Table 1.
Drug | Type | Mechanism | Dosage forms | Efficacy | Adverse reactions (TOP 3) | Adverse reactions (general) | Recommendation and Strenght rating | Contraindication | Preacaution (specific) | Precaution (general) |
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Tamsulosin | Selective α1-blockers | Relaxes smooth muscle in prostate and bladder neck and decreases urethral resistance through the blockade of α1-adrenergic receptors | Tamsulosin 0.4mg | Treatment of BPH a. Improving LUTS, Q-max and QOL rapidly b. Maintaining long-term efficacy c. Terazosin and doxazosin are also anti-hypertensive drugs. |
a.Headache b.Dizziness c.Abnormal Ejaculation |
a.Cardiovarscular events Dizziness 1.the most common adverse reaction of α1-blockers 2.the most common: terazosin, doxazosin Postural hypotension most common agents: terazosin, doxazosin less common agents: alfuzosin, tamsulosin least common agents: silodosin Asthenia b.EjD most common agents: silodosin, tamsulosin less common agents: terazosin, doxazosin least common agents: alfuzosin c.IFIS most common agents: tamsulosin others are relatively low. d.Nonselective α1-blockers have more side effects than selective α1-blockers. |
a.Offer α1-blockers to men with moderate-to-severe LUTS (Strength rating: Strong) |
Patients known to be hypersensitive to tamsulosin. | a.Orthostasis b.Drug-Drug Interactions: strong inhibitors of CYP3A4 (ketoconazole), CYP2D6 inhibitors (paroxetine,terbinafine), cimetidine, other α-blockers, warfarin. |
a. α1-blockers do not prevent the occurrence of urinary retention or need for surgery (all five α1-blockers) b.PDE5Is: The combination of α1-blocker and PDE5Is may cause symptomatic hypotension (all five α1-blockers) c. IFIS:Ophthalmologists should be informed about α1-blocker use prior to cataract surgery (all five α1-blockers) d. EjD: Sexually active patients treated with selective α1-blockers should be counselled about the risk of EjD (silodosin and tamsulosin) e.Dose titration and blood pressure monitoring. (doxazosin and terazosin) f.Priapism:All α1-blockers may cause priapism, although the risk is low. |
Silodosin | Silodosin 8mg | a.Retrograde Ejaculation b.Dizziness c.Diarrhea |
a.Severe renal impairment (CCr < 30 mL/min) b.Severe hepatic impairment (Child-Pugh score ≥ 10) c. Concomitant administration with strong Cytochrome P450 3A4 (CYP3A4) inhibitors (e.g., ketoconazole, clarithromycin, itraconazole, ritonavir) |
a.Postural hypotension may develop when beginning silodosin treatment. b. Hepatic or renal impairment c.Drug-Drug Interactions: CYP3A4 inhibitors |
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Alfuzosin | Non-selective α1-blockers | Alfuzosin 2.5mg | a.Dizziness b.Upper respiratory tract infection c.Headache |
a.Moderate or severe hepatic insufficiency b.CYP3A4 inhibitors: ketoconazole, itraconazole, and ritonavir c.Patients known to be hypersensitive to alfuzosin |
a. Drug-Drug Interactions: NOT to be used in combination with other α-blockers. b.Coronary Insufficiency: Alfuzosin should be discontinued if the symptoms of angina pectoris newly appear or worsen. c. QT prolongation history |
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Alfuzosin 10mg | ||||||||||
Terazosin | Terazosin 1mg Dose titration | a.Dizziness b.Asthenia c.Postural hypotension |
Patients known to be hypersensitive to terazosin | a.Syncope and ‘‘First-dose'' Effect: Treatment should always be initiated with a 1 mg dose, given at bedtime, then dosage should be increased slowly. b.Orthostatic Hypotension c.Anti-hypertensive drugs: significant hypotension should beconsidered when terazosin is administered concomitantly with other antihypertensive agents, especially the calcium channel blocker verapamil. |
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Doxazosin | Doxazosin 1mg Dose titration | a.Dizziness b.Fatigue c.Hypotension |
Patients known to be hypersensitive to doxazosin | a.Postural hypotension may develop when beginning doxazosin treatment. b. Drug-Drug Interactions: CYP3A4 inhibitors |
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Dutasterde | 5-ARIs (type I and type II 5-ARIs) | Inhibits the conversion of testosterone to DHT through the inbibition of type I and type II 5α-reductase | Dutasteride: 0.5mg | Treatment of BPH a. Reducing PV and the serum PSA level b. Improving Q-max, QOL, LUTS and nocturia c. Preventing disease progression d.Reduction in the risk of AUR and the need for surgical intervention. |
a.Impotence b.Decreased libido c.Ejaculation dysfunction | a.No Significant difference between dutasteride and finasteride b.Finasteride has fewer sexual side effects and breast complications . |
a.Use 5-ARIs in men who have moderate-to-severe LUTS and an increased risk of disease progression (e.g. prostate volume > 40 mL). (Strength rating: Strong) b.Counsel patients with regards to the onset of action (three to six months) of 5-ARIs. (Strength rating: Strong) |
a.Women and children: contraindicated for use in women and children. b.Patients with known hypersensitivity to dutasteride, other 5-ARIs |
a. Large PVR and/or severely diminished urinary flow may not be good candidates for 5-ARIs therapy b. Men being treated with dutasteride should not donate blood until at least 6 months have passed following their last dose. c. Caution should be used in the administration of dutasteride to patients with liver disease d. Care should be taken when administering dutasteride to patients taking potent, chronic CYP3A4 enzyme inhibitors(e.g., ritonavir) |
a.5-ARIs are suitable only for long-term treatment (years), because of the slow onset of action. b.The effect of 5-ARIs on the serum PSA concentration needs to be considered in relation to prostate carcinoma screening and PSA measure. c.Exposure of Women-Risk to Male Fetus: women who are pregnant or may be pregnant should not handle. d.5-ARIs are not indicated for use in women and children. |
Finasteride | 5-ARIs (type II 5-ARIs) |
Inhibits the conversion of testosterone to DHT through the inbibition of type II 5α-reductase | Finasteride 5mg | a.Impotence b.Decreased Libido c.Breast Enlargement |
a.Women and children: contraindicated for use in women and children. b.Patients with known hypersensitivity to finasteride, other 5-ARIs |
a.Increased risk of high-grade prostate cancer (Gleason score 8-10 prostate cancer) b.Mild effect on semen characteristics (not clinically meaningful) |
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Tolterodine | MRAs | Relaxes smooth muscle in bladder through inhibition of muscarinic receptors | Tolterodine 1mg | a.Improving storage LUTS and nocturia b.Treatment of OAB | a.Dry mouth b.Constipation c. Headache |
a. Use MRAs in men with moderate-to-severe LUTS who mainly have bladder storage symptoms. (Strength rating: Strong) b. Do not use MRAs in men with a PVR > 150 mL. (Strength rating: Weak) |
a.Patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. b.Patients with known hypersensitivity to tolterodine. |
a.High risk of Urinary Retention: For patients with clinically significant bladder outflow obstruction. b.High risk of Gastric Retention:For patients with gastrointestinal obstructive disorders, such as pyloric stenosis. c.Decreased gastrointestinal motility: Patients with decreased gastrointestinal motility should be carefully treated by tolterodine d.Patients being treated for narrow-angle glaucoma e.CNS Effects: Patients should be monitored for signs of anticholinergic CNS effects, particularly after beginning treatment or increasing the dose. f.Patients with Myasthenia Gravis g.Patients with Congenital or Acquired QT Prolongation h.Anaphylaxis and angioedema may occour after the first dose of tolterodine |
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Mirabegron | Beta-3 agonists | Relaxes the detrusor smooth muscle during the storage phase of the urinary bladder fill-void cycle by activation of β3-adrenergic receptor | Mirabegron 25mg | a.Improving OAB b. Increasesing bladder capacity |
a.Hypertension b.Nasopharyngitis c.Urinary tract infection | Use beta-3 agonists in men with moderate-to-severe LUTS who have mainly bladder storage symptoms. (Strength rating: Weak) |
Patients with known hypersensitivity to mirabegron. | a.Patients with hypertension: Periodic determination of blood pressure is recommended, especially in hypertensive patients. b.Urinary retention may occur in patients with Bladder Outlet Obstruction c.Urinary retention may occur in patients taking muscarinic antagonist medications for the treatment of OAB d.Angioedema: Angioedema may occur after the first dose of mirabegron e.Drugs Metabolized by CYP2D6: Appropriate monitoring and dose adjustment may be necessary, with drugs metabolized by CYP2D6, such as thioridazine, flecainide, and propafenone. |
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Tadalafil-Efficacy | PDE5Is | Relaxes urinary smooth muscle and the bladder detrusor by increasing the concentration of intracellular cGMP | Tadalafil 5mg | a. Treatment of BPH b. Treatment of ED c. Treatment of BPH and ED d. Combination therapy with finasteride for BPH e. Treatment of PAH |
a.Headache b.Dyspepsia c.Back pain | Use PDE5Is in men with moderate-to-severe LUTS with or without ED. (Strength rating : Strong) |
a.Nitrates b.Patients with a known serious hypersensitivity to tadalafil c.Concomitant Guanylate Cyclase Stimulators, such as riociguat d.Cardiovascular disease : • myocardial infarction within the last 90 days • unstable angina or angina occurring during sexual intercourse • New York Heart Association Class 2 or greater heart failure in the last 6 months • uncontrolled arrhythmias, hypotension (<90/50 mm Hg), or uncontrolled hypertension • stroke within the last 6 months. e.Renal impairment: patients with creatinine clearance less than 30 mL/min. f.Severe hepatic impairment |
a.Physicians should consider the cardiovascular status of their patients. b.Physicians should consider continuous plasma tadalafil levels when evaluating the potential for interactions with medications (e.g., nitrates, α-blockers,antihypertensives and potent inhibitors of CYP3A4 and with substantial consumption of alcohol. c.Prolonged Erection d.Priapism e.Sudden loss of vision in one or both eyes: physicians should stop PDE5Is immediately. f.Sudden Hearing Loss: stop PDE5Is immediately. g.Physicians should discuss with patients the potential for tadalafil to augment the blood-pressure-lowering effect of α-blockers and antihypertensive medications h.Substantial consumption of alcohol in combination with tadalafil can increase the potential for orthostatic signs and symptoms. i.Concomitant Use of Potent Inhibitors of CYP3A4 j.Combination With Other PDE5 Inhibitors or ED therapies k.Effects on Bleeding |
These data come from the EAU guideline (European Association of Urology, 2019) and the website of FDA. BPH, benign prostatic hyperplasia; LUTS, lower urinary tract symptoms; IFIS, intraoperative floppy iris syndrome. Orthostasis symptoms include: postural hypotension, dizziness, and vertigo. Priapism, persistent painful penile erection unrelated to sexual activity; AUR, acute urinary retention; CNS Effects, central nervous system effects including: dizziness, syncope; OAB, overactive bladder; cGMP, cyclic guanosine monophosphate; ED, erectile dysfunction; EjD, Ejaculation dysfunction; PAH, pulmonary arterial hypertension. Orthostatic signs and symptoms include: increase in heart rate, decrease in standing blood pressure, dizziness, and headache. CYP3A4, cytochrome P450 3A4; CYP2D6, cytochrome P450 2D6; PVR, post-void residual volume; 5-ARIs, 5α-reductase inhibitors; MRAs, muscarinic receptor antagonists; PDE5Is, phosphodiesterase type 5 inhibitors; Q-max, maximum urinary flow rate; QOL, quality of life; DHT, Dihydrotestosterone; PV, prostate volume; PSA, prostate-specific antigen; AUR, acute urinary retention; AUA-SI, American Urology Association Symptom Index; CCr, creatinine clearance.