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General Description:

Ipecac, identified by CAS number 8012-96-2, is a notable compound with significant therapeutic applications. 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.

Indications:

This drug is primarily indicated for: 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. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Ipecac undergoes metabolic processing primarily in: 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. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Ipecac are crucial for its therapeutic efficacy: 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. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Ipecac is an important consideration for its dosing schedule: 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. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Ipecac exhibits a strong affinity for binding with plasma proteins: This pharmacokinetic property is not relevant as the absorbed dose of ipecac is minimal. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Ipecac from the body primarily occurs through: 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. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Ipecac is distributed throughout the body with a volume of distribution of: The volume of distribution is thought to be large based on the prolonged excretion. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Ipecac is a critical factor in determining its safe and effective dosage: The urinary excretion of the main components of ipecac accounts for 75% of the administered dose 48 hours after initial administration. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Ipecac exerts its therapeutic effects through: 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. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Ipecac functions by: 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. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Categories:

Ipecac is categorized under the following therapeutic classes: Agents Causing Muscle Toxicity, Antidotes, Autonomic Agents, Biological Products, Central Nervous System Agents, Complex Mixtures, Cough and Cold Preparations, Cytochrome P-450 CYP2D6 Substrates, Cytochrome P-450 CYP3A Substrates, Cytochrome P-450 CYP3A4 Substrates, Cytochrome P-450 Substrates, Drugs that are Mainly Renally Excreted, Emetics, Expectorants, Gastrointestinal Agents, Peripheral Nervous System Agents, Plant Extracts, Plant Preparations. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Ipecac include:

• Water Solubility: Soluble
• logP: 5.0
• pKa: 6.64-6.77