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Pharm > Depressants > Flashcards

Depressants Flashcards

1
Q

What are the four lobes of the cerebrum?

A

Frontal
Temporal
Parietal
Occipital

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2
Q

What is the diencephalon? What are the structures that are included in this?

A

Area of the brain that encloses the 3rd ventricle

Thalamus
Hypothalamus

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3
Q

What is the function of the thalamus?

A

Integration of sensory relays

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4
Q

What is the function of the hypothalamus?

A

Regulates temperature, appetite, emotional and hormonal regulation

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5
Q

What is the mesencephalon?

A

Midbrain, the serves as a bridge between the cerebrum/diencephalon, and the brainstem

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6
Q

What are the structures that are contained within the brainstem?

A

Pons

Medulla oblongata

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7
Q

What is the function of the pons and the medulla?

A

Controls respiration and cardiovascular function

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8
Q

What is the function of the reticular formation within the brainstem?

A

Control of consciousness, arousal, and alertness

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9
Q

Where are the basal ganglia located?

A

deep within the cerebral hemispheres

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10
Q

What is the function of the basal ganglia?

A

Control of motor activities, and repressing unwanted movements

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11
Q

What are the four components of the basal ganglia?

A 
Cortex
Striatum
Pallidum
Thalamus
**AND BACK TO CORTEX!!**
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12
Q

What are the two components of the striatum?

A

caudate nucleus and putamen

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13
Q

What are the four major areas of the brain that are part of the limbic system?

A

Amygdala
Hippocampus
Cingulate gyrus
Prefrontal cortex

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14
Q

What is the function of the amygdala?

A

Regulation of fear

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15
Q

What is the function of the Hippocampus?

A

Memory formation, conversion of short term memory into long term

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16
Q

What is gray matter?

A

Synaptic connections between various neurons

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17
Q

What is white matter?

A

Myelinated axons of neurons, grouped in ascending or descending tracts

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18
Q

What forms the Blood brain barrier?

A

Tight junctions between endothelial cells on the CNS capillaries

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19
Q

What is the function of astrocytes?

A

Homeostatic support roles for neuron (maintain nutrition etc)

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20
Q

What is the function of oligodendrocytes?

A

Glial cells that wrap around the axons of projection neurons in the CNS forming the myelin sheath

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21
Q

What are the cells that myelinate CNS neurons? PNS?

A 
CNS = oligodendrocytes
PNS = Schwann cells
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22
Q

What are microglia?

A

Glial cells derived from the bone marrow specialized in immune defense of the brain

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23
Q

What are the two components that create the blood brain barrier?

A

Tight junction around capillary endothelial cells

Astrocyte foot processes

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24
Q

What is the protein in neuronal terminals that interacts with Ca, and allows for the release of neurotransmitters?

A

Calmodulin

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25
Q

What are ionotropic receptors?

A

receptors on synapses that activate an ion channel

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26
Q

What are metabotropic receptors?

A

receptors coupled to a second messenger enzyme system (e.g. adenylate cyclase)

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27
Q

What is the only enzymes that breaks down 5HT?

A

monoamine oxidase

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28
Q

What are electrical synapses?

A

junctions between cells that allow for ion fluxes, and immediate transmission of signal

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29
Q

What is EPSP?

A

Excitatory postsynaptic potential

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30
Q

What are IPSPs?

A

Inhibitory postsynaptic potentials

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31
Q

What are the roles of acetylcholine in the brain?

A

Memory and learning
Attention
Sleep

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32
Q

What is the function of dopamine?

A

brain circuits that control movement (think parkinson’s)

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33
Q

What is the function of glutamate in the CNS?

A

major excitatory neurotransmitter and CNS

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34
Q

What is the function of GABA in the brain?

A

Major inhibitory neurotransmitter in the CNS

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35
Q

What is the function of substance P in the CNS?

A

Excitatory transmitter involved in spinal processing

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36
Q

What is the function of endorphins, enkephalins, and dynorphins?

A

Inhibit pain sensation

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37
Q

What is CNS depression?

A

Decreased neuronal excitability

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38
Q

What are CNS depressants?

A

agents that are mainly used to treat anxiety states and sleep disorders

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39
Q

What are hypnotics?

A

Agents that produce drowsiness and encourage the onset and maintenance of a state of sleep

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40
Q

What stages of sleep are amplified with hypnotics, and which are depressed?

A 
Amplified = stage 2
Decreased = REM and 4NREM
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41
Q

True or false: any sedative anxiolytic given in a high enough dose will induce sleep

A

True

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42
Q

What are the four stages of effects of increasing doses of hypnotics?

A

Sedation
Hypnosis
Anesthesia
Coma

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43
Q

What is the cause of death with depressant overdoses?

A

Respiratory depression

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44
Q

What are the two types of sedative hypnotics that have a linear slope of CNS effects, and will cause coma/death at high enough doses?

A

barbituates

Alcohols

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45
Q

What is the major type of drugs that reach a plateau in CNS depression, and are thus less likely to cause deatj?

A

Benzodiazepines

46
Q

Why are depressants used for Szs?

A

Depress the CNS activity

47
Q

What is the MOA of CNS depressants in causing muscle relaxation?

A

inhibition of polysynaptic reflexes and skeletal neuromuscular junction

48
Q

What type of drugs have a -pam suffix? What are the two exceptions to this?

A

Benzodiazepines

Alprazolam
Clorazepate

49
Q

What is flunitrazepam?

A

Roofies

50
Q

What functional group on benzodiazepines is responsible for their sedative hypnotic effects?

A

Electronegative substituent in the 7 position

51
Q

What route of administration is the best for benzodiazepines?

A

Oral

52
Q

How are benzodiazepines metabolized? (what oran/enzymes)

A

In the liver by p450 CYP3A4 + glucuronidation

53
Q

What are the two benzodiazepines that are metabolized into inactive water soluble glucuronides? How fast is this?

A

Lorazepam and oxazepam

Fast metabolism

54
Q

What are the benzodiazepines that are metabolized into weakly active, and have short lived active metabolites?

A

Alprazolam

Triazolam

55
Q

true or false: most benzos have long lived active metabolites

A

True

56
Q

What is the primary indication of, and relative half life of: midazolam?

A

Preanesthetic

Short acting

57
Q

What is the primary indication of, and relative half life of: triazolam

A

Insomnia

Preanesthetic

58
Q

What is the primary indication of, and relative half life of: alprazolam

A

Anxiety, antidepressant

Intermediate acting

59
Q

What is the primary indication of, and relative half life of: clonazepam

A

seizures

Intermediate acting

60
Q

What is the primary indication of, and relative half life of: estazolam

A

insomnia

Intermediate acting

61
Q

What is the primary indication of, and relative half life of: lorazepam

A

anxiety, insomnia, szs, preanesthetic

Intermediate acting

62
Q

What is the primary indication of, and relative half life of: oxazepam

A

Anxiety

Intermediate acting

63
Q

What is the primary indication of, and relative half life of: temazepam

A

Insomnia

Intermediate acting

64
Q

What is the primary indication of, and relative half life of: chlordiazepoxide

A

Anxiety, withdrawal states

Long lasting

65
Q

What is the primary indication of, and relative half life of: clorazepate

A

Anxiety and szs

66
Q

What is the primary indication of, and relative half life of: diazepam

A

Anxiety and withdrawal states

Long lasting

67
Q

What is the primary indication of, and relative half life of: Flurazepam

A

Insomnia

Long lasting

68
Q

What is the primary indication of, and relative half life of: prazepam

A

Anxiety

Long lasting

69
Q

What is the primary indication of, and relative half life of: quazepam

A

Insomnia

Long lasting

70
Q

What are the two drugs used to treat alcohol withdrawal?

A

diazepam and oxazepam

71
Q

What is the influence of age on metabolism of benzodiazepines?

A

Slower hepatic processing

72
Q

What happens to Vd in old age? Why?

A

Goes up due to decreased lean body mass

73
Q

What happens to the rate of elimination of benzodiazepines in the elderly?

A

Decreased

74
Q

What is the MOA of benzodiazepines?

A

Potentiate the effects of GABA(A) receptors, which are Cl- channels, by increasing the frequency of opening of the channels

75
Q

What happens when GABA receptors are depolarized?

A

Cl- influx, increases membrane hyperpolarization and overall neuronal inhibition

76
Q

What are the three effects produced by alpha 1 GABA subunit receptors?

A

Sedation
Anticonvulsant
Anterograde amnesia

77
Q

What are the three effects produced by alpha 2-4 GABA subunit receptors?

A

Anxiolysis

78
Q

What are the major side effects and toxicity of benzodiazepines?

A

Respiratory depression

Anterograde amnesia

79
Q

What is the general principle behind withdrawal symptoms?

A

Opposite effect of taking them will occur

80
Q

What are the relative contraindications to benzodiazepines? (non-obvious ones anyway)

A

Prego

Sleep disorders

81
Q

What are the drugs that have an additive effect on benzodiazepines? (besides obvious) (4)

A

Phenothiazine
Opioids
antihistamines
tricyclic antidepressants

82
Q

What is the antidote to benzodiazepines?

A

Flumazenil

83
Q

What is the MOA of flumazenil?

A

Competitive inhibit that binds to the BZ receptor

84
Q

What is the relative half life for flumazenil?

A

Short duration

85
Q

What are the three newer types of benzodiazepines?

A

Eszopiclone
Zolpidem
Zaleplon

86
Q

What is eszopiclone?

A

Newer benzo (lunesta)

87
Q

What is zolpidem?

A

Newer benzo (ambien)

88
Q

What is zaleplon?

A

newer benzo (sonata)

89
Q

What is the general clinical use of the newer benzos?

A

treat insomnia

90
Q

What is the antidote for newer benzos?

A

Flumazenil

91
Q

What are the four major barbiturates?

A

Pentobarbital
Phenobarbital
Secobarbital
Thiopental

92
Q

What type of drug is pentobarbital?

A

Barbiturate

93
Q

What type of drug is phenobarbital?

A

Barbiturate

94
Q

What type of drug is secobarbital?

A

Barbiturate

95
Q

What type of drug is thiopental?

A

Barbiturate

96
Q

What are the four major clinical uses of barbiturates?

A

Anesthesia
Sedative
Anticonvulsant
Medically induced coma

97
Q

How are barbiturates metabolized How fast is this? What are the metabolites?

A

In the liver by microsomal enzymes

Slow

No active metabolites

98
Q

What is the one barbiturate that is metabolized/excreted by the kidney?

A

Phenobarbital

99
Q

What is the MOA of barbiturates?

A

Increase the duration of the GABA gated chloride channel opening, via NONCOMPETITIVE ation

100
Q

Which increases the rate of opening, and which increases the duration of opening: benzos vs barbiturates?

A

Benzos = increase rate

Barbiturates = duration

101
Q

What is the MOA of ramelteon?

A

Melatonic receptor agonist

102
Q

What are the clinical uses of ramelteon?

A

Sedative agent for insomnia

103
Q

What are the two melatonin receptors, and what is the function of each?

A 
MT1 = sleep onset
MT2 = circadian pattern
104
Q

How are melatonin receptor agonists metabolized?

A

Extensive first pass effect via p450 enzymes

105
Q

True or false: there is a high abuse liability for melatonin receptor agonists like ramelteon

A

False

106
Q

What is the MOA of buspirone? Indication?

A

Partial 5HT-1A receptor agonist

Anxiolytic

107
Q

Is there a high or low abuse liability with buspirone?

A

Low

108
Q

What is the function of 5HT-1A receptors, and how does buspirone’s MOA relate to this?

A

Inhibits presynaptic release of 5HT, thus causes anxiolytic properties of buspirone

109
Q

What is the role of propranolol in anxiolysis?

A

Inhibits the somatic manifestations of anxiety

110
Q

What is the role of hydroxyzine and diphenhydramine in anxiolysis?

A

Mild sedative

111
Q

What is the role of meprobamate in anxiolysis?

A

Sedative

Pharm (73 decks)

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