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BarryPharmII

Pharmacolgy II

QuestionAnswer
stimulation of this receptor relaxes smooth muscles causing vasodilation, bronchodilation, and relaxation of the uterus, bladder and gut beta 2 receptors
receptors are located on the post-synaptic membranes in the heart. Stimulation causes increase heart reate, increased conduction, and increased contractility. beta 1 receptors
Receptors located on the pre-synaptic nerve terminal. In the CNS, post-synaptic receptors decrease sympathetic outflow. alpha 2 receptors
Receptors located in post synaptic nerve terminals located in smooth muscle throughout the body. Stimulation causes bronchoconstriction, vasoconstriction, mydriasis, and uterine contraction. alpha 1 receptors
Synthesis of catecholamines begin with which amino acid L-tyrosine
Postganglionic fibers in the sympthatetic nervous system release which neurotransmitters norepinephrine, epinephrine, dopamine
L-tyrosine is converted into L-dopa by which enzyme tyrosine hydroxylase
L-dopa is converted into dopamine by which enzyme dopa decarboxylase
dopa decarboxylase(DD) is also known as L-amino acid decarboxylase
In norepinephrine neurons which enzyme is present in the vesicles that catalyzes the conversion of dopamine into norepinephrine. dopamine beta hydroxylase
In epinephrine neurons which cytoplasmic enzyme converts norepinephrine to epinephrine PNMT
T or F. Dopa decarboxylase is a fairly selective enzyme. False
Enzyme that converts 5-hydroxytryptophan to 5-hydroxytryptamine dopa decarboxylase
What is methylnorepinephrine? a false neurotransmitter.
Enzyme the converts alpha-methyldopa to alpha-methyldopamine, which is further converted to alpha-methylnorepinephrine dopamine beta hydroxylase
Cytoplasmic NE acts in the feedback loop on which two enzymes tyrosine hydroxlase, dopa decarboxylase
In the cytoplasm NE acts to feedback on __ production. dopamine
NE in the cytoplasm of the ___chromaffin cells is converted to EPI before packaging in the vesicles adrenal medulla
The enzyme alpha-methyl-p-tyrosine inhibits which enzyme tyrosine hydroxylase (TH)
The enzyme alpha-metly-dopa inhibits which enzyme dopa decarboxylase
In the cytoplasm NE acts to feedback on __ production. dopamine
NE in the cytoplasm of the ___chromaffin cells is converted to EPI before packaging in the vesicles adrenal medulla
The enzyme alpha-methyl-p-tyrosine inhibits which enzyme tyrosine hydroxylase (TH)
alpha-metly-dopa inhibits which enzyme dopa decarboxylase
In the cytoplasm NE acts to feedback on __ production. dopamine
Other than Dopamine, DBH, and other proteins what else is NE in a complex with inside the granules at a 4:1 ratio ATP
The enzyme alpha-methyl-p-tyrosine inhibits which enzyme tyrosine hydroxylase (TH)
The enzyme alpha-metly-dopa inhibits which enzyme dopa decarboxylase
Disulfiram (Antabuse) inhibits dopamine beta hydroxylase
All enzymes usually require __ to catalyze a reaction cofactors
T of F. Neurotransmitters are taken up in favor of the concentration gradient back into the vesicle. False. against concentration gradient
T or F. Some of the released neurotransmitter in the synapse can act on presynaptic alpha-2 heteroreceptors. False. autoreceptors
Two principle enzymes responsible for the degradation of catecholamines MAO, COMT
Which form of MAO is the most active form Type A
Which organ has a lot of MAO and COMT The liver
Clonidine has more agonist potentcy for which receptor alpha 2
Phenylephrine is very potent at which receptor alpha 1
All alpha 2 receptors inhibit ___ by G-protein interaction, causing hyperpolarizaton adenyl cyclase
Alpha 1 stimulation triggers increased intracellular __ release Calcium
Norepinephrine is most potent at which beta receptor beta 1
Epinephrine is most potent at which beta receptor beta 2
Beta 3 receptors have been discovered where colon and adipose tissue
Which catecholamine is the most potent at beta 3 NE
In smooth muschle, increased cAMP leads to muscle ___ as the membrane hyperpolarizes relaxation
Adrenergic agonist that is a : – Potent vasoconstrictor and inotropic agent – L-isomer much more potent than d-isomer --More α than β activity Norepineprine
Adrenergic agonist that: – Does not increase myocardial O2 consumption. – Normally given only via IV, with rapid onset and short (1 - 2 minute) duration. – Does not cross the BBB. – Use limited, mainly used for shock and severe hypotension. Norepinephrine
Adrenergic agonist that is: – Administered parenterally, via inhalation, or topically to eye. – Used as a cardiac stimulant and bronchodilator (anaphylactic shock). ---Opthalmic use a diagnostic aide Epinephrine
Adrenerfic agonist that causes: – α stimulation in liver increases gluconeogenesis and inhibits insulin release. β stimulation (β3) in adipose tissue causes catabolism and increased free fatty acids in plasma. Epinephrine
Adrenergic agonist: Selective β1 agonist . Stimulates rate and contraction of heart, increasing CO. Increased coronary blood flow and myocardial O2 demand seen Dobutamine
Adrenergic agonist: – Relatively selective β2 agonist. – Structurally similar to Albuterol. – Used for asthma and bronchospasms. Pirbuterol (Maxair)
Coronary blood flow is controlled by what factor myocardial oxygen demand
antianginals that prevent or terminate angina by increasing oxygen supply are called coronary vasodilators
antianginals that prevent or terminate angina by decreasing oxygen demand are known as negative chronotropes, negative inotropes and vasodilators
coronary vessel vasodilation is mediated by which receptors beta receptors
For acute management of angina, which agent causes systemic venodilation, reduce myocardlal wall tension and oxygen requirement, and dilate epicardial capacitance vessels sublingual nitroglycerin
The vasodilation, from nitrates, is mediated by the production of _____, and increased levels of intracellular cGMP in vascular smooth muscle. Nitric oxide
Short acting nitrate (lasts about 30 minutes) that is more effective at preventing angina than stopping it once it has begun. Glyceryl trinitrate (Nitroglycerin)
Nitric oxide synthetase produces endogenous nitrates by action on which amino acid L-arginine
headaches from Nitrates is caused by dilation of meningeal vascular dilation
drugs that reduce the increases in heart rate and contractility due to adrenergic activity beta-receptor blockers
ß-Adrenoceptor Antagonists are not effective in which type of angina variant (Prinzmetal)
Coronary vasodilators that reduce arterial pressure and myocardial contractility. Also effectively treats variant angina Calcium Channel Antagonist
Three subgroups of Calcium Channel Antagonist are papaverine derivatives, benzothiazepines, and dihydropyridines. Which group is more myocardium selective Papaverine derivatives (phenylkalkylamines). Ex Verapamil
3 subgroups of Calcium Channel Antagonist are papaverine derivatives, benzothiazepines, and dihydropyridines. Which group works more on vasculature? Most agents in this class are not used for angina due to relfex tachycardia with the exception of 2 drugs Dihydropyridines. Ex Nifedipine, Amlodipine
Three subgroups of Calcium Channel Antagonist are papaverine derivatives, benzothiazepines, and dihydropyridines. Which group effects both vasculature and myocardium Benzothiazepines. Ex Diltiazem
Calcium channel blockers reduce afterload by arterial dilation
Which Calcium channel blockers also have an anti-arrhythmic affect Verapamil and Diltiazem
All calcium antagonists have a negative inotropic effect, especially verapamil, and should not be used in patients with Cardiac heart failure
Worsening of myocardial ischemia may be observed with ____since these Calcium Blockers are more likely to produce excessive vasodilatation and reflex mediated tachycardia. Dihydropyridines
hypertension with no obvious cause is called essential hypertension
As a rule, elective surgery should be delayed if the resting diastolic pressure is greater than 110mmHg
Which group of anti-hypertensive agents reduce sodium and extracellular volume and are often the first-line drugs of choice Diuretics
Type of hypertension seen as wide pulse pressure and can be caused either by conditions of decreased aortic compliance or to increased stroke volume systolic hypertension
Type of hypertension caused by increased peripheral vascular resistance systolic and diastolic hypertension
Renal, endocrine, and neurogenic disorders will most likely cause which type of hypertension systolic and diastolic hypertension
A principal mechanism for arterial blood pressure control is the ____ reflex Baroreceptor
Baroreceptor input to the ___ of the medulla results in inhibition of the vasoconstrictor center and excitation of the vagal centers. Tractus solitarius
In patients with asthma or chronic obstructive pulmonary disease (COPD) the use of a ______ may be contraindicated since agents belonging to this drug class may cause bronchoconstriction. Beta adrenoreceptor antagonist
Type of diuretics that promote potassium loss and increases in serum lipids Thiazides
Definition of hypertensive crisis is when Diastolic blood pressure is above 130mmHG
Ingestion of tyramine-rich foods in patients taking ____ can cause hypertensive crisis MAO inhibitors
Thiazide (e.g. Hydroclorthiazide) diuretics cause an inhibition of NaCl transport in the ___ Distal convoluted tubule
This K+ sparing diuretic blocks sodium channels in the luminal membrane in the late distal tubule and collecting duct and limits the amount of Na entering the cell. Amiloride
Potassium sparing diuretic that is an antagonist at mineralocorticoid receptors Aldactone
T or F. “High-ceiling" loop diuretics acting primarily at the descending limb of the loop of Henle. False. Ascending
These types of diuretics are rarely used in the management of hypertension because of their short duration of action and the availability of better drugs. Loop diuretics
Furosemide (Lasix) and ethacrynic acid (Edecrin) block renal excretion of uric acid by competition with renal secretory and biliary secretory systems. Therefore these agents can precipitate what disorder gout
Thesse diuretics can cause ototoxicity and potassium loss Loop diuretics
Centrally-acting sympatholytic agents are adrenoreceptor agonists at which receptor. Alpha 2
These drugs can cause sedation and xerostomia (dry mouth) during the initial phase of treatment. A withdrawal syndrome occurs upon sudden discontinuation and can involve significant hypertension. Centrally acting sympatholytics
A prodrug which is metabolized to the active agent, alpha-methylnorepinephrine. Methyldopa
Guanabenz acetate, clonidiine, and methlydopa are centrally acting sympatholytics
Adrenergic agent that inhibits sympathetic function at the level of the nerve ending. Acts by depleting NE and dopamine from vesicles. Antihypertensive effects result from the inability of the sympathetic nervous system to produce vasoconstriction. Reserpine
The protype agent for Beta-adrenergic receptor antagonists Propranolol (Inderal)
Beta adrenergic receptor blocker classification is based on receptor selectivity and intrinsic ____activity sympathomimetic
Antihypertensive properties of beta-blockers may be reduced by concurrent administration of ____ NSAIDS
Prazosin (Minipress), Terazosin (Hytrin), and Doxazosin (Cardura) are in what drug class Peripheral alpha-1 adrenergic receptor antagonists
Antihypertensive: A competitive antagonist at both α1 and ß-adrenergic receptors (non-selective). It also has a partial agonist effect at some ß2 receptors Labetalol (Trandate)
Hydralazine and Minoxidil are what type of antihypertensive medication vasodilators
Antihypertensive: Dilation effect greater on arterioles, compared to venules Most pronounced dilation: • coronary, renal, splanchnic, and cerebral circulation Vasodilation may be mediated by vascular smooth muscle calcium ion transport inhibition hydralazine
Antihypertensive: • Extensive hepatic first pass effect • Major route metabolism: acetylation • Pts categorized as "rapid acetylators": reduce bioavailability (30% bioavailability); "slow acetylators" (50% bioavailability) (following oral administratio hydralazine
Antihypertensive; • Excellent absorption following oral administration (90%, gastrointestinal) • Substantial metabolism (glucuronidation; only 10% excreted unchanged) Minoxidil
Antihypertensive: • Direct-acting, nonselective peripheral vasodilator • Relaxation of arterial and venous vascular smooth muscle – Structure: • Ferrous iron center complex with five cyanide moieties and a nitrosyl group (44% cyanide by weight) Nitroprusside
interacts with oxyhemoglobin, forming methemoglobin with cyanide ion and nitric oxide (NO) release Nitroprusside
Nitroprusside radicals decompose releasing five cyanide ions. One cyanide reacts with methemoglobin to form what? cyanomethemoglobin
This drug may worsen myocardial infarction damage due to "coronary steal", where blood is directed away from ischemic areas by arteriolar vasodilation Nitroprusside
• For low-renin hypertensive patients (elderly and African-American groups), ____appear good choices for monotherapy (single drug) control. Calcium Channel Blockers
In anesthetized patients with preexisting left ventricular dysfunction, which Ca Channel blocker results in myocardial depression and reduced cardiac output. Verapamil
The drugs potentiate depolarizing and nondepolarizing neuromuscular-blocking drug effects. Calcium Channel Blockers
Drug is effective in treating hypertension because they reduce peripheral resistance. • have relatively little effect on reducing myocardial contractility compared to verapamil (Isoptin, Calan) or diltiazem (Cardiazem). Norvasc
Has a direct negative chronotropic effect on the heart sufficient to block reflex-mediated tachycardia secondary to the decrease in peripheral resistance. The reflex-mediated adrenergic stimulation tends to counteract negative inotropic properties Diltiazem (Cardiazem)
Antihypertensive: • Highly lipid-soluble Nifedipine analog • Ready access to the CNS -- reduces large cerebral arterial contraction • Clinical Use: Cerebral Vasospasm Nimodipine
This drug class is considered first line treatment in patients with: – systemic hypertension – congestive heart failure – mitral regurgitation ACE inhibitors
Drugs of choice in treatment of hypertensive patients who have hypertrophic left ventricles and or diabetes. ACE inhibitors
Should not be used during pregnancy. Also cause dry cough, rhinorrhea, allergic-like symptoms ACE inhibitors
ACE inhibitor that is: • well absorbed; 25%-30% protein bound • rapid enzyme inhibition (within 15 minutes following oral administration) • 50% drug excreted unchanged • elimination half-life: two hours -- oxidation, renal excretion Captopril
– Angiotensin II receptor antagonist which acts by blocking the interaction between angiotensin II and its receptor (AT1) in vascular smooth muscle. – Metabolized to active metabolite that is 10 – 40 times more active. t1/2 ~ 6 hrs Losartin (Cozaar)
Caused by coronary vasospasm Variant or Prinzmetal's angina
THe most common cause of angina atheroma
Symptoms include retrosternal chest pain or tightness, which often radiates to the arms. Pain is caused or increased by exercise and relieved by rest and treatment of nitrates Angina
Myocardial ischemia is usually caused by coronary vessel atherosclerosis T or F. True
If the plaque size results in greater than about 50% reduction, sufficient coronary blood flow during exertion is still available and anginal symptoms are not usually present T or F False
Coronary blood flow is controlled by the _________ ________ _______and modulated by varying coronary vascular resistance myocardial oxygen demand
Anti-anginal drugs nitrates, beta blockers, and calcium channel blockers
Normally there are not increases in coronary blood flow in a denervated heart in response to increased myocardial contractility and rate T or F. False
Coronary vascular bed has both alpha and beta- adrenoceptors. T or F True
Associated with a reduced life expectancy, increase risk for stroke and CAD, and end-organ disease hypertension
For acute management of angina what drug rapidly terminates angina? Sublingual nitroglycerin
Which agents cause systemic venodilation and therefore reduce mycoardial wall tension and oxygen requirements? Nitrates
Nitrates dilate ________ ________ _______ vessels thereby increasing blood flow in collateral vessels. epicardial coronary capacitance
For chronic management of angina, medical management is individualized for each patient, including patient education and counseling to assist in reduction of risks of coronary heart disease. T or F True
Cardiac output is usually unchanged or decreased slightly, and a reflex tachycardia occurs in normal subjects when given nitrates. T or F True
In patients with heart failure, who have a high systemic vascular resistance, cardiac output may decrease and there is change in the heart rate. T or F False
Glyceryl trinitrate (Nitroglycerin) is a long acting nitrate with a DOA of 60 minutes. It is more useful in preventing attackes of angina than in stopping them once they have begun. T or F False, short-acting and 30 min.
Long acting nitrates that are more stable and may be effective for several hours isosorbide dinitrate (Isordil) and isosorbide mononitrate (Imdur)
Unwanted side effects of nitrates are headaches, tachycardia, hypotension, and tolerance to nitrates. T or F True
Nitrates should be given continuously to prevent tolerance from developing. T or F False: intermittently
Elective surgery should be postponed if diastolic BP is greater than ___ mmHg 110
Term for high blood pressure with no obvious cause essential hypertension
Pathogenesis of ___ includes 1) increased symp. activity, 2) Na retention & increase circulating volume, 3) increase vascular rigidity and reactivity, 4) increase circulating catecholamines & activation of RAA system, 5) abnormal baroreceptor responses hypertension
Caused by either decreased aortic compliance or increased stroke volume systolic hypertension
systolic and diastolic hypertension is due to ... increased peripheral vascular resistance
First-line drugs for treating hypertension is ... diuretics
>90% of all hypertension cases are called ... essential hypertension
Essential hypertension is also known as ___ or idiopathic hypertension primary
Increase ___ and increase ___ leads to increase stroke volume , which leads to increase arterial pressure preload, contractility
If CO = SV x HR, if stroke volume remains the same, an increase in ___ results in increased arterial pressure heart rate
For a given CO, blood pressure only depends on ___ peripheral resistance
What reflex is initiated by the stretch receptors in the wall of the aortic arch and others that are in the internal carotid artery Baroreceptor reflex
In a baroreceptor response, if pressure increases, baroreceptor input to the tractus solitarius of the medulla results in ___ of the vasoconstrictor center and ____ of the vagal centers inhibition, excitation
Inhibition of the vasoconstrictor center & excitation of the vagal centers of the medulla causes vaso___ and ____ chronotropic and inotropic effects of the heart... dilation, negative
In the anesthetized pt treated with anti-htn meds, orthostatic hypotension , excessive systemic-blood pressure responses(decreases), altered responses to direct and indirect acting sympathomimetic agents is due to decrease ___ activity SNS
T/F ... Maintenance of anti-htn drug treatment during peri-op time frame increases the likelihood of arrhythmias False
Adrenergic agonist – Synthetic compound similar in structure to isoproterenol. – More β2 selective than isoproterenol (but less than Albuterol). – Exclusively used as a bronchodilator. Metaproterenol
Adrenergic Agonist – Selective β2 agonist. – Indications - bronchospasm in patients with obstructive airway disease, asthma. – Adverse reaction - nervousness, tremor, tachycardia, palpitations. Albuterol (Ventolin)
Adrenergic Agonist – β2 agonist. – Much more selective for β2 than albuterol. – For chronic treatment of asthma (BID dosing, due to longer half-life). – Side effects include tachycardia, palpitations, hypersensitivity, tremor, and headaches. Salmeterol (Serevent)
Adrenergic Agonist – β2 agonist. – Used for bronchospasms and asthma, emphysema. – Side effects include tremor, nervousness, tachycardia, palpitations, nausea and vomiting. Terbutaline Sulfate
Adrenergic Agonist: – Selective α2 agonist. – More CNS activity than peripheral. – α2 receptor stimulation in the CNS leads to decreased sympathetic outflow, increased parasympathetic outflow. – Indicated for HTN – S.E. include dry mouth, skin irrita Clonidine (Catapres)
Used as vasoconstrictor to maintain B/P during surgery, decongestant, mydriatic (w/o cycloplegia). Contraindicated in narrow angle glaucoma, V-tach, aneurysms. S.E. bradycardia, decreased CO, arrhythmias, angina, dizziness, CNS excitation. Phenylephrine
– A parenterally administered potent vasoconstrictor (α1). – Used to prevent surgical (spinal anesthesia) hypotension and shock. – Adverse reactions include anxiety, cardiac arrhythmias, and hypertension. metaraminol (Bitartrate)
– Forms α-methyl NE - acts as a false transmitter - less potent than NE. – Used to treat hypertension. – Contraindicated in patients with hepatic disease. – Side effects include angina, congestive heart failure, orthostatic hypotension, bradycardia, et Methyldopa
– Inhibits amine re-uptake pump, thus causing increases stimulation. (Indirect effect). – Also has L.A. effects - blocks Na+ channels of nerve membranes. – Used for local (topical) anesthesia of mucous membranes in mouth, laryngeal and nasal cavities. Cocaine
Indirect Adrenergic Agonist: – Stimulates sympathetic neurons to release neurotransmitter. – Also has direct post-synaptic effect (mixed action). – Used for Narcolepsy, ADD, obesity. – Contraindicated in any cardiovascular disease, HTN, hyperthyroid Amphetamine (Adderall, Dexedrine)
Indirect Adrenergic Agonist. Stimulates α & β receptors. Peripheral actions are d/t to NE release and partly to direct effect on receptors. Produce mainly relaxation of smooth muscle and, if NE stores are intact, cardiac stimulation & ^ b/p. Ephedrine
– Potent sympathomimetic, they possess direct α1, β1 and β2 activity in addition to triggering the release of catacholamines from the nerve terminal (mixed effects). – Used mainly for asthma, stimulant (OTC) preps. – Contraindicated in CV disease, HTN Pseudoephedrine (Sudafed)
Sympathomimetic (not used clinically) – Taken up into nerve terminal and converted to false transmitter that has less activity, leading to decreased sympathetic tone. – Slight direct α activity. – Triggers release of NT from neuron. - Found in some fo Tyramine
Methamphetamine (Desoxyn), Methylphenidate (Ritalin, and Phentermine (Adipex) are classified as Indirect Adrenergic Agonists
Pharmacology of nitrates Nitrates/nitrites--> guanylyl cyclase--> cGMP-->vasodilation T or F False; nitrates are denitrated to produce NO which activates guanylyl cyclase
Nitric oxide synthase produces endogenous nitrates by action on L-arginine. T or F True
Effectiveness of sublingual nitroglycerin in treating Prinzmetal's variant angina is due to the indirect vasodilation of the large vessel. T or F False; direct
Nitrates dilate meningeal vascular vessels causing headache. T or F True
What are the 3 beta-adrenergic blockers used in the management of chronic, classical angina? Propranolol, atenolol, and nadolol.
Beta-blockers should be used for angina in patient with the diagnosis of asthma. T or F False; causes bronchoconstriction.
Overall, ____ receptor agonists will increase arterial tone, increase TPR, increase diastolic pressure, decrease heart rate (reflex), and increase venous tone. Alpha 1
Overall, ___ receptor agonist willl increase tone in large arteries, increase TPR (post synaptic), and increase coronary vasodilation Alpha 2
Overall, ___ receptor agonist will increase heart rate, increase O2 consumption, increase automaticity, conduction velocity, increased force of contraction, increased stroke volume and CO, decrease filling volume, and ^ coronary vasodilation. Beta 1
Overall, ____ receptor agonist decrease arterial tone, decrease TPR, decrese diastolic pressure, and increase heart rate (reflexive) Beta 2
– α1 and α2 antagonist (‘irreversible’ - covalent binding).. – Most effective at smooth muscle & exocrine glands. – Used for: pre-op tx of pheochromocytoma to block potential hypertensive crisis during surgery, vasospastic disorders, & frostbite therapy Phenoxybenzamine (Dibenzyline)
In patients with reduced right ventricular function and limited myocardial reserve, beta-receptor blockade may precipitate heart failure by blocking essential sympathetic drive. T or F False; left ventricle
What are the 3 calcium antagonists sub groups? papervine derivatives (phenylalkyamines), Dihydropyrines, and benzothiazepines.
Diltiazem is a papeverine derivative. T or F False; benzothiazepines
Dihydropyridines primary effect on vasculature. T or F True
Nifedipine and Amlodipine are dihydropyridines. T or F True
Calcium antagonists reduce preload by arterial vasodilation, dilate coronary arteries, and reduce cardiac work. T or F False; afterload
All calcium antagonists have a negative inotropic effect and should not be used in patients with cardiac failure. T or F True
Classical angina symptoms occur with exertion. T or F True
The normal myocardium accounts for __ % of the total body oxygen consumption, but the coronary circulation receives only __% of the cardiac output. 11 and 4
The myocardium is one of the most perfused tissue in the body. T or F False; least perfused
Myocardial oxygen supply involves HR, coronary perfusion, arterial oxygen content, and coronary artery diameter. T or F True
Myocardial oxygen demand involves heart rate, ventricular preload and afterload, and contractility. True
– α1 and α2 competitive antagonist.   – Shorter duration of action of action than phenoxybenzamine. – Parenteral dosing. – Used for: pheochromocytoma diagnosis, pheochromocytomectomy, MAO induced hypertensive crisis, impotence. Given parentally. Phentolamine (Regitine)
Selective α1 antagonist. For treating HTN S.E: dizziness, h/a, drowsiness, palpitations, ^ HR, orthostatic hypotension. B/c it does not block α2 receptors, there is no excessive release of NE from neurons, and less of a risk of reflexive tachycardia.. Prazosin (Minipress)
– Selective α1 antagonist. – related to prazosin, but less potent. –  More H2O soluble & higher bioavailability that prazosin, and also has a longer t1/2 (12 hrs), and can be used qD. – Used mainly for tx of hypertension and benign prostatic hyperplasi Terazosin (Hytrin)
– Selective α1 antagonist. – Also closely related to prazosin. – Similar bioavailability as prazosin, but has a longer t1/2 (20 hrs), and can be used qD. – Used mainly for treatment of hypertension and benign prostatic hyperplasia (BPH). Doxazosin (Cardura)
– Selective α1 antagonist. – related to prazosin. – Similar bioavailability as prazosin, but with a slightly longer t1/2 (3-5 hrs). – For treatment of BPH- relaxes smooth muscle in bladder neck and prostate. – Available in extended release oral form. Alfuzosin (Uroxatral)
– Selective α1A antagonist (but limited α1B activity, which controls vascular smooth muscle). – Therefore, somewhat more selective at treating BPH, with little effect on blood pressure. – t1/2  of 5-10 hrs. – Metabolized mainly by P-450 system. Tamsulosin (Flomax)
Selective competitive alpha 2 antagonist. S.E: antidiuretic effects, CNS excitation, HTN, tachycardia, increased motor activity, nervousness, irritability, nausea & vomiting. Local injections into penile shaft to ^ erections. Yohimbine (Yocon)
T or F. Yocon blocks central alpha-2 receptors leading to ^ B/P and HR (decreased parasympathetic outflow, and ^ sympathetic outflow), possible aphrodisiac properties d/t peripheral alpha 2 blockade and parasymp override. True
– Prototype β blocker. – Non-selective (blocks both β1 and β2 receptors). – Used for hypertension, ‘speakers’ nerves, angina, arrhythmias, migraines, pheochromocytoma. – Has membrane stabilizing effect (local anesthetic). Propranolol (Inderal)
– Non-selective β antagonist. – For treating angina, HTN – Contraindicated in bradycardia, bronchial asthma, shock, heart block, M.I. – S.E. include: bradycardia, cardiac failure, conduction disturbances,, dizziness, bronchospasm, diarrhea, impotence.. Nadolol (Corgard)
– Non-selective β antagonist. – For treating hypertension, ocular hypertension (wide angle glaucoma). – Contraindications include asthma, COPD, bradycardia, heart failure. – Side effects include fatigue, bradycardia, dizziness, cold hands and feet. Timolol (Timoptic)
– Non-selective β antagonist with some sympathetic agonist activity. – A vasodilatory β blocker (due to strong β2 agonist activity). – Also not as much bronchoconstriction as with other β2 blockers. – Used to treat hypertension. Pindolol
–α1, β1 and β2 antagonist. – ^ β:α blockade than labetolol (and longer duration). – Indications: angina, CHF (NYHA type II and III), HTN. – Contraindications: bronchospasm, emphysema, COPD, asthma, DM, HF (NYHA type IV), liver disease, pheochromocytoma Carvedilol (Coreg)
–β1 antagonist. – Used to treat hypertension and angina pectoris. – Contraindications: bradycardia, heartblock, shock, M.I. – Side effects include dizziness, bradycardia, nightmares, CHF, peripheral edema, bronchospasms, nausea, diarrhea. Metoprolol (Lopressor)
– Mostly β1 blockade, but also a partial sympathetic agonist (non-selective). – Low lipid solubility, so little CNS S.E – Membrane stabilizing effect on action potential, but < propranolol. – Used in HTN and to control arrhythmias. – Doesn't cause as
– α1 and α2 competitive antagonist.   – Shorter duration of action of action than phenoxybenzamine. – Parenteral dosing. – Used for: pheochromocytoma diagnosis, pheochromocytomectomy, MAO induced hypertensive crisis, impotence. Given parentally. Phentolamine (Regitine)
Selective α1 antagonist. For treating HTN S.E: dizziness, h/a, drowsiness, palpitations, ^ HR, orthostatic hypotension. B/c it does not block α2 receptors, there is no excessive release of NE from neurons, and less of a risk of reflexive tachycardia.. Prazosin (Minipress)
– Selective α1 antagonist. – related to prazosin, but less potent. –  More H2O soluble & higher bioavailability that prazosin, and also has a longer t1/2 (12 hrs), and can be used qD. – Used mainly for tx of hypertension and benign prostatic hyperplasi Terazosin (Hytrin)
– Selective α1 antagonist. – Also closely related to prazosin. – Similar bioavailability as prazosin, but has a longer t1/2 (20 hrs), and can be used qD. – Used mainly for treatment of hypertension and benign prostatic hyperplasia (BPH). Doxazosin (Cardura)
– Selective α1 antagonist. – related to prazosin. – Similar bioavailability as prazosin, but with a slightly longer t1/2 (3-5 hrs). – For treatment of BPH- relaxes smooth muscle in bladder neck and prostate. – Available in extended release oral form. Alfuzosin (Uroxatral)
– Selective α1A antagonist (but limited α1B activity, which controls vascular smooth muscle). – Therefore, somewhat more selective at treating BPH, with little effect on blood pressure. – t1/2  of 5-10 hrs. – Metabolized mainly by P-450 system. Tamsulosin (Flomax)
Selective competitive alpha 2 antagonist. S.E: antidiuretic effects, CNS excitation, HTN, tachycardia, increased motor activity, nervousness, irritability, nausea & vomiting. Local injections into penile shaft to ^ erections. Yohimbine (Yocon)
T or F. Yocon blocks central alpha-2 receptors leading to ^ B/P and HR (decreased parasympathetic outflow, and ^ sympathetic outflow), possible aphrodisiac properties d/t peripheral alpha 2 blockade and parasymp override. True
– Prototype β blocker. – Non-selective (blocks both β1 and β2 receptors). – Used for hypertension, ‘speakers’ nerves, angina, arrhythmias, migraines, pheochromocytoma. – Has membrane stabilizing effect (local anesthetic). Propranolol (Inderal)
– Non-selective β antagonist. – For treating angina, HTN – Contraindicated in bradycardia, bronchial asthma, shock, heart block, M.I. – S.E. include: bradycardia, cardiac failure, conduction disturbances,, dizziness, bronchospasm, diarrhea, impotence.. Nadolol (Corgard)
– Non-selective β antagonist. – For treating hypertension, ocular hypertension (wide angle glaucoma). – Contraindications include asthma, COPD, bradycardia, heart failure. – Side effects include fatigue, bradycardia, dizziness, cold hands and feet. Timolol (Timoptic)
– Non-selective β antagonist with some sympathetic agonist activity. – A vasodilatory β blocker (due to strong β2 agonist activity). – Also not as much bronchoconstriction as with other β2 blockers. – Used to treat hypertension. Pindolol
–α1, β1 and β2 antagonist. – ^ β:α blockade than labetolol (and longer duration). – Indications: angina, CHF (NYHA type II and III), HTN. – Contraindications: bronchospasm, emphysema, COPD, asthma, DM, HF (NYHA type IV), liver disease, pheochromocytoma Carvedilol (Coreg)
–β1 antagonist. – Used to treat hypertension and angina pectoris. – Contraindications: bradycardia, heartblock, shock, M.I. – Side effects include dizziness, bradycardia, nightmares, CHF, peripheral edema, bronchospasms, nausea, diarrhea. Metoprolol (Lopressor)
Mostly B-1 blockade, but is also a partial sympathetic agonist (non-selective). Low lipid solubility, so little CNS effect. Membrane stabalizing effect on the action potential is present, but less than propranolol. Used for HTN and ventricular arrhythmias Acebutolol (Sectral)
– Does not cause as much bronchoconstriction as non-selective β blockers. – Less likely to cause bradycardia than other β1 blockers, due to its intrinsic sympathomimetic activity. – S.E.: alopecia, dizziness, angina, fatigue, heart failure. Acebutolol (Sectral)
– Blocks β1 mostly. – Used to treat hypertension, acute myocardial infarction, angina pectoris. – Contraindicated in bradycardia, heart block, shock, cardiac failure. – Adverse reactions include bradycardia, dizziness, fatigue. Atenolol (Tenormin)
–β1 antagonist. – Given by IV infusion. – Used for A.fib or flutter, paroxysmal supraventricular tachycardia. – Contraindications: bronchospasms, bradycardia, shock. – S.E.: AV block, cardiac arrest, hypotension, bradycardia. – T1/2 of only a few min Esmolol (Brevibloc)
– Inhibitor of tyrosine hydroxylase. – Used for pheochromocytoma. – Contraindicated in hepatic disease, Parkinson's disease. – Adverse reactions include anxiety, confusion, crystalluria, depression, Parkinsonism, salivation. Metyrosine (Demser)
Adrenergic Antagonist – Blocks catecholamine release from nerve terminal. – Used for ventricular tachycardia, prophylaxis of ventricular fibrillation. – Adverse reactions: hypotension, bradycardia. Bretylium (Bretylol)
Inhibits storage of catecholamines (and serotonin) in granules, leading to depletion. Initial effects may cause transient release. Used for HTN & schizo. S.E: vomiting, diarrhea, dry mouth, syncope, angina, etc Reserpine (Serpalan)
Created by: Bvaleris