Talk:Tadalafil: Difference between revisions

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'''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 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]]

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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.

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-'''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 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]]
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 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.