Phenobarbital


Phenobarbital is a barbiturate with anticonvulsant and sedative effect, which takes place in the treatment of epilepsy and in preparation for the application of anesthesia.
Mode of action
Acts as a barbiturate phenobarbital on the binding and activation of the inhibitory-acting GABAA receptors in the central nervous system (CNS). This occurs through the binding of phenobarbital to a domain of the GABAA receptor ligand to the opening of ion channels.
Metabolism
After oral administration of phenobarbital leads to an almost complete inclusion of the drug. The time to reach the maximum effect level is dependent on the application form.
Maximum effect level
Application form Time
orally 6-18 hours
intramuscular (i.m.) 3-5 hours
intravenous (i.v.) 20-60 minutes

Phenobarbital is metabolized in the liver, but also partly excreted unchanged in urine. The half-life is approximately 2-4 days in adults.

Applications
Phenobarbital is its use today, especially in the preparation and anesthesia in the treatment of epilepsy. Because of its sedative effects, it has long been used as a sleep aid. Due quickly and its side effects depending on the patient’s evolving, it is not approved for this indication since 1992 more.
Side effects
Phenobarbital know in addition to the highly addictive effect, inter alia, the following side effects:
* Dizziness
* Headache
* Ataxia
* Confusion
* Extended Response
* Paradoxical excitement

In case of overdose:
* Respiratory depression to apnea
* Coma
* Hypotension
* Ataxia
* Kidney failure

Since phenobarbital in the liver triggers the production of drug metabolising enzyme, can lead to increased degradation of other parallel given medication. These include:

* Thyroid hormones
* Doxycycline
* Chloramphenicol
* Oral contraceptives

At the same time, it leads to some medications increase the effect, especially in the administration of other centrally acting drugs and intoxication with alcohol.

Contraindications
Phenobarbital should not be used in:
* Metabolic disorders such as porphyria
* Liver problems
* Renal failure
* Severe cardiovascular disease
* Severe chronic pulmonary disease (COPD, asthma)
Intoxication
Like all barbiturates, there is also Penthobarbital no antidote, which can be administered in an accidental or intentional (suicidal) overdose. The goal of treatment of overdose is the stabilization of the circulation and possibly the removal of the Giftfokusses.


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