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Apo-alpraz
0.25 mg and 0.5 mg aiprazolam
Anxiolytic-Sedative
Pharmacology
APO-ALPRAZ (alprazolam) is a benzodiazepine with anxiolytic properties.
Orally administered alprazolam is readily absorbed in man with peak plasma
concentrations occurring 1 to 2 hours following administration. The
half-life range of alprazolam is 6 to 20 hours following single dose
administration. With multiple doses, given 3 times daily, steady state is
reached within 7 days. Alprazolam and its metabolites are excreted primarily
in the urine. Degradation of alprazolam occurs mainly by oxidation yielding
the primary metabolites a-hydroxy-alprazolam and a benzophenone derivative.
The a-hydroxy-metabolite is further transformed to demethylalprazolam. The
a-hydroxy-alprazolam and demethylalprazolam are active and appear to have
half-lives similar to alprazolam but are present at only low levels in the
plasma. Alprazolam is 80% protein-bound.
In sleep laboratory studies in man, alprazolam decreased sleep latency,
increased duration of sleep and decreased the number of nocturnal
awakenings. Alprazolam produced small decreases in both stage 3 and 4 and
REM sleep. Alprazolam increased REM latency in a dose-related manner.
Alprazolam 0.5mg, administered 3 times a day for 14 days, did not affect
prothrombin times or plasma warfarin levels in male volunteers administered
sodium warfarin orally.
Indications
APO-ALPRAZ (alprazolam) is indicated for the short-term
symptomatic relief of excessive anxiety in patients with anxiety neurosis.
Adverse Effects
The most frequently reported adverse reactions with APO-ALPRAZ
(alprazolam) were drowsiness, coordination difficulties and dizziness.
Release of hostility and other paradoxical effects such as irritability,
excitability and hallucinations are known to occur with the use of
benzodiazepines.
Other side effects less frequently reported, listed by body systems, include
the following :
Neurologic : Blurred vision, headache, seizures, slurred speech, difficulty
in depth perception.
Psychiatric : Agitation, mental confusion, depression, irritability,
nervousness, sleep disturbances, euphoria, lethargy, stupor.
Gastrointestinal : Dry mouth, nausea, non-specific gastrointestinal
disturbances, vomiting.
Musculoskeletal : Muscle spasm, muscle weakness.
Cardiovascular : Hypotension,
palpitations, tachycardia.
Dermatologic : Pruritus, rash.
Genitourinary : Incontinence, change in libido.
Hematologic : Decreased hemoglobin and hematocrit increased and decreased
WBC.
Hepatic : Elevations of alkaline phosphatase, bilirubin, SGOT, SGPT.
Miscellaneous : Increased and decreased blood sugar levels.
Precautions /Warnings
Use in the Elderly : Elderly and debilitated patients, or those with organic
brain syndrome, have been found to be prone to the CNS depressant activity
of benzodiazepines even after low doses. Manifestations of this CNS
depressant activity include ataxia, over-sedation and hypotension.
Therefore, medication should
be administered with caution to these patients, particularly if a drop in
blood pressure might lead to cardiac complications. Initial doses should be
low and increments should be made gradually, depending on the response of
the patient, in order to avoid oversedation, neurological impairment and
other possible adverse reactions.
Dependence Liability : Alprazolam should not be administered to individuals
prone to drug abuse. Caution should be observed in all patients who are
considered to have potential for psychological dependence. Withdrawal
symptoms have been observed after abrupt discontinuation of benzodiazepines.
These include irritability, nervousness, insomnia, agitation, tremors,
convulsions, diarrhea, abdominal cramps, vomiting and mental impairment.
Since these symptoms may be similar to those for which the patient is being
treated, it may appear that he has suffered a relapse upon discontinuation.
It is suggested that alprazolam should be withdrawn gradually if the
individual is suspected of having become dependent, or the drug perhaps has
been used in prolonged high doses.
Use in Mental and Emotional Disorders :
It should be recognized that suicidal tendencies may be present in patients
with emotional disorders, particularly when depressed and that protective
measures and appropriate treatment may be necessary and should be instituted
without delay.
Since excitement and other paradoxical reactions can result
from the use of anxiolytic-sedatives in psychotic patients, alprazolam
should not be used in patients suspected of having psychotic tendencies. As
with other benzodiazepines, alprazolam should not be used in individuals
with physiological anxiety or normal stress of daily living but only in the
presence of disabling manifestations of an appropriate pathological anxiety
disorder. The drugs are not effective in patients with characterological and
personality disorders or those with obsessive-compulsive disorders.
Alprazolam is not recommended for the management of depressive or psychotic
disorders.
Use in Patients with Impaired Renal or Hepatic Function : If
treatment is necessary in patients with impaired hepatic or renal function,
therapy should be initiated at a very low dose and the dosage increased only
to the extent that it is compatible with the degree of residual function of
these organs. Such patients should be followed closely and have periodic
laboratory assessments.
Laboratory Tests : If alprazolam is administered for
repeated cycles of therapy, periodic blood counts and liver function tests
are advisable.
Epileptic Patients : Since benzodiazepines may occasionally exacerbate grand
mal seizures, caution is required when alprazolam is used in epileptic
patients and an adjustment may be necessary in their anticonvulsive
medication. Abrupt withdrawal of alprazolam should be avoided.
APO-ALPRAZ (alprazolam)
is not recommended for use in patients whose primary diagnosis is psychosis
or depression.
Anaphylaxis (severe allergic reaction) and angioedema (severe facial
swelling) which can occur as early as the first time the product is taken.
Complex sleep-related behaviors which may include sleep driving, making
phone calls, preparing and eating food (while asleep).
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