PHARM: Unit 1: Module 1: Drugs used to Treat Anxiety & Sleep Disorders

benzodiazepines key drugs

suffix: "pam" "lam"

Diazepam (Valium)

Lorazepam (Ativan)

Midalozam (Versed)

Temazepam (Restoril)

non-benzodiazepine/misc. key drugs

Eszopiclone (Lunesta)

Ramelteon (Rozerem)

Zaleplon (Sonata)

Zolpidem (Ambien)

Buspirone (BuSpar)

barbiturates key drugs

Phenobarbital

Pentobarbital

Muscle relaxants key drugs

Baclofen (Lioresal)

Cyclobenzaprine (Flexeril)

treatment of insomnia and anxiety

many of the same types of meds are used for treating these disorders, likely to cause some drowsiness

these meds are used as aids to minimizes the feelings of distress so patients can cope with the underlying cause in anxiety and sleep disorders

sleep

a state of unconsciousness from which a person can be aroused by appropriate stimulus

this is needed to maintain psychiatric equilibrium and strengthen the immune system

-gives the body time to repair itself

-increases in serotonin help maintain healthy sleep

what are the most commonly sold OTC meds?

OTC sleep aids

phases of sleep

REM (rapid eye movement) associated with dreaming, loss of muscle tone

-most restorative sleep occurs here

NREM is divided into 4 stages

stage I of NREM

dozing off or drifting off to sleep

2-5% of sleep time

stage II of NREM

sleep is starting to get deeper. higher arousal threshold

50% of sleep time

stage III of NREM

deep sleep - difficult to wake the person

AKA - "delta sleep" very high arousal threshold (10%-15% sleep time)

stage IV of NREM

deepest form of sleep

person groggy when awakened

sleepwalking and bed wetting occur during this type of sleep (25-35% sleep)

what are factors contributing to patterns of inadequate sleep?

stress, anxiety, illness, change of environment, longer working hours, alcohol use, drug use, medication use, caffeine

insomnia

the most common sleep disorder, usually mild and short lived

common causes:

-lifestyle or environmental changes

-pain, illness, anxiety

-large amounts of caffeine

-large meals before bedtime

more common in women, can increase during certain junctures in a woman's life ex: pregnancy, postpartum, menopause

initial insomnia

difficulty falling asleep

intermittent insomnia

difficulty staying asleep

terminal insomnia

waking up and an inability to fall back to sleep

non-pharmacological treatment for insomnia

These should be implemented first to try to enhance sleep

1st: find out what the pt. is doing that may be interfering with their sleep

-Avoid caffeine

-Relaxation therapy

-Avoid daytime napping

-Get into a regular sleep schedule

-Exercise 30 minutes/day

-Take a warm bath/shower right before bed

-Complementary therapies

*develop a healthy routine

OTC medications for insomnia

these often include antihistamines and pain relievers

-have a CNS depressant effect

Benadryl, NyQuil, Tylenol PM,

herbal medicines/remedies for insomnia

Kava

Valerian

Melatonin

St. John's Wart

Chamomile Tea

Lavender

complimentary therapies for insomnia

stress & relaxation techniques such as

-yoga

-acupuncture

-meditation

-deep breathing

-prayer

*shown to be helpful for older folks in particular

culture & sleep

sleeping with pets --> American

Siesta (afternoon nap) --> Spanish

al fresco naps (Outdoor naps, even in winter) -Scandinavian

Napping in public --> Japanese

Worry dolls --> Guatemalan

hypnotic

a drug that produces sleep. Are more potent than sedatives

sedative

drug that relaxes a patient but is not necessarily accompanied by sleep

sedative-hypnotic

drug that acts as either a sedative or a hypnotic depending upon the dose and the patient's response

small dose acts as a sedative, large doses acts as a hypnotic

sedative/hypnotics

Actions: Sedatives produce increased relaxation and rest and decrease anxiety. Hypnotics produce sleep - have a more potent effect on the CNS.

Uses: Temporary treatment of insomnia, decrease anxiety and increase relaxation, before diagnostic or operative procedures.

Effect: Increase total sleeping time, mainly in stages II and IV. Decreases number of REM cycles and amount of REM sleep. May cause REM rebound when a drug is stopped

rebound insomnia

occurs when a sedative drug is discontinued abruptly or after it has been taken for a long time, and sleeplessness/anxiety become much worse

anxiety

an unpleasant state of mind characterized by a sense of fear and dread

anticipation or past experiences

normal reaction to stress

environmental factors: elements in the environment around an individual can increase anxiety. stress from a personal relationship, job, school, or financial predicament can contribute greatly to anxiety disorders

genetics: people who have family members with an anxiety disorder are more likely to have one themselves

medical factors: side effects of medication, symptoms of a disease, or stress from a serious underlying medical condition

brain chemistry: stressful or traumatic experiences and genetic factors can alter brain structure and function to react more vigorously to triggers that would not previously have caused anxiety

use of or withdrawal from an illicit substance: there are stress of day-to-day living combined with any of the above might serve as key contributors

types of anxiety disorders

1. generalized anxiety disorder

2. panic disorder

3. phobia related disorders

generalized anxiety disorder (GAD)

people with this display excessive anxiety or worry

-feeling restless, wound up, or on-edge

-easily fatigued

-having difficulty concentrating

-irritability

-muscle tension

-difficulty controlling feelings of worry

-sleep problems

panic disorder

An anxiety disorder marked by recurrent unexpected panic attacks, which are sudden periods of intense fear that come on quickly.

-heart palpitations, pounding heartbeat, and accelerated heart rate

-sweating

-trembling or shaking

-shortness of breath

-feelings of impending doom

-feelings of being out of control

phobia related disorders

An intense fear of specific objects or situations. The fear people with this feel is out of proportion to the actual danger caused by the situation or object.

-May have an irrational or excessive worry about encountering the feared object or situation.

-Take active steps to avoid the feared object or situation.

-Experience immediate intense anxiety upon encountering the feared object or situation

-Endure unavoidable objects objects and situations with intense anxiety

anxiolytics

includes Benzodiazepines & misc. drug Buspirone

-Benzodiazepines are the most commonly prescribed

Used as adjunct therapy for depression since symptoms go hand in hand

Barbituates

Mechanism of Action: Schedule 2,3,4 drugs

-CNS depressants that act in the reticular formation of the brainstem

-Effects are DOSE related

-Inhibit nerve impulse transmission by potentiating the action of GABA

Indications:

-Anesthesia for short surgical procedures

-Control of convulsions (common)

-Reduce intracranial pressure in neurosurgical patients

-Prophylaxis of epileptic seizures

-No longer used to treat sleep disorders

-Not commonly used due to efficacy and safety of benzodiazepines

barbiturates: adverse effects

deprived of REM sleep

hangover feeling, paradoxical drowsiness

dizziness

hypotension

nausea

respiratory depression

short acting barbituates

Pentobarbital (Nembutal)

Secobarbital (Seconal)

intermediate acting barbituates

Butarbital

Long acting barbituates

Phenobarbital (prototype)

Mephobarbital

benzodiazepines

most commonly prescribed sedative/hypnotic used to reduce anxiety and tension to promote sleep

wider margin of safety

preferred medications to treat anxiety and insomnia

more than 200 types

safer than barbituates

do not cause life threatening respiratory depression

shorten the time to fall asleep and reduce frequency of uninterrupted sleep

small set are used clinically

-mostly Ativan and Versed

-used as a pre-op sedative and IV sedative for diagnostic procedures ex: colonoscopy

reversal agent for benzodiazepines

Flumazenil (Romazicon)

benzodiazepines mechanism of action

Affect type 1 and type 2 GABA (gamma amino butyric acid) receptors: bind to the receptors to stimulate the release of GABA

Metabolized in the liver, excreted in urine

Schedule IV drug --> potentially habit forming

they enhance the neurotransmitter inhibitory action of gamma

individual drugs in this class are prescribed based on their site of action within the CNS

potentiate the effects of other CNS depressants (alcohol, narcotics, barbituates)

when stopped, a rebound effect may occur

nursing interventions benzodiazepines

monitor VS, especially orthostatic BP

monitor lab results for hepatic function

indications for benzodiazepines

sedation

decreased agitation/anxiety

treatment of anxiety related depression

sleep induction

treatment of acute seizure disorders

in combination with anesthetics to help reduce memory of painful procedures

given 30 minutes before bedtime if for sleep

side effects of benzodiazepines

drowsiness, sedation, lethargy, decreased alertness

hypotension

confusion, agitation, amnesia, hepatotoxicity

tolerance and habituation

*meant for short term use

contraindications/precautions of benzodiazepines

allergies

pregnancy/lactation = category X

glaucoma

children less than 18

use caution with:

renal/hepatic impairment

suicidal ideation

sleep apnea

smoking

alcohol dependency

adverse effects of benzodiazepines

-harmful if given in excessive doses - use lowest dose possible

-DO not mix with alcohol

-increased risk for falls

-hangover effects

-rebound insomnia

-paradoxical reaction in older adults

muscle relaxants

mechanism of action: works within the CNS, affects skeletal muscle by decreasing the amount of calcium released from storage sites in muscle fibers

indications: relief of painful muscle spasms (trauma, inflammation, anxiety, and pain closely associated)

multiple sclerosis

treatment of malignant hyperthermia (Dantrolene)

contraindications: allergies

muscle relaxants adverse effects

lightheadedness

drowsiness

fatigue

GI upset

miscellaneous agents for sleep

Eszopiclone (Lunesta)

Remlteon (Roseram)

Zolpidem (Ambien)

miscellaneous agents for anxiety

Busprione (BuSpar)

miscellaneous agents

actions: variable effects on REM sleep; enhance inhibitory effects of GABA

uses: sedative & hypnotic effects, used short term (7-10 days)

adverse reactions: hangover, sedation, lethargy, decreased level of alertness, anxiety

precautions: take on an empty stomach, no alcohol, contraindicated in children less than 18

most commonly used in this category: Benadryl, Ambien, Lunesta, Chlorahydrate

nursing interventions:

-VS, orthostatic BP

-lab tests for hepatic function

-pt edu no to abruptly stop these meds after long term use

-physical dependency

nursing process

-Before administering a sedative/hypnotic, determine the need for it.

-Pts with a history of sleep apnea or respiratory difficulties are at a higher risk for respiratory depression if sedative/hypnotics are taken

-History of drug/alcohol use

-Older adults may react paradoxically (opposite effect)

-Sleep patterns change when hypnotics are discontinued

-Perform ongoing monitoring for therapeutic and adverse effects

-Document findings

-Follow policies and procedures of the organization

nursing assessment

complete assessment/history (behavior, mental affect, mood, etc.)

involve pt and family in goal setting

discuss medication and benefits

vital signs (BP)

assess for increase sedation

dietary intake

avoid sudden discontinuation (withdrawal symptoms)

nursing interventions

Always try non-pharmaceutical means first!

determine activities done just before bed

ask about patient stressors

always try to provide other methods of relaxation techniques prior to sleep first (warm bath, massage, music, calm, quiet environment)

create an environment conducive for sleep

pt eduation

encourage a standard bedtime

avoid late, heavy meals

limit caffeine and alcohol intake

smoking cessation

control sleep environment

promote stress reducing techniques

discuss benefits of medication compliance and non-pharmacological interventions

Diazepam (Valium)

therapeutic class: anti anxiety agents, anticonvulsants, sedative/hypnotics, skeletal muscle relaxants (central acting)

pharmacological class: benzodiazepines

Controlled substance schedule IV

indications: treatment of anxiety, a centrally acting muscle relaxer, adjunctive analgesic, treatment of Stiff Man syndrome, preoperative sedation, conscious sedation, treatment of seizures, management of the symptoms of alcohol withdrawal

action: depresses the CNS, probably by potentiating GABA, an inhibitory transmitter; produces skeletal muscle relaxation by inhibiting poly synaptic afferent pathways, has anticonvulsant properties due to enhanced presynaptic inhibition

therapeutic effects: relief of anxiety, sedation, amnesia, skeletal muscle relaxation, decreased seizure activity

adverse effects: respiratory depression, dizziness, drowsiness, lethargy, constipation, N/V

Lorazepam (Ativan)

therapeutic class: anti anxiety agents, analgesic adjuncts, sedative/hypnotics

pharmacological class: benzodiazepines

controlled substance schedule IV

indications: anxiety disorder (PO), preanesthetic to produce sedation, decrease pre-op anxiety and induce amnesia (IM/IV)

action: depresses the CNS, probably by potentiating GABA, an inhibitory transmitter

therapeutic effects: sedation, decreased anxiety, decreased seizure

adverse effects: apnea, cardiac arrest, dizziness, drowsiness, lethargy, hangover, hypotension

Midazolam (Versed)

therapeutic class: antianxiety agent, sedative/hypnotic

pharmacological class: benzodiazepine

controlled substance schedule IV

indications: promotion of presurgical sedation and axiolyiss in pediatric clients and adult clients, commonly used for conscious sedation, aids in the induction of anesthesia and as part of balanced anesthesia, provision of sedation of mechanically ventilation clients in a critical care setting

action: acts at many levels of the CNS to produce generalized CNS depression; effects may be mediated by GABA an inhibitory neurotransmitter

therapeutic effects: short term sedation, postoperative amnesia, termination of seizure activity

adverse effects: suicidal thoughts, cardiac arrest, apnea, laryngospasm, respiratory depression, phlebitis at IV site

Temazepam (Restoril)

therapeutic class: sedative/hypnotics

pharmacological class: benzodiazepines

controlled substance schedule IV

indications: short term management of insomnia (less than 4 weeks)

action: acts at many levels of the CNS, producing generalized depression; effects may be mediated by GABA, an inhibitory neurotransmitter

therapeutic effects: relief of insomnia

adverse effects: hangover

Eszopiclone (Lunesta)

therapeutic class: sedative/hypnotics

pharmacological class: cyclopyrrolones

controlled substance schedule IV

indications: insomnia

action: interacts with GABA receptor complexes; not a benzodiazepine

therapeutic effects: improved sleep with decreased latency and increased maintenance of sleep

adverse effects: complex sleep behaviors

client should go to bed immediately after taking, as it has rapid onset

Ramelteon (Rozerem)

therapeutic class: sedative/hypnotics

pharmacological class: melatonin receptor antagonists

indications: treatment of insomnia characterized by difficult sleep onset

action: activates melatonin receptors, which promotes maintenance of circadian rhythm, a part of the sleep-wake cycle

therapeutic effects: earlier onset of sleep

adverse effects: angioedema, anaphylaxis

Zaleplon (Sonata)

therapeutic class: sedative/hypnotics

pharmacological class: hypnotics

controlled substance schedule IV

indications: short term management of insomnia in patients unable to get at least 4 hours of sleep; especially useful in sleep initiation disorders

actions: produces CNS depression by binding to GABA receptors in the CNS; has no analgesic properties

therapeutic effects: induction of sleep

adverse effects: complex sleep behaviors (sleep driving, sleep walking)

Zolpidem (Ambien)

therapeutic class: sedative/hypnotics

controlled substance schedule IV

indications: insomnia with difficulties in sleep initiation

action: produces CNS depression by binding to GABA receptors in the CNS; has no analgesic properties

therapeutic effects: sedation and induction of sleep

adverse effects: complex sleep behaviors, hypersensitivity reactions, daytime drowsiness, dizziness

Buspirone (BuSpar)

therapeutic class: anti anxiety agent

indications: management of generalized anxiety disorder

action: binds to serotonin and dopamine receptors in the brain; increases norepinephrine metabolism in the brain

therapeutic effects: relief of anxiety

adverse effects: dizziness, drowsiness, excitement, fatigue, headache, insomnia, nervousness, weakness, blurred vision, nasal congestion, sore throat, tinnitus, chest pain, palpitations, tachycardia, rashes, myalgia, incoordination, numbness, paresthesia, clamminess, sweating

Phenobarbital (Luminal)

therapeutic class: anticonvulsants, sedative/hypnotics

pharmacological class: barbiturates

controlled substance schedule IV

indications: anticonvulsant in tonic-clonic (grand mal), partial, and febrile seizures in children; preoperative sedation and in other situations in which sedation may be required, hypnotic (short term)

actions: produces all levels of CNS depression, depresses the sensory cortex, decreases motor activity, and alters cerebellar function; inhibits transmission in the nervous system and raises the seizure threshold

therapeutic effects: anticonvulsant activity, sedation

adverse effects: laryngospasm, angioedema, serum sickness, hangover

Pentobarbital (Nembutal)

therapeutic class: anticonvulsants, sedative/hypnotics

pharmacologic class: barbiturates

controlled substance schedule II

indications: hypnotic agent (short term), pre-op sedation and other situations which may require sedation, treatment of seizures

actions: Depresses the CNS, probably by potentiating GABA, an inhibitory neurotransmitter, Produces all levels of CNS depression, including the sensory cortex, motor activity, and altered cerebellar function, Anticonvulsant effect due to decreased synaptic transmission and increased seizure threshold, May decrease cerebral blood flow, cerebral edema, and intracranial pressure (IV only).

therapeutic effects: sedation and/or induction of sleep

adverse effects: laryngospasm, angioedema, serum sickness, drowsiness, hangover, lethargy

Baclofen (Lioresal)

therapeutic class: anti spasticity agents, skeletal muscle relaxants (centrally acting)

indications: PO treatment of reversible spasticity due to multiple sclerosis or spinal cord lesions, unlabeled use in management of pain in trigeminal neuralgia

actions: inhibits reflexes at the spinal level

therapeutic effects: decreased muscle spasticity; bowel and bladder function may also be improved

adverse effects: seizures, dizziness, drowsiness, fatigue, weakness, nausea

Cyclobenzaprine (Flexeril)

therapeutic class: skeletal muscle relaxants (centrally acting)

indications: management of acute painful musculoskeletal conditions associated with muscle spasm

actions: reduces tonic somatic muscle activity at the level of the brainstem; structurally similar to tricyclic antidepressants

therapeutic effects: reduction in muscle spasm and hyperactivity without loss of function

adverse effects: dizziness, drowsiness, dry mouth