pharm wk 2 Flashcards
what are 2 examples of incretic mimetics
semaglutide and liraglutide
work on GLP1 or GIP
what is the example of appetite suppressant
buproprion
what is the lipase inhibitor example
orlistat
what is the goal of therapy for obesity
reduce excess body fat for health and not for cosmetic reasons; reducing weight by 5–10% can result in important health benefits
prevent weight regain
prevent and treat comorbidities
2 treatment phases of obesity
Induction of weight loss – achieved through caloric restriction
Prevention of weight regain – countering the neurobehavioural changes that seek to restore body weight to its original level
drugs associated with weight gain (5)
antidepressants - TCAs (amitriptyline)
antipsychotics (1st and 2nd generations)
corticosteroids (i.e. prednisone)
antihyperglycemic drugs (sulfonylureas. meglitinides, thiazolidinediones, insulin)
lithium (for mania)
what are the 2 appetite suppressants
bupropion and naltrexone (can combine)
what type of drug is bupropion
sympathomimetic (acts like NE/E and is stimulating)
what type of release does bupropion have
sustained release formula
other than appetite suppression, what else can bupropion be used for
antidepressant and smoking cessation aid
who is bupropion/naltrexone recommended for
Indicated for weight management alongside diet and exercise for those with a BMI of 30 or higher (27 if weight-related comorbidity present)
what hormones does bupropion/naltrexone mediate
Mediates hormones involved in appetite and reward
Adverse effects of bupropion
Dry mouth, constipation, agitation, insomnia, anxiety
Can cause seizures in rare instances with higher doses
Caution in patients with hepatic impairment
adverse effects of combining bupropion and naltrexone
Nausea, vomiting, constipation, headache, dizziness, insomnia, dry mouth
Contraindicated with concurrent opioid therapy (due to precipitation of opioid withdrawal)
Patients must be opioid free for 7 days prior to initiation of treatment
cautions for bupropion and naltrexone use
Avoid concurrent use of drugs that lower the seizure threshold.
Minimize or avoid alcohol consumption.
Avoid in patients with uncontrolled hypertension, seizure disorder, severe hepatic impairment, or end-stage renal failure.
what food should you take bupropion and naltrexone away from
high fat meal
orlistat îs a
lipase inhibitor
what does orlistat do ? by what %?
dont absorb fat
Pancreatic and gastric lipase inhibitor that reduces dietary fat absorption by 30%
adverse effects or orlistat
Oily spotting, flatus with discharge, fecal urgency.
Decreased absorption of fat-soluble vitamins
Contraindicated in patients with chronic malabsorption syndrome or cholestasis.
cautions with orlistat
Advise patients to take a multivitamin daily ≥2 h before or after orlistat or at bedtime
A high fat intake is poorly tolerated
who is orlistat less effective in
Less effective in patients on low-fat diets and is difficult to take for individuals with irregular eating patterns
2 major incretin hormones in humans are
glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)
what do incretin hormones do
responsible for most of the glucose-induced insulin secretory response following glucose ingestion
what are GLP-1 and GIP (incretins) metabolized by
by the enzyme dipeptidyl peptidase 4 (DPP4)
what effects does GLP-1 have
GLP-1 is also responsible for the reduction of food intake and appetite, increased satiety, and decreased gastric emptying
GLP-1 also affects reward-related systems in the brain
GIP effects on the body
GIP has less effect on other organs, but also delays gastric emptying and seems to play a role in fat deposition
what is liraglutide
GLP-1 agonist
how to administer liraglutide
subcutaneous injection
what is liraglutide fro
Originally approved for type 2 diabetes and then rebranded for obesity
adverse effects of liraglutide
Nausea, vomiting, constipation, and diarrhea are most common
Gastrointestinal side effects can be minimized by a slow titration.
Can cause pancreatitis in rare instances
Severe hypoglycemia observed in patients with type 2 diabetes; adjustment of diabetes medications may be required
cautions for liraglutide
Caution in patients with heart rhythm disturbances, hepatic insufficiency, and severe renal impairment.
Should not be used in inflammatory bowel disease.
Contraindicated in pregnancy, breastfeeding, personal or family history of medullary thyroid carcinoma or multiple endocrine neoplasia syndrome type 2 (MEN 2).
Discontinue after 12 weeks if body weight loss <5%
what is semaglutide
GLP-1 agonist
what is the difference between semaglutide and liraglutide
GLP-1 agonist like liraglutide but with a longer half-life (165 hours compared to liraglutide’s 13 – 15 hours)
how to administer semaglutide
weekly subcutaneous injections
what is better at weight loss; semaglutide or liraglutide
semaglutide
adverse effects of semaglutide
Similar to liraglutide
Nausea, diarrhea, abdominal pain, vomiting, constipation, digestive upset, fatigue, dizziness
Increase in amylase and lipase (suggesting possible pancreatitis)
what is obesity during pregnancy associated with
gestational diabetes, gestational hypertension, preeclampsia, birth defects, caesarean delivery, fetal macrosomia, perinatal deaths, postpartum anemia and childhood obesity in offspring
Increased risk of complications following caesarean delivery
Labor is longer
what is not recommended during pregnancy
Despite the increased risks of obesity and pregnancy, weight loss during pregnancy is not recommended
what is the recommended weight targets for pregnancy
NOT WEIGHT LOSS
weight gain targets (to gain no more than 5 – 9.1 kg (11 – 20 lb) during pregnancy
what drugs for pregnancy vs not
Orlistat is specifically not recommended during pregnancy due to reduced fat-soluble vitamin absorption
Evidence for bupropion is conflicting. It should not necessarily be withheld for continuation of therapy if patient is already taking it
meta analysis of liraglutide, semaglutide and GLP-1 infusions
what do most studies show
evidence of appetite suppression, delayed gastric emptying, and changes in taste and food preferences
high dose semaglutide in obesity STEP trail
drug group vs drug and calorie restriction and exercise
Additional mean change in weight for the drug group: 12.6%
Which of the following medications is expected to cause the greatest amount of weight loss?
A. Liraglutide
B. Orlistat
C. Bupropion
D. Semaglutide
D. Semaglutide
how much % weight is loss using bupropion / naltrexone
Net weight loss of 4.2% over 48 weeks
how much weight loss % using orlistat
Compared to placebo: 2.9% additional weight loss over 1 year
how much weight loss using liraglutide
3 mg SC can induce 8 kg of weight loss over 2 years of therapy in conjunction with lifestyle measures
how much weight loss using semaglutide
Shown to reduce weight by approximately 16 kg over 2 years of therapy (double of that or liraglutide)
