TENUATE DOSPAN

Indications

• Obesity
• Weight management in conjunction with diet and exercise

Dosage

Children: Diethylpropion is not recommended for use in children and adolescents under the age of 16 years.

Adults: The usual dose for adults is 25 mg taken three times a day, one hour before meals. The dose may be increased to a maximum of 75 mg per day if needed.

Mechanism of action

Diethylpropion stimulates neurons to release or maintain high levels of catecholamines, including dopamine and norepinephrine. This elevation of catecholamines suppresses hunger signals and appetite. It is theorized that diethylpropion can also raise leptin levels in the brain, signaling satiety. Additionally, increased catecholamines may inhibit neuropeptide Y, which promotes eating and fat storage. Overall, it functions similarly to amphetamines by acting on the lateral hypothalamic feeding center to decrease appetite.

Pharmacodynamics

Diethylpropion is classified as a sympathomimetic stimulant and is marketed as an appetite suppressant. Its pharmacological profile shares similarities with other appetite suppressants, such as sibutramine and phentermine. It is the N,N-diethyl analog of cathinone and primarily acts by stimulating the release of norepinephrine and dopamine in the central nervous system, leading to reduced appetite and potentially increased energy expenditure.

Pharmacokinetics

Diethylpropion is absorbed rapidly following oral administration, with its absorption not significantly affected by food. Peak plasma concentrations occur within 2 to 3 hours. It is metabolized in the liver, primarily through N-deethylation and subsequent conjugation, resulting in active metabolites. The elimination half-life is approximately 3 to 6 hours, with renal excretion playing a significant role in the clearance of the drug and its metabolites.

Adverse effects

• Insomnia
• Dry mouth
• Increased heart rate
• Nausea
• Constipation
• Anxiety
• Dizziness
• Hypertension

Interactions

• Monoamine oxidase inhibitors (MAOIs) may increase the risk of hypertensive crisis
• Other sympathomimetic agents may enhance adverse cardiovascular effects
• CNS stimulants may increase the risk of side effects

Precautions

• Use with caution in patients with a history of cardiovascular disease
• Monitor for potential abuse and dependence
• Consider potential psychiatric effects, especially in patients with a history of mental illness

Pregnancy

There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether diethylpropion is excreted in human milk. Caution is advised when administering to nursing women.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Oral tablets

Mechanism of action

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. It is also theorized that increased levels of the catecholamines are partially responsible for halting another chemical messenger known as neuropeptide Y. This peptide initiates eating, decreases energy expenditure, and increases fat storage. Although the mechanism of action of the sympathomimetic appetite suppressants in the treatment of obesity is not fully known, these medications have pharmacological effects similar to those of amphetamines. Amphetamine and related sympathomimetic medications ... are thought to stimulate the release of norepinephrine and/or dopamine from storage sites in nerve terminals in the lateral hypothalamic feeding center, thereby producing a decrease in appetite. ... It has not been established that the actions of these medications in treating obesity is primarily suppression of appetite; other CNS actions and/or metabolic effects, such as decreased gastric acid secretion or increased energy expenditure, may be involved.

Pharmacodynamics

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.