Anti-inflammatories, Biologics, Corticosteroids, Gout, & Osteoporosis Flashcards
Peptide blocker of N-type voltage gated calcium channels administered intrathecally for refractory pain
Ziconotide
PEGylated version of recombinant mammalian uricase used to treat chronic gout in those refractory to conventional therapy
Pegloticase
NSAID ingredient of topical gel that is perhaps the most effective topical pain remedy for osteoarthritis
Diclofenac
Can occur in the jaw of people using bisphosphonates (or denosumab); can be triggered by dental work
Osteonecrosis
Osteoporosis monoclonal antibody therapy that binds RANKL (receptor activator of nuclear factor kappaB ligand) to decrease formation and function of osteoclasts
Denosumab
Patients with pain due to rheumatoid arthritis are often administered NSAIDs or glucocorticoids despite their lack of effect on disease progression while waiting for a drug from this class to begin exertings its effects
DMARD
Classic NSAID with COX1 selectivity, remains a drug of choice for treating acute gouty arthritis
Indomethacin
The interaction between cyclooxygenase and aspirin is _________, which is not the case as with the other NSAIDs
Irreversible
Patient population at greater risk for serious adverse effects of NSAIDs
Elderly
Uricosuric agent acting similar to probenicid, both require GFR >60 ml/min
Sulfinpyrazone
Disrupts pyrimidine synthesis, a second-choice traditional DMARD due to more common serious adverse effects
Leflunomide
Exerts its pain-relieving effects by binding to the alpha-2-delta subunit of N-type voltage-gated calcium channels
Gabapentin
Anti-TNF biologic DMARD, this humanized monoclonal antibody is administered subcutaneously every 2 weeks; also used for psoriatic arthritis, ankylosing spondylitis, and Crohns disease
Adalimumab
Antagonist at NMDA-type glutamate receptors that relieves pain; also used to reduce amount of morphine needed by humans; adverse effects include agitation and hallucinations
Ketamine
Fusion protein made from Fc portion of IgG and two TNF receptors, a biologic DMARD administered 1-2x/week by subcutaneous injection; also used for psoriasis
Etanercept
______ syndrome is associated with swelling of the liver and brain due to use of aspirin by children with viral illness
Reye
_________ of methotrexate is associated with its low-dose ability to treat RA and the persistence of beneficial effects for some time after drug discontinuation
Polyglutamation
Drugs such as lidocaine and pramoxine that can help treat neuropathic pruritis or pruritis due to CKD
Local anesthetics
Cyclooxygenase that is induced in response to pathologic stimuli; unfortunately, its selective blockade was found to increase risk for vascular thrombosis as balance between local TXA2 and PGI2 was altered to favor platelet aggregation and vasoconstriction
COX-2
Refers to the use of methotrexate, hydroxychloroquine, and sulfasalazine together to treat RA
Triple therapy
Relieves inflammation from gout if administered within 12-24 hrs of symptom onset by blocking the tubulin polymerization (microtubule formation) needed by leukocytes of migration and phagocytosis; can cause GI distress when used for prophylaxis
Colchicine
Cleaved from cell membrane phospholipids by PLA2 in response to ‘stimuli’, converted to eicosanoids such as prostaglandins and thromboxanes
Arachidonic acid
Synthesized by platelets; causes vasoconstriction and promotes platelet aggregation
TXA2
Classic alpha2-adrenergic agonist administered PO to reduce blood pressure, also administered intrathecally as adjunct therapy for severe cancer pain not treated effectively by opioids alone
Clonidine
Can be triggered by aspirin, presumably because local leukotriene effects predominate over prostaglandin effects
Asthma
Enzyme that converts uric acid to allantoin, mutated/nonfunctional in humans
Uricase
Biologic DMARD of limited efficacy, recombinant version of endogenous human IL-1 receptor antagonist
Anakinra
Calcium-receptor sensitizer, acts to lower PTH secretion in chronic kidney disease
Cinacalcet
Most effective and fastest acting of the traditional DMARDs, monitor for myelosuppression but generally well tolerated at low doses, often added to biologic DMARDs
Methotrexate
Formed by endothelial cells that causes local vasodilation and inhibits platelet aggregation
PGI2
Antiepileptic drug also used to treat neuropathic pain of diabetes, shingles, and fibromyalgia
Pregabalin
Dexamethasone, betamethasone, and triamcinolone are among the _________ prednisolones, which have much greater potency and/or half life than natural hydrocortisone
Fluorinated
Allopurinol is among the widely used drugs that can cause this potential syndrome of epidermal necrolysis
Stevens Johnson
Class of drugs widely used for tx of pain and inflammation, but significant CV/Resp/Renal/GI contraindications and can cause HSR skin reactions
NSAIDs
Cells that are particularly vulnerable to the effects of ASA as they cannot synthesize replacement cyclooxygenase
Platelets
Class of antidepressant drugs having the most evidence of benefit for treating neuropathic pain; AEs include dry mouth, constipation, tachycardia, palpitations, nausea, and sedation
TCAs
Nonpegylated recombinant uricase administered for prevention of acute uric acid nephropathy due to tumor lysis syndrome
Rasburicase
Capsaicin and camphor stimulation of ________ gives a sensation of “heat” that can be a useful counterirritant to reduce pain
TRPV1
“Cold” receptor stimulated by menthol in IcyHot
TRPM8
Prostaglandin that has widespread effects throughout the body including increasing vascular permeability, mucosal protection in the gut, fever in CNS, pain sensation in the periphery, and salt/water homeostasis in the kidney
PGE2
Cyclooxygenase that is constitutive in all tissues; has physiologic role and contributes to pathologic responses
COX-1
Blocking the effects of ______ inflammatory mediator is a common target in tx of RA and various other autoimmune diseases
TNF
Chimeric (human and mouse) monoclonal antibody directed against TNF that can be administered IV every 6 weeks as a biologic DMARD
Inflixumab
COX-2 inhibitor that can be administered to tx pain and inflammation of RA if benefits > risks (e.g., if pt has ulcers, bleeding risk); only member of its class still marketed in US
Celecoxib
JAK3 antagonist used as a biologic DMARD, novel in that it is orally active
Tofacitinib
Expensive non-purine xanthine oxidase inhibitor useful for reducing urate levels in those with allopurinol intolerance
Febuxostat
Blocks urate reabsorption by URAT1 transporter in proximal tubule to increase fractional excretion of filtered urate in urine
Probenicid
Alpha-2-adrenergic agonist administered IV for pain and sedation
Dexmedetomidine
Agent used as a traditional DMARD alone or in combo and also to tx IBD, GI side effects are a common reason for discontinuing
Sulfasalazine
Glucocorticoid, prednisolone prodrug, short-term use is useful in therapy for RA until DMARD effects are seen
Prednisone
Non-aspirin NSAID with long half-life that can be useful for treating inflammation and/or pain of arthritis, a recommended drug of choice when benefis still outweigh concurrent cardiovascular risks
Naproxen
Along with chondroitin, widely used in hope of treating osteoarthritis but little evidence of benefit beyond placebo effect
Glucosamine
Damage to the ______ is a serious side effect of hydroxychloroquine, but little risk from low doses now used to treat RA
Retina
Antidote for acetaminophen poisoning, substitutes for depleted glutathione in liver cells
N-acetylcysteine
Targets CD20 antigen of B cells to cause a B cell “do-over”, used to treat NHL and CLL and can be effective in some antibody-dependent autoimmune diseases
Rituximab
Absolute contraindication for tx of RA with methotrexate, reason to choose hydroxychloroquine instead
Pregnancy
Bisphosphonate administered by IV injection once per year; also associated with highest incidence of osteonecrosis of the jaw
Zolendronic acid
NSAID notable for often being administered IV or IM
Ketorolac
Suppresses fever and pain but not inflammation, presumably in part by inhibiting prostaglandin synthesis in the CNS
Acetaminophen
Drugs that lower serum urate levels by increasing its fractional excretion by the kidneys
Uricosurics
Refers to the pt with hyperuricemia due to excess synthesis, excess diet intake, and/or excess cell turnover (e.g., tumor lysis syndrome)
Overproducer
Antimalarial also used as a traditional DMARD; used alone or in combo, alters antigen presentation by disrupting lysosomal pH
Hydroxychloroquine
1-34 PTH, only agent that forms bone but must be administered in PULSED manner…otherwise leads to bone resorption
Teriparatide
Methotrexate, hydroxychloroquine, and sulfasalazine are examples of this type of DMARD
Traditional
A weak mu agonist that also blocks 5-HT and NE reuptake, used by many to tx moderate to severe pain
Tramadol
Biologic DMARD that is a humanized antihuman IL-6 receptor antibody, among its effects is to decrease acute-phase response of liver
Tocilizumab
Drug class associated with atypical bone fractures (e.g., simple fracture of compact bone like femur)
Bisphosphonates
Calcitonin from this species has a longer half-life and greater potency than human calcitonin, can be administered intranasally or parenterally to treat established osteoporosis
Salmon
_______ accumulates outside the cell as a consequence of AICAR accumulation inside cells due to action of polyglutamated methotrexate; binds to purinergic GPCR on cell surface to exert anti-inflammatory response
Adenosine
Competitive xanthine oxidase inhibitor that lowers serum urate levels, preferred/standard-of-care therapy for tx of recurrent gout if low GFR or past urate stone or to reduce effects of urate overproduction (e.g., due to tumor lysis)
Allopurinol
SERM with agonist effects on bone but not breast or uterus used to treat osteoporosis
Raloxifene
Prototypical example in drug class of first choice for treating osteoporosis, its incorporation into bone inhibits the number and activity of osteoclasts
Alendronate
Irreversible COX inhibitor used to relieve inflammation and pain of RA, dose not alter disease progression
Aspirin
Biologic DMARD, fusion protein blocks T cell CD80/86 co-stimulatory signal needed for activation
Abatacept
