Alprazolam is a drug that belongs to the benzodiazepine family and is used for the treatment of anxiety states, especially in panic attacks, agoraphobia, panic attacks and intense stress. It is sold under a generic name or under different trade names depending on the country, all with identical effects, only practically changing the excipient or the design of the pill/tablet. It has a hypnotic effect (promoting sleep in the short term) and works by decreasing the excitement of the brain. Alprazolam has sedative, hypnotic, and anticonvulsant properties, but the most notable effect is anxiolytic. However, due to its addictive potential and the development of tolerance after a relatively short period of a few weeks, its administration is recommended only in short-term treatments.

What is anxiety?

Occasional anxiety is a normal part of life. However, those suffering from anxiety disorder have intense, excessive and persistent fears very frequently in everyday situations. Frequently, in anxiety disorders, there are repeated episodes of sudden feelings of intense anxiety and fear or terror that peak in a matter of minutes (panic attacks). Feelings of panic and anxiety are sometimes very difficult to control as they are disproportionate to reality and can last a long time, leading to interference with daily activities. Agoraphobia belongs to the spectrum of anxiety disorders and consists of the fear of places and situations capable of generating panic or the feeling of being trapped, ashamed or defenceless. Panic disorder consists of several episodes of unexpected feelings of very intense anxiety or fear that can reach very high levels in a matter of minutes (panic attacks). The person may experience sensations of catastrophe, dyspnea, chest pain, or heart palpitations. Once these attacks happen, the patient will cause the person to worry and watch for them to happen one more time and will try to avoid the situations in which they have happened previously.

Main uses of Xanax Anxiety disorders

The fundamental indication for Xanax is in anxiety-type disorders. Among these disorders, we can highlight panic disorder with or without agoraphobia and generalized anxiety disorder.

Adaptive

Adaptive disorders are those in which some type of derived and explicable symptoms appear from the experience of a specific event or psychosocial stress, are also often treated with alprazolam and other benzodiazepines.

Depression

This is not a formal indication. However, Xanax has been used in depressive disorders that are associated with anxiety disorders. However, this application should be evaluated and applied with great caution in patients with suicidal ideations and severe depression, as it can potentially enhance symptoms.

Social phobia

One of the indications for alprazolam is found in patients with social phobia, helping to reduce the level of anxiety at the prospect of being exposed to other people.

Chemotherapy

Alprazolam has also been shown to be useful in treating the discomfort and anxiety generated by chemotherapy in patients who must undergo it due to some type of tumour.

Background and history

Let’s go back to the 1960s for a moment. Psychiatric treatments were the new norm and the new fashion of the day. Everyone was talking about it, and many were undergoing such treatments. It was the mainstream thing to do at that point. Researchers decided to develop ways to help people who were suffering from insomnia, mostly due to anxiety as the main cause. That’s when Dr Leo Sternbach created benzodiazepine (which was Librium) in 1956. His goal was simple for the public to understand: to create a safer, theoretically less addictive alternative to traditional tranquilisers of the time such as barbiturates. Dr Sternbach is credited with creating Klonopin, Valium and other drugs of a similar nature. The first patent for alprazolam was approved and granted during the ’70s. It was developed by J.B. Hester at the former Upjohn Company laboratories (which later became part of Pfizer Inc). Alprazolam, the generic name for the later Xanax, was first made with the idea of aiding sleep as well as acting as a muscle relaxer. By the 1970s, the most famous prescription drug in the United States was Valium, and Alprazolam was following the heels of it. Although Valium was very popular, it was not patented for the treatment of anxiety and panic. That’s when the creators of the early Xanax found an opportunity to market it. It was launched by Upjohn company in 1981; perfect timing as the third edition of the Diagnostic and Statistical Manual of Mental Disorders (DSM-III), published by the American Psychiatric Association in 1980 had included anxiety disorders in the clinical category. The FDA approved the drug in 1981. The patent came just before the Valium patent was about to expire. Dr David Sheehan was one of the first researchers to demonstrate this drug’s effectiveness in treating panic disorders, anxiety and so on. In fact, its effects are known to be rapid as well as not lose effectiveness over time. After its first two years on the market, Xanax had become the new antidote of the day in the United States.

Characteristics of Xanax

Alprazolam is a drug with psychoactive or psychotropic properties that is classified within anxiolytics, substances used to treat anxiety and its manifestations. Among the anxiolytics, it is part of the benzodiazepines, these are one of the most popular types of psychoactive drugs and consumed by the population (being much safer, more effective and with fewer side effects than their predecessors, barbiturates). In the same way as the rest of the benzodiazepines, the mechanism of action of Xanax consists of its interaction with GABA, one of the most important neurotransmitters for the inhibition of the central nervous system. Xanax acts by stimulating positively on GABA A receptors, thus favouring the inhibition of action potentials in neurons. In other words, it reduces the activity of neurons in certain parts of the brain. This activity is completed dominatingly on the limbic system (profoundly activated in anxiety) and the cerebral cortex. In the specific case of alprazolam, we are dealing with an intermediate-acting benzodiazepine, which implies that it takes a shorter time to start to take effect in the body compared to a long-acting one, but at the same time that its effects last for less time than these. and vice versa in the case that we compare it with a short-acting one. Its effect lasts between 12 and 24 hours approximately. This represents a great advantage since the probabilities of dependence and addiction to the drug are reduced. So small doses are necessary to achieve a longer effect, without the need for it to take too long to take effect.

Alprazolam vs. diazepam vs. bromazepam

Generally speaking, they all work by helping to increase the activity of gamma-aminobutyric acid (GABA). GABA is a neurotransmitter, a chemical messenger that transmits signals throughout the body. If the body does not have enough GABA, the individual may feel depressed. These medicines are used to treat these types of disorders, even alprazolam works to calm panic attacks. Instead, diazepam also addresses other conditions, such as acute alcohol withdrawal, skeletal muscle spasms, seizure disorders, and chronic sleep disorder. With regard to bromazepam, in addition to fighting the symptoms of anxiety, its consumption can alleviate digestive, respiratory or heart rhythm problems that nervousness can imply. Although these three drugs seem very similar and their purpose is the same, they also have some differences that may determine their use. Of course, it is very important to clarify that the consumption of one drug or another will depend on the patient’s condition and the doctor’s recommendations. But going back to its characteristics, if we compare, for example, diazepam and bromazepam, the duration of its effects does show some changes. The former can improve the individual’s condition for up to 50 hours, while bromazepam reduces its performance by half, although its maximum action extends to three hours. In contrast, diazepam loses effectiveness one hour after its ingestion. However, of the three, alprazolam is the most potent, so it is recommended to take it with caution. In addition, according to a survey, in which more than 12,000 users participated, the drugs that provide the highest perceived efficacy are bromazepam and alprazolam compared to diazepam, which is also the one that receives the lowest score in terms of satisfaction with the absence of side effects.

Alprazolam vs. lorazepam

Since they are two medicines in the same family, their mechanism of action is common. They act as allosteric modulators of the GABA receptor, favouring the entry of chlorine into the neuron and causing its inhibition. Due to its way of acting in the body, its effects are limited to a few hours after administration. They do not have a long-term effect, so they are not recommended in chronic situations, as we will see below. Both Lorazepam and Alprazolam treat anxiety. The two drugs have a relatively rapid onset of action, an intermediate duration, and are potent anxiolytics compared to other benzodiazepines. Therefore, if the use of a benzodiazepine is indicated to treat anxiety, the use of both may be appropriate, always under medical prescription. The duration of the effect of these drugs is established according to their half-life. Based on this criterion, benzodiazepines are divided into long, intermediate, short, or ultrashort half-life benzodiazepines. Alprazolam and Lorazepam have an intermediate half-life, between 10 and 15 hours. Alprazolam has a slightly shorter half-life than Lorazepam. In this sense, there are few differences between the two drugs. Having an intermediate half-life makes them good drugs for treating anxiety, anxiety attacks, and insomnia. Since drugs with a very short half-life can produce a rebound effect and drugs with a very long half-life, a lot of hangovers. Both Alprazolam and Lorazepam take effect fairly quickly after administration compared to other benzodiazepines. Although it is true that the effect will be more immediate if it is administered sublingually.

The adverse effects of alprazolam are, in general, frequent and moderately important. The toxicological profile of this drug is similar to that of the other anxiolytic benzodiazepines. By and large, adverse responses are a prolongation of pharmacological activity and essentially affect the central nervous system. 50% of patients experience transient drowsiness during the first days of treatment. Infrequently, patients treated with this medication are compelled to stop treatment. The most characteristic adverse reactions are:

Frequently:

drowsiness, confusion and ataxia, especially in the elderly and debilitated; if these symptoms persist, the dose should be reduced.

Occasionally:

dizziness, sedation, headache, depression, disorientation, dysphasia or dysarthria, reduced concentration, tremor, changes in libido, urinary incontinence, urinary retention, nausea, vomiting, diarrhoea, constipation, dry mouth, hypersalivation, pain epigastric.

Exceptionally:

hepatitis, jaundice, dermatitis, urticaria, pruritus, leukopenia, agranulocytosis, anaemia, thrombocytopenia, eosinophilia, behavioural disturbances, anterograde amnesia, paradoxical excitement, psychosis, vision disturbances, diplopia, nystagmus, hearing disturbances.

Rarely:

respiratory depression, hypotension, hypertension, bradycardia, tachycardia, palpitations, episodes of mania and hypomania. With prolonged use, a dependence develops. The abrupt interruption of treatment at usual doses can cause a withdrawal syndrome (anxiety, agitation, aggressiveness, insomnia, tremor, muscle spasm). If the treatment is with high doses, the withdrawal syndrome can be severe (delirium and seizures). The treatment will not be interrupted abruptly, nor will the doses be modified, without consulting the doctor (the interruption will be done gradually). Warn the patient of the possibility of anterograde amnesia (forgetting about upcoming events).

Contraindicaciones

• Myasthenia gravis: the muscle relaxant activity of benzodiazepines can lead to a worsening of the disease, with increased muscle fatigue.
• Respiratory insufficiency: its muscle relaxant effect can enhance respiratory depression.
• Narrow angle glaucoma: the possible anticholinergic effect of benzodiazepine can increase intraocular pressure and aggravate the disease.
• Sleep apnea there is a danger of exacerbation.
• Hepatic insufficiency: due to the associated risk of encephalopathy.
• Acute ethyl poisoning, coma or syncope: due to additive depression on the central nervous system.
• History of drug dependence: prolonged use or high doses of benzodiazepines can cause mental or physical dependence.
• Kidney insufficiency: since it is mainly eliminated via the kidneys, the dose should be adjusted to the degree of renal functional disability.

Dependence

Treatment with benzodiazepines can lead to the development of physical and mental dependence. The risk of dependence increases with the dose and duration of treatment and is also higher in patients with a history of drug abuse or alcohol use. Once physical dependence has developed, abrupt termination of treatment may be accompanied by withdrawal symptoms, such as headaches, muscle aches, marked anxiety, tension, restlessness, confusion, and irritability. In severe cases, the following symptoms have been described: depersonalization, hyperacusis, tingling and cramps in the extremities, intolerance to light, sounds and physical contact, hallucinations or seizures.

Can I take Xanax if I am pregnant?

Although no congenital abnormalities have been attributed to the use of alprazolam during pregnancy, malformations have been reported after exposure to the drug during the first trimester with other drugs from the same therapeutic group. Human studies have shown risks to the fetus, although in specific circumstances the potential benefits may outweigh the risks to the fetus and / or pregnancy. It may be acceptable if it is needed in a life-threatening situation for the pregnant woman, in which other safer medications cannot be used or are ineffective.

Can I take Xanax if I am breastfeeding?

Alprazolam is excreted in human milk at a low level. However, alprazolam is not recommended during breastfeeding. It is necessary to decide whether breastfeeding or alprazolam treatment should be discontinued/avoided considering the benefit of breastfeeding for the baby and the benefit of treatment for the woman.

How quickly does treatment work?

After oral administration, Alprazolam is easily absorbed and peak plasma concentrations are obtained 1 to 2 hours after it. If you put it under your tongue, it will go faster than taken with a glass of water.

Is it safe to take Xanax?

Alprazolam may affect your ability to drive or operate machinery, as it may make you drowsy, decrease your attention, or decrease your ability to react. The appearance of these effects is more likely at the beginning of treatment or when the dose is increased. Prescribing guidelines typically limit the use of these types of medications to two weeks, due to tolerance and dependency issues.

How long does a dose of Xanax last?

While the half-life of Alprazolam is intermediate, from 12 to 15 hours. In the case of Alprazolam, there is a delayed-release formulation (Alprazolam retard) with a half-life of up to 20 hours  

Are there any side effects of the treatment?

Yes, the most frequent side effects of Xanax, are the following:

• Anterograde amnesia
• Ataxia and slurred speech
• Disinhibition
• Drowsiness, dizziness, tiredness, poor coordination and vertigo
• Dry mouth
• Hallucinations
• Jaundice
• Skin rash

Do I require a prescription for taking Xanax?

Alprazolam has a place with a gathering of meds called benzodiazepines. It is utilized for short-term alleviation of anxiety or for treatment of panic disorders. It is a prescription only medication.

Why is it not safe to buy Xanax online?

Buying drugs online may be dangerous. First, for using Xanax, you need a prescription, which means that a doctor should examine you before prescribing any drugs, because not everybody is able to use this drug. On the other hand, there is the risk of buying drugs from an unknown origin when you are buying medication online. We recommend not to take unnecessary risks.

Is this treatment option safe for children and elderly?

Children: Alprazolam isn’t suggested for youngsters and youths under 18 years old. Benzodiazepines should not be given to children unless strictly necessary and prescribed by the doctor. The efficacy and safety of alprazolam in children under 18 years of age have not been established. Elderly: Alprazolam may affect this group of patients more than young patients. Your doctor may decrease the dosage and check your reaction to treatment. Benzodiazepines and related products should be used with caution in elderly patients, due to the risk of sedation and/or musculoskeletal weakness that can lead to falls, often with serious consequences in this population.

How long do I have to take Xanax for?

The term of treatment ought to be pretty much as short as could be expected. The patient should be reassessed after no more than 4 weeks and the need to continue with the treatment should be evaluated, especially if the patient is free of symptoms. The total duration of treatment should not exceed, as a general rule, 8 to 12 weeks in cases of anxiety, including the process of gradually decreasing the dose.

Can I take Xanax with other medications?

You should avoid taking zolpidem at the same time as any of the following medications:  

• Oral contraceptives, and cimetidine.
• Erythromycin, fluoxetine, and
• Ketoconazole, nefazodone, and ritonavir.
• Carbamazepine, digoxin, and lithium salts.
• Tobacco
• Theophylline and valproic acid

 

Does Xanax create tolerance?

No significant tolerance is observed in patients treated with Xanax for less than 4 weeks. Repeated use of benzodiazepines for a few weeks may cause some loss of efficacy of their hypnotic effects.

Who shouldn’t take Xanax?

You should not take Xanax if you have a severe liver problem if you have a problem where you temporarily stop breathing while you are sleeping (sleep apnea syndrome) if you have myasthenia gravis (fluctuating muscle weakness) if you are a child under the age of 18 years.

Does Xanax cause dependence?

The use of benzodiazepines can lead to physical and psychological dependence. The risk of dependence increases with the dose and duration of treatment; it is also higher in patients with a history of alcohol and drug abuse. Drug dependence can also appear in therapeutic doses and/or in patients without individualized risk factors. There is an increased risk of drug dependence with the combined use of several benzodiazepines, regardless of the anxiolytic or hypnotic indication.