Table 4.
Other Drugs Commonly Used as Hypnotics1
| Class/Drug | T Max (hours) | Half Life (hours) |
Mechanism2 | Usual Hypnotic Dose (mg) |
FDA Approved Indication |
Comments, Side Effects |
|---|---|---|---|---|---|---|
| Melatonin agonist drugs | ||||||
| Melatonin | 0.3 – 1 | 0.6 – 1 | MT1, MT2 agonist | 0.5 – 3 | No FDA approval | FDA defined as a dietary supplement |
| Ramelteon | 0.75 (0.5 – 1.5) | 1 – 2.6 | MT1, MT2 agonist | 8 | Insomnia | Main effect on sleep latency |
| Sedating antidepressant drugs | ||||||
| Doxepin | 3.5 (1.5 – 4) | 15 (10 – 30) | Low dose: H1 antagonist Higher doses: 5HT2, α1, M1, antagonist; NE, 5HT reuptake inhibitor |
3 – 6 (Silenor®) 10 – 100 (generic) |
Insomnia Depression Anxiety |
3-6 mg dose approved for insomnia; Side effects at higher doses: orthostatic hypotension, anticholinergic, cardiac conduction delay |
| Amitriptyline | 2 – 5 | 30 (5 – 45) | 5HT2, α1, M1 antagonist; NE, 5HT reuptake inhibitor |
10 – 100 | Depression | Side effects at higher doses: orthostatic hypotension, anticholinergic, cardiac conduction delay |
| Trazodone | 1 – 2 | 9 (7 – 15) | 5HT2, α1, H1 antagonist; 5HT reuptake inhibitor |
25 – 150 | Depression | Side effects: dizziness, risk of priapism |
| Mirtazapine | 2 (1 – 3) | 30 (20 – 40) | 5HT2-3, α1-2, H1, M1 antagonist; 5HT reuptake inhibitor |
7.5 – 30 | Depression | Increased appetite, weight gain, anticholinergic |
| Sedating antipsychotic drugs | ||||||
| Olanzapine | 4 – 6 | 20 – 54 | 5HT2, D1-4, α1, H1, M1-5 antagonist |
2.5 – 20 | Schizophrenia Bipolar Disorder |
Hypotension weight gain, akathisia, dizziness |
| Quetiapine | 1 – 2 | 6 | 5HT1-2, D1-2, α1-2, H1 antagonist |
25 – 50 | Schizophrenia Bipolar Disorder |
Dry mouth, constipation, weight gain, asthenia, headache |
| Antihistamine drugs | ||||||
| Diphenhydramine | 1 – 4 | 4 – 8 | H1, M1 antagonist | 25 – 50 | Allergic reactions, motion sickness, Parkinsonism |
Anticholinergic |
| Doxylamine | 2 – 3 | 10 | H1, M1 antagonist | 25 mg | Allergies, hypersensitivity, insomnia |
Anticholinergic; Dystonic reaction |
| Anticonvulsant drugs | ||||||
| Gabapentin | 1.6 – 3 | 5 – 9 | Uncertain. GABA analog, but does not have activity at GABA receptors. Possible alpha2- delta receptor ligand |
100 – 900 | Post herpetic neuralgia; epilepsy |
Renal excretion, non-linear pharmacokinetics (reduced bioavailability at higher doses); izziness, ataxia, fatigue |
| Pregabalin | 1.5 | 6.3 | alpha2-delta receptor ligand. GABA analog, but does not have activity at GABA receptors. |
50 – 300 | Diabetic peripheral neuropathy; Post herpetic neuralgia; Adjunct for partial seizures; Fibromyalgia |
Renal excretion; dizziness, headache, weight gain, dry mouth |
1
Sources: FDA-approved prescribing information and sources57;58. Published pharmacokinetic data are not consistently reported for all drugs.
2
MT = Melatonin receptor; H = Histamine receptor; 5HT = Serotonin; M = Muscarinic cholinergic receptor; α = alpha adrenergic receptor; D = Dopamine receptor; GABA = Gamma-aminobutyric acid