Ipecac API Manufacturers & Suppliers
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Ipecac | CAS No: 8012-96-2 | GMP-certified suppliers
A medication that induces vomiting to reduce toxin absorption in poisoning cases and has historical use as an expectorant for respiratory conditions.
Therapeutic categories
Primary 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
Product Snapshot
- Ipecac is available primarily as an oral syrup or tablet formulation
- It is used mainly as an emetic agent for the induction of vomiting in cases of systemic poisoning
- Ipecac has an approved status in the US and Canada but has also been withdrawn in some markets
Clinical Overview
Clinically, ipecac’s principal indication is the induction of emesis following ingestion of certain poisons. At lower doses, ipecac has also been employed as an expectorant, though this use is largely obsolete. The compound’s emetic action is mediated through both local irritation of the gastric mucosa and stimulation of the chemoreceptor trigger zone in the central nervous system. These mechanisms typically result in vomiting within approximately 20 minutes after oral administration.
Pharmacodynamically, ipecac induces emesis through its bioactive alkaloids, emetine and cephaeline. Emetine particularly acts on smooth muscle and nerve endings to provoke gastric contractions and vomiting reflexes. In pediatric clinical studies, mean onset of vomiting post-dose was about 21.7 minutes.
Absorption and metabolism details for ipecac alkaloids indicate they are substrates of cytochrome P450 enzymes including CYP2D6 and CYP3A4, which may have implications for drug interactions. Renal excretion is a primary route of elimination for these components.
Safety considerations include the potential for muscle toxicity, as emetine is associated with cardiotoxic and myopathic effects at higher or repeated doses. Due to such risks, routine use of ipecac syrup has been largely discontinued and is no longer recommended in many markets. In Canada, previous over-the-counter ipecac products have been withdrawn. The U.S. FDA does not currently approve any marketed ipecac products but permits limited OTC sale in 30 ml emergency doses for poisoning treatment.
Given the complexity and safety concerns of ipecac, sourcing pharmaceutical-grade API demands strict quality controls. Suppliers should provide comprehensive certificates of analysis confirming identity, purity, and alkaloid content. Consistency in raw plant material sourcing and compliance with regulatory standards is essential to ensure safe use in authorized clinical or emergency settings.
Identification & chemistry
| Generic name | Ipecac |
|---|---|
| Molecule type | Small molecule |
| CAS | 8012-96-2 |
| UNII | 62I3C8233L |
| DrugBank ID | DB13293 |
Pharmacology
| Summary | Ipecac contains emetine and cephaeline, which induce vomiting by locally irritating the gastric mucosa and activating the central chemoreceptor trigger zone. Its primary therapeutic use is as an emetic agent for the removal of ingested toxic substances before systemic absorption. The pharmacodynamic effect typically occurs within 20 to 22 minutes post-administration. |
|---|---|
| Mechanism of action | The emetic components of ipecac, emetine and cephaeline, act centrally and locally in the gastrointestinal tract to cause vomiting. The mechanism by which ipecac performs his effect is by irritating the stomach lining and chemically stimulating the chemoreceptor trigger zone. |
| Pharmacodynamics | 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. |
ADME / PK
| 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. |
|---|---|
| Half-life | The effect of ipecac is done in about 20 minutes and the elimination of the little-absorbed dose is reported to be very rapid. Thus, the half-life is thought to be of about 0.5-1 hour. |
| Protein binding | This pharmacokinetic property is not relevant as the absorbed dose of ipecac is minimal. |
| 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. |
| Route of elimination | Due to the emetic function, even 76% of the administered dose is vomited. From the absorbed dose, the elimination from plasma is relatively rapid. In some clinical trials, the alkaloids were not observed in plasma 6 hours after administration. When the patient does not vomit any part of the administered dose, there could be traces in plasma after 24 hours. The component alkaloids are eliminated via the bile and urine as it has been observed a persistence in urine after chronic administration. Biliary and urinary excretion of ipecac corresponds to 57.5% and 16.5% of the administered dose respectively. From the excreted dose, unchanged cephaeline accountd for 42.4% of the eliminated dose in feces. |
| Volume of distribution | The volume of distribution is thought to be large based on the prolonged excretion. |
| Clearance | The urinary excretion of the main components of ipecac accounts for 75% of the administered dose 48 hours after initial administration. |
Formulation & handling
- Ipecac is a small molecule API primarily formulated for oral administration in syrup, tablet, or liquid forms.
- Due to its oral route, formulation must ensure palatability and stability in aqueous syrup solutions.
- Handling considerations include protection from contamination and maintaining solution homogeneity during storage.
Regulatory status
| Lifecycle | The API's key patent protections have expired in the US and Canada, allowing for generic entry and increased market competition. As a result, the product is in a mature phase across these markets. |
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| Markets | US, Canada |
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Supply Chain
| Supply chain summary | The manufacturing and supply landscape of Ipecac involves several originator companies producing branded products primarily marketed in the US and Canada. The presence of multiple branded formulations, including syrups and tablets, indicates established brand recognition in these regions. Patent expiry timelines are not specified, but the availability of various branded generics suggests existing generic competition in the market. |
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Safety
| 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. |
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- Overdose may result in severe toxicity including myopathy and cardiopulmonary complications
- Chronic exposure can cause muscle weakness and impaired cardiac function
- Handling requires caution to avoid unintentional ingestion or exposure due to emetic and toxic properties
Ipecac is a type of Antidotes, Deterrents, and Toxicologic Agents
Antidotes, Deterrents, and Toxicologic Agents are an important category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that play a critical role in healthcare and toxicology. These substances are designed to counteract the effects of poisons, toxins, and overdoses, thereby saving lives and preventing severe health consequences.
Antidotes are substances that neutralize the toxic effects of certain drugs, chemicals, or poisons. They work by either directly binding to the toxic substance or by blocking its harmful actions on the body. Antidotes are administered in emergency situations to quickly reverse the effects of poisoning and restore normal physiological functions.
Deterrents, on the other hand, are pharmaceutical agents used to discourage or prevent harmful behaviors, such as substance abuse. They are designed to make the ingestion or misuse of certain substances unpleasant or less desirable. Deterrents can be formulated to cause unpleasant side effects, such as nausea or vomiting, when a particular substance is consumed in excessive amounts.
Toxicologic agents encompass a broad range of pharmaceutical APIs used in toxicology studies and research. These substances are employed to investigate the toxicity, metabolism, and mechanisms of action of various chemicals and compounds. Toxicologic agents are vital for understanding the potential hazards and risks associated with certain substances, ensuring the safety of drugs, and developing effective treatments for poisoning cases.
In conclusion, Antidotes, Deterrents, and Toxicologic Agents are essential categories of pharmaceutical APIs that address poisoning emergencies, deter harmful behaviors, and enable toxicological research. Their development and availability are crucial for safeguarding public health, enhancing patient care, and advancing our understanding of toxicology.
