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
Rare, but fatal side effect associated with combination of halogenated inhalation anesthetic and depolarizing neuromuscular blocker
malignant hyperthermia
Close to ideal inhalation anesthetic that exhibits rapid and smooth induction and recovery, with little organ system toxicity
sevoflurane
Barbiturate used for the induction of anesthesia
thiopental
A short-acting benzodiazepine commonly used adjunctively with inhalation anesthetics and opioid analgesics for a balanced anesthesia
midazolam
Opioid safe for use of analgesia and anesthesia during cardiac surgery
fentanyl
Produces both rapid anesthesia and recovery, has antiemetic activity, but may cause marked hypotension
propofol
Produces dissociative anesthesia but has significant analgesic activity
ketamine
Mechanism of action of ketamine
block NMDA receptor
Side effects of dissociative anesthetic, ketamine (4)
Cardiovascular stimulation, increased cerebral blood flow, vivid dreams, hallucinations
Neuroleptanesthesia can be produced by a combination of these two agents
Fentanyl and droperidol
Mechanism of action of local anesthetics
Block voltage-gated sodium channels
This condition(environment) may necessitate larger doses of local anesthetics because the drugs become ionized and cannot penetrate the neuronal membranes
low pH
Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors to prolong activity
vasodilation
The only local anesthetic with vasoconstrictive property, but due to abuse potential, only occasionally used for nasal surgery
cocaine
This type of local anesthetic is more likely to cause hypersensitivity reactions
Ester-type (local anesthetic with one “I” in name)
Local anesthetic most widely used for obstetric anesthesia but causes the most cardiac depression
Bupivacaine
Side effect of most local anesthetics
CNS excitation
Common side effect of antipsychotics, MPTP (contaminant in illicit meperidine analog), and cholinergic excess
drug-induced parkinsonism
Precursor of dopamine that can cross the blood-brain-barrier and used to alleviate motor dysfunction in Parkinson’s disease
levodopa (L-dopa)
Inhibits peripheral DOPA decarboxylase, reduces peripheral side effects of dopamine precursor and enhances its delivery to the brain
carbidopa
Two fluctuations in clinical response associated with long-term use of dopamine precursor
“Wearing off” and “on-off-phenomenon”
Inhibits monoamine oxidase type B (MAO-B), used as monotherapy for early or mild Parkinson’s disease or adjunct to improve motor function in patients with fluctuations in clinical response
Selegiline
Inhibits of catechol-O-methyltransferase (COMT), used as adjunct to improve motor function in Parkinson’s patients with fluctuations in clinical response
Entacapone, tolcapone
Ergot type 2 dopamine receptor (D2) agonist, used as adjunct to improve motor function in Parkinson’s patients with fluctuations in clinical response
bromocriptine
Non ergot type 2 dopamine receptors (D2) agonist, used for Parkinson’s and restless legs syndrome
Pramipexole and ropinirole
An antiviral that enhances dopamine release from nigrostriatal neurons
amantadine
A centrally-acting anticholinergics useful for tremor and rigidity but have little effect on bradykinesia in patients with Parkinson’s
benztropine
Drug of choice indicated for familial or essential tremors
propranolol
Two drugs that inhibit vesicle monoamine transporter used for Huntington’s
tetrabenazine, resrpine
An antipsychotic with dopamine receptor antagonist activity used for Huntington’s
haloperidol
Three centrally-acting cholinesterase inhibitors used for Alzheimer’s
Donepezil, rivastigmine, galantamine
Noncompetitive antagonist of NMDA receptors used for Alzheimer’s
memantine
Three main classes of CNS depressant drugs of abuse
alcohol, opioid, barbituates/benzodiazepine
Agent that is metabolized by alcohol dehydrogenase or microsomal ethanol-oxidizing system (MEOS) to acetaldehyde; displays zero-order kinetics of elimination
ethanol
Enzyme that is induced through chronic exposure to alcohol, may contribute to tolerance
microsomal ethanol oxidizing system (MEOS)
Complications of the gastrointestinal system associated with chronic alcohol use
Mallory-Weiss syndrome, hepatitis, cirrhosis, pancreatitis
Neurological abnormality caused by chronic alcohol use and thiamine deficiency
Wernicke-Korsakoff syndrome
The most common neurologic abnormality in chronic alcoholics
Neurologic deficits (Peripheral neuropathy)
Life-threatening alcohol withdrawal syndrome that peaks at 5 days after the last drink
delirium tremens
Inhibits aldehyde dehydrogenase and used as deterrent for alcohol use
disulfiram
Opioid receptor antagonist used to prevent alcohol abuse
naltrexone
Competes for alcohol dehydrogenase and is used in methanol or ethylene glycol poisoning
Fomepizole, ethanol
Most commonly abused opioids
Heroin, morphine, oxycodone
Respiratory and CNS depression, pinpoint pupils, seizures, and needle track marks are symptoms of this intoxication
opioid
Opioid receptor antagonist that is used to treat opioid intoxication, may cause more rapid and intense symptoms of withdrawal
naloxone
Opioids used for long-term maintenance from opioid withdrawal
methadone, buprenorphine
Most widely abused sedative hypnotics
short-acting barbiturates (pentobarbital)
Two date rape drugs that work through enhancement of GABA receptors in the brain
Flunitrazepam, GHB (γ-hydroxybutyrate)
Benzodiazepine antagonist used to treat benzodiazepine intoxication
flumazenil
Four major CNS stimulant drugs of abuse
Caffeine, nicotine, cocaine, amphetamines
Treatments available for nicotine addiction
Patch, gum, lozenge, bupropion, varenicline
CNS stimulant that acts by inhibiting reuptake of neurotransmitters; may cause pupil dilation, alter tactile sensation, irregular breathing, and cardiac toxicity
cocaine
Amphetamine derivatives commonly abused
Methamphetamine (crystal meth), MDMA (methylenedioxymeth-amphetamine, or ecstasy)
Drug of abuse that was developed as a dissociative anesthetic; intoxication leads to both horizontal and vertical nystagmus, analgesia, psychosis, delirium, and seizures
PCP (phencyclidine, or angel dust)
Synthetic ergot derivative that can produce perceptual hallucinations and used as an illicit drug; may cause paranoia
LSD (lysergic acid diethylamide)
Active ingredient is tetrahydrocannabinol (THC); side effects include impairment of judgment, altered sense of time, increased appetite, and hallucinations
marijuana
Use of all antipsychotic medication in this group of patients is associated with increased risk of deaths
Elderly with dementia-related psychosis
Antipsychotics that repress primarily the positive symptoms of schizophrenia
typical antipsychotics
Primary mechanism of action of typical antipsychotics
inhibits D2 receptors
Common endocrine side effects of all typical antipsychotic drugs
Hyperprolactinemia, galactorrhea
Two low potency, typical antipsychotic drugs
Chlorpromazine, thioridazine
Typical antipsychotic associated with retinopathy and cardiac toxicity
thioridazone
Common side effects of low potency typical antipsychotic drugs
Dry mouth (anticholinergic), sedation (antihistamine), hypotension (α1 block)
Three high potency, typical antipsychotic drugs
Haloperidol, fluphenazine, trifluoperazine
Typical antipsychotic that can also be used for Tourette syndrome
haloperidol
Side effects more commonly associated with high potency typical antipsychotic drugs
Dystonia, akathisia, bradykinesia, tardive dyskinesia (extrapyramidal symptoms)
Treatment for drug-induced acute extrapyramidal symptoms
Benztropine, diphenhydramine
Life-threatening side effect associated with typical antipsychotic drugs
Neuroleptic malignant syndrome
Treatment for drug-induced neuroleptic malignant syndrome
dantrolene
Advantage of atypical over typical antipsychotics
Less extrapyramidal symptoms, more effect against negative symptoms of schizophrenia
Primary mechanism of action of atypical antipsychotics
Inhibit 5-HT2 receptors
Atypical antipsychotic that can produce potentially fatal agranulocytosis and increase incidence of seizures
clozapine
Two atypical antipsychotics that can cause weight gain
Clozapine, olanzapine
Two atypical antipsychotics that can prolong the QT interval
Risperidone, ziprasidone
Atypical antipsychotic that can increase prolactin levels and cause gynecomastia and irregular menstruation in men and women, respectively
risperidone
Atypical antipsychotic that can also be used to treat irritability in autistic children
Aripiprazole
Tricyclic antidepressants
-iptyline, -ipramine, doxepin, amoxapine
Mechanism of action of tricyclic antidepressants
Block serotonin and norepinephrine reuptake
Common side effects of tricyclic antidepressants
Autonomic (block muscarinic and α1), sedation
Tricyclic secondary amines that produce less sedation and autonomic side effects (compared with tricyclic tertiary amines)
Nortriptyline, desipramine
Three life-threatening side effects associated with tricyclic antidepressants
convulsion, cardiotoxicity, coma (3 C’s)
Tricyclic antidepressant used for enuresis
imipramine
Tricyclic antidepressant used in obsessive compulsive disorder
clomipramine
Tricyclic antidepressant with antihistamine effect and is indicated for insomnia
doxepin
Class of antidepressants that has fewer sedative and autonomic side effects than tricyclic antidepressants and indicated for panic disorder, generalized anxiety disorder, social phobias, bulimia, obsessive compulsive behavior, and post-traumatic stress disorder
SSRI
Four selective serotonin reuptake inhibitors
Fluoxetine, paroxetine, sertraline, citalopram
Serious side effect of selective serotonin reuptake inhibitors when used with other drugs such as monoamine oxidase inhibitors, serotonin-norepinephrine reuptake inhibitors, or tricyclic antidepressants
serotonin syndrome
Two selective serotonin-norepinephrine reuptake inhibitors
Duloxetine, venlafaxine
Class of drugs that is most useful in patients with anxiety, hypochondriasis, and depression that is refractory to other antidepressants
monoamine oxidase inhibitors
Mechanism of action of isocarboxazid, phenelzine, and tranylcypromine
Irreversible inhibition of monoamine oxidase A and B
Mechanism of action of selegiline
Selectively inhibits monoamine oxidase B
A fatal condition that results from combination of monoamine oxidase inhibitors with tyramine-containing foods
Hypertensive crisis
Antidepressant that non-selectively inhibits neuronal reuptake; less likely to cause sedation, autonomic, cardiovascular, or sexual dysfunction; also used for smoking cessation
Bupropion
Antidepressant that inhibits serotonin reuptake but also antagonizes 5HT-2 receptors; causes priapism
trazodone
Antidepressant that inhibits alpha 2, 5HT-2, and 5HT-3 receptors to increase release of norepinephrine and serotonin
mirtazapine
First line drug for classic bipolar disorder with euphoric mania
lithium
Major route of elimination for Lithium
kidneys
Side effects of lithium (4)
Tremor, hypothyroidism, nephrogenic diabetes insipidus, fetal cardiac defects
