Tadalafil and sildenafil are well known as the active ingredients in Cialis and Viagra for treating erectile dysfunction. The commercially available tadalafil and sildenafil are in tablet form. Compounding pharmacies are able to make these drugs in the form of troches. This drug form is preferred by many patients and may provide a more rapid onset of action that is not affected by food ingestion.

Tadalafil and Sildenafil Tablets – Oral Administration

Tadalafil and sildenafil are PDE5 inhibitors used to treat erectile dysfunction. These types of medications work by improving blood flow the penis. They inhibit the breakdown of cGMP in smooth muscle of the corpus cavernosum, which the effect of vasodilation and improved erection. This effect is dependent on blood flow to the penis so there will not be an effect without sexual stimulation. As far as treatments for erectile dysfunction go, PDE5 inhibitors are the gold standard and work for many men.

Millions of prescriptions have been written for tadalafil and sildenafil in their FDA approved form of a tablet for oral administration. Tablets are the preferred drug form for most drug manufacturers. They can be made shelf stable with the addition of excipients and allow for a standardized dosage form. Troches (lozenges) tend to be less shelf stable and are not as frequently found in manufactured drugs. However compounding pharmacies frequently make troches for multiple active ingredients that patients sometimes prefer.

The half life of tadalafil is longer than sildenafil and sometimes tadalafil is prescribed to be taken daily. This allows for a continuous presence of the drug in the body so that sexual activity can be more spontaneous. Sildenafil is always taken as-needed and tadalafil can be taken as-needed as well before sexual activity. Because they are absorbed in the gastrointestinal system, the effect of these tablets can vary depending on when the individual eats or drinks before or after taking them.

Tadalafil and Sildenafil Troches – Buccal Administration

Troches are a dosage form that dissolves in your mouth as opposed to being swallowed. The troche is held between the cheek and the gum line. This means that the medication avoids metabolism in the gastrointestinal tract and the medication is instead absorbed directly into the blood stream. This method is called buccal administration – in which the medication is diffused through the oral mucosa. For some drugs buccal administration provides a more rapid onset of action and better bioavailability.

Underneath the epithelium in the oral cavity is connective tissue that is rich in blood vessels. This allows drugs to be rapidly absorbed into the blood stream. The method of administration is easy for the majority of patients to use. One interesting additional benefit is that if any adverse effects are experience while the troche is in the mouth it can easily be spit out – which is less than a full dose that is producing side effects. Troches should always be used in an upright position to avoid accidental swallowing.

The absorption of a troche can be influenced by how dry the mouth is as well as pH. If the mouth is dry, there may be less absorption of the drug. If there is too much saliva, the troche may be swallowed accidentally before it is allowed to completely absorb. The use of certain medications can affect the flow of saliva. In addition, smoking can cause vasoconstriction of blood vessels in the mouth and result in decreased absorption through the oral mucosa.

Compounding pharmacies can make PDE5 inhibitors like tadalafil and sildenafil in troches with a prescription. Patients report that this method of administration provides a more rapid onset of action and more consistent effects. When you take a medication orally, its absorption can often be affected by any food or liquid that is consumed. Buccal administration allows for greater flexibility in when food can be eaten as the absorption of the medication is in the mouth and not the gastrointestinal system.

Buccal administration is not ideal if the goal is to have the medication work over an extended period of time. The buccal administration with a troche has a more immediate effect and absorbs more quickly than oral administration. For example, if you are taking tadalafil daily instead of as-needed the tablet form may be preferred. However this decision is ultimately up to the patient in communication with their doctor.

Compounding Tadalafil and Sildenafil Troches

Tadalafil is compounded in the following dosages:

• 2.5mg, 5mg troches for daily use
• 5mg, 10mg, 20mg troches for use as-needed

Sildenafil is compounded in the following dosages:

• Available in 50mg and 100mg Lozenges

Articles

Sublingual sildenafil in the treatment of erectile dysfunction: faster onset of action with less dose – International Journal of Urology

Advances in Nanoparticulate Drug Delivery Approaches for Sublingual and Buccal Administration – Frontiers in Pharmacology