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89 Cards in this Set
- Front
- Back
CCB mechanism in VASCULAR smooth muscle (3)
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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 |
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CCB mechanism in cardiac myocyte (3)
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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 |
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Benefit from CCB is derived from.... (4)
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1)ARTERIAL DILATION
2)decr in afterload 3)(-) inotropic = decr cardiac work 4)CORONARY VASCULAR DILATION = incr O2 delivery to ischemic areas of myocardium |
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Advantage of dihydropyridine CCB's (2)
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1)mostly cause arterial dilation
2)do NOT depress myocardium as much as other CCB's |
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ADR's of CCB (7)
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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) |
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BB mechanism and use
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1)block effect of adrenergic nerve stimulation of heart
2)primary use in treating exertional angina attacks |
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Major benefit of BB is derived from.... (6)
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1)(-) chronotroptic
2)(-) inotropic effects 3)these decr cardiac work 4)decr SBP 5)decr myocardial O2 consumption 6)decr adrenergic tone to periphery |
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ADR of BB (3)
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1)bradycardia, AV block, heart failure
2)CNS depression (fatigue, insomnia, depression) 3)caution w/ asthma, DM pts |
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Problem w/ BB and DM (2)
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1)block tachycardia in hypoglycemia
2)blocks glycogenolysis in hypoglycemia |
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___ & ____ & ____ are all equivalent
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1)CHD
2)CAD 3)IHD |
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#1 reason ppl die of an MI
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LV arrthymias
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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 |
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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 |
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COX1 (4)
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1)constitutive
2)less affected by inflammatory stimuli 3)CAUSES PLATELET AGGREGATION 4)in platelets, kidney, stomach |
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COX2 (5)
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1)inducible
2)incr 10x by inflammatory stimuli 3)INHIBITS PLATELET AGGREGATION 4)causes vasodilation 5)in monocytes, macrophages |
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Angina is considered chronic stable angina if...
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stable for 3 months
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Taking NTG in SECONDARY intervention (2)
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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 |
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1 dose of NTG will relieve pain in...
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75% of pts in 3min
15% ar relieved by 15min |
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Other very important counsel pt w/ nitro
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HAVE PT DATE THE BOTTLE
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Antiplatelets in SECONDARY prevention (2) and schedule
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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 |
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When to start chronic stable angina MAINTENANCE therapy?
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have more than 3 attacks per week
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BB delay ST changes, is this good or bad?
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Good; ST changes means problem with ventricular muscle
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Good candidates for BB in MAINTENANCE therapy (3)
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1)previous MI
2)heart failure 3)concurrent HTN |
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Which BB to be avoided? and which to use
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ISA BB, acebutolol, pindolol, labetalol
USA non-ISA BB (b/c these will reduce HR and the others wont); atenolol, metoprolol, carvedilol, propanolol, timolol |
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BB in MAINTENANCE therapy "clinical points" (4)
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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 |
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Which CCB to NOT use in MAINTENANCE and why?
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1)short acting
2)IR nifedipine 3)nicardipine induce tachycardia |
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Which CCB to use? (and doses) (5)
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1)felodipine 5-10qd
2)amlodipine 5-10qd 3)nifedipine XR 30-180qd 4)diltiazem 5)verapamil |
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DILTIAZEM DOSING IN MAINTENANCE (2 and bad SE)
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1)IR 30-180 qid
2)XR 120-320 qd/bid negative inotropic |
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VERAPAMIL DOSING IN MAINTENANCE (2 and bad SE)
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1)IR 80-160 tid
2)XR 120-480 qd negative inotropic |
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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 |
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Big ADR's of CCB (2)
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1)peripheral edema (dhp)
2)constipation (verap) |
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Long acting nitrates dosing schedule (3)
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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 |
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Nitrates should not be given as....
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MONOTHERAPY
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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 |
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Nitrate products w/...
a)fast onset (2) b)slow onset (3) |
a)IV, SL (tablet/spray)
b)oral, ointment, patch |
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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 |
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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 |
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Ranolazine ADR's (5)
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1)dizziness
2)HA 3)constipation/nausea 4)elevated SCr/BUN 5)QT prolongation (incr time b/w ventricle depo and repo) |
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Ranolazine Drug interactions (6)
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1)azole antifungales
2)diltiazem/verapamil 3)amiodarone 4)digoxin 5)statins 6)macrolides |
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Coronary Artery Spasm (variant angina) treated w/...(4)
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1)SL NTG
2)CCB 3)LA NTG 4)avoid BB |
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Silent myocardial ischemia treated w/...(2)
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1)SL NTG
2)BB alone or w/ CCB |
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Syndrome X ischemia treated w/....(2)
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1)BB
2)ACEI |
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Coronary Artery Spasm, silent myocardial ischemia, syndrome X NOT treated w/ ASA b/c....
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NOT associated w/ platelet aggregation
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Anticoagulation in SECONDARY prevention (2)
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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 |
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When to use antiplatelet and warfarin in SECONDARY prevention and what INR wanted? (7)
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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 |
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Inhibition of RAAS in SECONDARY prevention in WHO? (4)
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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 |
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Inhibition of RAAS in SECONDARY prevention WHY? (3)
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1)decr recurrent MI
2)decr progression of heart failure 3)decr mortality |
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Inhibition of RAAS in SECONDARY prevention HOW/WHEN? (3)
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1)wait until thrombolytic treatment is complete
2)BP is stabilized 3)but ultimately ASAP after MI |
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Inhibition of RAAS in SECONDARY prevention CI (4)
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1)SCr greater than 3
2)hx of angioedema or hyperkalemia 3)bilateral renal artery stenosis 4)pregnancy |
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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 |
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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 |
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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 |
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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 |
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Anti-anginals in SECONDARY prevention in WHO?
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EVERYONE with diagnosis of IHD
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Anti-anginals in SECONDARY prevention WHY?
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immediate treatment of ischemia w/ it can incr myocardial O2 supply and decr myocardial oxygen demand
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Anti-anginals in SECONDARY prevention SL dose
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0.3-0.4mg prn
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BB in SECONDARY prevention in WHO? (5)
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1)MI/previous MI
3)over 65yo 4)vertricular ectopy 5)evidence of heart failure 6)pts who are hemodynamically stable |
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BB in SECONDARY prevention WHY? (3)
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1)decr ventricular arrhythmias
2)decr recurrent ischemia or re-infarction 3)decr mortality |
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BB in SECONDARY prevention in HOW/WHEN? (4)
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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 |
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Metoprolol 2 brand names
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1)lopressor (IR)
2)toprol (xr) |
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Lopressor
a)available strengths b)goal dose |
a)50, 100mg
b)100mg bid |
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Toprol XL
a)available strengths b)goal dose |
a)25, 50, 100, 200mg
b)200mg qd |
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Atenolol
a)brand name b)available strengths c)goal dose |
a)tenormin
b)25, 50, 100mg c)100mg qd |
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Statins in SECONDARY prevention in WHO (1) and WHY (3)?
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1)all pts after ACS regardless of LDL
1)reduces progression of atherosclerosis 2)decr CV events 3)decr mortality |
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Statins in SECONDARY prevention HOW/WHEN? (3)
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1)ASAP during acute event
2)use high dose (lipitor 80mg qd) 3)monitor liver enzymes and lipid panel |
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Drug therapye after a stent placement (b/c they are thrombogenic) (3)
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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 |
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Drugs to avoid in pts w/ IHD (2)
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1)sympathomimetics
2)COX2's and NSAIDS (b/c no longer balanced w/ COX1) |
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Vitamins/anti-oxidants in heart health
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VitE, VitC, B-carotene showed NO DIFFERENCE FROM PLACEBO
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Hormone replacement therapy and heart health (4)
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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 |
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Vasodilators generally have what structural feature?
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N-rich rings
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Hydralazine structural features (2)
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1)ortho N's in
2)naphazoline ring |
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Minoxidil has what N rich ring
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pyrimidine ring
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Prazosin structural features (2)
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1)meta N's in...
2)quinazoline ring |
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Sodium Nitroprusside contains/mechanism
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IS INORGANIC; has Fe and cyano--the cyano is turned to N = vasodilation
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Nitrates contain what (structurally)... (3)
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1)nitrous/nitric acid
2)ester of polyol's (poly alcohcol) 3)N's are NOT directly attached to a C; have O inbetween |
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Nitrates 2 properties
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1)avoid moisture in storage to eliminate hydrolysis
2)nonpolar so rapid absorption thru biomolecules |
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If a nitrate/ite has (0.25:1) next to it what does that mean?
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0.25min til onset of axn
1min is duration of axn |
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Which act quicker Nitrous or nitric acid? and name ex
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Nitrous acids; amyl nitrite
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Relationship b/w # nitrous/ic acids in the nitrate and activity?
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NONE
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Enzyme that metabolizes nitrates? and location
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glutiathione-nitrate reductase (hepatic/first pass and extrahepatic)
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Structural similarites b/w classes of CCB's
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NONE
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1,4DHP derivative CCB properties (5)
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1)Usually has 2CH3
2)2 esters 3)an N @ 1 w/ an H 4)R group at 4 5)N-benzene ring |
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Benzothiazepine derivative CCB properties (2)
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1)benzene and
2)7 member ring w/ S,N (thiazepine) |
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Aralkylamine derivatives CCB properties (1)
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1)basic N w/ alkyl/aryl
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How do you make a CCB's half-life longer? (2)
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1)add lipophilic structural features like...
2)make one of those methyl's an ether |
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LOOK AT DR. B'S NOTES AND RECOGNIZE THE DIFF CCB'S
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n/a
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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 |
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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 |
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In CCB's with chiral C's what isomer is more potent?
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+ isomer
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