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Pharmacology > CNS - Sedative And Hypnotics > Flashcards

CNS - Sedative And Hypnotics Flashcards

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1
Q

Alzheimer’s disease is due to

A

Lack of Acetylcholine

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2
Q

Depression is due to

A

Depletion of Norepinephrine, Serotonin and Dopamine

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3
Q

Schizophrenia is due to

A

Excessive amount of Dopamine in the Frontal lobe

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4
Q

Parkinson’s disease is due to

A

Destruction of the substantia nigra and destruction of Dopamine

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5
Q

Epilepsy is due to

A

Lack of inhibitory neurotransmitters such as GABA or

Increase of excitatory neurotransmitters like GLUTAMATE

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6
Q

Huntington’s disease is due to

A

Chronic reduction of GABA

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7
Q

Different phases of sleep

A

Stage 0 (awake) - 1-2% of sleep time
Lying down to falling asleep
Eye movement - irregular or slowly moving

Stage 1 (dozing) - 3-6% of sleep time
Eye movement - reduced
Neck muscles - relaxed

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8
Q

Different phases of sleep

A

Stage 2 (unequivocal sleep)- 40-50% of sleep time
Eye movement - little
Subjects easily aroused

Stage 3 (deep sleep transition) - 5-8% of sleep time
Eye movement - very little
Subject not easily aroused

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9
Q

Different phases of sleep

A

Stage 4 (cerebral sleep) - 10-20% of sleep time
Deepest level of sleep
Metabolic rate is less
Growth hormone secretion is high
Eye movement - fixed
Subjects difficult to arouse
Night terror occurs at this time

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10
Q

Different phases of sleep

A

REM Sleep (Rapid eye movement) / Paradoxical sleep
20-30% of sleep
Eye movement - marked, irregular & rapid eye movement
Dreams and nightmares occur which can be recalled
HR & BP Fluctuates
Respiration - irregular
Muscles - fully relaxed
Erection - males

Stages 0-4 & REM Sleep - 80-100mins

Stages 1-4& REM sleep repeated cyclically

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11
Q

Classification of Benzodiazepines

Hypnotic -

A

diazepam, flurazepam, nitrazepam, alprazolam, lorazepam, temazepam, triazolam

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12
Q

Classification of Benzodiazepines

Antianxiety-

A

diazepam, chlordiazepoxide, oxazepam, lorazepam

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13
Q

Classification of Benzodiazepines

Anticonvulsants -

A

clonazepam, lorazepam, diazepam

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14
Q

Classification of Benzodiazepines

Non- benzodiazepine hypnotics

A

Zolpidem, zaleplon, zopiclone, eszopiclone

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15
Q

Barbiturates

Long-acting

A

Phenobarbitone

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16
Q

Barbiturates

Short acting

A

Butobarbitone, Pentonarbitol

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17
Q

Barbiturates

Ultra short-acting

A

Thiopental, Methohexital

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18
Q

Atypical Anxiolytics

A

Buspirone, Ipsapirone, Gepirone

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19
Q

Beta-adrenoreceptor antagonist

A

Propranolol

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20
Q

Miscellaneous

A

Melatonin, Ramelteon, Triclophor

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21
Q

MOA of Barbiturates

A

Acts at the GABA: BZD receptor chloride channel complex

Potentiates the GABA-mediated inhibitory effects by INCREASING THE DURATION OF CHLORIDE CHANNEL OPENING

At higher doses, it INCREASES THE CHLORIDE ION CONDUCTANCE (GABA mimetic action)

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22
Q

Pharmacokinetics of Barbiturates

A

Metabolized by phase 1 and 2 processes

Excreted through urine

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23
Q

Actions of Barbiturates on CNS

A

Sedation and hypnosis
Induce sleep
Prolong sleep duration
Alters NREM & REM sleep cycle
Anaesthesia
Anticonvulsant

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24
Q

Actions of Barbiturates on Respiratory System

A

Respiratory Depression

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25
Actions of Barbiturates on CVS
Higher doses decrease BP & HR and depress Myocardium
26
Actions of Barbiturates on GIT
Decrease in tone and amplitude of GIT smooth muscles
27
Actions of Barbiturates on Liver
Enzyme induction drug interactions
28
Therapeutic Uses of Barbiturates In anaesthesia -
ultra-short-acting (Thiopental) as inducing agent
29
Therapeutic Uses of Barbiturates As Anticonvulsants -
long-acting (Phenobarbital)
30
Therapeutic Uses of Barbiturates In Neonates
To treat Hyperbilirubinemia Increases the activity of glucuronyl transferase - increase the conjugation of bilirubin - decrease the risk of Kernicterus
31
Contraindications in the use of Barbiturates
Liver dysfunction Kidney Disease Sever pulmonary insufficiency Acute intermittent porphyria - Barbiturates cause induction of ALA -synthase enzyme in mitochondria - leads to increased porphyrins
32
Acute barbiturate poisoning Cause and presentation of pt.
Mostly suicidal, sometimes accidental Patient is flabby and comatose with shallow and failing respiration, fall in BP
33
TXT of Acute barbiturate poisoning
No specific antidote Maintenance of pt. Vitals Gastric lavage - activated charcoal * ALKALINE DIURESIS - SODIUM BICARBONATE Hemodialysis and hemoperfusion
34
Drug Interaction with barbiturate
Induce metabolism of warfarin, steroids, OCP, chloramphenicol, tolbutamide Alcohol, antihistamines, opioids - CNS Depression Phenobarbitone reduces the absorption of Griseofulvin from gut
35
Benzodiazepines?
Enhances the effects of neurotransmitter GABA-A which is an inhibitory resulting in sedative, hypnotic, anxiolytic, Anticonvulsants and muscle relaxant properties
36
MOA of Benzodiazepines
Binds specific site at the GABA-BZD Receptor Enhances the receptor affinity for GABA *INCREASES THE FREQUENCY OF OPENING OF CL CHANNEL Increase cl conduction Neural membrane hyperpolarization Decrease sympathetic transmission CNS depression
37
Pharmacokinetics of Benzodiazepines; does it cross BBB & metabolised by?
Except Midazolam, all can be given orally * Metabolised in liver by CYP3A4 and CYP2CI9 Excreted in urine Crosses BBB
38
Contraindication of Benzodiazepines
Crosses BBB - Contraindicated in PREGNANCY
39
Therapeutic use of Benzodiazepines
Txt anxiety & insomnia Preanaesthetic medication Skeletal muscle relaxants Anticonvulsant *TXT ALCOHOL WITHDRAWAL
40
AE of Benzodiazepines
Dose-dependent drowsiness, fatigue, disorientation, lethargy and psychomotor skills impairment Fast IV injection - cardiac arrest BZD WITHDRAWAL INCLUDES Anxiety, insomnia, impaired conc., headache, irritability, tremors, palpitation and *VIVID DREAMS
41
Flunitrazepam use and effect
Sedative amnesic effect Misused in sexual assaults to wipe out memory of events
42
Drug interaction of Benzodiazepines
*BZD potentiates the effects of CNS depressants like alcohol, hypnotic, neuroleptics *Smoking decreases the activity of BZDS *Enzyme inhibitors like Cimetidine and Ketoconazole enhance BZD action
43
Benzodiazepine antagonists
Flumazenil
44
Benzodiazepine antagonists MOA
Selective competitive antagonist of Benzodiazepine Competes with BZD agonist and INVERSE AGONIST - reverse their action Injected IV Action starts in seconds and lasts for 1-2hrs Elimination half-life - 1 hr
45
Benzodiazepine antagonists Use
Reverse BZD anaesthesia BZD overdose
46
Benzodiazepines over Barbiturates as Sedative and Hypnotics. Why?
*BZD have flat DRC whereas Barbiturates have a steep DRC BZD doesn't effect REM sleep and cause less hangover whereas Barbiturates cause marked suppression of REM sleep, hence rebound increases REM sleep on withdrawal *BZD are not enzyme inducers, less likely to cause drug interactions whereas Barbiturates are potent enzyme inducers
47
Benzodiazepines over Barbiturates as Sedative and Hypnotics. Why?
Bzds has low abuse liability whereas barbiturates exhibit tolerance as well as physical and psychological dependence *Bzds cause amnesia with no phenomenon of automatism while barbiturates are characterized by amnesia with automatism
48
Benzodiazepines over Barbiturates as Sedative and Hypnotics. Why?
Bzds shows no hyperalgesia while it is seen with barbiturates *Bzds poisoning can be treated with Flumazenil an antagonist while no antidote for barbiturates poisoning
49
Cause and Txt of Insomnia Last < 7 days
Caused by Brief environmental or situational stressors (jet lag, overnight train journey, shift work) Sleep hygiene rules Hypnotics should be used at the lowest dose
50
Cause and Txt of Insomnia 1 to 3 weeks
Causes by personal stressors such as illness, grief or occupational problems Education about sleep hygiene Intermittent use of Hypnotics - with the pt. Skipping a dose after 1-2 days of good sleep
51
Cause and Txt of Insomnia >3 weeks
No specific stressor Underlying disease or personality disorder Non-pharmacological measures Treatment of underlying illness Intermittent use of long-acting hypnotic may be used
52
Importance of Non-pharmacological measures
Effective in reducing sleep onset latency
53
Non-benzodiazepine hypnotics
Zolpidem, Zopiclone, Zaleplon Also called Z drugs
54
Moa of Non-benzodiazepine hypnotics
Not BZDs *Acts on alpha 1 BZD site Produce sedative and hypnotic and weak anxiolytic action with negligible anticonvulsant, central muscle relaxant and amnesic action Least disruption of sleep architecture Least abuse potential Used for both transient and short-term insomnia
55
Overdose of Non-benzodiazepine hypnotics txt
Antagonized by Flumazenil (benzodiazepine competitive antagonist)
56
Moa of Zolpidem
Imidazopyridine derivative Rapid onset (30-60mins) *Reduces the sleep latency and prolongs the total sleep duration Sedation action > anxiolytic
57
Moa of Zolpidem cont’d
Hypnotic is seen for a week without rebound insomnia after the withdrawal *food reduces the absorption In elderly and hepatic dysfunction dose should be reduced to half
58
Late night administration of Zolpidem may cause
Delayed reaction time, morning sedation and anterograde amnesia
59
Moa of Zaleplon
Pyrazolopyrimidine derivative Sustained efficacy on prolonged use - no tolerance and no rebound insomnia
60
Late-night administration of Zaleplon may cause
Does not cause Delayed reaction time, morning sedation and anterograde amnesia - can be taken by pt. who is awake in the middle of the night and not able to sleep
61
Moa of Zolpiclone
Cuclopyrolone derivative Useful for short-term treatment of insomnia *Prolongs stage 3 and 4 sleep but does not suppress REM sleep
62
AE of Zolpiclone
Metallic taste, reduced alertness and mental disturbance
63
Moa of Eszopiclone
Active enantiomer of Zolpiclone *Reduces sleep latency, number of awakenings, increase sleep time and helps in maintenance of sleep Used for short and long term treatment of insomnia for 1 yr
64
AE of Eszopiclone
Bitter taste
65
Moa of Melatonin
Hormone synthesized and released from pineal gland during night Maintains the circadian rythm and sleep-wakefulness cycle Reset the circadian rythm which is disturbed in jet lag
66
Use of Melatonin
As Chronobiotic Low dose - increases the tendency to fall asleep but no CNS depression High dose - produce hypnotic effects
67
What is a Chronobiotic
Agents that reset the biological clock or timing of circadian rhythm
68
Types of melatonin receptors
3 types of melatonin receptors - MT1, MT2, MT3
69
Action of the 3 types of melatonin receptors
MT1 and MT2 concerned with circadian rhythm MT3 - related to intraocular tension
70
Moa of Ramelteon
Selective MT1 and MT2 receptor agonist - Used for txt of insomnia Reduces sleep latency and improves sleep time Suitable for sleep onset insomnia More efficacious than melatonin but less efficacious than benzodiazepine
71
Moa of Ramelteon cont’d
No next day sedation No rebound insomnia, no addiction liability
72
Ramelteon leads to
Increased level of prolactin Decrease level of testosterone
73
AE of Ramelteon
Headache, dizziness, fatigue, somnolence
74
Modafinil moa
Sedative hypnotic Wake promoting agent Low abuse liability
75
Use of Modafinil
For hypersomnias (narcolepsy or sleep apnoea syndrome) Maintain wakefulness in shift work sleep disorder
76
Suvorexant moa
Orexin receptor antagonist Acts as a central promoter of wakefulness Hasten sleep onset, sleep maintenance and increase the total sleep duration
77
Suvorexant is metabolized by
CYP3A4 Excreted in faeces
78
AE of Suvorexant
Dose-related Day time somnolence. Impaired driving, unconscious night time behaviour
79
What are the atypical anxiolytics
Buspirone, Ipsapirone, Gepirone
80
Moa of atypical anxiolytics
* Acts as a Partial Agonist primarily at brain 5HT1A receptors * Not suitable in case of acute anxiety No muscle relaxant, anticonvulsant or hypnotic action Minimum abuse liability Less psychomotor skill impairment and does not potentiate the CNS depressant effects of alcohol
81
AE of atypical anxiolytics
Tachycardia, nervousness, GIT distress
82
What are the beta-adrenoreceptor antagonist
Propranolol
83
Use of beta-adrenoreceptor antagonist
To reduce anxiety under conditions which provoke nervousness and anxiety Blocks peripheral manifestation of anxiety (palpitations, tremors)
84
Site of action of sedatives
Limbic system (that regulates thought and mental function)
85
Site of action of hypnotics
Midbrain and ascending reticular formation (which maintains wakefulness)

Pharmacology (8 decks)

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