differ in AR
Take 2-4 weeks
Given orally
Liver metabolism, interactions
MOA:
Changes in the receptors
General Characteristics of Antidepressants indications
Depression
Anxiety
Panic Disorder
Fibromyalgia
Neuralgia
General Characteristics of Antidepressants contraindications
Acute Schizophrenia
Mixed mania & depression
Suicidal tendencies
Severe renal, hepatic, CV disease
Narrow angle glaucoma
Seizures
Tricyclic Antidepressants (TCA) - Impramine
½ life 8-21 hr, liver
MOC: blocks norepi, serotonin and ACh.
Uses: 2nd line treatment
NARROW therapeutic index (2-3)
Tricyclic Antidepressants (TCA) - Impramine adverse rxn
Anti-ACh, sedation, orthostatic BP, weight gain, cardiac dysrhythmias.
Tricyclic Antidepressants (TCA) - Impramine BBW
suicidal thoughts/ideation
Selective Serotonin Reuptake Inhibitors (SSRI) - Fluoxetine (Prozac)
Long ½ life
Uses: depression, OCD, bulimia, premenstrual dysphoric disorder
Safer in older adults
Selective Serotonin Reuptake Inhibitors (SSRI) - Fluoxetine (Prozac) adverse rxn
GI, sexual, CNS stimulation
Selective Serotonin Reuptake Inhibitors (SSRI) - Fluoxetine (Prozac) caution
renal caution
Selective Serotonin Reuptake Inhibitors (SSRI) - Fluoxetine (Prozac) BBW
suicidal ideation children/adolescents/young adults
Serotonin Syndrome is a medical emergency
Serotonin-Norepinephrine Reuptake Inhibitors (SNRI) Venlafaxine (Effexor)
Uses: depression, anxiety disorders
Safe in older adults, NO use in children
Take with food
Serotonin-Norepinephrine Reuptake Inhibitors (SNRI) Venlafaxine (Effexor) BBW
suicidal ideation
Serotonin-Norepinephrine Reuptake Inhibitors (SNRI) Venlafaxine (Effexor) caution / adverse rxn
Caution: renal and hepatic
Adverse Rxn: CNS, GI, GU, CV
Serotonin-Norepinephrine Reuptake Inhibitors (SNRI) other meds
Desvenlafaxine (Pristiq)
Duloxetine (Cymbalta)
Neuropathic pain
Monoamine Oxidase Inhibitors (MOI) Phenelzine (Nardil)
3rd line
Mood elevation: 2-8 weeks
Caution in older adults, NO use in children
HUGE risk of hypertensive crisis if taken with tyramine-foods (wine, aged cheese, processed meats, beer, dried fruit, liver, sauerkraut, sourdough, soy products, yeast)
TREATMENT: phentolamine
Atypical Antidepressants Bupropion (Wellbutrin)
Depression, seasonal affective disorder, smoking cessation
Adverse Rxns: higher doses
Seizures, CNS effects
BBW: increased risk of suicide, no longer used for smoking cessation
Atypical Antidepressants Mirtazapine (Remeron)
Decreases agitation, anxiety, insomnia, migraine headaches
Must monitor for agranulocytosis
Atypical Antidepressants Trazodone
Used more for sleep and sedation
Given with food
Adverse Rxn: sedation, dizziness, edema, priapism
Often given in tandem with other meds
Bipolar Disorder
Characteristics alternating moods between depression or overexcitement
Bipolar I
M:F, major depression with mania
Bipolar II
F>M, major depression with hypomania
There is a genetic link
Onset 20-25 years
Treatment:
Mood stabilizers & some may require neuromodulation therapy
Mood Stabilizers Lithium
MOA: unknown
Route: oral, effect 7-10 days
Renal/cardiac & thyroid must be ok
Contraindications: Pregnancy D (there is potential harm to the unborn baby if the medication is used during pregnancy, but in some cases, the benefit of using the medication may outweigh the risks)
Narrow therapeutic index ( .5-1.2)
Adverse Rxn: metallic taste, polyuria, polydipsia, muscle weakness, tremors, diarrhea
Aripiprazole (Abilify)
Monotherapy for mixed bipolar
Headache NV sedation
BBW: compulsive/uncontrollable urges
Children 8-17
Olanzapine (ZyPREXA)
Monotherapy
Dose related
BBW: DRESS (Drug Reaction with Eosinophilia and Systemic Symptoms. It can cause rash, fever, and organ damage, and it needs immediate medical attention.)
Quetiapine (Seroquel)
Bipolar & Schizophrenia
Given on an empty stomach
Risperidone(Risperdal)
Atypical antipsychotic
IM or po
Adolescent 10-17 Type I
BBW: ↑ mortality in elderly with dementia related psychosis
Ziprasidone (Geodon)
Atypical antipsychotic
Psychosis
Severe mental disorder
Emotional
Behavior
Hallucinations
Schizophrenia- auditory
Delirium: tactile or visual
Dementia: visual
Paranoia
Can be acute or chronic
Schizophrenia
Thought to be related to intrauterine event, strong genetic link
M:F
Clinical Domains
Delusions
Hallucinations
Disorganized speech
Grossly disorganized motor
Antipsychotics
Reduce psychotic symptoms
Bind to dopamine
Can be given orally, IM, some are given as a long-acting IM
Children present with more severe symptoms
Classified by generation & nonphenothiazines or phenothiazines
1st Generation Antipsychotics Phenothiazine - Chlorpromazine
Indication: excessive anxiety
Route: po IM
Pharm: liver, duration 4-6 hours
Caution: renal/liver, older
1st Generation Antipsychotics Phenothiazine - Chlorpromazine adverse rxn
Tardive dyskinesia - involves involuntary movements, such as repetitive facial grimacing, tongue protrusion, or rapid blinking
Akathisia - feelings of restlessness and an inability to sit still
Dystonia - involuntary muscle contractions, leading to repetitive or twisting movements and abnormal postures
CV, Heme, drug-induced Parkinsonism
Neuroleptic malignant syndrome
1st Generation Antipsychotics Phenothiazine - Chlorpromazine drug to drug
multiple, NO kava
1st Generation Antipsychotics Phenothiazine - Chlorpromazine nursing considerations
Need ECG prior to administration
Usually given with benztropine (Cogentin)
Must keep patients in a safe environment
Assess for fluid deficit & urinary retention – strict I&O
Monitor CBC
Monitor LOC
1st Generation Nonphenothiazine Haloperidol (Haldol)
Uses: excessive anxiety
Route: po, IM duration 4-8 hours
Pharm: liver
Adverse Rxn: same as Chlorpromazine
cautions: renal, liver
1st Generation Nonphenothiazine Haloperidol (Haldol) drug to drug
↑ETOH, CNS depressants, antidepressants, antihistamines, NSAIDS, ACE inhibitors, lithium ↓Antacids, Rifampin
1st Generation Nonphenothiazine Haloperidol (Haldol) BBW
none in older adults with dementia induced psychosis; EPS (extrapyramidal symptoms. These symptoms may include muscle stiffness, tremors, and abnormal movements.) and withdrawal in infants
1st Generation Nonphenothiazine Haloperidol (Haldol) nursing consideration
Given with full glass of water
IM (no more than 3 ml), deep, large muscle, must be stored in a light protected vial
Assess for sedation, tachycardia, onset of neuroleptic malignant syndrome (high fever, muscle stiffness, confusion, and other symptoms like sweating and fast heart rate. NMS can be life-threatening and requires immediate medical attention.)
2nd Generation Atypical Antipsychotics Clozapine (Clozaril)
Route oral
MOA: unknown
Pharm: ½ life 12 hours, liver
Caution: hepatic
2nd Generation Atypical Antipsychotics Clozapine (Clozaril) BBW
risk of death in older patients w/dementia
Risk of seizures in ↑doses
Agranulocytosis, hyperglycemia
2nd Generation Atypical Antipsychotics Clozapine (Clozaril) contraindications
CNS depression, seizures, CV disease, acute narrow-angle glaucoma, uncontrolled DM, hx of agranulocytosis
2nd Generation Atypical Antipsychotics Clozapine (Clozaril) adverse rxns
CV: Hypotension, tachycardia, myocarditis
GI: constipation
Heme: ↓neutrophils
DM: weight gain & hyperglycemia
2nd Generation Atypical Antipsychotics Clozapine (Clozaril) nursing considerations
Baseline CBC, blood sugar
Must be tapered.
Olanzapine (ZyPREXA)
Schizophrenia, mixed bipolar
Adverse Rxn: leukopenia/neutropenia, EPS (extrapyramidal symptoms. These symptoms may include muscle stiffness, tremors, and abnormal movements.) , drowsiness, elevated LFTs
D-D: Multiple, foods grilled meat, cabbage, broccoli, St John’s Wort
Lurasidone (Latuda)
Schizophrenia/bipolar
BBW: older adults w/dementia
Adverse Rxn: same as Olanzapine
D-D: ketoconazole, rifampin