Pharm Flashcards
NSAID ingredient of topical gel that is perhaps the most effective pain remedy for osteoarthritis
diclofenac
biologic DMARD of limited efficacy, recombinant version of endogenous human IL-1 receptor antagonist
Anakinra
JAK3 antagonist used as a biologic DMARS, novel in that it is orally active
Tofacitinib
Peptide blocker of N-type voltage gated calcium channels administered intrathecally for refractory pain
ziconotide
classic NSAID with COX1 selectivity, remains a drug of choice for treating acute gouty arthritis
Indomethacin
Drugs that relieve pain without causing loss of consciousness
Analgesics
Noteworthy because it suppresses fever and pain but not inflammation, presumably in part by inhibiting prostaglandin synthesis in the CNS
Aceetaminophen
COX-2 inhibitor that can be administered to treat pain and inflammation of RA if the benefits outlay the risk; only member of its class still marketed in the US
Celecoxib
Accumulates outside of the cell as a consequence of AICAR accumulation inside cells due to the action of polyglutamated methotrexate; binds to purinergic GPCR on cell surface to exert anti-inflammatory response
Adenosine
Pts with pain due to RA are often administered NSAIDs or glucocorticoids despite their lack of effect on disease progression while waiting for a drug from this class to begin exerting its effects
DMARD
Abbreviation for a prostaglandin that has widespread effects throughout the body including inc vascular permeability, mucosal protection in the gut, fever in the CNS, pain sensation in the periphery, and salt & water homeostasis in the kidney
PGE-2
What class of drugs do lidocaine and pramoxine that can help treat things such as neuropathic pruritus or pruritus due to CKD belong to?
Local anesthetics
Prototypical bisphosphonate, drug class of first choice for treating osteoporosis, its incorporation into bone inhibits the number and activity of osteoclasts
Alendronate
Osteoporosis monoclonal Ab therapy that binds RANKL (receptor activator of NF-kB ligand) to decrease formation and function of osteoclasts
Denosumab
Potentially lethal consequence of acetaminophen overdosage
Hepatic necrosis
disrupts pyrimidine synthesis, a second choice traditional DMARD due to more common serious adverse effects
Leflunomide
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
This is cleaved from cell membrane phospholipids by phospholipase A2 in response to ‘stimuli’, converted to eicosanoids such as prostaglandins and thromboxjnes
Arachidonic acid
What pt population is at greater risk for serious adverse effects of NSAIDS?
Elderly
Antidote for acetaminophen poisoning, substitutes for depleted glutathione in liver cells
Acetylcysteine
Local anesthetics such as lidocaine interfere with this component of pain sensation
Transmission
The dorsal horn of the SC is where descending inhibitory fibers and various drugs such as ketamine and SNRI’s influence this component of pain sensation
Modulation
Biologic DMARS, fusion protein blocks T cell CD80/86 co-stimulatory signal needed for activation
Abatacept
This structure can be closed prematurely by NSAIDS
Ductus arteriosus
COX that is induced in response to pathologic stimuli; unfortunately its selective blockade was found to inc the risk for vascular thrombosis as balance between local TxA2 and PGI2 was altered to favor platelet aggregation and vasoconstriction
COX-2
Dexamethasone, betamethasone, and triamcinolone are among the ____________ prednisolone, which have much greater potency and/or 1/2 life than natural hydrocortisone
Fluorinated
Fusion protein made from Fc portion of IgG and 2 TNF receptors, a biologic DMARD administered 1-2x/wk by subcutaneous injection; also used for psoriasis
etanercept
a weak mu agonist that also blocks 5-HT and NE re-uptake, used by many to treat moderate to severe pain
tramadol
Damage to this is a serious side effect of hydroxycloroquine, but little risk from low doses now used to treat RA
retina
Expensive non-purine xanthine oxidase inhibitor used for reducing rate levels in those with allopurinol intolerance
Febuxostat
abbreviation for the class of antidepressant drugs having the most evidence of benefit for treating neuropathic pain; SE’s include dry mouth, constipation, tachycardia, palpitations, nausea and sedation
TCA
Drugs that lower serum urate levels by increasing its fractional excretion by the kidneys
Uricosuric
SERM with agonist effects on bone but not breast or uterus used to treat osteoporosis
Raloxifene
Bisphosphonate administered by IV injection once per year; also assoc with highest incidence of osteonecrosis of the jaw
Zolendronic acid
Antagonist at NMDA-type glutamate receptors that relieves pain, widely used veterinary anesthetic also used to reduce amount of morphine needed by humans; SE’s are agitation and hallucination
Ketamine
Blocks urate reabsorption by URAT1 transporter in PCT to inc fractional excretion of filtered urate in the urine
Probenecid
happens during the initial phase of aspirin poisoning
Respiratory alkalosis
Blocking the effects of this inflammatory mediator is a common target when treating RA and various other autoimmune diseases
TNF
Calcitonin from this species has a longer 1/2 life and greater potency than human calcitonin, can be administered intranasally or parenterally to treat established osteoporosis
Salmon
What is the preferred/standard of care therapy for treatment of recurrent gout if low GFR or past urate stone or to reduce effects of urate overproduction from things such as tumor lysis syndrome?
allopurinol
Type of nociceptive pain that tends to be poorly localized, deep, dull and cramping
Visceral
abruptly doing this with exogenous glucocorticoids can be deadly
Stopping
Mammalian enzyme that converts uric acid to allantoin, mutated/nonfuncitonal in humans
Uricase
Antiepileptic drug also used to treat neuropathic pain of diabetes, shingles and fibromyalgia
pregabalin
Abbreviation for the prostaglandin formed by endothelial cells that causes local vasodilation and inhibits platelet aggregation
PGI2
Its presence greatly increases risk of developing gastric ulcer in response to NSAID therapy
H. Pylori
This can be triggered by aspirin, presumably because local leukotriene effects predominate over prostaglandin effects
Asthma
biologic DMARd that is humanized antihuman IL-6 receptor Ab, among its effects is to dec acute phase response of the liver
Tocilizumab
1-34 PTH, only agent that forms bone but must be administered in a pulsed manner otherwise leads to bone resorption
Teriparatide
nature of the interaction between COX and aspirin, but not other NSAIDs
irreversible
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
Allopurinol is among the widely used drugs that can cause this potential syndrome of epidermal necrolysis
steven johnson syndrome
absolute contraindication for tx of RA with methotrexate, reason to choose hydroxychloroquine instead
Pregnancy
NSAID notable for often being administered IM or IV
Ketorolac
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
uricosuric agent acting similar to probenecid, both require GFR > 60
Sulfinpyrazone
Exerts its pain relieving effects by binding to the alpha2-Delta subunit of N-type voltage-gated Ca channels (contrary to what its name might suggest)
Gabapentin
Happens to methotrexate, appears to be responsible for its low dose ability to treat RA and reason its beneficial effects persist for some time after drug discontinuation
polygutamation
opioids, alpha2-agonists and general anesthetics are among the pharmacological agents that interfere with this component of pain
perception
alpha2-adrenergic agonist administered IV for pain and sedation
Dexmedetomidine
Antimalarial that is also a traditional DMARD used alone or in combo, alters Ag presentation by disrupting lysosomal pH
hydroxychloroquine
non-aspirin NSAID with long 1/2 life that can be useful for treating inflammation and/or pain of arthritis, a recommended drug of choice when benefits still outweigh concurrent CV risks
naproxen
never do this with biologic DMARDs
combine
drug class associated with atypical fractures (ex. simple fracture of compact bone such as the shaft of the femur)
bisphosphonates
seen during second potentially lethal phase of salicylate poisoning
Metabolic acidosis
COX that is constitutive in all tissues, has physiological role and contributes to pathological responses
COX-1
Abbreviation for the thromboxane synthesized by platelets that causes vasoconstriction and promotes platelet aggregation
TXA-2
Chimeric (human and mouse) monoclonal Ab directed against TNF that can be administered IV every 6wks as a biologic DMARD
infliximab
methotrexate, hydroxychloroquine, and sulfasalazine are examples of this type of DMARD
traditional
Relieves inflammation from gout if administered with 12-24hrs of sx onset by blocking the tubular polymerization (microtubule formation) needed by leukocytes of migration and phagocytosis; can cause GI distress when used for prophylaxis
colchicine
AutoAbs present in a majority of RA pts target arginine residues in proteins that have been converted to this
Citrulline
Targets CD20 Ag of B cells to cause a B cell ‘do-over’ used to treat non-hodgkin lymphoma and CLL, and can be effective in some Ab-dependent autoimmune diseases
rituximab
along with chondroitin, widely used in hopes of treating osteoarthritis but little evidence of benefit beyond placebo effect
Glucosamine
can occur in the jaw of people using bisphosphonates, can be triggered by dental work
Osteonecrosis
These cells are particularly vulnerable to the effects of aspirin as they cannot synthesize replacement COX
platelets
PEGylated version of recombinant mammalian uricase used to treat chronic gout in those refractory to conventional therapy
Pegloticase
Dietary supplements for adolescents, postmenopausal women and elderly to treat mild hypocalcemia by facilitating bone growth or limited bone loss
Calcium salts
non-PEGylated recombinant uricase administered for prevention of acute uric acid nephropathy due to tumor lysis syndrome
Rasburicase
What is the common triple therapy used to treat RA?
Methotrexate
hydroxychloroquine
Sulfasalazine
**all used together
Pain due to nerve damage rather than stimulation of nociceptors
Neuropathic
anti-TNF biologic DMARD, this is humanized monoclonal Ab administered subcutaneously every 2 weeks; also used for psoriatic arthritis, ankylosing spondylitis, Crohn’s disease
Adalimumab
irreversible COX inhibitor used to relieve inflammation and pain of RA, does not alter disease progression
Aspirin
Capsaicin and camphor stimulation of these receptors gives a sensation of “heat” that can be useful counterirritant to reduce pain
TRPV-1
“Cold” receptor stimulated by menthol in IcyHot
TRPM-8
