Декстроамфетамин: Стимулятор ЦНС и его применение.

CNS stimulant and isomer of amphetamine

Dextroamphetamine (INN:dexamfetamine) is a potent central nervous system (CNS) stimulant and enantiomer|group = "note" |name="Enantiomer" levoamphetamine and dextroamphetamine. Dextroamphetamine is the dextrorotatory, or 'right handed', enantiomer and exhibits more pronounced effects on the central nervous system than levoamphetamine. Pharmaceutical dextroamphetamine sulfate is available as both a brand name and generic drug in a variety of dosage forms. Dextroamphetamine is sometimes prescribed as the inactive prodrug lisdexamfetamine dimesylate, which is converted into dextroamphetamine after absorption. Dextroamphetamine, like other amphetamines, elicits its stimulating effects via several distinct actions: it inhibits or reverses the transporter proteins for the monoamine neurotransmitters (namely the serotonin, norepinephrine and dopamine transporters) either via trace amine associated receptor 1 (TAAR1) or in a TAAR1 independent fashion when there are high cytosolic concentrations of the monoamine neurotransmitters In 2021, it was the 17th most commonly prescribed medication in the United States, with more than 30.3million prescriptions.

Dextroamphetamine is used to treat attention deficit hyperactivity disorder (ADHD) and narcolepsy (a sleep disorder), Large recreational doses of dextroamphetamine may produce symptoms of dextroamphetamine overdose. Immediate release formulations have higher potential for abuse via insufflation (snorting) or intravenous injection due to a more favorable pharmacokinetic profile and easy crushability (especially tablets). The reason for using crushed spansules for insufflation and injection methods is evidently due to the "instant release" forms of the drug seen in tablet preparations often containing a sizable amount of inactive binders and fillers alongside the active d amphetamine, such as dextrose. Injection into the bloodstream can be dangerous because insoluble fillers within the tablets can block small blood vessels. Amphetamine also interacts with MAOIs (monoamine oxidase inhibitors), particularly monoamine oxidase A inhibitors, since both MAOIs and amphetamine increase plasma catecholamines (i. e., norepinephrine and dopamine); The human serotonin transporter and norepinephrine transporter do not contain zinc binding sites.

Dextroamphetamine is the active metabolite of the prodrug lisdexamfetamine (L lysine dextroamphetamine), available by the brand name Vyvanse (Elvanse in the European market) (Venvanse in the Brazil market) (lisdexamfetamine dimesylate). Dextroamphetamine is liberated from lisdexamfetamine enzymatically following contact with red blood cells. The conversion is rate limited by the enzyme, which prevents high blood concentrations of dextroamphetamine and reduces lisdexamfetamine's drug liking and abuse potential at clinical doses. Vyvanse is marketed as once a day dosing as it provides a slow release of dextroamphetamine into the body. Vyvanse is available as capsules, and chewable tablets, and in seven strengths; 10 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg, and 70 mg. The conversion rate between lisdexamfetamine dimesylate (Vyvanse) to dextroamphetamine base is 29.5%.