Pharm test 4 Flashcards

1
Q

Drugs for inflammatory bowel diseases

A

5-aminosalicylates
corticosteroid
immunomodulators
biologic agents

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2
Q

Mesalamine compounds

A

consist of single 5-ASA molecule enclosed within an enteric coat or a semipermeable membrane

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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

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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

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5
Q

What should you administer with 5-Aminosalicylates

A

folate supplement

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6
Q

Sulphapyridine

A

responsible for adverse effects
occur in 45% of patients

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7
Q

AEs of sulphapyridine

A

headache
nausea
fatigue
dose related
blood dyscrasia
hepatitis
allergic reaction
low sperm counts in male (reversible)

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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

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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

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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

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11
Q

Timing of mesalamine treatment

A

initial therapy is 4-8 weeks and then transition to maintenance treatment

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12
Q

Effects of cortisol

A

promotes catabolic effects
increases insulin resistance

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13
Q

Synthetic glucocorticoids

A

have same effect as endogenous cortisol
increase neutrophils in blood
decrease lymphocyte, monocyte, basophil, and eosinophil counts

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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

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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

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16
Q

Intermediate acting synthetic glucocorticoids

A

duration of action 12-36 hours
4-5x more potent
prednisone
prednisolone
methylprednisolone
triamcinolone

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17
Q

Prednisone and prednisolone

A

metabolically interconvertible
rapidly absorbed
peak plasma concentration after 1-3 hours

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18
Q

Half-life of prednisone vs. prednisolone

A

prednisone is slightly longer (3.4-3.8hr) vs. prednisolone (2.1-3.5 hr)

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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

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20
Q

long-acting synthetic glucocorticoids

A

25x more potent than short-acting
duration of action is 36-72hrs
betamethasone and dexamethasone

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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

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22
Q

Synthetic glucocorticoid MOA

A

activation of anti-inflammatory gene expression
suppression of activated inflammatory genes

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23
Q

Drugs that increase concentration of synthetic glucocorticoid

A

oral contraceptives, clarithromycin, ritonavir, telithromycin, and antifungals (inhibitors of CYP3A4) increase concentration of corticosteroid

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24
Q

Drugs that reduce the concentration of corticoid steroid

A

antiacid due to decreased absorption
carbamazepine, phenytoin, rifampin (inducers of CYP3A4)

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25
Q

Do synthetic glucocorticoids need to be given with food?

A

YES!

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26
Q

Dose ranges for prednisone

A

Low to moderate dose- up to 1mg/kg per day of in children or 40mg per day in adults

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27
Q

Budesonide safety profile

A

excellent compared with conventional corticosteroid
d/t local delivery and high first-pass metabolism
less systemic adverse effects

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28
Q

Azathioprine

A

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

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29
Q

AEs of Azathioprine

A

malaise, N/V/D
hematologic and oncologic: leukopenia, neoplasia, lymphoma, thrombocytopenia
increased susceptibility to infection
check CBC frequently

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30
Q

Mercaptopurine

A

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

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31
Q

Mercaptopurine for IBD

A

limited use due to concerns of toxicity
bone marrow suppression and hepatotoxicity
monitoring of CBC and LFTs recommended in all patients

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32
Q

Methotrexate

A

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

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33
Q

Common AEs of methotrexate

A

headache, nausea, vomiting, abdominal discomfort, serum aminotransferase elevations, rash

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34
Q

Common side effects of biologic agents for IBD

A

redness, swelling, itching, pain, rahs, bruising of skin
URI
headache
nausea
rash
diarrhea
stomach pain

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35
Q

Serious side effects of biologic agents

A

Infection
-TB
-Sepsis
Lymphoma
Blood dyscrasia
HF

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36
Q

TNF-alpha inhibitors

A

effective for both induction and maintenance of remission
indicated in both moderate-severe CD and UC
Reserved as second-line agents in patients

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37
Q

Precations for TNF-alpha inhibitor use

A

evaluate for TB
treatment for latent TB prior to use

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38
Q

Integrin antagonist

A

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

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39
Q

Iron metabolsim

A

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

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40
Q

Iron deficiency anemia

A

Ferritin level <15ng/L
low serum ferritin level may be the only indication of IDA in early stages

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41
Q

Treatment options for iron deficiency anemia

A

treat underlying etiologies
dietary modification
oral iron
IV iron

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42
Q

Oral vs IV iron replacement

A

most patients treatment with oral iron
(effective, available, inexpensive, safe)

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43
Q

AEs of oral iron replacement

A

up to 70% of patients (especially on ferrous sulfate) report GI side effects

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44
Q

Indications for Oral Iron replacement

A

treatment of iron deficiency anemia, iron deficiency without andemia, nutritional support to prevent deficiency
dose is indicated by either total iron or elemental iron

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45
Q

Elemental iron

A

total amount of iron in a supplement available for absorption by our body

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46
Q

Types of oral iron

A

iron salts
-ferrous gluconate (12% elemental iron)
-325mg_36mg
polysaccharide iron complex
-contains ferric iron- better tolerability and taste
dose indicated as elemental iron

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47
Q

Choice of oral iron

A

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

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48
Q

Dosing of oral iron

A

no reason to give more than one dose- increase AEs without increasing iron level
can do alternate day dosing

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49
Q

AEs of oral iron

A

GI side effects
metallic taste
itching, black/green or tarry stools

50
Q

Strategies to improve tolerability of oral iron

A

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
Q

Indications for IV iron

A

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
Q

IV iron dose calculation

A

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
Q

Premedication of IV iron

A

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
Q

Use of H1 antihistamines to prevent or treat IV iron reactions

A

DO NOT USE H1 antihistamines with IV iron reaction

55
Q

Preferred IV Iron

A

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
Q

AEs of Iv iron

A

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
Q

F/U of iron deficiency anemia

A

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
Q

In premenopausal women with iron deficiency anemia the AGA suggests

A

bidirectional endoscopy over iron replacement therapy only

59
Q

In postmenopausal women and men with iron-deficiency anemia, the AGA recommends

A

bidirectional endoscopy over no endoscopy

60
Q

Primary therapeutic options in anemia of CKD

A

iron
erythropoiesis-stimulating agents (ESAs)
rarely RBC transfusions

61
Q

Erythropoiesis-stimulating agents

A

Epoetin alfa
Darbepoetin alfa
Methoxy polyethylene glycol-epoetin beta

62
Q

Role of erythropoietin

A

controls red blood cell production by regulating the differentiation and proliferation of erythroid progenitor cells in the bone marrow

63
Q

Recombinant Human EPO (rh EPO)

A

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
Q

Dosing of rh EPO

A

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
Q

High doses of ESA have been associated with…

A

increased mortality and cardiovascular events independent of Hb level

66
Q

AEs of rh EPO

A

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
Q

Vaccine

A

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
Q

Categories of vaccines

A

prevent disease (prophylactic)
treat disease (therapeutic)

69
Q

Types of Vaccines

A

Live-attenuated
Inactivated (killed antigen)
Subunit (purified antigen)
Toxoid (Inactivated toxins)
Whole pathogen vaccines
Subunit vaccines
Nucleic acid vaccines

70
Q

Whole pathogen vaccines

A

consist of entire pathogens that have been killed or weakened
can elicit strong protective immune responses
include Live-attenuated and Inactivated/killed

71
Q

Live-attenuated vaccines

A

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
Q

Rare potential effect of live-attenuated vaccines

A

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
Q

Inactivated vaccines

A

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
Q

Subunit vaccine

A

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
Q

Protein-based vaccines

A

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
Q

Toxoid vaccines

A

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
Q

Conjugated subunit vaccine

A

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
Q

Severe vaccine reactions

A

seizures
thrombocytopenia
hypotonic hyporesponsive episodes
anaphylaxis

79
Q

Most common signs and symptoms of anaphylactic reaction to vaccine

A

cutaneous symptoms (generalized urticaria, angioedema, flushing, pruritus)
10-20% of findings have no skin findings

80
Q

Danger signs of anaphylactic reaction to vaccine

A

rapid progression of symptoms, respiratory distress, vomiting, abdominal pain, hypotension, dysrhythmia, chest pain, collapse

81
Q

Epinephrine for treatment of anaphylactic reaction to vaccine

A

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
Q

Use of epinephrine at alpha-1 receptor

A

increased vasoconstriction
increased peripheral vascular resistance
increased blood pressure
decreased mucosal edema

83
Q

Use of epinephrine at beta-1 repeptor

A

increased heart rate
increased force of cardiac contraction

84
Q

Use of epinephrine at beta-2 receptor

A

decreased mediator release from mast cells and basophils
increased bronchodilation
increased vasodilation

85
Q

Minor vaccine reactions (delayed)

A

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
Q

Possible immunization error-related reaction

A

local injection site reaction, sepsis, toxic shock syndrome, blood borne transmission, death, local abscess, vaccine ineffective, effect of drug

87
Q

Influenza vaccine

A

inactivated viral components (IM)
live-attenuated viruses (intranasal)

88
Q

Meningococcal polysaccharide (MPSV4)

A

bacterial polysaccharide (SC)

89
Q

Meningococcal conjugate (MCV4)

A

bacterial polysaccharide-protein conjugate (IM)

90
Q

MMR & MMRV

A

live-attenuated (SC)

91
Q

Pneumococcal conjugate polysaccharide (PPSV)

A

bacterial polysaccharide (IM or SC)

92
Q

Pneumococcal conjugate (PCV)

A

bacterial polysaccharide-protein conjugate (IM)

93
Q

Poliovirus (IPV)

A

inactivated virus (SC or IM)

94
Q

Rotavirus (RV1 and RV5)

A

live-attenuated virus (oral)

95
Q

Tdap

A

Toxoids and inactivated bacterial components (IM)

96
Q

Tetanus

A

toxoid (IM)

97
Q

Varicella

A

Live-attenuated virus (SC)

98
Q

Pediatric vaccines

A

all IM route
Diptheria-tetanus (DT, Td)
DTaP, (DTaP-IPV, DTaP-IPV/Hib)
Hepatitis A
Hepatitis B
Hib
HPV

99
Q

Contraindications to vaccine administration

A

anaphylaxis
encephalopathy- pertussis
severe combined immunodeficiency- rotavirus vaccine
a history of intussusception: rotavirus vaccine
Live vaccines: pregnancy and immunosuppression

100
Q

invalid contraindications to vaccines

A

mild illness
pregnancy/breastfeeding
allergies
antibiotics
household contacts who are immunosuppressed
preterm birth
TB skin test

101
Q

Drugs for obesity

A

drugs that alter fat digestion- Orlistat
GLP-1 receptor agonist- Liraglutide
Combination drugs- Phentermine-topiramate
Bupropion- naltrexone
Sympathomimetics

102
Q

Orlistat (Xenical)

A

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
Q

Orlistat dosing

A

120mg 3x daily with fat containing meals
not a controlled substance

104
Q

Orlistat AEs

A

fecal urgency and increased defication
cramps, flatulence, fecal incontinence
impaired absorption of fat-soluble vitamins
contraindicated during pregnancy

105
Q

Liraglutide (Saxenda)

A

GLP-1 receptor agonist
reduces food intake by enhancing satiety
slows down GI motility
increases postprandial insulin production

106
Q

Liraglutide dosing

A

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
Q

Liraglutide AEs

A

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
Q

Phentermine-topiramate (Qsymia)

A

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
Q

Dosing of phentermine-topiramate

A

3.75mg phentermine/23mg topiramate once daily then titrated up
controlled substance (C-IV)

110
Q

Phentermine-topiramate AEs

A

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
Q

Bupropion- Naltrexone (Contrave)

A

not first-line therapy
no data for CV safety
could be useful for smoker who wants smoking cessation and weight loss

112
Q

Bupropion-Naltrexone dosing

A

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
Q

Bupropion-Naltrexone AEs

A

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
Q

sympathomimetic drugs for weight loss

A

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
Q

phentermine dosing

A

15-37.5mg daily or divided in BID dosing (C-IV)

116
Q

Initial management of obesity

A

counseling, lifestyle modification, addressing underlying comorbidities

117
Q

Drug categories that cause weight loss

A

anticonvulsants, antidepressants, antipsychotics, ADHD medication

118
Q

Drug categories that cause weight gain

A

Antidepressants, antipsychotics, diabetes meds, glucocorticoids, hormonal agents, anticonvulsants, neurologic and mood-stabilizing agents, antihistamines, alpha blockers, beta blockers

119
Q

First and second line weight loss drugs

A

first line: liraglutide
second line: orlistat, phentermine
use single agent over combination drugs

120
Q

Monitoring for weight loss drugs

A

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