Ipecac

Absorption

The main components of ipecac are rapidly absorbed from the GI tract, this absorption depends on the amount of emesis produced by the administered dose. The peak plasma concentration of 10-16 ng/ml is attained 20 minutes after first administration. The bioavailability of ipecac is reduced over time from 67-11% after 5-60 minutes of administration.

Toxicity

An overdose of an ipecac preparation may cause serious poisoning. If emesis is not provoked after two doses of ipecac, a gastric lavage is recommended. The overdose of the components such as emetine is reported to cause the onset of myopathy. Chronic use of this drug has been indicated to produce muscle weakness, waddling gait, dyspnea, left atrial enlargement and reduced left ventricular ejection fraction.

The Uses of Ipecac

Ipecac Syrup (cas# 8012-96-2) is a compound useful in organic synthesis.

Indications

Ipecac is indicated as an emetic agent for the induction of vomiting in poisoning victims who ingested systemic poison in order to prevent absorption of the chemicals through the gastrointestinal tract. In low doses, ipecac was also used as an expectorant.
Reports have suggested that ipecac was vastly used in patients with eating disorders to produce vomiting.

Background

Ipecac is obtained from the plant Cephaelis ipecacuanha and contains a number of emetic alkaloids including emetine and cephaeline. Ipecac was approved by Health Canada as an OTC but all those products are now discontinued. The FDA does not have currently any approved product containing ipecac, however, ipecac as an ingredient is accepted to be sold over the counter in packages of 1 fluid ounce (30 ml) for the emergency use to cause vomiting in poisoning.

Pharmacokinetics

An effective and safe dose of ipecac may cause vomiting within 20 minutes of the administration. In prospective studies with children, the mean time to vomit was reported to be of 21.7 minutes.

Metabolism

The main components of ipecac have been shown in microsomal enzyme systems that emetine is converted to cephaeline and 9-O-demethylemetine by CYP2D6. On the other hand, CYP3A4 produces the transformation of emetine to 9-O-demethylemetine and 10-O-demethylemetine. In preclinical studies, it was shown that cephaline is conjugated with glucuronice to form cephaeline-6'-O-glucuronide for biliary excretion whereas emetine gets demethylated to cephaline and 9-O-demethylemetine before glucuronidation.