Muscle Relaxants  Continuous muscle spasm that causes stiffness, rigidity, or
tightness that can interfere with normal walking, talking or
Muscle Relaxants
 Often used as an adjunct to other medications, mostly
NSAIDs in patients with myofascial pain
 Used to treat muscle spasms or muscle spasticity
 Muscles work together to allow free flow of impulses into
and out of the system to coordinate posture, balance, and
movement
 When injuries, diseases, and toxins affect the normal flow
of information into and out of the CNS and motor
pathways, many clinical signs and symptoms may develop;
ranging from simple muscle spasms to muscle spasticity or
sustained muscle spasm and paralysis
NEUROMUSCULAR ABNORMALITIES
MUSCLE SPASM:
 Injury to the musculoskeletal system
o Overstretching a muscle
o wrenching a joint
o Tearing a tendon or ligament
 Can cause violent and painful involuntary muscle
contractions
o The contractions cuts off blood flow to the muscle
fibers in the injured area
 Causes the release of lactic acid causing pain
o The new flood of sensory impulses caused by the
pain may lead to further muscle contraction
 Sudden, involuntary contractions of a muscle group
o Can be caused by too much muscle strain and leads
to pain
 Associated with conditions
o Lower back pain
o Neck pain
o Fibromyalgia
 Overstretching a joint
o Sprain
 Injury to a ligament
o Strain
 Injury to a muscle or connecting tendon
o wrenching a joint
 Twist or turn suddenly or forcibly
MUSCLE SPASTICITY:
 Damage to neurons within the CNS rather than peripheral
structures
 Permanent
o Spasticity is caused by nerve damage in the CNS
movement
 Caused by injury to parts of the brain or spinal cord
involved with movement
 Conditions that can cause it
o Multiple sclerosis
o Cerebral palsy
o Amyotrophic lateral sclerosis
 Increase in excitatory influences or a decrease in inhibitory
influences within CNS
o excessive stimulation of muscles (hypertonia) and
loss of coordinated muscle activity (cerebral palsy or
paraplegia)
o contractures and permanent structural changes
CLASSIFICATIONS:
 Centrally-Acting Muscle Relaxants
 Direct-Acting Skeletal Muscle Relaxants
o Most work in the brain and spinal cord where they
interfere with the cycle of muscle spasm and pain
CENTRALLY ACTING MUSCLE RELAXANTS:
 Relieve the discomfort associated with various
musculoskeletal conditions
 Upper levels of CNS interfering reflexes that cause muscle
spasms
 Spasmolytics
o Destroy or lyse muscles
Examples:
 Balcofen (Lioresal)
 Carisoprodol (Soma)
 Chlorphenesin (Maolate)
 Tizanidine (Zanaflex)
 Diazepam (Valium)
o Widely used as an anxiety agent also effective as a
centrally acting muscle relaxant
o Advantage when anxiety precipitates the muscle
spasm
 Rest of the affected muscle
 Heat applications - to increase blood flow to the area
 Physical therapy
 Anti-inflammatory agents including NSAIDs
Therapeutic Action:
 Work in CNS to interfere with the reflexes that causes
muscle spasm
 Use in skeletal muscle spasms of local origins
 Exact mechanism of action is not known.
 Increase inhibition of presynaptic motor neurons in the CNS.
Indication:
 Relief of discomfort associated with acute, painful
musculoskeletal conditions.
Pharmacokinetics:
 Antispastics are used to treat muscle spasticity, should not
be used to treat muscle spasms
 Baclofen is available in oral and intrathecal forms and can
be administered via a delivery pump.
o Block nerve signals form the spinal cord that cause
the muscles to spasm
o Oral and intrathecal forms
o Intrathecal Pump - medications directly into the
space between the spinal cord and the protective
sheet that surrounds it
 Cyclobenzaprine- is available in a controlled release form for
continual control of the discomfort without repeated dosing.
o Prolongs action
o Attempts to maintain drug levels within the
therapeutic effect to avoid potential y hazardous
ticks in drug concentration following ingestion or
injection and to maximize therapeutic efficiency
Adverse Effects:
 CNS depression: drowsiness, fatigue, weakness, confusion,
headache
 GI (may be linked to CNS depression of the parasympathetic
reflexes): nausea, dry mouth, anorexia and constipation
 Urinary frequency, feelings of urinary urgency
 Chlorzoxazone: discolors urine, becoming orange to purple
red when metabolized and excreted
 Avoid alcohol when taking muscle relaxants; CNS depression
may increase
Prototype: Baclofen
Indication:
 Alleviation of signs and symptoms of spasticity; spinal cord
injuries
 All centrally acting muscle relaxants must be used in caution
in the following circumstances
o History of epilepsy; exacerbate the seizure disorder
o Cardiac dysfunction
DIRECT-ACTING SKELETAL MUSCLE RELAXANTS:
 Inhibits muscle contraction by decreasing calcium release
from the sarcoplasmic reticulum n the muscle cells
Dantrolene (Dantrium)
 Modulating the skeletal muscle contractions at the site
beyond the myoneural junction
 Directly affects peripheral muscle contraction
 Neuromuscular disorders
 It works by acting directly on the skeletal muscles to relax
the muscle spasm
 For muscle spasm caused by spinal cord injury, stroke,
cerebral palsy, multiple sclerosis
 Not for musculoskeletal injury or rheumatic disorders;
because of the most serious adverse effect --> muscular
weakness
Therapeutic Actions and Indications
 Acts within skeletal muscle fibers --> interfere in the
release of Ca from the muscle tubules --> prevention of
contraction
 Also for prevention of malignant hyperthermia
o Intense muscle contraction -- > hyperpyrexia
(abnormally high fever)
Pharmacokinetics
 Oral or parenteral forms
 Slowly absorbed from GI tract
 Metabolized in the liver
 Half-life 4-8 hours
 Excretion; urine
Adverse Effects:
 CNS depression: drowsiness, fatigue, weakness, confusion,
headache and insomnia, and visual disturbances.
 GI effects: GI irritation diarrhea, constipation, and abdominal
cramps.
 Hepatocellular damage or hepatitis
 Urinary frequency, feelings of urinary urgency
 Crystalline in urine and pain or burning
 Acne, abnormal hair growth, rashes, photosensitivity,
abnormal sweating, chills and myalgia.
Clinical Drug-Drug Interaction:
 Dantrolene combined with Estrogens, the incidence of
hepatocellular toxicity is apparently increased