Diethylpropion

Diethylpropion is a sympathomimetic amine belonging to an anorectic agent

Diethylpropion is used in the treatment of short-term Weight management.

Diethylpropion is rapidly absorbed from the GI tract after oral administration. It is extensively metabolized through a complex pathway of biotransformation involving N-dealkylation and reduction. Many of these metabolites are biologically active and may participate in the therapeutic action of diethylpropion. Diethylpropion is rapidly absorbed from the GI tract after oral administration and is extensively metabolized through a complex pathway of biotransformation involving N-dealkylation and reduction. Diethylpropion and/or its active metabolites are believed to cross the blood-brain barrier and the placenta. Diethylpropion and its metabolites are excreted mainly by the kidney.

The Tmax of Diethylpropion is approximately 1-4 hours.

Diethylpropion shows common side effects like Insomnia, Dizziness, Headache, Dry mouth, Nervousness, Restlessness, Diarrhea, Constipation, Increased heart rate, and High blood pressure.

Diethylpropion is available in the form of tablets.

Diethylpropion is available in India, Germany, Canada, Italy, USA

Diethylpropion is a sympathomimetic amine with pharmacologic properties similar to amphetamines. It is also structurally similar to bupropion. The mechanism of action in reducing appetite appears to be secondary to CNS effects, including stimulation of the hypothalamus to release norepinephrine.

Diethylpropion is available in the form of tablets.

Immediate release: Administer 1 hour before meals; may also administer 1 tablet midevening (to overcome night hunger).

Controlled release: Swallow whole; administer at midmorning.

Bariatric surgery: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. Do not cut, crush, or chew. Switch to IR tablet.

Diethylpropion is used in the treatment for short-term of Weight management.Diethylpropion is approved for use in the following clinical indications

Weight management, short-term: Short-term (few weeks) in the management of exogenous obesity. Therapy should be used in conjunction with a comprehensive weight management program.

Diethylpropion is an amphetamine that stimulates neurons to release or maintain high levels of a particular group of neurotransmitters known as catecholamines; these include dopamine and norepinephrine. High levels of these catecholamines tend to suppress hunger signals and appetite. Diethylpropion (through catecholamine elevation) may also indirectly affect leptin levels in the brain. It is theorized that diethylpropion can raise levels of leptin which signal satiety.

Diethylpropion is approved for use in the following clinical indications

Weight management, short-term: Short-term (few weeks) in the management of exogenous obesity. Therapy should be used in conjunction with a comprehensive weight management program.

Weight management, short-term (alternative agent):

Note: Avoid use due to side effects (eg, tachycardia, hypertension), the Diethylpropion is available in various strengths as 25 mg, 75 mg.potential for abuse, and availability of preferred weight-reducing drugs. Limit use to patients who cannot take preferred agents and who have a BMI ≥30 kg/m2 or patients with a BMI ≥27 kg/m2 and ≥1 weight-associated comorbidity (eg, dyslipidemia) and who do not have contraindications for use. Evaluate weight loss after 4 weeks; continue therapy only if satisfactory weight loss (eg, 4 pounds, or as clinically appropriate) has occurred.

Maximum duration: 12 weeks.

Immediate release: Oral: 25 mg 3 times daily 1 hour before meals; a fourth dose may be taken in the evening as needed for hunger.

Controlled release: Oral: 75 mg once daily in the midmorning.

Dosage Adjustment for Pediatric Patients:-

Adolescents >16 years: Refer to adult dosing.

Diethylpropion is available in various strengths as 25 mg, 75 mg.

Diethylpropion is available in the form of tablets

• CNS effects: Amphetamines may impair the ability to engage in potentially hazardous activities (eg, driving or operating machinery).

• Heart failure: In a scientific statement from the American Heart Association, diethylpropion has been determined to be an agent that may cause direct myocardial toxicity (magnitude: major)

• Primary pulmonary hypertension (PPH): A rare, frequently fatal disease of the lungs, PPH has been found to occur with increased frequency in patients receiving some anorexigens, including diethylpropion; use of anorexigens for >3 months has been associated with a 23-fold increase in risk of pulmonary hypertension. If the patient develops signs or symptoms of pulmonary hypertension (eg, exertional dyspnea, angina, syncope, lower extremity edema), discontinue use immediately and evaluate.

• Valvular heart disease: The use of some anorexigens, including diethylpropion, has been associated with the development of valvular heart disease. The risk may be increased with extended use, higher than recommended doses, or concomitant use with other anorexigens. Avoid stimulants in patients with known serious structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, or other serious cardiac problems that could increase the risk of sudden death that these conditions alone carry.

Pregnancy Category C

Common Adverse effects:

Dizziness, Headache, Dry mouth, Nervousness, Restlessness, Diarrhea, Constipation, Increased heart rate, High blood pressure, Palpitations, Tremors, Sweating, Dizziness

Less Common Adverse effects:

Mood changes, Hallucinations,Blurred vision,Difficulty urinating, Rash, Itching, Swelling, Difficulty breathing, Chest pain, Fainting, Seizures, Abdominal pain, Yellowing of the skin or eyes (jaundice)

Rare Common Adverse effects:

Allergic reactions such as anaphylaxis or angioedema, Psychotic reactions such as delusions or paranoia, Suicidal thoughts or behavior, The reported oral LD50 for mice is 600 mg/kg, for rats is 250 mg/kg and for dogs is 225 mg/kg. Manifestation of acute overdosage include restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, and panic states.Stroke, Heart attack, Pulmonary hypertension, Primary pulmonary hypertension, Cardiac valvulopathy, Neuroleptic malignant syndrome, Stevens-Johnson syndrome

The reported oral LD50 for mice is 600 mg/kg, for rats is 250 mg/kg and for dogs is 225 mg/kg. Manifestation of acute overdosage include restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, and panic states.

Diethylpropion is a sympathomimetic stimulant drug marketed as an appetite suppressant. Chemically, it is the N,N-diethyl analog of cathinone. Its mechanism of action is similar to other appetite suppressants such as sibutramine, phentermine and dextroamphetamine.

● https://clinicaltrials.gov/ct2/show/NCT04430790

● https://clinicaltrials.gov/ct2/show/NCT02820025

● https://pubmed.ncbi.nlm.nih.gov/27612991/

● https://clinicaltrials.gov/ct2/show/NCT03894189

● https://www.rxlist.com/dopram-drug.htm

● https://www.mims.com/india/drug/info/Diethylpropion?type=full&mtype=generic

● https://go.drugbank.com/drugs/DB00561

● https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7003846/