Pharm one-liners Flashcards
Common side effect of sedative hypnotics
CNS depression
Occurs when sedative hypnotics are used long-term
Tolerance and physical dependence
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
Anxiety, insomnia, alcohol detoxification, status epilepticus, spasticity
Reason why benzodiazepines are safer than barbiturates
Benzodiazepines work only in presence of GABA
Mechanism of action of barbiturates
Increase duration of GABAA chloride channel opening
Most serious side effects of barbiturates
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
Mechanism of action of opioids on analgesia
Activate mu receptors to 1. close presynaptic Ca2+ channels to inhibit neurotransmitter release, 2. open postsynaptic K+ channels to hyperpolarize cell membrane
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
Miosis, constipation
Strong opioid agonists
Morphine, methadone, meperidine, and fentanyl
Opioids used in anesthesia
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
Methadone, Buprenorphine
Opioid that can cause hyperpyrexic coma with MAOI and serotonin syndrome with SSRI
Meperidine
Moderate opioid agonists
Codeine, hydrocodone, and 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
Dextromethorphan, Codeine
Opioids indicated for use as antidiarrheal
Diphenoxylate, Loperamide
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
Two centrally-acting anticholinergics useful for tremor and rigidity but have little effect on bradykinesia in patients with Parkinson’s
Benztropine, Trihexylphenidyl
Drug of choice indicated for familial or essential tremors
Propranolol
Two drugs that inhibit vesicle monoamine transporter used for Huntington’s
Tetrabenazine, reserpine
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, barbiturate/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
Sweating, dilated pupils, piloerection, and flu-like symptoms are symptoms of withdrawal from this class of drugs
Opioid
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
