drugs: anesthetics & ADHD and Narcolepsy – Flashcards
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benzocaine
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local anesthetic - ester type treatment of sunburn, pruritus, sore throat, insect bites, mouth & gum irritation (toothache, teething, canker sores, etc.)
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Proparacaine
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local anesthetic - ester type eye surgery and other ophthalmic procedures
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Lidocaine
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local anesthetic - amide type Lidocaine with EPI may be used in the face (including the nose and ear), digit, or penis. However, use of lidocaine + EPI in patients with known peripheral artery disease is generally avoided
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Bupivacaine
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local anesthetic - amide type used for epidural, infiltration, nerve block and spinal anesthesia, but differ in potency and duration of action
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Mepivacaine
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local anesthetic - amide type used for epidural, infiltration, nerve block and spinal anesthesia, but differ in potency and duration of action
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Ropivacaine
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local anesthetic - amide type used for epidural, infiltration, nerve block and spinal anesthesia, but differ in potency and duration of action
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Dibucaine
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local anesthetic - amide type ointment for hemorrhoids
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MOA of local anesthetics
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Mechanism of action Block voltage-gated Na+ channels (reversibly) Greater affinity for Na+ channels that in the depolarized state - i.e., the neurons that are firing due to pain or itching Hence, sensory nerves are blocked more easily than motor nerves
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AE for local anesthetics
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CNS: stimulation (restlessness, tremor, euphoria) followed by inhibition (drowsiness and sedation); overdoses lead to a pattern of seizures -> coma -> respiratory failure Cardiovascular: hypotension and cardiac depression (usually manifests as an arrhythmia)
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Nitrous oxide ("laughing gas")
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Inhalational Anesthetics - Very low potency and hence cannot reduce consciousness to the level needed for major surgery by itself (i.e., will typically get the patient to early stage II) - Used for minor surgery and dental procedures - Produces significant analgesia - Induction and recovery are very rapid - Produces virtually no cardiovascular or respiratory depression - Chronic exposure is known to cause megaloblastic anemia by interfering with vitamin B12 metabolism - *Contraindicated in COPD*
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desflurane
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Inhalational Anesthetics - halogenated irritating to the respiratory tract
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enflurane
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Inhalational Anesthetics - halogenated very low risk for cardiac dysrhythmias and produce more muscle relaxation than most inhalational anesthetics; however, they cause more respiratory depression
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isoflurane
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Inhalational Anesthetics - halogenated very low risk for cardiac dysrhythmias and produce more muscle relaxation than most inhalational anesthetics; however, they cause more respiratory depression
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sevoflurane
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Inhalational Anesthetics - halogenated is considered the "best" of the lot because it produces very little organ system effects and typically has a rapid and smooth induction and recovery
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all halogenated products can trigger
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malignant hyperthermia
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MOA for inhalation anesthetics
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1.) Potentiate GABA activity at GABAA receptors to increase Cl- influx, thereby hyperpolarizing neurons 2.) Inhibit Na+ and Ca+2 influx, thereby hyperpolarizing neurons
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uses of Parenteral Anesthetics
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- To induce anesthesia in patients undergoing a major surgical procedure, which is then followed by administration of an inhalational anesthetic to maintain anesthesia - To induce and maintain anesthesia during minor surgical and diagnostic procedures
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Propofol
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Parenteral Anesthetics Rapid onset and recovery Main use is for induction of anesthesia; its use is followed by administration of an inhalational anesthetic to maintain anesthesia Has antiemetic, antipruritic and anticonvulsant properties but no analgesic properties (hence, pain may be felt when administered IV) *MOA:* Agonist at GABA(A) receptors Causes reductions in BP, CO, RR and TV
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Etomidate
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*Parenteral Anesthetics* Rapid onset and recovery similar to propofol BUT DOES NOT DECREASE BP or CO Main use is for induction of anesthesia; its use is followed by administration of an inhalational anesthetic to maintain anesthesia Has anticonvulsant properties but no analgesic or antiemetic properties; in fact, it has a very high rate of PONV *MOA:* Agonist at GABAA receptors
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Ketamine
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*Parenteral Anesthetics* Rapid onset and recovery a bit slower than propofol Main use is for* induction and maintenance of anesthesia in patients with hemodynamic instability due to hypovolemia, hemorrhage or sepsis* because it INCREASES BP, HR and CO in most patients Produces "dissociative anesthesia": analgesia, reduces sensory perception, immobility and amnesia MOA: Blocks glutamate from binding to NMDA (N-Methyl-D-Aspartate) receptors *main disadvantage*: During the recovery phase, delirium, hallucinations and irrational behavior are very common
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Opiates and Benzodiazepines in adjuvant w anesthetics
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These are often used as adjuvant medications during induction of general anesthesia to supplement the effects of the primary anesthetic induction agent (and/or to reduce its dose) For example: An opiate may be used in conjunction with propofol to reduce its dose and to minimize the pain caused by IV injection A benzodiazepine may be used in conjunction with propofol in extremely anxious patients
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Atomoxetine
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MOA: selective NE reuptake inhibitor -used to treat ADHD in children, adolescents, and adults. *It is not a controlled substance.* - alternative to stimulants for children (?6 years) and adolescents who have a substance abuse problem, family member with a substance abuse problem, tics, or severe side effects with stimulants. *General adverse effects: *weight loss, decreased appetite, vomiting, nausea, dyspepsia, headache, dizziness and irritability Same CV adverse effects as traditional stimulants (but also rare) Has a boxed warning and additional warning statements regarding the *increased risk of suicidal thinking in children and adolescents* Contraindications -Hypersensitivity to atomoxetine or any component -Concurrent use or use within 14 days of the administration of monoamine oxidase inhibitors -Glaucoma -Current or past history of pheochromocytoma -Severe cardiovascular disorders in which increases in diastolic blood pressure >15 mmHg, systolic blood pressure >20 mmHg, or heart rate >20 beats per minute would be expected to cause clinical deterioration
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buproprion
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adult ADHD 3rd line
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TCA
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adult ADHD 3rd line
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venlafaxine
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adult ADHD 3rd line
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clonidine
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pediatric ADHD 3rd line
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guanfacine
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pediatric ADHD 3rd line
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Modafinil
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Drugs Specific for Improving Wakefulness - selective, non-amphetamine wakefulness-promoting agent. It reduces excessive daytime sleepiness seen in narcolepsy without inducing anxiety or physical symptoms of CNS stimulation such as palpitations that are commonly caused by CNS stimulants. - *Narcolepsy*: To improve wakefulness in adult patients with excessive sleepiness associated with narcolepsy. -*Obstructive sleep apnea*: To improve wakefulness in adult patients with obstructive sleep apnea (OSA) -*Shift work sleep disorder*: To improve wakefulness in adult patients with shift work sleep disorder (SWSD)
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off label uses for modafanil
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ADHD but causes serious dematologic and psychiatric reaction (Stevens Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms, anxiety, mania, hallucinations, suicidal ideation) DON'T USE IN CHILDREN
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AE of modafanil
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headache, nausea, nervousness, rhinitis, decreased appetite, diarrhea, back pain, anxiety, insomnia, dizziness, and dyspepsia