Talk:Tadalafil: Difference between revisions

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{{SubstanceBox/Tadalafil}}
{{SubstanceBox/Tadalafil}}


'''Tadalafil''' is a [[phosphodiesterase type 5 (PDE5) inhibitor]] marketed under the trade name '''Cialis''' primarily used to treat [[erectile dysfunction (ED)]].<ref>{{cite web|url=https://www.mayoclinic.org/drugs-supplements/tadalafil-oral-route/description/drg-20068537|title=Tadalafil Oral|publisher=Mayo Clinic|access-date=January 24, 2023}}</ref> It is a post-synaptic [[agonist]] of the [[effect::cyclic guanosine monophosphate (cGMP)|cGMP]]-specific phosphodiesterase type 5 (PDE5) enzyme, preventing cGMP breakdown and enhancing smooth muscle relaxation in the corpus cavernosum of the [[penis]].<ref name="EMA">{{cite web|url=https://www.ema.europa.eu/en/documents/product-information/cialis-epar-product-information_en.pdf|title=Cialis: EPAR Product Information|publisher=European Medicines Agency (EMA)|access-date=January 24, 2023}}</ref>
'''Tadalafil''' is a phosphodiesterase type 5 (PDE5) inhibitor marketed under the trade name '''Cialis''' primarily used to treat erectile dysfunction (ED), benign prostatic hyperplasia (BPH) and Pulmonary Arterial Hypertension (PAH).<ref name="hahappbig">{{cite web | last=Fahmy | first=George | last2=Hess | first2=Jaclyn | title=Tadalafil | publisher=StatPearls Publishing | date=2024-03-20 | pmid=38753929 | url=https://www.ncbi.nlm.nih.gov/books/NBK603743/ | access-date=2024-10-09}}</ref> It is a post-synaptic [[agonist]] of the cGMP-specific phosphodiesterase type 5 (PDE5) enzyme, preventing cGMP breakdown and enhancing smooth muscle relaxation in the corpus cavernosum of the penis.<ref name="EMA">{{cite web|url=https://www.ema.europa.eu/en/documents/product-information/cialis-epar-product-information_en.pdf|title=Cialis: EPAR Product Information|publisher=European Medicines Agency (EMA)|access-date=January 24, 2023}}</ref>


[[File:Tadalafil_structure.png|thumb|Chemical Structure of Tadalafil]]
[[File:Tadalafil_structure.png|thumb|Chemical Structure of Tadalafil]]


==Pharmacology==
==Pharmacology==
Tadalafil is a selective [[PDE5 inhibitor]], showing a [[selectivity]] of preference for [[PDE5]] over other PDE isozymes including PDE1, PDE2, PDE3, PDE4, PDE6, PDE7, PDE8, PDE9, PDE10 and PDE11. PDE5 is found predominantly in the corpus cavernosum, prostate, liver and platelets.<ref>{{cite journal|last1=Ghofrani|first1=H. A.|last2=Barst|first2=R. J.|last3=Grimminger|first3=F.|last4=Humbert|first4=M.|last5=Wedzicha|first5=J. A.|last6=Wilkins|first6=M. R.|last7=Schermuly|first7=R. T.|title=Sildenafil for the treatment of lung fibrosis and pulmonary hypertension: from animal disease models to clinical trials|journal=Journal of the American College of Cardiology|volume=45|issue=10|pages=1699-706|year=2005|doi=10.1016/j.jacc.2005.02.054|pmid=15893196|issn=1552-0767}}</ref>
Tadalafil is a selective PDE5 inhibitor, showing a [[selectivity]] of preference for PDE5 over other PDE isozymes including PDE1, PDE2, PDE3, PDE4, PDE6, PDE7, PDE8, PDE9, PDE10 and PDE11. PDE5 is found predominantly in the corpus cavernosum, prostate, liver and platelets.<ref>{{cite journal|last1=Ghofrani|first1=H. A.|last2=Barst|first2=R. J.|last3=Grimminger|first3=F.|last4=Humbert|first4=M.|last5=Wedzicha|first5=J. A.|last6=Wilkins|first6=M. R.|last7=Schermuly|first7=R. T.|title=Sildenafil for the treatment of lung fibrosis and pulmonary hypertension: from animal disease models to clinical trials|journal=Journal of the American College of Cardiology|volume=45|issue=10|pages=1699-706|year=2005|doi=10.1016/j.jacc.2005.02.054|pmid=15893196|issn=1552-0767}}</ref>


Tadalafil has an [[elimination half-life]] of 17.5 hours (range of 13-19 hours), longer than other PDE5 inhibitors: sildenafil (4-6 hours), vardenafil (4-5 hours) and avanafil (6-7 hours). Its relatively long half-life enables it to be prescribed for a frequency of once per day as needed.<ref>{{cite journal|last1=Semprini|first1=P.|last2=Moenne|first2=L.|last3=Leung|first3=B. S.|title=Surreptitious sildenafil overdose requiring intensive critical care support|journal=Annals of Internal Medicine|volume=157|issue=11|pages=823-824|year=2012|doi=10.7326/0003-4819-157-11-201212040-00010|issn=0003-4819}}</ref>
Tadalafil has an elimination half-life of 17.5 hours (range of 13-19 hours), longer than other PDE5 inhibitors: sildenafil (4-6 hours), vardenafil (4-5 hours) and avanafil (6-7 hours). Its relatively long half-life enables it to be prescribed for a frequency of once per day as needed.


Tadalafil's effects on phosphodiesterase 5 last approximately 36 hours after a single 20 mg dose. This allows improved sexual flexibility with spontaneously occurring moments of intimacy. However, the risk of side-effects also generally increases the higher the dosage. It exhibits a dose-response relationship, with higher doses producing stronger erections which are maintained for longer durations.
Tadalafil's effects on phosphodiesterase 5 last approximately 36 hours after a single 20 mg dose. This allows improved sexual flexibility with spontaneously occurring moments of intimacy. However, the risk of side-effects also generally increases the higher the dosage. It exhibits a dose-response relationship, with higher doses producing stronger erections which are maintained for longer durations.
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==Subjective effects==
==Subjective effects==


The primary effects of tadalafil stem from inhibition of [[phosphodiesterase type 5]] (PDE5) within the corpus cavernosum of the [[penis]]. This relaxes [[Smooth muscle|smooth muscle]] and widens [[blood vessels]], allowing blood flow to increase. Consequently, the user may experience:
The primary effects of tadalafil stem from inhibition of phosphodiesterase type 5 (PDE5) within the corpus cavernosum of the penis. This relaxes smooth muscle and widens blood vessels, allowing blood flow to increase. Consequently, the user may experience:


*- Enhanced capacity for sexual arousal and erection hardness when physically and psychologically stimulated
*- Enhanced capacity for sexual arousal and erection hardness when physically and psychologically stimulated
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==Legal Status==
==Legal Status==


Tadalafil is legally available as a prescription medication in most jurisdictions for the treatment of [[erectile dysfunction]] and [[benign prostatic hyperplasia]]. However, recreational use is illegal without a valid prescription.
Tadalafil is legally available as a prescription medication in most jurisdictions for the treatment of erectile dysfunction and benign prostatic hyperplasia. However, recreational use is illegal without a valid prescription.


United States: It is a Schedule IV controlled substance.
United States: It is a Schedule IV controlled substance.
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