tadalafil


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tadalafil

Cialis, Adcirca

Pharmacologic class: Phosphodiesterase type 5 (PDE5) inhibitor

Therapeutic class: Anti-erectile dysfunction agent

Pregnancy risk category B

Action

Inhibits PDE5, increasing cyclic guanosine monophosphate level and enhancing erectile function; also relaxes pulmonary vascular smooth muscle cells and vasodilation of the pulmonary vascular bed

Availability

Tablets: 2.5 mg, 5 mg, 10 mg, 20 mg, 40 mg

Indications and dosages

Erectile dysfunction (for as-needed use)

Adults: Initially, 10 mg (Cialis) P.O. before anticipated sexual activity; may increase to 20 mg or decrease to 5 mg based on patient response and tolerance. For most patients, maximum recommended dosing frequency is once daily.

Erectile dysfunction (for daily use)

Adults: 2.5 mg (Cialis) P.O. once daily, given at approximately the same time without regard to sexual activity; may increase to 5 mg P.O. once daily based on efficacy and tolerability

Benign prostatic hyperplasia (BPH); concurrent erectile dysfunction and BPH

Adults: 5 mg (Cialis) P.O. daily at approximately the same time each day.

Pulmonary hypertension

Adults: 40 mg (Adcirca) P.O. daily

Dosage adjustment

• Mild to moderate hepatic impairment or renal impairment

• Administration with alpha blockers or potent CYP3A4 inhibitors such as ketoconazole or ritonavir

Contraindications

• Hypersensitivity to drug or its components

• Concurrent use of organic nitrates (regularly or intermittently)

Precautions

Use cautiously in:

• mild to moderate hepatic or renal impairment

• severe renal impairment (avoid Adcirca use; once-daily Cialis use not recommended)

• severe hepatic impairment (Cialis use not recommended; avoid Adcirca use)

• cardiac risk that makes sexual activity inadvisable, left ventricular outflow obstruction, myocardial infarction within last 90 days, unstable angina or angina occurring during sexual intercourse, New York Heart Association Class II or greater heart failure in last 6 months, uncontrolled arrhythmias, blood pressure below 90/50 mm Hg, uncontrolled hypertension (blood pressure above 170/100 mm Hg), stroke within last 6 months, pulmonary veno-occlusive disease), erectile dysfunction whose cause hasn't been evaluated, conditions that increase risk of priapism (use not recommended)

• concurrent use of potent CYP450-3A4 inhibitors or inducers, or other PDE5 inhibitors (avoid use)

• concurrent use of alpha blockers (except tamsulosin 0.4 mg/day), antihypertensives, or alcohol

• pregnant or breastfeeding patients

• children (safety and efficacy not established).

Administration

• Know that patient should take drug with or without food and that patient should take Cialis before anticipated sexual activity when given on an as-needed basis.

Adverse reactions

CNS: headache, fatigue, dizziness, insomnia, hyperesthesia, paresthesia, drowsiness, vertigo, asthenia, transient global amnesia

CV: angina pectoris, chest pain, hypertension, hypotension, orthostatic hypotension, palpitations, syncope, tachycardia, myocardial infarction

EENT: blurred vision, color vision changes, conjunctivitis, eye pain, increased lacrimation, eyelid swelling, epistaxis, nasal congestion, pharyngitis

GI: nausea, vomiting, diarrhea, dyspepsia, esophagitis, gastroesophageal reflux, gastritis, upper abdominal pain, dysphagia, dry mouth

GU: increased or spontaneous erection

Musculoskeletal: myalgia; back, neck, limb, and joint pain

Respiratory: dyspnea

Skin: pruritus, rash, sweating

Other: facial edema, pain

Interactions

Drug-drug. Alpha-adrenergic blockers (except tamsulosin 0.4 mg/day): marked blood pressure decrease

Angiotensin receptor blockers, enalapril, metoprolol: decreased blood pressure

CYP450-3A4 inducers (such as carbamazepine, phenobarbital, phenytoin, rifampin): decreased tadalafil blood level

CYP450-3A4 inhibitors (such as erythromycin, itraconazole, ketoconazole, ritonavir): increased tadalafil blood level

Theophylline: slight increase in heart rate

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, lactate dehydrogenase, uric acid: increased levels

Drug-food. Grapefruit juice: increased drug blood level

Drug-behaviors. Alcohol use: decreased blood pressure

Patient monitoring

• Monitor for drug efficacy.

Patient teaching

• Advise patient taking Cialis for erectile dysfunction on an as-needed basis to take before anticipated sexual activity.

• Instruct patient that when taking Cialis on a daily basis he should take tablet at approximately the same time every day, without regard to sexual activity.

• Instruct patient to take Adcirca tablets one after the other every day and not to split the dose.

Caution patient never to take concurrently with nitrates.

Instruct patient to stop sexual activity and contact prescriber immediately if chest pain, dizziness, or nausea occurs.

Advise patient to seek immediate medical attention if sudden loss of vision or sudden decrease in or loss of hearing occurs.

• Instruct patient not to take other PDE5 inhibitors.

• Instruct patient to contact prescriber if erection lasts more than 4 hours.

• Tell patient drug can cause serious interactions with many common drugs. Instruct him to tell all prescribers he is taking it.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• Inform patient that drug may cause temporary blood pressure drop, leading to light-headedness if he stands up suddenly. Advise him to rise slowly and carefully.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and foods mentioned above.

tadalafil

(tə-dā′lə-fĭl′)
n.
A drug that inhibits phosphodiesterase, C22H19N3O4, used to treat erectile dysfunction by increasing the level of cyclic GMP, which increases blood flow to the erectile tissues.

tadalafil

an impotence agent.
indication This drug is used in the treatment of erectile dysfunction.
contraindications Known hypersensitivity to this drug prohibits its use. Patients who are taking organic nitrates either regularly or intermittently and patients taking any alpha-adrenergic antagonist other than tamsulosin (0.4 mg once daily) should not take this drug.
adverse effects Adverse effects of this drug include back pain or myalgia, blurred vision, changes in color vision, and pruritus. Life-threatening side effects include myocardial infarction, cardiovascular collapse, and sudden death. Common side effects include headache, flushing, dizziness, dyspepsia, nasal congestion, urinary tract infection, and diarrhea.

tadalafil

An inhibitor of the enzyme phosphodiesterase-5 which limits penile erection (see SILDENAFIL CITRATE for fuller details), used in the treatment of impotence. The drug takes effect within half an hour, reaches maximum blood concentration in two hours and remains effective for up to 36 hours. It has been available in Britain since February 2003. A brand name is Cialis.
References in periodicals archive ?
The supply of SLAM Natural Formula 29000 mg capsules containing undisclosed substances dapoxetine and tadalafil is illegal.
Ancak PT grubunda CAT aktivitesinin kontrol degerlerine yukselmesi, tadalafil tedavisinin suresi veya dozundaki artislarin UUO'da bobrekler icin koruyucu olabilecegini dusundurmektedir.
Tadalafil administered once daily for lower urinary tract symptoms secondary to benign prostatic hyperplasia: a dose finding study.
During this period among 956 patients started on tadalafil 10 mg daily for their erectile dysfunction after baseline investigation, those who developed back pain or myalgia with tadalafil and wanted to stop the drug in spite of repeated reassurance that pain is self-limiting were segregated.
There were no significant differences in change in standing systolic blood pressure with tadalafil with placebo, doxazosin, or tamsulosin.
Sildenafil and vardenafil both are metabolised primarily in the liver via the cytochrome P450 (CYP) pathway, mostly by CYP 3A4 and to a lesser extent by CYP 2C9, while tadalafil is metabolised almost solely by the cytochrome P450 3A4 [13, 14].
Tadalafil already is a well-studied and well-known medication that enjoys a very favorable side-effect profile.
Objective: To assess and compare the efficacy of on-demand versus daily dosages of tadalafil in the treatment of erectile dysfunction.
I was taken off warfarin (Coumadin) and was put on tadalafil (Adcirca).
No significant difference in visual and anatomy testing of the eye was found in the group of men who took tadalafil (Cialis[R]) or sildenafil versus the placebo groups.
Randomized clinical trials in monotherapy or combination therapy have been conducted in PAH with sildenafil and tadalafil which significantly improve clinical status, exercise capacity and hemodynamics of PAH patients.