Pharm Quiz 6 Flashcards
Ester-type Anesthetics
Procaine and Cocaine
Low allergy
Metabolized by plasma esterases
Amide-type Anesthetics
Lidocaine
Very low allergy
Metabolized by liver
MOA Local Anesthetics
Block sodium channels in axons
Order of feelings that are lost with local anesthetics:
Pain, Cold, Warm, Touch, Deep Pressure
Why is epi used with local anesthetics?
It prolongs length and decreases toxicity.
Local Anesthetic SA
CNS excitation followed by depression.
Bradycardia
Cross-sensitivity has not been observed.
Methemoglobinemia -Hgb cannot release O2. Do not give topical benzocaine to children under 2.
Procaine
Must be injected. Low risk for toxicity. Higher risk for allergy.
Lidocaine
Topical or injection. Stronger than Procaine. Higher risk for toxicity.
Cocaine
Used for ENT. Causes vasoconstriction by blocking NorEpi, which also effects the SNS.
Topical Local Anesthetic Administration
Location: skin or mucous membranes
Systemic toxicity can be avoided by avoiding heat, wrapping, and exercise which can increase absorption.
Infiltration Anesthesia
Lidocaine and Bupivacaine are used in the general area of procedure.
Nerve Block Anesthesia
Short Procedures: Lidocaine or Mepivacaine
Long Procedures: Bupivacaine
What happens when opioid agonists are combined with agonist-antagonists?
Withdrawal reaction
Opioid induced Neurotoxicity
Cause: Renal impairment, cognitive impairment, long-term use
Prevention: Switching different types of opioids
Tx: Hydration and dose reduction
Fentanyl Patch
Takes 24h to kick in and lasts for 48 hours.
Should only be given to tolerant patients or respiratory depression will result.
Transmucosal Fentanyl
Only for patients >18 with break through cancer pain who are opioid dependent defined as 30mg Oxy, 25mcg Fent/hr, 8mg Hydromorphone.
Methadone SA
Due to QT prolongation consultation with a pain specialist is recommended. Patients should receive and EKG before, 30 days after, and then annually.
Strong Opioid Agonists
Morphine, Fentanyl, Methadone, Hydromorphone, Oxymorphone, Levorphanol
Moderate to Strong Opioid Agonists
Codeine
Agonist-Antagonist Opioids
Buprenorphine, Butorphanol, Nalbuphine, Pentazocine
Codeine
Schedule II
30mg = 325mg of Tylenol
Antitussive = 10mg (Schedule V)
Codeine BB
Ultrarapid metabolizers (specifically children) converts to Morphine and can cause death.
Oxycodone
Schedule II
Analgesic effects = Codeine
Hydrocodone
Schedule II
ER always combined with NSAID.
Tapentadol
Blocks reuptake of NorEpi and causes less constipation.
Pentazocine
Mild to moderate pain
Antagonizes u. Agonizes K –> respiratory depression (not dose dependent), analgesia, sedation.
Dependence is possible but withdrawal is minimal.
Buprenorphine
Schedule III
Partial agonist at u. Antagonist at K.
No tolerance. No severe respiratory depression.
Naloxone does not readily reverse.
QT prolongation
Naloxone
Antagonizes Mu, Kappa, and Sigmoid
Mehtylnaltrexone, Naloxegol, Naldemedine
Selectively antagonizes Mu. They only help with constipation.
Naltrexone
Used for ETOH and opioid addiction. Prevents euphoria but not craving.
Complete opioid antagonist which completely blocks euphoria. Should only be given after patient has detoxed.
Embeda
When swallowed intact, only Morphine is absorbed. Otherwise Naltrexone will prevent high. Only used when abuse is suspected. ETOH accelerates absorption leading to fatality.
Tramadol MOA
Slightly Agonizes Mu. Mostly blocks uptake of Serotonin and NorEpi.
Tramadol Use
Schedule IV
Moderate pain
Onset: 1 hr Duration: 6h
Tramadol Drug Interactions
MAOI
Serotonin Syndrome with SNRIs, SSRIs, TCAs
What drugs does the Risk Evaluation and Mitigation Strategy included?
IR opioids, ER opioids, and long-acting prescription opioids to educate members of the healthcare team.
CDC Guidelines for safe opioid prescribing:
- Establish realistic goals for pain
- Discuss known risks continuously
- Start with IR
- Evaluate before prescribing >50 Morphine milligram equivalents and avoid adjusting a dose to >90 MMEs
- Long-term dependence often starts with acute pain. Pain medication for 3 days is often sufficient.
- Prescribe with Naloxone when given with Benzo or >50 MME
- Avoid prescribing opioids with Benzos.
Avoiding a withdrawal reaction
Dependence can start after 20 days, so taper off over 3-10 days.
Characteristics of Migraines
Usually unilateral
Usually with aura
Hyperalgesia -augmented responses to painful stimuli
Allodynia -Painful response to unpainful stimuli
Start in the morning and last 4-72 hours
Family history is normal
How does CGRP affect migraines?
CGRP rises during a migraine.
Sumatriptan decreases CGRP.
Stimulation of neurons in the trigeminal vascular system –> CGRP release –> inflammation and dilation
How does Serotonin affect migraines?
Serotonin drops during a migraine.
Depletion of serotonin can precipitate a migraine.
Administration of Serotonin can abort an attack.
Drug selection for Migraines:
NSAID
Migraine-specific drug (triptan or ergot alkaloid)
Opioid agonist
How often can abortive medications be used?
1-2x/weeks at most or a medication overdose headache can occur.
What antiemetic is used for migranies?
Metoclopramide and Prochlorperazine
What medication combination works as well as Sumatriptan?
ASA and metoclopramide
Excedrin
Tylenol (should not be used alone), ASA, and caffeine
What opioid medication is used for migraines?
Butorphanol nasal spray
Triptans
Abortive
40% of patients will have another migraine in 24h
Serotonin receptor agonists constrict intracranial blood vessels and decrease secretion of inflammatory neuropeptides
Triptan AE
Bad taste
Chest pressure
Coronary vasospasm
Teratogenesis
Ergotamine MOA
Decreases CGRP
Enhances Serotonin
Decreases vasodilation
Ergotamine therapeutic use
Second-line after triptans due to dependence
Ergotism
Ischemia in peripheral arteries
Dihydroergotamine
Given IM, IV, or SQ.
Less effective than triptan but better at reducing recurrence.
Ergotamines BB
CYP3AV inhibitors can raise levels to dangerous amounts.
When should preventative migraine agents be given?
If patients have >3 attacks/month, they are more severe than usual, do not respond to abortive agents.
Prophylactic medications for migraines:
Propanolol
Depakote
TCA
Estrogen
Depakote (Divalproex) BB
Pancreatitis and Hepatitis
Medications for menstrualy associated migraine:
Estrogen 2 days within the onset of menses.
Triptans for 6 days starting 2 days before menses.
Naproxen sodium given 6 days before menses
Erenumab
Monoclonal antibody that decreases CGRP.
Botulinum Toxin
For patients with >15 migraines per month. Only decreases amount by 2.
Cluster HA Characteristics
Occur every day for 2-3 months and can be separated by months to years.
Unilateral near the eye.
Causes ptosis, lacrimation, nasal congestion, and miosis.
Occur more in males.
Prophylaxis medications for cluster HA
Verapamil
Suboccipital steroid injections
Glucocorticoids
Lithium
Cluster HA Abortive Meds:
Sumatriptan SQ
Oxygen 7-10L for 10-15 min
When should antidepressants be discontinued?
For 4-9 months after alleviation of symptoms. Slowly taper down.
What are SSRIs indicated for?
Bipolar
Premenstrual Dysphoric Disorder
Bulimia
Fluoxetine SA
Sexual Dysfunction, Weight Gain, Serotonin Syndrome, teratogenesis.
Fluoxetine Withdrawal
Withdrawal symptom starts within 1-3 days and lasts up to 3 weeks. It causes dizziness, headaches, dysphoria, and anxiety.
SSRIs
Escitalopram
Citalopram
Fluvoxamine
Paroxetine
Sertraline
SNRIs
Venlafaxine
Duloxetine
Desvenlafaxine
Levomilnacipran
Venlafaxine Therapeutic Uses
Depression
Anxiety
Panic Disorder
Social Anxiety Disorder
TCA AE
Sedation, OH, Anticholinergic, Diaphoresis, Cardiac dysfunction, Seizures
TCA MOA
Block reuptake of MOA and Serotonin
TCA Therapeutic Uses
Anxiety
Fibromyalgia
Neuropathic pain
ADHD
TCA Drug Interactions
Epi and Dopamine
Amphetamine
Ephedrine
MAOI MOA
Increase amount of NE and Serotonin available for release.
MAOI Therapeutic Use
Atypical Depression