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Demerol Injection (Meperidine Hydrochloride) - Description and Clinical Pharmacology

 
 



DEMEROL®
Meperidine Hydrochloride, USP

CII

WARNING: May be habit forming

Rx only

DESCRIPTION

Meperidine hydrochloride is ethyl 1-methyl-4-phenylisonipecotate hydrochloride, a white crystalline substance with a melting point of 186°C to 189°C. It is readily soluble in water and has a neutral reaction and a slightly bitter taste. The solution is not decomposed by a short period of boiling.

Demerol injectable is supplied in Carpuject ®, CARPUJECT with InterLink®, CARPUJECT with Luer Lock and CARPUJECT with blunt cannula of 2.5% (25 mg/1 mL), 5% (50 mg/1 mL), 7.5% (75 mg/1 mL), and 10% (100 mg/1 mL). Uni-Amp® unit dose pak-ampuls of 5% solution (25 mg/0.5 mL), (50 mg/1 mL), (75 mg/1.5 mL), (100 mg/2 mL), and 10% solution (100 mg/1 mL). Multiple-dose vials of 5% and 10% solutions contain metacresol 0.1% as preservative.

The pH of Demerol solutions is adjusted between 3.5 and 6 with sodium hydroxide or hydrochloric acid.

Demerol, brand of meperidine hydrochloride, 5 percent solution has a specific gravity of 1.0086 at 20°C and 10 percent solution, a specific gravity of 1.0165 at 20°C.

CLINICAL PHARMACOLOGY

Meperidine hydrochloride is a narcotic analgesic with multiple actions qualitatively similar to those of morphine; the most prominent of these involve the central nervous system and organs composed of smooth muscle. The principal actions of therapeutic value are analgesia and sedation.

There is some evidence which suggests that meperidine may produce less smooth muscle spasm, constipation, and depression of the cough reflex than equianalgesic doses of morphine. Meperidine, in 60 mg to 80 mg parenteral doses, is approximately equivalent in analgesic effect to 10 mg of morphine. The onset of action is slightly more rapid than with morphine, and the duration of action is slightly shorter. Meperidine is significantly less effective by the oral than by the parenteral route, but the exact ratio of oral to parenteral effectiveness is unknown.

In clinical studies reported in the literature, changes in several pharmacokinetic parameters with increasing age have been observed. The initial volume of distribution and steady-state volume of distribution may be higher in elderly patients than in younger patients. The free fraction of meperidine in plasma may be higher in patients over 45 years of age than in younger patients.

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