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2H- Pharmacology- Sedative and Hypnotics > Introduction to the Pharmacology of CNS Drugs by Castor > Flashcards

Introduction to the Pharmacology of CNS Drugs by Castor Flashcards

1
Q

§Nearly all drugs with CNS effects act on specific receptors that modulate neurotransmission

A
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2
Q

_________ have nonspecific actions on membranes

A

General anesthetics and alcohol

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3
Q

___________- fast action potentials

A

Voltage gated channels

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4
Q

____________- weakly sensitive to membrane potential;

fast synaptic transmission, typical of heirarchical CNS pathways

A

Ligand gated channels

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5
Q

Central neurotransmitters

A
  • §Amino acids- GABA, Glycine, Glutamate
  • §Monoamines- Dopamine, Norepinephrine
  • §Peptides- opioids, cholecystokinin
  • §Nitric oxide
  • §Endocannabinoids
    *
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6
Q

Central neurotransmitters

§Amino acids-

A

GABA, Glycine, Glutamate

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7
Q

Central Neurotransmitters

Monoamines

A

Dopamine, Norepinephrine

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8
Q

peptides-

A

opioids, cholecystokinin

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9
Q

Neurotransmitter Mechanisms

Acetylcholine

A

§Acetylcholine: M1 and Nicotinic- Excitatory,

                       M2 Inhibitory
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10
Q

Neurotransmitter Mechanisms

dopamine

A

inhibitory

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11
Q

Neurotransmitter mechanism

§GABA:

A

inhibitory

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12
Q

Neurotransmitter mechanism

§Glutamate

A

: Excitatory except at ACPD receptor- inhibitory

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13
Q

Neurotransmitter mechanism

§Glycine:

A

inhibitory

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14
Q

Neurotransmitter mechanism

§Serotonin:

A

Excitatory except at 5HT1A- inhibitory

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15
Q

Neurotransmitter mechanism

§NE:

A

Excitatory at Alpha 1 and Beta I,

Inhibitory at Alpha 2 and Beta 2

**Pansin mo kpag 2 inhibitory? **Kasi mga 2nd placer( mistress), inhibitors ng happiness ng love sa first wife!!!!

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16
Q

Neurotransmitter mechanism

§Histamine

A

: Excitatory

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17
Q

Neurotransmitter mechanism

§Histamine

A

inhibitory

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18
Q

Neurotransmitter mechanism

§Opioids:

A

inhibitory

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19
Q

Neurotransmitter mechanism

§Tachynins:

A

Excitatory

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20
Q

What is with GABA?

A
  • §Major inhibitory neurotransmitter in the CNS
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21
Q

____________ potentiate GABAergic inhibition at all levels ot the neuraxis ( SC, Hypothalamus, Hippocampus, Substantia Nigra, Cortex)
§BZs increase the effiiency of GABAergic synaptic inhibition
§Increased frequency of channel opening events

A

BZs

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22
Q

________ also facilitate GABA at multiple sites but increases the duration of GABA gated Cl channel openings, and a high doses, are GABA mimetic, directly activating CL channels
§

A

Barbiturates

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23
Q

_______ also depress excitatory neurotransmitters (glutamic acid)
§

A

Barbiturates

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24
Q

Sedative Hypnotic Drugs

A
  • §Induces drowsiness and sleep
  • §Antianxiety agents
  • §Sedation
  • §General anesthesia
  • §Respiratory and cardiovascular depression
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25
Q

§Most commonly used anxiolytics, safer than barbiturates
§Indicated for anxiety and insomnia,
§Alcohol and other withdrawal symptoms
§Spasticity and skeletal muscle spasm
§Status epilepticus
§Petit mal seizure

A

BZs

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26
Q

What is the pharmacologic property of BZs?

A

§Acts by potentiating neural inhibitions that are normally mediated by GABA.

§Binds to receptors near those of GABA, increases GABA binding, which in turn decreases neuronal activity.

§Mechanism of action requires GABA release, neuronal depression is self limiting ( accounts for drug safety).

.

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27
Q

§Effects on respiration are minimal, with hypnotic doses having no effect.
§
§Pre anesthetic doses decrease BP and increase HR

A

BZs

28
Q

What is the Lipophilicity of BZs?

A

varies by more than 50 fold

29
Q

BZs Crosses the BBB?

A

Yes

CSF levels = Plasma free drug levels

§70-99% of BZs or its metabolites are bound to plasma proteins

30
Q

Does BZ undergo hepatic metabolism?

A

Undergo extensive metabolism by hepatic microsomal enzyme systems

§Produces active metabolites

31
Q

What is the effect of BZs on sleep latency?

A

Decreases sleep latency = increases total sleep time

32
Q

Bzs Decreased time in REM sleep, except?

A

Flurazepam ( does not decrease REM sleep)

33
Q

Classification according to duration of action

A

§Short acting : less than 24 hours
§
§Long acting: over 24 hours

34
Q

Short acting BZs ( , 24 Hours)

A
  • §Oxazepam
  • §Triazolam
  • §Quazepam
  • §Alprazolam:
  • §Lorazepam
  • §Temazepam
  • §Midazolam:
35
Q

_________ : BZs used for sleep induction, rebound insomnia common

A

§Triazolam

36
Q

:BZs used for Panic disorders

A

Alprazolam

37
Q

:BZs Status epilepticus

A

Lorazepam

38
Q

: BZs rapid onset, short t1/2 Used for induction of anesthesia

A

Midazolam

Si Mids pala tulog sa class!!!!

39
Q

Long acting BZs ( > 24 Hours)

A
  • Clorazepate:
  • Diazepam:
  • Flurazepam:
  • Chloridazepoxide

CDCF

40
Q

Long acting BZs ( > 24 Hours)

Used in epilepsy

A

Clorazepate:

41
Q

Long acting BZs ( > 24 Hours)

: most commonly used BZ

A

Diazepam

42
Q

Long acting BZs ( > 24 Hours)

no rebound insomnia noted upon discontinuation

A

Flurazepam

43
Q

Long acting BZs ( > 24 Hours)

Ethanol withdrawal

A

Chloridazepoxide:

44
Q

Indications for use BZs

A
  • Anxiety and insomnia: Anxiolytic is the most common use
  • Alcohol and some withdrawal syndromes: usually Chlordiazepoxide
  • Spasticity and skeletal muscle spasm: Diazepam IV, Lorazepam
  • Petit mal seizures- Clonazepam
45
Q

Side effects and toxicity Bzs

A
  • §Drowsiness, Ataxia, Confusion, impaired short term memory, blurring of vision, Vertigo, Headache
  • §Impaired performance of complex tasks such as driving, operating machinery and answering questions via the TC exam format.
  • §Withdrawal syndromes: seizures, psychoses may occur with sudden discontinuation of the drug
  • Hypotension
  • Blood dyscrasias
  • Allergy, Jaundice ( RARE )
  • Respiratory depression
  • Teratogenic effects are controversial
  • Tolerance occurs, (+) cross tolerance with Barbiturates, Methaqualone and to a certain extent, ethanol
  • Dependence/ Abuse§
46
Q

BZs Overdosage is rarely fatal and recovery is usually complete

Fatalities usually occur when used with other drugs

A
47
Q

Drug Interactions of BZs

§Increase BZ levels:

A
  • Paracetamol: decreased diazepam renal excretion
  • Cimetidine, Disulfiram, Ethanol, INH, Valproic acid decreases metabolism
  • Valproic acid: displacement from binding sites
48
Q

Drug Interactions of BZs

Decrease levels

A

Antacids: decrease absorption

OCP, RIF: Increased metabolism

49
Q

Drug Interactions BZs

A
  • §BZs increase CNS depressive effects of Alcohol and other agents
50
Q

What is the effect BZs on Digoxin?

A

Decrease renal excretion Digoxin

51
Q

What is the effect of BZs on Levodopa?

A

decrease the effect Levodopa

52
Q

What is the effect of BZs + Lithium?

A

** Hypothermia**

53
Q

Bzs has Prolonged neuromuscular blockade with _________

A

succinylcholine

54
Q

Newer drugs for Anxiety and sleep Disorders

A

§Buspirone

§Zolpidem

§Zaleplon

55
Q

Describe Buspirone.

A
  • Non BZ anxiolytic
  • Interferes with certain 5 HT receptors and can also bind to dome dopaminergic receptors
  • No muscle relaxant or anticonvulsant activity
  • Causes less psychomotor impairment than Diazepam,
  • does not affect driving
56
Q

What are the side effects of Buspirone?

A

include headache and dizziness, dose dependent pupillary constriction
§

57
Q

Buspirone Increased BP with ?

A

MAOIs

58
Q

What are the Analogs of Buspirone?

A

Ipsapirone, Gepirone, Tandospirone

59
Q

What is with Zolpidem?

A
  • Minimal muscle relaxing and anticonvulsant properties
  • Amnestic effects with doses greater than recommended. Amnesia is common during exams.
  • Can suppress REM sleep at higher doses
  • Respiratory depression at high doses and with Ethanol
    *
60
Q

What is wtih Zaleplon?

A
  • Rapid GI absorption
  • Decreases sleep latency but has little effect on total sleep time
  • Amnestic effects and next day impairment of psychomotor performance
  • Low potential for tolerance, withdrawal and dependence
61
Q

BZ antagonist FLUMAZENIL

A
  • High affinity to the BZ receptor
  • Competitive antagonist
  • Blocks BZ action
  • Does not antagonize CNS effects
  • Effects on respiratory depression is less predictable
  • (+) arrhythmias when used for BZ overdose + TCA
  • Improvement of mental status when used in hepatic encephalopathy
62
Q

What are your Barbiturates?

A
  • Thiopental:
  • Phenobarbital:
  • Amobarbital, Pentobarbital, Secobarbital:
  • Barbiedal:
63
Q

What is your ultra short acting ( 30 Minutes) Barbiturates?

A

Thiopental

64
Q

What is your longest acting Barbiturates?

A

Phenobarbital

65
Q

What are your Short acting barbiturates?

A
  • Amobarbital,
  • Pentobarbital,
  • Secobarbital
66
Q

What is your non acting barbiturates?

A

Barbiedal

67
Q
A

2H- Pharmacology- Sedative and Hypnotics (13 decks)

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