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Greater caution is recommended with this drug due to it being a deliriant.
These combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.
Ethanolamine-class antihistamines are thought to have relatively low abuse liability due to their dysphoric and unpleasant side-effect profile. While recreational use as a deliriant does occur, the experience is typically not reinforcing.
Considerable overdosage can lead to myocardial infarction, serious ventricular arrhythmias, coma, and death. In children, overdose may lead to hallucinations, convulsions, or death. Adults experiencing overdose may present with drowsiness, convulsions, coma, or respiratory depression.
| Species | Route | Value |
|---|---|---|
| mouse | oral | 203 mg/kg |
| rat | oral | 1320 mg/kg |
| mouse | intraperitoneal | 149 mg/kg |
Considerable overdosage can cause serious cardiovascular complications including myocardial infarction and ventricular arrhythmias; tachycardia occurs during intoxication as an expected anticholinergic effect.
Continuous and cumulative use of anticholinergic medications including first-generation antihistamines is associated with higher risk of cognitive decline and dementia in older people; this association is not considered clinically relevant for younger individuals.
Anticholinergic toxicity manifests at the neuromuscular junction and sympathetic post-ganglionic junctions, causing ataxia, urinary retention, pupil dilation, irregular urination, and dry red skin; these effects are dose-dependent and occur primarily at recreational or overdose doses.
As a deliriant, dimenhydrinate produces hallucinations, delirium, and psychosis at recreational doses. Effects include realistic visual and auditory hallucinations, paranoia, confusion, and unusual sensitivity to sudden sounds. These psychotomimetic effects are an expected consequence of high-dose anticholinergic intoxication rather than an adverse reaction.
Convulsions are reported in overdose situations in both children and adults. Tremors may occur at recreational doses. Extrapyramidal side effects have also been noted.
Dimenhydrinate, originally designated Compound 1694, was developed through serendipitous observation rather than targeted research. In 1947, allergists Dr. Leslie Gay and Dr. Paul Carliner at Johns Hopkins Hospital were testing the compound as a potential treatment for hay fever and hives. Among…
Available over-the-counter as oral tablets (commonly sold under brand name Gravol). Injectable formulations require a prescription and have been marketed since 1973.
FDA approved on May 31, 1972. Oral tablet formulations are available over-the-counter without prescription. Injectable formulations (50 mg/mL intramuscular/intravenous) are available by prescription.
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