Acetaminophen is commonly known as [...]
Tylenol
[...] is commonly known as Tylenol
Acetaminophen
True or False: All NSAIDS are ""non-opioid Analgesics"" making acetaminophen an NSAID. [...]
False, Acetaminophen is a non-opioid analgesic like all other NSAIDS but is not an NSAID
Why is acetaminophen not classified as an NSAID? [...]
It does not have anti-inflammatory properties that other NSAIDS have Does have Antipyretic and analgesic affects however.
Acetaminophens chemical name is [...]
Acetyl para-amino phenol (APAP)
Normal dosing for acetaminophen is [...] every 4 hours. Just like aspririn.
650-1000 mg (2/3 tabs)
True or False: Acetaminophen is well absorbed from the GI tract. [...]
True
Acetaminophen is metabolized in the [...]
Liver
What CYP enzyme conjugates acetaminophen in the liver? [...]
CYP2E1
Acetaminophens pharmacological effects are [...] and [...]
Analgesia and Anti-pyresis
The key difference between acetaminophen and other non-opioid analgesics/ NSAIDS is that it does not have [...]
Anti-inflammatory effects
Three important reasons we would use acetaminophen over aspirin: [...], [...], [...]
No GI effects, No association with Reyes Syndrome, Safe to use in pregnancy
What is the maximal dosage set for acetaminophen? [...]
4 g/day Adverse effects are serious enough to set a maximal amount you can use in a day.
What is the major concern associated with using acetaminophen? [...]
Hepatic damage Hepatic damage can increase with long term use. Other possible adverse effects include: skin rash, drug fever and mucosal lesions.
Alcohol consumption increases risk of [...] when combined with acetaminophen use.
hepatic damage
[...] increases risk of hepatic damage when combined with acetaminophen use.
Alcohol consumption
Chronic abuse of acetaminophen can lead to [...]
Nephrotoxicity
What is the overdose toxicity dosage of acetaminophen? [...]
10-25 g, (10-50x greater than normal)
After the first 24 hours of acetaminophen overdose toxicity [...] is the first complaint.
toxicity GI distress
What is the most serious concern of acetaminophen overdose? [...]
Hepatotoxicity
True or False: Hepatotoxicity in acetaminophen overdose is never reversible [...]
False, however, hepatic coma and death do occur
In acetaminophen toxicity, hepatic coma occurs when the formation of a reactive electrophile called [...] inactivates liver proteins.
N-acetyl-p-benzoquinone-imine (NAPQI)
In acetaminophen toxicity, hepatic coma occurs when the formation of a reactive electrophile called N-acetyl-p-benzoquinone-imine (NAPQI) inactivates [...].
liver proteins
[CYP Enzyme] converts excess acetaminophen into NAPQI
CYP2E1
CYP2E1 converts excess acetaminophen into [...]
NAPQI
Preferred treatment of choice for acetaminophen overdose within the first 4 hours? [...]
Activated charcoal Second choic would be vomiting or gastric lavage
What is the preferred treatment for acetaminophen overdose after the first 4 hours? [...]
N-Acetyl-Cystein (Acetadote) Functions to restore endogenous glutathione
Liver damage occurs at about hour [...] of acetaminophen overdose.
8
Important to note: Liver damage is time and concentration dependent, lower toxic levels allow us a longer window to treat toxicicty, higher toxic levels more susceptible for immediate liver damge.
The most common form of arthritis associated with advancing age. [...]
Osteoarthritis
Inflammation is a [major/minor] component of osteoarthritis.
minor
Treatment for most patients with osteoarthritis includes [...] and [...]
Therapy and Acetaminophen
What differentiates osteoarthritis from rheumatoid arthritis? [...]
It is a chronic disease only.
- Rheumatoid arthritis is a chronic disease as well but presents with acute flares of inflammation where osteoarthritis doesn't.
Rheumatoid arthritis is a disease that mainly attacks the [...]
Synovial membranes
What joints are most commonly affected by rheumatoid arthritis? [...]
Small joints of the hands and feet
What is the first line treatment of rheumatoid arthritis [...]
Physical therapy
- Use physical therapy to prevent muscular atrophy
Drugs are a necessary part of the RA treatment plan because they help to [...]
Minimize tissue destruction caused by inflammation
DMARD stands for [...]
Disease-Modifying-Anti-Rheumatic-Drugs
[...] stands for Disease-Modifying-Anti-Rheumatic-Drugs
DMARD
What are the two classes of DMARDS? [...] and [...]
Traditional and Biologic Response Modifiers
Traditional DMARDS compared to Biologics are much [smaller/bigger]
smaller
True or false: Biologics are a much smaller drug than traditional DMARDS. [...]
False, They are a much larger drug than TDMARDS
Traditional DMARDs are commonly delivered [...]
Orally
Biologics are commonly administered via [...]
Injection
True or False: NSAIDs can be used as monotherapeutic drugs in the treatment of RA. [...]
False, They are never sufficient for use in RA, they don't modify the disease like DMARDS do. Commonly see NSAIDs Used in conjunction with DMARDS for acute treatment of pain.
What is the most commonly used glucocorticoid in the treatment of RA? [...]
Prednisone
Although glucocorticoids are are highly effective they are [...]
extremely toxic
Ideally glucocorticoids are not used alone in treatment of RA but are useful as a [...] agent.
bridge
Methotrexate is often abbreviated as [...]
MTX
[...] is a very toxic but very effective TDMARD used for treating RA.
Methotrexate
[...] is generally the first choice drug for initial therapy of RA.
Methotrexate
Methotrexates route of administration is usually [...]
oral
When giving methotrexate, if a provider wanted to prevent hepatotoxicity, they could administer the drug [...]
Subcutaneously
Besides being less hepatotoxic the subcutaneous administration of methotrexate has a better [...] than its oral counterpart.
bioavailability
It takes about [...] for the effects of methotrexate to take effect.
4-6 weeks
Methotrexate is a [chemical] analog.
folic acid
How does methotrexate get in to the cell? [...]
Folate transporters
[...] is the process by which methotrexate gets trapped in a cell.
Poly-glutamation
Methotrexates first mechanism of action is acting as an anti-metabolite to inhibit [...]
Purine and pyrimidine synthesis
- This is important because new cells cant be made without purine or pyrimidine.
methotrexate when acting as an anti metabolite specifically inhibits the enzyme [...] and formation of Tetrahydrofolate (FH4)
Dihydrofolate Reductase (DHFR)
methotrexate when acting as an anti metabolite specifically inhibits the enzyme Dihydrofolate Reductase (DHFR) and formation of [...]
Tetrahydrofolate (FH4)
Whats the second mechanism of action for methotrexate? [...]
Inhibition of the AICAR Transforymylase Enzyme Inhibition of AICAR will inhibit purine synthesis
Inhibition of the AICAR Transformylase enzyme increases the anti-inflammatory mediator [...] in addition to inhibiting purine synthesis.
adenosine
Increased adenosine levels will contribute to the [...] in those with RA
resolution of inflammation
The major mechanism of action for methotrexate is thought to be inhibition of the enzyme [...]
AICAR transformylase
The third mechanism of action for methotrexate is [...]
Inhibition of the thymidylate synthetase enzyme
- Ultimately inhibits proliferation of inflammatory cells.
[...] is a major concern if high doses of methotrexate are given.
Hepatotoxicity
Many of the side effects of methotrexate are related to the induced [...] deficiency it causes.
folate
Methotrexate is eliminated by the [...]
kidneys
Methotrexate is contra-indcated in [...] and [...]
Pregnant women and nursing mothers
- It is considered a teratogenic agent. can be excreted in breast milk
[...] is an anti-malarial drugs that also has anti-inflammatory properties.
Hydroxychloroquine
Hydroxychloroquine is an [...] drugs that also has anti-inflammatory properties.
anti-malarial
Hyrdorxychloroquine is administered [...]
orally
Pt dosing for methotrexate is weekly as opposed to hydroxychlorquine which is [...]
daily
What is the half-life for hydroxychloroquine? [...]
45 days
True or False: Hyrdorxychloroquine has a lifetime dosage limit of 1000 grams. [...]
True
What is the life time dosage limit of hydroxychloroquine? [...]
1000 grams
Long term use of hyrdroxychloroquine can lead to these 2 serious side effects: [...] and [...]
Retinal Damage and Hypoglycemia in Diabetics
Why can Hydroxychloroquine cause retinal damage? [...]
The drug accumulates in melanin-containing tissues, particularly in the eyes.
True or False: Hydroxychloroquine has been reported to have adverse effects in pregnancy and nursing mothers. [...]
False, It has not been reported to have adverse effects in either. It is secredted into breast milk but considered safe.
Which is more toxic, Chloroquine or Hydroxychloroquine? [...]
Chloroquine
Sulfasalizine is a [ Traditional DMARD/Biologic DMARD]
TDMARD
Sulfasalazine is administered [...]
orally
True or False: Sulfasalazine is administered daily. [...]
True
Where is sulfasalzine metabolized? [...]
The Gut, Prior to absorption
When sulfasalazine is metabolized, it is metabolized into what 2 products? [...] and [...]
Salicylate and Sulfapyridine
Common side effects of sulfasalazine? [...], [...] and [...]
GI distress, Anorexia and Skin reactions
What are the 2 major concerns of sulfasalazine use? [...] and [...]
Blood Dyscrasias and Reduced Folate absorption
Triple Therapy is often called [...]
Nebraska Therapy GBR
Leflunomide is a [ TDMARD/Biologic DMARD]
TDMARD
Leflunomide inhibits the enzyme [...] which inhibits pyridine synthesis.
enzyme Dihydro-orotate dehydrogenase
Leflunomide inhibits the enzyme Dihydro-orotate dehydrogenase which inhibits [...] synthesis.
pyridine
What are the 2 overall effects of leflunomide therapy? [...] and [...]
Inhibition of T cell proliferation and Reduced Antibody production by B-cells
True or False: Leflunomide is considered a pro-drug [...]
True
Leflunomide is a drug that is administered [Route], [frequency]
Orally, every day
What contribues to the extremely long effective half-life of leflunomide? [...]
Entero-hepatic recirculation
Two common side effects of luflonamide therapy? [...] and [...]
Diarrhea and Alopecia
What Family of liver enzymes does leflunomide inhibit? [...]
CYP450's
Leflunomide can be both a [...] and [...] drug.
Carcinogenic and Teratogenic
Leflunomide use is strictly and absolutely contraindicated before and during [...]
Pregnancy
Minocycline is a [TDMARD/ Biologic DMARD]
TDMARD
Minocycline inhibits [...]
collagenase
- Also inhibits matri metallo-proteinases
Minocycline is administered [route], [Frequency]
Orally, 1-2x Daily
One grossly visible side effect of minocycline use is [...]
Hyperpigmentation
Biologics are possible because of [...] technology.
Recombinant DNA
True or False: All Biologics are Immunosuppressive Agents. [...]
True
True or False: Biologics act by targeting broad groups of mediators responsible for inflammation. [...]
False, One of the benefits of using biologics is that they target very specific mediators of inflammation.
What are 4 side effects common to all biologics? [...], [...], [...], and [...]
Increased risk of infection, Blood Dyscrasias, Increase cancer incidence, and GI problems
What are the three sub-groups of biologic DMARD's? [...], [...], [...]
Anti-TNF Drugs, T & B Cell targeted drugs, Cytokine specific drugs
[subtype] biologics are the most commonly used biologics in the treatment of RA
Anti-TNF
What are the two types of TNF receptors? [...] and [...]
P55 and P75
Entanercept is an [Subtype] Biologic.
Anti-TNF
Entanercept functions to prevent TNF from binding to its cellular receptor [...]
P75
Etanercept is administered [route] by injection, [frequency]
Subcutaneously, Weekly
[...] has the shortest duration of action of all Anti-TNF biologics used.
Etanercept
What is a new major concern of etanercept use? [...]
Development of Progressive Multifocal Leukoencephalopathy (PML)
Etanercept has a black box warning for [...]
Lymphomas
Infliximab is a [TDMARD/ Biologic DMARD]
Biologic DMARD
Infliximab bind to [...] similar to how etanercept does.
TNF
Infliximab is administered every [Frequency], Via [Route]
4-8 weeks, Via IV
When treating with Infliximab we always combine it with [...] or [...]
MTX or Other t-DMARDS
Infliximab and Etanercept have similar side effects, except infliximab can cause [...] where etanercept does not.
Hypotension
- Should not be used in heart failure patients.
Adalimumab just like infliximab share similar properties in that they are both [...]
Anti-TNF Monoclonal Antibodies
How are adalimumab and Infliximab different in their properties? [...]
Adalimumab is fromed from a fully human protein whereas infliximab is a chimeric protein (Human+ mouse)
Adalimumab is administered [route], [frequency]
Subcutaneously, 2x a month
Adalimumab has similar side effects to other anti-TNF drugs but is also indicated in [...]
Demyelinating Diseases
- Avoid use in patients with demyelinating diseases like multiple sclerosis.
Infliximab is what type of biologic drug? [...]
Anti-TNF drug
Adalimumab is what type of biologic drug? [...]
Anti-TNF drug
Abatacept is what type of biologic drug? [...]
T and B cell targeted drug
Abatacepts mechanism of action is [...]
Inhibition of T-cells
- Specifically inhibitis it by acting as an antaganist to CD28: A known T-cell surface protein that promotes T-cell activation and inflammation.
Abatacept can be administered [Route] every [...] or [Route] every [...]
Every week or Intraveinous every Month
Riuximab is what type of biologic drug? [...]
T and B cell Targeted Drug
Rituximab is an [...] monoclonal antibody.
Anti-CD20
Since rituximab is an anti-CD20 monoclonal antibody it is a [...] inhibitor.
B-Cell
The first month of administration for rituximab is [...] every [...]
IV every 2 weeks
After the initial IV administration of rituximab it not given again for at least [...]
6 months
- Commonly used in combination with MTX
Tocilizumab is what type of biologic drug? [...]
Cytokine specific drug
Tocilizumab speifically acts to inhibit the cytokine [...].
IL-6
[...] speifically acts to inhibit the cytokine IL-6.
Tocilizumab
What is a common complication of tocilizumab use? [...]
GI Perforation w/ Diverticulitis
Tofacitinib is [Enzyme] inhibitor.
Janus Kinase (Jak) inhibitor
Tofacitinib blocks signaling of the cytokine [...]
IL-6
[...] is the only oral biologic agent thusfar.
Tofacitinib
A concern of tofacitinib use is that it increases risk of [...]
VZV reactivation