INDICATIONS AND USAGE
Agents for the treatment of erectile dysfunction, including sildenafil, should be used with caution in patients with anatomical deformation of the penis (such as angulation, cavernosal fibrosis or Peyronie's disease), or in patients who have conditions which may predispose them to priapism (such as sickle cell anaemia, multiple myeloma or leukaemia). Prolonged erections and priapism have been reported with sildenafil in post-marketing experience.
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The co-administration of PDE5 inhibitors, including sildenafil, with guanylate cyclase stimulators, such as riociguat, is contraindicated as it may potentially lead to symptomatic hypotension (see section 4.5). Agents for the treatment of erectile dysfunction, including sildenafil, should not be used in men for whom sexual activity is inadvisable (e.g. patients with severe cardiovascular disorders such as unstable angina buy cenforce 120mg or severe cardiac failure). Sildenafil is contraindicated in patients who have loss of vision in one eye because of non-arteritic anterior ischaemic optic neuropathy (NAION), regardless of whether this episode was in connection or not with previous PDE5 inhibitor exposure (see section 4.4). The safety of sildenafil has not been studied in the following sub-groups of patients and its use is therefore contraindicated: severe hepatic impairment, hypotension (blood pressure <90/50 mmHg), recent history of stroke or myocardial infarction and known hereditary degenerative retinal disorders such as retinitis pigmentosa (a minority of these patients have genetic disorders of retinal phosphodiesterases).
11 Description
A medical history and physical examination should be undertaken to diagnose erectile dysfunction and determine potential underlying causes, before pharmacological treatment is considered. Prior to initiating any treatment for erectile dysfunction, physicians should consider the cardiovascular status of their patients, since there is a degree of cardiac risk associated with sexual activity. Sildenafil has vasodilator properties, resulting in mild and transient decreases in blood pressure (see section 5.1). Prior to prescribing sildenafil, physicians should carefully consider whether their patients with certain underlying conditions could be adversely affected by such vasodilatory effects, especially in combination with sexual activity. Patients with increased susceptibility to vasodilators include those with left ventricular outflow obstruction (e.g., aortic stenosis, hypertrophic obstructive cardiomyopathy), or those with the rare syndrome of multiple system atrophy manifesting as severely impaired autonomic control of blood pressure. Concomitant use with other PDE5 inhibitors or other treatments for erectile dysfunction The safety and efficacy of combinations of sildenafil with other PDE5 Inhibitors, or other pulmonary arterial hypertension (PAH) treatments containing sildenafil (REVATIO), or other treatments for erectile dysfunction have not been studied. Therefore the use of such combinations is not recommended. Cases of visual defects have been reported spontaneously in connection with the intake of sildenafil and other PDE5 inhibitors (see section 4.8). Cases of non-arteritic anterior ischaemic optic neuropathy, a rare condition, have been reported spontaneously and in an observational study in connection with the intake of sildenafil and other PDE5 inhibitors (see section 4.8). Patients should be advised that in the event of any sudden visual defect, they should stop taking Sildenafil and consult a physician immediately (see section 4.3).
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Co-administration of sildenafil with ritonavir is not advised (see section 4.5). Caution is advised when sildenafil is administered to patients taking an alpha-blocker, as the co-administration may lead to symptomatic hypotension in a few susceptible individuals (see section 4.5).
Side Effects
Clinical particulars4.1 Therapeutic indications4.2 Posology and method of administration4.3 Contraindications4.4 Special warnings and precautions for use4.5 Interaction with other medicinal products and other forms of interaction4.6 Fertility, pregnancy and lactation4.7 Effects on ability to drive and use machines4.8 Undesirable effects4.9 Overdose5. Pharmacological properties5.1 Pharmacodynamic properties5.2 Pharmacokinetic properties5.3 Preclinical safety data6. Pharmaceutical particulars6.1 List of excipients6.2 Incompatibilities6.3 Shelf life6.4 Special precautions for storage6.5 Nature and contents of container6.6 Special precautions for disposal and other handling7. Date of first authorisation/renewal of the authorisation10. This information is for use by healthcare professionals Last updated on emc: 07 Jul 2023 Each film-coated tablet contains 25 mg of sildenafil (as citrate).
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Each film-coated tablet contains 50 mg of sildenafil (as citrate). Each film-coated tablet contains 100 mg of sildenafil (as citrate). For the full list of excipients, see section 6.1. 7.20 mm in diameter film-coated tablets debossed with 124 on one side and J on the other side. 9.00 mm in diameter film-coated tablets debossed with 125 on one side and J on the other side with the score line. This is most likely to occur within 4 hours post sildenafil dosing. In order to minimise the potential for developing postural hypotension, patients should be hemodynamically stable on alpha-blocker therapy prior to initiating sildenafil treatment.
- Mean half-life is 27 hours, allowing convenient once-daily dosing.
- In elderly, half-life may extend to 35 hours due to reduced clearance.
- Hepatic impairment increases half-life; dose adjustment is necessary.
- Renal impairment has minimal effect on half-life.
Initiation of sildenafil at a dose of 25 mg should be considered (see section 4.2).
Interaction with drugs
The score line is only to facilitate breaking for ease of swallowing and not to divide into equal doses. 12.00 mm in diameter scored film-coated tablets debossed with 126 on one side and J on the other side with score line. Sildenafil is indicated in adult men with erectile dysfunction, which is the inability to achieve or maintain a penile erection sufficient for satisfactory sexual performance. In order for Sildenafil to be effective, sexual stimulation is required. The recommended dose is 50 mg taken as needed approximately one hour before sexual activity.
Sildenafil Citrate
Based on efficacy and tolerability, the dose may be increased to 100 mg or decreased to 25 mg. The maximum recommended dose is 100 mg. If Sildenafil is taken with food, the onset of activity may be delayed compared to the fasted state (see section 5.2). Dosage adjustments are not required in elderly patients (≥ 65 years old). The dosing recommendations described in 'Use in adults' apply to patients with mild to moderate renal impairment (creatinine clearance = 30-80 mL/min). In addition, physicians should advise patients what to do in the event of postural hypotensive symptoms. Studies with human platelets indicate that sildenafil potentiates the antiaggregatory effect of sodium nitroprusside in vitro. There is no safety information on the administration of sildenafil to patients with bleeding disorders or active peptic ulceration. Therefore, sildenafil should be administered to these patients only after careful benefit-risk assessment.
- "Blue 100 pills" might be prescribed for specific health conditions under medical supervision.
- Misusing prescription "blue 100" medications can result in legal issues and health risks.
- Proper disposal of unused pills is crucial to prevent misuse or accidental ingestion.
- Keep medications out of reach of children to prevent accidental poisoning.
Sildenafil is not indicated for use by women.
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Since sildenafil clearance is reduced in patients with severe renal impairment (creatinine clearance <30 mL/min) a 25 mg dose should be considered. Based on efficacy and tolerability, the dose may be increased step-wise to 50 mg up to 100 mg as necessary. Since sildenafil clearance is reduced in patients with hepatic impairment (e.g. cirrhosis) a 25 mg dose should be considered. Sildenafil is not indicated for individuals below 18 years of age.
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Use in patients taking other medicinal products With the exception of ritonavir for which co-administration with sildenafil is not advised (see section 4.4) a starting dose of 25 mg should be considered in patients receiving concomitant treatment with CYP3A4 inhibitors (see section 4.5). In order to minimise the potential of developing postural hypotension in patients receiving alpha-blocker treatment, patients should be stabilised on alpha-blocker therapy prior to initiating sildenafil treatment. In addition, initiation of sildenafil at a dose of 25 mg should be considered (see sections 4.4 and 4.5). Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. Consistent with its known effects on the nitric oxide/cyclic guanosine monophosphate (cGMP) pathway (see section 5.1), sildenafil was shown to potentiate the hypotensive effects of nitrates, and its co-administration with nitric oxide donors (such as amyl nitrite) or nitrates in any form is therefore contraindicated. This medicine contains less than 1 mmol sodium (23 mg) per film-coated tablet, that is to say essentially 'sodium-free'.
More about sildenafil
Sildenafil potentiates the hypotensive effect of nitrates (see section 4.3). Serious cardiovascular events, including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmia, cerebrovascular haemorrhage, transient ischaemic attack, hypertension and hypotension have been reported post-marketing in temporal association with the use of sildenafil. Most, but not all, of these patients had pre-existing cardiovascular risk factors. Many events were reported to occur during or shortly after sexual intercourse and a few were reported to occur shortly after the use of sildenafil without sexual activity. It is not possible to determine whether these events are related directly to these factors or to other factors. Effects of other medicinal products on sildenafil Sildenafil metabolism is principally mediated by the cytochrome P450 (CYP) isoforms 3A4 (major route) and 2C9 (minor route).
| Ingredient | Quantity per Pill | Source |
|---|---|---|
| Acetaminophen | 500 mg | Pharmaceutical Grade |
| Sildenafil | 100 mg | Synthetic Compound |
| Fillers | 50 mg | Inert Substances |
| Coloring Agent | FD&C Blue #2 | Food Grade Dye |
Although no increased incidence of adverse events was observed in these patients, when sildenafil is administered concomitantly with CYP3A4 inhibitors, a starting dose of 25 mg should be considered. Co-administration of the HIV protease inhibitor ritonavir, which is a highly potent P450 inhibitor, at steady state (500 mg twice daily) with sildenafil (100 mg single dose) resulted in a 300% (4-fold) increase in sildenafil Cmax and a 1,000% (11-fold) increase in sildenafil plasma AUC.
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