Ultiva
Ultiva
Generic Name
Ultiva
Brand Names
for pentobarbital – a short‑acting barbiturate used primarily for procedural sedation and as a euthanasia agent.*
Mechanism
- Potentiation of GABAA receptor activity: Enhances chloride influx → neuronal hyperpolarization.
- Direct inhibition of voltage‑gated Na⁺ and Ca²⁺ channels: Reduces excitatory neurotransmission.
- Rapid CNS depression → loss of consciousness, muscle relaxation, and analgesia.
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Pharmacokinetics
| Parameter | Value | Comment |
| Absorption | Parenteral only (IV, IM). 100 % bioavailability. | Oral absorption poor; not used clinically. |
| Distribution | LogP ≈ 3.1; extensive lipid solubility; ~70 % protein‑binding. | Rapid brain penetration → quick onset. |
| Metabolism | Hepatic via CYP2B6, CYP2C9, CYP2C19. Phase I oxidative metabolism. | Short half‑life in healthy adults: 45–90 min. |
| Elimination | Renal excretion of metabolites; active secretion via OATP1B1/B3. | Clearance ~12 mL/kg/min. |
| Half‑life | 30–60 min (terminal). | Allows repeat dosing after 1–2 h. |
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Indications
- Procedural sedation (e.g., dental, minor surgery, endoscopy) when rapid onset & short duration desired.
- Euthanasia in animals (veterinary use; not approved for human euthanasia).
- Adjunct to anesthesia when other agents insufficient for depth of sedation.
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Contraindications
- Known hypersensitivity to barbiturates or any component.
- Severe hepatic or renal impairment – altered clearance → prolonged sedation.
- Uncontrolled hypertension or cardiac arrhythmias – risk of hypotension and arrhythmogenicity.
- Pregnancy/Breastfeeding – fetotoxic and harmful to nursing infants.
- Concurrent use of strong CYP2B6 inhibitors (e.g., clopidogrel) may increase exposure.
- Use with other CNS depressants (opioids, benzodiazepines, alcohol) raises risk of respiratory depression.
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Dosing
| Setting | Dose | Route | Frequency |
| Adult procedural sedation | 2 mg/kg IV *max 100 mg* | IV push over 30 s | Repeat 1–3 mg/kg after 30–60 min if depth insufficient. |
| Adult rapid‑sequence induction | 1–2 mg/kg IV | IV | Single dose. |
| Animal euthanasia (dogs, cats) | 100–200 mg/kg IV | IV | Single dose; verify cessation of cardiac activity. |
• Infusion: 0.5–1 mg/min IV for continuous sedation; monitor depth of anesthesia closely.
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Adverse Effects
- Common (up to 30 %):
- Nausea & vomiting
- Drowsiness, dizziness
- Flushing, tremor
- Transient bradycardia
- Serious (rare):
- Respiratory depression, apnea
- Seizures (rebound post‑administration)
- Hypotension, cardiovascular collapse
- Allergic reactions (anaphylaxis)
- Long‑term dependence with misuse
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Monitoring
- Level of sedation: Ramsay or MOAA/S score every 5–10 min.
- Airway patency & ventilation: SpO₂, end‑tidal CO₂; support with bag‑mask ventilation if needed.
- Cardiovascular: HR, BP, ECG; watch for arrhythmias.
- Temperature: Monitor for hyperthermia in prolonged sedation.
- Post‑procedural: Recovery time to baseline consciousness; note any dysphoria.
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Clinical Pearls
- Sharp “on‑set, off‑set”: Ideal for short procedures; unlike propofol, has less hypotension early on.
- Avoid rapid IV push >30 s; slow infusion reduces risk of sudden apnea.
- Reverse overdose with flumazenil? – *Not effective.* Use supportive measures (ventilation, lipid emulsion).
- Drug‑drug interactions: Ketamine may blunt pentobarbital recovery due to opposing mechanisms; combine with caution.
- Storage: Keep in a sealed vial; stable at room temperature for up to 90 days (subject to manufacturer).
- Euthanasia compliance: Verify species‑specific dosing; confirm heart‑stop per local regulations.
*For the most current dosing recommendations and regulatory status, consult the USP or local veterinary guidelines.*
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