| Drug | β-Receptor | Selectivity Dose |
|---|---|---|
| Propranolol | β1 and β2 | 20-80 mg bid |
| Metoprolol | β1 | 50-200 mg bid |
| Atenolol | β1 | 50-200 mg daily |
| Nebivolol | β1 | 5-40 mg daily |
| Nadolol | β1 and β2 | 40-80 mg daily |
| Timolol | β1 and β2 | 10-30 mg tid |
| Acebutolol* | β1 | 200-600 mg bid |
| Bisoprolol | β1 | 10-20 mg daily |
| Esmolol (IV) | β1 | 50-300 µg/kg/min |
| Labetalol | Combined α, β1, β2 | 200-600 mg bid |
| Pindolol* | β1 and β2 | 2.5-7.5 mg tid |
| Carvedilol | Combined α, β1, and β2 | 3.125-25 mg bid |
* intrinsic sympathomimetic activity.
| Drug | Duration of Action | Usual Dosage |
|---|---|---|
| Dihydropyridines | ||
| Nifedipine | Long | 30-180 mg/d |
| Amlodipine | Long | 5-10 mg/d |
| Felodipine (SR) | Long | 5-10 mg/d |
| Isradipine | Medium | 2.5-10 mg/d |
| Nicardipine | Short | 20-40 mg tid |
| Nondihydropyridines | ||
| Diltiazem | ||
| Immediate release | Short | 30-90 mg qid |
| Slow release | Long | 120-360 mg/d |
| Verapamil | ||
| Immediate release | Short | 80-160 mg tid |
| Slow release | Long | 120-480 mg/d |
| Preparation | Dosage | Onset (min) | Duration |
|---|---|---|---|
| Sublingual nitroglycerin | 0.3-0.6 mg PRN | 2-5 | 10-30 min |
| Aerosol nitroglycerin | 0.4 mg PRN | 2-5 | 10-30 min |
| Oral isosorbide dinitrate | 5-40 mg tid | 30-60 | 4-6 h |
| Oral isosorbide mononitrate | 10-20 mg bid | 30-60 | 6-8 |
| Oral isosorbide mononitrate SR | 30-120 mg daily | 30-60 | 12-18 h |
| 2% Nitroglycerin ointment | 0.5-2.0 in. tid | 20-60 | 3-8 h |
| Transdermal nitroglycerin patches | 5-15 mg daily | >60 | 12 h |
| Intravenous nitroglycerin | 10-200 µg/min | <2 | During infusion |
| Medication | Dosage | Comments |
|---|---|---|
| Aspirin (ASA) | 162-325 mg initial, then 75-100 mg | In patients taking ticagrelor, the maintenance dose of ASA should not exceed 100 mg. |
| Clopidogrel | 300-600 mg loading dose, 75 mg daily | In combination with ASA, clopidogrel (300-600 mg loading dose, then 75 mg/d) decreased the composite end point of cardiovascular death, MI, or stroke by 18-30% in patients with UA/NSTEMI |
| Ticagrelor | 180 mg loading dose, then 90 mg bid | Ticagrelor reduced incidence of vascular death, MI, or CVA (9.8% vs. 11.0%) but with higher major bleeding not related to CABG (4.5% vs. 3.8%) as compared to clopidogrel |
| Prasugrel | 60 mg loading dose, 10 mg daily | Prasugrel has increased antiplatelet potency compared to clopidogrel. Prasugrel reduced the incidence of cardiovascular death, MI, and stroke (9.9% vs. 12.1%) at the expense of increased major (2.4% vs. 1.1%) and fatal bleeding (0.4% vs. 0.1%), compared to clopidogrel |
| Eptifibatide | 180 µg/kg IV bolus, 2 µg/kg/mina | Eptifibatide reduces the risk of death or MI in patients with ACS undergoing either invasive or noninvasive therapy in combination with ASA and heparin. Compared to abciximab and tirofiban, eptifibatide has the most consistent effects on platelet inhibition with shortest on-time and drug half-life. |
| Tirofiban | 0.4 µg/kg IV bolus, 0.1 µg/kg/min | Tirofiban reduces the risk of death or MI in patients with ACS undergoing either invasive or noninvasive therapy in combination with ASA and heparin. |
| Abciximab | 0.25 mg/kg IV bolus, 10 µg/min | Abciximab reduces the risk of death or MI in patients with ACS undergoing coronary intervention. It should not be used in patients in whom percutaneous intervention is not planned. Platelet inhibition may be reversed by platelet transfusion. |
| Medication | Dosage | Comments |
|---|---|---|
| Heparin (UFH) | 60 units/kg IV bolus (maximum dose: 4000 units), 12-14 units/kg/h | Heparin therapy, when used in conjunction with ASA, has been shown to reduce the early rate of death or MI by up to 60%. The aPTT should be adjusted to maintain a value of 1.5-2.0 times control. |
| Enoxaparin (LMWH)a | 1 mg/kg SC bid | LMWH is at least as efficacious as UFH and may further reduce the rate of death, MI, or recurrent angina. LMWH may increase the rate of bleeding and cannot be reversed in the setting of refractory bleeding. LMWH does not require monitoring for clinical effect. |
| Fondaparinux | 2.5 mg SC daily | Fondaparinux has efficacy similar to that of LMWH with possibly reduced bleeding rates. |
| Bivalirudinb | 0.75 mg/kg IV bolus, 1.75 mg/kg/h | When used in conjunction with ASA and clopidogrel, bivalirudin is at least as effective as the combination of ASA, UFH, clopidogrel, and GPIIb/IIIa antagonists with decreased bleeding rates. May increase risk for stent thrombosis. Monitoring is required with a goal aPTT of 1.5-2.5 times control. |
a LMWH should be given at reduced dose (50%) in patients with a serum creatinine >2 mg/dL or GFR <30 mL/min.
b Bivalirudin requires dosage adjustment in patients with a GFR less than 30 mL/min or those on hemodialysis.
| Medication | Dosage | Comments |
|---|---|---|
| Aspirin (ASA) | 162-325 mg | Non-enteric-coated formulations (chewed or crushed) given orally or rectally facilitate rapid drug absorption and platelet inhibition. |
| Clopidogrel | 600 mg loading dose, 75-150 mg/d | 600 mg loading dose followed by 150 mg maintenance dose for 7 d may reduce the incidence of stent thrombosis and MI compared to the standard 300 mg loading dose and 75 mg maintenance dose. Caution should be used in the elderly because clinical trials validating clopidogrel use in STEMI either did not include elderly patients or did not use a loading dose. |
| Prasugrel | 60 mg loading dose, 10 mg/d | Compared to clopidogrel, prasugrel is a quicker acting and more potent antiplatelet agent with improved efficacy but did significantly increase CABG bleeding rates. Prasugrel should not be used in patients >75 y old, <60 kg, or with a history of stroke/TIA. |
| Ticagrelor | 180 mg loading, then 90 mg bid | ASA dose should not exceed 100 mg. Ticagrelor has shown mortality benefit over clopidogrel at the expense of higher bleeding rates. |
| Unfractionated heparin (UFH) | 60 units/kg IV bolus, 12 units/kg/h | UFH should be given to all patients undergoing PCI and those receiving thrombolytics with the exception of streptokinase. The maximum IV bolus is 4000 units. |
| Enoxaparin (LMWH) | 30 mg IV bolus, 1 mg/kg SC bid | Patients >75 y old should not be given a loading dose and receive 0.75 mg/kg SC bid. An additional loading dose of 0.3 mg/kg should be given if the last dose of LMWH was >8 h prior to PCI. The use of LMWH is only validated in thrombolysis and rescue PCI. |
| Bivalirudin | 0.75 mg/kg IV bolus, 1.75 mg/kg/h | Bivalirudin has been validated in patients undergoing PCI and has not been studied in conjunction with thrombolysis. Patients who received a heparin bolus prior to bivalirudin had a lower incidence of stent thrombosis than those who only received bivalirudin. |
| Fondaparinux | 2.5 mg IV bolus, 2.5 mg SC daily | Shown to be superior to UFH when used during thrombolysis with decreased bleeding rates. Fondaparinux increases the risk of catheter thrombosis when used during PCI. |
| Nitroglycerin | 0.4 mg SL or aerosol infusion; 10-200 µg/min IV | Sublingual or aerosol nitroglycerin can be given every 5 min for a total of three doses in the absence of hypotension. IV nitroglycerin can be used for uncontrolled chest discomfort. |
| Metoprolol | 25 mg PO qid, uptitrate as needed | β-Blockers should be avoided in patients with evidence of heart failure, hemodynamic instability, marked first-degree AV block, advanced heart block, and bronchospasm. |
| Medication | Dosage | Comments |
|---|---|---|
| Streptokinase (SK) | 1.5 million units IV over 60 min | Produces a generalized fibrinolytic state (not clot specific). SK reduces mortality following STEMI (18% RRR and 2% ARR). Skin rashes, fever, and anaphylaxis. Occasional in 10%, usually responds to volume expansion. If previously treated with SK, give alternate. |
| Recombinant tissue plasminogen activator (rt-PA) | 15 mg IV bolus | 0.75 mg/kg over 30 min (maximum 50 mg) 0.50 mg/kg over 60 min (maximum 35 mg) |
| Fibrin-selective agent with improved clot specificity compared to SK. | Does not cause allergic reactions or hypotension. | Mortality benefit compared to SK at the expense of an increased risk of intracranial hemorrhage. |
| Reteplase (r-PA) | Two 10-unit IV boluses administered 30 min apart | Fibrin selective agent with a longer half-life but reduced clot specificity compared to rt-PA. Mortality benefit equivalent to that of rt-PA. |
| Tenecteplase (TNK-tPA) | 0.50 mg/kg IV bolus (total dose 30-50 mg) | Genetically engineered variant of rt-PA with slower plasma clearance, improved fibrin specificity, and higher resistance to PAI-1. Mortality benefit equivalent to that of rt-PA with reduced bleeding rates (Lancet 1999;354:716). Monitoring is required with a goal aPTT of 1.5-2.5 times control. |