Table 1.
Current Over-the-Counter Treatment Approaches for Occasional Disturbed Sleepa
| Drug (chemical name), Dose | Mechanism of Action (if known) | Example Branded Products (manufacturer) | Overview of Pharmacokinetic Properties | Adverse Reactions (most frequent) | Drug-Drug Interactionsb |
| Diphenhydramine HCl (2-[diphenylmethoxy]-N, N-dimethylethylamine hydrochloride), 25 mg or 50 mg taken at bedtime | First-generation H1 antagonist with nonspecific anticholinergic and sedative effects | ZzzQuil Nighttime Sleep-Aid LiquiCaps (P&G) Unisom SleepMelts (Chattem Inc) Simply Sleep (McNeil PPC Inc) Nytol (GlaxoSmithKline) |
tmax: 1–4 h Half-life: 2.4–9.3 h Half-life and clearance are age-related14 |
Sedation, sleepiness, dizziness, disturbed coordination, epigastric distress, thickening of bronchial secretions | Metabolized primarily by CYP2D615 28 major drug interactions, including acetaminophen |
| Doxylamine succinate, 25 mg 30 min before bedtime | First-generation H1 antagonist with nonspecific anticholinergic and sedative effects | Unisom SleepTabs (Chattem Inc) Medi-Sleep Sleep Aid (Various) Aldex AN (Pernix LLC) |
tmax: ∼2.4 h (25 mg) Half-life: 10–15 h Clearance reduced in elderly men16–18 |
Dizziness; drowsiness; dry mouth, throat, and nose; thickening of mucus in nose or throat | 31 major drug interactions, including acetaminophen, aspirin |
| Melatonin (N-acetyl-5-methoxy-tryptamine), 5 mg 3–4 h prior to bedtime | Melatonin receptor agonist | Nature Made Melatonin | tmax: 30–60 min (2 mg) Half-life: 0.54–0.67 h19 |
Depression, dizziness, enuresis, excessive daytime somnolence, headache, nausea | Metabolized primarily by CYP1A220 7 moderate drug interactions |
| Valerian (Valeriana officinalis L), 400–600 mg valerian extract 1–2 h before bedtime | Not fully understood; proposed central actions on GABA, serotonin, and adenosine receptors | Nature’s Way Valerian Root GNC Herbal Plus Standardized Valerian Root |
tmax: 1–2 h (600 mg) Half-life: 1.1 h21 |
Headache, upset stomach, thinking problems, dry mouth, feeling excited or uneasy, strange dreams, daytime drowsiness | 3 major drug interactions, including sodium oxybate and buprenorphine |
a
Information obtained from http://www.drugs.com/pro/12 unless otherwise referenced. Information is intended as a summary; health care providers should consult detailed, up-to-date product information.
b
According to http://www.drugs.com, major interaction is defined as highly clinically significant, avoid combinations, the risk of the interaction outweighs the benefit. Moderate interaction is defined as moderately clinically significant, usually avoid combinations, use only under special circumstances.
Abbreviations: CYP = cytochrome P450, GABA = γ-aminobutyric acid, tmax = time of maximal (peak) plasma concentration.