Celeste 20mg (4pcs Box)

Indications

Tadalafil is indicated for the treatment of Erectile Dysfunction (ED) in adults and Pulmonary Arterial Hypertension (PAH).

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Pharmacology

Pharmacodynamic Properties: In case of Erectile Dysfunction (ED), Tadalafil inhibits phosphodiesterase type 5 (PDE5) enzymes. This inhibition of phosphodiesterase type 5 (PDE5) enhances erectile function by increasing the amount of cGMP. Increased Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. Increased cGMP results in increased blood flow into the corpus cavernosum, thereby solves the problem of Erectile Dysfunction (ED).

Pharmacokinetic Properties: After single oral-dose administration, the maximum observed plasma concentration (Cmax) of Tadalafil is achieved between 30 minutes and 6 hours (median time of 2 hours). The mean apparent volume of distribution following oral administration is approximately 63 L, indicating that tadalafil is distributed into tissues. At therapeutic concentrations, 94% of Tadalafil in plasma is bound to proteins. Less than 0.0005% of the administered dose appeared in the semen of healthy subjects. Tadalafil is predominantly metabolized by CYP3A4 to a catechol metabolite. The catechol metabolite undergoes extensive methylation and glucuronidation to form the methylcatechol and methylcatechol glucuronide conjugate, respectively. The mean oral clearance for Tadalafil is 2.5 L/hr and the mean terminal half-life is 17.5 hours in healthy subjects. Tadalafil is excreted predominantly as metabolites, mainly in the feces (approximately 61% of the dose) and to a lesser extent in the urine (approximately 36% of the dose).

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Dosage & Administration

The dosage and administration of Tadalafil has two basis

As needed basisFor Erectile Dysfunction (ED): 10 mg prior sex is generally indicated which may be reduced to 5 mg or increased up to 20 mg upon response of the patient.

Regular Basis: For Pulmonary Arterial Hypertension (PAH): 40 mg (i.e. 2 tablets of 20 mg at a time) once daily is recommended. Dividing the dose (Taking total 40 mg as 20 mg in the morning and remaining 20 mg in the evening) over the course of the day is not recommended.This may be taken with or without food.

Missed Dose: No significant effects are found if any dose is missed. It is advised to discard this issue and continue from the next available timing.

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Interaction

Tadalafil is principally metabolized by CYP3A4. A selective inhibitor of CYP3A4, ketoconazole, increased Tadalafil AUC by 107%, relative to the AUC values for Tadalafil alone (10 mg dose). Although specific interactions have not been studied, some protease inhibitors, such as ritonavir and saquinavir and other CYP3A4 inhibitors, such as erythromycin, clarithromycin and itraconazole should be co-administered with caution as they would be expected to increase plasma concentrations of Tadalafil. Consequently the incidence of the undesirable side effects mentioned above might increased.Excess intake of alcohol must be avoided. When taken in excess, alcohol can increase chances of getting a headache, increasing heart rate, or lowering blood pressure.

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Contraindications

Nitrates — Administration of Tadalafil to patients who are using any form of organic nitrate, either regularly and/or intermittently, is contraindicated. Hypersensitivity — Tadalafil is contraindicated for patients with a known hypersensitivity to Tadalafil or any component of the tablet.

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Side Effects

Few side effects like – myalgia, fatigue, pain, hypotension, palpitations, diarrhea, dry mouth, dizziness, tinnitus, spontaneous penile erection etc. have been reported.

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Pregnancy & Lactation

Pregnancy Category-B: There are no adequate and well-controlled studies of Tadalafil in pregnant women. It is not known if Tadalafil and/or its metabolites is excreted in human breast milk. Use of Tadalafil in nursing mothers is not recommended.

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Precautions & Warnings

Alpha-blockers: Caution is advised when PDE5 inhibitors are coadministered with alpha-blockers. Sometimes this can lower blood pressure significantly which may lead to symptomatic hypotension (e.g. fainting).

Renal Insufficiency: No dose adjustment is needed in patients with mild-moderate renal insufficiency. The highest dose for Tadalafil should be limited to 5 mg not more than once daily in patients with severe renal insufficiency or end-stage renal disease.

Hepatic Impairment: In patients with mild or moderate hepatic impairment, the highest dose of Tadalafil should not exceed 10 mg.Priapism (pain full and/or longer erection than 4-6 hrs)Tadalafil should be used with caution in patients who have conditions that might predispose them to priapism (such as sickle cell anemia, multiple myeloma, or leukemia), or in patients with anatomical deformation of the penis (such as angulation, cavernosal fibrosis or Peyronie’s disease). This is because Priapism, if not treated promptly, can result in irreversible damage to the erectile tissue. Therefore, patients who have an erection lasting greater than 4 hours, should seek emergency medical attention, whether painful or not.

Storage Conditions

Store in a cool and dry place away from light. Keep out of the reach of children.

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