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neuro pharm complex

neuro pharm

diazepam (valium) benzodiazepine (LA GABA(B) agonist); anti-anxiety
triazolam (halcion) benzodiazepine (SA GABA(B) agonist); sleep induction
zolpidem (Ambien) NBRA (non-benzo hypnotic); short-term insomnia
eszopiclone (lunesta) NBRA (non-benzo hypnotic); short-term insomnia
flumazenil benzo antagonist; treat benzo OD
disulfiram (antabuse) blocks aldehyde DH; treat alcohol dependence
acamprosate (compral) inhibits NMDARs (prevent glutamate toxicity); treat alcohol w/drawal
baclofen GABA(B) agonist; treat spasticity, alcohol dependence (dec alcohol w/drawal sx/anxiety/craving)
β-carboline carboxyethyl ester inverse benzo agonist; causes anxiety, muscle spasms, proconvulsant state
fomepizole alcohol DH inhibitor; treat methanol intoxication
phenelzine MAOI A (CNS, SNS, liver, gut, skin) and MAOI B; irreversible, non-selective; treat depression w/ intesnse anxiety
tranylcypromine MAOI A (CNS, SNS, liver, gut, skin) & MAOI B; irreversible, non-selective; treat depression w/ intesnse anxiety
selegiline MAOI B (CNS, liver, plt); selective at low dose; treat depression w/ intesnse anxiety
moclobemide MAOI; reversible; treat depression w/ intesnse anxiety
amitriptyline TCA; 3° amine
nortriptyline TCA; 2° amine; best tolerated, blood level corresponds to daily dose
desipramine TCA; 2° amine; selective inhibition NE uptake
clomipramine TCA; 3° amine; selective inhibition 5HT reuptake
imipramine TCA; 3° amine; inhibits both NE and 5HT uptake
protriptyline TCA; 2° amine
doxepin TCA; 3° amine
fluoxetine SSRI; inhibt 5HT reuptake
sertraline SSRI; inhibt 5HT reuptake
citalopram SSRI; inhibt 5HT reuptake
escitalopram SSRI; inhibt 5HT reuptake
paroxetine SSRI; inhibt 5HT reuptake
venlafaxine SNRI; facilitate 5HT & NE neurotransmission
desvenlafaxine SNRI; facilitate 5HT & NE neurotransmission
duloxetine SNRI; facilitate 5HT & NE neurotransmission
buproprion atypical antidepressant; weak neuronal uptake of NE, 5HT, DA; treat depression, smoking cessation, ADHD
mirtazipine atypical antidepressant; Noradrenergic and specific serotonergic antidepressant (NaSSA); 5HT2 & α2R antagonist, antihistamine
trazadone atypical antidepressant; 5HT2A R effect, antihistamine; antidepressant, sleep aid; SE: priapism
Vilazodone atypical antidepressant; partial agonist 5HT1A R, modest 5HT reuptake inhibition
Nefazodone atypical antidepressant
Lithium treat bipolar disorder, unipolar depression augmentation
chlorpromazine phenothiazine antipsychotic; low potency block D2R; SE: sedation (H1 block), postural hypotension (α1 block), dry mouth/urin retent/cognitive impair (muscarinic anticholinergic)
perphenizine thioxanthene antipsychotic; mid potency block D2R
haloperidol butyrophenone antipsychotic; high potency block D2R; hyperprolactinemia SE
Risperidone atypical antipsychotic; highest potency D2R inhibition, 5HT2a R inhibition; SE: hyperprolactinemia
Palliperidone atypical antipsychotic; D2R & 5HT2a R inhibition
Ziprasidone atypical antipsychotic; D2R & 5HT2a R inhibition
Olanzapine atypical antipsychotic; D2R & 5HT2a R inhibition; SE: sedation, dry mouth/urin retent, cognitive impair
Clozapine atypical antipsychotic; D2R & 5HT2a R inhibition; SE: postural hypotension, sedation, dry mouth/urin retent/cognitive impair
Quetiapine atypical antipsychotic; lowest potency D2R & 5HT2a R inhibition; SE: sedation (H1), postural hypotension (α1)
Aripiprazole atypical antipsychotic; D2R & 5HT1aR partial agonist & 5HT2a R inhibitor
morphine strong opioid R agonist; high affinity μR; analgesic, euphoria, cough depression, miosis, emesis, antidiarrheal, urine retention, cerebral vasodilator (CO2 retent), urticaria, decreased uterine contractions in labor
methadone strong opioid R agonist; μR; analgesic and controlled w/drawal opioid dependency
meperidine strong opioid R agonist; μR>κR, potent analgesic, euphoric, high abuse liability, midriasis, no affect on labor contractions; MAOI contraindicated (hypertensive crisis)
fentanyl strong opioid R agonist; μR, miosis, 100x potency of morphine, highly lipophilic, p450 metab
oxycodone strong opioid R agonist; semisynthetic derivative of morphine commonly compounded with acetaminophen & asa
heroin strong opioid R agonist; illicit use only, diacetylation of morphine increases potency 3x, increased lipophilicity and cerebral bioavailability
codeine moderate opioid R agonist; analgesic, converted to morphine, anti-tussive effect, less abuse liability b/c less analgesic/euphoric, compounded with asa & acetaminophen commonly
propoxyphene moderate opioid R agonist; methadone derivative, mild analgesic, 1/2 potency of codeine, OD extremely dangerous (resp dep, cardiotoxicity)
hydroxycodone moderate opioid R agonist
pentazocine mixed opioid R agonist/antagonist; κR agonist/weak antag; μR antagonist; can ppt w/drawal sx from morphine, increases BP
buprenorphine partial opioid R agonist; treats opioid dependence; morphine-like in naïve, w/drawal in users
tramadol partial opioid R agonist (weak μ agonist); inhibit 5HT & NE reuptake
naloxone opioid R antagonist; potent agonist μ>κ R's, used for rapid reversal opioid OD; resp dep reversal with some sparing of analgesia
naltrexone opioid R antagonist; long t1/2; decreases rewarding effects of alcohol; used for outpt treatment of opioid and EtOH abuse
marijuana endocannabinoid R agonist; euphoria, perceptual change
ketamine NMDA R antagonist (facilitate DA release); dissociative analgesic; high pain tolerance, vertical nystagmus, hyperthermia, hallucination
phenycyclidine (PCP) NMDA R antagonist (facilitate DA release); dissociative analgesic; high pain tolerance, vertical nystagmus, hyperthermia, hallucination
MDMA (ecstasy) complex effects on monoamines; empathogenic, euphoric, hallucinogenic effects
methylxanthines (caffeine, theophylline, theobromine) phosphodiesterase inhibition and adenosine R antagonism; inc alert, positive inotropic effects, mild diuresis, increase gastric acid secretion
nicotine nicotinic cholinergic R agonist
cocaine CNS blockade of monoamine transport, esp DA 7 NE, prolonging catecholamine effects; peripheral Na channel inhibition
amphetamine indirect agonist enhancing catecholamine release; increases euphoria, attentiveness, pressor effects
methylphenidate decreases DA reuptake by inhibiting DAT; derivative that may be smoked
dextroamphetamine indirect agonist enhancing catecholamine release; treat ADHD, narcolepsy, pain adjuvant
varenicline partial nicotinic cholinergic R agonist for treating nicotine addiction
Created by: childeb



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