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NEW Medication: Ranolazine (Ranexa)  is a very interesting medicine. While it did not save lives, it substantially improved ischemic signs and symptoms. It acts by influencing the late sodium channel. This changes the diastolic properties of the heart. It changes the perfusion in the smaller blood vessels as well as improving the oxygen requirements. Indication of Use:  Angina pectoris, chronic Mechanism:  Ranolazine is a piperazine derivative and the mechanism of action of its anti-anginal and anti-ischemic effect is unknown. The anti-anginal and anti-ischemic action of ranolazine is not dependent upon heart rate or blood pressure reduction and does not increase myocardial workload. At therapeutic levels, ranolazine can inhibit the inactivating component of the sodium current (I(Na)) although its relationship to angina symptoms is uncertain. It also inhibits the rapid inward rectifying current (I(Kr)), thereby prolonging the ventricular action potential [3]. Adult Dosing: Angina pectoris, chronic: initial, 500 mg ORALLY twice daily; increase to the maximum recommended dose of 1000 mg ORALLY twice daily as needed based on clinical symptoms. Dose Adjustment: Concomitant moderate CYP3A inhibitors: maximum ranolazine dose is 500 mg twice daily Concomitant P-gp inhibitors: down-titrate ranolazine dose based on clinical response hepatic impairment (clinically significant); use is contraindicated renal impairment; plasma level increases up to 50% Contraindications: concurrent use of CYP3A inducers (eg, rifampin, rifabutin, rifapentine, phenobarbital, phenytoin, carbamazepine, and St. John's wort)   concurrent use of strong CYP3A inhibitors (eg, ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, and saquinavir)   hepatic impairment, clinically significant   Precautions: QTc interval prolongation may occur Side Effects: Gastrointestinal: Constipation (4.5% ), Nausea (4.4% ) Neurologic: Dizziness (6.2% ), Headache (5.5% ) Cardiovascular: Prolonged QT interval, Syncope How Supplied:  Oral Tablet, Extended Release: 500 MG, 1000 MG 5-2011

Adenosine (Adenocard) 6 mg IV bolus, may repeat at 12 mg IV bolus. for SVT, Narrow Complex Tachycardia or Wide Complex Tachycardia (Ref: NEJM 12/1991;325:1621 Review) * Adverse effects: dyspnea, flushing, chest discomfort or pain. * Supply: 6mg/2mL vial * Duration: less than 1 minute. Amrinone (Inocor) 0.75 mg/kg loading over 2-3 min, may repeat loading dose x1 30 min later prn, then 5-10 ug/kg/min. (Max: <10mg/kg/day) * Adverse risks: thrombocytopenia, arrhythmia, hypotension * Supply: 20 mL ampule of 5mg/mL Atropine 0.5 - 1.0 mg IV * Adverse risks: increased myocardial O2 consumption with tachycardia, ventricular tachycardia or fibrillation * Supply: 1 mg/10 ml, 0.5 mg/5 ml Bretylium (Bretylol) 250 - 500 mg or 5 mg/kg IV bolus, may repeat in 5 min at 10mg/kg, then 1 - 2 mg/min infusion * Adverse risks: N&V, postural hypotension, bradycardia, increased PVC, dizziness * Supply: 500 mg/10 ml; add 1 gm to 100-250 mL D5W (10-4 mg/mL conc.) Cardizem (Diltiazem) IV bolus for rate control of atrial fib/flutter. * Start 0.25 mg/kg IVP over 2 min (ave pt= 20mg dose), after 15 min if inadequate response, 0.35 mg/kg (ave pt = 25 mg dose) over 2 min; Infusion Rx start at 5 mg/h, range 10 - 15 mg/h. * Adversr risks: hypotension, arrhythmia, bradycardia, AV block, CHF, dizziness. * Supply: 5-10 mL vial of 5 mg/mL Dobutamine (Dobutrex) start 2 - 3 ug/kg/min, increase by 2 - 3 ug/kg/min q10 - 15min IV infusion, optimal maintenance doses : 7.5 - 20 ug/kg/min (Max: 40 ug/kg/min) * Adverse risks: tachycardia, dysrhythmias, headaches, anxiety, tremors, etc. * Supply: 250 mg/20 mL vial; add 250 mg in 250-500 mL D5W (1000-500 ug/mL conc.) * Duration: 10 - 12 min Dopamine (Intropin) usually up to 20 ug/kg/min IV infusion; (Max 20-50 ug/kg/min) (1-2 ug/kg/min dopaminergic; 2-5 ug/kg/min inotropic; 5-20 ug/kg/min vasoconstriction Alpha1) * Adverse risks: tachyarrhythmia, GI upset, angina, excessive vasoconstriction. * Supply: 200 mg/5 mL; add 200 mg in/ 500 mL D5W = 400 ug/mL) Epinephrine 0.5 - 1.0 mg IV * Adverse risks: tachyarrhythmia & increased myocardial O2 use. * Supply: 1 mg/1 ml of 1:1000, 1 mg/10 ml of 1:10,000 Isoproterenol (Isusprel) 2 - 20 ug/min IV (B agent effects: inotropic, chronotropic, vasodilatation, bronchodilatation)) * Usual dose 1 - 5 ug/min, up to 20 ug/min * Adverse risks: tachyarrhythmia, PVC & increased myocardial O2 use. * Supply: 1 mg/5 ml amp, may be added in 250-500 ml D5W = 4-2 ug/ml conc. Lidocaine 50 - 100 mg or 1 - 1.5 mg/kg IV bolus, may repeat in 3-5min upto total 3mg/kg loading, then 1 - 4 mg/min infusion * Adverse risks: CNS & myocardial depression, seizure * Supply: 100 mg/10 ml (1%), 100 mg/5 ml (2%); add 1 gm in 250 mL D5W = 4 mg/mL conc. Nitroglycerin (Tridil) IV infusion, start at 5 ug/min, then may increase at increment of 5 ug/min q3 - 5min till response seen. May give up to 80 - 160 ug/min if needed. * Adverse risks: hypotension * Supply: 1 amp=50mg/10ml added in 250 - 500 ml D5W Nitroprusside (Nipride) IV infusion * Ave dose 3 ug/kg/min, range 0.5 - 8 ug/kg/min (Max=800 ug/min) * Adverse risks: hypotension, N&V, headache, dizziness, restlessness, muscle twitching; cyanide poisoning (check blood thiocyanate, >10mg/100ml is considered toxic, >20mg/100ml may be fatal. * Supply: 1 amp=50 mg, added in 500 ml = 100 ug/ml. Procainamide (Pronestyl) 200 - 1000 mg IV, usually start @ 20 mg/min till total of 1 g (17mg/kg) or hypotensive, or QRS >50% wider, or PVC suppressed; then maintenance dose 2 - 6 mg/min. * Adverse risks: hypotension, prolonged QRS & QT interval * Supply: 2 mL vial of 500mg/mL, 10 mL vial of 100 mg/mL; add 1 gm in 250 mL = 4 mg/mL Propranolol (Inderal) usual dose 1 - 3 mg IV or at rate 0.5 - 1 mg/min to total dose of 0.15 - 0.2 mg/kg * Adverse risks: bradycardia, AV block, hypotension, mental depression, bronchospasm, etc. * Supply: 1mg/1mL ampule Verapamil (Isoptin) 0.075 - 0.15 mg/kg IV (usually about 5 - 10 mg IVP) * Adverse risks: bradycardia, AV block, hypotension, tachycardia, dizziness, etc. * Supply: 5mg/2mL, 10mg/4mL vial

Thrombolytics for acute myocardial infarction   2009  Indications of Thrombolytic RX in acute MI: ECG criteria: ST elevation > 1 mm in 2 contiguous limb leads or > 2 mm in 2 contiguous precordial leads obtain V3R and V4R if inferior or lateral changes consider if highly suggestive history and physical and any of left bundle branch block (LBBB) pathologic Q waves > 2 mm T wave inversion second or third degree AV block any arrhythmia Contraindications for Thrombolytic Rx: Absolute contraindications any  history of prior intracranial hemorrhage known structural cerebral vascular lesion (e.g. arteriovenous malformation) known malignant intracranial neoplasm (primary or metastatic) ischemic stroke within 3 months except acute ischemic stroke within 3 hours suspected aortic dissection  - mmediate CT with contrast or transesophageal echocardiography active bleeding or bleeding diathesis (excluding menses); history of bleeding disorder or anticoagulation, abnormal PT/PTT    significant closed-head or facial trauma within 3 months Relative contraindications severe uncontrolled hypertension on presentation (systolic blood pressure > 180 mm Hg or diastolic blood pressure > 110 mm Hg) chronic, severe, poorly controlled hypertension history of ischemic stroke > 3 months ago dementia known intracranial pathology not covered in absolute contraindications traumatic or prolonged (> 10 minutes) cardiopulmonary resuscitation within 3 weeks major surgery within 3 weeks internal bleeding within 4 weeks noncompressible vascular punctures pregnancy active peptic ulcer current use of vitamin K antagonists (higher international normalized ratio correlated with higher risk of bleeding) for streptokinase/anistreplase: prior exposure (> 5 days ago) ; prior allergic reaction to these agents * If excluded  from thrombolytic Rx, consider immediate percutaneous coronary intervention (PCI) Adjunctive Therapy to Thrombolytic Rx in acute MI Heparin: IV heparin is currently recommended by American College of Cardiology and American Heart Association for MI patients who have received thrombolytic therapy use of heparin after thrombolytics is controversial evidence does not support use of heparin after thrombolytics enoxaparin may be associated with fewer reinfarctions but more major bleeding than unfractionated heparin in patients treated with tenecteplase   Aspirin: aspirin 162 mg prior to thrombolysis might be as effective as aspirin 325 mg dose with lower risk of bleeding Abciximab (ReoPro) - antiplatelet agent abciximab in patients with acute ST-segment elevation myocardial infarction (STEMI) reduces mortality in patients treated with primary angioplasty but not in patients treated with fibrinolysis Dose: IV (adults) 250 mcg (0.25 mg/kg) bolus 10-60 min prior to PCI, followed by 0.125 mcg/kg/min (up to 10 mcg/min) continuous infusion for 12 hours; In patients wtih unstable angina not responding to conventional therapy & who are planned to undergo PCI within 24 hours, give 250 mcg (0.25 mg/kg) bolus followed by 10 mcg/min continuous infusion for 18-24 hr, ending 1hr after PCI.

Agents FDA approved for acute myocardial infarction: alteplase (Activase) - 2 doses infusion over 90 min anistreplase (Eminase) - single dose: 30 units over 3-5 minutes reteplase (Retavase) - double bolus, 30 min apart   streptokinase (Streptase or Kabikinase) - infusion over 60 min tenecteplase (TNKase) - single bolus over 5 seconds lanoteplase - new

Tenecteplase (TNKase) - easier to administer, single bolus over 5 seconds. For weight  > 90 kg: 50 mg given as single bolus dose over 5 seconds For weight 80-90 kg: 45 mg For weight 70-80 kg: 40 mg For weight 60-70 kg: 35 mg For weight  < 60 kg: 30 mg all patients given aspirin and heparin - Actions:  Binds to fibrin and converts plasminogen to plasmin.  It is a relatively fibrin-selective plasminogen activator, has greater resistance to plasminogen-activator inhibitors than alteplase.

Reteplase (Retavase) - double bolus, 30 min apart   given as double bolus dosing without continuous infusion, 10 units IV bolus over 2 minutes, repeated 30 minutes later; withhold second dose if serious bleeding or anaphylaxis occurs at least as effective as streptokinase, and without need for continuous infusion, may find role in prehospital care (The Medical Letter 1997 Feb 28;39(995):17) reteplase easier to administer when compared to alteplase with no significant differences in mortality or stroke

Streptokinase (Streptase/ Kabikinase): streptokinase 1.5 million units IV over 1 hour for acute MI circulating half-life - 23 minutes antigenic, so not recommended if patient has had prior streptokinase use should be given with aspirin and heparin (controversial) start heparin when aPTT < 50 seconds   For PE or DVT: 250,000 u IV over 30 min, followed by 100,000 u/hr infusion for 24-72 hr. Adverse risks: bleeding, fever & chills, rare anaphylactoid reaction Supply: 1.5 million u, 250,000 u 750,000 u vials.

t-PA:  Alteplase (Activase) - - also called recombinant tissue plasminogen activator (rt-PA) accelerated t-PA (tissue plasminogen activator) with IV heparin restricted to patients < 75, anterior AMI, symptoms < 4 hours t-PA 15 mg bolus, 0.75 mg/kg (up to 50 mg) over 30 minutes, 0.5 mg/kg (up to 35 mg) over 60 minutes heparin 5,000 units IV bolus and 1,000 units/hour, maintain PTT 60-85 seconds (1.5-2 times control) standard t-PA 100 mg over 3 hours IV given as 10 mg IV bolus, 50 mg over first hour, 20 mg/hour over next 2 hours, heparin same as for accelerated t-PA not antigenic, fibrin specific circulating half-life - 5 minutes given with aspirin and IV heparin For PE: 100 mg infusion over 2 hours. Adverse risks: bleeding, arrhythmias. Supply: 100mg. 50 mg, 20 mg vial

Anistreplase (Eminase) - Standard APSAC (anisoylated plasminogen/streptokinase activator complex) 30 units over 3-5 minutes circulating half-life - 90 minutes antigenic should be given with aspirin start heparin when aPTT < 50 seconds Adverse risks: arrhythmia/conduction disorders (38%), hypotension (10%), bleeding Supply: 30 units vial

Lanoteplase   a new thrombolytic in phase III clinical trials which allows single dosing genetically engineered recombinant form of plasminogen activator with long plasma half-life weight-adjusted single dose of lanoteplase vs. 90-minute infusion of t-PA in randomized trial of 15,078 patients within 6 hours of symptom onset of acute MI produced similar 6.77% vs. 6.6% all-cause mortality at 30 days, 1.13% vs. 0.62% intracranial hemorrhage (NNH 196)

Anti-arrhythmic Agents: Class IA: Quinidine, Procainamide, Norpace (Disopyramide) - increase QRS & QT interval, decrease conduction velocity & automaticity, increse effective refractory period & action potential duration. Class IB: Lidocaine, Phenytoin (Dilantin), Mexiletine (Mexitil), Tonocard (Tocainide), Moricizine (Ethmozine) - phenytoin decreases QT interval, others may or may not;  decrease conduction velocity & automaticity, may decrease effective refractory period & action potential duration. Class IC: Flecainide (Tambocar), Propafenone (Rythmol), Encainide, Lorcainide Flecainide 300 mg PO for PSVT or atrial fibrillation conversion; maintenance 100-200 mg bid PO Propafenone (Rythmol) 150-300 mg bid PO - increase QRS & QT & PR interval, decrease conduciton velocity & automaticity, increase effective refractory period, may increase action potential duration. Class II:  Beta blockers as Propranolol (Inderal), Sectral (acebutolol), Esmolol - decrease QT interval, decrease conduction velocity  & automaticity, increase effective refractive period. Class III: Amiodarone (Cordarone) 200 mg, Sotalol (Betapace), Bretylium Amiodarone 200 mg tab, start high loading dose of 800 mg for a few days, then 400 mg/d Sotalol 80-160-240 mg tab.  Start 80 mg bid, up to 160 mg bid PO - increase QRS, QT, PR intervals, decrease conduction velocity & automaticity, increase effective refractory period & action potential duration. Class IV: Calcium blockers as verapamil, diltiazem - no change in QRS or QT interval, may or may not increase PR interval, no change in conductin velocity or automaticity, or effective refractory period, decrease action potential duration.

      2011