Thiopentobarbitone

Thiopentobarbitone Uses, Dosage, Side Effects, Food Interaction and all others data.

Thiopentobarbitone, a barbiturate, is used for the induction of anesthesia prior to the use of other general anesthetic agents and for induction of anesthesia for short surgical, diagnostic, or therapeutic procedures associated with minimal painful stimuli. Thiopentobarbitone is an ultrashort-acting depressant of the central nervous system which induces hypnosis and anesthesia, but not analgesia. It produces hypnosis within 30 to 40 seconds of intravenous injection. Recovery after a small dose is rapid, with some somnolence and retrograde amnesia. Repeated intravenous doses lead to prolonged anesthesia because fatty tissues act as a reservoir; they accumulate Pentothal in concentrations 6 to 12 times greater than the plasma concentration, and then release the drug slowly to cause prolonged anesthesia

Thiopentobarbitone 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.

Trade Name Thiopentobarbitone
Availability Discontinued
Generic Thiopental
Thiopental Other Names Penthiobarbital, Pentothiobarbital, Thiopental, Thiopentobarbital, Thiopentobarbitone, Thiopentobarbituric acid, Thiopentone, Tiopentale
Related Drugs diazepam, topiramate, fentanyl, levetiracetam, lidocaine, Keppra, Topamax, Valium, haloperidol, prochlorperazine
Type
Formula C11H18N2O2S
Weight Average: 242.338
Monoisotopic: 242.10889852
Protein binding

Approximately 80% of the drug in the blood is bound to plasma protein.

Groups Approved, Vet approved
Therapeutic Class General (Intravenous) anesthetics
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Thiopentobarbitone
Thiopentobarbitone

Uses

Thiopentobarbitone 500 mg injection: Each box contains 1 vial of 500 mg Thiopentobarbitone Sodium for Injection (a sterile mixture of Thiopentobarbitone Sodium and anhydrous Sodium Carbonate as a buffer) & 1 ampoule of 10 ml Water for Injection.

Thiopentobarbitone 1 gm injection: Each box contains 1 vial of 1 gm Thiopentobarbitone Sodium for Injection (a sterile mixture of Thiopentobarbitone Sodium and anhydrous Sodium Carbonate as a buffer) & 2 ampoules of 10 ml Water for Injection.

Thiopentobarbitone Sodium for Injection is used-

  • As the sole anesthetic agent for brief (15 minutes) procedures,
  • For induction of anesthesia prior to administration of other anesthetic agents,
  • To supplement regional anesthesia,
  • To provide hypnosis during balanced anesthesia with other agents for analgesia or muscle relaxation,
  • For the control of convulsive states during or following inhalation anesthesia, local anesthesia, or other causes,
  • In neurosurgical patients with increased intracranial pressure, if adequate ventilation is provided, and
  • For narcoanalysis and narcosynthesis in psychiatric disorders.

Thiopentobarbitone is also used to associated treatment for these conditions: Seizures

How Thiopentobarbitone works

Thiopentobarbitone 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.

Dosage

Thiopentobarbitone dosage

Thiopentobarbitone Injection is administered intravenously normally as a 2.5% w/v solution. On occasions it may be administered as a 5% w/v solution (500 mg in 10 ml). The intravenous injection preparation should be used after reconstitution of the sterile powder with Water for Injections, usually to produce a 2.5% w/v solution.

Premedication: Premedication usually consists of atropine or scopolamine to suppress vagal reflexes and inhibit secretions. In addition, a barbiturate or an opiate is often given. Ideally, the peak effect of these medications should be reached shortly before the time of induction.

Test dose: It is advisable to inject a small "test" dose of 25 mg to 75 mg of Thiopentobarbitone Sodium for Injection to assess tolerance or unusual sensitivity to Thiopentobarbitone Sodium for Injection, and pausing to observe patient reaction for at least 60 seconds. If unexpectedly deep anesthesia develops or if respiratory depression occurs, consider these possibilities:

  1. The patient may be unusually sensitive to Thiopentobarbitone Sodium for Injection,
  2. The solution may be more concentrated than had been assumed, or
  3. The patient may have received too much.

Use in anaesthesia: Normal dosage for the induction of anesthesia is 100 mg to 150 mg injected over 10 to 15 seconds. If necessary, a repeat dose of 100 mg to 150 mg may be given after one minute. No fixed dosage recommendations for the intravenous injection can be given, since the dosage will need to be carefully adjusted according to the patient's response. Factors such as age, sex, and weight of the patient should be taken into consideration. Thiopentobarbitone Sodium reaches effective concentrations in the brain within 30 seconds and anesthesia is normally produced within one minute of an intravenous dose.

  • Adult: 100 mg to 150 mg intravenously over 10 to 15 seconds, normally as a 2.5% w/v solution. A repeat dose of 100 mg to 150 mg may be given after one minute. The intravenous injection should be given slowly and the amount given titrated against the patient's response to minimize the risk of respiratory depression or the possibility of over dosage. The average dose for an adult of 70 kg is roughly 200 mg to 300 mg (8 mls to 12 mls of a 2.5% w/v solution) with a maximum of 500 mg.
  • Children: 2 mg/kg to 7 mg/kg bodyweight, intravenously over 10 to 15 seconds, normally as a 2.5% w/v solution. A repeat dose of 2 mg/kg to 7 mg/kg may be given after one minute. The dose is 2 mg/kg to 7 mg/kg based on the patient's response. The dose for children should not exceed 7 mg/kg.
  • Elderly: Smaller adult doses are advisable.

Use in convulsive states: 75 mg to 125 mg (3 mls to 5 mls of a 2.5% w/v solution) should be given as soon as possible after the convulsion begins. Further doses may be required to control convulsion following the use of a local anesthetic. Other regimens, such as the use of intravenous or rectal diazepam, may be used to control convulsive states.

Side Effects

Hypersensitivity reactions have been reported. Other adverse reactions to thiopental sodium include the followings: respiratory depression, myocardial depression, cardiac arrhythmias, prolonged somnolence and recovery, hypotension, tachycardia, sneezing, coughing, bronchospasm, laryngospasm and shivering. Anaphylactic reactions have been reported. Symptoms, e.g., urticaria, bronchospasm, vasodilation and edema.

Toxicity

Overdosage may occur from rapid or repeated injections. Too rapid injection may be followed by an alarming fall in blood pressure even to shock levels. Apnea, occasional laryngospasm, coughing and other respiratory difficulties with excessive or too rapid injections may occur. Lethal blood levels may be as low as 1 mg/100 mL for short-acting barbiturates; less if other depressant drugs or alcohol are also present.

Precaution

A person competent in anesthesia management should be in constant attendance and adequate facilities for support of respiration and circulation should be available when Thiopentobarbitone Sodium for injection is being used. Thiopentobarbitone Sodium for Injection should be administered with caution to patients with preexisting hypotension or in conditions where the hypnotic effect may be prolonged or intensified, such as in the presence of liver disease and renal disease.

This product may be habit forming. Keep resuscitative and endotracheal intubation equipment and oxygen readily available. Maintain patency of the airway at all times. Only persons qualified in the use of anesthetics should administer this drug. Avoid extravasations or intra-arterial injection.

Interaction

Possible increase in difficulty in producing anaesthesia in patients taking alcohol or CNS depressants. Additive action with other CNS depressants including sedatives, hypnotics, nitrous oxide or alcohol. Increased hypotension and excitatory effects with phenothiazine antipsychotics. Increased hypnotic effect with antipsychotic. Decreased requirement of thiopental sodium with metoclopramide, sulfisoxazole, aspirin, meprobamate, probenecid and other highly protein bound drugs.

Food Interaction

No interactions found.

Thiopentobarbitone Alcohol interaction

[Major] GENERALLY AVOID:

Concurrent acute use of barbiturates and ethanol may result in additive CNS effects,

including impaired coordination, sedation, and death.

Tolerance of these agents may occur with chronic use.

The mechanism is related to inhibition of microsomal enzymes acutely and induction of hepatic microsomal enzymes chronically.



The combination of ethanol and barbiturates should be avoided.

Elimination Route

Rapidly absorbed.

Half Life

3-8 hours

Pregnancy & Breastfeeding use

Pregnancy Category C. Animal reproduction studies have not been conducted with Thiopentobarbitone. It is also not known whether Thiopentobarbitone can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Thiopentobarbitone should be given to a pregnant woman only if clearly needed. Thiopentobarbitone sodium readily crosses the placental barrier and small amounts may appear in the milk of nursing mothers following administration of large doses.

Contraindication

Absolute Contraindication:

  • Absence of suitable veins for intravenous administration
  • Hypersensitivity (allergy) to barbiturates
  • Variegate porphyria (South African) or acute intermittent porphyria
  • Status asthmaticus

Relative Contraindication:

  • Severe cardiovascular disease
  • Hypotension or shock
  • Conditions in which the hypnotic effect may be prolonged or potentiated, eg, excessive premedication, Addison's disease, hepatic or renal dysfunction, myxedema, increased blood urea, severe anemia, asthma, myasthenia gravis

Acute Overdose

Overdosage may occur from too rapid or repeated administration. Too rapid injection may be followed by an alarming fall in blood pressure even to shock levels. Apnoea, occasional laryngospasm, coughing and other respiratory difficulties with excessive or too rapid injections may occur. In the event of suspected or apparent overdosage, the agent should be discontinued.

Storage Condition

Store at controlled room temperature of 15° C to 30° C. Solutions should be freshly prepared and used immediately. Any portion of the contents remaining should be discarded.

Innovators Monograph

You find simplified version here Thiopentobarbitone

Thiopentobarbitone contains Thiopental see full prescribing information from innovator Thiopentobarbitone Monograph, Thiopentobarbitone MSDS, Thiopentobarbitone FDA label

FAQ

What is Thiopentobarbitone used for?

Thiopentobarbitone is used for the induction of general anaesthesia and is also used as an adjunct to provide hypnosis during balanced anaesthesia with other anaesthetic agents, including analgesics and muscle relaxants.

How safe is Thiopentobarbitone?

Thiopentobarbitone is the most extensively studied intravenous anesthetic agent and has been shown to be safe in obstetric patients.

When is Thiopentobarbitone used?

Thiopentobarbitone slows the activity of your brain and nervous system. Thiopentobarbitone is used to help you relax before you receive general anesthesia with an inhaled medication.

What are the common side effects of Thiopentobarbitone?

Common side effects of Thiopentobarbitone are include:

  • coughing,
  • sneezing,
  • hiccups,
  • slowed breathing,
  • slow heart rate,
  • cardiac arrhythmias,
  • prolonged sleepiness and recovery, and.
  • shivering.

Is Thiopentobarbitone a sedative?

Thiopentobarbitone is another short-acting barbiturate sedative, lasting about 5-20 minutes.

Is Thiopentobarbitone safe during pregnancy?

Thiopentobarbitone can be used without adverse effects during pregnancy although the total dose should not exceed 250mg. However, when considering use of Thiopentobarbitone the clinician should only use the drug when the expected benefits outweigh any potential risks.

Is Thiopentobarbitone safe during breastfeeding?

Breast-feeding should be temporarily suspended for at least 12 hours or breast milk expressed before the induction of anesthesia.

Can I drink alcohol with Thiopentobarbitone?

Drinking alcohol while taking Thiopentobarbitone will increase the chances of dizziness and drowsiness. The fact that both alcohol and Thiopentobarbitone are central nervous system depressants only makes the combination more dangerousavoid all alcohol consumption when preparing for Thiopentobarbitone.

Is Thiopentobarbitone a controlled drug?

Thiopentobarbitone is classified as a Schedule III controlled substance.

Can I drive after taking Thiopentobarbitone?

It may cause dizziness, drowsiness or lightheadedness, do not drive a car or operate machinery while taking this medication. 

How long does Thiopentobarbitone take to work?

Thiopentobarbitone reaches effective concentrations in the brain within 30 seconds and anaesthesia is normally produced within one minute of an intravenous dose.

How does Thiopentobarbitone work in the body?

Thiopentobarbitone slows the activity of your brain and nervous system. Thiopentobarbitone is used to help you relax before you receive general anesthesia with an inhaled medication. It may be used for other purposes not listed in this medication guide.

How is Thiopentobarbitone given?

Thiopentobarbitone is injected into a vein through an IV. A healthcare provider will give you this injection.
You will be given this medication while you are lying down. You will fall asleep very quickly after Thiopentobarbitone  is injected.Your breathing, blood pressure, oxygen levels, kidney function, and other vital signs will be watched closely while you are receiving Thiopentobarbitone.

What happens if I miss a dose?

Since Thiopentobarbitone is usually given just for anesthesia, you are not likely to be on a dosing schedule.

What happens if I overdose?

Since Thiopentobarbitone is given by a healthcare professional in a medical setting, an overdose is unlikely to occur.

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