Pharmacology 05-06 - Skeletal Muscle Relaxants - Msk

Front 1

What is the Neuromuscular blocker that depolarizes the synapse?

Back 1

Succinylcholine - agonist at the nicotinic end plate receptor

Front 2

What are the neruromuscular blockers that non-depolarize the synapse?

Back 2

Long duration = dubocurarine, short duration - mivacurium

Front 3

Non-depolarizing drugs MOA

Back 3

Prevent action of Ach at the skeletal muscle end plate -> thus action potential cannot fire

Front 4

Depolarizing drugs MOA

Back 4

Succinylcholine(nicotinic agonist) -> depolarizes the enruomuscular end plate -> initial depolarization = twitching/fasiculations -> since muscle contraction cannot be maintained b/c of continuous depolarization -> muscle relaxes -> muscle becomes paralyzed

Front 5

Drug that facilitates GABA-mediated presynaptic inhibition

Back 5

Diazepam

Front 6

Drug that acts as a GABAB agonist causing membrane hyperpolarization via ↑ K+ conductance, an action that ↓ the release of excitatory neurotransmitters?

Back 6

Baclofen

Front 7

Drug that has significant alpha-2 agonist activity, reinforces both presynaptic and post-synaptic inhibition in the spinal cord.

Back 7

Tizanidine

Front 8

Drug that acts in skeletal muscle cell to reduce the release of activator calcium from the sarcoplasmic reticulum via interaction with the ryanodine receptorchannel

Back 8

Dantrolene-treats malignant hyperthermia in general anesthesia

Front 9

Drug that acts in the brain stem, interfering with polysynaptic reflexes that maintain skeletal muscle tone

Back 9

cyclobenzaprine

Front 10

Trachea intubation

Back 10

Use skeletal muscle relaxants

Front 11

Execution

Back 11

Sodium pentothal (fast acting barbituate), neuromuscular blocker -> complete paralysis of skeletal muscles -> paralyze diaphram (tubocurarine), potassium bromide -> stops heart

Front 12

Spasmolytic drugs

Back 12

Drugs used to ↓ muscle tone(treats spasms from UMN damage)

Front 13

Define: spasm

Back 13

Sudden, violent, painful, INVOLUNTARY contractions of muscle or groups of muscles

Front 14

What type of NT used in NMJ?

Back 14

NMJ uses Ach -> nicotinic receptors are located on muscle part of synapse -> contraction

Front 15

What are the common causes of spasticity?

Back 15

Head injuries, cerebral palsy, multiple sclerosis, stroke (UMN injuries)

Front 16

Spasm vs spasticity

Back 16

Spasm = LMN - sudden violent painful involuntary contraction, spasticity = UMN - ↑ muscle tone or muscle contraction that cause stiff, awkward movement

Front 17

What are the neuromuscular blocker drugs we need to know

Back 17

Atracurium, pancuronium, gallamine

Front 18

What are the spasmolytic we need to know?

Back 18

Baclofen, diazepam, tizanidne

Front 19

Dantrolene

Back 19

Acts as a spasmolytic that works in the periphery

Front 20

What are the central acting skeletal muscle relaxants

Back 20

Treats spasticity (UMN Lesion) - baclofen, botulinum toxin, diazepam, tizanidine

Front 21

What are the peripherally-acting spasmolytic?

Back 21

dantrolene

Front 22

MOA of baclofen

Back 22

Acts in the spinal cord -> suppresses hyperactive reflexes involved in regualtion of muscle movement(structural analog of GABA-B-> inhibits CNS)

Front 23

Diazepam

Back 23

Facilitates GABA-mediated pre-synaptic inhibition(reinforces the depressor)

Front 24

What drug is preferred over dantrolene in patient whose spasticity is associated with significant muscle weakness

Back 24

baclofen

Front 25

Baclofen

Back 25

Interferes w/release of excitatory transmitters (stops the exciter) -> acts at the level of spinal cord to restore inhibiting tone

Front 26

What are the adverse effects of baclofen

Back 26

CNS = drowsiness, dizziness, weakness, fatigue; contraindicated in alcohol and other CNS depressants b/c baclofen potentiates the depressant action of these drugs(since MOA = inhibition of excitatory impulses via GABA)

Front 27

MOA of diazepam?

Back 27

Act within CNS by facilitating GABA-A-mediated presynaptic inhibition

Front 28

Treatment for muscle spasm and local muscle trauma(UMN lesion)

Back 28

diazepam

Front 29

Side effect of diazepam?

Back 29

sedation

Front 30

What is the MOA of dantrolene in the periphery

Back 30

Act on skeletal muscle -> relieves spasticity -> suppresses Ca2+ release from sarcoplasmic reticulum -> ↓ ability of skeletal muscle to contract

Front 31

Treatment for malignant hyperthemia(lidocane induced contraction of muscle -> ↑ temp)

Back 31

Dantrolene - inhibits ryanadine receptors directly

Front 32

What is the side effect of dantrolene

Back 32

hepatotoxicity

Front 33

Tizanidine

Back 33

alpha- 2 agonist -> hypotension, drowsiness, and dry mouth

Front 34

Botulinum toxin

Back 34

Spasticity from cerebral palsy -> cosmetic surgery

Front 35

What is the contraindications for baclofen

Back 35

Skeletal muscle spasms caused by RA

Front 36

What is the contraindications for carisoprodol

Back 36

Pt with hypersensitivity to meprobamate

Front 37

What is the contraindications for cyclobenzaprine

Back 37

MI, cardiac conduction disorders, hyperthyroidism

Front 38

What is the contraindications for dantrolene

Back 38

Active hepatic disease, muscle spasm caused by RA

Front 39

Cerebral palsy

Back 39

Damage to the motor centers in the brain during pregnancy -> age 3

Front 40

Cyclobenzaprine

Back 40

Treats acute temporary muscle spasm caused by local trauma or strain; ineffective in muscle spasm due to cerebral palsy or spinal cord injury

Front 41

Which skeletal muscle relaxtants have a high protein binding affinity?

Back 41

Cyclobenzaprine + Dantrolene -> thus have to be careful when giving another protein binding drug. U might ↑ its concentration too much