pharm exam 2 Flashcards
ASA
Salicylic asid
only one that does IRREVERSIBLE binding
ASA
pain
fever
swelling
anti-clot
(ALL 4 benefits)
ASA fatal dose
“Acute salicylic poisoning”
20 g of ASA
Reyes syndrome in kids (brain edema w/viral infection)
NSAIDs
pain
fever
swelling
NSAIDs
Celocoxib (cox 2) Indomethacin Diclofenac Ketorolac (Toradol) Ibuprofen (Motrin) Naproxen Piroxican and Meloxican Phenylbutazone
Only NSAID that binds Cox2 specifically
Celecoxib
Really good for Anti-inflammatory, but CVD risk!
Indomethacin
Use for Patent Ductus Arteriosus
Diflofenac (voltaren)
Often combined w Misopristol to decrease GI side effects
Ketorolac (Toradol)
Post-operative pain
Often combined w Opiates
Ibuprofen (Motrin)
DOC bc of lowest side effects
Give every 6 hrs
Naproxen
known to LAST ALL DAY
but takes 1-2 hrs for effects to onset
CONTRA: pregnant
Piroxicam and Meloxicam
Inhibit PNM migration, lymphocyte fx
Phenylbutazone
not given in US
SE: GI stuff and Bone marrow!
Acetaminophen (Tylenol)
safe for kids!!
Acetaminophen (Tylenol)
pain
fever
no effect on Cox in the periphery
no anti-inflammatory effects
SE if overdose on Acetaminophen (Tylenol)
Liver toxicity
“Fatal liver death” but takes 2-3 days for this to happen, metabolites build up, person turns yellow
Acetaminophen (tylenol) can be used for
adjunct to Anti-inflammatory meds
Caution in these ppl when giving Acetaminophen (Tylenol)
Chronic Alcohol Drinkers
Toxicity d/t metabolite buildup
PUD considerations with these drugs
Hx of PUD but not active: Celecoxib or Some other NSAIDS + “Prazols”/ Misopristol
Active PUD: Acetaminophen (Tylenol) only!! possibly + Codeine
Acting on TNFa
Infliximab
Adalimumab
Certolizumab, Golimumab
Etanercept
Inhibit B cell diff and T cell activation
Rituximab
Abatacept
Inhibit nucleic acid synth
Leflunomide
Micophenolate
Interleukin receptor antag
Anakinra
Tocilizumab
JAK inhibitor
Tofacitinib
Baricitinib
Gold salts
rarely used now
Suppress cell immunity
SE: Bone marrow damage, Enterocolitis
Penicillamine (cuprimine)
Chelating drug
Use: RA, Wilson’s dz (Copper)
Downfall of Penicillamine (cuprimine)
TONS of SE
blood, protein, Lupus like, Goodpasture synd, myasth gravis
Pts >65YO higher risk of SE
Hydroxychloroquine (Plaquenil)
Many mechanisms
Toxicity: Hemolysis (G6PD), Ototoxic (ear), Retinopathy (eye), Periph Neuropathy
Sulfasalazine (Azulfidine)
Better tolerated than Gold salts and Hydroxychloroquine
An option for RA
The DOC for RA
Methotrexate
What must you monitor for when on Sulfasalazine?
Hepatitis (LIVER) and
Bone marrow Suppression (BONE)
Infliximab (Remicade)
TNFa
chimeric IgG1k monoclonal antibody
Human AND Murine
Infliximab (Remicade) use
Crohn’s, RA
combined with MTX
Adalimumab (Humira)
ONLY Human monoclonal antibody, 100% human
Adalimumab (Humira)
Formally approved for MONOTHERAPY in tx of RA
“Copy cats” of Adalimumab (Humira)
Certrolizumab pegol,
Golimumab
Etanercept (Enbrel)
a “FAKE” TNF receptor
fusion protein produced by recombinant DNA technology
Etanercept (Enbrel) mechanism
TNF receptor, therefore the TNF binds to this and takes away the Pro-inflammatory effects that it would normally have
Etanercept (Enbrel) simple way to put mechanism
“FAKE” receptor
Inhibits TNF
Etanercept (Enbrel) CONTRA
The basic ones: pregnancy, breastfeeding, Infection, children + PLUS:
Bone marrow suppression, Diabetes mellitus, Sepsis, Vaccination, Varicella
Inhibitors of B cell diff and T cell activation
Rituximab and Abatacept
Rituximab (Rituxan)
Chimeric Murine/Human antibody
Binds CD20
Rituximab (Rituxan) use
Non-hodkin lymphoma
B cell CA
Chronic lymphocytic leukemia
Abatacept
Fully human fusion protein
Blocker of T cell activation
Abatacept use
RA
All TNFa and Bcell/Tcell are administered
IV or SubQ
Drugs that are administered SubQ
Adalimumab (Humira)
Etanercept (Enbrel)
B cell/T cell drugs:
Rituximab
Abatacept
both administered
IV
Leflunomide (Arava)
Inhibit Dihydro-orotate DH
key step in synth of Pyrimidine
Leflunomide (Arava)
Inhibits DHODH
Inhibit tyrosine kinase activity
AND
Inhibit COX-2
Use: RA
What drug do we give following Organ transplant?
Mycophenolate Mofetil (cellcept)
Mycophenolate mofetil
Inhibit synth of Purine
by inhibiting enzyme: inosine monophosphate DH (IMPDH)
Inhibitors of Nucleic Acid synth
Leflunomide (use for RA, Pyrimidine)
Mycophenolate (use for organ transplant, Purine)
Anakinra (Kineret)
IL-1RA
Interleukin 1 receptor antag
Anakinra use
RA
Tocilizumab
Interleukin 6 receptor antag
IL-6RA
Tofacitinib (Xeljanz)
Inhibit JAK 1 and 3
Tofacitinib (Xeljanz) use
Pts with RA who have not responded to or cannot tolerate MTX
Use this med ALONE
Serious infections and CA may be precipitated by:
Tofacitinib
JAK 1 and 3
Baricitinib (olumiant)
JAK 1 and 2
Use for: RA
mono or combo with MTX
Box warnings for Baricitinib
JAK 1 and 2
Serious infection
CA
Thrombosis (clots)
NSAIDs used for acute mgmt of Gout
Naproxen
Indomethacin
Sulindac
NSAIDs that are contra-indicated in the treatment of Gout
ASA because acids make it worse
Colchicine mechanism
Inhibit Microtubule assembly
Anti-inflammatory bc it inhibits Leukocyte migration and Phagocytosis
Does Colchicine have any direct effect on pain?
No, no analgesic direct effect
It affects inflammation, therefore secondarily improving pain when the swelling goes down
Uricosuric agents
Probenacid
Lesinurad (newer)
Uricosuric agents
increase excretion of Uric acid by blocking the active reabsorption of uric acid
Drink LOTS of water to decrease risk of kidney stone
When taking a Uricosuric agent (Probenacid) or Xanthine Oxidase Inhibitor (Allopurinol or Febuxostat), need to
take Colchicine prophylactically
Probenacid
Lesurinad
Uricosuric agents
Lesinurad (more specifically is a URAT1 inhibitor)
Xanthine Oxidase Inhibitors are known for
DRUG INTERACTIONS
Increase toxicity of 6MP (mercaptopurine)
Inhibit 5FU
Xanthine Oxidase Inhibitors
Allopurinol
Febuxostat
Serious SE including Agranulocytosis, Vasculitis, Hypersensitivity
Xanthine Oxidase Inhibitors
- Allopurinol
- Febuxostat
Meds that are enzymes that actually convert Uric Acid –> Allantoin which is then easily excreted
Rasburicase (fungal form of enzyme)
and
Peglioticase (similar to above, just a newer drug)
Rasburicase
Fungal enzyme
used in Children CAs
caution with Hypersensitivity rxns bc it’s a fungal enzyme
Migraine symptomatic tx
NSAIDs
Analgesics
Seretonin (5HT) Agonists
“Triptans” treatment for migraines
Seretonin 5HT agonist
given PO or SubQ
Vasoconstricting and decrease release of neuropeptides
SE of “Triptans” and Ergots
d/t Vasoconstricting properties!!
Ergotamine tantrate
5HT agonist AND
Alpha1 agonist
so the constricting SE are even worse
“triptans” have a short half life so often
required 2nd dose
“St Anthony Fire”
CNS side effects
Chronic Ergot use
Migraine prophylaxis
Beta blocker (propranolol) CCB (verapamil) Antidepresssant (Amitriptyline, fluoxetine) Anticonvulsant (Valproate, Topiramate) Botox ACE-I ARBs Erenumab (monoclonal antibody)
Valproic acid
CAUTION HEPATOTOXIC
Misoprostol
protective agent for stomach
Pepto bismu
Bismul subsalicylate
Magnesium
diarrhea
Aluminum
constipation