TADALAFIL (Cialis): What is used for?

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What is Tadalafil?

Tadalafil is an active ingredient used for the treatment of erectile dysfunction in adults and pulmonary arterial hypertension.

The brand names of Tadalafil in the United States are: Cialis, Adcirca and Alyq.

Tadalafil’s mechanism of action (MOA)

Potent and selective inhibitor of phosphodiesterase 5 (PDE5), an enzyme of the corpora cavernosa responsible for the degradation of cGMP.

Therapeutic indications, uses and benefits of Tadalafil

• Erectile dysfunction in adults.
• Treatment of signs and symptoms of benign prostatic hyperplasia in adult men including those with erectile dysfunction (5 mg dose only).
• Pulmonary arterial hypertension (PAH) functional class II and III (WHO) in adults to improve exercise capacity (efficacy has been demonstrated in idiopathic PAH and PAH associated with connective tissue disease).

Dosage of Tadalafil

Oral Dose

Adults and the elderly:

– Erectile dysfunction: 10 mg/ at least 30 min before expected sexual activity, with or without food; if no adequate effect occurs, increase to 20 mg. Max. frequency 10-20 mg/day (1 dose/day). Not recommended for daily use. In patients who foresee more frequent use (at least 2 times/week) recommended dose: 5 mg/day, at the same time. The dose may be reduced to 2.5 mg/day, depending on tolerability.

– Benign prostatic hyperplasia in adult men: 5 mg/day, at the same time, with or without food.

Severe renal failure: maximum 10 mg. Not recommended with severe renal failure doses of 2.5 or 5 mg daily.
Liver failure: max. 10 mg.
Severe liver failure: limited data (assess benefit/risk).

– PAH: 40 mg /1 time daily, with or without food. Mild-moderate renal failure: 20 mg/day, based on efficacy and tolerability increase to 40 mg/day.
Mild-moderate liver failure: 20 mg (assess risk/benefit).

Mode of administration of Tadalafil

Oral use

a) Erectile dysfunction: administer with or without food. However, you may notice that it takes a little longer to take effect if taken with a large meal. Drinking alcohol may temporarily impair your ability to get an erection.

b) Pulmonary Arterial Hypertension: Administer with or without food.

Contraindications of Tadalafil

• Hypersensitivity, history of cardiovascular disease.
• AMI in the previous 90 days, hypotension (blood pressure <90/50 mm Hg), treatment with any form of organic nitrate, patients presenting vision loss due to anterior ischemic non-arteritic optic neuropathy independently or not of previous exposure to a PDE5 inhibitor.
• Unstable angina or angina produced during sexual activity,  heart failure corresponding to class II or higher in the previous 6 months, uncontrolled arrhythmias or uncontrolled ETS, stroke in the previous 6 months.
• Joint administration of PDE5 inhibitors, including tadalafil, with guanylate cyclase stimulators, such as riociguat, as it can potentially produce symptomatic hypotension.

Warnings and precautions with Tadalafil

Liver failure (assess risk benefit), severe renal failure (not recommended), anatomic deformity of the penis (angulation, cavernous fibrosis, Peyronie’s disease) or history predisposing to priapism (sickle cell anemia, multiple myeloma or leukemia).

Not recommended in: cardiovascular disease (clinically significant aortic and mitral valve disease, pericardial constriction, restrictive or congestive cardiomyopathy, significant left ventricular dysfunction, arrhythmias, symptomatic coronary heart disease, uncontrolled ETS), venous occlusive lung disease, retinitis pigmentosa.

Risk of visual disturbances and cases of non-arteritic anterior ischemic optic neuropathy. Before starting treatment, rule out the presence of prostate carcinoma.

Not recommended combination with: alpha blockers (doxazosin), nor with other PDE5 inhibitors or other tto. for erectile dysfunction, nor in patients who are chronically taking potent inducers (rifampicin) or potent inhibitors (ketoconazole or ritonavir) of CYP3A4.
Risk of priapism (see a doctor if you experience erections of 4 hours or more).

Warnings and precautions in patients with treatment with bosentan or with prostacyclins or their analogues. Avoid excessive alcohol consumption.
Concomitant use with antihypertensives, adjust doses of the latter.
Effectiveness is unknown in patients with spinal cord injuries and undergoing pelvic surgery or radical prostatectomy without preservation of neurovascular fascicles.

Not recommended in < 18 years. If cardivascular symptoms appear at the onset of sexual activity, it is recommended not to continue and inform the specialist.

Liver failure

– Erectile dysfunction: precaution in hepatic insufficiency, recommended 10 mg. In severe liver failure, limited data (evaluate benefit/risk); daily administration regimen has not been studied.

– Pulmonary arterial hypertension: mild-moderate cirrhosis: after single doses of 10 mg, consider starting dose of 20 mg (risk/benefit assessment). Not recommended in severe hepatic insufficiency.

Renal Insufficiency

– Erectile dysfunction: caution in severe renal failure, max. 10 mg (daily administration not recommended).

– Pulmonary arterial hypertension: severe renal insufficiency: not recommended. Mild-moderate renal insufficiency: initial 20 mg/day, based on efficacy increase 40 mg/day.

Tadalafil Interactions

Plasma concentration decreased by: phenobarbital, phenytoin, carbamazepine, rifampicin.

Pregnancy and Tadalafil

Limited data on pregnant women. Avoid during pregnancy.

Breastfeeding

Pharmacodynamic/toxicological data available in animals have shown tadalafil excretion in milk.
A risk in the nursing baby cannot be excluded.
It should not be used during lactation.

Effects on driving ability

There have been no studies of the effects on the ability to drive and use machines.
Although in clinical trials the frequency of notification of dizziness was similar in the two treatment arms, tadalafil and placebo, patients should consider how they react before driving or using machines.

Adverse reactions and side effects of Tadalafil

Hypersensitivity reactions; headache, syncope, migraine; blurred vision; chest pain, palpitations, flushing, hypotension.

Nasopharyngitis (including nasal congestion, sinus congestion, and rhinitis), epistaxis; nausea, dyspepsia (including abdominal pain/discomfort), vomiting, gastroesophageal reflux; rash.

Myalgia, back pain in extremities (including discomfort in extremities); increased uterine bleeding; facial edema, peripheral edema, fatigue; chest pain; diarrhea at > 65 years.

⭐⭐⭐⭐⭐ VIDEO OF TADALAFIL/CIALIS (DRUG)

Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).

In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.

Resources:

UNII: 742SXX0ICT
ChemIDplus
DrugPortal
PubChem CID: 110635
NCI Thesaurus: C47743