Zolam® [alprazolam] – Anxiolytic And Sedative

Composition

Each tablet contains: Alprazolam: 0.25 or 0.50 mg.

Properties

Zolam® (alprazolam) is a benzodiazepine that is used as anxiolytic, sedative, anticonvulsant and skeletal muscle relaxant.

(alprazolam) produces its central anxiolytic and sedative effects via interaction with neuroreceptor site termed the gamma aminobutyric acid (GABA) benzodiazepine receptor binding.

Benzodiazepine facilitates binding and action of the endogenous neurotransmitter (GABA) which is an inhibiting neurotransmitter introducing anxiolytic, sedative, skeletal muscle relaxant and anticonvulsant effects.

It is extensively absorbed from the gastronintestinal tract.

The oral bioavilability is 92%. Peak plasma concentration occurs in 1-2 hours. The mean half-life is 12-15 hours. The drug is bound 70-80% to plasma protein.

Zolam® (alprazolam) is eliminated largely by oxidation metabolism in the liver followed by excretion of metabolites in the urine. The predominant metabolites are 1- and 4-hydroxy alprazolam.

The plasma levels of the metabolites are low and the biological activity of 1- hydroxylalprazolam is approximately half that of alprazolam.

Indications

Anxiety states (anxiety neurosis) : Symptoms include: anxiety, tension, agitation, insomnia, apprehension, irritability, and/or autonomic hyperactivity resulting in a variety of somatic complaints.

Mixed anxiety-depression : Symptoms of both anxiety and depression occur simultaneously in such patients

Neurotic or reactive depression : Primarily exhibited as a depressed mood or a pervasive loss of interest or pleasure. Symptoms of anxiety, psychomotor agitation and insomnia are usually present.

Other characteristics include appetite disturbances, changes in weight, somatic complaints, cognitive disturbances, decreased energy, feeling of worthlessness or guilt, or thoughts of death suicide.

Anxiety states, mixed anxiety-depression, or depression : Associated with other diseases such as the chronic phase of alcohol withdrawal and functional or organic disease, particularly certain gastrointestinal, cardiovascular or dermatological disorders

Panic related disorders: With or without phobia. It is also indicated for the blocking or attenuation of panic attacks and phobias in patients who have agoraphobia with panic attacks.

The effectiveness in the treatment of anxiety, anxiety associated with depression and neurotic (reactive) depression for long-term use exceeding six moths has not been established by systemic clinical trials; however, patients with panic-related disorders have been effectively treated for up eight moths.

Contraindications

In patients with known hypersensitivity to the benzodiazepines.

Precautions

Benzodiazepines should be used with caution and, large quantities of the drug should not be prescribed for patients with suicidal tendencies or whose history indicates that they may increase dosage on their own initiative

In pregnancy safety of alprazolam has not been established; careful consideration of risk/benefit is necessary

Alprazolam should be used with caution in severe renal or hepatic impaired patients

Adverse Reactions

Overdosage, of benzodiazepines may cause drowsiness, sedation, confusion, ataxia and coma. There are minimal respiratory or cardiovascular effects unless large doses are combined with alcohol or other CNS depressants, when synergism may occur.

Psychological and physical dependence on benzodiazepines has been widely described together with a specific withdrawal syndrome comprising; anxiety, tension, insomnia, trembling and dizziness.

The CNS depressant effects of alprazolam are identical to those of other benzodiazepines. These include; fatigue, somnolence, muscle weakness, ataxia, dizziness, impairment of memory, confusion, depression and changes in libido.

Dosage and Administration

Dosage of Zolam® must be individualized according to severity of symptoms and patient response. In patients who require high doses, dosage should be increased gradually to avoid adverse effects.

Usual initial dosage Usual maintenance dosage
Anxiety0.25 mg to 0.50 mg given 3 times daily.  0.50 mg to 4.0 mg daily given in divided doses.
Depression 0.50 mg given 3 times daily. 1.5 mg to 4.5 mg daily, given in divided doses.
Geriatric patients or in the presence of debilitating disease.0.25 mg given 2-3 times daily. 0.50 mg to 0.75 mg daily, given in divided doses to be gradually increased if needed and tolerated.
Panic-related disorders 0.50 mg to 1.5 mg given at bedtime or 0.5 mg 3 times daily.The doses should be adjusted to patient response. Dosage adjustments should be in increments not greater than 1 mg every 3-4 days.


Additional doses can be added until a TID or QID schedule is achieved.


The mean dose in a large multiclinic study was 5.7± 2.3 mg/day with rare patients requiring a maximum of 10 mg daily.

How Supplied

Strips of 10 tablets in packs of 1 strips.

Keep all medicaments out of reach of children

Product of: AMOUN PHARMACEUTICAL CO. El-Obour City, Cairo, Egypt. ATC Code: N05BA12