Muscle Relaxants, CNS Depressants, Stimulants

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Ohio State University Nursing 385.03

What are the two general types of musculoskeletal relaxants?

centrally acting skeletal muscle relaxants and direct acting skeletal muscle relaxants

How do centrally acting skeletal muscle relaxants work?

they depress the CNS like sedatives, have no direct action on the muscles, enhance GABA inhibitory effects in the cord

Centrally acting skeletal muscle relaxants work directly in the _____ and the _____.

brain and cord

What are all muscle relaxants generally used to treat?

spasticity

What two things can muscle relaxants be used to treat?

chronic debilitating disorders (e.g. MS, strokes, cerebral palsy, etc), spasms from muscle injury

What are some chronic debilitating disorders that muscle relaxants can be used to treat?

MS, strokes, cerebral palsy, head injuries

What do spasms from muscle injury cause?

pain and limited mobility

What are the common side effects of all muscle relaxants? What two systems do they generally affect?

drowsiness, dizziness, lightheadedness, N/V/D, abdominal distress. CNS and GI side effects.

Why would a person on a muscle relaxant have GI side effects?

because the muscle relaxant will "sedate" the muscles

What two types of muscle relaxants can cause anticholingergic side effects?

Cyclobenzaprine and orphenadrine (Norflex)

What is the most effective centrally acting muscle relaxant? Why it that?

Baclofen (Lioresal). it is VERY similar to GABA

Baclofen (Lioresal) relieves muscle spasms in _____ and _____ _____ _____.

MS and spinal cord lesions

What is an example of a muscle relaxant that is direct acting? What is it used to treat spasms in?

Dantrolene (Dantrium). spinal cord injury, stroke, MS, CP

How does Dantrolene (Dantrium), a direct acting muscle relaxant, work?

decreases calcium release from the sarcoplasmic reticulum in muscle cells

What is a muscle relaxant used to manage spasticity in spinal cord injury and MS?

Tizanidine (Zanaflex)

What can Diazepam (Valium) be used to treat? What is its therapeutic class?

anxiolytic and anticonvulsant. relieves muscle spasms in paraplegia and CP.

What are two muscle relaxants that are used for acute/severe/short-term treatment? Are they centrally acting or direct acting?

Cyclobenzaprine HCl (Flexeril), Methocarbamol (Robaxin). centrally-acting

What are depolarizing muscle relaxants used in adjunct to? What are they also referred to as? What do they induce? What are they NOT used for? What are some examples of drugs that fall into this category?

anesthesia. neuromuscular blockers. skeletal muscle relaxation. NOT used for spasticity. Pavulon, Vecuronium, Succinylcholine.

What is a unique route for Baclofen? What is this used for and when especially would it be used? What is a special consideration for this though that the patient must meet?

baclofen pump, intrathecal (into CSF). used with spasticity or dystonia when the patient is having excessive problems with daily cares, bathing and/or pain. the patient must have a big enough body to hold the pump which is placed in their abdominal SQ tissue.

What are the two types of CNS depressants? What is the difference between them? What does the classification one way or the other depend on?

sedatives and hypnotics. a sedative will relax the person but a hypnotic will put them to sleep. the degree to which the drug inhibits transmission of nerve impulses to the CNS.

Central nervous system depressants work to potentiate what neurotransmitter?

the inhibitory neurotransmitter, GABA

What are sedatives also called? What three things do they help to reduce? What do they NOT cause? What can they become if the dose is too high?

anxiolytics. nervousness, excitability, irritability. don't cause sleep. hypnotic

What do hypnotics cause?

sleep

What are the three main groups of central nervous system depressants?

barbituates, benzodiazepines and miscellaneous

What are side effects/adverse reactions common in ALL central nervous system depressants?

hangover, REM rebound (hypnotics), dependence, tolerance, excessive depression, respiratory depression, hypersensitivity

What are the side effects associated with hangover?

residual drowsiness and impaired reaction time

What is the REM rebound that may occur with hypnotics?

vivid dreaming when the hypnotic is stopped after prolonged use

Dependence to sedatives and hypnotics can be both _____ and _____.

physical and psychological

What does the tolerance associated with sedatives and hypnotics mean for dosing?

the dose must be increased over time to obtain the desired effect

What can prevent withdrawal symptoms with hypnotics?

gradual withdrawal from hypnotics

What are the types of barbituates?

ultra-short, short-acting, intermediate-acting, long-acting

What is an example of an ultra-short barbituate? What is it used for?

thiopental (Pentothal). general anesthesia

What are some examples of short-acting barbituates? (2) What are they used for?

Pentobarbital (Nembutal), Secobarbital (Seconal). used to induce sleep

What are some examples of intermediate-acting barbituates? (3) What are they used for?

Amobarbital (Amytal), Aprobarbital (Alurate), Butabarbital (Butisol). used to sustain sleep

What is an example of a long-acting barbituate? What is it used for?

phenobarbital (Luminal). seizures

What class of controlled substance are barbituates? What are some characteristics of this class?

Class II. high abuse potential but still accepted medical use. few are used today. habit forming and have a low therapeutic index.

What is a class I controlled substance?

heroine

What do barbituates potentiate?

the action of GABA

What controlled substance class are benzodiazepines? What are some characteristics of this class?

class IV. less abuse potential than class III. accepted medical use. limited physical and psychological dependency.

What are the two general purposes of benzodiazepines?

anti-anxiety, sleep

What selected benzodiazepines are used for sleep, or as hypnotics?

Flurazepam (Dalmane), Temazepam (Restoril), Triazolam (Halcion).

While benzodiazepines are very safe if taken alone, what are some of their drug-drug interactions?

alcohol, antidepressants, narcotics

What is a benzodiazepine that is used for procedures? What purpose does it serve? What types of procedures is it used with?

Midazolam (Versed). anxiolytic and to cause amnesia. those that require conscious sedation.

What was the first ever benzodiazepine? What three things is it used as?

Diazepam (Valium). muscle relaxant, anxiolytic and anti-convulsant

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