Term
| What are the two categories of CCBs? |
|
Definition
| nondihydropyridines (NDH) and dihydropyridines (DH) |
|
|
Term
| The catagories of CCB are based on the drug's predominant___________. |
|
Definition
|
|
Term
| nondihydropyridine (NDH)reduce ________ and affect cardiac ______ & ______. |
|
Definition
reduce permeability affect cardiac contractility and conduction |
|
|
Term
| Dihydropyridine (DH) vaso_____. |
|
Definition
|
|
Term
| DH generally have neutral or increased effects on vascular __________. |
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Definition
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|
Term
| What are two examples of NDHs? |
|
Definition
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|
Term
| This NDH is dosed at bedtime, PO or IV and can be given up to QID. |
|
Definition
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|
Term
| This NDH is dosed daily and is as known as Cardizem? |
|
Definition
|
|
Term
| What are some examples of Dihydropyridines (DH)? |
|
Definition
| "-pine": amlodipine (norvasc), Nicardipine (cardene), Clevidipine (cleviprex) |
|
|
Term
| What effect do CCBs have on myocardial oxygen demand and blood sypply? |
|
Definition
decreases myocardial oxygen demand increase myocardial blood sypply |
|
|
Term
| T/F: CCBs inhibit smooth muscle contration via dilating blood vessels and decreasing resistance to blood flow. |
|
Definition
|
|
Term
| CCBs dilate peripheral vessels. What is the effect of dilation? |
|
Definition
| decreased SVR, BP, and SVR...leading to decreased workload for the heart |
|
|
Term
| What do CCBs do that improves coronary blood flow? |
|
Definition
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|
Term
| Verapamil and Diltizem have what effect on contraction? |
|
Definition
| decrease myocardial contractile force leading to a negative inotropic effect |
|
|
Term
| Verapamil and Diltiazem delay impulse transmission through the ___ node by direct action. |
|
Definition
|
|
Term
| Nifedipine is a potent ____ vasodilator to create marked decrease in PVR. |
|
Definition
|
|
Term
| By decreasing PVR, Nifedipine reflexly stimulates the _______, leading to a slight increase in HR and may increase myocardial oxygen demand. |
|
Definition
|
|
Term
| Verapamil and Diltiazem is able to prevent reflex tachy through this mechanism. |
|
Definition
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|
Term
| Why might verapamil and diltiazem not be indicated for a pt with CHF? |
|
Definition
| they are more likely to worsen ventricular function in pt with CHF, leading to systolic dysfunction |
|
|
Term
| What are the five componets to the MOA of CCBs? |
|
Definition
1) inhibit the L-type Ca channel 2) bind to receptors 3) decrease in transmembrane Ca current 4) decrease sinus node conduction velocity 5) decrease AV node conduction velocity |
|
|
Term
| Where are L-type Ca channels present? |
|
Definition
| cardiac and smooth muscle |
|
|
Term
| By binding to receptors, CCBs convert this function of the channel. |
|
Definition
| convert the mode of operation of the channel |
|
|
Term
| What is the result of decreasing the transmembrane Ca current? |
|
Definition
| smooth muscle relaxation and reduction in contractility throughout the heart |
|
|
Term
| Vascular smooth muscle normally has high OR low intracellular Ca? |
|
Definition
|
|
Term
| smooth muscle contrations depends on an _______ of extracellular Ca through Ca channels located on the cell _______. |
|
Definition
| smooth muscle contraction depends on an INFLUX of extracellular Ca through Ca channels located on the cell MEMBRANE. |
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|
Term
| Pharmacologic effects of Verapamil |
|
Definition
Peripheral Vasodilation: increased!! HR: decrease!!! Contractility: decrease!! SA/AV conduction: decrease!! Coronary vasodilation: increase!! |
|
|
Term
| Pharmacologic effects of Diltiazem |
|
Definition
Peripherial vasodilation: increase!! HR: decrease!! contractility: decrease SA/AV conducion: decrease Coronary vasodialtion: increase!!! |
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|
Term
| Pharmacologic effects of dihydrophyridines (DH) |
|
Definition
peripheral vasodilation: increase!!! HR: increase/no effect contractility: decrease/no effect SA/AV conduction: no effect Coronary vasodilation: increase!!! |
|
|
Term
| what four areas of organ systems effects of seen with CCBs? |
|
Definition
| smooth, cardiac, and skeletal muscle effects, along with cerebral vasospasm |
|
|
Term
| T/F: Most types of smooth muscle are dependent on transmembrane Ca EFLUX for normal resting tone and contaractile responses? |
|
Definition
|
|
Term
| CCBs ______ smooth muscle |
|
Definition
|
|
Term
| In regards to arteries over veins, vascular smooth muscle is _______ sensitive to CCBs. |
|
Definition
most sensitive some activity is seen in broncholar, GI, and uterine smooth muscle |
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|
Term
| Cardiac muscle is highly dependent upon Ca influx for normal function. What do verapamil and diltiazem do to cardiac muscle? |
|
Definition
| they interact kinetically with the Ca channel receptor in a different manner than the dihydropyridines and block tachy in the Ca dependent cells more selectively |
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|
Term
| Is there an affect on skeletal muscle? |
|
Definition
| not affected, although Verapamil does prolong muscle paralysis (vecuronium) |
|
|
Term
| Cerebral vasospams and infarcts following SAH are treated with this drug |
|
Definition
|
|
Term
| How does nimodipine work(SAH and ruptured cerebral aneurysms)? |
|
Definition
| increases lipophilicity and cerebrovascular selectivity to improve outcomes due to cerebral artery spasm and subsequent neurologic deficits |
|
|
Term
| What organ metabolizes CCBs? |
|
Definition
|
|
Term
| If a patient has renal impairment: what is their CLcr and what % of the normal dose of Verapamil should be given |
|
Definition
CLcr < 10 (likely on dialysis) Dose: 50-75% dose |
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|
Term
| Is it okay to use diltiazem with active renal impairment? |
|
Definition
| use with caution (may start with 50% of the normal dose) |
|
|
Term
| If a patient has hepatic impairement what cautions should be taken with verapamil? |
|
Definition
| reduce dose to 20-50% of normal and monitor ECG |
|
|
Term
| What are the 5 clinical uses of CCBs? |
|
Definition
HTN SVT Coronary artery vasospasm angina cerebral artery vasospasm |
|
|
Term
| Verapamil is a nondihydropyridine. What are its uses? |
|
Definition
angina (vasospastic, angina perctoris, and unstable) arrhythmias: A fib or flutter and PSVT HTN HA prevention CHF (diastolic dysfunction) Bipolar (manic manifestations) |
|
|
Term
| True/False: Oral Verapamil IR would take 6-8 hours to have effect? |
|
Definition
|
|
Term
| What are some contraindications to Verapamil? |
|
Definition
a fib or flutter CHF cardiogenic shock hypersensitivity to CCBs symptomatic HYPOtension (SBP <90) 2nd or 3rd degree heart block ventricular tachycardia, wide-complex (QRS >/= 1.2 sec) |
|
|
Term
| When using Verapamil, what might be seen with combining inhalation anesthetics with its administration? |
|
Definition
decrease in INFLUX of Ca ions depressed cardiovasculature (may be excessive if not titrating each carefully) |
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|
Term
| What drug is absolutely contraindicated with the concomitant administration of verapamil? |
|
Definition
|
|
Term
| When giving Verapamil with Dofetilide (Tikosyn) what will be seen with plasma levels of dofetilide and what may occur? |
|
Definition
| 43% increase in plasma levels can cause serious ventricular arrhythmias (QT prolongation and/or torsades) |
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|
Term
| if a patient is taking an ACE inhibitor, diuretic, or beta blocker (oral anti-HTN agents), what symptoms may be seen? |
|
Definition
| an additive effect on lowing BP and HR |
|
|
Term
| Chronic verapamile treatment can increase these levels 50-75% during the first week? |
|
Definition
| Digoxin (doses must be properly adjusted to be well tolerated) |
|
|
Term
| Why would you monitor for signs of midazolam toxity if your patient is taking verapamil? |
|
Definition
| midazolam dosage reductions of up to 50% are suggested |
|
|
Term
| Why is it a concern to use verapamil with an HMG Co-A reductase inhibitor? |
|
Definition
| verapamil is an inhibitor of CYP 3A4 (simvastatin, lovastatin and atorvastatin are metabolized by CYP 3A4 adn these levels may be increased and place the pt at risk for toxicity) |
|
|
Term
| What are some contraindications to the use of Diltiazem? |
|
Definition
AMI with pulmonary congestion recent use of IV beta-blockers newborns (IV only r/t alcohol contents) ventricular tachy/fib(IV only) a fib/flutter causing fatal HR changes cardiogenic shock heart block symptomatic BP = 90 SSS without a venticular pacemaker |
|
|
Term
| What are the uses for Diltiazem? |
|
Definition
Like Verapamil: angina (vasospastic, angina perctoris, and unstable) arrhythmias: A fib or flutter and PSVT HTN HA prevention CHF (diastolic dysfunction) Bipolar (manic manifestations) |
|
|
Term
| True/False: Diltiazem PO has a faster onset than Verapamil? |
|
Definition
| True: 30-60 min vs. 1-2 hours |
|
|
Term
| What drugs interact with Diltiazem? |
|
Definition
| cyclosporine, carbamazepine,cimetidine, alfentanil, sufentanil, remifentanil, fentanyl, amiodarone, atazanavir(reyataz), enflurane, beta blocker, midazolam, digoxin, HMG Co-A reductase inhibitor |
|
|
Term
| What must happen to maintain cyclosporine trough levels similar to those prior to the addition of diltiazem? |
|
Definition
|
|
Term
| What may be seem with carbamazepine if given with diltiazem? |
|
Definition
| toxicity r/t elevated plasma levels (40-72%) |
|
|
Term
| Cimetidine use with have what effect on diltiazem plasma levels? |
|
Definition
| increase in peak levels (58%) and area-under-the curve (35%) after 1 week course of cimetidine |
|
|
Term
| What is increased when alfentanil and diltiazem interact? |
|
Definition
| alfentanil's half-life increases by 50%, CNS depressant time |
|
|
Term
| What enzyme is inhibited by diltiazem that metabolizes alfentanil? |
|
Definition
|
|
Term
| When giving alfentanil, should you reduce its dose or the dose of diltiazem? |
|
Definition
| dose of alfentanil may be reduced |
|
|
Term
| When giving verapamil or diltiazem these pain treatments may enhance bradycardic effects and hypotensive effects? |
|
Definition
| alfentanil, sufentanil, remifentanil, and fentanyl |
|
|
Term
| What may result if amiodarone is given with diltiazem? |
|
Definition
| brady, AV block and/or sinus arrest |
|
|
Term
| Does amiodarone inhibit CYP 450 3A4? |
|
Definition
|
|
Term
| What may occur if atazanavir (reyataz) is given with diltiazem and which drug shoudl be decreased in doseage? |
|
Definition
cardiotoxicity (prolonged PR interval), inhibition of diltiazem metabolism (CYP3A) Decrease diltiazem dose by 50% |
|
|
Term
| This inhaled anesthesic, when given with diltiazem, may result in additive depressant effect on AV nodal conduction and sinus node function? |
|
Definition
|
|
Term
| If you use CCBs, Beta blockers, and fentanyl what may happen to pt's BP? |
|
Definition
|
|
Term
| What may occur if you use a beta blocker with diltiazem? |
|
Definition
| hypotension, LVF, and AV disturbances |
|
|
Term
| How much should the dose of midazolam be reduced when using diltiazem? |
|
Definition
| 50% and monitor for toxicity |
|
|
Term
| True/False: when using diltiazem with digoxin there may be a 50% DECREASE in serum digoxin concentrations? |
|
Definition
| False: 50% increase in digoxin |
|
|
Term
| What will happen to the levels of HMG Co-A reductase inhibitors when used with diltiazem? |
|
Definition
| level can be increased, placing the pt at risk for toxicity |
|
|
Term
| how are dihydropyridines (DH) categorized? |
|
Definition
| based upon half-life and effect on contractility |
|
|
Term
| what is a short-acting PO DH? |
|
Definition
| nifedipine (capsule containing liquid) |
|
|
Term
| with is a short-acting injectable DH? |
|
Definition
|
|
Term
| What is the cardiac response to a longer-acting DH? |
|
Definition
| little cardiac depressant activity: felodipine, isradipine, nicardipine, nifedipine gtts and CC, and nisoldipine |
|
|
Term
| What longer-acting DH has no cardiac depressant activity? |
|
Definition
|
|
Term
| What are the uses of dihyropyridines (DH)? |
|
Definition
angina HTN renal protection in diabetics cerebral spasm r/t SAH (nimodipine) raynaud's phenomenon (nifedipine) |
|
|
Term
| What patients need to take precaution with the use of DH? |
|
Definition
CHF hypersensitivity to CCB SBP = 90 axacerbated angina liver impairment aortic stenosis defective lipid metabolism (clevidipine is in a lipid diluent) |
|
|
Term
| Should you use Nifedipine for HTN urgencies? |
|
Definition
| NO! Its use may be associated with severe hypotension, cerebral ischemia, AMI, fetal distress, conduction abnormalities and death |
|
|
Term
| The FDA indicates that Clevidipine (Cleviprex) may be used for what instances? |
|
Definition
reduction of BP when oral therapy is not feasible or desireable and is shown effective in perioperative control of BP an din patients with severe HTN SE: HA, N/V, A fib |
|
|
Term
| How soon can you double your initial IV dose of Clevidipine? |
|
Definition
| double dose in 90 second intervals |
|
|
Term
| Once you meet your BP goal, reduce the dose to < 2 times the dose what should the time between adjustments be increased to? |
|
Definition
|
|
Term
| What is the max dose of clevidipine in a 24 hour period and why? |
|
Definition
| max of 1000ml dose due to lipid load restriction |
|
|
Term
| How would you know if your clevidipine has reached an effective onset? |
|
Definition
| there would be a 3-5% decrease in SBP |
|
|
Term
| How long does it usually take to see a 15% decrease in SBP in a perioperative pt who has just recieved clevidipine? |
|
Definition
|
|
Term
| If you do not transition a pt to oral clevidipine, what may be seen? |
|
Definition
| rebound HTN after 72 hours |
|
|
Term
| When should you expect to see BP return to baseline after stopping a clevidipine infusion? |
|
Definition
|
|
Term
| How long is a clavidipine vial viable after the stopper has been punctured? |
|
Definition
|
|
Term
| what drugs interact with dihydropyridines (DH)? |
|
Definition
| beta blockers, cimetidine, cyclosprine, digoxin, fentanyl, triazole antifungals and imidazole antifungals |
|
|
Term
| What may be seen when using DH with a beta blocker? |
|
Definition
| hypotension or impair cardiac performance |
|
|
Term
| True/False: cimetidine may cause serum level elevations for most avaiable CCBs? |
|
Definition
|
|
Term
| True/False: Cimetidine is most contraindicated with nifedipine and diltiazaem r/t hemodynamic responses? |
|
Definition
|
|
Term
| IF you give cyclosprine with nifidipine you should expect to see an elevation in which drugs levels? |
|
Definition
|
|
Term
| Minimal effects on cyclosporine blood levels are seen when given with what three drugs? |
|
Definition
| nifedipine, isradipine, and nitrendipine |
|
|
Term
| What age group is at most risk for ginigival hyperplasia when using cyclosporine and nifedipine? |
|
Definition
|
|
Term
| What is significant to remeber when taking digoxin with CCBs (nigedipine, diltiazem, nicardipine, verapamil? |
|
Definition
| serum digoxin level increase by 50% |
|
|
Term
| The increase seen in digoxin serum levels when taking a CCB is dependent on what? |
|
Definition
|
|
Term
| What group of pt's are at highest risk for digoxin toxicity when taking a CCB? |
|
Definition
| those with a higher pre-existing serum digoxin concentration |
|
|
Term
| If a pt were to be given a CCB or beta blocker while undergoing fentanyl anesthesia would they develope HTN or hypotension? |
|
Definition
|
|
Term
| What is key when administering an antifungal to a pt on dihydropyridine CCBs? |
|
Definition
| antifungals inhibit CYP3A4 which is responsible for the metabolism of these CCBs and you may need to decrease the dose of your CCB due to the decreased metabolism |
|
|
Term
| When using a CCB and an antifungal what effects may be seen? |
|
Definition
| substantial peripheral edema and/or elevated CCB serum levels |
|
|