Doxylamine succinate vs diphenhydramine

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Comparison of Doxylamine Succinate and Diphenhydramine

Pharmacokinetics of Doxylamine Succinate vs. Diphenhydramine

Peak Plasma Concentration and Time to Peak

Doxylamine succinate and diphenhydramine hydrochloride exhibit different pharmacokinetic profiles. In a study involving women on low-dose estrogen oral contraceptives, the peak plasma concentration for doxylamine was found to be approximately 100 ng/ml, with a time to peak of around 2 hours. In contrast, diphenhydramine had a lower peak plasma concentration of about 73.8 ng/ml and a slightly longer time to peak of 2.2 hours .

Elimination Half-Life and Clearance

The elimination half-life of doxylamine succinate was observed to be around 10 hours, whereas diphenhydramine had a shorter half-life of approximately 5.1 hours. Additionally, the total clearance rates were 3.88 ml/min/kg for doxylamine and 25.5 ml/min/kg for diphenhydramine, indicating a faster clearance for diphenhydramine .

Analytical Methods for Determination

High Performance Thin Layer Chromatography (HPTLC)

A quantitative method using HPTLC has been developed to determine the presence of diphenhydramine hydrochloride and doxylamine succinate in pharmaceutical products. This method involves automated sample application and UV-absorption scanning densitometry, providing precise and accurate measurements. The precision of this method ranged from 0.69% to 2.36% relative standard deviation, and the accuracy was validated through standard addition experiments .

Adverse Reactions

Contact Dermatitis

Diphenhydramine hydrochloride has been reported to cause contact dermatitis in some individuals. Patients who develop this condition should avoid both oral and parenteral administration of diphenhydramine, as it may lead to localized or generalized dermatitis flares. Other ethanolamine antihistamines, including doxylamine succinate, may cross-react with diphenhydramine and should also be avoided in sensitive patients .

Conclusion

In summary, while both doxylamine succinate and diphenhydramine hydrochloride are effective antihistamines, they differ in their pharmacokinetic profiles, with doxylamine having a longer half-life and slower clearance. Analytical methods like HPTLC are effective for determining their presence in pharmaceutical products. However, caution should be exercised with diphenhydramine due to the potential for contact dermatitis and cross-reactivity with other ethanolamine antihistamines.

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Most relevant research papers on this topic

Doxylamine and Diphenhydramine Pharmacokinetics in Women on Low‐Dose Estrogen Oral Contraceptives

Low-dose estrogen-containing oral contraceptives do not significantly influence the pharmacokinetics of antihistamines doxylamine and diphenhydramine in women.

RCT

1989·

24citations

·B. Luna et al.

DETERMINATION OF THE SLEEP AID INGREDIENTS DIPHENHYDRAMINE HYDROCHLORIDE AND DOXYLAMINE SUCCINATE IN PHARMACEUTICAL PRODUCTS BY QUANTITATIVE HPTLC

The developed HPTLC method effectively determines diphenhydramine hydrochloride and doxylamine succinate in pharmaceutical sleep aid products, with high precision and accuracy.

1999·

11citations

·D. Digregorio et al.

Contact dermatitis caused by diphenhydramine hydrochloride.

Patients with contact dermatitis should avoid diphenhydramine hydrochloride and other ethanolamine antihistamines, as they may cross-react and cause flare-ups.

Case Report

1983·

8citations

·R. Coskey

Pharmacokinetic Dose Proportionality Between Two Strengths (12.5 mg and 25 mg) of Doxylamine Hydrogen Succinate Film-Coated Tablets in Fasting State: A Single-Dose, Randomized, Two-Period Crossover Study in Healthy Volunteers

Doxylamine hydrogen succinate 12.5 mg and 25 mg tablets show dose proportionality similar to each other in healthy volunteers, with 25 mg showing higher sedative effects.

RCT

2013·

12citations

·S. Videla et al.

Over-the-counter medications containing diphenhydramine and doxylamine used by older adults to improve sleep

Most older adults in a limited sample in the United States are taking over-the-counter sleep medications containing diphenhydramine or doxylamine, which are potentially inappropriate for them.

Observational Study

2017·

33citations

·Olufunmilola Abraham et al.

Chiral separation of (d)- and (l)-enantiomers of doxylamine succinate in rat plasma

The developed chiral ultra fast liquid chromatography method effectively separates and quantifies (d)- and (l)-enantiomers of doxylamine succinate in rat plasma, aiding in pharmacokinetics determination.

2015·

3citations

·T. Sirisha et al.

Over-the-Counter Agents for the Treatment of Occasional Disturbed Sleep or Transient Insomnia: A Systematic Review of Efficacy and Safety.

Common over-the-counter sleep-aid agents, especially diphenhydramine and valerian, lack robust clinical evidence supporting efficacy and safety for occasional disturbed sleep or transient insomnia.

Systematic Review

2015·

39citations

·L. Culpepper et al.

The hypnotic efficacy of doxylamine

Doxylamine succinate is an effective nighttime hypnotic drug, generally better than secobarbital sodium, with mild side effects, except for a more frequent "hangover" after doxylamine and secobarbital.

RCT

1967·

31citations

·F. Sjöqvist et al.

Suicide through doxylamine poisoning.

Doxylamine poisoning, a common sleep-inducing agent, can cause fatalities when combined with other drugs, such as diphenhydramine, in the Federal Republic of Germany.

Case Report

2001·

21citations

·Britta Bockholdt et al.

A Phase I Study of the Pharmacokinetics and Pharmacodynamics of Intranasal Doxylamine in Subjects with Chronic Intermittent Sleep Impairment

Intranasal doxylamine did not increase absorption or systemic bioavailability compared to the oral tablet, and common adverse events were nasal congestion, dryness, and frontal headache.

RCTRigorous Journal

2018·

11citations

·M. Allison et al.

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