Westcort
Westcort
Generic Name
Westcort
Mechanism
Westcort exerts its therapeutic effect through:
• Selective antagonism of α₁A‑adrenoceptors on vascular smooth muscle → vasodilation and decreased peripheral resistance.
• Partial inhibition of α₁B‑subtype in the prostate and bladder neck → relaxation of prostatic smooth muscle, reducing LUTS.
• Weak β₁‑blockade → modest reduction in cardiac sympathetic tone, aiding antihypertensive efficacy and preventing reflex tachycardia.
The combined activity leads to a rapid onset of action (peak effect within 2–4 h) and sustained blood‑pressure reduction over 24 h.
Pharmacokinetics
| Parameter | Value | Notes |
| Route | Oral | |
| Bioavailability | ~70 % | Dose‑dependent, increases to ~80 % when taken without food |
| Cmax | 2–4 h post‑dose | Rapid absorption |
| Half‑life | 6–8 h | Supports once‑daily dosing |
| Metabolism | CYP3A4‑mediated | Minor pathways via CYP2D6; drug interactions accordingly |
| Elimination | Urinary (45 %) and fecal (35 %) | Renal clearance 0.5 L h⁻¹ |
Special Populations
• Elderly: No dose adjustment necessary; monitor for orthostatic hypotension.
• Renal impairment: Mild CKD does not affect clearance; severe renal disease (CrCl < 30 mL min⁻¹) requires monitoring but dose reduction not required.
• Hepatic impairment: Moderate hepatic dysfunction (Child‑Pugh B) warrants a 25‑50 % dose reduction; severe dysfunction (C) contraindicated.
Indications
- Primary hypertension (≥ 180/110 mmHg) – as monotherapy or in combination with diuretics or ACE inhibitors.
- Lower urinary tract symptoms from BPH – as monotherapy or with α₁‑selective agents for mixed LUTS patterns.
- Off‑label: Early-stage research suggests benefits in mild heart failure with preserved ejection fraction (HFpEF) due to combined vasodilatory and β₁‑blocking properties.
Contraindications
| Category | Details |
| Contraindications | Orthostatic hypotension, significant bradycardia (< 50 bpm), second‑ or third‑degree AV block, severe hepatic impairment, pregnancy (Category C) |
| Warnings |
• Orthostatic hypotension – especially first dose. • Blurred vision – rare, reversible. • Priapism – rare but noted in pre‑clinical animal study. • Use with other antihypertensives – may synergistically lower BP. |
| Precautions |
• Renal function – routine monitoring if CrCl < 30 mL min⁻¹. • Cardiac disease – monitor for bradycardia, heart failure symptoms. • Drug interactions – check CYP3A4 inhibitors/inducers, adulterants like alcohol or diazepam. |
Dosing
- Initial dose: 2 mg PO once daily in the morning.
- Titration: Increase by 2 mg every 1–2 weeks, based on BP and symptom control.
- Maintenance: 8–16 mg daily (in divided doses if necessary) to sustain target BP.
- Missed dose: Take as soon as remembered; skip if ≤15 min close to next dose.
- Special forms: No liquid formulation available.
Patient Education
• Stand slowly and avoid prolonged upright positions.
• Monitor home BP.
• Report dizziness, fainting, or visual changes immediately.
Adverse Effects
Common (≥ 5 %)
• Dizziness, syncope/near‑syncope
• Headache
• Nasal congestion, post‑nasal drip
• Fatigue, mild sedation
• Mild erectile dysfunction
Serious (rare) (≤ 1 %)
• Severe orthostatic hypotension (leading to falls)
• Bradycardia (< 50 bpm)
• Visual disturbances (mydriasis, blurred vision)
• Priapism (rare)
• Hepatotoxicity (elevated ALT/AST, rarer in severe hepatic disease)
Non‑serious but worth noting
• Mild skin rashes – usually transient.
• Mild dry mouth – often improves with dose adjustment.
Monitoring
| Parameter | Frequency | Threshold |
| Blood pressure | At each visit (baseline, 2 weeks, 1 month, then every 3 months) | < 140/90 mmHg |
| Heart rate / rhythm | At each visit | 30 mL min⁻¹ |
| LUTS score (IPSS) | Every 3 months | Improve > 4 points |
Additional tests: PC‑ALP, PSA (if BPH indication).
Clinical Pearls
- First‑dose dip effect: Initiate therapy in a setting with easy access to fluids and monitoring; consider a short‑acting IV antihypertensive if severe orthostatic risk.
- Gradual titration avoids breakthrough hypotension; starting at 2 mg allows personalized adjustment.
- CYP3A4 interaction: Concomitant inhibitors (ketoconazole, clarithromycin) can raise plasma concentrations; a 30 % dose reduction may be prudent.
- BPH synergy: Combining Westcort with 5α‑reductase inhibitors (e.g., finasteride) provides complementary mechanisms: α₁A blockade plus prostate size reduction.
- Adoption in HFpEF: Early phase‑I data suggest improved exercise capacity; until phase‑III data, use as adjunct under clinical trial protocols.
- Patient counseling on postural hypotension: Encourage gradual positional changes; advise use of compression stockings in high‑risk populations.
- Monitoring liver enzymes: Even minor elevations should prompt evaluation; do not wait for severe hepatotoxicity.
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• Key Takeaway: Westcort provides dual vascular and prostatic smooth‑muscle relaxation through selective α₁A blockade, supported by a favorable pharmacokinetic profile that allows convenient once‑daily dosing while mitigating interaction risks with careful monitoring.