SIHD CCBs and nitrate tolerance

Question 1

what is the cardiac MOA of CCBs?

Answer 1

decrease influx of trigger Ca2+ in myocytes
decrease chronotrophy in nodal cells and inotrophy in myocytes

Question 2

what is vascular MOA of CCBs?

Answer 2

vasodilation

Question 3

how do DHPs affect HR?

Answer 3

increase due to reflex

Question 4

how do DHPs affect myocardial contractility?

Answer 4

decrease
no change (nifedipine)

Question 5

how do DHPs affect AV Nodal conduction?

Answer 5

no change

Question 6

how do DHPs affect vasodilation?

Answer 6

+++ in peripheral
++ in coronary

Question 7

how does verapamil affect HR?

Answer 7

decrease

Question 8

how does verapamil affect myocardial contractility?

Answer 8

double decrease

Question 9

how does verapamil affect AV nodal conduction?

Answer 9

double decrease

Question 10

how does verapamil affect vasodilation?

Answer 10

++ peripheral
+ coronary

Question 11

how does diltiazem affect HR?

Answer 11

decrease

Question 12

how does diltiazem affect myocardial contractility

Answer 12

decrease

Question 13

how does diltiazem affect AV nodal conduction?

Answer 13

decrease

Question 14

how does diltiazem affect vasodilation?

Answer 14

+ peripheral
++ coronary

Question 15

what CBBs have a 1:1 ratio?

Answer 15

verapamil, diltiazem
means equal vascular and myocardial selectivity

Question 16

what CCBs have a 10:1 ratio?

Answer 16

nifedipine
amlodipine

Question 17

what CCBs have a 100:1 ratio?

Answer 17

felodipine, isradipine, nicardipine
associated with vascular effects in toxicity

Question 18

what CCBs should be avoided due to reflex tachycardia?

Answer 18

nifedipine (procardia, adalat) 10-20mg TID
nicardipine (cardene) 20-40mg TID

Question 19

what CCBs are medium-acting?

Answer 19

nicardipine-SR (cardene SR)
isradipine (dynacirc)

Question 20

what DHP-CBBs are long acting?

Answer 20

amlodipine
felodipine ER
nifedipine-CC
nifedipine XL
nisoldipine-ER

Question 21

what is the brand name and dosing for felodipine-ER?

Answer 21

plendil - 5 to 10mg QD

Question 22

what is the brand and dosing for nifedipine XL/CC?

Answer 22

CC (Adalat-CC) 30-60mg QD
XL (Procardia) 30-60mg QD

Question 23

what is the brand and dosing of verapamil?

Answer 23

calan, isoptin
60-90mg TID-QID

Question 24

what is the brand and dosing for verapamil-SR?

Answer 24

calan-SR, isoptin-SR, covera-HS, verelan
240mg QD

Question 25

what is the brand and dosing of diltiazem?

Answer 25

cardizem 80-120mg TID

Question 26

what is the brand and dosing of diltiazem-SR

Answer 26

cardizem SR 60-120mg BID

Question 27

what is the brand and dosing of diltiazem-CD?

Answer 27

cardizem-CD 180-360mg QD

Question 28

what is the brand and dosing of diltiazem-XR?

Answer 28

dilacor-XR 180-540mg QD

Question 29

what is the brand and dosing of diltiazem-ER?

Answer 29

tiamate, tiazac 180-360mg QD

Question 30

what is the AE of DHP CBBs?

Answer 30

hypotension - flushing, HA, dizziness peripheral edema reduced myocardial contractility reflex adrenergic activation

Question 31

what is the AE of non-DHP CCBs?

Answer 31

reduced myocardial contractility AV/SA nodal conduction disturbances (bradycardia and AV block) hypotension - flushing, HA, dizziness constipation

Question 32

are verapamil or diltiazem AE worse?

Answer 32

verapamil

Question 33

what is nitrate tolerance?

Answer 33

decrease response in the presence of continuously or frequently administered nitrates

Question 34

how long should a nitrate free period be?

Answer 34

at least 10-12 hours biopharmaceutics and PK contribute to the amount of time required

Question 35

what type of modification occurs in nitrate tolerance?

Answer 35

covalent reversible modification on ALDH2 (inactivation on mitochondria)

Question 36

how is NTG SR tabs/caps dosed?

Answer 36

2-4 times day

Question 37

how is NTG ointment dosed?

Answer 37

3-4 times per day first dose: 7am then remove last 7-9 pm

Question 38

how is NTG patch dosed?

Answer 38

once daily on for 12-14hrs (starting at 7am) then off for 10-12hours (between 7-9pm)

Question 39

how is ISDN tabs dosed?

Answer 39

10mg 2-3 times per day 8am, 12pm, 4pm

Question 40

how is ISDN SR caps/tabs dosed?

Answer 40

1-2 times per day

Question 41

how is ISMN tabs dosed?

Answer 41

20mg 2 times per day 7 hours apart (8am, 3PM)

Question 42

how is ISMN SR tabs dosed?

Answer 42

30mg once daily at 8am not effective at night

Question 43

where should a NTG patch be placed?

Answer 43

between elbows and knees in a clean, dry, hairless skin that is not irritated, scarred, burned, broken, or calloused

Question 44

can you shower while wearing NTG patch?

Answer 44

yes

Question 45

what are other counseling points with NTG patches?

Answer 45

choose a different area each day do not cut patch wash hands before and after

Question 46

what is counseling associated with NTG ointment?

Answer 46

same as patch do not rub or massage ointment do not cover the area

Question 47

what is the moa of ranolazine?

Answer 47

inhibition of late inward Na+ current in ischemic myocytes decrease intracellular Na+ causes decrease in Ca2+ influx

Question 48

what does ranolazine not effect?

Answer 48

HR BP inotrophy perfusion like tradition anti-ischemic agents

Question 49

what is the dosing of ranolazine (ranexa ER)

Answer 49

500mg BID to 1000 BIG titrate over 1-2 weeks

Question 50

what is ranolazine indicated for in Europe (EMA)?

Answer 50

add on therapy for symptomatic treatment of pts with stable angina pectoris who are inadequately controlled or intolerant to first-line anti-anginal therapies

Question 51

what is ranolazine indicated for in the US?

Answer 51

treatment of chronic angina

Question 52

should ranolazine be used in combination therapy?

Answer 52

can add to CCBs, BB, or nitrates when inadequate response to monotherapy

Question 53

when should ranolazine be used as a monotherapy?

Answer 53

only when BP/HR is too low with first-line agent

Question 54

why is ranolazine prone to drug-drug interactions?

Answer 54

metabolized by CYP3A4 and CYP2D6 cannot be used with KTZ, ITZ, Pis, or clarithromycin OR CBZ, RIF, St johns wort

Question 55

what drugs require a limited dose of ranolazine?

Answer 55

diltiazem verapamil erythromycin fluconazole 500mg BID

Question 56

what is the AE of ranolazine?

Answer 56

CN dizziness HA dose-related increase in QT interval