Benzphetamine

Concurrent use /of other CNS stimulation-producing medications or thyroid hormones with appetite suppressants / may increase the CNS stimulant effects of either these medications or the appetite suppressant. /Appetite suppressants, sympathomimetic/

The sympathomimetic effects of appetite suppressants /when used with monoamine oxidase (MAO) inhibitors, including furazolidone, procarbazine, and selegiline/ may be potentiated, possibly resulting in a hypertensive crisis; concurrent use is contraindicated; appetite suppressant should not be administered during or within 14 days following the administration of and MAO inhibitor. /Appetite suppressants, sympathomimetic/

Vasopressant effect may be potentiated; if necessary to administer a pressor amine agent to a patient who has recently received an appetite suppressant, initiating pressor therapy in reduced dosage and monitoring blood pressure at frequent intervals are recommended. /Appetite suppressants, sympathomimetic/

Anorectic effects of the appetite suppressant may be antagonized /when used with phenothiazines/. /Appetite suppressants, sympathomimetic/

For more Interactions (Complete) data for BENZPHETAMINE (10 total), please visit the HSDB record page.

Using large amounts of these drugs can result in a condition known as amphetamine psychosis -- which can result in auditory, visual and tactile hallucinations, intense paranoia, irrational thoughts and beliefs, delusions, and mental confusion.

TERRESTRIAL FATE: Based on a classification scheme(1), an estimated Koc value of 8.0X10+4(SRC), determined from a structure estimation method(2), indicates that benzphetamine is expected to be immobile in soil(SRC). The estimated pKa of benzphetamine is 8.8(3), indicating that this compound will primarily exist in the cation form in the environment and cations generally adsorb more strongly to organic carbon and clay than their neutral counterparts(4). Volatilization of benzphetamine from moist soil surfaces is not expected to be an important environmental fate process(SRC) given an estimated Henry's Law constant of 4.2X10-7 atm-cu m/mole(SRC), using a fragment constant estimation method(5). Benzphetamine is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 1.0X10-4 mm Hg(SRC), determined from a fragment constant method(6). Biodegradation data were not available(SRC, 2005).

AQUATIC FATE: Based on a classification scheme(1), an estimated Koc value of 8.0X10+4(SRC), determined from a structure estimation method(2), indicates that benzphetamine is expected to adsorb to suspended solids and sediment(SRC). Volatilization from water surfaces is expected(3) based upon an estimated Henry's Law constant of 4.2X10-7 atm-cu m/mole(SRC), developed using a fragment constant estimation method(4). However, the estimated pKa of benzphetamine is 8.8(5), indicating that this compound will primarily exist in the cation form at pH values of 5 to 9 and therefore volatilization from water surfaces is not expected to be an important fate process(6). According to a classification scheme(7), an estimated BCF of 300(SRC), from an estimated log Kow of 3.0(8) and a regression-derived equation(9), suggests the potential for bioconcentration in aquatic organisms is high, provided the compound is not metabolized by the organism(SRC). Biodegradation data were not available(SRC, 2005).

ATMOSPHERIC FATE: According to a model of gas/particle partitioning of semivolatile organic compounds in the atmosphere(1), benzphetamine, which has an estimated vapor pressure of 1.0X10-4 mm Hg at 25 °C(SRC), determined from a fragment constant method(2), is expected to exist in both the vapor and particulate phases in the ambient atmosphere. Vapor-phase benzphetamine is degraded in the atmosphere by reaction with photochemically-produced hydroxyl radicals(SRC); the half-life for this reaction in air is estimated to be 3.5 hours(SRC), calculated from its rate constant of 1.1X10-14 cu cm/molecule-sec at 25 °C(SRC) that was derived using a structure estimation method(3). Particulate-phase benzphetamine will be removed from the atmosphere by wet and dry deposition. Benzphetamine does not contain chromophores that absorb at wavelengths >290 nm and therefore is not expected to be susceptible to direct photolysis by sunlight(SRC).

IDENTIFICATION: Benzphetamine is a centrally acting antiobesity agent. Benzphetamine is a clear liquid which is insoluble in water. Soluble in ethanol, methanol, chloroform, acetone, ether or benzene. Benzphetamine hydrochloride is a solid crystalline material. HUMAN EXPOSURE: Main risks and target organs: Acute central nervous system stimulation, cardiotoxicity causing tachycardia, arrhythmias, hypertension and cardiovascular collapse. High risk of dependency and abuse. Cardiovascular: Palpitation, chest pain, tachycardia, arrhythmias and hypertension are common; cardiovascular collapse can occur in severe poisoning. Myocardial ischemia, infarction and ventricular dysfunction are described. Central Nervous System (CNS): Stimulation of CNS, tremor, restlessness, agitation, insomnia, increased motor activity, headache, convulsions, coma and hyperreflexia are described. Stroke and cerebral vasculitis have been observed. Gastrointestinal: Vomiting, diarrhea and cramps may occur. Acute transient ischemic colitis has occurred with chronic methamphetamine abuse. Genitourinary: Increased bladder sphincter tone may cause dysuria, hesitancy and acute urinary retention. Renal failure can occur secondary to dehydration or rhabdomyolysis. Renal ischemia may be noted. Dermatologic: Skin is usually pale and diaphoretic, but mucous membranes appear dry. Endocrine: Transient hyperthyroxinemia may be noted. Metabolism: Increased metabolic and muscular activity may result in hyperventilation and hyperthermia. Weight loss is common with chronic use. Fluid/Electrolyte: Hypo- and hyperkalemia have been reported. Dehydration is common. Musculoskeletal: Fasciculations and rigidity may be noted. Rhabdomyolysis is an important consequence of severe amphetamine poisoning. Psychiatric: Agitation, confusion, mood elevation, increased wakefulness, talkativeness, irritability and panic attacks are typical. Chronic abuse can cause delusions and paranoia. A withdrawal syndrome occurs

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 (such as benzphetamine) 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. This release is mediated by the binding of benzphetamine to centrally located adrenergic receptors.

Using a structure estimation method based on molecular connectivity indices(1), the Koc of benzphetamine can be estimated to be 8.0X10+4(SRC). According to a classification scheme(2), this estimated Koc value suggests that benzphetamine is expected to be immobile in soil. The estimated pKa of benzphetamine is 8.8(3), indicating that this compound will primarily exist in the cation form in the environment and cations generally adsorb more strongly to organic carbon and clay than their neutral counterparts(4).

/SIGNS AND SYMPTOMS/ Acute overdosage with amphetamines may result in restlessness, tremor, tachypnea, confusion, assaultiveness and panic states. Fatigue and depression usually follow the central stimulation. Cardiovascular effects include arrhythmias, hypertension or hypotension, and circulatory collapse. Gastrointestinal symptoms include nausea, vomiting, diarrhea, and abdominal cramps. Hyperpyrexia and rhabdomyolysis have been reported and can lead to a number of associated complications. Fatal poisoning is usually preceded by convulsions and coma.

/SIGNS AND SYMPTOMS/ Manifestation of chronic intoxication with anorectic drugs include severe dermatoses, marked insomnia, irritability, hyperactivity and personality changes. The most severe manifestation of chronic intoxication is psychosis, often clinically indistinguishable from schizophrenia. /Benzphetamine hydrochloride/

/SIGNS AND SYMPTOMS/ Palpitation, tachycardia, and increased blood pressure may occur in patients receiving benzphetamine. Pulmonary hypertension and cardiomyopathy, usually manifested as ventricular hypertrophy and/or congestive heart failure, have occurred in patients receiving amphetamines chronically (e.g., chronic abusers) and is potentially fatal; the cardiomyopathy is similar to adrenergic cardiomyopathies (e.g., that associated with pheochromocytoma).

0M3S43XK27

BENZPHETAMINE

Physiologic Effects [PE] - Appetite Suppression

Physiologic Effects [PE] - Increased Sympathetic Activity

Established Pharmacologic Class [EPC] - Sympathomimetic Amine Anorectic

Benzphetamine is a Sympathomimetic Amine Anorectic. The physiologic effect of benzphetamine is by means of Appetite Suppression and Increased Sympathetic Activity.

A loosely defined group of drugs that tend to increase behavioral alertness, agitation, or excitation. They work by a variety of mechanisms, but usually not by direct excitation of neurons. The many drugs that have such actions as side effects to their main therapeutic use are not included here.

Drugs that mimic the effects of stimulating postganglionic adrenergic sympathetic nerves. Included here are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters.

Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.

Drugs that act on adrenergic receptors or affect the life cycle of adrenergic transmitters. Included here are adrenergic agonists and antagonists and agents that affect the synthesis, storage, uptake, metabolism, or release of adrenergic transmitters.

Drugs that block the transport of adrenergic transmitters into axon terminals or into storage vesicles within terminals. The tricyclic antidepressants (ANTIDEPRESSIVE AGENTS, TRICYCLIC) and amphetamines are among the therapeutically important drugs that may act via inhibition of adrenergic transport. Many of these drugs also block transport of serotonin.

Drugs that block the transport of DOPAMINE into axon terminals or into storage vesicles within terminals. Most of the ADRENERGIC UPTAKE INHIBITORS also inhibit dopamine uptake.

Readily absorbed from the gastro-intestinal tract and buccal mucosa. It Is resistant to metabolism by monoamine oxidase.

... Benzphetamine /is/ distributed into breast milk. ...

Benzphetamine is readily absorbed from the gastrointestinal tract.

Benzphetamine is readily absorbed from the GI tract and effects persist for about 4 hours after oral administration.