Diethylpropion (Anorex) - Uses, Dose, Side effects, MOA, Brands

Diethylpropion is a sympathomimetic amine that acts as an appetite suppressant. It is used for the short-term management of obesity, typically as an adjunct to diet and exercise. This medication works by stimulating the release of norepinephrine in the brain, which leads to decreased appetite. Diethylpropion is similar in mechanism of action to other appetite suppressants like phentermine.

Diethylpropion (Anorex) is a stimulant drug that causes decreases appetite via central mechanisms. It is used for the short-term treatment of exogenous obesity.

Diethylpropion Uses:

  • Obesity:
    • It is indicated for the short-term treatment of obesity as an adjunct to diet and exercise.
  • Weight loss treatment is indicated in patients who have a body mass index of 30 kg/m² or more or 27 kg/m² or more in the presence of other metabolic risk factors like hypertension, diabetes, and/or dyslipidemia or a high waist circumference.
  • Weight loss treatment must be used in conjunction with a comprehensive weight management program.

Diethylpropion (Anorex) Dose in Adults:

Diethylpropion (Anorex) Dose in the treatment of Obesity: Oral:

  • Immediate release tablets: Take 25 mg three to four times a day. That means you'd take it three to four times spread out over the day.
  • Controlled release tablets: Take 75 mg once a day. This kind of tablet slowly releases the medication into your body throughout the day.

Use in Children:

Refer to adults dosing.   


Pregnancy Risk Factor B

  • Diethylpropion has a pregnancy risk factor of B, which means that while animal studies haven't shown any harm to the fetus, it does cross the placenta in humans.
  • Some rare cases of birth defects have been reported, but it's not clear if diethylpropion is the cause.
  • However, newborns might experience withdrawal symptoms if their mothers took diethylpropion during pregnancy.
  • It's important for pregnant women to discuss the risks and benefits of taking diethylpropion with their doctors before using it.

Diethylpropion use during breastfeeding:

  • Diethylpropion can pass into breast milk, so caution is advised when giving it to nursing mothers.
  • This means that if a breastfeeding mother takes diethylpropion, the medication could potentially be passed on to her baby through breast milk.

Dose in Kidney Disease:

  • The manufacturer's instructions do not include specific dosage adjustments for people with kidney problems when using diethylpropion.
  •  However, caution should still be exercised when prescribing this medication to individuals with renal impairment.

Dose in Liver disease:

  • The manufacturer's instructions do not include specific dosage adjustments for individuals with liver impairment when using diethylpropion.
  • However, it's crucial to exercise caution when prescribing this medication to patients with liver issues.
  • Liver impairment can affect how the body processes medications, potentially leading to an increased risk of side effects or complications.

Side effects of Diethylpropion (Anorex):

  • Cardiovascular:
    • Cardiac Arrhythmia
    • Cerebrovascular Accident
    • ECG Changes
    • Heart Valve Disease
    • Hypertension
    • Palpitations
    • Tachycardia
  • Central Nervous System:
    • Anxiety
    • Depression
    • Dizziness
    • Drowsiness
    • Dysphoria
    • Euphoria
    • Headache
    • Insomnia
    • Jitteriness
    • Malaise
    • Nervousness
    • Overstimulation
    • Precordial Pain
    • Psychosis
    • Restlessness
    • Seizure
  • Dermatologic:
    • Alopecia
    • Diaphoresis
    • Ecchymoses
    • Erythema
    • Skin Rash
    • Urticaria
  • Endocrine & Metabolic:
    • Changes In Libido
    • Gynecomastia
    • Menstrual Disease
  • Gastrointestinal:
    • Abdominal Distress
    • Constipation
    • Diarrhea
    • Dysgeusia
    • Nausea
    • Vomiting
    • Xerostomia
  • Genitourinary:
    • Dysuria
    • Impotence
  • Hematologic & Oncologic:
    • Agranulocytosis
    • Bone Marrow Depression
    • Leukopenia
  • Neuromuscular & Skeletal:
    • Dyskinesia
    • Myalgia
    • Tremor
  • Ophthalmic:
    • Blurred Vision
    • Mydriasis
  • Renal:
    • Polyuria
  • Respiratory:
    • Dyspnea
    • Pulmonary Hypertension
  • Miscellaneous:
    • Tachyphylaxis

Contraindications to Diethylpropion (Anorex):

  • Diethylpropion should not be used in individuals who have a hypersensitivity or idiosyncrasy to diethylpropion or other sympathomimetic amines, as this could lead to adverse reactions.
  • It is also contraindicated in those with advanced arteriosclerosis, severe hypertension, pulmonary hypertension, hyperthyroidism, glaucoma, agitated states, or a history of drug abuse.
  • Additionally, diethylpropion should not be used during or within 14 days following MAO inhibitor therapy, as this combination can lead to serious, potentially life-threatening reactions.
  • Concurrent use with other anorectic agents is also not recommended due to the potential for additive effects and increased risk of adverse events.

Warnings and precautions

CNS effects

  • Amphetamines, including diethylpropion, can affect the central nervous system (CNS) and may impair a person's ability to safely engage in activities that require focus and coordination, such as driving or operating machinery.
  • These medications can cause dizziness, drowsiness, or blurred vision, which can increase the risk of accidents or injuries.
  • It's important for individuals taking diethylpropion to be aware of these potential side effects and to avoid activities that require alertness and concentration until they know how the medication affects them personally.

Heart failure:

  • According to a scientific statement from the American Heart Association, diethylpropion has been identified as a medication that may cause direct toxicity to the heart muscle (myocardium), with the magnitude of this effect considered major.
  • This means that diethylpropion has the potential to negatively impact the function of the heart, particularly in individuals with existing heart conditions or those at risk of developing heart failure.

Primary pulmonary hypertension (PPH).

  • Primary pulmonary hypertension (PPH) is a rare and often fatal lung disease that has been observed more frequently in patients taking certain appetite suppressants, including diethylpropion.
  • Research suggests that using these appetite suppressants for more than three months could significantly increase the risk of developing pulmonary hypertension, with some studies indicating a 23-fold increase in risk.
  • If a patient using diethylpropion experiences symptoms such as shortness of breath during exertion, chest pain (angina), fainting spells (syncope), or swelling in the legs (edema), it's crucial to stop using the medication immediately and seek medical evaluation.
  • These symptoms could be indicative of pulmonary hypertension, and prompt action is necessary to assess and manage the condition effectively.

Heart disease of the valvular kind:

  • The use of certain appetite suppressants, like diethylpropion, has been linked to the development of valvular heart disease.
  • This risk may rise with prolonged use, taking higher doses than prescribed, or using multiple appetite suppressants together.
  • It's essential to avoid stimulants in patients with known serious heart conditions, such as structural heart abnormalities, cardiomyopathy, significant heart rhythm issues, or other cardiac problems that could increase the risk of sudden death on their own.
  • These precautions are crucial to minimize the potential risks associated with diethylpropion and other similar medications and to ensure patient safety.

Diabetes:

  • Patients with diabetes mellitus should use diethylpropion with caution.
  • The medication may affect the requirements for antidiabetic agents, such as insulin or oral medications, due to changes in appetite and dietary habits caused by the use of anorexigens like diethylpropion.
  • Additionally, dietary restrictions often accompany the use of diethylpropion as part of a weight loss regimen, which can further impact blood sugar levels and the management of diabetes.

Hypertension:

  • Patients with hypertension should approach the use of diethylpropion with caution, as the medication can potentially exacerbate high blood pressure or heart rate, which may worsen cardiovascular conditions.
  • It is especially important to avoid diethylpropion in individuals with severe hypertension, as the medication could further elevate blood pressure to dangerous levels.

Psychiatric disorders

  • Patients with preexisting psychiatric disorders, such as psychosis or bipolar disorder, should use diethylpropion with caution.
  • This medication has the potential to induce mixed or manic episodes in individuals with bipolar disorder and may worsen symptoms of behavior and thought disorders in psychotic patients.
  • Stimulants like diethylpropion can also trigger new-onset psychosis or mania, particularly in susceptible individuals.

Seizure disorders:

  • Patients with a history of seizure disorders should avoid diethylpropion if possible, or use it with caution under close medical supervision.
  • There is a risk that diethylpropion could lower the seizure threshold, potentially increasing the likelihood of seizures in susceptible individuals.

Tourette's syndrome

  • Patients with Tourette's syndrome should use diethylpropion with caution, as stimulant medications like diethylpropion have the potential to unmask or exacerbate tics associated with Tourette's syndrome.

Diethylpropion: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).

Alcohol (Ethyl)

May increase the toxic/adverse effects of Diethylpropion

Amifampridine

Agents with Seizure Threshold Lower Potential can enhance the neuroexcitatory or seizure-potentiating effects of Amifampridine.

AtoMOXetine

Might increase the hypertensive effects of Sympathomimetics. AtoMOXetine could increase the tachycardic effects of Sympathomimetics.

BuPROPion

Agents with Seizure Threshold Lowering Potential may increase the neuroexcitatory or seizure-potentiating effects.

Cannabinoid-Containing Products

Sympathomimetics may increase the tachycardic effects of Sympathomimetics. Cannabidiol is an exception.

Doxofylline

Doxofylline may be more toxic or harmful if taken with Sympathomimetics.

Esketamine

CNS stimulants may increase hypertension.

Guanethidine

May increase the arrhythmogenic effects of Sympathomimetics. The hypertensive effects of Sympathomimetics may be enhanced by Guanethidine.

Solriamfetol

Sympathomimetics could increase the hypertensive effects of Solriamfetol.

Solriamfetol

The hypertensive effects of Solriamfetol may be augmented by CNS stimulants.

Sympathomimetics

May increase the toxic/adverse effects of other Sympathomimetics.

Risk Factor D (Consider therapy modifications)

Topical Cocaine

Sympathomimetics may increase hypertensive effects. Management: If possible, consider other options to this combination. Concurrent use of this combination can cause significant elevations in blood pressure and heart rate. You should also be aware of any signs of myocardial injury.

Iohexol

Agents with Seizure Threshold Lowering Potential can increase the toxic/adverse effects of Iohexol. The risk of seizures could be elevated. Management: Stop using agents that lower the seizure threshold 48 hrs before you start intrathecal iohexol. To resume these agents, wait at least 24 hours following the procedure. Consider using prophylactic anticonvulsants in non-elective procedures.

Iomeprol

Agents with Seizure Threshold Lowering Potential can increase the toxic/adverse effects of Iomeprol. The risk of seizures could be elevated. Management: Stop using agents that lower the seizure threshold 48 hrs before you start intrathecal iomeprol. To resume these agents, wait at least 24 hours following the procedure. Consider using prophylactic anticonvulsants in non-elective procedures.

Iopamidol

Agents with Seizure Threshold Lowering Potential can increase the toxic/adverse effects of Iopamidol. The risk of seizures could be elevated. Management: Stop using agents that lower the seizure threshold 48 hrs before you start intrathecal iopamidol. To resume these agents, wait at least 24 hours following the procedure. Consider using prophylactic anticonvulsants in non-elective procedures.

Risk Factor X (Avoid Combination)

Acebrophylline

CNS stimulants may have a stronger stimulatory effect.

Iobenguane Radiopharmaceutical Products

CNS stimulants can decrease the therapeutic effects of Iobenguane Radiopharmaceutical Products. Management: Stop using any drugs that could inhibit or interfere catecholamine transport and uptake for at most 5 biological half-lives prior to iobenguane Administration. These drugs should not be administered until 7 days following each iobenguane dosage.

Monoamine Oxidase Inhibitors

May increase the hypertensive effects of Diethylpropion

Monitoring parameters:

Baseline Cardiac Evaluation:

  • Before starting diethylpropion, patients should undergo a cardiac evaluation to assess for preexisting valvular heart disease and pulmonary hypertension.
  • This evaluation helps determine if diethylpropion is safe for the patient's heart health.

Echocardiogram During Therapy:

  • Patients may need to undergo echocardiograms (heart ultrasound) periodically during diethylpropion therapy.
  • This helps monitor for any changes in heart function or the development of heart-related issues during treatment.

Monitoring Weight, Waist Circumference, and Blood Pressure:

  • Healthcare providers will regularly measure the patient's weight, waist circumference, and blood pressure during diethylpropion therapy.
  • This monitoring helps track the effectiveness of the medication in aiding weight loss and ensures that blood pressure remains within a safe range.

Renal Function in Elderly Patients:

  • Elderly patients may need special attention to their kidney function while taking diethylpropion.

How to administer Diethylpropion (Anorex)?

Immediate Release:

  • Take 1 hour before meals: It's best to take diethylpropion immediate-release tablets about 1 hour before meals.
  • Take 1 tablet midevening: If experiencing nighttime hunger, one tablet can also be taken in the middle of the evening to help manage hunger during the night.

Controlled Release:

  • Swallow whole: Diethylpropion controlled-release tablets should be swallowed whole without chewing, breaking, or crushing them.
  • Administer at midmorning: Take the controlled-release tablets in the midmorning, typically after breakfast, to provide extended appetite suppression throughout the day.

Mechanism of action of Diethylpropion (Anorex):

  • Diethylpropion is a type of medication that mimics the actions of certain chemicals in the body, similar to amphetamines.
  • Its structure is also similar to another medication called bupropion.
  • The main way it works to reduce appetite is by affecting the central nervous system (CNS), particularly by stimulating a part of the brain called the hypothalamus.
  • This stimulation leads to the release of a neurotransmitter called norepinephrine, which helps to decrease feelings of hunger.
  • In simpler terms, diethylpropion helps control appetite by influencing how the brain works.

Metabolism:

  • Diethylpropion is metabolized in the body to form active metabolites through processes called N-dealkylation and reduction.

Half-life elimination:

  • The half-life of the active metabolites, known as aminoketone metabolites, is approximately 4 to 6 hours.
  • This means that it takes this amount of time for half of the active metabolites to be eliminated from the body.

Excretion:

  • Diethylpropion and its metabolites are primarily excreted from the body through urine. They are eliminated from the body via the urinary system.

International Brand Names of Diethylpropion:

  • Anorex
  • Apisate
  • Atractil
  • Bonumin
  • Delgamer
  • Dietil Retard
  • Dietil-retard
  • Dipion
  • Dobesin
  • Linea
  • Lipomin
  • Moderatan
  • Nulobes
  • Prefamone
  • Prefamone Chronule
  • Prothin
  • Regenon
  • Regenon Retard
  • Tenuate
  • Tenuate Dospan

Diethylpropion Brand Names in Pakistan:

Not Available.