Note: If therapy is discontinued for more than several days, begin with initial dose and retitrate as needed due to risk of orthostatic hypotension.
Benign prostatic hyperplasia (monotherapy or combination therapy):
Note: In patients with moderate to severe predominant storage lower urinary tract symptoms, use in combination with beta-3 agonist or anticholinergic agent. In patients with a significantly enlarged prostate (prostate volume >30 mL, prostate-specific antigen >1.5 ng/dL, or palpable prostate enlargement on digital rectal exam), use in combination with 5-alpha reductase inhibitor (Ref).
Immediate release: Oral: Initial: 1 mg once daily in the morning or evening; may titrate by doubling the daily dose (eg, to 2 mg, then 4 mg, then 8 mg) at 1- to 2-week intervals up to 8 mg once daily based on patient response and tolerability; maximum dose: 8 mg/day.
Extended release: Oral: 4 mg once daily in the morning; may titrate based on response and tolerability after 3 to 4 weeks to 8 mg once daily; maximum dose: 8 mg/day.
Conversion to extended release from immediate release: If immediate release is normally taken in the evening, do not administer evening dose. Then start extended-release product the following morning at lowest dose (4 mg once daily) and titrate.
Hypertension (alternative agent):
Note: Not recommended for initial management but may be considered as additional therapy for resistant hypertension in patients who do not respond adequately to combination therapy with preferred agents (Ref).
Immediate release: Oral: Initial: 1 mg once daily; titrate gradually as needed based on response and tolerability up to a dose of 16 mg once daily (Ref).
Ureteral stone(s) expulsion (off-label use):
Note: Consider for use in patients with ureteral stones >5 and ≤10 mm (Ref). Although most evidence exists for distal ureteral stones, given the low side effect profile of alpha-blockers, may consider use in patients with stones in any location of ureter (Ref). Additionally, may consider for use after shock wave lithotripsy to help pass stone fragments (Ref). A uroselective alpha-blocker (eg, tamsulosin) may be preferred to decrease risk of hypotension (Ref).
Immediate release: Oral: 4 mg once daily in the evening until stone passage or for up to 4 weeks (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
Altered kidney function: No dosage adjustment necessary for any degree of kidney dysfunction (Ref).
Hemodialysis, intermittent (thrice weekly): Not significantly dialyzed (Carlson 1986): No supplemental dose or dosage adjustment necessary (Ref).
Peritoneal dialysis: Unlikely to be significantly dialyzed (highly protein bound): No dosage adjustment necessary (Ref).
CRRT: No dosage adjustment necessary (Ref).
PIRRT (eg, sustained, low-efficiency diafiltration): No dosage adjustment necessary (Ref).
Mild to moderate impairment (Child-Pugh class A or B): There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.
Severe impairment (Child-Pugh class C): Use is not recommended.
Refer to adult dosing.
Avoid use for hypertension treatment (alternative agents have superior risk-benefit profiles) (Ref).
(For additional information see "Doxazosin: Pediatric drug information")
Note: If drug is discontinued for greater than several days, consider beginning with initial dose and retitrate as needed.
Dysfunctional voiding: Limited data available, efficacy results variable: Children ≥3 years and Adolescents: Oral: Immediate release: Initial: 0.5 mg once daily at bedtime; some trials maintained a fixed dose; others titrated at weekly or biweekly intervals to effect as tolerated (maximum daily dose: 2 mg/day) (Ref). In some trials, a larger initial dose (1 mg/day) was used in patients weighing >40 to 50 kg (Ref).
Hypertension: Limited data available: Children and Adolescents: Oral: Immediate release: Initial: 1 mg/day; maximum daily dose: 4 mg/day (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in manufacturer's labeling; however, limited data suggest renal impairment does not significantly alter pharmacokinetic parameters.
Mild to moderate impairment: There are no dosage adjustments provided in the manufacturer's labeling; use with caution and monitor closely.
Severe impairment: There are no dosage adjustments provided in the manufacturer's labeling; use is not recommended in adult patients with severe hepatic impairment (Child-Pugh class C).
Intraoperative floppy iris syndrome (IFIS) has been reported in patients with current or prior use of alpha-1 blockers undergoing cataract surgery (Ref). Studies report significantly higher surgical complication rates for patients who experience IFIS (Ref).
Mechanism: Not completely established; may be related to a combination of the pharmacologic action (ie, inhibition of the iris dilator smooth muscle contraction) and long-term smooth muscle atrophy from accumulation in iris pigment epithelial cells (Ref).
Onset: Varied; may occur with current (within a few days to months of initiation) or prior use (years following discontinuation) (Ref). A minimum 3-month duration of alpha-1 blocker use has been proposed as a risk for IFIS (Ref).
Risk factors:
• Individual alpha-1 blocker (risk highest with tamsulosin) (Ref)
• Hypertension (Ref)
• Males (Ref)
• Older age (Ref)
• Decreased preoperative dilated pupil diameter (Ref)
Doxazosin is associated with orthostatic hypotension, which can manifest as dizziness and vertigo; however, some studies suggest that the differences in blood pressure reduction in the standing versus sitting position are not significantly different with use of doxazosin (Ref).
Mechanism: Dose-related; related to the pharmacologic action (ie, inhibition of vascular smooth muscle contraction and vasodilation) (Ref).
Onset: Varied; “first dose” orthostatic hypotension may occur 2 to 6 hours after dose. However, has also occurred months after initiation (Ref).
Risk factors:
• Individual alpha-1 blocker (risk lowest with tamsulosin) (Ref)
• First dose or redose after dose interruption (Ref)
• Rapid increase in dose
• Concurrent medications that cause orthostatic hypotension (eg, antihypertensives, nitrates, phosphodiesterase-5 inhibitors) (Ref)
• Females >65 years of age (Ref)
• Alcohol use (Ref)
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.
>10%: Nervous system: Dizziness (≤19%) (table 1) , fatigue (≤12%), malaise (≤12%), vertigo (≤16%) (table 2)
Drug (Doxazosin) |
Placebo |
Dose |
Dosage Form |
Indication |
Number of Patients (Doxazosin) |
Number of Patients (Placebo) |
Comments |
---|---|---|---|---|---|---|---|
16% |
9% |
1 to 16 mg once daily in hypertensives and 0.5 to 8 mg once daily in normotensives |
Immediate-release tablets |
Benign prostatic hyperplasia |
665 |
300 |
Including vertigo |
19% |
9% |
1 to 16 mg once daily |
Immediate-release tablets |
Hypertension |
339 |
336 |
N/A |
9% |
2% |
1 to 8 mg once daily |
Immediate-release tablets |
Hypertension |
651 |
156 |
N/A |
5% |
2% |
4 to 8 mg once daily |
Extended-release tablets |
Hypertension |
666 |
156 |
N/A |
Drug (Doxazosin) |
Placebo |
Dose |
Dosage Form |
Indication |
Number of Patients (Doxazosin) |
Number of Patients (Placebo) |
Comments |
---|---|---|---|---|---|---|---|
16% |
9% |
1 to 16 mg once daily in hypertensives and 0.5 to 8 mg once daily in normotensives |
Immediate-release tablets |
Benign prostatic hyperplasia |
665 |
300 |
Including dizziness |
4% |
0.6% |
1 to 8 mg once daily |
Immediate-release tablets |
Hypertension |
651 |
156 |
N/A |
2% |
0.6% |
4 to 8 mg once daily |
Extended-release tablets |
Hypertension |
666 |
156 |
N/A |
1% to 10%:
Cardiovascular: Edema (≤3%), hypotension (≤2%), orthostatic hypotension (1% to 2%) (table 3)
Drug (Doxazosin) |
Placebo |
Dose |
Dosage Form |
Indication |
Number of Patients (Doxazosin) |
Number of Patients (Placebo) |
---|---|---|---|---|---|---|
2% |
0.6% |
1 to 8 mg once daily |
Immediate-release tablets |
Hypertension |
651 |
156 |
1% |
0.6% |
4 to 8 mg once daily |
Extended-release tablets |
Hypertension |
666 |
156 |
Gastrointestinal: Abdominal pain (2%), dyspepsia (1%), nausea (1% to 2%), xerostomia (1%)
Genitourinary: Urinary tract infection (1%)
Nervous system: Asthenia (4% to 7%), drowsiness (1% to 5%), headache (6%)
Neuromuscular & skeletal: Myalgia (≤1%)
Renal: Polyuria (2%)
Respiratory: Dyspnea (1% to 3%), respiratory tract infection (5%), rhinitis (3%)
<1%:
Cardiovascular: Angina pectoris, chest pain, palpitations, syncope, tachycardia
Endocrine & metabolic: Decreased libido, hot flash
Gastrointestinal: Diarrhea
Genitourinary: Dysuria, impotence
Neuromuscular & skeletal: Arthralgia
Respiratory: Epistaxis
Frequency not defined: Hematologic & oncologic: Decreased neutrophils
Postmarketing:
Cardiovascular: Acute myocardial infarction, bradycardia (Pigot 2022), cardiac arrhythmia
Dermatologic: Alopecia, pruritus, skin rash, urticaria
Endocrine & metabolic: Gynecomastia (Viola 2014)
Gastrointestinal: Anorexia, gastrointestinal obstruction, vomiting
Genitourinary: Hematuria, nocturia, priapism (Avisrror 2000), urinary frequency
Hematologic & oncologic: Leukopenia, purpuric disease, thrombocytopenia
Hepatic: Abnormal hepatic function tests, cholestatic hepatitis, hepatitis, jaundice
Hypersensitivity: Angioedema (Piller 2006)
Nervous system: Agitation, cerebrovascular accident (Mansoor 2002), hypoesthesia, myasthenia, nervousness, paresthesia
Neuromuscular & skeletal: Muscle cramps
Ophthalmic: Blurred vision, intraoperative floppy iris syndrome (cataract surgery) (Haridas 2013)
Respiratory: Aggravated bronchospasm
Hypersensitivity to doxazosin, other quinazolines (eg, prazosin, terazosin), or any component of the formulation.
Canadian labeling: Additional contraindications (not in US labeling): Galactose intolerance, the congenital lactase deficiency or glucose-galactose malabsorption.
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).
• Hematologic effect: Decreases in WBC and neutrophil count have been reported; WBC and neutrophils returned to normal after discontinuation.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with heart failure, angina pectoris, or recent acute myocardial infarction (within the last 6 months). If symptoms of angina pectoris appear or worsen, discontinue use. In a scientific statement from the American Heart Association, doxazosin has been determined to be an agent that may exacerbate underlying myocardial dysfunction (magnitude: moderate) (AHA [Page 2016]).
• Hepatic impairment: Use with caution in patients with mild to moderate impairment (Child-Pugh class A and B); monitor blood pressure and for symptoms of hypotension. Not recommended in severe impairment (Child-Pugh class C) (extensively metabolized).
Special populations:
• Cataract surgery patients: Intraoperative floppy iris syndrome has been observed in cataract surgery patients who were on or were previously treated with alpha-1 blockers; there appears to be no benefit in discontinuing alpha-blocker therapy prior to surgery. May require modifications to surgical technique; instruct patients to inform ophthalmologist of current or previous alpha-1 blocker use when considering eye surgery.
Dosage form specific issues:
• Extended release: Consists of drug within a nondeformable matrix; following drug release/absorption, the matrix/shell is expelled in the stool. The use of nondeformable products in patients with known stricture/narrowing of the GI tract has been associated with symptoms of obstruction. Use caution in patients with increased GI retention (eg, chronic constipation) as doxazosin exposure may be increased.
Other warning/precautions:
• Appropriate use: Extended release: Not indicated for use in women or for the treatment of hypertension.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tablet, Oral:
Cardura: 1 mg
Cardura: 1 mg [DSC], 2 mg [scored]
Cardura: 2 mg [DSC] [scored; contains fd&c yellow #6 (sunset yellow), quinoline yellow (d&c yellow #10)]
Cardura: 4 mg [scored]
Cardura: 4 mg [DSC] [scored; contains fd&c yellow #6 (sunset yellow)]
Generic: 1 mg, 2 mg, 4 mg
Tablet, Oral, as mesylate:
Cardura: 8 mg [scored]
Cardura: 8 mg [DSC] [scored; contains fd&c blue #2 (indigotine,indigo carmine), quinoline yellow (d&c yellow #10)]
Generic: 8 mg
Tablet Extended Release 24 Hour, Oral:
Cardura XL: 4 mg, 8 mg
May be product dependent
Tablet, 24-hour (Cardura XL Oral)
4 mg (per each): $7.93
8 mg (per each): $8.33
Tablets (Cardura Oral)
1 mg (per each): $6.90
2 mg (per each): $6.90
4 mg (per each): $7.24
8 mg (per each): $7.61
Tablets (Doxazosin Mesylate Oral)
1 mg (per each): $1.02 - $1.35
2 mg (per each): $0.97 - $1.35
4 mg (per each): $1.03 - $1.42
8 mg (per each): $1.49
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Generic: 1 mg, 2 mg, 4 mg
Oral:
Extended release: Swallow tablets whole; do not crush, cut, chew, or divide. Administer with morning meal.
Bariatric surgery: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. Switch to IR formulation.
Immediate release: Administer daily dose either in the morning or evening.
Oral: Immediate release: Administer without regard to meals at the same time each day
Benign prostatic hyperplasia: Treatment of signs and symptoms of benign prostatic hyperplasia.
Hypertension (immediate release only): Management of hypertension. Note: Alpha blockers are not recommended as first-line therapy (ACC/AHA [Whelton 2018]).
Ureteral stone(s), expulsion
Doxazosin may be confused with doxapram, doxepin, DOXOrubicin
Cardura may be confused with Cardene, Cordarone, Cordran, Coumadin, K-Dur, Ridaura
Beers Criteria: Doxazosin is identified in the Beers Criteria as a potentially inappropriate medication for hypertension in patients 65 years and older due to its high risk of orthostatic hypotension. Avoid use for hypertension treatment (alternative agents have superior risk-benefit profiles) (Beers Criteria [AGS 2019]). Note: Updates for the American Geriatrics Society 2023 AGS Beers Criteria for Potentially Inappropriate Medication Use in Older Adults are in process.
Substrate of CYP2C19 (minor), CYP2D6 (minor), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alpha-/Beta-Agonists: Alpha1-Blockers may diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Similarly, Alpha-/Beta-Agonists may antagonize Alpha1-Blocker vasodilation. Risk C: Monitor therapy
Alpha1-Agonists: Alpha1-Blockers may diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1-Blocker vasodilation. Risk C: Monitor therapy
Alpha1-Blockers: May enhance the antihypertensive effect of other Alpha1-Blockers. Risk X: Avoid combination
Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider therapy modification
Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor therapy
Arginine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Brigatinib: May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Risk X: Avoid combination
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Doxazosin. Risk C: Monitor therapy
Dapoxetine: May enhance the orthostatic hypotensive effect of Alpha1-Blockers. Risk C: Monitor therapy
Dexmethylphenidate: May diminish the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Risk C: Monitor therapy
Flunarizine: May enhance the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Herbal Products with Blood Pressure Increasing Effects: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Herbal Products with Blood Pressure Lowering Effects: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy
Levodopa-Foslevodopa: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Foslevodopa. Risk C: Monitor therapy
Loop Diuretics: May enhance the hypotensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Risk C: Monitor therapy
Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Risk D: Consider therapy modification
Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Alpha1-Blockers (Nonselective). Management: Ensure patient is stable on one agent prior to initiating the other, and always initiate combination using the lowest possible dose of the drug being added. When tadalafil is used for treatment of BPH, concurrent alpha 1-blockers are not recommended. Risk D: Consider therapy modification
Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Rilmenidine: Alpha1-Blockers may enhance the hypotensive effect of Rilmenidine. Risk C: Monitor therapy
Medications considered acceptable for the treatment of chronic hypertension during pregnancy may generally be continued in patients trying to conceive. Doxazosin is not considered a preferred agent for use in pregnant patients; consider transitioning to a preferred agent in patients planning to become pregnant (ACC/AHA [Whelton 2018]; ACOG 2019; NICE 2019).
Doxazosin crosses the placenta (Versmissen 2016).
Chronic maternal hypertension is associated with adverse events in the fetus/infant. Chronic maternal hypertension may increase the risk of birth defects, low birth weight, premature delivery, stillbirth, and neonatal death. Actual fetal/neonatal risks may be related to the duration and severity of maternal hypertension. Untreated chronic hypertension may also increase the risks of adverse maternal outcomes, including gestational diabetes, preeclampsia, delivery complications, stroke, and myocardial infarction (ACOG 2019).
Patients with preexisting hypertension may continue their medication during pregnancy unless contraindications exist (ESC [Regitz-Zagrosek 2018]). When treatment of chronic hypertension during pregnancy is indicated, agents other than doxazosin may be preferred (ACOG 2019; ESC [Cífková 2020]; ESC [Regitz-Zagrosek 2018]; SOGC [Magee 2022]).
Untreated hypertension due to a pheochromocytoma during pregnancy is associated with a high rate of maternal and fetal mortality; therefore, treatment is recommended (ESC [Cífková 2020]). Case reports describe the use of doxazosin for the treatment of hypertension due to pheochromocytoma or paraganglioma in pregnant patients (Bettencourt 2022; Chu 2020; Giampaolino 2018; van der Weerd 2017). Doxazosin is a recommended option for the treatment of hypertension due to pheochromocytoma during pregnancy (Gruber 2021; Lenders 2019; Pacu 2021).
Although alpha-blockers may be used to facilitate ureteral stone expulsion, treatments other than doxazosin are preferred if stone removal is needed during pregnancy (AUA/ES [Assimos 2016]; Juliebø-Jones 2022; Lee 2021; Lloyd 2016).
Doxazosin is present in breast milk.
Data related to the presence of doxazosin in breast milk are available from a single case report following a maternal dose of doxazosin 4 mg every 24 hours for 2 doses for urinary stones. Milk samples were obtained at various intervals over 24 hours, beginning ~17 hours after the first dose. Maternal serum samples were obtained at nearly the same times, beginning ~1 hour later. The highest serum and milk concentrations of doxazosin were observed ~1 hour after the dose. Using the highest milk concentration (4.15 mcg/L), the estimated dose to the breastfeeding infant was calculated to be <1% of the weight-adjusted maternal dose (Jensen, 2013). In general, breastfeeding is considered acceptable when the relative infant dose of a medication is <10% (Anderson 2016; Ito 2000).
In a second case report, doxazosin was not present in breast milk when sampled 30 hours after the last maternal dose. In this case, maternal doxazosin was administered for hypertension due to a pheochromocytoma, surgically removed after delivery. Doxazosin 4 mg once daily was used during pregnancy, increased to 6 mg/day prior to delivery, and 8 mg/day 3 days postpartum prior to being discontinued (Versmissen 2016).
Administer extended-release tablet with morning meal.
BP.
Benign prostatic hyperplasia: International Prostate Symptom Score (baseline and 4 to 12 weeks after treatment initiation); urinalysis (baseline); objective and subjective signs of relief of benign prostatic hyperplasia and lower urinary tract symptoms (AUA [Lerner 2021]).
Hypertension: Competitively inhibits postsynaptic alpha1-adrenergic receptors which results in vasodilation of veins and arterioles and a decrease in total peripheral resistance and blood pressure; ~50% as potent on a weight by weight basis as prazosin.
BPH: Competitively inhibits postsynaptic alpha1-adrenergic receptors in prostatic stromal and bladder neck tissues. This reduces the sympathetic tone-induced urethral stricture causing BPH symptoms.
Duration: >24 hours
Protein binding: ~98%
Metabolism: Extensively hepatic to active metabolites; primarily via CYP3A4; secondary pathways involve CYP2D6 and 2C9
Bioavailability: Immediate release: ~65%; Extended release relative to immediate release: 54% to 59%
Half-life elimination: Immediate release: ~22 hours; Extended release: 15 to 19 hours
Time to peak, serum: Immediate release: 2 to 3 hours; Extended release: 8 ± 3.7 to 9 ± 4.7 hours
Excretion: Feces (~63%, primarily as metabolites [4.8% as unchanged]); urine (9%, primarily as metabolites)
Hepatic function impairment: Immediate release: 40% increase in exposure in mild impairment (Child-Pugh class A).
Older adult: Extended release: Cmax and AUC increased 27% and 34% respectively in elderly patients.
آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟