pharm quiz 2 Flashcards
3 types of sedative-hypnotics
- Benzodiazepines
- Barbiturates
- Nonbarbiturate Hypnotics
Alprazolam (Xanax) Lorazepam (Ativan) Midazolam (Versed) Temazepam (Restoril) Triazolam (Halcion)
benzodiazepines used as anxiolytic hypnotics
Mechanism of Action: enhance the action of gamma-aminobutyric acid (GABA) in the CNS
Pharmacokinetics
Absorbed from GI track with peak levels in 30 minutes to 2 hours
Distributed throughout body; lipid soluble
Metabolized in liver
Excreted in urine
Cross placenta and enter breast milk
benzodiazepines used as anxiolytic hypnotics
CNS depression—lightheaded, drowsiness
Anterograde amnesia
Paradoxical responses—insomnia, excitation, rage
Respiratory depression with IV administration
Physical dependence and withdrawal symptoms if rapid discontinuation
Acute toxicity if overdose—drowsy, lethargic, confused, respiratory depression; Note that Flumazenil (Romazicon) is administered to counteract sedation and reverse effects of overdose
S/S of Benzodiazepines Used as Anxiolytic-Hypnotics
Known allergy
Pregnant/lactating
Sleep apnea, respiratory depression, presence of organic brain disease
Avoid alcohol and other CNS depressants such as Barbiturates and Opioids
Use cautiously if history of substance use disorder, liver dysfunction, kidney failure, and in elderly
contraindications of Benzodiazepines Used as Anxiolytic-Hypnotics
depress the sensory cortex, decrease motor activity, and alter cerebellar function; produce sedation, hypnosis, and anesthesia
Barbiturates Used as Anxiolytics-Hypnotics
Amobarbital (Amytal Sodium) Butabarbital (Butisol) Pentobarbital (Nembutal) Phenobarbital (Luminal) Secobarbital (Seconal)
Barbiturates Used as
Anxiolytics-Hypnotics
Absorbed in GI track with peak levels in 20-60 minutes
Metabolized in liver; lipid soluble
Excreted in urine
Readily cross the placenta and enter breast milk
Barbiturates Used as
Anxiolytics-Hypnotics
CNS depression—drowsiness, lethargy, vertigo, ataxia, feeling “hung-over”, paradoxical excitement, anxiety
GI—nausea, vomiting, constipation, diarrhea, epigastric pain
Cardiovascular—bradycardia, hypotension, syncope
Serious hypoventilation and respiratory depression can occur
Rash, serum sickness, Stevens-Johnson Syndrome
Barbiturates Used as
Anxiolytics-Hypnotics
Known allergy
Severe hepatic, renal, cardiac, or respiratory disease
History of drug abuse or dependence
Porphyria; uncontrolled pain
Lactation
Use cautiously with children, elderly or debilitated individuals; hepatic, renal, cardiac, or respiratory impairment; depressed/suicidal individuals; pregnancy
Note: Several drug to drug interactions and additive CNS depression with alcohol
contraindications Barbiturates Used as Anxiolytics-Hypnotics
Eszopiclone (Lunesta)
Zalepton (Sonata)
Zolpidem (Ambien)
nonbarbiturate hypnotics
Mechanism of Action: enhance the action of GABA in the CNS
Absorbed by GI track
Metabolized in liver
Excreted in urine
Can cross the placenta and enter breast milk
nonbarbiturate hypnotics
Daytime sleepiness and lightheadedness—so advise to take med just before bedtime and allow for at least 8 hours of sleep
use in caution in elderly, impaired kidney, liver or respiratory function
nonbarbituate hypnotics
CNS stimulation is mediated by release of norepinephrine from central noradrenergic neurons in the cerebral cortex, reticular activating system (RAS), and brainstem. However, the action in the treatment of ADHD is unclear.
CNS stimulants used to treat ADHD
calming hyperexcitability through CNS stimulation that is seen in ADHD is believed to be related to increased stimulation of the immature RAS, which leads to the ability to be more selective in response to incoming stimuli
paradoxical effect
Methylphenidate (Ritalin, Concerta) Dexmethylphenidate (Focalin) Dextroamphetamine (Dexedrine) Amphetamine Mixture (Adderall) Lisdexamfetamine dimesylate (Vyvanse)
controlled substances of CNS stimulants used to treat ADHD
CNS stimulation (insomnia, restlessness)
Weight loss, anorexia, nausea
Cardiovascular effects
Hallucinations; paranoia
Withdrawal reaction if abruptly discontinued
Hypersensitive skin reaction to transdermal Methylphenidate
CNS stimulants for ADHD
Caution parents and the patient regarding physical and psychological dependence; need to taper dose under MD supervision if meds discontinued; and safe storage of these controlled substances
Big teaching point – can’t just give it when it’s due. Needs to be locked up/monitored to prevent complications with children
CNS stimulants for ADHD
Avoid concurrent use of MAOIs; caffeine; over the counter (OTC) cold medications and decongestants
OTC: increase BP and heart rate and the stimulant itself already increases this
Use caution if concurrent use of Methylphenidate with Phenytoin (Dilantin), Warfarin (Coumadin), and Phenobarbital—as Methylphenidate inhibits metabolism of these meds leading to increased serum levels
*As with all medications, inform MD about current meds so an informed decision can be made prior to prescribing additional meds/using OTC meds
interactions with CNS stimulants for ADHD
Atomoxetine (Strattera)—not a controlled substance
Other meds to treat ADHD