Drug information of Butabarbital

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Butabarbital

فارسی

Butabarbital is a barbiturate with a particularly fast onset of effects and short duration of action compared to other barbiturates. This makes butabarbital a useful drug for certain applications such as treating severe insomnia and relieving anxiety before surgical procedures.

Mechanism of effect

Butabarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.

Pharmacodynamic

Butabarbital belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.

Pharmacokinetics

Half-Life: ~100 hr

Duration: 6-8 hr

Onset: 45-60 min

Enzymes induced: CYP1A2, CYP2C9/10, CYP3A4

Excretion: Urine

Drug indications

Anxiety , Insomnia

Dosage

Adult

Sedative or Hypnotic

Hypnotic: 50-100 mg qHS

Daytime sedation: 15-30 mg q6-8hr

Preoperative sedation: 50-100 mg 60-90 minutes before surgery

Pediatric

Sedation

Preoperative sedation: 2-6 mg/kg; not to exceed 100 mg/dose 

Alerts

  • Because sleep disturbances may be the presenting manifestation of a physical and/or psychiatric disorder, symptomatic treatment of insomnia should be initiated only after a careful evaluation of patient; failure of insomnia to remit after 7 to 10 days of treatment may indicate presence of a primary psychiatric and/or medical illness that should be evaluated
  • Worsening of insomnia or emergence of new thinking or behavior abnormalities may be the consequences of an unrecognized psychiatric or physical disorder; it is important to use smallest possible effective dose, especially in the elderly
  • Complex behaviors such as “sleep driving” (i.e., driving while not fully awake after ingestion of a sedative-hypnotic, with amnesia for event) reported; events can occur in sedative-hypnotic-naive as well as in sedative-hypnotic-experienced persons; the use of alcohol and other CNS depressants with sedative-hypnotics appears to increase risk of such behaviors; due to risk to patient and community, discontinuation of sedative-hypnotics should be strongly considered for patients who report a “sleep driving” episode
  • Other complex behaviors (e.g., preparing and eating food, making phone calls, or having sex) reported in patients who are not fully awake after taking a sedative-hypnotic; patients usually do not remember these events
  • Because drug can cause drowsiness and a decreased level of consciousness, patients, particularly the elderly, are at a higher risk of falls
  • Rare cases of angioedema involving tongue, glottis or larynx reported; some patients have had additional symptoms such as dyspnea, throat closing, or nausea and vomiting that suggest anaphylaxis; if angioedema involves tongue, glottis or larynx, airway obstruction may occur and be fatal; patients who develop angioedema with sedative-hypnotics should not be rechallenged with drug
  • Barbiturates may be habit forming; tolerance, psychological and physical dependence may occur with continued use; to minimize possibility of overdosage or development of dependence, prescribing and dispensing of sedative-hypnotic barbiturates should be limited to amount required for interval until next appointment; abrupt cessation after prolonged use in dependent person may result in withdrawal symptoms, including delirium, convulsions, and possibly death; withdraw barbiturates gradually from patient known to be taking excessive dosage over long periods of time
  • Use caution when barbiturates are administered to patients with acute or chronic pain; paradoxical excitement could be induced, or important symptoms could be masked; however, use of barbiturates as sedatives in postoperative surgical period, and as adjuncts to cancer chemotherapy, is well established
  • Administer with caution, if at all, to patients who are mentally depressed, have suicidal tendencies, or a history of drug abuse
  • Elderly or debilitated patients may react to barbiturates with marked excitement, depression, and confusion; in some persons, barbiturates repeatedly produce excitement rather than depression
  • In patients with hepatic damage, barbiturates should be administered with caution and initially in reduced doses; drug should not be administered to patients showing the premonitory signs of hepatic coma

Points of recommendation

  • Tell all of your health care providers that you take butabarbital. This includes your doctors, nurses, pharmacists, and dentists.
  • Avoid driving and doing other tasks or actions that call for you to be alert after you take butabarbital. You may still feel sleepy the day after you take butabarbital. Avoid these tasks or actions until you feel fully awake.
  • Have your blood work checked if you are on butabarbital for a long time. Talk with your doctor.
  • This medicine may be habit-forming with long-term use.
  • When sleep drugs are used nightly for more than a few weeks, they may not work as well to help sleep problems. This is known as tolerance. Only use sleep drugs for a short time. If sleep problems last, call the doctor.
  • Do not take butabarbital for longer than you were told by your doctor.
  • If you have been taking butabarbital for many weeks, talk with your doctor before stopping. You may want to slowly stop butabarbital.
  • Avoid alcohol while taking butabarbital. Do not take butabarbital if you drank alcohol that evening or before bed.
  • Talk with your doctor before you use other drugs and natural products that slow your actions.
  • Some people have done certain tasks or actions while they were not fully awake like driving, making and eating food, and having sex. Most of the time, people do not remember doing these things. Tell your doctor if this happens to you.
  • If you are allergic to tartrazine, talk with your doctor. Some products have tartrazine.
  • This medicine may make you feel sleepy and less alert. This may lead to falling. The chance of falling is higher in older people. If you have questions, talk with the doctor.
  • Birth control pills and other hormone-based birth control may not work as well to prevent pregnancy. Use some other kind of birth control also like a condom when taking butabarbital.
  • This medicine may cause harm to the unborn baby if you take it while you are pregnant. If you are pregnant or you get pregnant while taking butabarbital, call your doctor right away.
  • Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

For sleep:

  • Take butabarbital at bedtime.
  • Take butabarbital right before you get into bed.
  • Do not take butabarbital unless you can get a full night's sleep (at least 7 to 8 hours) before you need to be active again.
  • If you still have trouble sleeping after 7 to 10 days, call your doctor.
  • Take a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.

Side effects

difficulty urinating

Drug contraindications

Hypersensitivity to this drug

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