Centrally Acting Muscle Relaxants: Examples
- baclofen (Lioresal)
- carisoprodol (Soma)
- chlorzoxazone (Parafon)
- cyclobenzaprine (Flexeril)
Centrally Acting Muscle Relaxants: Pharmacologic Action
- Enhance the inhibitory effects of GABA on receptors in the spinal cord, resulting in
suppression of hyperactive reflexes
Centrally Acting Muscle Relaxants: Adverse Drug Reactions
- Drowsiness and dizziness, weakness and fatigue that often subside w/ continued used
- Nausea, vomiting, constipation, and urinary retention
- Does not cause physical dependence
- withdrawal symptoms can occur if clients abruptly discontinue them after long-term
therapy
- Symptoms of withdrawal: anxiety, restlessness, visual hallucinations, and seizures
Centrally Acting Muscle Relaxants: Interventions
- give lowest effective dose and gradually increase it to minimize adverse effects
- take oral doses w/ food to decrease gastric irritation
- drink plenty of water and increase dietary fiber (constipation is a side effect)
Centrally Acting Muscle Relaxants: Administration
- start at lowest effective dose and gradually increase by 5 mg increments every 3 days
until you are giving a 20 m does 3-4 times a day
- give w/ food or milk to prevent stomach upset
- if oral does are ineffective, administer baclofen by intrathecal infusion directly into the
spine via a needle attached to a pump
Safety Alert: if you stop intrathecal admin abruptly, you run the risk of rebound spasticity
and fever and muscle damage. That can lead to organ failure and even death. Abrupt
withdrawal can also cause intense muscle contractions, resulting in muscle damage
(rhabdomyolysis) and release of toxins into the body that can damage organs such as
the kidneys. If organ damage is extensive, clients can die
Centrally Acting Muscle Relaxants: Contraindications and Precautions
- known hypersensitivity
- do not take concurrent w/ Monoamine oxidase inhibitors (MAOIs) as it could result in
hypotensions or increase CNS depression
- Cyclobenzaprine is contraindicated for clients taking MAOIs antidepressants within
past 2 wks
- use w/ caution w/ older adults, childre, and clients w/ severe mental illness, a seizure
disorder, or have had a cerebrovascular accident
Centrally Acting Muscle Relaxants: Interactions
- avoid drinking alcohol and taking other CNS depressants due to the risk of increased
sedation
- use of cyclobenzaprine w/ MAOI antidepressants may cause a hyperpyretic crisis and
seizures
,- Serotonin syndrome can happen if cyclobenzaprine is administered to a client taking
SSRIs, SSNRIs, and tricyclic antidepressants
Peripherally acting muscle relaxants/ Direct acting skeletal Muscle Relaxers
- Peripherally acting or direct acting muscle relaxants relax skeletal muscle spasms that
occur as a result of cerebrovascular accident or stroke, spinal cord injury, multiple
sclerosis, and cerebral palsy
- They also prevent and treat malignant hyperthermia, and a dangerous adverse effect
of general anesthesia
Peripherally acting muscle relaxants/ Direct acting skeletal Muscle Relaxers:
Prototype and Other Drugs
- dantrolene (Dantrium)
Peripherally acting muscle relaxants/ Direct acting skeletal Muscle Relaxers:
Pharm Action
- act directly on skeletal muscle tissue by inhibiting the release of calcium, which is
necessary for normal muscle contraction
Peripherally acting muscle relaxants/ Direct acting skeletal Muscle Relaxers:
Adverse Drug Reactions (Dantrolene)
- Muscle weakness, drowsiness, dizziness, and diarrhea
- liver toxicity- occurs more frequently w/ higher doses and long-term therapy
Peripherally acting muscle relaxants/ Direct acting skeletal Muscle Relaxers:
Interventions (Dantrolene)
- monitor for side effects that relate to CNS depression (ex: drowsiness)
- assist clients w/ ambulation if they feel weak or dizzy.
- start orally at low doses & gradually increase to prevent CNS side effects
- Monitor for diarrhea, esp. early in treatment, and treat it if it occurs
- monitor liver function closely throughout therapy (potential for liver toxicity)
Safety Alert: inhibition of the release of calcium in skeletal muscle may decrease
strength & function in relieving spasticity. Monitor client's muscle strength during
treatment to make sure that muscle weakness does not develop, as it will make
ambulation dangerous
Peripherally acting muscle relaxants/ Direct acting skeletal Muscle Relaxers:
Administration (Dantrolene)
- available oral or IV
- most w/ spasticity take oral form
- to help prevent malignant hyperthermia in clients who have a personal or family
history, make sure they take the drug orally for 1-2 days preoperatively
- use the IV form of dantrolene to treat malignant hyperthermia and give it via IV bolus
due to the critical and life-threatening nature of the complication
Peripherally acting muscle relaxants/ Direct acting skeletal Muscle Relaxers:
Contraindications and Precautions (Dantrolene)
- clients who have liver disease
- caution w/ clients w/ cardiac/ pulmonary disease or a neuromuscular disorder
- The incidence of liver damage increases in clients older than age 35, so closely
monitor clients of this age taking the drug
, Peripherally acting muscle relaxants/ Direct acting skeletal Muscle Relaxers:
Interactions (Dantrolene)
- women older than 35 who use estrogen have an increase risk of liver toxicity if they
use dantrolene
- concurrent admin of CNS depressants, such as alcohol, w/ any drug that is also a
CNS depressant or has CNS depressant effects increases the risk for excessive
sedation
- drug may cause severe cardiac dysrhythmias in clients who also take calcium channel
blockers
Traditional AEDs Hydantoins
- AEDs: anti-epileptic drugs
- help control tonic-clonic seizures (grand mal seizures), which involve the entire body
- they help control partial seizures, which affect one part of the brain and subsequently
one part of the body
Traditional AEDs Hydantoins: Prototype and other Drugs
- Drug Class: Hydantoins
- phenytoin (Dilantin)
- fosphenytoin (Cerebyx)
Traditional AEDs Hydantoins: Pharm Action
- decrease the neuronal activity of seizure- generating cells in the brain by inhibiting the
influx of sodium through sodium channels
Traditional AEDs Hydantoins: Adverse Drug Reactions
- mild drowsiness and other CNS depressant effects
- Gingival hyperplasia, an abnormal growth of tissue around the gums, is common in
children and adolescents who take this drug
- occasionally can cause skin rash- can be an indication of a serious side effect
Safety Alert: taking for long period of time should not stop abruptly. This can lead to the
recurrence of seizures, including a series of prolonged seizures called status epilepticus
Traditional AEDs Hydantoins: Interventions
- monitor for excessive drowsiness and other CNS effects
- effects should be mild if the client's dose is at a therapeutic level, but excessive
drowsiness may indicate toxicity
- Be sure to observe the gingiva or gums of children and adolescents for hyperplasia or
overgrowth and note its degree if it's present
- monitor for rashes
Safety Alert: Monitor for rash that occurs after drug therapy starts, as epidermal
necrolysis or Stevens- Johnson syndrome can develop. Fever, damage to skin and
internal organs, and sepsis can result. If this type of rash occurs, discontinue the drug
immediately
Traditional AEDs Hydantoins: Administration (phenytoin)
- give w/ meals to prevent gastrointestinal distress
- during IV injection, cardiac collapse can occur if you give the drug too quickly, due to
the effects phenytoin has on the influx of sodium in neurons in both the brain and the
heart. If you give Iv injection, inject no more than 50 mg per minute. For older adults,