tadalafil (Rx)
Dosing & Uses.
Erectile Dysfunction (ED)
PRN use: 10 mg PO initially before sexual activity, with or without food; may be increased to 20 mg or reduced to 5 mg on basis of efficacy and tolerability; in most patients, maximum dosing frequency is once daily Once-daily use: 2.5 mg/day PO in single daily dose, without regard to timing of sexual activity, with or without food; may be increased to 5 mg/day on basis of efficacy and tolerability.
PRN use: Decrease dose with concomitant use of potent CYP3A4 inhibitor (eg, ritonavir, ketoconazole, itraconazole); not to exceed 10 mg/72 hr Once-daily use: Decrease dose with concomitant use of potent CYP3A4 inhibitor (eg, ritonavir, ketoconazole, itraconazole); not to exceed 2.5 mg/day.
Benign Prostatic Hyperplasia.
Treatment of signs and symptoms of benign prostatic hyperplasia (BPH); daily use also indicated for treatment of patients with both BPH and erectile dysfunction.
BPH: 5 mg PO once daily BPH with erectile dysfunction: 5 mg PO once daily, taken at approximately same time each day without regard to timing of sexual activity With finasteride for BPH: tadalafil 5 mg plus finasteride 5 mg PO once daily for ≤26 weeks.
Pulmonary Arterial Hypertension (PAH)
40 mg PO once daily; dividing dose for more frequent dosing is not recommended Patients also taking ritonavir: 20 mg PO once daily initially for ≥1 week; may be increased to 40 mg/day on basis of tolerability.
If possible, avoid coadministration with CYP3A4 inhibitors; if coadministration is essential, long-term therapy is indicated, or strong CYP3A4 inhibitors are required, modify or hold dose Patients already taking strong CYP3A4 inhibitor who require tadalafil: 20 mg PO once daily; may be increased to 40 mg/day on basis of tolerability Patients already taking tadalafil who require strong CYP3A4 inhibitor: Avoid using tadalafil while starting strong CYP3A4 inhibitor; stop tadalafil ≥24 hours before starting strong CYP3A4 inhibitor; after 1 week, resume tadalafil at 20 mg PO once daily; may be increased to 40 mg/day on basis of tolerability.
Geriatric Dosing.
Erectile Dysfunction (ED)
Cialis: No dosage adjustment is warranted solely on basis of age; however, greater sensitivity to medications in some older individuals should be considered.
Pulmonary Arterial Hypertension (PAH)
Adcirca: Lower dose or reduced dosing frequency may be required in elderly because of decreased renal or hepatic clearance.
Dosing Modifications.
Renal impairment (ED)
Cialis (PRN use) Mild (CrCl ≥51 mL/min): No dosage adjustment needed Moderate (CrCl 30-50 mL/min): Not to exceed 5 mg PO once daily initially; maximum dosage, 10 mg PO q48hr Severe (CrCl <30 mL/min and on hemodialysis): Not to exceed 5 mg PO q72hr Cialis (once daily use) CrCl ≥30 mL/min: No dosage adjustment needed CrCl <30 mL/min: Not recommended.
Renal impairment (PAH)
Adcirca Mild-to-moderate (CrCl 31-80 mL/min): 20 mg PO once daily initially; may be increased to 40 mg once daily on basis of tolerability Severe (CrCl <30 mL/min and on hemodialysis): Avoid use.
Hepatic impairment (ED)
Cialis (PRN use) Mild-to-moderate (Child-Pugh class A or B): Not to exceed 10 mg PO once daily Severe (Child-Pugh class C): Not recommended Cialis (once daily use) Mild-to-moderate (Child-Pugh class A or B): Data limited; caution advised Severe (Child-Pugh class C): Not recommended.
Hepatic impairment (PAH)
Adcirca Mild-to-moderate (Child-Pugh class A or B): Consider starting dosage of 20 mg PO once daily Severe (Child-Pugh class C): Avoid use.
Muscular Dystrophy (Orphan)
Orphan designation for Duchenne muscular dystrophy (DMD)
Eli Lilly and Company; Lilly Corporate Center; Indianapolis, IN 46285.
Pulmonary Arterial Hypertension (Orphan)
Orphan designation of a fixed dose combination of macitentan and tadalafil for treatment of pulmonary arterial hypertension.
Actelion Clinical Research, Inc; 1820 Chapel Avenue West, Suite 300; Cherry Hill, New Jersey 08002.
Safety and efficacy not established.
Interactions.
Interaction Checker.
Contraindicated.
Serious – Use Alternative.
Significant – Monitor Closely.
Adverse Effects.
Respiratory tract infection (3-13%)
Nasal congestion (≤9%)
Gastroesophageal reflux disease (1-3%)
Genitourinary tract infection (≤2%)
Change in color vision.
Postmarketing reports.
Visual field defect, retinal vein occlusion, retinal artery occlusion, and non–arteritic anterior ischemic optic neuropathy (NAION)
Contraindications.
Hypersensitivity, including Stevens-Johnson syndrome and exfoliative dermatitis.
Soluble guanylate cyclase (sGC) stimulators (eg, riociguat); concomitant use can cause hypotension.
Coadministration with nitrates.
Coadministration with nitrates (either regularly and/or intermittently) and nitric oxide donors Consistent with the effects of PDE5 inhibition on the nitric oxide/cyclic guanosine monophosphate pathway, PDE5 inhibitors may potentiate the hypotensive effects of nitrates A suitable time interval following PDE5 dosing for the safe administration of nitrates or nitric oxide donors has not been determined.
Use caution in patients with anatomic deformation of penis, cardiovascular disease, left ventricular outflow obstruction, myocardial infarction in preceding 90 days, unstable angina, angina occurring during sexual intercourse, NYHA class 2 or greater heart failure in preceding 6 months, uncontrolled arrhythmias, hypotension, uncontrolled hypertension, cerebrovascular accident in preceding 6 months, bleeding disorders, active peptic ulcer disease, liver disease, renal impairment, conditions predisposing to priapism, concomitant use of CYP3A4 inhibitors.
May cause dose-related impairment of color discrimination; use caution in patients with retinitis pigmentosa.
Evaluate underlying causes of erectile dysfunction or BPH before initiating therapy.
May increase risk of sudden vision loss attributed to nonarteritic ischemic optic neuropathy; if vision problems arise, discontinue, and contact physician.
Risk of sudden hearing loss.
CYP3A4 inhibitors (eg, erythromycin, ketoconazole, itraconazole, indinavir, ritonavir) may significantly increase tadalafil serum levels.
CYP3A4 inducers (eg, rifampin, St John’s wort) may decrease tadalafil serum levels.
Potentiates hypotensive effect of nitrates (see Contraindications)
Concomitant use with alpha blockers (other than tamsulosin 0.4 mg/day) should be stabilized before initiation of phosphodiesterase (PDE)-5 inhibitors; patients with instability on alpha-blocker therapy alone are at increased risk for symptomatic hypotension with concurrent PDE-5 inhibitor therapy.
Not to be taken with other PDE-5 inhibitors (eg, sildenafil, vardenafil)
Not recommended in patients with pulmonary veno-occlusive disease.
Advise patients to seek emergency treatment if an erection lasts >4 hr.
Pregnancy & Lactation.
Not indicated for use in females; there are no data in pregnant women to inform any drug-associated risks for adverse developmental outcomes; in animal reproduction studies, no adverse developmental effects observed with oral administration of tadalafil to pregnant rats or mice during organogenesis at exposures up to 11 times the maximum recommended human dose (MRHD) of 20 mg/day.
Not indicated for use in females; there is no information on presence of tadalafil and/or metabolites in human milk; effects on breastfed child, or on milk production; drug and/or its metabolites are present in milk of lactating rats at concentrations approximately 2.4-fold greater than found in plasma.
Pregnancy Categories.
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology.
Mechanism of Action.
Erectile dysfunction: Inhibits PDE-5, increasing cyclic guanosine monophosphate (cGMP) to allow smooth-muscle relaxation and inflow of blood into corpus cavernosum.
Pulmonary arterial hypertension (PAH): Inhibits PDE-5, increasing cGMP to allow relaxation of pulmonary vascular smooth-muscle cells and vasodilation of pulmonary vasculature.
Absorption.
Peak plasma time: Erectile dysfunction, 0.5-6 hr; PAH, 2-8 hr.
Distribution.
Protein bound: 94%
Vd: Erectile dysfunction, 63 L; PAH, 77 L.
Metabolism.
Metabolized in liver by CYP3A4.
Elimination.
Half-life: Erectile dysfunction, 15-17.5 hr; PAH (not on bosentan), 35 hr.
Total body clearance: Erectile dysfunction, 2.5 L/hr; PAH (not on bosentan), 1.6 L/hr.
Excretion: Feces (61%), urine (36%)
Administration.
Instructions.
Erectile dysfunction (PRN use): Take before anticipated sexual activity.
Erectile dysfunction (once-daily use): Take at approximately same time each day without regard to timing of sexual activity.
Patient Handout.
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Cialis Indications Contraindications
