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برگه جديد - نام را وارد نماييد

برگه جديد - نام را وارد نماييد

Tadalafil

Category:

Category:
Erectile dysfunction treatment. (PDR 2005)
Composition:
Each scored film coated tablet contains 10 or 20 mg of Tadalafil.
Chemistry:
Pyrazino (1, 2: 1,6) pyrido (3,4-b) - indole - 1,4 - dione, 6 - (1,3 - benzodioxol - 5 - yl) - 2, 3, 6, 7, 12, 12a - hexahydro - 2 - methyl - (6R, 12aR).

C₂₂H₁₉N₃O₄ Mw=389.41 (PDR 2005)
Mechanism of Action:
Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle.
This response is mediated by the release of nitric oxide from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells.
Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) enhances erectile function by increasing the amount of cGMP. Tadalafil inhibits PDE5, because sexual stimulation is required to initiate the local release of nitric oxide, the inhibition of PDE5 by Tadalafil has no effect in the absence of sexual stimulation. (PDR 2005)
Pharmacokinetics:
Tadalafil is well absorbed after a dose by mouth. Peak plasma concentration are attained within 2 hours. The rate of absorption is not affected by food. Tadalafil is widely distributed into tissuesand is approximately 94% bound to plasma proteins. It is metabolised in the liver primarily by the cytochrome P₄₅₀ isoenzyme CYP₃A₄. The major metabolite, the methylcatechol glucuronide, is inactive. The mean half life of Tadalafil is about 17.5 hours. Tadalafil is excreted, predominantly as metabolites, in the faeces (61% of the dose) and to a lesser extent the urine (36% of the dose). Clearance may be reduced in the elderly and in patients with renal impairment. (Martindale 2005)
Indications:
Tadalafil is indicated for the treatment of erectile dysfunction. (PDR 2005)
Precautions:
Tadalafil should be used with caution in cardiovascular disease, anatomical deformation of the penis (e.g. angulation, cavernosal fibrosis, peyronie’s disease) and in those with a predisposition to prolonged erection. Tadalafil also should be used with caution in hepatic and renal impairment.
(BNF 47)
Pregnancy:
There are no adequate and well controlled studies of Tadalafil in pregnant women. It is not indicated for use in women. (PDR 2005)
Breast feeding:
Use of Tadalafil in nursing mothers is not recommended. (PDR 2005)
Drug interactions:
• Cytochrom P₄₅₀ inhibitors:
ketoconazole, HIV protease inhibitor (such as ritonavir), erythromycin, itraconazole, grapefruit juice.
• Cytochrom P₄₅₀ inducers:
Rifampin, carbamazepine, phenytoin, phenobarbital
• Antacids
• Alcohol
• Anti-hypertensives:
a - blockers (Doxazosin, Tamsulosin), Amlodipine, Metoprolol, Enalapril. (PDR 2005)
Contraindications:
• Tadalafil is contraindicated for patients with a known hypersensitivity to Tadalafil or any component of the tablet. (PDR 2005)
• Administration with nitrates and nitric oxide donors
• Coadministration with alpha-blockers other than O.4 mg/day Tamsulosin. (Facts 2005)
• Hypotension, recent stroke, unstable angina, myocardial infarction, moderate heart failure, uncontrolled arrhythmias, uncontrolled hypertension. (BNF 47)
Warnings:
• Priapism
• Cardiovascular
The following groups of patients with cardiovascular disease were not included in clinical safety and efficacy:
• Patients with an MI within the last 90 days
• Patients with unstable angina or angina occurring during sexual intercourse.
• Patients with New York Heart Association class 2 or greater heart failure in the last 6 months.
• Patients with uncontrolled arrhythmias, hypotension (BP less than 90/50 mm Hg) or uncontrolled hypertension (BP greater than 170/100 mm Hg)
• Patients with a stroke within the last 6 months. (Facts 2005)
Adverse Reactions:
• Cardiovascular: Hypertension, MI
• CNS: Dizziness
• Dermatologic: Rash
• GI: Diarrhea, gastroesophageal reflux, GGTP increased, loose stools, nausea, upper abdominal pain.
• Gu: Erection increased, spontaneous penile erection.
• Musculoskeletal: Arthralgia, neck pain.
• Respiratory: Epistaxis, dyspnea, pharyngitis.
Special senses: Conjunctivitis, eye pain, blurred vision, conjunctival hyperemia, eyelid swelling, lacrimation increased, change in color vision.
Miscellaneous: Asthenia, face edema, pain, fatigue. (Facts 2005)
• Stop use of all PDE 5 inhibitors, and seek medical attention in the event of a sudden loss of vision in one or both eyes. such an event may be a sign of non arteritic anterior ischemic optic
neuropathy (NAION) (FDA)
Dosage and administration:
The recommended starting dose of Tadalafil in most patients is 10 mg, taken prior to anticipated sexual activity. The dose may be increased to 20 mg or decreased to 5 mg, based on individual efficacy and tolerability. The maximum recommended dosing frequency is once per day. Tadalafil may be taken without regard to food. (PDR 2005)
Storage:
Store at 25°C. (PDR 2005)
How supplied:
Tadalafil is available as a brown, barrel shaped scored film coated tablet.

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