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374 Cards in this Set
- Front
- Back
|
Common side effect of hypnotic agents
|
Sedation
|
|
|
Occurs when sedative hypnotics are used chronically or at high doses
|
Tolerance
|
|
|
The most common type of drug interaction of sedative hypnotics with other depressant medications
|
Additive CNS depression
|
|
|
Major effect of benzodiazepines on sleep at high doses
|
REM is decreased
|
|
|
Neurologic SE of benzodiazepines
|
Anterograde amnesia
|
|
|
Reason benzos are used cautiously in pregnancy
|
Ability to cross the placenta
|
|
|
Main route of metabolism for benzodiazepines
|
Hepatic
|
|
|
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
|
Lorazepam, oxazepam, and temazepam
|
|
|
MOA for benzodiazepines
|
increase the FREQUENCY of GABA-mediated chloride ion channel opening
|
|
|
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
|
Flumazenil
|
|
|
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
|
Diazepam
|
|
|
Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
|
Clonazepam
|
|
|
Benzodiazepines that are the most effective in the treatment of panic disorder
|
Alprazolam and Clonazepam
|
|
|
Benzodiazepine that is used for anesthesia
|
Midazolam
|
|
|
DOC for status epilepticus
|
Diazepam
|
|
|
Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
|
Chlordiazepoxide and Diazepam
|
|
|
Agents having active metabolites, long half lives, and a high incidence of adverse effects
|
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
|
|
|
Barbiturates may precipitate this hematologic condition
|
Acute intermittent porphyria
|
|
|
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
|
Liver enzyme INDUCTION
|
|
|
Barbiturates MOA
|
Increase the DURATION of GABA-mediated chloride ion channels
|
|
|
Barbiturate used for the induction of anesthesia
|
Thiopental
|
|
|
Important drug interaction with chloral hydrate
|
May displace coumadin from plasma proteins
|
|
|
Site of action for zaleplon and zolpidem
|
Benzodiazepine receptor BZ1 (although are not considered benzodiazepines)
|
|
|
Good hypnotic activity with less CNS SE than most benzodiazepines
|
Zolpidem, zaleplon
|
|
|
Agent that is a partial agonist for the 5-HT1A receptor
|
Buspirone
|
|
|
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
|
Buspirone
|
|
|
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
|
Ethanol
|
|
|
Agent with zero-order kinetics
|
Ethanol
|
|
|
Rate limiting step of alcohol metabolism
|
Aldehyde dehydrogenase
|
|
|
System that increases in activity with chronic exposure and may contribute to tolerance
|
MEOS
|
|
|
Agent that metabolize acetaldehyde to acetate
|
Aldehyde dehydrogenase
|
|
|
Agents that inhibit alcohol dehydrogenase
|
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
|
|
|
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
|
Disulfiram
|
|
|
The most common neurologic abnormality in chronic alcoholics
|
Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
|
|
|
Agent that is teratogen and causes a fetal syndrome
|
Alcohol
|
|
|
Agent that is the antidote for methanol overdose
|
Alcohol
|
|
|
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
|
Fomepizole
|
|
|
Most frequent route of metabolism
|
Hepatic enzymes
|
|
|
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
|
Sodium blockade
|
|
|
MOA for benzodiazepines and barbiturates
|
GABA-related targets
|
|
|
MOA for Ethosuximide
|
Calcium channels
|
|
|
MOA for Valproic acid at high doses
|
Affect calcium, potassium, and sodium channels
|
|
|
Drugs of choice for generalized tonic-clonic and partial seizures
|
Valproic acid and Phenytoin
|
|
|
DOC for febrile seizures
|
Phenobarbital
|
|
|
Drugs of choice for absence seizures
|
Ethosuximide and valproic acid
|
|
|
Drug of choice for myoclonic seizures
|
Valproic acid
|
|
|
Drugs of choice for status epilepticus
|
IV diazepam or phenytoin (for prolonged therapy not acute)
|
|
|
Drugs that can be used for infantile spasms
|
Corticosteroids
|
|
|
Anti-seizure drugs used also for bipolar affective disorder (BAD)
|
Valproic acid, carbamazepine, phenytoin and gabapentin
|
|
|
Anti-seizure drugs used also for Trigeminal neuralgia
|
Carbamazepine
|
|
|
Anti-seizure drugs used also for pain of neuropathic orgin
|
Gabapentin
|
|
|
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
|
Phenytoin
|
|
|
SE of phenytoin
|
Gingival hyperplasia, nystagmus, diplopia and ataxia
|
|
|
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida
|
Carbamazepine
|
|
|
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
|
Valproic acid
|
|
|
Laboratory value required to be monitored for patients on valproic acid
|
Serum ammonia and LFT's
|
|
|
SE for Lamotrigine
|
Stevens-Johnson syndrome
|
|
|
SE for Felbamate
|
Aplastic anemia and acute hepatic failure
|
|
|
Anti-seizure medication also used in the prevention of migraines
|
Valproic acid
|
|
|
Carbamazepine may cause
|
Agranulocytosis
|
|
|
Anti-seizure drugs used as alternative drugs for mood stabilization
|
Carbamazepine, gabapentin, lamotrigine, and valproic acid
|
|
|
MOA of general anesthetics
|
Unclear, thought to increase the threshold for firing of CNS neurons
|
|
|
Inhaled anesthetic with a low blood/gas partition coefficient
|
Nitrous oxide
|
|
|
Inversely related to potency of anesthetics
|
Minimum alveolar anesthetic concentration (MAC)
|
|
|
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
|
Halothane and methoxyflurane
|
|
|
Most inhaled anesthetics SE
|
Decrease arterial blood pressure
|
|
|
Inhaled anesthetics are myocardial depressants
|
Enflurane and halothane
|
|
|
Inhaled anesthetic causes peripheral vasodilation
|
Isoflurane
|
|
|
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
|
Halothane
|
|
|
Inhaled anesthetics, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
|
Nitrous oxide
|
|
|
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
|
Methoxyflurane
|
|
|
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
|
Nitrous oxide
|
|
|
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
|
Desflurane
|
|
|
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
|
Dantrolene
|
|
|
IV barbiturate used as a pre-op anesthetic
|
Thiopental
|
|
|
Benzodiazepine used adjunctively in anesthesia
|
Midazolam
|
|
|
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
|
Flumazenil
|
|
|
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
|
Ketamine
|
|
|
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
|
Fentanyl
|
|
|
State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
|
Neuroleptanesthesia
|
|
|
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
|
Propofol
|
|
|
MOA of local anesthetics (LA's)
|
Block voltage-dependent sodium channels
|
|
|
This may enhance activity of local anesthetics
|
Hyperkalemia
|
|
|
This may antagonize activity of local anesthetics
|
Hypercalcemia
|
|
|
Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity
|
Vasodilation
|
|
|
Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery
|
Cocaine
|
|
|
Longer acting local anesthetics which are less dependent on vasoconstrictors
|
Tetracaine and bupivacaine
|
|
|
These LA's have surface activity
|
Cocaine and benzocaine
|
|
|
Most important toxic effects of most local anesthetics
|
CNS toxicity
|
|
|
Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction
|
Cocaine
|
|
|
LA causing methemoglobinemia
|
Prilocaine
|
|
|
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
|
Neuromuscular blocking drugs
|
|
|
These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
|
Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
|
|
|
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)
|
Nondepolarizing type antagonists
|
|
|
Agent with long duration of action and is sost likely to cause histamine release
|
Tubocurarine
|
|
|
Non-depolarizing antagonist has short duration
|
Mivacurium
|
|
|
Agent can blocking muscarinic receptors
|
Pancuronium
|
|
|
Agent undergoing Hofmann elimination (breaking down spontaneously)
|
Atracurium
|
|
|
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, xcuses muscle pain postoperatively and myoglobinuria may occur
|
Succinylcholine
|
|
|
During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
|
Cholinesterase inhibitors
|
|
|
Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
|
Spasmolytic drugs
|
|
|
Facilitates GABA presynaptic inhibition
|
Diazepam
|
|
|
GABA agonist in the spinal cord
|
Baclofen
|
|
|
Similar to clonidine and may cause hypotension
|
Tizanidine
|
|
|
DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
|
Dantrolene
|
|
|
Agent used for acute muscle spasm
|
Cyclobenzaprine
|
|
|
Antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible
|
Drug induced Parkinsonism
|
|
|
Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
|
L-dopa
|
|
|
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)
|
Carbidopa
|
|
|
Clinical response that may fluctuate in tx of Parkinson's dx
|
"On-off-phenomenon"
|
|
|
Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
|
Levodopa
|
|
|
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
|
Bromocriptine
|
|
|
Non ergot agents used as first-line therapy in the initial management of Parkinson's
|
Pramipexole and ropinirole
|
|
|
Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis
|
Amantadine
|
|
|
Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt's
|
Selegiline
|
|
|
Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
|
Entacapone and Tolcapone
|
|
|
Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
|
Benztropine
|
|
|
Agent effective in physiologic and essential tremor
|
Propranolol
|
|
|
Agents used in Huntington's Disease
|
Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic)
|
|
|
Agents used in Tourette's dx
|
Haloperidol or pimozide
|
|
|
Chelating agent used in Wilson's disease
|
Penicillamine
|
|
|
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
|
Older antipsychotic agents, D2 receptors
|
|
|
Side effects occuring in antipsychotics that block dopamine
|
Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
|
|
|
Antipsychotics that reduce positive symptoms only
|
Older antipsychotics
|
|
|
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
|
Olanzapine, aripiprazole, and sertindole
|
|
|
Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
|
Risperidone
|
|
|
Atypical antipsychotic causing high prolactin levels
|
Risperidone
|
|
|
Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes
|
Olanzapine
|
|
|
Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker
|
Haloperidol
|
|
|
Drug used in neuroleptic malignant syndrome
|
Dantrolene
|
|
|
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
|
Muscarinic blockers
|
|
|
Antipsychotic having the strongest autonomic effects
|
Thioridazine
|
|
|
Antipsychotic having the weakest autonomic effects
|
Haloperidol
|
|
|
Antipsychotic that does not block muscarinic or histamine receptors, and it prolongs the QT interval
|
Sertindole
|
|
|
Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias
|
Thioridazine
|
|
|
Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause agranulocytosis
|
Clozapine
|
|
|
Anti-psychotic not shown to cause tardive dyskinesia
|
Clozapine
|
|
|
Anti-psychotics available in depot preparation
|
Fluphenazine and haloperidol
|
|
|
Reduced seizure threshold
|
Low-potency typical antipsychotics and clozapine
|
|
|
Orthostatic hypotension and QT prolongation
|
Low potency and risperidone
|
|
|
Increased risk of developing cataracts
|
Quetiapine
|
|
|
Major route of elimination for Lithium
|
Kidneys
|
|
|
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
|
Lithium toxicity
|
|
|
Common side effect of hypnotic agents
|
Sedation
|
|
|
Occurs when sedative hypnotics are used chronically or at high doses
|
Tolerance
|
|
|
The most common type of drug interaction of sedative hypnotics with other depressant medications
|
Additive CNS depression
|
|
|
Major effect of benzodiazepines on sleep at high doses
|
REM is decreased
|
|
|
Neurologic SE of benzodiazepines
|
Anterograde amnesia
|
|
|
Reason benzos are used cautiously in pregnancy
|
Ability to cross the placenta
|
|
|
Main route of metabolism for benzodiazepines
|
Hepatic
|
|
|
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
|
Lorazepam, oxazepam, and temazepam
|
|
|
MOA for benzodiazepines
|
increase the FREQUENCY of GABA-mediated chloride ion channel opening
|
|
|
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
|
Flumazenil
|
|
|
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
|
Diazepam
|
|
|
Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
|
Clonazepam
|
|
|
Benzodiazepines that are the most effective in the treatment of panic disorder
|
Alprazolam and Clonazepam
|
|
|
Benzodiazepine that is used for anesthesia
|
Midazolam
|
|
|
DOC for status epilepticus
|
Diazepam
|
|
|
Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
|
Chlordiazepoxide and Diazepam
|
|
|
Agents having active metabolites, long half lives, and a high incidence of adverse effects
|
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
|
|
|
Barbiturates may precipitate this hematologic condition
|
Acute intermittent porphyria
|
|
|
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
|
Liver enzyme INDUCTION
|
|
|
Barbiturates MOA
|
Increase the DURATION of GABA-mediated chloride ion channels
|
|
|
Barbiturate used for the induction of anesthesia
|
Thiopental
|
|
|
Important drug interaction with chloral hydrate
|
May displace coumadin from plasma proteins
|
|
|
Site of action for zaleplon and zolpidem
|
Benzodiazepine receptor BZ1 (although are not considered benzodiazepines)
|
|
|
Good hypnotic activity with less CNS SE than most benzodiazepines
|
Zolpidem, zaleplon
|
|
|
Agent that is a partial agonist for the 5-HT1A receptor
|
Buspirone
|
|
|
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
|
Buspirone
|
|
|
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
|
Ethanol
|
|
|
Agent with zero-order kinetics
|
Ethanol
|
|
|
Rate limiting step of alcohol metabolism
|
Aldehyde dehydrogenase
|
|
|
System that increases in activity with chronic exposure and may contribute to tolerance
|
MEOS
|
|
|
|
|
|
|
Agent that metabolize acetaldehyde to acetate
|
Aldehyde dehydrogenase
|
|
|
Agents that inhibit alcohol dehydrogenase
|
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
|
|
|
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
|
Disulfiram
|
|
|
The most common neurologic abnormality in chronic alcoholics
|
Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
|
|
|
Agent that is teratogen and causes a fetal syndrome
|
Alcohol
|
|
|
Agent that is the antidote for methanol overdose
|
Alcohol
|
|
|
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
|
Fomepizole
|
|
|
Most frequent route of metabolism
|
Hepatic enzymes
|
|
|
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
|
Sodium blockade
|
|
|
MOA for benzodiazepines and barbiturates
|
GABA-related targets
|
|
|
MOA for Ethosuximide
|
Calcium channels
|
|
|
MOA for Valproic acid at high doses
|
Affect calcium, potassium, and sodium channels
|
|
|
Drugs of choice for generalized tonic-clonic and partial seizures
|
Valproic acid and Phenytoin
|
|
|
DOC for febrile seizures
|
Phenobarbital
|
|
|
Drugs of choice for absence seizures
|
Ethosuximide and valproic acid
|
|
|
Drug of choice for myoclonic seizures
|
Valproic acid
|
|
|
Drugs of choice for status epilepticus
|
IV diazepam or phenytoin (for prolonged therapy not acute)
|
|
|
Drugs that can be used for infantile spasms
|
Corticosteroids
|
|
|
Anti-seizure drugs used also for bipolar affective disorder (BAD)
|
Valproic acid, carbamazepine, phenytoin and gabapentin
|
|
|
|
|
|
|
Anti-seizure drugs used also for Trigeminal neuralgia
|
Carbamazepine
|
|
|
|
|
|
|
Anti-seizure drugs used also for pain of neuropathic orgin
|
Gabapentin
|
|
|
|
|
|
|
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
|
Phenytoin
|
|
|
|
|
|
|
SE of phenytoin
|
Gingival hyperplasia, nystagmus, diplopia and ataxia
|
|
|
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida
|
Carbamazepine
|
|
|
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
|
Valproic acid
|
|
|
Laboratory value required to be monitored for patients on valproic acid
|
Serum ammonia and LFT's
|
|
|
SE for Lamotrigine
|
Stevens-Johnson syndrome
|
|
|
SE for Felbamate
|
Aplastic anemia and acute hepatic failure
|
|
|
Anti-seizure medication also used in the prevention of migraines
|
Valproic acid
|
|
|
Carbamazepine may cause
|
Agranulocytosis
|
|
|
Anti-seizure drugs used as alternative drugs for mood stabilization
|
Carbamazepine, gabapentin, lamotrigine, and valproic acid
|
|
|
MOA of general anesthetics
|
Unclear, thought to increase the threshold for firing of CNS neurons
|
|
|
Inhaled anesthetic with a low blood/gas partition coefficient
|
Nitrous oxide
|
|
|
Inversely related to potency of anesthetics
|
Minimum alveolar anesthetic concentration (MAC)
|
|
|
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
|
Halothane and methoxyflurane
|
|
|
Most inhaled anesthetics SE
|
Decrease arterial blood pressure
|
|
|
Inhaled anesthetics are myocardial depressants
|
Enflurane and halothane
|
|
|
Inhaled anesthetic causes peripheral vasodilation
|
Isoflurane
|
|
|
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
|
Halothane
|
|
|
Inhaled anesthetics, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
|
Nitrous oxide
|
|
|
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
|
Methoxyflurane
|
|
|
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
|
Nitrous oxide
|
|
|
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
|
Desflurane
|
|
|
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
|
Dantrolene
|
|
|
IV barbiturate used as a pre-op anesthetic
|
Thiopental
|
|
|
Benzodiazepine used adjunctively in anesthesia
|
Midazolam
|
|
|
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
|
Flumazenil
|
|
|
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
|
Ketamine
|
|
|
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
|
Fentanyl
|
|
|
State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
|
Neuroleptanesthesia
|
|
|
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
|
Propofol
|
|
|
MOA of local anesthetics (LA's)
|
Block voltage-dependent sodium channels
|
|
|
This may enhance activity of local anesthetics
|
Hyperkalemia
|
|
|
This may antagonize activity of local anesthetics
|
Hypercalcemia
|
|
|
Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity
|
Vasodilation
|
|
|
Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery
|
Cocaine
|
|
|
Longer acting local anesthetics which are less dependent on vasoconstrictors
|
Tetracaine and bupivacaine
|
|
|
These LA's have surface activity
|
Cocaine and benzocaine
|
|
|
Most important toxic effects of most local anesthetics
|
CNS toxicity
|
|
|
Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction
|
Cocaine
|
|
|
LA causing methemoglobinemia
|
Prilocaine
|
|
|
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
|
Neuromuscular blocking drugs
|
|
|
These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
|
Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
|
|
|
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)
|
Nondepolarizing type antagonists
|
|
|
Agent with long duration of action and is sost likely to cause histamine release
|
Tubocurarine
|
|
|
Non-depolarizing antagonist has short duration
|
Mivacurium
|
|
|
Agent can blocking muscarinic receptors
|
Pancuronium
|
|
|
Agent undergoing Hofmann elimination (breaking down spontaneously)
|
Atracurium
|
|
|
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, xcuses muscle pain postoperatively and myoglobinuria may occur
|
Succinylcholine
|
|
|
During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
|
Cholinesterase inhibitors
|
|
|
Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
|
Spasmolytic drugs
|
|
|
Facilitates GABA presynaptic inhibition
|
Diazepam
|
|
|
GABA agonist in the spinal cord
|
Baclofen
|
|
|
Similar to clonidine and may cause hypotension
|
Tizanidine
|
|
|
DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
|
Dantrolene
|
|
|
Agent used for acute muscle spasm
|
Cyclobenzaprine
|
|
|
Antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible
|
Drug induced Parkinsonism
|
|
|
Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
|
L-dopa
|
|
|
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)
|
Carbidopa
|
|
|
Clinical response that may fluctuate in tx of Parkinson's dx
|
"On-off-phenomenon"
|
|
|
Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
|
Levodopa
|
|
|
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
|
Bromocriptine
|
|
|
Non ergot agents used as first-line therapy in the initial management of Parkinson's
|
Pramipexole and ropinirole
|
|
|
Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis
|
Amantadine
|
|
|
Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt's
|
Selegiline
|
|
|
Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
|
Entacapone and Tolcapone
|
|
|
Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
|
Benztropine
|
|
|
Agent effective in physiologic and essential tremor
|
Propranolol
|
|
|
Agents used in Huntington's Disease
|
Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic)
|
|
|
Agents used in Tourette's dx
|
Haloperidol or pimozide
|
|
|
Chelating agent used in Wilson's disease
|
Penicillamine
|
|
|
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
|
Older antipsychotic agents, D2 receptors
|
|
|
Side effects occuring in antipsychotics that block dopamine
|
Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
|
|
|
Antipsychotics that reduce positive symptoms only
|
Older antipsychotics
|
|
|
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
|
Olanzapine, aripiprazole, and sertindole
|
|
|
Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
|
Risperidone
|
|
|
Atypical antipsychotic causing high prolactin levels
|
Risperidone
|
|
|
Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes
|
Olanzapine
|
|
|
Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker
|
Haloperidol
|
|
|
Drug used in neuroleptic malignant syndrome
|
Dantrolene
|
|
|
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
|
Muscarinic blockers
|
|
|
Antipsychotic having the strongest autonomic effects
|
Thioridazine
|
|
|
Antipsychotic having the weakest autonomic effects
|
Haloperidol
|
|
|
Antipsychotic that does not block muscarinic or histamine receptors, and it prolongs the QT interval
|
Sertindole
|
|
|
Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias
|
Thioridazine
|
|
|
Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause agranulocytosis
|
Clozapine
|
|
|
Anti-psychotic not shown to cause tardive dyskinesia
|
Clozapine
|
|
|
Anti-psychotics available in depot preparation
|
Fluphenazine and haloperidol
|
|
|
Reduced seizure threshold
|
Low-potency typical antipsychotics and clozapine
|
|
|
Orthostatic hypotension and QT prolongation
|
Low potency and risperidone
|
|
|
Increased risk of developing cataracts
|
Quetiapine
|
|
|
Major route of elimination for Lithium
|
Kidneys
|
|
|
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
|
Lithium toxicity
|
|
|
Drug increases the renal clearance hence decreases levels of lithium
|
Theophylline
|
|
|
Lithium is associated with this congenital defect
|
Cardiac anomalies and is contraindicated in pregnancy or lactation
|
|
|
DOC for bipolar affective disorder
|
Lithium
|
|
|
SE of lithium
|
Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
|
|
|
Example of three antidepressants that are indicated for obsessive compulsive disorder
|
Clomipramine, fluoxetine and fluvoxamine
|
|
|
Neurotransmitters affected by the action of antidepressants
|
Norepinephrine and serotonin
|
|
|
Usual time needed for full effect of antidepressant therapy
|
2 to 3 weeks
|
|
|
Population group especially sensitive to side effects of antidepressants
|
Elderly patients
|
|
|
All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion
|
Side-effect profile and prior pt response
|
|
|
Well-tolerated and are first-line antidepressants
|
SSRI's, bupropion, and venlafaxine
|
|
|
Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression
|
Monamine oxidase inhibitors
|
|
|
Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)
|
Hypertensive crisis
|
|
|
MAOI should not be administered with SSRI's or potent TCA's due to development of this condition
|
Serotonin syndrome
|
|
|
Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly
|
Tricyclic antidepressants (TCA)
|
|
|
Three C's associated with TCA toxicity
|
Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)
|
|
|
Agents having higher sedation and antimuscarinic effects than other TCA's
|
Tertiary amines
|
|
|
TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects
|
Amitriptyline
|
|
|
TCA used in chronic pain, enuresis, and ADD
|
Imipramine
|
|
|
TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep
|
Doxepin
|
|
|
TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms
|
Clomipramine
|
|
|
Secondary amines that have less sedation and more excitation effect
|
Nortriptyline, Desipramine
|
|
|
Antidepressant associated with neuroleptic malignant syndrome
|
Amoxapine
|
|
|
Antidepressant associated with seizures and cardiotoxicity
|
Maprotiline
|
|
|
Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure
|
Venlafaxine
|
|
|
Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake
|
Venlafaxine
|
|
|
Antidepressant also used for sleep that causes priapism
|
Trazodone
|
|
|
Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure
|
Nefazodone
|
|
|
Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures
|
Bupropion
|
|
|
Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating
|
Mirtazapine
|
|
|
SE of mirtazapine
|
Liver toxicity, increased serum cholesterol
|
|
|
Except for these agents all SSRI have significant inhibition of CytP450 enzymes
|
Citalopram and its metabolite escitalopram
|
|
|
SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx
|
Fluoxetine
|
|
|
SSRI indicated for premenstrual dysphoric disorder
|
Fluoxetine (Sarafem)
|
|
|
Some of SSRIs' therapeutic effects beside depression
|
Panic attacks, social phobias, bulimia nervosa, and PMDD premenstrual dysphoric disorder), OCD
|
|
|
SSRI's less likely to cause a withdrawal syndrome
|
Fluoxetine
|
|
|
Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
|
Ascending pathways
|
|
|
Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
|
Presynaptic mu, delta, and kappa receptors
|
|
|
Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
|
Postsynaptic Mu receptors
|
|
|
Tolerance to all effects of opioid agonists can develop except
|
Miosis and constipation
|
|
|
All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
|
Meperidine
|
|
|
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
|
Opioid Analgesics
|
|
|
Strong opioid agonists
|
Morphine, methadone, meperidine, and fentanyl
|
|
|
Opioids used in anesthesia
|
Morphine and fentanyl
|
|
|
Opioid used in the management of withdrawal states
|
Methadone
|
|
|
Opioid available trans-dermally
|
Fentanyl
|
|
|
Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
|
Morphine
|
|
|
Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome
|
Meperidine
|
|
|
Moderate opioid agonists
|
Codeine, hydrocodone, and oxycodone
|
|
|
Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures
|
Propoxyphene
|
|
|
Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal
|
Buprenorphine
|
|
|
Opioid antagonist that is given IV and had short DOA
|
Naloxone
|
|
|
Opioid antagonist that is given orally in alcohol dependency programs
|
Naltrexone
|
|
|
These agents are used as antitussive
|
Dextromethorphan, Codeine
|
|
|
These agents are used as antidiarrheal
|
Diphenoxylate, Loperamide
|
|
|
Inhalant anesthetics
|
NO, chloroform, and diethyl ether
|
|
|
Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation
|
Fluorocarbons and Industrial solvents
|
|
|
Cause dizziness, tachycardia, hypotension, and flushing
|
Organic nitrites
|
|
|
Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression
|
Steroids
|
|
|
Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
|
Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
|
|
|
Most commonly abused in health care professionals
|
Heroin, morphine, oxycodone, meperidine and fentanyl
|
|
|
This route is associated with rapid tolerance and psychologic dependence
|
IV administration
|
|
|
Leads to respiratory depression progressing to coma and death
|
Overdose of opioids
|
|
|
Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome
|
Abstinence syndrome
|
|
|
Treatment for opioid addiction
|
Methadone, followed by slow dose reduction
|
|
|
This agent may cause more severe, rapid and intense symptoms to a recovering addict
|
Naloxone
|
|
|
Sedative-Hypnotics action
|
Reduce inhibition, suppress anxiety, and produce relaxation
|
|
|
Additive effects when Sedative-Hypnotics used in combination with these agents
|
CNS depressants
|
|
|
Common mechanism by which overdose result in death
|
Depression of medullary and cardiovascular centers
|
|
|
"Date rape drug"
|
Flunitrazepam (rohypnol)
|
|
|
The most important sign of withdrawal syndrome
|
Excessive CNS stimulation (seizures)
|
|
|
Treatment of withdrawal syndrome involves
|
Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
|
|
|
These agents are CNS depressants
|
Ethanol, Barbiturates, and Benzodiazepines
|
|
|
Withdrawal from this drug causes lethargy, irritability, and headache
|
Caffeine
|
|
|
W/D from this drug causes anxiety and mental discomfort
|
Nicotine
|
|
|
Treatments available for nicotine addiction
|
Patches, gum, nasal spray, psychotherapy, and bupropion
|
|
|
Chronic high dose abuse of nicotine leads to
|
Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures
|
|
|
Tolerance is marked and abstinence syndrome occurs
|
Amphetamines
|
|
|
Amphetamine agents
|
Dextroamphetamines and methamphetamine
|
|
|
These agents are congeners of Amphetamine
|
DOM, STP, MDA, and MDMA "ecstasy"
|
|
|
Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)
|
Cocaine "super-speed"
|
|
|
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
|
PCP
|
|
|
Removal of PCP may be aided
|
Urinary acidification and activated charcoal or continual nasogastric suction
|
|
|
THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur
|
Marijuana
|
