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Block 3 > Pharm > Flashcards

Pharm Flashcards

1
Q

describe enteric nervous system

A

innervates GI –> GI motility & secretion, indep ctrl but regulated by auto nervous system & higher CNS

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2
Q

Somatic vs autonomic nervous system

A

skel muscle; vol movements; regulated by corticospinal tracts & spinal reflexes vs sm muscles, exo > endocrine glands, cardiac tissue; involuntary; reg by brainstem centers

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3
Q

NT: Ach vs NE

A

released by cholinergic neurons; in autonomic ganglia, parasympathetic & somatic and some sympathetic neuroeffector jxns vs released by adrenergic neurons (epi = principal catecholamine); in sympathetic neuroeffector jxns

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4
Q

parasympathetic/trophotropic vs sympathetic/ergotropic nervous system sxs. where do ANS & endo system integrate?

A

CN 3/7/9/10, S2-4 (pelvic splanchnic n), rest & digest; anabolic; broncho/pupil constrict, vasodil, dec bp/HR, ctx blad/relaxes urin sphincter vs T1-L2/3, f/light; catabolic; broncho/pupil dil, vasoconstrict, inc bp/HR, relaxes blad/ctx urin sphincter. midbrain & medulla

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5
Q

7 Steps of synaptic neurotransmission. KNOW CHOLINERGIC VS ADRENERGIC TRANSMISSION

A
  1. synthesis & storage
  2. AP & depol
  3. activate voltage-gated Ca2+ channels
  4. vesicle fusion & release
  5. receptor binding
  6. signal termination in synaptic cleft
  7. termination of postsynaptic intracellular signaling
    JOE’s sTUDY GUIDE, PG 2
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6
Q

Gs vs Gi vs Gq

A

all = alpha subunits. inc cAMP –> excite skel muscle, relax smooth muscle vs dec cAMP –> relax skel muscle, excite smooth muscle vs inc Ca2+ –> excite skel & smooth muscles

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7
Q

what does AchE do? reversible AchE inhibitors can be non vs covalent and bind to what part of enzyme?

A

degrades Ach to choline + acetate to stop neurotransmission in cholinergic synpases. bind to anion AchE –> rapid hydrolysis –> short acting vs bind to AchE –> slow hydrolysis –> intermediate acting

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8
Q

which reversible AchE inhibitors tx MG, postop urin retention vs glaucoma vs Alzheimer’s?

A

neo/pyridostigmine (covalent) vs physostigmine (covalent) vs donepezil, galantamine, rivastigmine

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9
Q

what’s Myasthenia Gravis? tx? AE?

A

autoab form against Nm receptor at NM jxn –> dec # of Nm receptors –> skel muscle weakness that worsens w/ activity & improves w/ rest, ptosis, diplopia, dysarthria/phagia, loss facial expressions. IV Edrophonium (AchE inhibitor) to amplify Ach effects –> restore muscle strength; oral pyridostigmine QD w/ concomitant immunosuppressants. abd cramps, diarrhea

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10
Q

what do irreversible AchE inhibitors do? examples & fxn?

A

phosphorylate AchE –> slow hydrolysis –> long acting. organophosphates in pesticides & nerve gases, high soluble in lipids –> absorb in skin & GI, activate musc & nico receptors; echothiopate for glaucoma; malathion for pediculosis –> kill ova & lice

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11
Q

organophosphate poisoning: insecticides vs toxic nerve gases. sxs? tx?

A

para/malathion vs sarin, soman, tabun, VX. cholinergic side effects (diarrhea, urin, miosis, bronchospasm, bradycard, excitation, lacrim, sweats, salivate) + paralysis + CNS –> resp depression, sz, coma. supportive, tx shock, cholinergic receptor antag, diazepam for sz, pralidoxime regen cholinesterase

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12
Q

organophosphate poisoning: intermediate syndrome

A

low AchE, severe muscle weakness w/ sx delay 1-2d

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13
Q

mushrooms = muscarinic agonists

A

ino/clitocybe have muscarine but toxic –> diarrhea, sweats, salivation, lacrimation

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14
Q

nicotine

A

activates vasc system (symp) –> inc HR/bp; and GI (parasymp) –> diarrhea, urin. crosses BBB –> alertness, emesis, tremors, convulsion, coma

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15
Q

nicotinic receptor agonists: nicotine replacement therapy vs varenicline

A

give small dose of nicotine to dec cravings vs partial agonist in Nn receptors in brain –> dec cravings, smoking cess, w/drawal effects BUT suicidal ideation, depression, behav change

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16
Q

what does Ach do in general? on M2 vs M3?

A

activate muscarinic receptors M1-5 –> parasymp nerves, dec HR, inc GI motility vs inc GI motility, constrict iris/airway/ciliary mm, vasodil, inc secretions

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17
Q

short term vs long term MS tx goal meds. targets?

A

IV solumedrol, prednisone, ACTHar; steroids don’t prevent further dmg or modify dz vs dz modifying therapy –> dec disability, future exac, dmg on MRI. prevent Tcells crossing BBB, become antinflamm cells, seq them to LN, T/B cell autoimmune destruction

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18
Q

glatiramer acetate = subq injection daily to 3x/wk. mechanism? side effects?

A

polymer of most common aa in myelin basic protein –> proinflam Th1 switch to antiinflam Th2 –> dec exac & new MRI lesions. injection site rxn, flushing, palpitations, lipoatrophy

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19
Q

interferon B meds: low dose B-1a vs high dose B-1a vs high dose B-1b. mechanism? side effects?

A

avonex IM wkly, plegridy subq qowk vs rebif subq 3x/wk vs betaseron, extavia subq qod. dec T cell activation, prolif, migration to CNS; antagonize effects of proinflam cytok –> dec new MRI lesion, disability. flu like, inc LFT, depress, hypothyroid

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20
Q

teriflunomide freq & mechanism. side effects? downside?

A

daily oral; inhib de novo pyrimidine synthesis –> slow rep of T cells –> dec MRI lesion, slow dz progression. hair thin, inc bp & LFT, HA, diarrhea, TB reactivation, birth defects. slow metab (stays for 2y) –> rapid elim protocol w/ cholestyramine or activated charcoal

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21
Q

fumarates freq & mechanism. side effects?

A

bid oral; activates Nrf-2 in oxidative stress –> exhaled out –> dec new MRI lesion, slow progression. flushing, GI, lymphopenia, PML

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22
Q

S1P receptor modulators freq & mechanism. side effects?

A

1/3/4/5 block lymphocytes from leaving LN –> dec lymphocytes in CNS –> dec new MRI lesion, slow progression. bradycardia, AV block, inc LFT, leukopenia, HA, macular edema, PML

23
Q

Oral cladribine. side effects?

A

2 5-6d cycles 2y in a row; purine nucleoside analog –> incorporates into T/B DNA to prevent DNA synthesis. lymphopenia, fever, nausea/abd pain, HA, infxn, ca if >2y in a row

24
Q

natalizumab. side effects?

A

monoclonal ab fusion q28d; blocks alpha-4 subunit on intgerin –> prevent lymphocytes from mig to CNS –> dec new MRI lesion & slow progression. infusion rxn, inc LFT, dec WBC, PML

25
Q

CD-20 depleting gents: ocreliz/ofatumumab. side effects?

A

q6mo/qwk self injection; monoclonal ab against CD20 B cells –> autoimmune destruction –> dec new MRI lesions. infxn, brca, reactivated hep B

26
Q

aleutuzumab

A

1wk/year infusion x2y; monoclonal ab against CD52 T/B cells –> dec new MRI lesions. infusion rxns, autoimmune thyroiditis/kid/PLT, malig, infxn

27
Q

how can vit D3 vs alpha lipoic acid tx MS?

A

dec dz progression –> drs recommend supplement vs OTC –> dec immune cell mig & chemotaxis, inhibits matrix metalloproteinase

28
Q

how to tx gait?

A

PT, stretch, dalfampriine –> bid oral, K+ channel blockade, improve walking speed, cause sz so don’t use if prev sz or renal failure

29
Q

how to tx spasticity?

A

PT, stretch; tizanidine –> alpha-2 adrenergic agonist –> presynaptic inhibitor of motor neurons, sleepiness/weak muscles; baclofen –> GABA agonist in spinal cord –> dec substance P release, sleepiness/weak muscles; hydro/cryotherapy

30
Q

how to tx fatigue?

A

amantadine
ar/modafinil inhib dop reuptake –> activate glutamic circuits while inhib GABA
serotonin-norep reuptake inhibitors
amphetamines inc dop release & inhib dop reuptake

31
Q

how to tx pain?

A

cannabis
sedating antiepi meds –> gabapentin, phenytoin
tricyclic antidep –> ami/nortriptyline
SNRIs –> duloxetine

32
Q

how to tx blad?

A

oxybutynin, tolterodine, solifenacin, timed voids, self-cath

33
Q

neuromyelitis optica vs dx vs tx

A

demyelination of CNS similar to MS; affects optic n & spinal cord. typical MS txs don’t work vs AQ-4 ab, CSF w/ inc WBC; optic neuritis, transverse myelitis vs rituximab –> depletes CD20 B cells similar to ocrelizumab; ecluzimab –> blocks complement from depositing on nerve terminal

34
Q

sympathomimetics vs sympatholytics

A

drugs enhance/mimic noradrenergic transmission –> facilitate release, block reuptake, receptor agonists vs drugs dec noradrenergic transmission –> inhib release & synthesis, disrupt vesicular transport & storage, receptor antag

35
Q

D1 vs D2 vs imidazoline receptors vs trace amine-assoc receptor 1

A

relaxation in vasc smooth muscle vs NT release vs natriuresis, dec sympathetic outflow vs biogenic amine fxn

36
Q

natural vs synthetic catecholamines w/ their indications. inactivated by what?

A

norepi for neurogenic/septic shock; epi for cardiac arrest, prolong anesthesia, anaphylactic shock; dopamine for cardiogenic, neuro/septic shock vs isoproterenol for bradycard/AV block, dobutamine for acute heart failure, cardiogenic shock. MAO & COMT in gut & liver

37
Q

AE of catecholamines

A

vasoconstrict –> ischemia/nec; cardiac stim –> arrhythmia; glycogenolysis –> hyperglycemia

38
Q

alpha agonist of noncatecholamines: phenylephrine MOA vs ADME vs indications

A

activate alpha1 receptors vs oral, topical, IV; partly metab by MAO in liver/intest vs viral/allergic rhinitis allergic conjunctivitis, mydriasis; hypoTN/shock d/t vasodil, drugs, neuro/septic shock

39
Q

alpha agonist of noncatecholamines: midorine MOA vs ADME vs indications vs AE

A

activates alpha1 receptor –> vasoconstrict vs oral; metab in liver vs orthostat hypoTN vs HTN esp when supine

40
Q

beta2 agonists: albuterol, salmeterol, formoterol, bitoterol, terbutaline MOA vs indication vs AE

A

activate beta2 receptors –> relax bronchial, ut, vasc sm muscles vs COPD, asthma vs tachcard, skel muscle tremor, nervous

41
Q

imidazolines: oxymetazoline vs apracl/brimonidine vs clonidine; dexmedetomidine

A

activate alpha1 receptor –> nasal & ocular decongestant vs activate alpha2 receptor –> dec intraocular pressure w/ ocular surgery vs activate alpha2 & imidazoline receptor –> tx HTN by dec periph resistance, HR, cardiac output but can cause dry mouth, sedate, dizzy; sedation during mech ventilation

42
Q

indirect acting adrenergic agonists: amphetamine MOA vs ADME vs indication vs AE

A

inhib norepi storage in neuron vesicles –> reverse transport back into synapse –> inc norepi in CNS & periph vs lipid soluble vs ADHD vs vasoconstrict, cardiac & CNS
stim, inc bp

43
Q

indirect acting adrenergic agonists: cocaine MOA vs indication vs AE

A

block neuronal uptake of norepi at central & periph synapse –> stim sympathetic nervous system vs local anesthesia vs vasoconstrict, cardiac & CNS
stim, inc bp

44
Q

mixed acting adrenergic agonists: pseudo/epherine MOA vs ADME vs indication vs AE

A

activate alpha1 receptor –> vasoconstrict, inc bp, urin retention; activate beta1 receptor –> tachycardia; activate beta2 receptor –> bronchodil vs lipid soluble, resistant to MAO & COMT vs vasopressors, decongestants vs CNS stim –> insomnia

45
Q

selective alpha1 adrenergic antag: prazosin/doxazosin/terazosin MOA vs indication vs AE. uroselective meds?

A

competitive alpha1 receptor antag for 6/30/20h–> vasodil/dec bp, relax blad/urethra/prostatic sm muscle vs HTN vs hypoTN, dizzy, sedate. alfuzosin/tamsulosin –> tx urin freq/incont d/t BPH

46
Q

selective alpha2 antag: yohimbine MOA vs indication

A

selective competitive alpha2 antag –> inc bp/HR, motor activity; opposite of clonidine vs male ED

47
Q

alpha blocking neuroleptic agents: chlorpromazine, phenothiazines, haloperidol

A

block D2 & alpha receptors –> induce side effects via alpha2 blockade

48
Q

amantadine. AE?

A

2nd in line NMDA antag that txs dyskinesia from L/C. livedo reticularis

49
Q

memantine. PK vs AE vs DI

A

for mod to severe Alz; prevents gluE tox and can be used alone or w/ AchEI. hepatic metab, renal elim vs HA/dizzy/confusion, constipation; skin d/o, sz, ophthalmo d/o vs carbonic anhydrase inhibitors, NMDA antag

50
Q

nicotinic Nn vs Nm receptors

A

both open Na/K+ channels. pentamer of alpha/beta subunits in postganglion neurons & presynaptic cholinergic terminals vs pentamer of alpha/beta/delta subunits in skel muscle motor end plates

51
Q

alpha 1 vs 2 receptors

A

by Gq; ctx blad, prostate, heart; dil pupil vs by Gi; relax sm muscle

52
Q

beta1 vs 2 vs 3 receptors

A

all by Gs. inc heart ctx, force, condux vel vs relax resp & sm muscle, glycogenolysis vs relax blad sm muscle, lipolysis

53
Q

anticholinergic ganglion blocking agents: hexmethonium vs trimethapan vs mecamylamine

A

not used anymore vs for aortic dissect to lower bp –> block sympathetic response vs orphan drug for Tourettes

Block 3 (23 decks)

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