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Questions and Answers
What is a commonly reported adverse effect of bupropion when used as an appetite suppressant?
What is a commonly reported adverse effect of bupropion when used as an appetite suppressant?
Which of the following accurately describes the primary action of lipase inhibitors in obesity treatment?
Which of the following accurately describes the primary action of lipase inhibitors in obesity treatment?
What is the significant risk associated with the use of bupropion in patients?
What is the significant risk associated with the use of bupropion in patients?
What is the expected average net weight loss associated with bupropion when administered at a dosage of 400 mg for 24 weeks?
What is the expected average net weight loss associated with bupropion when administered at a dosage of 400 mg for 24 weeks?
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Which of the following medications is contraindicated when initiating bupropion/naltrexone therapy?
Which of the following medications is contraindicated when initiating bupropion/naltrexone therapy?
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What mechanism is primarily targeted by incretin mimetics, such as semaglutide and liraglutide, in the treatment of obesity?
What mechanism is primarily targeted by incretin mimetics, such as semaglutide and liraglutide, in the treatment of obesity?
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What is one of the key adverse effects associated with the combination of bupropion and naltrexone for weight management?
What is one of the key adverse effects associated with the combination of bupropion and naltrexone for weight management?
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What is a common gastrointestinal side effect of liraglutide?
What is a common gastrointestinal side effect of liraglutide?
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Which drug class is specifically noted for causing substantial weight gain, particularly in longer-term therapy?
Which drug class is specifically noted for causing substantial weight gain, particularly in longer-term therapy?
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What is the function of orlistat as a lipase inhibitor?
What is the function of orlistat as a lipase inhibitor?
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Which appetite suppressant is exclusively approved in Canada for weight management, often used in combination with naltrexone?
Which appetite suppressant is exclusively approved in Canada for weight management, often used in combination with naltrexone?
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Which condition contraindicates the use of orlistat?
Which condition contraindicates the use of orlistat?
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Which weight management strategy has shown to be superior in achieving long-term weight loss of 5-10%?
Which weight management strategy has shown to be superior in achieving long-term weight loss of 5-10%?
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Which incretin hormone is primarily responsible for reducing food intake and appetite?
Which incretin hormone is primarily responsible for reducing food intake and appetite?
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What dietary recommendation should be given to patients taking orlistat?
What dietary recommendation should be given to patients taking orlistat?
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What serious potential side effect can occur with the use of liraglutide?
What serious potential side effect can occur with the use of liraglutide?
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Liraglutide is primarily administered through which method?
Liraglutide is primarily administered through which method?
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Patients on orlistat should ideally limit dietary fat intake because:
Patients on orlistat should ideally limit dietary fat intake because:
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What is the primary aim of drug therapy in managing obesity?
What is the primary aim of drug therapy in managing obesity?
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What is a significant barrier that complicates obesity management?
What is a significant barrier that complicates obesity management?
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Which medication is associated with an average weight gain of 2 kg during a six-month course?
Which medication is associated with an average weight gain of 2 kg during a six-month course?
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What percent weight loss can be expected with bupropion/naltrexone combination therapy over 48 weeks?
What percent weight loss can be expected with bupropion/naltrexone combination therapy over 48 weeks?
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Which class of drugs is known to cause substantial weight gain, particularly in psychiatric treatments?
Which class of drugs is known to cause substantial weight gain, particularly in psychiatric treatments?
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When should treatment with bupropion/naltrexone be initiated concerning opioid therapy?
When should treatment with bupropion/naltrexone be initiated concerning opioid therapy?
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What is a common adverse effect when using bupropion as an appetite suppressant?
What is a common adverse effect when using bupropion as an appetite suppressant?
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What is the established weight of the net weight loss from bupropion at a dose of 300 mg for 24 weeks?
What is the established weight of the net weight loss from bupropion at a dose of 300 mg for 24 weeks?
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Prior to initiating orlistat, what dietary recommendation is usually suggested to the patient?
Prior to initiating orlistat, what dietary recommendation is usually suggested to the patient?
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Which pharmacological option is specifically noted to be used in combination with naltrexone in Canada for weight management?
Which pharmacological option is specifically noted to be used in combination with naltrexone in Canada for weight management?
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What is the primary mechanism through which lipase inhibitors like orlistat aid in weight loss?
What is the primary mechanism through which lipase inhibitors like orlistat aid in weight loss?
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Which of the following adverse effects is most commonly associated with liraglutide?
Which of the following adverse effects is most commonly associated with liraglutide?
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In which clinical scenario might orlistat be contraindicated?
In which clinical scenario might orlistat be contraindicated?
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Which underlying condition requires caution when administering liraglutide?
Which underlying condition requires caution when administering liraglutide?
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What is a significant effect of the hormone GLP-1 in the context of obesity treatment?
What is a significant effect of the hormone GLP-1 in the context of obesity treatment?
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Which dosage of liraglutide has been shown to produce significant weight loss when combined with lifestyle measures?
Which dosage of liraglutide has been shown to produce significant weight loss when combined with lifestyle measures?
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What impact does a high fat intake have on the effectiveness of orlistat?
What impact does a high fat intake have on the effectiveness of orlistat?
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What common gastrointestinal side effect does orlistat share with liraglutide?
What common gastrointestinal side effect does orlistat share with liraglutide?
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What is the primary reason for integrating pharmacologic therapy with lifestyle modifications in obesity management?
What is the primary reason for integrating pharmacologic therapy with lifestyle modifications in obesity management?
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Which substance is specifically mentioned as a necessary consideration when initiating bupropion/naltrexone therapy?
Which substance is specifically mentioned as a necessary consideration when initiating bupropion/naltrexone therapy?
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What is a critical aspect of the management goals for obesity therapy?
What is a critical aspect of the management goals for obesity therapy?
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What long-term weight maintenance is expected after discontinuation of anti-obesity medication?
What long-term weight maintenance is expected after discontinuation of anti-obesity medication?
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Which adverse effect is most concerning at higher doses of bupropion?
Which adverse effect is most concerning at higher doses of bupropion?
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Which antidepressant is specifically noted for its association with weight gain during therapy?
Which antidepressant is specifically noted for its association with weight gain during therapy?
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What combination of drugs is primarily approved for appetite suppression in Canada?
What combination of drugs is primarily approved for appetite suppression in Canada?
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Which of the following medications is associated with a weight gain of up to 8 kg during intensive treatment courses?
Which of the following medications is associated with a weight gain of up to 8 kg during intensive treatment courses?
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What mechanism is associated with appetite suppression mediated by bupropion/naltrexone?
What mechanism is associated with appetite suppression mediated by bupropion/naltrexone?
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What is a crucial factor to monitor in patients taking drugs that lower the seizure threshold?
What is a crucial factor to monitor in patients taking drugs that lower the seizure threshold?
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What is the mechanism through which GLP-1 influences food intake in obesity treatment?
What is the mechanism through which GLP-1 influences food intake in obesity treatment?
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Which aspect should be monitored carefully due to potential complications in patients using liraglutide?
Which aspect should be monitored carefully due to potential complications in patients using liraglutide?
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What is the recommended action regarding vitamin intake for patients on orlistat?
What is the recommended action regarding vitamin intake for patients on orlistat?
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Why is a high fat diet poorly tolerated in patients taking orlistat?
Why is a high fat diet poorly tolerated in patients taking orlistat?
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What factors limit the effectiveness of orlistat in weight management?
What factors limit the effectiveness of orlistat in weight management?
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In which scenario should liraglutide be avoided due to increased risk?
In which scenario should liraglutide be avoided due to increased risk?
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What is a common gastrointestinal side effect associated with both orlistat and liraglutide?
What is a common gastrointestinal side effect associated with both orlistat and liraglutide?
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What is the primary action of dipeptidyl peptidase 4 (DPP4) in relation to incretin hormones?
What is the primary action of dipeptidyl peptidase 4 (DPP4) in relation to incretin hormones?
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Study Notes
Obesity Treatment
- Obesity is a complex chronic condition with no single treatment and no cure
- There are numerous psychosocial, emotional, or physical barriers to engaging in treatment strategies
- The goal of all treatment strategies is to reduce excess body fat for health benefits
- Reducing weight by 5-10% can lead to improved health
- Focus is on stabilizing and preventing further weight gain, not just cosmetic reasons
- Treatment includes two phases
- Induction of weight loss achieved through caloric restriction
- Prevention of weight regain countering neurobehavioural changes that attempt to restore body weight
Medications Contributing to Weight Gain
- Medications known to be linked to weight gain include several classes:
- Antidepressants, including tricyclic antidepressants
- Antipsychotics, both first and second generations
- Corticosteroids
- Antihyperglycemic drugs, including sulfonylureas, meglitinides, thiazolidinediones and insulin
- Lithium
Pharmacologic Treatments for Obesity
- Lifestyle modification and anti-obesity therapies are more effective in achieving weight loss than lifestyle modification alone
- Goal is to achieve a target weight loss of 5-10%
- Discontinuation of anti-obesity medication typically leads to weight regain
Appetite Suppressants
- Only approved appetite suppressants in Canada are Bupropion and Bupropion/Naltrexone
- Bupropion is a sympathomimetic drug, also used as an antidepressant and smoking cessation aid
- 300mg for 24 weeks results in a net weight loss of 2.2%; 400mg results in 5.1% weight loss
- Weight loss is maintained for 48 weeks
- Bupropion is a sympathomimetic drug, also used as an antidepressant and smoking cessation aid
- Bupropion/Naltrexone is indicated for weight management alongside diet and exercise
- For individuals with a BMI of 30 or higher, or 27 with weight-related comorbidities
- Mediates hormones involved in appetite and reward
- Net weight loss of 4.2% over 48 weeks
Bupropion Side Effects
- Dry mouth, constipation, agitation, insomnia, anxiety
- Can cause seizures in rare instances with higher doses
- Caution recommended in patients with hepatic impairment
Bupropion/Naltrexone Side Effects
- Nausea, vomiting, constipation, headache, dizziness, insomnia, dry mouth
- Contraindicated with concurrent opioid therapy due to the risk of opioid withdrawal
- Patients must be opioid-free for 7 days before treatment
Bupropion/Naltrexone Precautions
- Avoid concurrent use of drugs that lower seizure threshold
- Minimize or avoid alcohol consumption
- Avoid consumption with high-fat meals
- Avoid in patients with uncontrolled hypertension, seizure disorder, severe hepatic impairment, or end-stage renal failure
Lipase Inhibitors
- Orlistat is a pancreatic and gastric lipase inhibitor that reduces dietary fat absorption by 30%
- For an average diet of 60g of fat per day, it results in a 180kcal/d reduction
- Compared to placebo, it leads to an additional 2.9% weight loss over 1 year
Orlistat Side Effects
- Oily spotting, flatus with discharge, fecal urgency
- Decreased absorption of fat-soluble vitamins
- Contraindicated in patients with chronic malabsorption syndrome or cholestasis
Orlistat Precautions
- Advise patients to take a multivitamin daily at least 2 hours before or after orlistat or at bedtime
- High fat intake is poorly tolerated
- Less effective in patients on low-fat diets and difficult to take for those with irregular eating patterns
Incretin Mimetics
- Glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are responsible for most of the glucose-induced insulin secretory response following glucose ingestion
- Both are metabolized by the enzyme dipeptidyl peptidase 4 (DPP4)
- GLP-1 is responsible for reduction of food intake and appetite with increased satiety and decreased gastric emptying
- Also affects reward-related systems in the brain
- GIP has less effect on other organs, but also delays gastric emptying and plays a potential role in fat deposition
Liraglutide
- GLP-1 agonist
- Administered by subcutaneous injection
- Originally approved for type 2 diabetes, then rebranded for obesity
- 3mg SC can induce 8kg of weight loss over 2 years of therapy in conjunction with lifestyle measures
Liraglutide Side Effects
- Nausea, vomiting, constipation, and diarrhea are common
- Side effects can be minimized by slow titration
- Rare instances of pancreatitis reported
- Severe hypoglycemia observed in patients with type 2 diabetes; adjustments to their diabetes medication may be required
Liraglutide Precautions
- 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)
Obesity
- Complex chronic condition with no single management strategy for every patient
- Psychosocial, emotional, or physical barriers can hinder treatment adherence
- There is no cure - Focus on patient education and lifestyle changes
- Until recently, no medications specifically indicated for obesity
Goals of Therapy
- Reduce excess body fat for health, not cosmetic reasons (5-10% can result in significant health benefits)
- Stabilize and prevent further weight gain
- Prevent weight regain
- Prevent and treat obesity-related comorbidities and complications
Treatment Phases
- Induction of weight loss: Achieved through caloric restriction and medication
- Prevention of weight regain: Countering the body's natural tendency to regain lost weight
Drugs Associated with Weight Gain
- Antidepressants: Particularly tricyclic antidepressants (e.g., amitriptyline can cause 1.8kg weight gain in first 3 months)
- Antipsychotics: First and second generations (between 9 and 12 kg weight gain)
- Corticosteroids: (e.g. prednisone, average 2kg during 6-month course)
- Antihyperglycemic drugs: Sulfonylureas, meglitinides, thiazolidinediones (up to 5kg within 3-12 months)
- Insulin: Intensive 3-month course can cause 8kg weight gain
- Lithium: Used for mania, can lead to 10kg or more weight gain over 6-10 years.
Pharmacological Choices
- Lifestyle modification combined with anti-obesity therapy superior to lifestyle changes alone
- Discontinuation of anti-obesity medication generally results in weight regain
Appetite Suppressants
- Bupropion: Sympathomimetic drug (sustained-release)
- Used for antidepressant and smoking cessation, prescribed for weight management
- 300mg for 24 weeks associated with 2.2% weight loss; 400 mg with 5.1%, sustained for 48 weeks
- Bupropion/naltrexone indicated for BMI ≥ 30 (27 if comorbidity present)
- Mediates hormones involved in appetite and reward
- Net weight loss of 4.2% over 48 weeks
Bupropion - Adverse Effects
- Dry mouth, constipation, agitation, insomnia, anxiety
- Can cause seizures in rare instances with higher doses
- Exercise caution in patients with hepatic impairment
Bupropion/Naltrexone - Adverse Effects
- Nausea, vomiting, constipation, headache, dizziness, insomnia, dry mouth
- Contraindicated with concurrent opioid therapy (can induce withdrawal)
- Opioid-free for 7 days before starting treatment
Bupropion - Cautions
- Avoid concurrent use of drugs that lower the seizure threshold
- Minimize or avoid alcohol consumption
- Avoid consumption with a high-fat meal
- Avoid in patients with uncontrolled hypertension, seizure disorder, severe hepatic impairment, or end-stage renal failure.
Lipase inhibitors
- Orlistat: Pancreatic and gastric lipase inhibitor, reduces dietary fat absorption by 30%
- Average diet of 60g fat per day, results in 180kcal/day reduction
- Compared to placebo: 2.9% additional weight loss over 1 year
Orlistat - Adverse Effects
- Oily spotting, flatus with discharge, fecal urgency
- Decreased absorption of fat-soluble vitamins
- Contraindicated in patients with chronic malabsorption syndrome or cholestasis
Orlistat - Cautions
- Advise patients to take a multivitamin daily (≥ 2 hours before/after or at bedtime)
- High fat intake poorly tolerated
- Less effective in patients on low-fat diets, difficult for those with irregular eating patterns
Incretin Mimetics
- Glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)
- Responsible for glucose-induced insulin secretory response after glucose ingestion
- Metabolized by the enzyme dipeptidyl peptidase 4 (DPP4)
GLP-1 Action
- Reduces food intake and appetite, increased satiety, decreased gastric emptying
- Affects reward-related systems in the brain
GIP Action
- Less effect on other organs, but also delays gastric emptying, may play a role in fat deposition
Liraglutide
- GLP-1 agonist
- Administered by subcutaneous injection
- Originally approved for type 2 diabetes, rebranded for obesity
- 3mg SC can induce 8kg weight loss over 2 years with lifestyle measures
Liraglutide - Adverse Effects
- Nausea, vomiting, constipation, and diarrhea (can be minimized with slow titration)
- Pancreatitis in rare instances
- Severe hypoglycemia observed in patients with type 2 diabetes (adjust diabetes medications)
Liraglutide - Cautions
- Exercise 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).
Obesity Management
- Obesity is a complex, chronic condition
- No single management strategy fits all patients
- There is no cure for obesity
- Until recently, there were no medications specifically indicated for obesity
Goals of Obesity Therapy
- Reduce excess body fat for health reasons
- Reducing weight by 5-10% can have significant health benefits
- Stabilize and prevent further weight gain
- Prevent weight regain
- Prevent and treat obesity-related comorbidities and complications
Treatment Phases of Obesity
- Induction of weight loss achieved through caloric restriction
- Prevention of weight regain countering neurobehavioural changes that seek to restore body weight to its original level
Drugs Associated with Weight Gain
-
Antidepressants:
- Particularly tricyclic antidepressants (e.g., Amitriptyline)
- Associated with weight gain of 1.8kg over 3 months of therapy
- Particularly tricyclic antidepressants (e.g., Amitriptyline)
-
Antipsychotics:
- Both first and second generations
- Associated with weight gain of 9-12kg
- Both first and second generations
-
Corticosteroids:
- (e.g., Prednisone)
- Average weight gain of 2 kg during a 6-month daily course of therapy
- (e.g., Prednisone)
-
Antihyperglycemic drugs:
- Sulfonylureas, meglitinides, thiazolidinediones
- Weight gain of up to 5kg over 3-12 months of treatment
- Insulin
- Weight gain of up to 8kg during intensive 3-month course of therapy
- Sulfonylureas, meglitinides, thiazolidinediones
-
Lithium:
- Used in mania treatment
- Weight gain of 10kg or more over 6-10 years of therapy
- Used in mania treatment
Pharmacological Choices in Obesity
- Lifestyle modification and anti-obesity therapy is superior to lifestyle modification alone for achieving a target weight loss of 5-10% over the long term.
- Discontinuation of anti-obesity medication generally results in weight regain
Appetite Suppressants
-
Bupropion alone or in combination with naltrexone:
- Only options approved in Canada
- Bupropion (Sympathomimetic) is a sustained-release antidepressant and smoking cessation aid
- 300mg for 24 weeks associated with a net weight loss of 2.2%
- 400mg for 24 weeks associated with a net weight loss of 5.1%
- Weight loss maintained for 48 weeks
-
Bupropion/naltrexone
- Indicated for weight management alongside diet and exercise, for those with a BMI of 30 or higher (27 if weight-related comorbidity present)
- Mediates hormones involved in appetite and reward
- Net weight loss of 4.2% over 48 weeks
Adverse Effects - Bupropion
- Dry mouth, constipation, agitation, insomnia, anxiety
- Can cause seizures in rare instances with higher doses
- Caution in patients with hepatic impairment
Adverse Effects - Bupropion/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
Precautions for Bupropion and Bupropion/Naltrexone
- Avoid concurrent use of drugs that lower the seizure threshold
- Minimize or avoid alcohol consumption
- Avoid consumption with a high-fat meal
- Avoid in patients with uncontrolled hypertension, seizure disorder, severe hepatic impairment, or end-stage renal failure
Lipase Inhibitors
-
Orlistat
- Pancreatic and gastric lipase inhibitor that reduces dietary fat absorption by 30%
- For an average diet of 60g of fat per day, results in a 180kcal/d reduction
- Compared to placebo, it provides 2.9% additional weight loss over 1 year
Orlistat – Adverse Effects
- Oily spotting, flatus with discharge, fecal urgency
- Decreased absorption of fat-soluble vitamins
- Contraindicated in patients with chronic malabsorption syndrome or cholestasis
Orlistat - Cautions
- Advise patients to take a multivitamin daily ≥2 hours before or after orlistat, or at bedtime
- A high-fat intake is poorly tolerated
- Less effective in patients on low-fat diets and is difficult to take for individuals with irregular eating patterns
Incretin Mimetics
- The two major incretin hormones in humans are glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)
- They are responsible for most of the glucose-induced insulin secretory response following glucose ingestion
- Both are metabolized by the enzyme dipeptidyl peptidase 4 (DPP4)
GLP-1 and GIP Properties
- 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 has less effect on other organs, but also delays gastric emptying and seems to play a role in fat deposition
Liraglutide
- A GLP-1 agonist
- Administered by subcutaneous injection
- Originally approved for type 2 diabetes and then rebranded for obesity
- 3mg SC can induce 8kg of weight loss over 2 years of therapy in conjunction with lifestyle measures
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).
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Description
Explore the complexities of obesity treatment, focusing on the various psychosocial and physical challenges faced. This quiz discusses the goals of weight loss, phases of treatment, and medications that can contribute to weight gain. Test your knowledge on effective strategies for managing obesity and understanding the role of medications.