Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
68 Cards in this Set
- Front
- Back
Differentiate sedative drugs from hypnotic drug in terms of their ability to facilitate sleep.
|
sedatives do not produce sleep while hypnotics produces drowsiness and facilitates the onset and maintenance of sleep
|
|
Differentiate sedative drug s from hypnotic drugs in terms of the time of day there are usually give.
|
sedatives are usually given during daytime hours while hypnotic drugs are given at night
|
|
Complaint of inadequate sleep
|
insomnia
|
|
T/F. One of the symptoms of insomnia can be fatigue despite sleep of adequate duration
|
T
|
|
Unpleasant state tension, apprehension or uneasiness
|
Anxiety
|
|
Anxiety Disorder characterized by ongoing state of excessive anxiety lacking any clear reason or focus
|
Generalized anxiety disorder
|
|
Anxiety disorder characterized sudden attacks of overwhelming fear with somatic symptoms such as sweating, tachycardia, chest pains, trembling and choking
|
Panic Disorder
|
|
Anxiety disorder which is characterized by strong fears of specific objects or situations
|
phobias
|
|
Anxiety triggered by recall of past stressful experiences
|
post-traumatic stress disorder
|
|
Anxiety disorder which is characterized by ritualistic behavior driven by irrational anxiety
|
Obsessive-compulsive disorder
|
|
Barbiturates were formerly the mainstay agents in sedating patients or inducing and maintaining sleep. Why are they now replaced by benzodiazepines?
|
Barbiturates induce 1)tolerance 2)drug-metabolizing enzymes 3)physical-dependence 4)severe-withdrawal symptoms 5)coma in toxic doses
|
|
Describe the chemical structure of barbiturates |
w/ 2, 4, 6-trioxohydroxypyrimidine |
|
Describe the MOA of barbiturates
|
they increase the duration of opening of GABA-gated chloride channels. They are GABA-mimetic-at high concentrations, it directly activates chloride channels. They also inhibit the excitatory neurotransmitter, glutamate by binding to AMPA receptor
|
|
T/F. The multiplicity in sites of action of barbiturates may be the basis for their ability to induce full surgical anesthesia and for their more pronounced central depressant effects
|
T
|
|
Characterize the following barbiturates whether they are ultra-short-acting, short-acting, intermediate acting, or long acting: Thioamylal, Pentobarbital, Secobarbital, Amobarbital, Methohexital, Thiopental, Butabarital, Phenobarbital, Mephobarbital, and Methabarbital
|
ultra-short-acting= Methohexital, Thiopental,Thioamylal ; short-acting= Pentobarbital, Secobarbital,; intermediate acting= Amobarbital, Butabarital; long acting=Phenobarbital, Mephobarbital, and Methabarbital |
|
What is the duration of action of barbiturates ultra-short-acting, short-acting, intermediate-acting, and long-acting?
|
Ultra-short-acting= 20 minutes or less, short-acting= <3 hours, and intermediate-acting= 3-6 hours, and long-acting= >6 hours |
|
Ultra-short-acting barbiturates is for anesthetic. How about long-acting barbiturates?
|
selective anticonvulsant
|
|
Most commonly used barbiturates?
|
Thiopental
|
|
First-line anticonvulsant drug?
|
Phenobarbital
|
|
DOC for treatment of young children with recurrent febrile seizures?
|
phenobarbital
|
|
Long-acting barbiturate that is used as a long term management of tonic-clonic seizures, status epilepticus, and eclampsia
|
phenobarbital
|
|
What is the major complication of barbiturate anesthesia?
|
Laryngospasm
|
|
T/F/ Barbiturates may induce hypersensitivity causing Steven Johnson’s Syndrome.
|
T
|
|
With the chronic use of phenobarbital, what blood related AE can it produce?
|
Megaloblastic anemia
|
|
T/F. Barbiturates inhibit CYP450 system.
|
F. They induce. |
|
Barbiturates increase _ synthesis?
|
Porphyrin. It is contraindicated to patients with acute intermittent porphyria or porphyria variegata
|
|
In severe toxicity with barbiturates, describe the AE related to breathing.
|
Cheyne-stokes (irregular) respiration
|
|
Treatment for Barbiturate toxicity?
|
artificial respiration, forced alkaline diuresis, and hemodialysis- necessary only rarely
|
|
Describe the chemical structure of benzodiazepines. What s essential for activity?
|
w/ 1, 4-benzodiazepine; A Halogen or Nitro group on position 7 is essential for activity
|
|
Describe the MOA of benzodiazepines
|
they increase the frequency of opening of chloride channels; they induce inhibitory postsynaptic potential via hyperpolarization and decreased neuronal excitability
|
|
Major inhibitory neurotransmitter in the CNS
|
GABA (gamma-amino butyric acid) Receptors
|
|
GABA Receptors are synthesized from? Via?
|
Glutamate via glutamic acid decarboxylase
|
|
Group the related terms. GABA-A Receptors, Metabotropic, coupled to g receptor and inhibit Ca2+ channels or activate K+ channels, Ionotropic, pentameric structures selectively permeable to Cl-, GABA-B Receptors,
|
GABA-A Receptors,Ionotropic, pentameric structures selectively permeable to Cl- GABA-B Receptors, Metabotropic, coupled to g receptor and inhibit Ca2+ channels or activate K+ channels |
|
GABA-A Receptor agonist
|
Muscimol
|
|
GABA-A Receptor antagonists
|
Bicuculine/ Picrotoxin
|
|
GABA-B Receptor Agonist
|
Baclofen
|
|
GABA-B Receptor Antagonist
|
2-OH Saclofen
|
|
T/F. The action of benzodiazepines is dose dependent
|
T. At low doses, it is an anxiolytic/sedative drug; at high doses, it is a hypnotic drug.
|
|
Characterize the following benzodiazepines whether they are short-acting, intermediate acting, or long acting: Midazolam, Alprazolam, Clorazepate, Chlordiazepoxide, Diazepam, Flurazepam, Estazolam, Oxazepam, Triazolam, Lorazepam, Temazepam, and Quazepam.
|
Short-acting= Midazolam, Oxazepam, and Triazolam; Intermediate-acting= Alprazolam, Estazolam, Lorazepam, and Temazepam; Long-acting= Clorazepate, Chlordiazepoxide, Diazepam, Flurazepam, and Quazepam.
|
|
Which benzodiazepine is used for short and long-term treatment of panic disorders?
|
Alprazolam
|
|
Which benzodiazepine is used for patients with anxiety that may require treatment for prolonged periods of time?
|
Diazepam
|
|
Which benzodiazepine can be used for the chronic treatment of epilepsy?
|
Clonazepam
|
|
Which benzodiazepine is used for the treatment of skeletal muscle spasms and spasticity from degenerative disorders (Multiple sclerosis and cerebral palsy)
|
Diazepam
|
|
DOC for grand mal seizures status epilepticus?
|
Diazepam
|
|
Which benzodiazepine is used to reduce both sleep induction time and the number of awakenings? It increases duration of sleep; it is long acting and can maintain effectiveness up to 4 weeks; it may cause little rebound insomnia and daytime sedation.
|
Flurazepam
|
|
Which benzodiazepine is used for patients who experience frequent wakening or those who have inability to stay asleep? |
Temazepam |
|
How should Temazepam be taken?
|
Should be given several hours before bedtime
|
|
Which benzodiazepine is used to induce sleep in patients with recurring insomnia? Used for patients who have difficulty in going to sleep?
|
Triazolam
|
|
Commonly used to sedate hospitalized patients.
|
Triazolam
|
|
Benzodiazepines that can induce Stage III Anesthesia (surgical anesthesia).
|
Diazepam, Lorazepam, and Midazolam
|
|
Benzodiazepines that can be used as acute treatment of alcohol withdrawal.
|
Diazepam, Lorazepam, and Midazolam
|
|
Describe the metabolism of benzodiazepines.
|
Through hepatic metabolism; it undergoes microsomal oxidation (phase I reactions) and subsequently conjugated (phase II reactions) to form glucuronides that are secreted in the urine
|
|
Which benzodiazepines have less probability of cumulative residual effects because they immediately undergo conjugation instead of oxidation then conjugation?
|
Oxazepam and Lorazepam
|
|
T/F. Benzodiazepines unlike barbiturates no longer produce dependence and tolerance.
|
F. They still can occur if high doses are given over a prolonged period of time.
|
|
What is the treatment for Benzodiazepine toxicity? Example is when the patient experiences severe respiratory depression (because it is given with other CNS depressants).
|
Flumazenil (IV only)
|
|
Flumazenil, aside from being a benzodiazepine receptor antagonist, also blocks the actions of what drugs?
|
Eszopiclone, Zaleplon, and Zolpidem
|
|
Other names of Chloral hydrate?
|
Mickey Finn, Knockout drops
|
|
Chloral hydrate is reduced to what compound which is a potent alcohol responsible for it pharmacologic activity?
|
trichloroethanol
|
|
Zolpidem, Flurazepam, and Triazolam shorten sleep latency. What is the advantage of Zolpidem over the other two?
|
1) No withdrawal effects 2) Minimal rebound insomnia 3) Little or no tolerance occurs with prolonged use 4) rarely associated with respiratory depression even in overdose
|
|
Both diazepam and Buspirone can be used to treat anxiety. What is the advantage of Buspirone?
|
Minimal sedation and psychomotor and cognitive dysfunction 2) dependence is unlikely (Disadvantage: slow onset of action)
|
|
This drug has antihistamine and antiemetic activity; it is used for patients with anxiety, who have a history of drug abuse; it is often used for sedation prior to dental procedures or surgery.
|
Hydroxyzine
|
|
This drug is indicated as a pediatric or geriatric hypnotic; it can be used as a preanesthetic agent for minor surgical and dental procedures.
|
Chloral hydrate
|
|
Non-Rx effective in treating mild types of insomnia but they have numerous side effects that make them less useful than benzodiazepines.
|
Diphenhydramine and Doxylamine
|
|
These drugs hypnotic drugs are unrelated to benzodiazepines but they share a similar MOA (binding to GABA-A receptor)
|
Zaleplon and Eszopiclone
|
|
New hypnotic drug; agonist at MT1 and MT2 melatonin receptors located in the suprachiasmatic nuclei of the brain; it appears to be distinctly more efficacious than melatonin as hypnotic
|
Ramelteon
|
|
What compound is in Sleepasil? What is significant regarding its onset of action?
|
Melatonin. It takes 2 weeks before one experiences the hypnotic effect.
|
|
Brand name of Methohexital?
|
Brevital
|
|
Brand name of Thiopental?
|
Penthotal
|