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13 Cards in this Set
- Front
- Back
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Angina pectoris: pharmacotherapy
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Balancing the O2 demand/supply equation
BB, NTG, CCB ↑ O2 Supply by vasodilation -↑Coronary flow --Nitroglycerin (nitrates/NTG) --Dihydropyridine (DHP) CCBs -Prevent thrombus formation --Aspirin --Thienopyridines (clopidogrel ↓ O2 Demand -↓HR --Beta Blockers (BB) --Non-dihydropyridine (NDHP) CCBs -↓Ventricular Wall Force --BB --ACEI/ARB -↓Preload --NTG |
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Beta blockers
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Atenolol
Metabolism: Renal Receptor Activity: B1 Lipid Solubility: Low ISA: No Carvedilol Metabolism: Hepatic Receptor Activity: a1, B1, B2 Lipid Solubility: Moderate ISA: No Labetalol Metabolism: Hepatic Receptor Activity: a1, B1, B2 Lipid Solubility: Low ISA: No Metoprolol Metabolism: Hepatic Receptor Activity: B1 Lipid Solubility: Moderate ISA: No Pindolol Metabolism: Hepatic Receptor Activity: B1, B2 Lipid Solubility: Moderate ISA: Yes Propanolol Metabolism: Hepatic Receptor Activity: B1, B2 Lipid Solubility: High ISA: No |
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Beta blocker adjunctive therapies and contraindications
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Maintenance therapy (Post-MI period)
Titrate doses (switch metoprolol to bid) Goals: HR ____ bpm, BP _____mm Hg Contraindications -Hypotension, Bradycardia -Decompensated HF -Active bronchoconstriction |
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Nitrates: mechanism
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↑ intracellular cGMP
venodilator =↓ preload arterial vasodilator = ↑ O2 supply |
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Short duration nitrates formulation, onset, duration, monitoring, side effects
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Sublingual NTG
<1-3 min onset 10-30 min duration Spray NTG 2-4 min onset 10-30 min duration IV NTG <1 min onset 3-5 min duration Ointment NTG <30 min onset 4-8 hour duration Monitor BP and HR Side effects: Headache |
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Longer duration nitrates formulation, onset, duration
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Sustained release ISDN
15-40 min onset 4-8 hr duration Patch NTG 30 min onset 12-16 hour duration Oral ISMN 30-60 min onset 16 hour duration ISDN = Isosorbide DiNitrate NTG = Nitroglycerin ISMN = Isosorbide MonoNitrate |
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Nitrates: tolerance, contraindications
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Nitrate Tolerance
-Need to become activated -Reactive molecules that combine with nitrates to activate are depleted from body -Treat with nitrate free interval Contraindications -Co-administration with sildenafil (Viagra®), vardenafil (Levitra®), tadalafil (Cialis®) -Right Ventricular (RV) infarcts -Critical aortic valve stenosis Evidence of improved survival? -not been proven -good for symptomatic relief only |
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CCB (non-DHP)
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Verapamil and diltiazem
Metabolism: Hepatic Compelling indications: Angina, AFib w/ rapid ventricular response (RVR) Contraindications: Bradycardia, systolic HF Decreases HR contractility and vascular resistance |
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CCB (DHP)
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End in -dipine
-ex: Amlodipine Metabolized by liver Compelling indication: Angina, CKD Contraindication: Hypertensive emergency, AMI Causes reflex tachycardia Decreases vascular resistance Not shown to improve survival -symptomatic relief Side effect: pedal edema |
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Ranolazine mechanism, use, drug interactions, side effects
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Inhibits late Na+ entry into cell/prevents Ca+2 overload
Chronic stable angina -Add-on to background Tx -Intolerance to traditional Tx 500-1000mg twice daily Drug Interactions -CYP 3A4 substrate & inhibitor --(diltiazem, verapamil, simvastatin, SSRIs) -CYP 2D6 inhibitor --(Tricyclic antidepressants, antipsychotics) -Digoxin QT prolongation |
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Prinzmetal's angina (Vasospastic angina)
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Acute clamping down of coronary artery
Usually not associated with thrombus formation May or may not be associated with atherosclerosis Treatments -Nitrates (long acting) --NTG patches, Isosorbide mononitrate -CCBs (DHP or non-DHP) --SR diltiazem, verapmail; amlodipine, felodipine -Avoid BB |
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Anti-angina drugs with other medical conditions
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HTN
-BB, CCB Migraines -BB, CCB Asthma -NDHP CCB -Avoid BB (especially noncardioselective) Hyperthyroidism -BB Diabetes -BB with caution, CCB Systolic HF -BB, nitrates, may consider DHP -Avoid NDHP CCB Diastolic HF -BB or NDHP CCB -Avoid DHP CCB Afib/flutter -BB or NDHP CCB Bradyarrhythmias -DHP CCB -Avoid BB, NDHP CCB Supraventricular arrhythmias -BB or NDHP CCB Ventricular arrhythmias -BB |
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Anti-platelet therapies
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Aspirin
Indication: ACS, CSA, stroke prophylaxis MOA: TxA2 inhibition by blocking cyclooxygenase irreversible Onset: 5 min Duration: 5 days Side effects: GI upset, angioedema Ticlopidine Indication: Thrombotic stroke, PCI/stent MOA: PGY-12 inhibition (ADP) irreversible Onset: 6 hrs; 3-5 day peak Duration: 5 days Side effects: rash, neutropenia, GI upset, TTP Clopidogrel Indication: ACS, PCI/stent, PAD, thrombotic stroke MOA: PGY-12 inhibition irreversible Onset: 2 hours; 3-7 days Duration: 5 days Side effects: Rash, TTP Prasugrel Indication: ACS, PCI/stent MOA: PGY-12 inhibition irreversible Onset: .5-1 hr; 3-7 days Duration: 7-10 days Side effects: Rash, avoid use in TIA/stroke, age >75, <60kg Ticagrelor Indication: ACS, PCI/stent MOA: PGY-12 inhibition reversible Onset: 2 hours Duration: up to 5 days Side effects: Dyspnea, increased serum creatinine, increased uric acid |
