Butalbital

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Butalbital is a barbiturate of medium-duration action. Butalbital is often combined with other drugs, such as acetaminophen (paracetamol) or aspirin, and is commonly prescribed for the treatment of pain and headaches. Various formulations combined with FDA approved codeine for the treatment of tension headaches. Butalbital has the same chemical formula as talbutal but different structure - which presents 5-allyl-5-isobutylbarbituric acid.

Video Butalbital

Preparasi

Combinations include:

• Butalbital and acetaminophen (paracetamol) (trade names: Axocet, Bucet, Bupap, Cephadyn, Dolgic, Phrenilin, Phrenilin Forte, Sedapap)
• Butalbital, paracetamol (acetaminophen), and caffeine (trade names: Fioricet, Esgic, Esgic-Plus)
• Butalbital and aspirin (trade name: Axotal)
• Butalbital, aspirin, and caffeine (trade names Fiorinal, Fiormor, Fiortal, Fortabs, Laniroif)
• Butalbital, paracetamol (acetaminophen), caffeine, and codeine phosphate (Fioricet # 3 with Codeine)
• Butalbital, aspirin, caffeine, and codeine phosphate (trade name: Fiorinal # 3 with Codeine)
• Ergotamine tartrate, caffeine, butalbital, belladonna alkaloids (trade name: Cafergot-PB)

Maps Butalbital

Contraindications

Butalbital is not recommended as first-line treatment for headaches for damaging vigilance, carries the risk of addiction and addiction, and increases the risk that episodic headaches will become chronic. When other treatments fail or are not available, butalbital may be appropriate to treat headaches if the patient can be monitored to prevent the development of chronic headaches.

There are specific treatments that are appropriate to target migraines and headaches that are better than butalbital when available as an option. This is the most preferred option to use if other available treatments fail.

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Side effects

Side effects for any psychoactive drug are unpredictable, although butalbital is usually well tolerated. Commonly reported side effects for butalbital, which tend to subside with ongoing use, include:

Rare side effects include Stevens-Johnson syndrome, adverse reactions to barbiturates, and anaphylaxis.

The risks and severity of all side-effects are greatly increased when butalbital (or butbital-based, such as Fioricet) drugs are combined with other sedatives (eg ethanol, opiates, benzodiazepines, antihistamines), and other side effects, which are not normally associated with butalbital, can occur. CYP3A4 liver enzyme inhibitors can also increase the risk, severity, and duration of side effects, many drugs inhibit this enzyme as well as some foods such as oranges and orange blood. Taking a butalbital based drug with some other medications may also increase the side effects of other drugs.

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Danger and risk

Butalbital can cause addiction, addiction, or both. Mixing with alcohol increases the risk of poisoning, increases respiratory depression, and increases liver toxicity when it is a combination of butalbital including paracetamol (acetaminophen). Many opioid-dependent people often use barbiturates as potentiators for their normal opiate dose to increase the effect, or with less than normal doses as a means to preserve their supply. Especially when used with stronger narcotics, suicide or unintentional death occur much more often than first reported with one drug alone. The use of alcohol, benzodiazepines, and other CNS depressants often also contribute to respiratory depression, coma, and in extreme cases of death.

When benzodiazepine is given in conjunction with barbiturates, the effect of drug quantities is much greater than expected by considering the effects of these two drugs separately. This is due to the complementary mechanism of GABA _A receptors, in which benzodiazepines increase the rate of opening of chloride channels while barbiturates increase duration. The dose of benzodiazepine causes a normally open channel every 30 seconds to open 3 times faster, while barbiturates cause the channel to pass through three chloride ions per opening, not the normal one. When combined, the channel now passes through nine ions every 30 seconds instead of one, a 9-fold increase in activity.

Like most barbiturates, butalbital is a common inducer of P450 enzymes in both rodents and humans, especially CYP3A4 (thereby inducing metabolism alone), CYP2D6, and CYP2C9, although the induction of P450 enzyme is much less than the phenobarbital equivalent dose. or secobarbital (the most powerful enzyme inducer known in the molecular family of barbiturates). At very high doses it has also been shown to induce glutathione S-transferase A1/glutathione S-transferase A2 in mice, although the dose required to achieve this effect to a clinically significant level falls within the range of LD50 butalbitals, making its use for this purpose impractical and extremely dangerous (this effect has not been tested on the human model, therefore it is unknown whether or not GS-T induced an important role in the human butalbital effect, or even occurred at all).

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References

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External links

"Butalbital". Kamus Kedokteran On-line . Diperoleh 26 Juni, 2005 . " Butalbital dan Acetaminophen (Systemic) ". Informasi Obat MedicinePlus . Diarsipkan dari aslinya pada 30 Desember 2006 . Diperoleh 31 Desember, 2006 . " Controlled Substances dalam Jadwal III ". Administrasi Pemberantasan Narkoba. 2007. Diarsipkan dari aslinya pada 2007-02-02 . Diperoleh 2007-01-13 .

Source of the article : Wikipedia