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Timolol hemihydrate 5 mg/mL Solution/ Drops, 1 bottle — NDC 70069-516-01 (Billing 70069-0516-01)

by Somerset Therapeutics, LLC · 1 BOTTLE in 1 CARTON / 2.5 mL in 1 BOTTLE

This is a package of 1 bottle of Timolol hemihydrate 5 mg/mL Solution/ Drops from Somerset Therapeutics, LLC, marketed since Jul 2024 and currently FDA-listed; retail pharmacies pay about $21.81 per mL (NADAC). It is this product's only package size.

NDC 70069-0516-01
🏷️ FDA NDC (as labeled) 70069-516-01 billing pads the product segment with a zero
Rx only Generic On market Non-controlled ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

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Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

NDC database record

One package, one record: these facts belong to NDC 70069-516-01 alone.

Record
FDA NDC Directory package listing · Human prescription drug
Code segments
70069 labeler · 516 product · 01 package
Package marketed since
Jul 9, 2024
Sample package
No — commercial package
Listing certified through
Dec 31, 2026
Barcode (UPC)
0370069517017, 0370069516010
FDA record last changed
Jul 24, 2026

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 70069-516-01
Product NDC 70069-516
11-digit billing NDC 70069051601
NCPDP billing unit ML — per mL (volume)
RxCUI 1992299
UNII P8Y54F701R
UPC 0370069517017, 0370069516010
Application # ANDA216653
SPL Set ID bfd95433-e47a-4c5c-9bdf-77bffc13544d
Established class (EPC) beta-Adrenergic Blocker
Mechanism of action Adrenergic beta-Antagonists
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2024-07-09
Route OPHTHALMIC
Dosage form SOLUTION/ DROPS
Substance TIMOLOL MALEATE
TE code (Orange Book) AT2 · RLD · RS

Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification

GPI-14 86250030102060
GCN Seq No 059074
GCN 24615
HICL code 002105
Ingredient (HICL) Timolol Maleate
HIC1 code Q
Therapeutic class — broad (HIC1) Ear/Eye/Nose/Rectum/Topical/Vagina/Other
HIC2 code Q6
Therapeutic class — intermediate (HIC2) Ophthalmic Preparations
HIC3 code Q6G
Therapeutic class — specific (HIC3) Miotics And Other Intraocular Pressure Reducers
AHFS code 52:40.08.00
AHFS class Beta-Adrenergic Blocking Agents (52:40)
FDB label name TIMOLOL 0.5% EYE DROP
FDB brand name Timolol Maleate
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 059074
  • GCN: 24615
  • GPI-14 (Medi-Span): 86250030102060
  • HICL (First Databank): 002105
  • AHFS class code: 52:40.08.00
  • RxCUI (RxNorm): 1992299
Why two NDCs? The FDA registers this code as 70069-516-01 — 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 → 70069-0516-01. 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 beta-Adrenergic Blocker class.

Pharmacologic class beta-Adrenergic Blocker
Drug family (ATC) Beta blocking agents, non-selective, Beta blocking agents
How it works Adrenergic beta-Antagonists
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.

Clinical

Label name TIMOLOL 0.5% EYE DROP Ingredient Timolol Maleate
📗 Our plain-language guide HelloPharmacist
  • It depends on the form. The eye drops lower high pressure in the eye from ocular hypertension or open-angle glaucoma. The tablets treat high blood pressure, lower the risk of death...
  • Put the drop in the affected eye as directed, usually once or twice a day depending on your product. If yours is a gel-forming type, shake the closed bottle once first. Wait at lea...
  • Burning or stinging right after the drops go in is the most common. Blurred vision, redness, itching and headache can also happen. Call your doctor if you notice wheezing, a very s...
  • If your drops contain benzalkonium chloride, soft lenses can absorb it. Take your lenses out before using the drops and wait 15 minutes before putting them back in.
📖 Read our full Timolol guide →

Supplement & herbal interactions

🌿 Drug–supplement interaction checker →
1
Nutrient depletion considerations

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

🧪 Full Timolol nutrient depletion report →
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.

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 mLPer package
Retail pharmacies payNADAC · weekly $21.806 $54.51 / 2.5 ml
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · Q2 2026 $43.15 $107.87 / 2.5 ml
NADAC price history (per mL) — tap or hover for the price & month
Dec 2025 Mar 2026 Jun 2026 Sep 2026 $21.806 $8.703
▲ Up 151% over the last 10 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.

Packaging — all sizes for this product

Package NDCDescription Marketing startMarketing endStatus
70069-0516-01 You're viewing this Main listing 1 BOTTLE in 1 CARTON / 2.5 mL in 1 BOTTLE 2024-07-09 — Active

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Timolol hemihydrate 5 mg/mLthis 70069-0516-01 Somerset 1 bottle $21.806 AT2 Availability likely —
Timolol hemihydrate 5 mg/mL 70069-0517-01 Somerset 1 bottle $22.290 AT2 Availability likely +2%
Timolol Maleate 5 mg/mL 82260-0045-05 Bausch 1 bottle $22.290 AT2 Availability likely +2%
Timolol Maleate 5 mg/mL 68682-0045-25 Oceanside 1 bottle $26.378 AT2 Discontinued +21%
Istalol 5 mg/mL 24208-0004-01 Bausch 1 bottle $79.763 AT2 Availability likely +266%
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

🏛️
2024
On the market since
Jul 2024
📍
2026
Currently FDA-listed
2 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.

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.

Loading inactive ingredients from the official FDA label in the background. No external source is being called by this page request.
Where does this data come from?
Source: official FDA Structured Product Labeling (SPL) via DailyMed and the openFDA label index. Structured IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.

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.

Manufacturer & labeler

LabelerSomerset Therapeutics, LLC
Application holderSOMERSET THERAPEUTICS LLC
FDA applicationANDA216653 (ANDA)
Labeler code70069
First marketedJul 2024
Product typeHuman Prescription Drug
Portfolio184 products on file

More NDCs from Somerset Therapeutics, LLC labeler code 70069

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.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📋 Description 💬 Information for Patients 🍼 Nursing Mothers 🧬 Pharmacokinetics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 Package Label / Principal Display Panel
🎯 Indications and Usage 61 words ▾

1 INDICATIONS AND USAGE Timolol maleate ophthalmic solution 0.5% is a non-selective beta-adrenergic receptor blocking agent indicated in the treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma. Timolol maleate ophthalmic solution is a non-selective beta-adrenergic receptor blocking agent indicated for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma (1)

⏱️ Dosage and Administration 38 words ▾

2 DOSAGE AND ADMINISTRATION One drop of timolol maleate ophthalmic solution 0.5% should be administered in the affected eye(s) once a day in the AM. One drop in the affected eye(s) once a day in the AM (2)

💊 Dosage Forms and Strengths 28 words ▾

3 DOSAGE FORMS AND STRENGTHS Topical ophthalmic solution, USP containing 5 mg/mL timolol (6.8 mg/mL of timolol maleate). Topical ophthalmic solution containing timolol maleate, 0.5% (5 mg/mL) (3)

⛔ Contraindications 136 words ▾

4 CONTRAINDICATIONS Bronchial asthma, a history of bronchial asthma, severe chronic obstructive pulmonary disease . (4.1, 5.1, 5.3) Sinus bradycardia, second or third degree atrioventricular block, overt cardiac failure, cardiogenic shock . (4.2, 5.2) Hypersensitivity to any component of this product (4.3)

4.1Asthma, COPD Timolol maleate ophthalmic solution is contraindicated in patients with bronchial asthma; a history of bronchial asthma; severe chronic obstructive pulmonary disease [see Warnings and Precautions, (5.1, 5.3)] .

4.2Sinus Bradycardia, AV Block, Cardiac Failure, Cardiogenic Shock Timolol maleate ophthalmic solution is contraindicated in patients with sinus bradycardia; second or third degree atrioventricular block; overt cardiac failure; cardiogenic shock [see Warnings and Precautions, (5.2)] .

4.3Hypersensitivity Reactions Timolol maleate ophthalmic solution is contraindicated in patients who have exhibited a hypersensitivity reaction to any component of this product in the past.

⚠️ Warnings and Cautions ~2 min read ▾

5 WARNINGS AND PRECAUTIONS Potentiation of Respiratory Reactions Including Asthma (5.1) Cardiac Failure (5.2) Obstructive Pulmonary Disease (5.3) Increased Reactivity to Allergens (5.4) Potentiation of Muscle Weakness (5.5) Masking of Hypoglycemic Symptoms in Patients with Diabetes Mellitus (5.6) Masking of Thyrotoxicosis (5.7)

5.1Potentiation of Respiratory Reactions Including Asthma Timolol maleate ophthalmic solution contains timolol maleate; and although administered topically, it can be absorbed systemically. Therefore, the same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory reactions and cardiac reactions including death due to bronchospasm in patients with asthma, and rarely death in association with cardiac failure, have been reported following systemic or ophthalmic administration of timolol maleate [see Contraindications, (4.1)] .

5.2Cardiac Failure Sympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition of beta-adrenergic receptor blockade may precipitate more severe failure. In patients without a history of cardiac failure, continued depression of the myocardium with beta-blocking agents over a period of time can, in some cases, lead to cardiac failure. At the first sign or symptom of cardiac failure, timolol maleate ophthalmic solution should be discontinued [see contraindications, (4.2)] .

5.3Obstructive Pulmonary Disease Patients with chronic obstructive pulmonary disease (e.g., chronic bronchitis, emphysema) of mild or moderate severity, bronchospastic disease, or a history of bronchospastic disease [other than bronchial asthma or a history of bronchial asthma in which timolol maleate ophthalmic solution is contraindicated [see Contraindications, (4.2)] should, in general, not receive beta-blocking agents, including timolol maleate ophthalmic solution.

5.4Increased Reactivity to Allergens While taking beta-blockers, patients with a history of atopy or a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated accidental, diagnostic, or therapeutic challenge with such allergens. Such patients may be unresponsive to the usual doses of epinephrine used to treat anaphylactic reactions.

5.5Potentiation of Muscle Weakness Beta-adrenergic blockade has been reported to potentiate muscle weakness consistent with certain myasthenic symptoms (e.g., diplopia, ptosis, and generalized weakness). Timolol has been reported rarely to increase muscle weakness in some patients with myasthenia gravis or myasthenic symptoms.

5.6Masking of Hypoglycemic Symptoms in Patients with Diabetes Mellitus Beta-adrenergic blocking agents should be administered with caution in patients subject to spontaneous hypoglycemia or to diabetic patients (especially those with labile diabetes) who are receiving insulin or oral hypoglycemic agents. Beta-adrenergic receptor blocking agents may mask the signs and symptoms of acute hypoglycemia.

5.7Masking of Thyrotoxicosis Beta-adrenergic blocking agents may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-adrenergic blocking agents that might precipitate a thyroid storm.

5.8Contamination of Topical Ophthalmic Products After Use There have been reports of bacterial keratitis associated with the use of multidose containers of topical ophthalmic products. These containers had been inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of the ocular epithelial surface [see Patient Counseling Information, (17)].

5.9Impairment of Beta-adrenergically Mediated Reflexes During Surgery The necessity or desirability of withdrawal of beta-adrenergic blocking agents prior to major surgery… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~2 min read ▾

6 ADVERSE REACTIONS The most frequently reported adverse reactions have been burning and stinging upon instillation in 38% of patients treated with timolol maleate ophthalmic solution. Additional reactions reported with timolol maleate ophthalmic solution at a frequency of 4 to 10% include: blurred vision, cataract, conjunctival injection, headache, hypertension, infection, itching and decreased visual acuity . (6) To report SUSPECTED ADVERSE REACTIONS, contact Somerset Therapeutics, LLC at 1-800-417-9175 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch

6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The most frequently reported adverse reactions have been burning and stinging upon instillation in 38% of patients treated with timolol maleate ophthalmic solution. Additional reactions reported with timolol maleate ophthalmic solution at a frequency of 4 to 10% include: blurred vision, cataract, conjunctival injection, headache, hypertension, infection, itching and decreased visual acuity.

The following additional adverse reactions have been reported less frequently with ocular administration of this or other timolol maleate formulations. Timolol (Ocular Administration) Body as a Whole: Asthenia/fatigue and chest pain; Cardiovascular: Bradycardia, arrhythmia, hypotension, syncope, heart block, cerebral vascular accident, cerebral ischemia, cardiac failure, worsening of angina pectoris, palpitation, cardiac arrest, pulmonary edema, edema, claudication, Raynaud's phenomenon and cold hands and feet; Digestive: Nausea, diarrhea, dyspepsia, anorexia, and dry mouth; Immunologic: Systemic lupus erythematosus; Nervous System/Psychiatric: Dizziness, increase in signs and symptoms of myasthenia gravis, paresthesia, somnolence, insomnia, nightmares, behavioral changes and psychic disturbances including depression, confusion, hallucinations, anxiety, disorientation, nervousness and memory loss; Skin: Alopecia and psoriasiform rash or exacerbation of psoriasis; Hypersensitivity: Signs and symptoms of systemic allergic reactions, including angioedema, urticaria, and localized and generalized rash; Respiratory: Bronchospasm (predominantly in patients with pre-existing bronchospastic disease), respiratory failure, dyspnea, nasal congestion, cough and upper respiratory infections; Endocrine: Masked symptoms of hypoglycemia in diabetic patients [see Warnings and Precautions (5.6)] ; Special Senses: Signs and symptoms of ocular irritation including conjunctivitis, blepharitis, keratitis, ocular pain, discharge (e.g., crusting), foreign body sensation, itching and tearing, and dry eyes; ptosis, decreased corneal sensitivity; cystoid macular edema; visual disturbances including refractive changes and diplopia; pseudopemphigoid; choroidal detachment following filtration surgery [see Warnings and Precautions, (5.12)] ; Urogenital: Retroperitoneal fibrosis, decreased libido, impotence, and Peyronie's disease.

6.2Postmarketing Experience Oral Timolol/Oral Beta-Blockers The following additional adverse effects have been reported in clinical experience with ORAL timolol maleate or other ORAL beta-blocking agents and may be considered potential effects of ophthalmic timolol maleate: Allergic: Erythematous rash, fever combined with aching and sore throat, laryngospasm with respiratory distress; Body as a Whole: Extremity pain, decreased exercise tolerance, weight loss; Cardiovascular: Worsening of arterial insufficiency, vasodilatation; Digestive : Gastrointestinal pain, hepatomegaly, vomiting, mesenteric arterial thrombosis, ischemic colitis; Hematologic : Nonthrombocytopenic purpura; thrombocytopenic purpura, agranulocytosis; Endocrine: Hyperglycemia, hypoglycemia; Skin: Pruritus, skin irritation, increased pigme… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions ~1 min read ▾

7 DRUG INTERACTIONS Concomitant use with systemic beta-blockers may potentiate systemic beta- blockade. (7.1) Oral or intravenous calcium antagonists may cause atrioventricular conduction disturbances, left ventricular failure, and hypotension . (7.2) Catecholamine-depleting drugs may have additive effects and produce hypotension and/or marked bradycardia .

(7.3) Digitalis and calcium antagonists may have additive effects in prolonging atrioventricular conduction time. (7.4) Potentiated systemic beta-blockade (e.g., decreased heart rate) has been reported during combined treatment with quinidine and timolol. (7.5)

7.1Beta-Adrenergic Blocking Agents Patients who are receiving a beta-adrenergic blocking agent orally and timolol maleate ophthalmic solution should be observed for potential additive effects of beta-blockade, both systemic and on intraocular pressure. The concomitant use of two topical beta-adrenergic blocking agents is not recommended.

7.2Calcium Antagonists Caution should be used in the co-administration of beta-adrenergic blocking agents, such as timolol maleate ophthalmic solution, and oral or intravenous calcium antagonists because of possible atrioventricular conduction disturbances, left ventricular failure, and hypotension. In patients with impaired cardiac function, co-administration should be avoided.

7.3Catecholamine-Depleting Drugs Close observation of the patient is recommended when a beta-blocker is administered to patients receiving catecholamine-depleting drugs such as reserpine, because of possible additive effects and the production of hypotension and/or marked bradycardia, which may result in vertigo, syncope, or postural hypotension.

7.4Digitalis and Calcium Antagonists The concomitant use of beta-adrenergic blocking agents with digitalis and calcium antagonists may have additive effects in prolonging atrioventricular conduction time.

7.5CYP2D6 Inhibitors Potentiated systemic beta-blockade (e.g., decreased heart rate) has been reported during combined treatment with CYP2D6 inhibitors (e.g., quinidine) and timolol.

7.6Clonidine Oral beta-adrenergic blocking agents may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. There have been no reports of exacerbation of rebound hypertension with ophthalmic timolol maleate.

👥 Use in Specific Populations ~1 min read ▾

8 USE IN SPECIFIC POPULATIONS

8.1Pregnancy Teratogenic Effects: Teratogenicity studies have been performed in animals. Teratogenicity studies with timolol in mice, rats, and rabbits at oral doses up to 50 mg/kg/day (7,000 times the systemic exposure following the maximum recommended human ophthalmic dose) demonstrated no evidence of fetal malformations. Although delayed fetal ossification was observed at this dose in rats, there were no adverse effects on postnatal development of offspring.

Doses of 1000 mg/kg/day (142,000 times the systemic exposure following the maximum recommended human ophthalmic dose) were maternotoxic in mice and resulted in an increased number of fetal resorptions. Increased fetal resorptions were also seen in rabbits at doses of 14,000 times the systemic exposure following the maximum recommended human ophthalmic dose, in this case without apparent maternotoxicity. There are no adequate and well-controlled studies in pregnant women.

Timolol maleate ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

8.3Nursing Mothers Timolol has been detected in human milk following oral and ophthalmic drug administration. Because of the potential for serious adverse reactions from timolol maleate ophthalmic solution in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

8.4Pediatric Use Safety and effectiveness in pediatric patients have not been established.

8.5Geriatric Use No overall differences in safety or effectiveness have been observed between elderly and younger patients.

🤰 Pregnancy 155 words ▾

8.1Pregnancy Teratogenic Effects: Teratogenicity studies have been performed in animals. Teratogenicity studies with timolol in mice, rats, and rabbits at oral doses up to 50 mg/kg/day (7,000 times the systemic exposure following the maximum recommended human ophthalmic dose) demonstrated no evidence of fetal malformations. Although delayed fetal ossification was observed at this dose in rats, there were no adverse effects on postnatal development of offspring.

Doses of 1000 mg/kg/day (142,000 times the systemic exposure following the maximum recommended human ophthalmic dose) were maternotoxic in mice and resulted in an increased number of fetal resorptions. Increased fetal resorptions were also seen in rabbits at doses of 14,000 times the systemic exposure following the maximum recommended human ophthalmic dose, in this case without apparent maternotoxicity. There are no adequate and well-controlled studies in pregnant women.

Timolol maleate ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

🧒 Pediatric Use 13 words ▾

8.4Pediatric Use Safety and effectiveness in pediatric patients have not been established.

🧓 Geriatric Use 18 words ▾

8.5Geriatric Use No overall differences in safety or effectiveness have been observed between elderly and younger patients.

🆘 Overdosage 79 words ▾

10 OVERDOSAGE There have been reports of inadvertent overdosage with timolol maleate ophthalmic solution resulting in systemic effects similar to those seen with systemic beta-adrenergic blocking agents such as dizziness, headache, shortness of breath, bradycardia, bronchospasm, and cardiac arrest. An in vitro hemodialysis study, using 14 C timolol added to human plasma or whole blood, showed that timolol was readily dialyzed from these fluids; however, a study of patients with renal failure showed that timolol did not dialyze readily.

🧬 Clinical Pharmacology ~2 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Timolol maleate is a beta 1 and beta 2 (non-selective) adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. Beta-adrenergic receptor blockade reduces cardiac output in both healthy subjects and patients with heart disease. In patients with severe impairment of myocardial function, beta adrenergic receptor blockade may inhibit the stimulatory effect of the sympathetic nervous system necessary to maintain adequate cardiac function.

Beta-adrenergic receptor blockade in the bronchi and bronchioles results in increased airway resistance from unopposed parasympathetic activity. Such an effect in patients with asthma or other bronchospastic conditions is potentially dangerous. Timolol maleate ophthalmic solution, when applied topically on the eye, has the action of reducing elevated as well as normal intraocular pressure, whether or not accompanied by glaucoma.

Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss. The higher the level of intraocular pressure, the greater the likelihood of glaucomatous visual field loss and optic nerve damage. The onset of reduction in intraocular pressure following administration of timolol maleate ophthalmic solution can usually be detected within one-half hour after a single dose.

The maximum effect usually occurs in one to two hours and significant lowering of intraocular pressure can be maintained for periods as long as 24 hours with a single dose. Repeated observations over a period of one year indicate that the intraocular pressure lowering effect of timolol maleate ophthalmic solution is well maintained. The precise mechanism of the ocular hypotensive action of timolol maleate ophthalmic solution is not clearly established at this time.

Tonography and fluorophotometry studies in man suggest that its predominant action may be related to reduced aqueous formation. However, in some studies a slight increase in outflow facility was also observed.

12.3Pharmacokinetics In a study of plasma drug concentration in 12 healthy subjects, the systemic exposure to timolol was determined following twice daily administration of timolol maleate ophthalmic solution (exaggerated regimen) for eight days. With timolol maleate ophthalmic solution mean plasma concentrations of timolol were 0.68 ng/mL and 0.88 ng/mL two hours after the first dose and the dose on the eighth day, respectively.

🧬 Mechanism of Action ~1 min read ▾

12.1Mechanism of Action Timolol maleate is a beta 1 and beta 2 (non-selective) adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. Beta-adrenergic receptor blockade reduces cardiac output in both healthy subjects and patients with heart disease. In patients with severe impairment of myocardial function, beta adrenergic receptor blockade may inhibit the stimulatory effect of the sympathetic nervous system necessary to maintain adequate cardiac function.

Beta-adrenergic receptor blockade in the bronchi and bronchioles results in increased airway resistance from unopposed parasympathetic activity. Such an effect in patients with asthma or other bronchospastic conditions is potentially dangerous. Timolol maleate ophthalmic solution, when applied topically on the eye, has the action of reducing elevated as well as normal intraocular pressure, whether or not accompanied by glaucoma.

Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss. The higher the level of intraocular pressure, the greater the likelihood of glaucomatous visual field loss and optic nerve damage. The onset of reduction in intraocular pressure following administration of timolol maleate ophthalmic solution can usually be detected within one-half hour after a single dose.

The maximum effect usually occurs in one to two hours and significant lowering of intraocular pressure can be maintained for periods as long as 24 hours with a single dose. Repeated observations over a period of one year indicate that the intraocular pressure lowering effect of timolol maleate ophthalmic solution is well maintained. The precise mechanism of the ocular hypotensive action of timolol maleate ophthalmic solution is not clearly established at this time.

Tonography and fluorophotometry studies in man suggest that its predominant action may be related to reduced aqueous formation. However, in some studies a slight increase in outflow facility was also observed.

📦 How Supplied / Storage and Handling 59 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING Timolol maleate ophthalmic solution, USP 0.5% is supplied in white LDPE bottles with 15 mm HDPE yellow caps and 15 mm LDPE white dropper tips as follows: 5 mL in 10mL container (NDC 70069- 517 -01) 2.5 mL in 5mL container (NDC 70069- 516 -01) STORAGE Store at 15º – 25ºC (59º – 77ºF).

📋 Description 184 words ▾

11 DESCRIPTION Timolol maleate ophthalmic solution 0.5% is a non-selective beta-adrenergic receptor blocking agent. Its chemical name is (-)-1-( tert -butylamino) -3- [(4-morpholino 1,2,5-thiadiazol-3-yl)oxy]-2-propanol maleate (1:1) (salt). Timolol maleate possesses an asymmetric carbon atom in its structure and is provided as the levo-isomer.

Its molecular formula is C 13 H 24 N 4 O 3 S-C 4 H 4 O 4 and its structural formula is: Timolol maleate has a molecular weight of 432.49. It is a white or almost white, crystalline powder which is soluble in water, sparingly soluble in ethanol, slightly soluble in chloroform, practically insoluble in ether. Timolol maleate ophthalmic solution is stable at room temperature.

Timolol maleate ophthalmic solution is supplied as a sterile, isotonic, buffered, aqueous solution of timolol maleate in a single strength. It has a pH of 6.5-7.5 and an osmolality of 275-330 mOsm/kg. Each mL of timolol maleate ophthalmic solution contains the active ingredient 5 mg of timolol (6.8 mg of timolol maleate) with the inactive ingredients benzalkonium chloride (0.05 mg/mL), monobasic sodium phosphate monohydrate, potassium sorbate 0.47%, sodium chloride, sodium hydroxide, and purified water.

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💬 Information for Patients 200 words ▾

17 PATIENT COUNSELING INFORMATION Patients with bronchial asthma, a history of bronchial asthma, severe chronic obstructive pulmonary disease, sinus bradycardia, second or third degree atrioventricular block, or cardiac failure should be advised not to take this product [see Contraindications (4.1, 4.2)] . Patients should also be instructed that ocular solutions, if handled improperly or if the tip of the dispensing container contacts the eye or surrounding structures, can become contaminated by common bacteria known to cause ocular infections.

Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions [see Warnings and Precautions (5.8)] . Patients should also be advised that if they have ocular surgery or develop an intercurrent ocular condition (e.g., trauma or infection), they should immediately seek their physician's advice concerning the continued use of the present multidose container. If more than one topical ophthalmic drug is being used, the drugs should be administered at least five minutes apart.

Patients should be advised that timolol maleate ophthalmic solution contains benzalkonium chloride which may be absorbed by soft contact lenses. Contact lenses should be removed prior to administration of the solution. Lenses may be reinserted 15 minutes following timolol maleate ophthalmic solution administration.

🍼 Nursing Mothers 57 words ▾

8.3Nursing Mothers Timolol has been detected in human milk following oral and ophthalmic drug administration. Because of the potential for serious adverse reactions from timolol maleate ophthalmic solution in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

🧬 Pharmacokinetics 64 words ▾

12.3Pharmacokinetics In a study of plasma drug concentration in 12 healthy subjects, the systemic exposure to timolol was determined following twice daily administration of timolol maleate ophthalmic solution (exaggerated regimen) for eight days. With timolol maleate ophthalmic solution mean plasma concentrations of timolol were 0.68 ng/mL and 0.88 ng/mL two hours after the first dose and the dose on the eighth day, respectively.

🔬 Clinical Studies 106 words ▾

14 CLINICAL STUDIES In a controlled, double-masked, parallel study in 332 patients with untreated intraocular pressures of 22 mm Hg or greater, timolol maleate ophthalmic solution 0.5% administered once daily (AM) was equivalent to timolol maleate ophthalmic solution 0.5% administered twice daily. In both groups, mean intraocular pressure decreased from 25 mm Hg at baseline to 18 mm Hg at peak and 19 mm Hg at trough. timolol maleate ophthalmic solution was generally well tolerated, and 3% of patients had treatment discontinued for adverse events judged related to treatment.

There was a slight decrease in cardiovascular function consistent with known systemic absorption of a b-adrenoceptor antagonists.

🧪 Nonclinical Toxicology ~2 min read ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility In a two-year study of timolol maleate administered orally to rats, there was a statistically significant increase in the incidence of adrenal pheochromocytomas in male rats administered 300 mg/kg/day (approximately 42,000 times the systemic exposure following the maximum recommended human ophthalmic dose). Similar differences were not observed in rats administered oral doses equivalent to approximately 14,000 times the maximum recommended human ophthalmic dose.

In a lifetime oral study in mice, there were statistically significant increases in the incidence of benign and malignant pulmonary tumors, benign uterine polyps and mammary adenocarcinomas in female mice at 500 mg/kg/day, (approximately 71,000 times the systemic exposure following the maximum recommended human ophthalmic dose), but not at 5 or 50 mg/kg/day (approximately 700 or 7,000, respectively, times the systemic exposure following the maximum recommended human ophthalmic dose). In a subsequent study in female mice, in which post-mortem examinations were limited to the uterus and the lungs, a statistically significant increase in the incidence of pulmonary tumors was again observed at 500 mg/kg/day.

The increased occurrence of mammary adenocarcinomas was associated with elevations in serum prolactin which occurred in female mice administered oral timolol at 500 mg/kg/day, but not at doses of 5 or 50 mg/kg/day. An increased incidence of mammary adenocarcinomas in rodents has been associated with administration of several other therapeutic agents that elevate serum prolactin, but no correlation between serum prolactin levels and mammary tumors has been established in humans. Furthermore, in adult human female subjects who received oral dosages of up to 60 mg of timolol maleate (the maximum recommended human oral dosage), there were no clinically meaningful changes in serum prolactin.

Timolol maleate was devoid of mutagenic potential when tested in vivo (mouse) in the micronucleus test and cytogenetic assay (doses up to 800 mg/kg) and in vitro in a neoplastic cell transformation assay (up to 100 mcg/mL). In Ames tests the highest concentrations of timolol employed, 5,000 or 10,000 mcg/plate, were associated with statistically significant elevations of revertants observed with tester strain TA100 (in seven replicate assays), but not in the remaining three strains. In the assays with tester strain TA100, no consistent dose response relationship was observed, and the ratio of test to control revertants did not reach 2.

A ratio of 2 is usually considered the criterion for a positive Ames test. Reproduction and fertility studies in rats demonstrated no adverse effect on male or female fertility at doses up to 21,000 times the systemic exposure following the maximum recommended human ophthalmic dose.

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility ~2 min read ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility In a two-year study of timolol maleate administered orally to rats, there was a statistically significant increase in the incidence of adrenal pheochromocytomas in male rats administered 300 mg/kg/day (approximately 42,000 times the systemic exposure following the maximum recommended human ophthalmic dose). Similar differences were not observed in rats administered oral doses equivalent to approximately 14,000 times the maximum recommended human ophthalmic dose.

In a lifetime oral study in mice, there were statistically significant increases in the incidence of benign and malignant pulmonary tumors, benign uterine polyps and mammary adenocarcinomas in female mice at 500 mg/kg/day, (approximately 71,000 times the systemic exposure following the maximum recommended human ophthalmic dose), but not at 5 or 50 mg/kg/day (approximately 700 or 7,000, respectively, times the systemic exposure following the maximum recommended human ophthalmic dose). In a subsequent study in female mice, in which post-mortem examinations were limited to the uterus and the lungs, a statistically significant increase in the incidence of pulmonary tumors was again observed at 500 mg/kg/day.

The increased occurrence of mammary adenocarcinomas was associated with elevations in serum prolactin which occurred in female mice administered oral timolol at 500 mg/kg/day, but not at doses of 5 or 50 mg/kg/day. An increased incidence of mammary adenocarcinomas in rodents has been associated with administration of several other therapeutic agents that elevate serum prolactin, but no correlation between serum prolactin levels and mammary tumors has been established in humans. Furthermore, in adult human female subjects who received oral dosages of up to 60 mg of timolol maleate (the maximum recommended human oral dosage), there were no clinically meaningful changes in serum prolactin.

Timolol maleate was devoid of mutagenic potential when tested in vivo (mouse) in the micronucleus test and cytogenetic assay (doses up to 800 mg/kg) and in vitro in a neoplastic cell transformation assay (up to 100 mcg/mL). In Ames tests the highest concentrations of timolol employed, 5,000 or 10,000 mcg/plate, were associated with statistically significant elevations of revertants observed with tester strain TA100 (in seven replicate assays), but not in the remaining three strains. In the assays with tester strain TA100, no consistent dose response relationship was observed, and the ratio of test to control revertants did not reach 2.

A ratio of 2 is usually considered the criterion for a positive Ames test. Reproduction and fertility studies in rats demonstrated no adverse effect on male or female fertility at doses up to 21,000 times the systemic exposure following the maximum recommended human ophthalmic dose.

📄 Package Label / Principal Display Panel 92 words ▾

PACKAGE LABEL.PRINCIPAL DISPLAY PANEL Container Label – 2.5 mL NDC 70069-516-01 Rx only Timolol Maleate Ophthalmic Solution USP 0.5% 2.5 mL Sterile Carton Label – 2.5 mL NDC 70069-516-01 Rx only Timolol Maleate Ophthalmic Solution USP 0.5% For topical application in the eye 2.5 mL Sterile Container Label – 5 mL NDC 70069-517-01 Rx only Timolol Maleate Ophthalmic Solution USP 0.5% 5 mL Sterile Carton Label – 5 mL NDC 70069-517-01 Rx only Timolol Maleate Ophthalmic Solution USP 0.5% For topical application in the eye 5 mL Sterile Image Image Image Image

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

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 Timolol Hemihydrate — the ingredient across all brands.

Top reported reactions

Confusional State3
Death3
Fatigue2
Abdominal Pain1
Acute Kidney Injury1
Adverse Drug Reaction1
Amnesia1

Reporter sex

13 reports
Male · 33%
Female · 67%

Serious outcomes

Hospitalization5
Reports over time (by year) — tap or hover for the count & year
2019 2021 2023 2026 2 0
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.
← 70069-0506-25 · Somerset 70069-0517-01 · Somerset →
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.