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CNS- stimulants/ASA
| Question | Answer |
|---|---|
| Caffeine | Methylxanthine non-selective antagonist of adenosine receptors, phosphodiesterase inhibition Use: apnea, fatigue, drowsiness, analgesic, respriatory depression |
| Doxapram HCl- Dopram | analeptic stimulate peripheral carotid chemoreceptors Use: post anesthesia, apnea, CNS depression |
| Modafinil- Provigil | Analeptic Narcolepsy MOA: unknown; wakefulness promoting effect similar to NT racemic drug has different half lives |
| Armodafinil- Nuvigil | Analeptic Narcolepsy MOA: unknown; wakefulness promoting effect similar to NT R-enantiomer has 3X the lifetime |
| Dextroamphetamine Sulfate- Dexedrine | Amphetamine single enantiomer; increased potency |
| Adderall | mixture of various amphetamine salts (Extended release) |
| Methamphetamine- Desoxyn | Amphetamine Racemic Also used as an anorexiant |
| Lisdexamfetamine dimesylate- Vyvanse | amphetamine prodrug that provides once daily dosing with less abuse potential Cleaved by GI protease |
| Amphetamines | MOA: prevent reuptake of NE and DA and increase release ADHD and narcolepsy |
| D-(-)-ephedrine | Substituted amphetamines Decongestant-more effective than pseudoephedrine CNS effects Use caution in enlarged prostate, HTN, MAO inhibitors |
| Pseudoephedrine | substituted amphetamine Decongestant--given to reduce side effects (CNS!!) |
| Methylphenidate- Ritalin | Amphetamine-like Use: ADHD, narcolepsy Mild CNS stimulant similar to amphatamines (unknown) take dose prior to 6pm |
| Dexmethylphenidate- Focalin | (R,R)+ Diastereomer that is more pharmacologically active Amphetamine-like drug |
| Pemoline- Cylert | amphetamine like drug off the marked due to risk of liver failure |
| Sodium oxybate- Xyrem | Cataplexy treatment, EDS in narcolepsy Schedule III-available only through specialized pharmacy COmmon date rape drug MOA: unknown; suppressed REM: GHB receptors in brain--derived from GABA rapid metabolization in krebs |
| Atomoxetine HCl- Strattera | ADHD in children AND adults (first non-stimulant to treat disorder in 30years) selective inhibitor of presynaptic NE transporter CYP2D6 followed by glucoronidation (pharmacogenomics) |
| Guanifacine HCl- Tenex | Centrally actin alpha-adrenergic agonist approved for ADHD Also: HTN, heroine withdrawal |
| Benzphetamine HCl- Didrex | anorexiant Direct stimulation on satiety center in hypothalamic and limbic regions Best if taken on empty stomach; avoid taking late in day; do not crush; can produce psychological disturbances; monitor BP |
| Diethylpropion HCl- Tenuate | anorexiant Direct stimulation on satiety center in hypothalamic and limbic regions Best if taken on empty stomach; avoid taking late in day; do not crush; can produce psychological disturbances; monitor BP |
| Mazindol- Mazanor | Anorexiant Take with meals to avoid GI upset |
| Phendimetrazine- Plegine, Adipost | anorexiant Direct stimulation on satiety center in hypothalamic and limbic regions Best if taken on empty stomach; avoid taking late in day; do not crush; can produce psychological disturbances; monitor BP |
| Phenteramine- Ionamin, Fastin | anorexiant Direct stimulation on satiety center in hypothalamic and limbic regions Best if taken on empty stomach; avoid taking late in day; do not crush; can produce psychological disturbances; monitor BP |
| Orlistat- Xenicall, Alli | lipase inhibitor for weight loss |
| Morphine- Avinza | opiate agonist- phenanthrene analgesic, anesthetic Full agonist at Mu receptor |
| Heroin | 3,6- diacetyl morphine acetylation greatly increases lipophilicity |
| Codeine | Opiate agonist- phenanthrene: natural product Partial agonist at Mu receptor Methyl-ether of morphine: less effect as analgesic, less resp depression and constipation; effective anti-tussive |
| Opium tincture: Paregoric | schedule III (camphorated) treatment of diarrhea and as an analgesic |
| Hydrocodone- Iodussin, Vicodin | Opiate agonist- phenanthrene: semisynthetic full agonist at the Mu receptor Less effect as analgesic and less respiratory depression (not used for analgesic effects) Antitussive effects |
| Oxycodone- Oxycontin, Roxicodone | Opiate agonist- phenanthrene: semisynthetic full agonist at the Mu receptor equipotent as morphine |
| Percodan | Oxycodone + APAP |
| Hydromorphone- Dilaudid | Opiate agonist- phenanthrene: semisynthetic full agonist at the Mu receptor equipotent as analgesic and respiratory depression, less constipation refrigerate suppositories |
| Oxymorphone-Numorphone, Opana | Opiate agonist- phenanthrene: semisynthetic full agonist at the Mu receptor 10X as potent as morphine IV; weakest antitussive; MOST potent resp depression and intense physical dependence do NOT use <18years |
| Levorphanol- LevoDromoran | Opiate agonist- phenanthrene: semisynthetic full agonist at the Mu receptor equipotent as analgesic and respiratory depression; less constipation |
| Mepiridine- Demerol | Opioid agonist- Synthetic Phenylpiperidines less smooth muscle spasms, constipation and depression of cough reflex |
| Sufentanil- Sufenta | Opioid agonist- Synthetic Phenylpiperidines VERY potent exceptional analgesic equal potent to remifentanil |
| Alfentanil- Alfenta | Opioid agonist- Synthetic Phenylpiperidines analgesic adjunct in incremental dosing (syringe) during NO anesthesia Dosing must be individualized; not for <12 years |
| Fentanyl | Opioid agonist- Synthetic Phenylpiperidines breakthrough cancer pain Serious life threatening hypoventilation possible |
| Remifentani- Ulvita | Opioid agonist- Synthetic Phenylpiperidines extremely potent: tied with sufentanil caution during interruption of infusion (rapid clearance and rapid offset of action) do not administer same IV tubing as blood products |
| Methadone- Dolophine, Methadose | Opioid agonist- Synthetic Diphenylheptadines relief of severe pain; detox of narcotic addiction (special clinic) not useful preoperatively to reduce anxiety or induction |
| Buprenorphine HCl- Buprenex | opiate agonist/antagonist--lower abuse potential compete at Mu receptor displacing other agents (antagonistic activity)--equipotent to naloxone hepatic metabolism; can produce withdrawal |
| Naloxone HCl- Narcan | opiate pure antagonist treat opiate overdosage to reduce resp depression very short DOA--will induce withdrawal symptoms immediately may be useful in alcoholism |
| Butorphanol tartrate- Stadol | Opiate agonist/antagonist Nasal spray: migraine Injection: pain management, anasthesia 1/40th antagonistic activity of naloxone K agonist with 5X potency of morphine |
| Dezocine- Dalgan | Opioid agonist/antagonist Aminotetralin chemical series comparable to morphine antagonistic activity 1/120th of naloxone |
| Nalbuphine HCl- Nubain | opiate antagonist/agonist equipotent to morphine, 2nd weakest antagonist |
| Pentazocone HCl- Talwin | opioid agonist/antagonist use as a heroine substitute in combo with tripelenamine: T's and blues caution in renal/hepatic |
| Tramadol: Ultram | Central analgesic agent (non-schedule with narcotic opioid agonist activity) binds mU receptors and prevents reuptake of NE and serotonin in CNS hepatic metabolism and renal excretion (not if CrCl <30) |
| Clonidine- Duraclon | Central analgesic agents via epidural route: A2 agonist in spinal cord (use in combo with opiates) NOT recommended for ostetrical, post partum or peri-op pain management) Antihypertensive with the most off-label uses |
| Tapentadol HCl- Nucynta | Central Analgesic New 2008 Opioid for relief of moderate to severe acute pain in patients >18 years (18X less potent than morphine) Mu-opioid and inhibits NE reuptake extensive first pass; CYP2C9 demethylation; no inhibition/induction/ minimal protein |
| APAP | antypyretic; inhibits prostaglandin synthase in the CNS Interaction with warfarin |
| Zirconitide- Prialt | Conopeptides or conotoxins binds to N-type Ca2+ channels Use: management of severe chronic pain in patients intolerant to other treatments potentiate opiate induced decrease in GI motility (does NOT potentiate respiratory depression) |
| Pregabalin- Lyrica | structural analog of GABA (does not bind receptors) Neropathic pain, postherpatic neuralgia, fibromyalgia Unknown mechanism (binda to the alpha2-delta and decrease NT) negligible metabolism; schedule 5; thiazolidinediones inc. peripheral edema/weight g |
| Capsaicin patch- Qutenza | post herpetic neuralgia MOA: Capsaicin binds VR1: permits cations to pass through the cell membrane and produce the same sensation the excessive heat or abrasive damage |
| Acetylsalicylic Acid- Aspirin | Inhibitor of prostaglandin synthase by acetylating COX-1 Irreversible inhibitor of platelet aggregation by preventing synthesis of thromboxane A2 Large doses inhibit synthesis of PGI2 (inhibitor of platelet aggregation) |
| Choline Salicylate- Anthropan | liquid product Fewer GI side effects than aspirin |
| Diflunisal- Dolobid | non-selective COX inhibitor Mild-moderate pain, OA, RA |
| Magnesium Salicylate- Extra Strength Doan's Pills | sodium free salicylate with low GI upset Mg toxicity in renal insufficiency |
| Salicylsalicyclic acid- Disalcid | insoluble in gastric secretions and NOT absorbed until small intestine |
| Sodium Salicylate | enteric coated Less effective at preventing fever and relieving pain Patients hypersensitive to ASA may tolerate Platelet function not effected; but increase PT |
| Sodium Thiosalicylate- Rexolate injection | IM injection acute gout, muscular pain, musculo-skelatal disturbances, rheumatic fever |
Created by:
jallais2