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87 Cards in this Set
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Alprazolam XANAX
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anxiolytic BDZ, especially for panic disorder
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BDZ pharmacokinetics
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USE DEPENDENCE
lipid soluble binds plasma proteins wo interactions hepatic microsomal system wo interactions contraindicated for sleep apnea |
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TRIAZOLAM (HALCION)
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insomnia BDZ
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ESTAZOLAM (PROSOM)
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insomnia BDZ
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TEMAZEPAM (RESTORIL)
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insomnia BDZ
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CLONAZEPAM (KLONOPIN)
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anxiety BDZ
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DIAZEPAM (VALIUM)
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anxiety BDZ
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insomnia v. anxiety for BDZ
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fast acting - insomnia
slow - anxiety |
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Barbiturates general points
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not only potentiate but activate, induce hepatic microsoaml system, high toxicity, rapid tolerance
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THIOPENTAL
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barbiturate - induces anesthesia
effects terminated by re-distribution |
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METHOHEXITAL
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barbiturate - induces anesthesia
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PHENOBARBITAL
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barbiturate - anti-convulsant, especially useful for seizures in children, also used for epilepsy
elimination liver, 25% straight out kidney can cause hyperalgesia |
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BUSPIRONE
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partial 5HT Ag, for TX of GAD, LONG to work
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ZALEPLON (SONATA)
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very short t1/2 to induce sleep
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ZOLPIDEM (AMBIEN)
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acts specifically on BDZ1 to induce sleep
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PROPRANOLOL
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beta blocker, eases peripheral effects on anxiety
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FLUMAZENIL
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BDZ ANT, given for BDZ OD, can precipitate withdrawal in BDZ-dependent patients
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BDZ effect on sleep
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increase stage 2
decrease stage 3/4 (slow wave) variable effect on REM |
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contraindications for BDZ
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sleep apnea
CV? teratogenic? |
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psychosis
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set of sxs where ability to organize relaity is impaired
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catalepsy
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waxy flexibility
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brief psychotic disorder
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1 schizo episode in less than 1 month
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shizophreniform
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shizo for less than 6 months
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shizoaffective
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shizo and MDD with at least 1 episode of pure shizo
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shizophrenia (DX)
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at leasts 2: CONTINOUS FOR <6 months)
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Positive SXs of shizo
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delusions, hallucinations (usually auditory), disorganized speech, disorganized or catatonic behavior,
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negative SXs of shizo
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the As: avolition, alogia, anhedonia, asociality, flat affect
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positive or negative sxs better prognosis in schizo
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+
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comorbidity of shizo
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depression 25% SA 50% pot and EToH
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Etiology of shizo
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polygenic genetic, exposure to virus in uteor (2nd tri), excess DA - disorder of synaptic f(x) in prefrontal) - SYNAPSES NOT DELETED
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The DA tracts
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mesolimbic: VTA --> amygdala (hallucinations); Mesocortical: VTA--> olfactory bulb hippocampus and prefrontal (negative and cognitive SXs); Nigrostriatal: sub. N --> caudate/putamen (Motor SX); tuberoinfundibular arcuate n. of hypothalamus ---> med. eminence (inhibit release of prolactin, assoc. with SE of anti-pyshotics)
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CHLORPROMAZINE
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anti-psychotic worst TI, can lower seizure threshold
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THIORIDAZINE
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anti-psychotic, reduces EPS, may induce arrythmias
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FLUPHENAZINE
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anti-psychotic ok for CV pts
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THIOTHIXENE
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anti-psychotic (rarely used)
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HALOPERIDOL (HALDOL)
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anti-psychotic, best TI, can't OD, good for CV pts, most used
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None
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OLANZAPINE
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anti-psychotic(atypical) - low EPS risk
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RISPERIDONE
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anti-psychotic(atypical) low EPS risk
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CLOZAPINE
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anti-psychotic(atypical) low EPS risk, risk of AGRANULOCYTOSIS
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D2
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activating D2 is inihibitory --> inihibits AC
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Extrapyramidal Syndrome
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SE of anti-pyscho: acute block of DA --> SE of Parkinsonism, dystonia (grimacing, torticollus), akathesia(motor restlessness), neuroleptic malignant syn
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Tardive dyskinesia
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SE of anti-pyscho: chronic block of DA --> SE of Huntingtons(oral twitching, lip smacking, may be caused by DA R supersensitivty in striatum, can be irreverisble
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atypicals v. older generation
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atypical acts on 5HT, old on DA2
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neuroleptic malignnat syn
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effect of extrapyramidal syn, parkin with catatonia, hyperthermia. TX: dantroline, bromocriptine (DA Ag)
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Side effects of anti-pyschotics
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anti-cholinergic, anti-alpha adrenergic, endocrine (bc of prolactin), weight gain
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Drug interactions of anti-[yschotics
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liver metabolism, interacts with TCAs
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Kinetics and metabolism of anti-pyschotics
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t1/2>24hrs, lipophilic, repository preps available for compliance
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None
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TCA
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conduction abnormalities, induce p450, 5HT, NE>DA
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MAO
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hypertensive crisis with tyramine
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Paroxetine (Paxil)
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SSRI
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Fluoxetine PROZAC
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SSRI longer than 24 hr to stead state, 1 week
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Sertraline ZOLOFT
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SSRI longer than 24 hr to stead state, 1 week
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Escitalopram LEXAPRO
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SSRI
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Citalopram CELEXA
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SSRI
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Venlafaxine EFFEXOR
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SNRI
SE: upset stomach |
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Mirtrazapine REMERON
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SNRI
SE: upset stomach |
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Duloxetine CYMBALTA
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SNRI
peripheral neuropathy SE: upset stomach |
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Buprionion WELLBUTRIN
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atypical, no effect on 5HT, best AD for bipolar, CONTRADINDICATED in EATING DISORDERS
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Lithium
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Mood stabilizer, good for +/-Sxs of Bipolar, bad for mixed or rapid cyclers, easy to OD, exacerbated by kidney dysfunction, epstein's anaomly!
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L-Dopa
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TXs PD
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Carbidopa
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inhibits L-amino acid decarboxylase - keeps LDopa from getting digested
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Tolcapone
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inhibits COMT (PD)
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Selegeline
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inihibits MAOb
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Amantadine
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anti-viral, release DA
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Pergolide
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D1, D2 AG (PD)
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Bromocriptine
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D2 AG (PD)
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Ropinirole
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D2 Ag (PD)
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MR ANT
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promotes indirect
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Haloperidol
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Blocks D1, D2
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Phenobarbital (LUMINAL)
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Seizure type: non-specific
Very sedating, cheap, used for status epileptica to put them into coma Mechanism: • Blocks Na, Ca, Glu, GABA increased, decreased repetitive firing of high frequency neurons Kinetics: metabolized in liver, can induce enzymes |
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o Phenytoin (DILANTIN)
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Seizure type: non-specific
Mech: blocks sustained repetitive firing, prolongs inactivation of Na channels Kinetics: • Highly protein bound • Dose dependent metabolism • Induces liver, stimulates its own metabolism • Drug interactions relating to protein binding o Important to look at albumin(low makes more sensitive to drug) |
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o Carbamazapine (TEGRETOL)
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FROM BP: mania, rapid cycling, Stevens Johnson rash
Seizure type: non-specific Mech: blocks high freq, blocks Na, blocks presynaptic transmission Kinetics: • Induces hepatic enzymes • Less protein bound SE: aplastic anemia, agranulocytosis, low Na, STEVEN JOHNSON USED TO TREAT RC BP, Mixed, Mania side only |
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o Lamotrigine (LAMICTAL)
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FROM BP:
good adjunct, delays next cycle, TXs MDD Seizure type: primary generalized, partial onset, lennox gastaut WORKS ON BOTH POS AND NEG BP Mech: dec. high freq neurons, dec Glu, dec Na, Ca Kinetics: only 55% protein bound SE: Steven-Johnson, dizziness, diplopia, nausea, sleepiness, somnolence |
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o Topiramate (TOPAMAX)
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FROM BP: adjunct SE: --> weight loss!
used to tx Binge Eating Disorder USE: partial onset, PG T/C Mech: Dec firing, dec Glu, block Ca, inc GABA Kinetics: most excreted through kidney, long t1/2, doesn’t induce enzymes • IMP. Can increase metabolism of BIRTH CONTROL also used for bullimia and binge eatting disorders also used to tx bipolar as ADJUNCT for WEIGHTLOSS |
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o Levetricetam (KEPPRA)
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SE: Aggressive behavior
Use; partial onset Designer drug • Made as add-on med for seizure in children that were hard to control • Now used in a variety of different ways Mech: affects synaptic vesicle f(x) dec Glu, inc, GABA Kinet: minimal drug interactions, low protein binding |
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o Gabapentin (NEURONTIN)
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USE: partial onset
Mech: inc GABA, dec Glu Kinetics: GOOD, not metabolized, not protein bound, negligible interactions |
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o Valproic Acid (DEPAKOTE)
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FROM BP: for rapid cycling, mixed, faciliate GABA SE: weight gain, teratogenic, liver)
USE: partial onset, absence • used also for mood stabilization Mech: multiple, blocks NMDA, inc GABA, blocks Na, blocks repetitive firing loop Kinetics: • Highly protein bound, displaces phenytoin! INHIBITS METABOLISM OF OTHER DRUGS SE: (REQUIRES A LOT OF MONITORING) • Steven-Johnson, hepatotoxicity, thrombocytopenia, tremors, teratogenic(NTD) |
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o Ethosuximide (ZARONTIN)
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PRIMARY CHOICE FOR ABSENCE SEIZURES
Mech: decreased T type Ca in THALAMUS Kinetics: no protein binding, long t1/2, complete metabolism • Valproic acid decreases clearance |
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o BDZ
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Used for status epilepticus (last 20-30 min or longer or pt doesn’t wake up between seizures)
Diazepam and Lorazepam used • For status epilepticus specifically, Lorazepam acts longer than Diazepam - Rapid onset, L longer t1/2, sedating and dev tolerance |
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Methadone
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opioid, used to tx heroine addiction
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buprenorphine
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gamma part ag, lambda, kappa ant, used to tx heroine
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varenicline CHANTIX
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partial NR ag (tx. cigs)
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rimonabanat ACOMPLA
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Cannabinoid R ANT (tx all addictions?)
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naltrexone, nalmefene
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opioid ANT, decreases pleasure from drinking
SE: with opioids can cause withdrawal syn |
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disulfiram ANANTABUSE
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makes you sick with you drink - acts on ALDH enz
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acamprosate
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normalezied NTs with ETOHmimics EtOH at GABAa
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baclofen
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GABAb Ag, anti-addiction
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