alprazolam

Absorption: Well absorbed (90%) from the GI tract; absorption is slower with extended-release tablets.

Distribution: Widely distributed; crosses blood-brain barrier. Accumulation is minimal.

Metabolism/Excretion: Metabolized by the liver by the CYP3A4 isoenzyme to an active compound that is subsequently rapidly metabolized.

Half-Life: 12–15 hr.

Time/Action Profile ⬆ ⬇

(sedation)

ROUTE	ONSET	PEAK	DURATION
PO	1–2 hr	1–2 hr	up to 24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Cross-sensitivity with other benzodiazepines may exist;
Pre-existing CNS depression;
Severe uncontrolled pain;
Angle-closure glaucoma;
Obstructive sleep apnea or pulmonary disease;
Concurrent use with itraconazole or ketoconazole;
Lactation: Lactation.

Use Cautiously in:

Renal impairment (↓ dose);
Hepatic impairment (↓ dose);
History of suicide attempt or alcohol/drug dependence, debilitated patients (↓ dose);
OB: Use late in pregnancy can result in sedation (respiratory depression, lethargy, hypotonia) and/or withdrawal symptoms (hyperreflexia, irritability, restlessness, tremors, inconsolable crying, feeding difficulties) in neonates;
Pedi: Safety and effectiveness not established in children;
Geri: Appears on Beers list. ↑ risk of cognitive impairment, delirium, falls, fractures, and motor vehicle accidents in older adults. If possible, avoid use in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: rash

EENT: blurred vision

GI: constipation, diarrhea, nausea, vomiting, weight gain

Neuro: dizziness, drowsiness, lethargy, confusion, depression, hangover, headache, paradoxical excitation

Misc: physical dependence, psychological dependence, tolerance

Interactions ⬆ ⬇

Drug-drug:

Use with opioids or other CNS depressants, including other benzodiazepines, nonbenzodiazepine sedative/hypnotics, anxiolytics, general anesthetics, muscle relaxants, antipsychotics, and alcohol, may cause profound sedation, respiratory depression, coma, and death; reserve concurrent use for when alternative treatment options are inadequate.
Hormonal contraceptives, disulfiram, fluoxetine, isoniazid, metoprolol, propranolol, valproic acid, and CYP3A4 inhibitors (erythromycin, ketoconazole, itraconazole, fluvoxamine, cimetidine, nefazodone) ↑ levels and effects; dose adjustments may be necessary; concurrent use with ketoconazole and itraconazole contraindicated.
May ↓ efficacy of levodopa.
CYP3A4 inducers, including rifampin, carbamazepine, or barbiturates, may ↓ levels and effectiveness.
Sedative effects may be ↓ by theophylline.
Cigarette smoking may ↓ levels and effectiveness.

Drug-Natural Products:

Kava-kava, valerian, or chamomile can ↑ risk of CNS depression.
St. John's wort may ↓ levels and effectiveness.

Drug-Food:

Grapefruit juice may ↑ levels and risk of toxicity.

Route/Dosage ⬆ ⬇

Anxiety

PO (Adults ): 0.25–0.5 mg 2–3 times daily (not to exceed 4 mg/day).
PO Geriatric Patients ): Begin with 0.25 mg 2–3 times daily.

Panic Attacks

PO (Adults ): 0.5 mg 3 times daily; may ↑ by ≤1 mg every 3–4 days as needed (not to exceed 10 mg/day). Extended-release tablets: 0.5–1 mg once daily in the morning; may ↑ every 3–4 days by not more than 1 mg/day; up to 10 mg/day (usual range 3–6 mg/day).

Availability ⬆ ⬇

(Generic available)

Tablets: 0.25 mg; 0.5 mg; 1 mg; 2 mg
Extended-release tablets: 0.5 mg; 1 mg; 2 mg; 3 mg
Orally disintegrating tablets orange flavor: 0.25 mg; 0.5 mg; 1 mg; 2 mg
Oral solution (concentrate): 1 mg/mL

Assessment ⬆ ⬇

Assess degree and manifestations of anxiety and mental status (orientation, mood, behavior) prior to and periodically during therapy.
Assess for drowsiness, light-headedness, and dizziness. These symptoms usually disappear as therapy progresses. Dose should be ↓ if these symptoms persist.
Geri: Assess CNS effects and risk of falls. Institute falls prevention strategies.
Assess risk for addiction, abuse, or misuse before administration and periodically during therapy.
Prolonged high-dose therapy may lead to psychological or physical dependence. Risk is greater in patients taking >4 mg/day. Restrict the amount of drug available to patient. Assess regularly for continued need for treatment.

Lab Test Considerations:

Monitor CBC and liver and renal function periodically during long-term therapy. May ↓ hematocrit and cause neutropenia.

Toxicity and Overdose:

Flumazenil is the antidote for alprazolam toxicity or overdose. Flumazenil may induce seizures in patients with a history of seizures disorder or who are taking tricyclic antidepressants.

Implementation ⬆ ⬇

Do not confuse Xanax with Fanapt.
- Do not confuse alprazolam with clonazepam or lorazepam.
- If early-morning anxiety or anxiety between doses occurs, same total daily dose should be divided into more frequent intervals.
PO: May be administered with food if GI upset occurs. Administer greatest dose at bedtime to avoid daytime sedation.
- Tablets may be crushed and taken with food or fluids if patient has difficulty swallowing. DNC: Do not crush, break, or chew extended-release tablets.
- Taper by 0.5 mg every 3 days to prevent withdrawal; may require even more gradual taper if withdrawal symptoms (heightened sensory perception, impaired concentration, dysosmia, clouded sensorium, paresthesias, muscle cramps, muscle twitch, diarrhea, blurred vision, ↓ appetite, weight loss) occur. Some patients may require longer tapering period (wks to >12 mo).
- For orally disintegrating tablets: Remove tablet from bottle with dry hands just before taking medication. Place tablet on tongue. Tablet will dissolve with saliva; may also be taken with water. Remove cotton from bottle and reseal tightly to prevent moisture from entering bottle. If only ½ tablet taken, discard unused portion immediately; may not remain stable.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise to read Patient Information before starting therapy. Instruct patient to take medication as directed; do not skip or double up on missed doses. If a dose is missed, take within 1 hr; otherwise, skip the dose and return to regular schedule. If medication is less effective after a few wk, check with health care provider; do not ↑ dose.
Caution patient not to stop taking alprazolam without consulting health care provider. Abrupt withdrawal may cause sweating, vomiting, muscle cramps, tremors, and seizures; may be life-threatening.
Advise patient to avoid the use of alcohol or other CNS depressants, including opioids, concurrently with alprazolam; may cause respiratory depression and overdose. Instruct patient to consult health care provider before taking Rx, OTC, or herbal products concurrently with this medication, especially St. John's wort.
Advise patient to avoid drinking grapefruit juice during therapy. May ↑ levels and risk of toxicity.
Advise patient to not take more than prescribed or share medication with anyone.
Advise patient that alprazolam is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed. Store out of sight and reach of children, and in a location not accessible by others.
May cause drowsiness or dizziness. Caution patient to avoid driving and other activities requiring alertness until response to the medication is known. Geri: Instruct patient and family how to reduce falls risk at home.
Inform patient that benzodiazepines are usually prescribed for short-term use and do not cure underlying problems.
Rep: May cause fetal harm. Advise patient to notify health care provider if pregnancy is planned or suspected or if breastfeeding. Monitor neonates exposed to benzodiazepines during pregnancy (especially during 3rd trimester) and labor for signs of sedation (respiratory depression, lethargy, hypotonia) and/or withdrawal symptoms (hyperreflexia, irritability, restlessness, tremors, inconsolable crying, and feeding difficulties) in the neonate. Monitor neonates and infants exposed to alprazolam during breastfeeding for sedation and withdrawal symptoms. Inform women who take alprazolam during pregnancy about the National Pregnancy Registry for Other Psychiatric Medications to monitor pregnancy outcomes in women exposed to alprazolam during pregnancy. Enroll patient by calling 1-866-961-2388 or visiting online at https://womensmentalhealth.org/research/pregnancyregistry/.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆ ⬇

Contr. Subst. Schedule ⬆ ⬇

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