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130 Cards in this Set
- Front
- Back
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the generic name will be listed. name the corresponding Trade name and indication. benztropin |
Cogentin Parkinson's |
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dicyclomine |
Bentyl IBS - diarrhea |
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meclizine |
Dramamine N/V |
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oxybutynin |
Ditropan incontinence and overactive bladder |
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solifenacin |
VESIcare incontinence and overactive bladder |
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rivastigmine |
Exelon dementia |
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tiotropium |
Spiriva COPD |
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tolterodine |
Petrol incontinence and overactive bladder |
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varenicline |
Chantix smoking addiction |
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the following are adrenergic. Albuterol |
ProAir HFA |
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Atenolol |
Tenormin |
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Bisoprolol |
Zebeta |
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Carvedilol |
Coreg |
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Clonidine |
Catapres |
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Dexmethylphenidate |
Focalin treats ADHD - it is a CNS stimulant |
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Doxazosin |
Cardura HTN or BPH alpha blocker - relaxes arteries and relaxes muscles in prostate |
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Labetalol (2) |
Normodyne Trandate HTN |
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Lisdexamfetamine |
Vyvanse ADHD |
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Methylphenidate |
Concerta ADD, ADHD, narcolepsy |
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Metoprolol |
Lopressor beta blocker used to treat angina + HTN |
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Mixed Amphetamine Salts |
Adderall |
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Nebivolol |
Bystolic HTN - beta blocker that slows the heart |
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Phentermine |
Adipex-P treat obesity - suppresses appetite |
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Propranolol |
Inderal beta blocker to tx angina, HTN |
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Tamsulosin |
Flomax alpha blocker that relaxes muscles in prostate, used for BPH |
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Terazosin |
Hytrin HTN + BPH |
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M1 receptors do |
secretions of GI tract |
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M2 receptors do |
slow HR and conduction velocity |
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M3 receptors do |
many parasympathetic functions miosis bronchoconstriction GI motility increases bladder contracts |
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name 6 direct muscarinic agonists |
Ach Methacholine Bethanechol Carbachol Cevimeline Pilocarpine |
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which direct muscarinic agonists can cross the BBB? why |
Ceimeline Pilocarpine they are tertiary amines, so they are uncharged and can cross membrane. |
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Methacholine used for |
inhaled to diagnosis bronchiole airway hyperreactivity (via M3 function) |
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Bethanechol used for |
bladder and bowel activation |
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name 3 clinical uses for muscarinic agonists. |
glaucoma urine retention diagnosis of bronchial hyperreactivity |
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why are muscarinic agonists indicated for urine retention? |
muscarinic agonists promote the parasympathetic response of increased urination via M3 receptors that contract the detrusor muscle |
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major contraindications for muscarinic agonists? (4) |
ulcers asthma heart disease (meds will slow the heart further) bladder or GI obstruction |
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name the 3 types of Cholinesterase Inhibitors |
carbamates organophosphates centrally acting agents |
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how do carbamates work? |
carbamates bind and reversibly "carbamylate" the cholinesterase enzyme |
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two major drugs that are carbamates? |
phygostigmine edrophonium |
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what is Edrophonium used for? |
it is a cholinesterase inhibitor used to diagnose myasthenia gravis |
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what is the key difference between carbamates and organophosphates? |
both are cholinesterase inhibitors, but organophosphates bind irreversibly to cholinesterase |
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what is the immediate effect of organophosphate poisoning? the delayed effect? |
immediate - SLUD delayed - demyelination results in paralysis |
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what happens if you have too much cholinesterase inhibitor? |
toxic - so much Ach is left to work in the synapse that it triggers tachyphylaxis --> SLUD |
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what do you do once organophosphate poisoning is suspected? |
1. give atropine that saves the pt 2. give 2-PAM that saves the enzyme |
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what class does atropine fall into? |
muscarinic antagonist |
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what are the general effects of muscarinic antagonists? |
they are BLOCKING THE PARASYMPATHETIC RESPONSE - so inhibit sweating dilate pupil urine retention etc. |
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muscarinic antagonists block the parasympathetic response. we would expect the heart rate to increase. why doesn't it? |
atropine blocks the presynaptic receptor first, which is a modulating receptor - it will enhance Ach release causing the heart to remain slow. |
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what is concerning about muscarinic antagonists and long term use? |
all show tolerance must take drug holiday to keep benefit |
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give examples of other muscarinic antagonists (atropine is prototypical) (5) |
meclizine oxybutynin solifenacin tiotropium tolterodine |
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contraindications for muscarinic antagonists? (3) |
children (inhibits sweating = hyperthermia) heart problems (further slows the heart rate) benign prostatic hypertrophy (causes urinary retention making the problem worse) |
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what effect does nicotine have on the heart? |
increase HR and BP |
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the heart is a muscarinic organ. why then does nicotine increase HR and BP? |
nicotine causes adrenal release of NE + E, which activate B1 receptors in the heart to increase HR. |
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how does Botox work? |
inhibits Ach release so the muscle is paralyzed |
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what drug is a neuromuscular stimulant? how does it work |
Guanidine stimulates the release of Ach |
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describe how Depolarizing Neuromuscular Blockers work and what it results in |
overstimulates the NMJ by inducing desensitization, leading to muscle weakness. |
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what is the prototypical neuromuscular depolarizing blocker? |
succinylcholine |
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describe a scenario where succinylcholine is used and how it is broken down. |
used to paralyze muscles for quick procedures like intubation. it is quickly broken down by pseudocholinesterase. |
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what are the adverse effects of succinylcholine? (1) |
malignant hyperthermia when the body is coming out of paralysis, muscles can generate discontinuous muscle contracting causing extreme heat |
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what drug should be avoided in treating succinylcholine paralysis? |
cholinesterase inhibitors will cause even more Ach to be left in the synapse strengthening the tachyphylaxis --> muscle paralysis |
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describe how Non-depolarizing Neuromuscular Blockers work |
cause slower paralysis work as competitive, reversible blockers at NMJ |
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main difference between Depolarizing and Non-depolarizing Neuromuscular Blockers? |
cholinesterase inhibitors can only be used to reverse the paralysis from NON-depolarizing neuromuscular blockers |
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which should be used in an eye exam to dilate the pupil - anticholinergic or a1 agonist? why |
a1 agonist because it will dilate the pupil without causing a change in IOP |
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what are the actions of B1 receptors? (2) |
1 heart - increase HR and contraction increase renin release |
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what are the actions of B2 receptors? (4) |
2 lungs - relax bronchioles mild vasodilation of BV promote contraction of skeletal muscle relax uterus to delay labor |
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what is the action of B3 receptors? (1) |
relax detrusor muscle in bladder |
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what is the action of D1 receptors? (1) |
vasodilate mesentery and renal vasculature |
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name the classic adrenergic agonists (4) |
NE E dopamine isoproterenol |
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NE acts on what receptors? |
both alphas and B1, B3 |
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what effect does NE have on HR and why? |
NE decreases HR NE activates alpha receptors, causing vasoconstriction and increased PR. this also causes increased BP. the baroreceptors trigger the vagus nerve to slow the HR to combat this increase in BP. |
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adverse effects of NE? |
the vasoconstriction in tissues can be so intense it is O2 deprived, leading to necrosis. |
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NE indications? |
maintain arterial BP in shock and hypotension vasoconstrict extremities to provide blood for core organs |
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epinephrine acts on what receptors? |
all alphas and betas |
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what tone is dominant when using epinephrine? |
betas are the dominant tone. |
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explain what epinephrine does when activating B2 receptors |
B2s vasodilate, so peripheral resistance drops, meaning diastolic drops. |
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explain what epinephrine does when activating B1 receptors |
B1 causes increase in HR, meaning systolic increases. |
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Isoproterenol acts on what receptors? |
betas |
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why does the BP fall when using isoproterenol? |
B2 receptors are activated, causing vasodilation and huge drop in peripheral resistance, dropping diastolic more than the systolic is rising. |
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what are the two main effects of B2 activation in general? |
bronchodilation vasodilation of periphery |
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what is the main effect of B1 activation generally? |
increase in HR |
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dopamine acts on what receptors? |
all the 1s |
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after giving dopamine, what happens to PR? |
PR drops because dopamine causes blood pooling in the mesentery and kidney vasculature |
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after giving dopamine, what happens to heart rate? |
increases due to B1 activation |
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after giving dopamine, what happens to BP?
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increases |
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what is dopamine used for? |
short-term CV support particularly good during shock because it maintains blood flow to kidneys |
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dobutamine is another adrenergic agonist. what receptors does it act on? |
a1 and betas |
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in dobutamine, what effect predominates? |
beta |
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when is dobutamine used? |
acute mgmt of heart failure, when the heart isn't producing enough strength of contraction to give enough blood flow |
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explain how dobutamine acts on a1 and B1 why is this important? |
a1 - increases force of contraction B1 increases rate force of contraction the force is 2x for every 1x beating |
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give an example of the prototypical B2 selective agonist |
Albuterol (ProAir HFA) |
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B2 selective agonists work by (2) |
bronchodilators smooth muscle relaxants |
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B2 agonists indicated for (2) |
asthma slow down premature labor |
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adverse effects of B2 agonists (2) |
tremor tachycardia (after you use asthma medication you have tremor and racing heart) |
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what is an example of a B3 selective agonist? |
Mirabegron |
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what is Mirabegron used for? |
relax detrusor smooth muscle to increase bladder capacity |
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give 2 examples of a1 selective agonists |
Afrin (oxymetazoline) phenylephrine |
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what are a1 selective agonists used for? think Afrin. |
a1s vasoconstrictor like made, so they are good decongestants because congestion is caused by edema from nose vasculature. |
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a1 selective agonists are used for (3) |
decongestants mydriasis maintain BP during surgery |
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name two a2 selective agonists |
Clonidine alpha-methyl dopa |
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a2 selective agonists are used for |
antihypertension |
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how do a2 selective agonists reduce BP |
work in brainstem by stimulating a2 receptors to reduce sympathetic outflow, dropping BP |
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Clonidine adverse effects? |
Rebound effect can occur with abrupt stopping of meds --> hypertensive crisis |
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why does alpha-methyl dopa have less severe rebound effect than Clonidine? |
alpha-methyl dopa is a substrate for the catecholamine synthesis pathway alpha-methyl dopa --> alpha-methyl dopamine --> alpha-methyl NE it is recyclable, so some amounts will still be left in the body when you stop the drug. |
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Alpha-methyl dopa has less rebound effect than Clonidine, so why is Clonidine used more often? |
alpha-methyl dopa has serious side effects of Parkinson's like state and painful breast development in men |
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why does alpha-methyl dopa cause breast development in men? |
alpha-methyl dopamine is a partial agonist of dopamine, and in the brain this makes dopamine less effective. dopamine usually inhibits prolactin, but once prolactin levels rise --> breast development occurs. |
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mixed action agonists are "the speeds". name 3 examples |
Adderall Concerta Adipex-P |
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what is the name for Concerta |
methylphenidate |
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what is the name for Adipex-P
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phentermine |
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what effects do mixed agonists have on the CNS? (think speed) (4) |
increased respiration alertness psychogenic effects suppress appetite |
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what effects do mixed agonists have on the heart? (think speed) |
cardiac acceleration HTN |
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adverse effects of mixed action agonists? (3) |
drug dependence induce psychological disorders pulmonary HTN esp. in women |
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if something is a non-selective alpha antagonist what does this mean |
it blocks a1 and a2 |
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examples of non-selective alpha antagonist (2) |
Phenoxybenzamine Phentolamine |
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what effects are non-selective alpha antagonists going to have on the body (CV) |
vasodilation hypotension tachycardia (HR tries to compensate for hypotension) |
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what is the serious side effect of Phenoxybenzamine? |
First Dose Effect orthostatic hypotension - passing out when standing |
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Phenoxybenzamine causes orthostatic hypotension, so it is only indicated in a serious situation such as |
BP control in pheochromocytoma |
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what is another non-selective alpha antagonist that is better than Phenoxybenzamine? what is the main difference |
Phentolamine it is a reversible antagonist |
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what is a common adverse effect for ANY alpha blocker? |
sex problems |
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what drugs end in "OSIN" |
alpha blockers |
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what are general indications for alpha blockers (2) |
HTN BPH |
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the drug suffix "lol" refers to what kind of drugs |
beta blockers |
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B1 antagonists what is the suffix and first letter |
start with BEAM and end with "olol" |
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what are the 3 rules in Beta Blockers? |
1. careful in asthmatics 2. careful in diabetics 3. careful in PAD |
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why must you be careful giving beta blockers to an asthmatic? |
if you block B2 receptor increases risk of bronchoconstriction |
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why must you be careful giving beta blockers to diabetics? |
masks symptoms of hypoglycemia like racing heart |
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beta blocker toxicity causes what 3 things |
depression blunted responses from hypoglycemia elevated LDL and triglycerides |
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Atenolol is classified as |
B1 antagonist (starts with BEAM) |
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what about beta blockers with additional actions? what does this mean |
drug suffix is different (-alol or -ilol) blocks betas + blocks a1 |
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what are Beta Blockers with ISA? |
Intrinsic Sympathetic activity means they are antagonists and agonists at the same time |
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2 examples of Beta Blockers with ISA? |
Pindolol Acebutolol |
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Beta Blockers with ISA have what indication? |
pt with resting HR below 50 bpm |
