Prazepam

Registered South African indications:

• Anxiety

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to other benzodiazepines
• Acute pulmonary insufficiency
• Myasthenia gravis
• Severe respiratory insufficiency
• Severe hepatic insufficiency
• Sleep apnoea syndrome
• Pregnancy
• Breastfeeding

Cautions

• Renal impairment
• Hepatic impairment
• Elderly
• Prolonged use
• Abrupt withdrawal
• Debilitated patients
• Pulmonary disease
• Underlying depressive disorder
• Myasthenia gravis
• Psychotic illness
• High doses
• History of drug or alcohol abuse
• May impair ability to drive and operate machinery

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

Anxiety-tension states resulting from stressful circumstances
Anxiety associated with anxiety neurosis and other psychoneurosis

• Oral (tab): 20-60mg/day in divided doses; Max: 60mg/24hrs; Usual single bedtime dose: 20-40mg; Treatment duration: 6-8 weeks

Discontinue gradually

Not established for use in children below 18 years

Pregnancy

• Contraindicated; Administration of benzodiazepines is not recommended in the event of suspected or confirmed pregnancy and while breastfeeding
• Studies carried out to date on prazepam have not yet established whether there is a risk of congenital malformation when this product is used during pregnancy
• As the indications are rarely vitally urgent, it is preferable not to administer prazepam during the first trimester of pregnancy
• Children whose mothers have taken benzodiazepines during pregnancy may show malformations. When the product is administered for medical reasons during the last part of pregnancy or during labour, hypothermia, hypotonia and respiratory depression may develop in the newborn
• Since infants whose mothers have taken benzodiazepines during pregnancy may develop a physical dependency, withdrawal symptoms may occur during postnatal development
• When prazepam is prescribed to a woman of child-bearing age, the woman should be advised to inform her doctor if she wishes to become or is already pregnant, so that the doctor can make the decision to discontinue treatment

Breastfeeding

• Contraindicated; Administration of benzodiazepines is not recommended in the event of suspected or confirmed pregnancy and while breastfeeding
• Administration of prazepam is not advisable during labour and while breast-feeding, because of the risk of hypotension, hypothermia and even withdrawal symptoms in the newborn
• Benzodiazepines cross the foeto-placental barrier and are excreted in the mother's milk

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Mild to moderate: Caution; no dose adjustment recommended
• Severe: Contraindicated

Elderly

• Caution; dose adjustment recommended

Porphyria Information

• Not yet classified (NC)

Central Nervous System Disorders

• Confusion
• Depression
• Vivid dreams
• Drowsiness
• Dizziness
• Lightheadedness
• Ataxia
• Headache
• Tremor
• Slurred speech
• Stimulation
• Syncope
• Fatigue

Cardiovascular Disorders

• Palpitation
• Hypotension

Gastrointestinal Disorders

• Dry mouth
• Gastrointestinal complaints

Hepatobiliary Disorders

• Abnormal hepatic function tests

Genitourinary Disorders

• Genitourinary complaints

Endocrine and Metabolic Disorders

• Increased weight

Musculoskeletal Disorders

• Joint pains
• Swollen feet

Skin and Subcutaneous Tissue Disorders

• Diaphoresis
• Rash
• Pruritis

Sensory Disorders

• Blurred vision

• Central nervous system depressants
• CYP3A4 inhibitors
• Oral contraceptives
• Clozapine

None routine

Prazepam is a benzodiazepine derivative with anxiolytic and central muscle relaxant activity. Benzodiazepines exert their effects through enhancement of the gamma aminobutyric acid (GABA)-benzodiazepine receptor complex. GABA is an inhibitory neurotransmitter that exerts its effects at specific receptor subtypes. GABA-A is the primary receptor subtype in the central nervous system (CNS) and is thought to be involved in most of the inhibitory neurotransmission in the CNS. Benzodiazepines enhance the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. Benzodiazepines reportedly act as agonists at the benzodiazepine receptors, which have been shown to form a component of a functional supramolecular unit known as the benzodiazepine-GABA receptor-chloride ionophore complex.

Tablet 10mg

• Demetrin (Pfizer) originator