In adrenocortical cell suspensions, medetomidine (0–1 µM, 1 hour) suppresses the release of aldosterone [7]. Cyprids' kicking reaction is activated by 10 nM metetomidine [8]. By stimulating beta-like receptors in CHO cells, metetomidine (1 µM) raises the amount of cAMP produced by the cells [8].

Cats may get drowsy when given metetomidine (200 μg/kg orally or intramuscularly) [4]. Dogs respond sedatively and analgesically to intravenous medetomidine (20 µg/kg) [5]. In mice, diazinon-induced poisoning can be avoided using metetomidine (0.05–0.3 mg/kg, subcutaneous injection) [6].

Animal/Disease Models: Diazinon (75 mg/kg, oral) induced poisoning in mice [6] Doses: 0.05, 0.1 and 0.3 mg/kg
Route of Administration: subcutaneous injection, 15 minutes before diazinon.
Experimental Results: Mice were protected from diazinon-induced toxicity. Reduces the occurrence of strew tail, hypersalivation and tremors. The latency to onset of tremor and death was increased compared with controls.

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Animal/Disease Models: dog [5]
Doses: 20 µg/kg
Route of Administration: intravenous (iv) (iv)injection
Experimental Results:It has sedative and analgesic effects. SAP, MAP, DAP, MPAP, PCWP, CVP, SVR, PVR, increased core body temperature. HR, CO, CI, SV, SI, RR, pH diminished.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Limited data suggest that very small amounts of dexmedetomidine are excreted into breast milk within 4 to 6 hours after intravenous infusion. The drug is no longer present in breast milk within 24 hours after infusion. Sublingual administration is expected to result in lower levels of the drug in breast milk compared to intravenous infusion. Due to the low dose in breast milk and poor oral bioavailability, dexmedetomidine is not expected to have adverse effects on breastfed infants or newborns. Breastfed infants should be monitored for irritability during sublingual administration.
◉ Effects on Breastfed Infants
No published information found as of the revision date.
◉ Effects on Lactation and Breast Milk
A double-blind study randomized 160 women undergoing elective cesarean section with spinal anesthesia to two groups: one group received patient-controlled intravenous analgesia (standard treatment) with sufentanil, and the other group received dexmedetomidine in addition to standard treatment. The initial dose of dexmedetomidine was 5 mcg/kg, followed by a continuous infusion of 0.5 mcg/kg/hour until the end of the surgery. The latter group of patients received patient-controlled intravenous analgesia (PCA) with dexmedetomidine and sufentanil for 2 days postoperatively. Patients treated with dexmedetomidine had shorter time to first lactation (28 hours vs. 34 hours), faster achievement of exclusive breastfeeding (8 days vs. 11 days), and greater milk production on the second postpartum day. A retrospective study compared three medication regimens in women undergoing cesarean section: dexmedetomidine before anesthesia and during delivery (n = 115), saline before anesthesia and during delivery, and dexmedetomidine postpartum (n = 109), and saline before anesthesia and during delivery (n = 168). The results showed that women who used dexmedetomidine before anesthesia and during delivery had lower doses of sufentanil and ondansetron during hospitalization and a slightly shorter time to first lactation than other groups (25 minutes vs. 27 to 28 minutes).

[1]. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Acute effects of medetomidine, a selective alpha 2-adrenoceptor agonist, on anterior pituitary hormone and cortisol secretion in man. Acta Endocrinol (Copenh). 1988 Sep;119(1):11-5.

[3]. Characterization of the selectivity, specificity and potency of medetomidine as an a2-adrenoceptor agonist.

[4]. Comparing oral and intramuscular administration of medetomidine in cats.

[5]. Comparative cardiovascular, analgesic, and sedative effects of medetomidine, medetomidine-hydromorphone, and medetomidine-butorphanol in dogs. Am J Vet Res. 2004 Jul;65(7):931-7.

[6]. Medetomidine protection against diazinon-induced toxicosis in mice. Toxicol Lett. 1997 Sep 19;93(1):1-8.

[7]. Effects of atipamezole, detomidine and medetomidine on release of steroid hormones by porcine adrenocortical cells in vitro. Eur J Pharmacol. 1998 Apr 3;346(1):71-6.

[8]. Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine.

Medetomidine belongs to the imidazole class of compounds. Medetomidine is a synthetic compound used as a surgical anesthetic and analgesic. It is usually found in its hydrochloride form, i.e., medetomidine hydrochloride. Medetomidine is an intravenously administered α2-adrenergic receptor agonist. This drug was developed by Orion Pharma. In the United States, it is currently approved for canine veterinary use and is distributed by Pfizer Animal Health. In Canada, medetomidine is distributed by Novartis Animal Health. The commercially available product is a racemic mixture of two stereoisomers, with dexmedetomidine being the predominant active isomer. It is an α2-adrenergic receptor agonist used in veterinary medicine for its analgesic and sedative effects. It is the racemic form of dexmedetomidine. See also: Medetomidine hydrochloride (salt form).

C13H16N2

200.2795

200.131

86347-14-0

Dexmedetomidine;113775-47-6;Dexmedetomidine hydrochloride;145108-58-3;Medetomidine hydrochloride;86347-15-1

68602

White to off-white solid powder

1.1±0.1 g/cm3

381.9±11.0 °C at 760 mmHg

151.5 - 152.5ºC

191.3±5.7 °C

0.0±0.8 mmHg at 25°C

1.570

3.1

1

1

2

15

205

0

CUHVIMMYOGQXCV-UHFFFAOYSA-N

InChI=1S/C13H16N2/c1-9-5-4-6-12(10(9)2)11(3)13-7-14-8-15-13/h4-8,11H,1-3H3,(H,14,15)

5-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~250 mg/mL (~1248.25 mM)
H2O : < 0.1 mg/mL

Solubility in Formulation 1: ≥ 2.5 mg/mL (12.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (12.48 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (12.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)