Shelf: Lippincot's CNS
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- amantadine
-
tx Parkinson's
antiviral drug for influenza -> who would have thought?
enhances synthesis, release and re-uptake of DA unless DA release is already at a maximum
less efficacious than levodopa
tolerance develops faster
good for rigidity and bradykinesia -
antimuscarinic agents
benztropine
trihexyphenidyl
biperiden -
tx Parkinson's
blocking cholinergic transmission -> effects similar to augmentation of DA transmission (creates an imbalance in DA/ACh ratio) - bromocriptine
-
tx Parkinson's
DA agonist
used w/ levodopa
must be built up slowly over 2-3 mo, serious side effects include:
hallucinations, confusion, delirium, nausea, orthostatic hypotension, worsens MI and ulcers - carbidopa
-
tx Parkinson's
DOPA decarboxylase inhibitor that doesn't cross BBB
it increases the action of levodopa and diminishes its side effects - deprenyl (selegiline)
-
tx Parkinson's
inhibits MAOB -> dec metabolism of DA -> inc levels
may prolong the period before severe symptoms set in - levodopa
-
tx Parkinson's
DA precursor that enters CNS and is decarboxylated to DA
also greatly decarboxylated in periphery unless co-administered w/ carbidopa
side effects -> nausea, vomiting, arrhythmias, hypotension - pramipexole
-
tx Parkinson's
non-ergot DA agonists
alleviate the motor deficitis in levodopa-naive patients and patients taking levodopa
less side effects - ropinirole
-
tx Parkinson's
non-ergot DA agonist
alleviate the motor deficits in levodopa-naive patients and patietns taking levodopa
less side effects - tolcapone
-
tx Parkinson's
nitrocatechol derivative-
selectively and reversibly inhibits both peripheral and central COMT
reduces the on-off phenomenon - excitatory pathways
-
excitatory neuron releases NE or ACh ->
bind to receptor on post-synaptic membrane ->
transient inc in Na permeability ->
Na influx ->
slight depolarization or EPSP - inhibitory pathways
-
inhibitory neuron releases GABA or glycine ->
binds to receptor on post-synaptic membrane ->
transient inc in K and Cl permeability ->
Cl influx and K efflux ->
slight hyperpolarization or IPSP - pyridoxine
-
B6
increases peripheral breakdown of levodopa - MAOIs and levodopa
- hypertensive crisis
- levodopa and glaucoma
- can make glaucoma worse
- levodopa and anti-psychotics
- have opposing actions -> don't give them to the same patient
- aprazolam
-
benzo anxiolytic-
when GABA binds its receptor -> opens Cl channel -> Cl influx -> hyperpolarization
the benzos bind a separate receptor that enhances GABA's affinity for its receptor - chlordiazepoxide
-
benzo anxiolytic
tx alcohol withdrawal
long acting - clonazepam
-
anti-epileptic
myoclonic - clorazepate
-
benzo anxiolytic
tx alcohol withdrawal
long acting - diazepam
-
anti-epileptic
status epilepticus - lorazepam
- benzo anxiolytic
- quazepam
-
benzo hypnotic
long acting - midazolam
- benzo hypnotic
- estazolam
- benzo hypnotic
- flurazopam
-
benzo hypnotic
tx sleep disorder- long acting - temazepam
-
benzo hypnotic
tx sleep disorder- int acting- inability to stay asleep - triazolam
-
benzo hypnotic
tx sleep disorder- short acting- difficulty in getting to sleep - buspirone
-
anxiolytic
tx GAD
affinity for D2 and serotonin receptors
no anticonvulsant or muscle relaxant properties - hydroxyzine
-
anxiolytic
anti-histamine w/ antiemetic activity
great for drug addicts and for sedation before dental work or surgery - zolpidem
-
anxiolytic
acts on bezo receptors
- has no muscle relaxing or anticonvulsant properties
side effects include nightmares - flumazenil
-
benzo antagonist
GABA receptor antagonist
admin may precipitate withdrawal in dependent patients - amobarbital
-
barbituate
short acting - phenobarital
-
barbituate
long term management of tonic-clonic seizures
long acting - pentobarbital
-
barbituate
short acting - secobarbital
-
barbituate
short acting - thiopental
-
barbituate
short acting- good to induce anesthesia -
antihistamines
diphenhydramine
doxylamine -
sedatives
good for very mild insomnia - chloral hydrate
-
sedative
derivative of acetaldehyde -> converted to trichloroethanol
induces sleep in 30 minutes and lasts about 6 hours - ethanol
- sedative
- disulfiram
-
inhibit aldehyde dehydrogenase
(antabuse) - amphetamine
-
psychomotor stimulant
riases intracellular stores of catecholamines and blocks MAO
major actions due to release of DA, not NE
tx ADD
overdose tx w/ chlorpromazine - caffeine
-
psychomotor stimulant
a methylxanthine - cocaine
-
psychomotor stimulant
prolongation of DA action produces intense euphoria
used therapeutically as topical anesthetic (blocks voltage gated Na channels)
vasoconstriction causes necrosis and perforation of nasal septum - methylphenidate
-
psychomotor stimulant
tx narcolepsy (an amphetamine) - nicotine
-
psychomotor stimulant
2nd to caffeine as most widely used stimulant
2nd to alcohol as most widely abused drug - theobromine
-
psychomotor stimulant
a methylxanthine found in coco - theophylline
-
psychomotor stimulant
a methylxanthine found in tea - Lysergic acid diethylamide (LSD)
-
psychotomimetic
acts at presynaptic 5-HT receptors
haloperidol can shorten its action - phencyclidine (PCP)
-
psychotomimetic
inhibits reuptake of DA, serotonin and NE
also anticholinergic (yet it causes salivation)
an analog of ketamine
produces dissociative anesthesia (insensitivity to pain, without loss of consciousness) and analgesia -
tetrahydrocannabinol (THC)
dronabinol -
psychotomimetic
high dose may lead to psychosis
tx severe emesis in cancer patients -
anticholinergics
scopolamine -
preanesthetic medication
prevent bradycardia and secretion of fluids into respiratory tract -
antiemetics
dropendol - preanesthetic medication
- antihistamines
-
preanesthetic medication
prevention of allergic reactions (diphenhydramine)
or to decrease gastric acidity (cimetidine) -
barbituates
phenobarbital -
preanesthetic medication
for sedation
thiopental (fast acting short lived barbituate) helps avoid stage II of anesthesia -
benzodiazepines
diazepam -
preanesthetic medication
relieves anxiety and facilitates amnesia -
opiods
fentanyl -
preanesthetic medication
for analgesia - atracurium
- mm relaxant
- succinylcholine
- mm relaxant
- vecuronium
- mm relaxant
- enflurane
- inhaled anesthetic
- halothane
-
inhaled anesthetic
best agent in pediatrics, bronchial sm mm relaxation good for patients w/ asthma
reduces hepatic and renal blood flow, lowers BP, sensitizes myocardium to actions of catecholamines, hepatic toxicity and arrhythmias - isoflurane
-
inhaled anesthetic
good mm relaxant, rapid recovery, stability of CO, does no raise intracranial pressure, no sensitization of myocardium - methoxyflurone
- inhaled anesthetic
- nitrous oxide
-
inhaled anesthetic
good analgesia, rapid onset/recovery, safe, nonirritating
incomplete anesthesia, no mm relaxation - sevoflurane
- inhaled anesthetic
- amitriptyline
- TCA
- amoxapine
- TCA- 2nd gen
- desipramine
- TCA
- doxepine
- TCA
- imipramine
- TCA
- maprotiline
- TCA- 2nd gen
- nortriptyline
- TCA
- protriptyline
- TCA
- trimipramine
- TCA
- fluoxetine
- SSRI
- fluvoxamine
- SSRI
- nefazodone
- SSRI
- paroxetine
- SSRI
- sertraline
- SSRI
- trazodone
- SSRI
- venlafaxine
- SSRI
- isocarboxazid
- MAOI
- phenelzine
- MAOI
- tranylcypromine
- MAOI
- lithium salts
- drugs used to treat mania
- chlorpromazine
-
phenothiazine (neuroleptic)<br />lots of adverse effects
tx hiccups - fluphenazine
-
phenothiazine (neuroleptic)
available as slow release - prochlorperazine
- phenothiazine (neuroleptic)
- promethazine
- phenothiazine (neuroleptic)
- thioridazine
-
phenothiazine (neuroleptic)<br />strong muscarinic antagonist
good anti-emetic - risperidone
- benzisoxazole (neuroleptic)
- clozapine
-
dibenzodiazepine (neuroleptic)
agranulocytosis - haloperidol
-
butyrophernone (neuroleptic)
little adrenergic or muscarinic activity; available as slow release - thiothixene
- thioxanthene (neuroleptic)
- fentanyl
-
opiod agonist
80x analgesic potential of morphine, short duration of action
(anesthesiologists get addicted to this stuff) - heroin
- opiod agonist
- meperidine
-
opiod agonist
tx acute pain - methadone
- opiod agonist
- morphine
-
opiod agonist<br /><br />miosis via Edinger-Westphal<br />emesis via trigger zone<br /><br />not for asthmatics (releases histamine)
morphine-6-glucoronide = potent
morphine-3-glucoronide = not potent - sufentanil
-
opiod agonist
even more potent than fentanyl - codeine
-
opiod agonist (moderate)
(** in most new cough medicines, codeine has been replaced w/ detromethorphan) - propoxyphene
-
opiod agonist (moderate)
dextro-isomer -> for pain
levo isomer -> antitussive
(VERY bad when taken w/ alcohol and even naloxone can't overcome the cardiotoxicity) - buprenorphine
- mixed opiod agonist/antagonist
- pentazocine
-
mixed opiod agonist/antagonist
can induce withdrawal in morphine addicts - naloxone
-
opiod antagonist
tx overdose (works within 30 seconds! to relieve respiratory depression and coma)
may produce withdrawal sx in morphine or heroin abusers - naltrexone
-
opiod antagonist
blocks the effect of injected heroin for up to 48 hours
-> used to tx opiate-dependence - carbamazepine
-
anti-epileptic<br /><br />partial simple<br />partial complex<br />tonic clonic
can cause bone marrow suppression - corazepate
- anti-epileptic
- ethosuximide
-
anti-epileptic<br /><br />absence
can cause Stevens-Johnson - gabapentin
- anti-epileptic
- lamotrigine
-
anti-epileptic (new)
inhibits glutamate and aspartate release
bloks Na channels - phenobarbital
-
anti-epileptic<br /><br />febrile seizures in children
causes sedation - phenytoin
-
anti-epileptic
partial simple
partial complex
grand mal
status epilepticus - primidone
-
anti-epileptic
phenobarbital is its metabolite - tiagabine
- anti-epileptic
- topiramate
- anti-epileptic
- valproic acid
-
anti-epileptic
myoclonic - viagabatrin
- anti-epileptic