Dosing & Uses
Dosage Forms & Strengths
tablet (Adcirca, Alyq, generic)
- 20mg
tablet (Cialis, generic)
- 2.5mg
- 5mg
- 10mg
- 20mg
Erectile Dysfunction
Indicated for treatment of erectile dysfunction (ED)
Cialis or generic equivalent only
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
Dosing considerations
- 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
Indicated for treatment of signs and symptoms of benign prostatic hyperplasia (BPH); daily use also indicated for treatment of patients with both BPH and erectile dysfunction
Cialis or generic equivalent only
BPH: 5 mg PO once daily
BPH with ED: 5 mg PO once daily, taken at approximately same time each day without regard to timing of sexual activity
Coadministration with finasteride for BPH: Tadalafil 5 mg plus finasteride 5 mg PO once daily for ≤26 weeks; incremental benefit of tadalafil decreases from 4 weeks until 26 weeks, and the benefit beyond 26 weeks is unknown
Pulmonary Arterial Hypertension
Indicated for pulmonary arterial hypertension (PAH) (WHO Group 1) to improve exercise ability; studies establishing effectiveness included predominately patients with NYHA Functional Class II – III symptoms and etiologies of idiopathic or heritable PAH (61%) or PAH associated with connective tissue diseases (23%)
Adcirca, Alyq, or generic equivalent only
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
Dosing considerations
- 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
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)
- ED (CrCl ≥30 mL/min): No dosage adjustment needed
- BPH or BPH/ED (CrCl 30-50 mL/min): 2.5 mg/day starting dose recommended; may increase to 5 mg according to individual response
- ED or BPH (CrCl <30 mL/min:) Not recommended
Renal impairment (PAH)
Adcirca or Alyq
- 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 or Alyq
- 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)
Sponsor
- 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
Sponsor
- Actelion Clinical Research, Inc; 1820 Chapel Avenue West, Suite 300; Cherry Hill, New Jersey 08002
Safety and efficacy not established
Erectile Dysfunction
Indicated for treatment of erectile dysfunction (ED)
Cialis or generic equivalent only: 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
Indicated for pulmonary arterial hypertension (PAH) (WHO Group 1) to improve exercise ability; studies establishing effectiveness included predominately patients with NYHA Functional Class II – III symptoms and etiologies of idiopathic or heritable PAH (61%) or PAH associated with connective tissue diseases (23%)
Adcirca, Alyq, or generic equivalent only: Lower dose or reduced dosing frequency may be required in elderly because of decreased renal or hepatic clearance
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Headache (11-42%)
Myalgia (1-14%)
Respiratory tract infection (3-13%)
Nasopharyngitis (2-13%)
Dyspepsia (1-13%)
Flushing (1-13%)
Back pain (2-12%)
Nausea (10-11%)
1-10%
Nasal congestion (≤9%)
Gastroesophageal reflux disease (1-3%)
Hypertension (1-3%)
Bronchitis (≤2%)
Genitourinary tract infection (≤2%)
<1%
Amnesia
Angina pectoris
Arthralgia
Change in color vision
Conjunctival hyperemia
Dyspnea
Epistaxis
Postmarketing reports
Hypotension
Visual field defect, retinal vein occlusion, retinal artery occlusion, and non–arteritic anterior ischemic optic neuropathy (NAION)
Hearing loss
Priapism
Warnings
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
Cautions
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
Do not use nitrates within 48 hours of last dose of tadalafil
Drug has vasodilatory properties that may result in transient decreases in blood pressure; prior to prescribing, carefully consider whether patients with underlying cardiovascular disease could be affected adversely by such vasodilatory effects; patients with preexisting hypotension, with autonomic dysfunction, with left ventricular outflow obstruction, may be particularly sensitive to actions of vasodilators
When used to treat erectile dysfunction, non-arteritic anterior ischemic optic neuropathy (NAION), a cause of decreased vision including permanent loss of vision, reported postmarketing; 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
Pregnancy
Limited data from case series with use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes
Pregnant women with untreated pulmonary arterial hypertension are at risk for heart failure, stroke, preterm delivery, and maternal and fetal death
Animal data
- In animal reproduction studies, no adverse developmental effects were observed with oral administration to pregnant rats or mice during organogenesis at exposures 7 times the exposure at maximum recommended human dose (MRHD) of 40 mg/day based on AUC
Lactation
There are no data on presence of drug and/or its 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-times that found in the plasma; when a drug is present in animal milk, it is likely that the drug will be present in human milk
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
Duration: ≤36 hr
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
Oral Administration
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
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Patient Handout
Formulary
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