Antianginal drugs

Question 1

Nitrates, Nitroglycerin, Isosorbide Type & indication

Answer 1

terminate or prevent (prophylactic) exercise induced-myocardial ischemia. Can use for all three types of angina (stable/unstable/Prinzmetal), HTN emergencies, CHF

Question 2

Nitrates, Nitroglycerin, Isosorbide MOA

Answer 2

Relaxation is endothelium INDEPENDENT–even in presence of damaged endothelium. Effects on heart (coronary vasodilation) and on systemic circulation (BOTH arterial and venules) reducing venous return to heart (dilate capacitance vessels, veins), which decreases wall tension/preload to heart).

Question 3

Nitrates, Nitroglycerin, Isosorbide Drug Action/Pd

Answer 3

Activates GC, and increases cGMP, dephosphorylates myosin light chains, leads to vasodilation. NO donor. Four big effects (both ARTERY & VEIN): Decreased Venous Return (Dilated Venous Capacitance Vessels); Reduced LV Wall tension (decreased preload); Reduced Afterload (arterial effects); Direct coronary artery vasodilation (increased perfusion to subendocardium)

Question 4

Nitrates, Nitroglycerin, Isosorbide PK

Answer 4

note that nitroglycerin is not given orally..but isosorbide dinitrate can be given orally

Question 5

Nitrates, Nitroglycerin, Isosorbide Route of Admin

Answer 5

nitroglycerin–sublingual, spray, patch, ointment isosorbide nitrate–sublingual, chewable, oral. These 2 are the most popular.

Question 6

Nitrates, Nitroglycerin, Isosorbide Adverse Effects

Answer 6

largely due to therapeutic exaggeration: orthostatic hypertension (decreased venous return), reflex tachycardia (baroreceptor), “pounding” headache (vasodilation of the cerebral vessels). Also nitrate tolerance.

Question 7

Nitrates, Nitroglycerin, Isosorbide Contra-indication

Answer 7

do not give nitrates to men on Viagra, Cialis or any ED vasodilator drugs–they can have a hypotensive episode and die (albeit with a boner).

Question 8

Nitrates, Nitroglycerin, Isosorbide Notes

Answer 8

Note that you generally give something else with nitrates (B-Blockers, etc) to prevent reflex tachycardia. Note nitroprusside cannot be given orally b/c it will convert to cyanide and poison patients!

Question 9

Verapamil, Diltiazem, Nefedipine Type & indication

Answer 9

L-Type Ca channel blockers (CCB’s): angina pectoris, HTN, arrythmias, hypertrophic cardiomyopathy (HOMI), migraine, Raynaud’s phenomenon

Question 10

Verapamil, Diltiazem, Nefedipine MOA

Answer 10

WORKS ON ARTERIES & on Cardiac PACEMAKER (upstroke of AP is Ca for SA/AV nodes) and Cardiac MUSCLE! Negative inotropy (contractility)-Negative chronotropy (heart rate), Vasodilatory effects (smooth mm around arteries)

Question 11

Verapamil, Diltiazem, Nefedipine Drug Action/Pd

Answer 11

most cardiologists use Diltiazem for treatment b/c moderate vasodilatory effects (hi vasodilation can lead to reflex tachy) and intermediate effect on inotropy & chronotropy.

Question 12

Verapamil, Diltiazem, Nefedipine PK

Answer 12

Contractility: Vera, Dilt, Nife Chronotropy: Vera, Dilt, Nife Vasodilatory: Nife, Dilt, Vera

Question 13

Verapamil, Diltiazem, Nefedipine Adverse Effects

Answer 13

Vera & Dila: Bradycardia leading to CHF/Heart Block, Hypotension (extreme effect). Nefedipine (dihydropyriadine): Reflex Tachy (vasodilation), Peripheral Edema (hydrostatic P in arts), Hypotension.

Question 14

Verapamil, Diltiazem, Nefedipine Contra-indication

Answer 14

don’t give CCB’s if you suspect heart failure (CHF) in your patient–you don’t want to compromise inotropy/contractility!

Question 15

Verapamil, Diltiazem, Nefedipine Notes

Answer 15

note that Ca channel in skeletal mm is structurally distinct!; artery selectivity can result in coronary steal! This is why they usually don’t use Nefedipine b/c it acts so selectively on vessels!

Question 16

B-Blockers Type & indication

Answer 16

angina pectoris, HTN, arrythmias (class II), post-MI (improves survival), Dissecting Aortic Aneurysm, Mitral Valve Prolapse, Hyperthyroidism (acutely), Migraine

Question 17

B-Blockers MOA

Answer 17

Reduce demand on the heart. Note B-Receptor on heart (B1) is hooked up to Gs and increases cAMP. cAMP opens L-type Ca channels, increases Ca reuptake, increases pacemaker current and increases rate of conduction. If B-receptor is blocked then cAMP is lowered and all of these effects are decreased.

Question 18

B-Blockers Drug Action/Pd

Answer 18

Some are cardioselective B1-Atenolol, Metoprolol. Some are not selective-Propranolol, Nadolol.

Question 19

B-Blockers PK

Answer 19

Duration of action may vary–Esmolol very short, Nadolol 2x daily dosing. Watch lipid soluability too*.

Question 20

B-Blockers Route of Admin

Answer 20

oral

Question 21

B-Blockers Adverse Effects

Answer 21

Bronchospasm, Peripheral Vasospasm (B2), bradycardia, CNS effects (worse if lipid soluable: depression, insomnia, fatigue), Sexual dysfunction.

Question 22

B-Blockers Contra-indication

Answer 22

watch diabetics (decreased response to hypogly, B2 liver), asthmatics or lung problem (block of B2 vasodilation), existing bradycardia, heart block, acute CHF, PVD.

Question 23

B-Blockers Notes

Answer 23

BB’s not recommended in prinzmetal (vasospasm) angina