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PHTH 561 > Musculoskeletal Pharmacology Part I > Flashcards

Musculoskeletal Pharmacology Part I Flashcards

1
Q

Skeletal Muscle Relaxants

A
  • treat conditions with hyperexcitable skeletal muscle (i.e. spasticity and muscle spasms)
  • goal is to normalize muscle excitability without profound decrease in muscle function
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1
Q

UMN Lesions

A
  • Site: Cerebral hemispheres, cerebellum, brainstem, spinal cord
  • Muscle weakness: quadriplegia, hemiplegia, diplegia, paraplegia
  • Muscle tone: spasticity, rigidity
  • Sensory loss: cortical sensations
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2
Q

LMN Lesions

A
  • Site: AHC, Nerve roots, peripheral nerves, NMJ, muscles
  • Muscle weakness: proximal (myopathy), distal (neuropathy)
  • Muscle tone: hypotonia
  • Sensory loss: peripheral sensations
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3
Q

Spasticity

A
  • velocity dependent increase in muscle tone caused by increased excitability of muscle stretch reflex
  • central disorder (UMN)
  • symptoms include stiffness, hypertonicity, hyperreflexia
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4
Q

Spasms

A
  • involuntary, sudden muscle contractions
  • peripheral disorders (LMN), muscle sprain or injury, nerve compression, inflammation, electrolyte imbalances
  • symptoms include jerks, twitches, cramps
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5
Q

Spasticity common neurologic disorders

A
  1. multiple sclerosis
  2. stroke
  3. CP
  4. SCI, brain injuries
  5. Neurodegernative disorders affected UMN, pyramidal and extrapyramidal pathways
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6
Q

Common symptoms of severe spasticity

A
  • muscle stiffness (flexing or extending)- adducted shoulder with IR, flexed elbow, pronated forearm, flexed wrist and fingers, thumb in palm, clenched fist
  • muscle spasms
  • Clonus- rapid muscle contractions
  • Contractures- fixed joints
  • Exxagerated muscle jerks
  • pain or tightness around joints
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7
Q

Primary goal of skeletal muscle relaxants

A
  1. selective decrease in skeletal muscle excitability
  2. decrease pain
  3. without causing profound decrease in muscle function
  4. either antispasticity or antispasmodic (spasmolytic) agents
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8
Q

Baclofen

A
  • common antispasticity drug
  • Acts on GABA-B receptors in spinal cord to inhibit reflexes and decrease spasticity
  • can be taken orally or adminstered into spinal fluid
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9
Q

Dantrolene

A
  • common anti-spasticity drug
  • acts directly on skeletal muscle, inhibits calcium release and thus muscle contraction
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10
Q

Tizanidine

A
  • common anti-spasticity drug
  • Alpha-2 adrenergic agonist that reduced spasticity by increase presynaptic inhibition
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11
Q

Botulinum toxin

A
  • common anti spasticity drug
  • injected directly into spastic muscles, inhibits ACh release, reducing muscle contractoin
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12
Q

Carisoprodol (Soma)

A
  • common spasmolytic
  • exact mechanism unknown, alters interneuronal activity in spinal cord and descending reticular formation in brain
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13
Q

Cyclobenzaprine (Flexeril)

A
  • common spasmolytic
  • works centrally, decreases activity in brainstem to relieve muscle spasms
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14
Q

Methocarbamol (Robaxin)

A
  • common spasmolytic
  • mechanism not fully understoof, central muscle relaxant properties
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15
Q

Orphenadrine (Norflex)

A
  • common spasmolytic
  • Anti cholinergic properties are believed for be responsible for muscle relaxant effect
16
Q

Key differences between spasmolytics and anti-spasticity drugs

A
  1. target: anti spasticity mainly target conditions with increased muscle tone due to CNS disorders, spasmolytics target PNS conditions involving acute, painful muscle contractions
  2. Mechanicsm: anti spasticity drugs have more specific targets (NMJ), spasmolytics less clear and can be diverse
  3. Usage: anti spasticity drugs more chronic in nature (treating MS, CP, etc.), spasmolytics used for acute conditions (muscle strain, injury)
17
Q

Polysynaptic Inhibitors (Antispasm drugs)

A
  • diverse group of drugs including carisoprodol (SOMA), cyclobenzaprine (Flexeril), Methocarbamol (Robaxin), Orphenadrine citrate (Norflex)
  • adjuncts to rest and PT for relief of spasms
  • may be incorporated into alagesics (acetaminophen or aspirin): norgesic
  • MOA: theorized to act on polysynaptic reflex arc in spinal cord, could decrease alpha motor neuron excitability causing relaxation of skeletal muscle
  • AE: drowsiness, dizziness, nausea, lightheadedness, vertigo, ataxia, headache, tolerance, and physical dependence
18
Q

Diazepam (Valium)

A
  • Benzodiazepine agent, developed originally as antianxiety drug
  • MOA: Increases inhibitory effects at CNS synapses that use GABA
19
Q

GABA

A

primary neurotransmitter that causes inhibition at pre/post synaptic neurons in brain and spinal cord (alpha receptors)

PHTH 561 (3 decks)

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