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Pharmacology
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Sedative
drugs that have an inhibitory effect on the CNS to the degree that they reduce: Nervousness, excitability, irritability
Hypnotics
cause sleep
much more potent effect on CNS than sedatives
Sedative-hypnotics dose dependent→
Barbiturate → benzodiazepines → Miscellaneous drugs
CNS Depressants: Benzodiazepines
formerly the most commonly prescribes sedative-hypnotic drugs
sedative-hypnotic
Anxiolytic (anti-anxiety)
work on GABA- A receptors
safer than barbiturates, needs more to OD, leads to falls
Benzodiazepines: effects
calming effect on the CNS
Useful in controlling agitation
inducing sleep
Benzodiazepines: Indications
Sedation
sleep induction
treatment of acute seizure disorders
treatment of alcohol withdrawal
Benzodiazepines contraindication
drug allergy
narrow-angle glaucoma- dilation of eyes
pregnancy ** - miscarriage/ preterm birth
can cause hangover effect
Benzodiazepines: adverse effects
cognitive impairment
vertigo (dizzy!!!)
lethargy
fall hazard for older adults
“Daytime sleepiness”
Benzodiazepines: Anxiolytics (anti-anxiety)
Alprazolam (Xanax) PO
diazepam (Valium) half-life 48 hours PO/ IM/ IV/ Rectal
lorazepam (Ativan) status epilepticus- seizure that never stops over 5 min, IM/ IV
Midazolam (Versed)- preop surgery/ reduces anxiety/ sedation- agitation PO/ Nasal/ Buccal/ IV/ IM/ can cause amnesia
Benzodiazepines: Hypnotics
temazepam (Restoril)- sleep
Triazolam (Halcion)-sleep,
causes you to sleep within 20-40 min- take an hour before going to bed, need 6-8 hours of sleep
Librium (chlordiazepoxide)
slow acting benzodiazepine, releases Gaba creating a calming effect. Acute symptoms of alcohol syndrome/
IV → PO
Side effects
drowsiness, dizziness, loss of muscle contraction
Adverse Effects
confusion, respiratory depression caused by ongoing use
When providing education to the patient on the use of
a benzodiazepine medication, the nurse will include
which information?
A. These medications have little effect on the
normal sleep cycle.
B. Using this medication may cause drowsiness the
next day.
C. It is safe to drive while taking this medication.
D. These drugs are safe to use with alcohol.
B. Using this medication may cause drowsiness the next day.
Benzodiazepines and Alcohol
DANGEROUS
both increase GABA activity in the brain
causes compounding effects that can cause you to stop breathing
Barbiturates MOA
site of action: brainstem (reticular formation)
by potentiating the action of GABA. nerve impulses traveling in the cerebral cortex are inhibited
short ac
Barbiturates Indications:
Short acting
sedation and control of seizure
Intermediate acting
Sedation and control of seizure
Long Acting
Seizure prophylaxis
Very narrow therapeutic window
Barbiturates Contraindications
pregnancy
significant respiratory difficulties
severe kidney or liver disease
caution in older adults- organs are in worse shape than someone who is younger
Barbiturates adverse effects
similar to benzo, but more severe
reduced REM sleep- agitation and inability to deal with normal stress
overdose frequently leads to respiratory depression and subsequent respiratory arrest
Barbiturate: Phenobarbital
prototypical
long acting
uses: prevention of generalized tonic-clonic seizures and febrile convulsions
alcohol withdrawal
rarely used as sedative- no longer used as hypnotic
Barbiturates have a low therapeutic index. How
does the nurse interpret this?
A. Low doses are most therapeutic
B. The toxic range is narrow
C. They are habit forming
D. The effective, safe dosage range is narrow
D. The effective, safe dosage range is narrow
MISC. Drugs Hypnotics
Nonbenzodiazepine: Eszopiclone (Lunesta)
first hypnotic to be FDA approved for long term use
binds to GABA receptors
instant effect
designed to provide a full 8 hours of sleep
more potent
longer half-life
Zolpidem (Ambien)
shorter acting
lower incidence of daytime sleepiness compared with benzodiazepine hypnotics
sleepwalking
Muscle Relaxants: MOA
Act to relieve pain associated with skeletal muscle spasms
Majority are centrally acting
-CNS is the site of action
-similar in structure and action to other CNS depressants
Direct acting
Muscle Relaxants: Indications
relief of painful musculoskeletal conditions
_muscle spasms (pregnancy, overuse, stroke)
_Management of spasticity of sever chronic disorders (multiple sclerosis, cerebral palsy)
works best when used along with physical therapy
Muscle relaxants: adverse effects/ Toxicity
adverse effects:
extension of effects on CNS and skeletal muscles
euphoria
drowsiness
muscle weakness
dry mouth
Toxicity
primarily involve the CNS
no specific antidote or reversal
can cause coma
avoid driving, (benzo) alcohol, confusion and falls, very addictive,
Common Muscle Relaxants
Baclofen (Lioresal)
used through pump → spinal fluid. allows for lower dosage
severe withdrawal symptoms, confusion, muscle spasms, sweating anxiety, with PT
should not suddenly stop
Cyclobenzaprine (Flexeril)
deep sedation
Carisoprodol (Soma)
Methocarbamol (Robaxin)
AT risk for fall because cause hyoptension
Which statement regarding muscle relaxants does the nurse identify as
being accurate?
A. Baclofen (Lioresal) is available as an injectable form for use with an
implantable pump device.
B. Cyclobenzaprine (Flexeril) produces little sedation.
C. Patients taking muscle relaxants are at high risk of developing
hypertension.
D. Patients taking muscle relaxants should be told to stop taking the
medication if they feel sleepy
A. Baclofen (Lioresal) is available as an injectable form for use with an implantable pump device
Nursing implications: CNS Depressants
give hypnotics 30-60 min before bedtime for maximum effectiveness in inducing sleep
most benzos cause REM rebound and a tired feeling the next day; use with caution in older adults
instruct patients to avoid alcohol and other CNS depressants
rebound insomnia may occur for a few nights after a 3-4week regimen has been discontinued
safety is important
Physchotherapeutic Drugs
3 main types
antianxiety
antidepressant
antpsychotic
Antidepressant Drugs Indications & MOAs
Indications
▪ Major depressive disorders
▪ Eating disorders
▪ Personality disorders
▪ Various medical conditions
Mechanism of Action
▪ Increase the levels of neurotransmitter
concentration in CNS
Most common antidepressant
SSRIs- selective serotonin reuptake inhibitors
Antidepressants: Classes
selective serotonin reuptake inhibitors (SSRI’s)
tricyclic antidepressants- (TCA’s)
Monoamine oxidase inhibitors (MOAI’s)
Second generation/ SSRI’s MOA
Fewer adverse effect than TCAs and MOAIs
very few drug-drug or drug-food interactions
still take about 4 to 6 weeks to reach maximum clinical effectiveness
now considered first-line drugs for depression
MOA
inhibition of serotonin reuptake and possible effects on norepinephrine and dopamine reuptake
SSRI adverse effects
insomnia
weight gain
sexual dysfunction (erectile)
Serotonin syndrome READ BOOOK ***
Common symptoms
insomnia, headache, sexual dysfunction, nausea, dizziness, sweating, agitation, restlessness, clonus (rhythmic muscle spasm), tremor, rash, dry mouth, ocular clonus, confusion, delirium, hyperreflexia, loss of consciousness, high BP,
Late symptoms: seizures, rhabdomyolysis (muscle pain, weakness, dark urine, feeling tired, severe muscle cramps, confusion), renal failure, death
Commonly used SSRI
Citalopram (Celexa)
fluoxetine (Prozac)
duloxetine (Cymbalta)
mirtazapine (Remeron) - sedation occurs, give at HS,
Sertraline (Zoloft)
Escitalopram (Lexapro)
Tricyclic antidepressants MOA
Block reuptake of neurotransmitters, causing accumulation at the nerve endings
2nd line medications
Tricyclic indications
Depression
OCDs (clomipramine)
Pain
Tricyclic
amitriptyline
desipramine
doxepin
imipramine
nortriptyline
protriptyline
TCAs can be added to
pain medication because it gets a better synergistic effect
trigeminal neuralgia
intense pain in the face
dehabilit
TCA no no
NO PREGNANCY
sedation (geriatric shouldn’t need)
impotence (Erectile dysfunction)
orthostatic hypotension
TCA overdose
Lethal: 70%-80% die before reaching the hospital
CNS and cardiovascular systems are mainly affected
no specific antidote
death from seizure or dysrhythmia
activated charcoal-
alkaline promoting food
sodium bicarbonate, fruits and vegetable
MOAIS
rarely used for depression
used for Parkinson’s disease
disadvantage: potential to cause hypertensive crisis when taken with tyramine
ingestion of food or drinks with tyramine leads to hypertensive crisis, which may lead to cerebral hemorrhage, stroke, coma, or death (aged cheese, smoked, pickled or aged meats, sausage, yeast extracts, red wines, bologna)
avoid foods that contain tyramine
MAO Inhibitors READ*
-Nardil- NO
-Parnate- POPULAR
-Marplan- MEDS
barbiturates
tricyclic antidepressants
antihistamines
CNS depressants
antihypertensives
OTC cold medication
causes sweating, tremors, elevated temp, bounding heart, high BP
Antidepressant Nursing Implications
Inform patients that it may take several weeks to see
therapeutic effects.
▪ Monitor patients closely during this time, assess for
suicidal tendencies and provide support.
▪ Assist older adult and weakened patients with
ambulation and other activities because falls may
occur because of drowsiness or postural
hypotension.
▪ Caffeine and cigarette smoking may decrease
effectiveness of medication therapy.
▪ With MAOIs, instruct patients and family regarding
tyramine-containing foods and signs and symptoms
of hypertensive crisis.
When patients are taking selective
SSRIs for the first time for
depression, which is most important
to monitor for during the first few
weeks of therapy?
A. Hypertensive crisis
B. Suicidal thoughts
C. Convulsions
D. Orthostatic hypotension
B. Suicidal Thoughts
Antipsychotics
First Generation
Haloperidol (Haldol)
Chlorpromazine (Thorazine)
thioridazine (Mellaril)
Second Generation
Aripiprazole (Abilify)
Brexpiprazole (rexulti)
Clozapine (Clozaril)
Lurasidone (Latuda)
Quetiapine (Seroquel)
Ziprasidone (Geodon)
Olanzapine (Zyprexa, Lybalvi, Symbyax)
Antipsychotics MOA
dopamine levels in CNS are decreased
drug-induced psychoses, schizophrenia, and autism
used to treat extreme mania
BLACK BOX
dementia
Adverse effects:
CNS effects
-drowsiness
-neuroleptic malignant syndrome (NMS)
_ potentially life threatening
_high fever, unstable blood pressure (BP), myoglobinemia
-Extrapyramidal symptoms (EPS): pseudo parkinsonism-akathisia
-tardive dyskinesia
Weight Gain (abdominal obesity)
Metabolic Syndrome
Antipsychotic typicals
much more side effects
EPS
older drugs
higher tardive dyskinesia risk
Antipsychotic atypicals
Newer drugs
treats psychosis, bipolar, depression,
more likely to cause weight gain, diabetes
lower tardive dyskinesia risk
Antipsychotics Nursing Implications
monitor for therapeutic effects
monitor for adverse effects
advise patients to avoid abrupt withdrawal
antiparkinsonian drugs
chronic, progressive, degenerative disorder
affects dopamine-producing neurons in the brain (affects movement)
slowness of gait, droopy face, no expression, slow movements
antiparkinsonian drugs: symptoms of PD
Classic symptoms include:
-tremor
-rigidity
-akinesia
-postural instability
-TRAP acronym
Staggering Gait
Drooling
Dopamine Replacement Drugs
Carbidopa-Levodopa (Sinemet)
Given with Carbidopa
Adverse effects:
delay use as long as possible because it only goes so far
causes lots of nausea
cardiac dysthymias
GI distress
muscle cramps
all about function
empty stomach!!
Antiparkinsonian Drugs: Nursing Implications
-Inform patient not to take other medications with PD drugs
- Administer oral doses with food to minimize GI upset.
- Encourage patient to force fluids to at least 3000 mL/day (unless contraindicated).
- Taking levodopa with MAOIs may result in hypertensive crisis.
- Patient should be taught not to discontinue antiparkinson drugs suddenly
hyperpyrexia syndrome- febrile, neurological emergency
PHC