Aminopentamide Hydrogen Sulfate (Centrine)

By | 2013-07-18

Anticholinergic/Antispasmodic

Highlights Of Prescribing Information

Anticholinergic/antispasmodicfor GI indications in small animals

Typical adverse effect profile (“dry, hot, red”); potentially could cause tachycardia

Contraindicated in glaucoma; relatively contraindicated in tachycardias, heart disease, GI obstruction, etc.

What Is Aminopentamide Hydrogen Sulfate Used For?

The manufacturer states that the drug is indicated “in the treatment of acute abdominal visceral spasm, pylorospasm or hypertrophic gastritis and associated nausea, vomiting and/or diarrhea” for use in dogs and cats.

Pharmacology/Actions

Aminopentamide is an anticholinergic agent that when compared to atropine has been described as having a greater effect on reducing colonic contractions and less mydriatic and salivary effects. It reportedly may also reduce gastric acid secretion.

Pharmacokinetics

No information was located.

Before you take Aminopentamide Hydrogen Sulfate

Contraindications / Precautions / Warnings

The manufacturer lists glaucoma as an absolute contraindication to therapy and to use the drug cautiously, if at all, in patients with pyloric obstruction. Additionally, aminopentamide should not be used if the patient has a history of hypersensitivity to anticholinergic drugs, tachycardias secondary to thyrotoxicosis or cardiac insufficiency, myocardial ischemia, unstable cardiac status during acute hemorrhage, GI obstructive disease, paralytic ileus, severe ulcerative colitis, obstructive uropathy or myasthenia gravis (unless used to reverse adverse muscarinic effects secondary to therapy).

Antimuscarinic agents should be used with extreme caution in patients with known or suspected GI infections, or with autonomic neuropathy. Atropine or other antimuscarinic agents can decrease GI motility and prolong retention of the causative agent(s) or toxin(s) resulting in prolonged clinical signs.

Antimuscarinic agents should be used with caution in patients with hepatic disease, renal disease, hyperthyroidism, hypertension, CHF, tachyarrhythmias, prostatic hypertrophy, esophageal reflux, and in geriatric or pediatric patients.

Adverse Effects

Adverse effects resulting from aminopentamide therapy may include dry mouth, dry eyes, blurred vision, and urinary hesitancy. Urinary retention is a symptom of too high a dose and the drug should be withdrawn until resolved.

Overdosage / Acute Toxicity

No specific information was located regarding acute overdosage clinical signs or treatment for this agent. The following discussion is from the Atropine monograph that could be used as a guideline for treating overdoses:

If a recent oral ingestion, emptying of gut contents and administration of activated charcoal and saline cathartics may be warranted. Treat clinical signs supportively and symptomatically. Do not use phenothiazines as they may contribute to the anticholinergic effects. Fluid therapy and standard treatments for shock may be instituted.

The use of physostigmine is controversial and should probably be reserved for cases where the patient exhibits either extreme agitation and is at risk for injuring themselves or others, or for cases where supraventricular tachycardias and sinus tachycardias are severe or life threatening. The usual dose for physostigmine (human) is: 2 mg IV slowly (for average sized adult), if no response, may repeat every 20 minutes until reversal of toxic antimuscarinic effects or cholinergic effects takes place. The human pediatric dose is 0.02 mg/kg slow IV (repeat q10 minutes as above) and may be a reasonable choice for treatment of small animals. Physostigmine adverse effects (bronchoconstriction, bradycardia, seizures) may be treated with small doses of IV atropine.

How to use Aminopentamide Hydrogen Sulfate

Aminopentamide Hydrogen Sulfate dosage for dogs:

a) May be administered every 8-12 hours via IM, SC or oral routes. If the desired effect is not attained, the dosage maybe gradually increased up to 5 times those listed below: Animals weighing: 10 lbs or less: 0.1 mg; 11-20 lbs: 0.2 mg; 21-50 lbs: 0.3 mg; 51 -100 lbs: 0.4 mg; over 100 lbs: 0.5 mg (Package Insert; Centrine — Fort Dodge)

b) To decrease tenesmus in malabsorption/maldigestion syndromes: 0.1-0.4 mg SC, or IM twice daily-three times daily ()

c) As an antiemetic: 0.1-0.4 mg SC, or IM two to three times daily ()

Aminopentamide Hydrogen Sulfate dosage for cats:

a) As in “a” above in dogs

b) As an antiemetic: 0.1-0.4 mg SC, or IM two to three times daily ()

c) As second-line adjunctive therapy for refractory IBD: 0.1-0.4 mg/kg SC two to three times daily ()

Client Information

■ Contact veterinarian if animal has difficulty urinating or if animal is bothered by dry eyes or mouth

Chemistry / Synonyms

An antispasmodic, anticholinergic agent, aminopentamide hydrogen sulfate has a chemical name of 4-(dimethylamino)-2,2-diphenylvaleramide.

Aminopentamide hydrogen sulfate may also be known as dimevamid or Centrine.

Storage / Stability

Store aminopentamide tablets and injection at controlled room temperature (15-30°C; 59-86°F).

Dosage Forms / Regulatory Status

Veterinary-Labeled Products:

Aminopentamide Hydrogen Sulfate Tablets: 0.2 mg; Centrine (Fort Dodge); (Rx). Approved for use in dogs and cats only.

Aminopentamide Hydrogen Sulfate Injection: 0.5 mg/mL in 10 mL vials; Centrine (Fort Dodge); (Rx). Approved for use in dogs and cats only.

Human-Labeled Products: None