|Systematic (IUPAC) name|
|Metabolism||hepatic mainly CYP3A4|
|Half-life||35 hours |
|(what is this?)|
Butalbital is a barbiturate with an intermediate duration of action. Butalbital is often combined with other medications, such as acetaminophen (paracetamol) or aspirin, and is commonly prescribed for the treatment of pain and headache. The various formulations combined with codeine are FDA approved for the treatment of tension headaches. Butalbital has the same chemical formula as talbutal but a different structure—one that presents as 5-allyl-5-isobutylbarbituric acid,
- 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)
Butalbital is not suggested as a first-line treatment for headache because it impairs alertness, brings risk of dependence and addiction, and increases the risk that episodic headaches will become chronic. Opioids also can cause heightened sensitivity to headache pain. When other treatments fail or are unavailable, butalbital may be appropriate for treating headache if the patient can be monitored to prevent the development of chronic headache.
There are specific treatments which are appropriate for targeting migraines and headaches which are preferable to butalbital when available as an option. It is a least preferable option to be used if other available treatments fail.
Side effects for any psychoactive drug are difficult to predict, but commonly reported side effects for butalbital include:
Butalbital has a very long half-life and accumulates in the body following repeated doses, although therapeutic effects tend to wear off after a few hours the risk of side effects following repeated doses increases with each subsequent dose, as does the severity of side effects which have already presented. Sedation, memory loss, and ataxia are very common after taking fioricet multiple times in one day. The long half-life also means that side effects can persist for hours or days after the last dose and care must be taken when returning to normal activities after each use, motor impairment may be present even after other effects such as sedation have worn off.
The risk and severity of all side effects is greatly increased when fioricet is combined with other sedatives (ex. ethanol, opiates, benzodiazepines, antihistamines), and other side effects which are not typically associated with fioricet may occur. Inhibitors of the hepatic enzyme CYP3A4 may also increase the risk, severity, and duration of side effects, many drugs inhibit this enzyme as do some foods such as grapefruit and the blood orange. Taking fioricet with some other drugs may also increase the side effects of the other medication.
Dangers and risks
Butalbital is a physically and psychologically addictive barbiturate. Mixing with alcohol increases the risk of intoxication, increases respiratory depression, and increases liver toxicity when it is a butalbital combination including paracetamol (acetaminophen). Many opioid-dependent persons frequently use barbiturates as a potentiator to their normal dose of opiates in order to increase the effects, or with a less than normal dose as means of conserving their supply. Especially when used with the stronger narcotics, suicide or accidental death occurs much more frequently than first reported with one drug alone. Use of alcohol, benzodiazepines, and other CNS-depressants often also contribute to respiratory depression, coma, and in extreme cases fatality.
When benzodiazepines are co-administered with barbiturates, the sum effect of the drugs is far greater than would be expected considering the effect of both drugs separately. This is due to complimentary mechanisms at the GABAA receptor, where benzodiazepines increase the rate of chloride channel opening while barbiturates increase the duration. A dose of a benzodiazepine causes a channel which normally opens once every 30 seconds to open 3 times faster, while a barbiturate causes the channel to pass three chloride ions per opening instead of the normal one. When combined, the channel is now passing nine ions every 30 seconds instead of one, a 9-fold increase in activity.
- DE Patent 526854
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