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167 Cards in this Set
- Front
- Back
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Common side effect of hypnotic agents |
Sedation
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Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog)
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Drug induced Parkinsonism
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Occurs when sedative hypnotics are used chronically or at high doses
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Tolerance
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Most frequent route of metabolism
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Hepatic enzymes
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The most common type of drug interaction of sedative hypnotics with other depressant medications
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Additive CNS depression
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Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
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L-dopa
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Benzodiazepines used to promote sleep
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Temazpam, trizolam, flurazepam
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MOA of general anesthetics
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Most are thought to act at GABA-A receptor - chloride channel
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Benzodiazepine used for anxiety
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Alprazolam
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This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)
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Carbidopa
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Non-benzodiazepine used as an anxiolytic
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Buspirone
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Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
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Sodium channel blockade
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Non-benzodiazepine used for sleep
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Zolpidem
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Clinical response that may fluctuate in tx of Parkinson's dx
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"On-off-phenomenon"
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Major effect of benzodiazepines on sleep at high doses
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REM is decreased
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Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
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Ascending pathways
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Neurologic SE of benzodiazepines
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Anterograde amnesia
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Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
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Levodopa
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Reason benzos are used cautiously in pregnancy
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Ability to cross the placenta
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MOA for benzodiazepines and barbiturates
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GABA-related targets
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Main route of metabolism for benzodiazepines
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Hepatic
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Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia
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Bromocriptine
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Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
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Lorazepam, oxazepam, and temazepam
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Inhaled anesthetic with a low blood/gas partition coefficient
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Nitrous oxide
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MOA for benzodiazepines
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increase the FREQUENCY of GABA-mediated chloride ion channel opening
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Non ergot agents used as first-line therapy in the initial management of Parkinson's
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Pramipexole and ropinirole
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Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
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Flumazenil
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MOA for Ethosuximide
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Calcium channels
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Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
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Diazepam
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Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis
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Amantadine
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Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
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Clonazepam
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Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction
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Pilocarpine, carbachol, physostigmine
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Benzodiazepines that are the most effective in the treatment of panic disorder
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Alprazolam and Clonazepam
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Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients
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Selegiline
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Benzodiazepine that is used for anesthesia
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Midazolam
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MOA for Valproic acid at high doses
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Affect calcium, potassium, and sodium channels
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DOC for status epilepticus
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Diazepam
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Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
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Entacapone and Tolcapone
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Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
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Chlordiazepoxide and Diazepam
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Inversely related to potency of anesthetics
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Minimum alveolar anesthetic concentration (MAC)
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Agents having active metabolites, long half lives, and a high incidence of adverse effects
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Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
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Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
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Benztropine
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Barbiturates may precipitate this hematologic condition
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Acute intermittent porphyria
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Drugs of choice for generalized tonic-clonic and partial seizures
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Valproic acid and Phenytoin
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Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
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Liver enzyme INDUCTION
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Agent effective in physiologic and essential tremor
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Propranolol
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Barbiturates MOA
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Increase the DURATION of GABA-mediated chloride ion channels
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Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
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Presynaptic mu, delta, and kappa receptors
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Barbiturate used for the induction of anesthesia
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Thiopental
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Agents used in Huntington's Disease
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Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic)
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Site of action for zaleplon and zolpidem
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Benzodiazepine receptor BZ1 (although are not considered benzodiazepines)
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DOC for febrile seizures
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Phenobarbital
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Good hypnotic activity with less CNS SE than most benzodiazepines
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Zolpidem, zaleplon
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Agents used in Tourette's dx
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Haloperidol or pimozide
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Agent that is a partial agonist for the 5-HT1A receptor
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Buspirone
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Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
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Halothane and methoxyflurane
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Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
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Buspirone
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Chelating agent used in Wilson's disease
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Penicillamine
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Drugs of choice for absence seizures
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Ethosuximide and valproic acid
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Inhalant anesthetics
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NO, chloroform, and diethyl ether
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Drug of choice for myoclonic seizures
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Valproic acid
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Most inhaled anesthetics SE
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Decrease arterial blood pressure
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Drugs of choice for status epilepticus
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IV diazepam for short term (acute) treatment; phenytoin for prolonged therapy
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Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
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Postsynaptic Mu receptors
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Drugs that can be used for infantile spasms
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Corticosteroids
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Inhaled anesthetics are myocardial depressants
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Enflurane and halothane
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Anti-seizure drugs used also for bipolar affective disorder (BAD)
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Valproic acid, carbamazepine, phenytoin and gabapentin
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Nonselective alpha agonists that increases outflow, probably via the uveoscleral veins
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Epinephrine, dipivefrin
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Anti-seizure drugs used also for Trigeminal neuralgia
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Carbamazepine
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Inhaled anesthetic causes peripheral vasodilation
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Isoflurane
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Anti-seizure drugs used also for pain of neuropathic origin
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Gabapentin
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Tolerance to all effects of opioid agonists can develop except
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Miosis and constipation
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Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
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Phenytoin
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Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
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Halothane
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SE of phenytoin
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Gingival hyperplasia, nystagmus, diplopia and ataxia
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Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation
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Fluorocarbons and Industrial solvents
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Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida
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Carbamazepine
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Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
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Nitrous oxide
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Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
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Valproic acid
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All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
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Meperidine
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Laboratory value required to be monitored for patients on valproic acid
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Serum ammonia and LFT's
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Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
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Methoxyflurane
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SE for Lamotrigine
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Stevens-Johnson syndrome
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Selective alpha agonists that decreases aqueous secretion
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Apraclonidine, brimonidine
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SE for Felbamate
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Aplastic anemia and acute hepatic failure
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Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
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Nitrous oxide
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Anti-seizure medication also used in the prevention of migraines
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Valproic acid
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SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone
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Opioid Analgesics
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Carbamazepine may cause
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Agranulocytosis
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Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
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Desflurane
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Anti-seizure drugs used as alternative drugs for mood stabilization
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Carbamazepine, gabapentin, lamotrigine, and valproic acid
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Cause dizziness, tachycardia, hypotension, and flushing
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Organic nitrites
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DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
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Dantrolene
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Strong opioid agonists
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Morphine, methadone, meperidine, and fentanyl
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IV barbiturate used as a pre-op anesthetic
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Thiopental
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These Beta blockers decrease aqueous secretion
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Timolol (nonselective), betaxolol (selective)
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Benzodiazepine used adjunctively in anesthesia
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Midazolam
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Opioids used in anesthesia
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Morphine and fentanyl
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Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
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Flumazenil
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Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression
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Steroids
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This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
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Ketamine
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Opioid used in the management of withdrawal states
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Methadone
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Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
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Fentanyl
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This diuretic decreases aqueous secretion due to lack of HCO3- ion. Causes drowsiness and paresthesias, alkalinization of the urine may precipitate calcium salts, hypokalemia, acidosis
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Acetazolamide
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State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
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Neuroleptanesthesia
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Opioid available trans-dermally
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Fentanyl
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Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
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Propofol
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Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
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Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
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MOA of local anesthetics (LA's)
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Block voltage-dependent sodium channels
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Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
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Morphine
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This may enhance activity of local anesthetics
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Hyperkalemia
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This agent cause increased aqueous outflow
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Prostaglandin PGF2a
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This may antagonize activity of local anesthetics
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Hypercalcemia
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Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome
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Meperidine
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Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity
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Vasodilation
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Most commonly abused in health care professionals
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Heroin, morphine, oxycodone, meperidine and fentanyl
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Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery
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Cocaine
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Moderate opioid agonists
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Codeine, hydrocodone, and oxycodone
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Longer acting local anesthetics which are less dependent on vasoconstrictors
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Tetracaine and bupivacaine
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This route is associated with rapid tolerance and psychologic dependence
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IV administration
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These LA's have surface activity
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Cocaine and benzocaine
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Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures
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Propoxyphene
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Most important toxic effects of most local anesthetics
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CNS toxicity
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Leads to respiratory depression progressing to coma and death
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Overdose of opioids
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Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction
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Cocaine
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Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal
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Buprenorphine
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LA causing methemoglobinemia
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Prilocaine
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Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome
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Abstinence syndrome
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Opioid antagonist that is given IV and had short DOA
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Naloxone
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Treatment for opioid addiction
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Methadone, followed by slow dose reduction
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Opioid antagonist that is given orally in alcohol dependency programs
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Naltrexone
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This agent may cause more severe, rapid and intense symptoms to a recovering addict
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Naloxone
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These agents are used as antitussive
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Dextromethorphan, Codeine
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Sedative-Hypnotics action
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Reduce inhibition, suppress anxiety, and produce relaxation
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These agents are used as antidiarrheal
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Diphenoxylate, Loperamide
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Additive effects when Sedative-Hypnotics used in combination with these agents
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CNS depressants
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Common mechanism by which overdose result in death
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Depression of medullary and cardiovascular centers
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"Date rape drug"
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Flunitrazepam (rohypnol)
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The most important sign of withdrawal syndrome
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Excessive CNS stimulation (seizures)
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Treatment of withdrawal syndrome involves
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Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
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These agents are CNS depressants
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Ethanol, Barbiturates, and Benzodiazepines
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Withdrawal from this drug causes lethargy, irritability, and headache
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Caffeine
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W/D from this drug causes anxiety and mental discomfort
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Nicotine
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Treatments available for nicotine addiction
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Patches, gum, nasal spray, psychotherapy, and bupropion
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Chronic high dose abuse of nicotine leads to
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Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures
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Tolerance is marked and abstinence syndrome occurs
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Amphetamines
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Amphetamine agents
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Dextroamphetamines and methamphetamine
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These agents are congeners of Amphetamine
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DOM, STP, MDA, and MDMA "ecstasy"
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Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)
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Cocaine "super-speed"
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Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of both horizontal and vertical nystagmus is pathognomonic
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PCP
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Removal of PCP may be aided
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Urinary acidification and activated charcoal or continual nasogastric suction
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THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur
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Marijuana
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Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation
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Neuromuscular blocking drugs
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These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
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Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
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These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)
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Nondepolarizing type antagonists
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Agent with long duration of action and most likely to cause histamine release
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Tubocurarine
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Non-depolarizing antagonist has short duration
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Mivacurium
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Agent can blocking muscarinic receptors
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Pancuronium
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Agent undergoing Hofmann elimination (breaking down spontaneously)
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Atracurium
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One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur
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Succinylcholine
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During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
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Cholinesterase inhibitors
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Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
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Spasmolytic drugs
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Facilitates GABA presynaptic inhibition
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Diazepam
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GABA agonist in the spinal cord
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Baclofen
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Similar to clonidine and may cause hypotension
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Tizanidine
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DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
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Dantrolene
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Agent used for acute muscle spasm
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Cyclobenzaprine
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