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neuro pharm complex
neuro pharm
| Question | Answer |
|---|---|
| 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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