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Pharmacology 2 Exam2

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A focus a group of neurons with synchronous, high frequency discharge
Causes of seizures genetic defects, hypoxia at birth, head trauma, tumor
Partial or local seizures starting at a focus, with limited spread
Generalized seizures widespread seizure activity involving both hemispheres
Simple partial seizures symptoms depend on the location of abnormal activity in the brain
Complex partial seizures confused behavior and impairment of consciuosness
Tonic-clonic seizures (Grnad mal): muscle rigidity followed by synchronous muscle jerks
Myoclonic seizures sudden muscle contractions
Absence seizures (Petit Mal): very frequent but brief (10-30seconds) episodes of loss of consciousness
Atonic seizures sudden loss of muscle tone
Febrile seizures fever-associated seizures in children (6 months to 5 years)
Status epilepticus seizure activity that persists for a long time
Prolongation of Na+ channel inactivation to treat seizures Phenytoin, carbamazepine, valproate, lamotrigine
Suppression of Ca2+ influx to treat seizures valproate, ethosuximide
Potentiation of Gaba action to treat seizures tiagabine: increased gaba action by prolonging the presence of GABA in the synapse vigabatrin: increased gaba action by inhibitng the enzyme that degrades gabe in the synapse benzo's and barb's: increase gaba action by binding directly to gaba receptors
Time course of local anesthesia rapid onset 2-5 minutes 10-15 minutes
Time course of local anesthesia Slow and variable recovery 15-60 minutes, hours
Congenital insensitivity to pain inability to feel pain from birth
Allodynia pain due to a stimulus that does not normally provoke pain
Dysfuntional pain pain with no known tissue injury, or noxious stimulus (tension headache, IBS)
Central sensitization leads to hyperalgesia and allodynia
mu opiod receptor mediates almost all morphine-produced effects
delta opiod receptor central excitation, analgesia
kappa opiod receptor analgesia, dysphoria
Strong opiod agonists morphine, heroin, hydromorphone, oxymorphone, methadone, meperidine, fentanyl, levorphano
Metabolism of heroin Heroin --> MAM --> Morphine
Opiod withdrawal syndrome occurs within hours after last dose of morphine
Opiod withdrawal syndrome symptoms 8-16 hours... lacrimation, rhinorrhea, sweating, mydriasis, anorexia, nervousness, irritability, tremors, anxiety, restless sleep
Opiod withdrawal syndrome symptoms within 36 hours... skeletal muscle fasciculation and twitch, severe painful cramps, uncontrolled vomiting, salivation, diarrhea, weakness, depression, unable to sleep, increased respiratory rate, BP, temp, blood sugar
Opiod withdrawal syndrome symptoms peak at _____ and subsides over the next ______ 48-72 hours 10 days
Why is methadone used in treatment of opiod dependence? methadone withdrawal is slower in onset, longer in duration, much less intense
Meperidine (Demerol) mu-agonist The constipation and urinary retention is less common than with morphine
Meperidine toxicity large repeated doses can lead to an excitatory syndrome -- hallucinations, tremors, muscle twitches, dilated pupils -- due to accumulation of its metabolite Normeperidine Not drug of choice for treatment of severe, prolonged pain
Fentanyl mu receptor agonist 80 times more potent than morphine as an analgesic
Mild to moderate opiod agonists codeine, oxycodone, hydrocodone, propoxyphene
Pentazocine and butorphanol antagonist at mu receptor and agonist at kappa receptor
Naloxone and naltrexone central and peripheral antagonists at mu and kappa receptors
Methylnaltrexone and Avimopan peripheral only antagonist at mu and kappa receptors
Naloxone clinical use treatment of opiod toxicity, especially respiratory depression Reverses effects of mu opiod agonists
Naltrexone used in long-term management of opiod addiction Long duration of action
Methylnaltrexone Peripheral only - used to treat opiod-induced constipation and block the peripheral actions of opiods dissociates from mu, delta, and kappa quickly
Alvimopan blocks the peripheral action of opiods - used to treat opiod induced constipation mu > delta = kappa receptor affinity slow dissociation rate
Tramadol activates mu opiod receptor inhibits NE and 5-HT intake less efficacious than morphine less opiod-like adverse effects
Tapentadol (Nucynta) Atypical Opiod Activates mu opiod receptors and inhibits NE reuptake Comparable analgesic efficacy with morphine, less opiod-like adverse effects, less addiction potential, better GI tolerability
Gabapentin Anti-convulsant effective for neuropathic pain, epilepsy Acts on a2delta subunit of voltage-dependent calcium channels, thus decreasing neural excitability
Pregabalin (Lyrica) Anti-convulsant effective for neuropathic pain, epilepsy Acts on a2delta subunit of voltage-dependent calcium channels, thus decreasing neural excitability
Duloxetin (Cymbalta) antidepressant Treats diabetic neuropathy, depression, fibromyalgia, chronic musculoskeletal pain SNRI
Ziconotide used in Severe chronic pain must be delivered through intrathecal pump system N-type voltage-gated calcium channel blocker
Aura phase predicting that migraine will occur
Triptins (Sumatriptan) Selective 5-HT1B/1D receptor agonist Reduce both sensory activation in the periphery and nociceptive transmission in the brainstem Causes vasoconstriction -> contraindication coronary heart disease
Created by: Newby549



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