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Terazosin Hydrochloride

Class: alpha-Adrenergic Blocking Agents
VA Class: CV150
Chemical Name: Piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl-)carbonyl)-, monohydrochloride, dihydrate
CAS Number: 70024-40-7


Postsynaptic α1-adrenergic blocking agent; quinazoline derivative.1 2 3 4 5 6 8 9 10

Uses for Terazosin Hydrochloride


Management of hypertension (alone or in combination with other classes of antihypertensive agents).1 3 4 6 8 11 12 13 14 30 31 32 500

Not considered a preferred agent for initial management of hypertension, but may be useful in the management of resistant hypertension as a component of combination therapy.501 502 503 504

Most effective when used in combination with a diuretic; beneficial effects of α1-blockers on blood glucose and lipid concentrations also may mitigate some adverse metabolic effects of diuretics.504

Some experts state that an α1-blocker may be a useful component of antihypertensive treatment regimens in older men with coexisting benign prostatic hyperplasia (BPH);504 however, the American Urology Association (AUA) states that monotherapy with these drugs is not optimal in hypertensive patients with lower urinary tract symptoms (LUTS) or BPH and that such conditions should be managed separately.230

Benign Prostatic Hyperplasia

Reduction of urinary obstruction and relief of associated manifestations in patients with symptomatic BPH.1 5 9 17 18 21 23 25 33

Although drug therapy usually is not as effective as surgical therapy, it may provide adequate symptomatic relief with fewer and less serious adverse effects compared with surgery.59

May consider combined therapy with an α1-adrenergic blocker and 5α-reductase inhibitor for men with bothersome moderate to severe BPH and demonstrable prostatic enlargement.59 Has been more effective than therapy with either drug alone in preventing long-term BPH symptom progression.59 Men at risk for BPH progression are most likely to benefit from combination therapy.59

Terazosin Hydrochloride Dosage and Administration



  • Carefully monitor BP during initial titration or subsequent upward dosage adjustment.500 501

  • Goal is to achieve and maintain optimal control of BP; individualize specific target BP based on consideration of multiple factors, including patient age and comorbidities, and currently available evidence from clinical studies.500 501


Oral Administration

Food may delay time to peak plasma concentrations by about 40 minutes but has little effect on extent of absorption.1 28 Manufacturer makes no specific recommendations regarding administration with meals.1


Administer initial dose at bedtime; may administer maintenance doses in the morning.1

Administer once daily or, if needed for optimal BP control, in 2 divided doses at 12-hour intervals.1 500


Administer once daily at bedtime.1


Available as terazosin hydrochloride; dosage expressed in terms of terazosin.1

Individualize dosage according to patient response and tolerance.1 3 Initiate at low dosage to minimize frequency of postural hypotension and syncope.1

Monitor BP 2–3 hours after dosing and at end of dosing interval to determine whether peak and trough responses are similar and to assess potential manifestations (e.g., dizziness, palpitations) of an excessive response.1

If therapy is interrupted for several days or longer, restart using initial dosage regimen.1

Pediatric Patients


Initially, 1 mg once daily.76 Increase dosage as necessary up to a maximum of 20 mg once daily.76



Initially, 1 mg daily at bedtime.1 3 May increase dosage gradually to 5 mg daily,1 3 with further titration up to 20 mg daily if BP is not controlled.1 500

Each increase should be delayed until BP has stabilized at a given dosage.1 3


Initially, 1 mg daily at bedtime.1 9 May increase daily dosage to 2 mg and thereafter to 5 mg and 10 mg, if necessary, to reduce symptoms and/or improve urinary flow rates.1 9

Prescribing Limits

Pediatric Patients


Maximum 20 mg daily.76



Maximum 40 mg daily;1 however, dosages >20 mg daily do not appear to improve BP control.1 3


Maximum 20 mg daily.1

Special Populations

Hepatic Impairment

Manufacturer makes no specific dosage recommendations; effects on the pharmacokinetics of terazosin have not been elucidated.1

Renal Impairment

Clinically important alterations in the pharmacokinetics of terazosin not observed to date;1 3 28 29 dosage adjustment not necessary.3 28 29 33

Administration of supplemental doses of the drug following hemodialysis does not appear to be necessary.1

Geriatric Patients

Use with caution; generally, increase dosage more slowly in geriatric patients than in younger adults.7 9

Cautions for Terazosin Hydrochloride


  • Known hypersensitivity to terazosin, quinazolines (e.g., doxazosin, prazosin), or any ingredient in the formulation.1 33



Postural Hypotension

Marked hypotension, especially in the upright position, can occur; may be accompanied by syncope, palpitations, and other postural effects (e.g., dizziness, lightheadedness, vertigo).1 2 3 4 6 9 13 30

Postural effects are most common after an initial dose, shortly after dosing (e.g., within 90 minutes), when dosage is increased, or when therapy is resumed after an interruption exceeding a few days.1

To decrease risk of excessive hypotension and syncope, initiate therapy at low dose and titrate carefully, lessen level of salt restriction, and avoid diuretics just prior to initiation of terazosin therapy.1 3 4 6 30


Priapism reported rarely; may lead to permanent impotence if not treated promptly.1 48 49 (See Advice to Patients.)

General Precautions

Prostate Cancer

Exclude possibility of prostate cancer before initiation of therapy for BPH.1 9

Specific Populations


Category C.1


Not known whether terazosin is distributed into milk.1 Caution if used in nursing women.1

Pediatric Use

Safety and efficacy not established in patients <21 years of age.1 33

Geriatric Use

Geriatric patients may be particularly susceptible to postural effects and other adverse effects.9 (See Geriatric Patients under Dosage and Administration.)

Common Adverse Effects

In the treatment of hypertension: dizziness, headache, asthenia (weakness, tiredness, lassitude, fatigue), nasal congestion, peripheral edema, somnolence, nausea, palpitation.1 3 4 6 13

In the treatment of BPH: dizziness, asthenia, headache, postural hypotension, somnolence.1 9

Interactions for Terazosin Hydrochloride

Antihypertensive Agents

Possible rapid fall in BP and exacerbation of postural effects.1 9 Use with caution; may need to reduce and/or retitrate dosage.1

Specific Drugs




No interaction observed1

β-Adrenergic blocking agents (e.g., atenolol, propranolol)

No interaction observed1


No interaction observed1


No interaction observed1

Antihistamines (e.g., chlorpheniramine)

No interaction observed1


Increased peak plasma concentrations of terazosin1


No interaction observed1


No interaction observed1


No interaction observed1


No interaction observed1

Diuretics, thiazide (e.g., hydrochlorothiazide)

No interaction observed1


No interaction observed1

Hypoglycemic agents

No interaction observed1

NSAIAs (e.g., aspirin, ibuprofen, indomethacin)

No interaction observed1

Sympathomimetic (adrenergic) agents (e.g., phenylephrine, pseudoephedrine)

No interaction observed1


Increased AUC of terazosin; decreased time to peak plasma terazosin concentrations1

Terazosin Hydrochloride Pharmacokinetics



Rapidly and almost completely absorbed from the GI tract following oral administration.1 2 Peak plasma concentration attained in about 1 hour.1


Food has minimal effect on extent of absorption; however, time to peak plasma concentration is delayed by about 40 minutes.1 28



Not known whether terazosin is distributed into breast milk.1

Plasma Protein Binding

90–94%.1 a



Extensively metabolized in the liver,a with minimal first-pass metabolism.1

Elimination Route

Excreted in urine (40%) and in feces (60%).1


Adults: approximately 12 hours.1

Geriatric patients: approximately 14 hours.1

Special Populations

In geriatric patients, plasma clearance is decreased by about 30%.1





20–25°C.1 Protect from light and moisture.1


  • Reduces peripheral vascular resistance and BP as a result of vasodilating effects; produces both arterial and venous dilation.1 3 4 6 10

  • Binds to α1-adrenergic receptors in the prostate and the bladder trigone, resulting in decreased urinary outflow resistance in men.5 9

  • May improve to limited extent the serum lipid profile (e.g., small increases in HDL/total cholesterol ratio; small decreases in LDL, total cholesterol, and triglyceride concentrations).1 3 8 9 10 11 28 31 32

Advice to Patients

  • Possible syncopal and orthostatic symptoms, especially at initiation of therapy; importance of avoiding driving or other hazardous tasks for 12 hours after first dose, a dosage increase, or when resumed after therapy interruption.1 9

  • Importance of sitting or lying down when symptoms of lowered BP occur, and of rising carefully from a sitting or lying position.1

  • Importance of informing clinician if bothersome dizziness, lightheadedness, or palpitations occur.1

  • Possible drowsiness or somnolence; use caution when operating machinery or driving a motor vehicle until effects on individual are known.1 9

  • Importance of men seeking medical treatment if painful or sustained (for hours) erection occurs.1 48 49

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as concomitant illnesses.1

  • Importance of advising patients of other important precautionary information.1 (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Terazosin Hydrochloride


Dosage Forms


Brand Names




1 mg (of terazosin)*

Terazosin Hydrochloride Capsules

2 mg (of terazosin)*

Terazosin Hydrochloride Capsules

5 mg (of terazosin)*

Terazosin Hydrochloride Capsules

10 mg (of terazosin)*

Terazosin Hydrochloride Capsules

AHFS DI Essentials. © Copyright 2018, Selected Revisions February 13, 2015. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.


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