Drug Detail:Alprazolam (Alprazolam)
Drug Class: Benzodiazepines
1. How it works
- Alprazolam calms and sedates and may be used for the short-term treatment of anxiety and seizure disorders.
- Experts aren't exactly sure how alprazolam works, but believe its effects are due to its ability to strongly bind to the GABA-benzodiazepine receptor complex, which enhances the affinity for GABA (a neurotransmitter that blocks impulses between nerve cells in the brain). Low levels of GABA have been linked to anxiety disorders.
- Alprazolam belongs to the class of medicines known as benzodiazepines.
2. Upsides
- May be used for the short-term relief of anxiety or to help induce sleep at night.
- When used to help sleep at night, the short-acting version is less likely to cause daytime sedation.
- Available in a variety of dosage forms (short-acting tablets, long-acting tablets, oral solution, and orally-dissolving tablets).
- Generic alprazolam is available.
3. Downsides
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Low blood pressure, dizziness on standing (may increase the risk of falls), and heart palpitations.
- Stomach upset including constipation and nausea. Dry mouth, headache and a decrease in libido (sexual drive) are also common.
- May impair reaction skills and affect a person's ability to drive or operate machinery. Avoid alcohol (can enhance the sedative effect).
- Alprazolam is potentially addictive and may cause emotional and physical dependence. The lowest dose should be used for the shortest possible time. Alprazolam supplies may be sought out by drug seekers.
- Withdrawal symptoms (including convulsions, tremor, cramps, vomiting, sweating, or insomnia) may occur with abrupt discontinuation of extended therapy; taper off slowly under a doctor's supervision.
- May rarely cause respiratory depression (unusually slow and shallow breathing). The risk is greater with larger dosages of alprazolam, in people with pre-existing respiratory conditions, or if alprazolam is used in addition to other medications that also cause respiratory depression (such as opioids).
- Although alprazolam has been used off-label (not an FDA-approved use but still a common use) in the past to aid sleep, it should not be promoted for this purpose unless there is no other alternative. Benzodiazepines such as alprazolam reduce the duration of deep or slow-wave sleep, (correlates to how refreshed you feel in the morning) and are also associated with addiction, dependence, and tolerance (where progressively larger dosages of the same drug are needed to obtain the same effect). Abrupt discontinuation of alprazolam, when used for sleep, has been associated with rebound insomnia that may be worse than the initial sleeping problem.
- Occasionally, paradoxical reactions (the opposite of what is to be expected) may occur. Symptoms include anxiety, agitation, rage, sleep disturbances, sexual disinhibition, or hallucinations.
- May interact with a number of other medications including those that inhibit or induce hepatic enzymes CYP3A4 such as ketoconazole, itraconazole, nefazodone, erythromycin; and drugs that also cause sedation such as opioids, antipsychotics, antidepressants, or sedative antihistamines. Alcohol should be avoided when taking alprazolam.
- May not be suitable for some people including those with pre-existing respiratory disease (such as COPD or sleep apnea), acute narrow-angle glaucoma, a history of drug or alcohol abuse, at high risk of falls, women who are pregnant or breastfeeding, or people with kidney or liver disease. The elderly or frail may be especially sensitive to alprazolam's effects.
- Avoid combining alprazolam with other benzodiazepines (such as diazepam) or opioids such as oxycodone or hydrocodone. Profound sedation, respiratory depression (abnormally slow and shallow breathing), coma, and death may result. May also interact with several other drugs including those that induce or inhibit CYP 3A hepatic enzymes. Do not use in people taking strong CYP3A inhibitors such as ketoconazole or itraconazole. There have been reports of death in people with severe pulmonary disease given alprazolam.
- May worsen depression in some people. Monitor.
- People who smoke nicotine-containing cigarettes may have less of a response to alprazolam. People of Asian descent may be more sensitive to alprazolam's effects. The effects of alprazolam may last longer in people who are overweight or obese.
- If alprazolam is given to pregnant women during the later stages of pregnancy, sedation, respiratory depression, lethargy, hypotonia, and withdrawal symptoms may occur in the newborn. Avoid unless benefits outweigh the risks and observe infant if given. Women should not breastfeed their baby while receiving alprazolam.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Tips
- Alprazolam may be taken with or without food.
- Take the lowest effective dose as directed by your doctor. Do not increase the dosage without your doctor's permission.
- Avoid operating machinery, driving, or performing tasks that require mental alertness while taking this medicine.
- Use dry hands to place orally-dissolving tablets on the tongue and allow to dissolve slowly.
- Withdrawal symptoms (blurred vision, insomnia, sweating, rarely seizures) may occur if long-term alprazolam is stopped abruptly; discontinue slowly on a doctor's advice.
- Talk to your doctor or pharmacist before taking any other medications with alprazolam, including those bought over the counter, to check that they are compatible with alprazolam.
- Keep out of reach of children and pets.
- Grapefruit juice or grapefruit products may increase blood levels of alprazolam; avoid concurrent use.
- Paradoxical reactions (the opposite of what is expected), such as over-excitation, anxiety, hallucinations, insomnia, and rage have been reported by people taking alprazolam. Seek medical advice if these occur.
- Avoid drinking alcohol while taking alprazolam because it may enhance the side effects of sedation and respiratory depression.
- Alprazolam may make you feel dizzy, increasing your risk of falls. Be careful when sitting or standing up after lying down.
- If you think you have become dependant on alprazolam or are addicted to it, talk with your doctor.
- If your mood changes or you experience depression or a worsening of depression, talk with your doctor.
- Do not use alprazolam if you are allergic to it or other benzodiazepines like diazepam, lorazepam, or oxazepam.
- Do not start or discontinue alprazolam during pregnancy without speaking to your provider first.
5. Response and effectiveness
- Peak concentrations of alprazolam occur 1-2 hours following administration of immediate-release and orally disintegrating tablets; consistent levels are reached within 5 to 11 hours with extended-release forms.
- Peak concentrations of alprazolam and the duration of effect varies widely between individuals (people of Asian descent may be more sensitive to the effects of alprazolam); with weight (drug may last for longer in the body in people who are obese); in people who smoke; and with different formulations.
6. Interactions
Medicines that interact with alprazolam may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with alprazolam. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with alprazolam include:
- anti-anxiety medications, including other benzodiazepines, such as lorazepam and oxazepam
- anticonvulsants such as valproate
- antidepressants, such as amitriptyline, imipramine, nortriptyline
- antihistamines that cause sedation, such as diphenhydramine
- aprepitant
- azelastine
- barbiturates
- cannabidiol
- cannabis
- chlormethiazole
- clozapine
- CYP 3A4 inducers, such as phenobarbital, phenytoin, rifampicin, St. John's Wort, or glucocorticoids
- CYP 3A4 inhibitors, such as clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal, or grapefruit
- duloxetine
- fusidic acid
- monoamine oxidase inhibitors, such as selegiline, isocarboxazid, or phenelzine
- opioid analgesics such as buprenorphine, codeine, oxycodone and morphine
- oral contraceptives
- muscle relaxants such as cyclobenzaprine
- probenecid
- scopolamine
- sleeping pills, such as zolpidem
- some medications used to treat mental illness, such as clozapine and thioridazine
- theophylline.
Alcohol may worsen the side effects of alprazolam such as drowsiness and dizziness.
Note that this list is not all-inclusive and includes only common medications that may interact with alprazolam. You should refer to the prescribing information for alprazolam for a complete list of interactions.