U.S. BRAND NAMES — Activase®; Cathflo® Activase®
PHARMACOLOGIC CATEGORY
Thrombolytic Agent
DOSING: ADULTS
Coronary artery thrombi: I.V. Front loading dose (weight-based):
Patients >67 kg: Total dose: 100 mg over 1.5 hours; infuse 15 mg over 1-2 minutes. Infuse 50 mg over 30 minutes. Infuse remaining 35 mg of alteplase over the next hour. See "Note."
Patients 67 kg: Infuse 15 mg I.V. bolus over 1-2 minutes, then infuse 0.75 mg/kg (not to exceed 50 mg) over next 30 minutes, followed by 0.5 mg/kg over next 60 minutes (not to exceed 35 mg). See "Note."
Note: Concurrently, begin heparin 60 units/kg bolus (maximum: 4000 units) followed by continuous infusion of 12 units/kg/hour (maximum: 1000 units/hour) and adjust to aPTT target of 1.5-2 times the upper limit of control.
Acute pulmonary embolism: I.V.: 100 mg over 2 hours.
Acute ischemic stroke: I.V.: Doses should be given within the first 3 hours of the onset of symptoms; recommended total dose: 0.9 mg/kg (maximum dose should not exceed 90 mg) infused over 60 minutes.
Load with 0.09 mg/kg (10% of the 0.9 mg/kg dose) as an I.V. bolus over 1 minute, followed by 0.81 mg/kg (90% of the 0.9 mg/kg dose) as a continuous infusion over 60 minutes. Heparin should not be started for 24 hours or more after starting alteplase for stroke.
Central venous catheter clearance: Intracatheter (Cathflo® Activase® 1 mg/mL):
Patients <30>185 mm Hg systolic or >110 mm Hg diastolic); seizure at the onset of stroke; active internal bleeding; intracranial neoplasm; arteriovenous malformation or aneurysm; known bleeding diathesis including but not limited to: current use of anticoagulants or an INR >1.7, administration of heparin within 48 hours preceding the onset of stroke and an elevated aPTT at presentation, platelet count <100,000/mm3.>400 mg/dL, arterial puncture at a noncompressible site or lumbar puncture within 1 week, clinical presentation suggesting post-MI pericarditis, pregnancy, breast-feeding.
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Arrhythmias: Coronary thrombolysis may result in reperfusion arrhythmias. Bleeding: Doses >150 mg are associated with increased risk of intracranial hemorrhage; monitor all potential bleeding sites. If serious bleeding occurs, the infusion of alteplase and heparin should be stopped.
Disease-related concerns: Conditions that increase bleeding risk: For the following conditions, the risk of bleeding is higher with use of thrombolytics and should be weighed against the benefits of therapy: Recent (within 10 days) major surgery (eg, CABG, obstetrical delivery, organ biopsy, previous puncture of noncompressible vessels), cerebrovascular disease, recent gastrointestinal or genitourinary bleeding, recent trauma, hypertension (systolic BP >175 mm Hg and/or diastolic BP >110 mm Hg), high likelihood of left heart thrombus (eg, mitral stenosis with atrial fibrillation), acute pericarditis, subacute bacterial endocarditis, hemostatic defects including ones caused by severe renal or hepatic dysfunction, significant hepatic dysfunction, diabetic hemorrhagic retinopathy or other hemorrhagic ophthalmic conditions, septic thrombophlebitis or occluded AV cannula at seriously infected site and/or any other condition in which bleeding constitutes a significant hazard or would be particularly difficult to manage because of location. Myocardial infarct (MI): Appropriate use: Follow standard management for MI while infusing alteplase. Stroke: Appropriate use: Treatment of patients with acute ischemic stroke more than 3 hours after symptom onset is not recommended. Treatment of patients with minor neurological deficit or with rapidly improving symptoms is not recommended.
Concurrent drug therapy issues: Anticoagulants: Use with caution in patients receiving oral anticoagulants; increased risk of bleeding. Heparin: Concurrent heparin anticoagulation may contribute to bleeding.
Special populations: Elderly: Use with caution in patients with advanced age (eg, >75 years); increased risk of bleeding. Pregnancy: Use with caution in pregnancy; increased risk of bleeding.
Dosage form specific issues: Cathflo® Activase®: When used to restore catheter function, use Cathflo® cautiously in those patients with known or suspected catheter infections. Evaluate catheter for other causes of dysfunction before use. Avoid excessive pressure when instilling into catheter.
Other warnings/precautions: Administration: Intramuscular injections and nonessential handling of the patient should be avoided. Venipunctures should be performed carefully and only when necessary. If arterial puncture is necessary, use an upper extremity vessel that can be manually compressed.
DRUG INTERACTIONS
Aminocaproic acid (antifibrinolytic agent) may decrease effectiveness.
Drugs which affect platelet function (eg, NSAIDs, dipyridamole, ticlopidine, clopidogrel, IIb/IIIa antagonists) may potentiate the risk of hemorrhage; use with caution.
Heparin and aspirin: Use with aspirin and heparin may increase the risk of bleeding. However, aspirin and heparin were used concomitantly with alteplase in many patients in myocardial infarction or pulmonary embolism trials. This combination was prohibited in the NINDS tPA stroke trial.
Nitroglycerin may increase the hepatic clearance of alteplase, potentially reducing lytic activity (limited clinical information).
Warfarin or oral anticoagulants: Risk of bleeding may be increased during concurrent therapy.
ETHANOL / NUTRITION / HERB INTERACTIONS — Herb/Nutraceutical: Avoid cat's claw, dong quai, evening primrose, feverfew, red clover, horse chestnut, garlic, green tea, ginseng, ginkgo (all have additional antiplatelet activity).
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Excretion in breast milk unknown/use caution
MONITORING PARAMETERS
When using for central venous catheter clearance: Assess catheter function by attempting to aspirate blood.
When using for management of acute myocardial infarction: Assess for evidence of cardiac reperfusion through resolution of chest pain, resolution of baseline ECG changes, preserved left ventricular function, cardiac enzyme washout phenomenon, and/or the appearance of reperfusion arrhythmias; assess for bleeding potential through clinical evidence of GI bleeding, hematuria, gingival bleeding, fibrinogen levels, fibrinogen degradation products, prothrombin times, and partial thromboplastin times.
REFERENCE RANGE
Not routinely measured; literature supports therapeutic levels of 0.52-1.8 mcg/mL
Fibrinogen: 200-400 mg/dL
Activated partial thromboplastin time (aPTT): 22.5-38.7 seconds
Prothrombin time (PT): 10.9-12.2 seconds
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include increased incidence of intracranial bleeding.
CANADIAN BRAND NAMES — Activase® rt-PA; Cathflo® Activase®
INTERNATIONAL BRAND NAMES — Actilyse (AE, AR, AT, AU, BE, BF, BG, BH, BJ, BR, CH, CI, CL, CN, CO, CY, CZ, DE, DK, EE, EG, ES, ET, FI, FR, GB, GH, GM, GN, GR, HK, HU, ID, IN, IQ, IR, IT, JO, KE, KR, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NL, NO, NZ, OM, PH, PL, PT, PY, QA, SA, SC, SD, SE, SG, SL, SN, SY, TH, TW, TZ, UG, UY, YE, ZA, ZM, ZW); Activacin (JP); Activase rt-PA (CA); Cathflo Activase (CA)
MECHANISM OF ACTION — Initiates local fibrinolysis by binding to fibrin in a thrombus (clot) and converts entrapped plasminogen to plasmin
PHARMACODYNAMICS / KINETICS
Duration: >50% present in plasma cleared ~5 minutes after infusion terminated, ~80% cleared within 10 minutes
Excretion: Clearance: Rapidly from circulating plasma (550-650 mL/minute), primarily hepatic; >50% present in plasma is cleared within 5 minutes after the infusion is terminated, ~80% cleared within 10 minutes
Saturday, April 26, 2008
Alprostadil
U.S. BRAND NAMES — Caverject Impulse®; Caverject®; Edex®; Muse®; Prostin VR Pediatric®
PHARMACOLOGIC CATEGORY
Prostaglandin
DOSING: ADULTS
Erectile dysfunction:
Intracavernous (Caverject®, Edex®): Individualize dose by careful titration; doses >40 mcg (Edex®) or >60 mcg (Caverject®) are not recommended: Initial dose must be titrated in physician's office. Patient must stay in the physician's office until complete detumescence occurs; if there is no response, then the next higher dose may be given within 1 hour; if there is still no response, a 1-day interval before giving the next dose is recommended; increasing the dose or concentration in the treatment of impotence results in increasing pain and discomfort.
Vasculogenic, psychogenic, or mixed etiology: Initiate dosage titration at 2.5 mcg, increasing by 2.5 mcg to a dose of 5 mcg and then in increments of 5-10 mcg depending on the erectile response until the dose produces an erection suitable for intercourse, not lasting >1 hour; if there is absolutely no response to initial 2.5 mcg dose, the second dose may be increased to 7.5 mcg, followed by increments of 5-10 mcg
Neurogenic etiology (eg, spinal cord injury): Initiate dosage titration at 1.25 mcg, increasing to a dose of 2.5 mcg and then 5 mcg; increase further in increments 5 mcg until the dose is reached that produces an erection suitable for intercourse, not lasting >1 hour
Maintenance: Once appropriate dose has been determined, patient may self-administer injections at a frequency of no more than 3 times/week with at least 24 hours between doses
Intraurethral (Muse® Pellet):
Initial: 125-250 mcg
Maintenance: Administer as needed to achieve an erection; duration of action is about 30-60 minutes; use only two systems per 24-hour period
DOSING: PEDIATRIC
(For additional information see "Alprostadil: Pediatric drug information")
Patent ductus arteriosus I.V.:
Prostin VR Pediatric®: I.V. continuous infusion into a large vein, or alternatively through an umbilical artery catheter placed at the ductal opening: 0.05-0.1 mcg/kg/minute with therapeutic response, rate is reduced to lowest effective dosage. With unsatisfactory response, rate is increased gradually; maintenance: 0.01-0.4 mcg/kg/minute.
Note: PGE1 is usually given at an infusion rate of 0.1 mcg/kg/minute, but it is often possible to reduce the dosage to 1/2 or even 1/10 without losing the therapeutic effect. The mixing schedule is shown in the table.
Mixing Schedule
Note: 500 mcg equals 1 ampul. For a concentration of 2 mcg/mL, add 500 mcg to 250 mL; infuse at 0.05 mL/kg/minute (72 mL/kg/24 hours) For a concentration of 5 mcg/mL, add 500 mcg to 100 mL; infuse at 0.02 mL/kg/minute (28.8 mL/kg/24 hours) For a concentration of 10 mcg/mL, add 500 mcg to 50 mL; infuse at 0.01 mL/kg/minute (14.4 mL/kg/24 hours) For a concentration of 20 mcg/mL, add 500 mcg to 25 mL; infuse at 0.005 mL/kg/minute (7.2 mL/kg/24 hours)
Note: Therapeutic response is indicated by increased pH in those with acidosis or by an increase in oxygenation (PO2) usually evident within 30 minutes.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution:
Caverject®: 20 mcg, 40 mcg [contains lactose; diluent contains benzyl alcohol]
Caverject Impulse®: 10 mcg, 20 mcg [prefilled injection system; contains lactose; diluent contains benzyl alcohol]
Edex®: 10 mcg, 20 mcg, 40 mcg [contains lactose; packaged in kits containing diluent, syringe, and alcohol swab]
Injection, solution: 500 mcg/mL (1 mL)
Prostin VR Pediatric®: 500 mcg/mL (1 mL) [contains dehydrated alcohol]
Pellet, urethral (Muse®): 125 mcg (6s), 250 mcg (6s), 500 mcg (6s), 1000 mcg (6s)
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution: 10 mcg, 20 mcg, 40 mcg
Caverject®: 20 mcg, 40 mcg
Caverject Impulse®: 10 mcg, 20 mcg
Edex®: 10 mcg, 20 mcg, 40 mcg
Injection, solution: 500 mcg/mL (1 mL)
Prostin VR Pediatric®: 500 mcg/mL (1 mL)
Pellet, urethral: 125 mcg, 250 mcg, 500 mcg, 1000 mcg
Muse®: 125 mcg (6s), 250 mcg (6s), 500 mcg (6s), 1000 mcg (6s)
GENERIC EQUIVALENT AVAILABLE — Yes: Solution for injection
ADMINISTRATION — Erectile dysfunction: Use a 1/2 inch, 27- to 30-gauge needle. Inject into the dorsolateral aspect of the proximal third of the penis, avoiding visible veins; alternate side of the penis for injections.
USE
Prostin VR Pediatric®: Temporary maintenance of patency of ductus arteriosus in neonates with ductal-dependent congenital heart disease until surgery can be performed. These defects include cyanotic (eg, pulmonary atresia, pulmonary stenosis, tricuspid atresia, Fallot's tetralogy, transposition of the great vessels) and acyanotic (eg, interruption of aortic arch, coarctation of aorta, hypoplastic left ventricle) heart disease.
Caverject®: Treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology; adjunct in the diagnosis of erectile dysfunction
Edex®, Muse®: Treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology
USE - UNLABELED / INVESTIGATIONAL — Investigational: Treatment of pulmonary hypertension in infants and children with congenital heart defects with left-to-right shunts
ADVERSE REACTIONS SIGNIFICANT
Intraurethral:
>10%: Genitourinary: Penile pain, urethral burning
2% to 10%:
Central nervous system: Headache, dizziness, pain
Genitourinary: Vaginal itching (female partner), testicular pain, urethral bleeding (minor)
<2%>10%: Genitourinary: Penile pain
1% to 10%:
Cardiovascular: Hypertension
Central nervous system: Headache, dizziness
Genitourinary: Prolonged erection (>4 hours, 4%), penile fibrosis, penis disorder, penile rash, penile edema
Local: Injection site hematoma and/or bruising
<1%>10%:
Cardiovascular: Flushing
Central nervous system: Fever
Respiratory: Apnea
1% to 10%:
Cardiovascular: Bradycardia, hyper-/hypotension, tachycardia, cardiac arrest, edema
Central nervous system: Seizures, headache, dizziness
Endocrine & metabolic: Hypokalemia
Gastrointestinal: Diarrhea
Hematologic: Disseminated intravascular coagulation
Neuromuscular & skeletal: Back pain
Respiratory: Upper respiratory infection, flu syndrome, sinusitis, nasal congestion, cough
Miscellaneous: Sepsis, localized pain in structures other than the injection site
<1%>120 hours has been associated with antral hyperplasia and gastric outlet obstruction.
Special populations: Neonates: Use with caution in neonates with bleeding tendencies.
Dosage form specific issues: Muse®: When used in erectile dysfunction, syncope occurring within 1 hour of administration has been reported. The potential for drug-drug interactions may occur when prescribed concomitantly with antihypertensives. Some lowering of blood pressure may occur without symptoms, and swelling of leg veins, leg pain, perineal pain, and rapid pulse have been reported in <2%>4 hours to a prescriber immediately; inform a prescriber as soon as possible if any new penile pain, nodules, hard tissue, or signs of infection develop; the risk of transmission of blood-borne diseases is increased with use of alprostadil injections since a small amount of bleeding at the injection site is possible. Do not drive or operate heavy machinery within 1 hour of administration.
(For additional information see "Alprostadil: Patient drug information")
Erectile dysfunction: If the patient is going to be self-injecting at home, carefully assess his aseptic technique for injection and knowledge of proper disposal of the syringe, needle, and vial. Observe for signs of infection, penile fibrosis, and significant pain or priapism
PHARMACOLOGIC CATEGORY
Prostaglandin
DOSING: ADULTS
Erectile dysfunction:
Intracavernous (Caverject®, Edex®): Individualize dose by careful titration; doses >40 mcg (Edex®) or >60 mcg (Caverject®) are not recommended: Initial dose must be titrated in physician's office. Patient must stay in the physician's office until complete detumescence occurs; if there is no response, then the next higher dose may be given within 1 hour; if there is still no response, a 1-day interval before giving the next dose is recommended; increasing the dose or concentration in the treatment of impotence results in increasing pain and discomfort.
Vasculogenic, psychogenic, or mixed etiology: Initiate dosage titration at 2.5 mcg, increasing by 2.5 mcg to a dose of 5 mcg and then in increments of 5-10 mcg depending on the erectile response until the dose produces an erection suitable for intercourse, not lasting >1 hour; if there is absolutely no response to initial 2.5 mcg dose, the second dose may be increased to 7.5 mcg, followed by increments of 5-10 mcg
Neurogenic etiology (eg, spinal cord injury): Initiate dosage titration at 1.25 mcg, increasing to a dose of 2.5 mcg and then 5 mcg; increase further in increments 5 mcg until the dose is reached that produces an erection suitable for intercourse, not lasting >1 hour
Maintenance: Once appropriate dose has been determined, patient may self-administer injections at a frequency of no more than 3 times/week with at least 24 hours between doses
Intraurethral (Muse® Pellet):
Initial: 125-250 mcg
Maintenance: Administer as needed to achieve an erection; duration of action is about 30-60 minutes; use only two systems per 24-hour period
DOSING: PEDIATRIC
(For additional information see "Alprostadil: Pediatric drug information")
Patent ductus arteriosus I.V.:
Prostin VR Pediatric®: I.V. continuous infusion into a large vein, or alternatively through an umbilical artery catheter placed at the ductal opening: 0.05-0.1 mcg/kg/minute with therapeutic response, rate is reduced to lowest effective dosage. With unsatisfactory response, rate is increased gradually; maintenance: 0.01-0.4 mcg/kg/minute.
Note: PGE1 is usually given at an infusion rate of 0.1 mcg/kg/minute, but it is often possible to reduce the dosage to 1/2 or even 1/10 without losing the therapeutic effect. The mixing schedule is shown in the table.
Mixing Schedule
Note: 500 mcg equals 1 ampul. For a concentration of 2 mcg/mL, add 500 mcg to 250 mL; infuse at 0.05 mL/kg/minute (72 mL/kg/24 hours) For a concentration of 5 mcg/mL, add 500 mcg to 100 mL; infuse at 0.02 mL/kg/minute (28.8 mL/kg/24 hours) For a concentration of 10 mcg/mL, add 500 mcg to 50 mL; infuse at 0.01 mL/kg/minute (14.4 mL/kg/24 hours) For a concentration of 20 mcg/mL, add 500 mcg to 25 mL; infuse at 0.005 mL/kg/minute (7.2 mL/kg/24 hours)
Note: Therapeutic response is indicated by increased pH in those with acidosis or by an increase in oxygenation (PO2) usually evident within 30 minutes.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution:
Caverject®: 20 mcg, 40 mcg [contains lactose; diluent contains benzyl alcohol]
Caverject Impulse®: 10 mcg, 20 mcg [prefilled injection system; contains lactose; diluent contains benzyl alcohol]
Edex®: 10 mcg, 20 mcg, 40 mcg [contains lactose; packaged in kits containing diluent, syringe, and alcohol swab]
Injection, solution: 500 mcg/mL (1 mL)
Prostin VR Pediatric®: 500 mcg/mL (1 mL) [contains dehydrated alcohol]
Pellet, urethral (Muse®): 125 mcg (6s), 250 mcg (6s), 500 mcg (6s), 1000 mcg (6s)
DOSAGE FORMS: CONCISE
Injection, powder for reconstitution: 10 mcg, 20 mcg, 40 mcg
Caverject®: 20 mcg, 40 mcg
Caverject Impulse®: 10 mcg, 20 mcg
Edex®: 10 mcg, 20 mcg, 40 mcg
Injection, solution: 500 mcg/mL (1 mL)
Prostin VR Pediatric®: 500 mcg/mL (1 mL)
Pellet, urethral: 125 mcg, 250 mcg, 500 mcg, 1000 mcg
Muse®: 125 mcg (6s), 250 mcg (6s), 500 mcg (6s), 1000 mcg (6s)
GENERIC EQUIVALENT AVAILABLE — Yes: Solution for injection
ADMINISTRATION — Erectile dysfunction: Use a 1/2 inch, 27- to 30-gauge needle. Inject into the dorsolateral aspect of the proximal third of the penis, avoiding visible veins; alternate side of the penis for injections.
USE
Prostin VR Pediatric®: Temporary maintenance of patency of ductus arteriosus in neonates with ductal-dependent congenital heart disease until surgery can be performed. These defects include cyanotic (eg, pulmonary atresia, pulmonary stenosis, tricuspid atresia, Fallot's tetralogy, transposition of the great vessels) and acyanotic (eg, interruption of aortic arch, coarctation of aorta, hypoplastic left ventricle) heart disease.
Caverject®: Treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology; adjunct in the diagnosis of erectile dysfunction
Edex®, Muse®: Treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology
USE - UNLABELED / INVESTIGATIONAL — Investigational: Treatment of pulmonary hypertension in infants and children with congenital heart defects with left-to-right shunts
ADVERSE REACTIONS SIGNIFICANT
Intraurethral:
>10%: Genitourinary: Penile pain, urethral burning
2% to 10%:
Central nervous system: Headache, dizziness, pain
Genitourinary: Vaginal itching (female partner), testicular pain, urethral bleeding (minor)
<2%>10%: Genitourinary: Penile pain
1% to 10%:
Cardiovascular: Hypertension
Central nervous system: Headache, dizziness
Genitourinary: Prolonged erection (>4 hours, 4%), penile fibrosis, penis disorder, penile rash, penile edema
Local: Injection site hematoma and/or bruising
<1%>10%:
Cardiovascular: Flushing
Central nervous system: Fever
Respiratory: Apnea
1% to 10%:
Cardiovascular: Bradycardia, hyper-/hypotension, tachycardia, cardiac arrest, edema
Central nervous system: Seizures, headache, dizziness
Endocrine & metabolic: Hypokalemia
Gastrointestinal: Diarrhea
Hematologic: Disseminated intravascular coagulation
Neuromuscular & skeletal: Back pain
Respiratory: Upper respiratory infection, flu syndrome, sinusitis, nasal congestion, cough
Miscellaneous: Sepsis, localized pain in structures other than the injection site
<1%>120 hours has been associated with antral hyperplasia and gastric outlet obstruction.
Special populations: Neonates: Use with caution in neonates with bleeding tendencies.
Dosage form specific issues: Muse®: When used in erectile dysfunction, syncope occurring within 1 hour of administration has been reported. The potential for drug-drug interactions may occur when prescribed concomitantly with antihypertensives. Some lowering of blood pressure may occur without symptoms, and swelling of leg veins, leg pain, perineal pain, and rapid pulse have been reported in <2%>4 hours to a prescriber immediately; inform a prescriber as soon as possible if any new penile pain, nodules, hard tissue, or signs of infection develop; the risk of transmission of blood-borne diseases is increased with use of alprostadil injections since a small amount of bleeding at the injection site is possible. Do not drive or operate heavy machinery within 1 hour of administration.
(For additional information see "Alprostadil: Patient drug information")
Erectile dysfunction: If the patient is going to be self-injecting at home, carefully assess his aseptic technique for injection and knowledge of proper disposal of the syringe, needle, and vial. Observe for signs of infection, penile fibrosis, and significant pain or priapism
Alprazolam
U.S. BRAND NAMES — Alprazolam Intensol®; Niravam™; Xanax XR®; Xanax®
PHARMACOLOGIC CATEGORY
Benzodiazepine
DOSING: ADULTS — Note: Treatment >4 months should be re-evaluated to determine the patient's continued need for the drug
Anxiety: Oral: Immediate release: Effective doses are 0.5-4 mg/day in divided doses; the manufacturer recommends starting at 0.25-0.5 mg 3 times/day; titrate dose upward; usual maximum: 4 mg/day. Patients requiring doses >4 mg/day should be increased cautiously. Periodic reassessment and consideration of dosage reduction is recommended.
Anxiety associated with depression: Oral: Immediate release: Average dose required: 2.5-3 mg/day in divided doses
Ethanol withdrawal (unlabeled use): Oral: Immediate release: Usual dose: 2-2.5 mg/day in divided doses
Panic disorder: Oral:
Immediate release: Initial: 0.5 mg 3 times/day; dose may be increased every 3-4 days in increments 1 mg/day. Mean effective dosage: 5-6 mg/day; many patients obtain relief at 2 mg/day, as much as 10 mg/day may be required
Extended release: 0.5-1 mg once daily; may increase dose every 3-4 days in increments 1 mg/day (range: 3-6 mg/day)
Switching from immediate release to extended release: Patients may be switched to extended release tablets by taking the total daily dose of the immediate release tablets and giving it once daily using the extended release preparation.
Preoperative sedation: Oral: 0.5 mg in evening at bedtime and 0.5 mg 1 hour before procedure
Dose reduction: Abrupt discontinuation should be avoided. Daily dose may be decreased by 0.5 mg every 3 days, however, some patients may require a slower reduction. If withdrawal symptoms occur, resume previous dose and discontinue on a less rapid schedule.
DOSING: PEDIATRIC
(For additional information see "Alprazolam: Pediatric drug information")
Anxiety (unlabeled use): Oral: Immediate release: Initial: 0.005 mg/kg/dose or 0.125 mg/dose 3 times/day; increase in increments of 0.125-0.25 mg, up to a maximum of 0.02 mg/kg/dose or 0.06 mg/kg/day (0.375-3 mg/day). See "Dose Reduction" comment in adult dosing.
Note: Treatment >4 months should be re-evaluated to determine the patient's continued need for the drug.
DOSING: ELDERLY — Initial: 0.125-0.25 mg twice daily; increase by 0.125 mg/day as needed. The smallest effective dose should be used.
Immediate release: Initial 0.25 mg 2-3 times/day
Extended release: Initial: 0.5 mg once daily
DOSING: RENAL IMPAIRMENT — No guidelines for adjustment; use caution.
DOSING: HEPATIC IMPAIRMENT — Oral: Reduce dose by 50% to 60% or avoid in cirrhosis.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, oral [concentrate]:
Alprazolam Intensol®: 1 mg/mL (30 mL)
Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Xanax®: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Tablet, extended release: 0.5 mg, 1 mg, 2 mg, 3 mg
Xanax XR®: 0.5 mg, 1 mg, 2 mg, 3 mg
Tablet, orally disintegrating [scored]:
Niravam™: 0.25 mg, 0.5 mg, 1 mg, 2 mg [orange flavor]
DOSAGE FORMS: CONCISE
Solution, oral [concentrate]:
Alprazolam Intensol®: 1 mg/mL
Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Xanax®: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Tablet, extended release: 0.5 mg, 1 mg, 2 mg, 3 mg
Xanax XR®: 0.5 mg, 1 mg, 2 mg, 3 mg
Tablet, orally disintegrating [scored]:
Niravam™: 0.25 mg, 0.5 mg, 1 mg, 2 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Extended release tablet, immediate release tablet
ADMINISTRATION
Immediate release preparations: Can be administered sublingually with comparable onset and completeness of absorption.
Extended release tablet: Should be taken once daily in the morning; do not crush, break, or chew.
Orally-disintegrating tablets: Using dry hands, place tablet on top of tongue. If using one-half of tablet, immediately discard remaining half (may not remain stable). Administration with water is not necessary.
USE — Treatment of anxiety disorder (GAD); panic disorder, with or without agoraphobia; anxiety associated with depression
USE - UNLABELED / INVESTIGATIONAL — Anxiety in children
ADVERSE REACTIONS SIGNIFICANT
>10%:
Central nervous system: Abnormal coordination, cognitive disorder, depression, drowsiness, fatigue, irritability, lightheadedness, memory impairment, sedation, somnolence
Gastrointestinal: Appetite increased/decreased, constipation, salivation decreased, weight gain/loss, xerostomia
Genitourinary: Micturition difficulty
Neuromuscular & skeletal: Dysarthria
1% to 10%:
Cardiovascular: Hypotension
Central nervous system: Agitation, attention disturbance, confusion, depersonalization, derealization, disorientation, disinhibition, dizziness, dream abnormalities, fear, hallucinations, hypersomnia, nightmares, seizure, talkativeness
Dermatologic: Dermatitis, pruritus, rash
Endocrine & metabolic: Libido decreased/increased, menstrual disorders
Gastrointestinal: Salivation increased
Genitourinary: Incontinence
Hepatic: Bilirubin increased, jaundice, liver enzymes increased
Neuromuscular & skeletal: Arthralgia, ataxia, myalgia, paresthesia
Ocular: Diplopia
Respiratory: Allergic rhinitis, dyspnea
<1%>10 days). Hepatic impairment: Use with caution in patients with hepatic impairment. Impaired gag reflux: Use with caution in patients with an impaired gag reflux. Renal impairment: Use with caution in patients with renal impairment or predisposition to urate nephropathy; has weak uricosuric properties. Respiratory disease: Use with caution in patients with respiratory disease.
Concurrent drug therapy issues: CNS depressants/psychoactive medications: Use with caution in patients receiving other CNS depressants or psychoactive medication; effects with other sedative drugs or ethanol may be potentiated. High potential for interactions: Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates (see Drug Interactions); consider alternative agents that avoid or lessen the potential for CYP-mediated interactions.
Special populations: Debilitated patients: Use with caution in debilitated patients. Elderly: Use with caution in the elderly; benzodiazepines have been associated with falls and traumatic injury. Fall risk: Use with extreme caution in patients who are at risk of falls; benzodiazepines have been associated with falls and traumatic injury. Obese patients: Use with caution in obese patients; may have prolonged action when discontinued.
Other warnings/precautions: Appropriate use: Does not have analgesic, antidepressant, or antipsychotic properties. Breakthrough anxiety: At the end of dosing interval, breakthrough anxiety may occur. Withdrawal: Rebound or withdrawal symptoms, including seizures, may occur 18 hours to 3 days following abrupt discontinuation or large decreases in dose (more common in patients receiving >4 mg/day or prolonged treatment). Use caution when reducing dose or withdrawing therapy; decrease slowly and monitor for withdrawal symptoms. Flumazenil may cause withdrawal in patients receiving long-term benzodiazepine therapy.
RESTRICTIONS — C-IV
DRUG INTERACTIONS — Substrate of CYP3A4 (major)
CNS depressants: Sedative effects and/or respiratory depression may be additive with CNS depressants. Includes ethanol, barbiturates, opioid analgesics, and other sedative agents; monitor for increased effect.
CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of alprazolam. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.
CYP3A4 inhibitors: May increase the levels/effects of alprazolam. Example inhibitors include azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin, and verapamil. Contraindicated with itraconazole and ketoconazole.
Fluoxetine: May increase plasma concentrations/effects of alprazolam.
Oral contraceptives: May increase serum levels/effects of alprazolam.
Theophylline: May partially antagonize some of the effects of benzodiazepines; monitor for decreased response; may require higher doses for sedation.
Tricyclic antidepressants: Plasma concentrations of imipramine and desipramine have been reported to be increased 31% and 20%, respectively, by concomitant administration; monitor.
ETHANOL / NUTRITION / HERB INTERACTIONS
Cigarette smoking: May decrease alprazolam concentrations up to 50%.
Ethanol: Avoid ethanol (may increase CNS depression).
Food: Alprazolam serum concentration is unlikely to be increased by grapefruit juice because of alprazolam's high oral bioavailability. The Cmax of the extended release formulation is increased by 25% when a high-fat meal is given 2 hours before dosing. Tmax is decreased 30% when food is given immediately prior to dose. Tmax is increased by 30% when food is given 1 hour after dose.
Herb/Nutraceutical: St John's wort may decrease alprazolam levels. Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).
PREGNANCY RISK FACTOR — D (show table)
PREGNANCY IMPLICATIONS — Benzodiazepines have the potential to cause harm to the fetus, particularly when administered during the first trimester. In addition, withdrawal symptoms may occur in the neonate following in utero exposure. Use during pregnancy should be avoided.
LACTATION — Enters breast milk/not recommended (AAP rates "of concern")
BREAST-FEEDING CONSIDERATIONS — Symptoms of withdrawal, lethargy, and loss of body weight have been reported in infants exposed to alprazolam and/or benzodiazepines while nursing. Breast-feeding is not recommended.
PRICING — (data from drugstore.com)
Tablet, 24-hour (Alprazolam)
0.5 mg (30): $31.99
1 mg (30): $69.99
2 mg (30): $106.45
Tablet, 24-hour (Xanax XR)
0.5 mg (30): $70.04
1 mg (30): $89.89
2 mg (30): $116.75
3 mg (30): $175.13
Tablet, orally-disintegrating (Niravam)
0.5 mg (30): $41.99
0.25 mg (30): $33.99
1 mg (30): $56.99
2 mg (30): $94.99
Tablets (Alprazolam)
0.5 mg (30): $7.99
0.25 mg (30): $9.99
1 mg (30): $7.99
2 mg (30): $8.99
Tablets (Xanax)
0.5 mg (30): $40.85
0.25 mg (30): $34.09
1 mg (30): $54.86
2 mg (30): $86.39
MONITORING PARAMETERS — Respiratory and cardiovascular status
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include somnolence, confusion, coma, and diminished reflexes. Treatment for benzodiazepine overdose is supportive. Mechanical ventilation is rarely required. Flumazenil has been shown to selectively block the binding of benzodiazepines to CNS receptors, resulting in a reversal of benzodiazepine-induced sedation; however, its use may not alter the course of overdose.
CANADIAN BRAND NAMES — Alti-Alprazolam; Apo-Alpraz® TS; Apo-Alpraz®; Gen-Alprazolam; Novo-Alprazol; Nu-Alprax; Xanax TS™; Xanax®
INTERNATIONAL BRAND NAMES — Aceprax (PY, UY); Afobam (PL); Alcelam (TH); Alganax (ID); Alnax (TH); Alpaz (PE); Alplax (AR); Alpralid (IL); Alpram (KR); Alprax (AU, HK, IN, TH); Alprazomerck (PL); Alprocontin (IN); Alprox (IL, PL, TW); Alti-Alprazolam (CA); Alviz (ID); Alzam (ZA); Alzax (KR); Alzolam (IN); Anax (TH); Anpress (TH); Ansiopax (CL); Anxirid (ZA); Apo-Alpraz (CA, SG); Apo-Alpraz TS (CA); Apraz (BR); Azor (ZA); Calmlet (ID); Cassadan (DE); Constan (JP); Daclor (DO); Dixin (CO); Drimpam (ZA); Feprax (ID); Frontal (BR); Frontin (PL); Gen-Alprazolam (CA); Helex (HR); Kalma (AU, TW); Kinax (TW); Marzolam (TH); Nalion (HK); Neupax (MX); Neurol (PL); Nirvan (CO); Novo-Alprazol (CA); Nu-Alprax (CA); Pacyl (IN); Panix (ZA); Pharnax (TH); Prazol (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Prinox (AR); Renax (HK); Solanax (JP); Tafil (CR, DE, DK, GT, HN, MX, NI, PA, SV, VE); Tafil D (MU); Tensivan (CO); Trankimazin (ES); Tranquinal (BR, EC, PE, PY, UY); Tricalma (CL, PE); Valeans (IT); Xanacine (TH); Xanagis (IL); Xanax (AE, AN, AR, AU, BB, BE, BF, BG, BH, BJ, BM, BS, BZ, CA, CH, CI, CO, CY, CZ, DE, EC, EE, EG, ET, FR, GB, GH, GM, GN, GR, GY, HK, HR, HU, IE, IQ, IR, IT, JM, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MY, NE, NG, NL, NZ, OM, PE, PK, PL, PT, QA, SA, SC, SD, SL, SN, SR, SY, TH, TT, TW, TZ, UG, YE, ZM, ZW); Xanax SR (SG); Xanax TS® (CA); Xanax XR (TW); Xanolam (ZA); Xanor (AT, FI, NO, PH, SE, ZA); Xanor XR (PH); Zacetin (KR); Zanapam (AE, BH, CY, EG, IL, IQ, IR, JO, KR, KW, LB, LY, OM, QA, SA, SY, YE); Zolam (IN); Zolarem (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TZ, UG, YE, ZA, ZM, ZW); Zoldac (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Zomiren (PL); Zopax (ZA); Zotran (CL); Zypraz (ID)
MECHANISM OF ACTION — Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.
PHARMACODYNAMICS / KINETICS
Distribution: Vd: 0.9-1.2 L/kg; enters breast milk
Protein binding: 80%
Metabolism: Hepatic via CYP3A4; forms two active metabolites (4-hydroxyalprazolam and alpha-hydroxyalprazolam)
Bioavailability: 90%
Half-life elimination:
Adults: 11.2 hours (range: 6.3-26.9)
Elderly: 16.3 hours (range: 9-26.9 hours)
Alcoholic liver disease: 19.7 hours (range: 5.8-65.3 hours)
Obesity: 21.8 hours (range: 9.9-40.4 hours)
Time to peak, serum: 1-2 hours
Excretion: Urine (as unchanged drug and metabolites)
PATIENT INFORMATION — Avoid alcohol and other CNS depressants; avoid activities needing good psychomotor coordination until CNS effects are known; drug may cause physical or psychological dependence; avoid abrupt discontinuation after prolonged use; do not crush, break, or chew extended release tablets
PHARMACOLOGIC CATEGORY
Benzodiazepine
DOSING: ADULTS — Note: Treatment >4 months should be re-evaluated to determine the patient's continued need for the drug
Anxiety: Oral: Immediate release: Effective doses are 0.5-4 mg/day in divided doses; the manufacturer recommends starting at 0.25-0.5 mg 3 times/day; titrate dose upward; usual maximum: 4 mg/day. Patients requiring doses >4 mg/day should be increased cautiously. Periodic reassessment and consideration of dosage reduction is recommended.
Anxiety associated with depression: Oral: Immediate release: Average dose required: 2.5-3 mg/day in divided doses
Ethanol withdrawal (unlabeled use): Oral: Immediate release: Usual dose: 2-2.5 mg/day in divided doses
Panic disorder: Oral:
Immediate release: Initial: 0.5 mg 3 times/day; dose may be increased every 3-4 days in increments 1 mg/day. Mean effective dosage: 5-6 mg/day; many patients obtain relief at 2 mg/day, as much as 10 mg/day may be required
Extended release: 0.5-1 mg once daily; may increase dose every 3-4 days in increments 1 mg/day (range: 3-6 mg/day)
Switching from immediate release to extended release: Patients may be switched to extended release tablets by taking the total daily dose of the immediate release tablets and giving it once daily using the extended release preparation.
Preoperative sedation: Oral: 0.5 mg in evening at bedtime and 0.5 mg 1 hour before procedure
Dose reduction: Abrupt discontinuation should be avoided. Daily dose may be decreased by 0.5 mg every 3 days, however, some patients may require a slower reduction. If withdrawal symptoms occur, resume previous dose and discontinue on a less rapid schedule.
DOSING: PEDIATRIC
(For additional information see "Alprazolam: Pediatric drug information")
Anxiety (unlabeled use): Oral: Immediate release: Initial: 0.005 mg/kg/dose or 0.125 mg/dose 3 times/day; increase in increments of 0.125-0.25 mg, up to a maximum of 0.02 mg/kg/dose or 0.06 mg/kg/day (0.375-3 mg/day). See "Dose Reduction" comment in adult dosing.
Note: Treatment >4 months should be re-evaluated to determine the patient's continued need for the drug.
DOSING: ELDERLY — Initial: 0.125-0.25 mg twice daily; increase by 0.125 mg/day as needed. The smallest effective dose should be used.
Immediate release: Initial 0.25 mg 2-3 times/day
Extended release: Initial: 0.5 mg once daily
DOSING: RENAL IMPAIRMENT — No guidelines for adjustment; use caution.
DOSING: HEPATIC IMPAIRMENT — Oral: Reduce dose by 50% to 60% or avoid in cirrhosis.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, oral [concentrate]:
Alprazolam Intensol®: 1 mg/mL (30 mL)
Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Xanax®: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Tablet, extended release: 0.5 mg, 1 mg, 2 mg, 3 mg
Xanax XR®: 0.5 mg, 1 mg, 2 mg, 3 mg
Tablet, orally disintegrating [scored]:
Niravam™: 0.25 mg, 0.5 mg, 1 mg, 2 mg [orange flavor]
DOSAGE FORMS: CONCISE
Solution, oral [concentrate]:
Alprazolam Intensol®: 1 mg/mL
Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Xanax®: 0.25 mg, 0.5 mg, 1 mg, 2 mg
Tablet, extended release: 0.5 mg, 1 mg, 2 mg, 3 mg
Xanax XR®: 0.5 mg, 1 mg, 2 mg, 3 mg
Tablet, orally disintegrating [scored]:
Niravam™: 0.25 mg, 0.5 mg, 1 mg, 2 mg
GENERIC EQUIVALENT AVAILABLE — Yes: Extended release tablet, immediate release tablet
ADMINISTRATION
Immediate release preparations: Can be administered sublingually with comparable onset and completeness of absorption.
Extended release tablet: Should be taken once daily in the morning; do not crush, break, or chew.
Orally-disintegrating tablets: Using dry hands, place tablet on top of tongue. If using one-half of tablet, immediately discard remaining half (may not remain stable). Administration with water is not necessary.
USE — Treatment of anxiety disorder (GAD); panic disorder, with or without agoraphobia; anxiety associated with depression
USE - UNLABELED / INVESTIGATIONAL — Anxiety in children
ADVERSE REACTIONS SIGNIFICANT
>10%:
Central nervous system: Abnormal coordination, cognitive disorder, depression, drowsiness, fatigue, irritability, lightheadedness, memory impairment, sedation, somnolence
Gastrointestinal: Appetite increased/decreased, constipation, salivation decreased, weight gain/loss, xerostomia
Genitourinary: Micturition difficulty
Neuromuscular & skeletal: Dysarthria
1% to 10%:
Cardiovascular: Hypotension
Central nervous system: Agitation, attention disturbance, confusion, depersonalization, derealization, disorientation, disinhibition, dizziness, dream abnormalities, fear, hallucinations, hypersomnia, nightmares, seizure, talkativeness
Dermatologic: Dermatitis, pruritus, rash
Endocrine & metabolic: Libido decreased/increased, menstrual disorders
Gastrointestinal: Salivation increased
Genitourinary: Incontinence
Hepatic: Bilirubin increased, jaundice, liver enzymes increased
Neuromuscular & skeletal: Arthralgia, ataxia, myalgia, paresthesia
Ocular: Diplopia
Respiratory: Allergic rhinitis, dyspnea
<1%>10 days). Hepatic impairment: Use with caution in patients with hepatic impairment. Impaired gag reflux: Use with caution in patients with an impaired gag reflux. Renal impairment: Use with caution in patients with renal impairment or predisposition to urate nephropathy; has weak uricosuric properties. Respiratory disease: Use with caution in patients with respiratory disease.
Concurrent drug therapy issues: CNS depressants/psychoactive medications: Use with caution in patients receiving other CNS depressants or psychoactive medication; effects with other sedative drugs or ethanol may be potentiated. High potential for interactions: Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates (see Drug Interactions); consider alternative agents that avoid or lessen the potential for CYP-mediated interactions.
Special populations: Debilitated patients: Use with caution in debilitated patients. Elderly: Use with caution in the elderly; benzodiazepines have been associated with falls and traumatic injury. Fall risk: Use with extreme caution in patients who are at risk of falls; benzodiazepines have been associated with falls and traumatic injury. Obese patients: Use with caution in obese patients; may have prolonged action when discontinued.
Other warnings/precautions: Appropriate use: Does not have analgesic, antidepressant, or antipsychotic properties. Breakthrough anxiety: At the end of dosing interval, breakthrough anxiety may occur. Withdrawal: Rebound or withdrawal symptoms, including seizures, may occur 18 hours to 3 days following abrupt discontinuation or large decreases in dose (more common in patients receiving >4 mg/day or prolonged treatment). Use caution when reducing dose or withdrawing therapy; decrease slowly and monitor for withdrawal symptoms. Flumazenil may cause withdrawal in patients receiving long-term benzodiazepine therapy.
RESTRICTIONS — C-IV
DRUG INTERACTIONS — Substrate of CYP3A4 (major)
CNS depressants: Sedative effects and/or respiratory depression may be additive with CNS depressants. Includes ethanol, barbiturates, opioid analgesics, and other sedative agents; monitor for increased effect.
CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of alprazolam. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.
CYP3A4 inhibitors: May increase the levels/effects of alprazolam. Example inhibitors include azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin, and verapamil. Contraindicated with itraconazole and ketoconazole.
Fluoxetine: May increase plasma concentrations/effects of alprazolam.
Oral contraceptives: May increase serum levels/effects of alprazolam.
Theophylline: May partially antagonize some of the effects of benzodiazepines; monitor for decreased response; may require higher doses for sedation.
Tricyclic antidepressants: Plasma concentrations of imipramine and desipramine have been reported to be increased 31% and 20%, respectively, by concomitant administration; monitor.
ETHANOL / NUTRITION / HERB INTERACTIONS
Cigarette smoking: May decrease alprazolam concentrations up to 50%.
Ethanol: Avoid ethanol (may increase CNS depression).
Food: Alprazolam serum concentration is unlikely to be increased by grapefruit juice because of alprazolam's high oral bioavailability. The Cmax of the extended release formulation is increased by 25% when a high-fat meal is given 2 hours before dosing. Tmax is decreased 30% when food is given immediately prior to dose. Tmax is increased by 30% when food is given 1 hour after dose.
Herb/Nutraceutical: St John's wort may decrease alprazolam levels. Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).
PREGNANCY RISK FACTOR — D (show table)
PREGNANCY IMPLICATIONS — Benzodiazepines have the potential to cause harm to the fetus, particularly when administered during the first trimester. In addition, withdrawal symptoms may occur in the neonate following in utero exposure. Use during pregnancy should be avoided.
LACTATION — Enters breast milk/not recommended (AAP rates "of concern")
BREAST-FEEDING CONSIDERATIONS — Symptoms of withdrawal, lethargy, and loss of body weight have been reported in infants exposed to alprazolam and/or benzodiazepines while nursing. Breast-feeding is not recommended.
PRICING — (data from drugstore.com)
Tablet, 24-hour (Alprazolam)
0.5 mg (30): $31.99
1 mg (30): $69.99
2 mg (30): $106.45
Tablet, 24-hour (Xanax XR)
0.5 mg (30): $70.04
1 mg (30): $89.89
2 mg (30): $116.75
3 mg (30): $175.13
Tablet, orally-disintegrating (Niravam)
0.5 mg (30): $41.99
0.25 mg (30): $33.99
1 mg (30): $56.99
2 mg (30): $94.99
Tablets (Alprazolam)
0.5 mg (30): $7.99
0.25 mg (30): $9.99
1 mg (30): $7.99
2 mg (30): $8.99
Tablets (Xanax)
0.5 mg (30): $40.85
0.25 mg (30): $34.09
1 mg (30): $54.86
2 mg (30): $86.39
MONITORING PARAMETERS — Respiratory and cardiovascular status
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include somnolence, confusion, coma, and diminished reflexes. Treatment for benzodiazepine overdose is supportive. Mechanical ventilation is rarely required. Flumazenil has been shown to selectively block the binding of benzodiazepines to CNS receptors, resulting in a reversal of benzodiazepine-induced sedation; however, its use may not alter the course of overdose.
CANADIAN BRAND NAMES — Alti-Alprazolam; Apo-Alpraz® TS; Apo-Alpraz®; Gen-Alprazolam; Novo-Alprazol; Nu-Alprax; Xanax TS™; Xanax®
INTERNATIONAL BRAND NAMES — Aceprax (PY, UY); Afobam (PL); Alcelam (TH); Alganax (ID); Alnax (TH); Alpaz (PE); Alplax (AR); Alpralid (IL); Alpram (KR); Alprax (AU, HK, IN, TH); Alprazomerck (PL); Alprocontin (IN); Alprox (IL, PL, TW); Alti-Alprazolam (CA); Alviz (ID); Alzam (ZA); Alzax (KR); Alzolam (IN); Anax (TH); Anpress (TH); Ansiopax (CL); Anxirid (ZA); Apo-Alpraz (CA, SG); Apo-Alpraz TS (CA); Apraz (BR); Azor (ZA); Calmlet (ID); Cassadan (DE); Constan (JP); Daclor (DO); Dixin (CO); Drimpam (ZA); Feprax (ID); Frontal (BR); Frontin (PL); Gen-Alprazolam (CA); Helex (HR); Kalma (AU, TW); Kinax (TW); Marzolam (TH); Nalion (HK); Neupax (MX); Neurol (PL); Nirvan (CO); Novo-Alprazol (CA); Nu-Alprax (CA); Pacyl (IN); Panix (ZA); Pharnax (TH); Prazol (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Prinox (AR); Renax (HK); Solanax (JP); Tafil (CR, DE, DK, GT, HN, MX, NI, PA, SV, VE); Tafil D (MU); Tensivan (CO); Trankimazin (ES); Tranquinal (BR, EC, PE, PY, UY); Tricalma (CL, PE); Valeans (IT); Xanacine (TH); Xanagis (IL); Xanax (AE, AN, AR, AU, BB, BE, BF, BG, BH, BJ, BM, BS, BZ, CA, CH, CI, CO, CY, CZ, DE, EC, EE, EG, ET, FR, GB, GH, GM, GN, GR, GY, HK, HR, HU, IE, IQ, IR, IT, JM, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MY, NE, NG, NL, NZ, OM, PE, PK, PL, PT, QA, SA, SC, SD, SL, SN, SR, SY, TH, TT, TW, TZ, UG, YE, ZM, ZW); Xanax SR (SG); Xanax TS® (CA); Xanax XR (TW); Xanolam (ZA); Xanor (AT, FI, NO, PH, SE, ZA); Xanor XR (PH); Zacetin (KR); Zanapam (AE, BH, CY, EG, IL, IQ, IR, JO, KR, KW, LB, LY, OM, QA, SA, SY, YE); Zolam (IN); Zolarem (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TZ, UG, YE, ZA, ZM, ZW); Zoldac (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Zomiren (PL); Zopax (ZA); Zotran (CL); Zypraz (ID)
MECHANISM OF ACTION — Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.
PHARMACODYNAMICS / KINETICS
Distribution: Vd: 0.9-1.2 L/kg; enters breast milk
Protein binding: 80%
Metabolism: Hepatic via CYP3A4; forms two active metabolites (4-hydroxyalprazolam and alpha-hydroxyalprazolam)
Bioavailability: 90%
Half-life elimination:
Adults: 11.2 hours (range: 6.3-26.9)
Elderly: 16.3 hours (range: 9-26.9 hours)
Alcoholic liver disease: 19.7 hours (range: 5.8-65.3 hours)
Obesity: 21.8 hours (range: 9.9-40.4 hours)
Time to peak, serum: 1-2 hours
Excretion: Urine (as unchanged drug and metabolites)
PATIENT INFORMATION — Avoid alcohol and other CNS depressants; avoid activities needing good psychomotor coordination until CNS effects are known; drug may cause physical or psychological dependence; avoid abrupt discontinuation after prolonged use; do not crush, break, or chew extended release tablets
Thursday, April 17, 2008
Alpha-1 proteinase inhibitor
U.S. BRAND NAMES — Aralast; Prolastin®; Zemaira®
PHARMACOLOGIC CATEGORY Antitrypsin Deficiency Agent
DOSING: ADULTS — Alpha1-antitrypsin deficiency: I.V.: 60 mg/kg once weekly
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Aralast, Prolastin®: 500 mg, 1000 mg [packaged with diluent]
Zemaira®: 1000 mg [packaged with diluent]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution[preservative free]: Aralast, Prolastin®: 500 mg, 1000 mg Zemaira®: 1000 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For I.V. infusion only; reduce rate or temporarily discontinue infusion if adverse effects occur. Infuse at ~0.08 mL/kg/minute; actual rate may be increased or decreased based on patient response. Emergency equipment (including epinephrine) should be available during infusion. Do not mix with other agents or solutions.
USE — Replacement therapy in congenital alpha1-antitrypsin deficiency with clinical emphysema
ADVERSE REACTIONS SIGNIFICANT >10%: Hepatic: ALT/AST increased (11%; ~4 times ULN)
1% to 10%: Respiratory: Pharyngitis (2%)
<1% (Limited to important or life-threatening): Allergic reactions, bilateral pulmonary infiltrates, bronchitis, chest pain, chills, cough increased, dizziness, dyspnea, fever <102ºF (delayed up to 12 hours after treatment), flu-like syndrome, headache, hypotension, leukocytosis, lightheadedness, pain, pruritus, rash, sinusitis, somnolence, tachycardia, vasodilation, vision abnormal. Severe reactions (anaphylaxis) may occur in patients with anti-IgA antibody.
CONTRAINDICATIONS — Hypersensitivity to any component of the formulation or other A1-PI products; selective IgA deficiency with known anti-IgA antibody
WARNINGS / PRECAUTIONS — Use caution in patients at risk for fluid overload. Products are made from pooled human plasma; risk of infection is theoretical, however, any infections thought to be transmitted by these products should be reported to the manufacturer. Hepatitis B immunization may be considered. Safety and efficacy in pediatric patients have not been established.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Sodium content of 1 L after reconstitution:
Aralast™: 230 mEq/L
Prolastin®: 100-210 mEq/L
MONITORING PARAMETERS — Alpha1-PI serum levels; vital signs during infusion
CANADIAN BRAND NAMES — Prolastin®
INTERNATIONAL BRAND NAMES — Prolastin (CA)
MECHANISM OF ACTION — Alpha1-antitrypsin (AAT) is the principle protease inhibitor in serum. Its major physiologic role is to render proteolytic enzymes (secreted during inflammation) inactive. A decrease in AAT, as seen in congenital AAT deficiency, leads to increased elastic damage in the lung, causing emphysema.
PHARMACODYNAMICS / KINETICS Half-life elimination: Metabolic: 5.9 days (Aralast™)
Time to peak, serum: Threshold levels achieved after 3 weeks
PATIENT INFORMATION — This medication is given by injection only.
PHARMACOLOGIC CATEGORY Antitrypsin Deficiency Agent
DOSING: ADULTS — Alpha1-antitrypsin deficiency: I.V.: 60 mg/kg once weekly
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Aralast, Prolastin®: 500 mg, 1000 mg [packaged with diluent]
Zemaira®: 1000 mg [packaged with diluent]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution[preservative free]: Aralast, Prolastin®: 500 mg, 1000 mg Zemaira®: 1000 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For I.V. infusion only; reduce rate or temporarily discontinue infusion if adverse effects occur. Infuse at ~0.08 mL/kg/minute; actual rate may be increased or decreased based on patient response. Emergency equipment (including epinephrine) should be available during infusion. Do not mix with other agents or solutions.
USE — Replacement therapy in congenital alpha1-antitrypsin deficiency with clinical emphysema
ADVERSE REACTIONS SIGNIFICANT >10%: Hepatic: ALT/AST increased (11%; ~4 times ULN)
1% to 10%: Respiratory: Pharyngitis (2%)
<1% (Limited to important or life-threatening): Allergic reactions, bilateral pulmonary infiltrates, bronchitis, chest pain, chills, cough increased, dizziness, dyspnea, fever <102ºF (delayed up to 12 hours after treatment), flu-like syndrome, headache, hypotension, leukocytosis, lightheadedness, pain, pruritus, rash, sinusitis, somnolence, tachycardia, vasodilation, vision abnormal. Severe reactions (anaphylaxis) may occur in patients with anti-IgA antibody.
CONTRAINDICATIONS — Hypersensitivity to any component of the formulation or other A1-PI products; selective IgA deficiency with known anti-IgA antibody
WARNINGS / PRECAUTIONS — Use caution in patients at risk for fluid overload. Products are made from pooled human plasma; risk of infection is theoretical, however, any infections thought to be transmitted by these products should be reported to the manufacturer. Hepatitis B immunization may be considered. Safety and efficacy in pediatric patients have not been established.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Sodium content of 1 L after reconstitution:
Aralast™: 230 mEq/L
Prolastin®: 100-210 mEq/L
MONITORING PARAMETERS — Alpha1-PI serum levels; vital signs during infusion
CANADIAN BRAND NAMES — Prolastin®
INTERNATIONAL BRAND NAMES — Prolastin (CA)
MECHANISM OF ACTION — Alpha1-antitrypsin (AAT) is the principle protease inhibitor in serum. Its major physiologic role is to render proteolytic enzymes (secreted during inflammation) inactive. A decrease in AAT, as seen in congenital AAT deficiency, leads to increased elastic damage in the lung, causing emphysema.
PHARMACODYNAMICS / KINETICS Half-life elimination: Metabolic: 5.9 days (Aralast™)
Time to peak, serum: Threshold levels achieved after 3 weeks
PATIENT INFORMATION — This medication is given by injection only.
Alpha-1 proteinase inhibitor
U.S. BRAND NAMES — Aralast; Prolastin®; Zemaira®
PHARMACOLOGIC CATEGORY Antitrypsin Deficiency Agent
DOSING: ADULTS — Alpha1-antitrypsin deficiency: I.V.: 60 mg/kg once weekly
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Aralast, Prolastin®: 500 mg, 1000 mg [packaged with diluent]
Zemaira®: 1000 mg [packaged with diluent]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution[preservative free]: Aralast, Prolastin®: 500 mg, 1000 mg Zemaira®: 1000 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For I.V. infusion only; reduce rate or temporarily discontinue infusion if adverse effects occur. Infuse at ~0.08 mL/kg/minute; actual rate may be increased or decreased based on patient response. Emergency equipment (including epinephrine) should be available during infusion. Do not mix with other agents or solutions.
USE — Replacement therapy in congenital alpha1-antitrypsin deficiency with clinical emphysema
ADVERSE REACTIONS SIGNIFICANT >10%: Hepatic: ALT/AST increased (11%; ~4 times ULN)
1% to 10%: Respiratory: Pharyngitis (2%)
<1% (Limited to important or life-threatening): Allergic reactions, bilateral pulmonary infiltrates, bronchitis, chest pain, chills, cough increased, dizziness, dyspnea, fever <102ºF (delayed up to 12 hours after treatment), flu-like syndrome, headache, hypotension, leukocytosis, lightheadedness, pain, pruritus, rash, sinusitis, somnolence, tachycardia, vasodilation, vision abnormal. Severe reactions (anaphylaxis) may occur in patients with anti-IgA antibody.
CONTRAINDICATIONS — Hypersensitivity to any component of the formulation or other A1-PI products; selective IgA deficiency with known anti-IgA antibody
WARNINGS / PRECAUTIONS — Use caution in patients at risk for fluid overload. Products are made from pooled human plasma; risk of infection is theoretical, however, any infections thought to be transmitted by these products should be reported to the manufacturer. Hepatitis B immunization may be considered. Safety and efficacy in pediatric patients have not been established.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Sodium content of 1 L after reconstitution:
Aralast™: 230 mEq/L
Prolastin®: 100-210 mEq/L
MONITORING PARAMETERS — Alpha1-PI serum levels; vital signs during infusion
CANADIAN BRAND NAMES — Prolastin®
INTERNATIONAL BRAND NAMES — Prolastin (CA)
MECHANISM OF ACTION — Alpha1-antitrypsin (AAT) is the principle protease inhibitor in serum. Its major physiologic role is to render proteolytic enzymes (secreted during inflammation) inactive. A decrease in AAT, as seen in congenital AAT deficiency, leads to increased elastic damage in the lung, causing emphysema.
PHARMACODYNAMICS / KINETICS Half-life elimination: Metabolic: 5.9 days (Aralast™)
Time to peak, serum: Threshold levels achieved after 3 weeks
PATIENT INFORMATION — This medication is given by injection only.
PHARMACOLOGIC CATEGORY Antitrypsin Deficiency Agent
DOSING: ADULTS — Alpha1-antitrypsin deficiency: I.V.: 60 mg/kg once weekly
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution [preservative free]:
Aralast, Prolastin®: 500 mg, 1000 mg [packaged with diluent]
Zemaira®: 1000 mg [packaged with diluent]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution[preservative free]: Aralast, Prolastin®: 500 mg, 1000 mg Zemaira®: 1000 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For I.V. infusion only; reduce rate or temporarily discontinue infusion if adverse effects occur. Infuse at ~0.08 mL/kg/minute; actual rate may be increased or decreased based on patient response. Emergency equipment (including epinephrine) should be available during infusion. Do not mix with other agents or solutions.
USE — Replacement therapy in congenital alpha1-antitrypsin deficiency with clinical emphysema
ADVERSE REACTIONS SIGNIFICANT >10%: Hepatic: ALT/AST increased (11%; ~4 times ULN)
1% to 10%: Respiratory: Pharyngitis (2%)
<1% (Limited to important or life-threatening): Allergic reactions, bilateral pulmonary infiltrates, bronchitis, chest pain, chills, cough increased, dizziness, dyspnea, fever <102ºF (delayed up to 12 hours after treatment), flu-like syndrome, headache, hypotension, leukocytosis, lightheadedness, pain, pruritus, rash, sinusitis, somnolence, tachycardia, vasodilation, vision abnormal. Severe reactions (anaphylaxis) may occur in patients with anti-IgA antibody.
CONTRAINDICATIONS — Hypersensitivity to any component of the formulation or other A1-PI products; selective IgA deficiency with known anti-IgA antibody
WARNINGS / PRECAUTIONS — Use caution in patients at risk for fluid overload. Products are made from pooled human plasma; risk of infection is theoretical, however, any infections thought to be transmitted by these products should be reported to the manufacturer. Hepatitis B immunization may be considered. Safety and efficacy in pediatric patients have not been established.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Sodium content of 1 L after reconstitution:
Aralast™: 230 mEq/L
Prolastin®: 100-210 mEq/L
MONITORING PARAMETERS — Alpha1-PI serum levels; vital signs during infusion
CANADIAN BRAND NAMES — Prolastin®
INTERNATIONAL BRAND NAMES — Prolastin (CA)
MECHANISM OF ACTION — Alpha1-antitrypsin (AAT) is the principle protease inhibitor in serum. Its major physiologic role is to render proteolytic enzymes (secreted during inflammation) inactive. A decrease in AAT, as seen in congenital AAT deficiency, leads to increased elastic damage in the lung, causing emphysema.
PHARMACODYNAMICS / KINETICS Half-life elimination: Metabolic: 5.9 days (Aralast™)
Time to peak, serum: Threshold levels achieved after 3 weeks
PATIENT INFORMATION — This medication is given by injection only.
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