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Alprazolam (Xanax) Pharmacology

Anxiolytic - Antipanic

Alprazolam (Xanax), a triazolo 1.4 benzodiazepine analog.  It binds with high affinity to the GABA benzodiazepine receptor complex. Other considerable evidence suggests that the central therapeutic/pharmacologic actions of Alprazolam (Xanax) (xanax) are mediated via interaction with this receptor complex.

Alprazolam (Xanax) is orally administered and is readily absorbed in man with peak plasma concentrations occurring 1 to 2 hours following it's oral administration. The half life range of Alprazolam (Xanax) is 6 to 20 hours following single dose administration. With multiple doses, given 3 times daily, a steady state is achieved within 7 days. Alprazolam (Xanax) (Xanax) 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 (Xanax) but are present at only low levels in the plasma. Alprazolam (Xanax) is 80% protein bound.

Alprazolam (Xanax) 500 mcg (0.5 mg), administered 3 times a day for 14 days, did not affect prothrombin times or plasma warfarin levels in any male volunteers administered sodium warfarin orally.

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Alprazolam (Xanax) Indications

Alprazolam (Xanax) is used 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 (Xanax).

Alprazolam (Xanax) is indicated for the treatment of Generalized Anxiety Disorder (GAD).  It is also indicated for the management of panic disorder with or without agoraphobia.

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Alprazolam (Xanax) Contraindications

Hypersensitivity to Alprazolam (Xanax) or other benzodiazepines. Alprazolam (Xanax) is also contraindicated in pregnancy, in infants and in patients with acute narrow angle glaucoma and myasthenia gravis.

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Alprazolam (Xanax) Warnings

Alprazolam (Xanax) is not for use in patients whose primary diagnosis is psychosis or depression.

Occupational Hazards:
As with other CNS depressant drugs, all patients should be strongly cautioned against activities requiring mental alertness, judgement and physical coordination such as driving and operating heavy machinery when using Alprazolam (Xanax).  Particularly in the early phases of treatment and until proper adjustment to side effects has been completely established. Alcohol and benzodiazepines should never be mixed when driving.  This results in unpredictable CNS depressant effects of this combination.

Pregnancy:
Safety in pregnancy has not been established and is 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.  Alprazolam (Xanax) is a benzodiazepine derivative and 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 may be pregnant.

Lactation:
Studies in rats have indicated that Alprazolam (Xanax) and its metabolites are secreted into the mother's milk. Therefore, nursing should not be undertaken while a patient is receiving Alprazolam (Xanax).

Safety and efficacy of Alprazolam (Xanax) in patients under the age of 18 years is not established.

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Alprazolam (Xanax) Adverse Effects

The most frequently reported adverse side effects 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:

Dermatologic:
Pruritus, rash.

Genitourinary:
Incontinence, change in libido.

Neurologic:
Blurred vision, slurred speech, difficulty in depth perception, headache, seizures .

Musculoskeletal:
muscle weakness, Muscle spasm.

Cardiovascular:
Hypotension, tachycardia, palpitations.

Hematologic:
Decreased hemoglobin and hematocrit, increased and decreased WBC.

Hepatic:
Elevations of alkaline phosphatase, bilirubin, AST (SGOT), ALT (SGPT).

Psychiatric:
Agitation, nervousness, sleep disturbances, euphoria, mental confusion, depression, irritability, lethargy, stupor.

Gastrointestinal:
Dry mouth, nonspecific gastrointestinal disturbances, nausea, vomiting.

Miscellaneous:
Increased and decreased blood sugar levels.

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in case of Alprazolam (Xanax) Overdose

Symptoms:
Manifested as an extension of Alprazolam (Xanax)'s pharmacologic activity. In more severe cases diminished reflexes, confusion and coma may ensue. 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. 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.

Treatment:
Vital signs should be monitored and general supportive measures should be employed as indicated. Vomiting may be induced if the patient is fully awake. I.V. fluids may be administered and an adequate airway should be maintained. Gastric lavage should be instituted as soon as possible.

This could be reversed with positive mechanical respiration and the i.v. infusion of levarterenol. Experiments in animals have indicated that cardiopulmonary collapse can occur with massive i.v. doses of Alprazolam (Xanax).

Animal experiments with Alprazolam (Xanax) and related compounds have suggested that hemodialysis and forced diuresis are probably of little value.

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Dosage of Alprazolam (Xanax)

As with all other anxiolytic-sedatives, short courses of your 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. Must be individualized and carefully titrated in order to avoid excessive sedation or mental and motor impairment. If necessary, drug dosage must be adjusted after 1 week. Prescriptions should be limited to short courses of therapy.

Adults:
Initially:

The optimal dosage is one that permits symptomatic control of excessive anxiety without impairment of mental and motor function. 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.  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 or decreased gradually depending on patient tolerance and response.

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how is Alprazolam (Xanax) Supplied

Xanax:
0.25 mg:

white, ovoid-shaped tablet, coded "Upjohn 29," contains: Alprazolam (Xanax) 0.25 mg (250 mcg). Gluten-free. Bottles of 100 and 1000.

0.5 mg:
peach, ovoid-shaped tablet, coded "Upjohn 55," contains: Alprazolam (Xanax) 0.5 mg (500 mcg). Gluten-free. Bottles of 100 and 1000.

1 mg:
lavender, ovoid-shaped tablet, coded "Upjohn 90" contains: Alprazolam (Xanax) 1 mg (1000 mcg). Gluten-free. Bottles of 100.

Xanax TS:
2 mg:

Each white, triscored tablet (3 scores), with the number "2" on one side and Xanax on the other side contains: Alprazolam (Xanax) 2 mg. The tablets can be broken into 4 equal parts of 0.5 mg. Bottles of 100.

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