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pharmacology test prep

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  • 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

    D. Atropine

    Absorption applies to all _________of administration except ________

    and _______?

    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.

    poor, central

    AcebutololAtenololEsmolol

    Metoprolol

    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

    equally, not

    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?

    Pharmacokinetics

  • Actions of the drug on the bodythat determine how the drug isused therapeutically. E.g. Doesdrug decrease blood pressure? Ordoes it block histamine?

    Pharmacodynamics

    Activation of muscarinic receptors onpresynaptic nerves inhibit furtherneurotransmitter releaseSo, the release of ACh fromparasympathetic nerve inhibits releaseof _________ from sympathetic nerves

    NE

    Activation of these receptorsmediate platelet aggregation and

    inhibit insulin secretion frompancreas

    Alpha 2

    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.

    reduce

  • 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________?

    SNS

    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

    System

    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)

    AlbuterolClonidineMidodrine

    OxymetazolinePhenylephrine

    Terbutaline

    Noncatecholamines

    All ACh receptors are the ________subtype (the nicotinic subtype arepreganglionic & skeletal muscleNOT at PNS target organs)

    muscarinic

    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

    their signalACh

  • 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:

    smooth

    Alpha 1 blockade ______ vascularand other smooth muscles.

    Beta 1 blockade _______stimulation of the heart.

    relaxes, reduces

    Alpha 1 Mediate _________ ofvascular smooth muscle, the irisdilator muscle, and smooth musclein the lower urinary tract (bladder,urethra, and prostate)

    contraction, dilator

    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

    selectivity)Phenylephrine

    ______, ______, ________, 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

    rate)

    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,

    hyperthermia

    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"

    any substanc