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Mechanism of action - benzodiazepines

Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.

 

Benzodiazepines:
alprazolam (Xanax ®)
buspirone (BuSpar ® )- Non-benzodiazepine
chlordiazepoxide (Librium ®)
clobazam -(ONFI®)
clorazepate (Tranxene ®)
clonazepam (Klonopin ®)
diazepam (Valium ®)
lorazepam (Ativan ®)
midazolam (Versed ®)
Oxazepam (Serax ®)
triazolam (Halcion ®)

Primary indication - Insomnia (includes non-benzodiazepines):
estazolam (ProSom ®)
eszopiclone (Lunesta ® )
flurazepam (Dalmane ®)
ramelteon (Rozerem ® )
Silenor® (doxepin)
suvorexant - BELSOMRA ®
temazepam (Restoril ®)
zaleplon (Sonata ® )
zolpidem (Ambien ®)

Benzodiazepine Converter

Alprazolam (xanax ®)

Short half-life
Dosing (Adults):
Anxiety: Immediate release: Effective doses are 0.5-4 mg/day in divided doses; the manufacturer recommends starting at 0.25-0.5 mg 3 times/day; titrate dose upward; maximum: 4 mg/day

Anxiety associated with depression: Immediate release: Average dose required: 2.5-3 mg/day in divided doses

Panic disorder:
Immediate release: Initial: 0.5 mg 3 times/day; dose may be increased every 3-4 days in increments </= 1 mg/day; many patients obtain relief at 2 mg/day, as much as 10 mg/day may be required

Extended release: 0.5-1 mg once daily; may increase dose every 3-4 days in increments </= 1 mg/day (range: 3-6 mg/day)

Switching from immediate release to extended release: Patients may be switched to extended release tablets by taking the total daily dose of the immediate release tablets and giving it once daily using the extended release preparation.

Dose reduction: Abrupt discontinuation should be avoided. Daily dose may be decreased by 0.5 mg every 3 days, however, some patients may require a slower reduction. If withdrawal symptoms occur, resume previous dose and discontinue on a less rapid schedule.

SUPPLIED:
Solution, oral (Alprazolam Intensol®): 1 mg/mL (30 mL)
Tablet (Xanax®): 0.25 mg, 0.5 mg, 1 mg, 2 mg
Tablet, extended release (Xanax XR®): 0.5 mg, 1 mg, 2 mg, 3 mg

Buspirone (buspar ® )

Non-Benzodiazepine (Anxiolytic)
Mechanism of Action
The mechanism of action of buspirone is unknown. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. In vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models.

Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems.

BuSpar is rapidly absorbed in man and undergoes extensive first-pass metabolism. In a radiolabeled study, unchanged buspirone in the plasma accounted for only about 1% of the radioactivity in the plasma. Following oral administration, plasma concentrations of unchanged buspirone are very low and variable between subjects. Peak plasma levels of 1 ng/mL to 6 ng/mL have been observed 40 to 90 minutes after single oral doses of 20 mg. The single-dose bioavailability of unchanged buspirone when taken as a tablet is on the average about 90% of an equivalent dose of solution, but there is large variability.

Dosing (Adults):
Generalized anxiety disorder:
Adults: 15 mg/day (7.5 mg twice daily); may increase in increments of 5 mg/day every 2-4 days to a maximum of 60 mg/day; target dose for most people is 30 mg/day (15 mg twice daily)

May take 2-3 weeks to see full effect. Avoid abrupt discontinuation - requires gradual reduction in dose.

Dosing adjustment in renal or hepatic impairment: Buspirone is metabolized by the liver and excreted by the kidneys. Patients with impaired hepatic or renal function demonstrated increased plasma levels and a prolonged half-life of buspirone. Therefore, use in patients with severe hepatic or renal impairment cannot be recommended.

SUPPLIED:
Tablet, as hydrochloride: 5 mg, 7.5 mg, 10 mg, 15 mg, 30 mg

Chlordiazepoxide (librium ®) 

Long half-life
Dosing (Adults):
Anxiety:
Oral: 15-100 mg divided 3-4 times/day.
I.M., I.V.: Initial: 50-100 mg followed by 25-50 mg 3-4 times/day as needed.

Preoperative anxiety: I.M.: 50-100 mg prior to surgery

Ethanol withdrawal symptoms: Oral, I.V.: 50-100 mg to start, dose may be repeated in 2-4 hours as necessary to a maximum of 300 mg/24 hours

Note: Up to 300 mg may be given I.M. or I.V. during a 6-hour period, but not more than this in any 24-hour period.

Dosing adjustment in renal impairment: Clcr<10 mL/minute: Administer 50% of dose
Dosing adjustment/comments in hepatic impairment: Avoid use

SUPPLIED:
Capsule, as hydrochloride: 5 mg, 10 mg, 25 mg

Injection, powder for reconstitution, as hydrochloride: 100 mg [diluent contains benzyl alcohol, polysorbate 80, and propylene glycol]

Clobazam -onfi ®

INDICATIONS AND USAGE
ONFI is a benzodiazepine indicated for adjunctive treatment of seizures associated with Lennox-Gastaut syndrome (LGS) in patients 2 years of age or older

DOSAGE AND ADMINISTRATION
•Patients ≤30 kg body weight: initiate therapy at 5 mg daily and titrate as tolerated up to 20 mg daily.
•Patients >30 kg body weight: initiate therapy at 10 mg daily and titrate as tolerated up to 40 mg daily.
•Doses above 5 mg/day should be administered in two divided doses.
•ONFI tablets can be administered whole, or crushed and mixed in applesauce.
•Reduce dose, or discontinue drug, gradually.

Dosage adjustment needed in the following groups:
•Geriatric patients
•Known CYP2C19 poor metabolizers
•Mild or moderate hepatic impairment; no information for severe hepatic impairment

HOW SUPPLIED
Tablet: 5 mg, 10 mg, or 20 mg

Clorazepate (tranxene ®) 

Long half-life
Dosing (Adults):
Anxiety:
Regular release tablets (Tranxene® T-Tab®): 7.5-15 mg 2-4 times/day .
Sustained release (Tranxene®-SD): 11.25 or 22.5 mg once daily at bedtime.

Ethanol withdrawal: Initial: 30 mg, then 15 mg 2-4 times/day on first day; maximum daily dose: 90 mg; gradually decrease dose over subsequent days

SUPPLIED:
Tablet, as dipotassium: 3.75 mg, 7.5 mg, 15 mg
Tranxene®-SD™: 22.5 mg [once daily]
Tranxene®-SD™ Half Strength: 11.25 mg [once daily]
Tranxene® T-Tab®: 3.75 mg, 7.5 mg, 15 mg

Clonazepam (klonopin ®)

Long half-life
Dosing (Adults):
Seizure disorders:
Initial daily dose not to exceed 1.5 mg given in 3 divided doses; may increase by 0.5-1 mg every third day until seizures are controlled or adverse effects seen (maximum: 20 mg/day)

Usual maintenance dose: 0.05-0.2 mg/kg; do not exceed 20 mg/day

Panic disorder: 0.25 mg twice daily; increase in increments of 0.125-0.25 mg twice daily every 3 days; target dose: 1 mg/day (maximum: 4 mg/day)

Discontinuation of treatment: To discontinue, treatment should be withdrawn gradually. Decrease dose by 0.125 mg twice daily every 3 days until medication is completely withdrawn.

Elderly: Initiate with low doses and observe closely

SUPPLIED:
Tablet: 0.5 mg, 1 mg, 2 mg
Tablet, orally-disintegrating [wafer]: 0.125 mg, 0.25 mg, 0.5 mg, 1 mg, 2 mg

Diazepam (valium ®) 

Long half-life
Dosing (Adults):
Anxiety/sedation/skeletal muscle relaxant:
Oral: 2-10 mg 2-4 times/day
I.M., I.V.: 2-10 mg, may repeat in 3-4 hours if needed

Sedation in the ICU patient: I.V.: 0.03 to 0.1 mg/kg every 30 minutes to 6 hours.

Status epilepticus: I.V.: 5-10 mg every 10-20 minutes, up to 30 mg in an 8-hour period; may repeat in 2-4 hours if necessary.

Rapid tranquilization of agitated patient (administer every 30-60 minutes): Oral: 5-10 mg; average total dose for tranquilization: 20-60 mg

Elderly: Oral: Initial:
Anxiety: 1-2 mg 1-2 times/day; increase gradually as needed, rarely need to use >10 mg/day (watch for hypotension and excessive sedation)

Skeletal muscle relaxant: 2-5 mg 2-4 times/day

Dosing adjustment in hepatic impairment: Reduce dose by 50% in cirrhosis and avoid in severe/acute liver disease

SUPPLIED:
Gel, rectal (Diastat®):
Adult rectal tip [6 cm]: 5 mg/mL (15 mg, 20 mg)
Pediatric rectal tip [4.4 cm]: 5 mg/mL (2.5 mg, 5 mg)
Universal rectal tip [for pediatric and adult use; 4.4 cm]: 5 mg/mL (10 mg)

Injection, solution: 5 mg/mL (2 mL, 10 mL)
Solution, oral: 5 mg/5 mL (5 mL, 500 mL)
Solution, oral concentrate (Diazepam Intensol®): 5 mg/mL (30 mL)

Tablet (Valium®): 2 mg, 5 mg, 10 mg

Estazolam (prosom ®) 

Intermediate half-life
Dosing (Adults):
Short-term management of insomnia:
Oral: 1 mg at bedtime, some patients may require 2 mg; start at doses of 0.5 mg in debilitated or small elderly patients.

INDICATIONS AND USAGE
Estazolam tablets are indicated for the short-term management of
insomnia characterized by difficulty in falling asleep, frequent
nocturnal awakenings, and/or early morning awakenings. Both outpatient
studies and a sleep laboratory study have shown that estazolam
administered at bedtime improved sleep induction and sleep maintenance

SUPPLIED:
Tablet: 1 mg, 2 mg

Eszopiclone (lunesta ® ) 

Non-Benzodiazepine (Sedative)
Dosing (Adults): Insomnia: Initial: 2 mg before bedtime (maximum dose: 3 mg). Concurrent use with strong CYP3A4 inhibitor: 1 mg before bedtime; if needed, dose may be increased to 2 mg.

Dosage adjustment in hepatic impairment:
Mild-to-moderate: Use with caution; dosage adjustment unnecessary
Severe: Maximum dose: 2 mg

Supplied
: 1 mg, 2 mg, 3 mg tablet.

Flurazepam (dalmane ®) 

Long half-life
Dosing (Adults):
Short-term treatment of insomnia: 15-30 mg at bedtime

Elderly: Insomnia: Oral: 15 mg at bedtime; avoid use if possible

SUPPLIED:
Capsule, as hydrochloride: 15 mg, 30 mg

Lorazepam (ativan ®) 

Intermediate half-life
Prolonged infusions have been associated with toxicity from propylene glycol and/or polyethylene glycol.

IV: Do not exceed 2 mg/minute
Dosing (Adults):
Anxiety/sedation: 1-10 mg orally in 2-3 divided doses. Usual dose: 2-6 mg/day in divided doses. Initial dose should not exceed 2 mg in debilitated patients.
Insomnia: 2-4 mg orally at bedtime.
Operative amnesia: I.V.: Up to 0.05 mg/kg; maximum: 4 mg/dose.
Status epilepticus: 4 mg IV over 2 to 5 minutes. May repeat in 10-15 minutes.
Usual maximum dose: 8 mg.

Agitation in the ICU patient --------------
Continuous infusion
:
1 to 10 mg/hr (0.01 to 0.1 mg/kg/hour).
Intermittent:
I.V.: 0.02-0.06 mg/kg every 2-6 hours

PHARMACODYNAMICS / KINETICS
Onset of action:
Hypnosis: I.M.: 20-30 minutes
Sedation: I.V.: 5-20 minutes
Anticonvulsant: I.V.: 5 minutes, oral: 30-60 minutes.
Severe Hyperosmolar Metabolic Acidosis Due to a Large Dose of Intravenous Lorazepam.
----
Previous cases of propylene glycol toxicity secondary to high-dose lorazepam infusion have occurred in patients with compromised renal function. Our patient's renal function remained stable throughout the hospital course, which caused us to look further for an explanation for the propylene glycol-induced lactic acidosis. Based on the Naranjo probability scale, propylene glycol was determined to be the probable cause of lactic acidosis. Since this case occurred, our intensive care unit has instituted recommendations for the prevention of lorazepam-associated propylene glycol toxicity.
CONCLUSIONS: Our case highlights the development of propylene glycol-induced lactic acidosis secondary to high-dose lorazepam infusion not associated with renal dysfunction.
----
The lorazepam solvents polyethylene glycol (PEG) and propylene glycol (PG) have been implicated as the cause of reversible acute tubular necrosis, lactic acidosis, and hyperosmolar states after prolonged high-dose infusions. The dosing threshold for this effect has not been prospectively defined, but these case reports described doses that exceeded 18 mg/hr and continued for longer than four weeks and higher doses (>25 mg/hr) continuing for hours to days. It seems prudent to avoid doses of this magnitude. Alternatively, lorazepam and diazepam may be administered via the enteral route in tablet or liquid form. Large doses of liquid lorazepam (i.e., 60 mg of 2 mg/mL every six hours) may lead to diarrhea because of the high PEG and PG content.

Midazolam  (versed ®)

Intermediate half-life
Intubated patients (Continuous infusion): 1 to 7 mg/hr.
Dosing (Adults)
Preoperative sedation:
I.M.: 0.07-0.08 mg/kg 30-60 minutes prior to surgery/procedure; usual dose: 5 mg; Note: Reduce dose in patients with COPD, high-risk patients, patients >/= 60 years of age, and patients receiving other narcotics or CNS depressants
I.V.: 0.02-0.04 mg/kg; repeat every 5 minutes as needed to desired effect or up to 0.1-0.2 mg/kg

Conscious sedation: I.V.: Initial: 0.5-2 mg slow I.V. over at least 2 minutes; slowly titrate to effect by repeating doses every 2-3 minutes if needed; usual total dose: 2.5-5 mg; use decreased doses in elderly. Healthy Adults <60 years: Initial: Some patients respond to doses as low as 1 mg; no more than 2.5 mg should be administered over a period of 2 minutes. Additional doses of midazolam may be administered after a 2-minute waiting period and evaluation of sedation after each dose increment. A total dose >5 mg is generally not needed. Maintenance: 25% of dose used to reach sedative effect.

Anesthesia: I.V.: Induction: Unpremedicated patients: 0.3-0.35 mg/kg (up to 0.6 mg/kg in resistant cases)
Premedicated patients: 0.15 to 0.35 mg/kg.
Maintenance: 0.05-0.3 mg/kg as needed, or continuous infusion 0.25-1.5 mcg/kg/minute.

Sedation in mechanically-ventilated patients: I.V. continuous infusion: 100 mg in 250 mL D5W or NS (if patient is fluid-restricted, may concentrate up to a maximum of 0.5 mg/mL); initial dose: 0.02-0.08 mg/kg (~1 mg to 5 mg in 70 kg adult) initially and either repeated at 5-15 minute intervals until adequate sedation is achieved or continuous infusion rates of 0.04-0.2 mg/kg/hour and titrate to reach desired level of sedation.

DOSING: ELDERLY — The dose of midazolam needs to be individualized based on the patient's age, underlying diseases, and concurrent medications. Decrease dose (by ~30%) if narcotics or other CNS depressants are administered concomitantly. I.V.: Conscious sedation: Initial: 0.5 mg slow I.V.; give no more than 1.5 mg in a 2-minute period. If additional titration is needed, give no more than 1 mg over 2 minutes, waiting another 2 or more minutes to evaluate sedative effect. A total dose >3.5 mg is rarely necessary.

Supplied: Injection, solution: 1 mg/mL (2 mL, 5 mL, 10 mL); 5 mg/mL (1 mL, 2 mL, 5 mL, 10 mL)

PHARMACODYNAMICS / KINETICS
Onset of action: I.M.: Sedation: ~15 minutes; I.V.: 1-5 min.
Peak effect: I.M.: 0.5-1 hour.
Duration: I.M.: Up to 6 hours; Mean: 2 hours.
Half-life elimination: 1-4 hours; prolonged with cirrhosis, congestive heart failure, obesity, and elderly.

Oxazepam (serax ®)

Short half-life
Dosing (Adults)
Anxiety: 10-30 mg 3-4 times/day

Ethanol withdrawal: 15-30 mg 3-4 times/day

Hypnotic: 15-30 mg

Elderly: Oral: Anxiety: 10 mg 2-3 times/day; increase gradually as needed to a total of 30-45 mg/day. Dose titration should be slow to evaluate sensitivity.

SUPPLIED:
Capsule: 10 mg, 15 mg, 30 mg
Tablet: 15 mg

Ramelteon (rozerem ® ) 

Non-Benzodiazepine (Sedative)
Melatonin receptor agonist.
Dosing (Adults)
Insomnia
:

  • Adult dose: 8 mg taken within 30 minutes of going to bed.
  • Should not be taken with or immediately after a high-fat meal.
  • Total daily dose should not exceed 8 mg.

WARNINGS AND PRECAUTIONS:

  • Severe anaphylactic/anaphylactoid reactions: Angioedema and anaphylaxis have been reported. Do not rechallenge if such reactions occur.
  • Need to evaluate for co-morbid diagnoses: Reevaluate if insomnia persists after 7 to 10 days of treatment.
  • Abnormal thinking, behavioral changes, complex behaviors: May include "sleep-driving" and hallucinations. Immediately evaluate any new onset behavioral changes.
  • Depression: Worsening of depression or suicidal thinking may occur.
  • CNS effects: Potential impairment of activities requiring complete mental alertness such as operating machinery or driving a motor vehicle, after ingesting the drug.
  • Reproductive effects: Include decreased testosterone and increased prolactin levels. Effect on reproductive axis in developing humans is unknown.
  • Patients with severe sleep apnea: Rozerem is not recommended for use in this population.

Supplied: 8 mg tablet.

Silenor® (doxepin)

Mechanism of Action
Doxepin binds with high affinity to the histamine H1 receptor (Ki < 1 nM) where it functions as an antagonist. The exact mechanism by which doxepin exerts its sleep maintenance effect is unknown but is believed due to its antagonism of the H1 receptor.

INDICATIONS AND USAGE
Silenor is indicated for the treatment of insomnia characterized by difficulty with sleep maintenance. The clinical trials performed in support of efficacy were up to 3 months in duration.

DOSAGE AND ADMINISTRATION
The dose of Silenor should be individualized.

Dosing in Adults
The recommended dose of Silenor for adults is 6 mg once daily. A 3 mg once daily dose may be appropriate for some patients, if clinically indicated.

Dosing in the Elderly
The recommended starting dose of Silenor in elderly patients (≥ 65 years old) is 3 mg once daily. The daily dose can be increased to 6 mg, if clinically indicated.

Administration
Silenor should be taken within 30 minutes of bedtime.

To minimize the potential for next day effects, Silenor should not be taken within 3 hours of a meal.

The total Silenor dose should not exceed 6 mg per day.

DOSAGE FORMS AND STRENGTHS
Silenor is an immediate-release, oval-shaped, tablet for oral administration available in strengths of 3 mg and 6 mg. The tablets are blue (3 mg) or green (6 mg) and are debossed with 3 or 6, respectively, on one side and SP on the other. Silenor tablets are not scored.

Temazepam (restoril ®)

Intermediate half-life
INDICATIONS AND USAGE
Restoril™ (temazepam) is indicated for the short-term treatment of insomnia (generally 7 to 10 days).

For patients with short-term insomnia, instructions in the prescription should indicate that Restoril™ (temazepam) should be used for short periods of time (7 to 10 days).

The clinical trials performed in support of efficacy were 2 weeks in duration with the final formal assessment of sleep latency performed at the end of treatment.

DOSAGE AND ADMINISTRATION
While the recommended usual adult dose is 15 mg before retiring, 7.5 mg may be sufficient for some patients, and others may need 30 mg. In transient insomnia, a 7.5 mg dose may be sufficient to improve sleep latency. In elderly or debilitated patients, it is recommended that therapy be initiated with 7.5 mg until individual responses are determined.

SUPPLIED:
Restoril®: 7.5 mg, 15 mg, 22.5mg, 30 mg

Triazolam (halcion ®)

Short half-life
Dosing (Adults)
Short-term treatment of insomnia
0.125-0.25 mg at bedtime (maximum dose: 0.5 mg/day)

Preprocedure sedation (dental): 0.25 mg taken the evening before oral surgery; or 0.25 mg 1 hour before procedure

Elderly: Insomnia (short-term use): 0.0625-0.125 mg at bedtime; maximum dose: 0.25 mg/day

SUPPLIED:
Tablet: 0.125 mg, 0.25 mg

Zaleplon (sonata ® )

Non-Benzodiazepine (Sedative)
INDICATIONS AND USAGE
Sonata is indicated for the short-term treatment of insomnia. Sonata has been shown to decrease the time to sleep onset for up to 30 days in controlled clinical studies. It has not been shown to increase total sleep time or decrease the number of awakenings.

The clinical trials performed in support of efficacy ranged from a single night to 5 weeks in duration. The final formal assessments of sleep latency were performed at the end of treatment.

CONTRAINDICATIONS
Hypersensitivity to zaleplon or any excipients in the formulation 

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DOSAGE AND ADMINISTRATION
--------------------------------------------------
The dose of Sonata should be individualized. The recommended dose of Sonata for most nonelderly adults is 10 mg. For certain low weight individuals, 5 mg may be a sufficient dose. Although the risk of certain adverse events associated with the use of Sonata appears to be dose dependent, the 20 mg dose has been shown to be adequately tolerated and may be considered for the occasional patient who does not benefit from a trial of a lower dose. Doses above 20 mg have not been adequately evaluated and are not recommended.

Sonata should be taken immediately before bedtime or after the patient has gone to bed and has experienced difficulty falling asleep (see package insert -PRECAUTIONS.). Taking Sonata with or immediately after a heavy, high-fat meal results in slower absorption and would be expected to reduce the effect of Sonata on sleep latency.
-----------------------------
Special Populations
Elderly patients and debilitated patients appear to be more sensitive to the effects of hypnotics, and respond to 5 mg of Sonata. The recommended dose for these patients is therefore 5 mg. Doses over 10 mg are not recommended.

Hepatic insufficiency: Patients with mild to moderate hepatic impairment should be treated with Sonata 5 mg because clearance is reduced in this population. Sonata is not recommended for use in patients with severe hepatic impairment.

Renal insufficiency: No dose adjustment is necessary in patients with mild to moderate renal impairment. Sonata has not been adequately studied in patients with severe renal impairment.

An initial dose of 5 mg should be given to patients concomitantly taking cimetidine because zaleplon clearance is reduced in this population

SUPPLIED:
Capsule: 5 mg, 10 mg

Zolpidem (ambien ®)

Non-Benzodiazepine (Sedative)
 INDICATIONS AND USAGE
Ambien, a gamma-aminobutyric acid (GABA) A agonist, is indicated for the short-term treatment of insomnia characterized by difficulties with sleep initiation. Ambien has been shown to decrease sleep latency for up to 35 days in controlled clinical studies.

DOSAGE AND ADMINISTRATION:

  • Use the lowest dose effective for the patient
  • Recommended initial dose is 5 mg for women and 5 or 10 mg for men, immediately before bedtime with at least 7-8 hours remaining before the planned time of awakening
  • Geriatric patients and patients with hepatic impairment: Recommended dose is 5 mg for men and women
  • Lower doses of CNS depressants may be necessary when taken concomitantly with Ambien
  • The effect of Ambien may be slowed if taken with or immediately after a meal

Dosing adjustment in hepatic impairment: Decrease dose to 5 mg

WARNINGS AND PRECAUTIONS:

  • CNS depressant effects: Impairs alertness and motor coordination. Instruct patients on correct use.
  • Need to evaluate for co-morbid diagnosis: Reevaluate if insomnia persists after 7 to 10 days of use.
  • Severe anaphylactic/anaphylactoid reactions: Angioedema and anaphylaxis have been reported. Do not rechallenge if such reactions occur.
  • "Sleep-driving" and other complex behaviors while not fully awake. Risk increases with dose and use with other CNS depressants and alcohol. Immediately evaluate any new onset behavioral changes.
  • Depression: Worsening of depression or suicidal thinking may occur. Prescribe the least amount of tablets feasible to avoid intentional overdose.
  • Respiratory Depression: Consider this risk before prescribing in patients with compromised respiratory function
  • WWithdrawal effects: Symptoms may occur with rapid dose reduction or discontinuation

SUPPLIED:
Tablet, as tartrate: 5 mg, 10 mg

Suvorexant - belsomra ® () 

Drug UPDATES
BELSOMRA ® (suvorexant) tablets, for oral use, C-IV
[Drug information  /  PDF]  
Dosing:  Click (+) next to Dosage and Administration section (drug info link)

Initial U.S. Approval:  2014

Mechanism of Action: The mechanism by which suvorexant exerts its therapeutic effect in insomnia is presumed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system is a central promoter of wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R is thought to suppress wake drive.

Antagonism of orexin receptors may also underlie potential adverse effects such as signs of narcolepsy/cataplexy. Genetic mutations in the orexin system in animals result in hereditary narcolepsy; loss of orexin neurons has been reported in humans with narcolepsy.

INDICATIONS AND USAGE:  BELSOMRA is an orexin receptor antagonist indicated for the treatment of insomnia, characterized by difficulties with sleep onset and/or sleep maintenance

HOW SUPPLIED: Tablets, 5 mg, 10 mg, 15 mg, 20 mg

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates.  A local search option of this data can be found here.

Benzodiazepines

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