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101 Cards in this Set
- Front
- Back
what is epinephrine |
A potent vasoconstrictor and cardiac stimulant. |
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The rise in systolic blood pressure that occurs after epinephrine is due to what |
positive inotropic and chronotropic actions on the heart (predominantly β1receptors) and the vasoconstriction induced in many vascular beds (a1receptors). |
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Epinephrine also activates what |
β2 receptors in skeletal muscle blood vessels |
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this activation causes what |
dilation |
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how does epinephrine affect exercise |
contributes to increased blood flow |
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Norepinephrine acts of which receptors |
alpha and beta |
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NE acts more on which receptor |
alpha |
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Norepinephrine _______peripheral resistance and both diastolic and systolic blood pressure |
increases |
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NE has _______inotropic effects on the heart |
positive |
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Phenylephrine acts mostly on which receptors |
a1 receptors |
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Phenylephrinedoes does what to TPR |
increases
|
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Phenylephrine does what to venous capacitance |
decreases |
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acts on what receptors in the iris? causes what effect? |
alpha 1 mydriasis |
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does what to blood pressure |
increases systolic and diastolic |
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acts on what receptors in the nasal mucosa? causes what effect? |
alpha 1 decongestion |
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what isIsoproterenol (isoprenaline) |
Potent β-receptor agonist |
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does it affect alpha receptors |
little effect |
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what type of chronotropic and inotropic action? why? |
positive because it activates β receptors almost exclusively. it is a potent vasodilator. |
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what happens to cardiac output and BP |
CO increases and diastolic and mean arterial pressure decreases |
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dopamine activates which receptors and leads to what? |
D1 receptors vasodilation |
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does dopamine act on dose dependent receptors? |
yes |
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at low doses, dopamine acts on which receptors? this causes what? |
dopaminergic receptors increased renal, coronary, and cerebral blood flow. |
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at what fusion rate does dopamine act on dopaminergic receptors |
2 to 5 mcg/kg/min |
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when does dopamine begin to act on β receptors? what happens? |
5mcg/kg/min increase in cardiac contractility and heart rate |
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when does dopamine begin to act at a-receptors in the periphery? what level of dosage is it considered to be? |
10 to 20 mcg/kg/min high |
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what is Dobutamine |
relatively β1-selective syntheticcate cholamine |
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does Amphetamine readily enters the CNS |
yes |
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what does it affect |
stimulant effect on mood and alertness and a depressant effect on appetite |
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Its peripheral actions are mediated primarily through the release of what |
catecholamines |
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what differentiates Methamphetamine(N-methylamphetamine) from amphetamine? |
Meth has higher ratio of central to peripheral actions |
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what is Ephedrine? what does it do? |
mild stimulant Displaces NE from storage vesicles in presynaptic neurons |
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what is Pseudoephedrine |
OTC component of many decongestant mixtures |
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what are Xylometazoline and Oxymetazoline |
Directly-acting a agonists |
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what are these drugs used for and why |
used as topical decongestants because of their ability to promote constriction of the blood vessels of the nasal mucosa |
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what is Rhinitis medicamentosa |
rebound nasal congestion due to down regulation of alpha receptors |
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what does it do |
decreased endogenous norepinephrine production, etc |
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2 types of a2 Selective Agonists |
Clonidine and Apraclonidine |
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what is clonidine used for |
Used in hypertension, diabetic diarrhea,narcotic addicts and to treat benzodiazepine withdrawal effects |
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what are its side effects |
Postural hypotension, dry mouth, sedation, rebound hypertension |
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what is Apraclonidine what is it used for |
A clonidine derivative Used in glaucoma |
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what is Cocaine |
local anesthetic with a peripheral sympathomimetic action |
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whats its action from |
inhibition of transmitter reuptake at noradrenergic synapses |
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does it readily enter the CNS? what does it produce? |
yes amphetamine - like effect that is shorter lasting and more intense. |
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the major action of cocaine on the CNS is to what |
inhibit dopamine reuptake |
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what is Tyramine |
normal by-product of tyrosine metabolism in the body |
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where is it also found |
in high concentrations in fermented foods such as cheese |
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what happens if administered parenterally |
it has an indirect sympathomimetic action caused by the release of stored catecholamines |
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its spectrum of action is similar to what |
NE |
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when is the effect of tyramine is greatly intensified |
In patients treated with MAO inhibitors (particularly MAO-A isoform) |
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who must avoid tyramine containing foods |
Patients taking MAO inhibitors |
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Increased sympathetic system activity can lead to what |
pathological conditions |
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Blockade of SNS can provide beneficial effect when______ |
there is increased SNS activity |
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Receptor specific blockers _______ the unwanted side effects associated with these blockers |
decreases |
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3 types of adrenergic drugs |
Alphablockers Betablockers Alphaplus beta blockers |
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2 types of alpha blockers |
Phenoxybenzamine Phentolamine |
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Phenoxybenzamine blocks what |
blocks α1> α2 |
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is it reversible or irreversible |
Irreversible,forms covalent bond with receptors |
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Phentolamine blocks what |
blocks α1= α2 |
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is it reversible or irreversible |
reversible |
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4 types of a1 selective blockers |
•Prazosin • Terazosin • Doxazocin • Tamsulocin |
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2 types of a2 selective blockers |
Yohimbine Mirtazapine |
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what is Mirtazapine used for |
antidepressant |
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Alpha Blockers used for Pheochromocytoma |
•Phenoxybenzamine / Phentolamine |
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Alpha Blockers used for essential HTN |
Prazosin |
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alpha blockers used for Hypertension due to clonidine withdrawal |
•phenoxybenzamine /Phentolamine. |
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which alpha blocker is used in Raynaud's Phenomenon |
prazosin |
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which one is used in Benign prostatic hyperplasia (BPH) |
a blockers- Prazosin a1a blockers - Tamsulosin is preferred |
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how do they work |
They decrease the tone of prostate/ bladder muscles |
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prostate has which receptors predominantly |
a1a |
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bladder has which receptors |
a1a receptor 1/3, a1d receptor 2/3 |
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what happens in Benign Prostate Hyperplasia (BPH) |
Overactive a1areceptors in bladder trigone,prostrate and prostatic urethra INCREASES smoothmuscle tone – urinary retention |
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Blockade of these receptors by what relaxesthese structures |
tamsulosin or terazosin |
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alpha blockers do what to the bladder |
Increase urinary flow rate-more complete emptying of the bladder |
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does it reverse the hyperplasia? |
no |
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does it offer symptomatic relief |
yes |
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best treatment for BPH |
tamsulosin+ finasteride |
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what does finasteride do? |
finasteride is5-α reductaseinhibitor - inhibits conversion of testosterone to more potent dihydrotestosterone |
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what is Yohimbine |
a2 selective blocker |
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what does it do? what are its potential uses? |
Enhances sexual activity – aphrodisiac Potential uses: postural hypotension and impotence |
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what is Mirtazapine |
a2 blocker |
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what is it used for |
used in depression |
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At higher doses, beta 1 selective drugs will also______ |
block beta 2 receptors |
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7 Non-selective β1 and β2 receptor blockers |
carteolol nadolol penbutolol pindolol propranolol sotalol timolol |
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7 Selective β1 receptor blockers |
atenolol acebutolol betaxolol bisoprolol esmolol metoprolol nebivolol |
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3 α and βreceptor blockers |
Carvedilol labetalol bucindolol |
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the Beta blockade consists of what |
b1 - Decreases HR, CO b1 - Decreases renin release b2 - Decreases aqueous humor production |
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6 b1 (Cardioselective) blockers (ABEAMN) |
•Atenolol •Betaxolol, bisoprolol •Esmolol •Acebutolol(with ISA) •Metoprolol •Nebivolol |
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which one has a short half life of 10 minutes |
Esmolol |
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advantages of b1 (Cardioselective) blockers |
safer in bronchial asthma, diabetes mellitus and peripheral vascular diseases |
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clinical uses of Nonselective Beta Blockers |
•Hypertension •Angina •Migraine headache •Cardiac arrhythmia •Glaucoma •Myocardial infarction •Essential tremors •Congestive cardiac failure •Hyperthyroidism •Stage fright / Performance anxiety |
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how are Nonselective Beta Blockers in MI's |
prevents reinfarction and improves long term survival |
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which one is used in CHF |
carvedilol |
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which one is used in glaucoma |
timolol |
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most common adverse effect of beta blockers |
bradycardia (inhibits AV conduction. If HR<60, should not use βblockers) |
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chronic use of beta blockers is associated with what |
raised lipid levels (LDL andTG)---- mechanism unknown |
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other adverse effects of beta blockers |
Weakness/Fatigue Hypotension hallucinations Impotence CHF Masks symptoms of hypoglycemia May cause hypoglycemia (decreases glycogenolysis)or hyperglycemia (inhibits insulin secretion). |
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beta blocker overdose can lead to what |
severe cardiac failure in susceptible individuals topical application can lead to toxicity |
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antidote for beta blocker overdose |
glucagon |
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what does it do |
binds to glucagon receptor - activates adenylyl cyclase - increases cAMP, and has inotropic and chronotropic effects on heart |
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3 Non-Selective Beta Blockers Contraindications |
bronchial asthma prinzmetal angina & peripheral vascular disease diabetes mellitus |
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Raynaud’s disease and Prinzmetal angina first drug of choice |
calcium channel blockers |