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tadalafil (Cialis, Adcirca, 'weekend Viagra')

Tradename: Cialis. New agent from Lilly & Icos. (2003) Available early 2004 [2] Indications: - erectile dysfunction - benign prostatic hyperplasia [7] - pulmonary hypertension [6] - adjunct treatment in Raynaud's phenomenon [9] - vascular dementia? - increases cerebral blood flow in all subcortical regions - largest effect in white matter hyperintensities - increase in cerebral blood flow is non-significant [10] Contraindications: 1) concurrent administration of nitrates [11] (amyl nitrite) 2) intermediate-high risk of coronary artery disease 3) retinitis pigmentosa 4) history of non-arteric ischemic optic neuropathy Dosage: - erectile dysfunction: 20 mg at least 1/2 hour before intercourse - BPH: start 2.5 mg QD, titrate to 5 mg QD [5] Pharmacokinetics: 1) duration of action 24-36 hours 2) metabolized by cyt P450 3A4 [3] Adverse effects: 1) see sildenafil (Viagra) 2) prolonged 1/2life could prolong adverse effects 3) non-arteritic ischemic optic neuropathy [4] Drug interactions: 1) prolonged 1/2life could prolong risk of drug interactions see sildenafil (Viagra) 2) reduce 20 mg dose with concurrent administration of potent inhibitors of cyt P450 3A4 -> erythromycin, ritonavir, ketoconazole, itraconazole 3) AVOID concurrent use of alpha blockers [3] a) Uroxatral, doxazosin, terazosin, prazosin b) increased risk of orthostatic hypotension c) use tamsulosin if alpha-blocker needed 4) concurrent administration of nitrates or amyl nitrite contraindicated Laboratory: - tadalafil in blood - tadalafil in serum/plasma - tadalafil in urine Mechanism of action: - more selective than sildenafil (Viagra) for inhibition of phosphodiesterase-5 - associated with less risk of heart failure, myocardial infarction, & mortality vs sildenafil or no treatment [12] Notes: - OTC tadalafil may be available by 2017. [8]

Interactions

drug interactions drug adverse effects (more general classes)

Related

phosphodiesterase 5; cGMP-specific phosphodiesterase

General

phosphodiesterase-5 inhibitor

Properties

INHIBITS: phosphodiesterase-5

Database Correlations

PUBCHEM correlations

References

  1. Prescriber's Letter 8(10):57 2001
  2. Prescriber's Letter 10(11):62 2003
  3. Prescriber's Letter 10(12):71 2003
  4. Prescriber's Letter 12(6): 2005 Viagra and Vision Loss Detail-Document#: 210611 (subscription needed) http://www.prescribersletter.com
  5. FDA NEWS RELEASE: Oct. 6, 2011 FDA approves Cialis to treat benign prostatic hyperplasia http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm274642.htm - Prescriber's Letter 18(11): 2011 Tadalafil (Cialis) for the Treatment of BPH Detail-Document#: 271102 (subscription needed) http://www.prescribersletter.com
  6. Deprecated Reference
  7. Roehrborn CG et al. Effects of tadalafil once daily on maximum urinary flow rate in men with lower urinary tract symptoms suggestive of benign prostatic hyperplasia. J Urol 2014 Apr; 191:1045 PMID: 24445278 http://dx.doi.org/10.1016/j.juro.2013.10.074#sthash.Z5obxJcP.dpuf
  8. Orciari Herman A Drug Makers Move Toward Over-the-Counter Cialis. Physician's First Watch, May 29, 2014 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org - Loftus P Lilly Strikes Licensing Deal With Sanofi for Over-the-Counter Cialis. A Nonprescription Version Still Needs Approval From Regulators. New York Times. May 28, 2014 http://online.wsj.com/news/articles/SB10001424052702304587704579588442314255198?mod=rss_Health&mg=reno64-wsj
  9. Shenoy PD, Kumar S, Jha LK et al Efficacy of tadalafil in secondary Raynaud's phenomenon resistant to vasodilator therapy: a double-blind randomized cross-over trial. Rheumatology (Oxford). 2010 Dec;49(12):2420-8 PMID: 20837499
  10. Pauls MMH, Binnie LR, Benjamin P et al The PASTIS trial: Testing tadalafil for possible use in vascular cognitive impairment. Alzheimer's & Dementia. 2022. Feb 8. PMID: 35135037 https://alz-journals.onlinelibrary.wiley.com/doi/10.1002/alz.12559
  11. Medical Knowledge Self Assessment Program (MKSAP) 19 American College of Physicians, Philadelphia 2022
  12. Ha A, Wayne G, Jacobs M et al PD11-10 PHOSPHODIESTERASE-5 INHIBITOR USE AND PROGRESSION TO HEART FAILURE IN MEN WITH CORONARY ARTERY DISEASE AND ERECTILE DYSFUNCTION. J Urol. 2023. 209(4):e336 April https://www.auajournals.org/doi/10.1097/JU.0000000000003251.10

Component-of

macitentan/tadalafil (Opsynvi)