Detomidine

For use as a sedative and analgesic to facilitate minor surgical and diagnostic procedures in mature horses and yearlings.

Detomequin™

For sedation and restraint in horses.

Federal law restricts this drug to use by or on the order of a licensed veterinarian. For sublingual use in horses only. Do not use in horses intended for human consumption.

Dormosedan Gel®

INDICATIONS: DetomequinTM is indicated for use as a sedative and analgesic to facilitate minor surgical and diagnostic procedures in mature horses and yearlings. It has been used successfully for the following: to calm fractious horses, to provide relief from abdominal pain, to facilitate bronchoscopy, bronchoalveolar lavage, nasogastric intubation, nonreproductive rectal palpations, suturing of skin lacerations, and castrations. Additionally, an approved, local infiltration anesthetic is indicated for castration.

DetomequinTM (detomidine hydrochloride)

Domidine™ is indicated for use as a sedative and analgesic to facilitate minor surgical and diagnostic procedures in mature horses and yearlings.

Domidine™

DORMOSEDAN GEL is indicated for sedation and restraint in horses.

DORMOSEDAN® GEL

Detomidine is a potent non-narcotic alpha2-adrenoceptor agonist which produces sedation with a central effect inhibiting the transmission of noradrenalin-mediated nervous impulses. Blood pressure is initially increased due to peripheral vasoconstriction, subsequently dropping to normal or slightly below normal levels. Vasoconstriction may cause mucous membranes to appear pale or mildly cyanotic. This initial vasopressor response is accompanied by a compensatory marked decrease in heart rate mediated by a vagal baroreceptor. The peripheral pulse may feel weak and a transient change in the conductivity of the cardiac muscle may occur, as evidenced by first and second degree atrioventricular blocks. Other arrhythmias may occur. Detomidine also decreases the respiratory rate and decreases body temperature. Detomidine causes depression of gastrointestinal motility due to decrease in smooth muscle activity, increases blood glucose levels due to inhibition of insulin release, and increases production of urine 2 to 4 hours after treatment. In some horses, sweating, salivation and slight muscle tremors may be seen. Partial, transient penis prolapse may occur in stallions and geldings. Because of continued lowering of the head during sedation, mucus discharges from the nose with occasional swelling of the head, particularly around the eyes, may be seen. Detomidine is oxidized mainly in the liver. Most metabolites are excreted in the urine. Halflife (T½) is 1-2 hours. Detomidine is rapidly distributed; volume of distribution (Vd) varies between 0.69 L/kg and 1.89 L/kg. Protein binding is about 85%. Detomidine is a high extraction ratio drug. Alterations in liver blood flow (the site of detomidine metabolism) can change the rate of drug clearance and, consequently, drug exposure. The sedative effects of detomidine (using head droop as a marker for sedation) are highly correlated to blood concentration, regardless of the route of administration. First pass effect results in a very small portion of drug reaching the systemic circulation if it is swallowed. Sedation achieved with the DORMOSEDAN GEL is attributable to sublingual drug absorption. Peak concentrations occur approximately 1.83 hours after sublingual administration of DORMOSEDAN GEL. The peak concentrations observed after administration of DORMOSEDAN GEL are approximately 40% of those observed after intramuscular injection of detomidine solution. The absolute bioavailability of detomidine in DORMOSEDAN GEL is 22%.

DORMOSEDAN® GEL

CLINICAL PHARMACOLOGY: DetomiSed™, a non-narcotic sedative and analgesic, is a potent α2-adrenoreceptor agonist which produces sedation and superficial and visceral analgesia which is dose dependent in its depth and duration. Profound lethargy and a characteristic lowering of the head with reduced sensitivity to environmental stimuli (sounds, etc.) are seen with detomidine. A short period of incoordination is characteristically followed by immobility and a firm stance with front legs well spread. The analgesic effect is most readily seen as an increase in the pain threshold at the body surface. Sensitivity to touch is little affected and in some cases may actually be enhanced. With detomidine administration, heart rate is markedly decreased, blood pressure is initially elevated, and then a steady decline to normal is seen. A transient change in the conductivity of the cardiac muscle may occur, as evidenced by partial atrioventricular (AV) and sinoauricular (SA) blocks. This change in the conductivity of the cardiac muscle may be prevented by IV administration of atropine at 0.02 mg/kg of body weight. No effect on blood clotting time or other hematological parameters was encountered at dosages of 20 or 40 mcg/kg of body weight. Respiratory responses include an initial slowing of respiration within a few seconds to 1 to 2 minutes after administration, increasing to normal within 5 minutes. An initial decrease in tidal volume is followed by an increase.

DetomiSedTM (detomidine hydrochloride)

CONTRAINDICATIONS: DetomequinTM should not be used in horses with pre-existing AV or SA block, with severe coronary insufficiency, cerebrovascular disease, respiratory disease, or chronic renal failure. Intravenous potentiated sulfonamides should not be used in anesthetized or sedated horses as potentially fatal dysrhythmias may occur. Information on the possible effects of detomidine hydrochloride in breeding horses is limited to uncontrolled clinical reports; therefore, this drug is not recommended for use in breeding animals.

DetomequinTM (detomidine hydrochloride)

DORMOSEDAN GEL is contraindicated in horses with known hypersensitivity to detomidine. Intravenous potentiated sulfonamides should not be used in anesthetized or sedated horses as potentially fatal dysrhythmias may occur. Do not use DORMOSEDAN GEL in horses with pre-existing atrioventricular (AV) or sino-atrial (SA) blocks, respiratory disease, or chronic renal failure.

DORMOSEDAN® GEL

HUMAN SAFETY INFORMATION: Care should be taken to assure that detomidine hydrochloride is not inadvertently ingested as safety studies have indicated that the drug is well absorbed when administered orally. Standard ocular irritation tests in rabbits using the proposed market formulation have shown detomidine hydrochloride to be nonirritating to eyes. Primary dermal irritation tests in guinea pigs using up to 5 times the proposed market concentration of detomidine hydrochloride on intact and abraded skin have demonstrated that the drug is nonirritating to skin and is apparently poorly absorbed dermally. However, in accordance with prudent clinical procedures, exposure of eyes or skin should be avoided and affected areas should be washed immediately if exposure does occur. As with all injectable drugs causing profound physiological effects, routine precautions should be employed by practitioners when handling and using loaded syringes to prevent accidental self-injection.

DetomequinTM (detomidine hydrochloride)

►WARNINGS: Do not use in horses intended for human consumption. Not for human use. Keep out of reach of children.◄

DetomiSedTM (detomidine hydrochloride)

For sublingual use in horses only. Do not use in horses intended for human consumption.

DORMOSEDAN® GEL

ADVERSE REACTIONS: Occasional reports of anaphylactic-like reactions have been received, including 1 or more of the following: urticaria, skin plaques, dyspnea, edema of the upper airways, trembling, recumbency, and death. The use of epinephrine should be avoided since epinephrine may potentiate the effects of α2-agonists. Reports of mild adverse reactions have resolved uneventfully without treatment. Severe adverse reactions should be treated symptomatically. As with all α2-agonists, the potential for isolated cases of hypersensitivity exist, including paradoxical response (excitation).

DetomequinTM (detomidine hydrochloride)

For Sedation: Administer Detomidine Hydrochloride intravenously (IV) or intramuscularly (IM) at the rates of 20 or 40 mcg detomidine hydrochloride per kg of body weight (0.2 or 0.4 mL per 100 kg or 220 pounds), depending on the depth and duration of sedation required. Onset of sedative effects should be reached within 2–4 minutes after IV administration and 3–5 minutes after IM administration. Twenty mcg/kg will provide 30–90 minutes of sedation and 40 mcg/kg will provide approximately 90 minutes to 2 hours of sedation. For Analgesia: Administer Detomidine Hydrochloride IV at the rates of 20 or 40 mcg detomidine hydrochloride per kg of body weight (0.2 or 0.4 mL per 100 kg or 220 pounds), depending on the depth and duration of analgesia required. Twenty mcg/kg will usually begin to take effect in 2–4 minutes and provide 30–45 minutes of analgesia. The 40 mcg/kg dose will also begin to take effect in 2–4 minutes and provide 45–75 minutes of analgesia. For Both Sedation and Analgesia: Administer Detomidine Hydrochloride IV at the rates of 20 or 40 mcg detomidine hydrochloride per kg of body weight (0.2 or 0.4 mL per 100 kg or 220 pounds), depending on the depth and duration of sedation and analgesia required.

Intravenous, Intramuscular

Detomequin™

For Sedation: Administer IV or IM at the rates of 20 or 40 mcg detomidine hydrochloride per kg of body weight (0.2 or 0.4 mL per 100 kg or 220 lb), depending on the depth and duration of sedation required. Onset of sedative effects should be reached within 2 to 4 minutes after IV administration and 3 to 5 minutes after IM administration. Twenty mcg/kg will provide 30 to 90 minutes of sedation and 40 mcg/kg will provide approximately 90 minutes to 2 hours of sedation. For Analgesia: Administer IV at the rates of 20 or 40 mcg detomidine hydrochloride per kg of body weight (0.2 or 0.4 mL per 100 kg or 220 lb), depending on the depth and duration of analgesia required. Twenty mcg/kg will usually begin to take effect in 2 to 4 minutes and provide 30 to 45 minutes of analgesia. The 40 mcg/kg dose will also begin to take effect in 2 to 4 minutes and provide 45 to 75 minutes of analgesia. For Both Sedation and Analgesia: Administer IV at the rates of 20 or 40 mcg detomidine hydrochloride per kg of body weight (0.2 or 0.4 mL per 100 kg or 220 lb), depending on the depth and duration of sedation and analgesia required. Before and after injection, the animal should be allowed to rest quietly.

Intramuscular, Intravenous

DetomiSed™

For sedation intravenously or intramuscularly, analgesia intravenously, or sedation and analgesia intravenously: 20 or 40 micrograms per kilogram (0.2 or 0.4 milliliter per 100 kilogram or 220 pounds) by body weight, depending on depth and duration required.

Intravenous, Intramuscular

Do not use in horses with pre-existing atrioventricular or sinoauricular block, with severe coronary insufficiency, cerebrovascular disease, respiratory disease, or chronic renal failure. Do not use in breeding animals. Not for use in horses intended for food. Federal law restricts this drug to use by or on the order of a licensed veterinarian.

Dormosedan™

Administered sublingually at 0.018 mg/lb (0.040 mg/kg).

Oral

Federal law restricts this drug to use by or on the order of a licensed veterinarian. For sublingual use in horses only. Do not use in horses intended for human consumption.

Dormosedan Gel®

DORMOSEDAN GEL produces sedation when administered sublingually at 0.018 mg/lb (0.040 mg/kg). DORMOSEDAN GEL must be placed beneath the tongue of the horse and is not meant to be swallowed. The dosing syringe delivers the product in 0.25 mL increments. The following dosing table may be used to determine the correct dose of DORMOSEDAN GEL (Table 1). Table 1: Sublingual dosing of DORMOSEDAN GEL Approximate body weight (lb) Range of doses (mg/lb) Approximate body weight (kg) Range of doses (mg/kg) Dose volume (mL) 330 - 439 0.023 – 0.017 150 - 199 0.051 – 0.038 1.00 440 - 549 0.022 – 0.017 200 - 249 0.047 – 0-038 1.25 550 – 659 0.021 – 0.017 250 – 299 0.046 – 0.038 1.50 660 - 769 0.020 – 0.017 300 – 349 0.044 – 0.038 1.75 770 - 879 0.019 – 0.017 350 – 399 0.043 – 0.038 2.00 880 - 989 0.019 – 0.017 400 – 449 0.043 – 0.038 2.25 990 - 1099 0.019 – 0.017 450 – 499 0.042 – 0.038 2.50 1100 - 1209 0.019 – 0.017 500 – 549 0.042 – 0.038 2.75 1210 - 1320 0.019 – 0.017 550 - 600 0.041 – 0.038 3.00 Use impermeable gloves when handling the product. Remove the syringe from the outer carton. While holding the plunger, turn the ring-stop on the plunger until the ring is able to slide freely up and down the plunger. Position the ring in such a way that the side nearest the barrel is at the desired volume marking. Turn the ring to secure it in place. Make sure that the horse's mouth contains no feed. Remove the cap from the tip of the syringe and save for cap replacement. Insert the syringe tip into the horse's mouth from the side of the mouth, placing the syringe tip beneath the tongue at the level of the commisure of the mouth. Depress the plunger until the ring-stop contacts the barrel, depositing the product beneath the tongue. The following picture demonstrates correct administration of DORMOSEDAN GEL beneath the tongue. Take the syringe out of the horse's mouth, recap the syringe and return it to the outer carton for disposal. Remove gloves for disposal. For the best results, allow adequate time (a minimum of 40 minutes) between administration of DORMOSEDAN GEL and beginning the procedure. In general, horses show sedative effects lasting approximately 90-180 minutes. Withhold food and water until the sedative effects of the product wear off.

SUBLINGUAL

DORMOSEDAN® GEL

DOSAGE AND ADMINISTRATION: For Sedation: Administer DetomequinTM IV or IM at the rates of 20 or 40 mcg detomidine hydrochloride per kg of body weight (0.2 or 0.4 mL of DetomequinTM per 100 kg or 220 lb), depending on the depth and duration of sedation required. Onset of sedative effects should be reached within 2-4 minutes after IV administration and 3-5 minutes after IM administration. Twenty mcg/kg will provide 30–90 minutes of sedation and 40 mcg/kg will provide approximately 90 minutes to 2 hours of sedation. For Analgesia: Administer DetomequinTM IV at the rates of 20 or 40 mcg detomidine hydrochloride per kg of body weight (0.2 or 0.4 mL of DetomequinTM per 100 kg or 220 lb), depending on the depth and duration of analgesia required. Twenty mcg/kg will usually begin to take effect in 2–4 minutes and provide 30–45 minutes of analgesia. The 40 mcg/kg dose will also begin to take effect in 2–4 minutes and provide 45–75 minutes of analgesia. For Both Sedation and Analgesia: Administer DetomequinTM IV at the rates of 20 or 40 mcg detomidine hydrochloride per kg of body weight (0.2 or 0.4 mL of DetomequinTM per 100 kg or 220 lb), depending on the depth and duration of sedation and analgesia required. Before and after injection, the animal should be allowed to rest quietly.

INTRAMUSCULAR, INTRAVENOUS

DetomequinTM (detomidine hydrochloride)

For sedation, analgesia, or sedation and analgesia: 20 or 40 micrograms per kilogram (0.2 or 0.4 milliliter per 100 kilogram or 220 pounds) by body weight, depending on depth and duration required. For sedation, administer by intraveneous (IV) or intramuscular (IM) injection; for analgesia, administer by IV injection; for both sedation and analgesia, administer by IV injection.

Intramuscular, Intravenous

Domidine™