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DEA NFLIS-Drug Category -> Stimulants

Pharmaceuticals -> Listed in ZINC15

1 G DISSOLVES IN 20 ML WATER, ABOUT 150 ML ETHANOL (95%); PRACTICALLY INSOL IN CHLOROFORM /SULFATE DIHYDRATE/

FREELY SOL IN ALCOHOL; SOL IN ETHER; PRACTICALLY INSOL IN WATER

4.57e-01 g/L

< 25 °C

YELLOW CRYSTALS; MP: 155-156 °C /PICRATE/

< 25 °C

10.37

PKA: 10.38

Warning

H336 (100%): May cause drowsiness or dizziness [Warning Specific target organ toxicity, single exposure; Narcotic effects]

P261, P271, P304+P340, P319, P403+P233, P405, and P501 (click each P-code to see the statement)

The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

IN ANESTHETIZED DOGS, RESERPINE POTENTIATED THE PRESSOR RESPONSE WHEN ADMIN AFTER MEPHENTERMINE.

C - Cardiovascular system

QC - Cardiovascular system

Mephentermine is a sympathomimetic agent with mainly indirect effects on adrenergic receptors. It is used to maintain blood pressure in hypotensive states, for example, following spinal anesthesia. Although the central stimulant effects of mephentermine are much less than those of amphetamine, its use may lead to amphetamine-type dependence. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1248)

Mephentermine is an alpha adrenergic receptor agonist, but also acts indirectly by releasing endogenous norepinephrine. Cardiac output and systolic and diastolic pressures are usually increased. A change in heart rate is variable, depending on the degree of vagal tone. Sometimes the net vascular effect may be vasodilation. Large doses may depress the myocardium or produce central nervous system (CNS) effects.

Mephentermine is a sympathomimetic drug that acts both directly and indirectly; it has many similarities to ephedrine. After an intramuscular injection, the onset of action is prompt (within 5 to 15 minutes), and effects may last for several hours.

Since the drug releases norepinephrine, cardiac contraction is enhanced and cardiac output and systolic and diastolic pressures are usually increased. The change in heart rate is variable, depending on the degree of vagal tone.

17 to 18 hours.

17 to 18 hours

Hepatic, by N-demethylation and then p-hydroxylation.

MEPHENTERMINE IS METABOLIZED IN THE LIVER BY N-DEMETHYLATION & SUBSEQUENT P-HYDROXYLATION TO NORMEPHENTERMINE & P-HYDROXYNORMEPHENTERMINE. /SULFATE/

MEPHENTERMINE WAS METABOLIZED IN VITRO BY RABBIT LIVER MICROSOMES TO PHENTERMINE (II), N-HYDROXYMEPHENTERMINE (III), & N-HYDROXYPHENTERMINE. METABOLITES (II) & (III) PLUS UNCHANGED MEPHENTERMINE FOUND IN URINE OF HUMAN ADMIN SINGLE DOSE OF MEPHENTERMINE SULFATE.

Metabolites of mephentermine (MP), phentermine (Ph), p-hydroxy-MP, p-hydroxy-Ph, N-hydroxy-MP and N-hydroxy-Ph on incubation with rat liver microsomal and cytosolic preparations were identified by glc and glc mass spectrometry. Identification of the metabolites indicated the following new metabolic routes of MP: NADPH dependent microsomal formation of p-hydroxy-MP from MP, of p-hydroxy-Ph from p-hydroxy-MP, and the NADH-dependent microsomal formation of Ph from N-hydroxy-Ph.