cholinergic- meynert, medial septal---dementia

seritonergic- raphe---emotion, sleep

histaminergic- tuberomammillary- ventral posterior hypothalamus, wakefullness, motion

seritonin syndrome- agitation, diarrh, inc hr/bp, hallucinations, fever, ataxia, hyperreflexia, shivering, sweating, tremor, n/v, myoclonus

AAD inhibitor, also benserazide

levi/carbi SE: anorexia, n/v, orthostasis, arrythmia, psychosis, agitation, neuroleptic malignant syndrome if withdrawal 

bromocriptine- d2 agonist, d1 ant - harder to titrate

pramipexole - d2 only

ropinirole

benztropine, trihexyphenadyl, biperidine, procyclidine

treats tremor and drooling, but side effects, discontinuation->exacerbation

rescue for "off" episodes

lots of emesis- trimethobenzamide or domipeirodne admin as well

entacapone, well tolerated, reduces off

tolcapone, more potent- hepatotox

anticholinergic, dopaminergic, anti-nmda

mild early PD symptoms

not in dementia

tetrabenazine, reserpine, amantadine

haloperidol, fluphenazine

riluzole

antaganizes kainate and NMDA glu receptors

baclofen- gabaB agonist, treats spasticity

tizanidine- a2 autoreceptor

chlorpormazine, fluphenazine, trifluoperazine, perphenazine, thioridazine (phenothiazines)

-little effect on negative symptoms,EPS, tardive dyskinesia

thiothixene, loxapine (low t1/2), haloperidol

SE: chlor- sedation, orthostasis, weight gain, antichol

fluphen/halo- more EPS than chlor

perphenazine, loxapine- less SE

all cause sexual dysf, hyperpro, tardive, NMS

tricyclic, 

agranulocytosis, d-d seizures, weight gain, gi hypermot, mycard

dibenzipenes

no agranulocytosis

weight gain, somnolence dizziniess, olanzapine more likely to have 1st gen SE

quetiapine- low t1/2

positive symptoms, modest negative

risp: orhtostasis, hyperprolac, d-d EPS

zipraz: somnolence, qt prolong

paliperadone: risperidone's active metabolite

partial d2/3 agonist, seritonin 1a agonist, 2a antagonist

 not as effective (because of 1a agonism)

(atypical)

nonselective

tranylcypromine

phenelzine

depression

tyramine -->hypertensive crisis

MOA SE: serotonin, NE, DA, Hist, a1, antichol

clomipramine- most SRI

desipramine- least anti-chol

imipramine- prodrug of desip

amitriptyline(pro), nortriptyline(product)

block NE and 5-HT reuptake

SE: block at: muscarinics, a-adrenergics, dopamine, histamine, Na channels (QTc)

->blurred vision, constipation, tremor, sedation,arrythmias, seizure (gaba block)

antidote: sodium bicarb

cyclobenzaprine- tricyclic muscle relaxant

fluoxetine, paroxetine, sertraline, excitalopram, citalopram

safer in OD than tricyclics

more n/v and sexual se

flu/par: p450 inh

cit: QTc

par: birth defects

SSRI+MAOI-->serotonin syndrome

duloxetine, venlafaxine, milnacipran

SE: hypertension, urinary retention, liver dz in alc with duloxetine

bupropion: NDRI (smoking cessation)

vilazodone: SPARI (better sex, worse GI)

mirtazapine: NASA (block a2, block HT2,3 allowing 1, antihistamine sedation, weight gain)

2a antagonists that inhibit reuptake (SARI)- trazodone, marked antihist->sedation

nefazodone-SNDRI with 2a antagonism, hepatotox

body water distribution

depletes ip3 (especially in a-adrenergic and muscarinic-cholinergic) maybe preference for active circuits

se: weight gain, drowsiness, polydipsia/uria

low margin of safety- od->n/v

gamma2 subunit of GABAa

diazepam, chlorodiazepoxide, lorazepam, flurazepam,

short t1/2: alprazolam, midazolam

others: clonazepam, flunitrazepam (roofie)

hypnotics: flurazepam, temazepam, triazolam

zolpidem, eszopiclone, zaleplon

short half life

thipental - fast-on/off

phenobarbital - t1/2 4-5 days (some anti-convulsant)

releives anxiety without sedation or other effects

agonist at seritonin 1a receptors?, histamine antagonist?

methacholine, pilocarpine, carbachol

indirect: echothiophate iodide

effect: constriction/increased of vitreous humor

atropine, scopolamine, homatropine, cyclopentolate, tropicamide

effect: dilation, ciliary body paralysis

eye exams and improve comfort in inflammation

nicotinic agonist at nmj

used to diagnose myasthenia gravis

dipivefrin, bromondine tartrate (alpha 2), apraclonidine (alpha)

pupil dilation, reduces intraocular pressure

cocaine, prevents NE reuptake, hydroxyamphetamine (releases NE)

dapiprazole: reverses tropicamide and phenylephrine

tomolol, levobunol, metipranolol, carteolol (general)

betaxolol (beta 1 specific)

latanoprost- stored in fridge, most used

bimatroprost, travoprost (african americans), unoprostone isopryl

increase unveoscleral outflow tihout effect on auious or trabecular outflow

miosis, convulsions, resp depression, antitussive, n/v, constipation, urinary retention, vasodilation, urticaria

glucuronidation in liver-->kidney excretion

m-6 morphine- active metabolite, m-3 not

codeine- 2d6 p450

tramadol- synthetic codeine, inhbits 5-HT and NE uptake, less constipating

normepiridine- toxicity-->mental status changes

propoxyphene- weak, norpropoxyphene is toxic

potent selective NMDA inhibitor (like n2o)

phencyclidine

norketamine is less active (p450)

analgesia, unconciousness, amnesia

nystagmus, lacrimation, salivation, incr musc tone

NOT in CAD, but good for hypovolemia

iso- most resistant to breakdown "mainstay 1.17%MAC

des, sevo- less soluble-->faster induction and emergence

6.6 and 1.8, sevo-possibly nephrotoic with co2, CO forming-> fires

d-d increase in cerebral blood flow/ICP--->blunted by deliberate hyperventilation and hypocapnia

also d-d decrease in SVR and BP

sympathetic organ blood distribution

d-d decrease in TV and ventilatory response

direct SkM relaxants

MH if susceptible

gabaA agonist, NMDA antagonist, a2 activity

rapid on/off

liver->kidney

anti-emetic  no MH

syndrome (with glucocort/catechol): acidosis, myocard failure, rhabdo, hyperK, renal fail

barbiturate---produce unconsciousness

rapid onset short duration

 no MH

imidazole

propylene glycol solvent

rapid on/off

subcortical disinhibition->myoclonus

n/v

inhibits cortisol synth, used in those with low cardiac reserve

gabaA agonist

a2 agonist, sedation in icu

awake craniotomies, awake intubation, narcotic withdrawal and detox

depolarizing nmj blocker

cardiac dysrhythm, hyperK, incr intraoc, intracran, intragastric pressures

anti-cholinesterases

ed: fastest, shortest

neo: more complete, most used

pyrido: longer lasting

requires glycopyrrolate(preferred) or atropine

pancuronium- 60-90min, vagolytic, urine unchanged

verocuronium: intermed, no circ effects, liver/kidn 

rocuronium: fast onset, 35 min duration, bile excr, no circ effects

sugammadex: selective, traps rocuronium

atracurium and cisatracurium

spontaneous degredation- adv in liver.renal dysf

histamine release with atra?

3-5 onset/20-35 min duration

Na channel inhibitors (stabilize inactive state): carbamazepine, oxcarbamazepine, lamotrigine, phenytoin

induce enzymes->contraceptive failure

t: sedation, ataxia, diplopia, rash, myelosuppression,

complex partial more than general, bipolar, neuropathic

preferred to phenobarb, valproate, phenytoin

due to less SE

needs extended release forms

primary, secondary, partial, absence

use in kids

not in myoclonic

bipolar, neuropathic pain

competes for excretion with valproate

--->synergy

broad spectrum, bipolar, migraine

gaba and na channels?

sedation, tremor, weight gain, birth defect

gaba analogs, inhibits l-type Ca currents

adjunct for partial

more for neuropathic pain

gabapentin-AA transporter in gut, t1/2 40-60,

ethosuxamide - t type Ca channel blocker, absence

AMPA, Kainate Ca channel blocker

some Na and gaba

partial, secondary and primary

migraine prophy

carbonic anhydrase inh

kidney stones

partial and secondary, some primary

binds synaptic vessel protein 2--> less transmitter release

well tolerated

sedation, irritability, thrombocytopenia

potent

partial with or without secondary

blocks NMDA

aplastic anemia, acute hepatic failure

refractory use only

vasoconstriction?

reduction in trigeminovascular response

serotonin agonists

se:n/v, parasthesia, chest pain, 

5-HT 1B-D agonists

80% effective SQ (sumatriptan)

helps with n/v, phono/photo

avoid in CV dz, prinzmetal

droperidol in n/v with headache

amitriptyline, nortriptyline, protriptyline

fluoxetine, paroxetine, sertraline

timolol, propranolol, nadolol, atenolol

verapamil- with disabling aura

valproate (needs base blood work), topiramate 

lithium in cluster

inhibits t-cell activation, shift to th2, inh lymph prolif, gamma antagonism, antiviral, inh lymp->cns

1a-Avonex low dose and Rebif high dose

1b-Betaseron and Extavia (high dose) better than avonex

se: anemia, flu-like, injection site, avonex has less

mbp-like causes apoptosis of t cells

shifts to th2

regulatory t cells->anergy

binds alpha-4 subunit of integrins and restricts BBB crossing

PML side effect

first oral-approved

prodrug, similarity to S1P

leads to sequestration of circulating lymphocytes

secondary progressive MS

synthetic anthracenedione

broad immunosuppressant

cardiac SE profile

acute leukemia

AchE inhibitors

riva: BuchE inh

gala: allosteric modulator of nicotinic

SE: sleep disturbances, n/v

ritalin

all stimulants block reuptake of NE and DA

narcolepsy, sleep apnea, shift work

agonize histamine and orexin

guanfacine and clonidine agonise a2

atomoxetine- block NE reuptake in cortex only

APAP antidote

prothrombin time, increased creatinine, encephalopathy, acidosis, VII/X ratio >30, rising lactate, rising phosphate