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Study cards 2 > Central Nervous System Depressants and Muscle Relaxants > Flashcards

Central Nervous System Depressants and Muscle Relaxants Flashcards

1
Q

Sedatives

A

Drugs that have an inhibitory effect on the central nervous system (CNS) to the degree that they reduce:
-Nervousness
-Excitability
-Irritability

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2
Q

Hypnotics

A

Cause sleep

Have much more potent effect on CNS than sedatives have

A sedative can become a hypnotic if given in large enough doses.

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3
Q

CNS Depressants

Classified into three main groups

A

Barbiturates

Benzodiazepines

Miscellaneous drugs

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4
Q

CNS Depressants facts

A

Sedative–hypnotics dose dependent

At low doses, calm the CNS without inducing sleep

At high doses, calm the CNS to the point of causing sleep

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5
Q

Sleep

A

Normal sleep is cyclic and repetitive.

A sleeping person’s response to stimuli is markedly reduced.

Sleep architecture
-Rapid eye movement (REM) sleep
-Non-REM sleep

REM interference

REM rebound

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6
Q

Benzodiazepines

A

Formerly the most commonly prescribed sedative–hypnotic drugs

Nonbenzodiazepines currently more frequently prescribed

Favourable adverse effect profiles, efficacy, and safety

Classified as either sedative–hypnotic or anxiolytic (medication that relieves anxiety)

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7
Q

Benzodiazepines:
3 Sedative–Hypnotic Types

A

long acting

intermediete acting

short acting

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8
Q

Benzodiazepines Long acting

A

diazepam (Valium®)

clonazepam (Rivotril®), flurazepam hydrochloride (Dalmane®)

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9
Q

Benzodiazepines
Intermediate acting

A

lorazepam (Ativan®)

alprazolam (Xanax®), bromazepam (Lectopam®), temazepam (Restoril®)

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10
Q

Benzodiazepines
Short acting

A

midazolam hydrochloride

triazolam, zolpidem tartrate (Sublinox®)

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11
Q

Benzodiazepines: Mechanism of Action

A

Depress CNS activity

Affect hypothalamic, thalamic, and limbic systems of the brain

Benzodiazepine receptors
Gamma-aminobutyric acid (GABA)

Do not suppress REM sleep as much as barbiturates do

Do not increase metabolism of other drugs

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12
Q

Benzodiazepines: Drug Effects

A

Calming effect on the CNS

Useful in controlling agitation and anxiety

Reduce excessive sensory stimulation, inducing sleep

Induce skeletal muscle relaxation

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13
Q

Benzodiazepines: Indications

A

Sedation
Sleep induction
Skeletal muscle relaxation
Agitation or anxiety relief
Anxiety-related depression

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14
Q

Benzodiazepines: Uses

A

Treatment of acute seizure disorders

Treatment of alcohol withdrawal

Short-term therapy for insomnia

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15
Q

Benzodiazepines: Adverse Effects

A

Mild and infrequent

Headache
Drowsiness
Paradoxical excitement of nervousness
Dizziness
Cognitive impairment
Vertigo
Lethargy
Fall hazard for older adults
“Hangover” effect or daytime sleepiness

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16
Q

Benzodiazepines: Toxicity and Overdose

A

Somnolence
Confusion
Coma
Diminished reflexes
Rarely results in hypotension and respiratory depression unless taken with other CNS depressants
Treatment symptomatic and supportive
-Flumazenil as an antidote

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17
Q

Benzodiazepines: Interactions

A

Azole antifungals, verapamil, diltiazem, protease inhibitors, macrolide antibiotics, grapefruit juice

CNS depressants (alcohol, opioids, muscle relaxants)

Kava and valerian

Food–drug interactions with grapefruit and grapefruit juice

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18
Q

diazepam (Valium®)

A

First clinically available benzodiazepine drug. It has varied uses, including treatment of anxiety.

Long acting benzodiazepine

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19
Q

Midazolam

A

Short acting

Most commonly used preoperatively and for procedural sedation

Causes amnesia and anxiolysis (reduced anxiety) as well as sedation

Normally administered by IV in adults

Liquid oral dosage form is also available for children.

20
Q

lorazepam (Ativan)

A

Intermediate-acting benzodiazepine

Also used to treat anxiety

Normally induces sleep within 30 to 60 minutes

Long onset of action, so it is recommended that patients take it about 1 hour prior to going to bed.

21
Q

nonbenzodiazepine: Ramelteon®

A

Structurally similar to the hormone melatonin; works as an agonist at melatonin receptors in the CNS

Not available in Canada.

Technically, not a CNS depressant; used as hypnotic

Not classified as a controlled substance

Indicated for patients who have difficulty with sleep onset rather than maintenance

22
Q

Nonbenzodiazepine: zopiclone (Imovane®, Rhovane®)

A

Short-acting benzodiazepinelike drug

Unique advantage of this drug stems from its very short half-life.

Short-term treatment of insomnia, 7 to 10 days.

23
Q

Nonbenzodiazepine: zolpidem tartrate (Sublinox®)

A

Short-acting nonbenzodiazepine hypnotic

Lower incidence of daytime sleepiness compared with benzodiazepine hypnotics

Onset of action approximately 30 minutes

24
Q

Herbal Products: Kava

A

Used to relieve anxiety, stress, and restlessness and to promote sleep

May cause temporary yellow skin discoloration (extended, continued intake), scaly skin, and visual disturbances

Potential interactions with alcohol, barbiturates, and psychoactive drugs

Contraindicated in liver disease, alcoholism, other conditions

Patient should not operate heavy machinery during use.

25
Herbal Products: Valerian
Used to relieve anxiety, restlessness, and sleep disorders May cause CNS depression, hepatotoxicity, nausea, vomiting, anorexia, headache, restlessness, insomnia Many interactions, including with CNS depressants, monoamine oxidase inhibitors (MAOIs), phenytoin, warfarin, and alcohol Contraindicated in cardiac and liver disease Patient should not operate heavy machinery during use
26
Barbiturates
First introduced in 1903; were the standard drugs for insomnia and sedation Habit forming; low therapeutic index Only a few commonly used today partly because of the safety and efficacy of benzodiazepines
27
Barbiturates: Mechanism of Action
Site of action: brainstem (reticular formation) By potentiating the action of GABA, nerve impulses traveling in the cerebral cortex are inhibited.
28
Barbiturates: Indications
Sedatives Anticonvulsants Anaesthesia for surgical procedures
29
Barbiturates: Adverse Effects
Body system/adverse effects Cardiovascular: Vasodilation, hypotension CNS: Drowsiness, lethargy, vertigo Respiratory: Respiratory depression, cough Gastrointestinal: Nausea, vomiting, diarrhea, constipation Hematological: Agranulocytosis, thrombocytopenia Other: Hypersensitivity reactions, Stevens-Johnson syndrome
30
Barbiturates: Toxicity and Overdose
Rarely used Overdose frequently leads to respiratory depression and subsequent respiratory arrest Overdose produces CNS depression (sleep to coma and death)
31
Barbiturates can be therapeutic for:
Anaesthesia induction Uncontrollable seizures Pentobarbital or phenobarbital (in Canada) coma
32
Barbiturates: Toxicity and Overdose Treatment of overdose
Symptomatic and supportive Maintain adequate airway Assisted ventilation or oxygen therapy Fluids Alkalization Activated charcoal
33
Barbiturates: Drug Interactions Additive effects Inhibited metabolism Increased metabolism
Additive effects Alcohol, antihistamines, benzodiazepines, opioids, tranquilizers Inhibited metabolism MAOIs prolong the effects of barbiturates. Increased metabolism Reduces anticoagulant response, leading to possible clot formation
34
Common Barbiturates
phenobarbital
35
Phenobarbital
Prototypical barbiturate Long-acting drug Uses: prevention of generalized tonic-clonic seizures and fever-induced convulsions, as well as treatment of hyperbilirubinemia in neonates Rarely used today as a sedative and is no longer recommended to be used as a hypnotic drug
36
Over-the-Counter Hypnotics 1. Examples 2. Facts
Doxylamine succinate (Unisom-2®), diphenhydramine hydrochloride (Sleep-Eze®), acetaminophen/diphenhydramine (Extra Strength Tylenol® Nighttime) – know names Nonprescription sleeping aids often contain antihistamines, which have CNS-depressant effect. As with other CNS depressants, concurrent use of alcohol can cause respiratory depression or arrest.
37
Muscle Relaxants
Act to relieve pain associated with skeletal muscle spasms
38
Majority of muscle relaxants are ? The rest are?
centrally acting the rest are direct acting
39
Centrally acting muscle relaxant 1. site of action 2. similar as?
Site of action: CNS Similar in structure and action to other CNS depressants
40
Direct acting
Act directly on skeletal muscle Closely resemble GABA
41
Muscle Relaxants: Indications
Relief of painful musculoskeletal conditions -Muscle spasms -Management of spasticity of severe chronic disorders (multiple sclerosis, cerebral palsy) Work best when used along with physical therapy
42
Muscle Relaxants: Adverse Effects
Extension of effects on CNS and skeletal muscles -Euphoria -Lightheadedness -Dizziness -Drowsiness -Fatigue -Confusion -Muscle weakness
43
Common Muscle Relaxants
Baclofen (Lioresal®) Cyclobenzaprine hydrochloride (Novo-Cycloprine®)
44
Nursing Implications
Before beginning therapy, obtain a thorough history regarding allergies, use of other medications, health history, and medical history. Obtain baseline vital signs and intake and output, including supine and erect blood pressure. Assess for potential disorders and conditions that may be contraindications and for potential drug interactions. Most benzodiazepines cause REM interference and a tired feeling the next day; use with caution in older adults. Instruct patients to avoid alcohol and other CNS depressants. Check with the prescriber before taking any other medications, including over-the-counter medications. Rebound insomnia may occur for a few nights after a 3- to 4-week regimen has been discontinued.
45
Administer hypnotics ___ to ___ minutes before bedtime for maximum effectiveness in inducing sleep (depends on drug’s onset).
30 to 60 minutes
46
Safety is important.
Keep side rails up or use bed alarms. Do not permit smoking. Assist patients (especially older adults) with ambulation . Keep call light within reach. Monitor for adverse effects.
47
Monitor for therapeutic effects.
Increased ability to sleep at night Fewer awakenings Shorter sleep-induction time Few adverse effects, such as “hangover” effects Improved sense of well-being because of improved sleep For muscle relaxants: decreased spasticity, decreased rigidity, pain relief

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