Does Tadalafil Make You Last Longer In Bed?
Starting with the 1980s, the inhibition of cyclic nucleotide phosphodiesterase type 5 (PDE5) as a therapeutic target has received considerable attention, particularly for the treatment of male erectile dysfunction and cardiovascular diseases, e.g., angina, hypertension, and congestive heart failure.
Around the mid-1980s scientists working at the Pfizer European Research Centre were interested in potential new approaches to the treatment of several cardiovascular diseases. After several months of research, being stimulated by the demonstration of the role of PDE5 in penile erection and the recognition that PDE5 inhibition would be useful in treating male erectile dysfunction, Pfizer advanced the Viagra regulatory dossier to be approved for the treatment of erectile dysfunction (ED). Viagra was available on market starting 1998.
Despite the efficacy of sildenafil, clinically significant adverse effects have been noted, and scientists reached the conclusion that some of these side-effects may be due to a lack of selectivity of sildenafil for PDE5.
Notably, visual disturbances could appear from inhibition of the retina-specific
phosphodiesterase enzyme type 6 (PDE6), involved in vision signal transduction.
Researchers were aiming to find a highly selective inhibitor and tadalafil, nicknamed the „weekend pill” was approved after intensive clinical research, five years later, in 2003, under the brand name Cialis. Being a highly selective inhibitor of the PDE5 enzyme, tadalafil’s 36-hour effectiveness offered patients more spontaneity and has the advantage of not causing visual disorders.
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How should I take tadalafil for erectile dysfunction?
Several years after the introduction of Cialis on the market, researchers toyed with the idea of a chronic, low-dose formulation to further enhance spontaneity.
In 2008, Eli Lilly obtained approval for the once-daily administration of tadalafil.
Currently, for erectile dysfunction, there are two ways to take Tadalafil, on as needed basis or on daily basis.
Tadalafil (Cialis) for use as needed:
- Do not take it more than one time each day;
- Take one Cialis tablet before you expect to have sexual activity. You may be able to have sexual activity at 30 minutes after taking Cialis and up to 36 hours after taking it;
- Your healthcare provider may change your dose of Cialis depending on how you respond to the medicine, and on your health condition.
Tadalafil (Cialis) for once-daily use is a lower dose you take every day.
- Do not take it more than one time each day;
- Take one Cialis tablet every day at about the same time of day. You may attempt sexual activity at any time between doses;
- If you miss a dose, you may take it when you remember but do not take more than one dose per day;
- Some form of sexual stimulation is needed for an erection to happen with Cialis;
- Your healthcare provider may change your dose of Cialis depending on how you respond to the medicine, and on your health condition.
- Tadalafil may be orally administered with or without food.
- Do not split tablets: the entire dose should be taken.
- Recommended starting doses of tadalafil are 10 mg for on-demand dosing and 2.5 mg for once-daily dosing, taken as needed before sexual activity (but not more than once-daily). The dose may be increased to 20 mg or decreased to 5 mg, per its efficacy and the individual tolerability.
- Interestingly, when daily dosing of 2.5–5 mg has been compared with on-demand dosing at 10–20 mg for tadalafil, the frequency of headaches has generally been 3–5 times less in the daily treatment arms.
Tadalafil: the generic version
In 2017, the Eli Lilly patent on Cialis ended in the EU, allowing generic manufacturers to start producing their own version. The generic version of the drug is known as Tadalafil (the same as the active ingredient in Cialis).
Tadalafil is a generic drug which means that its price is not controlled by a single manufacturer. Since several manufacturers produce Tadalafil, the market is very competitive, which has helped drive down the price substantially.
Tadalafil has been proven to be a very effective treatment for erectile dysfunction with over 80% of men finding it works for them.
Mechanism of action
Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cyclic guanosine monophosphate (cGMP) in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flows into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) enhances erectile function by increasing the amount of cGMP.
The local release of nitric oxide is initiated by the presence of sexual stimulation, thus the inhibition of PDE5 by any form of tadalafil has no effect in the absence of the latter. The effect of PDE5 inhibition on cGMP concentration in the corpus cavernosum and pulmonary arteries is also observed in the smooth muscle of the prostate, the bladder and their vascular supply.
How quickly does Tadalafil work?
Upon administration, Tadalafil reaches the maximum plasma concentration in 2 hours. Although peak concentrations take 2 hours, the onset of action has been reported within 15 minutes of dosing and the efficacy may persist for up to 36 hours.
However, the length of time Tadalafil takes to work can be affected by food, alcohol and sexual stimulation.
The fact that the effects are so long-lasting has been a major selling point for Tadalafil, which branded itself as “the weekend pill.”
Many men like the fact that they can take Tadalafil Friday night, and still experience its effects Sunday morning. The extended duration of Tadalafil’s effects allows for more spontaneity and less guesswork about when to take it.
Tadalafil therapy, taken as needed before sexual activity and with no restrictions on food or the timing of sexual activity, significantly improved erectile function and patient satisfaction. Tadalafil was effective, as measured by several variables, safe and well tolerated in the treatment of men with ED over a wide demographic range.
Consistent with its 17.5 h plasma half‐life, tadalafil allowed men to successfully engage in sexual intercourse at 0.5–36 h after dosing. Such flexibility is important, as many men and their partners desire to engage in spontaneous sexual intercourse without having to plan in advance.
Thus, one of the main advantages of tadalafil compared to other PDE5 inhibitors is that it may allow most patients with ED to return to the sex life that the couples enjoyed before having ED.
Will food and drink have an effect?
As demonstrated by a clinical study, food has little or no effect on Tadalafil effects. However, it is important to be careful with grapefruit. It is recommended that you do not eat or drink grapefruit juice with Tadalafil. This is because there is a chemical in grapefruit juice which can increase the amount of Tadalafil in your bloodstream (cytochrome P450 3A4 inhibitor) that could make side-effects more likely.
Tadalafil efficacy in clinical studies
Treatment with tadalafil in men with mild to severe ED was evaluated in a randomized, multicentric, double-blind clinical study including men volunteering in sites located in UK and Italy. Volunteers have a mean age of 53 years and 80% had a history of ED of ≥ 1 year. Nearly half of the volunteers (49%) were Viagra consumers before their enrolment in the study. The mean baseline erectile function (EF) domain score was 13.5, with 40.5% of patients in the severe category. Overall 220 volunteers joined this study. Men aged ≥ 18 years who had a minimum 3‐month history of mild‐to‐severe ED of organic, psychogenic or mixed causes (as determined by the study physician), and with a steady female partner, were eligible to participate in the study. Men requiring nitrates, antiandrogens or chemotherapy during the study period were excluded
For patients with moderate or severe ED at baseline, the improvement in erectile function after tadalafil treatment was significantly higher.
This population is similar to that in the Massachusetts Male Aging Study in age and causes of ED.
The efficacy of tadalafil was shown over multiple outcomes. Volunteers treated with tadalafil had improved erections, hardness, ability to penetrate their partner’s vagina and maintenance of erection. Volunteers declared that they had better intercourse satisfaction and overall satisfaction. At the end of the study, 82% of the volunteers treated with tadalafil stated that their treatment overall had improved their erections, compared with 23% of patients treated with placebo. A similar proportion of volunteers believed that tadalafil therapy overall had improved their sexual activity.
The results confirm those observed in an integrated analysis of five tadalafil studies conducted in a wide variety of patients from around the world.
Missed Dose?
If you take Tadalafil or Cialis on a regular schedule and you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume the usual dosing schedule.
It is not recommended to take more than 1 tablet in 24 hours.
Before using this medication, tell your doctor or pharmacist your medical history, especially of:
Before initiating treatment with Tadalafil or Cialis, the ED sufferer must be carefully evaluated. A medical history and physical examination should be undertaken to diagnose erectile dysfunction and determine potential underlying causes.
Prior to initiating any treatment for erectile dysfunction, physicians should consider the cardiovascular status of their patients, since there is a degree of cardiac risk associated with sexual activity. Tadalafil has vasodilator properties, resulting in mild and transient decreases in blood pressure and should not be administered in any circumstances to patients taking nitrates.
Prolonged erection
There have been reported rare cases of prolonged erections (erections that last more than 4 hours) and priapism (painful erections greater than 6 hours in duration) This is an uncommon and undesirable effect listed in Cialis summary of the safety profile.
Priapism, if not treated promptly, can result in irreversible damage to the erectile tissue.
Patients having an erection lasting more than 4 hours, whether painful or not, should seek emergency medical attention. Tadalafil should be used with caution in patients who have conditions that might predispose them to priapism (such as sickle cell anaemia, multiple myeloma, or leukaemia), or in patients with anatomical penile deformity (such as angulation, cavernosal fibrosis, or Peyronie’s disease).
Drug interactions
Nitrates. In clinical pharmacology studies, tadalafil was shown to potentiate the hypotensive effect of nitrates. The wash-out period between any dose of nitrates and tadalafil should d be at least 48 hours.
Alpha-blockers. Caution is advised when PDE5 inhibitors are co-administered with alpha-blockers. PDE5 inhibitors, including tadalafil, and alpha-adrenergic blocking agents are both vasodilators with blood-pressure-lowering effects. When vasodilators are used in combination, an additive effect on blood pressure may be anticipated.
Antihypertensives. PDE5 inhibitors, including tadalafil, are mild systemic vasodilators. Clinical pharmacology studies were conducted to assess the effect of tadalafil on the potentiation of the blood-pressure-lowering effects of selected antihypertensive medications (amlodipine, angiotensin II receptor blockers, bendrofluazide, enalapril, and metoprolol). Small reductions in blood pressure occurred following coadministration of tadalafil with these agents compared with placebo.
Alcohol. Substantial consumption of alcohol (e.g., 5 units or greater) in combination with tadalafil can increase the potential for orthostatic signs and symptoms, including an increase in heart rate, decrease in standing blood pressure, dizziness, and headache.
What is there to know from the Patient Information Leaflet?
Related to adverse reactions observed when administering tadalafil medicinal products, some events appear more frequent and some relatively rare.
The most common side effects (seen in 1 to 10 in every 100 patients) with Cialis and Tadalafil are a headache, back pain, muscle aches, pain in arms and legs, dyspepsia, facial flushing, nasal congestion, and indigestion, which are more common at higher doses.
Uncommon side effects (seen in 1 to 10 in every 1,000 patients) include allergic reactions, such as rashes, chest pain, dizziness, stomach ache, feeling sick, being sick (vomiting), reflux, blurred vision, eye pain, difficulty in breathing, presence of blood in urine, prolonged erection, pounding heartbeat sensation, a fast heart rate, high blood pressure, low blood pressure, nose bleeds, ringing in the ears, swelling of the hands, feet or ankles and feeling tired.
Rare side effects (seen in 1 to 10 in every 10,000 patients) are sudden decrease or loss of vision or hearing, a prolonged and possibly painful erection after taking Cialis, fainting, seizures and passing memory loss, swelling of the eyelids, red eyes, sudden decrease or loss of hearing, hives (itchy red welts on the surface of the skin), penile bleeding, presence of blood in semen and increased sweating.6
Cialis and Tadalafil must not be used where sexual activity is inadvisable (e.g. in men with heart disease). It must also not be taken by patients who have ever had loss of vision because of a problem with blood flow to the nerve in the eye (non-arteritic anterior ischemic optic neuropathy, NAION).
Cialis and Tadalafil must not be taken with nitrates (a type of medicine used for angina) or medicines of the class ‘guanylate cyclase stimulators’ such as riociguat (a medicine for high blood pressure in the vessels supplying the lungs, known as pulmonary hypertension).
What if I experience a problem?
If you take more than the recommended dose, you can increase the risk of experiencing side-effects as well as adverse reactions. If you suspect a drug overdose, you should contact your healthcare provider or seek emergency medical attention right away.
If any unpleasant effects appear, please address directly to our pharmacy and to our doctor at phone number 01625 460 621.
What Tadalafil does not do:
Tadalafil does not cure erectile dysfunction. It is a treatment for erectile dysfunction;
Tadalafil does not protect you or your partner from getting sexually transmitted diseases, including Human Immunodeficiency Virus;
Tadalafil has only been approved for use in adult men, and therefore should not be taken by women or children.
How do I decide whether the daily tablets or as needed tablets will be most suitable for me?
If you are likely to have sex three or more times a week or are in a long-term relationship, the daily dose may be the best option for you. Many patients and their partners dislike the necessity of on-demand treatment for erectile dysfunction, citing a desire for greater spontaneity with sexual interactions.
If you feel you don’t need erectile dysfunction medication every time or you have sex less regularly then the as needed dose may be the best option. The 20 mg dose can be effective for up to 36 hours after and it gained the popular nickname ‘The Weekender’. So, if taken on Friday evening it could be effective until Sunday morning. Whereas the 5 mg once-daily dose is generally effective for up to 24 hours hence the requirement to take it daily for uninterrupted effectiveness.
An important remark is that the efficiency of tadalafil does not decrease even after long-term use. There are many men who use it regularly for a long time and it works well each time. So, a regular tadalafil dosage does not usually require for a dosage increase.
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References:
- Rotella, D. P. Phosphodiesterase Type 5 Inhibitors: Discovery and Therapeutic Utility. Drugs Future 2001, 26, 153-162.
- Osterloh, I. H.; Collins, M.; Wicker, P.; Wagner, G. Sildenafil Citrate (Viagra): Overall Safety Profile in 18 Double-blind, Placebo Controlled, Clinical Trials. Int. J. Clin. Pract., Suppl. 1999, 102, 3-5.
- Huang SA, Lie JD. Phosphodiesterase-5 (PDE5) Inhibitors In the Management of Erectile Dysfunction. P T. 2013 Jul;38(7):407-19. Review. PubMed PMID: 24049429; PubMed Central PMCID: PMC3776492.
- Washington SL 3rd, Shindel AW. A once-daily dose of tadalafil for erectile dysfunction: compliance and efficacy. Drug Des Devel Ther. 2010 Sep 7;4:159-71.Review. PubMed PMID: 20856843; PubMed Central PMCID: PMC2939761.
- Eardley I, Gentile V, Austoni E, Hackett G, Lembo D, Wang C, Beardsworth A.Efficacy and safety of tadalafil in a Western European population of men with erectile dysfunction. BJU Int. 2004 Oct;94(6):871-7. PubMed PMID: 15476525.
- Brock GB, McMahon CG, Chen KK et al. Efficacy and safety of tadalafil for the treatment of erectile dysfunction: results of integrated analyses. J Urol 2002; 168: 1332–6
- Feldman HA, Goldstein I,Hatzichristou DG, Krane RJ, McKinlay JB.Impotence and its medical and psychosocial correlates: results of the Massachusetts Male Aging Study. J Urol1994; 151: 54–61
- https://www.ema.europa.eu/documents/product-information/cialis-epar-product-information_en.pdf
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