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Halothane | CAS No: 151-67-7 | GMP-certified suppliers
A medication that provides reliable induction and maintenance of general anesthesia with central nervous system depression, muscle relaxation, and controlled hypotensive effects for surgical procedures.
Therapeutic categories
Primary indications
- For the induction and maintenance of general anesthesia
Product Snapshot
- Halothane is an inhalation anesthetic available in aerosol, liquid, and solution formulations
- Its primary use is for the induction and maintenance of general anesthesia
- Halothane is approved for use in the United States and Canada, including veterinary approvals
Clinical Overview
Pharmacodynamically, halothane acts by depressing the central nervous system, leading to reductions in blood pressure and respiratory rate, along with a frequent decrease in pulse rate. It produces muscle relaxation and diminishes pain sensitivity primarily by altering tissue excitability. This is achieved through the modulation of gap junction-mediated cell-to-cell coupling and interference with ion channels responsible for action potential propagation.
The mechanism of action involves interaction with multiple ion channels, resulting in the depression of nerve conduction, respiratory drive, and cardiac contractility. Halothane exerts immobilizing effects attributed to its binding to potassium channels in cholinergic neurons. Additionally, it interacts with N-methyl-D-aspartate (NMDA) and calcium channels, causing neuronal hyperpolarization and contributing to its anesthetic properties.
Halothane’s metabolism involves cytochrome P450 enzyme subfamilies including CYP2A6, CYP2B6, CYP2C9, CYP2E1, and CYP3A4. These metabolic pathways may play a role in its biotransformation and potential toxicities. Safety considerations include the risk of hepatotoxicity, particularly associated with repeated exposure, and respiratory and cardiac depression; monitoring during clinical use is essential. Its depressant effects also necessitate cautious use in patients with compromised cardiovascular function.
The compound is approved for use in humans and veterinary medicine as a general inhalation anesthetic. While largely replaced in many regions by newer agents with more favorable safety profiles, halothane remains relevant in specific clinical or geographic contexts.
For API sourcing, it is critical to ensure compliance with pharmacopeial standards, especially regarding purity, residual solvent content, and absence of degradation products. Given halothane’s sensitivity to light and air, manufacturers should provide appropriate packaging to maintain API stability. Reliable suppliers must demonstrate consistent quality control measures, stability data, and traceability to support global regulatory requirements.
Identification & chemistry
| Generic name | Halothane |
|---|---|
| Molecule type | Small molecule |
| CAS | 151-67-7 |
| UNII | UQT9G45D1P |
| DrugBank ID | DB01159 |
Pharmacology
| Summary | Halothane is an inhalation anesthetic that induces general anesthesia by modulating multiple ion channels, including potassium, NMDA, calcium, and GABA(A) receptors. Its pharmacodynamic effects involve depression of nerve conduction, respiratory function, cardiac contractility, and muscle relaxation through altered tissue excitability and reduced gap junction coupling. The compound’s primary therapeutic intent is the induction and maintenance of general anesthesia. |
|---|---|
| Mechanism of action | Halothane causes general anaethesia due to its actions on multiple ion channels, which ultimately depresses nerve conduction, breathing, cardiac contractility. Its immobilizing effects have been attributed to its binding to potassium channels in cholinergic neurons. Halothane's effect are also likely due to binding to NMDA and calcium channels, causing hyperpolarization. |
| Pharmacodynamics | Halothane is a general inhalation anesthetic used for induction and maintenance of general anesthesia. It reduces the blood pressure and frequently decreases the pulse rate and depresses respiration. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Potassium channel subfamily K member 3 | Humans | binder |
| Potassium channel subfamily K member 9 | Humans | binder |
| GABA(A) Receptor | Humans | positive allosteric modulator |
ADME / PK
| Metabolism | Halothane is metabolized in the liver, primarily by CYP2E1, and to a lesser extent by CYP3A4 and CYP2A6. |
|---|
Formulation & handling
- Halothane is administered exclusively via respiratory inhalation, indicating formulation as a volatile liquid for inhalation delivery.
- Being a small molecule organofluoride with moderate water solubility and lipophilicity, halothane requires handling considerations to prevent volatilization and maintain stability.
- Formulations should account for its liquid state and potential interactions with container materials to preserve purity and efficacy during storage and use.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is approaching patent expiry in key markets including Canada and the US, leading to increased availability of generic formulations. This transition marks a shift toward greater market maturity and competitive pricing. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Halothane is supplied by multiple packagers serving primarily the US and Canadian markets. Branded products are established in North America, with limited presence reported elsewhere. Given the historical use of halothane and the availability of multiple brands, patent exclusivity is no longer a barrier, indicating existing generic competition. |
|---|
Safety
| Toxicity | Toxic effects of halothane include malignant hyperthermia and hepatitis. |
|---|
- Exposure to halothane vapors may induce malignant hyperthermia in susceptible individuals
- Halothane has been associated with hepatotoxicity
- Appropriate handling to minimize operator exposure is advised
Halothane is a type of Inhalation anesthetics
Inhalation anesthetics belong to the subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used for inducing general anesthesia. These specialized compounds are administered through inhalation, allowing them to be rapidly absorbed into the bloodstream and exert their anesthetic effects. Inhalation anesthetics are widely utilized in surgical procedures to achieve unconsciousness, analgesia (pain relief), muscle relaxation, and amnesia.
The primary mechanism of action of inhalation anesthetics involves targeting the central nervous system (CNS) and altering neuronal activity. By binding to specific receptors, these anesthetics modulate neurotransmitter release, resulting in the depression of neuronal signaling. This leads to a reversible loss of consciousness and pain sensation, enabling surgeons to perform invasive procedures without causing discomfort or distress to the patient.
Common inhalation anesthetics include volatile liquids such as sevoflurane, desflurane, and isoflurane, as well as nitrous oxide (N2O), which is a gas. These agents possess favorable characteristics, such as rapid onset and offset of action, high potency, and controllable depth of anesthesia. Inhalation anesthetics offer advantages like easy administration, precise dosage titration, and minimal metabolism-related side effects.
The pharmaceutical industry ensures the quality and safety of inhalation anesthetics through rigorous manufacturing processes and strict quality control measures. Stringent regulations are in place to maintain the purity, stability, and efficacy of these APIs. Additionally, continuous research and development efforts aim to improve the pharmacokinetics, safety profiles, and environmental impact of inhalation anesthetics, further enhancing patient care and surgical outcomes.
Halothane (Inhalation anesthetics), classified under Anesthetics
Anesthetics are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used in the field of medicine. These substances play a vital role in inducing a temporary loss of sensation or consciousness, enabling medical procedures to be performed without pain or discomfort. Anesthetics can be classified into two primary types: general anesthetics and local anesthetics.
General anesthetics act on the central nervous system, producing a reversible loss of consciousness. They are administered through inhalation or injection routes and are commonly employed for major surgeries or procedures that require deep sedation. Examples of general anesthetics include sevoflurane, propofol, and isoflurane.
On the other hand, local anesthetics primarily target a specific region or part of the body, temporarily numbing the area and blocking pain signals. These APIs are frequently used in dental procedures, minor surgeries, and childbirth. Common local anesthetics include lidocaine, bupivacaine, and ropivacaine.
Anesthetics work by interfering with the transmission of nerve signals or by altering the activity of certain receptors in the nervous system. They offer precise control over pain management, allowing medical professionals to perform complex procedures with reduced patient discomfort and anxiety.
The development and manufacturing of anesthetics APIs require stringent quality control measures to ensure safety and efficacy. Pharmaceutical companies adhere to strict regulatory guidelines to produce high-quality APIs. The demand for anesthetics remains consistently high, making this category of APIs a critical component of the pharmaceutical industry.
In conclusion, anesthetics are indispensable pharmaceutical APIs used to induce temporary loss of sensation or consciousness. They can be classified into general and local anesthetics, each serving distinct purposes in medical procedures. The proper development and manufacturing of anesthetics APIs are essential to ensure safe and effective pain management in various healthcare settings.
Halothane API manufacturers & distributors
Compare qualified Halothane API suppliers worldwide. We currently have 2 companies offering Halothane API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Piramal Healthcare | Producer | United Kingdom | India | CoA, GMP, WC | 31 products |
| Piramal Pharma Solutions | Producer | India | Unknown | CoA, JDMF | 44 products |
When sending a request, specify which Halothane API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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