Please wait while the formulary information is being retrieved.
Drug overview for GUANFACINE HCL (guanfacine hcl):
Generic name: GUANFACINE HCL (GWAN-fuh-seen)
Drug class: Central Adrenolytics
Therapeutic class: Cardiovascular Therapy Agents
Guanfacine is a phenylacetyl-guanidine derivative hypotensive agent; the drug is a selective alpha2-adrenergic agonist.
No enhanced Uses information available for this drug.
Generic name: GUANFACINE HCL (GWAN-fuh-seen)
Drug class: Central Adrenolytics
Therapeutic class: Cardiovascular Therapy Agents
Guanfacine is a phenylacetyl-guanidine derivative hypotensive agent; the drug is a selective alpha2-adrenergic agonist.
No enhanced Uses information available for this drug.
DRUG IMAGES
GUANFACINE 1 MG TABLET
GUANFACINE 2 MG TABLET
The following indications for GUANFACINE HCL (guanfacine hcl) have been approved by the FDA:
Indications:
Hypertension
Professional Synonyms:
Elevated blood pressure
Essential hypertension
Hyperpiesia
Hyperpiesis
Hypertensive disorder
Systemic arterial hypertension
Indications:
Hypertension
Professional Synonyms:
Elevated blood pressure
Essential hypertension
Hyperpiesia
Hyperpiesis
Hypertensive disorder
Systemic arterial hypertension
The following dosing information is available for GUANFACINE HCL (guanfacine hcl):
Dosage of guanfacine hydrochloride is expressed in terms of guanfacine.
No enhanced Administration information available for this drug.
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| GUANFACINE 2 MG TABLET | Maintenance | Adults take 1 tablet (2 mg) by oral route once daily at bedtime |
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| GUANFACINE 2 MG TABLET | Maintenance | Adults take 1 tablet (2 mg) by oral route once daily at bedtime |
| GUANFACINE 1 MG TABLET | Maintenance | Adults take 1 tablet (1 mg) by oral route once daily at bedtime |
The following drug interaction information is available for GUANFACINE HCL (guanfacine hcl):
There are 0 contraindications.
There are 2 severe interactions.
These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.
| Drug Interaction | Drug Names |
|---|---|
| Guanfacine/Strong & Moderate CYP3A4 Inhibitors SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Strong or moderate inhibitors of CYP3A4 may inhibit the metabolism of guanfacine.(1) CLINICAL EFFECTS: The concurrent administration of a strong or moderate CYP3A4 inhibitor may result in elevated levels of guanfacine, which may result in increased adverse effects such as hypotension, bradycardia, loss of consciousness, and drowsiness.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Patients maintained on guanfacine may need dosage adjustments if strong or moderate inhibitors of CYP3A4 are initiated or discontinued. The manufacturer of extended-release guanfacine recommends a starting dose of extended-release guanfacine initiated at half the recommended level of the weight based dosing in patients receiving strong or moderate inhibitors of CYP3A4. If a patient has been maintained on extended-release guanfacine and is started on a strong or moderate CYP3A4 inhibitor, the dose of extended-release guanfacine should be decreased to half the recommended weight based dose. If a patient has been maintained on extended-release guanfacine and a strong or moderate CYP3A4 inhibitor and the strong or moderate CYP3A4 inhibitor is discontinued, the dose of extended-release guanfacine may need to be increased to the recommended weight based dose based upon patient response. Extended-release guanfacine target dose range for attention deficit hyperactivity disorder is 0.05-0.12 mg/kg/day. Doses above 4 mg/day have not been evaluated in children ages 6-12 years and doses above 7 mg/day have not been evaluated in adolescents ages 13-17 years.(1) DISCUSSION: Ketoconazole (dosage not stated), a strong inhibitor of CYP3A4, increased the maximum concentration (Cmax) and area-under-curve (AUC) of guanfacine (dosage not stated) by approximately 1.75-fold and 3-fold, respectively.(1) Strong inhibitors of CYP3A4 include: adagrasib, boceprevir, ceritinib, clarithromycin, cobicistat, idelalisib, indinavir, itraconazole, josamycin, ketoconazole, levoketoconazole, lonafarnib, lopinavir/ritonavir, mibefradil, mifepristone, nefazodone, nelfinavir, nirmatrelvir/ritonavir, posaconazole, ribociclib, ritonavir, saquinavir, telaprevir, telithromycin, tipranavir, troleandomycin, tucatinib, and voriconazole.(1-3) Moderate inhibitors of CYP3A4 include: amprenavir, aprepitant, atazanavir, avacopan, berotralstat, clofazimine, conivaptan, crizotinib, darunavir, diltiazem, dronedarone, duvelisib, erythromycin, fedratinib, fluconazole, fluvoxamine, fosnetupitant, imatinib, isavuconazonium, lenacapavir, letermovir, netupitant, nilotinib, schisandra, tofisopam, treosulfan and verapamil.(1-3) |
AKYNZEO, APONVIE, APREPITANT, APTIVUS, ATAZANAVIR SULFATE, CARDIZEM, CARDIZEM CD, CARDIZEM LA, CARTIA XT, CINVANTI, CLARITHROMYCIN, CLARITHROMYCIN ER, CLOFAZIMINE, CONIVAPTAN-D5W, COPIKTRA, CRESEMBA, DANZITEN, DARUNAVIR, DIFLUCAN, DILT-XR, DILTIAZEM 12HR ER, DILTIAZEM 24HR ER, DILTIAZEM 24HR ER (CD), DILTIAZEM 24HR ER (LA), DILTIAZEM 24HR ER (XR), DILTIAZEM HCL, DILTIAZEM HCL-0.7% NACL, DILTIAZEM HCL-0.9% NACL, DILTIAZEM HCL-NACL, DILTIAZEM-D5W, E.E.S. 200, E.E.S. 400, EMEND, ERY-TAB, ERYPED 200, ERYPED 400, ERYTHROCIN LACTOBIONATE, ERYTHROCIN STEARATE, ERYTHROMYCIN, ERYTHROMYCIN ESTOLATE, ERYTHROMYCIN ETHYLSUCCINATE, ERYTHROMYCIN LACTOBIONATE, EVOTAZ, FLUCONAZOLE, FLUCONAZOLE-NACL, FLUVOXAMINE MALEATE, FLUVOXAMINE MALEATE ER, GENVOYA, GLEEVEC, GRAFAPEX, IMATINIB MESYLATE, IMKELDI, INREBIC, ITRACONAZOLE, ITRACONAZOLE MICRONIZED, KALETRA, KETOCONAZOLE, KISQALI, KORLYM, KRAZATI, LANSOPRAZOL-AMOXICIL-CLARITHRO, LOPINAVIR-RITONAVIR, MATZIM LA, MIFEPREX, MIFEPRISTONE, MULTAQ, NEFAZODONE HCL, NILOTINIB HCL, NORVIR, NOXAFIL, OMECLAMOX-PAK, ORLADEYO, PAXLOVID, POSACONAZOLE, PREVYMIS, PREZCOBIX, PREZISTA, RECORLEV, REYATAZ, RITONAVIR, SPORANOX, STRIBILD, SUNLENCA, SYMTUZA, TASIGNA, TAVNEOS, TIADYLT ER, TIAZAC, TOLSURA, TRANDOLAPRIL-VERAPAMIL ER, TUKYSA, TYBOST, VAPRISOL-5% DEXTROSE, VERAPAMIL ER, VERAPAMIL ER PM, VERAPAMIL HCL, VERAPAMIL SR, VFEND, VFEND IV, VIRACEPT, VOQUEZNA TRIPLE PAK, VORICONAZOLE, XALKORI, ZOKINVY, ZYDELIG, ZYKADIA |
| Guanfacine/Strong & Moderate CYP3A4 Inducers SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Strong or moderate inducers of CYP3A4 may induce the metabolism of guanfacine.(1) CLINICAL EFFECTS: The concurrent administration of a strong or moderate CYP3A4 inducer may result in decreased levels and effectiveness of guanfacine.(1) PREDISPOSING FACTORS: Induction effects may be more likely with regular use of the inducer for longer than 1-2 weeks. PATIENT MANAGEMENT: Patients maintained on guanfacine may need dosage adjustments if strong or moderate inducers of CYP3A4 are initiated or discontinued. The manufacturer of extended-release guanfacine recommends a starting dose of extended-release guanfacine initiated at up to double the recommended level of the weight based dosing in patients receiving strong or moderate inducers of CYP3A4. If a patient has been maintained on extended-release guanfacine and is started on a strong or moderate CYP3A4 inducer, the dose of extended-release guanfacine should be increased up to double the recommended weight based dose over 1 to 2 weeks. If a patient has been maintained on extended-release guanfacine and a strong or moderate CYP3A4 inducer, and the strong or moderate CYP3A4 inducer is discontinued, the dose of extended-release guanfacine may need to be decreased to the recommended weight based dose over 1 to 2 weeks. Extended-release guanfacine target dose range for attention deficit hyperactivity disorder is 0.05-0.12 mg/kg/day. Doses above 4 mg/day have not been evaluated in children ages 6-12 years and doses above 7 mg/day have not been evaluated in adolescents ages 13-17 years.(1) DISCUSSION: Rifampin (dosage not stated), a strong inducer of CYP3A4, decreased the maximum concentration (Cmax) and area-under-curve (AUC) of guanfacine (dosage not stated) by approximately 50%.(1) Strong inducers of CYP3A4 include: apalutamide, barbiturates, carbamazepine, encorafenib, enzalutamide, fosphenytoin, ivosidenib, lumacaftor, mitotane, phenobarbital, phenytoin, primidone, rifabutin, rifampin, rifapentine, and St. John's wort.(1-3) Moderate inducers of CYP3A4 include: belzutifan, bosentan, cenobamate, dabrafenib, efavirenz, elagolix, etravirine, lesinurad, lorlatinib, mavacamten, mitapivat, modafinil, nafcillin, pacritinib, pexidartinib, repotrectinib, sotorasib, telotristat, thioridazine, and tovorafenib.(1-3) |
ASA-BUTALB-CAFFEINE-CODEINE, ASCOMP WITH CODEINE, AUGTYRO, BOSENTAN, BRAFTOVI, BUTALB-ACETAMINOPH-CAFF-CODEIN, BUTALBITAL, BUTALBITAL-ACETAMINOPHEN, BUTALBITAL-ACETAMINOPHEN-CAFFE, BUTALBITAL-ASPIRIN-CAFFEINE, CAMZYOS, CARBAMAZEPINE, CARBAMAZEPINE ER, CARBATROL, CEREBYX, DILANTIN, DILANTIN-125, DONNATAL, DUZALLO, EFAVIRENZ, EFAVIRENZ-EMTRIC-TENOFOV DISOP, EFAVIRENZ-LAMIVU-TENOFOV DISOP, EPITOL, EQUETRO, ERLEADA, ETRAVIRINE, FIORICET, FIORICET WITH CODEINE, FOSPHENYTOIN SODIUM, INTELENCE, LORBRENA, LUMAKRAS, LYSODREN, MITOTANE, MODAFINIL, MYSOLINE, NAFCILLIN, NAFCILLIN SODIUM, OJEMDA, ORIAHNN, ORILISSA, ORKAMBI, PENTOBARBITAL SODIUM, PHENOBARBITAL, PHENOBARBITAL SODIUM, PHENOBARBITAL-BELLADONNA, PHENOBARBITAL-HYOSC-ATROP-SCOP, PHENOHYTRO, PHENYTEK, PHENYTOIN, PHENYTOIN SODIUM, PHENYTOIN SODIUM EXTENDED, PRIFTIN, PRIMIDONE, PROVIGIL, PYRUKYND, RIFABUTIN, RIFADIN, RIFAMPIN, SEZABY, SYMFI, SYMFI LO, TAFINLAR, TALICIA, TEGRETOL, TEGRETOL XR, TENCON, THIORIDAZINE HCL, THIORIDAZINE HYDROCHLORIDE, TIBSOVO, TRACLEER, TURALIO, VONJO, WELIREG, XCOPRI, XERMELO, XTANDI |
There are 2 moderate interactions.
The clinician should assess the patient’s characteristics and take action as needed. Actions required for moderate interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration.
| Drug Interaction | Drug Names |
|---|---|
| Tizanidine/Guanfacine; Methyldopa SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Tizanidine is an alpha-2 agonist. Concurrent use with antihypertensive agents may result in additive effects on blood pressure.(1) CLINICAL EFFECTS: Concurrent use of antihypertensives and tizanidine may result in hypotension.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Patients receiving concurrent therapy should be monitored for hypotension. The risk of hypotension may be decreased by careful titration of tizanidine dosages and monitoring for hypotension prior to dose advancement. Counsel patients about the risk of orthostatic hypotension.(1) DISCUSSION: Severe hypotension has been reported following the addition of tizanidine to existing lisinopril therapy.(2-4) |
TIZANIDINE HCL, ZANAFLEX |
| Apomorphine/Selected Antihypertensives and Vasodilators SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Apomorphine causes dose-dependent decreases in blood pressure. Concurrent use with antihypertensive agents may result in additive effects on blood pressure.(1) CLINICAL EFFECTS: Concurrent use of antihypertensives and apomorphine may result in orthostatic hypotension with or without dizziness, nausea, or syncope.(1) PREDISPOSING FACTORS: The risk of orthostatic hypotension may be increased during dose escalation of apomorphine and in patients with renal or hepatic impairment.(1) PATIENT MANAGEMENT: Patients receiving concurrent therapy should be monitored for hypotension. Counsel patients about the risk of orthostatic hypotension.(1) DISCUSSION: Healthy volunteers who took sublingual nitroglycerin (0.4 mg) concomitantly with apomorphine experienced a mean largest decrease in supine systolic blood pressure (SBP) of 9.7 mm Hg and in supine diastolic blood pressure (DBP) of 9.3 mm Hg, and a mean largest decrease in standing SBP and DBP of 14.3 mm Hg and 13.5 mm Hg, respectively. The maximum decrease in SBP and DBP was 65 mm Hg and 43 mm Hg, respectively. When apomorphine was taken alone, the mean largest decrease in supine SBP and DBP was 6.1 mm Hg and 7.3 mm Hg, respectively, and in standing SBP and DBP was 6.7 mm Hg and 8.4 mm Hg, respectively.(1) |
APOKYN, APOMORPHINE HCL, ONAPGO |
The following contraindication information is available for GUANFACINE HCL (guanfacine hcl):
Drug contraindication overview.
Guanfacine is contraindicated in patients with known hypersensitivity to the drug.
Guanfacine is contraindicated in patients with known hypersensitivity to the drug.
There are 0 contraindications.
There are 3 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Bradycardia |
| Hypotension |
| Suicidal ideation |
There are 3 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Alcohol intoxication |
| Drowsy |
| Orthostatic hypotension |
The following adverse reaction information is available for GUANFACINE HCL (guanfacine hcl):
Adverse reaction overview.
Common adverse effects in patients receiving guanfacine include dry mouth, somnolence, dizziness, constipation, fatigue, asthenia, impotence, and headache.
Common adverse effects in patients receiving guanfacine include dry mouth, somnolence, dizziness, constipation, fatigue, asthenia, impotence, and headache.
There are 11 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
| None. | None. |
| Rare/Very Rare |
|---|
|
Atrioventricular block Bradycardia Chest pain Encephalopathy Exfoliative dermatitis Hypersensitivity drug reaction Seizure disorder Sinus node dysfunction Suicidal Suicidal ideation Tachycardia |
There are 48 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Acute abdominal pain Dizziness Drowsy Fatigue Hypotension Insomnia Lethargy Nausea Sedation Weight gain Xerostomia |
Acute cognitive impairment Anorexia Constipation Dyspepsia Erectile dysfunction General weakness Headache disorder Increased urinary frequency Irritability Libido changes Nightmares Palpitations Pruritus of skin Urinary incontinence Vomiting |
| Rare/Very Rare |
|---|
|
Accidental fall Alopecia Arthralgia Blurred vision Conjunctivitis Cramps in legs Depression Dysgeusia Dyspnea Edema Hallucinations Malaise Myalgia Pallor Paresthesia Raynaud's phenomenon Skin inflammation Skin rash Symptoms of anxiety Syncope Tremor Vertigo |
The following precautions are available for GUANFACINE HCL (guanfacine hcl):
Safety and efficacy of guanfacine for the management of hypertension have not been established in children younger than 12 years of age; use in these pediatric patients is not recommended. For information on overall principles and expert recommendations for treatment of hypertension in pediatric patients, see Uses: Hypertension in Pediatric Patients, in the Thiazides General Statement 40:28.20.
Mania and aggressive behavioral changes have been reported in pediatric patients with ADHD receiving guanfacine (as conventional tablets)+; all patients had medical or family risk factors for bipolar disorder. All patients recovered following discontinuance of the drug.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Mania and aggressive behavioral changes have been reported in pediatric patients with ADHD receiving guanfacine (as conventional tablets)+; all patients had medical or family risk factors for bipolar disorder. All patients recovered following discontinuance of the drug.
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
Category B. (See Users Guide.) Guanfacine is not recommended for the treatment of acute hypertension associated with toxemia of pregnancy.
Guanfacine is distributed into milk in rats; it is not known whether the drug is distributed into human milk. Caution is advised if guanfacine is used in nursing women.
Clinical trial data for patients 65 years of age or older are insufficient to determine whether geriatric patients respond differently than younger adults. Other experience suggests that response is similar to that in younger adults. Dosage of guanfacine should be selected with caution because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.
The following prioritized warning is available for GUANFACINE HCL (guanfacine hcl):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for GUANFACINE HCL (guanfacine hcl)'s list of indications:
| Hypertension | |
| I10 | Essential (primary) hypertension |
| I11 | Hypertensive heart disease |
| I11.0 | Hypertensive heart disease with heart failure |
| I11.9 | Hypertensive heart disease without heart failure |
| I12 | Hypertensive chronic kidney disease |
| I12.0 | Hypertensive chronic kidney disease with stage 5 chronic kidney disease or end stage renal disease |
| I12.9 | Hypertensive chronic kidney disease with stage 1 through stage 4 chronic kidney disease, or unspecified chronic kidney disease |
| I13 | Hypertensive heart and chronic kidney disease |
| I13.0 | Hypertensive heart and chronic kidney disease with heart failure and stage 1 through stage 4 chronic kidney disease, or unspecified chronic kidney disease |
| I13.1 | Hypertensive heart and chronic kidney disease without heart failure |
| I13.10 | Hypertensive heart and chronic kidney disease without heart failure, with stage 1 through stage 4 chronic kidney disease, or unspecified chronic kidney disease |
| I13.11 | Hypertensive heart and chronic kidney disease without heart failure, with stage 5 chronic kidney disease, or end stage renal disease |
| I13.2 | Hypertensive heart and chronic kidney disease with heart failure and with stage 5 chronic kidney disease, or end stage renal disease |
| I15.1 | Hypertension secondary to other renal disorders |
Formulary Reference Tool