Sedatives And Hypnotics Block III Flashcards

1
Q

What is a sedative

A

reduces anxiety and exerts a calming effect with little or no effect on motor or mental function

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2
Q

Hypnotic

A

produces drowsiness and encourages the onset and maintenance of a state of sleep resembling natural sleep

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3
Q

What are the two major classes of Sedatives

A

BZD and barbiturates

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4
Q

How are most anxiety DO tx acutely

A

BZD, Barbiturates, SSRIs

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5
Q

What happens when GABA binds to the GABA receptor

A

When GABA binds to the GABA receptor it results in relaxation and sedation

Major inhibitor receptor

Cl- channel

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6
Q

Barbiturates are no longer indicated for what sleep DO

A

Insomina

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7
Q

What are the disadvantages of barbiturates

A

ability to cause coma in toxic doses, physical dependence, and severe withdrawal symptoms

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8
Q

What is methohexital

A

A barbituate that is shirt acting and used for anesthesia

C-IV

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9
Q

What is Pentobarbital

A

Short acting barbiturate that is C-II used for anesthesia

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10
Q

What is secobarbital

A

A short acting barbituate that is PO only and used for anesthesia

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11
Q

What is amobarbital

A

A short acting barbituate that is used for anesthesia, C-II

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12
Q

What are the ADE of Barbituates

A

CNS depression, hangover effect, WTHDRAWL

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13
Q

What are the clinical uses of barbituates

A

Induction of anesthesia, Status epilepticus, Insomina

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14
Q

What are the severe ADE of barbituates

A

SJS, bone marrow suppression, hepatotoxicity, osteopenia

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15
Q

What medication can be used for generally every SZR type

A

Phenobarbital

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16
Q

What are the ADE of phenobarbital

A

Bradycardia, Sex dysfunction, Drowsiness, cognitive impairment

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17
Q

What are the short acting BZD

A

T.O.M.

Triazolam
Oxazepam
Midazolam

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18
Q

What are the Intermediate acting BZD

A

T.E.A.L

Temezepam
Estazolam
Alprazolam
Lorazepam

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19
Q

BZD with long half life’s have more or less hangover and break through S/s

A

Withdrawal symptoms may be less pronounced
Less breakthrough symptoms
More “hangover” symptoms

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20
Q

BZDs with short half lives have more or less break through s/s

A

Tolerance of the hypnotic effect develops rapidly

Withdrawal is common (breakthrough symptoms)

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21
Q

What are the clinical uses of BZDs

A

Anxiolytic (Sedative)

Hypnotic: all benzodiazpines induce sleep if high enough doses are given

Muscle Relaxation

Anticonvulsant

Anesthesia/Amnesic actions

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22
Q

Do BZDs effect pain >?

A

NO !

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23
Q

Which two BZDs are indicated for alcohol withdrawal

A

Lorazepam and Diazepam

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24
Q

Which BZD is perferred in liver dz

A

Lorazepam

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25
Q

What should the BZD treatment period be restricted to

A

3-4 months

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26
Q

If you must use BZD in the elderly which should be used

A

LOT

Lorazepam
Oxazepam
Temazepam

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27
Q

What is the reversal agent for BZD

A

Flumazenil

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28
Q

What is the clinical use of busprione

A

Management of anxiety disorders or short-term relief of the symptoms of anxiety

Slower onset then BZD, but no abuse potential

Appropriate use is to start patient on BZD then switch while tapering BZD

Often used as a second line agent or when BZD should avoided

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29
Q

What is the MOA and clincal use of Zolpidem

A

acts on the benzodiazepine receptor by enhancing GABA activity (not chemically related to BZD)

Clinical Use:
Only use is for insomnia
IR for difficulty going to sleep
CR for sleep maintenance issues

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30
Q

What are the advantages of zolpidem to BZD

A

Less dependence and cravings

Lower risk of tolerance and withdrawal

Lacks respiratory depressant properties

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31
Q

What is the clinical use of Eszopiclone

A

Sleep initiation and maintenance

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32
Q

What are the ADE of the sleep drug eszopiclone

A

Metallic taste, SI, abnormal thinking (hallucinations)

Causes functional dependence

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33
Q

What is the MOA and clin use of Zaleplon

A

acts on BZD receptor, but is chemically not related to BZD

Clinical Use:
Short-term treatment of insomnia

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34
Q

Which of the hypnotics is least likes to causes daytime somnolence

A

Zaleplon

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35
Q

What is the MOA and Clincal use of Surorexant

A

Mechanism of Action: orexin-receptor antagonist

Clinical Use: treatment of insomnia

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36
Q

In gerenal the ADE of sleep agents and hypnotics are..

A

SI, somnolence, Hallucinations, abnormal thinking

37
Q

What is the MOA and clincal use of Ramelton

A

Mechanism of Action: melatonin receptor agonist.
[Melatonin maintains circadian rhythm (sleep-wake cycle)]

Clinical Use:
Treatment of insomnia characterized by difficulty with sleep onset

Not limited to short-term use

In studies only showed a 4.6min improvement in sleep latency and 7.3min increase in total sleep time

38
Q

What is the MOA of clinical use of Tasimelteon

A

melatonin receptor agonist

Clinical Use:
Non-24-hour sleep-wake disorder that is generally present in blind patients due to lack of stimulus from the sun

39
Q

What sleep DO is useful to blind pts.

A

Tasimelteon

40
Q

What is the non Pham approach to insomnia

A

Improve sleep hygiene
Sleep restrictive therapy
CBT

41
Q

What TCA can be used for insomnia

A

Amitryptyline

42
Q

What SRAs can be used for insomnia

A

Trazadone

Mirtazapine

43
Q

What are the DOC for anxiety DO

A

BZDs

44
Q

What drugs can be used in monotherapy of GAD if antidepressant meds are not necessary

A

Busprione and Pregabalin

45
Q

What are 1st line agents in social anxiety

What are second line

A

1: SSSRI, SNRI
2: Gabapentin and pregablin

46
Q

What anticonvulsants can be used in PTSD

A

Tiagabine, Topiramate, divalproex

47
Q

What is the most severe form of alcohol withdrawal

A

Delirium termens

48
Q

What is teh 1st line for prevention of SZR in alcohol withdrawal

A

BZDs

49
Q

What is the most frequently used medication in outpatient alcohol detox

A

Chlordiazepoxide

50
Q

What is wernickes encephalopathy

A

Presence of neurological symptoms, a triad of confusion, ataxia and ophthalmoplegia associated with ethanol withdraw due to chronic alcoholism

51
Q

How do we treat wernickes encephalopathy

A

IV mixture used to treat acute alcohol intoxication

Banana Bag – Multi Vitamins, Thiamine and Folic Acid in 1L NS

Electrolytes: monitor level

Vitamins: Folic acid and vitamin B12

Fluid Therapy

52
Q

What are the 1st line agents in alcohol abuse?

What are the second line

A

First Line:
Naltrexone (Vivitrol)
Acamprosate (Campral)

Second Line:
Disulfiram (Antabuse)
Topiramate (Topamax)
Gabapentin (Neurontin)
Baclofen (Lioresal)
SSRI’s
53
Q

How does naltrexone effect the liver

A

Liver toxicity (5x increase in liver enzymes)

54
Q

What is the MOA and clincal use of Acamprosate

A

Structurally similar to GABA; principal effect is believed to come from antagonism of glutamate neurotransmission.

Clinical Use:
Maintenance of abstinence from alcohol
Must be taken three times a day

55
Q

How is Acamprosate metabolized

A

Not metabolized by the liver

Excreted by kidneys; reduce or stop if renal insufficiency

56
Q

What is the MOA of disulfiram

A

Inhibits aldehyde dehydrogenase (ALDH), blocking the metabolism of ethanol at the acetaldehyde step.

If a patient drinks alcohol while taking disulfiram, it will cause them to have a “Disulfram Reaction”

57
Q

How does Disuflram effect alcohol cravings

A

Does NOT reduce cravings for alcohol, high relapse rate

58
Q

How should disulfiram be used

A

Has not shown better efficacy compared to placebo

Direct observed therapy: was effective

Only for patients who are motivated

Counseling, monitoring and support programs should be used in conjunction with disulfiram therapy

59
Q

What is the most common psych DO in children

A

ADHD

60
Q

What is the non-pharm approach to ADHD

A

Food additives, Refined Sugar, Food Sensitivity

61
Q

What should be checked prior to starting Pharm Tx on a ADHD child

A

Prior to initiating pharmacologic treatment check BP, HR, & Ht/Wt

62
Q

What are the non stim for ADHD

A

Atomoxetine
Clonidine
Guanfacine

63
Q

All amphetamine and stimulant derivatives are schedule what?

A

C-II

64
Q

What are the clin uses of stimulant and amphetamines

A

ADHD, narcolepsy, Obesity

65
Q

What are the ADE of Amphetamines and Stimulants

A

Insomina, SZR, tremor, INC. BP, HR, NVD anorexia
Decreased growth rate

Priapism in children and adults

66
Q

What is the contraindications for amphetamines and stimulants

A

Contraindicated in patients with hypertension, CV diseases, hyperthyroidism, and glaucoma

67
Q

Nonstimulants are 1st line therapy in pts with ADHD if…

A

There is a concern for medication abuse

A strong family/patient preference not to use a stimulant

The patient has a condition in which stimulants are not recommended (e.g. cardiac disease, glaucoma, loss of appetite)

68
Q

What is the MOA and Clin use of Atomoxetine

A

Not a controlled substance

First non-stimulant drug approved for ADHD

Mechanism of Action: blocks the reuptake of norepinephrine

Clinical Use:
Monotherapy for the treatment of ADHD in patients six years and older
Proven effective but not better or worse than stimulants
May be used as a first line agent

69
Q

What is a first line non stimulating monotherapty drug for ADHD in chlidren older than 6 yo

A

Atomoxetine

70
Q

What is the MOA and Clin use of Clonidine

A

Not a controlled substance

Mechanism of Action: central α2 agonist

Clinical Use:
Alternative for children who are intolerant to stimulants especially those with tics

FDA approved for monotherapy or as an add-on to stimulants

Concurrent disease treatment:
Impulsive behavior
Tourette’s Syndrome

71
Q

What non stimulant can be used for impulsive behavior and Tourette’s

A

Clonidine

72
Q

What is the MOA and Clin use of guanfacine

A

Not a controlled substance

Mechanism of Action: central α2 agonist

Clinical Use:
FDA approved for monotherapy or as an add-on to stimulants

Alternative for children who are intolerant to stimulants

Indicated for children with tic disorders

73
Q

Are SSRI useful in ADHD

A

NO!

74
Q

Which TCAs can be used in ADHD

A

Imipramine, and desipramine

75
Q

What is the clin use of Modafinil and Armodafinil

A

Mechanism of Action: Not fully known; May decrease GABA-medicated neurotransmission

Clinical Use: improve wakefulness in adult patients with excessive sleepiness associated with obstructive sleep apnea (OSA), narcolepsy or shift work disorder (SWD)

76
Q

What drugs can be used in obstructive sleep apnea and, narcolepsy, and shift work DO

A

Modafinil and Armodafinil

77
Q

What is the MOA and clin uses of caffeine

A

Caffeine is a methylxanthine (theophylline is a derivative)
Mechanism of Action: (multiple possible explanations)
Antagonist of adenosine receptors
Increases of cAMP by inhibiting phosphodiesterase
Increases medullary response to CO2

Clinical Use:
For migraine headaches in combination with other medications
Apnea of prematurity (neonates)

Non clinical uses:
Overcoming sleep deprivation, mental acuity and physical performance

78
Q

What is an overweight BMI

A

Greater than 25,

Greater than 40 is obesity

79
Q

What is the non pharm approach to Obesity

A

Behavior modification

Diet and Excercise

80
Q

Who is bariatric surgery indicated for

A

BMI greater than 35

81
Q

What is the pharm approach to obesity

A

Used to support non-pharmacologic therapy for patients with a BMI > 30kg/m2, OR BMI >27kg/m2 with a comorbidity (e.g. dyslipidemia, hypertension, type 2 diabetes)

In general, advise discontinuing medication if at least 5% weight loss is not achieved after 12 weeks of use

82
Q

How are amphetamines used in obesity control

A

Increase norepinephrine and dopamine release which suppresses appetite and increases thermogenesis

The dopaminergic activity is linked to their addictive properties (C-II)

These can lead to rebound binge eating, weight gain and depression when stopped

Rarely used specifically for obesity

83
Q

How are SSRIs used in obesity Tx

A

(fluoxetine and sertraline)

Suppress appetite and have been shown to be effective in weight loss but after one year but regaining weight is likely

84
Q

What is the MOA and Clin use of Phentermine/ Topiramate in Obesity

A

Mechanism of Actions:

Phentermine: promotes appetite suppression and decreased food intake secondary to its sympathomimetic activity

Topiramate: unknown regarding weight loss, but may cause appetite suppression and satiety through enhanced GABA activity

Should be taken in the morning to avoid insomnia

Taper to avoid seizures

85
Q

What ADE of topiramte

A

advanced atherosclerosis, cardiovascular disease, moderate to severe hypertension, hyperthyroidism

86
Q

What is the MOA and clin use of orlistat

A

Lipase Inhibitor: reduces fat absorption by inhibiting GI lipase activity in the small intestine
30% of ingested fat is excreted in the feces

Obestity

87
Q

What is the MOA of liraglutide

A

Type 2 Diabetic Agent (Victoza)

Mechanism of Action: GLP-1 agonist

88
Q

Can liraglutide be used in obese pts that are pregnant

A

NO

89
Q

What are the ADE of Liraglutide used for obesity

A

Pancreatitis

Symptomatic hypoglycemia is rare in patients without diabetes, but more in patients with diabetes
Suggest reducing the insulin dose by ≥ 20%
Suggest reducing sulfonylurea doses by ≥ 50%