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Pharm Test 2 > Chapter 12 Central Nervous System Depressants and Muscle Relaxants > Flashcards

Chapter 12 Central Nervous System Depressants and Muscle Relaxants Flashcards

1
Q

Sedatives

A

-Drugs that have an inhibitory effect on the CNS to the degree that they reduce:
Nervousness
Excitability
Irritability

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2
Q

CNS Depressants: Benzodiazepines

A

-Formerly the most commonly prescribed sedative-hypnotic drugs
-Favorable drug effect profiles, efficacy, and safety
-Classified as either:
Sedative-hypnotic
Anxiolytic (medication that relieves anxiety)

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3
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 rapid eye movement (REM) sleep as much as barbiturates do
-Do not increase metabolism of other drugs

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4
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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5
Q

Diazepam (Valium)

A

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

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6
Q

Midazolam (Versed)

A
  • Most commonly used preoperatively and for moderate sedation.
  • Causes amnesia and anxiolysis (reduced anxiety) as well as sedation.
  • Normally administered by injection in adults
  • Liquid oral dosage form is also available for children.
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7
Q

Temazepam (Restoril)

A
  • Intermediate-acting benzodiazepine
  • One of the metabolites of diazepam
  • Normally induces sleep within 20 to 40 minutes
  • Long onset of action, so it is recommended that patients take it about 1 hour prior to going to bed
  • Still an effective hypnotic; however, it has been replaced by newer drugs
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8
Q

Nonbenzodiazepine: Eszopiclone (Lunesta)

A
  • First hypnotic to be FDA approved for long-term use
  • Designed to provide a full 8 hours of sleep
  • Considered a short- to intermediate-acting agent
  • Patients should allot 8 hours of sleep time and should avoid taking hypnotics when they must awaken in less than 6 to 8 hours.
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9
Q

Nonbenzodiazepine: Ramelteon (Rozerem)

A
  • Structurally similar to the hormone melatonin: works as an agonist at melatonin receptors in the CNS
  • Technically, it is not a CNS depressant; used as hypnotic
  • Not classified as a controlled substance
  • Indicated for patients who have difficulty with sleep onset rather than sleep maintenance
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10
Q

Nonbenzodiazepine: Zaleplon (Sonata)

A
  • Short-acting nonbenzodiazepine hypnotic
  • Unique advantage of this drug stems from its very short half-life
  • Patients whose sleep difficulties include early awakenings can take a dose in the middle of the night as long as it is at least 4 hours before they must arise.
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11
Q

Nonbenzodiazepine: Zolpidem (Ambien)

A
  • Short-acting nonbenzodiazepine hypnotic
  • Lower incidence of daytime sleepiness compared with benzodiazepine hypnotics
  • Ambien CR is a longer acting form with two separate drug reservoirs
  • Somnambulation
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12
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) 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.
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13
Q

Herbal Products: Valerian

A
  • Used to relieve anxiety, restlessness, and sleep disorders
  • May cause CNS depression, hepatotoxicity, nausea, vomiting, anorexia, restlessness, insomnia
  • Many interactions, including with CNS depressants, -MAOIs, phenytoin, warfarin, and alcohol
  • Contraindicated in cardiac and liver disease
  • Patient should not operate heavy machinery during use.
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14
Q

Barbiturates

A
  • First introduced in 1903; were the standard drugs for insomnia and sedation
  • Habit forming; low therapeutic index
  • Only a handful commonly used today partly because of the safety and efficacy of benzodiazepines
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15
Q

Barbiturates:Mechanism of Action

A
  • Site of action: brainstem (reticular formation)

- By potentiating the action of GABA, nerve impulses traveling in the cerebral cortex are inhibited.

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16
Q

Barbiturates: Drug Effects

A
  • Low doses: sedative effects
  • High doses: hypnotic effects (also lower respiratory rate)
  • Notorious enzyme inducers
  • Stimulate liver enzymes that cause metabolism or breakdown of many drugs
  • Result in shortened duration of action
17
Q

Ultrashort acting Barbiturates

A

Anesthesia for short surgical procedures, other uses

18
Q

Short Acting Barbiturates

A

Sedation and control of convulsive conditions

19
Q

Intermediate Acting Barbiturates

A

Sedation and control of convulsive conditions

20
Q

Long Acting Barbiturates

A

Sleep induction, epileptic seizure prophylaxis

21
Q

Barbiturates: Adverse Effects

A

Cardiovascular Vasodilation, hypotension

CNS Drowsiness, lethargy, vertigo

Respiratory Respiratory depression, cough

22
Q

Barbiturates: Adverse Effects (Cont.)

A

GI Nausea, vomiting, diarrhea, constipation
Hematologic Agranulocytosis, thrombocytopenia

Other Hypersensitivity reactions, Stevens-Johnson syndrome

23
Q

Treatment of overdose for Barbiturates

A
  • Symptomatic and supportive
  • Maintain adequate airway
  • Assisted ventilation or oxygen therapy
  • Fluids
  • Pressor support
  • Activated charcoal
24
Q

Inhibited metabolism

A

MAOIs prolong the effects of barbiturates.

25
Q

Common Barbiturates

A
  • Pentobarbital (Nembutol)

- Phenobarbital

26
Q

Pentobarbital (Nembutal)

A
  • 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
27
Q

Over-the-Counter Hypnotics

A
  • Nonprescription sleeping aids often contain antihistamines, which have CNS depressant effect.
  • Doxylamine (Unisom) and diphenhydramine (Sominex), acetaminophen/diphenhydramine (Extra Strength Tylenol PM)
  • As with other CNS depressants, concurrent use of alcohol can cause respiratory depression or arrest.
28
Q

Low therapeutic index

A

Drugs with a low therapeutic index have only a narrow dosage range within which the drug is effective; above that range, they are rapidly toxic. `

29
Q

Muscle Relaxants

A

-Act to relieve pain associated with skeletal muscle spasms
-Majority are centrally acting
CNS is the site of action
Similar in structure and action to other CNS depressants
-Direct acting
Act directly on skeletal muscle
Closely resemble GABA

30
Q

Muscle Relaxants: Indications

A

-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

31
Q

Muscle Relaxants: Adverse Effects

A

Extension of effects on CNS and skeletal muscles

  • Euphoria
  • Lightheadedness
  • Dizziness
  • Drowsiness
  • Fatigue
  • Muscle weakness, others
32
Q

Nursing Implications

A
  • Give hypnotics 30 to 60 minutes before bedtime for maximum effectiveness in inducing sleep (depends on drug’s onset).
  • Most benzodiazepines cause REM rebound and a tired feeling the next day; use with caution in older adults.
  • Rebound insomnia may occur for a few nights after a 3- to 4-week regimen has been discontinued

Pharm Test 2 (8 decks)

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