Module 3

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Questions and Answers

What is the mechanism of action (MOA) of local anesthetics?

Local anesthetics work by blocking sodium channels in the neuronal cell membrane, preventing the initiation and conduction of nerve impulses.

Which properties determine the ability of local anesthetics to penetrate the axon membrane? (Select all that apply)

Concentration of the drug

Molecular size (correct)

Lipid solubility (correct)

Degree of ionization at tissue pH (correct)

Vasoconstrictors increase local blood flow and reduce the duration of anesthesia.

False

What is a blood dyscrasia associated with benzocaine?

Methemoglobinemia Signup and view all the answers

What are the three main classes of opioid receptors?

Mu (μ) Signup and view all the answers

What is the reversal drug for opiate effects?

Naloxone Signup and view all the answers

Which of the following are pure opioid agonists? (Select all that apply)

Hydromorphone Signup and view all the answers

What is a common adverse effect of opioids related to the gastrointestinal system?

Constipation Signup and view all the answers

Tramadol is associated with a decreased risk of seizures.

False Signup and view all the answers

Which of the following are characteristics of Cox-1 inhibitors? (Select all that apply)

Affect protective gastric mucosa Signup and view all the answers

What is an important drug interaction with Acetaminophen?

Alcohol Signup and view all the answers

Cox-2 inhibitors primarily target __________.

inflammatory pathways Signup and view all the answers

What is a common adverse effect of glucocorticoids?

Hyperglycemia Signup and view all the answers

What is the recommendation for tapering glucocorticoids?

Gradual reduction in dose to prevent adrenal insufficiency. Signup and view all the answers

Which of the following foods can trigger migraines? (Select all that apply)

Processed meats Signup and view all the answers

Triptans are known to cause overuse headaches.

True Signup and view all the answers

What is the primary action of NSAIDs in treating migraines?

Reduce inflammation and pain Signup and view all the answers

The drug class known for blocking calcitonin gene-related peptide to reduce migraine frequency is called ___.

CGRP monoclonal antibodies Signup and view all the answers

Which of the following are contraindications for triptans? (Select all that apply)

Severe liver disease Signup and view all the answers

What herbal medication used for migraines may cause gastrointestinal symptoms?

Feverfew Signup and view all the answers

Match the following abortive treatments with their characteristics:

Sumatriptan = Selective serotonin receptor agonist Ergotamine = Constricts blood vessels in the brain Zolmitriptan = Oral and intranasal administration Frovatriptan = Longest half-life of 26 hours Signup and view all the answers

What is the goal of treatment for rheumatoid arthritis?

Reduce inflammation and pain while preserving function and preventing joint damage/deformity. Signup and view all the answers

Which of the following is the first-line treatment for rheumatoid arthritis?

NSAIDs with DMARDs Signup and view all the answers

What is the first-line traditional DMARD for moderate to severe rheumatoid arthritis?

Methotrexate Signup and view all the answers

Which of the following is a potential side effect of Rituximab?

Infusion reactions Signup and view all the answers

All anti-TNF medications inactivate TNF.

True Signup and view all the answers

The first-line preventive medication for gout is __________.

Allopurinol Signup and view all the answers

What can excessive production of uric acid lead to?

Gout Signup and view all the answers

Which of the following indications suggests the initiation of preventive treatment for gout?

Presence of tophaceous gout Signup and view all the answers

What is the main cause of gout?

Excessive production of uric acid or impaired renal excretion of uric acid. Signup and view all the answers

Rituximab reduces the number of __________ cells.

B lymphocytes Signup and view all the answers

Study Notes

Local Anesthetics

Block sodium channels in neuronal cell membrane, preventing nerve impulses
Properties determining ability to penetrate axon membrane:
- Lipid solubility
- Molecular size
- Degree of ionization at tissue pH (pKa)
Lidocaine:
- Effects prolonged with epinephrine
- Can be used for cardiac dysrhythmias, suppresses cardiac excitability
Vasoconstrictors (e.g., epinephrine) reduce local blood flow, prolong anesthesia, and reduce systemic absorption and toxicity
Blood dyscrasia: methemoglobinemia from benzocaine
Application guidelines for topical anesthetics:
- Use smallest effective amount
- Apply to smallest surface area
- Avoid broken or irritated skin
- Avoid strenuous exercise
- Avoid heating site
- Do not use under occlusive dressings unless prescribed

Opioids

Three main classes of opioid receptors:
- Mu (μ) receptors: analgesia, respiratory depression, euphoria, sedation, and physical dependence
- Kappa (κ) receptors: analgesia, sedation
- Delta (δ) receptors: do not interact with opioids
Three classifications of drugs acting on opioid receptors:
- Pure opioid agonists (e.g., morphine, fentanyl): activate Mu and Kappa receptors
- Opioid agonist-antagonists (e.g., pentazocine, nalbuphine, butorphanol, buprenorphine): produce analgesia, but can antagonize pure agonists
- Pure opioid antagonists (e.g., naloxone, naltrexone): reverse respiratory and CNS depression caused by opioid agonists
Opioid medications and details:
- Morphine: severe acute pain, breakthrough pain, and around-the-clock dosing
- Hydrocodone: moderate to severe acute and persistent pain
- Oxycodone: moderate to severe persistent pain
- Fentanyl: persistent pain
- Hydrocodone/acetaminophen: acute, recurrent, and episodic breakthrough pain
- Oxycodone/acetaminophen: moderate to severe pain
Morphine:
- Pro-agonist
- Therapeutic uses: severe pain relief
- Side effects: euphoria, drowsiness, mental clouding, anxiety reduction, respiratory depression, constipation, cough suppression, biliary colic, tolerance, physical dependence, and histamine relief
- Black Box Warning: addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; neonatal opioid withdrawal syndrome
- Medications for opioid-induced constipation (OIC): methylnaltrexone, naloxegol, lubiprostone
- Reversal drug: naloxone
- Drug to discourage abuse: naltrexone

Nonopioid Centrally Acting Analgesics

Tramadol:
- Suicide risk: increased in patients with depression or suicidal tendencies
- Seizure risk: increased, especially with a history of seizures or taking medications that lower seizure threshold
Clonidine: used for hypertension and severe cancer pain (off-label)
Ziconotide: used for severe chronic pain via intrathecal route
Dexmedetomidine: used for sedation of patients on mechanical ventilation

Cyclooxygenase Inhibitors (Anti-Inflammatories)

Differentiate Cox 1 and Cox 2 drugs:
- Cox-1 inhibitors (e.g., aspirin, ibuprofen, naproxen): affect protective gastric mucosa, platelet aggregation, and support renal function
- Cox-2 inhibitors (e.g., celecoxib): produced at sites of tissue injury, target inflammatory pathways, with less GI side effects but increased cardiovascular risk
NSAIDs and Acetaminophen:
- Indications: Tx inflammatory disorders, mild to moderate pain, suppress fever, and relieve dysmenorrhea
- Examples: aspirin, ibuprofen, naproxen
Safety alert: increased risk of GI bleeding/ulceration, renal impairment with all first-generation NSAIDs
Second-generation NSAIDs: ONLY inhibit COX2
- Indications: suppress inflammation with fewer adverse effects, but less safe than first-gen due to increased risk of MI/stroke
- Examples: celecoxib
Celecoxib:
- Cardiovascular risk: hypertension, edema, increased risk of MI/Stroke
- A/E: MI/Stroke, sulfonamide allergy
- Cannot be used during pregnancy
ASA:
- Uses: analgesic, anti-pyretic, and anti-inflammatory, suppression of platelet aggregation, protection in thrombotic disorders, cancer prevention, and prevention of Alzheimer's
- Decreases risk for colorectal cancer at low dosage
- Drug interactions: increased bleeding risk with anticoagulants, corticosteroids, and alcohol
- Side effects: GI bleeding, renal impairment, Reye's syndrome in children
Acetaminophen:
- MOA: inhibits prostaglandin synthesis in CNS
- A/E: SJS, exanthematous pustulosis, toxic epidermal necolysis, and hepatotoxicity with overdose
- Drug interactions: alcohol, warfarin, vaccines
- Vaccines: can reduce immune response to some vaccines
- Treatment for overdose: N-acetylcysteine (NAC)

Glucocorticoids

MOA: inhibit synthesis of chemical mediators
Therapeutic uses: anti-inflammatory and immunosuppressive effects for conditions like asthma, OA/RA, lupus, tendonitis, synovitis, gouty arthritis, and disorders of the eye
Metabolic effects: hyperglycemia, increased fat deposition, muscle wasting, thinning of skin, growth retardation in children, cataracts/glaucoma, Cushing's syndrome
Adverse effects: osteoporosis, adrenal suppression, increased infection risk, GI ulceration, mood changes
Drug interactions: interact with NSAIDs, antidiabetic drugs, vaccines
Contraindicated: patients with systemic/fungal infections, live virus vaccines, caution use with peds, pregnant/breastfeeding
Tapering: gradual reduction in dose to prevent adrenal insufficiency, monitor for signs of insufficiency

Pathophysiology of Migraine

Abnormal brain activity affects nerve signals, chemicals, and blood vessels in the brain, triggered by factors such as hormonal changes, certain foods, stress, and environmental factors.

Foods that Trigger Migraines

Aged cheeses
Processed meats
Chocolate
Alcohol (especially red wine)
Caffeine
Artificial sweeteners

Abortive Treatment Drug Classes

Triptans

Examples: sumatriptan
Mechanism: selective serotonin receptor agonists reducing inflammation and constricting blood vessels
Sumatriptan:
- Adverse effects: bad taste, chest symptoms, coronary vasospasm, teratogenesis
- Contraindications: pregnancy, heart disease, not recommended for geriatric/severe liver disease/MAOIs use in past 2 weeks
- Lab tests: LFTs, creatinine clearance
Other triptans: zomitriptan (oral and intranasal, tastes bad), frovatriptan (longest half-life: 26 hours)

Ergot Alkaloids

Examples: ergotamine
Mechanism: constricting blood vessels in the brain
Ergotamine:
- Adverse effects: muscle pain, paresthesia, cold extremities, physical dependence
- Contraindications: hepatic/renal impairment, CAD, PVD, pregnancy
- Interactions: contraindicated with potent inhibitors of CYP (protease inhibitors, azole antifungals, and some macrolides)

NSAIDs

Examples: ibuprofen, naproxen
Mechanism: reducing inflammation and pain
Treximet: combination of sumatriptan and naproxen
Urbogepant:
- Can be used during breastfeeding
- Interactions: azoles, macrolides, floxins, grapefruit juice
Rimegepant:
- Can be abortive and preventive
- Dose: 75mg as needed, 75mg every other day (preventive)
Lasmitidan:
- First in class Serotonin 1F receptor agonist
- Adverse effect: drowsiness in geriatric

Overuse Headaches

All abortives can cause overuse headaches, which can be prevented by taking preventive medications.

Preventive Medications

Beta-Blockers

Examples: propranolol
Mechanism: reducing frequency and severity of migraines

Antiseizure Medications

Examples: topiramate, divalproex, tiagabapine
Mechanism: stabilizing nerve cell membranes

CGRP Monoclonal Antibodies

Examples: erenumab
Mechanism: blocking calcitonin gene-related peptide to reduce migraine frequency
Dose: subq injection dosed once monthly
Atogepant:
- Oral
- Renal dosing

Antidepressants

Examples: amitriptyline

Botulinum Toxin

Requires a lot of injections
Variable effects
Expensive

Herbal Medications

Butterbur: potential liver toxicity
Feverfew: gastrointestinal symptoms, mouth ulcers
Magnesium: diarrhea
Riboflavin (Vitamin B2): generally well-tolerated

Treatment for Menstrual Migraine

NSAIDs
Triptans
Hormonal therapy (e.g., estrogen patches)

Rheumatoid Arthritis (RA)

Autoimmune disorder characterized by chronic systemic inflammation of multiple joints' synovial membranes
Shortens lifespan and increases risk of cardiovascular disease and stroke
Goal of treatment: reduce inflammation and pain while preserving function and preventing joint damage/deformity

Treatment

First line treatment: NSAIDs with Disease-Modifying Antirheumatic Drugs (DMARDs)
Traditional DMARDs:
- Methotrexate (1st line for moderate-severe RA) with risks of bone marrow suppression, hepatic fibrosis, GI ulceration, and pneumonitis
- Hydroxychloroquine (2nd line for mild RA) with risk of retinal damage
- Leflunomide (teratogenic)
- Sulfasalazine (GI effects)
- Minocycline
- Penicillamine
- Azathioprine
- Cyclosporine
Biological response modifiers:
- Risk of cancer and infections
- Receive all recommended vaccinations
- Yearly TB testing required

Non-TNF Biological Response Modifiers

Rituximab:
- Reduces number of B lymphocytes
- Adverse effects: infusion reactions, mucocutaneous reactions, Hep B reactivation, progressive multifocal leukoencephalopathy
Abatacept:
- T-cell activation inhibitor
- Adverse effects: headaches, upper respiratory infections, nasal pharyngitis
- Avoid live vaccines
Anakinra:
- Blocks receptors for interleukin 1
- Adverse effects: infections
Tocilizumab:
- Interleukin-6 receptor antagonist
- Adverse effects: infections, GI perforation, liver injury, neutropenia/thrombocytopenia

Anti-TNF Biological Response Modifiers

Inactivate TNF
Examples:
- Etanercept:
  - Adverse effects: infections, heart failure, hematologic disorders
  - Avoid live viruses
- Infliximab
- Adalimumab
- Certolizumab
- Golimumab

Oral JAK Inhibitors

Tofacitinib
Ruxolitinib

Gout

Caused by excessive production of uric acid and impaired renal excretion
Common in great toe
Preventive medications:
- Xanthine oxidase inhibitors (agents that decrease uric acid production):
  - Allopurinol:
    - First-line treatment
    - Inhibition of xanthin oxidase
    - Adverse effects: hypersensitivity with HLA-B allele (Asian/AA decent must have HLA testing)
    - Dosage: 100mg or less daily, increases every 2-5 weeks for urate level

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Description

Quiz on local anesthetics, their mechanism of action, properties, and effects on nerve impulses and cardiac excitability. Includes discussion on Lidocaine and vasoconstrictors.