Dexmedetomidine hydrochloride 100 ug/mL Injection, Solution
Other active recalls for Dexmedetomidine Hydrochloride (different manufacturers) — 1 · tap to view
🆔 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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🧪 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/mLthis 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/2mL 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 | — |
| Dexmedetomidine Hydrochloride 100 ug/mL 70069-0759-04 | Somerset | 4 vials | — | AP | FDA listed | — |
| Dexmedetomidine Hydrochloride 100 ug/mL 70069-0758-04 | Somerset | 4 vials | — | 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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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 71872-7030-01 You're viewing this | 1 VIAL in 1 BAG (71872-7030-1) / 2 mL in 1 VIAL | 2020-02-28 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| 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. |
Questions about this listing
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Dexmedetomidine hydrochloride injection is a relatively selective alpha 2 -adrenergic agonist indicated for: Sedation of non-intubated patients prior to and/or during surgical and other procedures. ( 1.2 )
1.2Procedural Sedation Dexmedetomidine hydrochloride injection is indicated for sedation of non-intubated patients prior to and/or during surgical and other procedures.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Individualize and titrate dexmedetomidine hydrochloride injection dosing to desired clinical effect. ( 2.1 ) Administer dexmedetomidine hydrochloride injection using a controlled infusion device. ( 2.1 ) Dilute the 200 mcg/2 mL (100 mcg/mL) vial contents in 0.9% sodium chloride solution to achieve required concentration (4 mcg/mL) prior to administration.
( 2.4 ) For Adult Procedural Sedation: Generally initiate at one mcg/kg over 10 minutes, followed by a maintenance infusion 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 .( 2.2 ) Alternative Doses :Recommended for patients over 65 years of age and awake fiberoptic intubation patients. ( 2.2 )
2.1Dosing Guidelines Dexmedetomidine hydrochloride injection dosing should be individualized and titrated to desired clinical response. Dexmedetomidine hydrochloride injection is not indicated for infusions lasting longer than 24 hours. Dexmedetomidine hydrochloride injection should be administered using a controlled infusion device.
2.2Dosage Information Table 1: Dosage Information INDICATION DOSAGE AND ADMINISTRATION 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 hydrochloride 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 hydrochloride injection. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Dexmedetomidine hydrochloride injection, 200 mcg/2 mL (100 mcg/mL) Dexmedetomidine hydrochloride 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 hydrochloride injection and add to 48 mL of 0.9% sodium chloride injection to a total of 50 mL. Shake gently to mix well.
2.5Administration with Other Fluids Dexmedetomidine hydrochloride infusion should not be co-administered through the same intravenous catheter with blood or…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Dexmedetomidine hydrochloride injection Dexmedetomidine hydrochloride injection, 200 mcg/2 mL (100 mcg/mL) in a glass vial. To be used after dilution. Dexmedetomidine hydrochloride injection, 200 mcg/2 mL (100 mcg/mL) in a glass vial. To be used after dilution.
⛔ Contraindications ▾
4 CONTRAINDICATIONS None None. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Monitoring: Continuously monitor patients while receiving dexmedetomidine hydrochloride injection. ( 5.1 ) Bradycardia and sinus arrest: Have occurred in young healthy volunteers with high vagal tone or with different routes of administration, e.g., rapid intravenous or bolus administration. ( 5.2 ) Hypotension and Bradycardia: May necessitate medical intervention.
May be more pronounced in patients with hypovolemia, diabetes mellitus, or chronic hypertension, and in the elderly. Use with caution in patients with advanced heart block or severe ventricular dysfunction. ( 5.2 ) Co-administration with Other Vasodilators or Negative Chronotropic Agents: Use with caution due to additive pharmacodynamic effects.
( 5.2 ) Transient Hypertension: Observed primarily during the loading dose. Consider reduction in loading infusion rate. ( 5.3 ) Arousability: Patients can become aroused/alert with stimulation; this alone should not be considered as lack of efficacy.
( 5.4 ) Prolonged exposure to dexmedetomidine beyond 24 hours may be associated with tolerance and tachyphylaxis and a dose-related increase in adverse events. ( 5.6 )
5.1Drug Administration Dexmedetomidine hydrochloride injection should be administered only by persons skilled in the management of patients in the operating room setting. Due to the known pharmacological effects of dexmedetomidine hydrochloride injection, patients should be continuously monitored while receiving dexmedetomidine hydrochloride injection.
5.2Hypotension, Bradycardia, and Sinus Arrest Clinically significant episodes of bradycardia and sinus arrest have been reported with dexmedetomidine hydrochloride 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 hydrochloride infusion. Some of these cases have resulted in fatalities.
If medical intervention is required, treatment may include decreasing or stopping the infusion of dexmedetomidine hydrochloride injection, increasing the rate of intravenous fluid administration, elevation of the lower extremities, and use of pressor agents. Because dexmedetomidine hydrochloride 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 injection-induced bradycardia. However, in some patients with significant cardiovascular dysfunction, more advanced resuscitative measures were required. Caution should be exercised when administering dexmedetomidine hydrochloride injection to patients with advanced heart block and/or severe ventricular dysfunction.
Because dexmedetomidine hydrochloride 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 hydrochloride injection an additive pharmacodynamic effect was not observed. Nonetheless, caution should be used when such agents are administered concomitantly with dexmedetomidine hydrochloride injection.
5.3Transient Hypertension Transient hypertension has been observed primarily during the loading dose in association with the initial peripheral vasoconstrictive effects of dexmedetomidine hydrochloride injection. Treatment of the transient hypertension has generally not been necessary, although reduction of the loading infusion rate may be desirable.
5.4 Arousability Some patients receiving dexme…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The most common adverse reactions (incidence greater than 2%) are hypotension, bradycardia, and dry mouth. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Accord Healthcare Inc. at 1-866-941-7875 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical Studies 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 clinical trials of another drug and may not reflect the rates observed in practice. Use of dexmedetomidine hydrochloride injection has been associated with the following serious adverse reactions: Hypotension, bradycardia and sinus arrest [ see Warnings and Precautions (5.2) ] Transient hypertension [ see Warnings and Precautions (5.3) ] Most common treatment-emergent adverse reactions, occurring in greater than 2% of patients in procedural sedation studies include hypotension, bradycardia and dry mouth. *Average maintenance dose over the entire study drug administration Procedural Sedation Adverse reaction information is derived from the two trials for procedural sedation [see Clinical Studies (14.2)] in which 318 adult patients received dexmedetomidine.
The mean total dose was 1.6 mcg/kg (range: 0.5 to 6.7), mean dose per hour was 1.3 mcg/kg/hr (range: 0.3 to 6.1) and the mean duration of infusion of 1.5 hours (range: 0.1 to 6.2). The population was between 18 to 93 years of age, ASA I-IV, 30% ≥ 65 years of age, 52% male and 61% Caucasian. Treatment-emergent adverse reactions occurring at an incidence of >2% are provided in Table 6 .
The most frequent adverse reactions were hypotension, bradycardia, and dry mouth [ see Warnings and Precautions (5.2) ]. Pre- specified criteria for the vital signs to be reported as adverse reactions are footnoted below the table. The decrease in respiratory rate and hypoxia was similar between dexmedetomidine and comparator groups in both studies.
Table 6: Adverse Reactions With an Incidence > 2%—Procedural Sedation Population Adverse Event Dexmedetomidine (N = 318) (%) Placebo (N = 113) (%) Hypotension Hypotension was defined in absolute and relative terms as Systolic blood pressure of < 80 mmHg or ≤ 30% lower than pre-study drug infusion value, or Diastolic blood pressure of < 50 mmHg. 54% 30% Respiratory Depression Respiratory depression was defined in absolute and relative terms as respiratory rate (RR) < 8 beats per minute or > 25% decrease from baseline.
37% 32% Bradycardia Bradycardia was defined in absolute and relative terms as < 40 beats per minute or ≤ 30% lower than pre-study drug infusion value. 14% 4% Hypertension Hypertension was defined in absolute and relative terms as Systolic blood pressure > 180 mmHg or ≥ 30% higher than pre-study drug infusion value or Diastolic blood pressure of > 100 mmHg. 13% 24% Tachycardia Tachycardia was defined in absolute and relative terms as > 120 beats per minute or ≥ 30% greater than pre-study drug infusion value.
5% 17% Nausea 3% 2% Dry Mouth 3% 1% Hypoxia Hypoxia was defined in absolute and relative terms as SpO 2 < 90% or 10% decrease from baseline. 2% 3% Bradypnea 2% 4%
6.2Postmarketing Experience The following adverse reactions have been identified during post approval use of dexmedetomidine. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Hypotension and bradycardia were the most common adverse reactions associated with the use of dexmedetomidine during post approval use of the drug.
Table 7: Adverse Reactions Experienced During Post-approval Use of Dexmedetomidine System Organ Class Preferred Term Blood and Lymphatic System Disorders Anemia Cardiac Disorders Arrhythmia, atrial fibrillation, atrioventricular block, bradycardia, cardiac arrest, cardiac disorder, extrasystoles, myocardial infarction, supraventricular…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Anesthetics, Sedatives, Hypnotics, Opioids: Enhancement of pharmacodynamic effects. Reduction in dosage of dexmedetomidine hydrochloride injection or the concomitant medication may be required. (7.1)
7.1Anesthetics, Sedatives, Hypnotics, Opioids Co-administration of dexmedetomidine 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 and isoflurane, propofol, alfentanil and midazolam have been demonstrated.
However, due to possible pharmacodynamic interactions, when co-administered with dexmedetomidine, a reduction in dosage of dexmedetomidine 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 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.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Geriatric Patients: Dose reduction should be considered (2.2 , 2.3 , 5.1 , 8.5 ) Hepatic Impairment: Dose reduction should be considered (2.1 , 2.2 , 2.3 , 5.7 , 8.6 ) Pregnancy: Based on animal data, may cause fetal harm (8.1) Nursing Mothers: Caution should be exercised when administered to a nursing woman (8.3)
8.1Pregnancy Pregnancy Category C There are no adequate and well-controlled studies of dexmedetomidine 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 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 during labor and delivery has not been studied.
8.3Nursing Mothers It is not known whether dexmedetomidine 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 is administered to a nursing woman.
8.4Pediatric Use Safety and efficacy have not been established for Procedural Sedation in pediatric patients. The use of dexmedetomidine for procedural sedation in pediatric patients has not been evaluated.
8.5Geriatric Use 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 -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 recommended and a reduction in the maintenance infusion should be considered for patients greater than 65 years of age.
8.6Hepatic Impairment Since dexmedetomidine clearance decreases with increasing severity of hepatic impairment, dose reduction should be considered in patients with impaired hepatic function [ see Dosage and Administration (2.2) and Clinical Pharmacology (12.3) ].
🤰 Pregnancy ▾
8.1Pregnancy Pregnancy Category C There are no adequate and well-controlled studies of dexmedetomidine 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 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.
🧒 Pediatric Use ▾
8.4Pediatric Use Safety and efficacy have not been established for Procedural Sedation in pediatric patients. The use of dexmedetomidine for procedural sedation in pediatric patients has not been evaluated.
🧓 Geriatric Use ▾
8.5Geriatric Use 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 -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 recommended and a reduction in the maintenance infusion should be considered for patients greater than 65 years of age.
🆘 Overdosage ▾
10 OVERDOSAGE The tolerability of dexmedetomidine hydrochloride 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. One patient who received a loading bolus dose of undiluted dexmedetomidine (19.4 mcg/kg), had cardiac arrest from which he was successfully resuscitated.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Dexmedetomidine is a relatively selective alpha 2 -adrenergic agonist with sedative properties. Alpha 2 selectivity is observed in animals following slow intravenous infusion of low and medium doses (10 to 300 mcg/kg). Both alpha 1 and alpha 2 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 hydrochloride injection was administered by intravenous infusion at doses within the recommended dose range (0.2 to 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 hydrochloride 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 t 1/2 Presented as harmonic mean and pseudo standard deviation. , 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 ±
7.5V ss , liter 88.7 ± 22.9 102.4 ± 20.3 93.6 ± 17.0 99.6 ±
17.8Avg Css 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 hour 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. , ng/mL 0.27 ± 0.05 0.27 ± 0.05 0.67 ± 0.10 1.37 ±
0.20Dexmedetomidine pharmacokinetic parameters after dexmedetomidine hydrochloride injection maintenance doses of 0.2 to 1.4 mcg/kg/hr for >24 hours were similar to the PK parameters after dexmedetomidine hydrochloride 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 phenytoin, warfarin, ibuprofen, propranolol, theophylline an…
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Dexmedetomidine hydrochloride injection, 200 mcg/2 mL (100 mcg/mL) is available in 2 mL clear glass Vials. The strength is based on the dexmedetomidine base. Vials are intended for single dose only.
NDC No. Container Size 16729-239-30 Vial 2 mL Single Dose Vial 16729-239-93 Vial 25 Units of 2 mL Single Dose Vial in a Carton Store at controlled room temperature, 25°C (77°F) with excursions allowed from 15 to 30°C (59 to 86°F). [See USP.]
📋 Description ▾
11 DESCRIPTION Dexmedetomidine hydrochloride injection is a sterile, nonpyrogenic solution suitable for intravenous infusion following dilution. Dexmedetomidine hydrochloride is the S-enantiomer of medetomidine and is chemically described as (+)-4-(S)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole monohydrochloride. Dexmedetomidine hydrochloride 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 is a white or almost white powder that is freely soluble in water and has a pKa of 7.1. Its partition coefficient in-octanol: water at pH 7.4 is 2.89. Dexmedetomidine hydrochloride injection 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 equivalent to 100 mcg (0.1mg) 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. structural formula
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Dexmedetomidine hydrochloride injection is indicated for short-term intravenous sedation. Dosage must be individualized and titrated to the desired clinical effect. Blood pressure, heart rate and oxygen levels will be monitored both continuously during the infusion of dexmedetomidine hydrochloride injection and as clinically appropriate after discontinuation.
When dexmedetomidine hydrochloride injection is infused for more than 6 hours, patients should be informed to report nervousness, agitation, and headaches that may occur for up to 48 hours. Additionally, patients should be informed to report symptoms that may occur within 48 hours after the administration of dexmedetomidine hydrochloride injection such as: weakness, confusion, excessive sweating, weight loss, abdominal pain, salt cravings, diarrhea, constipation, dizziness or light-headedness. Manufactured For: Accord Healthcare, Inc., 1009, Slater Road, Suite 210-B, Durham, NC 27703, USA.
Manufactured By: Intas Pharmaceuticals Limited, Plot No. : 457, 458, Village – Matoda, Bavla Road, Ta.- Sanand, Dist.- Ahmedabad – 382 210, INDIA. 10 1651 0 672869 Issued December, 2016