Azolex Uses, Dosage, Side Effects, Food Interaction and all others data.

Azolex is a triazolo analogue of the 1,4-benzodiazepine class of drugs. It is an anxiolytic with hypnotic and anticonvulsive properties. Azolex is presumed to produce its effects via interacting with the Gamma Aminobutyric Acid (GABA) - benzodiazepine receptor complex. Like all benzodiazepines, it causes a dose related CNS depressant activity varying from mild impairment of task performance to hypnosis.

Azolex is indicated to treat anxiety and panic disorders. The mechanism by which its cell receptor interactions translate to a clinical effect is not known.

Azolex exerts its effects through interaction with BNZ-1, BNZ-2, and GABA-A receptors. Azolex binding to BNZ-1 is thought to influence sedation and anti-anxiety, BNZ-2 may influence memory, coordination, muscle relaxation, and anticonvulsive activity, and GABA-A may calm patients by increasing the affinity of GABA-A receptors for GABA.

The metabolism of alprazolam is mediated largely through the action of CYP3As and so alprazolam is contraindicated with CYP3A inhibitors such as ketoconazole and itraconazole.

Trade Name Azolex
Availability Prescription only
Generic Alprazolam
Alprazolam Other Names Alprazolam
Related Drugs sertraline, escitalopram, fluoxetine, duloxetine, hydroxyzine, clonazepam, Lexapro, Zoloft, Xanax, Cymbalta
Weight 0.5mg, 1mg
Type Tablet
Formula C17H13ClN4
Weight Average: 308.765
Monoisotopic: 308.082874143
Protein binding

Alprazolam is 80% protein bound in serum. The majority of this protein binding is to serum albumin. Alprazolam is also bound to alpha1-acid glycoprotein with low frequency.

Groups Approved, Illicit, Investigational
Therapeutic Class Benzodiazepine sedatives
Manufacturer Pharmacare Laboratories (pvt) Ltd,
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am


  • * Anxiety disorder
  • * Short term relief of anxiety
  • * Anxiety associated with depression
  • * Panic disorder, with or without agoraphobia.

Azolex is also used to associated treatment for these conditions: Anxiety, Generalized Anxiety Disorder (GAD), Panic Disorder

How Azolex works

Azolex is a triazolobenzodiazepine used to treat certain anxiety and panic disorders. Azolex acts on benzodiazepine receptors BNZ-1 and BNZ-2. The active metabolites 4-hydroxyalprazolam acts on these receptors with 0.20 times the potency of alprazolam and alpha-hydroxyalprazolam acts on these receptors with 0.66 times the potency.

The effect of alprazolam on BNZ-1 mediates the sedation and anti-anxiety effects of the drug while the action on BNZ-2 mediates effects on memory, coordination, muscle relaxation, and anticonvulsive activity.

Azolex also couple with GABA-A receptors to enhance GABA binding to its receptor. This interaction mediates inhibition of the nervous system and results in a calming effect.

The molecular mechanisms as well as the clinical effects of alprazolam have both been well demonstrated, however the means by which the molecular mechanism translates to a clinical effect is still not understood.


Azolex dosage

Treatment should be initiated with a dose of 0.25 to 0.5 mg three times daily. Depending on the response, dose may

be increased at intervals of 3 to 4 days in increments of no more than 1 mg per day. The maximum dose should not

exceed 4 mg/day. Occasional patients with panic disorder may need as much as 10 mg a day to achieve a

successful response and in these cases periodic reassessment and consideration of dosage adjustment is required.

Dosage should be individualized for maximum beneficial effect with a lowest possible dose. If side-effects occur at

starting dose, dose may be lowered. When discontinuing therapy, dosage should be reduced gradually by no more

than 0.5 mg every three days.

In elderly patients or in patients with advanced liver disease, the usual starting dose is 0.25 mg, two or three times

daily and may be gradually increased if needed and tolerated. Safety and effectiveness of Azolex in individuals

below 18 years of age have not been established.

Azolex XR 1 should be administered once daily, preferably in the morning by patients who are on multiple dosage

regimen of Azolex 0.25/0.5 mg. The tablets should be taken intact, they should not be chewed, crushed, or broken.

Side Effects

Side effects, if occur, are generally observed at the beginning of therapy and usually disappear upon continued medication. The most frequent side effects are drowsiness and light headedness. The other side effects, that may occur include depression, headache, confusion, dry mouth, constipation etc.


Azolex overdose can present as sleepiness, confusion, poor coordination, slow reflexes, coma, and death. Taking alprazolam with alcohol lowers the threshold for overdose. Patients should have their respiration, pulse, and blood pressure monitored. Patients can be treated by gastric lavage and intravenous fluids.. If hypotension occurs, patients may be treated with vasopressors. In known, or suspected overdoses, patients can be given the benzodiazepine receptor antagonist flumazenil in addition to other methods of management.

Oral LD50 in rats is 331-2171mg/kg.

Azolex is a pregnancy category D teratogen meaning there is evidence of risk to the fetus of a mother taking alprazolam but in some cases the benefit may outweigh the risk. Children born to these mothers are also at risk of withdrawal symptoms, flaccidity, and respiratory issues.

Benzodiazepines are expressed in human breast milk and so nursing is generally not recommended in mothers taking alprazolam.

Azolex is not associated with carcinogenicity, mutagenicity, or impairment of fertility.


Because Azolex may produce psychological and physical dependence, increment of dose or abrupt discontinuation of Azolex therapy should not be done without physician's advice. Duration of therapy must be determined by the physicians. Azolex should be administered with caution to patients with hepatic or renal disease, chronic pulmonary insufficiency or sleep apnea.


Azolex produces additive CNS depressant effects when co-administered with other psychotropic medications, anticonvulsants, antihistaminics, ethanol and other drugs which themselves produce CNS depression.

Food Interaction

  • Avoid alcohol. Alcohol may potentiate the CNS depressant effects of this drug.
  • Avoid grapefruit products.
  • Limit caffeine intake.
  • Take with or without food. Food increases the Cmax of extended release alprazolam by 25%, but the AUC and half life are not affected.

[Moderate] GENERALLY AVOID: The pharmacologic activity of oral midazolam, triazolam, and alprazolam may be increased if taken after drinking grapefruit juice.

The proposed mechanism is CYP450 3A4 enzyme inhibition.

In addition, acute alcohol ingestion may potentiate CNS depression and other CNS effects of many benzodiazepines.

Tolerance may develop with chronic ethanol use.

The mechanism may be decreased clearance of the benzodiazepines because of CYP450 hepatic enzyme inhibition.

Also, it has been suggested that the cognitive deficits induced by benzodiazepines may be increased in patients who chronically consume large amounts of alcohol.

MANAGEMENT: The manufacturer recommends that grapefruit juice should not be taken with oral midazolam.

Patients taking triazolam or alprazolam should be monitored for excessive sedation.

Alternatively, the patient could consume orange juice which does not interact with these drugs.

Patients should be advised to avoid alcohol during benzodiazepine therapy.

Volume of Distribution

Volume of distribution following oral administration is 0.8-1.3L/kg. Azolex crosses the blood-brain barrier.

Elimination Route

Oral bioavailability of a standard release tablet of alprazolam is 84-91% with a time to maximum concentration of 1.8 hours. A 1mg oral dose of alprazolam leads to a maximum plasma concentration of 12-22mcg/L. Azolex is rapidly absorbed in the gastrointestinal tract.

Data for the area under the curve and the effect of taking alprazolam with food are not readily available.

Half Life

11.2 hours in healthy patients. The half life is 16.3h in the elderly, 5.8-65.3h in patients with alcoholic liver disease, 9.9-40.4h in obese patients. The half life is 25% higher in Asian patients compared to Caucasians. Other studies have shown the half life to be 9-16h.


Oral clearance is 0.90±0.21mL/min/kg but this increases to 2.13±0.54mL/min/kg when given with CYP3A inducers. Other studies have demonstrated a clearance of 0.70-1.5mL/min/kg.

Elimination Route

Azolex is mainly eliminated in the urine. A large portion of the dose is eliminated as unmetabolized alprazolam. 2

Pregnancy & Breastfeeding use

Pregnancy: Azolex has been categorized in pregnancy category D; that means, it should be avoided in pregnancy.

Lactation: Like other benzodiazepines, Azolex is assumed to be excreted in breast milk. Therefore, nursing should not be undertaken by mothers who must use Azolex.


Contraindicated in patients with hypersensitivity to alprazolam or other benzodiazepines. Azolex is also contraindicated in patients with myasthenia gravis, acute narrow angle glaucoma, during pregnancy and also in infants.

Special Warning

Use in Children: Safety and efficacy of Azolex in patients under the age of 18 years has not been established.

Acute Overdose

Manifestations of Azolex over dosage include somnolence, confusion, impaired coordination, diminished reflexes and coma. In such cases of over dosage general supportive measures should be employed along with immediate gastric lavage.

Interaction with other Medicine

The CNS-depressant action of Azolex may be aggravated by concomitant use of other psychotropic drugs, anticonvulsants, antihistaminics, alcohol and oral contraceptives.

Storage Condition

Azolex tablets should be stored in a cool and dry place, protected from light and moisture.

Innovators Monograph

You find simplified version here Azolex

Azolex contains Alprazolam see full prescribing information from innovator Azolex Monograph, Azolex MSDS, Azolex FDA label


What does Azolex do?

Azolex is used to treat anxiety and panic disorders. It belongs to a class of medications called benzodiazepines which act on the brain and nerves (central nervous system) to produce a calming effect. It works by enhancing the effects of a certain natural chemical in the body (GABA).

What is Azolex used for?

Azolex is used to treat anxiety disorders and panic disorder (sudden, unexpected attacks of extreme fear and worry about these attacks). Alprazolam is in a class of medications called benzodiazepines. It works by decreasing abnormal excitement in the brain.

Is Azolex a sleeping pill?

Azolex belong to a class of medicines called benzodiazepines and hydrocodone belongs to the class of medicines called opioids. Both the classes cause sedation (increased tendency to sleep) and respiratory depression (slow and difficult breathing).

What are the side effects of Azolex?

Common side effects of Azolex include:

  • Drowsiness
  • Depression
  • Headache pain
  • Constipation
  • Diarrhea
  • Dry mouth
  • Impaired coordination
  • Increased or decreased appetite
  • Fatigue
  • Memory problems
  • Irritability
  • Decreased salivation
  • Cognitive disorders
  • Insomnia
  • Lightheadedness
  • Fainting
  • Difficulty speaking
  • Nausea/vomiting
  • Weight gain or weight loss
  • Nasal congestion
  • Decreased or increased libido
  • Menstrual disorder
  • Difficulty urinating
  • Fast heart rate
  • Confusion
  • Blurred vision
  • Low blood pressure (hypotension)
  • Agitation/restlessness
  • Dizziness
  • Increased salivation
  • Nervousness
  • Tremor
  • Talkativeness
  • Incontinence

What should avoid while taking Azolex?

Notes for Consumers: Grapefruit juice and grapefruit-containing foods may increase the actions or side effects (such as drowsiness or slowed breathing) of Azolex. Avoid taking Azolex with grapefruit juice (or grapefruit) whenever possible, and do not increase your intake of grapefruit while taking Azolex.

Does anyone take Azolex daily?

People stop feeling the effects of Azolex long before it leaves the body, which is why it is often taken more than once a day. It's important to take it as prescribed. Taking too many doses can lead to dependence and accidental overdose.

Is Azolex a steroid?

Azolex is a Schedule IV controlled substance and is a common drug of abuse.

Is Azolex an antidepressant?

Azolex appears to be an effective antidepressant in the treatment of outpatients who have a diagnosis of major depressive disorder. The authors have reviewed six controlled double-blind studies of Azolex in the treatment of depression.

Does Azolex cause liver damage?

Azolex, like other benzodiazepines, is rarely associated with serum ALT elevations, and clinically apparent liver injury from Azolex is extremely rare. There have been a few case reports of acute liver injury from Azolex and recurrence on reexposure has been reported.

Is one .25 Azolex a day addictive?

Azolex is a benzodiazepine used to treat anxiety and insomnia. The drug is extremely addictive and should only be used under a doctor's supervision.

Will doctors prescribe Azolex long-term?

It can be used short-term as a way to offer people immediate relief from their symptoms or as part of a long-term management plan for GAD or panic disorder. Azolex is often prescribed for panic attacks, which can occur as part of SAD.

How long should I take Azolex?

Azolex is a powerful benzodiazepine that is only recommended for use for up to six weeks.

Does Azolex cause memory loss?

Several research studies have found that chronic or heavy Azolex use can cause short-term memory loss. This is listed by the National Institutes of Health (NIH) as one of the more serious side effects of Azolex requiring immediate medical attention.

Does Azolex help with racing thoughts?

Azolex may be prescribed to treat symptoms of the manic phase of bipolar disorder. These symptoms include: racing thoughts and speech. high energy.

Can Azolex help mild depression?

Azolex is a medication that is approved by the Food and Drug Administration (FDA) to treat anxiety and panic disorders. Azolex, which is the Azolex name for the generic drug alprazolam, isn't usually used to treat depression because there are several newer and safer medications available.

Is Azolex safe to use?

Azolex is a safe and effective medication when used as directed. Benzodiazepines may produce emotional and/or physical dependence (addiction) even when used as recommended. Physical dependence may develop after 2 or more weeks of daily use.

What is the most Azolex a doctor can prescribe?

For anxiety disorders, the dosage for adults typically starts at 0.25 mg to 0.5 mg three times per day. A doctor may incrementally increase the dosage to maximize the effect. However, the maximum dosage does not usually exceed 4 mg per day. For panic disorders, the required dose of Azolex may exceed 4 mg per day.

Can Azolex make anxiety worse?

Recent studies evaluating the effectivity of Azolex for anxiety have shown that after just 8 weeks, those that were on a Azolex prescription had worse anxiety than those who took a placebo. Despite these results, doctors continue to prescribe these benzos for anxiety disorders at an alarming rate.

How long does the Azolex high last for?

Azolex has an average half-life of roughly 11 hours in healthy adults. In other words, it takes 11 hours for the average healthy person to eliminate half of the dose of Azolex.
*** Taking medicines without doctor's advice can cause long-term problems.