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Thread: Tadalafil Citrate

  1. #1
    Super Moderator heavyiron's Avatar
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    Default Tadalafil Citrate

    Tadalafil Citrate

    What Is Tadalafil

    Cialis is a brand name for a substance with the chemical name tadalafil. It's commonly used to treat men who experience difficulty having and maintaining an erection to orgasm.

    It was first introduced in February 2003 and it was approved by the FDA on November 21, 2003. Cialis was first marketed by Lilly ICOS, a joint venture between Eli Lilly and ICOS Corporation.

    The standa​rd starting dose size is 10 milligrams. In some cases a 20 milligram dose is necessary. Tadalafil should be taken orally 30 minutes or longer before sexual activity. Do not use without a doctors prescription.

    Medical testing
    has shown that tadalafil is effective in 60%-80%, of cases when used to treat erectile dysfunction in men. Most failure cases are from men that have had some form of surgery that made getting or maintaining an erection physically impossible. During PCT a man may find it more difficult to have or maintain an erection so tadalafil is a possible solution to that problem.

    Tadalafil produces results similar to viagra, but the effects of tadalafil last longer than viagra. In addition, tadalafil can be taken on an empty stomach or with a meal. When tadalafil and Viagra were compared in a study, tadalafil allowed for more sexual frequency and that in turn raised Testosterone levels higher in the tadalafil group.

    Viagra should not be taken with high fat foods because these foods reduce absorption of viagra in the human body. Tadalafil on the other hand may be used even when dining on high fat foods, with no decrease in effects.

    How Does T
    adalafil Work

    Compounds like tadalafil, viagra, and levitra work by inhibiting a chemical called phosphodiesterase type 5. Because of their mode of action, these drugs are commonly referred to simply as PDE5 inhibitors.

    When a man gets sexually excited, it triggers cells in the penis to produce nitric oxide. The increase in nitric oxide will in turn cause production of cyclic guanosine monophosphate (cGMP). The cGMP causes arteries in part of the penis to relax and allow more blood to flow through them. The increase in blood flow causes an erection.

    If the enzyme phosphodiesterase type 5 (PDE5) is of sufficient quantity, it will attack the cGMP and erection will not be maintained. Tadalafil and other PDE5 inhibitors reduce the amount of PDE5 available to attack cGMP. With a reduction of PDE5, most men are able to maintain an erection to orgasm.

    How Long Do the Effects of T
    adalafil Last

    The effects of tadalafil have been shown to last 24 to 36 hours in a majority of users. The effects of viagra have been shown to last 4 to 6 hours in a majority of users.

    Some men like the fact that tadalafil works for up to 36 hours and allows the user and his partner to relax, forget about planning intimacy and let things happen when the moment is right.

    24 to 36 hours might seem ideal but some men report they switched back to viagra because 6 hours or less was what they preferred. I have personally have had good results from tadalafil anywhere from 1-36 hours after taking it but 24 hours seems to be a peak time for me.

    Taking tadalafil does not increase sexual desire directly and it will not give you an erection for 36 hours. Most men who take tadalafil report that for up to 36 hours after taking tadalafil, an erection can be sustained when the penis was stimulated by touch. After orgasm, the penis will usually return to its pre-aroused state.

    Some men may be able to have one or more orgasms after the first but this an exception. In most cases, within 36 hours of taking 20 milligrams of tadalafil, you will be able to get and maintain an erection to orgasm one time.

    Most men that have had more than one orgasm from a single dose say they had the first orgasm within 60-180 minutes of taking tadalafil then were able to have one or more orgasms by waiting 60 minutes or longer before any more penis stimulation was attempted. This is something the user will have to experiment with to find out their own particular climax capacity.

    Information is for educational purposes ONLY. Consult a medical doctor before using any medication. heavyiron does not advocate readers engage in any illegal activity. Research chemicals are not meant for human consumption.
    Last edited by heavyiron; August 6th, 2014 at 12:18 PM.
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  2. #2
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    Type V phosphodiesterase inhibitor treatments for erectile dysfunction increase testosterone levels.

    Carosa E, Martini P, Brandetti F, Di Stasi SM, Lombardo F, Lenzi A, Jannini EA.
    Department of Experimental Medicine, University of L'Aquila, L'Aquila, Italy.

    OBJECTIVE: Lack of sexual activity due to erectile dysfunction (ED) decreases testosterone (T) levels through a central effect on the hypothalamic-pituitary axis. In this paper we studied the effect of different type V phosphodiesterase (PDE5) inhibitor treatments for ED on the reversibility of this endocrine pattern. DESIGN: Open-label, retrospective study. PATIENTS: Seventy-four consecutive patients were treated on demand with sildenafil (Sild) (50 mg) and tadalafil (Tad) 20 mg. MEASUREMENTS: The success in sexual intercourse was recorded and total (tT) and free testosterone (fT) levels were studied before and after 3 months of treatment. RESULTS: Basal level of tT and fT were at the bottom of the normal range and LH levels were at the top of the high normal range. After treatments, this endocrine pattern was reversed in both groups. However, the T increase in Sild-treated patients was significantly lower than in those treated with Tad (4.7 +/- 2.7 vs. 5.1 +/- 0.9, P < 0.001). fT levels followed a directly proportional pattern, while the inverse was found when LH production was studied. The intercourse rate reflected this effect: in fact, the Sild group showed a 4.9 +/- 2.9/month full sexual intercourse rate while in the Tad group a significantly higher rate of sexual intercourse was found (6.9 +/- 4.6/month, P = 0.04). However, drug consumption was comparable between the groups (Sild 4.9 +/- 2.9 vs. Tad 4.4 +/- 2.8 pills/month, P = 0.72). CONCLUSIONS: As it is unlikely that the two drugs have a different direct effect on the pituitary-testis axis, this effect is probably due to the higher frequency of full sexual intercourse in the Tad-treated group, because of the drug's longer half-life.

    PMID: 15355456 [PubMed - indexed for MEDLINE]
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  3. #3
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    Five-year experience with tadalafil in the UK: an effective treatment for erectile dysfunction.

    Dinsmore W.
    Royal Victoria Hospital, Grosvenor Road, Belfast, UK. wallace.dinsmore@royalhospitals.n-i.nhs.uk

    BACKGROUND: Erectile dysfunction (ED) is a common medical condition. In the UK, approximately 2.3 million men suffer from moderate-to-severe ED, many of whom do not consult a healthcare professional about the problem. Phosphodiesterase-type 5 (PDE5) inhibitors have revolutionised treatment for ED and three such drugs are currently available: sildenafil citrate, tadalafil and vardenafil HCl. METHODS: This article reviews available information on the efficacy and safety of tadalafil for the treatment of ED, with a focus on clinical experience in the UK. RESULTS: The clinical effects of tadalafil have been shown to last for up to 36 h after administration, longer than the other PDE5 inhibitors, which are effective for only 4-5 h after dosing. Extensive clinical experience with tadalafil, worldwide and in the UK, supports its efficacy and tolerability in many patient populations, including those with comorbidities often associated with ED. CONCLUSIONS: Studies have shown that tadalafil is an effective ED treatment, regardless of disease severity and cause, patient age and presence of comorbid conditions. As the treatments for ED have evolved, patient preference has emerged as an important aspect of ED therapy.

    PMID: 19624790 [PubMed - in process]
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    A 6-month study of the efficacy and safety of tadalafil in the treatment of erectile dysfunction: a randomised, double-blind, parallel-group, placebo-controlled study in Australian men.

    McMahon CG, Stuckey BG, Lording DW, Wittert GA, Murphy A, Shin J, Sutherland PD, Palmer NR, Lowy MP, Jesudason DR, Fredlund P.
    Australian Centre for Sexual Health, St Leonards, Sydney, New South Wales 2011, Australia. cmcmahon@acsh.com.au

    The efficacy and safety of tadalafil for the treatment of erectile dysfunction (ED) were assessed in a 6-month, randomised, double-blind, placebo-controlled study. Australian men with mild, moderate or severe ED of organic, psychogenic or mixed aetiology were randomised to tadalafil 20 mg as needed (n = 93) or placebo (n = 47). Efficacy assessments included the international index of erectile function (IIEF) and the sexual encounter profile (SEP) diary. Tadalafil significantly improved erectile function compared with placebo (p < 0.001, all measures). At the end of the study, the mean per-patient proportion of successful sexual intercourse attempts (SEP question three) was 73.5% for patients treated with tadalafil and 26.8% for placebo-treated patients. Improved erections were reported by 78% of tadalafil-treated patients compared to 12.8% of placebo-treated patients. The most common treatment-emergent adverse events--headache and dyspepsia--were generally mild or moderate. Tadalafil was effective and well tolerated in Australian men with mild to severe ED.

    PMID: 15854188 [PubMed - indexed for MEDLINE]
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  5. #5
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    J Am Coll Cardiol. 2012 Aug 21;60(8):768-74. doi: 10.1016/j.jacc.2012.05.004. Epub 2012 Jul 18.

    Tadalafil for the treatment of pulmonary arterial hypertension: a double-blind 52-week uncontrolled extension study.

    Oudiz RJ, Brundage BH, Gali? N, Ghofrani HA, Simonneau G, Botros FT, Chan M, Beardsworth A, Barst RJ; PHIRST Study Group.

    Source

    Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center, Torrance, CA, USA. roudiz@labiomed.org

    Abstract

    OBJECTIVES:
    The aim of this study was to evaluate the long-term safety and durability of efficacy of tadalafil for pulmonary arterial hypertension.

    BACKGROUND:

    Tadalafil is an oral phosphodiesterase-5 inhibitor approved for PAH treatment. In the multicenter, placebo-controlled, randomized, 16-week PHIRST (Pulmonary Arterial Hypertension and Response to Tadalafil) study, tadalafil 40 mg improved exercise capacity and delayed clinical worsening.

    METHODS:

    Eligible patients from PHIRST received once-daily tadalafil 20 mg (T20 mg) or 40 mg (T40 mg) (n = 357) in the double-blind, 52-week, uncontrolled extension study (PHIRST-2); 293 patients completed PHIRST-2. Durability of efficacy was explored using the 6-min walk distance (6MWD) test. Clinical worsening and changes in World Health Organization functional class were evaluated.

    RESULTS:

    The safety profile of tadalafil in PHIRST-2 was similar to that in PHIRST, with typical phosphodiesterase-5 inhibitor adverse events. The 6MWDs achieved in PHIRST for the subset of patients receiving T20 mg and T40 mg in both PHIRST and PHIRST-2 (406 ? 67 m [n = 52] and 413 ? 81 m [n = 59] at PHIRST-2 enrollment, respectively) were maintained at PHIRST-2 completion (415 ? 80 m [n = 51] and 410 ? 78 m [n = 59], respectively). Numerically fewer patients who were on T40 mg in PHIRST and PHIRST-2 experienced World Health Organization functional class deterioration (6% [n = 5]) compared with those randomized to T20 mg (9% [n = 7]) across both studies. Post hoc analyses showed that background bosentan use and higher 6MWD at PHIRST baseline were associated with fewer clinical worsening events.

    CONCLUSIONS:

    Long-term treatment with tadalafil was well tolerated in patients with pulmonary arterial hypertension. In patients receiving either T20 mg or T40 mg, the improvements in 6MWD demonstrated in the 16-week PHIRST study appeared sustained for up to 52 additional weeks of treatment in PHIRST-2. (Pulmonary Arterial Hypertension and Response to Tadalafil Study; NCT00549302).

    Copyright 2012 American College of Cardiology Foundation. Published by Elsevier Inc. All rights reserved.

    PMID: 22818063 [PubMed - indexed for MEDLINE]
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    J Urol. 2007 Apr;177(4):1401-7.
    Tadalafil relieves lower urinary tract symptoms secondary to benign prostatic hyperplasia.

    McVary KT1, Roehrborn CG, Kaminetsky JC, Auerbach SM, Wachs B, Young JM, Esler A, Sides GD, Denes BS.
    Author information


    Abstract

    PURPOSE:

    We assessed the efficacy and safety of tadalafil dosed once daily for lower urinary tract symptoms secondary to benign prostatic hyperplasia.
    MATERIALS AND METHODS:

    Following a 4-week, single-blind, placebo run-in 281 men were randomly assigned (1:1) to 5 mg tadalafil for 6 weeks, followed by dose escalation to 20 mg for 6 weeks or 12 weeks of placebo.

    RESULTS:

    Tadalafil significantly improved the mean change from baseline in International Prostate Symptom Score at 6 weeks (5 mg tadalafil -2.8 vs placebo -1.2) and at 12 weeks (5/20 mg tadalafil -3.8 vs placebo -1.7). Larger changes were observed with inclusion of the placebo run-in at 12 weeks (5/20 mg tadalafil -7.1 vs placebo -4.5). Significant improvements were also seen in the International Prostate Symptom Score irritative and obstructive domains, the International Prostate Symptom Score quality of life index, a question about urinary symptom improvement and the Benign Prostatic Hyperplasia Impact Index (significant at 12 weeks) vs placebo. International Prostate Symptom Score and International Index of Erectile Function erectile function domain scores significantly improved in the 56% of men with lower urinary tract symptoms/benign prostatic hyperplasia who were sexually active and had erectile dysfunction. Changes in uroflowmetry parameters were similar in the placebo and tadalafil groups. Commonly reported (2% or greater) treatment emergent adverse events were "erection increased," dyspepsia, back pain, headache, nasopharyngitis and upper respiratory tract infection (each 5.1% or less). No change in post-void residual volume was seen with tadalafil treatment.
    CONCLUSIONS:

    Tadalafil once daily was well tolerated and demonstrated clinically meaningful and statistically significant symptomatic improvement for lower urinary tract symptoms/benign prostatic hyperplasia. Tadalafil also improved erectile function in men with lower urinary tract symptoms and erectile dysfunction.


    PMID: 17382741 [PubMed - indexed for MEDLINE]
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    Am J Physiol Endocrinol Metab. 2012 Apr 15;302(8):E972-8. doi: 10.1152/ajpendo.00573.2011. Epub 2012 Feb 7.

    The phosphodiesterases type 5 inhibitor tadalafil reduces the activation of the hypothalamus-pituitary-adrenal axis in men during cycle ergometric exercise.

    Di Luigi L1, Sgrò P, Baldari C, Gallotta MC, Emerenziani GP, Crescioli C, Bianchini S, Romanelli F, Lenzi A, Guidetti L.
    Author information

    Abstract

    Phosphodiesterase type 5 inhibitors may influence human physiology, health, and performance by also modulating endocrine pathways. We evaluated the effects of a 2-day tadalafil administration on adenohypophyseal and adrenal hormone adaptation to exercise in humans. Fourteen healthy males were included in a double-blind crossover trial. Each volunteer randomly received two tablets of placebo or tadalafil (20 mg/day with a 36-h interval) before a maximal exercise was performed. After a 2-wk washout, the volunteers were crossed over. Blood samples were collected at -30 and -15 min and immediately before exercise, immediately after, and during recovery (+15, +30, +60, and +90 min) for adrenocorticotropin (ACTH), β-endorphin, growth hormone (GH), prolactin, cortisol (C), corticosterone, dehydroepiandrosterone-sulfate (DHEAS), and cortisol binding globulin (CBG) assays. C-to-CBG (free cortisol index, FCI) and DHEAS-to-C ratios were calculated. Exercise intensity, perceived exertion rate, O₂ consumption, and CO₂ and blood lactate concentration were evaluated. ACTH, GH, C, corticosterone, and CBG absolute concentrations and/or areas under the curve (AUC) increased after exercise after both placebo and tadalafil. Exercise increased DHEAS only after placebo. Compared with placebo, tadalafil administration reduced the ACTH, C, corticosterone, and FCI responses to exercise and was associated with higher β-endorphin AUC and DHEAS-to-C ratio during recovery, without influencing cardiorespiratory and performance parameters. Tadalafil reduced the activation of the hypothalamus-pituitary-adrenal axis during exercise by probably influencing the brain's nitric oxide- and cGMP-mediated pathways. Further studies are necessary to confirm our results and to identify the involved mechanisms, possible health risks, and potential clinical uses.


    PMID: 22318947 [PubMed - indexed for MEDLINE]
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