PHENOBARBITAL SODIUM injection

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

PHENOBARBITAL SODIUM (UNII: SW9M9BB5K3) (PHENOBARBITAL - UNII:YQE403BP4D)

Available from:

Bryant Ranch Prepack

Administration route:

INTRAMUSCULAR

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

- Sedative. Sedation is obtainable within an hour, and in adequate dosage, the duration of action is more than six hours. Included in the more common conditions in which the sedative action of this class of drugs is desired are anxiety-tension states, hyperthyroidism, essential hypertension, nausea and vomiting of functional origin, motion sickness, acute labyrinthitis, pylorospasm in infants, chorea and cardiac failure. Phenobarbital is also a useful adjunct in treatment of hemorrhage from the respiratory or gastrointestinal tract. Phenobarbital controls anxiety, decreases muscular activity and lessens nervous excitability in hyperthyroid patients. However, thyrotoxic individuals occasionally react poorly to barbiturates. - Hypnotic, for the short-term treatment of insomnia, since it appears to lose its effectiveness for sleep induction and sleep maintenance after 2 weeks (see CLINICAL PHARMACOLOGY ). - Preanesthetic. - Long-term anticonvulsant, (phenobarbital, mephobarbital and metharbital) for the treatment of generalized tonic-clonic and cortical focal seizures. And, in the emergency control of certain acute convulsive episodes, e.g., those associated with status epilepticus, cholera, eclampsia, cerebral hemorrhage, meningitis, tetanus, and toxic reactions to strychnine or local anesthetics. Phenobarbital sodium may be administered intramuscularly or intravenously as an anticonvulsant for emergency use. When administered intravenously, it may require 15 or more minutes before reaching peak concentrations in the brain. Therefore, injecting phenobarbital sodium until the convulsions stop may cause the brain level to exceed that required to control the convulsions and lead to severe barbiturate-induced depression. - Phenobarbital is indicated in pediatric patients as an anticonvulsant and as a sedative, including its preoperative and postoperative use. Barbiturates are contraindicated in patients with known barbiturate sensitivity. Barbiturates are also contraindicated in patients with a history of manifest or latent porphyria, marked impairment of liver functions or with severe respiratory distress where dyspnea or obstruction is evident. Large doses are contraindicated in nephritic subjects. Barbiturates should not be administered to persons with known previous addiction to the sedative-hypnotic group since ordinary doses may be ineffectual and may contribute to further addiction. Intraarterial administration is contraindicated. Its consequences vary from transient pain to gangrene. Subcutaneous administration produces tissue irritation, ranging from tenderness and redness to necrosis and is not recommended. (See DOSAGE AND ADMINISTRATION, Treatment of Adverse Effects Due to Inadvertent Error in Administration .) Phenobarbital Sodium Injection is a Schedule IV controlled substance. Barbiturates may be habit forming. Tolerance and psychological dependence and physical dependence may occur especially following prolonged use of high doses of barbiturates. As tolerance to barbiturates develops, the amount needed to maintain the same level of intoxication increases; tolerance to a fatal dosage, however, does not increase more than two-fold. As this occurs, the margin between an intoxicating dosage and fatal dosage becomes smaller. Symptoms of acute intoxication with barbiturates include unsteady gait, slurred speech and sustained nystagmus. Mental signs of chronic intoxication include confusion, poor judgment, irritability, insomnia and somatic complaints. Symptoms of barbiturate dependence are similar to those of chronic alcoholism. If an individual appears to be intoxicated with alcohol to a degree that is radically disproportionate to the amount of alcohol in his or her blood, the use of barbiturates should be suspected. The lethal dose of a barbiturate is far less if alcohol is also ingested. The symptoms of barbiturate withdrawal can be severe and may cause death. Minor withdrawal symptoms may appear 8 to 12 hours after the last dose of a barbiturate. These symptoms usually appear in the following order: anxiety, muscle twitching, tremor of hands and fingers, progressive weakness, dizziness, distortion in visual perception, nausea, vomiting, insomnia and orthostatic hypotension. Major withdrawal symptoms (convulsions and delirium) may occur within 16 hours and last up to 5 days after abrupt cessation of these drugs. Intensity of withdrawal symptoms gradually declines over a period of approximately 15 days. Individuals susceptible to barbiturate abuse and dependence include alcoholics and opiate abusers, as well as other sedative-hypnotic and amphetamine abusers. Drug dependence to barbiturates arises from repeated administration of a barbiturate or agent with barbiturate-like effect on a continuous basis, generally in amounts exceeding therapeutic dose levels. The characteristics of drug dependence to barbiturates include: (a) a strong desire or need to continue taking the drug, (b) a tendency to increase the dose, (c) a psychic dependence on the effects of the drug related to subjective and individual appreciation of those effects and (d) a physical dependence on the effects of the drug requiring its presence for maintenance of homeostasis and resulting in a definite, characteristic and self-limited abstinence syndrome when the drug is withdrawn. Individuals subject to barbiturate abuse and dependence include alcoholics and opiate abusers as well as other sedative-hypnotics and amphetamine abusers. Treatment of barbiturate dependence consists of cautious and gradual withdrawal of the drug. Barbiturate-dependent patients can be withdrawn by using a number of different withdrawal regimens. In all cases, withdrawal takes an extended period of time. One method involves substituting a 30 mg dose of phenobarbital for each 100 to 200 mg dose of barbiturate that the patient has been taking. The total daily amount of phenobarbital is then administered in 3 to 4 divided doses, not to exceed 600 mg daily. Should signs of withdrawal occur on the first day of treatment, a loading dose of 100 to 200 mg of phenobarbital may be administered IM in addition to the oral dose. After stabilization on phenobarbital, the total daily dose is decreased by 30 mg a day as long as withdrawal is proceeding smoothly. If withdrawal symptoms appear, dosage is maintained at that level or increased slightly until symptoms disappear. A modification of this regimen involves initiating treatment at the patient's regular dosage level and decreasing the daily dosage by 10 percent if tolerated by the patient. The symptoms of withdrawal can be severe and may cause death. Minor withdrawal symptoms (e.g., anxiety, muscle twitching, tremors, nausea, etc.) may appear 8-12 hours after the last dose of a barbiturate. Major withdrawal symptoms (convulsions and delirium) may occur within 16 hours and last up to five days after abrupt cessation of the barbiturate. The intensity of withdrawal symptoms gradually declines over a period of two weeks. Infants physically dependent on barbiturates may be given phenobarbital 3 to 10 mg/kg/day. After withdrawal symptoms (hyperactivity, disturbed sleep, tremors, hyperreflexia) are relieved, the dosage of phenobarbital should be gradually decreased and completely withdrawn over a 2-week period.

Product summary:

Phenobarbital Sodium Injection, USP is available in the following: 65 mg/mL, 1 mL vials packaged in 25s (NDC 72162-1329-2) 65 mg/mL, 1 mL vials packaged in 3s (NDC 72162-1329-4) Storage Store at 20°-25°C (68°-77°), excursions permitted to 15°-30°C (59°-86°F) [See USP Controlled Room Temperature]. Do not use if solution is discolored or contains a precipitate. To report SUSPECTED ADVERSE REACTIONS, contact the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. Repackaged/Relabeled by: Bryant Ranch Prepack, Inc. Burbank, CA 91504

Authorization status:

unapproved drug other

Summary of Product characteristics

PHENOBARBITAL SODIUM- PHENOBARBITAL SODIUM INJECTION
BRYANT RANCH PREPACK
_Disclaimer: This drug has not been found by FDA to be safe and
effective, and this_
_labeling has not been approved by FDA. For further information about
unapproved_
_drugs, click here._
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PHENOBARBITAL SODIUM INJECTION, USP
CIV
FOR IM OR SLOW IV ADMINISTRATION
DO NOT USE IF SOLUTION IS DISCOLORED OR CONTAINS A PRECIPITATE
RX ONLY
DESCRIPTION
The barbiturates are nonselective central nervous system (CNS)
depressants which are
primarily used as sedative hypnotics and also anticonvulsants in
subhypnotic doses. The
barbiturates and their sodium salts are subject to control under the
Federal Controlled
Substances Act (CIV).
Barbiturates are substituted pyrimidine derivatives in which the basic
structure common
to these drugs is barbituric acid, a substance which has no central
nervous system
activity. CNS activity is obtained by substituting alkyl, alkenyl or
aryl groups on the
pyrimidine ring.
Phenobarbital Sodium Injection, USP is a sterile solution for
intramuscular or slow
intravenous administration as a long-acting barbiturate. Each mL
contains phenobarbital
sodium either 65 mg or 130 mg, alcohol 0.1 mL, propylene glycol 0.678
mL and benzyl
alcohol 0.015 mL in Water for Injection; hydrochloric acid added, if
needed, for pH
adjustment. The pH range is 9.2-10.2.
Chemically, phenobarbital sodium is 2,4,6(1 _H_,3 _H_,5
_H_)-Pyrimidinetrione,5-ethyl-5-phenyl-
, monosodium salt and has the following structural formula:
The sodium salt of phenobarbital occurs as a white, slightly bitter
powder, crystalline
granules or flaky crystals; it is soluble in alcohol and practically
insoluble in ether or
chloroform.
CLINICAL PHARMACOLOGY
Barbiturates are capable of producing all levels of CNS mood
alteration from excitation
to mild sedation, to hypnosis, and deep coma. Overdosage can produce
death. In high
enough therapeutic doses, barbiturates induce anesthesia.
Barbiturates depress the sensory cortex, decrease motor activity,
alter cerebellar