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Pharm. Chapter 12 Central Nervous system Depressants and muscle Relaxants
Terms in this set (45)
Drugs that have an inhibitory effect on the Central Nervous System to the degree that they reduce:
Put you to sleep
Stronger then sedatives
What is the relationship between Hypnotics and Sedatives
Sedatives relax you while hypnotics put you to sleep; sedatives can be hypnotics in large doses
What are the Three Main groups of CNS Depressants
What was the most commonly prescribed sedative-hypnotic drug
Now nonbenzodiazepines are currently more frequently prescribed
-because they have a favorable drug effect profiles, efficacy, and safety
Classified as either Sedative-hypnotic, or Anxiolytic (medication that relieves Anxiety)
Long Acting Benzodiazepines
Diazepam (valium) Clonazepam (Klonopin)
Intermediate acting Benzodiazepines
Alprazolam(Xanax) Lorazepam(Ativan) Temazepam(Retoril)
Short Acting Benzodiazepines
Midazolam (Versed) triazolam (Halcion)
what are the mechanism of action of Benzodiazepines
-They Depress the Central Nervous System,
-affect hypothalamic, Thalamic, and limbic systems of the brain.
-They act like GABA
-They do not suppress Rapid Eye Movement AS MUCH AS barbiturates (But still interfere, and can cause a hangover effect)
- They Do not increase the Metabolism of other Drugs
What are the drug effects of Benzodiazepines
-Calming effect on the CNS
-Useful in controlling Agitation and anxiety
-Reduce excessive sensory stimulation, which induces sleep
-Induce skeletal muscle relaxation
What are Benzodiazepines used for (Indications)
Skeletal muscle Relaxation
Treatment of acute seizure disorders
Treatment of alcohol withdrawal
To balance anesthesia
What are the Adverse affects of Benzodiazepines
Headaches, Drowsiness, Dizziness, Cognitive Impairment,Vertigo, lethargy, Fall hazard for elderly people, "hangover" effect/daytime sleepiness
How would you treat an overdose of Benzodiazepines?
The treatment or antidote for benzodiazepines is FLUMAZENIL
Toxicity and Overdose
Can cause hypotension and reparatory depression if taken with other CNS depressants
What is an example of another CNS Depressant that if taken with BEnzodiazepines will cause hypotension and reparatory depression?
-It is considered a CNS depressant
Azole antifungals, Verapamil, Diltiazem, protease inhibitors, macrolide antibiotics, Grapefruit juice
CNS Depressants (Alcohol, Opioids)
Herbal therapies ( Kava [Piper Methysticum] Valerian [Valeriana Officinalis])
Share many characteristics of benzodiazepines
They are used to treat insomnia
What are examples of nonbenzodiazepine hypnotics
Zaleplon (Sonata) Zolpidem (Ambien)
-> can become addictive and then you can not sleep with out them.
Eszoplicone (Lunesta) Ramltoen (Rozerem)
Which nonbenzodiazepine is approved for long term therapy
Eszoplicone and extended release Zolpidem
which are more addictive benzodiazepine or nonbenzodiazpines
Benzodiazepines are more addictive then nonbenzodiazepine. However, nonbenzodiazepines can still become addictive
What is the order of addiction from most addictive to least addictive?
1 barbiturates are most addictive
2 Benzos are not as addictive as barbiturates
3 nonbenzos less addictive then benzos but still addictive
What is Kava for?
Used to relieve stress, anxiety, and restlessness and to promote sleep
What is a side effect of extended, continued intake of Kava?
May cause temporary yellow skin discoloration and visual disturbances
What are contraindications of KAVA
It is counter indicated in liver disease , alcoholism, and other conditions
what is VALERIAN used for?
Used to relieve anxiety, restlessness, and sleep disorders
what are side effects of VALERIAN?
May cause CNS derision, hepatotoxictiy, nausea, vomiting, anorexia, restlessness, insomnia
When is VALERIAN contraindicated
in cardiac and liver diseas
-First introduce in 1903, standard drugs for insomnia and sedation
-Are habit forming
-Low therapeutic index
-only a hand full used today due to the efficacy and safety of benzodiazeppines
Barbiturates Drug Effects
-Low Dose: Sedative effects
-High Dose: Hypnotic effects
-> also lower respiratory rate
- Stimulate liver enzymes that cause metabolism or breakdown of many drugs
-> Results in shortened duration of action
--> So you have to give the recommended dose then give it again
What are the reasons one would use Barbiturates?
As a sedative
As an Anticonvulsant
As anesthesia for surgical procedurs
Barbiturates are broken into what four groups
---Anesthesia for short surgical procedures, other uses
---Sedation and control of convulsive conditions
---Sedation and control of convulsive conditions
---Sleep induction, Epileptic seizure prophylaxis
what are adverse affects of Barbiturates
=Cardiovascular -> vasodilatation, Hypotension
=CNS -> Drowsiness, Lethargy, Vertigo, deprived REM Sleep
=Respiratory -> Respiratory Depression, Cough
=GI -> Nausea, Vomiting, Diarrhea, Constipation
=Hematologic (Blood) -> Agranulocytosis (lose of WBC), Thrombocytopenia (decrease number of platelets)
=Other -> Hypersensitivity reactions, Steven-Johndon syndrome
=Overdose frequently leads to respiratory depression and subsequent respiratory arrest
=Overdose produces CNS depression (Sleep to coma and death)
=Intentional overdose can be thraputic because of
----> anesthesia induction
----> phenobarbital Coma (Induced coma)
what is the antidote to barbiturate overdose?
What drugs will have an additive effect with barbiturates?
Alcohol, antihistamines, Benzodiazepines, Opioids, Tranquilizers
What drug interaction with Barbiturates will have an inhibit metabolism?
MAOIs will proloog effects of Barbiturates
what drug is a drug interaction with barbiturates that will cause an increase in metabolism?
Barbiturates reduce anticoagulant response, Leading to possible clot formations
--> Professor Dunn uses for her seizure patients
-Act to relieve pain associated with skeletal muscle spasms
-majority are centrally acting and the CNS is the site of action
- Direct-acting act directly on the skeletal muscle
when do muscle relaxants work best?
They work best when used with physical therapy
When do you use muscle relaxants?
-Used for relief of painful musculoskeletal conditions such as muscle spasms and can also be used for management of spasticity of severe chronic disorders (multiple sclerosis, cerebral plays)
When do muscle relaxants work best?
when used with physical therapy
What are the adverse effects of muscle relaxants?
What are some muscle relaxants
- Methocarbamol (Robaxin)
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