[Pharm] Week 12 Sleep Aids & Muscle Relaxants (unfinished)

Patients should heed caution using muscle relaxants with ___________

CNS depressants such as antihistamines, opioids, benzodiazepines, sedatives, hypnotics because they affect the CNS and could potentially increase respiratory depression

What is Kava used for?

Kava is an herbal supplement commonly used to reduce anxiety & insomnia by increases GABA activity & inhibiting noradrenaline. Kava causes sedation, analgesia, impaired gait, & pupil dilation Kava interacts with Benzodiazepine

The patient must have a healthy ___________ to use Ramelteon

Liver

Where is Ambieen metabolized and excreted?

Liver & kidneys

Sedative-Hypnotic drugs induce a calming effect at _____ doses while inducing sleep at _____ doses.

Low; High

Ramelteon (Rozerem) is a ______ agonist and is classified as a nonbenzodiasepine ________.

Melatonin; hypnotic

Ramelteon is contraindicated in people with

COPD, sleep apnea

If benzodiazepine is indicated for Hypnotics, then dosage frequency should: A. start with smallest dose likely to be effective and only titrate if tolerance occurs B. the lowest effective dose taken continuously, then titrate up after 2 weeks C. 15-30 mg PO D. be the lowest effective dose taken on an intermittent basis to prevent "hangover" effect

D.

Which Muscle Relaxant is the only direct acting muscle relaxant?

Dantrolene (Dantrium)

Why should the patient take eszopiclone immediately prior to going to bed?

Due to its rapid onset of action. Lunesta is rapidly absorbed after oral administration, reaching peak plasma levels 1 hour after administration & has a half life of 6 hours.

What is the only nonbenzodiazepne approved for long-term used?

Eszopiclone (Lunesta), long term use is considered less than or equal to 12 months

What are adverse effects of Muscle Relaxants?

Euphoria, lightheadedness, dizziness, drowsiness, fatigue, muscle weakness

People should not eat foods high in _______ when using Ramelteon (Rozerem) because food will delay the otherwise normally rapid oral onset

Fat

What is the most serious adverse effect of Dantrolene (Dantrium)?

Fatal hepatitis, with jaundice and other symptoms that usually occur within 1 month of start drug therapy

What are the [7] Adverse Effects of Benzodiazepines?

Headache "Hangover" effect/daytime sleepiness Drowsiness Dizziness Vertigo Lethargy Fall hazard (older adult)

what type of diets should a person avoid when prescribed Lunesta?

High-fat meals and diets. This is because the onset of action may be delayed by approximately 1 hour.

What is the function of a Sedative?

"Calming effect;" To promote relaxation and ease agitation.

What are some interactions of Benzodiazepines?

1. other CNS depressants (alcohol, opioids): will exacerbate respiratory depression 2. MAOIs: strong anti-depressants such as Prozac, Zoloft, Lexapro, & Paxil 3. Herbal products: Kava, Valerian, & Chamomile 4. Grapefruit: decreased metabolism and absorption of benzo, increasing toxicity

Diazepam's half-life is ________ hours & requires _______ days to reach steady state.

20-100 ; 5-7

Hypnotics should not be taken more than ______ nights per week, for ____ weeks.

3-4; 3

Ramelteon peaks in about ___________.

45 minutes

Sleep Aids should be used- A. short term, unless indicated B. long term, unless indicated

A. short term, unless indicated This is because sleep aids can develop physical dependency.

What is REM rebound?

REM rebound is considered an over abundance of REM sleep. This usually occurs in people who are sleep deprived for a prolonged amount of time, causing them to enter REM faster and more frequently than normal adults once they eventually sleep.

What are [2] indications of muscle relaxants?

Relief of painful musculoskeletal spasms Management of spasticity of severe chronic disorders (MS, cerebral palsy)

_____________ insomnia may occur for a night or two after stopping _________ & withdrawal symptoms may occur if it is stopped abruptly after approximately one week of regular use

Round ; 1-2 nights

During the sleep cycle, older adults spend more time in ________ and less time in __________.

Stage 2; REM sleep

What is a muscle spasm?

Sudden, involuntary, painful muscle contraction

What is valerian?

a root thought to have anxiolytic and hypnotic property by increase the amount of GABA in the brain, an inhibitory neurotransmitter, resulting in calming sedative effects Should not be taken if person has hepatic impairment, pregnant, or taken with CNS depressants.

What is the indication for Carisoprodol (Soma)?

relief of discomfort associated with acute painful musculoskeletal condition in which no alternative measure has relieved (rest, physical therapy, etc.)

What is the goal of Muscle relaxant treatment?

relieve pain, muscle spasms, and muscle spasticity without impairing ADLs/IADLs

Therapeutic doses of hypnotics taken at bedtime may have residual ______ effects

sedative

Treatment for Benzodiazepine overdose is

symptomatic & supportive the antidote (Flumazenil [Romazicon]) is usually reserved for patients on multiple CNS depressants

Mild & Infrequent Adverse effects of Benzodiazepines will occur if . . .

take short term at prescribed dosages

What is Baclofen used for?

to alleviate signs and symptoms of spasticity in patients with multiple sclerosis (flexor spasms, concomitant pain, muscular rigidity)

Dantrolene is contraindicated in patients with

active liver disease spasticity used to maintain an upright position, balance, and rheumatic conditions (inflammation affecting joints and connective tissue of the body)

What are the adverse effects of Eszopiclone (Lunesta)?

adverse effects include behavior changes such as reduced inhibition, aggression agitation, short-term memory loss (anterograde amnesia), worsening depression & suicidal ideation, hallucinations

What is the indication use for Dantrolene (Dantrium)?

alleviate spasticity related to multiple sclerosis, cerebral palsy, spinal cord injury and stroke

Small does of hypnotics have ____________ & _____________ effects.

anti anxiety & sedative .

Carisoprodol (Soma) is a _______ acting skeletal muscle relaxant

centrally. inhibits spinal reflexes

Baclofen is a _________ acting musculoskeletal relaxant

centrally. it is a GABA agonist which restricts the amount of calcium transferring to create excitatory action potentials

Cyclobenzaprine HCL (Flexeril) is a __________ acting

centrally. used for short-term basis for muscle spasms

Caution is warranted in patients with ____________ using Ramelteon as it can exacerbate suicidal ideations

depression

Ramelteon (Rozreem) is for treatment of insomnia characterized by

difficulty with sleep onset

Dantrolene (Dantrium) is a ______ acting muscle relaxant

direct. interferes with relate of calcium to skeletal muscles. does not affect neurotransmitter levels

Eszopiclone [does/ does not] reduce nighttime awakenings

does not

What are the contraindications of Lunesta?

hypersensitivity, depression, impaired hepatic or respiratory function, elderly patients (especially those with hepatic impairment or debilitating conditions) & those taking certain medications (antidepressants, antifungals, erythromycin, grapefruit, protease inhibitors, etc.)

Zolpidem (Ambien, Ambien CR) is a nonbenzodiazepine ___________

hypnotic

Muscle Relaxants are contraindicated in

impaired renal or hepatic function, respiratory depression or disorders, patients who required alertness for ADLs or occupation

What is muscle spasticity

increased muscle tone or contraction & stiff, awkward movements

Ramelteon (Rozerem) does not cause CNS depression, there it [is/ is not] classified as a controlled substance

is not

The majority of benzodiazepine metabolites are excreted through. . .

kidneys

Severe anxiety or agitation requires [larger/more frequent/discontinued/titrated] doses of benzodiazepines

larger-than-usual doses

Benzodiazepines are most given _______ but can be given ______ or ________>

orally ; orally; parenterally

Cyclobenzaprine HCL (Flexeril) is an adjunct to _______

physical therapy

Patients with liver dysfunction are at risk for _______ effects using benzodiazepines because benzodiazepines are metabolized in the _________

potentially unintended hypnotic; liver

When benzodiazepine causes toxicity and overdose, [4] adverse effects occur:

1. Somnolence 2. Confusion 3. Coma 4. Diminished Reflexes

What are [5] commonly used Muscle Relaxants?

1. Baclofen (Lioresal) 2. Cyclobenzaprine (Flexeril) 3. Dantrolene (Dantrium) 4. Tizanidine (Zanaflex) 5. Carisoprodol (Soma)

What [3] qualities make Benzodiazepines the most common Sedative-Hypnotic drug class used?

- Effect: does not effect certain behavior therapies - Efficacy: easy achieved therapeutic effect due to the broad therapeutic range - Safety: have a wide margin of safety between the therapeutic & toxic doses & rarely fatal if not combined with other CNS depressants or ETOH

What are [2] mechanism of action pathways of Muscle Relaxants?

1. Central Acting (majority): affects the CNS directly, similar to actions of CNS depressants 2. Direct-acting: direct effects the skeletal muscle by inhibiting calcium channels, resulting in decreased strength of muscle contractions

What are some examples of Nonbenzodiazepine Sedative-Hypnotic Agents?

1. Eszopiclone (Lunesta) 2. Ramelteon (Rozerem) 3. Zolpidem (Ambien, Ambien CR) Others . . .

What are the [4] major indication groups for use of Benzodiazepines?

1. Anti-anxiety, hypnotic, anticonvulsant 2. Preoperative sedation 3. Prevention of agitation & DTs in acute alcohol withdrawal 4. Concurrent use with antidepressants, antipsychotics & mood stabilizers

What are the [2] main functions of Eszopiclone (Lunesta)?

1. Increases total sleep time 2. Reduces the time needed to fall asleep

Sedatives inhibit effects of the CNS to the degree that they (select all that apply): A. Reduce Nervousness B. Reduce Excitability C. Initiate Sleep D. Decrease Irritability

A, B, & D.

Benzodiazepines (select all that apply) A. dosage is highly individualized B. metabolized more slowly in younger adults C. Is highly lipid soluble and enters the CNS rapidly D. Long-term use is associated with tolerance, dependency, withdrawal E. Can have hypnotic effects

A. Because the half-life and steady state is a broad range C. The sedation of effect cannot be measured via labs because it rapidly moves in and out of the CNS; this allows a patient to awaken even though the drug may remain in the blood and periphery tissue more many weeks before completely eliminated D. Due to being a Schedule IV drug, they may cause physiologic dependence & withdrawals occur if stopped abruptly E. hypnotic effects are based on the dosage and how long the drug stays in the person's system.

People should not take ramelteon with _____ because of resulting excessive sedation & respiratory depression

Alcohol

Patients on Lunesta should avoid _____ & ______ because it is considered a CNS depressant

Alcohol & other CNS depressants

What is the Benzodiazepine mechanism of action?

Benzo molecules bind to benzodiazepine receptors in nerve cells of the brain to produce a "calming effect": - inhibits effects of GABA - relieve anxiety, tension, & nervousness - produces sleep depending on the dosage

What Sedative-hypnotic drug class is commonly prescribed

Benzodiazepines

Zolpidem (Ambien) differs structurally from _________ but produces similar effects

Benzodiazepines

Diazepam (valium), Alprazolam, Clonazepam, Flurazepam, Lorazepam, Midazolam, & Oxazepam are all examples of what class of drug?

Benzodiazepines. They all end in the suffix (-pam) or (-lam).

REM rebound : A. Is good because it allows the person to be in the best stage of sleep more often B. Allows them to attain the health benefits of sleep and feel well rested C. Is counter productive because the rebound REM cause vivid dreams and nightmares, which could cause the person to awaken startled and not sleep D. Is caused my too much Sedative medication

C

If the benzodiazepine is indicated for anxiolytic, then dosage frequency should: A. initially start with regular dosing ranges and titrate up or down based on therapeutic reaction B. take smallest dose for 4-6 weeks, then titrate up to next dose regimen for an additional 4-6 weeks or until intended therapeutic effect met C. start with the smallest dose likely to be effective & adjust upward to relieve symptoms & avoid adverse effects D. 0.12-0.8 mg/kg/day in divided doses every 6-8 hours

C.

Benzodiazepines are a Schedule ____ drug under the Controlled Substances Act

IV

Ambien is a schedule ______ drug approved for ____ -term treatment for insomnia

IV, short

What Controlled Substance schedule is Eszopiclone (Lunesta)?

IV: this schedule are drugs with an accepted medical use in the U.S. but with some potential for abuse; all benzodiazepines & sedative-hypnotic drugs & prescription appetite suppressants

What is the mechanism of action of Lunesta (Eszopiclone)?

Interacting with GABA receptors, making them more effective with GABA neurotransmitters. GABA is the major inhibitory neurotransmitter in the CNS.

Muscle relaxants are typically scheduled in conjunction with

Physical therapy

What are the [2] classifications of Benzodiazepines?

Sedative-hypnotic & Anxiolytic

Contraindications of benzodiazepines are:

Severe respiratory disorders (COPD, sleep apnea) Severe liver or kidney disease History of alcohol or drug abuse

What are Muscle Relaxants used for?

Skeletal muscle relaxants are used to decrease muscle spasms or spasticity that occurs within neurologic & musculoskeletal disorders

Large doses of antianxiett & sedative drugs produce _______.

Sleep

What is the function of Hypnotics?

To induce sleep.