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Active pharmaceutical ingredient

Alprazolam

Alprazolam is a benzodiazepine anti-anxiety medicine, a Schedule IV controlled substance, that compounding pharmacies prepare as oral capsules and oral liquids.

About this ingredient

Alprazolam is a 1,4-benzodiazepine. It binds the benzodiazepine site on GABA-A receptors in the brain and strengthens the signal of GABA, the brain's main calming neurotransmitter. Manufactured products include Xanax tablets and Xanax XR extended-release tablets (Viatris), generic immediate-release, extended-release and orally disintegrating tablets, and an oral concentrate (Hikma). Xanax is FDA-approved for the acute treatment of generalized anxiety disorder in adults and for panic disorder, with or without agoraphobia, in adults. A prescriber may order alprazolam compounded when a patient needs a strength between the manufactured tablets, a capsule or liquid free of a specific dye, sweetener or filler (the manufactured disintegrating tablets contain aspartame), or a liquid in a concentration that is not manufactured. Alprazolam is a Schedule IV controlled substance. Compounded preparations are not FDA-approved and require a prescription.

Safety and interactions

Xanax carries a boxed warning covering three risks: combining benzodiazepines with opioids can cause profound sedation, slowed breathing, coma and death; benzodiazepines can be abused and misused and can lead to addiction, overdose or death; and continued use causes physical dependence, so stopping suddenly or cutting the dose quickly can trigger withdrawal reactions, including seizures, that can be life-threatening. Alprazolam should not be used by anyone allergic to benzodiazepines or anyone taking a strong CYP3A inhibitor such as ketoconazole or clarithromycin. Alcohol and other sedating medicines add to its effects, and it can raise digoxin levels. Use late in pregnancy can cause sedation and withdrawal in newborns, and the label advises against breastfeeding; LactMed notes that a shorter-acting benzodiazepine is preferred for repeated use while nursing. Common side effects are drowsiness and poor coordination. Do not stop on your own; if side effects are severe or do not go away, talk to your prescriber or pharmacist.

Alprazolam enhances GABA-mediated synaptic inhibition at the benzodiazepine site of GABA-A receptors. Oral absorption is rapid, with peak plasma concentration at 1 to 2 hours; oral bioavailability is about 80 to 100 percent; protein binding is about 80 percent, mostly to albumin. It is metabolized mainly by CYP3A4 to 4-hydroxy and alpha-hydroxy metabolites of low activity; mean elimination half-life is about 11.2 hours (range 6.3 to 26.9) in healthy adults and longer in elderly, obese and alcoholic liver disease patients. Labeled indications (Xanax, Viatris): acute treatment of generalized anxiety disorder and treatment of panic disorder with or without agoraphobia in adults. StatPearls lists insomnia, premenstrual syndrome and depression as non-labeled uses. Dosing, taper schedule and route are per prescriber; the label recommends dosage reduction in geriatric patients and a gradual taper on discontinuation. Monitoring: respiratory status and sedation, especially with opioids or other CNS depressants; abuse and misuse risk before and during treatment; neonates exposed in utero for sedation and withdrawal. Alprazolam is a Schedule IV controlled substance. Electronic prescribing of controlled substances is voluntary under federal DEA rules; CMS applies a prescriber-level threshold for Part D, and a number of states mandate it.

Sources

Compounded at Bayview

How we prepare this ingredient

Patient guides for the preparations we make most often. Each one is compounded to order and requires a prescription.

We do not have a patient page for this ingredient yet. That does not mean we cannot make it. Bayview compounds this ingredient to a prescriber's order, and our full compounding formulary lists every preparation we make. Viewing the formulary requires a prescriber account.

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For prescribers

Full formulary with this ingredient

Every preparation in our formulary that contains this ingredient. Strength, base and dose form are set by the prescription.

We compound this ingredient to a prescriber's order. Our full formulary lists every preparation we make with it, including strength, base and dose form. Sign in with a prescriber account to view it.

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Common questions

Frequently asked questions

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Related

Related active ingredients

Other salt forms of this molecule, and ingredients commonly compounded alongside it.

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Important information

This page describes an active pharmaceutical ingredient, not a finished drug product. Bayview Pharmacy compounds preparations containing it only on a prescriber's order for an individual patient.

Compounded preparations are not FDA-approved, and the FDA has not evaluated them for safety, effectiveness, or manufacturing quality. Nothing on this page is a claim that any preparation is effective for any condition.

A valid prescription is required. Availability depends on Bayview's licensure in your state. This page is general information, not medical advice. Discuss your situation with a licensed healthcare provider.

Talk to a compounding pharmacist

Our pharmacists work with prescribers to build preparations around a patient's dose, form and tolerances. Ask us what is possible with this ingredient.