Lormetazepam

Registered South African indications:

• Insomnia

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Severe hepatic impairment
• Severe respiratory insufficiency
• Sleep apnoea syndrome
• Myasthenia gravis

Cautions 

• Pregnancy
• Breastfeeding
• Renal impairment
• Mild to moderate hepatic impairment
• Elderly
• Porphyria
• Children
• Debilitated patients
• Chronic respiratory insufficiency
• Patients in whom a drop in blood pressure might lead to cardiovascular or cerebrovascular complications
• Primary treatment of psychotic illness or depressive disorders
• Monotherapy for depressed patients with associated insomnia
• Depression
• Suicidal tendencies
• High doses
• Prolonged treatment
• Abrupt withdrawal
• Acute narrow-angle glaucoma
• History of alcoholism or drug abuse
• Alcohol intake
• Significant personality disorders
• Pre-existing seizure disorder
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption
• May impair ability to drive and operate machinery

Forms avail in SA and covered in this monograph: cap, tab

Insomnia
- Short term treatment when insomnia is disabling or subjecting the individual to extreme distress

• Oral (tab): 0.5-1.5mg, at bedtime; Max treatment duration: 4 weeks

---

Patients should ensure that they will be able to have a period of uninterrupted sleep (7-8 hours) to allow dissipation of drug effect and minimize the risk of anterograde amnesia

---

Dosage and duration of therapy should be individualised; the lowest effective dose should be prescribed for the shortest time possible

---

Treatment should be withdrawn gradually to minimise possible withdrawal symptoms

---

Extension of treatment should not occur without re-evaluation of the need for continued therapy

---

Dose reduction should be considered in chronic respiratory insufficiency or hepatic impairment

Not established for use in children

Pregnancy

• Caution; positive evidence of risk
• Benzodiazepines should not be used during pregnancy, especially during the first and last trimesters
• Benzodiazepines may cause foetal damage when administered to pregnant women. If the medicinal product is prescribed to a woman of childbearing potential, she should be warned to contact her physician about stopping the drug if she intends to become, or suspects that she is, pregnant
• There is a possibility that infants born to mothers who take benzodiazepines chronically during the later stages of pregnancy may develop physical dependence. Infants of mothers who ingested benzodiazepines for several weeks or more preceding delivery have been reported to have withdrawal symptoms during the postnatal period. Symptoms such as hypoactivity, hypotonia, hypothermia, respiratory depression, apnoea, feeding problems, and impaired metabolic response to cold stress have been reported in neonates born of mothers who have received benzodiazepines during the late phase of pregnancy or at delivery

Breastfeeding

• Caution; not recommended
• Since limited data indicates that a small proportion of parent drug and its conjugate is excreted in breast milk, lormetazepam should not be given to breastfeeding women
• Sedation and inability to suckle have occurred in neonates of breastfeeding mothers taking benzodiazepines

Renal Impairment 

• Caution; no dose adjustment recommended
  Monitor frequently and adjust dosage carefully if necessary according to patient response. Lower doses may be sufficient in these patients

Hepatic Impairment 

• Mild to moderate: Caution; no dose adjustment recommended 
  Monitor frequently and adjust dosage carefully according to patient response. A dose reduction should be considered
• Severe: Contraindicated

Elderly

• Caution; dose adjustment recommended 
  The lower adult dose of 0.5mg is preferable for elderly patients. Since benzodiazepines may be associated with an increased risk of falling, caution should be exercised particularly when getting up at night

Porphyria Information

• Not yet classified (NC)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Daytime drowsiness
• Dizziness
• Ataxia
• Confusion
• Depression
• Unmasking of depression
• Numbed emotions
• Disinhibition
• Euphoria
• Appetite changes
• Sleep disturbance
• Change in libido
• Decreased orgasm
• Dependence
• Suicidal ideation/attempt
• Restlessness
• Agitation
• Irritability
• Aggressiveness
• Delusion
• Rage
• Insomnia
• Nightmares
• Hallucinations
• Psychosis
• Sexual arousal
• Inappropriate behaviour
• Sedation
• Headache
• Decreased alertness
• Dysarthria/slurred speech
• Transient anterograde amnesia or memory impairment
• Tremor
• Extrapyramidal reactions
• Coma
• Asthenia
• Drug withdrawal symptoms
  - Headaches
  - Muscle pain
  - Anxiety
  - Tension
  - Depression
  - Insomnia
  - Restlessness
  - Confusion
  - Irritability
  - Sweating
  - "Rebound" phenomena
  - Derealisation
  - Depersonalisation
  - Hyperacusis
  - Tinnitus
  - Numbness and tingling of the extremities
  - Hypersensitivity to light, noise, and physical contact
  - Involuntary movements
  - Hyperreflexia
  - Tremor
  - Nausea and vomiting
  - Diarrhoea
  - Abdominal cramps
  - Loss of appetite
  - Agitation
  - Palpitations
  - Tachycardia
  - Panic attacks
  - Vertigo
  - Short-term memory loss
  - Hallucinations/delirium
  - Catatonia
  - Hyperthermia
  - Seizures

Cardiovascular Disorders

• Hypotension

Respiratory Disorders

• Apnoea
• Worsening of sleep apnoea
• Worsening of obstructive pulmonary disease
• Respiratory depression

Gastrointestinal Disorders

• Nausea
• Constipation
• Salivation changes

Hepatobiliary Disorders

• Increased bilirubin
• Increased transaminases
• Increased alkaline phosphatase
• Jaundice

Genitourinary Disorders

• Impotence

Endocrine and Metabolic Disorders

• Inappropriate antidiuretic hormone secretion
• Hyponatraemia
• Hypothermia

Musculoskeletal Disorders

• Muscle weakness

Skin and Subcutaneous Tissue Disorders

• Rash
• Allergic dermatitis

Immune, Blood and Lymphatic System Disorders

• Thrombocytopenia
• Leucopenia
• Agranulocytosis
• Pancytopenia
• Hypersensitivity
• Anaphylaxis/anaphylactoid reactions

Sensory Disorders

• Diplopia
• Blurred vision

Other

• Falling

• Central nervous system depressants
• Barbiturates
• Antipsychotics
• Sedatives/hypnotics
• Anxiolytics
• Antidepressants
• Narcotic analgesics
• Sedative antihistamines
• Anticonvulsants
• Anaesthetics  
• Opioids
• CYP450 inhibitors
• Theophylline
• Aminophylline
• Antihypertensives
• Alcohol

None routine. Specific cases may require:

• Hepatic function
• Renal function

Risk from concomitant use of opioids

• Concomitant use of lormetazepam and opioids may result in sedation, respiratory depression, coma and death
• Because of these risks, concomitant prescribing of sedative medicines such as benzodiazepines or related drugs such as lormetazepam with opioids should be reserved for patients for whom alternative treatment options are not possible
• If a decision is made to prescribe lormetazepam concomitantly with opioids, the lowest effective dose should be used, and the duration of treatment should be as short as possible
• Patients should be followed closely for signs and symptoms of respiratory depression and sedation. In this respect, it is strongly recommended to inform patients and their caregivers (where applicable) to be aware of these symptoms

Lormetazepam is a benzodiazepine with anxiolytic, muscle relaxant, sedative and hypnotic properties. Clinical studies have shown minimal effects on REM sleep and on psychomotor performance on the day after treatment with lormetazepam.

Capsule 0.5mg

• Loramet (Pharmacare)

Capsule 1mg

• Loramet (Pharmacare)

Capsule 2mg

• Loramet (Pharmacare)