⭐ LECTURE 5: ANTI-SPASTICITY DRUGS AND MUSCLE RELAXANTS Flashcards

1
Q

Selective filtration of the CNS capillaries via tight junctions between capillary endothelial cells

A

BLOOD-BRAIN BARRIER (BBB)

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2
Q

nonpolar, lipid-soluble drugs

A

PASSIVE DIFFUSION

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3
Q

polar and lipophobic compounds

A

CARRIER-MEDIATED TRANSPORT

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4
Q

initiation of neurotransmitter release

A

PRESYNAPTIC ACTION POTENTIAL

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5
Q

no synthesis = no neurotransmitter

A

NEUROTRANSMITTER SYNTHESIS

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6
Q
A
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7
Q

storage of the neurotransmitter

A

STORAGE

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8
Q

block the transmitter catabolism in the presynaptic terminal

A

METABOLISM

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8
Q
A
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9
Q

site of drug action; increases synaptic activation

A

RELEASE

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10
Q

allows more neurotransmitters to stay in the synaptic cleft

A

RE-UPTAKE

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11
Q

serves as a negative feedback

A

IONIC CONDUCTANCE

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12
Q

Exerts a calming and relaxing effect

A

SEDATIVE-HYPNOTIC DRUG

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13
Q

Emotional state characterized by excessive feelings of worry, fear, and nervousness

Treated with anxiolytic drugs

A

ANXIETY

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14
Q

state of sleep

A

HYPNOSIS

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15
Q

inability to initiate, maintain, or achieve restful sleep

A

INSOMNIA

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16
Q

Reduces the activity level of a neuron making it less likely to fire

A

GABA

17
Q

GABAA RECEPTOR for sedation

A

Alpha-1
Beta-2
Gamma-2

18
Q

GABAA RECEPTOR for Anxiolytic

A

Alpha-2
Beta-3
Gamma-2

19
Q

abundant in the limbic system including amygdala for panic and fear response

A

GABAA

20
Q

Increase the affinitty of GABA that increases the influx of chloride ions at the postsynaptic cell and Results in decreased anxiety and greater feeling of calm

A

BENZODIAZEPINES

21
Q

Increase affinity of GABA → chloride channel opening → membrane hyperpolarization

A

NON-BENZODIAZEPINES

22
Q

Decrease the activity of excitatory neurotransmitters (ACh and Glutamate)

A

BARBITURATES

23
Q

Exaggerated muscle stretch reflex that occurs following an INJURY TO THE CNS

A

SPASTICITY

24
Q

Continuous, tonic contraction of specific muscles described as increased tension in skeletal muscle

A

SPASM

25
Q

Binds to GABAA receptor increasing GABA induced inhibition at the synapse

A

DIAZEPAM (VALIUM)

26
Q

Cause global decrease in CNS excitability → generalized sedation → skeletal muscle relaxation

A

CENTRALLY-ACTING ANTI SPASM DRUGS

27
Q

Blocks mono and polysynaptic reflexes by activating GABAB receptors and blocking release of excitatory neurotransmitters

A

BACLOFEN (LIORESAL, TRILAXANT)

28
Q

Stimulates alpha-2 adrenergic agonist receptors in the brainstem → decreased release of excitatory neurotransmitter (pre and postsynaptic inhibition)

A

CLONIDINE (CATAPRES) AND TIZANIDINE (ZANAFLEX)

29
Q

Peripherally acting

A

DANTROLENE SODIUM (DANTRIUM, RYANODEX)

30
Q

Blocks mono and poly synaptic reflexes by activating GABAA receptors that increases the influx of chloride ions at postsynaptic cell

A

DIAZEPAM (VALIUM, VALZEPAM, TRANKIL) AND CLONAZEPAM (RIVOTRIL, KLONOPIN)

31
Q

Antiepileptic drug

A

Gabapentin

32
Q

New analog of gabapentin that may also prove useful

A

Pregabalin

33
Q

Centrally acting muscle relaxant

A

Centrally acting muscle relaxant

33
Q

Inhibitory amino acid neurotransmitter

A

Glycine

33
Q

Centrally mediated and carries no direct peripheral action on the affected muscles

A

CYCLOBENZAPRINE

33
Q

Structurally related to diphenhydramine and carries relatively stronger anticholinergic weaker sedative properties

A

ORPHENADRINE

33
Q

Prescribed for nocturnal leg muscle cramps

A

QUININE

34
Q

Centrally acting muscle relaxant with an unknown mechanism

A

METAXALONE

35
Q

Produces its muscle relaxant effect by depressing the interneuronal activity at the spinal cord level as well as in the descending tracts of the reticular formation

A

CARISOPRODOL

36
Q

Prevents ACh release from presynaptic membrane, causing temporary calming of muscle contractions by blocking nerve impulse transmission at the neuromuscular junction

A

BOTULINUM TOXINS (BOTOX, DYSPORT, XEOMIN, MYOBLOC)

37
Q

Gamma fibers are demyelinated for about 6 months resulting in a less irritable, weakened muscle
and is peripherally acting

A

PHENOL