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63 Cards in this Set
- Front
- Back
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Bethanechol
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favors M3, improves bladder and GI function
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Cevimeline/Pilocarpine
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Used for dry mouth which increase Helpful Sjogrens syndrome(autoimmune disease which effects salivary glands).
Pilocarpine is generally more used for eye dryness/glaucoma |
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Name anti-muscarinic Drugs
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Atropine, Scopolamine, Ipratropium, Tolterodine, Oxybutyin
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What are the effects of anti-muscarinic drugs in each organ system?
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Eyes would dilate, heart rate would increase, if acetylcholine present it is blocked, bronchial relaxation, salivary secretions reduce, no eccrine sweat response
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Difference between Atropine and Scopolamine
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Atropine causes hallucination when it crosses BBB. Scopolamine causes sedation when it crosses BBB
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Describe Atropine
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40% transformed 60% excreted. It is well absorbed and well distributed and can be consumed in almost any context.
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Describe Scopolamine
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Similar to atropine. 40% transformed 60% excreted. It is well absorbed and well distributed and can be consumed in almost any context. Sometimes used for motion sickness.
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Describe Ipratropium
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Can only be taken by inhalation. Does NOT cross BBB and is poorly absorbed and is useful for like asthma attacks. It is an anti-muscarinic
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Donnatal
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Is 4 different anti-muscarinics used to treat IBS
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Lomotil
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used to treat travelers diarrhea. only has atropine to prevent abuse
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tolterodine, oxybutyin
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used for urinary incontinence or enuresis. It is an anti-muscarinic.
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xerostomia
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dry mouth
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cycloplegia
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paralysis of ciliary muscles
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tolterodine, oxybutyin
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Used to relieve bladder spasm and relieve incontinence. It is an anti-muscarinic drug.
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Edrophonium
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Only binds to anion site and is short acting. Used to diagnose a disease called myesthenia gravis. It is a reversible acetylcholinesterase inhibitor.
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Neostigmine, Pyridostigmine, Physostigmine
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Physostigmine readily crosses the BBB. The other two do not. These all bind both at the esteratic and anionic site.
Pyridistigmine is mostly used to treat myesthenia gravis They are all reversible acetylcholinesterase inhibitors. |
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Isofluorophate, Echothiophate,
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Organophosphates that covalently bind to the estheratic site and can be used to treat glaucoma. The phosphorus makes the covalent bond.
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Saron, Soman
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Deadly nerve gases that cause irreversible binding of Acetylcholinesterases.
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Pralidoxine
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It is an antidote for anti-acetylcholinesterase poisoning by binding to anionic site and then having a higher affinity for the phosphate group.
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Neostigmine
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It can be used to reverse the effects of a non-depolarizing neuromuscular blocking drug.
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Nicotine effects
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It is a ganglion blocker as well as a noradrenergic stimulator. It stimulates the release of norepinephrine and epinephrine from adrenal gland. As such it increase heart rate and blood pressure. However, it also has a parasympathetic effect wherein it increases secretions and GI tone/activity. It has complex CNS effects due to the release of dopamine.
He really stressed the importance of understanding that nicotine releases norepinephrine. |
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name common ache used to undo neuromuscular blockers
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neostigmine, pyridostygmine, edrophonium
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When will Ache not be useful to antagonize the effects of another drug?
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Phase I of succinylcholine
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Dantrolene
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Prevents release of calcium from sarcoplasmic reticulum. It blocks contraction and helps treat malignant hyperthermia.
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deinnervation supersensitivity
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Once muscle gets deinnervated you get tremendous upregulation of receptors along the entire muscle. As a result succinylcholine acts on every single receptor Sodium comes out, Potassium comes in but normally that is restricted to the end plate, but now it happens all along the muscle significant enough to cause cardiac problems.
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reserpine
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blocks dopamine or norepinephrine transport into the nerve terminal which then causes them to be destroyed by MAO
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Guanethidine
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Leads to the depletion of NE by slow displacement of the transmitter.
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alpha methyl p tyrosine
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blocks first step(rate limiting) of NE synthesis.
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Disulfiram
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Blocks step 3 of NE synthesis. Also known as antabuse by blocking alcohol dehydrogenase.
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amphetamine, tyramine, ephedrine
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Causes rapid displacement or release of transmitter(NE).
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Guanethidine, bretylium
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causes prevention of release of NE
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phenylephrine
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alpha 1 mimetic
substrate for MAO mydriasis without cycloplegia, pressor, nasal decongestant can be taken orally |
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clonidine
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alpha 2 mimetic
decreases sympathetic tone from CNS as such it decreases HR, contractility, renin release, vasoconstriction. side effects include sedation, dry mouth(decreases secretion) Gi, meaning it inhibits cAMP and increases K+ can be taken in almost any form. |
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isoproterenol
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this is a non selective beta adrenergic(beta 1 beta 2) that acts at the receptor level by mimicing the transmitter
NOT sensitive to MAO. Metabolized by COMT effective ionotropic agent. Effects more on contractility than HR. Bronchodilator. |
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dobutamine
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selective cardiac stimulation by mimicing beta 1 transmitter
very short half life. Must be used with IV drip. Will be used to treat acute heart failure and cardiogenic shock. It is more ionotropic than chronotropic. |
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terbutaline, metaproterenol, albuterol
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selective inhibition of smooth muscle contractions causing bronchodilation. So it can be used for Asthma and COPD. Especially better for COPD since its not a Beta 1 agonist(unless dose pushed).
Beta 2 also relaxes uterine smooth muscle to prevent premature labor(tocolytic) beta 2 agonist NOT metabolized by MAO or COMT |
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propranalol
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non selective beta adrenergic blocker(beta 1 beta 2)
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metoprolol
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selective beta 1 blocker
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phenoxybenzamine
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non selective alpha blocker
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Name the 6 types of effects from adrenergic agonists
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excitatory/inhibitory on smooth muscle/effectir organs
excitatory effects on heart metabolic effects(increase glucose) endocrine effects(inhibit insulin secretion) CNS effects |
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ephedrine
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CNS activity. Long lasting epinephrine. Mixed acting sympathomimetics.
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Dopamine
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indirect acting sympathomimetic that causes vasodilation. Can be useful in cardiogenic shock. Stimulates failing heart and dilates some vessels while it contracts others.
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Amphetamine
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Prototypical indirectly acting sympathomimetic that is nonselective. Can cause schizophrenia. Effective for ADHD and narcolepsy. It release dopamine, NE, etc.
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catecholamines
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Epinephrine, NE, isoproterenol, dopamine, dobutamine
Cannot be taken orally, rapid and brief duration of action, does not penetrate BBB |
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non catecholamines
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Phenylephrine, Clonidine, Terbutaline(Metaproteranol, albuterol, Amphetamine
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phenoxybenzamine
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reflex tachycardia, orthostatic hypertension
non-competitive inhibitor non-selective alpha antagonist can be taken in almost any way also blocks histamine, acetylcholine and serotonin receptors if dose is high enough hypertensive crisis |
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Phentolamine
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non-selective alpha antagonist
reflex tachycardia, potent vasodilator, block of presynaptic alpha 2 may promote NE release. hypertensive crisis |
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prazosin, terazosin, doxazosin, tamsulosin
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alpha 1 selective antagonist, decrease BP and PVR, cardiac stimulation is less because the inhibitory is not there in cardiac shit.
Used for benign prostatic hyperplasia. varying half life |
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alpha 1 receptor antagonists inhibit ejaculation
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okay just remember.
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nadolol
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penetrates BBB
beta blocker non selective 1st gen used for hypertension |
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pindolol
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only first gen with intrinsic sympathomimetic partial agonist.
membrane stabilizing less likely to cause bradycardia and lipid abnormalities used for hypertension, angina and migraines |
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timolol
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first drug used to treat wide angle glaucoma
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metropolol
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beta 1 selective antagonist which is 2nd gen. Do NOT use with asthma.
it is cardioselective(causes its only beta 1) less bronchoconstriction |
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side effects of beta blockers
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bradycardia, AV block, sedation, mask symptoms of hypoglycemia
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carevedilol
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non selective beta receptor antagonist that is also alpha 1 receptor antagonist that also has anti-oxidant effects
beta blocking activity prevents reflex tachycardia normally associated with alpha 1 antagonists |
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labetalol
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non-selective beta receptor antagonist and alpha 1 receptor antagonist
beta blocking activity prevents reflex tachycardia normally associated with alpha 1 antagonists |
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propranolol
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non-selective beta antagonist
lipophilic local anesthetic Decreased cardiac output and HR reduced Renin increases VLDL and decrease HDL inhibit lipolysi inhibits compensatory response in response to hypoglycemia increase bronchial airway resistance |
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contraindications of beta blockers
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Asthma, COPD, congestive heart failure
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Guanethidine
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taken up by same transporter as NE. Once it gets inside prevents release of NE. Then it prevents uptake of Dopamine and NE into vesicles. "False transmitter" because it takes the place of NE in vesicles but doesn't do anything.
No effects on CNS. Postural hypotension. used to treat hypertension |
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hallmark of anything blocking alpha receptors is...
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postural hypotension
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Reserpine
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CAN READILY cross membranes. doesn't need transporter.
its blocks dopamine and NE membrane into vesicles(uptake 2). slow onset. penetrates CNS possibly leading to depression. used for treatment of hypertension. |
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alpha metatyrosine
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blocks tyrosine hydroxylase which is ratelimiting step of NE synthesis. Useful for pheochromocytoma that is inoperable.
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alpha methyldopa
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just like clonidine. its a centrally acting alpha 2 agonist. methyldopa is a prodrug.
reduces sympathetic output from CNS thereby reducing hypertension. |
