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The physician’s psychoactive medication resource guide
25% of your patients taking an antidepressant will have
weight gain and the weight gain is directly caused by the antidepressant.
Anxiolytic - Antipanic
Alprazolam, a triazolo 1,4 benzodiazepine analog, binds with high affinity to the GABA
benzodiazepine receptor complex. Considerable evidence suggest that the central
pharmacologic/therapeutic actions of alprazolam are mediated via interaction with this receptor
Orally administered it is readily absorbed in man with peak plasma concentrations occurring 1
to 2 hours following administration. The half life range 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 occurs mainly
by oxidation yielding the primary and secondary metabolites which 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.
Alprazolam 500 mcg (0.5 mg), administered 3 times a day for 14 days, did not affect
prothrombin times or plasma warfarin levels in male volunteers administered sodium warfarin
For the management of anxiety disorders or the short-term symptomatic relief of symptoms of
excessive anxiety. Anxiety or tension associated with the stress of everyday life usually does
not require treatment with an anxiolytic.
Alprazolam is indicated for the treatment of Generalized Anxiety Disorder (GAD) and is also
indicated for the management of panic disorder with or without agoraphobia.
Hypersensitivity to alprazolam or other benzodiazepines. Alprazolam is also contraindicated in
pregnancy, in infants and in patients with myasthenia gravis and acute narrow angle glaucoma.
Alprazolam is not recommended for use in patients whose primary diagnosis is psychosis or
As with other CNS depressant drugs, patients should be cautioned against activities requiring
mental alertness, judgment and physical coordination such as driving or operating machinery,
particularly in the early phases of treatment and until proper adjustment to side effects has been
established. Alcohol and benzodiazepines should never be mixed when driving because of the
unpredictable CNS depressant effects of this combination.
Safety in pregnancy has not been established, therefore its use is not recommended. Studies
have suggested an increased risk of congenital malformations associated with the use of the
benzodiazepines, such as chlordiazepoxide, diazepam, and also meprobamate, during the first
trimester of pregnancy. Since alprazolam is a benzodiazepine derivative, its administration is
rarely justified in women of childbearing potential. If the drug is prescribed to a woman of child
bearing potential she should be warned to consult her physician regarding the discontinuation
of the drug if she intends to become or suspects that she is pregnant.
Studies in rats have indicated that alprazolam and its metabolites are secreted into the milk.
Therefore, nursing should not be undertaken while a patient is receiving the drug.
Safety and efficacy of alprazolam in patients under the age of 18 years has not been
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 include ataxia, oversedation 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.
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.
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.
Alprazolam should not be used in patients suspected of having psychotic tendencies since excitement and other paradoxical
reactions can result from the use of anxiolytic-sedatives in these patients. 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.
These 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.
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.
If alprazolam is administered for repeated cycles of therapy, periodic blood counts and liver function tests are advisable. Back to top
Since benzodiazepines may occasionally exacerbate grand mal seizures, caution is required when used in epileptic patients and an
adjustment may be necessary in their anticonvulsive medication. Abrupt withdrawal of alprazolam should be avoided.
Benzodiazepines may potentiate or interact with effects of other CNS acting drugs such as alcohol, narcotics, barbiturates,
nonbarbiturate hypnotics, antihistamines, phenothiazines, butyrophenones, MAO inhibitors, tricyclic antidepressants and
anticonvulsants. Therefore, if alprazolam is to be combined with other drugs acting on the CNS, careful consideration should be given
to the pharmacology of the agent involved because of the possible additive or potentiating effects. Patients should also be advised
against the simultaneous use of other CNS depressant drugs and should be cautioned not to take alcohol during the administration of
The most frequently reported are drowsiness, coordination difficulties with 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:
Blurred vision, headache, seizures, slurred speech, difficulty in depth perception.
Agitation, mental confusion, depression, irritability, nervousness, sleep disturbances, euphoria, lethargy, stupor.
Dry mouth, nausea, nonspecific gastrointestinal disturbances, vomiting.
Muscle spasm, muscle weakness.
Hypotension, palpitations, tachycardia.
Incontinence, change in libido.
Decreased hemoglobin and hematocrit, increased and decreased WBC.
Elevations of alkaline phosphatase, bilirubin, AST (SGOT), ALT (SGPT).
Increased and decreased blood sugar levels.
Manifested as an extension of alprazolam's pharmacologic activity. Varying degrees of CNS depressant effects such as somnolence
and hypnosis can occur. Other manifestations may include muscle weakness, ataxia, dysarthria and particularly in children
paradoxical excitement. In more severe cases diminished reflexes, confusion and coma may ensue. It should be remembered when
treating an overdose that multiple agents may have been ingested. Fatalities with benzodiazepines rarely occur except when other
drugs, alcohol or aggravating factors are involved.
Vomiting may be induced if the patient is fully awake. Vital signs should be monitored and general supportive measures should be
employed as indicated. Gastric lavage should be instituted as soon as possible. I.V. fluids may be administered and an adequate
airway should be maintained.
Experiments in animals have indicated that cardiopulmonary collapse can occur with massive i.v. doses of alprazolam. This could be
reversed with positive mechanical respiration and the i.v. infusion of levarterenol.
Animal experiments with alprazolam and related compounds have suggested that hemodialysis and forced diuresis are probably of
Must be individualized and carefully titrated in order to avoid excessive sedation or mental and motor impairment. As with other
anxiolytic-sedatives, short courses of treatment should be the rule for the symptomatic relief of excessive anxiety and the initial
course of treatment should not last longer than 1 week without reassessment. If necessary, drug dosage can be adjusted after 1
week. Prescriptions should be limited to short courses of therapy.
0.25 mg (250 mcg) given 2 or 3 times daily. If required, increases may be made in 0.25 mg (250 mcg) increments according to the
severity of symptoms and patient response. It is recommended that the evening dose be increased before the daytime doses. Very
severe manifestations of anxiety may require larger initial daily doses. The optimal dosage is one that permits symptomatic control of
excessive anxiety without impairment of mental and motor function. Exceptionally, it may be necessary to increase dosage to a
maximum of 3 mg daily, given in divided doses.
Elderly and Debilitated Patients:
The initial dosage is 0.125 mg (125 mcg) 2 or 3 times daily. If necessary, this dosage may be increased gradually depending on
patient tolerance and response.
Each scored white, ovoid-shaped tablet, coded "Upjohn 29," contains: Alprazolam 0.25 mg (250 mcg). Gluten-free. Bottles of 100 and
Each scored, peach, ovoid-shaped tablet, coded "Upjohn 55," contains: Alprazolam 0.5 mg (500 mcg). Gluten-free. Bottles of 100 and
Each scored, lavender, ovoid-shaped tablet, coded "Upjohn 90" contains: Alprazolam 1 mg (1000 mcg). Gluten-free. Bottles of 100.
Each white, triscored tablet (3 scores), with the number "2" on one side and Xanax on the other side contains: Alprazolam 2 mg. The
tablets can be broken into 4 equal parts of 0.5 mg. Bottles of 100.