Dexmedetomidine 200 ug/2mL Injection, Solution
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Central alpha-2 Adrenergic Agonist class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Dexmedetomidine is used to provide short-term sedation (you are relaxed, sleepy or in some cases asleep) for surgical procedures or during mechanical ventilation. Dexmedetomidine is in a class of medications called alpha2 receptor agonists. It works by changing the activity of certain natural substances in the brain.
Read the full MedlinePlus article ↗- Dexmedetomidine is used to keep patients calm and comfortable when they need a breathing machine or are going through a stressful procedure in a hospital setting. It helps reduce a...
- Why is my loved one getting dexmedetomidine in the ICU?
- Yes — low blood pressure and a slow heart rate are the most common serious risks with this medication. Your care team knows this and will continuously monitor your heart rate, bloo...
- Can dexmedetomidine cause my heart rate or blood pressure to drop dangerously low?
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Some supplements/herbs that may interact with Dexmedetomidine — tap one for details:
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🧪 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.
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UNII 451W47IQ8X
Sodium chloride is common table salt. It's used in medicines as a buffer to maintain proper pH, as a filler to add bulk, or to adjust the osmotic balance in liquid formulations.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
2 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient 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
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💲 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 system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| 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 · quarterly | No Part D plan price is available for this NDC in our data. | |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Dexmedetomidine HCl 100 ug/mL 00143-9532-25 | Hikma | 25 vials | — | AP | FDA listed | — |
| Precedex 100 ug/mL 00404-9938-02 | Henry | 1 vial | — | AP | FDA listed | — |
| Precedex 100 ug/mL 00409-1638-02 | Hospira, | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine 100 ug/mL 16729-0239-93 | Accord | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine Hydrochloride 100 ug/mL 36000-0262-05 | Baxter | 5 vials | — | AP | FDA listed | — |
| Dexmedetomidine Hydrochloride 100 ug/mL 42023-0146-25 | Par | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine 100 ug/mL 55150-0209-02 | Eugia | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine Hydrochloride 100 ug/mL 57664-0596-50 | Sun | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine Hydrochloride 100 ug/mL 63323-0421-02 | Fresenius | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine Hydrochloride 100 ug/mL 65219-0642-02 | Fresenius | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine 200 ug/2mL 66794-0230-42 | Piramal | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine 200 ug/2mL 66794-0233-42 | Piramal | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine 100 ug/mL 67457-0251-02 | Mylan | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine 100 ug/mL 68083-0527-25 | Gland | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine 100 ug/mL 71288-0505-03 | Meitheal | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine hydrochloride 100 ug/mL 71872-7030-01 | Medical | 1 vial | — | AP | FDA listed | — |
| Dexmedetomidine Hydrochloride 100 ug/mL 71872-7031-01 | Medical | 1 vial | — | AP | FDA listed | — |
| Dexmedetomidine Hydrochloride 100 ug/mL 71872-7122-01 | Medical | 1 vial | — | AP | FDA listed | — |
| Dexmedetomidine HCl 100 ug/mL 71872-7218-01 | Medical | 1 vial | — | AP | FDA listed | — |
| Dexmedetomidine 200 ug/2mLthis 71872-7323-01 | Medical | 1 vial | — | AP | FDA listed | — |
| Dexmedetomidine 100 ug/mL 83634-0600-02 | Avenacy | 25 vials | — | AP | FDA listed | — |
| Dexmedetomidine 200 ug/2mL 84549-0230-42 | ProPharma | 2 ml | — | AP | FDA listed | — |
| Dexmedetomidine 100 ug/mL 84549-0505-03 | ProPharma | 2 ml | — | AP | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 71872-7323-01 You're viewing this | 1 VIAL, GLASS in 1 BAG (71872-7323-1) / 2 mL in 1 VIAL, GLASS | 2024-01-22 | Active |
🧭 About this NDC listing & data coverage
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| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE
1.1Intensive Care Unit Sedation Dexmedetomidine injection is indicated for sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting. Dexmedetomidine injection should be administered by continuous infusion not to exceed 24 hours. Dexmedetomidine injection has been continuously infused in mechanically ventilated patients prior to extubation, during extubation, and post-extubation.
It is not necessary to discontinue dexmedetomidine injection prior to extubation.
1.2Procedural Sedation Dexmedetomidine injection is indicated for sedation of non-intubated patients prior to and/or during surgical and other procedures. Dexmedetomidine injection is a relatively selective alpha 2 -adrenergic agonist indicated for: Sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting. Administer dexmedetomidine injection by continuous infusion not to exceed 24 hours.
( 1.1 ) Sedation of non-intubated patients prior to and/or during surgical and other procedures. ( 1.2 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION
2.1Dosing Guidelines • Dexmedetomidine injection dosing should be individualized and titrated to desired clinical response. • Dexmedetomidine injection is not indicated for infusions lasting longer than 24 hours. • Dexmedetomidine injection should be administered using a controlled infusion device.
2.2Dosage Information Table 1: Dosage Information INDICATION DOSAGE AND ADMINISTRATION Initiation of Intensive Care Unit Sedation For adult patients: a loading infusion of one mcg/kg over 10 minutes. For adult patients being converted from alternate sedative therapy: a loading dose may not be required. For patients over 65 years of age: a dose reduction should be considered [see Use in Specific Populations ( 8.5 )].
For adult patients with impaired hepatic function: a dose reduction should be considered [see Use in Specific Populations ( 8.6 ), Clinical Pharmacology ( 12.3 )]. Maintenance of Intensive Care Unit Sedation For adult patients: a maintenance infusion of 0.2 to 0.7 mcg/kg/hour. The rate of the maintenance infusion should be adjusted to achieve the desired level of sedation.
For patients over 65 years of age: a dose reduction should be considered [see Use in Specific Populations ( 8.5 )]. For adult patients with impaired hepatic function: a dose reduction should be considered [see Use in Specific Populations ( 8.6 ), Clinical Pharmacology ( 12.3 )]. Initiation of Procedural Sedation For adult patients: a loading infusion of one mcg/kg over 10 minutes.
For less invasive procedures such as ophthalmic surgery, a loading infusion of 0.5 mcg/kg given over 10 minutes may be suitable. For awake fiberoptic intubation in adult patients: a loading infusion of one mcg/kg over 10 minutes. For patients over 65 years of age: a loading infusion of 0.5 mcg/kg over 10 minutes [see Use in Specific Populations ( 8.5 )].
For adult patients with impaired hepatic function: a dose reduction should be considered [see Use in Specific Populations ( 8.6 ), Clinical Pharmacology ( 12.3 )]. Maintenance of Procedural Sedation For adult patients: the maintenance infusion is generally initiated at 0.6 mcg/kg/hour and titrated to achieve desired clinical effect with doses ranging from 0.2 to 1 mcg/kg/hour. The rate of the maintenance infusion should be adjusted to achieve the targeted level of sedation.
For awake fiberoptic intubation in adult patients: a maintenance infusion of 0.7 mcg/kg/hour is recommended until the endotracheal tube is secured. For patients over 65 years of age: a dose reduction should be considered [see Use in Specific Populations ( 8.5 )]. For adult patients with impaired hepatic function: a dose reduction should be considered [see Use in Specific Populations ( 8.6 ), Clinical Pharmacology ( 12.3 )].
2.3Dosage Adjustment Due to possible pharmacodynamic interactions, a reduction in dosage of dexmedetomidine injection or other concomitant anesthetics, sedatives, hypnotics or opioids may be required when co-administered [see Drug Interactions ( 7.1 )]. Dosage reductions may need to be considered for adult patients with hepatic impairment, and geriatric patients [see Warnings and Precautions ( 5.7 ), Use in Specific Populations ( 8.6 ), Clinical Pharmacology ( 12.3 )].
2.4Preparation of Solution Strict aseptic technique must always be maintained during handling of dexmedetomidine injection. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Dexmedetomidine Injection, 200 mcg/2 mL (100 mcg/mL) Dexmedetomidine injection must be diluted with 0.9% sodium chloride injection to achieve required concentration (4 mcg/mL) prior to administration.
Preparation of solutions is the same, whether for the loading dose or maintenance infusion. To prepare the infusion, withdraw 2 mL of dexmedetomidine injection, and add to 48 mL of 0.9% sodium chloride injection to a total of 50 mL. Shake gently to mix well.
2.5 Ad…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Dexmedetomidine Injection, USP is clear and colorless and is available as follows. Dexmedetomidine Injection, USP 200 mcg/2 mL (100 mcg/mL) in a glass vial with pink cap. To be used after dilution. Dexmedetomidine Injection, USP 200 mcg/2 mL (100 mcg/mL) in a glass vial with pink cap. To be used after dilution. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS
5.1Drug Administration Dexmedetomidine injection should be administered only by persons skilled in the management of patients in the intensive care or operating room setting. Due to the known pharmacological effects of dexmedetomidine injection, patients should be continuously monitored while receiving dexmedetomidine injection.
5.2Hypotension, Bradycardia, and Sinus Arrest Clinically significant episodes of bradycardia and sinus arrest have been reported with dexmedetomidine injection administration in young, healthy adult volunteers with high vagal tone or with different routes of administration including rapid intravenous or bolus administration. Reports of hypotension and bradycardia have been associated with dexmedetomidine injection infusion. Some of these cases have resulted in fatalities.
If medical intervention is required, treatment may include decreasing or stopping the infusion of dexmedetomidine injection, increasing the rate of intravenous fluid administration, elevation of the lower extremities, and use of pressor agents. Because dexmedetomidine injection has the potential to augment bradycardia induced by vagal stimuli, clinicians should be prepared to intervene. The intravenous administration of anticholinergic agents (e.g., glycopyrrolate, atropine) should be considered to modify vagal tone.
In clinical trials, glycopyrrolate or atropine were effective in the treatment of most episodes of dexmedetomidine hydrochloride-induced bradycardia. However, in some patients with significant cardiovascular dysfunction, more advanced resuscitative measures were required. Caution should be exercised when administering dexmedetomidine injection to patients with advanced heart block and/or severe ventricular dysfunction.
Because dexmedetomidine injection decreases sympathetic nervous system activity, hypotension and/or bradycardia may be expected to be more pronounced in patients with hypovolemia, diabetes mellitus, or chronic hypertension and in elderly patients. In clinical trials where other vasodilators or negative chronotropic agents were co-administered with dexmedetomidine injection an additive pharmacodynamic effect was not observed. Nonetheless, caution should be used when such agents are administered concomitantly with dexmedetomidine injection.
5.3Transient Hypertension Transient hypertension has been observed primarily during the loading dose in association with the initial peripheral vasoconstrictive effects of dexmedetomidine injection. Treatment of the transient hypertension has generally not been necessary, although reduction of the loading infusion rate may be desirable.
5.4Arousability Some patients receiving dexmedetomidine injection have been observed to be arousable and alert when stimulated. This alone should not be considered as evidence of lack of efficacy in the absence of other clinical signs and symptoms.
5.5Withdrawal Intensive Care Unit Sedation With administration up to 7 days, regardless of dose, 12 (5%) dexmedetomidine injection adult subjects experienced at least 1 event related to withdrawal within the first 24 hours after discontinuing study drug and 7 (3%) dexmedetomidine injection adult subjects experienced at least 1 event 24 to 48 hours after end of study drug. The most common events were nausea, vomiting, and agitation. In adult subjects, tachycardia and hypertension requiring intervention in the 48 hours following study drug discontinuation occurred at frequencies of <5%.
If tachycardia and/or hypertension occurs after discontinuation of dexmedetomidine injection supportive therapy is indicated. Procedural Sedation In adult subjects, withdrawal symptoms were not seen after discontinuation of short-term infusions of dexmedetomidine injection (<6 hours).
5.6Tolerance and Tachyphylaxis Use of dexmedetomidine beyond 24 hours has been associated with tolerance and tachyphylaxis and a dose-related increase in adverse reactions [see Adverse Reactions ( 6.1 )…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: • Hypotension, bradycardia and sinus arrest [ see Warnings and Precautions ( 5.2 )] • Transient hypertension [see Warnings and Precautions ( 5.3 )]
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reactions 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. Most common treatment-emergent adverse reactions, occurring in greater than 2% of patients in both Intensive Care Unit and procedural sedation studies include hypotension, bradycardia and dry mouth. Intensive Care Unit Sedation Adverse reaction information is derived from the continuous infusion trials of dexmedetomidine injection for sedation in the Intensive Care Unit setting in which 1,007 adult patients received dexmedetomidine injection.
The mean total dose was 7.4 mcg/kg (range: 0.8 to 84.1), mean dose per hour was 0.5 mcg/kg/hr (range: 0.1 to 6.0) and the mean duration of infusion of 15.9 hours (range: 0.2 to 157.2). The population was between 17 to 88 years of age, 43% ≥65 years of age, 77% male and 93% Caucasian. Treatment-emergent adverse reactions occurring at an incidence of >2% are provided in Table 2.
The most frequent adverse reactions were hypotension, bradycardia and dry mouth [see Warnings and Precautions ( 5.2 )]. Table 2: Adverse Reactions with an Incidence >2%-Adult Intensive Care Unit Sedation Population <24 hours* Adverse Event All Dexmedetomidine Injection (N = 1007) (%) Randomized Dexmedetomidine Injection (N = 798) (%) Placebo (N = 400) (%) Propofol (N = 188) (%) Hypotension 25% 24% 12% 13% Hypertension 12% 13% 19% 4% Nausea 9% 9% 9% 11% Bradycardia 5% 5% 3% 0 Atrial Fibrillation 4% 5% 3% 7% Pyrexia 4% 4% 4% 4% Dry Mouth 4% 3% 1% 1% Vomiting 3% 3% 5% 3% Hypovolemia 3% 3% 2% 5% Atelectasis 3% 3% 3% 6% Pleural Effusion 2% 2% 1% 6% Agitation 2% 2% 3% 1% Tachycardia 2% 2% 4% 1% Anemia 2% 2% 2% 2% Hyperthermia 2% 2% 3% 0 Chills 2% 2% 3% 2% Hyperglycemia 2% 2% 2% 3% Hypoxia 2% 2% 2% 3% Post-procedural Hemorrhage 2% 2% 3% 4% Pulmonary Edema 1% 1% 1% 3% Hypocalcemia 1% 1% 0 2% Acidosis 1% 1% 1% 2% Urine Output Decreased 1% 1% 0 2% Sinus Tachycardia 1% 1% 1% 2% Ventricular Tachycardia <1% 1% 1% 5% Wheezing <1% 1% 0 2% Edema Peripheral <1% 0 1% 2% * 26 subjects in the all dexmedetomidine injection group and 10 subjects in the randomized dexmedetomidine injection group had exposure for greater than 24 hours Adverse reaction information was also derived from the placebo-controlled, continuous infusion trials of dexmedetomidine injection for sedation in the surgical intensive care unit setting in which 387 adult patients received dexmedetomidine injection for less than 24 hours.
The most frequently observed treatment-emergent adverse events included hypotension, hypertension, nausea, bradycardia, fever, vomiting, hypoxia, tachycardia and anemia (see Table 3). Table 3: Treatment-Emergent Adverse Events Occurring in >1% of All Dexmedetomidine-Treated Adult Patients in the Randomized Placebo-Controlled Continuous Infusion <24 Hours ICU Sedation Studies Adverse Event Randomized Dexmedetomidine (N = 387) Placebo (N = 379) Hypotension 28% 13% Hypertension 16% 18% Nausea 11% 9% Bradycardia 7% 3% Fever 5% 4% Vomiting 4% 6% Atrial Fibrillation 4% 3% Hypoxia 4% 4% Tachycardia 3% 5% Hemorrhage 3% 4% Anemia 3% 2% Dry Mouth 3% 1% Rigors 2% 3% Agitation 2% 3% Hyperpyrexia 2% 3% Pain 2% 2% Hyperglycemia 2% 2% Acidosis 2% 2% Pleural Effusion 2% 1% Oliguria 2% <1% Thirst 2% <1% In a controlled clinical trial, dexmedetomidine injection was compared to midazolam for ICU sedation exceeding 24 hours duration in adult patients.
Key treatment emergent adverse events occurring in dexmedetomidine or midazolam treated patients in the randomized active comparator continuous infusion long-ter…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS
7.1Anesthetics, Sedatives, Hypnotics, Opioids Co-administration of dexmedetomidine injection with anesthetics, sedatives, hypnotics, and opioids is likely to lead to an enhancement of effects. Specific studies have confirmed these effects with sevoflurane, isoflurane, propofol, alfentanil, and midazolam. No pharmacokinetic interactions between dexmedetomidine injection and isoflurane, propofol, alfentanil and midazolam have been demonstrated.
However, due to possible pharmacodynamic interactions, when co-administered with dexmedetomidine injection, a reduction in dosage of dexmedetomidine injection or the concomitant anesthetic, sedative, hypnotic or opioid may be required.
7.2Neuromuscular Blockers In one study of 10 healthy adult volunteers, administration of dexmedetomidine injection for 45 minutes at a plasma concentration of one ng/mL resulted in no clinically meaningful increases in the magnitude of neuromuscular blockade associated with rocuronium administration. Anesthetics, Sedatives, Hypnotics, Opioids: Enhancement of pharmacodynamic effects. Reduction in dosage of dexmedetomidine hydrochloride or the concomitant medication may be required.
( 7.1 )
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Pregnancy Category C There are no adequate and well-controlled studies of dexmedetomidine injection use in pregnant women. In an in vitro human placenta study, placental transfer of dexmedetomidine occurred. In a study in the pregnant rat, placental transfer of dexmedetomidine was observed when radiolabeled dexmedetomidine was administered subcutaneously.
Thus, fetal exposure should be expected in humans, and dexmedetomidine injection should be used during pregnancy only if the potential benefits justify the potential risk to the fetus. Teratogenic effects were not observed in rats following subcutaneous administration of dexmedetomidine during the period of fetal organogenesis (from gestation day 5 to 16) with doses up to 200 mcg/kg (representing a dose approximately equal to the maximum recommended human intravenous dose based on body surface area) or in rabbits following intravenous administration of dexmedetomidine during the period of fetal organogenesis (from gestation day 6 to 18) with doses up to 96 mcg/kg (representing approximately half the human exposure at the maximum recommended dose based on plasma area under the time-curve comparison).
However, fetal toxicity, as evidenced by increased post-implantation losses and reduced live pups, was observed in rats at a subcutaneous dose of 200 mcg/kg. The no-effect dose in rats was 20 mcg/kg (representing a dose less than the maximum recommended human intravenous dose based on a body surface area comparison). In another reproductive toxicity study when dexmedetomidine was administered subcutaneously to pregnant rats at 8 and 32 mcg/kg (representing a dose less than the maximum recommended human intravenous dose based on a body surface area comparison) from gestation day 16 through weaning, lower offspring weights were observed.
Additionally, when offspring of the 32 mcg/kg group were allowed to mate, elevated fetal and embryocidal toxicity and delayed motor development was observed in second generation offspring.
8.2Labor and Delivery The safety of dexmedetomidine injection during labor and delivery has not been studied.
8.3Nursing Mothers It is not known whether dexmedetomidine hydrochloride is excreted in human milk. Radio-labeled dexmedetomidine administered subcutaneously to lactating female rats was excreted in milk. Because many drugs are excreted in human milk, caution should be exercised when dexmedetomidine injection is administered to a nursing woman.
8.4Pediatric Use Safety and efficacy have not been established for Procedural or ICU Sedation in pediatric patients. One assessor-blinded trial in pediatric patients and two open label studies in neonates were conducted to assess efficacy for ICU sedation. These studies did not meet their primary efficacy endpoints and the safety data submitted were insufficient to fully characterize the safety profile of dexmedetomidine injection for this patient population.
The use of dexmedetomidine for procedural sedation in pediatric patients has not been evaluated.
8.5Geriatric Use Intensive Care Unit Sedation A total of 729 patients in the clinical studies were 65 years of age and over. A total of 200 patients were 75 years of age and over. In patients greater than 65 years of age, a higher incidence of bradycardia and hypotension was observed following administration of dexmedetomidine injection [see Warnings and Precautions ( 5.2 )].
Therefore, a dose reduction may be considered in patients over 65 years of age [see Dosage and Administration ( 2.2, 2.3 ), Clinical Pharmacology ( 12.3 )]. Procedural Sedation A total of 131 patients in the clinical studies were 65 years of age and over. A total of 47 patients were 75 years of age and over.
Hypotension occurred in a higher incidence in dexmedetomidine injection-treated patients 65 years or older (72%) and 75 years or older (74%) as compared to patients <65 years (47%). A reduced loading dose of 0.5 mcg/kg given over 10 minutes is…
🆘 Overdosage ▾
10 OVERDOSAGE The tolerability of dexmedetomidine injection was studied in one study in which healthy adult subjects were administered doses at and above the recommended dose of 0.2 to 0.7 mcg/kg/hr. The maximum blood concentration achieved in this study was approximately 13 times the upper boundary of the therapeutic range. The most notable effects observed in two subjects who achieved the highest doses were first degree atrioventricular block and second degree heart block.
No hemodynamic compromise was noted with the atrioventricular block and the heart block resolved spontaneously within one minute. Five adult patients received an overdose of dexmedetomidine injection in the intensive care unit sedation studies. Two of these patients had no symptoms reported; one patient received a 2 mcg/kg loading dose over 10 minutes (twice the recommended loading dose) and one patient received a maintenance infusion of 0.8 mcg/kg/hr.
Two other patients who received a 2 mcg/kg loading dose over 10 minutes, experienced bradycardia and/or hypotension. One patient who received a loading bolus dose of undiluted dexmedetomidine injection (19.4 mcg/kg), had cardiac arrest from which he was successfully resuscitated.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Dexmedetomidine injection is a relatively selective alpha2-adrenergic agonist with sedative properties. Alpha2 selectivity is observed in animals following slow intravenous infusion of low and medium doses (10-300 mcg/kg). Both alpha1 and alpha2 activity is observed following slow intravenous infusion of high doses (≥1000 mcg/kg) or with rapid intravenous administration.
12.2Pharmacodynamics In a study in healthy volunteers (N = 10), respiratory rate and oxygen saturation remained within normal limits and there was no evidence of respiratory depression when dexmedetomidine injection was administered by intravenous infusion at doses within the recommended dose range (0.2–0.7 mcg/kg/hr).
12.3Pharmacokinetics Following intravenous administration, dexmedetomidine exhibits the following pharmacokinetic parameters: a rapid distribution phase with a distribution half-life (t 1/2 ) of approximately 6 minutes; a terminal elimination half-life (t 1/2 ) of approximately 2 hours; and steady-state volume of distribution (V ss ) of approximately 118 liters. Clearance is estimated to be approximately 39 L/h. The mean body weight associated with this clearance estimate was 72 kg.
Dexmedetomidine exhibits linear pharmacokinetics in the dosage range of 0.2 to 0.7 mcg/kg/hr when administered by intravenous infusion for up to 24 hours. Table 8 shows the main pharmacokinetic parameters when dexmedetomidine injection was infused (after appropriate loading doses) at maintenance infusion rates of 0.17 mcg/kg/hr (target plasma concentration of 0.3 ng/mL) for 12 and 24 hours, 0.33 mcg/kg/hr (target plasma concentration of 0.6 ng/mL) for 24 hours, and 0.70 mcg/kg/hr (target plasma concentration of 1.25 ng/mL) for 24 hours.
Table 8: Mean ± SD Pharmacokinetic Parameters Parameter Loading Infusion (min)/Total Infusion Duration (hrs) 10 min/12 hrs 10 min/24 hrs 10 min/24 hrs 35 min/24 hrs Dexmedetomidine Target Plasma Concentration (ng/mL) and Dose (mcg/kg/hr) 0.3/0.17 0.3/0.17 0.6/0.33 1.25/0.70 t1/2*, hour 1.78 ± 0.30 2.22 ± 0.59 2.23 ± 0.21 2.50 ±
0.61CL, liter/hour 46.3 ± 8.3 43.1 ± 6.5 35.3 ± 6.8 36.5 ±
7.5Vss, liter 88.7 ± 22.9 102.4 ± 20.3 93.6 ± 17.0 99.6 ±
17.8Avg Css # , ng/mL 0.27 ± 0.05 0.27 ± 0.05 0.67 ± 0.10 1.37 ±
0.20Abbreviations: t 1/2 = half-life, CL = clearance, Vss = steady-state volume of distribution * Presented as harmonic mean and pseudo standard deviation. # Mean C ss = Average steady-state concentration of dexmedetomidine. The mean C ss was calculated based on post-dose sampling from 2.5 to 9 hours samples for 12 hours infusion and post-dose sampling from 2.5 to 18 hours for 24 hour infusions. The loading doses for each of the above indicated groups were 0.5, 0.5, 1 and 2.2 mcg/kg, respectively.
Dexmedetomidine pharmacokinetic parameters after dexmedetomidine injection maintenance doses of 0.2 to 1.4 mcg/kg/hr for >24 hours were similar to the pharmacokinetic (PK) parameters after dexmedetomidine injection maintenance dosing for <24 hours in other studies. The values for clearance (CL), volume of distribution (V), and t 1/2 were
39.4L/hr, 152 L, and 2.67 hours, respectively. Distribution The steady-state volume of distribution (V ss ) of dexmedetomidine was approximately 118 liters. Dexmedetomidine protein binding was assessed in the plasma of normal healthy male and female subjects.
The average protein binding was 94% and was constant across the different plasma concentrations tested. Protein binding was similar in males and females. The fraction of dexmedetomidine that was bound to plasma proteins was significantly decreased in subjects with hepatic impairment compared to healthy subjects.
The potential for protein binding displacement of dexmedetomidine by fentanyl, ketorolac, theophylline, digoxin and lidocaine was explored in vitro , and negligible changes in the plasma protein binding of dexmedetomidine were observed. The potential for protein binding displacement of p…
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Dexmedetomidine Injection, USP Dexmedetomidine injection, USP (dexmedetomidine hydrochloride) 200 mcg/2 mL (100 mcg/mL) is clear and colorless, and available in 2 mL clear glass vials with pink caps, supplied in packages of 25. The strength is based on the dexmedetomidine base. Vials are intended for single-dose only.
Discard unused portion. NDC No. Container Size 66794-230-02 Vial 2 mL Store at controlled room temperature, 25°C (77°F) with excursions allowed from 15°C to 30°C (59°F to 86°F). [See USP Controlled Room Temperature.]
📋 Description ▾
11 DESCRIPTION Dexmedetomidine injection, USP (dexmedetomidine hydrochloride) is a sterile, nonpyrogenic solution suitable for intravenous infusion following dilution. Dexmedetomidine hydrochloride, USP is the S-enantiomer of medetomidine and is chemically described as (+)-4-(S)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole monohydrochloride. Dexmedetomidine hydrochloride, USP has a molecular weight of 236.7 and the empirical formula is C 13 H 16 N 2 • HCl and the structural formula is: Dexmedetomidine hydrochloride, USP is a solid, white or almost white powder that is freely soluble in water and alcohols, slightly soluble in methylene chloride and acetone and has a pKa of 7.1.
Its partition coefficient in-octanol: water at pH 7.4 is 2.89. Dexmedetomidine injection, USP is supplied as a clear, colorless, isotonic solution with a pH of 4.5 to 7.0. Each mL contains 118 mcg of dexmedetomidine hydrochloride, USP equivalent to 100 mcg (0.1 mg) of dexmedetomidine and 9 mg of sodium chloride in water and is to be used after dilution.
The solution is preservative-free and contains no additives or chemical stabilizers. structure