Limitations Of Cialis

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Cialis is the brand name of tadalafil, and it belongs to the class of medicines called phosphodiesterase type 5 inhibitors.

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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.
Cialis received the approval to be used in Europe in 2002 and in the United States of America in 2003.
Four phosphodiesterase type 5 inhibitors are available on market: Sildenafil, Vardenafil Tadalafil and Avanafil.
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.
Due to its terminal half-life of 17.5 hours, Cialis is nicknamed the”weekend pill”.

 

What is erectile dysfunction?

The National Institute of Health defines the erectile dysfunction as the persistent inability to achieve or maintain an erection sufficient for satisfactory sexual performance.
Erectile dysfunction has a significant impact on the physical and psychological health of men worldwide and can also affect the quality of life of both the sufferers and their partners.
Erectile dysfunction (ED) affects 50% of men older than 40 years and it has a substantial effect on quality of life.
Multiple body systems are involved in the pathophysiology of erectile dysfunction, including neuronal, hormonal, mechanical and psychological.
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 venous-occlusive mechanism.

 

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Which are the risk factors involved in erectile dysfunction?

The most common causes of erectile dysfunction include:

  • heart disease and narrowing of blood vessels
  • diabetes
  • high blood pressure
  • high cholesterol
  • obesity and metabolic syndrome
  • Parkinson’s disease
  • multiple sclerosis
  • hormonal disorders including thyroid conditions and testosterone deficiency
  • structural or anatomical disorder of the penis, such as Peyronie disease
  • smoking, alcoholism, and substance abuse, including cocaine use
  • treatments for prostate disease
  • surgical complications
  • injuries in the pelvic area or spinal cord
  • radiation therapy to the pelvic region.

Drugs that could be involved in the occurrence of erectile dysfunction are:

  • drugs to control high blood pressure
  • heart medications (digoxin)
  • some diuretics
  • drugs that act on the central nervous system, including some sleeping pills and amphetamines
  • anxiety treatments
  • antidepressants (monoamine oxidase inhibitors, selective serotonin reuptake inhibitors and tricyclic antidepressants)
  • opioid painkillers
  • some cancer drugs, including chemotherapeutic agents
  • prostate treatment drugs
  • anticholinergics
  • hormone drugs
  • the peptic ulcer medication (cimetidine)

 

Treatment of erectile dysfunction

Nowadays, selective phosphodiesterase type 5 inhibitors (PDE5Is) are the mainstay of treatment for erectile dysfunction. These medications are highly efficacious, are well tolerated, and have very favourable safety profiles. Four phosphodiesterase type 5 inhibitors are available on market: sildenafil (Viagra®, Pfizer), vardenafil (Levitra®, Bayer), tadalafil (Cialis®, Lilly-ICOS) and avanafil (Stendra®). These agents do not directly cause penile erections but instead affect the response to sexual stimulation. Sildenafil was the first in this series of phosphodiesterase type 5 inhibitors. The newest phosphodiesterase type 5 inhibitor is avanafil, which was launched in the UK in March 2014. Each of these drugs is highly efficacious in the management of erectile dysfunction although pharmacokinetic and side-effect profiles differ and results for each drug may vary for individual men.
Phosphodiesterase type 5 inhibitors are recommended as the first-line therapy for erectile dysfunction. According to the European guidelines the choice between a short-acting phosphodiesterase type 5 inhibitor and a long-acting phosphodiesterase type 5 inhibitor depends on the frequency of intercourse (occasional use or regular therapy, 3-4 times weekly) and the patient’s personal experience.

 
What is Cialis?

Cialis is the brand name for tadalafil, a drug used to treat erectile dysfunction. It is similar to Viagra, Spedra and Levitra. Under the brand name Adcirca, tadalafil is used for pulmonary arterial hypertension.
Cialis belongs to a class of drugs called phosphodiesterase type 5 inhibitors. Cialis increases blood flow to the penis, and this enables a man to achieve an erection. Cialis is not effective without sexual stimulation. It should be used with caution, and only under medical supervision.
Tadalafil was approved by the European Medicine Agency (EMA) in 2002 and by the United States Food and Drug Administration (FDA) in 2003 for the treatment of erectile dysfunction. Tadalafil is also used to treat pulmonary arterial hypertension and benign prostatic hyperplasia, a condition in which the prostate gland becomes enlarged, causing problems with urination.

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How does Cialis work?

Tadalafil is a selective, reversible inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). 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).
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 smooth muscle. Following this process, it results in arterial dilatation, venous constriction, and the rigidity of penile erection.
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.
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.

 

Pharmacokinetic profile of Cialis (tadalafil)

After oral administration, tadalafil is easily absorbed and the mean maximum observed plasma concentration (Cmax) is achieved at a median time of 2 hours after dosing. 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. Tadalafil absorption differs from other phosphodiesterase types 5 inhibitors like sildenafil and vardenafil and it does not appear to be influenced by fatty meals and alcohol.
The mean volume of distribution is approximately 63 l, indicating that tadalafil is distributed into tissues. At therapeutic concentrations, 94% of tadalafil in plasma is bound to proteins. Protein binding is not affected by impaired renal function. Less than 0.0005% of the administered dose appeared in the semen of healthy subjects.
Tadalafil is predominantly metabolised by the cytochrome P450 (CYP) 3A4 isoform. First, tadalafil is metabolized to a catechol metabolite and further, the drug is metabolized to its major circulating metabolite, methylcatechol glucuronide. This metabolite is at least 13,000-fold less potent than tadalafil for the enzyme phosphodiesterase type 5. For this reason, tadalafil is not expected to be clinically active at observed metabolite concentrations.
Compared with other phosphodiesterase types 5 inhibitors, tadalafil is unique due to its long elimination half-time of approximately 18 hours. The prolonged half-life of tadalafil makes it suitable for daily dosing.
After taking a single tablet of tadalafil, the drug remains in your body for more than 2 days and it can remain longer at patients who suffer from kidney or liver problems.
Tadalafil is excreted predominantly as inactive metabolites, mainly in the faeces (approximately 61% of the dose) and to a lesser extent in the urine (approximately 36% of the dose).
Pharmacokinetics determined with a population approach in patients with erectile dysfunction is similar to pharmacokinetics in subjects without erectile dysfunction.

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Cialis side effects

Cialis oral tablet does not usually cause drowsiness, but it can cause other side effects.
More common side effects:

  • headaches
  • upset stomach
  • back pain
  • muscle aches
  • flushing (reddish skin)
  • stuffy or a runny nose
  • diarrhoea

If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.
Uncommon side effects:

  • 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,
  • nosebleeds,
  • ringing in the ears,
  • swelling of the hands, feet or ankles and
  • feeling tired.

Rare effects:

  • 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.

Serious side effects:
Call your doctor right away if you have serious side effects. Serious side effects and their symptoms can include the following:

  • Priapism (in men)
  • a prolonged and possibly painful erection that won’t go away
  • Vision changes
  • seeing a shade of blue when looking at objects
  • trouble telling the difference between the colours blue and green
  • a sudden decrease or loss of vision in one or both eyes
  • Hearing loss
  • a sudden loss or decrease in hearing
  • ringing in the ears
  • dizziness
  • Low blood pressure.
  • feeling lightheaded or dizzy
  • fainting
  • Angina (chest pain)

Limitation of Cialis. When is it not recommended to take Cialis?

It is important to know that you should take Cialis only with a prescription from your doctor. To ensure if this drug is safe for you, your doctor should evaluate your health condition.
Before taking Cialis, tell your doctor or your pharmacist if you suffer or ever suffered from:

  • 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 loses including NAION (Non-Arteritic Anterior Ischemic Optic Neuropathy),
  • stomach ulcer,
  • bleeding problems
  • a deformed penis shape,
  • retinitis pigmentosa, a rare genetic (runs in families) eye disease
  • blood cell problems like sickle cell anaemia, multiple myeloma, or leukaemia.

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Do not take tadalafil if you are taking the following drugs:

  • Nitrates (glyceryl trinitrate, isosorbide mononitrate, isosorbide dinitrate) and nitric acid donors (amyl nitrite nicorandil or sodium nitroprusside): these drugs are used in the treatment of angina pectoris or heart failure. The co-administration of Cialis with nitrates is contraindicated because Cialis was shown to potentiate the hypotensive effects of nitrates, leading to a dangerous fall in blood pressure.
  • Guanylate cyclase stimulators (riociguat): the co-administration may potentially lead to symptomatic hypotension.
  • Ritonavir, a drug used in the treatment of HIV infection: it is contraindicated to take Cialis when you are taking ritonavir because ritonavir has inhibitory effects in the enzyme CYP3A4 which is responsible for Cialis metabolism. Pharmacokinetic analysis of clinical trial data indicated a reduction in Cialis clearance when co-administered with CYP3A4 inhibitors.
  • Alpha-blockers (alfuzosin, doxazosin, tamsulosin), drugs used to treat urinary problems due to an enlarged prostate or occasionally high blood pressure.
  • Medicines for fungal infections (ketoconazole, intraconazole).
  • Erythromycin.
  • Any other treatment for erectile dysfunction

According to the Summary of Product Characteristics, healthy elderly subjects (65 years or over), had a lower oral clearance of tadalafil relative to healthy subjects aged 19 to 45 years. However, this effect of age is not clinically significant and does not warrant a dose adjustment.
In clinical pharmacology studies using single-dose tadalafil (5 to 20 mg), tadalafil exposure approximately doubled in subjects with mild (creatinine clearance 51 to 80 ml/min) or moderate (creatinine clearance 31 to 50 ml/min) renal impairment and in subjects with an end-stage renal disease on dialysis. In haemodialysis patients, Cmax was 41 % higher than that observed in healthy subjects. Haemodialysis contributes negligibly to tadalafil elimination.

 

How should I take Cialis?

Cialis comes as a tablet to be taken orally. It can be taken with or without food.
In erectile dysfunction, there are 2 different ways to take Cialis either daily or on an as-needed basis. Cialis for daily use comes as tablets of 2.5 mg and 5 mg, while Cialis for use as needed comes as tablets of 5 mg, 10 mg and 20 mg.
The pill should not be split, crushed, or chewed. It should be swallowed whole with a glass of water.
Cilais for use as needed should be taken 30 minutes before sexual activity and not more often than once every 24 hours. In this case, the first dose recommended is 10 mg. The dose should be adjusted depending on how you respond to the treatment. The dose could be increased to 20 mg or reduced to 5 mg depending on the efficacy and tolerability. The maximum dose of Cialis is 20 mg as a single dose.
Cialis for daily use does not necessarily need to be taken before sex, but it needs to be taken at the same time every day. This provides erectile potency 24 hours per day and can be used by men who anticipate engaging in intercourse two or more times per week. The indicated dose is 2.5 mg, but it can be increased to 5 mg based upon the efficacy and tolerability.

 

What should I take if Cialis is not good for me?

Sedentary lifestyle, smoking and obesity are important risk factors for erectile dysfunction. For this reason, changes in your lifestyle can have a good influence on your erectile function.
The following changes may be helpful for patients with erectile dysfunction:

  • eating a balanced diet;
  • maintaining a healthy body weight;
  • engaging in regular exercises;
  • quitting smoking;
  • avoiding to much alcohol and illicit drugs;
  • seeking help for emotional and physiological issues.

Also, natural remedies could be an option. Natural remedies for erectile dysfunction include:

  • Arginine;
  • Ginseng;
  • Horny goad weed;
  • Ginkgo Biloba.

 

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References:

  1. http://www.ema.europa.eu/Cialis- Summary of product characteristics
  2. http://www.cialis-database.com/description/the-history-of-cialis.html
  3. Al-Shaiji TF, Brock GB. Phosphodiesterase type 5 inhibitors for the management of erectile dysfunction: preference and adherence to treatment. Curr Pharm Des. 2009;15(30):3486-95.
  4. Gurtner K, Saltzman A, Hebert K, Laborde E. Erectile Dysfunction: A Review of Historical Treatments With a Focus on the Development of the Inflatable Penile Prosthesis. American Journal of Men’s Health. 2015;11(3):479-486.
  5. K. Hatzimouratidis (Chair), F. Giuliano, I. Moncada, A. Muneer, A. Salonia (Vice-chair), P. Verze EAU Guidelines on Erectile Dysfunction, Premature Ejaculation, Penile Curvature and Priapism
  6. Bella A, Lee J, Carrier S, Bénard F, Brock G. 2015 CUA Practice guidelines for erectile dysfunction. Canadian Urological Association Journal. 2015;9(1-2)
  7. DeLay K, Haney N, Hellstrom W. Modifying Risk Factors in the Management of Erectile Dysfunction: A Review. The World Journal of Men’s Health. 2016;34(2):89. Risk factors
  8. K. Hatzimouratidis (Chair), F. Giuliano, I. Moncada, A. Muneer, A. Salonia (Vice-chair), P. Verze EAU Guidelines on Erectile Dysfunction, Premature Ejaculation, Penile Curvature and Priapism
  9. https://www.medicalnewstoday.com/articles/5702.php
  10. Corbin J. Mechanisms of action of PDE5 inhibition in erectile dysfunction. International Journal of Impotence Research. 2004;16(S1): S4-S7. Mechanism
  11. https://emedicine.medscape.com/article/444220-clinical?src=refgatesrc1#showall
  12. https://www.medicalnewstoday.com/articles/314348.php

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