description
Xanax XR is an extended-release formulation of the benzodiazepine drug alprazolam, which is primarily used to treat anxiety disorders and panic disorder. It is designed to release alprazolam gradually over a 24-hour period to maintain consistent levels in the body.
Like other benzodiazepines, alprazolam in Xanax XR works by enhancing the effects of gamma-aminobutyric acid (GABA) in the brain. GABA is the primary inhibitory neurotransmitter that helps reduce neuronal excitability.
Alprazolam binds to specific GABA receptors, called GABAA receptors, and increases their affinity for GABA. This leads to an influx of chloride ions into neurons, causing hyperpolarization (decreased excitability). The end result is a reduction in overall brain activity, producing a calming, anti-anxiety effect.
After oral administration, Xanax tablets release alprazolam in a biphasic manner – an initial burst release followed by a slower, extended release over 24 hours. This allows for rapid onset of therapeutic effects as well as sustained levels throughout the day.
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Food can significantly increase the absorption of Xanax . A high-fat meal may increase peak plasma concentrations by about 25% and delay the time to reach peak levels compared to the fasted state. Alprazolam is highly protein bound (80%) and is metabolized primarily by the liver via the cytochrome P450 3A4 enzyme system. It has an elimination half-life of about 11 hours for the extended-release formulation.
Dosing and Administration
Xanax XR is available in 0.5mg, 1mg, 2mg, and 3mg strength tablets for once-daily oral administration. It should be taken in the morning, with or without food. The recommended starting dose for panic disorder is 0.5-1mg once daily, which can be increased every 3-4 days in 0.5-1mg increments until an optimal response is achieved. Most patients require 3-6mg per day.
For elderly or debilitated patients, the recommended initial dose is 0.5mg once daily to minimize side effects like sedation and unsteadiness. Xanax tablets should be swallowed whole and never crushed, chewed, or broken, as this can lead to rapid release and absorption of the full dose.
Clinical Efficacy
The efficacy of Xanax XR in treating panic disorder was demonstrated in two 6-week, placebo-controlled trials in adults. Patients treated with Xanax XR experienced significantly greater reductions in panic attack frequency and improvements in other panic disorder symptoms compared to placebo.
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Xanax XR has not been studied for longer than 8 weeks for panic disorder or more than 4 weeks for generalized anxiety disorder. Its role in long-term treatment remains to be determined.
Side Effects
The most common side effects of Xanax include sedation, somnolence, memory impairment, dysarthria (slurred speech), coordination abnormalities, and depression. Serious but rare side effects can include respiratory depression, suicidal ideation, psychosis, seizures, and paradoxical reactions like rage, aggression, or mania. Elderly patients are at higher risk of excessive sedation, impaired psychomotor function, falls, and cognitive impairment with Xanax .
Precautions and Contraindications
Xanax should be used with caution in patients with a history of substance abuse, respiratory disease, sleep apnea, acute narrow-angle glaucoma, myasthenia gravis, liver or kidney impairment, and depression. It is contraindicated in patients with known hypersensitivity to alprazolam or other benzodiazepines, as well as in those taking strong CYP3A4 inhibitors like ketoconazole or itraconazole due to potentially toxic alprazolam levels.
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Xanax XR can cause fetal abnormalities and should be avoided in pregnant women. Chronic use during pregnancy can also lead to neonatal withdrawal symptoms in newborns. Elderly and debilitated patients are more sensitive to the sedating effects of Xanax XR. Dosage adjustments are recommended in these populations.
Dependence and Withdrawal
Like other benzodiazepines, Xanax has a risk of causing physical and psychological dependence with long-term use, even at therapeutic doses. Abrupt discontinuation can precipitate withdrawal symptoms like seizures, tremors, muscle cramps, vomiting, and delirium. To reduce the risk of withdrawal reactions, Xanax should be tapered gradually under a doctor’s supervision when discontinuing therapy after extended use.
Drug Interactions
Xanax XR should be used cautiously with other CNS depressants like opioids, antipsychotics, and alcohol due to increased risks of excessive sedation and respiratory depression. Strong CYP3A4 inhibitors like ketoconazole can significantly increase alprazolam levels, while enzyme inducers like rifampin can decrease levels. Dose adjustments may be required. Digoxin, oral contraceptives, and cimetidine can also increase alprazolam concentrations when combined with Xanax .
Abuse Potential
As a Schedule IV controlled substance, Xanax has the potential for abuse, misuse, and addiction, which can lead to overdose. It should be prescribed and handled with appropriate caution to minimize these risks.
In summary, Xanax XR is an extended-release alprazolam formulation that provides a convenient once-daily dosing for anxiety disorders like panic disorder. While effective, it requires careful monitoring for adverse effects, drug interactions, and potential dependence with long-term use. Proper dosing and patient selection are critical for optimal safety and efficacy.
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