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100 Cards in this Set
- Front
- Back
ACH binding in the PNS,SNS, and CNS
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in the CNS ACH will bind to the nicotinic receptors which are attached to skeletal muscle
in the PNS ACH will bind to the nicotinic receptors on the ganglion, ACH will also activate to the post ganglionic muscarinic receptors, in the SNS ACH will only bind to the nicotinic receptors ganglia. |
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the binding of Nor.eppi
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Nor Epp. will bind at the post SNS pathway to the Alpha and Beta adrenergic receptors.
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location of the nicotinic receptors
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nicotinic receptors are located at the end of the somatic motor pathway, they are also located in the ganglionic neurons of the PNS and SNS,
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what is a sympatholytic blocker
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A sympatholytic drug is nothing more than an SNS blocker, or antagonist which inhibits the post ganglionic signals of epin, and nor. epin.
all SNS antagonist can be used as antihypertensives. |
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metyrosine
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metyrosine is a good sympatholytic blocker
it will inhibit the TH, or tyrosine hydroxylase step of dopa, Nor. epin formation remember that this is already the rate limiting step |
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guanadrel
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guanadrel is a good sympatholytic
it works by preventing VMAT from transporting Dopa inot the cell where it is made into Nor. epp this is an indirect reaction |
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bretylium
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bretylium pretends to be Nor. Epp so much that VMAT will transport it into vessicels. however, the drug is inactive when released
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muscarinic receptors. and the PNS
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drugs arn't selective towards the 5 subtypes of muscarinic receptors
lower HR, constriction of bronchioles. constriction of pupils, miosis (relief from glaucoma). increased secretions, digestion, urination and dilation of blood vessels. these drugs are most commonly used for the treatment of glaucoma |
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carbachol
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muscarinic receptors agonist or or parasympathomimetics
this drug is used as eye drops to treat glaucoma |
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pilocarpine
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muscarinic receptors agonist or or parasympathomimetics
very similar to carbachol. local administration for glaucoma |
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bethanechol
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(urecholine)
muscarinic receptors agonist or or parasympathomimetics specially to lower gastric secretions and to increase urinary retention |
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pilocarpine
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salagen
muscarinic receptors agonist or or parasympathomimetics usefull in treatment of showgrine syndrome by increasing salivation |
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cevimeline
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evoxac
muscarinic receptors agonist or or parasympathomimetics similar to pilocarpine in helping to increase salivation. |
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muscarine receptor antagonist.
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by blocking the PNS all dual connected tissues become at the mercy of the SNS and Nor. eppi.
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atropine
belladonna clidinium cycopentolate (cyclogyl) |
muscarinic receptor antagonist
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dicyclomine
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bentyl)
muscarinic receptor antagonist |
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flavoxate
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(urispas)
muscarinic receptor antagonist |
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fesoterodine
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(toviaz)
muscarinic receptor antagonist |
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glycopyrrolate
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muscarinic receptor antagonist
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hyoscyamine (levistin)
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muscarinic receptor antagonist
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mepenzolate
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muscarinic receptor antagonist
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mepenzolate
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muscarinic receptor antagonist
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oxybutynin
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(ditropan)
muscarinic receptor antagonist |
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propantheline
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muscarinic receptor antagonist
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scopolamine
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muscarinic receptor antagonist
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solifenacin
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vesicare
muscarinic receptor antagonist |
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tilerodine
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(detrol)
muscarinic receptor antagonist |
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tropicamide
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(mydriacyl)
muscarinic receptor antagonist |
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trospium
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(sanctura)
muscarinic receptor antagonist |
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parasympathomimetic, or PNS agonist
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review exam 2 medchem notes
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neostigmine
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ACHesterase inhibitor
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physostigmine
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ACHesterase inhibitor
reversible carbamate CHesterase inhibitor. commonly used for eye drops. |
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pyridostigmine
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(mestinon)
ACHesterase inhibitor remember gravis |
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ambenomium
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(mytelase)
ACHesterase inhibitor |
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echothiophate
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(phospholine iodide)
ACHesterase inhibitor |
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mestinon
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ACHesterase inhibitors
commonly used for chronic treatment of gravis
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edrophonium
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ACHesterase inhibitors
used for acute diagnosis of gravis as to why mestinon is not working correctly.
injectable
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irreversible ACHesterase inhibitors
bind with much stronger covalent bonds to ACHesterase |
examples are sarin (subway terrorist attacks)
parathion is an irreversible ACHesterase inhibitors which was used to kill larva of californian fruit fly. |
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malathion
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malathion ovide
irreversible ACHesterase inhibitors not bioaviable towards humans, but blocks irreversible ACHesterase inhibitors on insects and kills them all.. lice |
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where are nicotinic receptors located
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CNS, ganglia of PNS and SNS, in the neuromuscular jxn. and the adrenal medulla.
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nicotine's peripheral effects and nicotines central effects
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increased Br, Hr, sweating, GI motility, skeletal relaxation
increase alertness when drowsy, but also relax when tense. also stimulates reward pathways... dependence |
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varenicline
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(chantix)
partial agonist at nicotine receptor in CNS. binds with higher affinity, but less E max. this is the only nicotinic agonist, smoking sensation, chantex |
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Beta 2 receptor location
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primary locations are on the brachial, uterine, blood vessels, skeletal, liver, eyes,
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beta 2 receptor effects
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relaxation of muscles, in the brochi, bronchodialation. uterine relaxation, vasodilatation with a reflex increase in HR, increased production of glucose, tremors, and increased production of aqueous humor
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beta 2 receptor inhibitions (antagonist)
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similar to muscarinic agonist. broncho constriction (bad for asthmatics) , vasoconstriction (cold fingers). and a reduction in glycogenolysis, glucose production, and aqueous humor production.
these inhibitions are commonly only troublesome in people who have pre-existing problems
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beta 2 receptor inhibitions (antagonist)
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similar to muscarinic agonist. broncho constriction (bad for asthmatics) , vasoconstriction (cold fingers). and a reduction in glycogenolysis, glucose production, and aqueous humor production.
these inhibitions are commonly only troublesome in people who have pre-existing problems
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beta 2 adverse effects (of agonist)
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reflex, resulting in an increase of HR, tremors, an increase in blood glucose, and aqueous humor.
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albuterol
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Beta 2 selective agonist
has rapid onset, but is short acting
treating asthma with local administration inhalers
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bitolterol
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tornalate
a Beta 2 selective agonist treating asthma with local administration inhalers |
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isotharine
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foradil
Beta 2 selective agonist
treating asthma with local administration inhalers
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levabuterol
metaproterenol pirbuterol |
xopenex
Beta 2 selective agonist
treating asthma with local administration inhalers
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salmeterol
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servent
Beta 2 selective agonist
treating asthma with local administration inhalers
has a long onset of action, but also a long duration of action. |
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terbutaline
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Beta 2 selective agonist
can also be used IV, good for life threatening asthma
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ritodrine
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Beta 2 selective agonist
given IV as a baby pauser
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isoproterenol
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non selective beta agonist... activation of both Beta 1 and Beta 2 receptors
it will not only cause bronchodiatlion, but will also increase HR.
used more for its chronotropic effects... increasing HR
additive therapeutic effects of both beta 1 and beta 2 agonist.
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dobutamine
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a selective beta 1 agonist, this drug has greater inotropic effect than inotropic effect, increase force of contractions
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non selective beta antagonist
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will block both beta 1 and beta 2
will have additive effects of the beta 1 and beta 2 antagonist. making them less desirable for diabetes and asthmatics.
given to lower hypertension and HR. has many more side effects than the selective agonist up-regulation will occur when patients are on these antagonist. |
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propanolol
nadolol pindolol sotalol |
non selective beta antagonist
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timolol
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non selective beta antagonist,
giving as eye drops for glaucoma, not as bad for asthmatics or diabetics |
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levobunalol
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non selective beta antagonist
giving as eye drops for glaucoma, not as bad for asthmatics or diabetics |
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alpha 1 receptor of the SNS locations
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smooth muscle,
veins, nasal mucosa capillaries, bladder, urethra, prostate, and the radial muscle of the eye
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alpha 1 receptor effects
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vasoconstriction of veins, reflex will lower HR.
vasoconstriction of mucosa,
resistance to urine outflow,
mydriasis due to radial muscle contraction.
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alpha 1 agonist
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alpha 1 will contract the smooth muscle by releasing Ca into the cell from the sarcoplasmic reticulum.
when constricting muscles with an alpha 1 agonist the reflex response will be a reduction in HR.
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Beta 2 agonist
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dilate vessels, causing a reflex increase in HR.
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alpha 1 agonist effects on the nasal passage
prostate, and bladder
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the capillaries from the nasal mucosa will constrict, this will increase the volume of air capable of flowing through the nose... decongestion.
in the prostate and bladder, there will be a resistance to an outflow of urine |
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remember muscarinic receptors. and their relation to bladder excretion
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the muscarinic receptors contract and cause urine to flow out.
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medrysis
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SNS innervates the radial muscle contraction with an alpha agonist
also innervated with a muscarinic agonist.?
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alpha 1 receptors
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think smooth muscle and contraction
contraindications for people with high BP
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uses of alpha 1 agonist
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vasoconstriction is very helpful when patient is in shock because the constriction will increase BP
constriction of nasal passages will help as a decongestant contraindications for people with high BP and BPH |
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midodrine
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an alpha 1 receptor agonist,
used for effecons on hypotension, shock, and low BP
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phenylephrine
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neosynephrine
an alpha 1 receptor agonist,
oral tablets, eye drops, IVs for treating shock and hypotension
remember that histamine is a vasodilator. causing things to swell |
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pheudophedrine
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(sudafed)
an alpha 1 receptor agonist,
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oxymetazoline
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Afrin
an alpha 1 receptor agonist
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alpha 1 receptor agonist contraindications
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bad for people with High BP, also bad for people with BPH
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an alpha 1 receptor agonist therapeutic side effects,
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things like overactive bladder would be reduced, but we have better less negatively therapeutic drugs which will work better.
most useful for hypotension, shock, and nasal congestion. |
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alpha 1 receptor antagonist
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great for causing vasodilatation, this will result in an increase in HR because of the reflex response
will cause nasal congestion. and will increase urine outflow. vasodialation and its treatment of hypertension. decreasing peripheral resistance. bind to both alpha 1a and 1b, both in the prostate, and in the blood vessels |
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prazosin
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alpha 1 receptor antagonist
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perazosin
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hytrin
alpha 1 receptor antagonist
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doxazosin
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cardura
alpha 1 receptor antagonist
good for treating hypertension and good for treating BPH |
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alfuzosin
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uroxatral
alpha 1 receptor antagonist
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alpha 1 receptors in the prostate
alpha 1 receptors in the smooth muscle
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drugs can now be selective between these two locations
remeber that the alpha 1 ac receptors are in the bladder, and that the alpha 1b receptors are in the prostate |
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flowmax
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tamsulosin selective for the alpha 1a receptor, will not bind to the alhpa 1b receptor. remeber that the alpha 1 ac receptors are in the bladder, and that the alpha 1b receptors are in the prostate
less dizziness, less reflex tachycardia. |
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flowmax is selective, and not specific
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this means that tamsulosin will still have effects on the alpha 1b receptors in the prostate and bladder, but these effects will be much less than the effects being generated in the smooth muscle
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labetalol
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antagonist at the beta 1, beta 2, and alpha 1 receptors
almost like a combination of propanolol with prazosin good for antihypertensives blocking beta 2 is just soso, all we want is to block alpha 1 and beta 1 advantages over other drugs because it will lower HR, reduce cardiac output, and also vasodilatation, advantages over alpha 1 agonist, is that it will not vasodilatation, but also decrease HR |
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carvedilol
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antagonist at the beta 1, beta 2, and alpha 1 receptors
almost like a combination of propanolol with prazosin good for antihypertensives blocking beta 2 is just soso, all we want is to block alpha 1 and beta 1 advantages over other drugs because it will lower HR, reduce cardiac output, and also vasodilatation, advantages over alpha 1 agonist, is that it will not vasodilatation, but also decrease HR |
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mecamylamine.
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competitive antagonist as neural nicotinic receptor (ganglionic blocker)
excluding the vessels almost all tissues are always basiled together. mecamylamine will block all ganglionic nicotenic receptors, which are in both SNS and PNS. this results in reduced neuro transmission everywhere
needed for immediate reduction of hypertension |
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how does mecamylamine reduce hypertension
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mecamylamine will block both SNS and PNS. however because veins are only controlled over by SNS, when its presence is removed dialation occurs.
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muscle nicotinic receptor antagonist.
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learn how i work
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curonium
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any suffix of curonium translates into a muscle nicotinic receptor antagonist.
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atracuronium
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muscle nicotinic receptor antagonist
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what do muscle nicotinic receptor antagonist do? remember they also end with curonium
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these drugs cause the release of histamine from mast cells. which binds to receptors to begin allergic reactions... this leads to vasodilatation and and an increased Hr.
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muscle nicotinic receptor antagonist are medically useful for surgery. explain.
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they cause paralysis because they are competitive blockers of ACH which is needed for muscle contractions.
they may prevent the diaphragm from working. so when surgery is done to reverse paralysis administer ACHesterase inhibitors like neostigmine which will increase ACH levels in synapse, however neostigmine may also lower Hr, so it may be smart to also give atropine
will atropine only increase hr? or will it cause systemic effects thus hurting the diaphram even more. |
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succinylcholine problems
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succinylcholine may act as a depolarizing neuromuscular blockers and result in uncontrolled release of calcium from SR causing contractions. this produces lots of heat and increases the body temp.
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beta 2 receptor antagonist.
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preventing nor. epin from binding to beta 1 receptors will allow for vasodilatation, and decreases in HR
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acebutolol
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sectral
beta 2 receptor antagonist. |
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atenolol
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tenormin
beta 2 receptor antagonist. |
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betaxolol
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beta 2 receptor antagonist.
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bisoprolol
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beta 2 receptor antagonist.
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metoprolol
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lopressor, toprol,
beta 2 receptor antagonist. |
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esmolol
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brevibloc, good for treating acute arrhythmia's, very short acting, and give as an IV during emergencies, will be broken down by plasma esterase
beta 2 receptor antagonist. |