Loprazolam

Registered South African indications:

• Sleep disturbances

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Severe respiratory insufficiency
• Myasthenia gravis
• Phobic states
• Obsessive-compulsive disorder
• Sleep apnoea
• Monotherapy in depression 
• Anxiety associated with depression and psychosis
• Acute pulmonary insufficiency
• Coadministration with alcohol

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly
• Personality disorders
• Abrupt withdrawal
• Prolonged use
• Substance abuse
• Chronic respiratory insufficiency
• Cerebrovascular disease
• Suicide ideation and suicide attempt
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: tab

Insomnia
Sleep disturbances - elderly and pre-operative patients

• Oral (tab): 1-2mg, dly at night; Max duration: 4 weeks

Only indicated when the disorder is severe, disabling or subjecting the individual to extreme distress

Discontinue by down-titrating gradually

Not established for use in children

Pregnancy

• Caution
• If loprazolam is prescribed to a woman of childbearing potential, she should be warned to contact her physician regarding discontinuance of the product if she intends to become or suspects that she is pregnant
• If, for compelling medical reasons, the product is administered during the late phase of pregnancy, or during labour at high doses, effects on the neonate, such as hypothermia, hypotonia and moderate respiratory depression can be expected due to the pharmacological action of loprazolam
• Moreover, infants born to mothers who took benzodiazepines chronically during the latter stages of pregnancy may have developed physical dependency and may be at some risk for developing withdrawal symptoms in the postnatal period

Breastfeeding

• Caution; not recommended
• Since benzodiazepines are found in the breast milk, they should not be given to breastfeeding mothers

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly 

• Caution; dose adjustment recommended
  Dosage should not exceed 1mg daily (at bedtime)

Porphyria Information

• Probably not porphyrinogenic (PNP) 

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Headache
• Dizziness
• Ataxia
• Paradoxical aggression
• Excitement
• Confusion
• Suicidal tendencies
• Tolerance
• Dependence
• Hypotonia
• Anterograde amnesia

Cardiovascular Disorders

• Hypotension

Gastrointestinal Disorders

• Nausea and vomiting

Hepatobiliary Disorders

• Jaundice

Genitourinary Disorders

• Urinary retention

Endocrine and Metabolic Disorders

• Change in libido

Immune, Blood and Lymphatic System Disorders

• Blood dyscrasia

Sensory Disorders

• Speech disorders
• Blurred vision

• Central nervous systems depressants
• Muscle relaxants
• Cisapride
• Antipsychotics
• Sedative hypnotics
• Anxiolytics and sedatives
• Antidepressants
• Narcotic analgesics
• Anti-epileptics
• Anaesthetics
• Sedative antihistamines

None routine

Benzodiazepines should be used to treat insomnia only when it is severe, disabling or subjecting the individual to extreme distress. An underlying cause of insomnia should be sought before deciding upon the use of benzodiazepines for symptomatic relief

Loprazolam, a benzodiazepine, has a widespread action as a result of it's enhancing the release of gamma-aminobutyric acid (GABA), which is a major inhibitory neurotransmitter. Benzodiazepines increase GABA activity and therefore produce a calming effect, relaxing muscles and inducing sleep.

Tablet 2mg

• Dormonoct (Sanofi) originator