Buscopan Injectable Solution 20mg/ml - 50 ml

Buscopan is an antispasmodic (spasmolytic) and anticholinergic drug. It is meant for the control of abdominal pain (colic) associated with spasmodic colic, flatulent colic, and simple impactions in horses. Buscopan Injectable Solution requires a prescription from your veterinarian and is for intravenous use only.

Key Benefits

• Equine antispasmodic drug
• Easy to administer injectable
• Controls abdominal pain (colic)
• Suppresses spasms of the digestive system

How It Works

Buscopan Injectable Solution is an antispasmodic and anticholinergic drug that suppresses spasms of the digestive system.

Indications

Buscopan is indicated for the controlof abdominal pain (colic) associated with spas-modic colic, flatulent colic, and simple impactionsin horses.

View Buscopan Drug Facts Sheet.

Administer a singleinjection of 0.3 mg/kg body weight (0.14 mg/lb),slowly IV. This is equivalent to 30 mgN-butylscopolammonium bromide per 100 kg (220pounds) body weight or 1.5 mL of Buscopan Injectable Solution per 100 kg (220 pounds) bodyweight.

Caution:

Federal law restricts this drug to use by oron the order of a licensed veterinarian.

Contraindications:

Buscopan should not be usedin impaction colics associated with ileus, or inhorses with glaucoma.

Warnings:

Not for horses intended for human consumption. Not for use in humans.Keep out of reach of children. If ingested, contact a physician immediately.

Precautions:

Buscopan is not recommended for usein nursing foals or in pregnant or lactating mares,assafety has not been established. The effects of Buscopan may be potentiated by the concomitantuse of other anticholinergic drugs. Studies of con-comitant administration of Buscopan with otherdrugs have not been conducted. Drug compatibility should be monitored closely in patients requiring adjunctive therapy. The safety of Buscopan has notbeen established for intramuscular (IM) administra-tion. Administration of Buscopan results in heart rate elevation. Heart rate can not be used as a valid indicator of severity of pain for 30 minutes follow-ing IV injection.

Adverse Reactions:

Transient tachycardia and decreased borborygmal sounds lasted approxi-mately 30 minutes following administration.Transient pupillary dilation may also be observed.

Toreport suspected adverse reactions, to obtain aMaterial Safety Data Sheet (MSDS), or for technical assistance, call 1 800-821-7467.

Clinical Pharmacology:

Buscopan's spasmolytic action is based on anticholinergic effects resulting from competitive inhibition of parasympathetic activation (via muscarinic receptors) of smooth muscle cells. ¹The major side effect is a mild transient, elevated heart rate.

Pharmacokinetics:

Following single IV administra-tion of¹⁴C-Buscopan (0.4 mg/kg, side chainlabeled) in 3 horses, the major route of elimination of total radioactivity was via urine and feces almost equally. The bulk of the radioactivity (>96%) that represents all ¹⁴C-labeled moieties derived from the ¹⁴C-Buscopan dose was eliminated (urine andfeces) within the first 48 hours post-dosing. The elimination half-life of total plasma ¹⁴C was esti-mated to be approximately 6 hours. Therefore, the elimination half-life of the parent drug in plasma isequal to or shorter than 6 hours. The main radioac-tive component in the urine, which co-chromatographed with Buscopan using thin layer chromatography (TLC), accounted for approxi-mately 85% of the detected radioactivity.

Effectiveness:

A multi-centered, field study was conducted to establish the clinical effectiveness of Buscopan (0.3 mg/kg body weight) for the controlof abdominal pain (colic) associated with spas-modic, flatulent and simple impaction colics inhorses. A total of 217 cases were randomly assigned to the Buscopan or placebo group; inves-tigators were masked with respect to treatment.

Horses underwent a pretreatment colic examina-tion, with repeated exams at 5, 15, and 30 minutes following test article administration. A total colic score was assigned to each case based on 5 indi-vidual criteria (sweating, pawing, head and bodymovement, kicking, and desire to lie down). A gen-eral clinical impression was made at the 30-minutepost-treatment evaluation. No further evaluations were performed after 30 minutes.

Quarter Horses, Arabians, and Thoroughbreds accounted for the majority of the cases. Fifty-three percent of the horses were geldings, 39% were mares and 8% were stallions. Body weights ranged from 300-1700 lb (136-772 kg), with a mean of 968lb (440 kg). Ages ranged between 4 months and 35 years, with an average of 10.6 years.

Total colic scores decreased throughout the 30-minute post-treatment observation period for both Buscopan and placebo. Scores were significantly lower (p≤0.001) for the Buscopan treated horses. Also, 88% of the Buscopan cases were rated as a "success" (excellent, good, or moderate). This was significantly greater (p≤0.0001) than the 42% suc-cess rate for the placebo group.

The effectiveness of Buscopan was also supported by the overall improvement in the behavioral atti-tudes of the horses. A significantly higher percent-age of Buscopan treated horses were rated as "alert/calm" at 15 and 30 minutes post-treatment(p ≤ 0.005 and 0.0058, respectively), and a signifi-cantly (p≤0.006) greater proportion of placebo treated horses were "nervous/restless." A compa-rable number of cases for both the Buscopan and placebo groups were classified as "violent" or "drowsy/depressed" at all time points.

Post-treatment heart rates were significantly elevat-ed (p≤0.0001) for Buscopan treated horses at 5 and 15 minutes, compared to the placebo treated horses, as expected due to Buscopan's parasympa-tholytic effects. By 30 minutes post-treatment, the heart rates for the Buscopan group did not differ significantly from their pre-treatment heart rates. The intensity and frequency of borborygmi in all four abdominal quadrants was decreased for the Buscopan group at most post-treatment evalua-tion points (p≤0.02).

Animal Safety:

Target animal safety was evaluated in several studies, including dose tolerance, target animal safety, hemodynamics, and field safety.There were no signs of toxicity or adverse reactions. The pharmacological effects seen in these studies were consistent with those of anticholinergic drugs(see above).

In a target animal safety study, Buscopan was eval-uated in two phases. In the first phase, the drugwas administered intravenously at dosages of 1, 3,and 5 times the recommended level (30, 90 and150 mg per 100 kg body weight) once daily for three consecutive days. In the second phase it was given at the recommended therapeutic dosage (30 mg per kg body weight) at hourly intervals for three consecutive hours. Horses receiving Buscopan tended to have transient, reduced intensity of auscultated borborygmi, which can be attributed to the intended therapeutic effect of the drug. There was no evidence of gut stasis or colic. No other clinically significant effects were found. Though a transient effect on heart rate was noted inother studies, observations in this study (1-4 hoursafter drug administration) were made after the primary pharmacological activity for this drug had passed. Neither was there a significant association of dosage with pupil / pupillary light response as has been noted in other studies. Pupillary dilationis an expected pharmacological response to this class of drug (anticholinergic). The lack of a clinical response in this study is also likely related to the longer time after treatment at which the initial observations were made. In any event, this study shows that any effect on pupillary light response is indeed transient. There were no drug associated findings with respect to blood analyses, nor were there any effects evident at necropsy and histopathology.

In a tolerance study, four horses were administered 10 times the recommended Buscopan dosage (300mg/100 kg) and were examined at 10 minutes andthen at 1, 2, 3, 4, 24, and 72 hours post injection. All horses temporarily experienced dilated and fixed pupils at 10 minutes post injection. Normal pupillary light reflex returned in two horses at 4 hours and in the other two horses at 24 hours. Heart rates were increased at 10 and 60 minutes, but had returned to normal at 2 hours. Oral mucous membranes were dry at 10 minutes, but were normal at 2 hours. Gut motility, as judged by auscultated borborygmi, was absent at 10 minutes post injection, but had returned to baseline fre-quency and intensity by 3 hours in 2 horses and by 4 hours in the remaining horses. There were two incidences of colic, with one horse showing mild colic at 1 hour, and another with mild colic at 11 hours. Both colic episodes were transient and required no medication. There were no drug associ-ated changes in CBC, blood coagulation, or serum chemistry. Neither were there any drug-relatedgross or histopathological changes.

In a study of hemodynamic parameters, Buscopan decreased right atrial pressure, while cardiac output was maintained. The hemodynamic changes which occurred following Buscopan administration were of little clinical significance, being qualitatively sim-ilar to those reported for low doses of other anti-cholinergics such as atropine.

Storage:

Store at controlled room temperature, 59-86°F (15-30°C).