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Products > Human Product > CNS drugs > Alprazolam

Alprazolam


Category:

Antianxiety & Antipanic & Antitremor. (USP DI 2005)

Composition:

Each tablet contains Alprazolam 0.5 or 1 mg.

Chemistry:

: The chemical name of alprazolam is 8-Chloro-1-methyl-6-phenyl-4H-s-triazolo [4,3-a][1,4]benzodiazepine.The structural formula is

Pharmacokinetics:

Alprazolam is well absorbed from the gastrointestinal tract following oral administration , with peak plasma concentration being achieved with 1 to 2 hours of a dose. The half life in plasma is 11 to 15 hours. Alprazolam is 70 to 80% bound to plasma proteins. It is metabolised in the liver primarily to α-hydroxy alprazolam,which is reported to be approximately half as active as the parent compound, 4- hydroxy alprazolam, and an inactive benzophenone;plasma concentrations of metabolites are very low. It is excreted in urine as unchanged drug and metabolites.

Indications:

Alprazolam is a short acting benzodiazepine with general properties similar to those of diazepam. It also appears to possess antidepressant activity . It is used in the short-term treatment of anxiety disorders, anxiety associated with depression, panic disorders with or without agoraphobia and premenstrual syndrome.

Contraindications:

Alprazolam tablets are contraindicated in patients with known sensitivity to this drug or other benzodiazepines. It 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.

Pregnancy: Category D.

It should be considered that the child born of a mother who is receiving benzodiazepines may be at some risk for withdrawal symptoms from the drug during the postnatal period. Also , neonatal flaccidity and respiratory problems have been reported in children born of mothers who have been receiving benzodiazepines. Patients should be advised that if they become pregnant during therapy or intend to become pregnant they should communicated with their physicians about the desirability of discontinuing the drug.

Nursing mothers:

Benzodiazepines are known to be excreted in human milk. It should be assumed that Alprazolam is as well . As a general rule, nursing should not be undertaken by mothers who must use Alprazolam.

Precaution:

If Alprazolam tablets are to be combined with other psychotropic agents of anticonvulsant drugs , careful consideration should be given . In patients with impaired renal , hepatic or pulmonary function precautions should be observed. Episodes of hypomania and mania have been reported in patients with depression. A decreased systemic Alprazolam elimination rate has been observed in both alcoholic liver disease patients and obese patients receiving Alprazolam . Alprazolam has a weak uricosuric effect. Although other medications with weak uricosuric effect have been reported to cause acute renal failure , there have been no reported instances of acute renal failure attributable to therapy with Alprazolam.

Drug interaction:

Alprazolam , produce additive CNS depressant effects when Co-administered with other psychotropic medications,anticonvulsants, antihistaminics, ethanol and other drugs which themselves produce CNS depression.
Caution is recommended during coadministration with Alprazolam and fluoxetine, propoxyphene, oral contraceptives . Available data from clinical studies of benzodiazepines other than Alprazolam suggest a possible drug interaction with Alprazolam for the
following :
Diltiazem, isoniazid, macrolide antibiotics such as erythromycin and clarithromycin and grapefruit juice.

Adverse reactions:

Side effects to Alprazoalam tablets, if they occur, are generally observed at the beginning of therapy and usually disappear upon continued medication. In the usual patient, the most frequent side effects are likely to be an extension of the pharmacological activity of alprazolam, eg, drowsiness or light headedness. In addition to the relatively common, the following adverse events have been reported in association with the use of alprazolam: Impaired coordination, Dysarthria, Constipation, Increased Appetite, Weight Gain or loss, Micturition Difficulties.

Overdosage:

Manifestations of alprazolam overdosage include somnolence, confusion, impaired coordination, diminished reflexes and coma. Death has been reported in association with overdoses of alprazolam by itself, as it has with other benzodiazepines. In addition, fatalities have been reported in patients who have overdosed with a combination of a single benzodiazepine, including alprazolam and alcohol. General treatmest of overdose: As in all cases of drug overdosage, respiration, pulse rate and blood pressures should be monitored along with immediate gastric lavage.
Flumazenil, a specific benzodiazepine receptor antagonist is indicated for complete or partial reversal of sedative effect and maybe used in situation when an overdose with alprazolam is known or suspected but the prescriber should be awar of risk of seizure in association with flumazenil treatment, particularly in long – term benzodiazepine users and in cyclic auti depressant overdose.

Dosage & Administration:

It is used in the treatment of anxiety disorders in doses of 0.25 to 0.5 mg three times daily by mouth increased where necessary up to a total daily dose of 3 or 4 mg. In elderly or debilitated patients an initial dose of 0.25 mg two or three times daily has been suggested. Doses of up to 10 mg of Alprazolam daily have been used in the treatment of panic attack and depression.

Storage:

Store below 30ºC . Store in a tight, light – resistant container.

How supplied:

Alprazolam 0.5 mg is available as round light pink, scored tablet . There are 3 blisters, each contains 10 tablets in a box. Alprazolam 1 mg is available as round light blue, scored tablet . There are 2 blisters, each contains 20 tablets.

References:

1 – PDR 2008
2 – Martindale 35
3 – USP DI 2005
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