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Sublingual and Buccal Medication Administration: Why Are They So Important?

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In the world of pharmaceuticals, innovative methods of drug delivery have revolutionized the way certain meds are absorbed into the body. By administering drugs through the sublingual and buccal routes, we can achieve faster onset of action, improved bioavailability, and reduced side effects. This guide explores the science behind sublingual vs buccal absorption, the administration routes, their difference, and the advantages and disadvantages of these methods. 

What are sublingual and buccal absorption?

Sublingual absorption involves placing medication under the tongue, where it rapidly dissolves and gets absorbed directly into the bloodstream through the highly permeable mucous membrane. The rich supply of blood vessels under the tongue facilitates rapid drug absorption, and the drug then enters the systemic circulation without being metabolised by the liver, which is known as the first-pass effect. Some common medications that can be administered sublingually include nitroglycerin for the treatment of angina, certain opioid analgesics for rapid pain relief, and some anti-allergy medications.

Buccal administration is particularly useful for drugs that may be destroyed by digestive enzymes or have poor oral bioavailability due to limited absorption in the gut. It involves placing a med between your gums and cheek, where it also dissolves & is absorbed into your blood. By choosing the buccal route, the drug can maintain its stability and achieve higher systemic concentrations, which can be beneficial for certain medications that are susceptible to degradation in the acidic environment of the stomach. Common examples of meds that can be administered buccally include hormone replacement therapies, certain antiviral medications, and certain antiemetic drugs.

When to administer sublingual and buccal medication?

Sublingual and buccal medication administration is particularly beneficial in certain scenarios. When quick relief is necessary, such as in emergencies or acute conditions like angina, sublingual medications can provide almost immediate effects. Buccal administration is advantageous when drugs are sensitive to digestive enzymes or have poor gastrointestinal absorption. Moreover, both methods are valuable for patients who have difficulty swallowing tablets or capsules. Certain drugs, especially those prone to degradation or inactivation in the acidic environment of the stomach, may benefit from sublingual or buccal administration. By bypassing the stomach, these medications maintain their stability and efficacy. However, it’s essential to recognise that not all medications are suitable for sublingual or buccal administration. Drugs must have specific properties, such as being lipophilic (capable of dissolving in lipids) and non-irritating to the oral mucosa.

How to administer medication: sublingual route

When administering medication via the sublingual route, follow these steps:

  • Begin by washing your hands thoroughly with soap and water. Proper hand hygiene is essential to prevent contamination of the medication and ensure patient safety. 
  • Check the medication before administering any, verify the prescription, and ensure it’s intended for sublingual use. Some meds have specific formulations for sublingual administration, while others may not be suitable due to their chemical properties or potential for irritation.
  • Prepare the patient by explaining the procedure and ensuring they understand how to take the medication sublingually. Advise not to swallow or chew the medication and to keep their mouth closed during absorption;
  • Ask the patient to sit or lie down comfortably. This position helps prevent accidental swallowing of the medication during administration;
  • Place the medication under the tongue, preferably towards the centre, where the sublingual gland is located. The sublingual gland produces saliva that aids in the dissolution and absorption of the medication.
  • Dissolution and absorption instruct the patient not to swallow or move the medication around in their mouth. The medication should be allowed to dissolve naturally under the tongue. The sublingual mucosa is highly vascular, allowing for rapid absorption of the medication into the bloodstream.

Besides, avoid eating or drinking anything until the medication is fully absorbed. Eating or drinking can wash away the medication and reduce its effectiveness.

The procedure of administering buccal medication

Here’s a step-by-step guide on the procedure of administering buccal medication:

  • Begin by washing your hands thoroughly to ensure proper hygiene and reduce the risk of contamination
  • Double-check the prescription and the medication to ensure you have the correct drug and dosage for the patient
  • Position yourself comfortably in an upright or semi-reclining position. This position allows for easy access to the buccal area and minimises the risk of accidentally swallowing the medication;
  • Choose the appropriate side of the mouth for placing the medication. Place the medication on the opposite side of the mouth from the last dose to prevent irritation of the oral mucosa;
  • Place the medication gently between the cheek and the gum at the chosen buccal site. Ensure that the drug is in direct contact with the mucous membrane;
  • Don’t chew, crush, or swallow the medication. Keep your mouth closed during the absorption process;
  • allow the medication to dissolve or be absorbed completely. 

Consider that the time required for absorption may vary depending on the specific medication. Some meds may dissolve quickly, while others might take a few minutes. Refrain from eating, drinking, or rinsing their mouth until the absorption process is finished.

Benefits and disadvantages of buccal and sublingual Absorption

Buccal and sublingual absorption has both advantages and disadvantages. Advantages of sublingual and buccal absorption:

  • Avoiding first-pass metabolism. When drugs are ingested orally, they pass through the liver before entering the systemic circulation, where they may undergo significant metabolism known as the “first-pass effect”. This metabolism can reduce the drug’s bioavailability. Sublingual and buccal administration allows drugs to bypass the liver, thus avoiding first-pass metabolism. Consequently, the drugs reach higher concentrations in the bloodstream, leading to better therapeutic outcomes;
  • Rapid onset of action. By bypassing the gastrointestinal tract and entering directly into the bloodstream, medications take effect much more quickly compared to traditional oral routes;
  • High bioavailability. Sublingual and buccal routes offer higher bioavailability compared to oral administration. Since the medication directly enters the bloodstream without passing through the liver’s first-pass metabolism, a larger portion of the drug remains active, leading to better therapeutic outcomes with lower doses;
  • Avoiding digestive enzymes. Some medications are sensitive to the acidic and enzymatic environment of the stomach, which can lead to degradation and reduced effectiveness. By utilising the sublingual or buccal route, these drugs can avoid the harsh digestive environment, maintaining their potency and efficacy;
  • Improved patient compliance. For individuals who have difficulty swallowing tablets or capsules, sublingual and buccal medications provide a more convenient and tolerable option. This can enhance patient compliance, especially in pediatric or geriatric populations where swallowing may be challenging.

A popular drug, modafinil, is available as a tablet and sublingual. Modafinil sublingual is a new method of administering wakefulness-promoting medication. Placed under the tongue, modafinil sublingual rapidly enters the bloodstream, providing faster effects than traditional oral methods. This sublingual route offers potential advantages with a quicker onset and improved bioavailability, appealing to those seeking enhanced cognitive performance. Modafinil benefits include cognitive enhancement, improved alertness, planning and decision-making skills, concentration, memory, productivity, and reduced fatigue. It’s approved to treat sleep disorders like narcolepsy, sleep apnea, and shift work sleep disorder, offering effective relief to individuals facing sleep-related challenges. However, healthy individuals can use it as a cognitive augmenter since it’s a safe med.

Disadvantages of buccal and sublingual absorption

  • Limited drug selection. Not all medications are suitable for sublingual or buccal administration. The drug must have appropriate chemical properties to facilitate absorption through the oral mucosa. As a result, the range of medications available for these routes may be limited.
  • Taste and irritation. Some medications may have an unpleasant taste or irritate the mouth, making it challenging for patients to tolerate the sublingual or buccal administration. This can affect patient compliance and acceptance of this route.
  • Risk of swallowing. Proper administration of sublingual and buccal medications requires patients to avoid swallowing or chewing the medication during absorption. In some cases, patients may inadvertently swallow the medication, leading to reduced effectiveness or undesired systemic effects.
  • Inconsistent absorption. The rate and extent of absorption through the oral mucosa can vary among individuals, leading to potential differences in drug levels. Factors such as saliva production, oral hygiene, and mucosal health can influence absorption consistency.
  • Volume limitations. The amount of medication that can be effectively administered through the sublingual or buccal route is limited due to the small surface area available for absorption. This constraint may be a challenge for drugs requiring larger doses.
  • Dosing challenges. Precise dosing can be challenging with sublingual or buccal administration, as the drug may not evenly distribute in the mouth, leading to potential variability in drug absorption.

Despite these disadvantages, sublingual and buccal absorption remain valuable options in certain clinical scenarios. Healthcare professionals carefully consider the specific characteristics of the medication and the individual patient’s needs to determine the most appropriate administration route for optimal therapeutic outcomes.

Why are buccal and sublingual bioavailability so important?

Buccal and sublingual bioavailability is of paramount importance due to the numerous advantages these routes offer in drug administration. By bypassing the digestive system and liver metabolism, medications administered through the buccal and sublingual routes can achieve higher bioavailability, leading to faster onset of action and more potent therapeutic effects. These methods are particularly valuable in emergencies, acute conditions, and cases where patients have difficulty swallowing tablets or capsules. Moreover, by preserving the drug’s integrity and avoiding degradation by digestive enzymes, buccal and sublingual absorption ensure that the full therapeutic potential of the medication is realised. Embracing these innovative drug delivery techniques opens doors to improved patient compliance, reduced side effects, and enhanced treatment outcomes, ultimately contributing to better healthcare management and patient well-being.

Tim Williamson, a psychology graduate from the University of Hertfordshire, has a keen interest in the fields of mental health, wellness, and lifestyle.

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