Pharm test 4 Flashcards
1
Q
Drugs for inflammatory bowel diseases
A
5-aminosalicylates
corticosteroid
immunomodulators
biologic agents
2
Q
Mesalamine compounds
A
consist of single 5-ASA molecule enclosed within an enteric coat or a semipermeable membrane
3
Q
Azo Compounds
A
Prodrugs that consist of a 5-ASA molecule bound via an azo (N=N) bond to another molecule
Sulfasalazine
Balsalazine
Olsalazine
Azo bond prevents absorption in the stomach and small intestine
4
Q
Absorption of 5-Aminosalicylates
A
increases in more severe disease
coadministration of drugs may result in premature release of the 5-ASA before reaching site of action
inhibits intestinal folate absorption
rectal retention time affects absorption
5
Q
What should you administer with 5-Aminosalicylates
A
folate supplement
6
Q
Sulphapyridine
A
responsible for adverse effects
occur in 45% of patients
7
Q
AEs of sulphapyridine
A
headache
nausea
fatigue
dose related
blood dyscrasia
hepatitis
allergic reaction
low sperm counts in male (reversible)
8
Q
Dose adjustment for sulfasalazine if GI intolerance occurs
A
reduce dosage by 50% and gradually increase to target dose over sever days
if persists: stop therapy for 5-7 days and reintroduce at a lower dose
9
Q
Mesalamine
A
choose the lowest formulation that delivers mesalamine to the anatomic location of disease
oral tablets and capsules generally deliver mesalamine near the terminal ileum of the small intestine and throughout the large intestine
Pentasa- therapeutic quantities throughout both the small and large intestine
Rectal suppositories: deliver to rectum only
10
Q
Mesalamine dosing
A
initial dose for UC
doses >2g day are more effective than lower doses
oral tablets and capsules can be dosed once daily
11
Q
Timing of mesalamine treatment
A
initial therapy is 4-8 weeks and then transition to maintenance treatment
12
Q
Effects of cortisol
A
promotes catabolic effects
increases insulin resistance
13
Q
Synthetic glucocorticoids
A
have same effect as endogenous cortisol
increase neutrophils in blood
decrease lymphocyte, monocyte, basophil, and eosinophil counts
14
Q
Short-acting synthetic glucocorticoids
A
duration of action in 8-12 hours
turn cortisone into hydrocortisone
conversion does not happen in topical forms
15
Q
Hydrocortisone
A
chemically identical to cortisol
intramuscularly and intravenously
-go to target cell
-take effect rapidly
-short duration
-used for acute adrenal insufficiency
also topical form
16
Q
Intermediate acting synthetic glucocorticoids
A
duration of action 12-36 hours
4-5x more potent
prednisone
prednisolone
methylprednisolone
triamcinolone
17
Q
Prednisone and prednisolone
A
metabolically interconvertible
rapidly absorbed
peak plasma concentration after 1-3 hours
18
Q
Half-life of prednisone vs. prednisolone
A
prednisone is slightly longer (3.4-3.8hr) vs. prednisolone (2.1-3.5 hr)
19
Q
Budesonide
A
intermediate acting synthetic glucocorticoid
10-15% bioavailable without encapsulation system
oral and rectal formulation
delivers corticosteroid to a portion of inflamed intestine
20
Q
long-acting synthetic glucocorticoids
A
25x more potent than short-acting
duration of action is 36-72hrs
betamethasone and dexamethasone
21
Q
clinical use of anti-inflammatory/immunosuppressive therapy
A
asthma
conditions with autoimmune & inflammatory components (rheumatoid arthritis, crohn disease, UC, acute MS, idiopathic thrombocytopenic purpura)
inflammatory conditions of skin, ear, eye, nose
hypersensitivity states
prevent graft-vs-host disease
22
Q
Synthetic glucocorticoid MOA
A
activation of anti-inflammatory gene expression
suppression of activated inflammatory genes
23
Q
Drugs that increase concentration of synthetic glucocorticoid
A
oral contraceptives, clarithromycin, ritonavir, telithromycin, and antifungals (inhibitors of CYP3A4) increase concentration of corticosteroid
24
Q
Drugs that reduce the concentration of corticoid steroid
A
antiacid due to decreased absorption
carbamazepine, phenytoin, rifampin (inducers of CYP3A4)
25
Do synthetic glucocorticoids need to be given with food?
YES!
26
Dose ranges for prednisone
Low to moderate dose- up to 1mg/kg per day of in children or 40mg per day in adults
27
Budesonide safety profile
excellent compared with conventional corticosteroid
d/t local delivery and high first-pass metabolism
less systemic adverse effects
28
Azathioprine
injectible
derivative of mercaptopurine
MOA: incorporated into replicating DNA and halt replication
block the pathway for purine synthesis
off label IBD use in combination with anti-TNF agent
29
AEs of Azathioprine
malaise, N/V/D
hematologic and oncologic: leukopenia, neoplasia, lymphoma, thrombocytopenia
increased susceptibility to infection
check CBC frequently
30
Mercaptopurine
MOA: purine antagonist which inhibits DNA and RNA synthesis
have corticosteroid-sparing effects in patients with UC and CD
first line as monotherapy for maintenance of remission
31
Mercaptopurine for IBD
limited use due to concerns of toxicity
bone marrow suppression and hepatotoxicity
monitoring of CBC and LFTs recommended in all patients
32
Methotrexate
folate antimetabolite that inhibits DNA synthesis, repair, and cellular replication
only IM or SubQ of MTX has efficacy in Crohns
not recommended for maintenance of UC
daily administration of folic acid with MTX
-effective at reducing the incidence of GI adverse effects
33
Common AEs of methotrexate
headache, nausea, vomiting, abdominal discomfort, serum aminotransferase elevations, rash
34
Common side effects of biologic agents for IBD
redness, swelling, itching, pain, rahs, bruising of skin
URI
headache
nausea
rash
diarrhea
stomach pain
35
Serious side effects of biologic agents
Infection
-TB
-Sepsis
Lymphoma
Blood dyscrasia
HF
36
TNF-alpha inhibitors
effective for both induction and maintenance of remission
indicated in both moderate-severe CD and UC
Reserved as second-line agents in patients
37
Precations for TNF-alpha inhibitor use
evaluate for TB
treatment for latent TB prior to use
38
Integrin antagonist
MOA: reduces T-lymphocyte migration into the intestinal mucosa and inflammation
reserved for disease refractory to TNF alpha inhibitors
indicated for refractory UC and CD
39
Iron metabolsim
70% bound in hemoglobin and myoglobin
5% component of certain proteins and enzymes in our body
25% stored as ferritin in spleen, bone marrow, and liver
40
Iron deficiency anemia
Ferritin level <15ng/L
low serum ferritin level may be the only indication of IDA in early stages
41
Treatment options for iron deficiency anemia
treat underlying etiologies
dietary modification
oral iron
IV iron
42
Oral vs IV iron replacement
most patients treatment with oral iron
(effective, available, inexpensive, safe)
43
AEs of oral iron replacement
up to 70% of patients (especially on ferrous sulfate) report GI side effects
44
Indications for Oral Iron replacement
treatment of iron deficiency anemia, iron deficiency without andemia, nutritional support to prevent deficiency
dose is indicated by either total iron or elemental iron
45
Elemental iron
total amount of iron in a supplement available for absorption by our body
46
Types of oral iron
iron salts
-ferrous gluconate (12% elemental iron)
-325mg_36mg
polysaccharide iron complex
-contains ferric iron- better tolerability and taste
dose indicated as elemental iron
47
Choice of oral iron
enteric-coated or sustained release are not preferred due to poor absorption
heme iron polypeptide ProFerrin (no clinical data)
preparations such as polysaccharide-iron complex and heme iron
-more expensive
-equally effective but may have advantages such as better taste
48
Dosing of oral iron
no reason to give more than one dose- increase AEs without increasing iron level
can do alternate day dosing
49
AEs of oral iron
GI side effects
metallic taste
itching, black/green or tarry stools
50
Strategies to improve tolerability of oral iron
increase interval to every other day
make dietary modifications (take with food or milk)
switch to lower dose of elemental iron
switch from tablet to liquid
swish water in the mouth after the dose
51
Indications for IV iron
poor adherence or severe GI AEs of oral iron
preference to replenish in one dose vs over the course of several months
ongoing blood lose
condition that interferes with oral iron absorption
52
IV iron dose calculation
calculated on body weight, current hemoglobin level, and amount of elemental iron per mL of iron product
reasonable to use a fixed dose of approx 1000mg
no evidence that doses above 1000mg are clinically useful
53
Premedication of IV iron
not routine- use for patients with asthma, more than one drug allergy, inflammatory arthritis
use methylprednisolone and an H2 antihistamine
for inflammatory arthritis a short course of prednisone can also be given after infusion
54
Use of H1 antihistamines to prevent or treat IV iron reactions
DO NOT USE H1 antihistamines with IV iron reaction
55
Preferred IV Iron
LMW iron dextran
low cost and one dose
multiple doses of 100mg or single dose of 1000mg diluted in normal saline and given over 1 hour
give 0.5mL prior to first dose as a test dose
56
AEs of Iv iron
infusion reaction, anaphylaxis, shock, death
only should be given by providers who have knowledge of dosing and equipment to manage life-threatening adverse events
avoid IV iron in patients with active infections
57
F/U of iron deficiency anemia
Oral iron- reeval in 2-4 weeks
need to be off oral iron for at least 1-2 days before the test
IV iron retest in 4-8 weeks
58
In premenopausal women with iron deficiency anemia the AGA suggests
bidirectional endoscopy over iron replacement therapy only
59
In postmenopausal women and men with iron-deficiency anemia, the AGA recommends
bidirectional endoscopy over no endoscopy
60
Primary therapeutic options in anemia of CKD
iron
erythropoiesis-stimulating agents (ESAs)
rarely RBC transfusions
61
Erythropoiesis-stimulating agents
Epoetin alfa
Darbepoetin alfa
Methoxy polyethylene glycol-epoetin beta
62
Role of erythropoietin
controls red blood cell production by regulating the differentiation and proliferation of erythroid progenitor cells in the bone marrow
63
Recombinant Human EPO (rh EPO)
developed using living organisms with the help of biotechnology of genetic engineering
known as biologics, biopharmaceuticals, recombinant DNA expressed products, bioengineered, or genetically engineered drugs
administered IV (hemodialysis) or subcutaneously
Hemoglobin <10g/dL
64
Dosing of rh EPO
initial is 50-100 units/kg/week
lower doses reasonable in patients with pretreatment HgB levels near 10g/dL
weekly or less frequency dosing is effective and safe
use lowest effective dose
65
High doses of ESA have been associated with...
increased mortality and cardiovascular events independent of Hb level
66
AEs of rh EPO
increased mortality, cardiovascular events, and malignancy
increased risk of thrombosis
headache, arthralgia, tachycardia, nausea, diarrhea, fever, HTN
increased when ESAs are used after attaining a normal Hgb level
67
Vaccine
an inactivated or attenuated pathogen or component of a pathogen that when administered to the host stimulates a protective response of the cells in the adaptive immune system
68
Categories of vaccines
prevent disease (prophylactic)
treat disease (therapeutic)
69
Types of Vaccines
Live-attenuated
Inactivated (killed antigen)
Subunit (purified antigen)
Toxoid (Inactivated toxins)
Whole pathogen vaccines
Subunit vaccines
Nucleic acid vaccines
70
Whole pathogen vaccines
consist of entire pathogens that have been killed or weakened
can elicit strong protective immune responses
include Live-attenuated and Inactivated/killed
71
Live-attenuated vaccines
derived from disease-causing pathogens
weakened under lab conditions (suboptimal condition or genetic modification)
provide continual antigenic stimulation giving sufficient time for memory cell production (excellent immune response)
grow in a vaccinated person and stimulate an immune response
attenuated pathogen eliminated during immune response
72
Rare potential effect of live-attenuated vaccines
have rare potential to revert to pathogenic form and cause disease in vaccinees or their contacts
may cause very mild disease or not
should not be given to those with compromised immune system or during pregnancy
73
Inactivated vaccines
made from microorganisms (viruses, bacteria, other) that have been killed through physical or chemical processes
cannot cause disease
may not always induce an immune response and response may not be long-lived
several doses may be required to evoke a sufficient immune response
74
Subunit vaccine
consists of only the components or antigens that best stimulate the immune system
safer and easier to produce
do not contain live components of the pathogen
require incorporation of adjuvants to elicit a strong protective immune response
Recombinant protein vaccne
polysaccharide vaccine
conjugate vaccines
toxoid vaccines
75
Protein-based vaccines
present an antigen to the immune system using a specific, isolated protein of the pathogen without pathogen particles
acellular pertussis vaccine
Hepatitis B
-composed of the recombinant hepB virus surface antigen (HBsAg)
HPV vaccine
-consist only of the major viral capsid protein of HPV
Toxoid vaccine (Tetanus, Diptheria)
76
Toxoid vaccines
made with toxoid that is chemically inactivated toxin produced by certain bacteria
to increase immune response, the toxoid is absorbed to aluminum or calcium salt
no possibility of reversion to virulence
77
Conjugated subunit vaccine
made by conjugation, the process that combines the polysaccharide with a protein molecule
conjugated changes the immune response from T-cell independent to T-cell dependent
-increased immunogenicity in infants
-elicits antibody booster response to multiple doses of vaccine
hemophilus influenza type b conjugate
pneumococcal conjugate
meningococcal
78
Severe vaccine reactions
seizures
thrombocytopenia
hypotonic hyporesponsive episodes
anaphylaxis
79
Most common signs and symptoms of anaphylactic reaction to vaccine
cutaneous symptoms (generalized urticaria, angioedema, flushing, pruritus)
10-20% of findings have no skin findings
80
Danger signs of anaphylactic reaction to vaccine
rapid progression of symptoms, respiratory distress, vomiting, abdominal pain, hypotension, dysrhythmia, chest pain, collapse
81
Epinephrine for treatment of anaphylactic reaction to vaccine
IM 1mg/mL preparation
-children 0.01mg/kg (Max 0.5mg)
-adult 0.3 to 0.5mg
May repeat in 5-15 minutes
can use with H1 antihistamine, H2 antihistamine, glucocorticoid
82
Use of epinephrine at alpha-1 receptor
increased vasoconstriction
increased peripheral vascular resistance
increased blood pressure
decreased mucosal edema
83
Use of epinephrine at beta-1 repeptor
increased heart rate
increased force of cardiac contraction
84
Use of epinephrine at beta-2 receptor
decreased mediator release from mast cells and basophils
increased bronchodilation
increased vasodilation
85
Minor vaccine reactions (delayed)
resolve after short period of time and pose little danger
Local: pain, swelling or redness at the site of injection
Systemic: fever, malaise, muscle pain, headache, loss of appetite
86
Possible immunization error-related reaction
local injection site reaction, sepsis, toxic shock syndrome, blood borne transmission, death, local abscess, vaccine ineffective, effect of drug
87
Influenza vaccine
inactivated viral components (IM)
live-attenuated viruses (intranasal)
88
Meningococcal polysaccharide (MPSV4)
bacterial polysaccharide (SC)
89
Meningococcal conjugate (MCV4)
bacterial polysaccharide-protein conjugate (IM)
90
MMR & MMRV
live-attenuated (SC)
91
Pneumococcal conjugate polysaccharide (PPSV)
bacterial polysaccharide (IM or SC)
92
Pneumococcal conjugate (PCV)
bacterial polysaccharide-protein conjugate (IM)
93
Poliovirus (IPV)
inactivated virus (SC or IM)
94
Rotavirus (RV1 and RV5)
live-attenuated virus (oral)
95
Tdap
Toxoids and inactivated bacterial components (IM)
96
Tetanus
toxoid (IM)
97
Varicella
Live-attenuated virus (SC)
98
Pediatric vaccines
all IM route
Diptheria-tetanus (DT, Td)
DTaP, (DTaP-IPV, DTaP-IPV/Hib)
Hepatitis A
Hepatitis B
Hib
HPV
99
Contraindications to vaccine administration
anaphylaxis
encephalopathy- pertussis
severe combined immunodeficiency- rotavirus vaccine
a history of intussusception: rotavirus vaccine
Live vaccines: pregnancy and immunosuppression
100
invalid contraindications to vaccines
mild illness
pregnancy/breastfeeding
allergies
antibiotics
household contacts who are immunosuppressed
preterm birth
TB skin test
101
Drugs for obesity
drugs that alter fat digestion- Orlistat
GLP-1 receptor agonist- Liraglutide
Combination drugs- Phentermine-topiramate
Bupropion- naltrexone
Sympathomimetics
102
Orlistat (Xenical)
Pancreatic lipase inhibitor
MOA: blocks lipase activity which inhibits dietary triglycerides from being broken down into absorbable free fatty acids
about 30% of ingested triglycerides go undigested and are excreted
does not affect appetite
103
Orlistat dosing
120mg 3x daily with fat containing meals
not a controlled substance
104
Orlistat AEs
fecal urgency and increased defication
cramps, flatulence, fecal incontinence
impaired absorption of fat-soluble vitamins
contraindicated during pregnancy
105
Liraglutide (Saxenda)
GLP-1 receptor agonist
reduces food intake by enhancing satiety
slows down GI motility
increases postprandial insulin production
106
Liraglutide dosing
0.6mg SQ daily initially
increase at weekly intervals (1.2, 1.8, 2.5) until recommended dose of 3mg daily
not a controlled substance
107
Liraglutide AEs
N/V/D/C
hypoglycemia
dehydration
delay of gastric emptying
not recommended with severe renal or hepatic impairment
possible increased risk of thyroid cancer or other endocrine cancers
contraindicated in pregnancy
108
Phentermine-topiramate (Qsymia)
Phentermine- similar to amphetamine
Topiramate- antiseizure medication that causes visceral fat loss
blocks neuronal voltage-dependent sodium channels
antagonizes AMPA/kainate glutamate receptors
not recommended for patients with cardiovascular disease
no data for efficacy of generics
109
Dosing of phentermine-topiramate
3.75mg phentermine/23mg topiramate once daily then titrated up
controlled substance (C-IV)
110
Phentermine-topiramate AEs
dry mouth, taste disturbance, elevated heart rate, anxiety, cognitive disturbances
addictive
teratogenic- NO USE in pregnancy
taper off over 1 week
contraindicated in hyperthyroidism, glaucoma, use of MAOIs and pregnancy
111
Bupropion- Naltrexone (Contrave)
not first-line therapy
no data for CV safety
could be useful for smoker who wants smoking cessation and weight loss
112
Bupropion-Naltrexone dosing
Week 1: 1 tablet daily (8mg naltrexone/90mg bupropion)
Week 2: 1 tablet twice daily
Week 3: 2 tablets in the morning and 1 in the evening
Week 4: 2 tablets twice daily (max dose is 4 tabs)
Not a controlled substance
113
Bupropion-Naltrexone AEs
nausea, constipation, headache, vomiting, dizziness, insomnia, dry mouth
increase in BP and heart rate
contraindicated in HTN, seizure disorder, eating disorder, use of other bupropion-containing products, chronic opioid use, use with MAOIs, pregnancy or breastfeeding
114
sympathomimetic drugs for weight loss
phentermine, diethylpropion, benzphetamine, and phendimetrazine
short term treatment for obesity because of side effects and potential for abuse (12 weeks)
contraindicated in patients with Coronary heart disease, uncontrolled HTN, hyperthyroidism, or hx of drug abuse
115
phentermine dosing
15-37.5mg daily or divided in BID dosing (C-IV)
116
Initial management of obesity
counseling, lifestyle modification, addressing underlying comorbidities
117
Drug categories that cause weight loss
anticonvulsants, antidepressants, antipsychotics, ADHD medication
118
Drug categories that cause weight gain
Antidepressants, antipsychotics, diabetes meds, glucocorticoids, hormonal agents, anticonvulsants, neurologic and mood-stabilizing agents, antihistamines, alpha blockers, beta blockers
119
First and second line weight loss drugs
first line: liraglutide
second line: orlistat, phentermine
use single agent over combination drugs
120
Monitoring for weight loss drugs
weight and vital signs every six weeks
taper and discontinue if the patient does not lose 4-5% of body weight after 12 weeks of therapy
