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
Sodium bicarb
alka seltzer (or even baking soda)
when you’ve eaten too much and need relief
fast acting
makes you belch
caution with Heart Failure (bc of the Na)
Calcium bicarb
“milk alkali” synd if too much
NOT good for peptic ulcer, chronic stuff, GERD
acid rebound bc Ca stimulates acid production
Calcium carbonate
Drug interactions
TUMS can make Digoxin not work as well
Mg hydroxide
laxative
poorly absorbed but may accumulate if Renal (kidney fx) is poor
Magnesium (diarrhea) and
Aluminum (constipation)
can decrease absorption of other drugs
usually poorly absorbed but CAUTION if Renal (kidney) fx is poor
Sodium Bicarb
caution with HF
if on Tetracycline
avoid Calcium
H2 antagonist
“itidines”
block H2 receptor, inhibit cAMP
decrease GI acid formation
All are OTC
H2 blockers most effective when?
at night
PPI, use when?
morning
30 min b4 breakfast
Cimetidine is unique, why?
Anti-testosterone effects
May be useful in women!
(but in men, chronic doses cause Gynecomastia, loss libido, impotence)
Cimetidine other unique: DRUG INTXNS
inhibitor of CYP3A4
dangerous w drugs w narrow therap range:
Warfarin, Phenytoin, Thephylline, Digoxin
PPI are activated where?
gastric parietal cells
in the STOMACH, only work here. covalently bind to the pump
PPIs
“prazoles”
PPI effects last
2-3 days
bind to the pump and effects last until new pumps are formed
DOC for GERD
PPIs “prazoles”
PPI SE
decrease Ca absorption (increase risk Osteoporosis)
decrease Mg- muscle spasm
B12- need supplement
Omeprazole drug interaction w
may inhibit CYP..
Clopidogrel (making Plavix less effective)
switch to another “prazole” if using Clopidogrel (Plavix)
Misoprostol
Prostaglandin E1 analog
prevent NSAID induced damage
do NOT use Misoprostol in
Pregnancy!!
can induce contractions
Prokinetic agents
Metoclopramide
Bethanechol
Erythromycin
Metoclopramide
(prokinetic agent; get things moving)
D2 antagonist (acts on chemoreceptor trigger zone in CNS)
PARKINSON LIKE SX SE
Bethanechol
prokinetic agent; get things moving
Muscarinic agonist
Use: Post op ileus
Erythromycin
sometimes used in diabetic gastroparesis
acute situations, when other drugs haven’t worked
GI system is too active
Antispasmodic
Muscarinic antagonist
Amtriptyline
Eluxadoline
Glycopyrolate
Dicyclomine
commonly used to calm stomach down
They are Muscarinic antagonists; antispasmodic
SE: constipation, if slow it down tooo much!
Amitriptyline used for IBS is good in TWO ways
Muscarinic block, and
increased NE release stimulates a2 receptors- decrease pain
Block Musc: slow down bowel
NE in a2: decrease pain
TWO BENEFITS!
Eluxadoline
opioid agonist used to treat
IBS w diarrhea
Anti-nausea
5HT antagonist (seretonin)
“setrons”
“setrons” 5HT are good for
Chemo induced n/v, radiation, gastric dz, pre-op
NOT for motion sickness
What kind of block do we need to help w motion sickness?
Muscarinic block
Prochlorperazine
Promethazine
POST OP used often, gastroenteritis, chemo, motion sickness (not DOC tho) n/v
Block 3 types of receptors!
Dopamine, Muscarinic, AND Histamine
HIGHLY sedating
Bulk forming laxatives
Dietary
Methylcellulose
Psyllium
Polycarbophil
Osmotic laxatives
Mg hydroxide
Sodium salts
Sorbitol, mannitol
Polyethylene glycol
“Miralax”
Insoluble, holds water in intestine
Before Colonoscopy
In mild doses, for occasional constipation
Lactulose
chronolac
Osmotic laxative
UNIQUE bc the only time an osmotic laxative is used CHRONICALLY
for pts with Cirrhosis: decreases ammonia buildup
(converts ammonia –> amonium)
Lubiprostone and
Linaclotide
can be used for CHRONIC constipation
Lubirprostone
Prostaglandin analog
Activate Cl- channels
Linaclotide
Stimulate Cl- secretion
Cystic Fibrosis channel
Loperamide (imodium)
Opioid analog
treat diarrhea
Sulfasalazine is used for
Ulcerative Colitis (a type of Crohns)
Simethicone
Gas X
“Helidac” to treat H. Pylori consists of:
Bismuth sub (pepto bismol)
Metronidazole
Tetracycline
“Tritec” to treat H. Pylori consists of:
Ranitidine
Bismuth citrate
Clarithromycin
Eluxadoline and
Loperamide are similar how?
Eluxadoline: opioid
Loperamide: opioid analog
Use of Eluxadoline and
Loperamide
Eluxadoline: IBS diarrhea
Loperamide: diarrhea
Prochlorp
Promethazine
used post op n/v
block THREE receptor types:
histamine, dopamine, AND muscarinic
VERY sedating
Lubiprostone and
Linaclotide
Cl- channels
Lubiprostone: prostaglandin analog
Linaclotide: Cystic Fibrosis channels
What drug used to treat Ulcerative Colitis?
Sulfasalazine
Lactulose
SE: flatulence, diarrhea
Chronic use,
Used in Cirrhosis/ Liver dz to decrease blood Ammonia levels
Bisacodyl and Senna
Mild irritants
Stimulate peristalsis, get GI tract going
Docusate (colace)
Emulsifier, softens feces
usually an add-on, not very effective by itself
Glycerin
lubricant, not v effective
used in Enema
Linaclotide
guanlyate cyclase cGMP Cystic Fibrosis membrane Cl- Use: IBS w constipation
Always 1st thing to go for to treat Constipation
Bulk forming agents
Contra to Laxative use
N/v Abd cramps Undx abd pain Appendicitis Obstruction
Diphenoxylate/Atropine (Lomotil)
to tx diarrhea
Opioid with Atropine (reduce abuse potential)
Atropine
Anticholinergic
Antimuscarinic
Atropine used to treat
pesticide poisoning
Bismuth subsalicylate
treat diarrhea
Traveller’s diarrhea
Salicylate: anti-inflammatory properties
SE: black tongue, mouth, and stool!
Contra to Bismuch subsalicylate “pepto-bismul”
Allergy to ASA
Children (reyes)
Caution Asthmatics “ASA asthma”
Severe UC when others haven’t worked
Infliximab and
Adalumumab can be used (TNFa blockers)
have to make sure pt does NOT have TB!
Cox 1
Vasoconstricting
Clot forming
Thromboxane
Cox 2
Prostacyclin
vasodilating
inhibit clot
“ximab”
chimeric
50/50 murine and human
“cept”
fusion protein
B cell
RituximaB
CD20
AbaTacepT
T cell block
fully human fusion protein
Anakrina
IL-1 RA
Tocilizumab
IL-6 RA
Jak 1,3
Tofacitinib
for those intolerant to MTX
Monotherapy
Jak 1,2
Bari
Xanthine Oxidase Inhibitor important properties
Allopurinol, Febuxostat
Increase toxicity of 6MP
Decrease effectiveness of 5FU
Colchicine mechanism
microtubule
Diclofenac (voltaren)
often combined w Misoprostol to decrease the GI effects
Ketorolac (toradol)
post op pain
Dont use ASA w GOUT pts because
at low (therapeutic doses), ASA decreases uric acid excretion and elevates Plasma urate concentration
Cholinergic antagonist
COPD
Antimuscarinic
Theophylline
Long lasting Bronchodilation but LAST CHOICE bc Low therapeutic index
Drug interaction w Cimetidine
Theophylline mechanism
Blocks Adenosine
BUT good at preventing Diaphgragm fatigue
Tx of COPD
LABA or
Anticholinergic
Tx of COPD Exacerbation
Ipratropium
Albuterol
B2 agonist mechanism
Activate adenylate cyclase,
increase CAMP
relax sm muscle
Stabilize mast cells
Rapid and short action B2 agonists
SABA
1st line tx for Asthma
Albuterol
Levalbuterol
LABA
prophylactic
Salmeterol
Formoterol
Vilanterol
Combine beta agonist with steroid to
reduce the tolerance to the beta agonist
Ipratropium and
Tiotropium
Muscarinic antagonist
SE: cough, dry mouth, nausea
Tiotropium
longer duration of action than “Ipra”
once a day administration
Theophylline
CNS stimulant
acts like caffeine, decreases fatigue and elevates mood
Theophylline
Blockes adenosine
Phosphodiester inhibitor
increase cAMP
Very effective bronchoDILATOR
relaxes sm muscle, esp bronchioles
Theophylline is indicated in use for
Don’t respond to b2 agonists alone and in Severe COPD
SE of Theophylline
Nervous, Arrhythmia, weak diuretic
Good thing about Theophylline?
Decreases diaphragm fatigue
Leukotriene inhibitors
- Zafirlukast
- Montelukast (singulair)
- Zyflo
Decrease asthmatic response to EXERCISE or COLD AIR
decrease need for steroids
Benralizumab
Severe asthma w EISINOPHILIC type
What to add for Asthma if you’re taking B2 and ICS and still having exacerbations?
Leukotriene inhibitor
Montelukast
Theophylline
PDE5 inhibitor
COPD
Sedation and dry mouth SE
Benadryl
Pre surgery for colon
Polyethylene glycol “Miralax”
Cimetidine
inhibits Hepatic enzymes and decreases metabolism of many drugs
Diphenoxylate (Lomotil)
Opioid + Atropine
Probenacid
A uricosuric agent in tx of Gout that interferes/competes wtih elimination of Acids
Probenacid competes w elimination of the following drugs (bc they are Acids)
ASA Pen G Vit C Furosemide MTX Clofibrate NSAIDs
DES given to pregnant mothers was linked to what in their female daughters once they reached age 20s?
Adenocarcinoma
Toradol
Post op pain
Levothyroxine
safe in pregnancy
Mg
Diarrhea
“mega diarrhea”
Sumatriptan (Imitrex) properties
used for migraines
Produce vasoconstriction
produce coronary vasospasm
CONTRA in seizures
SE: abd pain and bloody diarrhea
ASA
low dose: respiraotry alkalosis
high dose: Acidosis (both types)
ASA is excreted more easily if the urine is
Alkaline
Ergot
5HT (seretonin) AND alpha 1 agonist
therefore it has more constricting side effects
5HT3 blockers that do NOT cause daytime sleepiness
used for N/V
Ondansetron
“setrons” are 5HT (seretonin) antagonists
safe for pregnancy
Ondansetron brand name is what
“Zofran”
can give to pregnant mommas
Probenacid and Lesinurad are what
Uricosuric agents used in the tx of Gout
Allopurinol and Febuxostat are what
Xanthine Oxidase Inhibitors used in the tx of Gout
Important considerations with XOIs (gout tx)
Increase toxicity of 6MP and decrease effectiveness of 5FU
Cetirizine (zyrtec) is excreted
SOLELY by kidney
Cromolyn
Cetirizine
Azelastine
All inhibit Histamine release from mast cells
Inhibits Histamine release AND blocks receptors
Azelastine
PROchlorperazine
PROmethazone
blocks 3 types of receptors and thus HIGHLY sedating
Dopamine
Muscarinic
Histamine
Amitriptyline is special why?
it does TWO beneficial things
Muscarinic antagonist A2 sitmulation (helps w pain)
anti-spasmodic
Senna
irritant laxative
Lubriprostone
Linaclotide
Chronic constipation
Lubiprostone
Females w IBS and constipation
Prostaglandin analog
Linaclotide
Cystic fibrosis
Cl-
Sulfasalazine
Ulcerative Colitis
Loperamide
Opioid analog
OTC for diarrhea
Benadryl mechanism
Competes w histamine
Blocks musc receptors
Severe allergic asthma
Omalizumab injection
Rebound acid productiion
Ca carbonate (Tums)
Can reduce oral absorption rate of ASA
Ca carbonate (Tums)