Lecture 18 Pharm Treatment Flashcards
Decrease stimulation of pain receptors
NSAIDS
APAP
What type of drug blocks conduction of pain signals?
anesthetics
What type of drug decreases pain reaction?
Narcotics
Pain is difficult to catch up with. When should analgesics be given?
Before pain increases
Corticosteroids increase or decrease blood sugar
increase
Corticosteroids increase or decrease sympathetic response
increase
Corticosteroids increase or decrease WBC’s
decrease
lower immune response
Corticosteroids increase or decrease cell injury
decrease
stabilize intracellular lysosomes
Corticosteroids increase or decrease inflammation
decrease
inhibit histamine, kinkins and prostaglandins
What is the prototype corticosteroid?
prednisone
Name 4 uses for Prednisone
Immunosuppressants
Decrease cell injury
Anti-inflammatory
Inhibit collagen synthesis - decrease scar tissue formation
What disease is prednisone used as replacement therapy?
Addison’s disease
What else are corticosteroids used to treat?
prevent organ transplant rejection auto-immune allergic reactions inflammation cerebral edema
Hydrocortisone is (more/less) potent than Dexamethasone and Betamethasone
LESS
What are some adverse effects of corticosteroids?
Hyperglycemia
Cushing’s syndrome
Decreased immune response
What glands will long term use will cause suppression of?
adrenal glands
What is important to remember when taking someone off long term use?
Taper with hydrocortisone
Can you administer live vaccines with corticosteroids?
NO bc decrease WBC’s
Why should you use caution when giving these to diabetics?
uncontrolled sugar levels
Name two negative effects of corticosteroids on the GI and skeletal systems
Peptic Ulcer Disease
Osteoporosis
Are corticosteroids safe for pregnant women?
no
How do NSAIDS work
Block production of prostaglandins via COX inhibition
What NSAID is the prototype and used for its cardiac benefits?
COX-1
ASA
irreversibly inhibits platelet aggregation
Name some diseases that NSAIDS are used to treat?
Rheumatoid arthritis
Osteoarthritis
Gout
Are NASIDS well absorbed?
yes
Do you need to monitor pt with renal and liver problems on NSAIDS?
yes
renal excretion
enterohepatic recycling
What is the main side effect of NSAIDS?
GI problems
nasuea, vomiting, GI bleeding, ulceration
Therapeutic dosing of NSAIDS for inflammation is (higher/lower) than over the counter dosing
much higher
What NSAIDS has opioid like effects but not addictive?
Ketorolac
Para-aminophenols
tylenol
2 uses of para-aminophenols:
fever reduction (antipyretic) pain reliever (analgesic)
Name 3 advantages of para-aminophenols over NSAIDS
no GI problems
no allergies
no bleeding
Name a disadvantage of para-aminophenols compared to NSAIDS and corticosteriods
poor anti-inflammatory action
What is the one major side-effect of para-aminophenols?
Liver toxicity
What is the prototype narcotic?
morphine
What type of receptors are activated in the thalamus and limbic system with narcotics?
mu
What are two major side effects of narcotics?
addiction
withdrawal
Why does someone have to keep increasing their dose to illicit the same effects of a narcotic?
tolerance build up
Why does codeine not have any affect on some people?
it is a pro-drug that some can’t metabolize into its active form
What opioid has a lot of side effects?
oxymorphone
What are the benefits of drug combinations with opioids?
antipyretic
less opiate given
What is one thing to watch out for in combination narcotic drugs?
APAP accumulation from multiple sorces
Methotrexate (MTX) falls under what category of DMARDs?
Non-biologics
What does MTX tx?
RA and some malignancies
A pt comes into your office and they leave with a dx of RA. What’s your first line of tx?
Methotrexate: alone or with a biologic combo
What’s the MOA for Methotrexate?
↓ cell proliferation
↑ apoptosis of T cells
↑ adenosine release (potent inhibitor of inflammation)
Alters expression of CAM (cellular adhesion molecules)
Inhibits pro-inflammatory cytokines
What are some side effects of MTX?
*Mucosal ulcers Nausea* (common chemo side effects) Stomatitis Diarrhea Alopecia Anemia
An RA pt comes in for a f/u who has been successfully tx with MTX and tells you she is pregnant. What should you do?
First congratulate her then CHANGE HER MEDS
TRUE or False: MTX is okay to use during pregnancy.
FALSE FALSE FALSE
Leflunomide (Arava) is what type of drug?
Non-biologic
What it the MOA of Leflunomide?
Inhibits mitochondrial dihydroorotate dehydrogenase (DHODH) ultimately resulting in decreased DNA and RNA in rapidly dividing cells
TRUE or FALSE: Leflunomide is okay to use during pregnancy
LeFALSEomide
Sulfasalazine (Azulfidine) is what type of drug?
Non-biologic
What is the MOA of Sulfasalazine?
Similar to MTX…
↓ cell proliferation
↑ apoptosis of T cells
↑ adenosine release (potent inhibitor of inflammation)
Alters expression of CAM (cellular adhesion molecules)
Inhibits pro-inflammatory cytokines
Name some side effects of Sulfasalazine?
N/V, HA, rash, rarely anemia and methemoglobinemia and neutropenia
True or False: Sulfasalazine is okay to to use in pregnancy.
TRUE
What is the thing to remember about fertility and using Sulfasalazine?
Reversible infertility in men but not women
Hydroxycholorquine (Plaquenil) is what type of drug?
Non-biologic
What is the MOA of Hydroxycholorquine?
Mechanism of action in RA is unclear.
NOTE: It’s an anti-malarial drug
How long does it take Hydroxycholorquine to work?
3-6 m before any improvement in symptoms
What are some side effects of Hydroxycholorquine?
Retinal damage if doses exceed 6 mg/kg/day (ophthalmologic exams yearly), GI issues, rash, nightmares
What are some other benefits seen from using Hydroxycholorquine? (diabetes & high lipids)
Improved glucose levels in diabetic pts & lower A1C
May improve LDL, HDL, and TG
True or False: Hydroxycholorquine is okay to use in pregnancy.
TRUE
Tolfacitinib (Xeljanz) is what type of drug?
Non-biologic
What is the MOA for Tolfacitinib?
Suppresses immune response
Tolfacitinib is usually given (alone or in combo)?
Either.
Combo with MTX or alone in moderate to severe disease where MTX failed or cannot be used
What cytochromes dose Tolfacitinib use?
CYP3A4 or CYP2C9 inhibitors
What are some side effects of Tolfactinib?
HA, diarrhea, URI, rarely GI perforation
Name the 2 classes of biologics?
Anti-TNF & non-TNF
Names some anti-TNF biologic agents.
Etanercept (Enbrel) Infliximab (Remicade) - IV Adalimumab (Humira) Certolizumab (Cimzia) Golimumab (Simponi)
Name some non-TNF biologic agents.
Abatacept (Orencia) (T cell costimulation inhibitor) - IV and SC
Rituximab (Rituxan) (B cell depleter) - IV
Tocilizumab (Actemra) (interleukin-6 inhibitor) - IV
What are some side effects of anti-TNF biologic agents?
Injection site reactions
Infection
New-onset psoriasis,
Increased risk of lymphoma and leukemia
What are some contraindications for anti-TNF biologic agents?
Presence of serious or recurrent infection
Pts w/ >= Class III HF & EF
What should you check before starting a pt on anti-TNF biologic agent?
Checked for TB
What are some of the side effects of Non-TNF agents B cell depleters?
Infusion reactions, rash (30%) with first infusion then decreases with subsequent infusions
What are some contraindications for Non-TNF agents B cell depleters?
presence of serious or recurrent infection, type 1 allergic reactions to murine proteins
What are some of the side effects of Non-TNF agents T cell costimulation inhibitors?
infusion reactions, increased risk of lymphoma
What are some contraindications for Non-TNF agents T cell costimulation inhibitors?
presence of serious or recurrent infection
What are some of the side effects of Non-TNF agents IL-6 inhibitors?
Infusion reactions, infection, increased lipids, URI, HA, HTN, elevated liver enzymes, decreased neutrophils, decreased platelets, GI perforation (esp in diverticulitis and on corticosteroids)
What should you check before starting a pt on IL-6 inhibitors?
Screen patients for TB prior to beginning tx
Dr. Lugo’s final take way points…
- Hydroxychloroquine & TNF inhibitors may decrease risk of diabetes according to some studies
- MTX and sulfasalazine have proven remission rates with MTX being standard of care
- Pregnancy is a contraindication for MTX & leflunomide
- Monotherapy for nonbiologics is recommended in early disease
- Biologics are recommended only after nonbiologic failure in patient with poor prognosis or failure of two nonbiologic regimens in patients without poor prognosis.
- Biologics are almost always given with MTX
What type of drug should you give during an acute gout attack?
Fast-acting NSAIDs: indomethacin, naproxen, sulindac
NOTE: Begin within first 24 hours
How long do you continue the therapy for an acute gout attack?
High dose for 2-3 days then step down over 2 weeks and continue for 2 days after resolution
What other meds can you prescribe for an acute gout attack?
COX-2 inhibitor, Corticosteroids (injections), Colchicine (Colcrys)
What is the standard of care medication for chronic management of gout?
Allopurinol
Give w/ NSAID or colchicine initially until uric acid levels are
What are some side effects of allopurinol?
GI disturbance, HA, rash, rarely cataracts, aplastic anemia, peripheral neuritis
Febuxostat (Uloric) is a xanthine oxidase inhibitor. It is used for what type of gout tx?
Chronic management
What side effects are there with Febuxostat?
elevated LFTs (liver fxn tests), diarrhea, HA, nausea
Pegloticase (Krystexxa) is a urate oxidase enzyme. It is used for what type of gout tx?
Chronic management
NOTE: After 6 months of treatment 45% of patients experienced complete resolution of tophi
What is a major contraindication of Pegloticase?
G6PD deficiency; screening of patients of African and Mediterranean decent recommended
What are some side effects of Pegloticase?
Infusion reactions (premed with antihistamine and corticosteroid), gout flares, nausea, bruising
How should you choose an agent for chronic tx?
Remove any offending drugs (i.e. thiazides…)
Decrease or eliminate alcohol intake
Renal vs hepatic
Cost
What are the two classes of local anesthetics?
Esters and Amides
Name some ester based local anesthetics
Cocaine
Procaine
Tetracaine
Benzocaine
Name some amide based local anesthetics.
Lidocaine Mepivacaine Bupivacaine (Marcaine) Ropivacaine Articaine
What is the MOA for local anesthetics?
Work on afferent nerve fibers; LA given in unionized form, enters neuron, ionizes and cannot leave cell, binds to NA channel , stops Na from entering neuron and prevents generation and conduction of action potential
What are some common additives found in many local anesthetics?
Epi, bases, opioids, Alpha-2 adrenergic agonists (i.e. clonidine)
What is one benefit and one disadvantage of Epi’s ability to vasoconstriction?
Benefit: Keeps the drug in the specific location
Disadvantage: Can cause skin necrosis
How are esters metabolized?
Hydrolyzed by pseudocholinesterases to PABA (allergy risk)
How are amides metabolized?
In liver by cytochromes
What are some issues we see with local anesthetics?
HA, dizziness, confusion, CNS depression
Lidocaine is ___________ & Bupivicaine is ___________, in terms of onset.
fast, slow
NOTE: Both are affect the heart in some way
What is Methemoglobinemia?
Ferric hemoglobin present instead of ferrous hemoglobin; poor O2 delivery
In what cases do we see methemoglobinemia in?
Chloraseptic throat sprays & teething babies
There is a risk of toxicity with some local anesthetics, one of which is Transient neurological symptoms (TNS). What is this?
Pain in lower extremities (gluteus and moving down)
Resolves within a week
Lidocaine more likely culprit
What 2 drugs cause arrhythmias?
Bupivacaine & ropivacaine
What do you do if a pt seizes after you administer a local anesthetic?
- Benzos
- ACLS but no big doses of epi; amiodarone for arrhythmias
- IV lipid is used to manage cardiovascular collapse
NOTE: Don’t use anesthetic type antiarrhythmics to treat arrhythmias from anesthesia
What is the MOA of Intra-articular Hyaluronic Acid?
Replaces OA synovial fluid with higher HA concentration improves viscosity
What are the side effects of Intra-articular Hyaluronic Acid?
Allergy, pain, swelling, heat, redness, and/or fluid build-up around the knee.
What are the contraindications for intra-articular hyaluronic acid?
Pts with known allergy
Pts w/ joint infections or skin diseases or infections in the area of the injection site.
What do you need to know about Taylor’s natural medicines?
These products are regulated as food, not drugs.
Best advice to a pt, stick with the food (med) that was studied in the study.
Purchase high quality
Glucosamine is legit. How does it work?
Tx OA pain; increases production of synovial fluid, repair of damaged tissue, new (knee) cartilage synthesis