What is Cialis?

Feb.26, 2018 Cialis

Short facts about phosphodiesterase type 5 (PDE5) inhibitors and Cialis

It is known that the discovery of phosphodiesterase type 5 (PDE5) inhibitors was a key element in erectile dysfunction treatment.
First PDE5 inhibitor was introduced in 1998.¹
Tadalafil, as active substance and its brand name Cialis, received the approval to be used in Europe in 2002 and in the United States of America in 2003.¹
Tadalafil is a selective, reversible inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).
Cialis (tadalafil) is nicknamed the “weekend pill”.
Cialis is marketed by a joint venture of Eli Lilly and ICOS Corporation called Lilly ICOS, LLC.
Cialis coated tablets are light yellow, almond shaped and they come in doses of 2.5, 5, 10 and 20 mg.
Cialis 5 mg only is used for the treatment of benign prostatic hyperplasia

What is erectile dysfunction, and which are the risk factors?

Erectile dysfunction represents the persistent inability to attain and maintain an erection sufficient to permit satisfactory sexual performance for at least 3 months. Erectile dysfunction has a significant impact on physical and psychological health of men worldwide and can also affect the quality of life of both the sufferers and their partners.

Penile erection is a complex phenomenon which involves a delicate and coordinated balance between neurological, vascular and tissue compartments. This includes arterial dilation, relaxation of the trabecular smooth muscle, and activation of the corporeal veno-occlusive mechanism.

The most common risk factors for erectile dysfunction include cardiovascular disease, hypertension, diabetes mellitus, hyperlipidemia, hypogonadism, lower urinary tract symptoms, metabolic syndrome, depression and smoking

Erectile dysfunction affects more than 150 million men worldwide, affecting men of different ages, even younger ones

Erectile dysfunction symptoms may appear to most men as transient, but in fact, the symptomatology is persistent. It can cause a lot of frustration if not treated. Most cases that confront with erectile dysfunction don’t admit that they have this problem and refuse to get an appointment to the sexologist.

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The history of Cialis

Cialis is the brand name of tadalafil, a phosphodiesterase type 5 inhibitor used for erectile dysfunction treatment.

Research for this drug began in 1993, when the Icos, an American biotechnology company started to study a phosphodiesterase type 5 inhibitor called IC351. Phase I clinical studies were conducted in 1995 and two years later the company started the first study in patients with erectile dysfunction.

Icos and Eli Lilly and Co. tried in 1998 to market the drug for the treatment of sexual dysfunction. After two years the molecule was renamed tadalafil. It was approved in Europe in 2002 and a year later in United States. ¹

Tadalafil was approved in 2009 by Food and Drug Administration (FDA) to improve exercise ability in people with pulmonary arterial hypertension, which is a rare, life-threatening lung disorder that causes high blood pressure in the lungs. ⁵

On October 2011, the US Food and Drug Administration (FDA) approved Cialis for treating signs and symptoms of benign prostatic hyperplasia and also for simultaneous benign prostatic hyperplasia and erectile disfunction. ⁶

How do phosphodiesterase type 5 inhibitors work in the treatment of erectile dysfunction?

In the past, the treatment of erectile dysfunction was limited on vacuum-constriction devices, prosthetic implants, intracavernosal injections, and intraurethral suppositories due to poor understanding of the physiological mechanism of erection. ⁷

The development of the phosphodiesterase type 5 inhibitors represented a key point in the management of Erectile dysfunction and they have become the first line therapy, recommended by both European Association of Urology (EAU) and American Urological Association (AUA). ⁷

Phosphodiesterase type 5 is an enzyme present mostly in the smooth muscle of the corpus cavernosum that selectively claves and degrades the cyclic guanosine monophosphate (cGMP) to 5’guanosine monophosphate (5’GMP). ⁷

Nitric oxide (NO) released from nerve terminals and endothelial cells in the corpus cavernosum during sexual arousal has the role to activate guanylate cyclase. Further, guanylate cyclase converts guanosine triphosphate (GTP) into cyclic guanosine monophosphate(cGMP). Cyclic GMP activates a cGMP-dependent protein kinase (PKG). Accumulation of cGMP and its interactions with protein kinase lead reduced calcium levels and finally to the relaxation of arterial and trabecular smoothmuscle. Following this process, it results arterial dilatation, venous constriction, and the rigidity of penile erection. ^7,8

Phosphodiesterase type 5 inhibitors decrease the activity of the enzyme phosphodiesterase type 5 which normally inhibits penile erection and they are effective only in the presence of the NO stimulation pathway. ^7,8

Pharmacokinetics properties of Cialis (tadalafil)

After oral administration, Cialis is easily absorbed and the maximum plasma concentration (C_max) is achieved after 2 hours. Its absorption is not influenced by food.

Cialis is distributed into tissues and at therapeutic concentrations; it is bound to plasma proteins in proportion of 94%.

It is predominately metabolized by CYP3A4 and the metabolites are excreted in the feces (approximately 61% of the dose) and lesser in the urine (approximately 36% of the dose). ⁹

Due to its terminal half-life of 17.5 hours, Cialis could be effective for a long period of time.

Cialis side effects

The adverse reactions are generally mild in nature and self-limited by continuous use.

The most common side effects of Cialis are: headache, indigestion, back pain, muscle aches, flushing, and stuffy or runny nose.

Stop using the drug and call immediately your healthcare professional if you experience any of the following side effects:

– allergic reactions including rashes

– chest pain

– priapism, an erection that last more than 4 hours

– sudden loss of vision in one or both eyes, which could be a sign of non-arthritic anterior ischemic optic neuropathy (NAION)

– sudden decrease or loss of hearing (sometimes with ringing in the ears and dizziness)

Uncommon side effects (reported in 1 to 10 in every 10000 patients) include: 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 (reported in 1 to 10 in every 1000 patients) that have been reported are: fainting, seizures and passing memory loss, swelling of the eyelids, red eyes, sudden decrease or loss of hearing, itchy red welts on the surface of the skin, penile bleeding, presence of blood in semen and increased sweating.

Which drugs could influence the action of Cialis?

Cialis is contraindicated to be administrated with any form of organic nitrates (nitroglycerine, isosorbide dinitrate, isosorbid mononitrate, nitroprusside, amyl nitrite,), medicines used to treat angina pectoris, because it increases the hypotensive effect of the nitrates. Using Cialis with this type of drugs may cause an excessive decrease of blood pressure and finally, cardiovascular colaps.
Cialis co-administrated with alpha androgenic blocking agents (doxazosin, tamsulosin, afluzosin) is not recommended because both drugs are vasodilators with blood pressure lowering
Hypotensive effects of riociguat, a drug used to treat pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension, have been shown to be increased when administering Cialis.
Other drugs may influence the pharmacokinetic properties of Cialis:

Antiacids modify the rate of absorbtion;
Therapeutic effects and side effects could be increased by inhibitors of CYP3A4, the enzyme involved in Cialis metabolism, such as ketoconazole or HIV protease inhibitors;
The antibiotic rifampicin, a CYP3A4 inducer reduces the effects of Cialis.

How should you take Cialis?

There are two types of Cialis: for daily use (2.5 mg and 5 mg) and for use as needed (5 mg, 10 mg, 20 mg).

You should take Cialis for daily use once daily, without regard to timing of sexual activity. The indicated dose is 2.5 mg, but it can be increased to 5 mg based upon the efficacy and tolerability.

Take Cialis for use as needed prior to sexual activity. The starting dose is 10 mg, but you could increase it to 20 mg or reduce to 5 mg depending on efficacy and tolerability. Cialis for use as needed as been shown to improve erectile function compared with placebo up to 36 hours after administration.

In the treatment of benign prostatic hyperplasia, the recommended dose of Cialis is 5 mg, taken at approximately the same time every day for up to 26 weeks associated with finasteride.

Facts that you should take in consideration before taking Cialis

Do not take Cialis if you have serious hypersensitivity to Tadalafil or if you are treated with nitrates or riociguat.

Cialis can be indicated for you but cannot be the right treatment for everyone.

Before taking Cialis, tell your doctor or your pharmacist if you suffer or ever suffered of:

– serious heart diseases (angina, heart failure, irregular heartbeats, heart attack),

– pulmonary hypertension,

– low blood pressure,

– uncontrolled arterial hypertension,

– stroke,

– serious liver problem

– serious kidney problem,

– severe vision lose including NAION (Non-Arteritic Anterior Ischemic Optic Neurophary),

– stomach ulcer,

– bleeding problems

– a deformed penis shape,

– retinitis pigmentosa, a rare genetic (runs in families) eye disease

– blood cell problems like sickle cell anemia, multiple myeloma, or leukemia.

In rare instances, men taking tablets for the treatment of erectile dysfunction, including Cialis, reported a sudden decrease or loss of vision or hearing (sometimes with ringing in the ears and dizziness). It’s not possible to determine if these events are related directly to the Erectile Dysfunction tablets or to other factors.

If you have a sudden decrease or loss of vision or hearing, stop taking any tadalafil product, including Cialis and call a healthcare provider right away.

Call your healthcare provider at phone number 0161 707 6800 if you get any side effect that bothers you or one that does not go away.

Why Cialis?

Compared with other phosphodiesterase type 5 (PDE5) inhibitors like Sildenafil (Viagra) or Vardenafil (Levitra), Cialis has the advantage of a longer half-life that provides a therapeutic window of 36 hours, hence the name of the ”weekend pill”.

Patients who have tried Cialis reported less side effects and long-lasting effectiveness than patients who have tried other phosphodiesterase- type 5 -inhibitors.

Due to its effectiveness that lasts up to 36 hours, Cialis could offer nearly continuous coverage when taken on a regular basis, allowing patients and their partners to choose freely when to have sexual activities without the need of timing it.

New medical approaches of Tadalafil

Tadalafil has been reported to be effective in patients with pulmonary arterial hypertension. The double-blind, placebo-controlled study lasted for 16 weeks and it was performed on 405 patients diagnosed with pulmonary arterial hypertension.

The patients were randomized to placebo or 2.5, 10, 20, or 40 mg orally once daily. The assessed outcomes were: change from baseline to week 16 in the distance walked in 6 minutes, organization functional class, clinical worsening, and health-related quality of life.

The results showed that Tadalafil 40 mg was well tolerated and improved exercise capacity and quality of life measures and reduced clinical worsening. ¹⁰

Tadalafil was also evaluated for the prevention of cardiomyopathy at mice and golden retriever muscular dystrophy dog models of Duchenne muscular dystrophy. The results showed that prophylactic use of tadalafil delays the onset of dystrophic cardiomyopathy and it could be a potential drug for slowing the development of cardiomyopathy in Duchenne muscular dystrophy patients.¹¹

Another clinical trial was performed to evaluate the effect of combination therapy with ambrisentan and tadalafil on left and right ventricular function in patients diagnosed with systemic sclerosis associated pulmonary arterial hypertension. The study was open-label, 36 weeks long and 25 patients were enrolled. Left and right ventricular functions were assessed by cardiac magnetic resonance. According to the results, the combination therapy was associated with a significant improvement of the ventricular parameters. ¹²

Post Marketing Surveillance Clinical Research Department Japan evaluated the safety and effectiveness of tadalafil in pediatric patients with pulmonary arterial hypertension. The analysis was performed on 391 pediatric patients. Safety was assessed from the frequency of adverse drug reactions, discontinuations due to adverse events, and serious adverse drug reactions. Effectiveness measurements included change in World Health Organization (WHO) functional classification of pulmonary arterial hypertension, cardiac catheterization (pulmonary arterial pressure: PAP), and echocardiography (tricuspid regurgitation pressure gradient: TRPG). Survival rate was also measured Patients were followed for up to 2 years. Among 391 patients analyzed for safety, the overall incidence rate of ADRs was 16.6%. The common adverse drug reaction (≥1%) were headache (2.8%), abnormal hepatic function (1.3%), platelet count decreased (1.3%), and epistaxis, (1.0%). Eleven patients reported 16 serious adverse drug reactions and 3 patients died secondary to serious adverse drug reactions. For the effectiveness analysis, the incidence of World Health Organization functional class improvement at 3 months, 1 year, and 2 years after the initiation of tadalafil were 16.5%, 19.7%, and 16.3%, respectively. At last observation, both pulmonary arterial pressure and tricuspid regurgitation pressure gradient showed a statistically significant reduction at last observation. ¹³

A randomized clinical trial performed from April 2015 to June 2016 at the Shahid Chamran Hospital of Isfahan, Iran evaluated the therapeutic and side effects of tadalafil compared with sildenafil after surgery in young infants with pulmonary arterial hypertension. Forty-two patients aged between 3 and 24 months with a large septal defect and pulmonary arterial hypertension were enrolled in the study and divided into 2 equal groups. First group received oral sildenafil (1–3 mg/kg/day every 8 hours), and the second group received oral tadalafil (1 mg/kg once a day) from 7–10 days before surgery to 3–4 weeks after surgery. The drugs were administrated through a nasogastric tube in both groups. The results of the study showed that tadalafil can be considered as a safe oral therapy for preoperative and postoperative management of pulmonary arterial hypertension in young infants. In addition, due to its long half-life, tadalafil can be used once daily, compared with sildenafil with three to four times daily doses, and with an appropriate safety profile.¹⁴

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