alprazolam

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

Distribution: Widely distributed, crosses blood-brain barrier. Probably crosses the placenta and enters breast milk. 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 required);
Hepatic impairment (↓ dose required);
History of suicide attempt or alcohol/drug dependence, debilitated patients (↓ dose required);
OB: Use late in pregnancy can result in sedation (respiratory depression, lethargy, hypotonia) and/or withdrawal symptoms (hyperreflexia, irritability, restlessness, tremors, inconsolable crying, and 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, non-benzodiazepine 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, 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 (rifampin, carbamazepine, or barbiturates) ↓ levels and effects.
Sedative effects may be ↓ by theophylline.
Cigarette smoking↓ levels and effects.

Drug-Natural Products:

Kava-kava, valerian, or chamomile can ↑ CNS depression.

Concurrent ingestion of grapefruit juice↑ levels and effects.

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 be ↑ by 1 mg or less 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 be ↑ 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 tabletsorange-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 patient for drowsiness, light-headedness, and dizziness. These symptoms usually disappear as therapy progresses. Dose should be reduced if these symptoms persist.
Geri: Assess CNS effects and risk of falls. Institute falls prevention strategies.
Assess risk for addiction, abuse, or misuse prior to 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 cause ↓ hematocrit and 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 decrease, weight loss) occur. Some patients may require longer tapering period (weeks to >12 mo).
- For orally disintegrating tablets: Remove tablet from bottle with dry hands just prior to 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 ⬆ ⬇

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 professional; do not increase dose. Caution patient not to stop taking alprazolam without consulting health care professional. Abrupt withdrawal may cause sweating, vomiting, muscle cramps, tremors, and seizures; may be life-threatening.
Advise patient to avoid drinking grapefruit juice during therapy.
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.
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 professional before taking Rx, OTC, or herbal products concurrently with this medication.
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 professional 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/.

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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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