Many medications presently available are known to be used for treating multiple conditions. These medications are known to have a common mechanism of action, which helps in creating different conditions. One of the more popular examples of such medications are anticholinergic agents. Typically used to treat an extensive list of conditions, anticholinergic drugs work by inhibiting the action of a neurotransmitter. By virtue of blocking out the neurotransmitter acetylcholine, these formulations help to manage certain muscle movements that are involuntary in nature. As a consequence of this, essential body functions are regulated, offering relief from a host of ailments.

The more common conditions that are treated by anticholinergic drugs include conditions associated with the bladder, Parkinson’s disease, disorders of the gastrointestinal tract and COPD (chronic obstructive pulmonary disease). Here is a detailed look at anticholinergic drugs that are used in treating various conditions. More like a quintessential guide, the exhaustive details covered below will give all the information that is necessary to know about the various use cases of anticholinergic drugs.

Anticholinergic drugs and formulations presently available for treating various conditions

In a nutshell, anticholinergic drugs refer to those medications that bind to cholinergic receptors without activating the receptors. As a consequence of this binding action, the drug inhibits the actions of acetylcholine. Presently a long list of medications used for treating various conditions belong to the category of anticholinergic agents or formulations. Despite the fact that these medications belong to the same broad category, there are critical differences in the medication. As a result of these differences in the formulation and dosage, the actual prescription of these medications for various conditions are determined by the specialist. It is incorrect to assume that medications can be used interchangeably for different conditions.

The mechanism of action of anticholinergics typically involves blocking of the neurotransmitter that is responsible for the symptoms associated with various conditions. Acetylcholine is known as a chemical messenger that moves signals between various parts of the body. The signals are responsible for controlling different functions of the organs in the body. For instance, involuntary movements in various parts of the body including the lungs, the urinary tract and the gastrointestinal tract are all controlled by the signals that are exchanged between various parts of the body. Acetylcholine is the neurotransmitter that moves the signals. By blocking the neurotransmitter, anticholinergics help to control various involuntary bodily functions that are responsible for some of the more common symptoms and conditions in various ailments. Different involuntary movements are responsible for different actions. For instance, urination, movements, salivation, and digestion are involuntary actions that are mainly controlled through these neurotransmitters. By selectively targeting and blocking these neurotransmitters, it is possible to regulate the involuntary bodily actions.

Common conditions that are treated with anticholinergics

While anticholinergics can be used to treat multiple conditions, the most common conditions that can be treated include overactive bladder, asthma, COPD (chronic obstructive pulmonary disorder) and bladder incontinence. Other conditions that are also treated with anticholinergics include movement disorders such as Parkinson’s disease. Additionally anticholinergics are also used prior to surgery during the stage of administering anaesthesia to a patient about to undergo surgical procedures.

Some of the more popular anticholinergics that are used for various conditions include the following :

· Clidinium
· Atropine
· Glycopyrrolate
· Belladonna alkaloids
· Benztropine mesylate
· Orphenadrine
· Cyclopentolate
· Darifenacin
· Flavoxate
· Fesoterodine
· Tiotropium
· Scopolamine
· Homatropine hydrobromide
· Hyoscyamine
· Ipratropium
· Trihexyphenidyl
· Propantheline
· Tolterodine
· Methscopolamine
· Solifenacin
· Trospium

With the possible exception of transdermal patches, all anticholinergic oral medications are prescription only formulations. In other words, the medications are available only when prescribed by a qualified and certified medical practitioner.

Mechanism of action of anticholinergics in treating asthma

By virtue of being muscarinic receptor antagonists, anticholinergics are used in the treatment of asthma and COPD. Studies have clearly established a link between acetylcholine and asthma. The mechanism of action of anticholinergics in inhibiting acetylcholine is regarded as the reason behind the effectiveness of the medication in treating the condition. Acetylcholine is known to induce inflammation and modification of the airway, which contributes to the manifestation of asthma and COPD. As very important parasympathetic neurotransmitter, acetylcholine contributes to the manifestation of asthma and COPD. In other words, the effect of acetylcholine in smooth muscle contraction and the secretion of mucus is known to contribute to the condition. Anticholinergics work by being effective muscarinic receptor antagonists. This in turn helps in treating COPD and asthma. The airway neurons and epithelial cells release acetylcholine. This in turn binds to the muscarinic receptors triggering the contraction of the smooth muscles and secretion of mucus. Various inflammatory mediators combine with other reflexes causing bronchoconstriction. Acetylcholine is also responsible for increasing the secretion of mucus which is known to aggravate asthma. Apart from the various contributing factors such as mucus secretion and bronchoconstriction, acetylcholine is also known to trigger inflammation of the airways. Anticholinergics are known to have strong effects on all of the contributing factors that are responsible for the condition. For instance, anticholinergics are credited with assessing the qualities to reduce inflammatory responses that are partly responsible for the conditions associated with asthma and COPD. Similarly different types of anticholinergic medications are known to significantly reduce the conditions that are attributed to allergens. As a result of reduced count of eosinophilia, the symptoms and conditions are controlled, and this includes airway inflammation. Another reason for the conditions associated with COPD and asthma are the structural changes that are experienced in the airways. As a consequence of the contraction of the smooth muscle, the pathways end up getting remodeled or restructured. Anticholinergics help to treat this restructuring of airways, which helps in alleviating the symptoms and conditions associated with asthma and COPD. Bronchoconstriction is also regarded as one of the reasons for restructuring of the airway. Anticholinergics, by virtue of being able to treat both bronchoconstriction and airway restructuring, are regarded as an effective medication for treating the condition. Among the anticholinergic that are used for treating COPD, the following medications have been used extensively for a very long period – aclidinium, umeclidinium, glycopyrronium, ipratropium and tiotropium. In the case of asthma, two different anticholinergic have been used extensively for treating the condition – tiotropium and ipratropium. The main properties of anticholinergics include the inhibition of receptors that are responsible for triggering the actions that cause the symptoms and conditions. This inhibition is reversible in nature and the actual action depends on the dosage of the medication. For instance, certain anticholinergics work on certain receptors, while other anticholinergics work on other receptors. Studies and data sets have revealed that anticholinergics are known to have a more effective result on both the conditions, when compared with other treatment regimen. Anticholinergics are broadly classified into short acting medications and long acting medication. The use of each type of medication actually depends on the condition and the manner in which patients are expected to respond to each medication. Some of the medications that are listed above are used only for one condition, while some medications are used for treating both the conditions. Certain medications are used for treating the condition, while certain medications are used mainly as maintenance therapy. In other words, certain types of medications are used for the purpose of managing the condition after it has been treated with a different line of treatment. Acetylcholine is responsible for the conditions that trigger COPD and asthma. The use of anticholinergic helps to significantly treat the condition by inhibiting the actions associated with acetylcholine.

Treating overactive bladder with anticholinergic agents

A considerable number of individuals suffer from a condition known as overactive bladder. As a result of this condition, individuals are known to take multiple washroom breaks. The condition also creates a situation where the individual needs to urinate multiple times in the night. There are other conditions that are attributed to frequent urination in the night, such as age related deterioration of the kidneys, or kidney problems. Individuals who do not suffer from either of the two conditions are most likely to have an overactive bladder. This condition seriously compromises the quality of life and is virtually impossible to manage through change in diet and lifestyle. The best option to treat an overactive bladder is to rely on anticholinergic medications. Specific formulations of anticholinergic medications are designed to help treat an overactive bladder. The mechanism of action of these drugs is primarily a relaxation of the bladder muscles. Additionally, the medications help to regulate the bladder spasm, which in turn helps to give more control over urination and the urge to pass urine. Typically available in oral formulations (capsules, tablets) anticholinergic medications for overactive bladder are also available as topical gel or patches that can be affixed on skin. The most commonly available anticholinergic medications for overactive bladder include the following – oxybutynin, tolterodine, fesoterodine, trospium, darifenacin, and solifenacin, among others. Most of the medications are prescribed to be taken on a daily basis. Depending upon the formulation – either immediate release medication or extended release formulation, it is necessary to take the medication multiple times in a day. The dosages of different medications need to be taken into consideration by individuals with an overactive bladder. This is especially important in the case of medications that have stronger dosage formulations. For instance, certain medications are known to have contraindications with other medications. Patients who are on medications for other conditions, need to explain the same clearly to the treating specialist. A significant number of anticholinergic medications for overactive bladder are in extended release form. This is because of the need to get the formulations to constantly exercise the anticholinergic action. The availability and use of immediate release formulations are primarily to handle the possible side effects of stronger medications. Some medications are also known to take some time before the effects are actually experienced by the patient. This could at times be as long as a couple of weeks from the time of commencing the medication. It is important that patients understand the mechanism of action and the average time taken for effects to be experienced. Lack of understanding about this, can have serious consequences. For instance, an individual who is not aware of the delayed effects, may end up opting for a higher dose or repeat dose in an attempt to experience outcomes of medication. This could in fact turn out to be an adverse reaction in some cases. It is essential for patients to stay away from alcohol during the period immediately after consumption of the oral medication. The combination of the medication with alcohol may result in impaired cognitive abilities or drowsiness. Some medications are known to have dual effects, such as treating the muscle spasm as well as the bladder spasm. Both of these actions are individually and collectively responsible for the condition. There are known side effects associated with anticholinergic medications for overactive bladder. This is especially true in the case of medications are with higher dosage or medications that come in extended release formulations. Some of the more common side effects associated with anticholinergic medications for overactive bladder include a feeling of drowsiness, dehydrated feeling in the mouth, possible constipation, inability to easily remember anything, and higher risk of enjoying oneself as a result of falling. One of the more tricky and adverse side reactions is the effect of anticholinergic agents on the heart rate. Patients are advised to seek immediate medical intervention, the moment a change in the heart rate is observed. All medications, including herbal formulations need to be brought to the notice of the specialist. This will help the doctor to alter the dosage or the formulation to ensure that no contraindications occur.

Known side effects of anticholinergic formulation

Some of the more common side effects associated with the anticholinergic medications include constipation, blurring of vision, retention of urine, dry eyes, imbalance in heart rate, business as a result of a dip in blood pressure when arising from a reclining position and memory related issues. Most of the side effects associated with anticholinergic medications are often resolved by modifying the dosage or ensuring that there is no contraindication as a result of interactions with other medications. Most of the side effects are relatively common in occurrence. As a result of these side effects, a significant percentage of elderly patients tend to discontinue use of the medication. By virtue of the nature of the medication and its use, it is important to understand that discontinuation will affect the line of treatment for which it was intended. Medical intervention will help resolve the side effects to a certain extent, helping the patient to continue the treatment without having to experience other side effects. Patients with certain pre existing conditions are categorised as high risk patients, and it is important to ensure that right medication and their prescribed dosage is used to avoid any adverse reaction. Patients with conditions such as glaucoma, dementia or other forms of cognitive impairment, abnormal or irregular heart rate, history of obstruction experienced during urination, constipation, colitis and postural hypotension are known to belong to the high risk category. Patients suffering from these conditions need coordinated and careful attention of specialists for both conditions. This will help pre-empt adverse reactions as a result of drug interaction.

The main contraindication or drug interactions of anticholinergic medications with other medications are essentially related to cholinergic agents. In other words, patients who are on medications or formulations that are known to have cholinergic actions need to avoid either of the two medications to prevent drug interaction. For instance, certain categories of medications are known to have an adverse or pronounced effect. Antihistamines that are typically used for treating asthmatic conditions, urticaria and hay fever are known to trigger adverse reactions when anticholinergic medications are taken alongside. Similarly, medications that belong to the category of potassium chloride tablets are also known to trigger adverse effects when taken alongside anticholinergic formulations. Finally, the entire category of antidepressant medications are also known to exercise some kind of adverse reaction when used in combination with anticholinergic medications.


Leave a Reply