Tuesday, March 11, 2008
Avoid Business Marketing Mistakes and Identify Profitable Opportunities
Without referring to statistics (assuming that such statistics exist) it's safe to say that most marketing campaigns, advertising promotions, and small business marketing ideas produce disappointing results and a smaller-than-expected ROI. The reasons for this include the following: advertising in the wrong medium, misidentifying your target market, selling a product or service for which there is little demand or too much competition, noncompetitive pricing, bad location, poor customer service, a weak sales strategy; or the absence of a compelling marketing message, a distinctive company identity, or unique selling proposition. In other words, the act of simply taking out newspaper ads, buying radio spots, making sales calls, and distributing brochures is not, in and of itself, going to make your phone ring off the hook or cause your cash register to overheat. The foundation of your marketing strategy must be rock solid, first!Remember, your target market is constantly being inundated withadvertising messages, commercials, sales pitches, and an endless parade of business signs, billboards, empty promises, special sales, shouting announcers, and dubious advertiser claims. The burning question for you, the small business owner, is: how do you reach the right people, stand out in the crowd, inspire believability, and get people to respond to your offer (preferably in droves)?Successful Advertising Campaigns Begin with a Captivating Advertising MessagePerhaps the most effective way to become attuned to what works and what doesn't is by getting in the habit of noticing and evaluating the hundreds of marketing messages and strategies that you're bombarded with every day. Constantly ask yourself what messages, advertising techniques, and images cause you to stop what you're doing and pay attention, whether it's a radio spot, billboard, a TV commercial, or a magazine ad? Chances are,the messages that do the best job of attracting your attention are the ones that focus on how a product or service will make you feel better, provide you with comfort, pleasure, solve a problem, infuse your marriage with romance, attract the oppositesex, bring your family closer together, make your life easier, healthier, safer, more secure, prosperous, exciting, or more fun. The list goes on and on; but the point is that the ads and marketing strategies that focus on the benefits, the good feelings, and the positive emotions that a product or service can evoke are the ones that typically generate the most responseand sales. In your ads, brochures, and sales presentations, emphasize the desirable outcomes, results, and benefits that your prospect will enjoy as the result of using your product or service. Features are important, too; but are generally secondarywhen talking about the powers of persuasion and sales success.As you begin to pay attention to and notice all the advertising messages that capture your attention and arouse your interest, give some thought to something else: how can you reach your target audience most effectively, without spending more marketingdollars than necessary. By paying attention to what other businesses and entrepreneurs are doing, and by thinking creatively, you will start formulating innovative and sometimes unconventional ideas that you can apply to profitably marketing your own products or services.Identifying Opportunities for Effective Target MarketingA successful marketing strategy often begins with looking for and identifying opportunities to cost-effectively reach your target market when they're in a receptive frame of mind. I observed a good example of this kind of opportunistic marketing while attending a crowded toy festival and parade over the summer. This festival was so popular that nearly every available parking spot on all the side streets was filled. When my family and I returned to our car after the parade, I immediately noticed that a bright yellow flyer (on card stock)was lodged under my windshield wiper. My first thought was that it was a parking ticket; but upon closer examination, I saw thatit was a promotional flyer for a children's party planning service. I looked up and down the street and noticed that every car had this same targeted advertisement in its window. As we drove through town, it was apparent that block after block of parked cars had this same advertising flyer inserted in their windows. The point is that some enterprising business owner realized that thousands of parents of young children are going to be in the same place at the same time, that they'll have just spent a fun day with their children, and they'll be in a receptive mood to learn about ways to make their children happier and to look good as parents. The owner of this children's party planning service figured out a way to inexpensively reach hundreds, maybe thousands of targeted prospects who, most likely, were very receptive to the service being marketed. I wouldn't be surprised if that flyer resulted in a lot of phone calls.It could have generated an even greater response if the copywriting and headlines were more captivating, if it used a couple of graphics to reinforce the message (rather than consisting of 100% text, with almost no margins), if it directed prospects to a website with more details and testimonials, plus photos of enthusiastic customers and successful parties... but that's a topic for another article!Successful advertising and marketing takes imagination, experimentation, and observation; but if the advertising message you develop doesn't paint an irresistible picture, create anticipation, and reach a targeted audience with the greatest tendency to respond to your offer, then your campaign will be ordinary and your results unremarkable. The principles in this article are not new, but they're probably ignored by the vast majority of those in the small business community. Commit these ideas to memory so that you're among the successfulminority!
Monday, March 10, 2008
Aluminum acetate
U.S. BRAND NAMES — Domeboro® [OTC]; Gordon Boro-Packs [OTC]; Pedi-Boro® [OTC]
PHARMACOLOGIC CATEGORY Topical Skin Product
DOSING: ADULTS — Dermal inflammation, dermatitis: Topical: Soak affected area in the solution 2-4 times/day for 15-30 minutes or apply wet dressing soaked in the solution for more extended periods; rewet dressing with solution 2-4 times/day every 15-30 minutes
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Powder, for topical solution: Domeboro®: Aluminum sulfate 1191 mg and calcium acetate 938 mg per packet (12s, 100s) Gordon Boro-Packs: Aluminum sulfate 49% and calcium acetate 51% per packet (100s) Pedi-Boro®: Aluminum sulfate 49% and calcium acetate 51% per packet (12s, 100s)
DOSAGE FORMS: CONCISE Powder, for topical solution: Domeboro® [OTC]: Aluminum sulfate 1191 mg and calcium acetate 938 mg per packet (12s, 100s) Gordon Boro-Packs: Aluminum sulfate 49% and calcium acetate 51% per packet (100s) Pedi-Boro® [OTC]: Aluminum sulfate 49% and calcium acetate 51% per packet (12s, 100s)
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For external use only. Do not occlude dressing to prevent evaporation.
USE — Astringent wet dressing for relief of inflammatory conditions of the skin; reduce weeping that may occur in dermatitis
WARNINGS / PRECAUTIONS — For external use only; avoid contact with eyes. Not for OTC use >7 days.
PHARMACOLOGIC CATEGORY Topical Skin Product
DOSING: ADULTS — Dermal inflammation, dermatitis: Topical: Soak affected area in the solution 2-4 times/day for 15-30 minutes or apply wet dressing soaked in the solution for more extended periods; rewet dressing with solution 2-4 times/day every 15-30 minutes
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Powder, for topical solution: Domeboro®: Aluminum sulfate 1191 mg and calcium acetate 938 mg per packet (12s, 100s) Gordon Boro-Packs: Aluminum sulfate 49% and calcium acetate 51% per packet (100s) Pedi-Boro®: Aluminum sulfate 49% and calcium acetate 51% per packet (12s, 100s)
DOSAGE FORMS: CONCISE Powder, for topical solution: Domeboro® [OTC]: Aluminum sulfate 1191 mg and calcium acetate 938 mg per packet (12s, 100s) Gordon Boro-Packs: Aluminum sulfate 49% and calcium acetate 51% per packet (100s) Pedi-Boro® [OTC]: Aluminum sulfate 49% and calcium acetate 51% per packet (12s, 100s)
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — For external use only. Do not occlude dressing to prevent evaporation.
USE — Astringent wet dressing for relief of inflammatory conditions of the skin; reduce weeping that may occur in dermatitis
WARNINGS / PRECAUTIONS — For external use only; avoid contact with eyes. Not for OTC use >7 days.
Altretamine
U.S. BRAND NAMES — Hexalen®
PHARMACOLOGIC CATEGORY Antineoplastic Agent, Miscellaneous
DOSING: ADULTS — Refer to individual protocols.
Ovarian cancer: Oral: 260 mg/m2/day in 4 divided doses for 14 or 21 days of a 28-day cycle Alternatively (unlabeled use): 4-12 mg/kg/day in 3-4 divided doses for 21-90 days Alternatively (unlabeled use): 240-320 mg/m2/day in 3-4 divided doses for 21 days, repeated every 6 weeks Alternatively (unlabeled use): 150 mg/m2/day in 3-4 divided doses for 14 days of a 28-day cycle
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gelcap: Hexalen®: 50 mg
DOSAGE FORMS: CONCISE Gelcap: Hexalen®: 50 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer total daily dose as 3-4 divided doses after meals and at bedtime.
USE — Palliative treatment of persistent or recurrent ovarian cancer
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Peripheral sensory neuropathy (31%; moderate-to-severe 9%), neurotoxicity (21%; may be progressive and dose-limiting) Gastrointestinal: Nausea/vomiting (33% to 70%; severe 1%), diarrhea (48%) Hematologic: Anemia (33%), leukopenia (5% to 15%; grade 4: 1%), neutropenia
1% to 10%: Central nervous system: Fatigue (1%), seizure (1%) Gastrointestinal: Stomach cramps, anorexia (1%) Hematologic: Thrombocytopenia (9%) Hepatic: Alkaline phosphatase increased (9%)
<1% (Limited to important or life-threatening): Alopecia, ataxia, depression, dizziness, hepatotoxicity, mood disorders, pruritus, rash, tremor, vertigo
CONTRAINDICATIONS — Hypersensitivity to altretamine or any component of the formulation; pre-existing severe bone marrow suppression or severe neurologic toxicity; pregnancy
WARNINGS / PRECAUTIONS Box warnings: Bone marrow suppression: See "Concerns related to adverse effects" below. Experienced physician: See "Other warnings/precautions" below. Neurotoxicity: See "Concerns related to adverse effects" below.
Special handling: Hazardous agent: Use appropriate precautions for handling and disposal.
Concerns related to adverse effects: Bone marrow suppression: [U.S. Boxed Warning]: Peripheral blood counts should be done routinely before and after drug therapy; bone marrow suppression is common. Use with caution in patients previously treated with other myelosuppressive drugs. Neurotoxicity: [U.S. Boxed Warning]: Neurologic examinations should be done routinely before and after drug therapy; neurotoxicity is common. USe with caution in patients with pre-existing neurotoxicity.
Disease-related concerns: Hepatic impairment: Use with caution in patients with hepatic impairment. Renal impairment: Use with caution in patients with renal impairment.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precautions: Experienced physician: [U.S. Boxed Warning]: Should be administered under the supervision of an experienced cancer chemotherapy physician.
DRUG INTERACTIONS MAO inhibitors: Altretamine may enhance the orthostatic effect of MAO inhibitors.
Pyridoxine: May diminish the therapeutic effect of altretamine; concurrent use not recommended.
Tricyclic antidepressants: Altretamine may enhance the orthostatic effect of tricyclic antidepressants.
PREGNANCY RISK FACTOR — D (show table)
PREGNANCY IMPLICATIONS — Teratogenic effects were noted in animal studies. There are no adequate and well-controlled studies in pregnant women. Women of childbearing potential should avoid becoming pregnant while on therapy.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — Due to the potential toxicity in the nursing infant, breast-feeding is not recommended.
DIETARY CONSIDERATIONS — Should be taken after meals at bedtime.
MONITORING PARAMETERS — CBC with differential, liver function tests; neurologic examination
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include nausea, vomiting, peripheral neuropathy, and severe bone marrow suppression. Treatment is symptom-directed and supportive.
CANADIAN BRAND NAMES — Hexalen®
INTERNATIONAL BRAND NAMES — Hexalen (AU, BG, CA, CN, GB, IE, IL, JP, NZ, SE, TH); Hexastat (DK, FR, NO, PT); Hexinawas (ES)
MECHANISM OF ACTION — Although altretamine's clinical antitumor spectrum resembles that of alkylating agents, the drug has demonstrated activity in alkylator-resistant patients. The drug selectively inhibits the incorporation of radioactive thymidine and uridine into DNA and RNA, inhibiting DNA and RNA synthesis; reactive intermediates covalently bind to microsomal proteins and DNA; can spontaneously degrade to demethylated melamines and formaldehyde which are also cytotoxic.
PHARMACODYNAMICS / KINETICS Absorption: Well absorbed (75% to 89%)
Distribution: Highly concentrated hepatically and renally; low in other organs
Protein binding: 50% to 94%
Metabolism: Hepatic; rapid and extensive demethylation to active metabolites (pentamethylmelamine and tetramethylmelamine)
Half-life elimination: 13 hours
Time to peak, plasma: 0.5-3 hours
Excretion: Urine (90%, <1% as unchanged drug)
PATIENT INFORMATION — Report any numbness or tingling in extremities. Nausea and vomiting may occur
PHARMACOLOGIC CATEGORY Antineoplastic Agent, Miscellaneous
DOSING: ADULTS — Refer to individual protocols.
Ovarian cancer: Oral: 260 mg/m2/day in 4 divided doses for 14 or 21 days of a 28-day cycle Alternatively (unlabeled use): 4-12 mg/kg/day in 3-4 divided doses for 21-90 days Alternatively (unlabeled use): 240-320 mg/m2/day in 3-4 divided doses for 21 days, repeated every 6 weeks Alternatively (unlabeled use): 150 mg/m2/day in 3-4 divided doses for 14 days of a 28-day cycle
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gelcap: Hexalen®: 50 mg
DOSAGE FORMS: CONCISE Gelcap: Hexalen®: 50 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer total daily dose as 3-4 divided doses after meals and at bedtime.
USE — Palliative treatment of persistent or recurrent ovarian cancer
ADVERSE REACTIONS SIGNIFICANT >10%: Central nervous system: Peripheral sensory neuropathy (31%; moderate-to-severe 9%), neurotoxicity (21%; may be progressive and dose-limiting) Gastrointestinal: Nausea/vomiting (33% to 70%; severe 1%), diarrhea (48%) Hematologic: Anemia (33%), leukopenia (5% to 15%; grade 4: 1%), neutropenia
1% to 10%: Central nervous system: Fatigue (1%), seizure (1%) Gastrointestinal: Stomach cramps, anorexia (1%) Hematologic: Thrombocytopenia (9%) Hepatic: Alkaline phosphatase increased (9%)
<1% (Limited to important or life-threatening): Alopecia, ataxia, depression, dizziness, hepatotoxicity, mood disorders, pruritus, rash, tremor, vertigo
CONTRAINDICATIONS — Hypersensitivity to altretamine or any component of the formulation; pre-existing severe bone marrow suppression or severe neurologic toxicity; pregnancy
WARNINGS / PRECAUTIONS Box warnings: Bone marrow suppression: See "Concerns related to adverse effects" below. Experienced physician: See "Other warnings/precautions" below. Neurotoxicity: See "Concerns related to adverse effects" below.
Special handling: Hazardous agent: Use appropriate precautions for handling and disposal.
Concerns related to adverse effects: Bone marrow suppression: [U.S. Boxed Warning]: Peripheral blood counts should be done routinely before and after drug therapy; bone marrow suppression is common. Use with caution in patients previously treated with other myelosuppressive drugs. Neurotoxicity: [U.S. Boxed Warning]: Neurologic examinations should be done routinely before and after drug therapy; neurotoxicity is common. USe with caution in patients with pre-existing neurotoxicity.
Disease-related concerns: Hepatic impairment: Use with caution in patients with hepatic impairment. Renal impairment: Use with caution in patients with renal impairment.
Special populations: Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precautions: Experienced physician: [U.S. Boxed Warning]: Should be administered under the supervision of an experienced cancer chemotherapy physician.
DRUG INTERACTIONS MAO inhibitors: Altretamine may enhance the orthostatic effect of MAO inhibitors.
Pyridoxine: May diminish the therapeutic effect of altretamine; concurrent use not recommended.
Tricyclic antidepressants: Altretamine may enhance the orthostatic effect of tricyclic antidepressants.
PREGNANCY RISK FACTOR — D (show table)
PREGNANCY IMPLICATIONS — Teratogenic effects were noted in animal studies. There are no adequate and well-controlled studies in pregnant women. Women of childbearing potential should avoid becoming pregnant while on therapy.
LACTATION — Excretion in breast milk unknown/not recommended
BREAST-FEEDING CONSIDERATIONS — Due to the potential toxicity in the nursing infant, breast-feeding is not recommended.
DIETARY CONSIDERATIONS — Should be taken after meals at bedtime.
MONITORING PARAMETERS — CBC with differential, liver function tests; neurologic examination
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include nausea, vomiting, peripheral neuropathy, and severe bone marrow suppression. Treatment is symptom-directed and supportive.
CANADIAN BRAND NAMES — Hexalen®
INTERNATIONAL BRAND NAMES — Hexalen (AU, BG, CA, CN, GB, IE, IL, JP, NZ, SE, TH); Hexastat (DK, FR, NO, PT); Hexinawas (ES)
MECHANISM OF ACTION — Although altretamine's clinical antitumor spectrum resembles that of alkylating agents, the drug has demonstrated activity in alkylator-resistant patients. The drug selectively inhibits the incorporation of radioactive thymidine and uridine into DNA and RNA, inhibiting DNA and RNA synthesis; reactive intermediates covalently bind to microsomal proteins and DNA; can spontaneously degrade to demethylated melamines and formaldehyde which are also cytotoxic.
PHARMACODYNAMICS / KINETICS Absorption: Well absorbed (75% to 89%)
Distribution: Highly concentrated hepatically and renally; low in other organs
Protein binding: 50% to 94%
Metabolism: Hepatic; rapid and extensive demethylation to active metabolites (pentamethylmelamine and tetramethylmelamine)
Half-life elimination: 13 hours
Time to peak, plasma: 0.5-3 hours
Excretion: Urine (90%, <1% as unchanged drug)
PATIENT INFORMATION — Report any numbness or tingling in extremities. Nausea and vomiting may occur
Alteplase
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 kg: 110% of the internal lumen volume of the catheter, not to exceed 2 mg/2 mL; retain in catheter for 0.5-2 hours; may instill a second dose if catheter remains occluded Patients 30 kg: 2 mg (2 mL); retain in catheter for 0.5-2 hours; may instill a second dose if catheter remains occluded
Acute peripheral arterial occlusive disease (unlabeled use): Intra-arterial: 0.02-0.1 mg/kg/hour for up to 36 hours Advisory Panel to the Society for Cardiovascular and Interventional Radiology on Thrombolytic Therapy recommendation: 2 mg/hour and subtherapeutic heparin (aPTT <1.5 times baseline)
DOSING: PEDIATRIC — Central venous catheter clearance: Intracatheter: Patients <30 kg: 110% of the internal lumen volume of the catheter, not to exceed 2 mg/2 mL; retain in catheter for 0.5-2 hours; may instill a second dose if catheter remains occluded
(For additional information see "Alteplase: Pediatric drug information")
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, recombinant: Activase®: 50 mg [29 million int. units; contains polysorbate 80; packaged with diluent]; 100 mg [58 million int. units; contains polysorbate 80; packaged with diluent and transfer device] Cathflo® Activase®: 2 mg [contains polysorbate 80]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution, recombinant: Activase®: 50 mg [29 million int. units]; 100 mg [58 million int. units] Cathflo® Activase®: 2 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION Activase®: Acute MI: Accelerated infusion: Bolus dose may be prepared by one of three methods: 1) removal of 15 mL reconstituted (1 mg/mL) solution from vial 2) removal of 15 mL from a port on the infusion line after priming 3) programming an infusion pump to deliver a 15 mL bolus at the initiation of infusion Remaining dose may be administered as follows: 50 mg vial: Either PVC bag or glass vial and infusion set 100 mg vial: Insert spike end of the infusion set through the same puncture site created by transfer device and infuse from vial If further dilution is desired, may be diluted in equal volume of 0.9% sodium chloride or D5W to yield a final concentration of 0.5 mg/mL AD
Cathflo® Activase®: Intracatheter: Instill dose into occluded catheter. Do not force solution into catheter. After a 30-minute dwell time, assess catheter function by attempting to aspirate blood. If catheter is functional, aspirate 4-5 mL of blood in patients 10 kg or 3 mL in patients <10 kg to remove Cathflo® Activase® and residual clots. Gently irrigate the catheter with NS. If catheter remains nonfunctional, let Cathflo® Activase® dwell for another 90 minutes (total dwell time: 120 minutes) and reassess function. If catheter function is not restored, a second dose may be instilled.
COMPATIBILITY — Stable in NS, sterile water for injection; incompatible with bacteriostatic water; variable stability (consult detailed reference) in D5W.
Y-site administration: Compatible: Lidocaine, metoprolol, propranolol. Incompatible: Dobutamine, dopamine, heparin, nitroglycerin.
Compatibility when admixed: Compatible: Lidocaine, morphine, nitroglycerin. Incompatible: Dobutamine, dopamine, heparin.
USE — Management of acute myocardial infarction for the lysis of thrombi in coronary arteries; management of acute ischemic stroke
Acute myocardial infarction (AMI): Chest pain 20 minutes, 12-24 hours; S-T elevation 0.1 mV in at least two ECG leads
Acute pulmonary embolism (APE): Age 75 years: Documented massive pulmonary embolism by pulmonary angiography or echocardiography or high probability lung scan with clinical shock
Cathflo® Activase®: Restoration of central venous catheter function
USE - UNLABELED / INVESTIGATIONAL — Acute peripheral arterial occlusive disease
ADVERSE REACTIONS SIGNIFICANT — As with all drugs which may affect hemostasis, bleeding is the major adverse effect associated with alteplase. Hemorrhage may occur at virtually any site. Risk is dependent on multiple variables, including the dosage administered, concurrent use of multiple agents which alter hemostasis, and patient predisposition. Rapid lysis of coronary artery thrombi by thrombolytic agents may be associated with reperfusion-related atrial and/or ventricular arrhythmia. Note: Lowest rate of bleeding complications expected with dose used to restore catheter function.
1% to 10%: Cardiovascular: Hypotension Central nervous system: Fever Dermatologic: Bruising (1%) Gastrointestinal: GI hemorrhage (5%), nausea, vomiting Genitourinary: GU hemorrhage (4%) Hematologic: Bleeding (0.5% major, 7% minor: GUSTO trial) Local: Bleeding at catheter puncture site (15.3%, accelerated administration)
<1% (Limited to important or life-threatening): Allergic reactions: Anaphylaxis, anaphylactoid reactions, laryngeal edema, rash, and urticaria (<0.02%); epistaxis; gingival hemorrhage; intracranial hemorrhage (0.4% to 0.87% when dose is 100 mg); pericardial hemorrhage; retroperitoneal hemorrhage
Additional cardiovascular events associated with use in MI: AV block, cardiogenic shock, heart failure, cardiac arrest, recurrent ischemia/infarction, myocardial rupture, electromechanical dissociation, pericardial effusion, pericarditis, mitral regurgitation, cardiac tamponade, thromboembolism, pulmonary edema, asystole, ventricular tachycardia, bradycardia, ruptured intracranial AV malformation, seizure, hemorrhagic bursitis, cholesterol crystal embolization
Additional events associated with use in pulmonary embolism: Pulmonary re-embolization, pulmonary edema, pleural effusion, thromboembolism
Additional events associated with use in stroke: Cerebral edema, cerebral herniation, seizure, new ischemic stroke
CONTRAINDICATIONS — Hypersensitivity to alteplase or any component of the formulation
Treatment of acute MI or PE: Active internal bleeding; history of CVA; recent intracranial or intraspinal surgery or trauma; intracranial neoplasm; arteriovenous malformation or aneurysm; known bleeding diathesis; severe uncontrolled hypertension
Treatment of acute ischemic stroke: Evidence of intracranial hemorrhage or suspicion of subarachnoid hemorrhage on pretreatment evaluation; recent (within 3 months) intracranial or intraspinal surgery; prolonged external cardiac massage; suspected aortic dissection; serious head trauma or previous stroke; history of intracranial hemorrhage; uncontrolled hypertension at time of treatment (eg, >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.
Other exclusion criteria (NINDS recombinant tPA study): Stroke or serious head injury within 3 months, major surgery or serious trauma within 2 weeks, GI or urinary tract hemorrhage within 3 weeks, aggressive treatment required to lower blood pressure, glucose level <50>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
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 kg: 110% of the internal lumen volume of the catheter, not to exceed 2 mg/2 mL; retain in catheter for 0.5-2 hours; may instill a second dose if catheter remains occluded Patients 30 kg: 2 mg (2 mL); retain in catheter for 0.5-2 hours; may instill a second dose if catheter remains occluded
Acute peripheral arterial occlusive disease (unlabeled use): Intra-arterial: 0.02-0.1 mg/kg/hour for up to 36 hours Advisory Panel to the Society for Cardiovascular and Interventional Radiology on Thrombolytic Therapy recommendation: 2 mg/hour and subtherapeutic heparin (aPTT <1.5 times baseline)
DOSING: PEDIATRIC — Central venous catheter clearance: Intracatheter: Patients <30 kg: 110% of the internal lumen volume of the catheter, not to exceed 2 mg/2 mL; retain in catheter for 0.5-2 hours; may instill a second dose if catheter remains occluded
(For additional information see "Alteplase: Pediatric drug information")
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, recombinant: Activase®: 50 mg [29 million int. units; contains polysorbate 80; packaged with diluent]; 100 mg [58 million int. units; contains polysorbate 80; packaged with diluent and transfer device] Cathflo® Activase®: 2 mg [contains polysorbate 80]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution, recombinant: Activase®: 50 mg [29 million int. units]; 100 mg [58 million int. units] Cathflo® Activase®: 2 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION Activase®: Acute MI: Accelerated infusion: Bolus dose may be prepared by one of three methods: 1) removal of 15 mL reconstituted (1 mg/mL) solution from vial 2) removal of 15 mL from a port on the infusion line after priming 3) programming an infusion pump to deliver a 15 mL bolus at the initiation of infusion Remaining dose may be administered as follows: 50 mg vial: Either PVC bag or glass vial and infusion set 100 mg vial: Insert spike end of the infusion set through the same puncture site created by transfer device and infuse from vial If further dilution is desired, may be diluted in equal volume of 0.9% sodium chloride or D5W to yield a final concentration of 0.5 mg/mL AD
Cathflo® Activase®: Intracatheter: Instill dose into occluded catheter. Do not force solution into catheter. After a 30-minute dwell time, assess catheter function by attempting to aspirate blood. If catheter is functional, aspirate 4-5 mL of blood in patients 10 kg or 3 mL in patients <10 kg to remove Cathflo® Activase® and residual clots. Gently irrigate the catheter with NS. If catheter remains nonfunctional, let Cathflo® Activase® dwell for another 90 minutes (total dwell time: 120 minutes) and reassess function. If catheter function is not restored, a second dose may be instilled.
COMPATIBILITY — Stable in NS, sterile water for injection; incompatible with bacteriostatic water; variable stability (consult detailed reference) in D5W.
Y-site administration: Compatible: Lidocaine, metoprolol, propranolol. Incompatible: Dobutamine, dopamine, heparin, nitroglycerin.
Compatibility when admixed: Compatible: Lidocaine, morphine, nitroglycerin. Incompatible: Dobutamine, dopamine, heparin.
USE — Management of acute myocardial infarction for the lysis of thrombi in coronary arteries; management of acute ischemic stroke
Acute myocardial infarction (AMI): Chest pain 20 minutes, 12-24 hours; S-T elevation 0.1 mV in at least two ECG leads
Acute pulmonary embolism (APE): Age 75 years: Documented massive pulmonary embolism by pulmonary angiography or echocardiography or high probability lung scan with clinical shock
Cathflo® Activase®: Restoration of central venous catheter function
USE - UNLABELED / INVESTIGATIONAL — Acute peripheral arterial occlusive disease
ADVERSE REACTIONS SIGNIFICANT — As with all drugs which may affect hemostasis, bleeding is the major adverse effect associated with alteplase. Hemorrhage may occur at virtually any site. Risk is dependent on multiple variables, including the dosage administered, concurrent use of multiple agents which alter hemostasis, and patient predisposition. Rapid lysis of coronary artery thrombi by thrombolytic agents may be associated with reperfusion-related atrial and/or ventricular arrhythmia. Note: Lowest rate of bleeding complications expected with dose used to restore catheter function.
1% to 10%: Cardiovascular: Hypotension Central nervous system: Fever Dermatologic: Bruising (1%) Gastrointestinal: GI hemorrhage (5%), nausea, vomiting Genitourinary: GU hemorrhage (4%) Hematologic: Bleeding (0.5% major, 7% minor: GUSTO trial) Local: Bleeding at catheter puncture site (15.3%, accelerated administration)
<1% (Limited to important or life-threatening): Allergic reactions: Anaphylaxis, anaphylactoid reactions, laryngeal edema, rash, and urticaria (<0.02%); epistaxis; gingival hemorrhage; intracranial hemorrhage (0.4% to 0.87% when dose is 100 mg); pericardial hemorrhage; retroperitoneal hemorrhage
Additional cardiovascular events associated with use in MI: AV block, cardiogenic shock, heart failure, cardiac arrest, recurrent ischemia/infarction, myocardial rupture, electromechanical dissociation, pericardial effusion, pericarditis, mitral regurgitation, cardiac tamponade, thromboembolism, pulmonary edema, asystole, ventricular tachycardia, bradycardia, ruptured intracranial AV malformation, seizure, hemorrhagic bursitis, cholesterol crystal embolization
Additional events associated with use in pulmonary embolism: Pulmonary re-embolization, pulmonary edema, pleural effusion, thromboembolism
Additional events associated with use in stroke: Cerebral edema, cerebral herniation, seizure, new ischemic stroke
CONTRAINDICATIONS — Hypersensitivity to alteplase or any component of the formulation
Treatment of acute MI or PE: Active internal bleeding; history of CVA; recent intracranial or intraspinal surgery or trauma; intracranial neoplasm; arteriovenous malformation or aneurysm; known bleeding diathesis; severe uncontrolled hypertension
Treatment of acute ischemic stroke: Evidence of intracranial hemorrhage or suspicion of subarachnoid hemorrhage on pretreatment evaluation; recent (within 3 months) intracranial or intraspinal surgery; prolonged external cardiac massage; suspected aortic dissection; serious head trauma or previous stroke; history of intracranial hemorrhage; uncontrolled hypertension at time of treatment (eg, >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.
Other exclusion criteria (NINDS recombinant tPA study): Stroke or serious head injury within 3 months, major surgery or serious trauma within 2 weeks, GI or urinary tract hemorrhage within 3 weeks, aggressive treatment required to lower blood pressure, glucose level <50>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
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% (Limited to important or life-threatening): Tachycardia, perineal pain, leg pain
Intracavernosal injection:
>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% (Limited to important or life-threatening): Balanitis, injection site hemorrhage, priapism (0.4%)
Intravenous:
>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% (Limited to important or life-threatening): Anemia, anuria, bleeding, bradypnea, bronchial wheezing, cerebral bleeding, CHF, gastric regurgitation, hematuria, hyperbilirubinemia, hyperemia, hyperextension of neck, hyperirritability, hyperkalemia, hypoglycemia, hypothermia, jitteriness, lethargy, peritonitis, second degree heart block, shock, stiffness, supraventricular tachycardia, thrombocytopenia, ventricular fibrillation
CONTRAINDICATIONS — Hypersensitivity to alprostadil or any component of the formulation; hyaline membrane disease or persistent fetal circulation and when a dominant left-to-right shunt is present; respiratory distress syndrome; conditions predisposing patients to priapism (sickle cell anemia, multiple myeloma, leukemia); patients with anatomical deformation of the penis, penile implants; use in men for whom sexual activity is inadvisable or contraindicated; pregnancy
WARNINGS / PRECAUTIONS Box warnings: Apnea: See "Concerns related to adverse effects" below.
Concerns related to adverse effects: Apnea: [U.S. Boxed Warning]: Apnea may occur in 10% to 12% of neonates with congenital heart defects, especially in those weighing <2 kg at birth. Apnea usually appears during the first hour of drug infusion.
Disease-related concerns: Erectile dysfunction: Appropriate use: When used in erectile dysfunction, priapism may occur; patient must be instructed to report to physician or seek immediate medical assistance if an erection persists for longer than 4 hours. Treat immediately to avoid penile tissue damage and permanent loss of potency; discontinue therapy if signs of penile fibrosis develop (penile angulation, cavernosal fibrosis, or Peyronie's disease). Patency of ductus arteriosus: Appropriate use: Infuse for the shortest time at the lowest dose consistent with good patient care. Use for >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% of patients during in-clinic titration and home treatment.
DRUG INTERACTIONS — Risk of hypotension and syncope may be increased with antihypertensives.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Avoid concurrent use (vasodilating effect).
PREGNANCY RISK FACTOR — X/C (show table) (Muse®)
PREGNANCY IMPLICATIONS — Alprostadil is embryotoxic in animal studies. It is not indicated for use in women. The manufacturer of Muse® recommends a condom barrier when being used during sexual intercourse with a pregnant women.
LACTATION — Not indicated for use in women
PRICING — (data from drugstore.com)Injection (reconstituted) (Caverject) 40 mcg (6): $230.47
Kit (Caverject Impulse) 10 mcg (2): $59.84 20 mcg (2): $74.54
Kit (Edex) 10 mcg (1): $56.92 10 mcg (1): $153.44 20 mcg (1): $71.83 20 mcg (6): $1167.41 40 mcg (1): $95.56 40 mcg (1): $266.87
Pellet (Muse) 125 mcg (6): $138.46 250 mcg (6): $145.67 500 mcg (6): $155.45 1000 mcg (6): $167.85
MONITORING PARAMETERS — Arterial pressure, respiratory rate, heart rate, temperature, degree of penile pain, length of erection, signs of infection
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms when treating patent ductus arteriosus include apnea, bradycardia, hypotension, and flushing. If hypotension or pyrexia occurs, the infusion rate should be reduced until the symptoms subside, while apnea or bradycardia requires drug discontinuation. If intracavernous overdose occurs, supervise until any systemic effects have resolved or until penile detumescence has occurred.
CANADIAN BRAND NAMES — Caverject®; Muse® Pellet; Prostin® VR
INTERNATIONAL BRAND NAMES — Alprostapint (PL); Befar (HK); Caverject (AE, AN, AR, AT, AU, BB, BH, BM, BR, BS, BZ, CA, CL, CN, CO, CR, CY, DE, EC, EG, FR, GB, GT, GY, HN, IE, IQ, IR, JM, JO, KR, KW, LB, LY, MX, MY, NI, NL, NO, NZ, OM, PA, PE, PL, PR, PY, QA, SA, SE, SG, SR, SV, SY, TT, TW, UY, VE, YE, ZA); Caverject Dual Chamber (HK); Caverject Impulse (AU); Caverjet (IL); Edex (FR, PL); Eglandin (KR); Gaverject (PK); Liple (JP); Lyple (JP); Minprog (AT); Muse (AE, BH, CY, EG, FR, GB, IE, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE, ZA); Muse Pellet (CA); Palux (JP); Prink (KR); Promostan (TW); Prostandin (JP, KR); Prostavasin (AR, BR, CN, HK, PH, PL, UY); Prostin VR (AE, AU, BE, BG, BH, CA, CH, CL, CO, CY, CZ, EG, GB, GR, HU, IE, IL, IN, IQ, IR, IT, JO, KW, LB, LY, NL, NZ, OM, PH, PL, QA, SA, SY, TH, TW, YE, ZA); Prostin VR Paedeatric (MY); Prostine VR (FR); Prostivas (DK, FI, NO, SE); Viridal (DE)
MECHANISM OF ACTION — Causes vasodilation by means of direct effect on vascular and ductus arteriosus smooth muscle; relaxes trabecular smooth muscle by dilation of cavernosal arteries when injected along the penile shaft, allowing blood flow to and entrapment in the lacunar spaces of the penis (ie, corporeal veno-occlusive mechanism)
PHARMACODYNAMICS / KINETICS Onset of action: Rapid
Duration: <1 hour
Distribution: Insignificant following penile injection
Protein binding, plasma: 81% to albumin
Metabolism: ~75% by oxidation in one pass via lungs
Half-life elimination: 5-10 minutes
Excretion: Urine (90% as metabolites) within 24 hours
PATIENT INFORMATION — Store in refrigerator; if self-injecting for the treatment of impotence, dilute with the supplied diluent and use immediately after diluting; see prescriber at least every 3 months to ensure proper technique and for dosage adjustment. Alternate sides of the penis with each injection; do not inject more than 3 times/week, allowing at least 24 hours between each dose; dispose of the syringe, needle, and vial properly; discard single-use vials after each use; report moderate to severe penile pain or erections lasting >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% (Limited to important or life-threatening): Tachycardia, perineal pain, leg pain
Intracavernosal injection:
>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% (Limited to important or life-threatening): Balanitis, injection site hemorrhage, priapism (0.4%)
Intravenous:
>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% (Limited to important or life-threatening): Anemia, anuria, bleeding, bradypnea, bronchial wheezing, cerebral bleeding, CHF, gastric regurgitation, hematuria, hyperbilirubinemia, hyperemia, hyperextension of neck, hyperirritability, hyperkalemia, hypoglycemia, hypothermia, jitteriness, lethargy, peritonitis, second degree heart block, shock, stiffness, supraventricular tachycardia, thrombocytopenia, ventricular fibrillation
CONTRAINDICATIONS — Hypersensitivity to alprostadil or any component of the formulation; hyaline membrane disease or persistent fetal circulation and when a dominant left-to-right shunt is present; respiratory distress syndrome; conditions predisposing patients to priapism (sickle cell anemia, multiple myeloma, leukemia); patients with anatomical deformation of the penis, penile implants; use in men for whom sexual activity is inadvisable or contraindicated; pregnancy
WARNINGS / PRECAUTIONS Box warnings: Apnea: See "Concerns related to adverse effects" below.
Concerns related to adverse effects: Apnea: [U.S. Boxed Warning]: Apnea may occur in 10% to 12% of neonates with congenital heart defects, especially in those weighing <2 kg at birth. Apnea usually appears during the first hour of drug infusion.
Disease-related concerns: Erectile dysfunction: Appropriate use: When used in erectile dysfunction, priapism may occur; patient must be instructed to report to physician or seek immediate medical assistance if an erection persists for longer than 4 hours. Treat immediately to avoid penile tissue damage and permanent loss of potency; discontinue therapy if signs of penile fibrosis develop (penile angulation, cavernosal fibrosis, or Peyronie's disease). Patency of ductus arteriosus: Appropriate use: Infuse for the shortest time at the lowest dose consistent with good patient care. Use for >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% of patients during in-clinic titration and home treatment.
DRUG INTERACTIONS — Risk of hypotension and syncope may be increased with antihypertensives.
ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Avoid concurrent use (vasodilating effect).
PREGNANCY RISK FACTOR — X/C (show table) (Muse®)
PREGNANCY IMPLICATIONS — Alprostadil is embryotoxic in animal studies. It is not indicated for use in women. The manufacturer of Muse® recommends a condom barrier when being used during sexual intercourse with a pregnant women.
LACTATION — Not indicated for use in women
PRICING — (data from drugstore.com)Injection (reconstituted) (Caverject) 40 mcg (6): $230.47
Kit (Caverject Impulse) 10 mcg (2): $59.84 20 mcg (2): $74.54
Kit (Edex) 10 mcg (1): $56.92 10 mcg (1): $153.44 20 mcg (1): $71.83 20 mcg (6): $1167.41 40 mcg (1): $95.56 40 mcg (1): $266.87
Pellet (Muse) 125 mcg (6): $138.46 250 mcg (6): $145.67 500 mcg (6): $155.45 1000 mcg (6): $167.85
MONITORING PARAMETERS — Arterial pressure, respiratory rate, heart rate, temperature, degree of penile pain, length of erection, signs of infection
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms when treating patent ductus arteriosus include apnea, bradycardia, hypotension, and flushing. If hypotension or pyrexia occurs, the infusion rate should be reduced until the symptoms subside, while apnea or bradycardia requires drug discontinuation. If intracavernous overdose occurs, supervise until any systemic effects have resolved or until penile detumescence has occurred.
CANADIAN BRAND NAMES — Caverject®; Muse® Pellet; Prostin® VR
INTERNATIONAL BRAND NAMES — Alprostapint (PL); Befar (HK); Caverject (AE, AN, AR, AT, AU, BB, BH, BM, BR, BS, BZ, CA, CL, CN, CO, CR, CY, DE, EC, EG, FR, GB, GT, GY, HN, IE, IQ, IR, JM, JO, KR, KW, LB, LY, MX, MY, NI, NL, NO, NZ, OM, PA, PE, PL, PR, PY, QA, SA, SE, SG, SR, SV, SY, TT, TW, UY, VE, YE, ZA); Caverject Dual Chamber (HK); Caverject Impulse (AU); Caverjet (IL); Edex (FR, PL); Eglandin (KR); Gaverject (PK); Liple (JP); Lyple (JP); Minprog (AT); Muse (AE, BH, CY, EG, FR, GB, IE, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE, ZA); Muse Pellet (CA); Palux (JP); Prink (KR); Promostan (TW); Prostandin (JP, KR); Prostavasin (AR, BR, CN, HK, PH, PL, UY); Prostin VR (AE, AU, BE, BG, BH, CA, CH, CL, CO, CY, CZ, EG, GB, GR, HU, IE, IL, IN, IQ, IR, IT, JO, KW, LB, LY, NL, NZ, OM, PH, PL, QA, SA, SY, TH, TW, YE, ZA); Prostin VR Paedeatric (MY); Prostine VR (FR); Prostivas (DK, FI, NO, SE); Viridal (DE)
MECHANISM OF ACTION — Causes vasodilation by means of direct effect on vascular and ductus arteriosus smooth muscle; relaxes trabecular smooth muscle by dilation of cavernosal arteries when injected along the penile shaft, allowing blood flow to and entrapment in the lacunar spaces of the penis (ie, corporeal veno-occlusive mechanism)
PHARMACODYNAMICS / KINETICS Onset of action: Rapid
Duration: <1 hour
Distribution: Insignificant following penile injection
Protein binding, plasma: 81% to albumin
Metabolism: ~75% by oxidation in one pass via lungs
Half-life elimination: 5-10 minutes
Excretion: Urine (90% as metabolites) within 24 hours
PATIENT INFORMATION — Store in refrigerator; if self-injecting for the treatment of impotence, dilute with the supplied diluent and use immediately after diluting; see prescriber at least every 3 months to ensure proper technique and for dosage adjustment. Alternate sides of the penis with each injection; do not inject more than 3 times/week, allowing at least 24 hours between each dose; dispose of the syringe, needle, and vial properly; discard single-use vials after each use; report moderate to severe penile pain or erections lasting >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
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