How can antihistamines be used to manage peripheral vertigo? What are the new developments in this area? Discover the latest insights.

The Prevalence and Impact of Peripheral Vertigo

Peripheral vertigo is a common condition that affects a significant portion of the population. Studies have shown that the prevalence of balance symptoms and disorders in the community can range from 5% to 10%, with vertigo being one of the most common manifestations. Vertigo, a hallmark symptom of peripheral vestibular disorders, can have a profound impact on an individual’s quality of life, leading to difficulties with daily activities, increased risk of falls, and significant socioeconomic burden.

The Role of the Vestibular System and Histamine

The vestibular system plays a crucial role in maintaining balance and spatial orientation. It consists of specialized sensory organs, the semicircular canals and otolith organs, which detect head and body movements and relay this information to the brain. Disruptions in the normal functioning of the vestibular system can lead to the development of vertigo and other balance disorders.

Histamine, a ubiquitous neurotransmitter and signaling molecule, has been found to play an important role in the regulation of vestibular function. Histamine receptors, including H1, H2, H3, and H4, have been identified in various parts of the vestibular system, including the hair cells, vestibular nuclei, and endolymphatic sac. These receptors are involved in modulating neurotransmission and influencing the sensitivity of the vestibular system to various stimuli.

The Use of Antihistamines for Peripheral Vertigo

Given the involvement of histamine in vestibular function, antihistamines have been explored as a potential treatment option for peripheral vertigo. Antihistamines work by blocking the action of histamine at its receptors, thereby potentially reducing the symptoms associated with vestibular disorders.

Traditionally, first-generation antihistamines, such as meclizine and dimenhydrinate, have been commonly used to manage the symptoms of peripheral vertigo. These medications have been shown to be effective in reducing dizziness and nausea associated with various vestibular disorders, including benign paroxysmal positional vertigo (BPPV) and vestibular neuritis.

Emerging Antihistamine Therapies for Peripheral Vertigo

While first-generation antihistamines have been the mainstay of treatment, there are new developments in the use of antihistamines for peripheral vertigo. Researchers have been exploring the potential of second-generation antihistamines, such as betahistine, which have a more selective affinity for specific histamine receptor subtypes.

Betahistine, for example, has been shown to have a dual mechanism of action, acting as a partial agonist at H1 receptors and an antagonist at H3 receptors. This unique profile may provide additional benefits in the management of vestibular disorders by potentially enhancing vestibular compensation and reducing vertigo symptoms.

The Blood-Labyrinth Barrier and Drug Delivery

One of the challenges in the treatment of inner ear disorders, including peripheral vertigo, is the presence of the blood-labyrinth barrier, which limits the delivery of systemic medications to the inner ear structures. Researchers are exploring novel drug delivery methods, such as intratympanic injections or the use of nanoparticle-based formulations, to improve the targeted delivery of antihistamines and other therapeutic agents directly to the affected inner ear.

The Future of Antihistamine Therapies for Peripheral Vertigo

As our understanding of the role of histamine in vestibular function continues to evolve, the development of new and more targeted antihistamine therapies for the management of peripheral vertigo holds promise. Ongoing research focused on optimizing drug delivery, exploring the potential of combination therapies, and understanding the precise mechanisms of action of different antihistamine subtypes may lead to more effective and personalized treatment options for individuals suffering from these debilitating vestibular disorders.

Conclusion

In summary, the management of peripheral vertigo with antihistamines has been an area of active research and clinical exploration. While traditional first-generation antihistamines have been widely used, the emergence of new antihistamine therapies, such as betahistine, and advancements in drug delivery methods offer exciting possibilities for the future of managing these challenging vestibular disorders. As the field continues to progress, patients with peripheral vertigo may benefit from more personalized and effective treatment options that leverage the role of histamine in vestibular function.

Management of peripheral vertigo with antihistamines: New options on the horizon

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Spinning out of control: Vertigo

Vertigo isn’t just a catchy song by the band U2, but is also a common symptom that has multiple potential causes. Although most people think that vertigo has to involve a spinning sensation, vertigo is actually the sensation that one is moving or that one’s surroundings are moving in the absence of any actual movement. To understand vertigo, one must understand that our sense of balance comes from multiple different systems in the body.

A balancing act: processing system inputs

There is your visual system, which tells you where your body is in space and time in relation to your surroundings. There is the sensory system, which allows your feet to send information to your brain about the terrain you are walking on. A third system, the vestibular system, often goes unappreciated in day-to-day life, but can cause havoc when not working properly. The vestibular system is composed of structures in your inner ear that function like a carpenter’s level.

Like a level, when the device is tilted in one direction or another, the bubble moves indicating imbalance. Similarly, during head and body movements, the inner ear transmits information regarding movement or balance to the brain. When there is a mismatch between the visual, sensory, or vestibular systems, people can at times have balance issues. Those balance issues can include vertigo.

Medications for the treatment of vertigo are used to target structures in the brain that process these at times conflicting signals. Antihistamines like dimenhydrinate (Dramamine), diphenhydramine (Benadryl), and meclizine (Antivert) can be useful treatments for vertigo. Anticholinergic medications like scopolamine can be particularly useful, as it comes in a patch form, which can be applied just prior to entering a situation where motion sickness can be anticipated.

Shipwrecked

One of the most common manifestations of vertigo occurs when someone travels on a boat. While on a boat, particularly when not standing on the deck, your visual system indicates that there is not much movement, and your surroundings appear still. The vestibular system (inner ear), on the other hand, is telling your brain that there is back and forth rocking movement, which naturally occurs with sea travel. The result is that one part of the brain is registering movement while the other part of the brain is registering no movement. This mismatch leads to vertigo, nausea, and at times vomiting, which is commonly known as seasickness.

Unfortunately, when people feel seasick many go below deck to lie down, which makes the problem worse. The best remedy for seasickness is actually to go above the deck, and look at the motion of the water or off at the horizon. By doing this, the visual system perceives the motion that the vestibular system perceives, which can alleviate the sense of imbalance. For many who have experienced seasickness, the symptoms can persist for hours to days after getting off the boat. Another place where such balance mismatches frequently occur is when transitioning onto or off of an escalator.

I explained this concept to one of my patients who is an avid fisherman as he complained about his wife, who frequently gets seasick. After providing the advice, he said, “Dr. Mathew, your care has been life-changing. As a thank you, you must join me on my boat some day.” I replied, “Thank you for the offer, but I am horrible at fishing.” He said, “Oh really, why is that?” I replied, ”Because it is difficult to catch any fish when you are holding two cocktails.” He chuckled, and proceeded to tell me about how he often catches mackerel, which other fishermen call inedible, advising him to throw it back in the water. He ignores their advice and keeps the mackerel, noting, “My wife loves that greasy fish.” I then asked him, “Is fishing a religious experience for you?” He said, “No doctor, why do you ask?” I then shrugged my shoulders and said, “Holy mackerel?” As he tried to hide a smile, he indicated that he was not amused. I then said, “Like the mackerel, I guess I should have thrown that bad joke overboard”, which caused him to laugh out loud. Apparently, the post-punch line was a bigger hit than the actual punch line.

Vertigo. Algorithm for diagnosis and treatment | Gorbacheva F.E.

From 5 to 30% of patients of various age groups consult a doctor with complaints of dizziness. It is not uncommon for patients to refer to dizziness as a feeling of lightheadedness, an impending loss of consciousness, a feeling of emptiness or “lightness in the head”, unsteadiness and staggering when walking, as well as a feeling of heaviness in the head, “internal dizziness” or a state similar to intoxication.

The term systemic vertigo refers to the sensation of rotation, falling, tilting or rocking of surrounding objects or one’s own body. Often, systemic dizziness is accompanied by nausea, vomiting, hyperhidrosis.

Systemic dizziness is usually characteristic of lesions of the vestibular apparatus, in particular, the peripheral and central sections. A feature of vestibular vertigo is its paroxysmal and periodicity, in contrast to the constant dizziness that develops with organic damage to the brain structures responsible for vestibulo-ocular reflexes, as well as with the use of ototoxic drugs.

One of the most common types of vertigo is benign paroxysmal positional vertigo (BPPV), which is more common in women and is characterized by the onset of dizziness with a rapid change in the position of the head and body when the patient is in a horizontal position or when bending forward and tilting the head back. Among elderly and senile patients, BPPV accounts for 35 to 40% of all forms of dizziness in this category of patients.

The main task of the doctor is to identify the cause of dizziness based on the clinical picture, the nature of the concomitant symptoms, the duration of vestibular disorders, the approximate localization of the lesion, and additional research data (Fig. 1).

Fig. 1. Algorithm for identifying the causes of dizziness

Treatment . If various diseases are identified as the cause of dizziness, it is possible to carry out etiotropic treatment (antiviral drugs for herpetic lesions of the Scarpa node, surgery for cholesteatoma and other tumors involving the vestibular analyzer, etc.). In most cases, the treatment of systemic vertigo is symptomatic.

Various drugs have the ability to stop or reduce the symptoms of dizziness, but many of them have side effects. Therefore, the choice of a particular drug is determined by the risk of side effects, on the one hand, and the severity of dizziness symptoms, on the other.

An important role in the functioning of the vestibular structures is played by the histaminergic system, which ensures the transmission of impulses from the vestibular nuclei. Therefore, for the purpose of symptomatic therapy of systemic dizziness, antihistamines are used.

Among the antihistamines used to relieve dizziness, promethazine is used . In order to reduce the manifestations of anxiety in dizziness, tranquilizers (diazepam, lorazepam) are used. Metoclopramide is prescribed to stop vomiting. betahistine hydrochloride0019 . Due to the blockade of H ₃ receptors, betahistine increases the release of neurotransmitters from the nerve endings of the presynaptic membrane, has an inhibitory effect on the vestibular nuclei of the brainstem and improves the blood supply to the inner ear. According to double-blind, randomized trials, betahistine dihydrochloride is effective in Meniere’s disease and other conditions accompanied by systemic vertigo. The drug is able to stop an attack of dizziness, as well as reduce the frequency of subsequent attacks.

The drug does not cause side effects, in particular, does not have a sedative effect, does not affect the level of blood pressure and heart rate. Therefore, it can be prescribed for a long time, for example, with Meniere’s disease.

Like other synthetic analogues of histamine, betahistine hydrochloride is contraindicated in exacerbations of duodenal ulcer and stomach ulcers, pheochromocytoma. The drug should be used with caution in bronchial asthma.

Cinnarizine Sopharma Tablets 25 mg 50 pcs

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Cinnarizine sopharma

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Product code:
11135

Manufacturer:
DOMINANTA-SERVICE

Country of origin:
Bulgaria

Release form:
Tablets

Active ingredients:
Cinnarizine

Dispensing order:
By prescription

There are contraindications, consult your doctor

Payment and methods of obtaining

Price:

119 ₽

+1 bonus

The price is valid only when ordering on the site

There are contraindications, consult a doctor

Manufacturer:
DOMINANTA-SERVICE

Country of origin:
Bulgaria

Release form:
Tablets

Active ingredients:
Cinnarizine

Dispensing order:
Prescription

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You can buy Cinnarizine Sopharma Tablets 25 mg 50 pcs at the price of 119₽ in GORZDRAV pharmacies in Moscow and the Moscow region

Features

Features

Minimum age from.	12 years old
Minimum allowable storage temperature, °С	2 °C
Maximum allowable storage temperature, °С	25 °C
Expiry date	36 months
Storage conditions	In a place protected from the sun
Release form	Tablet
Release procedure	Prescription
Active ingredient	Glycerylphosphorylcholine hydrate (Glycerylphosphorylcholine hydrate)
Application	Neurology
Pharmacological group	N07CA02 Cinnarizine
Registered as	Medicine
Pack quantity	50 pcs

Information

Instructions for use

Active ingredients Tablets

Composition

Composition 1 tab. cinnarizine 25 mg Excipients: wheat starch, lactose monohydrate, polyvinylpyrrolidone K25, aerosil 200, magnesium stearate, microcrystalline cellulose. 50 pcs. – blisters (1) – packs of cardboard.

Pharmacological effect

Cinnarizine improves cerebral and peripheral circulation by inhibiting the action of a number of endogenous vasoconstrictors and the flow of calcium ions into cells by blocking slow voltage-dependent calcium channels. It has a vasodilating effect, especially in relation to cerebral vessels, without significantly affecting blood pressure. Increases the elasticity of erythrocyte membranes, their ability to deform, reduces blood viscosity, increases the resistance of muscles to hypoxia. Shows moderate antihistamine activity, reduces the excitability of the vestibular apparatus, lowers the tone of the sympathetic nervous system.

Pharmacokinetics

Absorbed relatively slowly in the gastrointestinal tract. Cmax in plasma is achieved 1-3 hours after oral administration. It binds to plasma proteins by 80%, to erythrocytes by 13%. Distribution in tissues is more intense within 4 hours after ingestion. Completely metabolized in the liver, mainly by N-dealkylation. T1 / 2 is 3-6 hours, excreted as metabolites: 1/3 – by the kidneys and 2/3 – with feces.

Readings

Adults and children over 12 years of age: prevention and treatment of peripheral circulatory disorders (endarteritis obliterans, thromboangiitis obliterans, Raynaud’s disease, diabetic angiopathy, thrombophlebitis, trophic disorders (trophic and varicose ulcers), paresthesia, nocturnal spasms and coldness in the extremities). Prevention of kinetosis (road sickness, sea and air sickness). Symptomatic treatment of labyrinth and vestibular disorders of vascular origin, Meniere’s disease.

Contraindications

Pregnancy. lactation period. Children’s age up to 12 years. Lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome. Celiac disease (gluten enteropathy). Hypersensitivity to the components of the drug. Caution: Parkinson’s disease.

Precautions

From the side of the cardiovascular system: decrease in blood pressure. From the nervous system: headache, fatigue; in patients taking cinnarizine in high doses for a long time, extraliramide symptoms may appear (tremor of the limbs and increased muscle tone, hypokinesia, disorientation, imbalance), including Parkinson’s syndrome, depression. From the digestive system: dry mouth, pain in the epigastric region, dyspepsia; extremely rarely – cholestatic jaundice On the part of the skin: increased sweating; in extremely rare cases, lichen planus and lupus-like reactions.

Use in pregnancy and lactation

Due to the lack of well-controlled clinical studies on the safety of use in pregnant women, the use of cinnarizine during pregnancy is not recommended. In view of the lack of data on excretion into breast milk, the use of cinnarizine during breastfeeding is undesirable. In cases where the use of the drug is necessary, food feeding should be discontinued.

Dosage and administration

Adults and children over 12 years of age Inside, with plenty of liquid, after meals. In violation of peripheral circulation – 50-75 mg (2-3 tab /) 3 times / day. With high sensitivity to the drug, treatment begins with 1/2 dose, increasing it gradually. To achieve the optimal therapeutic effect, the drug should be taken continuously, for a long time – from several weeks to several months. With vestibular disorders – 25 mg 3 times / day / With kinetosis – 25 mg 30 minutes before the upcoming road (if necessary, re-take 25 mg after 6-8 hours). With labyrinth disorders – 25 mg 3 times / day. The maximum daily dose should not exceed 225 mg.

Side effects

The most common are drowsiness, gastrointestinal discomfort, which in most cases are transient and disappear with dose reduction. nervous system: headache, fatigue. Patients taking high doses of cinnarizine for a long time may experience extraliramide symptoms (tremor of the limbs and increased muscle tone, hypokinesia, disorientation, imbalance), including Parkinson’s syndrome, depression. On the part of the digestive system, dry mouth, pain in the epigastric region, dyspepsia. Very rarely – cholestatic jaundice. On the part of the skin: increased sweating. in extremely rare cases, lichen planus and lupus-like reactions. Allergic reactions, skin rash. Other: weight gain.

Overdose

Symptoms: vomiting, drowsiness, decreased blood pressure, tremor, coma. Treatment: in cases of overdose – gastric lavage, activated charcoal. Symptomatic agents are used. There is no specific antidote.

Interaction with other drugs

Enhances the effect of ethanol (alcohol) and sedative drugs. When used simultaneously with nootropic, antihypertensive and vasodilators, it enhances their effect. Reduces the effect of hypertensive drugs.

Special instructions

Cinnarizine may cause stomach discomfort. Taking tablets after meals reduces irritation of the gastric mucosa. In patients with Parkinson’s disease, cinnarizine should only be given if the benefits outweigh the potential risk of worsening the condition. Patients over 65 years of age with a family history or clinical symptoms of extrapyramidal disorders should be under constant medical supervision. In persons prone to a decrease in blood pressure (hypotension), it is necessary to control blood pressure values ​​during treatment. Cinnarizine may cause false positive reactions in anti-doping tests in athletes. With prolonged use, it is recommended to conduct a control examination of the function of the liver, kidneys, peripheral blood picture. Due to its antihistamine effects, cinnarizine may cause false negative results in skin tests for hypersensitivity. Treatment with cinnarizium should be discontinued 4 days prior to testing. Influence on the ability to drive vehicles and control mechanisms During the period of treatment, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Prescription

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