Tadalafil

Class
Vasoactive agents
Subclass
Phosphodiesterase-5 inhibitors
Substance name
Tadalafil
Brand names
Cialis®, Alyq®, Adcirca®
Common formulations
Film-coated tablet, Tablet
Contained in
Macitentan / tadalafil (Opsynvi®)
Dosage and administration
Adults patients
Treatment
BPH
•
5 mg PO daily, for up to 26 weeks when used with finasteride
Taken at the same time every day.
Erectile dysfunction
•
Start at: 10 mg PO PRN, taken before anticipated sexual activity
•
Maintenance: 5-20 mg PO PRN, taken before anticipated sexual activity
Titrate based on response and tolerance.
Alternative
•
Start at: 2.5 mg PO daily
•
Maintenance: 2.5-5 mg PO daily
Taken at the same time every day. Titrate based on response and tolerance.
Erectile dysfunction with BPH
•
5 mg PO daily
Taken at the same time every day.
Pulmonary arterial hypertension
•
40 mg PO daily
High-altitude pulmonary edema • Off-label
•
10 mg PO BID
Raynaud's phenomenon • Off-label
•
20 mg PO q48h
Prevention
Prevention of high-altitude pulmonary edema • Off-label
•
10 mg PO BID, started the day before the ascent if possible, and continued for 4 days after arrival at the target elevation when ascending at recommended rates, or for 4-7 days when ascending faster than recommended
Indications for use
Labeled indications
Adults
•
Treatment of BPH
•
Treatment of erectile dysfunction
•
Treatment of erectile dysfunction with BPH
•
Treatment of pulmonary arterial hypertension
Off-label indications
Adults
•
Treatment of Raynaud's phenomenon
•
Treatment of high-altitude pulmonary edema
•
Prevention of high-altitude pulmonary edema
Safety risks
Contraindications
Hypersensitivity to tadalafil or its components
HF
•
Do not use tadalafil in patients with a history of HF (NYHA class 2-4) in the past 6 months.
Retinitis pigmentosa or other hereditary degenerative retinal disorders
Concomitant use of guanylate cyclase stimulators
Warnings and precautions
Bleeding
•
Use caution in patients with bleeding disorders or active peptic ulcer disease.
Hearing loss
•
Maintain a high level of suspicion, as tadalafil has been associated with an increased risk of sudden hearing loss, which may be accompanied by tinnitus and dizziness.
Hypotension
•
Use caution in patients with resting hypotension, fluid depletion, severe LV outflow obstruction (aortic stenosis or idiopathic hypertrophic subaortic stenosis), autonomic dysfunction, or concomitant use of alcohol, antihypertensives, or α-blockers.
Increased serum tadalafil levels
•
Use caution in patients taking potent CYP3A4 inhibitors, such as ritonavir, ketoconazole, and itraconazole. Reduce dose to 10 mg every 72 hours. Maximum dose of 2.5 mg for once daily use.
Mask symptoms of prostate cancer
•
Maintain a high level of suspicion, as prostate cancer can present with symptoms of BPH, and the two disorders frequently coexist.
Priapism
•
Use caution in patients with anatomic penile abnormalities, such as angulation, cavernosal fibrosis, or Peyronie's disease, or conditions predisposing to priapism, such as sickle cell disease, multiple myeloma, or leukemia.
Vision loss, non-arteritic anterior ischemic optic neuropathy
•
Maintain a high level of suspicion, as sildenafil has been associated with an increased risk of sudden vision loss.
Specific populations
Renal impairment
CrCl 50-80 mL/min
•
Start at dose of 20 mg daily for pulmonary arterial hypertension. Maximal dose of 40 mg daily for pulmonary arterial hypertension. No dose adjustment required for erectile dysfunction or BPH.
CrCl 30-50 mL/min
•
Start at dose of 5 mg for as-needed use in erectile dysfunction and 2.5 mg for once-daily use in erectile dysfunction/BPH. Start at dose of 20 mg daily for pulmonary arterial hypertension. Maximal dose of 10 mg q48h for as-needed use in erectile dysfunction and 5 mg q24h for once-daily use in erectile dysfunction/BPH. Maximal dose of 40 mg daily for pulmonary arterial hypertension.
CrCl < 30 mL/min
•
Maximal dose of 5 mg q72h for as-needed use in erectile dysfunction. Do not use for once-daily use in erectile dysfunction. Avoid use in pulmonary arterial hypertension.
Renal replacement therapy
Continuous renal replacement
•
Avoid use.
Intermittent hemodialysis
•
Maximal dose of 5 mg q72h for as-needed use in erectile dysfunction. Do not use for once-daily use in erectile dysfunction/benign prostatic hyprplasia. Avoid use for pulmonary arterial hypertension.
Peritoneal dialysis
•
Maximal dose of 5 mg q72h for as-needed use in erectile dysfunction. Do not use for once-daily use in erectile dysfunction/benign prostatic hyprplasia. Avoid use for pulmonary arterial hypertension.
Hepatic impairment
Child-Pugh A (mild)
•
Use with caution. Start at dose of 20 mg daily for pulmonary arterial hypertension. Maximal dose of 10 mg once per day for as-needed use in erectile dysfunction.
Child-Pugh B (moderate)
•
Use with caution. Start at dose of 20 mg daily for pulmonary arterial hypertension. Maximal dose of 10 mg once per day for as-needed use in erectile dysfunction.
Child-Pugh C (severe)
•
Do not use.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: B1
•
Use only if benefits outweigh potential risks. Evidence of fetal harm in animals.
Breastfeeding
Use only if benefits outweigh potential risks.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Adverse reactions
Very common > 10%
•
Nasopharyngitis, back pain, dyspepsia, headache, myalgia, nausea, skin flushing
Common 1-10%
•
Conjunctivitis, esophagitis, eyelid swelling, gastroesophageal reflux disease, gastritis, gastrointestinal bleeding, hyperlacrimation, hypertension, ↑ liver enzymes, ↑ serum gamma-glutamyltransferase, myocardial infarction, orthostatic hypotension, renal insufficiency, arthralgia, asthenia, facial edema, peripheral edema, blurred vision, color vision impairment, chest pain, angina pectoris, hypotension, cough, diarrhea, dizziness, dry mouth, dysphagia, dyspnea, epigastric pain, eye pain, fatigue, hearing loss, hypoesthesia, insomnia, musculoskeletal pain, nasal congestion, neck pain, nosebleed, pain in extremity, palpitations, paresthesia, priapism, pruritus, skin rash, somnolence, sweating, syncope, tinnitus, vertigo, vomiting, rectal bleeding, respiratory tract infections, tachycardia, urinary tract infections
Unknown frequency
•
Exfoliative dermatitis, migraine, memory impairment, seizure, retinal thrombosis, visual field defect, Stevens-Johnson syndrome, stroke, urticaria
Interactions
Drug(s)
Check Interactions
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