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106 terms

Neuro Rx+

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alpha agonists
Epi, brimonidine

glaucoma --> decrease aqueous humor synth
Epinephrine
alpha agonist, glaucoma

ADR: mydriasis, stinging, not for use in closed-angle glaucoma
beta blockers - glaucoma
Timolol, betaxolol, carteolol

Decrease aqueous humor secretion
Acetazolamide
diurectic, glaucoma

inhib carbonic anhydrase --> decrease bicarb --> decrease aquesous humor secretion
cholinomimetics - glaucoma
Pilocarpine, carbachol, physostigmine, echothiophate

increase outflow of aqueous humor, contract ciliary muscle, open trabecular meshwork

ADR: miosis, cyclospasm
Pilocarpine
direct cholinomimetic

glaucoma emergencies
Latanoprost
prostaglandin, glaucoma

increase outflow of aqueous humor

ADR: browning of iris
Opiates
morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan

Analgestic, IV anesthetic

agonist at opioid receptors --> open K+ and close Ca2+ channels --> decreased synaptic transmission --> inhib release of ACh, NE, 5-HT, glutamate, substance P

ADR: addiction, respiratory depression, constipation, miosis, additive CNS depression with other drugs.
Rx opioid OD
naloxone, naltrexone

opioid receptor antagonist
Dextromethorphan
opioid analgesic, cough suppression
Loperamide
opioid analgesic, rx diarrhea
L
Diphenoxylate
opioid analgesic, rx diarrhea
D
Methadone
opioid analgesic

maintenance program for addicts
Butorphanol
Partial agonist at opioid mu receptors, full agonist at kappa receptors

causes less repiratory depression than full agonists
ADR: causes withdrawal if on full opioid agonist
Tramadol
Very weak opioid agonist, also inhib 5-HT, NE reuptake

use for chronic pain

ADR: similar to opioids, decreases seizure threshold
Epilepsy drugs
phenytoin, carbamazepine, lamotrigine, gabapentin, topiramate, phenobarbital, valproic acid, ethosuximide, BZD, tiagabine, vigabatrin, levetiracetam
BZD
Diazepam, Lorazepam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide, alprazolam

Increase frequency of Cl- channel opening --> Increase GABA(A) action, decrease REM sleep

First line for acute generalize seizure rx, seizures of eclampsia, anxiety, detox (EtOH), night terrors, sleepwalking, general anesthetic, hypnotic

ADR: sedation, tolerance, dependence
Carbamazepine
Rx partial and generalized tonic-clonic seizures, trigeminal neuralgia

increase Na channel inactivation

ADR: diplopia, ataxia, blood dyscrasias, liver toxicity, teratogenesis, induces P-450, SIADH, Stevens-Johnson syndrome
Ethosuximide
Rx generalized absence seizures

blocks thalamic T-type Ca2+ channels

ADR: GI distress, fatigue, HA, uriticaria, Stevens-Johnson synd
Phenobarbital
Rx partial and generalized tonic-clonic seizures, use in pregnant/children

ADR: sedation, tolerance, dependence, P-450 inducer
Phenytoin
Rx tonic-clonic seizures, class IB antiarrhythmic

use-dependent block of Na channels --> increase refractory period --> inhib glutamate release from excitatory presynaptic neuron

ADR: nystagmus, diplopia, ataxia, gingival hyperplasia, hirsutism, teratogenesis, SLE-like syndrome, P-450 inducer
Valproic acid
Rx partia, tonic-clonic, and absence seizures, myoclonic seizures

increase Na channel inaction, increase GABA concentration

ADR: GI distress, hepatotoxicity, neural tube defects, tremor
Lamotrigine
Rx partial and tonic-clonic seizures

block V-gated Na+ channels

ADR: Stevens-Johnson syndrome
Gabapentin
Rx partial and tonic-clonic seizures, peripheral neuropathy, bipolar disorder

Inhib HVA Ca2+ channels, GABA analog

ADR: sedation, ataxia
Topiramate
Rx partial and tonic-clonic seizures

blocks Na channels, increase GABA action

ADR: sedation, mental dulling, kidney stones, weight loss
Barbiturates
Phenobarbital, pentobarbital, thiopental, secobarbital

Increase duration of Cl- channel opening --> increase GABA(A) action --> decrease neuron firing

Sedative - anxiety, seizures, insomnia
IV anesthetic

ADR: dependence, additive CNS depression with EtOH, repisratory/CV depression, P-450 induction
Thiopental
Barbiturate

Induction of anesthesia
High potency, high lipid solubility, rapid entry into brain (low blood/gas partition coefficient)
Flumazenil
Rx BZD OD

Competitive antagonist at GABA BZD receptor
Short actin BZD (tom thumb)
Triazolam, oxazepam, midazolam

highest addictive potential
Inhaled anesthetics
Halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, NO

myocardial/resp depression, N/V, increased cerebral blood flow

Transfer of anesthetic --> brain starts only after blood is fully saturated. High blood/gas partition coefficient = slow onset of action
Pure motor hemiparesis
Lacunar infarct of posterior limb of internal capsule
Pure sensory stroke
Lacunar infarct of (ventroposterolateral/ventroposteromedial) thalamus
Ataxia hemiplegia syndrome
lacunar infarct of base of the pons
Dysarthria and clumsy hand syndrome
lacunar infarc of base of pons or genu of internal capsule
hemiballismus
infarct of contralateral subthalamic nucleus
Rx myasthenia gravis
AChE inhibitors
Edrophonium
Dx cholinergic crisis

If edrophonium improves sx of MG, increase AChe dose
If edrophonium has no effect on sx of MG, decrease AChe dose
Rx status epilepticus
1. IV lorazepam (stop seizure) followed by IV phenytoin (prevent recurrence)
2. Still seizing? phenobarbital
3. Still seizing? intubate and give general anesthesia
Halothane
Inhaled anesthetic

ADR: hepatotoxicity
Enflurane
Inhaled anesthetic

ADR: proconvulsant
Methoxyflurane
Inhaled anesthetic

ADR: nephrotoxicity
nitrous oxide
inhaled anesthetics

ADR: expansion of trapped gas
Midazolam
BZD, IV anesthetic

endoscopy

ADR: severe postop respiratory depression, hypoTN, amnesia
Ketamine
Arylcyclohexylamine, IV dissociative anesthetic

PCP analog, CV stimulant

ADR: disorientation, hallucination, bad dreams. Increases cerebral blood flow
Fentanyl
Opiate, IV anesthetic

used with other CNS depressants during general anesthesia
Propofol
IV anesthetic

used for rapid anesthesia induction and short procedurs
Less postop nausea than thiopental
Potentiates GABA(A)
Ester local anesthetics
procaine, cocaine, tetracaine

binds receptors inside activated Na channels --> blocks

ADR: allergy (give amide), CNS excitation, HTN, hypoTN
Amide local anesthetics
lidocaine, mepivacaine, bupivacaine

binds receptors inside activated Na channels --> block

ADR: CNS excitation, HTN, hypoTN, CV toxicity (bupivacaine)
Depolarizing NMJ blockers
Succinylcholine

paralysis
phase 1: prolonged depolarization (no antidote)
phase 2: repolarized by blocked

ADR: hypercalcemia, hyperkalemia
Reverse NMJ block
Cholinesterase inhibitor (e.g. neostigmine)
Nondepolarizing NMJ blockers
Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium

Compete with ACh for receptors
Dantrolene
rx malignant hyperthermia and neuroleptic malignant syndrome

prevents release of Ca2+ from SR of skeletal muscle
dopamine receptor agonists
Bromocriptine (pergolide, pramipexole, ropinirole)

rx parkinson's
Amantadine
increases dopamine

rx parkinson's, influenza A, rubella

ADR: ataxia
Selegiline
selective MAO(B) inhibitor --> inhib preferential metabolism of DA over NE and 5-HT

with L-dopa to rx Parkinson's
L-dopa
(carbidopa)

crosses BBB --> converted to dopamine in CNS
rx parkinson's

ADR: arrhthmias, dyskinesia (with akinesia btwn doses)
COMT inhibitors
Entacapone, tolcapone

prevent L-dopa degradation
parkinson's
Benztropine
antimuscarinic

parkinson's, improves tremor and rigidity, but has little effect on bradykinesia

curbs excess cholinergic activity
Rx tremor
(esstential/familial)

beta-blocker
Memantine
NMDA receptor antagonist
Alzheimer's

ADR: dizziness, confusion, hallucinations
AChesterase inhibitors
donepezil, galantamine, rivastigmine
Alzheimer's

ADR: N, dizziness, insomnia
Sumatriptan
5-HT agonist --> vasoconstriction, inhib trigeminal activation and vasoactive peptide release

acute migraine, cluster headache

ADR: coronary vasospasm
Rifampin
chemoprophylaxis in close contacts of pts with Neisseria meningitis
bzd
rx EtOH withdrawal
SSRI's
rx anorexia/bulimia
BZD, buspirone, SSRIs
rx anxiety
rx ADHD
Methylphenidate (ritalin), amphetamines (dexedrine)
MAOIs
rx atypical depression
rx bipolar
mood stabilizers: Li, valproic acid, carbamazepine
SSRIs, SNRIs, TCAs
rx depression
rx depression + insomnia
mirtazapine
rx OCD
SSRIs, clomipramine
SSRIs, TCAs, BZDs
rx panic
rx schizophrenia
antipsychotics
rx tourette's
haloperidol
SSRI
rx social phobia
Methylphenidate
increase presynaptic NE relsease
ADHD
antipsychotics
haloperiodl, trifluoperazine, fluphenazine, thioridazine, chlorpromazine (haloperidol + 'azine's)
schizophrenia, psychosis, acute mania, tourette's

block D2 receptors --> increase cAMP
Antipsychotic ADR
slowly removed from body (stored in fat)
extrapyramidal system effects
endocrine effects (D2 antagonis --> hyperprolactinemia --> galactorrhea)
dry mouth, constipation
hypoTN
sedation
neuroleptic malignant syndrome (fevere, encephalopathy, vitals changes, elevated enz, rigidity)
tardive dyskinesia
Chlorpromazine
antipsychotic

ADR: corneal deposits
Thioridazine
antipsychotic

ADR: retinal deposits
atypical antipsychotics
olanzapine, clozapine, quetiapine, risperidone, aripiprazole, ziprasidone

blocks 5-HT(2), alpha, H1, and DA receptors

ADR: fewer EPS and anticholinergic side effects
Olanzapine
atypical antipsychotic
schizophrenia, OCD, anxiety disorder, depression, mania, tourette's

ADR: weight gain
Clozapine
atypical antipsychotic, schizophrenia

ADR: weight gain, agranulocytosis (weekly WBC monitoring)
Lithium
mood stabilizer
bipolar, SIADH

maybe inhib phophoinositol cascade?

ADR: tremor, sedation, edema, heart block, hypothyroidism, polyuria, teratogenesis
buspirone
5-HT(1a) receptor agonist
generalized anxiety disorders
no sedation, addiction, tolerance
TCAs
imipramine, amitriptyline, desipramine, nortriptyline, clomipramine, doxepin, amoxapine

blocks reuptake of NE and serotonin

ADR: convulsion, coma, cardiotoxicity
SSRIs
fluoxetine, paroxetine, setraline, citalopram

ADR: sexual dysfunction, serotonin sydrome
cyproheptadine
5-HT receptor antagonist

rx serotonin syndrome
SNRIs
venlafaxine, duloxetine

inhib 5-HT and NE reuptake

ADR: HTN, sedation, N
MAOIs
phenelzine, tranylcypromine, isocarboxazid, selegiline

ADR: HTN crisis with tyramine ingestion and beta-agonists
Sturge-Weber Syndrome
port-wine stains (often in V1 area), ipsilateral leptomeningeal angioms, pheo

Can --> glaucoma, seizures, hemiparesis, MR
Tuberous sclerosis
Hemartomas in CNS, skin, organs; cardiac rhabdomyomal renal angiomyolipomal subependymal giant cell astrocytoma, MR; seizuresl sebaceous adenomal shagreen patch

AD
NF-I
PNS tumor syndrome

cafe-au-lait spots, lisch nodules, neurofibromas in skin, optic gliomas, pheo

AD
NF-II
...
von Hippel-Lindoau disease
cavernous hemangioma in skin/mucosa/organs, bilatera renal cell carcinoma, hemangioblastoma in retina/brainstem/cerebellum, pheo

AD
direct cholinergic agonists (cholinomimetics)
bethanechol, carbachol, pilocarpine, methacholine

Increases ACh
Cholinesterase inhibitors
Neostigmine, pyridostigmine, edrophonium, physostigmine, echothiophate
Sx of cholinergic overstimulation (DUMBBELSS)
diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle/CNS, lacrimation, sweating, salivation

caused by cholinomimetics, cholinesterase inhibitors, or organophosphate pesticides
rx. cholinergic overstimulation
atropine (muscarinic antagonist) and pralidoxime (regenerates active cholinesterase)
muscarinic antagonists
atropine, benztropine, scopolamine, ipratropium, oxybutynin, glycopyrrolate, methscopolamine
atropine
muscarinic antagonist

dilates pupil, decreases bronchosecretions, decreases gastric acid secretion, decreases gut motility, decreases bladder urgency

ADR: alice in wonderland, acute close-angle glaucoma (elderly), urinary retention (men with BPH), hyperthermia (infants)
atropine OD
Hot as a hare (feverish)
Dry as a bone (dry skin and mouth)
Red as a beet (flushed skin)
Blind as a bat (cycloplegia from pupillary dilation)
mad as a hatter (disoriented)

also, tachycardic and constipated
Dopamine
Increased in schizophrenia
Decreased in Parkinson's and depression

made in ventral tegmentum and SNc (substantia nigra, pars compacta)

mesolimbic-mesocortical pathway --> regulates behavior (schizophrenia)
nigrostriatal --> coordinates voluntary movement (Parkinsons)
Tuberoinfundibular --> controls prolactin secretion (hyperprolactinemia)
5-HT
Decreased in anxiety and depression

made in raphe nucleus
GABA
decreased in anxity and Huntington's

made in nucleus accumbens
atrophy of caudate in Huntington's