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Benzebar

Benzebar - General Information

Benzebar is a chiral compound. The racemic mixture can be divided into its optical antipodes: levo- and dextro-amphetamine. Benzebar is the parent compound of its own structural class, comprising a broad range of psychoactive derivatives, e.g., MDMA (Ecstasy) and the N-methylated form, methamphetamine. Benzebar is a homologue of phenethylamine.

 

Pharmacology of Benzebar

Benzebar and dextroamphetamine, non-catechloamine sypathomimetic agents, are used in combination to treat attention-deficit hyperactivity disorder (ADHD) or narcolepsy. Adderall consists of equivalent amounts of amphetamine aspartate, amphetamine sulfate, dextroamphetamine saccharate, and dextroamphetamine sulfate.

 

Benzebar for patients

Amphetamines may impair the ability of the patient to engage in potentially hazardous activities such as operating machinery or vehicles; the patient should therefore be cautioned accordingly.

 

Benzebar Interactions

Acidifying agents - Gastrointestinal acidifying agents (guanethidine,reserpine, glutamic acid HCl,ascorbic acid, fruit juices, etc.) lower absorption of amphetamines.
Urinary acidifying agents -(ammonium chloride, sodium acid phosphate, etc.) Increase the concentration of the ionized species of the amphetamine.
Primary excretion - Both Groups of agents lower blood levels and efficacy of amphetamines.
Adrenergic blockers - Adrenergic blockers are inhibited by amphetamines.
Alkalinizing agents -Gastrointestinal alkalinizing agents (sodium bicarbonate, etc.)increase absorption of amphetamines. Urinary alkalinizing agents (acetazolamide, some thiazides) increase the concentration of the non-ionized species of the amphetamine molecule, thereby decreasing urinary excretion. Both groups of agents increase blood levels and therefore potentate the actions of amphetamines.
Antidepressants, tricyclic - Amphetamines may enhance the activity of tricyclic or sympathomimetic agents; d-amphetamine with desipramine or protriptyline and possibly other tricyclics cause striking and sustained increases in the concentration of d-amphetamine in the brain; cardiovascular effects can be potentiated.
MAO inhibitors - MAO antidepressants, as well as a metabolite of furazolidone, slow amphetamine metabolism. This slowing potentiates amphetamines, increasing their effect on the release of norepinephrine and other monoamines from adrenergic nerve endings, this can cause headaches and other signs of hypertensive crisis. A variety of neurological toxic effects and malignant hyperpyrexia can occur, sometimes with fatal results.
Antihistamines - Amphetamines may counteract the sedative effect of antihistamines.
Antihypertensives - Amphetamines may antagonize the hypotensive effects of antihypertensives.
Chlorpromazine - Chlorpromazine blocks dopamine and norepinephrine receptors, thus inhibiting the central stimulant effects of amphetamines, and can be used to treat amphetamine poisoning.
Ethosuximide - Amphetamines may delay intestinal absorption of ethosuximide.
Haloperidol - Haloperidol blocks dopamine receptors, thus inhibiting the central stimulant effects of amphetamines.
Lithium carbonate - The anorectic and stimulatory effects of amphetamines may be inhibited by lithium carbonate.
Meperidine - Amphetamines pone the analgesic effect of meperidine.
Methenamine therapy - Urinary excretion of amphetamines is increased, and efficacy is reduced, by acidifying agents used in methenamine therapy.
Norepinephrine - Amphetamines enhance the adrenergic effect of norepinephrine.
Phenobarbital - Amphetamines may delay intestinal absorption of phenobarbital; co-administration of phenobarbital may produce a synergistic anticonvulsant action.
Phenytoin - Amphetamines may delay intestinal absorption of phenytoin; co-administration of phenytoin may produce a synergistic anticonvulsant action.
Propoxyphene - In cases of propoxyphene overdose, amphetamine CNS stimulation is potentiated and fatal convulsions can occur.
Veratrum alkaloids - Amphetamines inhibit the hypotensive effect of veratrum alkaloids.
Drug/Laboratory Test Interactions
Amphetamines can cause a significant elevation in plasma corticosteroid levels. This increase is greatest in the evening.
Amphetamines may interfere with urinary steroid determinations.

 

Benzebar Contraindications

Advanced arteriosclerosis, symptomatic cardiovascular disease, moderate to severe hypertension, hyperthyroidism, known hypersensitivity or idiosyncrasy to the sympathomimetic amines, glaucoma. Agitated states. Patients with a history of drug abuse. During or within 14 days following the administration of monoamine oxidase inhibitors (hypertensive crises may result).

 

Additional information about Benzebar

Benzebar Indication: For treatment of Attention Deficit Disorder with Hyperactivity (ADDH) and narcolepsy in children.
Mechanism Of Action: Benzebars stimulate the release of norepinephrine from central adrenergic receptors. At higher dosages, they cause release of dopamine from the mesocorticolimbic system and the nigrostriatal dopamine systems. Benzebar may also act as a direct agonist on central 5-HT receptors and may inhibit monoamine oxidase (MAO). In the periphery, amphetamines are believed to cause the release of noradrenaline by acting on the adrenergic nerve terminals and alpha- and beta-receptors. Modulation of serotonergic pathways may contribute to the calming affect.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Amphetamine
Synonyms: (+/-)-beta-Phenylisopropylamine; (+/-)-Benzedrine; (+/-)-Desoxynorephedrine; 1-Methyl-2-phenylethylamine; 1-Phenyl-2-aminopropane; 3-Methoxy-a-methylbenzeneethanamine; 3-Methoxyamphetamine; 3-Methoxyphenylisopropylamine; alpha-Methylbenzeneethaneamine; Amphetamine Sulfate; beta-Aminopropylbenzene; dl-1-Phenyl-2-aminopropane; DL-alpha-Methylphenethylamine; dl-Amphetamine; dl-Benzedrine; Fenylo-izopropylaminyl; m-Methoxy-a-methylphenethylamine; m-Methoxyamphetamine; Methamphetamine HCL; [1-(3-Methoxyphenyl)-2-propyl]amine; Phenylisopropylamine; Amfetamine; beta-phenyl-isopropylamine
Drug Category: Adrenergic Agents; Dopamine Agents; Dopamine Uptake Inhibitors; Adrenergic Uptake Inhibitors; Central Nervous System Stimulants; Amphetamines; Sympathomimetics
Drug Type: Small Molecule; Illicit; Approved
Other Brand Names containing Amphetamine: Actedron; Adipan; Allodene; Anorexide; Anorexine; Benzebar; Benzedrine; Benzolone; Desoxyn; Dexampex; Dexedrine; Dextrostat; Elastonon; Fenamin; Ferndex; Finam; Isoamycin; Isoamyne; Isomyn; Mecodrin; Methampex; Norephedrane; Novydrine; Oktedrin; Ortedrine; Paredrine; Percomon; Phenamine; Phenedrine; Profamina; Propisamine; Psychedrine; Raphetamine; Rhinalator; Simpatedrin; Simpatina; Sympamin; Sympamine; Sympatedrine; Weckamine;
Absorption: Amphetamine forms easily absorbed molecules that are highly lipid soluble
Toxicity (Overdose): LD50=180 mg/kg(subcutaneous injection in rat). The most common presenting symptoms seen are agitation, hallucinations, suicidal behaviour, and chest pain.
Protein Binding: 15-40%
Biotransformation: Hepatic
Half Life: 10 hours
Dosage Forms of Benzebar: Tablet Oral
Capsule, extended release Oral
Chemical IUPAC Name: (2S)-1-phenylpropan-2-amine
Chemical Formula: C9H13N
Amphetamine on Wikipedia: http://en.wikipedia.org/wiki/Amphetamine
Organisms Affected: Humans and other mammals