Pathopharm Exam 2-S4 Flashcards by Brad Koester

This receptor affects the arteries more than veins.
-Increases vascular tone by vasoconstriction to increase Blood pressure?

Alpha-1 receptor

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This receptor is found primarily on heart and increases heart rate and contractility.
-Also increases risk of arrhythmias?

Beta-1 receptor

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This receptor is found in arteries and veins and inhibits adenyl cyclase to decrease norepinephrine release and increase parasympathetic outflow?

Alpha-2 receptor

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This receptor causes smooth muscle relaxation and should be avoided with asthmatic patients?

Beta-2 receptor

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This drug is an alpha-1 and alpha-2 agonist.
- Endogenous catecholamine.
- Arterial and Venous constriction
- Increase BP, SVR and PVR
- may slow HR due to baroreceptor mechanism
- Does not increase myocardial O2 consumption
- Dose not cross BBB

Norepinephrine (Levophed)

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This drug is an alpha-1 agonist
- Causes vasoconstriction, bradycardia
- Coronary vasoconstrictor
- Increase BP, SVR, PVR, and afterload.
- May need to add dopamine to keep HR up.
- Often used in neurologic shock
- Contraindicated w narrow angle glaucoma

Neosynephrine (Phenylephrine)

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This drug is a beta-1 agonist
- Synthetic catecholamine
- reduced preload and afterload
- increases contractility, CO, HR and BP.
- Also increases myocardial O2 demand.
- May drop BP if patient is dehydrated.

Dobutamine

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This drug is a beta-1 and alpha-1 agonist and works at DA receptors
- First line agent for shock
- Naturally occurring catecholamine
- Precursor to norepi
- Dilates/increases renal blood flow

Dopamine

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Low dose Dopamine affects what?
1-3 mcg/kg/min

Renal, coronary and cerebral vasodilation. Increased urinary output

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Mid dose Dopamine affects what?
3-10 mcg/kg/min

Beta-1 stimulation with positive ionotropic effect.
Increased HR and small BP increase

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High dose Dopamine affects what?
>10 mcg/kg/min

Alpha-1 stimulation with potent vasoconstriction.
Increased BP and increased SVR

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This drug is a beta-1 and alpha-1 agonist
- Endogenous catecholamine
- causes peripheral and global vasoconstriction
- Bronchodilation
- NOT first line treatment
- Increases cardiac contractility and O2 demand.
- Increased HR, MAP, CO, SVR, PVR
- Risk of arrhythmia development
- Systolic increase and diastolic decrease
- Does not cross BBB

Epinephrine

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This drug is a VP-1 agonist
- ADH
- causes smooth muscle constriction
- Used in ACLS for pulseless VT and VF
- Less constriction at coronary and renal beds
- Vasodilates cerebral vasculature
- May enhance platelet aggregration in septic shock
- Increases BP, MAP, SVR, and UO

Vasopressin

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This drug is a vasopressin analog, agonist at VP-1
- IV only
- Control of Low BP
- Used for patients who do not respond to Norepi
- Useful to treat bleeding esophageal varices
- avoid use in hypoxic patients

Terlipressin

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This drug is a PDE-3 inhibitor
- Positive inotrope and vasodilator
- Cleared by liver, can accumulate with liver dz
- Increases cAMP causing increased Ca into cells to improve myocardial contractility and inhibit vasoconstriction.
- Increases CO
- Decreases CVP, SVR

Milrinone

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This drug is indicated for severely low BP in septic or distributive shock
- very short half life (1 min)
- IV infusion only
- titrate BP to proper range
- May cause clots and DVTs
- Must be given with anti-clotting therapeutics

Angiotensin II acetate (Giapreza)

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This drug is a Na/K ATPase inhibitor
- narrow therapeutic window
Used in systolic heart failure with decreased CO
- Used with atrial fib and SVT
- Increases Cardiac output
- Increases voltage at rest.
- Used more in outpatient PO

Digoxin

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NE > EPI > DA > ISO

Alpha-1 agonist potency

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EPI > NE > DA > ISO

Alpha-2 agonist potency

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ISO > EPI = NE > DA

Beta-1 agonist potency

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ISO > EPI > NE > DA

Beta- 2 agonist potency

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ISO = NE > EPI > DA

Beta-3 agonist potency

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Muscarinic receptor structure/function?

G-protein

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Nicotinic receptor structure/function?

Ionophore

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Alpha and Beta receptor structure/function?

G-protein

This drug is a selective central acting alpha-2 agonist - analog of Clonidine but 7x more selective - can be used as anesthetic

Dexmedetomidine (precedex)

This drug is last line treatment for HTN treatment - Forms A-methyl NE - False transmitter - contraindicated with hepatic dz - Decreases norepi release

Methyldopa

This drug is an Alpha-1 and Beta-1 agonist and mild at Beta-2 - causes peripheral norepi release - relaxation of smooth muscle and cardiac stimulation and increased blood pressure. - High abuse, can make meth

Ephedrine

This drug is an irreversible-covalent bind alpha-1 and alpha-2 antagonist. - Lasts 3 days - Most effective at smooth muscle and exocrine glands - Pre-op treatment for pheochromocytoma to block HTNcrisis - Oral

Phenoxybenzamine (Dibenzyline)

This drug is an alpha-1 and alpha-2 competitive antagonist. - shorter duration of action than phenoxybenzamine - used for pheochromocytoma diagnosis

Phentolamine (oraverse)

This drug is a selective alpha-1 antagonist - used to treat HTN - less risk of reflexive tachycardia than other alpha blockers

Prazosin (minipress)

Terazosin, Doxazosin, Alfuzosin, and Tamsulosin are all alpha-1 blockers than can be used to treat HTN and what else?

Benign prostatic hyperplasia (BPH)

This drug is a non-selective beta blocker beta-1 and beta-2. - treats HTN, speaker nerves, angina - contraindicated in shock, asthma, bradycardia - bronchospasm side effect

Propanolol

Timolol is a non-selective beta blocker most often used for treating what?

Ocular hypertension and wide angle glaucoma

This drug is a non-selective Alpha-1, Beta-1 and B-2 antagonist. - treating HTN - contraindications with asthma and CHF

Labetalol

This drug is a non-selective Alpha-1, Beta-1 and B-2 antagonist. - treating HTN - Higher beta: alpha block than labetalol - contraindications with bronchospasm, COPD, bradycardia

Carvedilol (coreg)

This drug is a selective Beta-1 antagonist - treat HTN and angina pectoris

Metoprolol (lopressor)

This drug is a selective Beta-1 antagonist used to decrease BP and control ventricular arrhythmias - side effects of alopecia

Acebutolol

This drug is a selective Beta-1 antagonist - IV infusion due to short half life - treatment of atrial fib or flutter, paroxysmal SVT

Esmolol

Sodium Channel blockers are which antiarrhythmic drug class?

Class Ia-Ic

Class Ia-Ic antiarrhythmic class?

Sodium Channel Blockers

Beta-adrenergic blockers are which antiarrhythmic drug class?

Class II

Class II antiarrhythmic class?

Beta-adrenergic blockers

Calcium Channel blockers are which antiarrhythmic drug class?

Class IV

Class IV antiarrhythmic class?

Calcium Channel blockers

Class III antiarrhythmics?

Potassium Channel blockers

What is the normal AV nodal delay in ms?

0.15 seconds or 150 ms

What neurotransmitter shortens the conduction time of action potential through AV node propagation?

Acetycholine (Catecholamines)

During the cardiac cycle which structure directly delivers action potential to the ventricular myocardium?

Purkinje fibers

The cardiac electrical impulse normally begins spontaneously in the SA node because of what?

It depolarizes more rapidly than other automatic cells of the heart. SA node is first

Which period follows depolarization of the myocardium and represents a period during which no new cardiac potential can be propagated?

Absolute Refractory Period

Where in the heart are the receptors for neurotransmitters located?

Myocardium and coronary vessels

What enables electrical impulses to travel in a continuous cell to cell fashion in myocardial cells?

Intercalated disks

Older children with unrepaired cardiac septal defect experience cyanosis because of which factor? - Right to left shunt - Left to right shunt?

Right to left shunt

The atria squeeze in which sequence?

Top down contraction

The ventricles squeeze in which sequence?

Bottom up contraction

The purkinje fibers stimulate what first?

The apex

Transmembrane potential is determined by which 3 ionic gradients?

Na K Ca

The maintenance of electrogenic ionic gradients and membrane potential comes from what?

NA/K ATPase pump 3 Na out for 2 K in

This ionic gradient is responsible for the resting membrane potential, it is relatively permeable?

K Potassium. -90mv membrane potential

Which phase corresponds to Na channel activation with rapid flow in?

Phase 0 Voltage now +10mv

Which phase corresponds to an early repolarizing K current in which Na channels close and K channel open?

Phase 1

Which phase is a combination of inward depolarizing Ca balanced by an outward repolarizing K current?

Phase 2

Which phase is repolarizing due to outward K current increasing which inward Ca current decreases?

Phase 3

Which phase is a balance between inward Na current and outward K current. The membrane potential drifts towards threshold?

Phase 4

Spontaneous depolarization is also called what?

Automaticity

Any change to which phase alters conduction?

Phase 4

Electrical gradient wants to _____ potassium which the concentration gradient wants to ______ potassium?

Electrical- hold in Concentration- push out

Ectopic pacemaker is facilitated by what? Treated by what?

Facilitated by hypokalemia Increasing potassium slow/stop ectopic activity

Increasing the maximum diastolic membrane potential can diminish automaticity by which two drugs?

Adenosine Acetylcholine

Decreasing the slope of phase 4 depolarization can diminish automaticity by which drugs?

Beta blockers

Increasing the action potential duration can diminish automaticity by which drugs?

K channel blockers AIDS

Raising the membrane threshold potential can diminish automaticity by which drugs?

Na channel blockers and Ca channel blockers

Which condition is caused by an accessory conduction pathway?

Wolf-Parkinson-White syndrome

Which drugs prolong nodal refractoriness and slow conduction? Can treat WPW syndrome

Ca channel blockers Beta blockers Digitalis glycosides Na channel blockers

This drug class is primarily used to slow the rate of action potential rise and prolong ventricular effective refractory period?

Sodium channel blockers Ia

This drug is a class Ia - Na channel blocker (activated only) - Used to terminate reentry arrhythmia - Antimalarial and antipyretic effects - Must be given slow IV - Accumulated in hepatic/renal dz pts - can also block K channels - Affects Phase 0 and Phase 4 - treat WPW syndrome - Cinchonism (N/V/D, blurred vision) - Antimuscarinic action on heart - Can develop Torsades de Pointes

Quinidine

This drug is a class Ia - Na channel blocker - long term use associated with Lupus - Cardioactive metabolite (NAPA) may lead to Torsades de Pointes - Does not exhibit antimuscarinic activity like Quinidine - Ganglionic blocking activity

Procainamide

Procainamide-induced Lupus syndrome occurs more frequently in which population?

Slow acetylators Europeans

This drug is a class Ia - Na channel blocker - Greater anti-muscarinic effects - Used for ventricular arrhythmias - Not an alpha- adrenergic blocker

Disopyramide (Norpace)

This drug is a class Ib - Na channel blocker - Blocks activated and inactivated - Reduces the phase 4 slope and increases threshold - requires IV administration due to extensive first pass - Rapidly dissociates in normal tissue (low affinity) - Remains bound in ischemic tissue (high affinity) - Major side effect is Seizure in rapid administration and cardiac depression

Lidocaine (Xylocaine)

This drug is a class Ib - Na channel blocker - Chronic treatment of Ventricular tachyarrhythmias - Amine analog of Lidocaine - Oral administration

Mexiletine Hydrochloride

This drug is a class Ib - Na channel blocker - effective in suppression of ventricular arrhythmias associated with digitalis toxicity - Least effective Na channel blocker - Shortens QT more than any agent - Can cause CNS disturbances (sedation, nystagmus, confusion, ataxia). - Causes hirsitism (hair growth)

Phenytoin (Dilantin)

Barbituates do what to phenytoin levels?

Lower phenytoin levels due to metabolizing enzyme induction

Warfarin, Isoniazid do what to phenytoin levels?

Increase phenytoin levels due to metabolism inhibition

This drug is a class Ib piperazine deriv -also blocks K and Ca conductance - used to treat chronic angina - decreases late Na inward current and intracellular Ca conc - Increases refractory period used for ventricular arrhythmias - Metabolized by CYP3A4 avoid grapefruit juice

Ranolazine (Ranexa)

This drug is a class Ic - Na channel blocker - more effective than Ia or Ib - suppresses pvcs and v-tach - effective in managing atrial tachyarrhythmias - effective in WPW syndrome treatment - Reserved for management of life threatening arrhythmias. - Not 1st line treatment - Proarrhythmic dangerous with MI patients

Flecainide Acetate

This drug is a class Ic - Na channel blocker - weak beta blocker - weak Ca channel blocker - active metabolite via liver metabolism - Proarrhythmic dangerous with MI patients

Propafenone (Rythmol)

This drug is a class II - beta blocker - decreases the slope of phase IV - Increases AV conduction time - treatment of atrial flutter and atrial fibrillation - can lead to bronchospasm, worsen CHF

Propranolol (Inderal)

This drug is a class II - beta blocker - very short acting (IV admin) - cardioselective - decreases the slope of phase IV - Increases AV conduction time - treatment of atrial fibrillation with RVR

Esmolol (Brevibloc)

This drug is a class III - potassium channel blocker - delays repolarization and prolongs action potential - increases refractory period - orthostatic hypotension with chronic use - increased ventricular action potential duration - Initial catecholamine release - used to manage serious ventricular arrhythmias caused by lidocaine or procainamide - Not first line treatment

Bretylium Tosylate

This drug is a cross between class I and III - K channel blocker - Na channel blocker - prolongs action potential duration - Treatment of ventricular arrhythmias - Can cause hypo/hyperthryoidism due to iodine content - Long term therapy can lead to pulmonary fibrosis (fatal) - Postoperative pulmonary edema - sinus arrest (risky drug)

Amiodarone (Nexterone)

This drug is a cross between class I and III - Increasing refractory period - alternative to amiodarone for atrial fib/flutter treatment - Black Box warning with CHF - greatest effect on K channels

Dronedarone (Multaq)

This drug acts as a class II and III - Nonselective beta blocker - K channel blocker - Prolongs refractory period - may cause HTN or vasospasm - Avoid in asthmatics - treats atrial fib/flutter

Sotalol (Betapace)

This drug is a class V - G-protein coupled - activates acetylcholine K current - decreases action potential duration - Rapidly terminates SVT

Adenosine

This drug is a class IV - Ca channel blocker - blocks the inward Ca current to slow conduction through AV node and decrease phase IV depolarization - Main action on the heart - used to convert atrial fib/flutter to NSR - Hypotension side effect - constipation

Verapamil and Diltiazem (Cardizem)

Which classes/drugs are ideal to treat Atrial fibrillation?

Calcium channel blockers- Verapamil/Diltiazem Beta blockers- Propranolol Digitalis glycosides- Digoxin

Which classes/drugs are ideal to treat and maintain Normal Sinus Rhythm?

Class Ia Sodium channel blockers Quinidine and Procainamide

Which classes/drugs are ideal to treat Paroxysmal SVT?

1. Valsalva maneuver 2. Alpha receptor agonist 3. Digoxin Adenosine, Verapamil, Diltiazem, Esmolol or Cardioversion.

Thiazide diuretics work in this part of the kidney?

Distal renal tubule Hydrochlothiazide

Potassium sparing diuretics work in which part of the kidney?

Late distal tubule and Collecting duct Amiloride, Triamterene, Spironolactone

High Ceiling Loop diuretics work in which part of the kidney?

Thick ascending limb in loop of Henle Lasix, Bumetanide

Which beta blocker's vasodilation affect includes potentiating Nitric Oxide?

Nebivolol (Bystolic)

Which drug works primarily to vasodilate the arteries thus having greater effect on diastolic BP?

Hydralazine

Minoxidil was once an orally active form of direct arteriole smooth muscle relaxation for HTN treatment but is now used for what?

Hair growth in women

This drug has a Ferrous iron center complex with 5 cyanide (44% by weight), requires IV administration due to short duration. Requires A-line monitoring and may result in coronary steal?

Nitroprusside

What is the active mediator responsible for direct nitroprusside vasodilating effect?

NItric oxide

The body sulfur stores can detoxify how many mg of nitroprusside into cyanide ions?

50mg

Which drug is most often used for hypertensive emergencies?

Nitroprusside

Which class of drugs can potentiate NMBA agents and make them last longer?

Calcium channel blockers

This drug is a diagnostic marker for ALL leukemia?

Entresto Neprilysin Inhibitor