⭐ LECTURE 5: ANTI-SPASTICITY DRUGS AND MUSCLE RELAXANTS

Question 1

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

Answer 1

BLOOD-BRAIN BARRIER (BBB)

Question 2

nonpolar, lipid-soluble drugs

Answer 2

PASSIVE DIFFUSION

Question 3

polar and lipophobic compounds

Answer 3

CARRIER-MEDIATED TRANSPORT

Question 4

initiation of neurotransmitter release

Answer 4

PRESYNAPTIC ACTION POTENTIAL

Question 5

no synthesis = no neurotransmitter

Answer 5

NEUROTRANSMITTER SYNTHESIS

Question 7

storage of the neurotransmitter

Answer 7

STORAGE

Question 8

block the transmitter catabolism in the presynaptic terminal

Answer 8

METABOLISM

Question 9

site of drug action; increases synaptic activation

Answer 9

RELEASE

Question 10

allows more neurotransmitters to stay in the synaptic cleft

Answer 10

RE-UPTAKE

Question 11

serves as a negative feedback

Answer 11

IONIC CONDUCTANCE

Question 12

Exerts a calming and relaxing effect

Answer 12

SEDATIVE-HYPNOTIC DRUG

Question 13

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

Treated with anxiolytic drugs

Answer 13

ANXIETY

Question 14

state of sleep

Answer 14

HYPNOSIS

Question 15

inability to initiate, maintain, or achieve restful sleep

Answer 15

INSOMNIA

Question 16

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

Answer 16

GABA

Question 17

GABAA RECEPTOR for sedation

Answer 17

Alpha-1
Beta-2
Gamma-2

Question 18

GABAA RECEPTOR for Anxiolytic

Answer 18

Alpha-2
Beta-3
Gamma-2

Question 19

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

Answer 19

GABAA

Question 20

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

Answer 20

BENZODIAZEPINES

Question 21

Increase affinity of GABA → chloride channel opening → membrane hyperpolarization

Answer 21

NON-BENZODIAZEPINES

Question 22

Decrease the activity of excitatory neurotransmitters (ACh and Glutamate)

Answer 22

BARBITURATES

Question 23

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

Answer 23

SPASTICITY

Question 24

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

Answer 24

SPASM

Question 25

Binds to GABAA receptor increasing GABA induced inhibition at the synapse

Answer 25

DIAZEPAM (VALIUM)

Question 26

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

Answer 26

CENTRALLY-ACTING ANTI SPASM DRUGS

Question 27

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

Answer 27

BACLOFEN (LIORESAL, TRILAXANT)

Question 28

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

Answer 28

CLONIDINE (CATAPRES) AND TIZANIDINE (ZANAFLEX)

Question 29

Peripherally acting

Answer 29

DANTROLENE SODIUM (DANTRIUM, RYANODEX)

Question 30

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

Answer 30

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

Question 31

Antiepileptic drug

Answer 31

Gabapentin

Question 32

New analog of gabapentin that may also prove useful

Answer 32

Pregabalin

Question 33

Centrally acting muscle relaxant

Answer 33

Centrally acting muscle relaxant

Question 33

Inhibitory amino acid neurotransmitter

Answer 33

Glycine

Question 33

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

Answer 33

CYCLOBENZAPRINE

Question 33

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

Answer 33

ORPHENADRINE

Question 33

Prescribed for nocturnal leg muscle cramps

Answer 33

QUININE

Question 34

Centrally acting muscle relaxant with an unknown mechanism

Answer 34

METAXALONE

Question 35

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

Answer 35

CARISOPRODOL

Question 36

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

Answer 36

BOTULINUM TOXINS (BOTOX, DYSPORT, XEOMIN, MYOBLOC)

Question 37

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

Answer 37

PHENOL