Altrox

Each tablet contains: Alprazolam, U.S.P. 250 mcg and 500 mcg.

Pharmacology: Alprazolam is a triazolo analogue of benzodiazepine, which is indicated as an anti-anxiety drug in various disorders associated with anxiety. Alprazolam has a dose related depressant effect on the central nervous system varying from mild to impairment of task performance to hypnosis.
Pharmacokinetics: Alprazolam is well absorbed from the gastrointestinal tract after oral doses, peak plasma concentrations being achieved within 1 to 2 hours of a dose. The mean plasma half-life is 11 to 15 hours. Alprazolam is 70 to 80% bound to plasma proteins, mainly albumin. It is metabolized in the liver, primarily by the cytochrome P450 isoenzyme CYP3A4. Metabolites include α-hydroxyalprazolam, which is reported to be about half as active as the parent compound, 4-hydroxyalprazolam, and an inactive benzophenone. Plasma concentrations of metabolites are very low. Alprazolam is excreted in urine as unchanged drug and metabolites.

It is indicated for the management of anxiety disorders and short term relief of the symptoms of anxiety, anxiety associated depression and for the treatment of panic disorders.

Dosage should be individualized for maximum beneficial effect. While the usual daily dosages given as follows will meet the needs of most patients, there will be some who require higher doses. In such cases, dosage should be increased cautiously to avoid adverse effects. Dosage should be reduced gradually when discontinuing therapy or when decreasing the daily dose. It is suggested that the daily dosage be decreased by no more than 500 mcg every 3 days. Some patients may require an even slower dosage reduction.
The lowest possible effective dose should be employed and the need for continued treatment reassessed frequently. The risk of dependence may increase with dose and duration of treatment.
Anxiety Disorders and Transient Symptoms of Anxiety: Treatment of anxiety disorders should be initiated with a dose of 250 mcg to 500 mcg three times daily. The dose may be increased to achieve a maximum therapeutic effect, at intervals of 3 to 4 days, to a maximum daily dose of 4 mg, given in divided doses.
Panic Disorder: Treatment of anxiety disorders should be initiated with a dose of 500 mcg three times daily. Depending on the response, the dose may be increased to at intervals of 3 to 4 days in increments of no more than 1 mg per day, to a maximum daily dose of 4 mg, given in divided doses. Occasional patients required as much as 10 mg a day to achieve a successful response.
Special Populations: For elderly, patients with advanced liver disease or with debilitating disease, the usual starting dose is 250 mcg, given two or three times daily. This may be gradually increased if needed and tolerated. The elderly may be especially sensitive to the effects of benzodiazepines. If side effects occur at the recommended starting dose, the dose may be lowered.
Or as prescribed by the physician.

Impairment of consciousness is fairly rapid in poisoning by benzodiazepines. Deep coma or other manifestations of severe depression of brainstem vital functions are rare; more common is a sleep-like state from which the patient can be temporarily roused by appropriate stimuli. There is usually little or no respiratory depression, and cardiac rate and rhythm remain normal in the absence of anoxia or severe hypotension. Since tolerance to benzodiazepines develops rapidly, consciousness is often regained while concentrations of drug in the blood are higher than those which induced coma. Anxiety and insomnia can occur during recovery from acute overdosage, while a full-blown withdrawal syndrome, possibly with major convulsions, can occur in patients who have previously been chronic users.
The treatment of benzodiazepine overdosage is generally symptomatic and supportive. Activated charcoal may be given orally within one hour of ingestion provided they are not too drowsy. Gastric lavage is generally not advocated in overdoses of benzodiazepines alone. The specific benzodiazepine antagonist, flumazenil, is rarely required and can be hazardous, particularly in mixed overdoses involving tricyclic antidepressants or in benzodiazepine-dependent patients. Flumazenil should be used on expert advice only.

Alprazolam is contraindicated in patients with known hypersensitivity to this drug or other benzodiazepines.
Alprazolam may be used in patients with open angle glaucoma who are receiving appropriate therapy, but is contraindicated in patients with acute narrow angle glaucoma.
Alprazolam is contraindicated with ketoconazole and itraconazole, since these medications significantly impair the oxidative metabolism mediated by cytochrome P450 3A (CYP3A).
It is also contraindicated in those with severe hepatic impairment.

Alprazolam should be avoided in patients with pre-existing CNS depression or coma, respiratory depression, acute pulmonary insufficiency, myasthenia gravis, or sleep apnoea, and used with care in those with chronic pulmonary insufficiency. Alprazolam should be given with care to elderly or debilitated patients who may be more prone to adverse effects. Caution is required in patients with muscle weakness, or those with hepatic or renal impairment, who may require reduced doses; its use should be avoided in severe hepatic impairment.
The sedative effects of alprazolam are most marked during the first few days of use; affected patients should not drive or operate machinery. Monitoring of cardiorespiratory function is generally recommended when benzodiazepines are used for deep sedation.
Alprazolam is not appropriate for the treatment of chronic psychosis or for phobic or obsessional states. Alprazolam-induced disinhibition may precipitate suicide or aggressive behaviour and it should not, therefore, be used alone to treat depression or anxiety associated with depression; it should also be used with care in patients with personality disorders. Caution is required in patients with organic brain changes particularly arteriosclerosis. Dependence characterized by a withdrawal syndrome may develop after regular use of alprazolam, even in therapeutic doses for short; because of the risk of dependence, alprazolam should be used with caution in patients with a history of alcohol or drug addiction. Dependence may be also a particular problem at the high doses used in the treatment of panic attacks.
This product also contains FDC Yellow # 5 (Tartrazine) which may cause allergic-type reaction (including bronchial asthma) to certain susceptible person.

Pregnancy Category D. Benzodiazepines can potentially cause fetal harm when administered to pregnant women. If Alprazolam is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. Because of experience with other members of the benzodiazepine class, Alprazolam is assumed to be capable of causing an increased risk of congenital abnormalities when administered to a pregnant woman during the first trimester. Because use of these drugs is rarely a matter of urgency, their use during the first trimester should almost always be avoided. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered. Patients should be advised that if they become pregnant during therapy or intend to become pregnant they should communicate with their physicians about the desirability of discontinuing the drug.
Although the effect of alprazolam on breast-fed infants is unknown, its use by mothers during breast feeding may be of concern since anxiolytic drugs do appear in breast milk and thus could conceivably alter CNS function in the infant both in the short and long term.

Drowsiness, sedation, muscle weakness, and ataxia are the most frequent adverse effects of alprazolam use. They generally decrease on continued dosage and are a consequence of CNS depression. Less frequent effects include vertigo, headache, confusion, depression, slurred speech or dysarthria, changes in libido, tremor, visual disturbances, urinary retention or incontinence, gastrointestinal disturbances, changes in salivation, and amnesia.
Some patients may experience a paradoxical excitation which may lead to hostility, aggression, and disinhibition. Jaundice, blood disorders, and hypersensitivity reactions have been reported rarely. Respiratory depression and hypotension occasionally occur with high dosage and parenteral use.
Raised liver enzyme values have occurred.
Overdosage can produce CNS depression and coma or paradoxical excitation. However, fatalities are rare when taken alone.
Use of alprazolam in the first trimester of pregnancy has occasionally been associated with congenital malformations in the infant but no clear relationship has been established.
Use of alprazolam in late pregnancy has been associated with intoxication of the neonate. Alprazolam on prolonged use may lead to habituation and dependence.

Enhanced sedation or respiratory and cardiovascular depression may occur if benzodiazepines are given with other drugs that have CNS depressant properties; these include alcohol, antidepressants, sedative antihistamines, antipsychotics, general anesthetics, other hypnotics or sedatives, and opioid analgesics. The sedative effect of benzodiazepines may also be enhanced by cisapride.
Pharmacokinetic interactions can occur when alprazolam is administered along with drugs that interfere with its metabolism. Compounds which inhibit certain hepatic enzymes (particularly cytochrome P450 3A4) may increase concentration of Alprazolam and enhance its activity.
Co-administration of Alprazolam with azole antifungal agents is not recommended.
Caution and consideration of dose reduction is recommended when alprazolam is co-administered with nefazodone, fluvoxamine and cimetidine.
Caution is recommended when alprazolam is co-administered with fluoxetine, propoxyphene, oral contraceptives, diltiazem, or macrolide antibiotics such as erythromycin and troleandomycin.
Interactions involving HIV protease inhibitors (such as ritonavir) and alprazolam are complex and time dependent. Low doses of ritonavir resulted in a large impairment of alprazolam clearance, prolonged its elimination half-life and enhanced clinical effects. However, upon extended exposure to ritonavir, CYP3A induction offset this inhibition. This interaction will require a dose-adjustment or discontinuation of alprazolam.
Increased digoxin concentrations have been reported when alprazolam was given, especially in elderly (>65 years of age). Patients who receive alprazolam and digoxin should therefore be monitored for signs and symptoms related to digoxin toxicity.
Steady state plasma concentrations of imipramine and desipramine have been reported to be increased an average of 31% and 20% respectively, by the concomitant administration of alprazolam in doses up to 4 mg/day. The clinical significance of these changes is unknown.

Store at temperatures not exceeding 30°C. Protect from light and moisture.

Anxiolytics

N05BA12 - alprazolam ; Belongs to the class of benzodiazepine derivatives anxiolytics. Used in the management of anxiety, agitation or tension.

EDD, Rx