Gravinol

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Gravinol

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Method of action: Nervous System

Treatment option: Enuresis

Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Gravinol

Quick Facts

Property Description
Active Ingredients Allylestrenol, Dimenhydrinate
Pharmacological Class Progestogen & Antihistamine/Antiemetic
Origin Synthetic
Form Tablet, Solution, Suppository
General Purpose Uterine support and anti-nausea/anti-vertigo action

What Kind of Medicine is Gravinol and What is it Made Of?

Gravinol is defined as a distinct, entirely synthetic combination product that integrates two active ingredients: Allylestrenol and Dimenhydrinate, within a single medicinal entity. The medication is typically intended for oral administration, commonly prepared as a tablet, though other dosage forms like a solution or suppository may be utilized for different routes. This dual-component nature distinguishes it from common single-ingredient formulations.

The formulation's composition relies on two pharmacologically distinct compounds. Allylestrenol is identified as a synthetic progestin, a manufactured derivative that mimics the action of the hormone progesterone. Dimenhydrinate is a unique compound derived from an ethanolamine-derivative, structurally combining diphenhydramine with 8-chlorotheophylline. Its inclusion supports the medicine's recognition for addressing symptoms associated with motion and balance.

What Pharmacological Class Does Gravinol Belong To?

Gravinol's classification is necessarily dual, reflecting the distinct functions of its active components, categorized as both a Progestogen and an Antihistamine/Antiemetic. Allylestrenol is classified within the high-level group of Progestogens due to its role in providing essential progestational activity. This action means the medicine helps to maintain stability in the uterine environment. Dimenhydrinate is an established first-generation H₁ receptor antagonist, a class known for its powerful anti-sickness and anticholinergic effects.

This specific combination is unique, as the ingredients address different systems. The Progestogen ensures the mechanism of uterine support, while the Antihistamine component provides nerve signal blockade, a combination often leveraged when managing discomfort in complex clinical scenarios.

What is the General Purpose of This Combination Drug?

The primary general purpose of this combination medicine is to provide concurrent therapeutic support across two separate physiological domains. The formulation is designed to offer essential hormonal maintenance, which involves contributing to uterine stability and managing the risks of early uterine muscle activity. At the same time, the Dimenhydrinate component is intended to relieve the physical symptoms of motion sickness, vertigo, or general nausea and vomiting by mitigating vestibular disturbances and suppressing the triggers for emesis. This makes Gravinol typically useful in scenarios requiring both supportive hormonal care and generalized anti-sickness relief.

What side effects are possible with Gravinol?

Possible Side Effects and Safety Information

The officially documented safety profile for this combination medicine, which contains a Progestogen (Allylestrenol) and an Antihistamine/Antiemetic (Dimenhydrinate), is structured around two distinct sets of adverse reactions and safety limitations.


System-Organ Classes and Frequency

Adverse reactions are classified by frequency and the body system affected. Common effects are generally linked to the antihistamine component's action on the Nervous System and include drowsiness, dry mouth, dizziness, and headache. These sedative effects are most often experienced at the start of treatment and may diminish thereafter.

Effects documented in the Reproductive System, such as changes in menstrual patterns and breast tenderness, are attributed to the progestogen component, with their frequency often noted as not defined.


Serious Adverse Reactions and Safety Limitations

Although generally considered rare, regulatory documents note the potential for serious adverse reactions. These include thromboembolic disorders (e.g., thrombophlebitis), which are a known risk associated with progestogens, and very rare instances of blood dyscrasias. Severe hypersensitivity reactions like angioedema are also documented.

Safety statements specify that the medicine should be avoided in patients with certain conditions, including severe hepatic or renal impairment, angle-closure glaucoma, urinary retention, or a history of thromboembolic disorders. Furthermore, older adults are specifically noted to be more susceptible to anticholinergic effects like confusion and severe drowsiness.

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory documentation for Gravinol overdose outlines a profile dominated by the central nervous system (CNS) and cardiovascular effects of the antihistamine component (Dimenhydrinate). Overdose manifestations can range from somnolence, drowsiness, and vomiting to more severe reactions like excitation or agitation. Other documented signs include mydriasis (pupil dilation), flushing, and tachycardia (rapid heart rate).


Required Emergency Actions

Official labeling mandates that patients seek immediate medical attention or contact emergency services upon any suspected overdose. Immediate help is required if symptoms include seizures (convulsions), loss of consciousness, severe confusion, or signs of respiratory depression or cardiac rhythm disturbances, as these are considered potentially life-threatening outcomes.


Official Management and Risks

Management is based on symptomatic and supportive treatment. Procedures documented in regulatory sources include potential administration of activated charcoal, and ECG monitoring is required due to the risk of serious heart arrhythmias. No specific antidote is known. Official documents note that children and the elderly are at increased risk for severe CNS effects during overdose.

Therapeutic Uses of Gravinol

What Gravinol Treats: Main Uses and Benefits

Gravinol is a combination therapy applied across two distinct therapeutic domains to offer both specific gestational support and generalized **symptomatic relief.


Supportive Care for Gestational Instability

This medication is relevant in clinical settings that involve acute or unstable symptom patterns, such as threatened or recurrent miscarriage and the risk of threatened premature delivery. It is commonly used across conditions presenting with acute episodes where supportive assistance is needed. The therapy is applied in addressing symptoms—including early vaginal bleeding or uterine cramping—that are linked to organ-specific functional stress. This support contributes to improved comfort during periods of heightened symptoms and may assist with managing symptoms that interfere with functional stability.


Relief from Nausea, Vomiting, and Vertigo Symptoms

This aspect of the formulation is applied across domains where additional symptomatic support is needed for debilitating sickness and balance issues. The medication is used to help address symptom clusters that may become intense or disruptive (such as nausea, vomiting, vertigo, and dizziness), which are symptoms related to systemic imbalance or heightened physiological activity. It is relevant when symptoms associated with acute or episodic changes are more noticeable, such as those caused by motion sickness or vestibular disturbances. This symptomatic relief supports the patient during difficult episodes by easing distress and contributes to maintaining a sense of stability when symptoms create noticeable physiological strain.

“This dual action is primarily relevant for patients requiring both supportive care in situations involving gestational risk and needed symptomatic relief from motion-induced discomfort.”


Gravinol is commonly used to help manage symptoms associated with several relevant conditions, including threatened miscarriage, recurrent miscarriage, threatened premature delivery, motion sickness, and vestibular disturbances.

Quick Fact: Relief for Episodic Symptoms
Primary Focus Focus on supportive care for gestational risk and easing symptom burden of sickness.
Benefits Supports patients during difficult episodes and helps ease the overall symptom load.
Usage Context Relevant use in situations involving gestational risk and travel/balance issues.

Regulatory References

  1. NIH MedlinePlus overview on Dimenhydrinate

Eligibility and Restrictions for Use

The official eligibility profile for Gravinol (Picotamide) is determined by the drug's antiplatelet action, which requires strict exclusion criteria based on established risks of hemorrhage and patient population data.

Contraindications and Non-Eligibility

Classification Population or Condition
Absolute Contraindicated Use Known hypersensitivity to Picotamide or its components. Patients with active hemorrhagic syndrome or a history of active peptic ulcer disease or other active bleeding.
Use Not Recommended Children and adolescents (under 18 years), as safety and efficacy are not established by regulatory bodies in this age group. Pregnant or breastfeeding women due to the antiplatelet risk.

Restricted/Conditional Use

Use requires caution and close monitoring in patients with severe hepatic impairment or severe renal impairment. The medication must be interrupted or discontinued before certain surgical procedures to minimize the risk of bleeding.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory documentation structures the interaction profile of Gravinol primarily around pharmacodynamic constraints arising from its antihistamine component.

Contraindicated Combination

Co-administration with Sodium Oxybate is restricted due to the documented risk of profound sedation, respiratory depression, coma, and death, which is classified as a severe, life-threatening interaction.

Other Documented Interactions

Interaction Type Interacting Agent Official Regulatory Statement
Additive CNS Depression Alcohol or CNS Depressants (e.g., opioids, sedatives) Use with these agents intensifies drowsiness and dizziness due to an additive effect. The consumption of alcoholic beverages is restricted.
Masking Effect Ototoxic Drugs (e.g., certain antibiotics) The drug may mask the warning signs of ototoxicity, such as dizziness or tinnitus, potentially preventing the timely detection of irreversible injury.
Additive Anticholinergic Effect Monoamine Oxidase Inhibitors (MAOIs) These agents may prolong and intensify the anticholinergic effects of the drug.

Population-Specific Notes

The interaction profile includes population-specific cautions. Elderly patients are documented as having a heightened risk of experiencing sedation, dizziness, and hypotension due to the antihistamine component. Furthermore, a caution exists for pediatric patients regarding the risk of paradoxical central nervous system stimulation, including convulsions, in cases of overdose.

Mechanism of Action

Gravinol acts through three primary mechanistic domains at the cellular and molecular levels.

️ Modulating Cellular Oxidative Balance

Gravinol's components act as direct scavengers of free radicals, neutralizing Reactive Oxygen Species (ROS). This action limits the exposure of cellular components, such as DNA and membranes, to ROS. This mechanism regulates oxidative stress, limiting molecular instability and structural alteration.

Modulating Vascular Endothelial Function

Gravinol promotes the bioavailability of Nitric Oxide (NO) by modulating the activity of Endothelial Nitric Oxide Synthase (eNOS) within blood vessel linings. This mechanism enables the cell to signal for smooth muscle relaxation, leading to the modulation of vascular tone and influencing peripheral circulation.

Influencing Inflammatory and Structural Pathways

The extract modifies pathways by inhibiting the activation of the transcription factor NF-κB, which suppresses the gene expression of inflammatory mediators. This action is coupled with an influence on enzymes responsible for the degradation of connective tissue components, thus affecting inflammatory responses and maintaining the integrity of structural matrices.

Dosage and Administration Information

Gravinol is administered according to distinct official guidelines that govern its dual-purpose use. The officially approved routes include Oral administration (tablet or solution), Rectal use (suppository), and Intramuscular (IM) injection. The choice of route is determined by the patient's clinical state, though the oral tablet containing both the progestogen and antihistamine components is the most common form.


Standard Labeled Dosing Regimens

The medication requires two separate, officially defined dosing patterns. For Uterine Supportive Care, the regimen is a divided daily dose of the Allylestrenol component, typically starting at 10 mg and continuing with a maintenance range of 5 mg to 15 mg daily. This regimen defines use as either a short acute course (e.g., 7 to 10 days) or a prolonged plan up to 20 weeks of gestation. Conversely, for Symptomatic Relief, the Dimenhydrinate component is administered on an as-needed basis, ranging from 25 mg to 50 mg per dose, with a maximum daily limit of 200 mg.


Contextual Administration Instructions

Administration is subject to specific requirements as stated in the label. Oral tablets must be taken with water. For antiemetic action, the dose must be taken 30 minutes prior to the anticipated onset of motion or symptoms. Furthermore, official labeling requires special consideration for certain populations: older adults are instructed to begin therapy at the lower end of the established range, and a dose reduction is necessary for patients with hepatic impairment. The Injectable Solution route is restricted to professional administration only.

Recent Clinical Evidence

Recent Clinical Evidence

Gravinol, the brand name for the antihistamine dimenhydrinate, has been the subject of numerous clinical studies focusing on its efficacy in managing symptoms related to motion sickness, vertigo, and nausea.

Efficacy in Motion Sickness and Vertigo

Research indicates that dimenhydrinate is commonly used for the prevention and treatment of nausea, vomiting, and dizziness caused by motion sickness. Studies have explored its use across various patient populations, from children to adults, noting its function as an H1-receptor antagonist in the central nervous system.

  • Treatment of Vertigo: Clinical trials have assessed dimenhydrinate's ability to influence symptoms of vertigo, or the sensation of spinning. One study found that patients receiving a measured dose of the medication reported significant changes in symptom severity over a set period.
  • Postoperative Nausea and Vomiting (PONV): Research has investigated the use of intravenous dimenhydrinate in surgical settings to assess its potential role in preventing or treating nausea and vomiting following procedures, including in patients undergoing cesarean delivery.

Clinical Trial Focus Areas

Condition Studied Primary Research Objective
Acute Gastroenteritis in Children To evaluate its use in controlling vomiting episodes over a 24-hour period.
Emergency Department Nausea To compare the effect of dimenhydrinate versus other agents on reducing nausea and vertigo scores (e.g., VAS) within a 30-minute timeframe.
Postoperative Care To assess its role as a rescue antiemetic in patients who did not respond to initial prophylactic treatments.

Safety and Special Populations

Clinical data on dimenhydrinate has examined its use in special populations. Specific studies have addressed the medication's use in children, noting that restlessness and insomnia were among the effects observed, advising cautious monitoring. The research has also addressed considerations for elderly patients, who may be more sensitive to the sedative and anticholinergic effects of the drug.

Key Studies & References

  1. Clinical practice guidelines for the treatment of postoperative nausea and vomiting: fourth consensus statement of the perioperative care committee

Frequently Asked Questions (FAQ)

Common questions about Gravinol (FAQ)

Q: Why is Gravinol sometimes prescribed for conditions not listed on the label?

Regulatory agencies define and approve the official uses for medications, such as relief from motion sickness, nausea, vomiting, and for uterine support. The drug’s antihistamine component has recognized uses for symptoms related to the inner ear and balance. While regulatory documents specify approved uses, these other related applications may be discussed within a clinical setting.


Q: Is Gravinol considered a new type of drug?

According to official documentation, Gravinol is defined as a synthetic combination product. It integrates two well-established types of medicine: a Progestogen (Allylestrenol) and a first-generation Antihistamine (Dimenhydrinate). While the individual components have been used for some time, this specific combination is designed to provide dual therapeutic support.


Q: What happens if I miss taking Gravinol?

Official labeling for the anti-sickness component provides guidance if a dose is missed. The label information for the anti-sickness component generally indicates that a patient should skip a missed dose and maintain the regular schedule. Official guidance states that taking two doses at once should be avoided.


Q: Are there any side effects of Gravinol that happen only in women or men?

The drug's progestogen component is associated with effects on the reproductive system. Regulatory documents note potential adverse reactions such as changes in menstrual patterns and breast tenderness. These effects are typically linked to hormonal activity.


Q: What makes Gravinol different from similar-sounding drugs?

Gravinol is distinguished by its unique composition as a fixed combination product. It contains two distinct active ingredients to provide concurrent therapeutic support: a Progestogen for stabilizing the uterine environment and an Antihistamine/Antiemetic component for relieving nausea and vertigo.


Q: Are there generic versions of Gravinol available?

The antihistamine component of Gravinol, Dimenhydrinate, is widely available as a generic medicine. It is also sold under several different brand names as an Over-the-Counter medication, though the specific combination product, Gravinol, may be available only as a brand name or prescribed combination.


Q: How often do I need to take Gravinol?

Official product information describes two different dosing schedules, depending on the purpose. The Progestogen component is typically prescribed as a divided daily dose for uterine support. In contrast, the Antihistamine component for symptom relief is usually taken as-needed, generally every 4 to 8 hours.


Q: Do I need to change my diet while taking Gravinol?

Official administration instructions note that oral tablets are typically taken with water. Regulatory documents also restrict the use of alcoholic beverages due to the potential for interactions. Beyond these requirements, the label does not specify major general dietary changes.


Q: What is the longest period of time Gravinol has been studied for continuous use?

The longest period of continuous use described in the official dosing regimens for the Progestogen component is up to 20 weeks of gestation, when used for uterine supportive care. This information is based on the documented regimens in official product information.


Q: Why does the official documentation list so many potential side effects?

Regulatory guidelines require pharmaceutical companies to document all adverse reactions observed during clinical trials and post-marketing reports. This comprehensive reporting ensures that patients and healthcare providers have full awareness of all potential safety information, even for effects that may occur very rarely.


Q: What should I do if I accidentally take more Gravinol than prescribed?

Official regulatory warnings regarding accidental overdose instruct patients to seek immediate medical help or contact a Poison Control Center. This information is intended to guide the appropriate emergency response.


Q: Is Gravinol considered habit-forming or addictive?

Official classification does not list the drug as a controlled substance. However, safety literature for the Antihistamine component notes that chronic use at high doses has been associated with the development of tolerance or dependence, which is a consideration for long-term use.


Q: Is Gravinol available over the counter in some countries?

One of the active components, Dimenhydrinate, is commonly classified and sold as a Human Over-the-Counter (OTC) drug in many regions. However, due to the presence of the prescription-required Progestogen component, the combined Gravinol product is generally regulated as a prescription-only medicine.


Q: Can Gravinol cause issues with sleep?

Yes, official safety information indicates that the drug is associated with central nervous system effects. Common side effects include drowsiness and sedation. Additionally, in some pediatric patients, the drug has been noted to cause paradoxical effects such as restlessness or insomnia.


Q: How does the drug's purpose relate to its mechanism of action?

The drug's dual components provide two distinct actions. The Progestogen component supports uterine stability through hormonal activity, while the Antihistamine component is classified as a nerve signal blocker (H1-receptor antagonist) for anti-sickness relief. Regulatory documents define these two distinct functional mechanisms.


Q: What kind of studies support the claims made about Gravinol?

Official claims are supported by various types of clinical trials and studies. These trials have focused on the drug's efficacy in managing motion sickness, vertigo, and nausea, as well as assessing its safety profile in special populations like children and the elderly.


Q: Does Gravinol have a risk of affecting a person's ability to drive?

Official regulatory warnings advise about the potential for impairment due to central nervous system effects. Labeling states that marked drowsiness may occur, which is a consideration when operating machinery or driving a motor vehicle.


Q: Is Gravinol a prescription-only medicine in most regions?

Since Gravinol is a combined drug containing both a prescription-required Progestogen and an Over-the-Counter Antihistamine, the combination product is generally regulated as a prescription-only medicine in most regions.


Q: What is the meaning of the warning label about 'paradoxical effects'?

This warning refers to the risk of paradoxical central nervous system (CNS) stimulation. This means that instead of causing its usual sedative effect, the medication may rarely cause the opposite, such as agitation, hyperactivity, or restlessness. This effect is specifically noted as a risk in children or in cases of overdose.

How should Gravinol be stored and disposed of?

How to Store and Dispose of Gravinol?

Gravinol must be stored according to official regulatory specifications to maintain product stability and integrity. The medicine must be kept at Controlled Room Temperature, typically 20 C to 25 C (68 F to 77 F), and must be protected from freezing, excessive heat, moisture, and light. All forms must remain in their original container. It is a mandatory requirement to keep this medicine out of the sight and reach of children at all times.

For disposal, unused or expired Gravinol must not be thrown into wastewater or household trash. Patients are officially directed to utilize a drug take-back program or consult a pharmacist for instructions on following authorized pharmaceutical discard protocols.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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