AGGRASTAT DRUG REVIEW

1. Generic Name: Tirofiban Hydrochloride.
Trade name : Aggrastat
Chemical Name
It worksby blockingplateletsfromstickingtogethertoformbloodclots
INDICATION
Aggrastatis indicatedforthe preventionof earlymyocardial infarctionin patientspresentingwithacute
coronary syndromeswithoutSTelevation(NSTE-ACS) withthe lastepisodeof chestpainoccurring
within12 hoursand withECG changesand/orelevatedcardiacenzymes.. who are to be
managed medically and those undergoing a PCI such as PTCA
CONTRAINDICATION
1.Patientswithactive internalbleedingora historyof bleedingdiathesiswithinthe previous30 days.
2.Known history of intracranial hemorrhage,intracranialneoplasm, arteriovenousmalformation,or
aneurysm
3.Historyof stroke within 30 daysor any historyof hemorrhagicstroke.
4. Major surgical procedure orsevere physical traumawithinthe previousmonth.
5.History,symptoms,orfindingssuggestive of aorticdissection.
6. Severe hypertension(systolicBPabove 180 mm Hg and/or diastolicBPabove 110 mmHg).
7.Historyof thrombocytopenia(Plateletcount>100,000/mm3
).
8.Prothrombintime >1.3 OR INR>1.5
9.Hypersensitivitytoanycomponentof the product.
10.Severe liverfailure
: C22H36N2O5S•HCl•H2O
Action:
Theyworkby preventingplateletaggregationandthrombusformation.They dosobythe inhibitionof
Gp11b/111A receptoron the surface of platelets.

2. Pharmacology / Pharmacokinetics:
Absorption :
Onset:Rapidonset90%inhibitionofplateletaggregationoccurs bythe end of theIV loadinginfusion
administration(30mts)
Duration:Shortdurationofactionplateletaggregationpersists duringmaintenance infusion.Platelet
function generallyrecoverswithin4–8hours followingdiscontinuanceofinfusion
Distribution:
Tirofibanisnothighlyboundtoplasmaproteinsandproteinbindingisconcentrationindependentover
the range of 0.01 to 25 mcg/mL. Unboundfractioninhuman plasmais35%. The steadystate volume of
distributionof tirofibanrangesfrom22 to 42 litres.Tirofibancrossesthe placentainratsand rabbits.
Metabolism
Profiling of -labeled tirofiban in urine and faeces indicates that the radioactivity was accounted for mainly
by unchanged tirofiban. Circulating plasma radioactivity is accounted for mainly by unchanged tirofiban
(up to 10 hours postdose). These data suggest limited metabolism of tirofiban.
Excretion
Excreted65% inurine and approximately25% infeces,bothprimarilyasunchangeddrug.Tirofibanhas
a half-lifeof approximately2hours.Inhealthysubjects,the plasmaclearance of tirofibanrangesfrom
213 to 314 mL/min.Renal clearance accountsfor39 to 69% of plasmaclearance.
Administration and Dosage:
Presentation: (0.25 mg/mL) 50mL glass vial containing 12.5mg of tirofiban.
Tirofiban is initially given as rapid intravenous infusion
at a rate of 0.4mcg/kg/min for 30 minutes. Upon completion of the initial infusion,infusion,
AGGRASTAT should be continued at a maintenance infusion rate of 0.1 mcg/kg/min.
Prepration.
Withdraw 50ml from a 250 ml bag of 0.9% sodiumchloride or 5% dextrose in water and replace this volume with
50ml of Tirofiban injection,to achieve a final concentration of 50mcg/ml(0.05mg/ml).Mix well prior to
administration

3. PatientWeight
(kg)
Most Patients Severe Renal Impairment
30 Min Loading
Infusion Rate
(mL/hr)
Maintenance
Infusion Rate
(mL/hr)
30 Min Loading
Infusion Rate
(mL/hr)
Maintenance
Infusion Rate
(mL/hr)
30-37 16 4 8 2
38-45 20 5 10 3
46-54 24 6 12 3
55-62 28 7 14 4
63-70 32 8 16 4
71-79 36 9 18 5
80-87 40 10 20 5
88-95 44 11 22 6
96-104 48 12 24 6
105-112 52 13 26 7
113-120 56 14 28 7
121-128 60 15 30 8
129-137 64 16 32 8
138-145 68 17 34 9
146-153 72 18 36 9

4. Nursing Implications:
PRIOR TO ADMIISTRATION
 Thisdrug isgivento minimizebloodclottingandcardiacdamage.It mustbe givenIV.
 Knowthat the followingside effectsmayoccur: dizziness,lightheadedness,bleeding.
 All Vascularpuncture sitesshouldbe documentedand closelymonitor.
 Assessment History:Allergytoany componentof thisproduct,bleedingdiasthesis,hemorrhagic
stroke,active,abnormal bleedingorstroke within30days,uncontrolledorsevere hypertension,
majorsurgerywithin6 wk,dialysis,low plateletcount,aorticaneurysm, aorticdissection,
pregnancy,lactation,renal dysfunction&DrugEffects.
 Lab tests:Monitor plateletcount,HgbandHct before treatment,(within6hof infusingloading
dose),
 CheckVital signs.
 Verifythe dosage

AFTER ADMINISTRATION
 Monitorplateletcount,Hgband Hct after start of therapyand atleastonce dailythereafter
monitoraPTT, INR,.
 Withholddrugandnotifyphysicianif thrombocytopenia(platelets<100,000) isconfirmed.
 MonitorcarefullyforandimmediatelyreportS&Sof internal orexternal bleeding.
 Minimize unnecessaryinvasive proceduresanddevicestoreduce the riskof bleeding..
 Minimize arterial andvenouspunctures,IMinjections,catheterizations,intubationswhile using
thisdrug to minimizebloodloss.
Report: lightheadedness, palpitations, pain at IV site, bleeding.
Transfusionsof bloodand/orthrombocytesshouldalsobe consideredAGGRASTATcanbe removedby
hemodialysis
Patient / Family Education:
 Advise patients towatchcloselyforanysignsof bleedingorbruisingandtoreportthese to their
healthcare providerwhentheyoccur.
OVERDOSE
In clinical trials, inadvertent overdosage with tirofiban occurred in doses up to 5 times and 2 times the
recommended dose for bolus administration and loading infusion, respectively. Inadvertent overdosage
occurred in doses up to 9.8 times the 0.15 mcg/kg/min maintenance infusion rate
Overdosage of AGGRASTAT should be treated by assessment of the patient's clinical condition and
cessation or adjustment of the drug infusion as appropriate.

5.  Advise patientstodiscusswiththeirhealthcare providertheiruse of anyothermedications,
includingover-the-counterorherbal productspriortoAGGRASTAT use.
 Get emergencymedical helpif youhave anyof these signsof anallergicreaction:hives;
difficultybreathing;swellingof yourface,lips,tongue,orthroat.
Advise patientsto discuss with theirhealth care provider if they have any of these serious
side effects:
 nosebleedorotherbleedingthatwill notstop;
 black,bloody,ortarry stools;
 coughingupbloodor vomitthat lookslike coffee grounds;
 chestpainor heavyfeeling,painspreadingtothe arm or shoulder,nausea,sweating,generalill
feeling;
 suddennumbnessorweakness, especiallyonone side of the body;
 suddenheadache,confusion,problemswithvision,speech,orbalance;
 fever,chills,bodyaches,flusymptoms;or
pale skin,easybruisingorbleeding,weakness,fever,andurinatingmore orlessthanusual
Lessserious side effectsmayalsooccur,such as:
 nausea,stomachpain;
 runnyor stuffynose,cough,sore throat;or
 mildheadache ordizziness.