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Sleep disorders: Medications summary

Table 12.1: Pharmacotherapies for sleep disorders

 

class name

(trade name)

 

half life, dose

and range

positives negatives

Benzodiazepine

     

Temazepam

(Restoril)

5 – 20 hours

 

15 and  30 mg

 

Maximum/

24 hours: 60 mg

• Initial insomnia

• Less hang- over effect

Withdrawals

• Addiction and dependence

• Tolerance

• Pregnancy and breastfeeding

• Elderly

Lorazepam

(Ativan)

10 – 20 hours

0.5, 1.0 and

2.0 mg

 

Maximum/

24 hours: 4 mg

• Insomnia

• Anxiety

• Safe in liver disease

• Withdrawal

• Addiction and dependence

• Tolerance

• Pregnancy and breast-feeding

• Elderly

Oxazepam

(Serax)

5 – 15 hours

10, 15 and  30 mg

 

Maximum/

24 hours: 30 mg)

• Anxiety

• Alcohol withdrawal

• Safe in liver disease

• Withdrawal

• Addiction and dependence

• Tolerance

• Pregnancy and breast-feeding

• Elderly
  Drug Interaction Best used for Side-effects
 

• CNS

depressants

• Insomnia

• Muscle relaxant

• Behaviour changes

• Confusion

• Irritability

• Balance issues

• Drowsiness

• Increased nervousness

• Mood changes

• Worsening of sleep apnea

• Withdrawal

• Seizure

• Headache

• REM suppression
 

• CNS

depressants

• Divalproex

• Phenytoin

• Theophylline

• Co-administra- tion of IM ben- zodiazepine and IM olanzapine

• Anxiety disorder

• Seizure disorder

• Insomnia

• Anterograde amnesia

• Confusion

• Behavioural changes

• Irritability

• Increased nervousness

• Mood changes

• Withdrawal, seizure

• Headaches

• Balance and fall issues
 

• CNS

depressants

• Co-adminstra- tion of IM ben- zodiazepine and IM olanzapine

• Phenytoin

• Theophylline

• Anxiety

• Alcohol withdrawal

• Anterograde amnesia

• Confusion

• Behavioural changes

• Irritability

• Increased nervousness

• Mood changes

• Withdrawal, seizure

• Headaches

• Balance and fall issues
Class Name (Trade Name) Half life, dose and range Positives Negatives

Alprazolam

(Xanax)

6 – 12 hours

 

0.25 mg, 0.5 mg,

2 mg

 

Maximum/

24 hours: 6 mg

• Helpful

for anxiety attacks

• Withdrawals

• Addiction and dependence

• Tolerance

• Pregnancy and breastfeeding

• Elderly

Clonazepam

(Rivotril)

18 – 50 hours

 

0.5 mg and 2 mg

 

Maximum/

24 hours: 4 mg

• Insomnia

• Anxiety

• Restless legs syn- drome

• Withdrawals

• Addiction and dependence

• Tolerance

• Pregnancy and breastfeeding.

• Narrow angle glaucoma

• Liver disease

• Kidney disease

• Sensitivity to diazepam

• Elderly

Diazepam

(Valium)

20 – 100 hours

 

5 mg, 10 mg

 

Maximum/

24 hours: 40 mg

• Status epilepticus

• Alcohol withdrawal

• Sedation for certain procedures such as en- doscopies

• Fewer withdrawal effects

• Addiction and dependence

• Tolerance

• Pregnancy and breastfeeding

• Narrow angle glaucoma

• Liver disease

• Kidney disease

• Elderly

• Respiratory disease

• Overdose

• Coma
  Drug Interaction Best used for  Side-effects
 

• CNS

depressants

• Imipramine and

Desipramine

• CYP3A inhibitors and inducers

• Generalized anxiety disorder

• Panic attacks

• Muscle relaxant

• Depression

• PTSD

• Short acting

• Behaviour changes

• Confusion

• Irritability

• Balance issues, falls

• Drowsiness

• Increased nervousness

• Mood changes

• Worsening of sleep apnea

• Withdrawals, seizure

• Headache
 

• CNS depres- sants

• Opioids

• Antihistamine

• Disulfiram

• Phenobarbital

• Phenytoin

• Carbamazepine

• Theophylline

• Rifampicin

• Insomnia

• Periodic limb move- ments

• Status epileptics

• Anxiety disorder

• Fatigue

• Sexual dysfunction

• Behaviour changes

• Confusion, irritability

• Balance issues

• Drowsiness

• Increased nervousness

• Mood changes

• Worsening of sleep apnea

• Withdrawals, seizure

• Headache

• REM suppression
 

• Barbiturates

• Phenothiazines

• Narcotics

• Antidepressants

• Agents that have an effect on he- patic cytochrome P450

• Status epilepticus

• Alcohol withdrawal

• Eclampsia

• Anxiety

• Panic attack

• Agitation

• Muscle relaxant

• Sedation for preoperative reasons

• Insomnia

• Slow elimination

• Behaviour changes, confusion

• Irritability

• Balance issues

• Drowsiness

• Increased nervousness

• Mood changes

• Worsening of sleep apnea

• Withdrawals, seizure

• Headache

• REM suppression

class name

(trade name)
half life, dose and range positives

negatives

Bromazepam

(Lectopam)

10 – 20 hours

 

1 mg, 3 mg, 6 mg

 

Maximum/

24 hours: 6 – 9 mg

• Initial insomnia

• Withdrawals

• Addiction and dependence

• Tolerance

• Pregnancy and breastfeeding

• Narrow angle glaucoma

• Liver disease

• Kidney disease

• Sensitivity to diazepam

• Elderly

• Overdose

Cannabanoid

     

Nabilone

(Cesamet)

2 – 35 hours

 

0.5 mg

 

Maximum/

24 hours:  1 mg

• Antiemetic

• Neuro- pathic pain

• Liver disease

• Hypertension

• Heart disease

• Mania

• Schizophrenia

• Allergy to compound

• Addiction

• Pregnancy

• Elderly

• Breastfeeding

• Overdose

  Drug interaction Best used for Side-effects
 

• Fluvoxamine

• Cimetidine

• Propranolol

• Anxiolytic

• Hypnotic at a high dose

• Behaviour changes

• Confusion, irritability

• Balance issues

• Drowsiness

• Increased nervousness

• Mood changes

• Withdrawals, seizure

• Headache

 

•  Anticholinergic

• Naltrexone

• Theophylline

• Antihistamine

• Barbiturate

• Benzodiazapine

• Carbamazepine

• Codeine

• Zolpidem

• Chlorpromazine

• Risperidone

• Trazodone

• Cough medica- tions

• Neuropathic pain

• Fibromyalgia

• Movement disorders

• Antiemetic for cancer chemotherapy

• Chronic pain

• Dizziness

• Dryness of mouth

• Euphoria

• Headache

• Sleep disturbance

• Memory problems

• Mood changes

• Confusion

class name

(trade name)

half life, dose and range positives 

negatives

Sedating antidepressant

     

Mirtazapine

(Remeron)

20 – 40 hours

 

15 mg, 30 mg

 

Maximum/

24 hours: up to

60 – 120 mg

• Sedating; promotes slow wave sleep

• Antidepres- sant

• Anxiolytic
• Weight gain

Clomipramine

(Anafranil)

21 hours

25 mg or 75 mg SR Maximum/

24 hours: 300 mg

• No addiction

• Sedation

• Withdrawals

• Pregnancy

• Breastfeeding

• Overdose

• Closed angle glaucoma

• Seizures

• Cardiovascular (premature ventricular contractions, ST changes)

• Blood pressure change

Trazodone

(Desryel)

5 – 9 hours

 

25 mg, 50 mg

 

Maximum/

24 hours: 600 mg

• Anxiolytic and hyp- notic, less prominent anticho- linergic and sexual

side-effects

• Pregnancy

• Lactation

• Overdose
  Drug interaction Best used for Side-effects
 

• Alcohol

• Barbiturates

• Carbamazepine

• Cimetidine

• Erythromycin

• Warfarin

• Depression

• Insomnia

• Anxiety disorders

• Dizziness

• Dryness of mouth

• Euphoria

• Headache

• Somnolence

• Weight gain

• Increased libido

• Constipation

• Vivid dreams
 

• MAO inhibitors

• CNS stimulants

• SSRI

• Tranquilizers

• Narcotics

• Alcohol

• Antihypertensive

• Cold medica- tions

• St. John's wort

• Obsessive- compulsive disorder

• Depression

• Panic disorder

• Narcolepsy

(cataplexy)

• Insomnia

• Premature ejaculation

• Depersonalization

• Panic disorder

• Enuresis

• Chronic pain

• Reduce relapse in cocaine addiction

• Dizziness

• Dryness of mouth

• Euphoria

• Headache

• Somnolence

• Weight gain

• Increased libido

• Constipation

• Vivid dreams

• Agitation, increased anxiety

• Anticholinergic

• Antiadrenergic side-effects

• Sexual problems

• Hypersensitivity reaction
 

• CYP3A4 inhibitors

• CNS depressant

• Depression, bipolar disorder

• Fibromyalgia

• Sleep disturbance

• Panic disorder

• Diabetic neuropathy

• Complex pain syn- drome

• Alcohol withdrawal

• Eating disorder

• Fatigue

• Lethargy, psychomotor retardation

• Confusion

• Memory loss

• Priapism

• Tremors

• Headache

• Hypertension

• Tachycardia, bradycardia, palpitation

• Nausea, vomiting

• Hypersensitivity reaction

class name

(trade name)

half life, dose and range positives  negatives

Melatonin receptor agonist

     
Ramelteon

0.8 – 2.6 hours

Maximum/

24 hours: 8 mg

• Initial insomnia

• Hypersensitivity to remelteon or any of its product ingredients

• Caution with he- patic impairment

Tryptophan

     

Tryptophan

(Tryptan)

2 – 6 hours

 

5 and 10 mg,

6.25 and 12.5 mg extended release

 

• Initial insomnia

• Less rebound insomnia

• Less risk of depen- dence

• Not available in

Canada

Z drugs

     

Zolpidem (Ambien, Ambien CR, Stilnox)

2 – 6 hours

 

5 and 10 mg,

6.25 and 12.5 mg extended release

 

• Initial insomnia

• Less rebound insomnia

• Less risk of depen- dence

 

Zopiclone

(Imovane)

3.5 – 6.5 hours

 

7.5 mg, 5 mg

 

Maximum/

24 hours: 15 mg

• Does not disrupt sleep archi- tecture

• Initial and middle insomnia

• Less addictive

• Taste side-effect

• Addiction and withdrawal

• Rebound insomnia

• Abuse

• Seizures

  Drug interaction Best used for Side-effects
  • Fluvoxamine • Sleep onset insomnia

• Headache

• Somnolence

• Fatigue

• Nausea

• Dizziness

• Insomnia

 

• Vitamin B6

• Citalopram

• Insomnia

• Pain syndrome

• Nausea

• Vomiting

• Headache

• Palpitation

• Agitation

 

• Chropromazine

• Fluconazole

• Imipramine

• Rifampacin

• Carbamazepine

• Phenytoin

• Initial insomnia

• Nausea, vomiting

• Headache

• Palpitation

• Agitation

• Anterograde amnesia, delusions

• Impaired judgement and reasoning

 

•Carbamazepine

• Phenytoin

• Erythromycin

• Rifampicin

• Ketoconozole

• Imipramine

• Initial, middle and late insomnia

• Gustatory side-effect

• Somnolence

• Confusion, memory impairment

• Headache, dizziness, fatigue

• Mood changes

• Nausea

class name

(trade name)

half life, dose and range positives 

negatives

Zaleplon

(Starnoc)

1 – 4 hours

 

10 mg

 

• Mainte- nance insomnia

• Less risk of depen- dence

• Rebound insomnia

• No hang- over

• Short acting

• Abuse

• Not routinely available in Canada

Melatonin

     
Melatonin

Unknown

2 mg, 3 mg

Maximum/

24 hours: 3-6 mg

• Phase delay syndrome

• Circadian rhythm disorder

• Shift work

• None

Antihistamine

     

Diphenhydramine

(Benadryl)

Short

 

25 mg, 50 mg

 

Maximum/

24 hours: 50 mg

• Sedative

• Anti-allergy

• Addiction

• To be used with caution

in children and in patients with lung disease

• Blood pressure

• Narrow angle glaucoma

• Heart disease

• Asthma

  Drug interaction Best used for Side-effects
 

• Cimetidine

• Rifampicin

• Thioridazine

• Middle of night insomnia

• Confusion

• Drowsiness, dizziness

• Headache

• Nausea, vomiting

• Tremors

• Memory problem

  • Unknown • Circadian rhythm disorder

• Drowsiness

• Fatigue

 

• Alcohol

• Anticholinergic

• Narcotics

• Tranquilizers

• Antipsychotic

• Anti-allergy

• Cough medication

• Drowsiness

• Confusion

• Dry mouth

• Appetite changes

• Headache

• Restlessness

class name

(trade name)

half life, dose and range positives  negatives

Chloral hydrate

     
Chloral hydrate

4 – 12 hours

Adults: 500 to

1 000 mg, 15 to

30 minutes before bedtime. Geriatrics: Initial

250 mg, 15 to

30 minutes before bedtime. 

Children: 50 mg/kg at bedtime,

maxi- mum 1 000 mg

per single dose

• Short-term treatment of insom- nia

• Sedative prior to EEG does not sup- press epi- leptiform discharges

• No REM

rebound

• Alcohol withdrawal

• Suppresses respiration and blood pressure

• Kidney disease

• Liver disease

• Heart and stom- ach problems

• Pregnancy, breastfeeding

• Asthma

• Overdose

• Abuse

• Withdrawal

Antipsychotic

     

Quetiapine

(Seroquel)

6 hours

 

25 mg, 50 mg,

100 mg

 

Maximum/

24 hours:

25 – 100 mg for insomnia

• Peak plasma level 1.5 hours, fast acting

• Morning sedation

• Acts at multiple receptors (adrenergic, muscarinic, serotonergic, dopaminergic)

• Not many studies done for insomnia

  Drug interaction Best used for Side-effects
 

• Anticoagulant

• Antihistamine

• Furosemide

(Lasix)

• Seizure medication

• Antidepressant

• Sleeping pills

• Short-term insomnia

• Prior to dental surgery

• Alcohol withdrawal

• Drowsiness

• Upset stomach, vomiting, diarrhea

 

 Drug interaction related to en- zyme induction and inhibition

• Antipsychotic

• Mood stabilizer

• Agitation

• Weight gain

• Metabolic side-effects

• Tardive dyskinesia

• Drowsiness, confusion

• Dry mouth

• Appetite changes

• Headache

• Restlessness

class name

(trade name)
half life, dose and range positives  negatives

Olanzapine

(Zyprexa)

20 – 50 hours

 

2.5 mg, 5 mg,

10 mg

 

Maximu/

24 hours: 15 mg for insomnia

• Sedating

• Hangover in the morning

• Metabolic side-effects

• Acts at multiple receptors (adren- ergic, muscarinic

serotonergic, dopaminergic)

• Not many studies done for insomnia

  Drug interaction Best used for Side-effects
 

• Drug interaction related to en- zyme induction and inhibition

• Antipsychotic

• Mood stabilizer

• Sedation

• Weight gain

• Metabolic side-effects more than Seroquel

• Drowsiness

• Confusion

• Dry mouth

• Appetite changes

• Headache

• Restlessness