pharmacopeia
GET
/api/v1/drug/tadalafil
2D structure
(2R,8R)-2-(1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
SMILES CN1CC(=O)N2[C@@H](C1=O)CC3=C([C@H]2C4=CC5=C(C=C4)OCO5)NC6=CC=CC=C36
InChIKey WOXKDUGGOYFFRN-IIBYNOLFSA-N

Mechanism of action

Sourced from openFDA

Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells.

Phosphodiesterase 5

Indications

Sourced from openFDA
  • Tadalafil is a phosphodiesterase 5 (PDE5) inhibitor indicated for the treatment of: erectile dysfunction (ED) ( 1.1 ) the signs and symptoms of benign prostatic hyperplasia (BPH) ( 1.2 ) ED and the signs and symptoms of BPH (ED/BPH) ( 1.3 ) If tadalafil is used with finasteride to initiate BPH treatment, such use is recommended for up to 26 weeks ( 1.4 ). 1.1 Erectile Dysfunction Tadalafil tablets are indicated for the treatment of erectile dysfunction (ED).ICD-10: N40.0, N52.9

Contraindications

Sourced from openFDA
  • Administration of tadalafil tablets to patients using any form of organic nitrate is contraindicated. Tadalafil was shown to potentiate the hypotensive effect of nitrates ( 4.1 ).contraindicated

Dosage & administration

Sourced from openFDA

Do not split tadalafil tablets; entire dose should be taken. Tadalafil tablets for use as needed: ED: Starting dose: 10 mg as needed prior to sexual activity. Increase to 20 mg or decrease to 5 mg based upon efficacy/tolerability. Improves erectile function compared to placebo up to 36 hours post dose. Not to be taken more than once per day ( 2.1 ). Tadalafil tablets for once daily use: ED: 2.5 mg taken once daily, without regard to timing of sexual activity. May increase to 5 mg based upon efficacy and tolerability ( 2.2 ). BPH: 5 mg, taken at approximately the same time every day ( 2.3 ) ED and BPH: 5 mg, taken at approximately the same time every day ( 2.3 , 2.4 ) Tadalafil tablets may be taken without regard to food ( 2.5 ). 2.1 Tadalafil Tablets for Use as Needed for Erectile Dysfunction The recommended starting dose of tadalafil tablets for use as needed in most patients is 10 mg, taken prior to anticipated sexual activity. The dose may be increased to 20 mg or decreased to 5 mg, based on individual efficacy and tolerability. The maximum recommended dosing frequency is once per day in most patients. Tadalafil tablets for use as needed were shown to improve erectile function compared to placebo up to 36 hours following dosing. Therefore, when advising patients on optimal use of tadalafil tablets, this should be taken into consideration.

Warnings & precautions

Sourced from openFDA

Evaluation of erectile dysfunction and BPH should include an appropriate medical assessment to identify potential underlying causes, as well as treatment options. Before prescribing tadalafil tablets, it is important to note the following: Patients should not use tadalafil tablets if sex is inadvisable due to cardiovascular status ( 5.1 ). Use of tadalafil tablets with alpha-blockers, antihypertensives or substantial amounts of alcohol (≥5 units) may lead to hypotension ( 5.6 , 5.9 ). Tadalafil tablets are not recommended in combination with alpha-blockers for the treatment of BPH because efficacy of the combination has not been adequately studied and because of the risk of blood pressure lowering. Caution is advised when tadalafil tablets are used as a treatment for ED in men taking alpha-blockers. ( 2.7 , 5.6 , 7.1 , 12.2 ) Patients should seek emergency treatment if an erection lasts >4 hours. Use tadalafil tablets with caution in patients predisposed to priapism ( 5.3 ). Patients should stop tadalafil tablets and seek medical care if a sudden loss of vision occurs in one or both eyes, which could be a sign of non-arteritic anterior ischemic optic neuropathy (NAION). Tadalafil tablets should be used with caution, and only when the anticipated benefits outweigh the risks, in patients with a history of NAION. Patients with a "crowded" optic disc may also be at an increased risk of NAION ( 5.4 , 6.2 ). Patients should stop tadalafil tablets and seek prompt medical attention in the event of sudden decrease or loss of hearing ( 5.5 ).

Adverse reactions

Sourced from openFDA

Most common adverse reactions (≥2%) include headache, dyspepsia, back pain, myalgia, nasal congestion, flushing, and pain in limb ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact VKT Pharma Pvt. Ltd at 1 844-387-1231 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Tadalafil was administered to over 9000 men during clinical trials worldwide. In trials of tadalafil tablets for once daily use, a total of 1434, 905, and 115 were treated for at least 6 months, 1 year, and 2 years, respectively. For tadalafil tablets for use as needed, over 1300 and 1000 subjects were treated for at least 6 months and 1 year, respectively. Tadalafil Tablets for Use as Needed for ED In eight primary placebo-controlled clinical studies of 12 weeks duration, mean age was 59 years (range 22 to 88) and the discontinuation rate due to adverse events in patients treated with tadalafil 10 or 20 mg was 3.1%, compared to 1.4% in placebo treated patients.

Use in specific populations

Sourced from openFDA

Hepatic Impairment ( 2.6 , 5.8 , 8.6 ): Mild or Moderate: Dosage adjustment may be needed. Severe: Use is not recommended. Renal Impairment ( 2.6 , 5.7 , 8.7 ): Patients with creatinine clearance 30 to 50 mL/min: Dosage adjustment may be needed. Patients with creatinine clearance less than 30 mL/min or on hemodialysis: For use as needed: Dose should not exceed 5 mg every 72 hours. Once daily use is not recommended. 8.1 Pregnancy Risk Summary Tadalafil tablets are not indicated for use in females. There are no data with the use of tadalafil tablets in pregnant women to inform any drug-associated risks for adverse developmental outcomes. In animal reproduction studies, no adverse developmental effects were 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 ( see Data). Data Animal Data Animal reproduction studies showed no evidence of teratogenicity, embryotoxicity, or fetotoxicity when tadalafil was given orally to pregnant rats or mice at exposures up to 11 times the maximum recommended human dose (MRHD) of 20 mg/day during organogenesis. In a prenatal/postnatal developmental study in rats, postnatal pup survival decreased following maternal exposure to tadalafil doses greater than 10 times the MRHD based on AUC.

Pharmacokinetics

Sourced from openFDA
Metabolism
Over a dose range of 2.5 to 20 mg, tadalafil exposure (AUC) increases proportionally with dose in healthy subjects. Steady-state plasma concentrations are attained within 5 days of once per day dosing and exposure is approximately 1.6-fold greater than after a single dose.

Overdosage

Sourced from openFDA

Single doses up to 500 mg have been given to healthy subjects, and multiple daily doses up to 100 mg have been given to patients. Adverse events were similar to those seen at lower doses. In cases of overdose, standard supportive measures should be adopted as required. Hemodialysis contributes negligibly to tadalafil elimination.

Approval history

Sourced from openFDA
  • Nov 21, 2003NDANDA021368Lilly
  • May 22, 2009NDANDA022332Eli Lilly Co
  • Feb 5, 2019ANDAANDA210572Chartwell Rx
  • Feb 5, 2019ANDAANDA209907Hetero Labs Ltd Iii
  • Feb 5, 2019ANDAANDA210255Cipla
  • Feb 5, 2019ANDAANDA206286Aurobindo Pharma Ltd
  • Jun 17, 2022NDANDA214522Cmp Dev Llc
  • Mar 22, 2024NDANDA218490Actelion

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
98,103 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Dyspnoea11,83712%
  2. 2Headache10,86011%
  3. 3Diarrhoea7,9198.1%
  4. 4Nausea6,6086.7%
  5. 5Death5,9616.1%
  6. 6Fatigue5,9576.1%
  7. 7Drug Ineffective5,5145.6%
  8. 8Dizziness5,2615.4%
  9. 9Cough4,3174.4%
  10. 10Pneumonia4,2794.4%
  11. 11Malaise3,7693.8%
  12. 12Vomiting3,4993.6%
  13. 13Pain3,3513.4%
  14. 14Asthenia3,3483.4%
  15. 15Pain In Extremity3,3423.4%

Literature

View JSON

Recent PubMed references pinned to Tadalafil as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

View JSON

The 10 most recently updated of 279 ClinicalTrials.gov registrations naming Tadalafil as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Tadalafil work?
Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells.
What is Tadalafil used for?
According to FDA labeling, Tadalafil carries indications including: Tadalafil is a phosphodiesterase 5 (PDE5) inhibitor indicated for the treatment of: erectile dysfunction (ED) ( 1.1 ) the signs and symptoms of benign prostatic hyperplasia (BPH) ( 1.2 ) ED and the signs and symptoms of BPH (ED/BPH) ( 1.3 ) If tadalafil is used with finasteride to initiate BPH treatment, such use is recommended for up to 26 weeks ( 1.4 ). 1.1 Erectile Dysfunction Tadalafil tablets are indicated for the treatment of erectile dysfunction (ED).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Tadalafil?
Tadalafil is classified as Drugs used in erectile dysfunction, Phosphodiesterase 5 Inhibitor, Phosphodiesterase 5 Inhibitors, Penile Venous Vasodilation, Pulmonary Venous Vasodilation.
What are the brand names for Tadalafil?
Tadalafil is marketed under brand names including Adcirca, Alyq, Cialis, Entadfi, Opsynvi, Tadliq.
What are the contraindications for Tadalafil?
Tadalafil labeling lists contraindications including: Administration of tadalafil tablets to patients using any form of organic nitrate is contraindicated. Tadalafil was shown to potentiate the hypotensive effect of nitrates ( 4.1 ).. Always consult the full prescribing information and a clinician.
Note. Data for tadalafil is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

Search pharmacopeia

Search drugs, classes, and ingredients