Tadalafil (CAS 171596-29-5)
Indications: Erectile dysfunction and pulmonary hypertension
Pharmacology: It is a selective reversible inhibitor of guanosine cyclophosphate (cGMP)-specific phosphodiesterase 5 (PDE5).When sexual stimulation leads to the local release of nitric oxide, PDE5 is inhibited by tadalafil, which increases the level of cGMP in the cavernous body of the penis, which leads to relaxation of smooth muscles and blood flowing into the penis tissue to produce an erection, such as asexual stimulation.
Compound Information : Cialis (Tadalafil)
| Category | Details |
|---|---|
| Name | Cialis (Tadalafil) |
| CAS Number | 171596-29-5 |
| Synonyms | Tadalafil; (6R,12aR)-6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1′,2′:1,6]pyrido[3,4-b]indole-1,4-dione; IC 351 |
| EINECS Number | 687-782-2 |
| Molecular Formula | C₂₂H₁₉N₃O₄ |
| Molecular Weight | 389.4 g/mol |
| Chemical Properties | |
| – Appearance | White to Off-White Crystalline Solid |
| – Melting Point | 298–300°C |
| – Solubility | DMSO (20 mg/mL, clear) |
| – Form | Powder |
| – Color | White to Beige |
| – Stability | Unstable in Methanol; store sealed in dry conditions at 2–8°C |
| InChIKey | WOXKDUGGOYFFRN-IIBYNOLFSA-N |
| SMILES | N1C2=C(C=CC=C2)C2C[C@]3([H])C(=O)N(C)CC(=O)N3C@HC1=2 |
Key Notes:
- Pharmacological Role:
- A phosphodiesterase type 5 (PDE5) inhibitor that relaxes smooth muscle in blood vessels, enhancing blood flow to the penis for erectile function.
- Dual-action: Treats erectile dysfunction (ED) and benign prostatic hyperplasia (BPH) by improving urinary flow.
- Clinical Applications:
- Approved Indications:
- Erectile dysfunction (ED): Improves erectile response up to 36 hours post-dose (“weekend pill”).
- BPH: Relieves urinary symptoms (e.g., frequent urination, weak stream).
- Dosage:
- On-demand ED treatment: 5–20 mg taken 30 minutes before sexual activity (max 1 dose/day).
- Daily BPH treatment: 2.5–5 mg taken at the same time daily.
- Approved Indications:
- Safety & Toxicity:
- Common Side Effects: Headache, flushing, back pain, muscle aches, nasal congestion.
- Rare but Severe Risks:
- Sudden vision/hearing loss.
- Priapism (prolonged erection >4 hours).
- Hypotension (when combined with nitrates).
- Contraindications & Interactions:
- Absolute Contraindications:
- Concomitant use with nitrates (e.g., nitroglycerin) due to life-threatening hypotension.
- Hypersensitivity to tadalafil or excipients.
- Drug Interactions:
- Alpha-blockers (e.g., tamsulosin): Risk of hypotension; use lowest effective dose.
- CYP3A4 inhibitors (e.g., ketoconazole): Reduce tadalafil dose (max 10 mg/72 hours).
- Absolute Contraindications:
- Supplier Information:
- Original Brand: Cialis® (Eli Lilly and Company).
- Pricing: Original drug ~20–40/tablet;generics 0.2–5/tablet (varies by region and dose).
Analytical & Handling Guidelines:
- Detection: UV-Vis spectroscopy (λmax = 288 nm in methanol).
- Storage: Protect from light and moisture; avoid freezing.
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