INDICATIONS FOR TAKING TADALAFILO CALOX 5 MG – Calox International
ADMINISTRATION ROUTE
Oral administration is the method of choice for Tadalafilo, which should be taken in a manner conducive to optimal absorption and effect.
PHARMACOLOGICAL PROPERTIES
Pharmacodynamics
Tadalafilo serves as a selective phosphodiesterase type 5 (PDE5) inhibitor, functioning primarily as a vasodilator. This makes it particularly effective for male patients dealing with erectile dysfunction, enhancing their ability to achieve and sustain an erection when sexually stimulated.
In the physiological context, PDE5 is responsible for the breakdown of cyclic guanosine monophosphate (cGMP) – a crucial molecule that is generated by the release of nitric oxide during sexual arousal. By preventing PDE5 from degrading cGMP, Tadalafilo prolongs the availability of this vasodilatory substance, thereby facilitating enhanced blood flow to the penis and assisting in erection maintenance. It is imperative to understand that Tadalafilo alone does not provoke an erection; sexual stimulation and an increase in nitric oxide are prerequisites for its efficacy.
Pharmacokinetics
Upon oral administration, Tadalafilo is swiftly absorbed through the gastrointestinal tract, reaching peak plasma levels within approximately 2 hours. Patients may begin to notice effects within 30 minutes, with these effects lasting for up to 36 hours. Regular intake of a 5 mg daily dose leads to steady-state concentrations in the plasma within about 5 days. Importantly, the absorption of Tadalafilo is not significantly influenced by food consumption.
The drug exhibits a high binding affinity to plasma proteins, approximately 94%, and is extensively distributed throughout body tissues, with a volume of distribution (Vd) of 63 liters. Its plasma half-life is reported at around 17.5 hours, with hepatic metabolism predominantly occurring via the cytochrome P450 system, specifically through the CYP3A4 isoenzyme. The metabolic byproducts are primarily excreted: 61% through feces and 36% via urine. Caution is warranted in cases of severe renal impairment and mild to moderate hepatic insufficiency; however, there are negligible modifications needed for patients over 65 years of age when prescribed Tadalafilo.
Preclinical investigations have not exhibited any evidence of carcinogenic potential, mutagenicity, teratogenicity, fetotoxicity, or detrimental effects on fertility related to this medication.
An additional study found no adverse impacts on sperm motility or morphology in healthy male participants after administering a 20 mg oral dose.
INDICATIONS
The primary indication for Tadalafilo is the treatment of erectile dysfunction.
POSOLOGY
Dose
Applicable only to adult patients
For on-demand use, a single dose of 20 mg is recommended.
For daily use, a standard dose of 5 mg is prescribed, facilitating ongoing treatment.
Maximum daily dosage
The usual prescribed dosage should be adhered to, as higher dosing may not deliver additional therapeutic benefits and may increase the risk of adverse side effects.
Dose in special populations
- Renal impairment: For individuals with moderate impairment (creatinine clearance: 30-50 ml/min), the maximum on-demand dose should not exceed 10 mg within a 48-hour period, nor should the daily dose exceed 5 mg. In severe renal impairment (creatinine clearance < 30 ml/min), the maximum on-demand dosage should be limited to 5 mg within a 72-hour timeframe; a daily regimen is contraindicated.
- Liver impairment: For mild to moderate hepatic insufficiency, an on-demand dose should not surpass 10 mg. The efficacy of a daily regimen in these patients remains unverified. In instances of severe liver impairment, Tadalafilo is contraindicated.
- Elderly: No adjustments to the standard dosage are typically necessary for elderly patients.
Mode of application or method of administration
On-demand or occasional use: Tadalafilo should be taken orally with water or other beverages approximately 30 minutes prior to sexual activity; it can be consumed without regard to meals. Re-dosing should not occur within a 36-hour interval.
Daily use: This medication should be taken orally at a consistent time each day, either with or without food.
Therapeutic effects: Typically, benefits are observed by the fifth day following the initiation of treatment.
Concurrent use with other PDE5 inhibitors or varying concentrations of Tadalafilo is not advised.
ADVERSE REACTIONS
Gastrointestinal disorders
Common issues include dyspepsia, abdominal pain, gastroesophageal reflux, nausea, vomiting, dry mouth, and instances of rectal bleeding.
Hepatobiliary disorders
Abnormal results in liver function tests may arise.
Renal and urinary disorders
Hematuria has been noted among some users.
Cardiovascular disorders
Possible reactions encompass flushing, palpitations, tachycardia, hypotension, orthostatic hypotension, hypertension, myocardial infarction, ventricular arrhythmias, chest pain, unstable angina, and instances of sudden cardiac death.
Neurological disorders
Patients may experience headache, dizziness, somnolence, insomnia, altered sensations, stroke (inclusive of hemorrhagic occurrences), syncope, migraines, temporary amnesia, transient ischemic attacks, or seizures.
Respiratory disorders
Nasal congestion, dyspnea, epistaxis, and upper respiratory tract infections have been reported.
Musculoskeletal disorders
Common symptoms encompass myalgia and back or limb pain.
Ear and labyrinth disorders
Issues such as vertigo, tinnitus, and sudden hearing loss or decline in auditory perception may arise.
Ocular disorders
Visual disturbances including blurred vision, color perception changes, conjunctival hyperemia, ocular discomfort, tearing, and serious conditions like non-arteritic anterior ischemic optic neuropathy (NAION), retinal vascular occlusion, and visual field defects have been noted.
Reproductive system and breast disorders
Reports of hematospermia, penile bleeding, prolonged erections, and priapism have been documented.
Skin and subcutaneous tissue disorders
Skin reactions may include rash and urticaria.
Immunological disorders
Hypersensitivity reactions, angioedema, exfoliative dermatitis, and in rare cases, Stevens-Johnson syndrome have been reported.
General disorders
Patients may experience chest pain, sweating, asthenia, fatigue, or facial edema.
INTERACTIONS
With medications, food, and beverages
CYP3A4 isoenzyme inhibitors (including ketoconazole, itraconazole, erythromycin, clarithromycin, ritonavir, and saquinavir) may diminish the hepatic metabolism of Tadalafilo, causing elevated plasma concentrations and increased risk of side effects. Conversely, CYP3A4 inducers (like rifampicin, phenobarbital, phenytoin, and carbamazepine) can lower serum levels of Tadalafilo, potentially decreasing its clinical efficacy.
The concomitant use of Tadalafilo with nitrates and organic nitrites can result in severe hypotension due to the augmented synthesis of cGMP in vascular smooth muscle; therefore, combining these substances is contraindicated.
Moreover, taking Tadalafilo alongside alpha-adrenoceptor blockers (e.g., alfuzosin, doxazosin, and tamsulosin) may result in symptomatic hypotension. The use of antacids (like magnesium hydroxide/aluminum hydroxide) can impair Tadalafilo's gastrointestinal absorption.
No interference with laboratory assessments has been documented.
WARNINGS AND PRECAUTIONS
General
Prior to considering treatment with Tadalafilo, a comprehensive medical history and physical examination are crucial to identifying any underlying causes of erectile dysfunction and formulating an appropriate therapeutic approach.
Patients with pre-existing cardiovascular diseases may face heightened cardiac risks associated with sexual activity due to increased workload and oxygen demand on the heart. Thus, a thorough cardiovascular evaluation is necessary before prescribing Tadalafilo, particularly in those whose cardiac conditions may contraindicate sexual activity.
As Tadalafilo possesses systemic vasodilatory characteristics that can lead to transient blood pressure reductions, caution is advised, especially in patients with significant cardiovascular comorbidities, and a risk assessment should be conducted before treatment initiation.
The safety and efficacy of Tadalafilo have not been established in patients with a recent history of myocardial infarction (less than 90 days), uncontrolled arrhythmias, hypotension (< 90/50 mm Hg), hypertension (> 170/110 mm Hg), unstable angina, or recent stroke or heart failure (NYHA class II or higher), rendering its use contraindicated in these scenarios.
Patients on antihypertensive medications or alpha-blockers should be counseled about the potential for exacerbated hypotension when using Tadalafilo due to its vasodilatory properties.
Patients must be adequately informed regarding the severe risks linked to co-administration with nitrates or other nitric oxide donors.
Following its market release, instances of non-arteritic anterior ischemic optic neuropathy (NAION), a rare ocular condition leading to sudden vision loss, have been documented with Tadalafilo usage. Although a direct causal link has not been firmly established, vigilance is required if patients report any visual disturbances.
Additionally, the safety profile of Tadalafilo in patients with hereditary degenerative retinal diseases such as retinitis pigmentosa remains unverified.
Reports of prolonged erections (lasting longer than 4 hours) and priapism (painful erections lasting over 6 hours) have been observed with PDE5 inhibitors, including Tadalafilo; patients should be instructed to seek immediate medical assistance if an erection persists beyond 4 hours to prevent irreversible penile tissue damage.
Patients with anatomical abnormalities of the penis or conditions that may predispose them to priapism, such as sickle cell disease or similar disorders, should be treated with caution.
Instances of sudden hearing loss or auditory decline have been noted in conjunction with PDE5 inhibitors like Tadalafilo; patients should be advised to discontinue the medication and seek medical attention immediately should such symptoms occur.
Limited safety information is available regarding Tadalafilo use in individuals with active bleeding disorders or peptic ulcer disease; clinical judgment should guide its use in these patients.
The effectiveness and safety of concomitant use with other erectile dysfunction treatments have not been evaluated; hence, such combinations should be avoided.
The safety and effectiveness of Tadalafilo have not been established in individuals younger than 18 years.
PREGNANCY
This product is not indicated for use in women and should be kept entirely out of reach of female individuals.
LACTATION
This product is not indicated for use in women and should not be used in breastfeeding mothers.
CONTRAINDICATIONS
– Known hypersensitivity to Tadalafilo or any excipient in the formulation.
– Co-administration with nitrates or any nitric oxide donor drugs.
– Prior episodes of non-arteritic anterior ischemic optic neuropathy.
– Hereditary conditions like retinitis pigmentosa.
– Severe hepatic insufficiency.
– Recent myocardial infarction (within 90 days).
– Uncontrolled arrhythmias.
– Severe hypotension (< 90/50 mm Hg).
– Severe hypertension (> 170/110 mm Hg).
– Unstable angina or episodes of angina upon exertion.
– Recent history (within 6 months) of stroke or heart failure classified as NYHA class II or higher.
OVERDOSAGE
Signs and Symptoms
Single doses of Tadalafilo of up to 100 mg administered to healthy volunteers or multiple daily doses of up to 100 mg in patients have demonstrated an incidence of adverse reactions similar to those seen at conventional therapeutic doses. Based on previous observations with other PDE5 inhibitors, symptoms such as headache, hypotension, syncope, visual disturbances, and prolonged erections should be anticipated in cases of overdose.
Treatment
Symptomatic and supportive measures are recommended for management. Given Tadalafilo's high plasma protein binding, dialysis may not be an effective means of clearing the drug from circulation.