Tadalafil Citrate Dose


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tadalafil (Rx)

Dosing & Uses

tablet (Adcirca, Alyq, generic)

  • 2.5mg
  • 5mg
  • 10mg
  • 20mg

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 Enter a drug name and tadalafil

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%)

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

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

Patient Handout

Adding plans allows you to compare formulary status to other drugs in the same class.

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
  • Manage and view all your plans together – even plans in different states.
  • Compare formulary status to other drugs in the same class.
  • Access your plan list on any device – mobile or desktop.

The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

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Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.

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Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.