Bioavailability of 50 mg dimenhydrinate granules taken with or without water versus reference formulations for nausea and vomiting in healthy volunteers
- Participants:Adults · Healthy volunteers
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Dimenhydrinate is a medication primarily used to prevent and treat nausea, vomiting, and dizziness associated with motion sickness, vertigo, and other conditions. It is commonly known by the brand name Dramamine in some countries, while in others it may be sold as Gravol [1]. The medication belongs to a class of drugs called antihistamines, specifically H1-receptor antagonists, which work on the central nervous system.
Dimenhydrinate functions by inhibiting the body's histamine receptors and cholinergic receptors in the brain. Specifically, it affects the vestibular system (the part of your inner ear that helps control balance) and the vomiting center in the brain [3].
When you experience motion sickness or vertigo, there is often an overstimulation of the labyrinthine function (structures in your inner ear). Dimenhydrinate has a depressant action on this hyper-stimulated function, which helps reduce the symptoms of dizziness and the associated nausea [3].
Dimenhydrinate has been extensively used for treating motion sickness, which is the feeling of nausea and dizziness that can occur during travel by car, boat, or plane [3]. It is also effective for treating various types of vertigo, which is the sensation that you or your surroundings are spinning or moving.
In clinical trials, dimenhydrinate was found to be effective in treating nausea due to vertigo. In one study, patients with vertigo who received 50 mg of dimenhydrinate showed significant improvement in their symptoms [3].
Vertigo describes the illusion of involuntary movement, usually rotational, which is caused by sudden tonic neural activity. Management of patients with spontaneous vertigo and related nausea-vomiting symptoms can be challenging, especially in emergency settings. Dimenhydrinate acts by inhibiting vomiting through affecting the histaminic receptor and cholinergic receptor function center of the vestibular nucleus in the central vestibular system [3].
Beyond motion sickness, dimenhydrinate is also used to treat general nausea and vomiting from various causes. It is particularly useful in cases where the nausea is related to inner ear disturbances [5].
In a study involving children with gastroenteritis (an infection that causes inflammation of the stomach and intestines), dimenhydrinate was tested for its effectiveness in controlling vomiting. The researchers noted that dimenhydrinate had the potential to be more cost-effective than other anti-nausea medications, with an average cost of $0.90 US per dose [5].
Dimenhydrinate has been shown to be effective in preventing and treating postoperative nausea and vomiting (PONV), which is a common complication after surgery [1][2].
In a clinical trial focusing on women undergoing abdominal hysterectomy, researchers investigated whether dimenhydrinate could lower the proportion of postoperative nausea and vomiting during the first day after surgery. Participants received either dimenhydrinate or a placebo intravenously after they returned to the ward, and their symptoms were monitored over the next 24 hours [1].
Another study examined the effectiveness of dimenhydrinate in preventing intraoperative nausea and vomiting in patients undergoing cesarean delivery. The medication was given before the induction of spinal anesthesia to determine if it would decrease the overall incidence of these side effects [2].
Dimenhydrinate can be administered in several ways, depending on the condition being treated and the patient's needs:
Oral tablets: Commonly available as over-the-counter medication for motion sickness prevention [2][4].
Intravenous (IV) injection: Used in hospital settings, particularly for severe nausea or postoperative situations [1][2][3].
Intravenous infusion: Sometimes given as a slow infusion over 15-30 minutes, diluted in normal saline [3].
In some studies, dimenhydrinate was administered as follows:
The dosage of dimenhydrinate varies depending on the condition being treated, the age of the patient, and the route of administration:
For adults:
For children:
The medication can be administered multiple times per day, usually every 4-6 hours as needed, but specific dosing schedules should be determined by healthcare providers.
While dimenhydrinate is generally considered safe when used as directed, it can cause several side effects:
Common side effects include:
Less common side effects may include:
Serious but rare side effects that require immediate medical attention:
In clinical studies, researchers monitored patients for specific side effects including tachycardia, dizziness, restlessness, dry mouth, and oxygen desaturation [2].
Before taking dimenhydrinate, consider the following precautions:
Several studies have compared dimenhydrinate to other medications for treating similar conditions:
Versus Metoclopramide for Vertigo-Related Nausea: One study compared 50 mg of dimenhydrinate to 10 mg of metoclopramide for treating nausea due to vertigo in emergency settings. Both medications were given intravenously as a slow infusion over 15 minutes [3].
Versus Meclizine for Peripheral Vertigo: Another trial compared dimenhydrinate (Dramin®) soft gel capsules to meclizine chlorhydrate (Meclin®) for treating symptoms of acute vertigo from peripheral origin. The study assessed various symptoms including distasia, instability when walking, spinning sensation, and tendency to fall [4].
Versus Piracetam for Peripheral Vertigo: A double-blind randomized clinical trial compared the efficacy of intravenous piracetam (2 g) and dimenhydrinate (100 mg) in patients with peripheral vertigo [11].
Versus Ondansetron for PONV: A study compared the effectiveness of preoperative oral dimenhydrinate (50 mg) versus intraoperative intravenous ondansetron (4 mg) in preventing postoperative nausea and vomiting in patients undergoing laparoscopic cholecystectomy [10].
In some multimodal approaches to preventing PONV, dimenhydrinate (25 mg) is used as part of a combination therapy along with other medications such as aprepitant, perphenazine, ondansetron, and dexamethasone [13].
Dimenhydrinate has been used in pregnant women, particularly for morning sickness and during cesarean deliveries. In one study, researchers investigated whether an intravenous dose of dimenhydrinate (Gravol) given before the induction of spinal anesthesia would decrease the incidence of intraoperative nausea and vomiting in patients undergoing cesarean delivery [2].
The study noted that dimenhydrinate "has been safely and widely used during pregnancy, labour and Cesarean deliveries," suggesting its relative safety in this population. However, as with any medication used during pregnancy, it should be taken under medical supervision [2].
Dimenhydrinate has been studied in children, particularly for treating vomiting due to gastroenteritis. In one trial, children from 1 to 12 years of age who had experienced at least 5 episodes of vomiting in the previous 12 hours and were diagnosed with acute gastroenteritis received either dimenhydrinate or placebo every six hours (1 mg/kg/dose, maximum dose 50 mg/dose) [5].
The researchers noted that restlessness and insomnia have been described as potential side effects in children, so careful monitoring is advised [5].
Elderly patients may be more sensitive to the side effects of dimenhydrinate, particularly its sedative and anticholinergic effects. This could include increased drowsiness, confusion, dry mouth, constipation, or urinary retention. Therefore, lower doses may be appropriate for elderly individuals, and they should be monitored more closely when taking this medication.
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