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137 Cards in this Set
- Front
- Back
5 categories of drugs used for glaucoma
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Alpha-agonists
Beta-blockers Diuretics Cholinomimetics Prostaglandin |
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Glaucoma drug to avoid in closed-angle glaucoma
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Alpha-agonists
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Two alpha agonists used in glaucoma
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Epi
Brimonidine |
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Mechanism of alpha-agonists for glaucoma
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Decrease AH synthesis
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3 beta blockers used in glaucoma
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Timolol, betaxolol, carteolol
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Mechanism of beta blockers for glaucoma
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Decrease AH secretion
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Diuretic used in glaucoma
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Acetazolamide
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Mechanism of acetazolamide in glaucoma
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Decrease AH secretion due to decreased HCO3- (via inhibition of carbonic anhydrase)
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Examples of direct and indirect cholinomimetics used for glaucoma
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Direct: pilocarpine, carbachol
Indirect: physostigmine, echothiophate |
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Mechanism of cholinomimetics for glaucoma
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Increase outflow of AH (contract ciliary muscle and open trabecular meshwork into canal of Schlemm)
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When is pilocarpine used in glaucoma?
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Emergenices
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Side effects of cholinomimetics for glaucoma
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Miosis
Cyclospasm |
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Prostaglandin used in glaucoma
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Latanoprost (PGF-2alpha)
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Mechanism of latanoprost for glaucoma
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Increase outflow of AH
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Side effect of latanoprost
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Darkens color of iris (browning)
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7 opioid analgesics
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Morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan
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3 intrinsic opioid receptors
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Mu = morphine
Delta = enkephalin Kappa = dynorphin |
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Opioids are agonists at opioid receptors, causing
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K+ channels to open (efflux)
Ca channels to close Both --> decreased synaptic transmission |
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Opioids decrease release of these 5 neurotransmitters
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ACh, NE, 5HT, glutamate, substance P
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Other than pain and methadone addiction programs, 3 clinical uses for opioids
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Cough suppression (dextromethorphan)
Diarrhea (loperamide and diphenoxylate) Acute pulmonary edema |
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7 side effects of opioids
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Addiction
Respiratory depression Constipation Miosis Addictive CNS depression with other drugs Biliary colic from smooth muscle cell contraction in the sphincter of Oddi Histamine-released --> vasodilation |
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Tolerance does not develop to these 2 opioid side effects
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Miosis
Constipation |
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Tolerance is mediated by ____ (neurotransmitter) activating ____ (its receptor), leading to ______ of the opioid receptors
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Glutamate ---> NMDA activation --> phosphorylation of opioid receptors
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Tolerance can be decreased with _____ antagonists
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NMDA (e.g. ketamine, dextromethorphan)
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Partial agonist at opioid mu receptors, agonist at kappa receptors
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Butorphanol
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Advantage of butorphanol over other opioids
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Less respiratory depression than full agonists
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Toxicity of butorphanol
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Causes withdrawal if on full agonist
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Tramadol is a ____ opioid agonist that also inhibits ____ and ____ reuptake
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Weak
Serotonin and NE |
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Additional side effect of tramadol
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Decreased seizure threshold
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12 epilepsy drugs
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Phenytoin
Carbamazepine Lamotrigine Gabapentin Topiramate Phenobarbital Valproic acid Ethosuximide Benzos Tiagabine Vigabatrin Levetiracetam |
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All epilepsy drugs can be used for partial seizures except
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Ethosuximide
Benzos |
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First line for tonic-clonic seizures (3)
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Phenytoin
Carbamazepine Valproic acid |
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First line Rx for absence seizures
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Ethosuximide (valproic acid also possibly)
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1st line of acute treatment of status epilepticus
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Benzos
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1st line for prophylaxis of status epilepticus
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Phenytoin
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Unique mechanism of ethosuximide
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Blocks thalamic T-type Ca2+ channels
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Epilepsy drugs that block/ inactivate Na channels (5)
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Phenytoin
Carbamazepine Lamotrigine Topiramate Valproic acid |
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Epilepsy drugs that increase GABA (7)
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Topiramate
Phenobarbital Valproic acid Benzos Tiagabine Vigabatrin Levetiracetam |
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Epilepsy drugs that work on both Na channels and GABA
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Topiramate
Valproic acid |
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Epilepsy drug that was designed as a GABA analog, but primarily inhibits HVA Ca channels
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Gabapentin
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Epilepsy drug to use in pregnant women or children
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Pehnobarbital
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Best drug for myoclonic seizures
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Valproic acid
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2 drugs to use in seizures of eclampsia
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Benzos
MgSO4 (1st line) |
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1st line drug for trigeminal neuralgia
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Carbamazepine
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Other uses of gabapentin besides epilepsy (3)
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Peripheral neuropathy
Bipolar disorder Fibromyalgia |
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Prodrome of malaise and fever followed by apid onset of erythematous/ purpuric macules (oral, ocular, genital); skin lesions may progress to epidermal necrosis and sloughing
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Stevens-Johnson Syndrome (and TEN)
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Anti-epileptic drugs (AED) that cause SJS (3)
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Carbamazepine
Ethosuximide Lamotrigine |
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Side effects of carbamazepine
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Diplopia
Ataxia Blood dyscrasias (agranulocytosis, aplastic anemia) Liver toxicity Teratogenesis Induction of P-450 SIADH SJS |
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AED that can cause urticaria
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Ethosuximide
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AED that can cause NTDs in fetus
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Valproic acid
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AED that can cause fatal hepatotoxicity (follow with LFTs)
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Valproic acid
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AED that can cause agranulocytosis
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Carbamazepine
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AED that can cause aplastic anemia
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Carbamazepine
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AED that can cause fetal hydantoin syndrome
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Phenytoin
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AED known for weight gain
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Valproic acid
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Side effects of phenytoin (10)
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Nystagmus
Diplopia Ataxia Sedation Gingival hyperplasia Hirsutism Megaloblastic anemia Teratogenesis (fetal hydantoin syndrome) SLE-like syndrome Induction of P450 |
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AED known for weight loss
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Topiramate
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AED known for mental dulling
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Topiramate
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AED associated w/ kidney stones
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Topiramate
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AED associated with megaloblastic anemia
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Phenytoin
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2 AEDs associated with diplopia and ataxia
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Carbamazepine and phenytoin
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Phenytoin is a class ___ antiarrhythmic
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1B
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AED associated with SLE-like syndrome
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Phenytoin
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Why does phenytoin cause a megaloblastic anemia?
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Decreased folate absorption
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Compare the mechanism of barbiturates to benzodiazepines
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Both facilitate GABA A action by acting on the Cl- channel
Barbiturates increase the duration of opening Benzos increase the frequency of opening |
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Rx for barbiturate overdose?
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Symptom management (assist respiration, increase BP)
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Effect of benzos on REM sleep
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Decrease it
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Benzos are used in treatment of withdrawal from?
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Alcohol (DTs)
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3 sleep problem indications for benzos
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Insomnia
Night terrors Sleepwalking |
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Short-acting benzos
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Triazolam
Oxazepam Midazolam Alprazolam |
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Which benzos should be used for acute anxiety?
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Short-acting
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Highest addictive potential with these benzos
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Short-acting
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Rx for benzo overdose
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Flumazenil (competitive antagonist at GABA benzo receptor)
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Best drugs for insomnia
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ZaZolEs
Zaleplon Zolpidem Eszopiclone |
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Action of ZaZolEs is reversed by
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Flumazenil
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3 toxicities of zazoles
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Ataxia, headaches, confusion
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Anesthetic principle: increased blood solubility causes ____ onset of action
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lower
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Inhaled anesthetics caused _____ cerebral blood flow
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Increased (and deceased cerebral metabolic demand)
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Toxicity of halothane
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Hepatotoxicity
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Toxicity of methoxyflurane
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Nephrotoxicity
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Inhaled anesthetic that is a proconvulsant
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Enflurane
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5 categories of IV anesthetics
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Barbiturates
Benzos Arylcyclohexylamines (ketamine) Opiates Propofol |
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Best for induction of anesthesia/ short procedures
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Barbiturates (also propofol, which has less postop nauseua than thiopental)
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Barbiturates ____ cerebral blood flow
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Decrease
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Ketamine ____ cerebral blood flow
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Increases
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2 groups of local anesthetics
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Esters
Amides (have 2 Is in name) |
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3 esters
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Procaine
Cocaine Tetracaine |
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3 amides
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Lidocaine
Mepivacaine Bupivacaine |
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Mechanism of local anesthetics
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Bind Na channels (receptors on inner portion)
Preferentially bind activated channels, so most effective in rapidly firing neurons |
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Local anesthetics penetrate membrane in _____ form, then bind to ion channels in ____ form
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Uncharged
Charged |
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In infected (acidic) tissue, is more or less anesthetic needed?
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More (alkaline anesthetics are charged and cannot penetrate)
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Order of pain blockade based on size and myelination
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Small myelinated
Small unmyelinated Large myelinated Large unmyelinated |
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Order of loss of neurons based on sensation transmitted
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Pain first > temp > touch > pressure (last)
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Local anesthetics should be given with what other drug class
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Vasoconstrictors (epinephrine)
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Why are local anesthetics given with EPI?
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To enhance local action and decrease bleeding
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Which local anesthetic is not given with EPI?
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Cocaine
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If a patient is allergic to esters, should give?
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Amides
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Toxicity of cocaine
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Arrhythmias
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Toxicity of bupivacaine
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Severe CV toxicity
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3 toxicities of local anesthetics
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CNS excitation
HTN Hypotension |
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Depolarizing NM blockade provided by
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Succinyl choline
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Nondepolarizing NM blockade provide by
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Tubocurarine and the curiums (e.g. atracurium, rocuronium)
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NM blockade drugs are selective for the ____ receptor
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Motor nicotinic (vs. autonomic nicotinic)
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3 complications of succinyl choline
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Hypercalcemia
Hyperkalemia Malignant HTN |
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2 phases of succinylcholine blockade (prolonged depolarization and repolarized but blocked): antidote for each?
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No antidote for Phase I (potentiated by cholinesterase inhibitors)
Phase II: cholinesterase inhibitors |
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Reversal of nondepolarizing NM blockade
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Cholinesterase inhibitors (neostigmine, edrophonium, etc.)
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Treatment of malignant HTN
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Dantrolene
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Another use of dantrolene
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Neuroleptic malignant syndrome (toxicity of antipsychotics)
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Mechanism of dantrolene
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Prevents release of Ca from sarcoplasmic reticulum
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4 strategies in PD treatment
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Agonize dopamine receptors
Increase dopamine Prevent dopamine breakdown Curb excess cholinergic activity |
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3 drugs that agonize dopamine receptors
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Bromocriptine
Pramipexole Ropinirole |
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Two drugs that increase dopamine
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Amantadine
L-dopa |
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Mechanism and toxicity of amantadine
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May increase dopamine release (also an antiviral)
Causes ataxia |
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Why is L-Dopa given instead of dopamine?
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Dopamine cannot cross BBB
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What drug is always given with L-Dopa?
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Carbidopa
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Mechanism of carbidopa
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Peripheral decarboxylase inhibitor (icnreases bioavailability of L-dopa in brain and limits peripheral side effects)
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Two drugs that prevent dopamine breakdown
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MAOB inhibitor (selegiline)
COMT inhibitors (entacapone, tolcapone) |
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Best antimuscarinic for PD?
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Benztropine
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Benzotropine improves ____ and _____ but has little effect on ____
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Tremor and rigidity
Bradykinesia |
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Best drugs for essential or familial tremors
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Beta-blockers
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L-dopa is converted to dopamine in the CNS by ______
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Dopa decarboxylase
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3 toxicities of L-dopa
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Arrhythmias (from peripheral conversion to dopamine)
Dyskinesia (from long-term use) Akinesia (btwn doses) |
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MAO-B selectivity metabolizes ____ over ____ and ____
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Dopamine
NE and 5HT |
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2 classes of drugs in Alzheimer's treatment
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NMDA receptor antagonists
Acetylcholinesterase inhibitors |
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NMDA receptor antagonist
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Memantine
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Memantine helps prevent _____, mediated by _____
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Excitotoxicity
Ca |
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3 toxicities of memantine
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Dizzines
Confusion Hallucinations |
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3 acetylcholinesterase inhibitors used in Alzheimer's
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Donepezil
Galantamine Rivastigmine |
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3 toxicities of cholinesterase inhibitors
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Nausea
Dizziness Insomnia |
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In Huntington's disease, ____ is increased while ___ and ___ are decreased
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Dopamine
GABA and ACh |
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Dopamine antagonist used in Huntington's
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Haloperidol
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Two amine depleting drugs used in Huntington's
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Reserpine
Tetrabenazine |
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Sumatriptan is a ______ agonist
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5HT-1B/1D agonist
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Sumatriptan has these 2 clinical uses
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Acute migraine
Cluster headaches |
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3 effects of sumatriptan
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Vasoconstriction
Inhibition of trigeminal activation Vasoactive peptide release |
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2 toxicities of sumatriptan
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Coronary vasospasm
Mild tingling |
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Sumatriptan is contraindicated in pts with ___ or _____
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CAD
Prinzmetal's angina |