Term
|
Definition
1.Reduction of apprehension and excitement
2.With minimal alteration of coordination and mental status |
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Term
|
Definition
Induction of sleep
Approximating the normal physiologic state |
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Term
|
Definition
| Reduction of apprehension and excitement more selectively than during sedation |
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Term
| almost all benzodiazepenes end with the letters |
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Definition
|
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Term
| all barbiturates end with the letters |
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Definition
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Term
| benzodiazepines are used in dentistry for 4 major reasons |
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Definition
1. Antianxiety drugs
Alprazolam (Xanax)
Diazepam (Valium)
Lorazepam (Ativan)
2. Sedative-hypnotics
Temazepam (Restoril)
Triazolam (Halcion)
3. Anticonvulsants
Clonazepam (Klonopin)
Clorazepate (Tranxene)
4. Anesthetic
Midazolam (Versed) |
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Term
| antianxiety benzod used in dentistry is sponsored by the ADL (3) |
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Definition
Alprazolam (Xanax)
Diazepam (Valium)
Lorazepam (Ativan) |
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Term
| Sedative-hypnotics used in dentistry (2) |
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Definition
Temazepam (Restoril)
Triazolam (Halcion |
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Term
| Anticonvulsants used in dentistry (2) |
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Definition
Clonazepam (Klonopin)
Clorazepate (Tranxene) |
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Term
Anesthetic benzo used in dentistry
(1) |
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Definition
|
|
Term
benzopiazepines.
for over 15 years ______ was most popular |
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Definition
|
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Term
benzodiazepines.
______ is now the most prescribed |
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Definition
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|
Term
benzodiazepine mechanism of action: binds to the _____ receptor on the _______ receptor complex.
interacts with _____ by increase /decrease binding?
leading to effect on _____ channel
and increasing __________ of channel opening |
|
Definition
1. Binding to benzodiazepine (w) receptor on the GABAA receptor complex
2. Interaction with g-aminobutyric acid (GABA)
a. improved GABA binding to GABAA receptor site
b. enhanced GABA effect on chloride channel; increases frequency of channel opening |
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Term
| GABA is the ________ _______ ______ NT of the ___ |
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Definition
| most important inhibitory NT of the CNS |
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Term
| ____ receptor is coupled to the ____receptor so that its activation facilitates the action of ____ on the _____ _____. Increased chloride influx leads to _____ _____ of the neuron |
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Definition
| Benzo receptor is coupled to the GABA receptor so that its activation facilitates the action of GABA on the chloride ionophore channel. Increased chloride influx leads to hyperpolarization (inhibition) of the neuron |
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Term
diazepam and midazolam are similar in structure except that...
which enhances the .....
so the drug is ...... acting |
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Definition
| midazolam has a nitrogen ring, which enhances the metabolism of the drug so they are shorter acting. |
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|
Term
gaba receptor complex has .... subunits
..... subunits must bind to be effective
the number of subunits may explain...... |
|
Definition
5
2
differences in the selectivity of the benzos |
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Term
| Pharmacologic effects of benzos |
|
Definition
Antianxiety effect.
CNS depression (dose-dependent).
Anticonvulsant action.
Centrally mediated muscle relaxation.
Anterograde amnesia.
Minimal cardiovascular depression (i.e. cardiac output, blood pressure).
Inhibition of stage 4 sleep (“night terrors”). |
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|
Term
names of benzos that provide
Acute and chronic anxiety relief: |
|
Definition
| alprazolam, diazepam, lorazepam |
|
|
Term
Therapeutic Uses of benzos
Perioperative sedation: |
|
Definition
| diazepam, lorazepam, midazolam, triazolam |
|
|
Term
| names of benzos used to treat Acute insomnia:hypnotics |
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Definition
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Term
|
Definition
|
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Term
|
Definition
|
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Term
|
Definition
| clonazepam, clorazepate, diazepam, lorazepam, midazolam |
|
|
Term
| Panic disorders and depression: |
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Definition
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Term
| Adverse effects of benzos (7) |
|
Definition
1. Respiratory depression
2. Drowsiness
3. Paradoxical excitement bec of lowered inhibitions
4. Vascular irritation with IV injection
5. Drug abuse (class IV)
6. Narrow-angle glaucoma attack 1 case
7. Teratogenesis (category D, X) tx seizure |
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|
Term
| benzos with shorter half life |
|
Definition
|
|
Term
| benzo Drug Interactions with Carbamazepine, rifampin |
|
Definition
| Increased rate of metabolism reduces the bioavailability |
|
|
Term
| benzo interaction with Cimetidine, diltiazem, verapamil, erthromycin, clarithromycin, protease inhibitors, ketoconazole, fluoxetine, trazodone |
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Definition
| Decreased rate of metabolism increases the bioavailability and significantly augments and prolongs their effects 3 fold even |
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|
Term
Inverse Agonist of benzo receptor
yield ______ pharmacologic effects |
|
Definition
opposite
inhibit the conventional agonist |
|
|
Term
benzo antagonist such as _____ can be used to treat ____
can reverse _____ in _ minutes
Can precipitate _____ in patients that are dependent on benzodiazepines |
|
Definition
Flumazenil (Romazicon)
OD's
sedation in 2 minutes
withdrawl |
|
|
Term
Selective BZ1-Receptor Agonists
3, catch your z's with these 3 |
|
Definition
Zolpidem (Ambien)
Zaleplon (Sonata)
Eszopiclone (Lunesta |
|
|
Term
Selective BZ1-Receptor Agonists
Mechanism of action |
|
Definition
| Stimulation of specific benzodiazepine receptors |
|
|
Term
Selective BZ1 Receptor Agonists
Pharmacologic characteristics
1.onset?
2.duration?
3.amnesia effect?
4.pregnancy category
5.sleep architecture
6.reversible? |
|
Definition
1.rapid
2.short
3.less
4.B zolpidem, C zaleplon
5. preserves it
6. reversivble with flumazenil |
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|
Term
Barbiturates used for
3
based on duration |
|
Definition
iv anesthetics very short. thiopental highly lipid sol
sedative hypnotics medium. pento lipid soluble
anticonvulsant long. |
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|
Term
Barbiturates
Mechanism of action
1.Binding to receptors on the ____ receptor/_____ channel
1A. Increased ____ effects
1B Increases _____ of GABA-mediated channel opening
1C _____ concentrations act directly on the ________, not requiring the presence of ____
2. _______effects on glutamate receptors |
|
Definition
1. Binding to receptors on the GABAA receptor/chloride channel
1A. Increased GABA effects
1B. Increases duration of GABA-mediated channel opening
1C. High concentrations act directly on the Cl- channel, not requiring the presence of GABA
2 Inhibitory effects on glutamate receptors |
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|
Term
Pharmacologic/toxic effects
CNS depression
occurs at 4 levels |
|
Definition
Sedation (50-100 mg pentobarbital)
Hypnosis (100-200 mg)
Anesthesia (300-400 mg)
Death (>600 mg) |
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Term
| Pharmacologic/toxic effects |
|
Definition
Analgesia and algesia
Cardiovascular depression
Anticonvulsant action
Respiratory reflex activity |
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|
Term
| Pharmacologic/toxic effects |
|
Definition
Decrease length of time in REM sleep
Liver microsomal stimulation
Multiple drug interactions
Contraindicated in porphyria
Teratogenesis
Tolerance, dependence, addiction |
|
|
Term
Miscellaneous agents
1Antianxiety drugs
1a Meprobamate (like barbiturates in humans)
1b Buspirone
1b1 Not a CNS depressant
1b2 Slow onset time (1-3 weeks)
1b3 5-HT1A receptor partial agonist |
|
Definition
|
|
Term
-Miscellaneous agents
Sedative-hypnotics
Chloral hydrate
Ramelteon (Rozerem)
-Centrally acting muscle relaxants
Methocarbamol (Robaxin |
|
Definition
|
|
Term
Chloral hydrate....
pediatrics? |
|
Definition
Similar margin of safety to barbiturates
Additional gastrointestinal disturbances
Possible arrhythmogenic effect
Carcinogenic effect?
there have been several reports of death with it that is unpredictable and not necessarily a result of an error with the drug. |
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Term
|
Definition
Melatonin (MT1 and MT2) receptor agonist
Very safe agent
Active metabolite = next-day grogginess
Only nonscheduled prescription drug for insomnia |
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Term
|
Definition
1. Sedative-hypnotic
2. Low margin of safety
3. Widespread uncontrolled use
4. Therapeutically useful when more effective drugs unacceptable to patient
5. Avoid when using another CNS depressant |
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|
Term
alcohol
Capacity-limited kinetics |
|
Definition
1. Eliminated at a constant rate (i.e. 16-25 mg/dl per hour) as opposed to a constant percentage like other drugs
2. At low to moderate doses, it then follows first-order kinetics |
|
|
Term
|
Definition
o EtOH --> Acetaldehyde by Alcohol dehydrogenase and 5% by Microsomal enzyme oxidation system
MEOS builds up in chronic alcohol use and then will metabolize more
This same NZ takes acetomeniphin and turns it into a toxic substance thus alcoholics can’t take normal acetomenophin doses
Paradoxically, to be safe when taking Tylenol, alcoholics should drink alcohol so MEOS system isn’t 100% free
o Acetaldehyde --> acetic acid by aldehyde dehydrogenase
Disulfram (antabause) inhibits this enzyme and you get a build up of acetic acid |
|
|
Term
|
Definition
Cirrhosis, hepatitis
Cardiomyopathy
Erosive gastritis, pancreatitis
Nutritional deficiencies and neuropsychiatric disorders
Fetal alcohol syndrome
Violent death |
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