Tx of Bone and Joint Disorders (Part II) Flashcards
NSAID’s – Naproxen Sodium: sub class ?
propionic acid
Naproxen Sodium trade ?
Naprosyn
Alieve
Naproxen Sodium indications ?
Anti-inflammatory
Osteoarthritis Rheumatoid arthritis Acute gout Mild – Moderate Pain Dysmenorrhea Fever
Naproxen Sodium adult dosing ?
220, 275, 550 mg naproxen sodium = 200, 250, 500 mg naproxen
Special Ped’s dosing 11-22 mg/kg/day
Divided dose q8-12 hrs
Naproxen Sodium BBW / caution ?
CABG / CAD / CHF / PUD
- *Watch its with NSAIDS if they are post CABG
- *
Naproxen Sodium preg. cat ?
C
IR(Imed release) doses expressed as ?
naproxen sodium
ER (extended release) doses expressed as ?
naproxen equivalents
NSAID Combo Cytoprotective example ?
Diclofenac/misoprostol
Diclofenac/misoprostol trade ?
Arthrotec
Cytotec)
Diclofenac/misoprostol (Arthrotec, Cytotec) MOA ?
Acts upon gastricparietal cells inhibiting the secretion ofgastric acid
Stimulate increased secretion of the protective mucus that lines theGI tractand increase mucosal blood flow, thereby increasing mucosal integrity
Misoprostol trade ?
Arthrotec, Cytotec
Misoprostol indicated ?
Indicated NSAID induced ulcer or protection
Misoprostol inhibits ____________ secretion and mucosal __________ ?
Inhibits gastric acid secretion and mucosal protections
Misoprostol used with ?
NSAID’s / ASA
Used in early pregnancy termination
**long standing NSAIDS use you want to use these protection agents
the proactive agents are used to stimulate contractions or bleeding after delivery for uterine bleeding agent **
Misoprostol BBW ?
Black Box warning with pregnancy / miscarriage, induce labor, uterine rupture
NSAID that has been discontinued in the US because of renal disease ?
Nabumetone (Relafen)
Muscle Relaxants examples ?
Metaxalone
Cyclobenzaprine
Baclofen
Tizanidine
Metaxalone trade ?
Skelaxin
Metaxalone (Skelaxin)
MOA ?
exact mechanism of action unknown; depresses CNS activity (centrally-acting muscle relaxant)
Metaxalone (Skelaxin)
indication ?
MS pain / Spasm
Metaxalone (Skelaxin) caution in ?
renal / Liver Dz
Metaxalone (Skelaxin) dosed ?
Dosed 800 mg tid/qid
Metaxalone (Skelaxin) is give on ______ stomach ?
empty
Metaxalone (Skelaxin) preg cat ?
C
Metaxalone (Skelaxin) peds ?
12 years old
Metaxalone (Skelaxin)
common reactions ? low incidence ?
drowsiness
dizziness
headache
nervousness
nausea
vomiting
dyspepsia
low incidence
Cyclobenzaprine trade ?
Flexeril
Cyclobenzaprine (Flexeril)
MOA ?
potentiates norepinephrine and binds to serotonin receptors, reducing spasticity (centrally-acting muscle relaxant)
Cyclobenzaprine (Flexeril)
indications ?
Muscle Spasm
Cyclobenzaprine (Flexeril)
dosing ?
Dosing 5-10 mg tid up to three weeks
Cyclobenzaprine (Flexeril)
pregnancy category ?
B
Cyclobenzaprine (Flexeril)
cautions ?
anticholinergic effects
CNS depression
lowers seizure threshold
Cyclobenzaprine (Flexeril)
can cause serotonergic effect which include what sxs ?
Increased heart rate, shivering, sweating, dilated pupils, myoclonus (intermittent jerking or twitching)
Hyper-reflexia
Hyperactive bowel sounds, high blood pressure
Hyperthermia - temperature as high as 40°C (104°F).
Baclofen trade ?
Lioresal
Baclofen (Lioresal)
class ?
GABA receptor Stimulant (agonist)
_____________ is an amino acid which acts as a neurotransmitter in the central nervous system.
Gamma-Amino Butyric acid(GABA-b)
Baclofen (Lioresal)
inhibits _____ ___________ in the brain, calming nervous activity
nerve transmission
Baclofen (Lioresal)
: “ Think of it as a ___ depressant “
CNS
Baclofen have what effects ?
Sedative effects (anxiolytics)
Baclofen MOA ?
Inhibits monosynaptic and polysynaptic spinal reflexes (centrally-acting muscle relaxant)
Baclofen indication ?
Spacity
A beneficial property of ________ is thattoleranceto its muscle-related therapeutic benefits
baclofen
Baclofen retains its therapeutic anti-spasmodic effects even after ?
many years of continued use
- *can be on these for a while and you dont become resistance - continuously same dose (no tolerance)
- *
Discontinuation of baclofen can be associated with a ?
withdrawal syndrome
** you can get WD sxs. - taper it cause we dont want spastic sxs. **
Resemblesbenzodiazepine or alcohol withdrawal ?
Baclofen WD
Baclofen route ?
PO / Intrathecal
Baclofen pump
**intrathecal cath. into L2 or L3 that is not a dispensing
it is set at a standard dose and they can get an extra dose by hitting the button
the port underneath the skin and they go in a fill back up the port depending on the dosage depends on how frequently you need to refill **
Tizanidine trade ?
Zanaflex
**non-narcotic narcotic **
Tizanidine (Zanaflex)
MOA ?
Centrally acting alpha-2 adrenergic receptor agonist (centrally-acting muscle relaxant)
Tizanidine (Zanaflex)
indication ?
spasticity
Tizanidine (Zanaflex)
dosing ?
Start at 2mg PO q6-8hr
Goal of Drugs Used to Treat Gout are used because they ?
End painful attacks of gout
Prevent the formation of uric stones in the kidney
Prevent complications from uric stone formation in the joints
Drugs Used to Treat Gout examples NSAID ?
Indomethacin or Indometacin (Indocin)
Indomethacin sub class?
Acetic acid
Indomethacin inhibits ?
production of prostaglandins
Indomethacin indication ?
Acute Gout
OA / RA
Bursitis / Tendonitis
Dysmennorrhea
Peds IV dosing for patient ductus arteriosus
Indomethacin (Indocin)
side effects same as ?
non-selective COX inhibitors / NSAIDS
Indomethacin (Indocin)
side effects ?
mostly renal
Edema from fluid retention
Hyperkalemia
Hypernatremia
HTN
Indomethacin cautions ?
HTN / CAD / CHF / Renal Dz / PUD
Indomethacin preg cat ?
C
Indomethacin dosing ?
25-50mg TID
Drugs Used to Treat Gout: Allopurinol trade ?
Zyloprim
Allopurinol (Zyloprim)
MOA ?
Inhibits the enzyme xanthine oxidase in purine metabolism
Allopurinol (Zyloprim)
blocks ?
formation of uric acid
Allopurinol (Zyloprim)
reduces ?
serum uric acid
Allopurinol (Zyloprim)
clinical uses ?
Chronic gouty arthritis (prophylaxis)
Prevention of uric acid calculi (common kidney stones)
Hyperuricemia (excess serum uric acid)
Calcium oxalate calculi (most common kidney stone)
Tumor Lysis Syndrome from chemotherapy (generates large quantities of nucleic acids, the purines )
Allopurinol (Zyloprim)
indication ?
Chronic gouty arthritis (prophylaxis)
NEVER in acute attack
Allopurinol (Zyloprim)
dosing ?
200-600 mg/day divided qd-qid
Allopurinol (Zyloprim)
preg cat ?
C
Drugs Used to Treat Gout: Cholchicine trade ?
Colcrys
Generic
Cholchicine: Toxic natural plant alkaloid extracted from Colchium plant believed to interfere with ?
WBC function, affecting the inflammatory response
Colchicine does not affect ______ levels in the serum ?
uric acid
Hyperuricemia
Colchicine (Generic)
clinical uses ?
treatment of acute gout attacks
Colchicine (Colcrys) side effects ?
GI at high doses
Diarrhea and stomach upset
Neutropenia
Damage bone nmarrow – anemia
Corneal clouding
Peripheral neuropathy
Colchicine (Colcrys)
facts ?
Generic production halted
Trade $$$$
Colchicine (Colcrys) route ?
PO
Colchicine (Colcrys) dosing ?
1.6 mg PO x1 then, 0.6 mg (30ea): $220.57
prevention is 0.6 bid
Colchicine (Colcrys) preg cat ?
C
Colchicine (Generic)
extreme caution in ?
renal patients
Drugs Used to Treat Gout : Probenecid trade ?
Probalan
Probenecid (Probalan)
MOA ?
Lowers serum levels of urate (hyperuricemia) by competitive inhibition of reabsorption in the renal tubules
increases uric acid excretion in the urine
Probenecid (Probalan)
clinical uses ?
Chronic gout
Hyperuricemia
Gonorrhea or neurosyphillis by delaying the excretion of penicillin
Drugs Used to Treat Gout : Sulfinpyrazone trade ?
Anturane
Sulfinpyrazone (Anturane)
MOA ?
Inhibits reabsorption of urates at the proximal tubule
Similar to probenecid
Increases uric acid excretion
COX-2 example ?
Celecoxib (Celebrex)
Only remaining COX-2 on the market ?
Celecoxib (Celebrex)
Celecoxib (Celebrex)
MOA ?
Inhibits prostaglandin synthesis by decreasing the activity of the COX-2 enzyme
Celecoxib (Celebrex)
does NOT exhibit ?
antiplatelet activity
Celecoxib (Celebrex)
clinical uses ?
Rheumatoid arthritis
Osteoarthritis
- Most common joint disorder in the United States
- Increased incidence of self-medication
- Degree of joint pain and dysfunction guides intervention
Dysmenorrhea
Systemic oral corticosteroids
are ?
Anti-inflammatory agents
Systemic oral corticosteroids
clinical uses ?
RA / OA
Acute Gout
Asthma: short-term burst therapy
COPD
Replacement therapy in adrenal insufficiency
Crohn’s disease
people who cant tolerate GOUT medications ( b/c kidney disease) then steroids are good for them
Systemic oral corticosteroids
examples ?
Hydrocortisone (Solu-Cortef)
Prednisone (Deltasone)
Methylprednisolone (Solu-Medrol)
Systemic oral corticosteroids contraindications ?
serious fungal, viral, or tubercle skin infection
Diabetes
Hydrocortisone trade ?
Solu-Cortef
Hydrocortisone (Solu-Cortef) route ?
IV / IM / PO
Hydrocortisone (Solu-Cortef) example doses ?
Solumedrol Medrol Dose Pack Prednisone Taper Dose Prednisone Decadron Prelone elixir
Hydrocortisone (Solu-Cortef) dosing ?
100-500 mg IM / IV
DMARDs Influence the disease process of rheumatoid arthritis by ?
preventing bone loss and cartilage erosion
DMARDs Are prescribed in combination with ?
biologic modifiers (such as etanercept, inflixamab) or in multiple drug regimens with :
NSAIDs
other DMARDs
w or w/o CCS
DMARDs examples ?
Methotrexate
Methotrexate trade ?
Rheumatrex, Trexall)
Methotrexate MOA ?
immunosuppressant
inhibits dihydrofolate reductase
inhibits lymphocyte proliferation (folate antagonist)
Folate antimetabolite that inhibits DNA synthesis
Methotrexate Appears to act as a _____________ with multiple effects when used to treat arthritis
cell anti-proliferative
for CA and mitochondrial proliferation
Methotrexate indications ?
RA Severe psoriasis ALL Osteosarcoma Ectopic Pregnancy SLE
Methotrexate BBW ?
Fetal death
Hepato-toxicity
Pulmonary toxicity – fibrosis
Tumor Lysis Syndrome
GI Toxicity
Methotrexate route ?
IV / PO form
Methotrexate side effects ?
Pulmonary Fibrosis
for these people on it long term they need serial CXRs
Blurred vision / transient blindness
Alopecia
N/V diarrhea
Anemia, Thrombocytopenia
bone marrow supression
Neuropathy
Hyperuricemia
make GOUT worse
**respiratory sxs. with this medication - pulmonary fibrosis **
Leflunomide is a ?
DMARDs
Leflunomide trade ?
Arava
Leflunomide (Arava) facts ?
1998 minimal use today
Indicated for RA, Crohns, Sarcoidosis
Immunomodulator
It is apyrimidine synthesis inhibitor (mitochondrial enzyme) reduction lymphocytes
Reduces signs and symptoms of rheumatoid arthritis and slows the progression of its associated joint damage
DMARDs:Hydroxychloroquine trade ?
Plaquenil
Hydroxychloroquine (Plaquenil)
suspected to decrease ?
T-cell response
Hydroxychloroquine (Plaquenil)
clinical uses ?
Used for years for treatment of malaria
Severe RA
Systemic lupus erythematous
Hydroxychloroquine (Plaquenil)
can cause ___________________ w/ resultant _________
irreversible retinopathy with resultant blindness;
ensure patient undergoes frequent eye examinations
Vomiting, Headache common
Used more so when others have failed
Gold Salts are ?
Ionic chemical compounds of gold
Gold Salts are used primarily to ?
reduce inflammation and to slow disease progression in patients with rheumatoid arthritis
Mechanism by which gold drugs affect arthritis is unknown
Slow acting
Toxic
Agents of last resort
Gold Compounds examples ?
Aurothioglucose suspension (Solganal)
Gold sodium aurothiomalate (Myochrysine)
Auranofin (Ridaura)
Auranofin trade ?
Ridaura
Auranofin (Ridaura)
is _____ acting and can be ____
slow
toxic
Rarely used today due to the advent of TNF
like last resort options for RA
Auranofin (Ridaura)
administered ?
IM
PO (lower efficacy)
Immune Modifying Agents or Biologicals
are used when ?
When corticosteroids fail or require long term therapy
Immune Modifying Agents or Biologicals not used in ?
acute flare-ups
__________ therapy that targets the rheumatoid process
Anticytokine
Tumor Necrosis Factor Inhibitors examples ?
Etanercept (Enbrel)
Infliximab (Remicade):
Adalimumab (Humira)
Anakinra (Kineret)
Etanercept (Enbrel): TNF receptor joined to a ______ ___ molecule
huma IgG
Infliximab (Remicade): _____________ monoclonal antibody
mouse/human
Adalimumab (Humira): TNF-inhibiting ___________?
anti-inflamatory
Anakinra (Kineret) blocks ?
interleukin-1
Class: Tumor Necrosis Factor (TNF) Inhibitors
examples ?
infliximab (Remicade)
etanercept (Embrel)
Adalimumab (Humira)
**use in OA, RA and crohns **
TNF inhibitors BBW ?
Chronic or recurrent infection
Pulmonary and extrapulmonary tuberculosis (TB)
Invasive fungal infections and other opportunistic infections incl. Legionella and Listeria
Consider all patients to be immunosuppressed! - if respiratory sxs.
TNF indications ?
Rheumatoid Arthritis
Ankylosing Spondylitis
Paoriasis
Crohns
Ulcerative Colitis
TNF reactions
serum sickness
infection, sepsis, pneumonia, opportunistic infection, tuberculosis, malignancy, lymphoma, hepatosplenic T-cell lymphoma (peds pts), leukemia, HBV reactivation, hepatotoxicity, CHF
anaphylactoid rxn
hypersensitivity rxn
**can cause malignancies to be exacerbated and CHF and patients will retain water **