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Guanfacine 1 mg Tablet, 100-count — NDC 27241-0242-01 package photo

Guanfacine 1 mg Tablet, 100-count

by Ajanta Pharma USA Inc. · 100 TABLET in 1 BOTTLE (27241-242-01)
NDC 27241-0242-01
🏷️ FDA NDC (as labeled) 27241-242-01 billing pads the product segment with a zero
Rx only Generic On market Non-controlled
🗂️ Data synced Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

🆔 Identity & classification

FDA NDC (as labeled) 27241-242-01
Product NDC 27241-242
11-digit billing NDC 27241024201
NCPDP billing unit EA — each (per item)
RxCUI 197745, 197746
UNII PML56A160O
UPC 0327241243011, 0327241242014
Application # ANDA217293
SPL Set ID 830c0be8-2137-46ee-94c6-aa048b7de35f
Established class (EPC) Central alpha-2 Adrenergic Agonist
Mechanism of action Adrenergic alpha2-Agonists
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2023-04-27
Route ORAL
Dosage form TABLET
Substance GUANFACINE HYDROCHLORIDE
GPI-14 36201025100320
GCN Seq No 000364
GCN 32480
HICL code 000120
Ingredient (HICL) Guanfacine Hcl
HIC1 code A
Therapeutic class — broad (HIC1) Cardiovascular System
HIC2 code A4
Therapeutic class — intermediate (HIC2) Antihypertensives
HIC3 code A4B
Therapeutic class — specific (HIC3) Antihypertensives, Sympatholytic
AHFS code 24:24.00.00
AHFS class Central Alpha-Agonists
FDB label name GUANFACINE 1 MG TABLET
FDB brand name Guanfacine Hcl
Legend status F — Federal legend — prescription drug or device
TE code (Orange Book) AB · RLD · RS
Why two NDCs? The FDA registers this code as 27241-242-01 — a 5-3-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the product segment → 27241-0242-01. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

🏷️ RxNorm drug class

This medicine belongs to the Central alpha-2 Adrenergic Agonist class.

Pharmacologic class Central alpha-2 Adrenergic Agonist
Drug family (ATC) Imidazoline receptor agonists
How it works Adrenergic alpha2-Agonists
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

🏭 Manufacturer & labeler

LabelerAjanta Pharma USA Inc.
Application holderAJANTA PHARMA LTD
FDA applicationANDA217293 (ANDA)
Labeler code27241
First marketedApr 2023
Product typeHuman Prescription Drug
Portfolio168 products on file
The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

🩺 Clinical

Label name GUANFACINE 1 MG TABLET Ingredient Guanfacine Hcl
📖 What it is MedlinePlus · NLM

Guanfacine tablets (Tenex) are used alone or in combination with other medications to treat high blood pressure. Guanfacine extended-release (long-acting) tablets (Intuniv) are used as part of a treatment program to control symptoms of attention deficit hyperactivity disorder (ADHD; more difficulty focusing, controlling actions, and remaining still or quiet than other people who are the same age) in children. Guanfacine is in a class of medications called centrally acting alpha2A-adrenergic receptor agonists. Guanfacine treats high blood pressure by decreasing heart rate and relaxing the blood...

Read the full MedlinePlus article ↗
📗 Our plain-language guide HelloPharmacist
  • It's used for both, depending on which form you have. The regular (immediate-release) tablet is prescribed for high blood pressure. The extended-release version — brand name Intuni...
  • What is guanfacine actually used for — is it for ADHD or blood pressure?
  • No, Intuniv is not a stimulant at all. It works on a different part of the brain than medications like Adderall or Ritalin. That's actually one reason it's sometimes used alongside...
  • My child takes Intuniv for ADHD — is it a stimulant?
📖 Read our full Guanfacine guide →
1
Nutrient depletion considerations

Guanfacine may be associated with lower levels of 1 nutrient — worth a chat with your pharmacist, not a cause for alarm.

An association is not a deficiency. Educational only — don't start or stop anything without professional guidance.
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

💊 What it looks like

Color White
ShapeOval
ImprintG2
Size1 mm
ScoringNot scored
One label can cover several strengths, so colors may be combined — always confirm a loose pill against the dispensed prescription label or a pharmacist.
Where does this data come from?
Physical description (imprint, shape, color, scoring, coating) from this product’s FDA Structured Product Labeling (SPL), mirrored from DailyMed / openFDA.

🧪 Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.

  • UNII XF417D3PSL
    Anhydrous citric acid is a sour, crystalline powder derived from citric acid with water removed. In medicines, it acts as a buffer to control pH, adds tartness to improve taste, and helps tablets disintegrate.
  • UNII OP1R32D61U
    Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
  • UNII O8232NY3SJ
    A plant-based carbohydrate derived from corn kernels. It acts as a filler to add bulk, a binder to hold ingredients together, and a disintegrant to help the tablet break apart in your stomach for absorption.
  • UNII 4ELV7Z65AP
    Stearic acid is a fatty acid derived from plant or animal sources. It acts as a binder and lubricant in tablets and capsules, helping them hold together and flow smoothly during manufacturing.

4 inactive ingredients listed in the exact product block matched to this NDC.

Where does this data come from?
Data sourced from official FDA Structured Product Labeling (SPL) via DailyMedingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

💲 Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer eaPer package
Retail pharmacies payNADAC · weekly $0.144 $14.42 / 100 tablets
Medicaid paysCMS SDUD · 12 mo $0.3423 $34.23 / 100 tablets
Medicare drug plans payPart D · quarterly No Part D plan price is available for this NDC in our data.
NADAC price history (per ea) — tap or hover for the price & month
Dec 2023 Dec 2025 Apr 2026 Aug 2026 $0.361 $0.140
▼ Down 59% over the last 12 months.
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

🔁 Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Guanfacine 1 mg 00591-0444-01 Actavis 100 tablets $0.144 Availability likely
Guanfacine 1 mg 00904-7140-04 Major 30 tablets $0.144 AB Availability likely
Guanfacine Hydrochloride 1 mg 24979-0198-01 TWi 100 tablets $0.144 AB Availability likely
Guanfacine 1 mgthis 27241-0242-01 Ajanta 100 tablets $0.144 AB Availability likely
Guanfacine Hydrochloride 1 mg 29300-0458-01 Unichem 100 tablets $0.144 AB Availability likely
Guanfacine 1 mg 42806-0048-01 Epic 100 tablets $0.144 AB Availability likely
Guanfacine Hydrochloride 1 mg 53746-0711-01 Amneal 100 tablets $0.144 AB Availability likely
Guanfacine 1 mg 59651-0840-01 Aurobindo 100 tablets $0.144 AB Availability likely
Guanfacine Hydrochloride 1 mg 60687-0710-21 American 30 tablets $0.144 AB Availability likely
Guanfacine Hydrochloride 1 mg 62135-0727-90 Chartwell 90 tablets $0.144 AB Availability likely
Guanfacine Hydrochloride 1 mg 68094-0065-62 Precision 30 tablets $0.144 AB Availability likely
Guanfacine Hydrochloride 1 mg 70700-0301-01 XIROMED, 100 tablets $0.144 AB Availability likely
Guanfacine 1 mg 72319-0018-04 i3 100 tablets $0.144 AB Availability likely
Guanfacine 1 mg 24658-0730-01 PuraCap 100 tablets AB FDA listed
Guanfacine Hydrochloride 1 mg 50090-6073-00 A-S 30 tablets AB FDA listed
Guanfacine 1 mg 63187-0302-30 Proficient 30 tablets AB FDA listed
Guanfacine Hydrochloride 1 mg 65162-0711-03 Amneal 30 tablets AB FDA listed
Guanfacine 1 mg 67046-1433-03 Coupler 30 tablets AB FDA listed
Guanfacine 1 mg 70518-4333-00 REMEDYREPACK 30 tablets AB FDA listed
Guanfacine Hydrochloride 1 mg 72603-0268-01 NORTHSTAR 100 tablets AB FDA listed
Guanfacine 1 mg 72888-0123-00 Advagen 1000 tablets AB FDA listed
Guanfacine 1 mg 73141-0018-04 A2A 100 tablets AB FDA listed
About this product: this is a generic version of the medicine. FDA equivalence ratings are shown when available, and other versions are listed above, least expensive first.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2023
On the market since
Apr 2023
📍
2026
Currently FDA-listed
3 years listed
🔓
·
Generic on the market
this product is a generic
This is a generic drug

This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.

Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

🗺️ Medicaid utilization & spend

📍 This exact package only: Medicaid data is reported per full 11-digit NDC — labeler, product and pack size — so every number here is for 27241-0242-01, not the drug overall. Other pack sizes report separately.
💊 Pharmacy benefit only: These are Medicaid outpatient pharmacy claims, billed by NDC. They exclude the medical benefit — clinic- or hospital-administered drugs billed under HCPCS J-codes — so drugs used mostly that way (e.g. Avastin, Lucentis, Keytruda) can look low or missing here. That’s expected, not an error.
📅 Q1 2025 – Q4 2025 · 4 quarters of data
ⓘ The newest quarter is usually incomplete when first published; states restate recent quarters in later CMS releases, so the latest figures typically revise upward. State coverage-policy changes can also shift quarter-to-quarter totals.
Prescriptions last 4 qtrs
227.4K
Units reimbursed last 4 qtrs
11.5M
Gross reimbursed last 4 qtrs
$3.94M
Avg / prescription
$17.35
Avg / unit
$0.3423
Latest quarter Q4 2025
65.5KRx
Medicaid pays / ea
$0.3423
gross reimbursed
vs
NADAC / ea
$0.1442
acquisition cost
=
Spread
+$0.1981
+137% vs cost
What Medicaid paid per ea (before rebates; includes the pharmacy’s dispensing fee) compared with NADAC — the average price pharmacies pay to buy the drug. A positive spread means Medicaid reimbursed more than the purchase price, before manufacturer rebates.
Fee-for-service vs managed care
34% FFS 66% MCO
Fee-for-service · 76,422 Rx Managed care · 150,998 Rx
State Medicaid map
Alaska: 14,014 units · 1,912 per 100k residents AK Maine: 174,343 units · 12,498 per 100k residents ME Washington: 259,977 units · 3,328 per 100k residents WA Idaho: 62,929 units · 3,204 per 100k residents ID Montana: 30,412 units · 2,687 per 100k residents MT North Dakota: 32,639 units · 4,168 per 100k residents ND Minnesota: 370,229 units · 6,453 per 100k residents MN Wisconsin: 220,369 units · 3,729 per 100k residents WI Michigan: 216,113 units · 2,153 per 100k residents MI New York: 908,740 units · 4,643 per 100k residents NY Vermont: 19,815 units · 3,063 per 100k residents VT New Hampshire: 43,097 units · 3,074 per 100k residents NH Oregon: 127,513 units · 3,012 per 100k residents OR Nevada: 21,288 units · 666 per 100k residents NV Wyoming: 14,190 units · 2,430 per 100k residents WY South Dakota: 31,966 units · 3,478 per 100k residents SD Iowa: 658,120 units · 20,521 per 100k residents IA Illinois: 486,326 units · 3,875 per 100k residents IL Indiana: 299,300 units · 4,362 per 100k residents IN Ohio: 621,131 units · 5,271 per 100k residents OH Pennsylvania: 1,715,635 units · 13,237 per 100k residents PA New Jersey: 226,792 units · 2,441 per 100k residents NJ Massachusetts: 111,634 units · 1,595 per 100k residents MA California: 585,347 units · 1,502 per 100k residents CA Utah: 33,694 units · 986 per 100k residents UT Colorado: 91,560 units · 1,558 per 100k residents CO Nebraska: 114,869 units · 5,807 per 100k residents NE Missouri: 450,402 units · 7,269 per 100k residents MO Kentucky: 519,831 units · 11,485 per 100k residents KY West Virginia: 154,207 units · 8,712 per 100k residents WV Virginia: 222,704 units · 2,555 per 100k residents VA Maryland: 187,258 units · 3,030 per 100k residents MD Connecticut: 46,577 units · 1,288 per 100k residents CT Rhode Island: 14,548 units · 1,329 per 100k residents RI Arizona: 87,392 units · 1,176 per 100k residents AZ New Mexico: 34,454 units · 1,630 per 100k residents NM Kansas: 83,858 units · 2,852 per 100k residents KS Arkansas: 352,654 units · 11,498 per 100k residents AR Tennessee: 181,876 units · 2,552 per 100k residents TN North Carolina: 244,262 units · 2,254 per 100k residents NC South Carolina: 125,101 units · 2,328 per 100k residents SC Delaware: 29,113 units · 2,824 per 100k residents DE Oklahoma: 128,486 units · 3,170 per 100k residents OK Louisiana: 174,398 units · 3,813 per 100k residents LA Mississippi: 270,834 units · 9,212 per 100k residents MS Alabama: 52,184 units · 1,022 per 100k residents AL Georgia: 281,350 units · 2,551 per 100k residents GA D.C.: 5,074 units · 747 per 100k residents DC Hawaii: 6,702 units · 467 per 100k residents HI Texas: 224,149 units · 735 per 100k residents TX Florida: 143,741 units · 636 per 100k residents FL
Units reimbursed · per 100k residents
46720,521
gray = no data reported
Colors are per 100,000 residents, so big states don’t automatically dominate. Tap or hover a state for its actual totals.
Tap or hover a state
…for its Medicaid breakdown
🏆 Top states by units · per 100k residents
1 Iowa 20,521 /100k
2 Pennsylvania 13,237 /100k
3 Maine 12,498 /100k
4 Arkansas 11,498 /100k
5 Kentucky 11,485 /100k
6 Mississippi 9,212 /100k
7 West Virginia 8,712 /100k
8 Missouri 7,269 /100k
National units — by quarter
💵 About the dollar figures: “reimbursed” is what Medicaid paid pharmacies before confidential manufacturer rebates, so the program’s real net cost is lower than these numbers. Fee-for-service and managed-care claims are combined unless split above. Source: CMS State Drug Utilization Data; per-100k rates use 2023 Census population estimates.

🔬 Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for Guanfacine — the ingredient across all brands.

Top reported reactions

Somnolence471
Aggression388
Fatigue351
Hypotension299
Dizziness291
Insomnia288
Headache283

Reporter sex

0 reports

Serious outcomes

Hospitalization1,909
Reports over time (by year) — tap or hover for the count & year
2021 2022 2024 2026 741 415
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

📦 Packaging — all sizes for this product

Package NDCDescription Marketing startStatus
27241-0242-01 You're viewing this 100 TABLET in 1 BOTTLE (27241-242-01) 2023-04-27 Active

📄 Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage 30 words

INDICATIONS AND USAGE Guanfacine tablets, USP are indicated in the management of hypertension. Guanfacine tablets, USP may be given alone or in combination with other antihypertensive agents, especially thiazide-type diuretics.

⏱️ Dosage and Administration 151 words

DOSAGE AND ADMINISTRATION The recommended initial dose of guanfacine tablets when given alone or in combination with another antihypertensive drug is 1 mg daily given at bedtime to minimize somnolence. If after 3 weeks to 4 weeks of therapy 1 mg does not give a satisfactory result, a dose of 2 mg may be given, although most of the effect of guanfacine tablets are seen at 1 mg (see CLINICAL PHARMACOLOGY ). Higher daily doses have been used, but adverse reactions increase significantly with doses above 3 mg/day.

The frequency of rebound hypertension is low, but it can occur. When rebound occurs, it does so after 2 days to 4 days, which is delayed compared with clonidine hydrochloride. This is consistent with the longer half-life of guanfacine.

In most cases, after abrupt withdrawal of guanfacine, blood pressure returns to pretreatment levels slowly (within 2 days to 4 days) without ill effects.

Contraindications 13 words

CONTRAINDICATIONS Guanfacine tablets are contraindicated in patients with known hypersensitivity to guanfacine hydrochloride.

🤒 Adverse Reactions ~3 min read

ADVERSE REACTIONS Adverse reactions noted with guanfacine hydrochloride are similar to those of other drugs of the central α 2 -adrenoreceptor agonist class: dry mouth, sedation (somnolence), weakness (asthenia), dizziness, constipation, and impotence. While the reactions are common, most are mild and tend to disappear on continued dosing. Skin rash with exfoliation has been reported in a few cases; although clear cause and effect relationships to guanfacine tablets could not be established, should a rash occur, guanfacine tablets should be discontinued and the patient monitored appropriately.

In the dose-response monotherapy study described under CLINICAL PHARMACOLOGY , the frequency of the most commonly observed adverse reactions showed a dose relationship from 0.5 mg to 3 mg as follows: Adverse Reaction Placebo n = 59 0.5 mg n = 60 1 mg n = 61 2 mg n = 60 3 mg n = 59 Dry Mouth 0 % 10 % 10 % 42 % 54 % Somnolence 8 % 5 % 10 % 13 % 39 % Asthenia 0 % 2 % 3 % 7 % 3 % Dizziness 8 % 12 % 2 % 8 % 15 % Headache 8 % 13 % 7 % 5 % 3 % Impotence 0 % 0 % 0 % 7 % 3 % Constipation 0 % 2 % 0 % 5 % 15 % Fatigue 2 % 2 % 5 % 8 % 10 % The percent of patients who dropped out because of adverse reactions are shown below for each dosage group.

Placebo 0.5 mg 1 mg 2 mg 3 mg Percent dropouts 0 % 2.0 % 5.0 % 13 % 32 % The most common reasons for dropouts among patients who received guanfacine were dry mouth, somnolence, dizziness, fatigue, weakness, and constipation. In the 12-week, placebo-controlled, dose-response study of guanfacine administered with 25 mg chlorthalidone at bedtime, the frequency of the most commonly observed adverse reactions showed a clear dose relationship from 0.5 mg to 3 mg as follows: Adverse Reaction Placebo n = 73 0.5 mg n = 72 1 mg n = 72 2 mg n = 72 3 mg n = 72 Dry Mouth 5 (7 %) 4 (5 %) 6 (8 %) 8 (11 %) 20 (28 %) Somnolence 1 (1 %) 3 (4 %) 0 (0 %) 1 (1 %) 10 (14 %) Asthenia 0 (0 %) 2 (3 %) 0 (0 %) 2 (2 %) 7 (10 %) Dizziness 2 (2 %) 1 (1 %) 3 (4 %) 6 (8 %) 3 (4 %) Headache 3 (4 %) 4 (3 %) 3 (4 %) 1 (1 %) 2 (2 %) Impotence 1 (1 %) 1 (0 %) 0 (0 %) 1 (1 %) 3 (4 %) Constipation 0 (0 %) 0 (0 %) 0 (0 %) 1 (1 %) 1 (1 %) Fatigue 3 (3 %) 2 (3 %) 2 (3 %) 5 (6 %) 3 (4 %) There were 41 premature terminations because of adverse reactions in this study.

The percent of patients who dropped out and the dose at which the dropout occurred were as follows: Dose Placebo 0.5 mg 1 mg 2 mg 3 mg Percent dropouts 6.9 % 4.2 % 3.2 % 6.9 % 8.3 % Reasons for dropouts among patients who received guanfacine were: somnolence, headache, weakness, dry mouth, dizziness, impotence, insomnia, constipation, syncope, urinary incontinence, conjunctivitis, paresthesia, and dermatitis. In a second 12-week placebo-controlled combination therapy study in which the dose could be adjusted upward to 3 mg per day in 1-mg increments at 3-week intervals, i.e., a setting more similar to ordinary clinical use, the most commonly recorded reactions were: dry mouth, 47 %; constipation, 16 %; fatigue, 12 %; somnolence, 10 %; asthenia, 6 %; dizziness, 6 %; headache, 4 %; and insomnia, 4 %.

Reasons for dropouts among patients who received guanfacine were: somnolence, dry mouth, dizziness, impotence, constipation, confusion, depression, and palpitations. In the clonidine/guanfacine comparison described in CLINICAL PHARMACOLOGY , the most common adverse reactions noted were as follows: Adverse Reactions Guanfacine (n = 279) Clonidine (n = 278) Dry Mouth 30 % 37 % Somnolence 21 % 35 % Dizziness 11 % 8 % Constipation 10 % 5 % Fatigue 9 % 8 % Headache 4 % 4 % Insomnia 4 % 3 % Adverse reactions occurring in 3 % or less of patients in the three controlled trials of guanfacine hydrochloride with a diuretic were: Cardiovascular- bradycardia, palpitations, substernal pain Gastrointestinal- abdominal pain, diarrhea, dyspepsia, dysphagia, nausea CNS- amnesia, confusion, depression, insomnia, libido decrease ENT disorders- rhinitis, taste perversion, tinnitus Eye disorders- conjunctivitis, i…

🧬 Clinical Pharmacology ~3 min read

CLINICAL PHARMACOLOGY Guanfacine hydrochloride is an orally active antihypertensive agent whose principal mechanism of action appears to be stimulation of central α 2 -adrenergic receptors. By stimulating these receptors, guanfacine reduces sympathetic nerve impulses from the vasomotor center to the heart and blood vessels. This results in a decrease in peripheral vascular resistance and a reduction in heart rate.

The dose-response relationship for blood pressure and adverse effects of guanfacine given once a day as monotherapy has been evaluated in patients with mild to moderate hypertension. In this study patients were randomized to placebo or to 0.5 mg, 1 mg, 2 mg, 3 mg, or 5 mg of guanfacine tablets. Results are shown in the following table.

A useful effect was not observed overall until doses of 2 mg were reached, although responses in white patients were seen at 1 mg; 24 hour effectiveness of 1 mg to 3 mg doses was documented using 24 hour ambulatory monitoring. While the 5 mg dose added an increment of effectiveness, it caused an unacceptable increase in adverse reactions. Mean Changes (mm Hg) from Baseline in Seated Systolic and Diastolic Blood Pressure for Patients Completing 4 Weeks to 8 Weeks of Treatment with Guanfacine Monotherapy * S/D = Systolic/diastolic blood pressure Mean change S/D* Seated n = (range) Placebo 0.5 mg 1 mg 2 mg 3 mg 5 mg White Patients 11 to 30 -1/-5 -6/-8 -8/-9 -12/-11 -15/-12 -18/-16 Black Patients 8 to 28 -3/-5 0/-2 -3/-5 -7/-7 -8/-9 -19/-15 Controlled clinical trials in patients with mild to moderate hypertension who were receiving a thiazide-type diuretic have defined the dose-response relationship for blood pressure response and adverse reactions of guanfacine given at bedtime and have shown that the blood pressure response to guanfacine can persist for 24 hours after a single dose.

In the 12-week placebo-controlled dose-response study, patients were randomized to placebo or to doses of 0.5 mg, 1 mg, 2 mg, and 3 mg of guanfacine, in addition to 25 mg chlorthalidone, each given at bedtime. The observed mean changes from baseline, tabulated below, indicate the similarity of response for placebo and the 0.5 mg dose. Doses of 1 mg, 2 mg, and 3 mg resulted in decreased blood pressure in the sitting position with no real differences among the three doses.

In the standing position, there was some increase in response with dose. Mean Decreases (mm Hg) in Seated and Standing Blood Pressure for Patients Treated with Guanfacine in Combination with Chlorthalidone * S/D = Systolic/diastolic blood pressure Mean Change n = Placebo 63 0.5 mg 63 1 mg 64 2 mg 58 3 mg 59 SD * Seated -5/-7 -5/-6 -14/-13 -12/-13 -16/-13 SD Standing -3/-5 -5/-4 -11/-9 -9/-10 -15/-12 While most of the effectiveness of guanfacine in combination (and as monotherapy in white patients) was present at 1 mg, adverse reactions at this dose were not clearly distinguishable from those associated with placebo.

Adverse reactions were clearly present at 2 mg and 3 mg (see ADVERSE REACTIONS ). In a second 12-week placebo-controlled study of 1 mg, 2 mg or 3 mg of guanfacine hydrochloride administered with 25 mg of chlorthalidone once daily, a significant decrease in blood pressure was maintained for a full 24 hours after dosing. While there was no significant difference between the 12 hour and 24 hour blood pressure readings, the fall in blood pressure at 24 hours was numerically smaller, suggesting possible escape of blood pressure in some patients and the need for individualization of therapy.

In a double-blind, randomized trial, either guanfacine or clonidine was given at recommended doses with 25 mg chlorthalidone for 24 weeks and then abruptly discontinued. Results showed equal degrees of blood pressure reduction with the two drugs and there was no tendency for blood pressures to increase despite maintenance of the same daily dose of the two drugs. Signs and symptoms of rebound phenomena were infrequent upon discontinuation of either d…

📦 How Supplied / Storage and Handling 123 words

HOW SUPPLIED Guanfacine tablets, USP are available in the following dosing strengths (expressed in equivalent amounts of guanfacine): 1 mg—White to off white, round, biconvex tablets, debossed with ‘G1’ on one side and plain on other side in bottles of 100 with child-resistant closure (NDC 27241-242-01). 2 mg—White to off white, oval, biconvex tablets, debossed with ‘G2’ on one side and plain on other side in bottles of 100 with child-resistant closure (NDC 27241-243-01). Store at 20ºC to 25ºC (68ºF to 77ºF); excursions permitted to 15ºC to 30ºC (59ºF to 86ºF) [see USP Controlled Room Temperature].

Dispense in a tight, light-resistant container . Product of Italy Manufactured by: Ajanta Pharma Limited, India Marketed by: Ajanta Pharma USA Inc. Bridgewater, NJ 08807.

Revised: 11/2025

📋 Description 100 words

DESCRIPTION Guanfacine hydrochloride, USP is a centrally acting antihypertensive with α 2 -adrenoceptor agonist properties in tablet form for oral administration. The chemical name of guanfacine hydrochloride, USP is N -Amidino- 2-(2,6-dichlorophenyl) acetamide monohydrochloride and its molecular weight is 282.55. Its structural formula is: Guanfacine hydrochloride, USP is a white to off-white powder; sparingly soluble in water and alcohol and very slightly soluble in acetone.

The tablets contain the following inactive ingredients: 1 mg—Anhydrous citric acid, microcrystalline cellulose, pregelatinized starch, stearic acid. 2 mg—Anhydrous citric acid, microcrystalline cellulose, pregelatinized starch, stearic acid. Guanfacine tablets meets USP Dissolution Test 2. structure

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗
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