ED Drugs Troches and Capsules- Recommendations

Nelson Vergel

Founder, ExcelMale.com
Thread starter #1


Compounded PDE-5 Inhibitor Compounded Formulations (Empower Pharmacy) by Dosage Form:

I. Buccal Troche

Definition: Troches are small lozenges that dissolve between the cheek and gum over a period of about 10-20 minutes. As the troche dissolves, the medication is gradually absorbed into the blood stream so that it can be absorbed more efficiently and in some cases more rapidly than if it was taken orally.
Anecdotal Benefits: Reported by some patients to have a faster onset than orally administered tablets.
Reported Negative: Some medications can leave a bitter aftertaste despite flavoring. Sometimes the troche does not completely dissolve and needs to be swallowed.
Route of Administration: Buccal administration refers to a topical route of administration by which drugs held or applied in the buccal area (in the cheek) diffuse through the oral mucosa (tissues which line the mouth) and enter directly into the bloodstream. If the troche is swallowed prior to dissolving, it will still absorb PO.
Storage: To prevent melting, troches should be stored at 70 degrees or lower. We suggest storing them in the refrigerator in warmer climates.

1. Sildenafil
Dosage form: Buccal troche
Available strength: 100 mg
Commercial version: Viagra; Revatio
Dose: Dissolve ½-1 troche between the gum and cheek (buccally) 60 min prior to sexual activity. Troches are small lozenges that dissolve between the cheek and gum over a period of about 10-20 minutes. As it dissolves, the medication is gradually absorbed into the bloodstream so that it can be absorbed more efficiently and in some cases faster than if the same medication was taken orally.

2. Tadalafil
Dosage form: Buccal troche
Available strength: 25 mg
Commercial version: Cialis
Dose: Dissolve one troche between the gum and cheek (buccally) 60 min prior to sexual activity. Do not take more than 25 mg every 36 hours. Tadalafil troches are scored and can be broken into smaller doses, this allows for a cost-effective method of administering smaller daily dosages.

3. Avanafil
Dosage form: Buccal troche
Available strength: 200 mg
Commercial version: Stendra
Dose: Dissolve one troche between the gum and cheek (buccally) 15-30 min prior to sexual activity. Based on individual efficacy and tolerability, the dose may be increased to 200 mg taken as early as approximately 15 minutes before sexual activity, or decreased to 50 mg (1/4 troche) taken approximately 30 minutes before sexual activity. The lowest dose that provides benefit should be used. The maximum recommended dosing frequency is once per day.

4. Vardenafil
Dosage form: Buccal troche
Available strength: 10 mg; 20 mg
Commercial version: Levitra
Dose: Dissolve one troche between the gum and cheek (buccally) 60 min prior to sexual activity. Recommended starting dose is 10 mg and can be increased to 20 mg depending on the patient’s tolerance.

5. Sildenafil/Testosterone
Dosage form: Buccal troche combination of sildenafil and micronized testosterone
Available strength: 20 mg/20 mg (Women) and 100 mg/100 mg (Men)
Commercial version: Available as a compounded medication only. No commercial equivalent.
Dose: Dissolve one troche between the gum and cheek (buccally) 60 min prior to sexual activity.

II. Capsules

Definition: Capsules have been used for administering medications to patients for more than a century and have an important role in drug delivery. When a primary care provider prescribes a tablet, the choice is usually, but not always, limited to commercially available products. A capsule, however, can be prepared extemporaneously, which provides dosing flexibility for the primary care provider and the pharmacist. Compounded capsules are usually gelatin based.
Benefits: Free of excipients and dyes. Can be made without fillers. Capable of sustained release, which alters the pharmacokinetics of the medication by slowing metabolism to lengthen duration of action.
Reported Negative: Cannot be broken into smaller dosages. The entire capsule must be administered at once.
Route of Administration: Taken by mouth (PO).
Storage: Room temperature.

1. Sildenafil SR
Dosage form: Sustained Release Capsule
Available strengths: 36 mg; 75 mg; 110 mg
Commercial version: Viagra; Revatio
Dose: Take 1 capsule 60min prior to sex. Allow only one dose within 24 hours. Do not combine with other PDE5 inhibitors or penile injections on the same day otherwise there is risk of priapism.

2. Tadalafil SR
Dosage form: Sustained release capsule
Available strengths: 3 mg; 7 mg; 12 mg; 25 mg
Commercial version: Cialis
Dose: Take one capsule 60min prior to sex. Do not take more than 25 mg every 36 hours. Alternatively, tadalafil can be taken daily at common doses of 3 mg- 7 mg taken at approximately the same time every day, without regard to timing of sexual activity.

3. Sildenafil/Tadalafil combination
Dosage form: Capsule
Available strength: 55 mg/12.5 mg (Sildenafil/Tadalafil)
Commercial version: Available as a compounded medication only. No commercial equivalent
Dose: Take 1 capsule 60min prior to sex. Allow only one dose within 24 hours. Do not combine with other PDE5 inhibitors or penile injections on the same day otherwise there is risk of priapism.

III. Oral Dissolvable Tablets (ODT)
Definition: An ODT is a solid dosage form that disintegrates and dissolves in the mouth (either on or beneath the tongue or in the buccal cavity) without water within 60 seconds or less. This dosage form is also helpful for patients who have difficulty swallowing.
Anecdotal Benefits: Faster onset of medication has been reported. Increased compliance in patients who have difficulty swallowing tablets. Can be taken without water.
Reported Negative: Some medications can leave a bitter aftertaste despite flavoring.
Route of Administration: Sublingual administration is when medication is placed under the tongue to be absorbed by the body. The word “sublingual” means “under the tongue.” Buccal administration involves placement of the drug between the gums and the cheek. If the troche is swallowed prior to dissolving, it will still absorb PO.
Storage: Room temperature.

1. Sildenafil
Dosage form: ODT
Available strengths: 36 mg; 75 mg; 110 mg
Commercial version: Viagra; Revatio
Dose: Place 1 tablet under tongue and dissolve sublingually 60min prior to sex. Allow only one dose within 24 hours. Do not combine with other PDE5 inhibitors or penile injections on the same day otherwise there is risk of priapism.

2. Tadalafil
Dosage form: ODT
Available strength: 3mg; 7mg; 12mg; 25 mg
Commercial version: Cialis
Dose: Place 1 tablet under tongue and dissolve sublingually 60 min prior to sexual activity. Do not take more than 25 mg every 36 hours.

3. Avanafil
Dosage form: ODT
Available strength: 100mg; 200 mg
Commercial version: Stendra
Dose: Place 1 tablet under tongue and dissolve sublingually 15min-30 min prior to sexual activity. Based on individual efficacy and tolerability, the dose may be increased to 200 mg taken as early as approximately 15 minutes before sexual activity, or decreased to 50 mg (1/2 100mg tablet) taken approximately 30 minutes before sexual activity. The lowest dose that provides benefit should be used. The maximum recommended dosing frequency is once per day.

4. Vardenafil
Dosage form: ODT
Available strength: 10 mg; 20 mg
Commercial version: Levitra
Dose: Place 1 tablet under tongue and dissolve sublingually 60 min prior to sexual activity. Recommended starting dose is 10 mg and can be increased to 20 mg depending on the patient’s tolerance.

Link: https://www.empowerpharmacy.com/erec…nction-ed.html


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#2
5. Sildenafil/Testosterone
Dosage form: Buccal troche combination of sildenafil and micronized testosterone
Available strength: 20 mg/20 mg (Women) and 100 mg/100 mg (Men)




How does a Testosterone Troches avoid first pass liver metabolism? Some goes into the blood via Buccal cavity, but how much? Is there data on Testosterone Troches? I found this but I'm highly skeptical and did not read the full paper to see what justifies the claim "The current state-of-the-art in testosterone replacement therapy comprises compounded testosterone troches..."

Compounded Testosterone Troches TO OPTIMIZE HEALTH AND THE TESTOSTERONE CONTROVERSY.


Int J Pharm Compd. 2015 May-Jun;19(3):195-203.

Abstract

As men age, testosterone levels progressively fall and inflammatory biomarkers increase. The gradual decline in testosterone production with aging, known as andropause, is common and may have deleterious effects on men including decreased overall well-being, increased sarcopenia, increased risk of cardiovascular disease, reduced sexual function, and bone loss.

Therefore, it comes as no surprise that an increasing number of men worldwide have begun requesting testosterone replacement therapy from their physicians. Occasionally, physicians discourage male patients from getting testosterone replacement therapy based on a few recent studies indicating the therapy causes cardiovascular events, including myocardial infarctions. Yet, an extensive review of the testosterone replacement therapy literature reveals that the majority of clinical studies show that properly administered testosterone replacement therapy, in which estradiol and dihydrotestosterone levels are also controlled, has no adverse effects on myocardial infarction risk.

The current state-of-the-art in testosterone replacement therapy comprises compounded testosterone troches; an aromatase inhibitor, such as generic Anastrazole, to control estradiol levels; and a 5α-reductase inhibitor, such as beneric Dutasteride or Finasteride, to control dihydrotestosterone. Compounded testosterone troches easily raise serum testosterone levels to the optimal range, are highly cost effective at $82 for a 180-day supply, and provide affordable access to testosterone replacement therapy to millions of men requesting it. Yet, the Blue Cross Blue Shield-associated firms have largely denied requests for coverage of compounded medications, including testosterone troches. Despite data demonstrating strong links between testosterone deficiency and significant comorbid conditions (including Type 2 diabetes and other metabolic syndrome diseases) as well as the health benefits of testosterone replacement therapy, some physian have been swayed against prescribing testosterone replacement therapy to their aging male patients. The testosterone controversy stems largely from poorly designed clinical studies in which patients were subjected to testosterone replacement therapy without having their estradiol and dihydrotestosterone levels properly controlled.
 
#3
Link Removed 2015 May-Jun;19(3):195-203.

The current state-of-the-art in testosterone replacement therapy comprises compounded testosterone troches; an aromatase inhibitor, such as generic Anastrazole, to control estradiol levels; and a 5α-reductase inhibitor, such as beneric Dutasteride or Finasteride, to control dihydrotestosterone. Compounded testosterone troches easily raise serum testosterone levels to the optimal range, are highly cost effective at $82 for a 180-day supply, and provide affordable access to testosterone replacement therapy to millions of men requesting it. Yet, the Blue Cross Blue Shield-associated firms have largely denied requests for coverage of compounded medications, including testosterone troches. Despite data demonstrating strong links between testosterone deficiency and significant comorbid conditions (including Type 2 diabetes and other metabolic syndrome diseases) as well as the health benefits of testosterone replacement therapy, some physian have been swayed against prescribing testosterone replacement therapy to their aging male patients. The testosterone controversy stems largely from poorly designed clinical studies in which patients were subjected to testosterone replacement therapy without having their estradiol and dihydrotestosterone levels properly controlled.
finasteride is state of the art? Uh, I think I will pass.
 
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