Oxazepam is a synthetic benzodiazepine derivative with anxiolytic and sedative-hypnotic properties. Although the mechanism of action has not been fully elucidated, oxazepam appears to enhance gamma-aminobutyric acid (GABA) receptor affinity for GABA, thereby prolonging synaptic actions of GABA.
Oxazepam is believed to stimulate GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation. It is the first of a chemical series of compounds known as the 3-hydroxybenzodiazepinones. A therapeutic agent providing versatility and flexibility in control of common emotional disturbances, this product exerts prompt action in a wide variety of disorders associated with anxiety, tension, agitation, and irritability.
Mechanism of Action of Oxazepam
Similar to other benzodiazepines, oxazepam exerts its anxiolytic effects by potentiating the effect of gamma-aminobutyric acid (GABA) on GABA-A receptors through a cooperative mechanism of action. GABA receptors are ionotropic chloride-linked channel receptors that produce inhibitory postsynaptic potentials. When activated by GABA, the GABA receptor/chloride ionophore complex undergoes a conformational change that allows the passage of chloride ions through the channel. Benzodiazepines are believed to exert their effect by increasing the effect of GABA at its receptor. Benzodiazepine binding increases chloride conductance in the presence of GABA by increasing the frequency at which the channel opens. In contrast, barbiturates increase chloride conductance in the presence of GABA by prolonging the time in which the channel remains open. There are 18 subtypes of the GABA receptor subunits. The α2 subunit of the α2β3γ2 receptor complex is thought to mediate anxiolytic effects while the α1 subunit of the α1β2γ2 receptor complex is thought to mediate sedative, anticonvulsant and anterograde amnesia effects.
Indications of Oxazepam
- Anxiety
- Insomnia
- Alcohol withdrawal
- Alcohol withdrawal syndrome
- Anxiety disorders
- Depression, anxiety
- Feeling anxious
- For the treatment of anxiety disorders and alcohol withdrawal.
Dosage of Oxazepam
Strengths: 15 mg; 10 mg; 30 mg
- Anxiety: 15-30mg three or four times a day.
- Anxiety associated with sleeplessness: 15-25mg one hour before going to bed, your doctor may increase this up to a maximum of 50mg.
- Elderly and patients sensitive to benzodiazepine drugs: 10-20mg three or four times a day.
- Children: Not recommended.
Anxiety
13 years and older
- 10 to 15 mg orally, 3 or 4 times per day
- 15 to 30 mg orally, 3 or 4 times per day
Alcohol Withdrawal
- 15 to 30 mg orally, 3 or 4 times per day
Adult Dose for Anxiety
- 10 to 15 mg orally, 3 or 4 times per day
Pediatric Dose for Anxiety
13 years and older
- 10 to 15 mg orally, 3 or 4 times per day
Side Effects of Oxazepam
The most common
- clumsiness or unsteadiness
- dizziness
- drowsiness
- dry mouth
- false sense of well-being
- increased watering of mouth
- lightheadedness
- constipation;
- vision changes;
- breast swelling (in men or women); or
- decreased sex drive, impotence, or difficulty having an orgasm.
- blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
- restless muscle movements in your eyes, tongue, jaw, or neck;
- a light-headed feeling, like you might pass out;
Common
- Drowsiness and lightheadedness the day after taking the medicine.
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Loss of memory (amnesia).
- Muscle weakness.
- Dizziness.
- Headache.
- Skin rashes.
- Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
- Difficulty in passing urine (urinary retention).
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Jaundice.
- Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
- Nightmares or hallucinations (tell your doctor if you experience this).
Serious
- agitation
- anxiety
- behavioural changes, including aggressiveness, angry outbursts, bizarre behavior, or decreased inhibitions
- confusion
- increased trouble sleeping
- memory problems
- muscle spasms
- shortness of breath
- signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
- sleepwalking
Drug Interactions of Oxazepam
Oxazepam may interact with following drugs, supplements & change the efficacy of drugs
- antihistamines such as diphenhydramine
- digoxin
- levodopa
- medication for depression, seizures, Parkinson’s disease, pain, asthma, colds, or allergies
- muscle relaxants
- oral contraceptives
- phenytoin
- sedatives
- sleeping pills
- theophylline
- tranquilizers
This is not a complete list of oxazepam drug interactions. Ask your doctor or pharmacist for more information.
Pregnancy & Lactation of Oxazepam
Pregnancy
You should not take Oxazepam tablets if you are pregnant, planning to become pregnant or are breastfeeding. If you take Oxazepam tablets late in your pregnancy or during labor your baby might have a low body temperature, floppiness, and breathing difficulties. If taken regularly during late pregnancy, your baby may develop withdrawal symptoms. Ask your doctor or pharmacist for advice before taking any medicine.
Lactation
It is not known if oxazepam crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication.
References