pen-toe-BAR-bi-tal

Therapeutic Classification: anticonvulsants, sedative/hypnotics

Pharmacologic Classification: barbiturates

• Hypnotic agent (short-term).
• Preoperative sedation and other situations in which sedation is required.
• Seizures.

Unlabeled Uses:

• IV: Induction of coma in selected patients with cerebral ischemia and management of increased intracranial pressure (high doses).

• Depresses the CNS, probably by potentiating GABA, an inhibitory neurotransmitter.
• Produces all levels of CNS depression, including the sensory cortex, motor activity, and altered cerebellar function.
• Anticonvulsant effect due to decreased synaptic transmission and increased seizure threshold.
• May decrease cerebral blood flow, cerebral edema, and intracranial pressure (IV only).

• Sedation and/or induction of sleep.

Absorption: IV administration results in complete bioavailability.

Distribution: Widely distributed; highest concentrations in brain and liver. Crosses the placenta; small amounts enter breast milk.

Metabolism/Excretion: Metabolized by the liver. Minimal renal excretion.

Half-life: Children: 25 hr; Adults: 35–50 hr.

(sedation)

†Noted as hypnotic effect; sedative effects are longer lasting.

Contraindicated in:

• Hypersensitivity
• Contains alcohol and propylene glycol and should be avoided in patients with known hypersensitivity or intolerance
• Comatose patients or those with pre-existing CNS depression (unless used to induce coma)
• Uncontrolled severe pain
• OB: Pregnancy (may affect child's brain development when used during 3rd trimester)
• Lactation: Lactation.

Use Cautiously in:

• Severe renal impairment
• Hepatic impairment
• Patients who may be suicidal or who may have been addicted to drugs previously
• Hypovolemic shock
• Pedi: Children <3 yr (may affect brain development)
• Geri: Older adults at ↑ risk of falls (initial dose ↓ recommended).

CV: hypotension.

Derm: rash, urticaria.

GI: constipation, diarrhea, nausea, vomiting.

Local: phlebitis.

MS: arthralgia, myalgia, neuralgia.

Neuro: drowsiness, hangover, lethargy, delirium, depression, excitation, vertigo.

Resp: bronchospasm, LARYNGOSPASM, respiratory depression.
Misc: (INCLUDING ANGIOEDEMA AND SERUM SICKNESS) HYPERSENSITIVITY REACTIONS , physical dependence, psychological dependence.

Drug-Drug:

• Additive CNS depression with other CNS depressants, including alcohol, antihistamines, opioids, and other sedative/hypnotics.
• May ↓ levels and effectiveness of oral contraceptives, warfarin, carbamazepine,chloramphenicol, cyclosporine, dacarbazine, doxycycline, corticosteroids, tricyclic antidepressants, and quinidine.
• May ↑ risk of hepatic toxicity of acetaminophen.
• MAO inhibitors, valproic acid, or divalproex may ↑ levels and ↑ sedation.

Drug-Natural Products:

• Concomitant use of kava, valerian, skullcap, chamomile, or hops can ↑ CNS depression.
• St. John's wort may ↓ levels and effectiveness.

• IM (Adults): Hypnotic/preoperative sedative: 150–200 mg.
• IM (Children): Sedative: 2–6 mg/kg/day in divided doses. Preoperative sedative: 2–6 mg/kg (up to 100 mg/dose).
• IV (Adults): Hypnotic/anticonvulsant: 100 mg initially; additional small doses may be given every min up to 500 mg total. Induction of coma: 5–7 mg/kg, then 3–4 mg/kg every 3–4 hr dose adjusted by serum level (unlabeled).
• IV (Children): Sedative: 1–3 mg/kg to a maximum of 100 mg until asleep.Conscious sedation: Initial 2 mg/kg, may repeat every 5–10 min with 1–2 mg/kg until adequate sedation achieved. Maximum total dose 6 mg/kg or 150–200 mg.Induction of coma: 10–15 mg/kg slowly over 1–2 hr, followed by a maintenance infusion of 1–3 mg/kg/hr.

(Generic available)

• Solution for injection: 50 mg/mL;

• Monitor respiratory status, pulse, and BP frequently in patients receiving pentobarbital IV. Equipment for resuscitation and artificial ventilation should be readily available. Respiratory depression is dose dependent.
  • Prolonged therapy may lead to psychological or physical dependence. Restrict amount of drug available to patient, especially if depressed, suicidal, or previously addicted.
  • Assess postoperative patients for pain. Pentobarbital may increase responsiveness to painful stimuli.
  • Therapeutic ranges: Sedation 1–5 mcg/mL; Sleep: 5–15 mcg/mL; Coma: 20–40 mcg/mL.
• Sleep: Assess sleep patterns prior to and periodically during therapy. Hypnotic doses of pentobarbital suppress REM sleep. Patient may experience an increase in dreaming upon discontinuation of medication.
• Cerebral Edema: Monitor intracranial pressure and level of consciousness in patients in barbiturate coma.
• Seizures: Assess location, duration, and characteristics of seizure activity. Implement seizure precautions.

• Do not confuse pentobarbital with phenobarbital.
  • Supervise ambulation and transfer of patients following administration. Remove cigarettes. Side rails should be raised and call bell within reach at all times. Keep bed in low position.
• IM: Do not administer SUBQ. Administer IM injections deep into the gluteal muscle to minimize tissue irritation. Do not inject more than 5 mL into any one site because of tissue irritation.

IV Administration:

• Doses may be given undiluted or diluted with sterile water, 0.45% NaCl, 0.9% NaCl, D5W, D10W, Ringer’s or LR, dextrose/saline combinations, or dextrose/Ringer’s or lactated Ringer’s combinations. Do not use solution that is discolored or that contains particulate matter.
  • Solution is highly alkaline; avoid extravasation, which may cause tissue damage and necrosis. If extravasation occurs, infiltration of 5% procaine solution into affected area and application of moist heat may be used.
• Rate: Administer each 50 mg over at least 1 min. Titrate slowly for desired response. Rapid administration may result in respiratory depression, apnea, laryngospasm, bronchospasm, or hypertension.
• Y-Site Compatibility:
  • acyclovir
  • aminocaproic acid
  • aminophylline
  • amphotericin B lipid complex
  • amphotericin B liposomal
  • anidulafungin
  • argatroban
  • arsenic trioxide
  • atropine
  • azathioprine
  • azithromycin
  • bivalirudin
  • bleomycin
  • bumetanide
  • calcium chloride
  • calcium gluconate
  • carboplatin
  • carmustine
  • chloramphenicol
  • cisplatin
  • cyanocobalamin
  • cyclophosphamide
  • cytarabine
  • dacarbazine
  • dactinomycin
  • dexamethasone
  • dexmedetomidine
  • digoxin
  • docetaxel
  • dopamine
  • doxorubicin liposomal
  • enalaprilat
  • ephedrine
  • epoetin alfa
  • eptifibatide
  • ertapenem
  • etoposide
  • etoposide phosphate
  • famotidine
  • fentanyl
  • fluconazole
  • fludarabine
  • fluorouracil
  • folic acid
  • foscarnet
  • fosphenytoin
  • furosemide
  • ganciclovir
  • gemcitabine
  • glycopyrrolate
  • granisetron
  • heparin
  • hydrocortisone
  • hydromorphone
  • ifosfamide
  • imipenem/cilastatin
  • indomethacin
  • insulin, regular
  • irinotecan
  • labetalol
  • leucovorin calcium
  • linezolid
  • lorazepam
  • magnesium sulfate
  • mannitol
  • mesna
  • methotrexate
  • methylprednisolone
  • metoclopramide
  • metoprolol
  • metronidazole
  • milrinone
  • mitoxantrone
  • multivitamins
  • nafcillin
  • naloxone
  • nitroglycerin
  • nitroprusside
  • octreotide
  • oxacillin
  • oxytocin
  • paclitaxel
  • pamidronate
  • pantoprazole
  • pemetrexed
  • phenobarbital
  • phenylephrine
  • phytonadione
  • piperacillin/tazobactam
  • potassium acetate
  • potassium chloride
  • procainamide
  • propofol
  • propranolol
  • sodium acetate
  • sodium bicarbonate
  • sufentanil
  • theophylline
  • thiotepa
  • tigecycline
  • tirofiban
  • vancomycin
  _vasopressin
  • vinblastine
  • vincristine
  • voriconazole
  • zoledronic acid
• Y-Site Incompatibility:
  • alemtuzumab
  • amikacin
  • amiodarone
  • ascorbic acid
  • atracurium
  • aztreonam
  • benztropine
  • buprenorphine
  • butorphanol
  • caspofungin
  • cefazolin
  • cefotaxime
  • cefotetan
  • cefoxitin
  • ceftazidime
  • ceftriaxone
  • cefuroxime
  • chlorpromazine
  • clindamycin
  • cyclosporine
  • dantrolene
  • daptomycin
  • daunorubicin
  • dexrazoxane
  • diazepam
  • diazoxide
  • diltiazem
  • diphenhydramine
  • dobutamine
  • doxorubicin hydrochloride
  • doxycycline
  • epinephrine
  • epirubicin
  • erythromycin
  • esmolol
  • gemtuzumab ozogamicin
  • gentamicin
  • haloperidol
  • hydralazine
  • hydroxyzine
  • idarubicin
  • isoproterenol
  • levofloxacin
  • lidocaine
  • meperidine
  • methadone
  • midazolam
  • minocycline
  • mitomycin
  • morphine
  • mycophenolate
  • nalbuphine
  • nicardipine
  • norepinephrine
  • ondansetron
  • palonosetron
  • papaverine
  • penicillin G
  • pentamidine
  • phentolamine
  • phenytoin
  • prochlorperazine
  • promethazine
  • protamine
  • pyridoxine
  • succinylcholine
  • thiamine
  • tobramycin
  • topotecan
  • verapamil
.

• Explain purpose of pentobarbital to patient and family.
• Discuss the importance of preparing environment for sleep (dark room, quiet, avoidance of nicotine and caffeine).
• May cause daytime drowsiness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
• Caution patient to avoid taking alcohol or other CNS depressants concurrently with this medication.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

• Improvement in sleep pattern without excessive daytime sedation. Therapy is usually limited to a 2-wk period.
• Prevention of cerebral anoxia.
• Decrease or cessation of seizures without excessive sedation.

Nembutal

Schedule II (C-II)