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Pharmacology > CNS Part 1: Anxiolytics, Hypnotics, Alcohol, & Opoids > Flashcards

CNS Part 1: Anxiolytics, Hypnotics, Alcohol, & Opoids Flashcards

1
Q
  • What effect does GABA have on the CNS?
A

GABA is the major INHIBITORY neurotransmitter of CNS (gaba normally causes opening of CL channels)

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2
Q

What effect do benzodiazepines have on GABA?

A

BZDs increase the affinity of GABA for GABA binding site (enhance CL channel opening & inhibitory effects in CNS)

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3
Q
  • Describe how BZDs are used for anxiety disorder
A

4 serious, persistant anxiety

-used for short term therapy since can be addictive

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4
Q

(USE) What is the BZD Diazepam used for?

A

Treatment of Muscle Spasm

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5
Q

What are BZDs used for?

A
  • Anxiety disorders
  • Muscle disorders
  • Amnesia
  • Sleep disorders
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6
Q

How long should BZDs for sleep disorders be given?

A

2 weeks to avoid tolerance & withdrawl

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7
Q

a) What class does Flurazepam (Dalmane) belong to

b) What is it used for?

A

a) Long-acting BZD

b) increases sleep time

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8
Q

a) What class does belong to Triazolam (Halcion)

b) What is it used for?

A

a) Short-acting BZD

b) sleep induction

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9
Q
  • What are the AE of Benzodiazepines?
A

Tolerance, Dependence, Withdrawl, CNS dependence (drowwsiness, & confusion, etc)

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10
Q
  • What type of drug is a BZD antagonist?
A

Flumazenil (Romazicon); it reverses the effects of BZD

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11
Q

What is the MOA of Buspirone (Burpar)?

A

-Does NOT work on BZD receptors

It has anxiolytic effects (anti-anxiety)

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12
Q

What is the MOA of Barbituates?

A

Acts on GABA-a receptors & causes sedative & hypnotic effects (CNS depression)

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13
Q

What are the uses of Barbituates?

A

ANTICONVULSANT, Anesthesia, Anxiolytic, Hypnotic

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14
Q

What is an AE of barbituates?

A

Induction of CYP450 (drug interactions) (as a result, the drug level in the blood goes down)

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15
Q

What is an ex of a hypnotic?

A

Zolpidem (Ambien)

MOA: acts on BZD 1 receptors

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16
Q

a)What are the kinetics of Eszopiclone (Lunesta)?

A

effective up to 6 months of continuous use

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17
Q

What is the MOA of Ramelteone (Rozerem)?

A

melatonin agonist (MT1 & MT2)

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18
Q

What is the use of Rmelteon (Rozerem)?

A

insomnia

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19
Q

What is the MOA of antihistamines?

A

Competitive histamine -1 (H1) antagonist

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20
Q

What types of drugs are Ramelteone (Rozerem) and Eszopiclone (Lunesta)?

A

Hypnotics

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21
Q

*What is the MOA of Disulfiram (Antabuse)?

A

Blocks oxidation of acetaldehyde to acetate

interferes with ethanol metabolism

22
Q
  • What is the use of Disulfiram (Antabuse)?
A

Deter alcohol use

23
Q
  • What is a major AE of Disulfiram (Antabuse)?
A

N/V

tachycardia, hyperventilation, flusing

24
Q

What is the MOA of opoids (pain)?

A

bind to opoid receptors in CNS to produce effects of neurotransmitters

25
Q

What are examples of opoids?

A

Endorphins, Enkephalins, Dynorphins

26
Q

Name the opoid receptors

A

mu, kappa (sedative), and delta

27
Q
  • What is the major receptor involved in opoid pain relied & respiratory depressant effects?
A

Mu

28
Q

What is the MOA of opoid receptors?

A

Inhibit adenyl cyclase

29
Q

What is the MOA of opoid analgesica

A

Bind to receptors in the CNS and inhibit the ascending pain pathway (CNS depression)

30
Q

Define analgesia

A

increase in pain tolerance, alters pain perception

31
Q

Define euphoria

A

sense of well being

32
Q

Define respiratory supression

A

decreased sensitivity to carbon dioxide

33
Q

*Define miosis

A

stimulation of mu and kappa receptors (enhanced parasympathetic stimulation of eye)

34
Q
  • What are the AE of opoids?
A

Analgesia, Euphoria, respiratory depression, cough reflex supression, miosis, emesis (N/V)

35
Q

Which RX should you not use in patients with head injuries?

A

Opoids

36
Q

What effect do opoids have on therespiratory system?

A

Causes respiratory depression–> carbon dioxide retention and dilation of cerebral vessels and increased CSF pressure

37
Q
  • Name a strong opoid agonist
A

Morphine

38
Q

*Name a moderate/low opoid agonist

A

Codeine

39
Q

*Name a mixed opoid agonist-antagonist

A

Pentazocine

40
Q
  • Name a partial opoid agonist
A

Buprenorphine

41
Q
  • Name a opoid antagonist
A

Naloxone

42
Q

What are the uses of morphine?

A

analgesia, acute pulmonary edema, relief of diarrhea, and relief of cough

43
Q

*What opoids suppress the cough reflex?

A

Codeine and dextromethorphan

44
Q

What opoids provide relief of diarrhea?

A

Loperamide and diphenoxylate

45
Q

What are the AE of morphine?

A

extension of opoid effects, increased ICP, urinary retention, stoppage of respiratory exchange

46
Q

What is Meperidine (Demerol ) used for?

A

OB: less likely to prolong labor (less effect on SM of uterus)

47
Q

What is an AE of meperidine (demerol)?

A

May cause pupil dilation, large dosing may cause toxic metabolite

48
Q

What patients shoudl not take meperidine (Demerol)

A

Elderly

49
Q

What is a use of methadone?

A

Controlled withdrawl from other opoids (heroin, morphine)

50
Q

What is the MOA of pentazocine?

A

Provides analgesia by acting on receptors in SC; blocks morphine effect

51
Q

What are the uses of opioid antagonists

A

reverse CNS depression of opiod overdose

52
Q
  • What are the 3 stages of opoid withdrwal symptoms?
A
  • Stage 1: Anxiety & drug craving
  • Stage 2: insomnia, Gi disturbance, Rhinorrhea, Mydiriasis, Diaphoresis
  • Stage 3: Tachycardia, N/V, HTN, diarrhea, Fever, Chills, Tremors, Seizure, Muscle spasms

Pharmacology (5 decks)

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