pharm 1 liners- CNS Flashcards
Ganglion blockers used in research; high affinity for neuronal nicotinic receptors
hexamethonium, trimethaphan
Two direct-acting cholinomimetics that increase aqueous outflow through ciliary muscle contraction and opening of trabecular meshwork
pilocarpine, carbachol
Two indirect-acting cholinomimetics that increase aqueous outflow through ciliary muscle contraction and opening of trabecular meshwork
physostigmine, echothiophate
Nonselective alpha agonist that decreases aqueous production
epinephrine
Selective alpha 2 agonist that decreases aqueous production
brimonidine
Three beta blockers that decrease aqueous production
timolol (nonselective), betaxolol 9selective), carteolol (nonselective)
Carbonic anhydrase inhibitor used to decrease aqueous humor production
acetazolamide
Prostaglandin E2 alpha analog used to increase aqueous humor outflow
latanoprost
Common side effect of sedative hypnotics
CNS depression
Mechanism of action of benzodiazepines
Increase frequency of GABA-mediated chloride ion channel (GABAA) opening
Main route of metabolism for benzodiazepines
hepatic
Useful side effect of benzodiazepines in patients undergoing stressful procedures or surgery
anterograde amnesia
Three benzodiazepines that are metabolized only by Phase II conjugation and therefore is useful in elderly patients
Lorazepam, oxazepam, and temazepam
Two benzodiazepines that have active metabolites with long half-lives
diazepam, chlordiazepoxide
Clinical uses of benzodiazepines (5)
Anxiety, insomnia, alcohol detoxification, status epilepticus, spasticity
Reason why benzodiazepines are safer than barbiturates
Benzodiazepines do not directly activate GABAA
Mechanism of action of barbiturates
Increase duration of GABAA chloride channel opening
Most serious side effects of barbiturates (2)
Respiratory and cardiovascular depression
Barbiturates may precipitate this hematologic condition
porphyria
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetic property
induce CYP450
Effect of benzodiazepines and barbiturates on sleep architecture
suppress REM
Three nonbenzodiazepine hypnotics that lack suppressive effect on REM and are preferred over benzodiazepines for the treatment of insomnia
Zolpidem, zaleplon, eszopiclone
Mechanism of action of zolpidem
Activates BZ1 subtype of GABAA receptor
Drug of choice for treatment of acute status epilepticus
benzodiazepine
Drug of choice for partial seizures
carbamazepine
Antiepileptic drug used as first line for trigeminal neuralgia
carbamazepine
Antiepileptic drug that can induce CYP450, is teratogenic, and can cause diplopia, ataxia, and blood dyscrasias; follows first order kinetics of elimination
crbamazepine
Drugs of choice for generalized tonic-clonic seizures
Carbamazepine, phenytoin, valproic acid
Mechanism of action of Phenytoin, Carbamazepine, Lamotrigine
blocks sodium channels
Antiepileptic agent that exhibits zero-order kinetics, causes fetal hydantoin syndrome, and induces CYP450
phenytoin
Side effects of phenytoin (4)
Gingival hyperplasia, nystagmus, diplopia and ataxia
Anticonvulsant used for absence seizures; also used to treat: bipolar disorder, myoclonic siezures and as migraine prophylaxis
valproic acid
Antiepileptic drug that can cause fatal hepatotoxicity and neural tube defects
valproic acid
Drug of choice for absence seizures
ethosuximide
Mechanism of action of Ethosuximide
Blocks T-type calcium channels
Antiepileptic drugs that may also be used for bipolar disorder (3)
Valproic acid, carbamazepine, lamotrigine
Antiepileptic drug used also for pain of neuropathic origin
gabapentin
Serious side effect of lamotrigine that makes it require slow titration
stevens-johnson syndrome
Mechanism of action of opioids on analgesia
activate mu receptors
Side effects of these drugs include nausea and vomiting, euphoria, dependence, tolerance, sedation, respiratory depression, constipation
opioids
Tolerance to all effects of opioid agonists can develop except (2)
miosis, constipation
Strong opioid agonists (4)
Morphine, methadone, meperidine, and fentanyl
Opioids used in anesthesia (2)
Morphine and fentanyl
Opioid that can be given PO, IV, IM, and intrathecal to relieve anxiety associated with pulmonary edema
morphine
Opioid available trans-dermally
fentanyl
Opioid with antimuscarinic activity
meperidine
Long-acting opioids used in the management of withdrawal states (2)
methadone, buprenorphine
Opioid that can cause hyperpyrexic coma with MAOI and serotonin syndrome with SSRI
meperidine
Moderate opioid agonists (3)
codeine, hydrocodone, oxycodone
Partial opioid agonist that has a long duration of action and is resistant to naloxone reversal
buprenorphine
Opioid antagonist that is given IV
naloxone
Opioid antagonist that is given orally
naltrexone
Opioids indicated for use as antitussive (2)
Dextromethorphan, Codeine
Opioids indicated for use as antidiarrheal (2)
Diphenoxylate, Loperamide
Directly proportional to the potency of inhalation anesthetics
lipid solubility
Inversely proportional to the potency of inhalation anesthetics
Minimal alveolar concentration (MAC)
Inversely proportional to the rate of induction and recovery of inhalation anesthetics
Blood:gas partition coefficient
Mechanism of action of inhalation anesthetics
Potentiation of GABA at GABAA receptors; also reduce Na and Ca influx
Currently the only non-halogenated inhalation anesthetic
Nitrous oxide
Inhalation anesthetic with the most analgesic activity
nitrous oxide
Inhalation anesthetic with the least respiratory and cardiovascular depression and therefore is used frequently as a component of balanced anesthesia
nitrous oxide
Inhalation anesthetic that can cause fatal hepatotoxicity and cardiac arrhythmia and is no longer used in the US
halothane
Inhalation anesthetic that is withdrawn from the market due to fatal nephrotoxicity
Methoxyflurane
Inhalation anesthetic that at high concentrations can produce CNS excitation, leading to seizures
enflurane