FYDI              

……………For Your Drug Information ………….

OSF Saint Francis Medical Center Peoria, IL

 May – June 2003

New FDA marketing approvals:  (work in progress)

1. (Factive®) Gemafloxacin mesylate – a new fluoroquinolone approved for the treatment of pneumonia.  Available from LG Life Sciences as a 320 mg tablet, the drug is dosed once daily for 5 days for acute exacerbations of chronic bronchitis OR once daily for 7 days for community-acquired pneumonia.

 

2. (Suboxone®) Buprenorphine/Naloxone – sublingual tablet combination approved for treatment of opioid dependence. The tablet comes in two sizes containing 2 mg buprenorphine/0.5 mg naloxone OR 8 mg buprenorphine/2 mg naloxone.  Prescribing will be limited to specific physicians and strict accountability of drug supply is required.  Manufactured by Reckitt Benckiser Pharmaceuticals.

 

3. (Zymar®) Gatifloxacin 0.3% Opthalmic Solution – fluoroquinolone antibiotic solution used for treatment of bacterial conjunctivitis.  On Day 1 & 2 instill one drop every 2 hours into affected eye while awake (up to 8 times daily). For day 3 through 7, instill one drop four times daily while awake.  The drug is manufactured by Allergan, Inc.

 

4.  (Velcade®) Bortezomib – a new chemotherapeutic agent used in the treatment of refractory multiple myeloma for patients who have failed at least two other conventional treatments.  Bortezomib is in a new class of anti-neoplastics called proteasome inhibitors.  Proteasomes are enzymes found in all eukaryotic cells, both healthy and malignant, which help to regulate cell function and growth.  Velcade® reversibly inhibits the 26S proteasome preventing proteolysis of enzymes involved in cellular homeostasis.  This inhibition alters the intracellular concentration of certain proteins and affects multiple signaling cascades.  Ultimately, the inhibition disrupts normal homeostatic mechanisms and may lead to cell death.  Velcade® is available as a 3.5mg vial and the usual dose is 1.3 mg/m2 per dose given as an IV bolus twice weekly for 2 weeks and cycled every 3 weeks.  There should be at least 72 hours between doses and 10 days between each cycle.  The most commonly reported side effects include nausea, vomiting, diarrhea, constipation, tiredness, thrombocytopenia (40%), orthostatic hypotension (12%), decreased appetite, and fever.  Velcade® was approved by the FDA in less than four months via a rapid approval process.  Safety and efficacy studies are now underway.  The approximate cost for a course of therapy will be $20,000.   Velcade® is manufactured by Millennium Pharmaceuticals Inc.

 

5.  (Iressa®) Gefitinib – a new chemotherapeutic agent used in the treatment of advanced cases of non-small cell lung cancer.  Gefitinib is a new class of anti-neoplastics called epidermal growth factor receptor inhibitors.  Available as a 250mg tablet and will be dosed at 250 mg orally once daily.  If the patient is on a potent CYP3A4 inducer such as rifampin or phenytoin the dose may be increased to 500 mg daily.  The drug is manufactured by AstraZeneca. 

 

6.  (Restasis®) Cyclosporine – a new eye drop preparation from Allergan. Available as a 0.05% opthalmic emulsion which is used to increase tear production in patients whose tear production is suppressed due to inflammation seen in kerato-conjunctivitis sicca.  One drop of the emulsion is instilled twice daily.

 

7.  (Prilosec® OTC) Omeprazole – On June 20th, the FDA approved Prilosec® OTC as the first over-the-counter treatment for heartburn that occurs two or more days per week (frequent heartburn).  Prilosec® OTC will be available as a 20mg delayed release tablet and should be taken once daily before a meal for fourteen days.  Per the package labeling, consumers are cautioned to contact their healthcare provider if heartburn returns soon after finishing the fourteen day course.  In addition, consumers are warned not to take a fourteen day course more frequently than every four months unless under the care of a physician.  Astra Zeneca will has a three year exclusivity agreement which will block the sale of generic equivalents until the agreement has expired.  Prilosec® will continue to be available per a prescription for ulcers, GERD, esophagitis, or other conditions requiring the care of a doctor.  

 

8.  (Reyataz®) Atazanavir sulfate – a new protease inhibitor from Bristol-Meyers Squibb.  This once daily protease inhibitor will help to decrease the pill burden of HIV patients.  The most common lab abnormality with Reyataz® was hyperbilirubinemia.  15-24% of subjects became jaundiced or had scleral icterus (yellowing of the eyes).  These conditions were reversed with discontinuation of Reyataz® and did not correlate with an increase risk of hepatic damage.  The most common reported side effects during clinical trials were nausea, infection, headache, vomiting, diarrhea, abdominal pain, somnolence, insomnia, and fever.  Unlike other protease inhibitors which may cause hyperlipidemia, Reyataz® appears to have a minimal effect on cholesterol and triglycerides.   

 

Drug Safety Notes:

 

New Warning – [Risperdal®] - incidence of cerebrovascular adverse events were increased in elderly patients taking risperidone for dementia-related psychosis.  Events included stroke and transient ischemic attack.  See Dear Healthcare Provider Letter dated 16April2003 from Janssen Pharmaceuticals.

 

New Warning – [Paxil®] - The FDA is currently reviewing reports of a possible increase in the number of suicidal thoughts and attempts in children under the age of eighteen who are being treated with Paxil® for a major depressive disorder.  The safety data under review resulted from clinical trials with Paxil® in pediatric patients.  Even though the investigation is still underway, the FDA recommends that Paxil® not be used in adolescents and children for the treatment of depression.  Presently, there is no approved indication for the use of Paxil® in children and adolescents.  Patients, caregivers, and healthcare providers should be cautioned against abrupt discontinuation of Paxil®.

 

Drug in Review

Ximelagatran (ExantaÒ)

 

By Christine Slingsby , Pharm.D. candidate.

 

An oral direct thrombin inhibitor that provides competitive, direct inhibition of both free and clot bound thrombin.  Thrombin is responsible for thrombus formation by activating platelets, subsequent platelet aggregation, and inducing formation of fibrin.

 

Ximelagatran is a prodrug, that when taken orally, is converted to the active drug melagatran.   Ximelagatran has been studied and has proven to be as effective as warfarin for the prevention of DVT or PE after total knee arthroplasty1.  Unlike warfarin, ximelagatran does not require frequent drug monitoring or dosing adjustments.  Ximelagatran produces anticoagulant effects through a vitamin K independent mechanism, therefore does not require strict diet or vitamin K intake. 

 

Currently, Ximelagatran is being studied for stroke prevention in patients with atrial fibrillation2.  Dosing for Ximelagatran for DVT prophylaxis is 24mg BID, beginning on post-op day 1.  Melagatran is excreted renally; therefore caution should be used in patients with renal failure. Further studies are also needed to adequately establish safety for long term use of this drug since it appears to elevate liver enzymes more than  warfarin in the SPORTIF trial ( ALT > 3x ULN : 6.5% ximelagatran vs 0.7% warfarin)2. Until FDA issues its final approval, this product is considered investigational.  

 

Edited by: Ruth Avelino, Pharm.D.

Reference:

1.             Francis CW, Davidson  BL,  Berkowitz SD, et. At. Ximelagatran versus warfarin for the prevention of venous thromboembolism after total knee arthroplasty. Ann Intern Med.2002;137:648-55.

2.             SPORTIF III trial – presented for American College of Cardiology : 52nd Annual Scientific Seminar. http://www.acc03online.acc.org/ondemand/trials3/sessions.asp?sid=3

Drug Information Notes:

1. New neonatal dosing for Acetaminophen: (CHOI – NICU protocol)

Acetaminophen dosing for CHOI NICU

 

Scheduled dosing as follows for 24 hours post op, post vaccination, etc. then change to PRN dosing if desired.

 

 

Loading dose (mg/kg)

Maintenance dose

(mg/kg)

Dosing interval

(hours)

Oral dosing

 

 

 

≤32 weeks PMA

25

12

12

32-36 weeks PMA

25

15

8

≥36 weeks PMA

25

15

6

Rectal dosing

 

 

 

≤32 weeks PMA

35

15

12

32-36 weeks PMA

35

20

8

≥ 36 weeks PMA

35

20

6

 PMA= postmenstrual age

 

References:

Anderson.  Anesthesiology 2002; 96:1336-45.

Anderson.  Br J Clin Pharmacol 2000; 50:125-134.

Arana.  Acta Anaesthesiol Scand 2001; 45(1):20-29.

Hansen.   Acta Anaesthesiol Scand 1999; 43(8):855-859.

VanLingen.  Arch Dis Child Fetal Neonatal Ed 1999; 80(1):59F-63F.

 

2.  Which weight would you use to dose an obese patient for ABELCET?

A:        Studies done by the drug company suggested using Lean body weight for which the closest estimate would be the IBW.

 

By Ruth Avelino

Reference:

  1. Personal Communication – Enzon Pharmaceuticals (1-866-792-5172)

 

 

3.  IV Administration of oral N-acetylcysteine in Acetaminophen Overdose

By:  Azra Hussain

 

N-acetylcysteine (NAC) is the only treatment approved by the FDA for acetaminophen poisoning.  Currently, only the oral preparation is available commercially.  An investigational intravenous formulation does exist; however, it is only available through an investigational protocol at a limited number of poison control centers in the United States.  This unavailability leaves patients who cannot receive or tolerate oral NAC administration with the limited option of receiving the oral preparation intravenously.  The following is a list of recommendations to aid in the decision of utilizing the oral preparation intravenously.   

 

Consent: Inform physician and/or patient that the IV preparation is not pyrogen free.

Prepare the physician and /or administering nurse what to expect for side-effects and potential treatments available.

 

Indications for IV Administration:

            Oral NAC cannot be tolerated                    

            Necessary ongoing GI decontamination (due to coingestant)

            GI bleeding or obstruction   

            Medical or surgical conditions preventing oral NAC administration      

            Acetaminophen toxicity presenting as encephalopathy

            Neonatal acetaminophen toxicity from maternal overdose

 

Dose:  The typical oral loading dose and maintenance dose of NAC is 140mg/kg

x 1 dose, then 70mg/kg Q4h x 17 doses (72 hours) respectively.  However, when oral NAC is given intravenously, the guidelines become less defined.  The most common dosing regimen for oral NAC administered intravenously is a loading dose of 140mg/kg x 1 dose followed by 12 doses of 70mg/kg Q4h (for a total of 48 hours). 

                       

IV Preparation:

                        Dilute 20% NAC solution to 3% solution with D5W

 

Administration:

LD & MD = Infuse over 1 hour through a peripheral line using an in-line 0.2

        micron Millipore filter

 

Adverse Events Associated with IV Administration of Oral NAC:

Initial Infusion related events :( Did not interfere with further NAC treatment)

1.)  Blotchy red face and confluent redness

      over neck upper chest (resolved spontaneously without tx)

2.)     Itching (resolved with benadryl)

3.)     Anaphylactic reaction (resolved with benadryl)

4.)     Red streak along IV site (resolved with rotating injection sites)

 

References: 

 

Bailey B, McGuigan M:  Management of Anaphylactoid Reactions to Intravenous

                N-acetylcysteine.  Annals of Emergency Medicine 1998; 31: 710-715.

Falk FL:  Oral N-acetylcysteine given intravenously for acetaminophen overdose: 

                We shouldn’t have to, but we must.  Critical Care Medicine 1998; 26: 7.

Smilkstein MJ, Bronstein AC, Linden C, et al:  Acetaminophen overdose:  a 48-

hour intravenous N-acetylcysteine treatment protocol.  Annals of

Emergency Medicine 1991; 20: 1058-1063.

Yip L, Dart RC, Hurlbut KM:  Intravenous administration of oral N-acetylcysteine. 

Crtical Care Medicine 1998; 26: 40-43.

 

4.  How is Erythropoietin (Epogen®/Procrit®) dosed in the treatment of anemia due to critical care? (amc)

This protocol has been purposed for use in SICU/MICU if Hematocrit is 30-36% / hemoglobin (10-13 g/dl).  The regimen is to start erythropoietin at 300 IU/kg/day on day 3 of ICU stay and continue for a total of 5 days.  Continue the patient on the same dose on a QOD regimen to achieve a hematocrit of >38%, for a minimum of 2 weeks or until discharged from the ICU or goal hematocrit is achieved.  The study utilizing this dosing regimen concluded the patients given erythropoietin required less transfusion of RBCs and the drug raised the hematocrit concentrations.

Patients must also be started on concurrent iron therapy with oral or parenteral iron.  Start oral therapy when bowel sounds are present at a dose of >/= 150 mg of elemental iron (a 325 mg tablet of ferrous sulfate is 65 mg of elemental iron) daily in divided doses.  Use parenteral iron therapy if unable to take oral therapy or if there is an inadequate response to oral therapy as measured by a transferrin saturation < 20% and a decrease in serum ferritin to < 100 ng/ml. 

There are other dosing regimens that have been studied but this should be the one most commonly seen in the ICUs at OSF Saint Francis Medical Center.  The same investigator, Howard Corwin did a follow-up study in December 2002 and used erythropoietin 40,000 units vs. placebo weekly for 3-4 doses. The study concluded with the same results as the one conducted in 1999.  Overall, there were no significant differences in morbidity or mortality observed between the 2 treatment groups.

The primary reason to use Epogen® in this patient population was to reduce the need for and risk of blood transfusion.  These studies were conducted in patients who were in an ICU setting and use on the general surgical floors should be investigated thoroughly by the pharmacist who receives an order for Epogen® for a non-ICU surgical patient.  The intent of these studies was to focus on “long-term” ICU patients who are likely to have the most transfusions.

 

It is also suggested that patients receiving these agents should have had a baseline iron studies done and should be on some iron supplement since the hormone would most likely put demands on the body’s existing iron stores.

 

References:

Corwin, HL. Gettinger, A. et al.  Efficacy of recombinant human erythropoietin in the critically ill patient: A randomized, double blind, placebo-controlled trial.  Critical Care Medicine 1999 Vol.27 (11); 234-2350.

Corwin, HL, Gettinger, A. et al.  Efficacy of recombinant human erythropoietin in critically ill patients: A randomized controlled trial.  JAMA December 2002 Vol 288(22); 2827-2835.

 

5.  How is NovoSeven® (recombinant activated factor VII) used for control of hemorrhaging in non-hemophiliac trauma patients? (amc)

Trauma patients who develop extensive, life-threatening bleeds suffer from a combination of trauma-induced coagulopathies and surgical bleeding.  Hemorrhage is often unresponsive to transfusion therapy or surgical intervention.  Case reports are starting to surface in the medical literature about the off-label use of NovoSeven® for the adjunctive treatment of hemorrhage in this trauma population.  The mechanism of action NovoSeven® at the site of injury suggests that it may stop bleeding without causing a systemic, hypercoagulable state.  The NovoSeven® reacts with tissue factor at the site of injury and triggers platelet aggregation.  In these case reports the NovoSeven® utilized after other conventional therapeutic options had been exhausted.  The doses that were utilized ranged from 40 mcg/kg to 144 mcg/kg as a one time dose in most cases.  There were a few cases that received repeat doses, with 3 total doses listed in several of the case studies.  The NovoSeven® was reconstituted and administered according to package insert instructions.1,2,3     

NovoSeven® has also been used for the rapid reversal of warfarin-induced anticoagulation in patients with life-threatening hemorrhage.  This is again an off-label use for the drug.  A treatment protocol and standing orders are currently under review by the P&T Committee which would outline specific criteria for use and provide dosing information utilizing a weight based nomogram to determine the amount of NovoSeven®  to be given.  The NovoSeven® would be given in conjunction with the usual “standard of care” for treating warfarin induced bleeding: fresh frozen plasma and Vitamin K.4, 5

Reference:

1.  O’Neill, PA.  Bluth, M. et al.  Successful Use of Recombinant Activated Factor VII for Trauma-Associated Hemorrhage in a Patient without Preexisting Coagulopathy.  The Journal of TRAUMA Injury, Infection, and Critical Care.  Feb. 2002 Vol.52(2); pp.400-405.

2.  Dutton, RP.  Hess, JR.  Scalea, TM.  Recombinant factor VIIa for control of hemorrhage: early experience in critically ill trauma patients.  Journal of Clinical Anesthesia.  May 2003 Vol.15(3).

3.  Martinowitz, U.  Kenet, G. et al.  Recombinant Activated Factor VII for Adjunctive Hemorrhage Control in Trauma.  The Journal of TRUAMA Injury, Infection, and Critical Care.  Sept. 2001 Vol.51 (3); pp.431-439.

4.  Micromedex 2003. Volume 116. Drug Evaluations: Factor VII, therapeutic uses: Anticoagulation reversal

5.  Deveras RAE. Kessler, CM.  Reversal of Warfarin-Induced Excessive Anticoagulation with Recombinant Human Factor VIIa Concentrate.  Annals of Internal Medicine. Dec. 2002.  Vol.137 (11); pp.884-888.

 

 

Investigational Drug Services Updates:

 

Pediatric Trials:

Acetaminophen Study                      Medication will be taken from Suremeds

ANGIOMAX Study                            Medication will be stored in Main Pharmacy

AT-3 ECMO Study                            Medication will be stored in Gerlach Pharmacy

CAPS Study                                      Medication will be stored in Gerlach Pharmacy

Ketorolac Study                                 Medication will be stored in Gerlach Pharmacy

RESOLVE Study                              Medication stored in Gerlach Rx refrigerator

RSV Thickened Formula Study       Randomization list will be in Gerlach Pharmacy ID Binder (no drug involved)

           

Adult Trials

ADDRESS Study                              Medication stored in Gerlach Rx refrigerator

APOLLO Study                                 Medication will be stored in Main Pharmacy

BAXTER rAHF-PFM Study             Medication will be stored in Main Pharmacy

CORLOPAM Study                           Medication will be stored in Gerlach Pharmacy

CancerVax Study                              Medication stored in Main Rx Nitrogen freezer

DEDAS Study                                   Medication stored in Gerlach Rx refrigerator

ESAI Study                                        Medication stored in Gerlach Rx refrigerator

EXCLAIM Study                                Medication will be stored in Main Pharmacy

ONO Stroke Study                            Medication will be stored in Gerlach Pharmacy

PREVENT Study                               Medication will be stored in Main Pharmacy

SYNERGY Study                               Medication will be stored in Gerlach Pharmacy