Anti-anxiety Agents, Sedatives and Hypnotics Flashcards
Anxiolytics and Sedative Hypnotics
CNS depressants that have similar effects
- Produces drowsiness, sedation, possibility of respiratory depression
- Anxiolytics promote relaxation, decreased anxiety
- Sedatives/Hypnotics promote relaxation and induce sleep
- Anxiolytics used for sleeping are referred to as sedative-hypnotics
- The difference DEPENDS ON THE DOSE
- Some of these drugs, due to their CNS depressant effects, are also used as anticonvulsants and anesthetics
- Benzodiazepines are the main drug used to treat anxiety and insomnia
- Antidepressants are increasingly being used
- Barbiturates were used in the past, but due to nasty side effects and high levels of
dependence they are no longer used
Anxiolytics promote
relaxation, decreased anxiety
Sedatives/Hypnotics promote
relaxation and induce sleep
Anxiolytics used for sleeping are referred to as
sedative-hypnotics
REM sleep is the MOST important for _________________ & Non REM is _______________
mental and emotional restoration
&
physically restorative
true or false: there is a wide safety margin between therapeutic and toxic doses of benzodiazepines
true
true or false: easy to overdose on benzodiazepines
Overdose not often fatal, unless combined with another CNS depressant
Benzodiazepine
CNS depressant used for sedation, reduce anxiety, muscle skeletal relaxation,
anticonvulsant effects
- It does NOT SUPPRESS REM sleep
Benzodiazepines indications
- Anti-anxiety
- Hypnotic
- Anticonvulsant
- Pre-op sedation (pre-surgery)
- Prevention of agitation and delirium tremens (DTs) in acute alcohol withdrawal
- Anxiety/agitation associated with depression, psychosis or mania
- Often given concurrently with anti-depressants, anti-psychotics and mood stabilizers
Half Life of Benzodiazepines: Diazepam
Flurazepam, and Chlordiazepoxide
form active metabolites that have long acting half lives (greater than 24 hours) and tend to accumulate, especially in older adults or those with impaired liver function
Diazepam: Valium = 20-100 hours
Half Life of Benzodiazepines: Alprazolam, Lorazepam, Clonazepam, Oxazepam, and Temazepam
immediate acting half lives of 6-24 hours which do not have active metabolites and generally do not accumulate
Lorazepam: Ativan = 10-20 hours
Half Life of Benzodiazepines: Midazolam and Triazolam
short acting half lives of less than 6 hours
why are half lives of benzodiazepines important
- The drugs with the shorter half life are best when a rapid response is needed and tend to be preferred as the adverse effects do not accumulate
- Benzos take 5-7 days to reach therapeutic effect, and side effects also tend to manifest at the 2-3 day mark
- These effects accumulate with chronic use and persist several days after the medication is
discontinued
Diazepam (Valium) used effectively in tx of?
usual dose?
max dose?
GAD, as a muscle relaxant, and alcohol withdrawal, IV sedation, seizures
- Usual dose is 5-60mg PO/IV, divided
- Maximum dose of 60mg per 24 hours
Lorazepam (Ativan) used effectively to treat?
ususal dose? Max Dose?
GAD, agitation, alcohol withdrawal
- Usual dose is 1-6mg SL/IV, divided
- Maximum dose of 10mg per 24 hours
Midazolam (Versed)
usual dose?
Max dose?
IV only for anesthesia and sedation.
IM for severe agitation
especially in ER
- Dosage of 0.07-0.08mg per kg
- Maximum dose of 5mg per 24 hours
Clonazepam (Rivotril) used for?
usual dose?
max dose?
seizure disorder as an adjunct, panic disorder, agitation/anxiety, mood stabilizer
- Dosage of 0.5-2mg, divided
- Longer half life than Ativan, takes longer to have an effect and lasts longer
- Less dependency issues tha Ativan
- Maximum 20mg in 24 hours for seizure treatment, maximum is way lower for
anxiety
Oxazepam (Serax) used for?
usual dose?
max dose?
Anxiety, alcohol withdrawal, still used for insomnia
- Dosage of 15-30mg, often divided
- Maximum 120mg per 24 hours
Advantages of Benzodiazepines
- Therapeutic doses have little effect on consciousness
- They are relatively safe
- There are few interactions with many other drugs (except other CNS depressants)
Disadvantages of Benzodiazepines
- Potentially habit forming and addictive
- Limit to TWO WEEKS of use
- DO NOT continue use after FOUR CONTINUOUS WEEKS
- Some have long half lives and can accumulate
- Memory and intellectual impairment
- Hangover
- Reduced motor coordination (driving hazard)
- Paradoxical confusion, agitation, insomnia especially with pediatric and older adult
clients
Adverse Effects of Benzodiazepines (CNS)
CNS effects:
- Diplopia (double vision)
- Tremors
- Ataxia (impaired coordination)
- Drowsiness
- Headache
- Nausea
- Vomiting
Adverse Effects of Benzodiazepines (Autonomic effects)
hanges in libido, constipation, incontinence, urinary retention, hypotension, and tachycardia, nasal congestion
- Accumulations effects: confusion, hypoactivity, intellectual impairment
Benzodiazepine Withdrawal
- Mild symptoms
occur with 6-12 weeks use. Includes:
- Anxiety, panic, hand tremors, sweating, restlessness, insomnia, weakness, aches and pains, blurred vision, palpitations
Benzodiazepine Withdrawal
- Severe symptoms
occur when regularly taken for 4 or more months. Includes: - Irritability, agitation, nervousness, diarrhea, vomiting, sweating
- Withdrawal symptoms are caused by the abrupt removal of benzo molecules from their receptor site resulting in an acute decrease of GABA neurotransmission
- Symptoms may occur within 24 hours with short acting, 4-5 days with long acting
- To prevent withdrawal, taper the drug by 10-25% every 1-2 weeks over 4-16 weeks
Benzodiazepine Toxicity
& antidote
- Excessive sedation
- Respiratory depression
- Coma
- Treatment is flumazenil (Anexate)
- It is an antagonist which competes for the benzo receptors and reverses toxicity**
Non-Benzodiazepines sedative-hypnotics
Chloral hydrate (Noctec) and zoplicone (Imovane)
Non-Benzodiazepines: Chloral hydrate
- Oldest sedative hypnotic
- Relatively safe, inexpensive and effective
- Does not suppress REM sleep
- Tolerance develops after about 2 weeks
- Can be abused and cause physical dependence
- Also used to reduce pre-operative and diagnostic testing anxiety
- Dosage of 500-2000mg daily
Non-Benzodiazepines: Zopiclone
- Differs structurally from benzo’s but has similar effects, binds with benzo receptors
- Use for symptomatic relief of transient and short term (7-10 days) insomnia,
characterized by difficulty falling and remaining asleep, and/or early morning awakenings - Delayed onset of REM sleep, DOES NOT reduce the total duration of REM periods
- Metabolized via the cytochrome P450 system (the enzymes essential for the metabolism;
over 60 enzymes included and 6 of these enzymes metabolize all of medications) - Several drug interactions (erythromycin can increase plasma levels. Carbamazepine and
phenytoin can decrease plasma levels) - Dosage is usually 7.5mg per 24 hours (half this dose in elderly patients)
Zopiclone considerations
- Should not be prescribed in quantities longer than one month
- Risk of dependence
- OD can be fatal
- Rebound insomnia common
- Taper slowly
- Less side effects than other sedative hypnotics
Non-Benzodiazepines: Antihistamines (OTC)
- Antihistamine with sedative and anti-emetic properties is sometimes used to treat anxiety
- Primarily hydroxyzine (Atarax), but also diphenhydramine (Benedryl) and dimenhydrinate (Gravol)
- It is used for anxiety, preoperative sedation, nausea, and vomiting associated with surgery or motion sickness, pruritus and urticaria associated with allergic dermatoses
Nursing Process: Patient Teaching
- Use with caution in the elderly and pediatric populations
- Baseline VS (including orthostatic BP)
- Hypnotics: 15-30 minutes pre bedtime for maximum effectiveness
- Avoid alcohol and other CNS depressants
- Avoid grapefruit juice
how soon do symptoms of benzodiazepine withdrawal occur
- short acting
- long acting
Symptoms may occur within 24 hours with short acting, 4-5 days with long acting
- To prevent withdrawal, taper the drug by 10-25% every 1-2 weeks over 4-16 weeks
