Pharm exam 3

What is sedation?

A decrease in anxiety and calming without loss of consciousness.

What is hypnosis?

Drug-induced sleep.

What determines whether a sedative-hypnotic causes sedation or hypnosis?

Dose (higher doses produce hypnosis).

What are the two primary therapeutic uses of sedative-hypnotics?

Anxiety and insomnia.

List three additional uses of benzodiazepines.

Seizures, muscle spasms, procedural sedation.

Lorazepam trade name?

Ativan®

Diazepam trade name?

Valium®

What drug class do lorazepam and diazepam belong to?

Benzodiazepines.

Do benzodiazepines directly activate GABA receptors?

No, they enhance GABA's effects.

How do benzodiazepines affect neuronal firing?

Increase GABA inhibition, decreasing action potentials.

Major adverse effects of benzodiazepines

Drowsiness, dizziness, confusion, dependence.

Antidote for benzodiazepine overdose

Flumazenil.

Zolpidem trade name

Ambien®

Primary use of zolpidem

Insomnia.

How does zolpidem differ from benzodiazepines?

Little effect on REM and Stage IV sleep; fewer daytime side effects.

Drug class with greatest overdose risk among sedatives

Barbiturates.

Secobarbital trade name

Secobarb®

Mechanism of barbiturates

Enhance GABA activity by prolonging chloride channel opening.

Most dangerous adverse effect of barbiturates

Respiratory depression.

Hydroxyzine trade name

Vistaril®

Therapeutic use of hydroxyzine

Sedation and anxiety.

What is chloral hydrate used for?

Pediatric sedation.

Why must pediatric chloral hydrate doses be weight-based?

To prevent overdose.

Valerian therapeutic use

Herbal treatment for insomnia.

Melatonin therapeutic use

Regulates sleep-wake cycle and treats insomnia.

What is acute pain?

Short-term pain related to injury or illness.

What is chronic pain?

Pain lasting longer than normal healing time.

Difference between an opiate and an opioid

Opiates are natural; opioids include natural and synthetic drugs.

Strong opioid agonist

Morphine.

Moderate opioid agonist

Codeine.

Strong opioid agonist used for severe pain

Oxycodone.

What receptor do opioids primarily stimulate?

Mu (μ) opioid receptors.

Effects of μ receptor activation

Analgesia, euphoria, sedation, respiratory depression.

Common opioid adverse effects

Constipation, nausea, respiratory depression, sedation.

Lifestyle change for chronic opioid users

Increase fiber and fluids to prevent constipation.

Classic opioid overdose triad

Coma, pinpoint pupils, respiratory depression.

Definition of tolerance

Need for higher doses to produce the same effect.

Definition of dependence

Withdrawal occurs if drug is stopped.

Naloxone trade name

Narcan®

Mechanism of naloxone

Competitive opioid receptor antagonist.

Primary use of naloxone

Reversal of opioid overdose.

Mixed opioid agonist-antagonist

Nalbuphine (Nubain®).

Main advantage of nalbuphine

Less respiratory depression and abuse potential.

OTC cough suppressant

Dextromethorphan.

Does dextromethorphan cause dependence?

No.

Prescription opioid cough suppressant

Codeine.

Definition of inflammation

Protective response to tissue injury.

Five classic signs of inflammation

Redness, heat, swelling, pain, loss of function.

Function of prostaglandins

Cause pain, fever, inflammation.

Function of leukotrienes

Inflammation and bronchoconstriction.

COX-1 function

Protects stomach, kidneys, and platelets.

COX-2 function

Produces inflammatory prostaglandins.

Nonselective NSAIDs

Aspirin and ibuprofen.

Selective COX-2 inhibitor

Celecoxib.

Major adverse effects of COX-1 inhibition

Gastric ulcers and bleeding.

Four adverse effects common to all NSAIDs

Kidney injury, hypertension, edema, cardiovascular risk.

Why was Vioxx withdrawn?

Increased cardiovascular events.

Therapeutic uses of acetaminophen

Pain and fever.

Does acetaminophen reduce inflammation?

No.

Major toxicity of acetaminophen

Liver failure.

When does acetaminophen liver toxicity appear?

24-48 hours after overdose.

Migraine abortive drug classes

Triptans and ergots.

Ergotamine trade name

Ergotrate®

Mechanism of ergots

Block serotonin receptors involved in migraine.

Sumatriptan trade name

Imitrex®

Advantage of triptans over ergots

More selective with fewer adverse effects.

Herbal migraine prophylaxis

Feverfew.

Definition of status epilepticus

A seizure lasting >5 minutes or repeated seizures without recovery.

Drug of choice for status epilepticus

Diazepam IV.

Drug with minimal interactions for partial seizures

Gabapentin.

Gabapentin trade name

Neurontin®

Mechanism of phenytoin

Prolongs sodium channel inactivation.

Phenytoin trade name

Dilantin®

Signs of phenytoin toxicity

Nystagmus and ataxia.

Valproate trade name

Depakote®

Mechanisms of valproate

Blocks sodium channels and increases GABA.

Drug of choice for absence seizures

Ethosuximide.

Ethosuximide trade name

Zarontin®

Mechanism of ethosuximide

Blocks T-type calcium channels.

Four major symptoms of Parkinson's disease

Tremor, rigidity, bradykinesia, postural instability.

Cause of Parkinson's disease

Loss of dopamine-producing neurons.

Most effective Parkinson drug

Levodopa.

Levodopa/carbidopa trade name

Sinemet®

Purpose of carbidopa

Prevents peripheral conversion of levodopa.

On-off effect of levodopa

Alternating periods of symptom control and symptom return.

Dopamine agonist

Ropinirole.

Ropinirole trade name

Requip®

MAO-B inhibitor for Parkinson's

Selegiline.

COMT inhibitor

Tolcapone.

Purpose of benztropine

Treats Parkinson tremor.

Benztropine trade name

Cogentin®

Main neurotransmitter deficient in Alzheimer's disease

Acetylcholine.

Donepezil trade name

Aricept®

Mechanism of donepezil

Acetylcholinesterase inhibitor.

Memantine trade name

Namenda®

Mechanism of memantine

Blocks glutamate (NMDA) receptors.

Positive symptoms of schizophrenia

Hallucinations, delusions, disorganized speech.

Negative symptoms of schizophrenia

Flat affect, lack of motivation, social withdrawal.

Main neurotransmitter involved in schizophrenia

Dopamine.

Typical antipsychotics mainly block

Dopamine receptors.