Centrally-Acting Skeletal Muscle Relaxants

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11 Terms

1

<p>What are antispastic drugs targeting<strong><em> GABA receptors?</em></strong></p>

What are antispastic drugs targeting GABA receptors?

Benzodiazepines
Baclofen

<ol><li><p>Benzodiazepines</p></li><li><p>Baclofen</p></li></ol><p></p>

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2

<p>Which antispastic drug targets <strong><em>alpha 2 adrenergic receptors?</em></strong></p>

Which antispastic drug targets alpha 2 adrenergic receptors?

Tizanidine

<p>Tizanidine</p>

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3

<p>Which antispastic drug <strong><em>directly targets skeletal muscle (direct-acting drug)?</em></strong></p>

Which antispastic drug directly targets skeletal muscle (direct-acting drug)?

Dantrolene

<p>Dantrolene</p>

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4

<p>What are muscle relaxants enhancing effects of GABA via interaction with GABAa receptors?</p>

What are muscle relaxants enhancing effects of GABA via interaction with GABAa receptors?

Benzodiazepines
1. Diazepam, Clonazepam, Lorazepam

<ol><li><p>Benzodiazepines</p><ol><li><p>Diazepam, Clonazepam, Lorazepam</p></li></ol></li></ol><p></p>

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5

<p>Describe baclofen regarding its structural feature, molecular target, MOA?</p>

Describe baclofen regarding its structural feature, molecular target, MOA?

GABAb receptor agonist
1. Opens K+ channels and hyperpolarizes the neuron
Looks like GABA with chlorophenyl group

<ol><li><p><span style="color: #e91f1f"><strong><em>GABAb receptor agonist </em></strong></span></p><ol><li><p>Opens K+ channels and hyperpolarizes the neuron</p></li></ol></li><li><p>Looks like GABA with <span style="color: green"><strong><em>chlorophenyl group </em></strong></span></p><p></p></li></ol><p></p>

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6

<p>Describe dantrolene regarding its structural feature, molecular target, and MOA?</p>

Describe dantrolene regarding its structural feature, molecular target, and MOA?

Binds to ryanodine receptor - antagonist
Inhibits calcium efflux
Hydrantoin derivative = phenytoin

<ol><li><p>Binds to ryanodine receptor - antagonist </p></li><li><p>Inhibits calcium efflux </p></li><li><p>Hydrantoin derivative = phenytoin </p></li></ol><p></p>

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7

<p>Describe tizanidine regarding its structural feature, molecular target, and MOA?</p>

Describe tizanidine regarding its structural feature, molecular target, and MOA?

Sympathetic antagonist - inhibits noradrenergic neurotransmission
a2 agonist
Contains 2-aminoimidazoline

<ol><li><p>Sympathetic antagonist - inhibits noradrenergic neurotransmission</p></li><li><p>a2 agonist </p></li><li><p>Contains 2-aminoimidazoline </p></li></ol><p></p>

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8

<p>Describe cyclobenzaprine regarding its structural feature, molecular target, MOA?</p>

Describe cyclobenzaprine regarding its structural feature, molecular target, MOA?

5-HT2 receptor antagonist
Methylidene group substituted by a 2- dimethylamino ethyl group

<ol><li><p>5-HT2 receptor antagonist </p></li><li><p>Methylidene group substituted by a 2- dimethylamino ethyl group </p></li></ol><p></p>

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9

<p>Orphenadrine binds and inhibits both _____ and ______ receptors?</p>

Orphenadrine binds and inhibits both _____ and ______ receptors?

NMDA
H1

<ol><li><p>NMDA</p></li><li><p>H1</p></li></ol><p></p>

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10

What muscle relaxants are carbamate esters?

Methocarbamol, carisoprodol

<ol><li><p>Methocarbamol, carisoprodol</p></li></ol><p></p>

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11

<p>What functional group can be found in metaxolone?</p>

What functional group can be found in metaxolone?

2-Oxazolidinone

<p>2-Oxazolidinone</p><p></p>

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