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Pharmacology > CNS Deppressants > Flashcards

CNS Deppressants Flashcards

1
Q

What are sedatives?

A

Drugs that have an inhibitory effect on the CNS until they reduce:

  • Nervousness
  • Excitability
  • Irritability

Without causes sleep

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2
Q

What’s an hypnotic?

A

Reduce CNS function to the point that they cause sleep

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

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3
Q

What is a more commonly used sedative-hypnotic?

A

Benzodiazepines

  • Better pharmacological profile
  • Better adverse effects profile
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4
Q

Which sedative-hypnotic is addictive?

A

Barbiturates

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5
Q

When should you use Barbiturates?

A

Antiepileptic

  • Can raise the seizure threshold - reducing seizures
  • Anaesthesia for surgical procedures (short)

Narrow therapeutic index

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6
Q

What is an example of a short acting, and a long acting barbiturate?

A
  • Pentobarbital (rarely used)
  • Short acting
  • Phenobarbital
  • Long acting
  • Antiepileptic
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7
Q

How do Barbiturates function?

A
  • Most have a broad CNS depression action
  • Potentiates GABA action and mimics GABA
  • Metabolized in liver and excreted in urine
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8
Q

What is the antidote to barbiturates?

A

Activated charcoal

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9
Q

How do barbiturates impact enzymes?

A
  • Notorious enzyme inducers

- Increase liver enzymes that metabolize many drugs

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10
Q

What are some drug interactions for barbiturates?

A

Lots of drug-drug interactions
- Use cautiously

  • Additive effects (other CNS depressants)
  • Alcohol, antihistamines, benzodiazepines, opioids

Inhibited metabolism
- MAOIs will prolong effects of barbiturates

  • Increased metabolism of other drugs
  • Reduces anticoagulant response of warfarin
  • Theophylline, phenytoin also reduce effects
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11
Q

What are the adverse effects of barbiturates?

A

Similar to alcohol intoxication
- Confusion, impaired judgement and speech, retarded reflexes, loss of muscle coordination

CNS
- Drowsiness, lethargy, vertigo, mental depression, coma

Resp
- Respiratory Depression, apnea, bronchospasm, cough

GI
- Nausea, vomiting, diarrhea, constipation

Other

  • Agranulocytosis (loss of WBC), vasodilation, hypotension, Stevens-Johnson syndrome
  • Reduces REM sleep causes agitation and inability to deal with normal stress
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12
Q

What happens with barbiturates overdose?

A
  • Leads to respiratory depression or arrest

- CNS depression (sleep-coma-death)

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13
Q

Why are barbiturates used less in clinical situations?

A
  • Tolerance
  • Physical dependence
  • Liver enzyme induction
  • *Abuse potential
  • Powerful respiratory depressants
  • No antidote
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14
Q

What are the two classifications of benzodiazepines?

A
  • Sedative-hypnotic

- Anxiolytic

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15
Q

What are the different acting classes of benzodiazepines?

A

Long acting
- Chlordiazepoxide, clorazepate, flurazepam

Intermediate acting
- *Lorazepam (ativan), oxazepam

Short acting

  • *Midazolam IV (Versed), triazolam
  • Conscious sedation - amnesic property
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16
Q

Which neurotransmitter do benzodiazepines enhance?

A

GABA

- Reduces excitability of neurons and depresses CNS activity

17
Q

How do benzodiazepines impact the body?

A

Affect hypothalamic, thalamic, and limbic systems of the brain

  • *Does not suppress REM as much as barbiturates
  • *Does not increase metabolism of other drugs
  • *PO admin does not depress respiration excessivley

Reduce excessive sensory stimulation, inducing sleep especially in short term use for insomnia due to anxiety
Much better than barbiturates

18
Q

What is the antidote for benzodiazepines?

A

Flumazenil

19
Q

When should benzodiazepines be used?

A 
Sedation
Sleep induction
Skeletal muscle relaxation (central effect)
Anxiety relief
Treatment of alcohol withdrawal 
Agitation
Epilepsy
Balanced anaesthesia
20
Q

What are some adverse effects for benzodiazepines?

A 
*Drowsiness
Headache
Dizziness
Vertigo
Lethargy
Paradoxical excitement (nervousness)
“Hangover effect”
21
Q

What are the drug interactions with benzodiazepines?

A

All other CNS depressants have additive effects
- Alcohol, opioids

Grapefruit alter drug absorption

Cimetidine inhibits benzodiazepine metabolism

22
Q

What are some other hypnotics?

A

Zolpidem (Ambien), zaleplon, zopiclone

Used for short-term use in management of insomnia

23
Q

When should muscle relaxants be used?

A

For the relief of painful musculoskeletal conditions

  • Muscle spasms
  • Management of spasticity of severe clinical disorders
  • MS, cerebral palsy
  • Dantrolene
  • For emergency treatment of malignant hyperthermia crisis
  • Treatment of spasticity associated with spinal cord injury, CVA, CP and MS
  • Acts directly on skeletal muscles causing relaxation
  • Especially effective for head and neck spasms
24
Q

What are some adverse effects of muscle relaxants?

A 
Euphoria 
Lightheadedness
Dizziness
Drowsiness
Fatigue
Muscle weakness

Pharmacology (29 decks)

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