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Drug class of lorazepam
Benzodiazepine
Drug class of alprazolam
Benzodiazepine
Drug class of midazolam
Benzodiazepine
Drug class of zolpidem
Benzodiazepine receptor agonist (Z-drug)
Drug class of phenobarbital
Barbiturate
Primary neurotransmitter affected by benzodiazepines
GABA
Do benzodiazepines work without GABA present?
No, GABA must already be present.
Mechanism of benzodiazepines
Positive allosteric modulators of GABA-A receptors that increase chloride influx.
Effect of chloride entering neurons
Hyperpolarization and inhibition of neuronal firing.
Primary effect of GABA
Inhibitory neurotransmitter in the CNS.
Clinical use of alprazolam
Acute anxiety and panic attacks.
Clinical use of midazolam
Anesthesia and procedural sedation.
Clinical use of lorazepam
Status epilepticus and anxiety.
Clinical use of zolpidem
Insomnia.
Clinical use of phenobarbital
Status epilepticus and anesthesia induction.
Benzodiazepines are used for which withdrawal syndrome?
Alcohol withdrawal.
Herbal product that interacts with GABA
Valerian.
Adverse effect common to all sedative-hypnotics
Sedation.
Which sedative causes impaired motor coordination?
Benzodiazepines and barbiturates.
Which sedatives commonly cause dependence?
Benzodiazepines and barbiturates.
Which sedative may cause complex sleep behaviors?
Zolpidem.
Which sedatives may cause birth defects?
Benzodiazepines and barbiturates.
Which sedatives cause respiratory depression with alcohol?
All sedative-hypnotics.
Antidote for benzodiazepines and zolpidem
Flumazenil.
Withdrawal from benzodiazepines may cause
Seizures.
Withdrawal from barbiturates may cause
Seizures.
Withdrawal from zolpidem commonly causes
Insomnia.
Which sedatives induce liver enzymes?
Barbiturates.
Which sedatives interact with alcohol?
All sedative-hypnotics.
Sedating prescription antihistamine
Hydroxyzine.
Common OTC sedating antihistamine
Diphenhydramine.
Drug class of suvorexant
Orexin receptor antagonist.
Mechanism of suvorexant
Blocks orexin receptors that promote wakefulness.
Unique adverse effects of suvorexant
Sleep paralysis and sleep-related behaviors.
Melatonin mechanism
Mimics endogenous melatonin to promote sleep.
Light has what effect on melatonin?
Suppresses melatonin release.
Common melatonin adverse effects
Nightmares and daytime drowsiness.
Definition of nociceptor
Pain-sensing primary afferent neuron.
Primary afferent pain neurotransmitters
Substance P and glutamate.
Descending pain pathway neurotransmitters
Norepinephrine and serotonin.
Afferent means
Arrives at the CNS.
Efferent means
Exits the CNS.
Drug class of morphine
Mu opioid agonist.
Drug class of oxycodone
Mu opioid agonist.
Drug class of codeine
Mu opioid agonist and cough suppressant.
Drug class of naloxone
Opioid antagonist.
Drug class of nalbuphine
Mixed opioid agonist-antagonist.
Drug class of buprenorphine
Partial mu agonist.
Drug class of dextromethorphan
Opioid-like cough suppressant.
Does dextromethorphan act on opioid receptors?
No.
Primary opioid receptor responsible for analgesia
Mu receptor.
Kappa receptor stimulation commonly causes
Dysphoria and hallucinations.
Major therapeutic uses of opioids
Pain relief, anesthesia, opioid use disorder.
Do opioids reduce inflammation?
No.
Classic opioid overdose triad
Respiratory depression, pinpoint pupils, unconsciousness.
Fatal adverse effect of opioids
Respiratory depression.
Most common chronic opioid adverse effect
Constipation.
Naloxone is used for
Opioid overdose reversal.
Buprenorphine advantage
Less respiratory depression than full agonists.
Nonselective NSAIDs
Aspirin and ibuprofen.
Selective COX-2 inhibitor
Celecoxib.
Primary uses of NSAIDs
Pain, inflammation, fever.
Low-dose aspirin prevents
Thrombosis.
Primary uses of acetaminophen
Pain and fever.
Do NSAIDs inhibit prostaglandin synthesis?
Yes.
Does acetaminophen reduce inflammation?
Very little; acts mainly in the brain.
Migraine drug to know
Sumatriptan.
Mechanism of triptans
Serotonin receptor agonists that inhibit CGRP and substance P.
Major acetaminophen toxicity
Liver toxicity.
Less common acetaminophen toxicity
Kidney toxicity.
Common triptan adverse effects
Chest tightness and abnormal skin sensations.
COX-1 protects
Stomach, kidneys, platelets.
COX-2 primarily produces
Inflammatory prostaglandins.
NSAID adverse effects
GI ulcers, kidney injury, bronchospasm, premature ductus arteriosus closure.
Drug of choice for status epilepticus
Lorazepam.
Phenobarbital mechanism
Enhances GABA.
Gabapentin clinical uses
Partial seizures and chronic pain.
Gabapentin major advantage
Few drug interactions and well tolerated.
Mechanism of phenytoin
Blocks sodium channels.
Mechanism of divalproex
Blocks sodium channels and increases GABA.
Divalproex also prevents
Migraines.
Major adverse effect of phenytoin
Gingival overgrowth.
Signs of phenytoin toxicity
Nystagmus and unsteady gait.
Major adverse effects of divalproex
Liver toxicity, weight gain, GI upset, birth defects.
Drug for absence seizures
Ethosuximide.
Mechanism of ethosuximide
Blocks T-type calcium channels.
Four cardinal signs of Parkinson disease
Tremor, rigidity, bradykinesia, postural instability.
Cause of Parkinson disease
Loss of dopamine-producing neurons.
Most effective Parkinson medication
Levodopa/carbidopa.
Purpose of carbidopa
Prevents peripheral metabolism of levodopa.
Major levodopa adverse effects
Nausea, orthostatic hypotension, dyskinesia.
Unique levodopa adverse effect
On-off effect.
Main pathology of Alzheimer's disease
Loss of cholinergic neurons.
Acetylcholinesterase inhibitor
Donepezil.
Mechanism of donepezil
Inhibits acetylcholinesterase, increasing acetylcholine.
Common donepezil adverse effects
GI upset and insomnia.
Mechanism of memantine
NMDA (glutamate) receptor antagonist.
Positive schizophrenia symptoms
Hallucinations, delusions, bizarre behavior, disorganized thinking.
Negative schizophrenia symptoms
Flat affect, lack of motivation, social withdrawal, reduced speech.
Typical antipsychotic example
Haloperidol.