Post on 08-Dec-2015
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DESCRIPTIONpharmacology test prep
A 43 year old male is brought to the ER by a friend. He is salivatingexcessively and he has had diarrhea and urinary incontinence.He is a migrant worker and had been picking vegetables in a fieldwhen the symptoms started. On physical exam he is wheezing.Which of the following drugs would have the best potential toimprove his symptoms? A. Acetylcholine (make it worse)B. Nicotine (paralysis)C. Edrophonium (bad effect)D. Atropine
Absorption applies to all _________of administration except ________
routes of entry, except topical(drugs applied directly on thetarget tissue) and IV (drug isalready in circulation, directly putin)
Absorption Of Indirect Cholinesterase Inhibitors:Organophosphates: Topical absorption is ________ (they can beabsorbed from whatever body surface they are placed on (skin,mucous membrane, eye, gut or lungs) & once absorbed they getinto the ________ nervous system.Because of their absorption they are good for killing _______; theycan be absorbed through the bugs exoskeleton & then affect it'snerves (more seen in pesticides than anything human). healthcare providers have a risk of exposure through their skin iftreating a patient with a nerve gas or insecticide toxicity
excellent, central, bugs
Absorption Of Indirect CholinesteraseInhibitors: Quaternary compounds:Topical absorption is ______ & they don'tget into the _______ nervous system verywell.
Selective 1 - blockers
Acetylcholine has an extremely_____ duration of action-works ____
& is gone ____short, fast, fast
Acetylcholine has limitedabsorption from the _______, somust give _________ (__, __, or __)
stomach, Parenterally (route otherthan the gastro-intestinal tract) M
and N receptors equally, SQ, IM, orIV)
ACh binds _______ well to both N &M receptors, but drugs do ____.Most drugs bind better to one
subtype or other
ACh receptors are receptors thatbind to ACh: Divided into 2 types
muscarinic and nicotinic
Actions of the body on the drug. Thisdetermines how and to who you give adrug. E.g. Does the body absorb it wellfrom the stomach so it can be givenorally, or does it need to be givendirectly into a vein?
Actions of the drug on the bodythat determine how the drug isused therapeutically. E.g. Doesdrug decrease blood pressure? Ordoes it block histamine?
Activation of muscarinic receptors onpresynaptic nerves inhibit furtherneurotransmitter releaseSo, the release of ACh fromparasympathetic nerve inhibits releaseof _________ from sympathetic nerves
Activation of these receptorsmediate platelet aggregation and
inhibit insulin secretion frompancreas
Additional Effects On Glands Of ACh:Increase _____, ______ and ____________gland secretion.Get sweaty, tearing eyes, & runny nosy.Clinically: give to help special cases of____ eyes
sweat, lacrimal andnasopharyngeal, dry
Adrenergic agonist are also given to_______ blood flow to certain areas as inwound stitching. Alpha receptors aregiven to cause vasoconstriction around awound to decrease blood flow from thewound while stitching the woundclosed.
Adrenergic agonists are used to increase blood______ & ______? A patient with a very low BP doesnot get enough blood to the organs like the brain& heart. Stimulating alpha receptors causes________ of the blood vessels in the periphery(periphery being anything that is not an organ),increasing BP & perfusion to critical organs
flow & BP, constriction
Adrenergic fibers have a morenarrow focus than cholinergic
fivers and are only found in the________?
Adrenergic Neurons? release Norepinephrine,Epinephrine, Dopamine
Adrenergic Receptors: Bind ______,______, or __________ to target
organs of the __________ nervoussystem
bind NE, Epi, or Dopamine to targetorgans of the Sympathetic Nervous
Adverse reactions of Alpha antagonists: 1. _______ ______.When you stand up, gravity sends blood to the legs. The bodyreflexively constricts veins to push blood back into body towardsbrain. Alpha blockers block this reflex, so blood stays in legs & BP goesvery low when standing. These drugs can cause light-headedness& passing out2. Reflex ___________3. Miosis (pupil ___________)4. Nasal stuffiness
Postural hypotension, tachycardia,constriction
After _____ half-lives get to steadystate level.
five (five doses)
All ACh receptors are the ________subtype (the nicotinic subtype arepreganglionic & skeletal muscleNOT at PNS target organs)
All drugs have some inherent_______. The ____ weighs whetherthe potential benefits of the drug
outweigh the risk.
Risks, FDA (most chemotherapy isNOT safe, but is relatively safe
when compared to the risk of thecancer
All preganglionic nerve fibers ofthe ANS release ______ to transmit
Almost all drugs __________ bind toplasma proteins, primarily _______?
reversibly, albumin (drugmolecules dissociate from plasmaproteins to maintain balancebetween free drug and bounddrug)
Alpha 1,2 and beta 2 adrenergicreceptors are found on arterial_______ muscle cells. Agonists(sympathomimetics) effect:
Alpha 1 blockade ______ vascularand other smooth muscles.
Beta 1 blockade _______stimulation of the heart.
Alpha 1 Mediate _________ ofvascular smooth muscle, the irisdilator muscle, and smooth musclein the lower urinary tract (bladder,urethra, and prostate)
Alpha 2 receptors are in the CNS and whenstimulated they elevate _____ & make more_____, decrease/suppress _______Clinical use; narcolepsy, ADD, +/- weightcontrol. Only adrenergic agonists that get intothe CNS have an effect here, more nextsemester
mood, alert, appetite
Alpha antagonists prevent arteriesfrom _________ by blocking alpha 1& 2. This _________ BP. Clinical use:
constricting, lowers, HTN
Alpha constriction of blood flow usedwith local anesthesia so ________ don'tbleed when you _____. Epi also is part ofthe ACLS protocols for its ___ effect &__________ for stimulation of all receptors
wounds, stitch, BP, anaphylaxis
alpha, no beta, constricts bloodvessels, no heart effects (until lose
______, ______, ________, and _______are affected the most by a drug
because they are highly perfused.Brain, Heart, Liver, Kidneys
_____, _______, and _______ tissue are thelowest perfused and may require ahigher does of a drug if you need toreach those lower perfused tissues andmay need to take drug longer.
Skin, Bone, and Adipose tissue
Another clinical use of anticholinergicsis cholinomimetic poisoning, such asorganophosphates, insecticides or nervegases. Toxicity occurs from ACh excessso give ________ to try and block effect.Works best with ________ inhibitors andnot well with ________ inhibitors.
atropine (muscarinic/cholinergicblocker), reversible, irreversible
Anticholinergic Organ System Effects:CVS: ________ heart rate with _____ effecton BP _________ AV conduction. Atropineis part of the ACLS (acute cardiac lifesupport) for significant _________.
Increase (Tachycardia), little,Increase, bradycardias (slow heart
Anticholinergic Organ System Effects: Eye:Pupillary constrictor muscles are _______ andget _____ pupils (mydriasis) & cycloplegia(_______ of the _________ muscles for nearvision causing ______ vision). ____ eyes (from_________ tearing) Clinical use: for eye examwhen want _______ pupil & ________ lens
inhibited (relax), dilated, paralysis,accommodation, blurred, Dry,decreased, dilated, paralyzed
Anticholinergic Organ System Effects: GITract: _________ secretions and _______ ofthe GI tract. (increased gastric emptyingtime and intestinal transit time =__________). Clinical use: treat symptomsof ________, ______ spasms
decreased, motility, Constipation,diarrhea, intestinal
Anticholinergic Organ System Effects:GU Tract: ______ smooth muscle of thebladder wall and ______ voiding. (Don'ttend to urinate as much).Clinical use: relieve bladder _______ andhelps those who ________ frequently(overactive bladder)
relaxes, slows, spasm, urinate
Anticholinergic Organ System Effects:Respiratory: Think ____________ & ________secretions. This effects is seen more in an airway or lungthat is _________ than it is in a healthy lung. Clinical use: ________ and occasionally in________.
Bronchodilation, decreased,diseased, chronic obstructive
pulmonary disease (COPD), asthma
Anticholinergic Organ System Effects: SweatGlands: _________ sweat, ________ temperature Leading to cutaneous _________ and skin becomes____, ____ & ______.Clinical use: ______, A major source of morbidity &mortality. When an anticholinergic drug causesdeath most often does so by __________.
decreased, increased, vasodilation,hot, dry & flushed, none,
Anticholinergic Toxicity: Adults: getannoying but generally not _____ effects. _____ mouth, eye _____, _____cardia, ___,____, ______ skin, agitation and delirium.Think: "___ as a bone, _____ as a bat, ____as a beet, _____ as a hatter"
severe, Dry mouth, mydriasis,tachycardia, hot dry flushed skin,agitation and delirium. "dry as abone, blind as a bat, red as a beet,mad as a hatter"