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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

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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
§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**
BZs
26
What is the pharmacologic property of BZs?
§Acts by **potentiating neural inhibitions** that are **normally mediated by GABA.** §**Binds to receptor**s *_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). .
27
§Effects on respiration are minimal, with hypnotic doses having no effect. § §Pre anesthetic doses decrease BP and increase HR
BZs
28
What is the Lipophilicity of BZs?
varies by more than 50 fold
29
BZs Crosses the BBB?
Yes CSF levels = Plasma free drug levels §70-99% of BZs or its metabolites are bound to plasma proteins
30
Does BZ undergo hepatic metabolism?
Undergo extensive metabolism by hepatic microsomal enzyme systems **§Produces active metabolites**
31
What is the effect of BZs on sleep latency?
**Decreases** sleep latency = **increases total sleep time**
32
Bzs Decreased time in REM sleep, **except**?
**Flurazepam (** does not decrease REM sleep)
33
Classification according to duration of action
§Short acting : less than 24 hours § §Long acting: over 24 hours
34
Short acting BZs ( , 24 Hours)
* §**O**xazepam * **§T**riazolam * §**Q**uazepam * §**Al**prazolam: * §**L**orazepam * §**T**emazepam * §**M**idazolam:
35
\_\_\_\_\_\_\_\_\_ : BZs used for sleep induction, rebound insomnia common
§Triazolam
36
:BZs used for Panic disorders
Alprazolam
37
:BZs Status epilepticus
Lorazepam
38
: BZs rapid onset, short t1/2 Used for **induction of anesthesia**
Midazolam Si Mids pala tulog sa class!!!!
39
Long acting BZs ( \> 24 Hours)
* Clorazepate: * Diazepam: * Flurazepam: * Chloridazepoxide CDCF
40
Long acting BZs ( \> 24 Hours) Used in epilepsy
Clorazepate:
41
Long acting BZs ( \> 24 Hours) : most commonly used BZ
Diazepam
42
Long acting BZs ( \> 24 Hours) no rebound insomnia noted upon discontinuation
Flurazepam
43
Long acting BZs ( \> 24 Hours) Ethanol withdrawal
Chloridazepoxide:
44
Indications for use BZs
* 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
Side effects and toxicity Bzs
* §**Drowsiness**, Ataxia, Confusion, impaired short term memory, blurring of vision, Vertigo, Headache * §**Impaired performance of complex task**s 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
BZs Overdosage is rarely fatal and recovery is usually complete Fatalities usually occur when used with other drugs
47
Drug Interactions of BZs §Increase BZ levels:
* **Paracetamol**: **decreased diazepam renal excretio**n * Cimetidine, Disulfiram, Ethanol, INH, Valproic acid decreases metabolism * Valproic acid: displacement from binding sites
48
Drug Interactions of BZs Decrease levels
Antacids: decrease absorption OCP, RIF: Increased metabolism
49
Drug Interactions BZs
* §BZs **increase** CNS depressive **effects of Alcohol and other agents**
50
What is the effect BZs on Digoxin?
Decrease renal excretion Digoxin
51
What is the effect of BZs on Levodopa?
decrease the effect Levodopa
52
What is the effect of BZs + Lithium?
** Hypothermia**
53
Bzs has Prolonged neuromuscular blockade with \_\_\_\_\_\_\_\_\_
succinylcholine
54
Newer drugs for Anxiety and sleep Disorders
§Buspirone §Zolpidem §Zaleplon
55
Describe Buspirone.
* 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
What are the side effects of Buspirone?
include headache and dizziness, dose dependent pupillary constriction §
57
Buspirone Increased BP with ?
MAOIs
58
What are the Analogs of Buspirone?
Ipsapirone, Gepirone, Tandospirone
59
What is with Zolpidem?
* **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
What is wtih Zaleplon?
* 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
BZ antagonist **FLUMAZENIL**
* 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
What are your Barbiturates?
* Thio**pental**: * Pheno**barbita**l: * Amobar**bital**, Pentobar**bital**, Secobar**bital**: * Barbiedal:
63
What is your ultra short acting ( 30 Minutes) **Barbiturates?**
**Thiopental**
64
What is your longest acting Barbiturates?
Phenobarbital
65
What are your Short acting barbiturates?
* Amobarbital, * Pentobarbital, * Secobarbital
66
What is your non acting barbiturates?
Barbiedal
67

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

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