Pain OPTION 2-FINAL Flashcards
Aspirin (ASA)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Irreversibly inhibits COX-1 and COX-2, decreasing prostaglandin synthesis.
Uses: Anti-inflammatory, analgesic, antipyretic, antiplatelet.
Special Considerations: Avoid in children with viral infections (Reye’s Syndrome), can cause GI bleeding, take with food.
Contraindications: Children with viral infections (Reye’s Syndrome), active GI bleeding, severe kidney disease.
Pregnancy/Lactation: Avoid in pregnancy (3rd trimester: premature ductus arteriosus closure), lactation caution.
Ibuprofen
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Reversibly inhibits COX-1 and COX-2, decreasing prostaglandin synthesis.
Uses: Pain relief, inflammation, fever reduction.
Special Considerations: Less GI risk than aspirin but still present, caution in kidney disease.
Contraindications: Severe renal impairment, history of GI bleeding, cardiovascular disease caution.
Pregnancy/Lactation: Avoid in 3rd trimester, caution in lactation.
Acetaminophen (Tylenol)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Inhibits prostaglandin synthesis in CNS, weak peripheral COX inhibition.
Uses: Pain relief, fever reduction.
Special Considerations: Hepatotoxic in overdose, avoid in severe liver disease, antidote is N-acetylcysteine.
Contraindications: Severe liver disease, alcoholism, chronic high doses.
Pregnancy/Lactation: Considered safe in pregnancy, caution in high doses.
Methotrexate
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Folic acid antagonist, inhibits cytokine production and purine synthesis.
Uses: RA, psoriasis, certain cancers.
Special Considerations: Monitor liver enzymes, contraindicated in pregnancy, give folic acid supplementation.
Contraindications: Pregnancy, liver disease, active infection, bone marrow suppression.
Pregnancy/Lactation: Contraindicated in pregnancy, avoid in lactation.
Hydroxychloroquine (Plaquenil)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Unclear, but modulates immune response.
Uses: RA, lupus.
Special Considerations: Risk of ocular toxicity, requires regular eye exams.
Contraindications: Retinal disease, known hypersensitivity.
Pregnancy/Lactation: Use caution, potential fetal risks.
Leflunomide (Arava)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Inhibits dihydroorotate dehydrogenase, preventing lymphocyte proliferation.
Uses: RA.
Special Considerations: Hepatotoxicity risk, contraindicated in pregnancy, long half-life.
Contraindications: Pregnancy, liver disease, immunosuppression.
Pregnancy/Lactation: Contraindicated in pregnancy and lactation.
Celecoxib (Celebrex)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Selective COX-2 inhibitor, reducing inflammation.
Uses: RA, OA, pain relief.
Special Considerations: Lower GI risk but increased CV risk compared to NSAIDs.
Contraindications: History of CV disease, active GI bleeding.
Pregnancy/Lactation: Avoid in pregnancy (CV risk), lactation caution.
Misoprostol (Cytotec)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: PGE1 analog, protects gastric mucosa, decreases acid secretion.
Uses: Prevention of NSAID-induced ulcers, induction of labor, misscarriage, abortion
Special Considerations: Contraindicated in pregnancy, can cause diarrhea.
Contraindications: Pregnancy, history of uterine disorders, inflammatory bowel disease.
Pregnancy/Lactation: Contraindicated in pregnancy (uterotonic effects), lactation caution.
TNF-α Inhibitors (Infliximab, Etanercept, Adalimumab)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Block TNF-α, reducing inflammation.
Uses: RA, Crohn’s disease, psoriasis.
Special Considerations: Risk of infections (TB, fungal), avoid live vaccines.
Contraindications: Active or latent TB, serious infections, history of malignancy.
Pregnancy/Lactation: Avoid in pregnancy (immunosuppression risk), lactation caution.
Tofacitinib (Xeljanz)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Janus kinase (JAK) inhibitor, modulating immune response.
Uses: RA, psoriatic arthritis, UC.
Special Considerations: Monitor for infections, anemia, increased malignancy risk.
Contraindications: Serious infections, active TB, demyelinating disease.
Pregnancy/Lactation: Avoid in pregnancy, lactation safety unknown.
Alprostadil (Caverject/Muse)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: PGE1 analog, vasodilator.
Uses: Erectile dysfunction, maintains ductus arteriosus in neonates.
Special Considerations: Administered via injection or urethral suppository, risk of hypotension.
Contraindications: Serious infections, active TB, concurrent biologics.
Pregnancy/Lactation: Avoid in pregnancy, lactation safety unknown.
Lubiprostone (Amitiza)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: PGE1 derivative, activates Cl- channels increasing intestinal fluid secretion.
Uses: Chronic idiopathic constipation, opioid-induced constipation, IBS-C.
Special Considerations: Can cause nausea, take with food. Only approved for WOMEN.
Contraindications: Severe infections, TB, recent live vaccines.
Pregnancy/Lactation: Avoid in pregnancy, lactation safety unknown.
Bimatoprost (Latisse/Lumigan)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Prostaglandin F2α analog, increases uveoscleral outflow.
Uses: Open-angle glaucoma, eyelash hypotrichosis.
Special Considerations: May cause iris pigmentation, increased eyelash growth.
Contraindications: Active TB, history of serious infections, lymphoma history.
Pregnancy/Lactation: Avoid in pregnancy, lactation safety unknown.
Latanoprost (Xalantan)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Prostaglandin F2α analog, increases aqueous humor outflow.
Uses: Glaucoma, ocular hypertension.
Special Considerations: Can change iris color, cause eye irritation.
Contraindications: Severe COPD, serious infections, live vaccines.
Pregnancy/Lactation: Avoid in pregnancy, lactation unknown.
Epoprostenol (Flolan/Veletri)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Prostacyclin (PGI2) analog, vasodilates pulmonary and systemic arteries.
Uses: Pulmonary arterial hypertension.
Special Considerations: Short half-life, continuous IV infusion required.
Contraindications: Serious infections, severe infusion reactions.
Pregnancy/Lactation: Avoid in pregnancy, lactation unknown.
Iloprost (Ventavis)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Prostacyclin analog, vasodilates pulmonary arteries.
Uses: Pulmonary arterial hypertension.
Special Considerations: Inhalation formulation, may cause dizziness, headache.
Contraindications: Serious infections, neutropenia, liver disease.
Pregnancy/Lactation: Avoid in pregnancy, lactation unknown.
Sulfasalazine (Azulfidine)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Unclear, modulates immune response.
Uses: RA, ulcerative colitis.
Special Considerations: Risk of GI upset, leukopenia, and anemia; monitor CBC.
Contraindications: Serious infections, hepatic impairment, GI perforation.
Pregnancy/Lactation: Avoid in pregnancy, lactation unknown.
Adalimumab (Humira)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: TNF-α inhibitor, reduces inflammation.
Uses: RA, Crohn’s disease, psoriasis.
Special Considerations: Risk of infection, avoid live vaccines.
Contraindications: Children with viral infections (Reye’s Syndrome), active GI bleeding, severe kidney disease.
Pregnancy/Lactation: Avoid in pregnancy (3rd trimester: premature ductus arteriosus closure), lactation caution.
Certolizumab (Cimzia)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: TNF-α inhibitor, neutralizes TNF-α.
Uses: RA, Crohn’s disease.
Special Considerations: PEGylated formulation extends half-life, increased infection risk.
Contraindications: Severe renal impairment, history of GI bleeding, cardiovascular disease caution.
Pregnancy/Lactation: Avoid in 3rd trimester, caution in lactation.
Etanercept (Enbrel)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: TNF-α receptor fusion protein, binds TNF-α.
Uses: RA, psoriasis, ankylosing spondylitis.
Special Considerations: Given subcutaneously weekly, increased risk of infections.
Contraindications: Severe liver disease, alcoholism, chronic high doses.
Pregnancy/Lactation: Considered safe in pregnancy, caution in high doses. (though research shows it crosses the placenta and has a small increase in risk of preterm birth)
Golimumab (Simponi)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Monoclonal antibody against TNF-α.
Uses: RA, psoriatic arthritis.
Special Considerations: Monthly SQ injection, risk of infection and liver enzyme elevations.
Contraindications: Pregnancy, liver disease, active infection, bone marrow suppression.
Pregnancy/Lactation: Contraindicated in pregnancy, avoid in lactation.
Infliximab (Remicade)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Chimeric monoclonal antibody against TNF-α.
Uses: RA, Crohn’s disease, psoriasis.
Special Considerations: Given IV, risk of infusion reactions, requires premedication.
Contraindications: Retinal disease, known hypersensitivity.
Pregnancy/Lactation: Use caution, potential fetal risks.
Abatacept (Orencia)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Costimulation modulator, blocks T-cell activation.
Uses: RA.
Special Considerations: Given IV, increased risk of infections, avoid in severe COPD.
Contraindications: Pregnancy, liver disease, immunosuppression.
Pregnancy/Lactation: Contraindicated in pregnancy and lactation.
Rituximab (Rituxin)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Monoclonal antibody against CD20, depletes B cells.
Uses: RA, B-cell malignancies.
Special Considerations: Risk of infusion reactions, premedicate with steroids, APAP, and antihistamines.
Contraindications: History of CV disease, active GI bleeding.
Pregnancy/Lactation: Avoid in pregnancy (CV risk), lactation caution.
Sarilumab (Kevzara)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Monoclonal antibody against IL-6 receptor.
Uses: RA.
Special Considerations: Given SQ, risk of neutropenia, increased LFTs.
Contraindications: Pregnancy, history of uterine disorders, inflammatory bowel disease.
Pregnancy/Lactation: Contraindicated in pregnancy (uterotonic effects), lactation caution.
Tocilizumab (Actemra)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Monoclonal antibody against IL-6 receptor.
Uses: RA, cytokine release syndrome.
Special Considerations: Given IV or SQ, monitor for liver toxicity and infections.
Contraindications: Active or latent TB, serious infections, history of malignancy.
Pregnancy/Lactation: Avoid in pregnancy (immunosuppression risk), lactation caution.
Meloxicam (Mobic)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Selective COX-2 inhibitor at low doses, inhibits prostaglandin synthesis.
Uses: Osteoarthritis, rheumatoid arthritis.
Special Considerations: Longer half-life allows once-daily dosing.
Contraindications: History of GI bleeding, severe renal impairment.
Pregnancy/Lactation: Avoid in third trimester, caution in lactation.
Ketorolac (Toradol)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Non-selective COX inhibitor, strong analgesic effect.
Uses: Moderate to severe pain, post-operative pain.
Special Considerations: High risk of GI ulceration, limited to 5-day use.
Contraindications: Active GI bleeding, severe renal impairment.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Naproxen (Naprosyn)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Non-selective COX inhibitor, reduces inflammation and pain.
Uses: Mild to moderate pain, arthritis, dysmenorrhea.
Special Considerations: Longer half-life allows BID dosing.
Contraindications: GI bleeding, cardiovascular disease.
Pregnancy/Lactation: Avoid in third trimester, caution in lactation.
Meperidine (Demerol)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Mu-opioid receptor agonist, inhibits pain transmission.
Uses: Short-term pain relief.
Special Considerations: Not recommended for chronic pain due to toxic metabolite (normeperidine).
Contraindications: Renal failure, seizures.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Codeine (CS III)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Weak mu-opioid receptor agonist, metabolized to morphine.
Uses: Mild to moderate pain, cough suppression.
Special Considerations: Metabolism varies between individuals, risk of respiratory depression.
Contraindications: Children under 12, respiratory depression.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Tapentadol (CS II/Nucynta)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Mu-opioid receptor agonist, inhibits norepinephrine reuptake.
Uses: Moderate to severe acute pain.
Special Considerations: Lower risk of respiratory depression than traditional opioids.
Contraindications: Severe respiratory depression, MAOIs.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Pentazocine (Talwin)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Mixed opioid agonist-antagonist.
Uses: Moderate pain relief.
Special Considerations: Can cause psychotomimetic effects.
Contraindications: History of opioid dependence.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Butorphanol (Stadol)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Partial opioid agonist, kappa receptor agonist.
Uses: Migraine, moderate pain relief.
Special Considerations: Can cause sedation and dizziness.
Contraindications: Opioid dependence.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Naratriptan (Amerge)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: 5-HT1B/1D receptor agonist, causes vasoconstriction.
Uses: Migraine abortive therapy.
Special Considerations: Longer half-life than sumatriptan.
Contraindications: Ischemic heart disease, uncontrolled hypertension.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Almortriptan (Axert)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: 5-HT1B/1D receptor agonist.
Uses: Migraine abortive therapy.
Special Considerations: Longer half-life, less recurrence.
Contraindications: Cardiovascular disease, MAOIs.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Eletriptan (Relpax)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: 5-HT1B/1D receptor agonist.
Uses: Migraine abortive therapy.
Special Considerations: More potent than sumatriptan.
Contraindications: Cardiovascular disease.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Ergotamine Tartrate (Cafergot)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Non-selective 5-HT receptor agonist, vasoconstrictor.
Uses: Migraine abortive therapy.
Special Considerations: Can cause nausea, vasospasm.
Contraindications: Pregnancy, cardiovascular disease.
Pregnancy/Lactation: Category X, contraindicated in pregnancy.
Dihydroergotamine (DHE)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: 5-HT receptor agonist, vasoconstrictor.
Uses: Refractory migraines.
Special Considerations: Less nausea than ergotamine.
Contraindications: Cardiovascular disease, pregnancy.
Pregnancy/Lactation: Category X, contraindicated in pregnancy.
Topiramate (Topamax)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Blocks voltage-gated Na+ channels, enhances GABA activity.
Uses: Migraine prevention (can be used in children), epilepsy.
Special Considerations: Can cause cognitive slowing, weight loss.
Contraindications: Pregnancy (teratogenic effects).
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Erenumab (Amovig)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Calcitonin gene-related peptide (CGRP) receptor antagonist.
Uses: Migraine prevention.
Special Considerations: SQ injection once monthly.
Contraindications: Hypersensitivity reactions.
Pregnancy/Lactation: Limited data, use with caution.
Best Way to Treat Migraine
Mechanism of Action: Multimodal approach.
Uses: Migraine management.
Special Considerations: Acute treatment: NSAIDs, triptans; Prevention: Beta-blockers, antiepileptics.
Contraindications: Varies by medication.
Pregnancy/Lactation: Consult physician for safest option.
Best Way to Treat Migraine in Children
Mechanism of Action: Pediatric-specific treatment approaches.
Uses: Migraine management in children.
Special Considerations: Acetaminophen, ibuprofen for acute; propranolol, topiramate for prevention.
Contraindications: Avoid triptans in younger children.
Indomethacin (Indocin)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Non-selective COX inhibitor, reduces inflammation.
Uses: Acute gout attack, arthritis.
Special Considerations: Preferred NSAID for gout, but can cause GI toxicity.
Contraindications: GI bleeding, severe renal impairment, cardiovascular disease.
Pregnancy/Lactation: Avoid in third trimester, caution in lactation.
Colchicine (Colcrys)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Inhibits microtubule polymerization, reducing neutrophil activity.
Uses: Acute gout attack, prophylaxis during urate-lowering therapy.
Special Considerations: GI side effects common, dose adjust in renal/hepatic impairment.
Contraindications: Severe renal or hepatic disease, pregnancy.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Allopurinol (Zyloric/Uricto)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Xanthine oxidase inhibitor, reduces uric acid production.
Uses: Chronic gout, tumor lysis syndrome.
Special Considerations: Rash risk (including Stevens-Johnson syndrome), dose adjust in renal disease.
Contraindications: Hypersensitivity, severe renal impairment.
Pregnancy/Lactation: Use caution in pregnancy, limited data in lactation.
Febuxostat (Uloric)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Selective xanthine oxidase inhibitor, reduces uric acid production.
Uses: Chronic gout in patients intolerant to allopurinol.
Special Considerations: Higher CV risk than allopurinol, requires liver function monitoring.
Contraindications: History of cardiovascular disease, severe liver impairment.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Probenecid (Probalan)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Uricosuric, increases renal excretion of uric acid.
Uses: Chronic gout (alternative to xanthine oxidase inhibitors).
Special Considerations: Not effective in renal impairment, can cause kidney stones.
Contraindications: Renal impairment, history of nephrolithiasis.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Pegloticase (Krystexxa)
MOA
Uses
Special Considerations
Contraindications
Pregnancy
Mechanism of Action: Recombinant uricase, converts uric acid to allantoin.
Uses: Chronic refractory gout.
Special Considerations: Risk of infusion reactions, requires premedication with antihistamines/steroids.
Contraindications: G6PD deficiency, severe hypersensitivity reactions.
Pregnancy/Lactation: Avoid in pregnancy, caution in lactation.
Drug of Choice for Acute Gout
Mechanism of Action: Suppresses inflammation in gouty joints.
Uses: Rapid relief of acute gout attacks.
Special Considerations: First-line: NSAIDs (Indomethacin preferred), colchicine if NSAIDs contraindicated, corticosteroids if NSAIDs/colchicine cannot be used.
Contraindications: Varies by drug; NSAIDs contraindicated in renal disease, colchicine in severe hepatic/renal disease.
Pregnancy/Lactation: Avoid NSAIDs in third trimester, colchicine with caution.
Gout Maintenance Drugs
Mechanism of Action: Reduce uric acid levels or increase excretion to prevent flare-ups.
Uses: Prevent recurrent gout attacks, reduce complications.
Special Considerations: Xanthine oxidase inhibitors (Allopurinol, Febuxostat) are first-line; Probenecid is an alternative if uric acid excretion is normal.
Contraindications: Severe renal impairment, hypersensitivity.
Pregnancy/Lactation: Use with caution, consult specialist.
Special Considerations in Gout Treatment
Mechanism of Action: Key factors in managing gout effectively.
Uses: Optimizing treatment strategy for individual patients.
Special Considerations: Start prophylaxis (Colchicine/NSAIDs) when initiating urate-lowering therapy to prevent flares; lifestyle modifications (low-purine diet, reduced alcohol intake) recommended.
Contraindications: N/A
Pregnancy/Lactation: Discuss case-specific recommendations with a specialist.