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PHARMA > CNS 2 > Flashcards

CNS 2 Flashcards

1
Q

Is a mediator of slow EPSPs in neurons involved in nociceptive sensory pathways in the spinal cord and brain stem.

A

peptide substance P

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2
Q

Neurotransmitters may
(A) Increase chloride conductance to cause inhibition
(B) Increase potassium conductance to cause inhibition
(C) Increase sodium conductance to cause excitation
(D) Increase calcium conductance to cause excitation
(E) Exert all of the above actions

A

Exert all of the above actions

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3
Q

This transmitter is mostly located in diffuse neuronal systems in the CNS, with cell bodies particularly in the raphe nuclei.It appears to play a major role in the expression of mood states, and many antidepressant drugs are thought to increase its functional activity.

A

Serotonin

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4
Q

This neurotransmitter, found in high concentrations in cell bodies in the pons and brain stem, can exert both excitatory and inhibitory actions. Multiple receptor subtypes have
been identified, some of which are targets for drugs that can exert both CNS and peripheral actions.

A

Norepinephrine

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5
Q

Reduction of anxiety. The administering of a sedative drug to produce a state of calm or sleep.

A

Sedation

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6
Q

The state of response to a drug whereby the drug taker feels compelled to use the drug and suffers anxiety when separated from it

A

Addiction

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7
Q

Loss of consciousness associated with absence of response to pain

A

Anesthesia

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8
Q

A drug that reduces anxiety, a sedative

A

Anxiolytic

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9
Q

The state of response to a drug whereby removal of the drug evokes unpleasant, possibly life-threatening symptoms, often the opposite of the drug’s effects

A

Dependence

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10
Q

Induction of sleep

A

Hypnosis

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11
Q

Phase of sleep associated with rapid eye movements. Most dreaming takes place during REM sleep.

A

REM sleep

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12
Q

Reduction in drug effect requiring an increase in dosage to maintain the same response

A

Tolerance

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13
Q

An unpleasant state of tension, apprehension, or uneasiness. A fear that seems to arise from a sometimes unknown source. It is the most common mental disturbances.

A

Anxiety

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14
Q

Are the most widely used anxiolytic drugs. They have largely replaced barbiturates and meprobamate in the treatment of anxiety, because the benzodiazepines are safer and
more effective.

A

Benzodiazepines

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15
Q

The targets for benzodiazepine actions are the ___. Binding of this to its receptor triggers an opening of a chloride channel, which leads to an increase in chloride conductance. The influx of chloride ions causes a small hyperpolarization that moves
the postsynaptic potential away from its firing threshold → inhibits the formation of action potentials.

A

GABAA receptors.

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16
Q

Tolerance occurs when used for more than one to two weeks. Cross-tolerance exists among this group of agents with ethanol.

A

benzodiazepines

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17
Q

They have neither antipsychotic activity nor analgesic action, and they do not affect the autonomic nervous system. These drugs exhibit the following actions to a greater or
lesser extent:
➢Reduction of anxiety:
▪ Low doses → anxiolytic
➢Sedative and hypnotic actions
▪ Higher doses → used to treat anxiety have some sedative properties, and some can produce hypnosis (artificially produced sleep)
➢Anterograde amnesia
▪ The temporary impairment of memory with use of this is also mediated by the GABAA receptors.
▪ This also impairs a person’s ability to learn and form new memories.
➢Anticonvulsant
▪ Several of the benzodiazepines have anticonvulsant activity and some are used to treat epilepsy (status epilepticus) and other seizure disorders.
▪ This effect is partially, although not completely, mediated by GABAA receptors.
➢Muscle relaxant:
▪ At high doses, these relax the spasticity of skeletal muscle, probably by increasing presynaptic inhibition in the spinal cord, where the GABAA receptors are located.

A

benzodiazepines

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18
Q

Are effective for the treatment of the anxiety symptoms secondary to panic disorder, generalized anxiety disorder, social anxiety disorder, performance anxiety, posttraumatic stress disorder, obsessive-compulsive disorder, and the extreme anxiety sometimes encountered with specific phobias, such as fear of flying. Can also be useful in treating anxiety that accompanies depression and schizophrenia.

A

Benzodiazepines

19
Q

Benzodiazepines should be reserved for continued severe anxiety, and then should only be used for short periods of time because of their

A

addiction potential

20
Q

The longer-acting agents, such as _____ are often preferred in those patients with anxiety that may require treatment for prolonged periods of time.

A
  • clonazepam
  • lorazepam
  • diazepam
21
Q

For panic disorders, ____ is effective for short- and long-term treatment, although it may cause withdrawal reactions in about 30 percent of sufferers.

A

alprazolam

22
Q

Is useful in the treatment of skeletal muscle spasms, such as occur in muscle strain, and in treating spasticity from degenerative disorders, such as multiple sclerosis and cerebral palsy.

A

Diazepam

23
Q

Is an injectable-only benzodiazepine also used for the induction of anesthesia.

A

Midazolam

24
Q

Is occasionally used in the treatment of certain types of epilepsy

A

Clonazepam

25
Q

Are the drugs of choice in terminating grand mal epileptic seizures and status epilepticus.

A

Diazepam and lorazepam

26
Q

Due to cross-tolerance, _____ are useful in the acute treatment of alcohol withdrawal and reducing the risk of withdrawal-related seizures.

A
  • chlordiazepoxide
  • clorazepate
  • diazepam
  • oxazepam
27
Q
  • They tend to decrease the latency to sleep onset and increase Stage II of non-rapid eye movement sleep (light sleep).
  • Both REM sleep and slow-wave sleep (deep sleep) are decreased.
  • In the treatment of insomnia, it is important to balance the sedative effect needed at bedtime with the residual sedation (hangover) upon awakening.
A

benzodiazepines

28
Q 
Commonly prescribed benzodiazepines for sleep disorders 
include: 
– long-acting: 
– intermediate-acting: 
– short-acting:
A

– long-acting flurazepam
– intermediate-acting temazepam
– short-acting triazolam

29
Q

– long-acting benzodiazepine
– significantly reduces both sleep-induction time and the number of awakenings
– increases the duration of sleep
– causes little rebound insomnia
– half-life of approximately 85 hours (3.5 days), which may result in daytime sedation and accumulation of the drug

A

Flurazepam

30
Q

– useful in patients who experience frequent wakening

– peak sedative effect occurs 1 to 3 hours after an oral dose → should be given 1 to 2 hours before the desired bedtime

A

Temazepam

31
Q

– has a relatively short duration of action → used to induce sleep in patients with
recurring insomnia
– whereas temazepam is useful for insomnia caused by the inability to stay asleep,
triazolam is effective in treating individuals who have difficulty in going to sleep.
– tolerance frequently develops within a few days
– withdrawal of the drug often results in rebound insomnia, leading the patient to demand another prescription or higher dose (dependence)
– therefore, this drug is best used intermittently rather than daily
– In general, hypnotics should be given for only a limited time, usually less than 2
to 4 weeks.

A

Triazolam

32
Q
  • The benzodiazepines are ____, and they are rapidly and completely absorbed after oral administration and distribute throughout the body.
  • Most benzodiazepines, including chlordiazepoxide and diazepam, are metabolized by the hepatic microsomal system to compounds that are also active.
  • The benzodiazepines are excreted in the urine as glucuronides or oxidized metabolites.
A

lipophilic

33
Q

Abrupt discontinuation of the benzodiazepines results in withdrawal symptoms, including:

A
  • Confusion
  • Anxiety
  • Agitation
  • Restlessness
  • Insomnia
  • Tension
  • Rarely, seizures
34
Q

Benzodiazepines w/ short half-lives, such as triazolam → induce ____ abrupt and ____ withdrawal reactions than those seen with drugs that are slowly eliminated, such as flurazepam.

A

more; severe

35
Q

The two most common side effects of the benzodiazepines.

A

Drowsiness and confusion

36
Q

Occurs at high doses and precludes activities that require fine motor coordination, such as driving an automobile

A

Ataxia

37
Q

One of the most potent oral benzodiazepines with the most rapid elimination,
often shows a rapid development of tolerance, early morning insomnia, and daytime anxiety, along with amnesia and confusion.

A

Triazolam

38
Q

Precautions using Benzodiazepines

A
  • liver disease.
  • with acute narrow-angle glaucoma
  • Alcohol and other CNS depressants enhance the sedative-hypnotic effects
  • less dangerous than the older anxiolytic and hypnotic drugs → drug overdose is seldom lethal unless other central depressants, such as alcohol, are taken concurrently.
39
Q

A GABA-receptor antagonist that can rapidly reverse the effects of benzodiazepines. Available for intravenous administration only

A

Flumazenil

40
Q
  • Useful in the treatment of generalized anxiety disorder and has an efficacy comparable to that of the benzodiazepines.
  • The actions appear to be mediated by serotonin (5-HT1A) receptors, although other receptors could be involved, because it displays some affinity for DA2 dopamine receptors and 5-HT2A serotonin receptors. Thus, its mode of action differs from that of the benzodiazepines.
A

Buspirone

41
Q
  • Lacks the anticonvulsant and muscle-relaxant properties of the benzodiazepines
  • Causes only minimal sedation
  • Causes hypothermia
  • Can increase prolactin and growth hormone
A

Buspirone

42
Q
  • An antihistamine with antiemetic activity.
  • It has a low tendency for habituation and, thus, is useful for patients with anxiety who have a history of drug abuse.
  • It is also often used for sedation prior to dental procedures or surgery.
  • Drowsiness is a possible adverse effect
A

Hydroxyzine

43
Q
  • The frequency of adverse effects is low
  • Most common effects: headaches, dizziness, nervousness, and light-headedness
  • Sedation and psychomotor and cognitive dysfunction are minimal, and dependence is unlikely.
  • It has the disadvantage of a slow onset of action.
A

Buspirone

PHARMA (26 decks)

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