Each tablet contains: Alprazolam 0.5mg
Pharmacology (Summary of Pharmacodynamics and Pharmacokinetics)
1. Alprazolam is a triazolo analog of the 1,4 benzodiazepine class of
central nervous system-active compounds. The chemical name is
8-chloro-1-methyl-6-phenyl-4H-striazolo (4,3-α)(1,4) benzodiazepine.
2. Alprazolam is readily absorbed from the gastrointestinal tract following
oral administration with peak plasma concentrations being achieved within
1-2 hours. The mean half-life in plasma is 12 to 15 hours. Alprazolam is
70-80% bound to plasma protein. It is metabolized in the liver primarily to
alpha-hydroxyalprazolam, which is reported to be approximately half as
active as the parent compound, and to an inactive benzophenone. Plasma
concentrations of metabolites are very low. Alprazolam and its metabolites
are excreted primarily in the urine.
3. Alprazolam did not affect the prothrombin times or plasma warfarin levels
in male volunteers administered sodium warfarin orally.
Anxiety States: Symptoms include anxiety, tension, agitation, insomnia,
apprehension, irritability and/or autonomic hyperactivity resulting in a
variety of somatic complaints.
Mixed Anxiety-Depression: Symptoms of both
anxiety and depression occur simultaneously. Neurotic or Reactive
Depression: Patients show a depressed mood or a pervasive loss of interest
or pleasure. Symptoms include anxiety, psychomotor agitation and insomnia.
Other characteristics are appetite disturbances, changes in weight, somatic
complaints, cognitive disturbances, decreased energy, feeling of
worthlessness or guilt or thoughts of death or suicide.
Alprazolam should not be used in patients whose primary symptom of
depression is psychomotor retardation, with a diagnosis of bipolar
depression, with psychotic symptoms. Anxiety states, mixed
anxiety-depression or neurotic depression associated with other diseases, eg
the chronic phase of alcohol withdrawal and functional or organic disease,
particularly certain gastrointestinal, cardiovascular or dermatological
Alprazolam is also indicated for the treatment of panic disorder, with or
without agoraphobia. The effectiveness of Alprazolam for long-term use
exceeding 6 months has not been established.
The physician should reassess the usefulness of the drug for the individual
patient from time to time.
Dosage and Administration
The optimum dosage of Alprazolam should be individualized based on the
severity of the symptoms and patient response for maximum beneficial effect.
The usual daily dosage (refer table) will meet the needs of most patients.
Dosage should be increased cautiously to avoid adverse effects. The evening
dose should be increased before the daytime doses.
Patients who have not previously received psychotropic medications will
require lower doses than those previously treated with minor tranquilizers,
antidepressants or hypnotics or those with a history of chronic alcoholism.
The general principle of using the lowest effective dosage should be
followed to preclude the development of oversedation or ataxia.
Usual Starting Dosage*
Usual Dosage Range
0.25-0.5 mg given 3 times
0.5-4 mg daily, given in
0.5 mg given 3 times
1.5-4.5 mg daily, given
in divided dose
or in the presence of
0.25 mg, given 2-3 times
0.5-0.75 mg daily, given
in divided dosage; to be gradually increased if needed and tolerated
0.5-1 mg, given at
The dose should be
adjusted to patient response. Dosage adjustments should be in
increments no greater than 1mg every 3-4 days. additional doses can
be added until 3 or 4 times daily schedule is achieved. The mean
dose in a large multi-clinic study was 5.7 ± 2.3 mg/day with rare
patients requiring a maximum of 10 mg daily.
* If side effects occur,
the dose should be lowered
Patients with known sensitivity to the benzodiazepines.
Side Effect(s) / Adverse Reaction(s)
Side effects are generally observed at the beginning of therapy and usually
disappear upon continued medication or decreased dosage. The most common
adverse reaction to Alprazolam was drowsiness. Other less common adverse
reactions include lightheadedness, blurred vision, coordination disorders,
various gastrointestinal symptoms and autonomic manifestations.
Withdrawal symptoms have occurred following rapid decrease or abrupt
discontinuance of 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
Anterograde amnesia may occur at therapeutic dosages and the
risk increasing at higher dosages.
Amnesic effects may be associated with
Pre-existing depression may be unmasked during benzodiazepam use.
Paradoxical reactions, eg stimulation, agitation, concentration
difficulties, confusion, hallucinations or other adverse behavioural
effects, may occur in rare instances and in a random fashion. They are more
likely to occur in children and the elderly. Patients who have borderline
personality disorder, a prior history of violent or aggressive behaviour, or
alcohol or substance abuse may be at risk of adverse behavioural effects.
Instances of irritability, hostility and intrusive thoughts have been
reported during discontinuance of alprazolam in patients with post-traumatic
Use of alprazolam (even at therapeutic doses) may lead to
the development of physical dependence. Discontinuation of the therapy may
result in withdrawal or rebound phenomena. Psychic dependence may also