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Innovative Medicines & Omics Pharmacotherapy of obesity

required, the dosage can be raised to 11.25 mg of extended- combination medication should be taken twice daily with
release topiramate and 37.5 mg of phentermine taken 32 mg of naltrexone and 360 mg of bupropion each time.
once daily, in the morning. The highest approved dose It comes in the form of extended-release tablets, allowing
for Qsymia is 15 mg of extended-release topiramate and for their dosage gradually increased over the course of
75 mg of phentermine taken once daily, in the morning. several weeks. The medication is designed to influence the
brain’s reward system, which helps to reduce appetite and
Weight loss may be possible with the topiramate and 67
phentermine for obesity combination; however, there may cravings, supporting weight loss goals.
be adverse effects which vary across users to varying degrees. The combination of naltrexone and bupropion can
The following list includes topiramate/phentermine side trigger several side effects, such as nausea, constipation,
effects that are common. Typical adverse effects include headache, dizziness, dry mouth, and insomnia. Some
dry mouth, constipation, fatigue or drowsiness, memory people may suffer from anxiety, increased blood pressure,
or concentration problems, anxiety, despair, mood swings, or elevated heart rate. In a few circumstances, it can lead
or irritation, speech difficulties or confusion, elevated to seizures, liver problems, or psychiatric symptoms like
heart rate or palpitations, elevated blood pressure, suicidal depression or suicidal thoughts. 68
thoughts or behavior, vision problems, and kidney stones. 64 The contraindications of naltrexone-bupropion are

The use of the combination of topiramate and multiple. For instance, people with a history of seizures,
phentermine, for the treatment of obesity, has certain eating disorders (e.g., anorexia or bulimia), or uncontrolled
contraindications. Topiramate should not be used by hypertension, should not take these medicines as
individuals with a history of kidney stones, glaucoma, liver bupropion can lower the seizure threshold and elevate
impairment, respiratory issues, and during pregnancy. blood pressure. Furthermore, they should not be used
On the contrary, people with cardiovascular diseases, with a combination of alcohol or opioid, as naltrexone
hyperthyroidism, glaucoma, during pregnancy or may precipitate withdrawal symptoms. Furthermore, it
breastfeeding, or with a history of substance abuse, should is contraindicated in patients taking monoamine oxidase
not use phentermine. In general, the combination of the inhibitors or within 14 days of discontinuing them, due to
69
two medicines should be avoided in pregnant women, potential interactions. Recently, in an attempt to bypass
severe cardiovascular conditions, glaucoma, or a history of these and other limitations, 3D printing technology has
70,71
kidney stones. 65 been utilized to develop personalized bupropion tablets.
11.5. Metreleptin
11.4. Νaltrexone/Bupropion
Metreleptin is considered an analog of leptin, a hormone
Bupropion is a norepinephrine-dopamine reuptake that plays an important role in controlling several
inhibitor that was initially approved for depression but has factors, including energy balance, fat storage, and
shown weight loss in several studies. The weight effects hunger. By binding to the leptin receptors (LEPR) in the
are variable; however, the systematic review indicates that hypothalamus, it helps decrease appetite, increase energy
bupropion generally causes weight loss rather than gain. expenditure, and encourage fat metabolism. In patients
On the other hand, naltrexone is an opioid antagonist with leptin deficiency or resistance, like those who have
that works by antagonizing central opioid receptors, thus certain types of lipodystrophy, metreleptin can aid in
reducing food intake due to the blockade of β-endorphin normal leptin function restoration, leading to improved
at the µ-opioid receptor. The result is a reduced intake of metabolic parameters such as better glucose control, lipid
foods, which supports weight reduction. The combination metabolism, and body weight. It is especially useful in
of bupropion and naltrexone exerts a synergistic effect on treating hormonal imbalances caused by leptin deficiency,
weight loss. Bupropion increases pro-opiomelanocortin which can result in severe obesity and related issues.
(POMC) firing, which is involved in appetite regulation;
naltrexone prevents the autoinhibitory feedback produced Metreleptin is administered as a subcutaneous injection.
by β-endorphin on the POMC neurons. The combination The typical starting dose for adults and pediatric patients
helps sustain weight loss and manage obesity more with generalized lipodystrophy is 0.06 mg/kg once daily.
effectively than either of the drugs given individually. For patients with partial lipodystrophy, the recommended
Although the exact mechanisms of actions are being starting dose is 0.03 mg/kg once daily. The dose may be
studied, this drug combination has shown promise in adjusted based on clinical response, but it should not
achieving marked weight loss among obese subjects. The exceed 1.0 mg/kg per day.
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purpose of naltrexone/bupropion medication is to aid in Metreleptin may cause side effects, including injection
weight loss for adults who are overweight or obese. This site reactions, headache, and abdominal pain. More

Volume 2 Issue 2 (2025) 10 doi: 10.36922/imo.8316