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CNS
1. MoA 2. Use 3. Side Effects, 4. Interactions
79
Pharmacology
Professional
04/14/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
midazolam
Definition
1. benzo; facilitate GABA via ↑ FREquency of Cl-Ch opening {Short acting, a "TOM thumb"}
2. anesthesia inducing
3. Dependence/Withdrawal; with ETOH = additive sedation effects
Term
flurazepam
Definition
1. benzo; facilitate GABA via ↑ FREquency of Cl-Ch opening
2. insomnia
3. Dependence/Withdrawal; with ETOH = additive sedation effects
Term
triazolam
Definition
1. benzo; facilitate GABA via ↑ FREquency of Cl-Ch opening {Short acting, a "TOM thumb"}
2. insomnia
3. Dependence/Withdrawal; with ETOH = additive sedation effects
Term
alprazolam
Definition
1. benzo; facilitate GABA via ↑ FREquency of Cl-Ch opening
2. anxiety
3. Dependence/Withdrawal; with ETOH = additive sedation effects
Term
lorazepam
Definition
1. benzo; facilitate GABA via ↑ FREquency of Cl-Ch opening
2. anxiety; Status Epilepticus, generalized seizures
3. Dependence/Withdrawal; with ETOH = additive sedation effects
Term
oxazepam
Definition
1. benzo; facilitate GABA via ↑ FREquency of Cl-Ch opening {Short acting, a "TOM thumb"}
2. anxiety
3. Dependence/Withdrawal; with ETOH = additive sedation effects
Term
temazepam
Definition
1. benzo; facilitate GABA via ↑ FREquency of Cl-Ch opening
2. insomnia
3. Dependence/Withdrawal; with ETOH = additive sedation effects
Term
clonazepam
Definition
1. benzo; facilitate GABA via ↑ FREquency of Cl-Ch opening
2. anxiety
3. Dependence/Withdrawal; with ETOH = additive sedation effects
Term
diazepam
Definition
1. benzo; facilitate GABA via ↑ FREquency of Cl-Ch opening
2. anxiety, status epilepticus, generalized seizures
3. Dependence/Withdrawal; with ETOH = additive sedation effects
Term
flumazenil
Definition
1. benzo GABA competitive antagonist
2. to tx benzo toxicity/overdose
3. can cause Benzo withdrawl sydrome; t1/2life = 30-60 mins
Term
buspirone
Definition
1. partial 5-HT1 & 5-HT2 receptor agonist
2. Long term anxiolytic (but long latency until effective)
3. agitation; Serotonin Syndrome
Term
eszopiclone
Definition
1. non-benzo GABA receptor agonist
2. insomnia
3. anterograde amnesia, odd sleep behaviors
Term
zaleplon
Definition
1. non-benzo GABA receptor agonist
2. insomnia
3. anterograde amnesia, odd sleep behaviors
Term
zolpidem
Definition
1. non-benzo GABA receptor agonist
2. insomnia
3. anterograde amnesia, odd sleep behaviors
Term
remelteon
Definition
1. melatonin receptor agonist
2. insomnia - aids in ONSET of sleep
3. elevate PRL levels; CONTRA to depression pts
Term
carbamazepine
Definition
1. stabilize inactive Na-Ch; inhibit Ca-Ch; Enzyme INDUCER
2. localization epilepsy; Trigeminal Neuralgia 1st line tx; Manic bipolar
3. epoxide metabolite = headaches, GI = limits rapid titration
Term
oxcarbazepine
Definition
1. stabilize inactive Na-Ch; inhibit Ca-Ch; Enzyme INDUCER
2. localization epilepsy
Term
ethosuximide
Definition
1. inhibit T-type Ca-Ch
2. Absence only!
3. rash, SJS
Term
gabapentin
Definition
1. inhibit Ca-Ch; enhance GABA synthesis but NO ACTION on GABA-R
2. Partial/T-C Seizures; post-herpetic neuralgia; bipolar; periph neuropathy
3. nausea, somnolence, lightheaded
4. minimal interactions, excreted in urine
Term
pregabalin
Definition
1. inhibit Ca-Ch; enhance GABA transport but NO ACTION on GABA-R
2. localization; neuropathic pain
3. slightly more potent = slightly more effects
4. minimal interactions, excreted in urine
Term
lacosamide
Definition
1. binds CRMP cell proteins needed for ion trafficking and neuronal sprouting; stabilize inactive Na-Ch
2. combo tx for localization
3. prolong PR = 1st degree AV block
Term
lamotrigine
Definition
1. stabilize inactive Na-Ch (inhibit Ca-Ch inhibits glutamate release)
2. lennox-gastaut generalized
3. Severe, life-threatening RASH
4. t1/2 signif increased with Valproate, shortened with other AEDs
Term
levetiracetam
Definition
1. inhibit Ca-Ch; interacts with unique synaptic vesicle proteins
2. localization & some generalized
3. behavioural probs
4. plays well with other drugs!
Term
phenobarbital
Definition
1. prolongs DURATION of time GABA is open (inhibit Ca-Ch; inhibit NMDA glutamate) LONG t1/2 = 60-110 hrs!
2. sedative for anxiety, seizure, insomnia; epilepsy - 1st line in pregnancy and kids
3. rash, depression, behavioural
4. Enzyme INDUCER
Term
phenytoin
Definition
1. stabilize inactive Na-Ch;
2. status epilepticus & T-C seizures
3. nystagmus, ataxia, gingival hyperplasia; ↓folate absorpt = megaloblast-anemia; TERATOGEN
4. Enzyme INDUCER and ZERO ORDER kinetics
Term
tiagabine
Definition
1. inhibit GABA reuptake
2. localization
Term
topiramate
Definition
1. potentiate GABA at own unique site; stabilize inactive Na-Ch; inhibit Ca-Ch; inhibit glutamate
2. localized, generalized; Migraines
3. risk for cleft palate defects; psychomotor slowing, parasthesias, kidney stones; WEIGHT LOSS
Term
zonisamide
Definition
1. potentiate GABA at own unique site; stabilize inactive Na-Ch; inhibit Ca-Ch; inhibit glutamate
2. localized, generalized; Migraines
3. risk for cleft palate defects; psychomotor slowing, parasthesias, kidney stones; WEIGHT LOSS
Term
valproate
Definition
1. promotes GABA synthesis, inhibitis GABA metobo; stabilize inactive Na-Ch; inhibit Ca-Ch
2. localized, generalized, ABSCENCE, Migraines
3. Weight GAIN, tremor, hair loss; risk for NTDs
4. ENZYME INHIBITOR (esp lamotrigine)
Term
chlorpromazine
Definition
1. Low Potency Typical Antipsychotic; blocks dopamine receptors
2. Psychosis/Schizophrenia
3. Malignant Neuroleptic Syndrome, EPS, Tardive Dyskinesia Anticholinergic & adrenergic effects, Endocrine disturbances
{NMS - tx with dantrolene or bromocriptine
Term
thioridazine
Definition
1. Low Potency Typical Antipsychotic; blocks dopamine receptors
2. Psychosis/Schizophrenia
3. Malignant Neuroleptic Syndrome, EPS, Tardive Dyskinesia Anticholinergic & adrenergic effects, Endocrine disturbances
{NMS - tx with dantrolene or bromocriptine
Term
fluphenazine
Definition
1. HIGH Potency Typical Antipsychotic; blocks dopamine receptors
2. Psychosis/Schizophrenia
3. Malignant Neuroleptic Syndrome, EPS, Tardive Dyskinesia Anticholinergic & adrenergic effects, Endocrine disturbances
{NMS - tx with dantrolene or bromocriptine
Term
haloperidol
Definition
1. HIGH Potency Typical Antipsychotic; blocks dopamine receptors
2. Psychosis/Schizophrenia
3. Malignant Neuroleptic Syndrome, EPS, Tardive Dyskinesia Anticholinergic & adrenergic effects, Endocrine disturbances
{NMS - tx with dantrolene or bromocriptine
Term
clozapine
Definition
1. Atypical Antipsychotic(spectrum of actions; Strong 5HT2 antag and NO EPS
2. parkinson patient
3. Severe Agranulocytosis
Term
aripiprazole
Definition
1. Atypical Antipsychotic(spectrum of actions; Partial Agonist at 5HT1 and D2, antag at 5HT2
2. milder antichol. - better if you want less sedation
Term
olanzapine
Definition
1. Atypical Antipsychotic(spectrum of actions; 5HT2 > D
3. Weight Gain, can induce DM and hyperglycemia; more antichol.
Term
quetiapine
Definition
1. Atypical Antipsychotic(spectrum of actions; potent a-adrenergic antagonism
3. ABUSE potential, orthostatic hypertension, tachycardia, weight gain
Term
risperidone
Definition
1. Atypical Antipsychotic(spectrum of actions; STRONG 5HT2 and D2 action
3. More likely to have EPS and ↑ PRL!; prolongs QT, weight gain
Term
ziprasidone
Definition
1. Atypical Antipsychotic(spectrum of actions; also an SSRI!
2. depression patients with psychosis
3. Prolong QT, but NO WEIGHT GAIN!
Term
trihexylphenidyl
Definition
1. Muscarinic anticholinergic
2. Parkinsons, esp early on, helps with tremor and rigidity; Dystonia
3. Atropine-like (dry mouth,
Term
benztropine
Definition
1. Muscarinic anticholinergic
2. Parkinsons, esp early on, helps with tremor and rigidity
3. Atropine-like (dry mouth,
Term
amatadine
Definition
1. make use of actions: antimuscarinic, enhance dopamine release, block dopamine reuptake, glutamate receptor antagonism
2. Early IPD, dyskinesias in late IPD
3. Livedo reticularis!
Term
selegiline
Definition
1. selective MAOI TypeB
2. IPD
3. amphetamine-like metabolite (insomnia), confusion
4. Selective so won't cause Wine&Cheese rxn
Term
rasagiline
Definition
1. IRREVERSIBLE selective MAOI TypeB
2. IPD
3. unknown
Term
bromocriptine
Definition
1. Dopamine Agonist Ergot Derivative
2. Now 1st Line in Parkinsons; to tx Neuroleptic Malignant Syndrome
3. SLEEP ATTACKS, Retroperitoneal Fibrosis, Raynauds, hallucinations, dyskinesias, GI distress, hypotension
Term
pramipexole
Definition
1. Dopamine Agonist, Non-Ergot
2. Now 1st Line in Parkinsons
3. like bromo + brings out compulsive behaviours!
Term
ropinirole
Definition
1. Dopamine Agonist, Non-Ergot
2. Now 1st Line in Parkinsons
3. like bromo + brings out compulsive behaviours!
Term
carbidopa/levodopa
Definition
1. Dopamine Agonist + carbidopa blocks peripheral dopa-decarboxylase
2. Mainstay IPD tx but pt must still have nigra cells left, shortest t1/2
3. GI, Hypotension, hallucinations, dyskinesias, motor flux
4. High PRO diet interferes- a saturable AA transportor needed for Levo absorption
Term
entacapone
Definition
1. COMT inhibitor peripherally
2. with levodopa to incr t1/2 by 50%
3. turns urine orange! + effects of incr dopamine
Term
apomorphine
Definition
1. non-narcotic morphine derivative that's a dopamine agonist
2. Rescue tx given Subcu injec.
3. Severe GI rxn (give anti-emetics)
Term
propranolol
Definition
betablocker helpful in Essential tremors
Term
primidone
Definition
barbiturate helpful in essential tremors
Term
gabapentin
Definition
GABA agonist helpful in essential tremors
Term
alprazolam
Definition
1. benzodiazepine
2. essential tremors, dystonia
Term
clonazepam
Definition
benzodiazepine
2. essential tremors, dystonia
Term
baclofen
Definition
1. GABA-B agonist
2. dystonia
3. Sedation; rapid dis-use can cause seizures or acute psychosis
Term
botulinum toxin
Definition
1. BotoxA binds SNAP-25, BotoxB bind synaptobrevin
2. dystonia
3. muscle weakness
Term
tranylcypromine
Definition
1. Irreversible MAOI
2. depression
3. Wine&Cheese, Serotonin Sydrome (pupils dilate, hypertherm, hyperReflex), Risk of Suicide
4. Tons, its metabolized via CYPs
Term
amitriptyline
Definition
1. Tertiary TCA; blocks 5HT reuptake > NE uptake
2. Depression, Fibromyalgia & Insomnnia
3. Anticholinergic (Urinary Retention); QT intv, Suicide Risk, weight gain
Term
imiprimine
Definition
1. Tertiary TCA; blocks 5HT reuptake > NE uptake
2. Depression, kids with ENURESIS
3. Anticholinergic (Urinary Retention); QT intv, Suicide Risk, weight gain
Term
nortriptyline
Definition
1. Secondary TCA; blocks NE reuptake > 5HT uptake 2. Depression, Fibromyalgia 3. Anticholinergic (Urinary Retention); QT intv, Suicide Risk, weight gain
Term
desiprimine
Definition
1. Secondary TCA; blocks NE reuptake > 5HT uptake
2. Depression
3. Anticholinergic (Urinary Retention); QT intv, Suicide Risk, weight gain
Term
fluoxetine
Definition
1. SSRI (also inhibit CYPs)
2. also for Premenstrual syndrome
3. Can Precipitate a bipolar's MANIC EPISDOE, Suicide Risk, Serotonin Syndrome
Term
paroxetine
Definition
1. SSRI (also inhibit CYPs)
2. also for Premenstrual syndrome
3. Can Precipitate a bipolar's MANIC EPISDOE, Suicide Risk, Serotonin Syndrome
Term
escitalopram
Definition
1. SSRI
2. also for Premenstrual syndrome
3. Can Precipitate a bipolar's MANIC EPISDOE, Suicide Risk, Serotonin Syndrome
Term
sertraline
Definition
1. SSRI
2. also for Premenstrual syndrome
3. Can Precipitate a bipolar's MANIC EPISDOE, Suicide Risk, Serotonin Syndrome
Term
venlafaxine
Definition
1. SNRI; blocks 5HT > NE
2. also for anxiety disorders
3. Suicide risk, serotonin syndrome; dry mouth, insomnia, sex-dysfx
Term
duloxetine
Definition
1. SNRI; blocks 5HT ~ NE
2. also for fibromyalgia & diabetic neuropathic pain
3. Suicide risk, serotonin syndrome; dry mouth, insomnia, sex-dysfx
Term
bupropion
Definition
1. Atypical; seems to block reuptake of NE and dopamine
2. decr nicotine cravings + minimal sexual side effects!
3. lowers seizure threshold, Suicide Risk
Term
mirtazapine
Definition
1. Atypical; blocks a2-adrenergics = incr NE transmission, 5HT2-3 antagonist, and antihistamine action
2. anti-emesis, anti-pruitis
3. increased appetite (good for some elderly)
Term
trazodone
Definition
1. atypical; weakly inhibit 5HT uptake, antag to 5HT1 presynaptic autoreceptors, antag to postsynaptic 5HT2 receptors
2. insomnia! (sedating side effect)
3. orthostatic hypotension; metabolized in 2 phases
Term
lithium carbonate
Definition
1. element; seems to affect phospholipids- PIP2 recycling = impedes signals from NE, Ach, and serotonin
(no effect on normal ppl)
2. Bipolar
3. TERATOGEN! DI (blocks ADH receptors), convulsions, tremors, arrhythmia, leukocytosis
4. High Na-intake promotes excretion, Thiazide diuretics inhibit excretion=potential for toxicity
Term
valproate
Definition
1. Antiepileptic Drug - "Mood Stabilizer"
2. can be used in bipolar
Term
lamotrigine
Definition
1. Antiepileptic Drug - "Mood Stabilizer"
2. can be used in bipolar
Term
carbamazepine
Definition
1. Antiepileptic Drug - "Mood Stabilizer"
2. can be used in bipolar
Term
paliperidone
Definition
1. Extended release for of Risperidone's major metabolite! (an atypical antipsychotic)
2. atypical antipsychotics particularly helpful in bipolar!
Term
sumatriptan
Definition

1. 5-HT1 receptor agonist likely mediates thru vasoconstriction and sensory neuron presynaptic inhibition

2. acute migraine (not prophylaxis)

3. iono- and chrono-tropic heart effects, nausea, dizzy, weak, contra to vasoconstrictive problems, MAOIs

Term
ergotamine
Definition

1. agonist OR antag to 5-HT1-R.

2. tx for migraine due to the agonist effects

3. CNS actions of nausea, vasoconstriction, leg weakness, muscle pain; Contra to Pregnancy bc they can stimulate the uterus and constrict uterine blood flow; fibrosis with long term tx

Term
methysergide
Definition

1. agonist OR antag to 5-HT1-R.

2. prophylaxis tx for migraine due to the ANTAGONIST effects

3. CNS actions of nausea, vasoconstriction, leg weakness, muscle pain; Contra to Pregnancy; fibrosis with long term tx

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