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Drugs that produce either sedation or hypnosis depending on the dosage of the drug administered and the patient’s response to it.
- Sedative Hypnotics
- Lower dosage of these drugs produce a calming effect (sedation) usually associated with a degree of drowsiness and motor incoordination (ataxia) wheras higher doses induce hypnosis (a state resembling physiologic sleep)
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Which are the sedative hypnotics?
- 1. Benzodiazepines
- Flurazepam, Temazepam, Triazolam, Lorazepam, Midazolam
- 2. Nonbenzodiazepines
- Zolpidem, Zaleplon, Eszopiclone
- 3. Chloral Derivatives: Chloral hydrate
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Sedative Which peak plasma levels develop within 30-60 min, Half life is 47-100 hours. Biotransformed in the liver (should be cautious with patients with hepatic dysfunction)
- Incidence of side effects is approximately 7%. Dizziness, drowsiness, lightheadness, staggering and ataxia are most common.
Usual dosage 30mg 1 hour before procedure (15mg is elderly/debilitated: Available in 15mg and 30mg capsules
Pregnancy class X
Flurazepam (Dalmane)
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Sedative which is absorbed slowly after oral administration, onset is within 20-30 minutes, but peak plasma levels at 2-3 hours Plasma half life is 10 hours. Primary use of this drug is patients who have difficulty remaining asleep once they fall asleep because of its slow onset of action. It is not useful for patients who have trouble falling asleep.
Usual dose is 30mg. 15mg can be used initially for elderly and debilitated patients. Available in 15mg and 30mg capsules
Pregnancy Category X
Temazepam (Restoril)
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Sedative which was approved for marketing as a hypnotic in 1982 has become the most prescribed psychoactive drug in the United States and has become the most prescribed psychoactive drug in the united states.
Valuable in dentistry because of its short half-life of 1.5-5.5 hours and peak plasma levels at 1.3 hours following oral administration. Very little “hangover”, used extensively in dentistry as an effective oral drug in the management of pretreatment anxiety. TRAVELERS AMNESIA, CAUTION HEAVY MACHINERY AND CNS DEPRESSANTS.
Dosage: .25mg 1 hour before dental treatment. .125mg may be enough for selected patients (initial dose for elderly or debilitated patient) BANNED IN UK
Availability: .125mg and .25mg
Halcion (Triazolam), PREGNANCY CLASS X
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Sedative absorbed slowly, peak plasma levels in 2 hours. Mean half life is 12 hours
**Contraindicated in patients with narrow angle glaucoma
***Not recommended for patients with a primary depressive disorder or psychosis
**Avoid driving and other CNS depressants (FOR ALL OF THESE DRUGS)
**Greater risk of unwanted sedation. its use in the immediate preoperative period should be discouraged
Dosage: 2-4mg 1 hour before treatment
Availability: .5, 1, 2mg tablets
Classified as an antipsychotic medication “major tranquilizer”
Lorazepam (Ativan) Pregnancy: Category D
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Sedative with peak action occurs within 30 minutes of oral administration (Fast!)
Obviously also used in the IV form!
Orally still quick acting option available in a syrup form FOR CHILDREN MOSTLY)
Dosage: .25-.5mg/kg not to exceed 20mg per dose
Available as 2.0 mg/ml syrupPregnancy Category D
Midazolam (Versed)
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A NonBenzodiazepine sedative approval 1993, Unrelated structurally to the benzodiazepines, interacts with GABA benzodiazepine receptor complex and shares some of the pharmacologic properties of benzodiazepines
Strong sedative with only mild anxiolytic properties
Following oral admin effects are seen in about 45 minutes. Peak effect in 1.6 hours. Elimination half life is 2.6 hours, VERY ADDICTIVE
Use very cautiously for dentistry
Dosage: 5-10 mg PO 1 hour previous
Pregnancy category: C
Zolpidem (ambien)
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NonBenzo Sedative/hypnotic that appears to be absorbed and eliminated more rapidly than ambien
Use with caution with patient who have a history of hypersensitivity to these types of drugs.
Dependency and abuse are potential problems with prolonged administration (similar to ambien) Indicated only for short term use
Hangover is common as with ambien
Dosage: 5-10mg orally 1 hour before
Pregnancy Category C
Zaleplon (Sonata)
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NonBenzo sedative/hypnotic Indicated for chronic treatment of insomnia, has rapid onset of action and should only be taken immediately before sleep
Properties are thought to be induced by modulation of the GABA receptor of chloride channel complex
Unrelated to benzos however non selectively binds to GAPA receptors so shows sedative effects similar to benzodiazepines
Sleepwalking and sleepdriving are risks (also for Ambien!)
Dosage: 1-3mg immediately before retiring (not used in dental procedures)
Pregnancy category C
Flumazenil reverses the effects !!
Eszopiclone (Lunesta)
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Sedative hypnotic non related to benzos or other derivatives that Was previously very widely used particularly in pediatric dentistry
Does not possess any analgesic properties!
Rapidly absorbed, Half life is 7-9.5 hours
isadvantages: unpleasant taste, GI upset, nausea, vomiting, ataxia, nightmares
CAUTION WITH COUMADIN or CNS Depressants
TOXIC DOSE: 10g but death has occurred with as little as 4g
Dose based on patient body weight. Range 25-60 mg/kg
Chloral Hydrate, pregnancy class C
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Two most commonly used for sedative-antianxiety purposes that are primarily histamine blockers
Promethazine and hydroxyzine
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Flumazenil dose
.2 (keep dosing until you reach 1mG)
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There is not an IV amoxicillin available. which is the option?
Ampicillin and Clindamycin
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