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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

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

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