希爱力(Tadalafil)的详细说明书：作用与功效,用法用量,副作用,注意事项

Cialis (Tadalafil) is a phosphodiesterase 5 (PDE5) inhibitor and needs to be taken under the guidance of a professional physician.

Indications of Cialis (Tadalafil)

1. Erectile dysfunction

It is suitable for the treatment of erectile dysfunction (ED).

2. Benign prostatic hyperplasia

Cialis is indicated for the treatment of the signs and symptoms of benign prostatic hyperplasia (BPH).

3. Erectile dysfunction and benign prostatic hyperplasia

Cialis is indicated for the treatment of the signs and symptoms of ED and BPH (ED/BPH).

4. Limitations of use

If Cialis is used in combination with finasteride to initiate BPH treatment, such use is recommended not to exceed 26 weeks, because the incremental benefit of Cialis gradually decreases from 4 weeks to 26 weeks, and the incremental benefit of Cialis beyond 26 weeks is unknown.

The pictures come from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Cialis (Tadalafil) usage and dosage

1. Take Cialis as needed to treat erectile dysfunction

For most patients treated as needed, the recommended starting dose of Cialis is 10 mg, taken before anticipated sexual activity.

Dose may be increased to 20 mg or reduced to 5 mg based on individual efficacy and tolerability. In most patients, the maximum recommended dosing frequency is once daily.

2. Take Cialis once a day to treat erectile dysfunction

The recommended starting dose of Cialis once a day is 2.5 mg, taken at about the same time every day, regardless of the time of sexual activity.

Based on individual efficacy and tolerability, the once-daily dose of Cialis may be increased to 5 mg.

3. Take Cialis once a day to treat benign prostatic hyperplasia

The recommended dose of Cialis to treat BPH is 5 mg, taken at about the same time every day.

When initiating BPH treatment with Cialis and finasteride, the recommended dose of Cialis is 5 mg once daily, taken at approximately the same time each day for up to 26 weeks.

4. Take Cialis once a day to treat erectile dysfunction and benign prostatic hyperplasia

The recommended dose of Cialis once a day to treat ED and BPH is 5 mg, taken at about the same time every day, regardless of the time of sexual activity.

5. How to take the medicine

Cialis can be taken with or without food.

6. Medication for specific groups

(1), renal insufficiency

Take Cialis as needed

Creatinine clearance 30 to 50 ml/minute: the recommended starting dose is 5 mg, not more than once a day, and the maximum dose is 10 mg, not more than once every 48 hours.

Creatinine clearance less than 30 ml/min or receiving hemodialysis: The maximum dose is 5 mg, not to exceed once every 72 hours.

Once-daily Cialis

Erectile Dysfunction

Creatinine clearance less than 30 ml/minute or receiving hemodialysis: Once-daily Cialis is not recommended.

Benign prostatic hyperplasia and erectile dysfunction/benign prostatic hyperplasia

Creatinine clearance 30 to 50 ml/minute: The recommended starting dose is 2.5 mg. Depending on individual response, an increase to 5 mg may be considered.

Creatinine clearance less than 30 ml/min or receiving hemodialysis: Once-daily use of Cialis is not recommended.

(2), Liver insufficiency

Take Cialis as needed

Mild or moderate (Child-Pugh Class A or B): Dosage should not exceed 10 mg once daily. It has not been extensively evaluated in patients with hepatic impairment and caution is recommended.

Severe (Child-Pugh C): Cialis is not recommended.

Once-daily Cialis

Mild or Moderate (Child-Pugh Class A or B): Once-daily Cialis has not been extensively evaluated in patients with hepatic impairment.

Severe (Child-Pugh C): Cialis is not recommended.

7. Combined use of medications

(1) Nitrates

It is prohibited to combine with any form of nitrates.

(2), α-blockers

When Cialis is used in combination with α-blockers to treat patients with ED, the patient should have been stably receiving α-blockers before starting treatment, and Cialis should be started at the lowest recommended dose.

The combination of Cialis and alpha-blockers is not recommended for the treatment of BPH.

Cialis (Tadalafil) Contraindications

1. Nitrates

It is prohibited to use Cialis in patients who are taking any form of organic nitrates (regular and/or intermittent). In clinical pharmacology studies, Cialis has been shown to enhance the blood pressure-lowering effects of nitrates.

2. Anaphylaxis

Cialis is contraindicated in patients with known severe allergic reactions to Cialis. Allergic reactions have been reported, including Stevens-Johnson syndrome and exfoliative dermatitis.

3. Concomitant use of guanylate cyclase (GC) stimulators

It is prohibited to use Cialis in patients who are taking GC stimulators (such as riociguat). PDE5 inhibitors, including Cialis, may enhance the antihypertensive effects of GC stimulants.

Cialis (Tadalafil) Precautions

1. Cardiovascular

Doctors should consider the patient's cardiovascular status, because sexual activity is associated with certain cardiac risks. Therefore, erectile dysfunction treatments, including Cialis, are not recommended for men who are not advised to engage in sexual activity due to underlying cardiovascular conditions. Patients who develop symptoms when initiating sexual activity should be advised to avoid further sexual activity and seek immediate medical attention.

2. Prolonged erection time

There are rare reports of erection lasting more than 4 hours and priapism (painful erection lasting more than 6 hours) of this type of compound. If priapism is not treated promptly, it may cause irreversible damage to the erectile tissue. Patients who have an erection that lasts more than 4 hours (whether painful or not) should seek emergency medical attention.

3. Effects on eyes

Patients should stop using all phosphodiesterase type 5 (PDE5) inhibitors, including Cialis, and seek medical assistance when they experience sudden vision loss in one or both eyes.

4. Sudden hearing loss

Doctors should advise patients to stop taking PDE5 inhibitors, including Cialis, and seek immediate medical assistance in the event of sudden hearing loss or loss.

5. Alpha-blockers and antihypertensive drugs

PDE5 inhibitors (including Cialis) and alpha-adrenergic blockers are vasodilators with antihypertensive effects. When vasodilators are used concomitantly, additive hypotensive effects may occur. In some patients, concomitant use of these two drug classes can significantly lower blood pressure, possibly resulting in symptomatic hypotension (e.g., syncope).

7. Renal insufficiency

Take Cialis as needed

For patients with end-stage renal disease whose creatinine clearance is less than 30 ml/min or who receive hemodialysis, Cialis should be limited to 5 mg, no more than once every 72 hours.

The starting dose of Cialis for patients with a creatinine clearance of 30-50 ml/min should be 5 mg, no more than once daily, and the maximum dose should be limited to 10 mg, no more than once every 48 hours.

8. Hepatic insufficiency

Take Cialis as needed

For patients with mild or moderate hepatic insufficiency, the dose of Cialis should not exceed 10 mg. Due to insufficient information in patients with severe hepatic impairment, the use of Cialis is not recommended in this group of patients.

9. Alcohol

Patients should be made aware that both alcohol and Cialis (a PDE5 inhibitor) have mild vasodilatory effects. When mild vasodilators are used concomitantly, the antihypertensive effect of each compound may be increased. Therefore, doctors should inform patients that combining heavy drinking with Cialis may increase the likelihood of orthostatic signs and symptoms, including increased heart rate, decreased orthostatic blood pressure, dizziness, and headache.

10. Use potent cytochrome P4503A4 (CYP3A4) inhibitors at the same time

Cialis is mainly metabolized by CYP3A4 in the liver. For patients taking strong CYP3A4 inhibitors (such as ritonavir, ketoconazole, and itraconazole), the as-needed dose of Cialis should be limited to 10 mg, no more than once every 72 hours.

For patients taking strong CYP3A4 inhibitors concurrently with once-daily Cialis, the maximum recommended dose is 2.5 mg.

11. Use in combination with other PDE5 inhibitors or erectile dysfunction treatments

The safety and effectiveness of Cialis when used in combination with other PDE5 inhibitors or erectile dysfunction treatments have not been studied. Inform patients not to take Cialis with other PDE5 inhibitors, including Adcirca.

12. Effect on bleeding

Although Cialis has not been shown to prolong bleeding time in healthy subjects, use in patients with bleeding disorders or significant active peptic ulcers should be determined based on careful risk-benefit evaluation and with caution.

Adverse reactions of Cialis (Tadalafil)

1. General body: fatigue, facial edema, fatigue, pain, peripheral edema

2. Cardiovascular: angina, chest pain, hypotension, myocardial infarction, orthostatic hypotension, palpitations, syncope, tachycardia

3. Digestive system: abnormal liver function tests , Dry mouth, dysphagia, esophagitis, gastritis, elevated GGTP, loose stools, nausea, epigastric pain, vomiting, gastroesophageal reflux disease, hemorrhoid bleeding, rectal bleeding

4. Musculoskeletal: joint pain, neck pain

5. Nervous system: dizziness, hypoesthesia, insomnia, paresthesia, drowsiness, vertigo

6. Kidney and urinary system : Renal function damage

7. Respiratory system: dyspnea, epistaxis, pharyngitis

8. Skin and appendages: itching, rash, sweating

9. Ophthalmology: blurred vision, color vision changes, conjunctivitis (including conjunctival congestion), eye pain, increased tears, eyelid swelling

10. Otology: sudden decrease or loss of hearing, ear disease Ming

11. Genitourinary system: increased erection, spontaneous penile erection

Cialis (Tadalafil) drug interactions

1. Potential pharmacodynamic interactions with Cialis

(1), α-blockers: caution should be used when PDE5 inhibitors are combined with α-blockers. PDE5 inhibitors (including Cialis) and alpha-adrenergic blockers are vasodilators with antihypertensive effects. When vasodilators are used concomitantly, additive hypotensive effects may occur. Clinical pharmacology studies have been conducted with tadalafil administered in combination with doxazosin, tamsulosin, or alfuzosin.

(2) Antihypertensive drugs: PDE5 inhibitors, including tadalafil, are mild systemic vasodilators. Clinical pharmacology studies have been conducted to evaluate the potentiation of the antihypertensive effects of tadalafil on selected antihypertensive agents (amlodipine, angiotensin II receptor blockers, profluromethiazide, enalapril, and metoprolol). Coadministration of tadalafil with these drugs resulted in a small decrease in blood pressure compared to placebo.

(3) Alcohol: Both alcohol and tadalafil (a PDE5 inhibitor) have a slight vasodilatory effect. When mild vasodilators are used concomitantly, the antihypertensive effect of each compound may be increased. Combining heavy alcohol consumption with Cialis can increase the likelihood of orthostatic signs and symptoms, including increased heart rate, decreased orthostatic blood pressure, dizziness, and headache.

Tadalafil does not affect alcohol plasma concentrations, and alcohol does not affect tadalafil plasma concentrations. [See Warnings and Precautions.

2. The potential of other drugs to affect Cialis

(1) Antacids: Taking antacids (magnesium hydroxide/aluminum hydroxide) and tadalafil at the same time reduces the apparent absorption rate of tadalafil, but does not change the exposure of tadalafil (AUC).

(2) H2 antagonist: The increase in gastric pH caused by taking nizatidine has no significant impact on the pharmacokinetics of tadalafil.

(3) Cytochrome P450 inhibitor: Cialis is a substrate of CYP3A4 and is mainly metabolized by it. Studies have shown that drugs that inhibit CYP3A4 can increase tadalafil exposure.

3. The potential of Cialis to affect other drugs

(1) Aspirin: Tadalafil will not enhance the prolonged bleeding time caused by aspirin.

(2) Cytochrome P450 substrate: Cialis is not expected to have clinically significant inhibitory or inducing effects on the clearance of drugs metabolized by cytochrome P450 (CYP) isoenzymes. Studies have shown that tadalafil does not inhibit or induce P450 isoenzymes such as CYP1A2, CYP3A4, CYP2C9, CYP2C19, CYP2D6 and CYP2E1.

Cialis (Tadalafil) medication for specific groups of people

1. Pregnancy

Cialis is not suitable for use by women. There are no data on the use of Cialis in pregnant women to inform of any risk of drug-related developmental adverse reactions.

2. Lactation period

Cialis is not suitable for use by women.

There is no information regarding the presence of tadalafil and/or metabolites in human milk, the effects on breastfed children, or the effects on milk production. Tadalafil and/or its metabolites are present in the milk of lactating rats at concentrations approximately 2.4 times those found in plasma.

3. Men of childbearing potential

Based on data from 3 studies of adult men, tadalafil reduced sperm concentration in the 6-month study of tadalafil 10 mg and the 9-month study of tadalafil 20 mg.

4. Pediatric use

Cialis is not suitable for pediatric patients, and its safety and effectiveness for patients under 18 years of age have not been established.

5. Elderly use

Patients aged 65 and above report diarrhea more frequently after taking Cialis. There is no need to adjust the dose based on age alone. It should be considered that some elderly people are more sensitive to the drug. .

6. Hepatic insufficiency

The tadalafil exposure (AUC) of subjects with mild or moderate hepatic impairment (Child-Pugh class A or B) is comparable to that of healthy subjects. Insufficient data are available for subjects with severe hepatic impairment (Child-Pugh class C).

Mechanism of action of Cialis (Tadalafil)

Inhibiting phosphodiesterase type 5 (PDE5) enhances erectile function by increasing the amount of cGMP. Tadalafil inhibits PDE5. Because sexual stimulation is required to initiate local nitric oxide release, Tadalafil has no effect on PDE5 inhibition in the absence of sexual stimulation.

The effects of PDE5 inhibition on cGMP concentrations in the corpus cavernosum and pulmonary artery were also observed in the smooth muscle of the prostate, bladder and their vascular supply. The mechanism for reducing BPH symptoms has not yet been determined.

Cialis (Tadalafil) Storage

Cialis (Tadalafil) is stored at 25°C (77°F); excursions allowed within the range of 15°C-30°C (59-86°F).

Please keep out of the reach of children.

Warm Tips

1. For men who take Cialis as needed to treat ED, patients should be instructed to take one tablet at least 30 minutes before expected sexual activity. For most patients, the ability to have sexual intercourse improves for up to 36 hours.

2. For men who take Cialis once a day to treat ED or ED/BPH, patients should be instructed to take one tablet at approximately the same time every day, regardless of the time of sexual activity. Cialis can effectively improve erectile function during treatment.

3. For men who take Cialis once a day to treat BPH, the patient should be instructed to take one tablet at approximately the same time every day.