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Testosterone Replacement, Low T, HCG, & Beyond
Testosterone Side Effect Management
Success stories for managing TRT induced increase in hematocrit?
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<blockquote data-quote="madman" data-source="post: 193249" data-attributes="member: 13851"><p>Pharmacokinetics of big pharma buccal troche.</p><p></p><p></p><p></p><p></p><p><strong><u>Testosterone Lozenges/Troches Each Striant™ lozenge (buccal system</u>) comes in a blister pack. The lozenge must be kept in the blister pack until ready for use.</strong></p><p></p><p>• Use: The lozenge has one flat side and one round side. The round side goes against the gums. The flat side goes against the cheek.</p><p></p><p>• When ready, put a lozenge in the mouth, start by putting the flat side of the lozenge on the fingertip. Place the lozenge up against the gums and to the left or right of the two front teeth. Gently push the lozenge up as high as it will go onto the gum. Take the finger out of the mouth and push on the lozenge from the outside of your upper lip for at least 30 s. The lozenge should stick to the gum. It is okay if it sticks to the cheek instead of the gum.</p><p></p><p>• Do not chew or swallow the lozenge. • Each time a new lozenge is used, put it on the side opposite from where the last lozenge was placed. If the morning lozenge was on the right side, put the evening lozenge on the left side.</p><p></p><p>• The lozenge will stay in the mouth all the time. It will get softer and slowly melt, but will not melt completely. It has to be removed after 12 h. Use the finger to gently loosen the lozenge. Then carefully slide it down along the tooth and take it out of the mouth.</p><p></p><p>• Unless changing lozenges, keep the lozenge in the mouth when eating or brushing the teeth. After eating or brushing the teeth, check to make sure the lozenge is still in place.</p><p></p><p>• Usual dose is two times a day, once in the morning and once in the evening (about 12 h apart). It may be easiest to put the lozenge on the gums after having eaten breakfast and brushing the teeth and after you have eaten the evening meal.</p><p></p><p></p><p></p><p></p><p><strong>STRIANT® (testosterone buccal system)</strong></p><p><strong>mucoadhesive</strong></p><p><strong></strong></p><p><strong></strong></p><p><strong>DESCRIPTION</strong></p><p><strong></strong></p><p><strong>Striant® (testosterone buccal system) is designed to adhere to the gum or inner cheek.<u> It provides a controlled and sustained release of testosterone through the buccal mucosa as the buccal system gradually hydrates</u>. <u>Insertion of Striant® twice a day, in the morning and in the evening, provides continuous systemic delivery of testosterone</u>.</strong></p><p><strong></strong></p><p><strong>Striant® is a white to off-white colored, monoconvex, tablet-like, mucoadhesive buccal system. Striant® adheres to the gum tissue above the incisors, with the flat surface facing the cheek mucosa.</strong></p><p><strong></strong></p><p><strong>The active ingredient in Striant® is testosterone. <u>Each buccal system contains 30 mg of testosterone</u>. Testosterone USP is practically white crystalline powder chemically described as 17-beta hydroxyandrost-4-en-3one.</strong></p><p><strong></strong></p><p><strong>Other pharmacologically inactive ingredients in Striant® are anhydrous lactose NF, carbomer 934P, hypromellose USP, magnesium stearate NF, lactose monohydrate NF, polycarbophil USP, colloidal silicon dioxide NF, starch NF, and talc USP.</strong></p><p><strong></strong></p><p><strong></strong></p><p><strong>CLINICAL PHARMACOLOGY</strong></p><p><strong></strong></p><p><strong>Striant® delivers physiologic amounts of testosterone to the systemic circulation, thereby producing circulating testosterone concentrations in hypogonadal males that approximate physiologic levels seen in healthy young men (300 - 1050 ng/dL).</strong></p><p><strong></strong></p><p><strong></strong></p><p><strong>Pharmacokinetics</strong></p><p><strong></strong></p><p><strong>Absorption</strong></p><p><strong></strong></p><p><strong><u>When applied to the buccal mucosa, Striant® slowly releases testosterone, allowing for the absorption of testosterone through gum and cheek surfaces that are in contact with the buccal system</u>.</strong> <strong>Since venous drainage from the mouth is to the superior vena cava, trans-buccal delivery of testosterone circumvents first-pass (hepatic) metabolism.</strong></p><p><strong></strong></p><p><strong><u>Following the initial application of Striant®, the serum testosterone concentration rises to a maximum within 10-12 hours</u>.</strong> <strong>The mean maximum (C max ) and mean average serum total testosterone concentrations for the 12 hour dosing period (C avg(0-12) ) are within the normal physiologic range.</strong></p><p><strong></strong></p><p><strong><u>Striant® is intended for twice-daily dosing</u>. <u>Serum concentrations of testosterone reach steady-state levels after the second dose of twice-daily Striant® dosing</u>.<u> Following removal of Striant®, the serum testosterone concentration decreases to a level below the normal range within 2-4 hours</u>.</strong></p><p><strong></strong></p><p><strong><u>With twice-daily repeated dosing, mean pharmacokinetic parameters at steady-state for total testosterone serum concentration were very similar between studies of 7-day and 12-week dosing durations</u>. Mean C avg(0-24) across the studies ranged from 520 to 550 ng/dL and these mean values were within the physiologic range</strong> (see <a href="https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=ac47efbe-025b-4688-bcd3-a10a0b012b34&type=display#table1" target="_blank">Table 1</a>).</p><p></p><p></p><p><strong>Table 1. Mean (±SD) Steady-State Serum Total Testosterone Concentrations During Treatment with Striant® (on Final Day of Treatment)</strong></p><p>[ATTACH=full]12338[/ATTACH]</p><p></p><p><strong>Although no specific food effect study was conducted, <u>pivotal Phase 3 study results showed that the consumption of food and beverage did not significantly affect the absorption of testosterone from Striant®</u>.</strong></p><p><strong></strong></p><p><strong>The effects of toothbrushing, mouth washing, chewing gum, and alcoholic beverages on the use and absorption of Striant® were not investigated in controlled studies, <u>however, Phase 3 clinical studies permitted patients to do these activities indicating the use of Striant® was not significantly affected by these activities</u>.</strong></p><p><strong></strong></p><p><strong></strong></p><p><strong></strong></p><p><strong>Clinical Studies</strong></p><p><strong></strong></p><p><strong>Striant® was evaluated in a multicenter, open-label, single-arm, Phase 3 trial in 98 hypogonadal men (Study 1). In this study, Striant® was administered twice daily for 12 weeks. The mean age was 53.6 years (range 20 to 75 years). Overall, 68 (69.4%) patients were Caucasian, 9 (9.2%) were African-American, 15 (15.3%) were Hispanic, 4 (4.1%) were Asian, and 2 (2.0%) were of another ethnic origin. At baseline, ten patients (10.2%) reported current use of tobacco, and forty-one (41.8%) drank alcohol. Of 82 patients who completed the trial and had sufficient data for full analysis, 86.6% had mean serum testosterone concentration (C avg(0-24) ) values within the physiologic range.</strong></p><p><strong></strong></p><p><strong><u>The mean (±SD) time-averaged steady-state daily testosterone concentration (C avg(0-24) ) at Week 12 was 520 (±205) ng/dL compared with a mean of 149 (±99) ng/dL at Baseline</u>.<u> At Week 12, the mean percentage of time over the 24-hour sampling period that total testosterone concentrations remained within the normal range of 300 - 1050 ng/dL was 76%</u>. Table 1 above provides the steady-state serum testosterone concentrations in greater detail.</strong></p><p><strong></strong></p><p><strong>Striant® was also evaluated in a 7-day multicenter, open-label, parallel study comparing Striant® and an approved testosterone transdermal system (Study 2). In this study, Striant® was again administered twice daily. <u>On Day 7, the mean C avg(0-24) for the 29 patients who received Striant® was 550 (±169) ng/dL compared with a mean of 119 (±78) ng/dL at Baseline</u>. <u>On Day 7, the mean percentage of time for Striant® over the 24-hour sampling period that testosterone concentrations remained within the physiologic range of 300-1050 ng/dL was 84%</u>. Additional pharmacokinetic data for this study are presented in Table 1 above.</strong></p><p></p><p><a href="https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=ac47efbe-025b-4688-bcd3-a10a0b012b34&type=display#fig1" target="_blank">Figure 1 </a><strong>below shows the mean total testosterone serum concentration versus time at steady-state for two representative consecutive dosing intervals from both the 7-day and 12-week studies. The figure shows that the concentration-time curves for the different duration studies are consistent.</strong></p><p><strong></strong></p><p><strong></strong></p><p><strong>Figure 1: Mean (SD) total testosterone concentration-time curves for two consecutive dosing intervals at steady-state for both the 12- week study (Study 1) and the 7-day study (Study 2) of Striant®. (The horizontal dotted lines represent the upper and lower limit of normal for the normal physiologic range in healthy adult males).</strong></p><p>[ATTACH=full]12339[/ATTACH]</p><p></p><p><strong><u>In both clinical trials, mean DHT concentrations increased in parallel with testosterone concentrations, with the total testosterone/DHT ratio (9 - 12) indicating no alteration in the metabolism of testosterone to DHT in testosterone deficient men treated with Striant® as compared with young, healthy eugonadal men</u>.</strong></p><p><strong></strong></p><p><strong><u>During continuous treatment, there was no accumulation of testosterone, and mean total testosterone, free testosterone, and DHT were maintained within their physiologic ranges</u>.</strong></p></blockquote><p></p>
[QUOTE="madman, post: 193249, member: 13851"] Pharmacokinetics of big pharma buccal troche. [B][U]Testosterone Lozenges/Troches Each Striant™ lozenge (buccal system[/U]) comes in a blister pack. The lozenge must be kept in the blister pack until ready for use.[/B] • Use: The lozenge has one flat side and one round side. The round side goes against the gums. The flat side goes against the cheek. • When ready, put a lozenge in the mouth, start by putting the flat side of the lozenge on the fingertip. Place the lozenge up against the gums and to the left or right of the two front teeth. Gently push the lozenge up as high as it will go onto the gum. Take the finger out of the mouth and push on the lozenge from the outside of your upper lip for at least 30 s. The lozenge should stick to the gum. It is okay if it sticks to the cheek instead of the gum. • Do not chew or swallow the lozenge. • Each time a new lozenge is used, put it on the side opposite from where the last lozenge was placed. If the morning lozenge was on the right side, put the evening lozenge on the left side. • The lozenge will stay in the mouth all the time. It will get softer and slowly melt, but will not melt completely. It has to be removed after 12 h. Use the finger to gently loosen the lozenge. Then carefully slide it down along the tooth and take it out of the mouth. • Unless changing lozenges, keep the lozenge in the mouth when eating or brushing the teeth. After eating or brushing the teeth, check to make sure the lozenge is still in place. • Usual dose is two times a day, once in the morning and once in the evening (about 12 h apart). It may be easiest to put the lozenge on the gums after having eaten breakfast and brushing the teeth and after you have eaten the evening meal. [B]STRIANT® (testosterone buccal system) mucoadhesive DESCRIPTION Striant® (testosterone buccal system) is designed to adhere to the gum or inner cheek.[U] It provides a controlled and sustained release of testosterone through the buccal mucosa as the buccal system gradually hydrates[/U]. [U]Insertion of Striant® twice a day, in the morning and in the evening, provides continuous systemic delivery of testosterone[/U]. Striant® is a white to off-white colored, monoconvex, tablet-like, mucoadhesive buccal system. Striant® adheres to the gum tissue above the incisors, with the flat surface facing the cheek mucosa. The active ingredient in Striant® is testosterone. [U]Each buccal system contains 30 mg of testosterone[/U]. Testosterone USP is practically white crystalline powder chemically described as 17-beta hydroxyandrost-4-en-3one. Other pharmacologically inactive ingredients in Striant® are anhydrous lactose NF, carbomer 934P, hypromellose USP, magnesium stearate NF, lactose monohydrate NF, polycarbophil USP, colloidal silicon dioxide NF, starch NF, and talc USP. CLINICAL PHARMACOLOGY Striant® delivers physiologic amounts of testosterone to the systemic circulation, thereby producing circulating testosterone concentrations in hypogonadal males that approximate physiologic levels seen in healthy young men (300 - 1050 ng/dL). Pharmacokinetics Absorption [U]When applied to the buccal mucosa, Striant® slowly releases testosterone, allowing for the absorption of testosterone through gum and cheek surfaces that are in contact with the buccal system[/U].[/B] [B]Since venous drainage from the mouth is to the superior vena cava, trans-buccal delivery of testosterone circumvents first-pass (hepatic) metabolism. [U]Following the initial application of Striant®, the serum testosterone concentration rises to a maximum within 10-12 hours[/U].[/B] [B]The mean maximum (C max ) and mean average serum total testosterone concentrations for the 12 hour dosing period (C avg(0-12) ) are within the normal physiologic range. [U]Striant® is intended for twice-daily dosing[/U]. [U]Serum concentrations of testosterone reach steady-state levels after the second dose of twice-daily Striant® dosing[/U].[U] Following removal of Striant®, the serum testosterone concentration decreases to a level below the normal range within 2-4 hours[/U]. [U]With twice-daily repeated dosing, mean pharmacokinetic parameters at steady-state for total testosterone serum concentration were very similar between studies of 7-day and 12-week dosing durations[/U]. Mean C avg(0-24) across the studies ranged from 520 to 550 ng/dL and these mean values were within the physiologic range[/B] (see [URL='https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=ac47efbe-025b-4688-bcd3-a10a0b012b34&type=display#table1']Table 1[/URL]). [B]Table 1. Mean (±SD) Steady-State Serum Total Testosterone Concentrations During Treatment with Striant® (on Final Day of Treatment)[/B] [ATTACH type="full" alt="Screenshot (3120).png"]12338[/ATTACH] [B]Although no specific food effect study was conducted, [U]pivotal Phase 3 study results showed that the consumption of food and beverage did not significantly affect the absorption of testosterone from Striant®[/U]. The effects of toothbrushing, mouth washing, chewing gum, and alcoholic beverages on the use and absorption of Striant® were not investigated in controlled studies, [U]however, Phase 3 clinical studies permitted patients to do these activities indicating the use of Striant® was not significantly affected by these activities[/U]. Clinical Studies Striant® was evaluated in a multicenter, open-label, single-arm, Phase 3 trial in 98 hypogonadal men (Study 1). In this study, Striant® was administered twice daily for 12 weeks. The mean age was 53.6 years (range 20 to 75 years). Overall, 68 (69.4%) patients were Caucasian, 9 (9.2%) were African-American, 15 (15.3%) were Hispanic, 4 (4.1%) were Asian, and 2 (2.0%) were of another ethnic origin. At baseline, ten patients (10.2%) reported current use of tobacco, and forty-one (41.8%) drank alcohol. Of 82 patients who completed the trial and had sufficient data for full analysis, 86.6% had mean serum testosterone concentration (C avg(0-24) ) values within the physiologic range. [U]The mean (±SD) time-averaged steady-state daily testosterone concentration (C avg(0-24) ) at Week 12 was 520 (±205) ng/dL compared with a mean of 149 (±99) ng/dL at Baseline[/U].[U] At Week 12, the mean percentage of time over the 24-hour sampling period that total testosterone concentrations remained within the normal range of 300 - 1050 ng/dL was 76%[/U]. Table 1 above provides the steady-state serum testosterone concentrations in greater detail. Striant® was also evaluated in a 7-day multicenter, open-label, parallel study comparing Striant® and an approved testosterone transdermal system (Study 2). In this study, Striant® was again administered twice daily. [U]On Day 7, the mean C avg(0-24) for the 29 patients who received Striant® was 550 (±169) ng/dL compared with a mean of 119 (±78) ng/dL at Baseline[/U]. [U]On Day 7, the mean percentage of time for Striant® over the 24-hour sampling period that testosterone concentrations remained within the physiologic range of 300-1050 ng/dL was 84%[/U]. Additional pharmacokinetic data for this study are presented in Table 1 above.[/B] [URL='https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=ac47efbe-025b-4688-bcd3-a10a0b012b34&type=display#fig1']Figure 1 [/URL][B]below shows the mean total testosterone serum concentration versus time at steady-state for two representative consecutive dosing intervals from both the 7-day and 12-week studies. The figure shows that the concentration-time curves for the different duration studies are consistent. Figure 1: Mean (SD) total testosterone concentration-time curves for two consecutive dosing intervals at steady-state for both the 12- week study (Study 1) and the 7-day study (Study 2) of Striant®. (The horizontal dotted lines represent the upper and lower limit of normal for the normal physiologic range in healthy adult males).[/B] [ATTACH type="full" alt="Screenshot (3121).png"]12339[/ATTACH] [B][U]In both clinical trials, mean DHT concentrations increased in parallel with testosterone concentrations, with the total testosterone/DHT ratio (9 - 12) indicating no alteration in the metabolism of testosterone to DHT in testosterone deficient men treated with Striant® as compared with young, healthy eugonadal men[/U]. [U]During continuous treatment, there was no accumulation of testosterone, and mean total testosterone, free testosterone, and DHT were maintained within their physiologic ranges[/U].[/B] [/QUOTE]
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Testosterone Replacement, Low T, HCG, & Beyond
Testosterone Side Effect Management
Success stories for managing TRT induced increase in hematocrit?
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