Each Tablet contains: Alprazolam 0.5 mg
It is a pale pink, oval-shaped, biconvex tablet.
(1) Pharmacodynamic properties
Alprazolam, like other benzodiazepines, has a high affinity for the
benzodiazepine binding site in the brain. It facilitates the inhibitory
neurotransmitter action of gamma-aminobutyric acid, which mediates both pre-
and post synaptic inhibition in the central nervous system (CNS).
(2) Pharmacokinetic properties
Alprazolam is readily absorbed. Following oral administration peak
concentration in the plasma occurs after 1 - 2 hours. The mean half-life is
12 - 15 hours. Repeated dosage may lead to accumulation and this should be
borne in mind in elderly patients and those with impaired renal or hepatic
function. Alprazolam and its metabolites are excreted primarily in the
In vitro alprazolam is bound (80%) to human serum protein.
Alprazolam is indicated for the short-term treatment of moderate or severe
anxiety states and anxiety associated with depression. It is only indicated
when the disorder is severe, disabling or subjecting the individual to
extreme distress. Alprazolam should not be used to treat short-term mild
anxiety, such as anxiety or tension associated with the stress of everyday
life. As the efficacy of Alprazolam in depression and in phobic or
obsessional states has yet to be established, specific treatment may have to
DOSAGE AND ADMINISTRATION
Treatment should be as short as possible. It is recommended that the patient
be reassessed at the end of no longer than 4 weeks' treatment and the need
for continued treatment established, especially in case the patient is
symptom free. The overall duration of treatment should not be more than 8-12
weeks, including a tapering off process.
In certain cases extension beyond the maximum treatment period may be
necessary; if so, it should not take place without re-evaluation of the
patient's status with special expertise. As with all benzodiazepines,
physicians should be aware that long-term use might lead to dependence in
The optimum dosage of Alprazolam should be based upon the severity of the
symptoms and individual patient response. The lowest dose which can control
symptoms should be used. Dosage should be reassessed at intervals of no more
than 4 weeks. The usual dosage is stated below; in the few patients who
require higher doses, the dosage should be increased cautiously to avoid
adverse effects. When higher dosage is required, the evening dose should be
increased before the daytime doses. In general, patients who have not
previously received psychotropic medications will require lower doses than
those so treated, or those with a history of chronic alcoholism.
Treatment should always be tapered off gradually. During discontinuation of
alprazolam treatment, the dosage should be reduced slowly in keeping with
good medical practice. It is suggested that the daily dosage of alprazolam
be decreased by no more than 0.5 mg every three days.
Some patients may require an even slower dosage reduction.
There is a reduced clearance of the drug and, as with other benzodiazepines,
an increased sensitivity to the drug in elderly patients. Anxiety: 250
micrograms (0.25 mg) to 500 micrograms (0.5 mg) three times daily increasing
if required to a total of 3 mg daily.
Geriatric patients or in the presence of debilitating disease: 250
micrograms (0.25 mg) two to three times daily to be gradually increased if
needed and tolerated.
Children: Not recommended.
If side-effects occur, the dose should be lowered. It is advisable to review
treatment regularly and to discontinue use as soon as possible. Should
longer term treatment be necessary, then intermittent treatment may be
considered to minimize the risk of dependence.
Sedation/drowsiness, light-headedness, numbed emotions, reduced alertness,
confusion, fatigue, headache, dizziness, muscle weakness, ataxia, double or
blurred vision, insomnia, nervousness/anxiety, tremor, change in weight,
These phenomena occur predominantly at the start of therapy and usually
disappear with repeated administration. Other side effects like
gastrointestinal disturbances, changes in libido or skin reactions have been
In addition, the following adverse events have been reported in association
with the use of alprazolam: dystonia, anorexia, slurred speech, jaundice,
musculoskeletal weakness, sexual dysfunction/changes in libido, menstrual
irregularities, incontinence, urinary retention, abnormal liver function and
hyperprolactinaemia. Increased intraocular pressure have been rarely
Withdrawal symptoms have occurred following rapid decrease or abrupt
discontinuance of benzodiazepines including alprazolam. These can range from
mild dysphoria and insomnia to a major syndrome, which may include abdominal
and muscle cramps, vomiting, sweating, tremor and convulsions. In addition,
withdrawal seizures have occurred upon rapid decrease or abrupt
discontinuation of therapy with alprazolam.
Anterograde amnesia may occur at therapeutic dosages, the risk increasing at
higher dosages. Amnesic effects may be associated with inappropriate
behaviour (see warnings and precautions).
Pre-existing depression may be unmasked during benzodiazepam use.
Psychiatric and 'paradoxical' reactions
Reactions like restlessness, agitation, irritability, aggressiveness,
delusion, rages, nightmares, hallucinations, psychoses, inappropriate
behaviour and other adverse behavioural effects are known to occur when
using benzodiazepines or benzodiazepine-like agents. They may be quite
severe with this product. They are more likely to occur in children and the
In many of the spontaneous case reports of adverse behavioural effects,
patients were receiving other CNS drugs concomitantly and/or were described
as having underlying psychiatric conditions. Patients who have borderline
personality disorder, a prior history of violent or aggressive behaviour, or
alcohol or substance abuse may be at risk of such events. Instances of
irritability, hostility and intrusive thoughts have been reported during
discontinuance of alprazolam in patients with post-traumatic stress
Use (even at therapeutic doses) may lead to the development of physical
dependence: discontinuation of the therapy may result in withdrawal or
rebound phenomena (see warnings and precautions). Psychic dependence may
occur. Abuse of benzodiazepines have been reported.