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163 Cards in this Set
- Front
- Back
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Triazolam (Halicon), Alprazolam (xanax), and Diazepam (Valium) Mechanisms
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Variable half lives, oral benzos, act as generalized CNS depressants (GABA Receptor agonists)
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Triazolam (Halicon), Alprazolam (xanax), and Diazepam (Valium) Uses
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Short Term pre surgical sedation, anxiety and insomnia
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Triazolam (Halicon), Alprazolam (xanax), and Diazepam (Valium) Side Effects
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No major respiratory or cardiac depression, no anestheric actions. Rebound anxiety and insomnia once drug wears off.
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Flumazenil Mechanism
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Benzo/GABA receptor antagonist
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Flumazenil Uses
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Brings dental patient out of benzo sedation after dental visit (so they can drive) and also prevents overdoeses
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Flumazenil Side Effects
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Any prior anxiety state is instantly restored or aggrevated (not likely a problem at dental office because apt is over when this medication is given)
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Thiopental (Pentothal) Mechanism
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Ultra short acting barb, acts as generalized CNS depressant (GABA receptor agonist). Ra[idly enters the brain so quickly induces anesthesia. Very lipids soluble so wears off as drug redistributes to fat stores
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Thiopental (Pentothal) Uses
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Short term surgical anesthetic
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Thiopental (Pentothal) Side Effects
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Major respiratory and cardiac depression in overdoses. Hangover intoxication occurs due to slow leaching out of fat stores and redistribution of drug.
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Secobarbital (Seconal) and Phenobarbital (Nembutal) Mechanism
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Immediate acting barbs, act as generalized CNS depressants. Metabolized slowly enough by liver to allow for use for insomnia.
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Secobarbital (Seconal) and Phenobarbital (Nembutal) Uses
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Short acting prescriptions for insomnia-tolerance to sedating doses but not to lethal doses and consequent diminishing TI (accidental suicide risk) develops if continuing use.
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Secobarbital (Seconal) and Phenobarbital (Nembutal) Side Effects
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Major respiratory and cardiac depression in overdoses. Overdose can be lethal. Drug hangover effect, physical dependence, and withdrawal from long term use and abuse.
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Phenobarbital (luminal) Mechanism
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Long acting oral barb, acts as a generalized CNS depressant. Very slowly metabolized by liver so lasts in body a long time.
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Phenobarbital (luminal) Uses
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Low dose use for epileptics for seizure prevention without tolerance developing for anti-seizure effects.
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Phenobarbital (luminal) Side Effects
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Major respiratory and cardiac depression in overdoses.
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Diphenhydramine (Benadryl) and Hydroxyzine (Atarax) Mechanism
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Anticholinergic action of antihistamines causes mild sedation
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Diphenhydramine (Benadryl) and Hydroxyzine (Atarax) Uses
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Insomnia (with or without running nose) and great for old people who need quick pre surgical calming drug but can't tolerate benzos anymore
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Diphenhydramine (Benadryl) and Hydroxyzine (Atarax) side effects
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None but some decongestants accompanying them in cold remedies can elevate bloop pressure-avoid such cocktails if taking MAO antidepressants
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Meprobamate (Equanil, Miltown) Mechanism
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Barb like action but can't produce surgical anesthesia
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Meprobamate (Equanil, Miltown) Uses
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Anxiety and insomnia. Commonly prescribed to zombify 1950s housewives who went batso over social restrictions. Rarely used today
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Meprobamate (equanil, Miltown) Side Effects
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Low TI. Anxiolytic doses were also, unfortunately, sedating, hence the stepford wife
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Chloral Hydrate (Noctec) Mechanism
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Liquid sedative with anesthetic like mechanism of action (but used only in low doses to sedate). Rapid onset, short duration.
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Chloral Hydrate (Notec) Uses
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Liquid form nice for sedating unruly children in dental offices.
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Chloral Hydrate (Notec) side effects
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Low TI
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NO Mechanism
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An early gas anesthetic
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NO Uses
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Ihanlant anesthetic, can be used for euphoric sedation, pre-anesthesia and anesthesia in dental surgery. Patient is unconcerned and groggy at low doses.
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NO Side effects
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No cardiac or respiratory suppression in appropriate doses but risk of bone marrow supression. Risk of abuse.
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Melatonin Mechanism
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Neurohormone made by the pineal gland; also made and sold as a dietary supplement. Mild hypnotic effect, can shift circadian rhythm, and sleep patterns.
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Melatonin Use
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Insomnia, jet lag. Not used in dentistry
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Melatonin side effects
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Dietary preparations can be uncontrolled in dose and not certified pure.
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Buspirone (Buspar) Mechanisms
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Serotonin 5-HT1Ar agnost used to reduce 5HT neurotransmitter and consequence fore brain hyperactivity
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Buspirone (Buspar) Uses
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Anxiolytic effect only. No sedation occurs. Takes a few weeks to work so it's not helpful in dentistry.
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Buspirone (Buspar) Uses
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No major side effects
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Z Drugs (Zolpidem/Ambien) Mechanism
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Not benzoa chemically but still act on benzo site at GABA receptor
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Z Drugs (Zolpidem/Ambien) Uses
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Insomnia only-not anxiolytic at non-sedating levels so not used for dentistry.
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Z-Drugs side effects
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Mild psychological dependence possible.
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Tizanidine
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CNS Active muscle relaxant. Alpha-2 adrenoreceptor agnoist. Causes dry mouth and drowsiness.
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Benzodiazepines
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diazepam (valium), midazolam. Facilitates action of GABA in CNS at GABA alpha receptors
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Cyclobenzaprine
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Inhibits muscle stretch reflex. The mechanism is uncertain
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Botulinum Toxin
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Natural bacterial toxin. Inhibits synaptic vesicle formation. Reduced ACH release causes reduced muscle contraction. Used to treat wrinkles, localized spastic disorders (Cerebral palsy), and TMJ
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Succinylcholine
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Depolarizing blockade initial wave of depolarization leads to contraction followed by relaxation. NAchRm agnoist (double Ach structure). Blocks Nm (nicotinic receptors for skeletal muscle). Fast acting. Slow metabolic clearance.
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Succinylcholine Side Effects
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Cardiac arrest in patients with excess K+, intraocular pressure, muscle pain, and histamine release.
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Tubocurarine
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Non-depolarizing blockade. Natural product. Competitive atagonist of NAchR. Does not cross the BBB; IV only. Flaccid paralysis. Inhibitor of cholinesterase for recovery (neostigmine). Use is proglonged paralysis for surgery and diagnosis; no longer in use.
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Tubocuraine
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1st generation nondepolarizing relaxant. Isoquinoline family of drugs. Problems include CV side effects, histamine release, and long duration time
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Cistracurium
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Isoquinoline Family, most widely used muscle relaxant in clinical practice. Reduced duration and increased potency compared to tubocruarine. Reduced histamine and fewer CV effects.
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Rocuronium
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Steroid derivative family drug. Reduced histamine release. Minimal CV effects. Lower potency than Tubocurarine or Cistracurium
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Dantrolene
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Spasmolytic drug that binds to Ryanodine receptor (Ca channel in muscles) and blocks channel opening. Inhibits Ca release from the SR. Reduces muscle contraction regardless of presyaptic input. Relatively specific for skeletal muscle (RyR1 receptor specific). Uses include TX for malignant hyperthermia.
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Morphine, Hydromorphone (Dilaudid), Oxymorphone (Numorphan) Metabolism
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Metabolized in the liver therefore it's parental activity>oral activity. Metabolites are from the conjugation of OH groups with glucornoic acid. Morphine-6-glucuronide is an active metabolite and could accumulate during chronic Tx. BBB limits the drug distribution into the CNS, speed and duration of activity do not equate to plasma concentration.
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Morphine, Hydromorphone (Dilaudid), Oxymorphone (Numorphan)
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Mu Agnoists used in Pain management. Highly addictive.
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Codeine, Oxycodon (Oxycotin), Hydrocodon (Hycodan)
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O-demethylated to morphine after oral administration therefore more efficacious than morphine orally. Similar pharmacological profile as morphine, hence very addictive.
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Tramadol (Ultram)
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A mu agnoist that also inhibits serotonin and NE uptake. Activities cannot be completely blocked by opioid antagonists. Highly addictive.
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Meperidine
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Profile similar to morphine. Readily partition into CNS therefore produce analgesia at lower systemic level (less constipation). Does not antagonize oxycotic's action or prolong labor. Less respiratory suppression in newborns. Metabolized by demethylation to generate normeperidine which could cause excitation, hallucinations, and convulsions. Potential drug interaction with MAOIs
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Fetanyl, Sufentanyl, Remifentanyl
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Most potent Mu agonist,80-100x morphine. Very lipophilic and therefore can be used in trans dermal patches. Distribute readily, fast onset and offset. Less peripheral hemodyamic effect than morphine.
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Methadone
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Long half life, 15 to 20 Hours and orally active. Same profile as morphine therefore can be addictive. No "Rush" because of slow onset and not preferred.
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Pentazocine
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Agonist at k receptor, partial agonist at u receptor. Can precipitate withdrawal in patients on morphine. Has effects on cardiac function. Formulation pentazocine (50mg) with naloxone (.5mg) Talwin NX can be used to prevent iv injection abuse.
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Butorphanol
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Profile similar to pentazocine but with higher u receptor activities. Major side effects are similar to that of u agnoist. Because of effects on the heart, less useful than morphine in patients with CHF or MI.
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Nalbuphine
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Structure similar to that of oxymorphone. Profile similar to that of pentazocine but is a more potent agonist in u receptors, hence can precipitate withdrawal in patients on morphine. Has ceiling effect on both analgesia and respiratory depression. At high doses will produce psycho-mimetic effects
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Buprenorphine
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High affinity partial agonist for the u receptor. Dissociates very slowly if at all. Can cause abstinence symptoms in patients on u agonists for weeks. Approved for use as a maintenance drug. Combines with naloxone to minimize abuse potential.
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Naloxone (Narcan)
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Opioid antagonist. Has a duration of 1-4 hours.
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Naltrexone (revia)
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Opioid antagonist. Has a duration of action of 24 hours
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N-methylnaltrxone (relistor)
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Opioid antagonist that exhibits minimal CNS penetration and therefore only active peripherally. Can be used to alleviate the constipation effect of morphine w/o altering the analgesic effect of the drug. Treat constipation in PT on palliative care.
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Alvimopan (Entereg)
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Opioid antagonist that exhibits minimal CNS penetration and therefore only active peripherally. Used to accelerate the time to upper and lower GI recovery following partial large or small bowel resection surgery with primary anastamosis.
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Cocaine
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Ester LA. Only LA that has vasoconstricting effects (it blocks the reuptake of NE). Only LA absorbed well by the GI tract. Excellent topical use for nose/eyes/sinus.
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Cocaine Properties
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Onset withint 1 min and lasts two hours. Conc of 4%
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Procaine
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Ester LA. 1st fully synthesized LA but no longer used in dental carpules. Most potent vasodilator of all LA.
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Procaine Properties
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Onset in 6-10 min. Duration is short (30 min) and half life is .1 hour. PH 5-6.5 plain or 3.5-5.5 with ep.
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Chloroprocaine
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Chlorinated procaine molecule. Limited use in medicine and not used in dentistry.
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Tetracaine
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Ester LA. Topical used in dentistry. Used in medicine for spinal anesthesia (crystals)
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Tetracaine Properties
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5-8 times as potent as cocaine. 45 min onset. 4% conc and very toxic.
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Benzocaine
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Ester LA. Topical only.
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Benzocaine Properties
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poor solubility. Remains at the site of application. System toxicity unknown. 14-20%.
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Lidocaine
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Amide LA. Current standard for all LA; others measured to it. First amide developed and only one used topically.
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Lidocaine Properties
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onset in 2-3 min. Potency 2x compared to procaine. Duration of 60-120 min. Half life of 1.6 hours. PH 6.5, or 5.0-5.5 with epi. Concentration at 2%
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Mepivacaine
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Most commonly used in dentistry. Amide LA.
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Mepivacaine properties
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onset in 2 min. Potency is X2 compared to procaine. Duration is 90-180 min. Half life of 1.9 hours. ph 4.5 plain or 3-3.5 vaso. Conc is 3% plain or 2% with levonordefrin.
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Prilocaine
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Possibly some met in lung after liver has metabolized. Reported to also cause methemoglobinemia.
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Articaine Properties
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onset 1-3 min. Potency is 1.5 compared to lidocaine. Duration is 90-180 min. Half life is 1.25 hours. ph is 4.4-5.2 with epi. Concentration is 4%
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Prilocaine Properties
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onset in 2-4 min. potency x2 to procaine. duration of 60-120. Half life of 1.6 hours. PH 4.5 plain or 3-5 with epi. Conc is 4%
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Articaine
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Most recent LA released in US. Reported to cause methemoglobinemia.
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Bupivacaine
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Amide LA. Cardiac toxicity, developed Ropivacaine that is an S enatiomer with less toxicity.
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Bupivacaine Properties
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Onset is 6-10 min, potency is 4x compared to procaine and lidocaine. Duration is 240-480 min. Half life is 2.7 hours. pH is 4.5-6 plain or 3-4.5 with epi. Concentration is .5%
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Etidocaine
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Amide LA. Less cardiac effects than bupivacaine and great % non ionized at body's pH.
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Etidocaine properties
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Onset is 1.5-3 min. Potency is 4x lido. Duration is 240-480. Half life is 2.6hours. pH is 4.5 plain and 3-3.5 with epi.
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Tetracaine and Oxymetazoline
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Nasal delivery of LA. Topical, no DDS needed for delivery.
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Benzo as GA
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IV GA> Rarely used alone for GA. Cannot easily induce and maintain GA. Lack analgesic properties. Used for sedative and amnestic effect.
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Opioids for GA
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IV GA. Decrease MAC of inhalation agents. Primarily used as an adjunct for GA. Respiratory depression.
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Ketamine
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IV GA. Duration of GA is 5-20 min. Metabolized in the liver. Increase in HR, BP and CO due to the sympathomimetic effects. Do not sure in patients that will not tolerate the above well. Stimulates saliva excretion. Emergence phenomenon 5-30%. Dissociative anesthesia. Amnesia, analgesia, and catalepsy. Thalamoneocortical and limbic systems. Protected reflexes maintained. NMDA antagonist. Affects mu opioid receptors.
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Ketamine properties
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Onset and peak plasma conc is 1 min after IV, 5-15 min after IM or 30 min PO. Half life is 11-16 min and elimination half life is 2-3 hours.
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Methohexital
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IV GA. 2.5 times more potent than thiopental. Shorter duration of action. Sleep time is 5-7 min. Mean elimination half life of 3.9 hours. bio-transformed in the liver. Excitatory phenomenon. Most often used in GA in OMS.
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Propofol
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IV GA. Unrelated to other GA. Oil in water emulsion. Rapid onset. Distribution half life of 1-8 min. Terminal elimination half life of 4-24 hours. Extensive tissue and protein binding. Disappears more rapidly than thiopental. Decreased MAP 20-30%. Apnea after 22-45% induction dose. Pain on injection. Less N and V. Discard unused portion after 6 hours.
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Nitrous Oxide
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Mac is 105%. Blood gas partition is .47%. With other gas concentration is 50-70%. Little effect on respiration. Elimination unchanged. Dysphoria and nausea with increased concentrations. Diffusion hypoxia. Can induce change in folate and amino acid metabolism.
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Sevoflurane
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MAC is 2.05%. Mild airway irritant. Suitable for mask induction. Rare hepatotoxicity.
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Desflurane
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Blood gas partition coefficient is .42. Irritating to airway. MAC is 6%. Required heated vaporizer. Expensive compared to other gases. Reduces SVR and MAP but increase in heart rate causing stable CO. Lower risk of hepatotoxicity. Rapid depth and recovery.
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Isoflurane (Forane)
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Anesthetic of choice. Vlood/gas partition coefficient is 1.4, MAC is 1.15%. Pungent odor. Can provide muscle relaxation. Does dependent depression of Myocardial contractility. Coronary vasodilation. CO maintained. Can use catecholamines. Respiratory depression. Neither nephrotoxic or hepatotoxic.
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Halothane
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Halogenated hydrocarbon. MAC is .75%. Blood gas is 2.3. Poor analgesic properties. Incomplete muscle relaxation. Decreased MAP. Depressant effect on Myocardial contractility. Vasodilator. Depressant on respiration. Elimination alveolar excretion and hepatic metabolism. sensitizes heart to catecholamines. Associated with hepatoxicity. Malignant hyperthermia.
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NO
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Only gaseous anesthetic still in use. Only inorganic substance used clincally as an anesthetic. Frequently used in combo with other anesthetics.
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NO Onset
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Very rapid (low blood solubility)
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NO MAC/Potency
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105% (used as supplement to volatile anesthetics). Normally not used at pp less greater than 70%. Used at 20-50% for conscious sedation and analgesia.
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NO Analgesia
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Good (even at sub-anesthetic concentrations)
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NO MM Relax
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Minimal
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NO C-vascular
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None (Unique to NO)
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NO Respiratory
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Minimal except in patients with COPD
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NO Adverse effects
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dysphoria and nuasea, impaired fertility, and increased abortion rates, abuse potential for those with access
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Desflurane/Suprane
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Newest inhalation anesthetic. No recommended for induction, children and pt with heart disease. Used in maintenance phase to rapidly adjust duration of anesthesia
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Desflurane/Suprane Onset
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RAPID. Blood gas coefficient is similar to NO
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Desflurane/Suprane MAC/Potency
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6-7%
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Desflurane/Suprane Analgesia
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Moderate
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Desflurane/Suprane MM Relax
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Good
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Desflurane/Suprane C-vascular
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increased rate at greater than 1.25 MAC. Decreased blood pressure.
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Desflurane/Suprane respiratory
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depression
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Desflurane/Suprane adverse effects
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Respiratory tract irritant. Can trigger malignant hyperthermia.
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Isoflurane/Forane
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Most widely used inhalation anesthetic. Anesthetic of choice for most purposes. Stable, non flammable, potent.
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Isoflurane/Forane Onset
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RAPID (Limited by pungent odor)
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Isoflurane/Forane MAC
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1.2%
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Isoflurane/Forane Analgesia
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Moderate
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Isoflurane/Forane MM Relax
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Moderate
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Isoflurane/Forane c-vascular
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minor depression in contractility and increase in rate. Decrease in blood pressure.
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Isoflurane/Forane Respiratory
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Moderate depression
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Isoflurane/Forane Adverse side effects
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Can trigger malignant hyperthermia.
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Barbiturates
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First drugs used as IV anesthetics. Most commonly used induction agents; used to treat seizures.
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Barbiturates Chemistry
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Highly lipid soluble. Rapidly crosses the BBB.
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Barbiturates Mechanism
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GABA receptor agonist and allosteric modulator.
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Barbiturates Kinetics
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Loss of consciousness in less than 30 sec. Regain in 10-20 min
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Barbiturates Analgesia
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Hyperalgesic (subanest doses used with analgesic).
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Barbiturates CV
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Decrease in BP and reflex heart rate increase.
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Barbiturates Respiratory
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Depression
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Barbiturates Averse effects
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Vasospasm. Use cautiously in elderly and asthmatics.
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Benzodiazepines
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Used widely as an adjunct to GA. Used for induction in patients with severe cardiac problems. Wised widely for deep and conscious sedation protocols. Produce anxiolysis, sedation, amnesia, skeletal muscle relaxation.
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Benzodiazepines Uses
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Declining in favor of the others
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Benzodiazepines Mechanism
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GABA receptor agonist/allosteric modulator
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Benzodiazepines Kinetics
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Rapid onset (less than 1 minute) and long lasting (1 hour)
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Benzodiazepines Analgesia
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None
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Benzodiazepines CV
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None
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Benzodiazepines Respiratory
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none
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Adverse effects
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long elimination half life so it causes drowsiness.
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Opioid
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Facilitates delivery of GA and sedation. Produce analgesia and sedation. Produce anxiolysis, sedation, amnesia, skeletal muscle relaxation. Can produce mood alteration, tolerance, phys. dependence, and addiction.
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Fentanyl/Subllimaze Chemistry
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Potency is 100 greater than morphine, High lipid solubility so rapid onset.
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Fentanyl/Subllimaze Mechanism
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Mu opioid receptor agonist
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Fentanyl/Subllimaze Analgesia
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Excellent
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Fentanyl/Subllimaze CV
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insignificant
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Fentanyl/Subllimaze Respiratory
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Profound depression; caution for COPD and asthma
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Fentanyl/Subllimaze Adverse effects
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Nausea and constipation
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Ketamine/Ketalar
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Produces a unique excitatory state. Dissociative anesthetic. Analgesia, amnesia, caralepsy, and protective relexes maintained. Used for rpeated dressing changes, radiological procedures, cardiac surgery, and patients in shock.
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Ketamine/Ketalar Chemistry
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Relative of phencyclidine PCP/Angel dust
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Ketamine/Ketalar Mechanism
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NMDA receptor antagonist
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Ketamine/Ketalar Administration
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IV, IM, PO, PR
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Ketamine/Ketalar Kinetics
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Rapid onset, duration is 5-20 min
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Ketamine/Ketalar CV
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Increased HR, output, and bood pressure
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Ketamine/Ketalar Respiratory
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Minimal
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Ketamine/Ketalar Adverse Effects
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Negative emergence phenomenon, (hallucinations, vomiting, etc)-given with bezos
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Propofol/Diprivan
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Unique structure, unlike any other GA. Can be used for conscious sedation and induction/maintenance in GA. Often used for sedation during intensive care. Recovery is faster than with barb/patients reported feeling better.
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Propofol/Diprivan Kinetics
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Rapid onset; duration of action is less than 10 min.
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Propofol/Diprivan Mechanism
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GABA receptor potentiation/endocannabinoid system
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Propofol/Diprivan Analgesia
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None
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Propofol/Diprivan CV
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Well tolerated in healthy patients
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Propofol/Diprivan Respiratory
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Depression
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Propofol/Diprivan Adverse effects
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Seizures and pain on injection.
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Indomethacin (indocin)
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Acetic Acid derivative. Older drug with larger side effect profile. Not used for routine analgesia. Not recommended for children under 14. Used for preterm labor and closure of ductus arteriosis.
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Diclofenac (Voltaren)
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effective analgesic. 50mg every 8 hours, 150mg/day limit. Available as a combination drug with misoprostol (Arthotec)
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Etodlac (Lodine)
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COX 2 inhibitor so less GI problems. Single dose post operatively every 6-8 hours.
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Ketorolac (Toradol)
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Can be given IV, IM, Orally or via the eyes. Very little anti-inflammatory activity. Similar potency to narcotics. Indicated for mild to moderate PO pain (not for arthritis). Prescription only. Reduces periodontal inflammatory disease in animal models.
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Nabumetone (Relafan)
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May be a selective COX 2 inhibitor. Better tolerated than some of the other NSAIDS. Once per day dosing.
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Celecoxib (Celebrex)
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Selective COX 2 inhibitor. Approved for use in osteoarthritis. Well tolerated and little GI side effects. Effective for dental pain. Controversy over long-term use and CV effects.
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