Names and pronunciation
(al-pray′zoe-lam) Xanax, Xanax XR
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Drug reference
(al-pray′zoe-lam) Xanax, Xanax XR
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Func. class.: Antianxiety
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Chem. class.: Benzodiazepine (short/ intermediate acting) Controlled Substance Schedule IV
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Do not confuse: ALPRAZolam/LORazepam Xanax/Zantac
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ACTION: Depresses subcortical levels of CNS, including limbic system, reticular formation
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USES: Anxiety, panic disorders with or without agoraphobia, anxiety with depressive symptoms
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Unlabeled uses: Premenstrual dys- phoric disorders, insomnia, PMS, alco- hol withdrawal syndrome
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CONTRAINDICATIONS: Preg- nancy, breastfeeding, hypersensitivity to benzodiazepines, closed-angle glau- coma, psychosis, addiction Precautions: Geriatric patients, debili- tated patients, hepatic disease, obesity, severe pulmonary disease
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SIDE EFFECTS CNS: Dizziness, drowsiness, confusion, headache, stimulation, poor coordination, suicide EENT: Blurred vision GI: Constipation, dry mouth, nausea, vom- iting, anorexia, diarrhea, weight gain/loss GU: Decreased libido INTEG: Rash, dermatitis
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INTERACTIONS Increase: ALPRAZolam action—CYP3A4 inhibitors (cimetidine, disulfiram, eryth- romycin, FLUoxetine, isoniazid, itracon- azole, ketoconazole, metoprolol, propran- olol, valproic acid); do not use together
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Black Box Warning: Increase: CNS depression—anticonvulsants, alcohol, antihistamines, sedative/hypnotics, opioids; avoid concurrent use Decrease: sedation—xanthines Decrease: ALPRAZolam action—CYP3A4 inducers (barbiturates, carBAMazepine rifAMPin), adjust dose as needed Decrease: action of levodopa Drug/Herb Increase: CNS depression—kava, mela- tonin, St. John’s wort, valerian Drug/Food Increase: product level—grapefruit juice; avoid concurrent use Drug/Lab Test Increase: AST/ALT, alkaline phosphatase Black Box Warning: For use with other CNS depressants or opioids, monitor for respiratory depression • Physical dependency, withdrawal symptoms: anxiety, panic attacks, agita- tion, seizures, headache, nausea, vomit- ing, muscle pain, weakness; withdrawal seizures may occur after rapid decrease in dose or abrupt discontinuation • Beers: avoid in older adults; increased risk of cognitive impairment
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TREATMENT OF OVERDOSE: Lavage, VS, supportive care, flumazenil
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DOSAGE AND ROUTES Anxiety disorder • Adult: PO 0.25-0.5 mg tid, may in- crease q3-4days if needed, max 4 mg/day in divided doses • Geriatric: PO 0.25 mg bid; increase by 0.125 mg as needed Panic disorder • Adult: PO 0.5 mg tid, may increase up to 1 mg/day q3-4days, max 10 mg/day; EXTENDED RELEASE (Xanax XR) give daily in AM, 0.5-1 mg initially, mainte- nance 3-6 mg/day, max 10 mg/day Hepatic dose • Reduce dose by 50%-60% Premenstrual dysphoric disorders/ PMS (unlabeled) • Adult: PO 0.25 mg bid-tid starting on day 16-18 of menses, taper over 2-3 days when menses occurs, max 4 mg/day
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Available forms: Tablets 0.25, 0.5, 1, 2 mg; extended-release tablets (Xanax XR) 0.5, 1, 2, 3 mg; orally disintegrating tablets 0.25, 0.5, 1, 2 mg; oral solution 1 mg/mL
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Administer: • Tablets may be crushed, mixed with food, fluids if patient is unable to swal- low medication whole; do not break, crush, chew extended release (XR), give extended-release tablets in AM; conver- sion from regular-release tablets to ex- tended release is at same dose • With food or milk for GI symptoms; high-fat meal will decrease absorption • To discontinue, decrease by 0.5 mg q3days • May divide total daily doses into more times/day if anxiety occurs between doses • Orally disintegrating tablets: place on tongue to dissolve and swallow; protect from moisture, discard unused portion of tablet if split • Oral solution: mix with water, juice, applesauce, or other soft foods; use cali- brated dropper supplied
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Assess: • Mental status: anxiety, mood, senso- rium, orientation, affect, sleeping pat- tern, drowsiness, dizziness, especially in geriatric patients both before and during treatment, suicidal thoughts, behaviors • Hepatic, blood studies: renal studies, AST, ALT, bilirubin, creatinine, LDH, alka- line phosphatase, CBC; may cause neutro- penia, decreased Hct, increased LFTs
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Evaluate: • Therapeutic response: decreased anxi ety, restlessness, sleeplessness, panic attacks
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Not to double doses; to take exactly as prescribed; if dose is missed, take within 1 hr as scheduled; that product may be taken with food • Not to use for everyday stress or for more than 4 mo unless directed by pre- scriber; not to take more than prescribed amount; that product may be habit form- ing; that memory impairment is a result of long-term use • To avoid OTC preparations unless ap- proved by prescriber, not to use with grapefruit juice • Not to discontinue medication abruptly after long-term use • To avoid driving, activities that require alertness because drowsiness may occur • To avoid alcohol, other psychotropic medications unless directed by prescriber • To rise slowly or fainting may occur, especially among geriatric patients • That drowsiness may worsen at begin- ning of treatment • Oral disintegrating tablet: to place on tongue and allow to dissolve; swallow; if only half tablet required, discard other half • Oral solution: to mix with water, juice, A or other soft foods; to use measuring device supplied • Pregnancy/breastfeeding: If planned or suspected; not to use in pregnancy, to avoid breastfeeding
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PHARMACOKINETICS PO: Well absorbed; widely distributed; onset 30 min; peak 1-2 hr; duration 4-6 hr; oral disintegrating tablet peak 1.5-2 hr; therapeutic response 2-3 days; metabolized by liver (CYP3A4), ex- creted by kidneys; crosses placenta, breast milk; half-life 12-15 hr, protein binding 80%
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• Adult: PO 0.25-0.5 mg tid, may in- crease q3-4days if needed, max 4 mg/day in divided doses
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• Geriatric: PO 0.25 mg bid; increase by 0.125 mg as needed Panic disorder
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• Adult: PO 0.5 mg tid, may increase up to 1 mg/day q3-4days, max 10 mg/day; EXTENDED RELEASE (Xanax XR) give daily in AM, 0.5-1 mg initially, mainte- nance 3-6 mg/day, max 10 mg/day Hepatic dose
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• Reduce dose by 50%-60% Premenstrual dysphoric disorders/ PMS (unlabeled)
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• Adult: PO 0.25 mg bid-tid starting on day 16-18 of menses, taper over 2-3 days when menses occurs, max 4 mg/day
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