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89 Cards in this Set

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CCB mechanism in VASCULAR smooth muscle (3)
1)block L-type Ca channels, blocking Ca from entering the cell and blocking the following cascade
2)Ca-calmodulin complex activates MLCK
3)Active MLCK acts w/ Actin to cause contraction
CCB mechanism in cardiac myocyte (3)
1)block L-type Ca channels, blocking Ca from entering the cell and blocking the following cascade
2)Ca-Troponin complex is formed
3)Ca-Troponin acts w/ actin/myosin to cause a contraction
Benefit from CCB is derived from.... (4)
1)ARTERIAL DILATION
2)decr in afterload
3)(-) inotropic = decr cardiac work
4)CORONARY VASCULAR DILATION = incr O2 delivery to ischemic areas of myocardium
Advantage of dihydropyridine CCB's (2)
1)mostly cause arterial dilation
2)do NOT depress myocardium as much as other CCB's
ADR's of CCB (7)
1)HA
2)dizzines/syncope
3)flushing
4)nausea
5)edema
6)bradycardia, AV block, heart failure
7)reflex incr in adrenergic tone to heart (reduce by giving BB)
BB mechanism and use
1)block effect of adrenergic nerve stimulation of heart
2)primary use in treating exertional angina attacks
Major benefit of BB is derived from.... (6)
1)(-) chronotroptic
2)(-) inotropic effects
3)these decr cardiac work
4)decr SBP
5)decr myocardial O2 consumption
6)decr adrenergic tone to periphery
ADR of BB (3)
1)bradycardia, AV block, heart failure
2)CNS depression (fatigue, insomnia, depression)
3)caution w/ asthma, DM pts
Problem w/ BB and DM (2)
1)block tachycardia in hypoglycemia
2)blocks glycogenolysis in hypoglycemia
___ & ____ & ____ are all equivalent
1)CHD
2)CAD
3)IHD
#1 reason ppl die of an MI
LV arrthymias
ASA in PRIMARY prevention of IHD
a)dose
b)strengths available
c)half-life thing
d)inhibits ___ more than ___
a)75-162mg qd (81mg in women)
b)81,325,500,650mg
c)half life of ASA is 2-6h, platelet half-life is 7-10d; need just qd dosing of ASA b/c of long half-life of platelet
d)50x more potent inhibitor of COX1 than COX2
Plavix in PRIMARY prevention
a)dose
b)strengths available
c)it and ASA in Primary prevention
a)75mg qd
b)75mg only
c)use ASA or plavix NOT both in primary prevention, plavix is mainly used if ASA not tolerated
COX1 (4)
1)constitutive
2)less affected by inflammatory stimuli
3)CAUSES PLATELET AGGREGATION
4)in platelets, kidney, stomach
COX2 (5)
1)inducible
2)incr 10x by inflammatory stimuli
3)INHIBITS PLATELET AGGREGATION
4)causes vasodilation
5)in monocytes, macrophages
Angina is considered chronic stable angina if...
stable for 3 months
Taking NTG in SECONDARY intervention (2)
1)take prn chest pain or prior to activites known to precipitate an an attack
2)take 1 dose, if pain not relieved in 5 min take another, if pain not relieved in 5 min take a 3rd. Call ambulance as taking 3rd dose
1 dose of NTG will relieve pain in...
75% of pts in 3min
15% ar relieved by 15min
Other very important counsel pt w/ nitro
HAVE PT DATE THE BOTTLE
Antiplatelets in SECONDARY prevention (2) and schedule
1)ASA 75-162mg qd (less than 100mg in pt w/ GI bleed)
2)Plavix 75mg qd

On both for a year after an event then drop the plavix
When to start chronic stable angina MAINTENANCE therapy?
have more than 3 attacks per week
BB delay ST changes, is this good or bad?
Good; ST changes means problem with ventricular muscle
Good candidates for BB in MAINTENANCE therapy (3)
1)previous MI
2)heart failure
3)concurrent HTN
Which BB to be avoided? and which to use
ISA BB, acebutolol, pindolol, labetalol

USA non-ISA BB (b/c these will reduce HR and the others wont); atenolol, metoprolol, carvedilol, propanolol, timolol
BB in MAINTENANCE therapy "clinical points" (4)
1)target resting HR is 55-60; max exercise HR of 100
2)start low dose and titrate up
3)do not abruptly withdraw due to rebound anginal episodes; taper off over 2days
4)frequently combined w/ nitrates
Which CCB to NOT use in MAINTENANCE and why?
1)short acting
2)IR nifedipine
3)nicardipine

induce tachycardia
Which CCB to use? (and doses) (5)
1)felodipine 5-10qd
2)amlodipine 5-10qd
3)nifedipine XR 30-180qd
4)diltiazem
5)verapamil
DILTIAZEM DOSING IN MAINTENANCE (2 and bad SE)
1)IR 30-180 qid
2)XR 120-320 qd/bid

negative inotropic
VERAPAMIL DOSING IN MAINTENANCE (2 and bad SE)
1)IR 80-160 tid
2)XR 120-480 qd

negative inotropic
CCB's (IR DHP, XR DHP, non-DHP)
a)effect on HR
b)effect on contractility
a)IR DHP sharp incr in HR, XR DHP little/none incr in HR, non-DHP's decr in HR
b)non-DHP's decr contractility
Big ADR's of CCB (2)
1)peripheral edema (dhp)
2)constipation (verap)
Long acting nitrates dosing schedule (3)
1)effects are minimal after 1wk of chronic, continuous use due to tolerance
2)NO can no longer be made due to depletion of co-factors
3)Need 8-12h nitrate-free to avoid tolerance
Nitrates should not be given as....
MONOTHERAPY
Long Acting nitrates
a)brand
b)generic
c)dose
a)isosorbide mononitrate (imdur) 30-240mg qd
b)isosorbide dinitrate (isordil) 5-20mg bid
c)transdermal ntg (nitro-dur) 0.1,0.2,0.4,0.6,0.8mg/hr
Nitrate products w/...
a)fast onset (2)
b)slow onset (3)
a)IV, SL (tablet/spray)
b)oral, ointment, patch
Ranolazine
a)mechanism (3)
1)partial FA oxidase inhibitor
2)reduce intracellular Na leading to reduced Ca overload
3)this reduces intra-myocardial wall tension and contractile dysfxn
Ranolazine
a)reserved for....
b)Dose
c)CI in....
d)____ drug
a)pts who do NOT have adequate response to other anti-anginals
b)500mg bid
c)pts w/ QT prolongation
d)anti-ischemic drug
Ranolazine ADR's (5)
1)dizziness
2)HA
3)constipation/nausea
4)elevated SCr/BUN
5)QT prolongation (incr time b/w ventricle depo and repo)
Ranolazine Drug interactions (6)
1)azole antifungales
2)diltiazem/verapamil
3)amiodarone
4)digoxin
5)statins
6)macrolides
Coronary Artery Spasm (variant angina) treated w/...(4)
1)SL NTG
2)CCB
3)LA NTG
4)avoid BB
Silent myocardial ischemia treated w/...(2)
1)SL NTG
2)BB alone or w/ CCB
Syndrome X ischemia treated w/....(2)
1)BB
2)ACEI
Coronary Artery Spasm, silent myocardial ischemia, syndrome X NOT treated w/ ASA b/c....
NOT associated w/ platelet aggregation
Anticoagulation in SECONDARY prevention (2)
1)use antiplatelets or antiplatelets & warfarin
2)ASA 75-162mg qd plus plavix 75mg qd for 1 month to 1yr; continue ASA alone after this
When to use antiplatelet and warfarin in SECONDARY prevention and what INR wanted? (7)
1)anterior acute MI
2)acute MI w/ LV dysfxn
3)concomitant heart failure
4)previous emboli
5)presence of mural thrombosis
6)A.Fib
7)want INR 2-2.5
Inhibition of RAAS in SECONDARY prevention in WHO? (4)
1)suspected anterior wall MI
2)MI w/ heart failure
3)pts w/ no CI to ACEI
4)pts w/ heart failure or LV dysfxn
Inhibition of RAAS in SECONDARY prevention WHY? (3)
1)decr recurrent MI
2)decr progression of heart failure
3)decr mortality
Inhibition of RAAS in SECONDARY prevention HOW/WHEN? (3)
1)wait until thrombolytic treatment is complete
2)BP is stabilized
3)but ultimately ASAP after MI
Inhibition of RAAS in SECONDARY prevention CI (4)
1)SCr greater than 3
2)hx of angioedema or hyperkalemia
3)bilateral renal artery stenosis
4)pregnancy
Lisinopril
a)brand name
b)strengths available
c)common initial dose
d)goal dose
a)zestril, prinivil
b)2.5, 5, 10, 20, 30, 40mg
c)5mg qd
d)10mg qd
Captopril
a)brand name
b)strengths available
c)common initial dose
d)goal dose
a)capoten
b)12.5, 25, 50, 100tab and 5mg/ml solution
c)6.25mg qd
d)50mg bid-tid
Enalapril
a)brand name
b)strengths available
c)common initial dose
d)goal dose
a)vasotec
b)2.5, 5, 10, 20mg
c)5mg bid
d)10mg bid
Ramipril
a)brand name
b)strengths available
c)common initial dose
d)goal dose
a)Altace
b)1.25, 2.5, 5, 10mg
c)2.5mg qd
d)10mg qd
Anti-anginals in SECONDARY prevention in WHO?
EVERYONE with diagnosis of IHD
Anti-anginals in SECONDARY prevention WHY?
immediate treatment of ischemia w/ it can incr myocardial O2 supply and decr myocardial oxygen demand
Anti-anginals in SECONDARY prevention SL dose
0.3-0.4mg prn
BB in SECONDARY prevention in WHO? (5)
1)MI/previous MI
3)over 65yo
4)vertricular ectopy
5)evidence of heart failure
6)pts who are hemodynamically stable
BB in SECONDARY prevention WHY? (3)
1)decr ventricular arrhythmias
2)decr recurrent ischemia or re-infarction
3)decr mortality
BB in SECONDARY prevention in HOW/WHEN? (4)
1)within a few days (24h if possible) of event
2)continue indefinitely
3)make sure BP(systolic) and HR are stable (over 100 and 60)
4)avoid ISA BB's
Metoprolol 2 brand names
1)lopressor (IR)
2)toprol (xr)
Lopressor
a)available strengths
b)goal dose
a)50, 100mg
b)100mg bid
Toprol XL
a)available strengths
b)goal dose
a)25, 50, 100, 200mg
b)200mg qd
Atenolol
a)brand name
b)available strengths
c)goal dose
a)tenormin
b)25, 50, 100mg
c)100mg qd
Statins in SECONDARY prevention in WHO (1) and WHY (3)?
1)all pts after ACS regardless of LDL

1)reduces progression of atherosclerosis
2)decr CV events
3)decr mortality
Statins in SECONDARY prevention HOW/WHEN? (3)
1)ASAP during acute event
2)use high dose (lipitor 80mg qd)
3)monitor liver enzymes and lipid panel
Drug therapye after a stent placement (b/c they are thrombogenic) (3)
1)ASA 325mg qd plus plavix 75mg qd for 1yr
2)then ASA indefinetly
3)rethrombosis is most common due to non-compliance w/ the regimen
Drugs to avoid in pts w/ IHD (2)
1)sympathomimetics
2)COX2's and NSAIDS (b/c no longer balanced w/ COX1)
Vitamins/anti-oxidants in heart health
VitE, VitC, B-carotene showed NO DIFFERENCE FROM PLACEBO
Hormone replacement therapy and heart health (4)
1)HRT did NOT decr CHD
2)more CHD events in 1st yr; fewer in 4th/5th years
3)higher risk of VTE, stroke, breast cancer
4)fewer cases of hip fractures
Vasodilators generally have what structural feature?
N-rich rings
Hydralazine structural features (2)
1)ortho N's in
2)naphazoline ring
Minoxidil has what N rich ring
pyrimidine ring
Prazosin structural features (2)
1)meta N's in...
2)quinazoline ring
Sodium Nitroprusside contains/mechanism
IS INORGANIC; has Fe and cyano--the cyano is turned to N = vasodilation
Nitrates contain what (structurally)... (3)
1)nitrous/nitric acid
2)ester of polyol's (poly alcohcol)
3)N's are NOT directly attached to a C; have O inbetween
Nitrates 2 properties
1)avoid moisture in storage to eliminate hydrolysis
2)nonpolar so rapid absorption thru biomolecules
If a nitrate/ite has (0.25:1) next to it what does that mean?
0.25min til onset of axn

1min is duration of axn
Which act quicker Nitrous or nitric acid? and name ex
Nitrous acids; amyl nitrite
Relationship b/w # nitrous/ic acids in the nitrate and activity?
NONE
Enzyme that metabolizes nitrates? and location
glutiathione-nitrate reductase (hepatic/first pass and extrahepatic)
Structural similarites b/w classes of CCB's
NONE
1,4DHP derivative CCB properties (5)
1)Usually has 2CH3
2)2 esters
3)an N @ 1 w/ an H
4)R group at 4
5)N-benzene ring
Benzothiazepine derivative CCB properties (2)
1)benzene and
2)7 member ring w/ S,N (thiazepine)
Aralkylamine derivatives CCB properties (1)
1)basic N w/ alkyl/aryl
How do you make a CCB's half-life longer? (2)
1)add lipophilic structural features like...
2)make one of those methyl's an ether
LOOK AT DR. B'S NOTES AND RECOGNIZE THE DIFF CCB'S
n/a
Diltiazem
a)CCB derivative
b)metabolized to...
c)feature
a)benzothiazepine
b)desacetyl derivative w/ 25-50% of parent activity
c)2 chiral C's
Verapamil
a)CCB derivative
b)structural features (2)
a)Aralkylamine
b1)chiral C near central N
b2)central basic N to which alkyl/aralkyl groups are attached affect both heart AND arterial bed
In CCB's with chiral C's what isomer is more potent?
+ isomer